Composite polyester membranes with embedded dendrimer hosts and bimetallic Fe/Ni nanoparticles: synthesis, characterisation and application to water treatment
- Malinga, S P, Arotiba, O A, Mapolie, S F, Krause, Rui W M, Mamba, Bhekie B, Diallo, M S
- Authors: Malinga, S P , Arotiba, O A , Mapolie, S F , Krause, Rui W M , Mamba, Bhekie B , Diallo, M S
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125086 , vital:35727 , https://doi.org/10.1007/s11051-013-1698-y
- Description: This study describes the preparation, characterization and evaluation of new composite membranes with embedded dendrimer hosts and Fe/Ni nanoparticles. These new reactive membranes consist of films of cyclodextrin–poly(propyleneimine) dendrimers (β-CD–PPI) that are deposited onto commercial polysulfone microporous supports and crosslinked with trimesoyl chloride (TMC). The membranes were subsequently loaded with Fe/Ni nanoparticles and evaluated as separation/reactive media in aqueous solutions using 2,4,6-trichlorophenol as model pollutant. The morphology and physicochemical properties of the composite membranes were characterised using high-resolution transmission electron microscopy (HR-TEM), atomic force microscopy and measurements of contact angle, water intake, porosity and water permeability. The sorption capacity and catalytic activity of the membranes were evaluated using ion chromatography, atmospheric pressure chemical ionisation-mass spectrometry and UV–Vis spectroscopy (UV–Vis). The sizes of the embedded Fe/Ni nanoparticles in the membranes ranged from 40 to 66 nm as confirmed by HR-TEM. The reaction rates for the dechlorination of 2,4,6-trichlorophenol ranged from 0.00148 to 0.00250 min−1. In all cases, we found that the reaction by-products consisted of chloride ions and mixtures of compounds including phenol (m/z = 93), 2,4-dichlorophenol (m/z = 163) and 4-chlorophenol (m/z = 128). The overall results of this study suggest that β-CD–PPI dendrimers are promising building blocks for the synthesis of composite and reactive membranes for the efficient removal of chlorinated organic pollutants from water.
- Full Text:
- Date Issued: 2013
- Authors: Malinga, S P , Arotiba, O A , Mapolie, S F , Krause, Rui W M , Mamba, Bhekie B , Diallo, M S
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125086 , vital:35727 , https://doi.org/10.1007/s11051-013-1698-y
- Description: This study describes the preparation, characterization and evaluation of new composite membranes with embedded dendrimer hosts and Fe/Ni nanoparticles. These new reactive membranes consist of films of cyclodextrin–poly(propyleneimine) dendrimers (β-CD–PPI) that are deposited onto commercial polysulfone microporous supports and crosslinked with trimesoyl chloride (TMC). The membranes were subsequently loaded with Fe/Ni nanoparticles and evaluated as separation/reactive media in aqueous solutions using 2,4,6-trichlorophenol as model pollutant. The morphology and physicochemical properties of the composite membranes were characterised using high-resolution transmission electron microscopy (HR-TEM), atomic force microscopy and measurements of contact angle, water intake, porosity and water permeability. The sorption capacity and catalytic activity of the membranes were evaluated using ion chromatography, atmospheric pressure chemical ionisation-mass spectrometry and UV–Vis spectroscopy (UV–Vis). The sizes of the embedded Fe/Ni nanoparticles in the membranes ranged from 40 to 66 nm as confirmed by HR-TEM. The reaction rates for the dechlorination of 2,4,6-trichlorophenol ranged from 0.00148 to 0.00250 min−1. In all cases, we found that the reaction by-products consisted of chloride ions and mixtures of compounds including phenol (m/z = 93), 2,4-dichlorophenol (m/z = 163) and 4-chlorophenol (m/z = 128). The overall results of this study suggest that β-CD–PPI dendrimers are promising building blocks for the synthesis of composite and reactive membranes for the efficient removal of chlorinated organic pollutants from water.
- Full Text:
- Date Issued: 2013
Un-functionalized gold nanoparticles as a simple colorimetric probe for sensitive and selective detection of dopamine
- Khanyile, Nokuthula, Krause, Rui W M, Vilakazi, Sibulelo, Torto, Nelson
- Authors: Khanyile, Nokuthula , Krause, Rui W M , Vilakazi, Sibulelo , Torto, Nelson
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195048 , vital:45522 , xlink:href="http://dx.doi.org/10.17159/0379-4350/2019/v72a27"
- Description: A dopamine (DA) colorimetric probe based on the growth and aggregation of un-functionalized gold nanoparticles (AuNPs) is reported. Upon addition of AuNPs to dopamine at various concentrations, the shape, size and colour change of the nanoparticles results in spectral shifts to higher wavelengths and hence colour change is the mode of detection. The colour change can be easily observed by the naked eye from as low as 5.0 nM DA, even under sub-optimal conditions. Under optimal pH conditions the calculated limit of detection was 2.5 nM (3σ). The probe was successfully applied to whole blood sample and showed good selectivity and sensitivity towards DA. The simple, sensitive and selective probe could be an excellent alternative for on-site and immediate detection of DA without the use of instrumentation and would thus be useful for rapid diagnostic applications.
- Full Text:
- Date Issued: 2019
- Authors: Khanyile, Nokuthula , Krause, Rui W M , Vilakazi, Sibulelo , Torto, Nelson
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195048 , vital:45522 , xlink:href="http://dx.doi.org/10.17159/0379-4350/2019/v72a27"
- Description: A dopamine (DA) colorimetric probe based on the growth and aggregation of un-functionalized gold nanoparticles (AuNPs) is reported. Upon addition of AuNPs to dopamine at various concentrations, the shape, size and colour change of the nanoparticles results in spectral shifts to higher wavelengths and hence colour change is the mode of detection. The colour change can be easily observed by the naked eye from as low as 5.0 nM DA, even under sub-optimal conditions. Under optimal pH conditions the calculated limit of detection was 2.5 nM (3σ). The probe was successfully applied to whole blood sample and showed good selectivity and sensitivity towards DA. The simple, sensitive and selective probe could be an excellent alternative for on-site and immediate detection of DA without the use of instrumentation and would thus be useful for rapid diagnostic applications.
- Full Text:
- Date Issued: 2019
Preparation and use of maize tassels’ activated carbon for the adsorption of phenolic compounds in environmental waste water samples
- Olorundare, O F, Msagati, T A M, Okonkwo, J O, Krause, Rui W M, Mamba, Bhekie B
- Authors: Olorundare, O F , Msagati, T A M , Okonkwo, J O , Krause, Rui W M , Mamba, Bhekie B
- Date: 2015
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125331 , vital:35773 , https://doi.org/10.1007/s11356-014-3742-6
- Description: The determination and remediation of three phenolic compounds bisphenol A (BPA), ortho-nitrophenol (o-NTP), parachlorophenol (PCP) in wastewater is reported. The analysis of these molecules in wastewater was done using gas chromatography (GC) × GC time-of-flight mass spectrometry while activated carbon derived from maize tassel was used as an adsorbent. During the experimental procedures, the effect of various parameters such as initial concentration, pH of sample solution, eluent volume, and sample volume on the removal efficiency with respect to the three phenolic compounds was studied. The results showed that maize tassel produced activated carbon (MTAC) cartridge packed solid-phase extraction (SPE) system was able to remove the phenolic compounds effectively (90.84–98.49 %, 80.75–97.11 %, and 78.27–97.08 % for BPA, o-NTP, and PCP, respectively) . The MTAC cartridge packed SPE sorbent performance was compared to commercially produced C18 SPE cartridges and found to be comparable. All the parameters investigated were found to have a notable influence on the adsorption efficiency of the phenolic compounds from wastewaters at different magnitudes.
- Full Text:
- Date Issued: 2015
- Authors: Olorundare, O F , Msagati, T A M , Okonkwo, J O , Krause, Rui W M , Mamba, Bhekie B
- Date: 2015
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125331 , vital:35773 , https://doi.org/10.1007/s11356-014-3742-6
- Description: The determination and remediation of three phenolic compounds bisphenol A (BPA), ortho-nitrophenol (o-NTP), parachlorophenol (PCP) in wastewater is reported. The analysis of these molecules in wastewater was done using gas chromatography (GC) × GC time-of-flight mass spectrometry while activated carbon derived from maize tassel was used as an adsorbent. During the experimental procedures, the effect of various parameters such as initial concentration, pH of sample solution, eluent volume, and sample volume on the removal efficiency with respect to the three phenolic compounds was studied. The results showed that maize tassel produced activated carbon (MTAC) cartridge packed solid-phase extraction (SPE) system was able to remove the phenolic compounds effectively (90.84–98.49 %, 80.75–97.11 %, and 78.27–97.08 % for BPA, o-NTP, and PCP, respectively) . The MTAC cartridge packed SPE sorbent performance was compared to commercially produced C18 SPE cartridges and found to be comparable. All the parameters investigated were found to have a notable influence on the adsorption efficiency of the phenolic compounds from wastewaters at different magnitudes.
- Full Text:
- Date Issued: 2015
Electronic and nonlinear optical properties of 2-(((5-aminonaphthalen-1-yl) imino) methyl) phenol
- Ojo, Nathanael D, Krause, Rui W M, Obi-Egbedi, Nelson O
- Authors: Ojo, Nathanael D , Krause, Rui W M , Obi-Egbedi, Nelson O
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193397 , vital:45328 , xlink:href="https://doi.org/10.1016/j.molliq.2020.114157"
- Description: In this study, solvent dependence of electronic and nonlinear optical properties of a new Schiff base, 2-(((5-aminonaphthalen-1-yl)imino)methyl) phenol (DANOHB), has been investigated. Electronic and optical properties of the Schiff base studied using Uv-visible absorption and fluorescence spectroscopic techniques in solution show that the Schiff base exhibits fluorescence with a quantum yield of 0.21 and a Stokes shift of 39 nm. Quantum chemical calculations were performed on the Schiff base at time-dependent density functional level of theory using Becke-3-Lee-Yang-Parr method with 6-311++G(d,p) basis set. Solvent dependence of the excited state energies (EE), energy gap (ΔE), first-order (β) and second-order (γ) hyperpolarizabilities were studied in gas, cyclohexane and ethanol. The medium perturbed the energy levels which implies that the reactivity, activity and stability of the system are solvent sensitive. The γ is more than thirty times higher than urea (standard NLO material) and this property is further enhanced in less polar medium. Small ΔE and large hyperpolarizabilities obtained for this system suggest its good potential in photonics and nonlinear optical devices.
- Full Text:
- Date Issued: 2020
- Authors: Ojo, Nathanael D , Krause, Rui W M , Obi-Egbedi, Nelson O
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193397 , vital:45328 , xlink:href="https://doi.org/10.1016/j.molliq.2020.114157"
- Description: In this study, solvent dependence of electronic and nonlinear optical properties of a new Schiff base, 2-(((5-aminonaphthalen-1-yl)imino)methyl) phenol (DANOHB), has been investigated. Electronic and optical properties of the Schiff base studied using Uv-visible absorption and fluorescence spectroscopic techniques in solution show that the Schiff base exhibits fluorescence with a quantum yield of 0.21 and a Stokes shift of 39 nm. Quantum chemical calculations were performed on the Schiff base at time-dependent density functional level of theory using Becke-3-Lee-Yang-Parr method with 6-311++G(d,p) basis set. Solvent dependence of the excited state energies (EE), energy gap (ΔE), first-order (β) and second-order (γ) hyperpolarizabilities were studied in gas, cyclohexane and ethanol. The medium perturbed the energy levels which implies that the reactivity, activity and stability of the system are solvent sensitive. The γ is more than thirty times higher than urea (standard NLO material) and this property is further enhanced in less polar medium. Small ΔE and large hyperpolarizabilities obtained for this system suggest its good potential in photonics and nonlinear optical devices.
- Full Text:
- Date Issued: 2020
Co-encapsulation of rifampicin and isoniazid in crude soybean lecithin liposomes
- Nkanga, Christian I, Noundou, Xavier S, Walker, Roderick B, Krause, Rui W M
- Authors: Nkanga, Christian I , Noundou, Xavier S , Walker, Roderick B , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183536 , vital:44005 , xlink:href="https://doi.org/10.17159/0379-4350/2019/v72a11"
- Description: Despite the well-known anti-mycobacterial actions of isoniazid (INH) and rifampicin (RIF), the clinical success of tuberculosis (TB) therapy requires prolonged administration of multiple drugs in high doses, which often result in frequent adverse effects and low patient adherence. Although liposomes are promising candidates for controlled delivery of anti-TB drug, the high cost of synthetic and highly purified natural lipids currently used in liposomal technology might preclude the universal application of therapeutic liposomes. This work aimed at evaluating the potential of a cost-effective lipid material, crude soybean lecithin (CL), to co-encapsulate RIF and INH for liposomal dual delivery. RIF was encapsulated in CL-liposomes with/without cholesterol using film hydration method, after which INH was incorporated using a freeze–thawing technique. Dynamic light scattering, differential scanning calorimetry, X-ray diffraction and dialysis were used for liposome characterization. Liposomes containing CL alone (CLL) exhibited 90%encapsulation efficiency for RIF and 59%for INH. The mean size and surface charge of CLL were 1114nm and –63mV, respectively. In addition, CLL showed a controlled release profile for the co-encapsulated drugs. CLL would be promising vehicles for macrophage-targeting drug delivery. The present findings demonstrate the feasibility of using CL for preparation of combination products for liposomal delivery.
- Full Text:
- Date Issued: 2019
- Authors: Nkanga, Christian I , Noundou, Xavier S , Walker, Roderick B , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183536 , vital:44005 , xlink:href="https://doi.org/10.17159/0379-4350/2019/v72a11"
- Description: Despite the well-known anti-mycobacterial actions of isoniazid (INH) and rifampicin (RIF), the clinical success of tuberculosis (TB) therapy requires prolonged administration of multiple drugs in high doses, which often result in frequent adverse effects and low patient adherence. Although liposomes are promising candidates for controlled delivery of anti-TB drug, the high cost of synthetic and highly purified natural lipids currently used in liposomal technology might preclude the universal application of therapeutic liposomes. This work aimed at evaluating the potential of a cost-effective lipid material, crude soybean lecithin (CL), to co-encapsulate RIF and INH for liposomal dual delivery. RIF was encapsulated in CL-liposomes with/without cholesterol using film hydration method, after which INH was incorporated using a freeze–thawing technique. Dynamic light scattering, differential scanning calorimetry, X-ray diffraction and dialysis were used for liposome characterization. Liposomes containing CL alone (CLL) exhibited 90%encapsulation efficiency for RIF and 59%for INH. The mean size and surface charge of CLL were 1114nm and –63mV, respectively. In addition, CLL showed a controlled release profile for the co-encapsulated drugs. CLL would be promising vehicles for macrophage-targeting drug delivery. The present findings demonstrate the feasibility of using CL for preparation of combination products for liposomal delivery.
- Full Text:
- Date Issued: 2019
A novel dimeric exoglucanase (GH5_38): Biochemical and Structural Characterisation towards its Application in Alkyl Cellobioside Synthesis
- Mafa, Mpho S, Dirr, Heinrich, Malgas, Samkelo, Krause, Rui W M, Pletschke, Brett I
- Authors: Mafa, Mpho S , Dirr, Heinrich , Malgas, Samkelo , Krause, Rui W M , Pletschke, Brett I
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193976 , vital:45412 , xlink:href="https://doi.org/10.3390/molecules25030746"
- Description: An exoglucanase (Exg-D) from the glycoside hydrolase family 5 subfamily 38 (GH5_38) was heterologously expressed and structurally and biochemically characterised at a molecular level for its application in alkyl glycoside synthesis. The purified Exg-D existed in both dimeric and monomeric forms in solution, which showed highest activity on mixed-linked β-glucan (88.0 and 86.7 U/mg protein, respectively) and lichenin (24.5 and 23.7 U/mg protein, respectively). They displayed a broad optimum pH range from 5.5 to 7 and a temperature optimum from 40 to 60 °C. Kinetic studies demonstrated that Exg-D had a higher affinity towards β-glucan, with a Km of 7.9 mg/mL and a kcat of 117.2 s−1, compared to lichenin which had a Km of 21.5 mg/mL and a kcat of 70.0 s−1. The circular dichroism profile of Exg-D showed that its secondary structure consisted of 11% α-helices, 36% β-strands and 53% coils. Exg-D performed transglycosylation using p-nitrophenyl cellobioside as a glycosyl donor and several primary alcohols as acceptors to produce methyl-, ethyl- and propyl-cellobiosides. These products were identified and quantified via thin-layer chromatography (TLC) and liquid chromatography–mass spectrometry (LC-MS). We concluded that Exg-D is a novel and promising oligomeric glycoside hydrolase for the one-step synthesis of alkyl glycosides with more than one monosaccharide unit.
- Full Text:
- Date Issued: 2020
- Authors: Mafa, Mpho S , Dirr, Heinrich , Malgas, Samkelo , Krause, Rui W M , Pletschke, Brett I
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193976 , vital:45412 , xlink:href="https://doi.org/10.3390/molecules25030746"
- Description: An exoglucanase (Exg-D) from the glycoside hydrolase family 5 subfamily 38 (GH5_38) was heterologously expressed and structurally and biochemically characterised at a molecular level for its application in alkyl glycoside synthesis. The purified Exg-D existed in both dimeric and monomeric forms in solution, which showed highest activity on mixed-linked β-glucan (88.0 and 86.7 U/mg protein, respectively) and lichenin (24.5 and 23.7 U/mg protein, respectively). They displayed a broad optimum pH range from 5.5 to 7 and a temperature optimum from 40 to 60 °C. Kinetic studies demonstrated that Exg-D had a higher affinity towards β-glucan, with a Km of 7.9 mg/mL and a kcat of 117.2 s−1, compared to lichenin which had a Km of 21.5 mg/mL and a kcat of 70.0 s−1. The circular dichroism profile of Exg-D showed that its secondary structure consisted of 11% α-helices, 36% β-strands and 53% coils. Exg-D performed transglycosylation using p-nitrophenyl cellobioside as a glycosyl donor and several primary alcohols as acceptors to produce methyl-, ethyl- and propyl-cellobiosides. These products were identified and quantified via thin-layer chromatography (TLC) and liquid chromatography–mass spectrometry (LC-MS). We concluded that Exg-D is a novel and promising oligomeric glycoside hydrolase for the one-step synthesis of alkyl glycosides with more than one monosaccharide unit.
- Full Text:
- Date Issued: 2020
Terminaliamide, a new ceramide and other phytoconstituents from the roots of Terminalia mantaly H. Perrier and their biological activities
- Mbosso, Emmanuel, Siwe-Noundou, Xavier, Fannang, Simon, Song, Achille M, Assob, Jules C N, Hoppe, Heinrich, Krause, Rui W M
- Authors: Mbosso, Emmanuel , Siwe-Noundou, Xavier , Fannang, Simon , Song, Achille M , Assob, Jules C N , Hoppe, Heinrich , Krause, Rui W M
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191779 , vital:45163 , xlink:href="https://doi.org/10.1080/14786419.2019.1647425"
- Description: Terminaliamide (1), a new ceramide was isolated from the roots of Terminalia mantaly H. Perrier (Combretaceae) along with 4 known compounds (2–5). The structures of the compounds were elucidated using 1D and 2D NMR spectroscopy analysis and mass spectrometry. Compound 1 exhibited moderated antibacterial activity towards Staphylococcus aureus with MIC value of 62.5 μg/mL. The crude MeOH extract (TMr) highly reduced Plasmodium falciparum growth with an IC50 value of 10.11 μg/mL, while hexane fraction (F1) highly reduced Trypanosoma brucei brucei growth with an IC50 value of 5.60 µg/mL. All tested samples presented little or no in vitro cytotoxicity on HeLa cell line. The present work confirms that T. mantaly is medicinally important and may be used effectively as an antimicrobial, an antiplasmodial and an antitrypanosomial with promising therapeutic index.
- Full Text:
- Date Issued: 2021
- Authors: Mbosso, Emmanuel , Siwe-Noundou, Xavier , Fannang, Simon , Song, Achille M , Assob, Jules C N , Hoppe, Heinrich , Krause, Rui W M
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191779 , vital:45163 , xlink:href="https://doi.org/10.1080/14786419.2019.1647425"
- Description: Terminaliamide (1), a new ceramide was isolated from the roots of Terminalia mantaly H. Perrier (Combretaceae) along with 4 known compounds (2–5). The structures of the compounds were elucidated using 1D and 2D NMR spectroscopy analysis and mass spectrometry. Compound 1 exhibited moderated antibacterial activity towards Staphylococcus aureus with MIC value of 62.5 μg/mL. The crude MeOH extract (TMr) highly reduced Plasmodium falciparum growth with an IC50 value of 10.11 μg/mL, while hexane fraction (F1) highly reduced Trypanosoma brucei brucei growth with an IC50 value of 5.60 µg/mL. All tested samples presented little or no in vitro cytotoxicity on HeLa cell line. The present work confirms that T. mantaly is medicinally important and may be used effectively as an antimicrobial, an antiplasmodial and an antitrypanosomial with promising therapeutic index.
- Full Text:
- Date Issued: 2021
Mg/Triethylammonium Formate: A Useful System for Reductive Dimerization of Araldehydes into Pinacols;Nitroarenes into Azoarenes and Azoarenes into Hydrazoarenes
- Pamar, M Geeter, Govender, P, Muthusamy, K, Krause, Rui W M
- Authors: Pamar, M Geeter , Govender, P , Muthusamy, K , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125107 , vital:35729 , https://doi.org/10.13005/ojc/290316
- Description: Studies are reported which describes the effectiveness of triethylammonium formate in the presence of magnesium for the efficient intermolecular pinacol coupling using MeOH as solvent. Various aromatic carbonyls underwent smooth reductive coupling to give the corresponding 1,2-diols. A series of azo compounds were obtained by the reductive coupling of nitroaromatics while azo compounds were reduced to the corresponding hydrazoarenes by this system. There was no adverse effect on the other reducible and hydrogenolysable groups such as ether linkage, hydroxy and halogens. The reactions are clean, high yielding and inexpensive. All the reactions proceeded smoothly at ambient temperature.
- Full Text:
- Date Issued: 2013
- Authors: Pamar, M Geeter , Govender, P , Muthusamy, K , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125107 , vital:35729 , https://doi.org/10.13005/ojc/290316
- Description: Studies are reported which describes the effectiveness of triethylammonium formate in the presence of magnesium for the efficient intermolecular pinacol coupling using MeOH as solvent. Various aromatic carbonyls underwent smooth reductive coupling to give the corresponding 1,2-diols. A series of azo compounds were obtained by the reductive coupling of nitroaromatics while azo compounds were reduced to the corresponding hydrazoarenes by this system. There was no adverse effect on the other reducible and hydrogenolysable groups such as ether linkage, hydroxy and halogens. The reactions are clean, high yielding and inexpensive. All the reactions proceeded smoothly at ambient temperature.
- Full Text:
- Date Issued: 2013
Blending problem-based learning and peer-led team learning, in an open ended ‘home-grown’pharmaceutical chemistry case study
- Sewry, Joyce D, Veale, Clinton G L, Krause, Rui W M
- Authors: Sewry, Joyce D , Veale, Clinton G L , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125691 , vital:35809 , https://doi.org/10.1039/C7RP00180K
- Description: Pharmaceutical chemistry, medicinal chemistry and the drug discovery process require experienced practitioners to employ reasoned speculation in generating creative ideas, which can be used to evolve promising molecules into drugs. The ever-evolving world of pharmaceutical chemistry requires university curricula that prepare graduates for their role as designers with the capability of applying complex concepts in pharmaceutical chemistry, thereby improving the decision-making process. Common methods of teaching drug discovery, including the linear nature of the traditional case study model, do not provide a realistic picture of the underlying complexity of the process, nor do they equip students with the appropriate tools for personal sense making and abstraction. In this work, we discuss the creation of an open-ended, nonlinear case study for 3rd year pharmaceutical chemistry students, developed from drug discovery research conducted at Rhodes University. Furthermore, we discuss blending problem based learning (PBL) with peer-led team learning (PLTL) in the context of curriculum transformation, underpinned by the theory of semantic waves, to assist students in the early attainment of abstract concepts and answer questions of contextualisation, personal sense making, relatability, relevance and ultimately the skills for lifelong learning.
- Full Text:
- Date Issued: 2018
- Authors: Sewry, Joyce D , Veale, Clinton G L , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125691 , vital:35809 , https://doi.org/10.1039/C7RP00180K
- Description: Pharmaceutical chemistry, medicinal chemistry and the drug discovery process require experienced practitioners to employ reasoned speculation in generating creative ideas, which can be used to evolve promising molecules into drugs. The ever-evolving world of pharmaceutical chemistry requires university curricula that prepare graduates for their role as designers with the capability of applying complex concepts in pharmaceutical chemistry, thereby improving the decision-making process. Common methods of teaching drug discovery, including the linear nature of the traditional case study model, do not provide a realistic picture of the underlying complexity of the process, nor do they equip students with the appropriate tools for personal sense making and abstraction. In this work, we discuss the creation of an open-ended, nonlinear case study for 3rd year pharmaceutical chemistry students, developed from drug discovery research conducted at Rhodes University. Furthermore, we discuss blending problem based learning (PBL) with peer-led team learning (PLTL) in the context of curriculum transformation, underpinned by the theory of semantic waves, to assist students in the early attainment of abstract concepts and answer questions of contextualisation, personal sense making, relatability, relevance and ultimately the skills for lifelong learning.
- Full Text:
- Date Issued: 2018
In vitro antimalarial, antitrypanosomal and HIV-1 integrase inhibitory activities of two Cameroonian medicinal plants
- Fouokeng, Yannick, Feumo Feusso, H M, Mbosso Teinkela, Jean E, Siwe-Noundou, Xavier, Wintjens, René T, Isaacs, Michelle, Hoppe, Heinrich, Krause, Rui W M, Azébazé, Anatole G B, Vardamides, Juliette C
- Authors: Fouokeng, Yannick , Feumo Feusso, H M , Mbosso Teinkela, Jean E , Siwe-Noundou, Xavier , Wintjens, René T , Isaacs, Michelle , Hoppe, Heinrich , Krause, Rui W M , Azébazé, Anatole G B , Vardamides, Juliette C
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195014 , vital:45519 , xlink:href="https://doi.org/10.1016/j.sajb.2018.10.008"
- Description: Antiplasmodial, antitrypanosomal and anti-HIV-1 activities of crude extracts, fractions and some isolated compounds from two Cameroonian medicinal plants: Antrocaryon klaineanum Pierre (Anacardiaceae) and Diospyros conocarpa Gürke ex K. Schum. (Ebenaceae) were assessed. The phytochemical studies led to the isolation of eight compounds (1–8) from Diospyros conocarpa and six compounds (6, 9–13) from Antrocaryon klaineanum. These compounds were identified as mangiferolic acid (1), 3β, 22(S)-dihydroxycycloart-24E-en-26-oic acid (2), lupeol (3), aridanin (4), betulin (5), betulinic acid (6), bergenin (7), D-quercitol(8), entilin C(9), entilin A(10), antrocarine A(11), 7R,20(S)-dihydroxy-4,24(28)-ergostadien-3-one(12) and stigmasterol glucoside (13). The criteria for activity were set as follows: an IC50 value more than 10 μg/mL for crude extracts and more than 1 μg/mL for pure compounds. The hexane/ethyl acetate (1:1) fraction of A.klaineanum root bark (AKERF1) and the hexane/ethyl acetate (1:1) fraction of A.klaineanum trunk bark (AKETF1) presented the strongest antiplasmodial activities with IC50 values of 0.4 and 4.4 μg/mL, respectively. Aridanin (4) and antrocarine A(11), as well as the crude extract of D.conocarpa roots (EDCR), AKERF1 and AKETF1 showed moderate trypanocidal effects. The crude extract of A.klaineanum root bark (AKER) and AKETF1 exhibited attractive activities on HIV-1 integrase with IC50 values of 1.96 and 24.04 μg/mL, respectively. The results provide baseline information on the use of A.klaineanum and D.conocarpa extracts, as well as certain components, as sources of new antiplasmodial, antitrypanosomal and anti-HIV drugs.
- Full Text:
- Date Issued: 2019
- Authors: Fouokeng, Yannick , Feumo Feusso, H M , Mbosso Teinkela, Jean E , Siwe-Noundou, Xavier , Wintjens, René T , Isaacs, Michelle , Hoppe, Heinrich , Krause, Rui W M , Azébazé, Anatole G B , Vardamides, Juliette C
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195014 , vital:45519 , xlink:href="https://doi.org/10.1016/j.sajb.2018.10.008"
- Description: Antiplasmodial, antitrypanosomal and anti-HIV-1 activities of crude extracts, fractions and some isolated compounds from two Cameroonian medicinal plants: Antrocaryon klaineanum Pierre (Anacardiaceae) and Diospyros conocarpa Gürke ex K. Schum. (Ebenaceae) were assessed. The phytochemical studies led to the isolation of eight compounds (1–8) from Diospyros conocarpa and six compounds (6, 9–13) from Antrocaryon klaineanum. These compounds were identified as mangiferolic acid (1), 3β, 22(S)-dihydroxycycloart-24E-en-26-oic acid (2), lupeol (3), aridanin (4), betulin (5), betulinic acid (6), bergenin (7), D-quercitol(8), entilin C(9), entilin A(10), antrocarine A(11), 7R,20(S)-dihydroxy-4,24(28)-ergostadien-3-one(12) and stigmasterol glucoside (13). The criteria for activity were set as follows: an IC50 value more than 10 μg/mL for crude extracts and more than 1 μg/mL for pure compounds. The hexane/ethyl acetate (1:1) fraction of A.klaineanum root bark (AKERF1) and the hexane/ethyl acetate (1:1) fraction of A.klaineanum trunk bark (AKETF1) presented the strongest antiplasmodial activities with IC50 values of 0.4 and 4.4 μg/mL, respectively. Aridanin (4) and antrocarine A(11), as well as the crude extract of D.conocarpa roots (EDCR), AKERF1 and AKETF1 showed moderate trypanocidal effects. The crude extract of A.klaineanum root bark (AKER) and AKETF1 exhibited attractive activities on HIV-1 integrase with IC50 values of 1.96 and 24.04 μg/mL, respectively. The results provide baseline information on the use of A.klaineanum and D.conocarpa extracts, as well as certain components, as sources of new antiplasmodial, antitrypanosomal and anti-HIV drugs.
- Full Text:
- Date Issued: 2019
Nanostructured β-cyclodextrin-hyperbranched polyethyleneimine (β-CD-HPEI) embedded in polysulfone membrane for the removal of humic acid from water
- Malinga, S P, Arotiba, O A, Mapolie, S F, Diallo, M S, Mamba, Bhekie B, Krause, Rui W M
- Authors: Malinga, S P , Arotiba, O A , Mapolie, S F , Diallo, M S , Mamba, Bhekie B , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125119 , vital:35732 , https://doi.org/10.1080/01496395.2013.809108
- Description: The synthesis of a new β-cyclodextrin-hyperbranched polyethyleneimine (β-CD-HPEI)/polysulfone (PSf) membranes via interfacial polymerization of trimesoyl chloride and β-CD-HPEI is described in this paper. The membranes were characterized by atomic force microscopy (AFM), high resolution scanning electron microscopy (HR-SEM) and contact-angle measurements. Water permeability and rejection data were obtained using a cross-flow filtration system at 0.69 MPa. The membranes were hydrophilic (25° to 63°), showed high humic acid rejection (>amp;80%), and maintained a constant flux throughout the filtration. The modified membranes were rougher than the pristine PSf membranes but they exhibited better antifouling properties due to the hydrophilic surface which acted as a barrier against humic acid deposition. The modification of PSf with β-CD-HPEI resulted in enhanced hydrophilicity and water permeability while still maintaining high humic acid rejection. Supplemental materials are available for this article. Go to the publisher's online edition of Separation Science & Technology to view the supplemental file.
- Full Text:
- Date Issued: 2013
- Authors: Malinga, S P , Arotiba, O A , Mapolie, S F , Diallo, M S , Mamba, Bhekie B , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125119 , vital:35732 , https://doi.org/10.1080/01496395.2013.809108
- Description: The synthesis of a new β-cyclodextrin-hyperbranched polyethyleneimine (β-CD-HPEI)/polysulfone (PSf) membranes via interfacial polymerization of trimesoyl chloride and β-CD-HPEI is described in this paper. The membranes were characterized by atomic force microscopy (AFM), high resolution scanning electron microscopy (HR-SEM) and contact-angle measurements. Water permeability and rejection data were obtained using a cross-flow filtration system at 0.69 MPa. The membranes were hydrophilic (25° to 63°), showed high humic acid rejection (>amp;80%), and maintained a constant flux throughout the filtration. The modified membranes were rougher than the pristine PSf membranes but they exhibited better antifouling properties due to the hydrophilic surface which acted as a barrier against humic acid deposition. The modification of PSf with β-CD-HPEI resulted in enhanced hydrophilicity and water permeability while still maintaining high humic acid rejection. Supplemental materials are available for this article. Go to the publisher's online edition of Separation Science & Technology to view the supplemental file.
- Full Text:
- Date Issued: 2013
Encapsulation and physicochemical evaluation of efavirenz in liposomes
- Okafor, Nnamdi Ikemefuna, Nkanga, Christian I, Walker, Roderick B, Noundou, Xavier S, Krause, Rui W M
- Authors: Okafor, Nnamdi Ikemefuna , Nkanga, Christian I , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183414 , vital:43988 , xlink:href="https://doi.org/10.1007/s40005-019-00458-8"
- Description: Antiretroviral therapy remains the most efective means of managing the human immune defciency virus/acquired immune defciency syndrome (HIV/AIDS). Application of therapeutics has been hampered by factors including poor bioavailability of most anti-retroviral compounds (ARV), side efects and an alarming emergence of drug resistant strains of the virus. Recent developments and use of drug delivery systems (DDS) has shown potential for improving the pharmacological profle of ARV. Amongst these complex DDS, liposomes have been explored for delivery of ARV. In this study, we have aimed at exploring efcient encapsulation of efavirenz (EFV), a potent ARV using diferent mass ratios of crude soybean lecithin and cholesterol. The EFV-loaded liposomes (EFL) were prepared using thin flm hydration and evaluated for particle size, zeta potential (ZP), encapsulation efciency (EE%), morphology and drug release studies. Diferential scanning calorimetry (DSC), X-ray difraction (XRD), energy dispersity spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy were used for comprehensive physicochemical characterization of EFL. EFL exhibited high encapsulation (99%) in 1:1 crude lecithin to cholesterol mass ratio. The average particle size and Zeta Potential of EFL were found to be 411.10±7.40 nm and −53.5.3±0.06 mV, respectively. EFL showed a relatively controlled EFV release behaviour that was similar to the dissolution profle of un-encapsulated EFV. This suggests that EFL represents a promising vehicle for efective EFV delivery while providing the advantages of a nano-scaled delivery system
- Full Text:
- Date Issued: 2020
- Authors: Okafor, Nnamdi Ikemefuna , Nkanga, Christian I , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183414 , vital:43988 , xlink:href="https://doi.org/10.1007/s40005-019-00458-8"
- Description: Antiretroviral therapy remains the most efective means of managing the human immune defciency virus/acquired immune defciency syndrome (HIV/AIDS). Application of therapeutics has been hampered by factors including poor bioavailability of most anti-retroviral compounds (ARV), side efects and an alarming emergence of drug resistant strains of the virus. Recent developments and use of drug delivery systems (DDS) has shown potential for improving the pharmacological profle of ARV. Amongst these complex DDS, liposomes have been explored for delivery of ARV. In this study, we have aimed at exploring efcient encapsulation of efavirenz (EFV), a potent ARV using diferent mass ratios of crude soybean lecithin and cholesterol. The EFV-loaded liposomes (EFL) were prepared using thin flm hydration and evaluated for particle size, zeta potential (ZP), encapsulation efciency (EE%), morphology and drug release studies. Diferential scanning calorimetry (DSC), X-ray difraction (XRD), energy dispersity spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy were used for comprehensive physicochemical characterization of EFL. EFL exhibited high encapsulation (99%) in 1:1 crude lecithin to cholesterol mass ratio. The average particle size and Zeta Potential of EFL were found to be 411.10±7.40 nm and −53.5.3±0.06 mV, respectively. EFL showed a relatively controlled EFV release behaviour that was similar to the dissolution profle of un-encapsulated EFV. This suggests that EFL represents a promising vehicle for efective EFV delivery while providing the advantages of a nano-scaled delivery system
- Full Text:
- Date Issued: 2020
In vitro antimicrobial activity of the methanol extract and compounds from the wood of Ficus elastica Roxb. ex Hornem. aerial roots
- Meyer, Franck, Fannang, Simone Véronique, Noundou, Xavier Siwe, Krause, Rui W M, Teinkela, Jean Emmanuel Mbosso, Vardamides, Juliette Cathérine, Mpondo, Albert Emmanuel Mpondo, Azebaze, Anatole Guy Blaise, Nguedia, Jules Clément Assob
- Authors: Meyer, Franck , Fannang, Simone Véronique , Noundou, Xavier Siwe , Krause, Rui W M , Teinkela, Jean Emmanuel Mbosso , Vardamides, Juliette Cathérine , Mpondo, Albert Emmanuel Mpondo , Azebaze, Anatole Guy Blaise , Nguedia, Jules Clément Assob
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126154 , vital:35854 , https://doi.org/10.1016/j.sajb.2017.03.026
- Description: Ficus elastica Roxb. ex Hornem., an edible plant belonging to the family of Moraceae, is traditionally used against skin infections and allergies besides having diuretic properties. This study aimed at investigating the antimicrobial activity of the wood of F. elastica aerial roots against a set of bacteria (Staphylococcus aureus; Escherichia coli, Proteus vulgaris, Providencia stuartii and Pseudomonas aeruginosa) and a yeast (Candida albicans). A mixture of linear aliphatic alkanes with n-hexacosane as major compound, β-sitosterol, biochanin A, sitosteryl 3-O-β-D-glucopyranoside (1), elasticamide (2), elastiquinone (3) and ficusoside B (4) were purified and characterized. Antimicrobial activities, expressed as minimum inhibitory concentration (MIC), indicated that the methanol extract showed MIC of 39.1 μg/mL; the lowest values were obtained for 3 and 4, with MIC as low as 4.9 μg/mL, smaller than the values of reference antibiotics (25 μg/mL). Furthermore, as most of the studied samples exhibited Minimum Microbicidal Concentration/Minimum Inhibitory Concentration (MMC/MIC) ratios lower than 4, a microbicidal effect was clearly exhibited. The overall results provided evidence that the wood of F. elastica aerial roots, as well as some of its isolated components might be potential sources of new antimicrobial drugs.
- Full Text:
- Date Issued: 2017
- Authors: Meyer, Franck , Fannang, Simone Véronique , Noundou, Xavier Siwe , Krause, Rui W M , Teinkela, Jean Emmanuel Mbosso , Vardamides, Juliette Cathérine , Mpondo, Albert Emmanuel Mpondo , Azebaze, Anatole Guy Blaise , Nguedia, Jules Clément Assob
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126154 , vital:35854 , https://doi.org/10.1016/j.sajb.2017.03.026
- Description: Ficus elastica Roxb. ex Hornem., an edible plant belonging to the family of Moraceae, is traditionally used against skin infections and allergies besides having diuretic properties. This study aimed at investigating the antimicrobial activity of the wood of F. elastica aerial roots against a set of bacteria (Staphylococcus aureus; Escherichia coli, Proteus vulgaris, Providencia stuartii and Pseudomonas aeruginosa) and a yeast (Candida albicans). A mixture of linear aliphatic alkanes with n-hexacosane as major compound, β-sitosterol, biochanin A, sitosteryl 3-O-β-D-glucopyranoside (1), elasticamide (2), elastiquinone (3) and ficusoside B (4) were purified and characterized. Antimicrobial activities, expressed as minimum inhibitory concentration (MIC), indicated that the methanol extract showed MIC of 39.1 μg/mL; the lowest values were obtained for 3 and 4, with MIC as low as 4.9 μg/mL, smaller than the values of reference antibiotics (25 μg/mL). Furthermore, as most of the studied samples exhibited Minimum Microbicidal Concentration/Minimum Inhibitory Concentration (MMC/MIC) ratios lower than 4, a microbicidal effect was clearly exhibited. The overall results provided evidence that the wood of F. elastica aerial roots, as well as some of its isolated components might be potential sources of new antimicrobial drugs.
- Full Text:
- Date Issued: 2017
Clinically established biodegradable long acting injectables
- Nkanga, Christian I, Fisch, Andreas, Rad-Malkshahi, Mazda, Romic, Marieta D, Kittel, Birgit, Ullrich, Thomas, Wang, Jing, Krause, Rui W M, Adler, Sabine, Lammers, Twan, Hennink, Wim E, Ramazani, Farshad
- Authors: Nkanga, Christian I , Fisch, Andreas , Rad-Malkshahi, Mazda , Romic, Marieta D , Kittel, Birgit , Ullrich, Thomas , Wang, Jing , Krause, Rui W M , Adler, Sabine , Lammers, Twan , Hennink, Wim E , Ramazani, Farshad
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193386 , vital:45327 , xlink:href="https://doi.org/10.1016/j.addr.2020.11.008"
- Description: Long acting injectable formulations have been developed to sustain the action of drugs in the body over desired periods of time. These delivery platforms have been utilized for both systemic and local drug delivery applications. This review gives an overview of long acting injectable systems that are currently in clinical use. These products are categorized in three different groups: biodegradable polymeric systems, including microparticles and implants; micro and nanocrystal suspensions and oil-based formulations. Furthermore, the applications of these drug delivery platforms for the management of various chronic diseases are summarized. Finally, this review addresses industrial challenges regarding the development of long acting injectable formulations.
- Full Text:
- Date Issued: 2020
- Authors: Nkanga, Christian I , Fisch, Andreas , Rad-Malkshahi, Mazda , Romic, Marieta D , Kittel, Birgit , Ullrich, Thomas , Wang, Jing , Krause, Rui W M , Adler, Sabine , Lammers, Twan , Hennink, Wim E , Ramazani, Farshad
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193386 , vital:45327 , xlink:href="https://doi.org/10.1016/j.addr.2020.11.008"
- Description: Long acting injectable formulations have been developed to sustain the action of drugs in the body over desired periods of time. These delivery platforms have been utilized for both systemic and local drug delivery applications. This review gives an overview of long acting injectable systems that are currently in clinical use. These products are categorized in three different groups: biodegradable polymeric systems, including microparticles and implants; micro and nanocrystal suspensions and oil-based formulations. Furthermore, the applications of these drug delivery platforms for the management of various chronic diseases are summarized. Finally, this review addresses industrial challenges regarding the development of long acting injectable formulations.
- Full Text:
- Date Issued: 2020
Steam activation, characterisation and adsorption studies of activated carbon from maize tassels.
- Olorundare, O F, Msagati, Titus A, Krause, Rui W M, Okonkwo, J O, Mamba, Bhekie B
- Authors: Olorundare, O F , Msagati, Titus A , Krause, Rui W M , Okonkwo, J O , Mamba, Bhekie B
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123847 , vital:35507 , https://doi.org/10.1080/02757540.2013.877001
- Description: In this paper, steam-produced activated carbon (STAC) from maize tassel (MT) was evaluated for its ability to remove basic dye (methylene blue MB) from aqueous solution in a batch adsorption process. The equilibrium experiments were conducted in the range of 50–300 mg/L initial MB concentrations at 30°C, for effect of pH, adsorbent dosage and contact time. The experimental data were analysed by Langmuir, Freundlich and Temkin isotherm models of adsorption. Freundlich adsorption isotherm was found to have highest value of R2(R2=0.97) compared to other models of Langmuir and Temkin having (0.96 and 0.95 respectively). STAC has a high adsorptive capacity for MB dye (200 mg/g) and also showed favourable adsorption for the dye with the separation factor for the dye-activated carbon system. The kinetic data obtained were analysed using pseudo first-order kinetic equation and pseudo second-order kinetic equation. The experimental data fitted well into pseudo second-order kinetic equation, as demonstrated by the high value of R2.
- Full Text:
- Date Issued: 2014
- Authors: Olorundare, O F , Msagati, Titus A , Krause, Rui W M , Okonkwo, J O , Mamba, Bhekie B
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123847 , vital:35507 , https://doi.org/10.1080/02757540.2013.877001
- Description: In this paper, steam-produced activated carbon (STAC) from maize tassel (MT) was evaluated for its ability to remove basic dye (methylene blue MB) from aqueous solution in a batch adsorption process. The equilibrium experiments were conducted in the range of 50–300 mg/L initial MB concentrations at 30°C, for effect of pH, adsorbent dosage and contact time. The experimental data were analysed by Langmuir, Freundlich and Temkin isotherm models of adsorption. Freundlich adsorption isotherm was found to have highest value of R2(R2=0.97) compared to other models of Langmuir and Temkin having (0.96 and 0.95 respectively). STAC has a high adsorptive capacity for MB dye (200 mg/g) and also showed favourable adsorption for the dye with the separation factor for the dye-activated carbon system. The kinetic data obtained were analysed using pseudo first-order kinetic equation and pseudo second-order kinetic equation. The experimental data fitted well into pseudo second-order kinetic equation, as demonstrated by the high value of R2.
- Full Text:
- Date Issued: 2014
5-Fu inclusion complex capped gold nanoparticles for breast cancer therapy
- Lakkakula, Jaya R, Krause, Rui W M, Divakaran, Deepika, Barage, Sagar, Srivastava, Rohit
- Authors: Lakkakula, Jaya R , Krause, Rui W M , Divakaran, Deepika , Barage, Sagar , Srivastava, Rohit
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191713 , vital:45150 , xlink:href="https://doi.org/10.1016/j.molliq.2021.117262"
- Description: We have attempted to prolong the circulation time and increase the solubility of 5-Fluorouracil by complexing it with cyclodextrin and then further conjugating onto the gold nanoparticle to form 5Fu ICAu. The 1H NMR and molecular docking studies suggested that 5-Fu was included within the 2HP-β-CD cavity and H-5 proton probably serves as the binding site for stabilization of the inclusion complex. The 5Fu-ICAu showed higher cell inhibition rate when studied on MDA-MB-231 and MCF-7 breast cancer cell lines due to the enhanced permeability and retention (EPR) effect by allowing the selective accumulation of nanoparticles at tumor site. This unique system can serve as a novel nanocarrier for delivery of hydrophobic drugs.
- Full Text:
- Date Issued: 2021
- Authors: Lakkakula, Jaya R , Krause, Rui W M , Divakaran, Deepika , Barage, Sagar , Srivastava, Rohit
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191713 , vital:45150 , xlink:href="https://doi.org/10.1016/j.molliq.2021.117262"
- Description: We have attempted to prolong the circulation time and increase the solubility of 5-Fluorouracil by complexing it with cyclodextrin and then further conjugating onto the gold nanoparticle to form 5Fu ICAu. The 1H NMR and molecular docking studies suggested that 5-Fu was included within the 2HP-β-CD cavity and H-5 proton probably serves as the binding site for stabilization of the inclusion complex. The 5Fu-ICAu showed higher cell inhibition rate when studied on MDA-MB-231 and MCF-7 breast cancer cell lines due to the enhanced permeability and retention (EPR) effect by allowing the selective accumulation of nanoparticles at tumor site. This unique system can serve as a novel nanocarrier for delivery of hydrophobic drugs.
- Full Text:
- Date Issued: 2021
In vitro antimalarial, antitrypanosomal and HIV-1 integrase inhibitory activities of two Cameroonian medicinal plants: Antrocaryon klaineanum (Anacardiaceae) and Diospyros conocarpa (Ebenaceae)
- Fouokeng, Y, Feusso, H M Feumo, Noundou, Xavier S, Krause, Rui W M, Teinkela, Jean E Mb, Wintjens, R, Hoppe, Heinrich C, Azebaze, Anatole G B, Vardamides, Juliette C, Isaacs, Michelle
- Authors: Fouokeng, Y , Feusso, H M Feumo , Noundou, Xavier S , Krause, Rui W M , Teinkela, Jean E Mb , Wintjens, R , Hoppe, Heinrich C , Azebaze, Anatole G B , Vardamides, Juliette C , Isaacs, Michelle
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126653 , vital:35908 , https://doi.org/10.1016/j.sajb.2018.10.008
- Description: Antiplasmodial, antitrypanosomal and anti-HIV-1 activities of crude extracts, fractions and some isolated compounds from two Cameroonian medicinal plants: Antrocaryon klaineanum Pierre (Anacardiaceae) and Diospyros conocarpa Gürke ex K. Schum. (Ebenaceae) were assessed. The phytochemical studies led to the isolation of eight compounds (1–8) from Diospyros conocarpa and six compounds (6, 9–13) from Antrocaryon klaineanum. These compounds were identified as mangiferolic acid (1), 3β, 22(S)-dihydroxycycloart-24E-en-26-oic acid (2), lupeol (3), aridanin (4), betulin (5), betulinic acid (6), bergenin (7), D-quercitol(8), entilin C(9), entilin A(10), antrocarine A(11), 7R,20(S)-dihydroxy-4,24(28)-ergostadien-3-one(12) and stigmasterol glucoside (13). The criteria for activity were set as follows: an IC50 value
- Full Text:
- Date Issued: 2018
- Authors: Fouokeng, Y , Feusso, H M Feumo , Noundou, Xavier S , Krause, Rui W M , Teinkela, Jean E Mb , Wintjens, R , Hoppe, Heinrich C , Azebaze, Anatole G B , Vardamides, Juliette C , Isaacs, Michelle
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126653 , vital:35908 , https://doi.org/10.1016/j.sajb.2018.10.008
- Description: Antiplasmodial, antitrypanosomal and anti-HIV-1 activities of crude extracts, fractions and some isolated compounds from two Cameroonian medicinal plants: Antrocaryon klaineanum Pierre (Anacardiaceae) and Diospyros conocarpa Gürke ex K. Schum. (Ebenaceae) were assessed. The phytochemical studies led to the isolation of eight compounds (1–8) from Diospyros conocarpa and six compounds (6, 9–13) from Antrocaryon klaineanum. These compounds were identified as mangiferolic acid (1), 3β, 22(S)-dihydroxycycloart-24E-en-26-oic acid (2), lupeol (3), aridanin (4), betulin (5), betulinic acid (6), bergenin (7), D-quercitol(8), entilin C(9), entilin A(10), antrocarine A(11), 7R,20(S)-dihydroxy-4,24(28)-ergostadien-3-one(12) and stigmasterol glucoside (13). The criteria for activity were set as follows: an IC50 value
- Full Text:
- Date Issued: 2018
Comparison between base metals and platinum group metals in nitrogen, M codoped TiO 2 (M= Fe, Cu, Pd, Os) for photocatalytic removal of an organic dye in water
- Kuvarega, Alex T, Mamba, Bhekie B, Krause, Rui W M
- Authors: Kuvarega, Alex T , Mamba, Bhekie B , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125129 , vital:35734 , https://doi.org/10.1155/2014/962102
- Description: The photocatalytic performance of a number of nonmetal and metal codoped TiO2 for the degradation of eosin yellow under simulated solar radiation was investigated. The synthesised materials were characterised by FTIR, Raman spectroscopy, XRD, DRUV-Vis, SEM, and TEM.The N, metal codoped TiO2 containing 0.5 wt.% of the metal consisted mainly of the anatase phase, with a particle size range of 15–28 nm. The particles were largely spherical and shifted the absorption edge well into the visible region. Band gap reduction was more pronounced for the N, PGM codoped TiO2 compared to N, base metal codoped samples. Codoping led to an enhancement in the photocatalytic activity of the materials for the degradation of eosin yellow. N, Pd codoped TiO2 was the most effective photocatalyst (99.9% dye removal) while N, Cu codoped TiO2 showed the least activity (25.5% removal). The mechanism for the photocatalytic enhancement was proposed on the basis of formation of an electron deficient Schottky barrier at the semiconductor-metal interface, which acts as an electron sink and thus retards electron-hole recombination. It was shown that the ability of the photocatalyst to degrade the dye depends on the nature and type of the metal dopant in the codoped TiO2 system.
- Full Text:
- Date Issued: 2014
- Authors: Kuvarega, Alex T , Mamba, Bhekie B , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125129 , vital:35734 , https://doi.org/10.1155/2014/962102
- Description: The photocatalytic performance of a number of nonmetal and metal codoped TiO2 for the degradation of eosin yellow under simulated solar radiation was investigated. The synthesised materials were characterised by FTIR, Raman spectroscopy, XRD, DRUV-Vis, SEM, and TEM.The N, metal codoped TiO2 containing 0.5 wt.% of the metal consisted mainly of the anatase phase, with a particle size range of 15–28 nm. The particles were largely spherical and shifted the absorption edge well into the visible region. Band gap reduction was more pronounced for the N, PGM codoped TiO2 compared to N, base metal codoped samples. Codoping led to an enhancement in the photocatalytic activity of the materials for the degradation of eosin yellow. N, Pd codoped TiO2 was the most effective photocatalyst (99.9% dye removal) while N, Cu codoped TiO2 showed the least activity (25.5% removal). The mechanism for the photocatalytic enhancement was proposed on the basis of formation of an electron deficient Schottky barrier at the semiconductor-metal interface, which acts as an electron sink and thus retards electron-hole recombination. It was shown that the ability of the photocatalyst to degrade the dye depends on the nature and type of the metal dopant in the codoped TiO2 system.
- Full Text:
- Date Issued: 2014
Biological activity of plant extracts and isolated compounds from Alchornea laxiflora: Anti-HIV, antibacterial and cytotoxicity evaluation
- Ndinteh, Derek T, Olivier, D K, Noundou, Xavier S, Krause, Rui W M, Mnkandhla, D, Isaacs, Michelle, Hoppe, Heinrich C, Muganza, F M, Mbafor, J T, Van Vuuren, S F, Patnala, S
- Authors: Ndinteh, Derek T , Olivier, D K , Noundou, Xavier S , Krause, Rui W M , Mnkandhla, D , Isaacs, Michelle , Hoppe, Heinrich C , Muganza, F M , Mbafor, J T , Van Vuuren, S F , Patnala, S
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126634 , vital:35907 , https://doi.org/10.1016/j.sajb.2018.08.010
- Description: This study was designed to assess the cytotoxicity, anti-HIV and antibacterial efficacy of various solvent extracts of roots, stem and leaves of Alchornea laxiflora, as well as five compounds isolated from its methanolic stem extract viz.; ellagic acid (1); 3-O-methyl-ellagic acid (2), 3-O-β-d-glucopyranosyl-β-sitosterol (3), 3-O-acetyl-oleanolic acid (4) and 3-O-acetyl-ursolic acid (5). The tested crude extracts were prepared from several solvent polarities including: hexane (Hex), chloroform (CHCl3), ethyl acetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O). The anti-HIV properties were assessed on HIV-1 subtype C integrase while the cytotoxicity was tested against Hela cells. The antibacterial activity was studied on a panel of pathogens including gastrointestinal, skin, respiratory and urinary-tract infection causing Gram positive bacteria viz.; Bacillus cereus (ATCC 11778), Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 25923) and Staphylococcus saprophyticus (ATCC 15305)] and Gram-negative bacteria, i.e., Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 13883), Moraxella catarrhalis (ATCC 23246). All the tested samples were determined to be non-toxic due to the low inhibitions observed. The most potent anti-HIV activity was observed for the methanolic extract of A. laxiflora root (ALR4) with an IC50 value of 0.21 ng/ml, which was more active than chicoric acid used as reference drug (6.82 nM). Roots, stem and leaves of A. laxiflora extracts exhibited antibacterial activities against most of the Gram-positive bacteria with the minimum inhibitory concentrations (MIC) ranging between 50 and 63 μg/ml. Compounds 1–5 displayed antibacterial activities against S. saprophyticus with MIC values as low as 4 μg/ml. The results inferred from this study demonstrate the potential of A. laxiflora root as a source for new anti-HIV drugs and scientifically validate the traditional use of A. laxiflora in the treatment of gastrointestinal, skin, respiratory and urinary tract related infections. These results reaffirm the ethnopharmacological significance of African traditional medicines.
- Full Text:
- Date Issued: 2018
- Authors: Ndinteh, Derek T , Olivier, D K , Noundou, Xavier S , Krause, Rui W M , Mnkandhla, D , Isaacs, Michelle , Hoppe, Heinrich C , Muganza, F M , Mbafor, J T , Van Vuuren, S F , Patnala, S
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126634 , vital:35907 , https://doi.org/10.1016/j.sajb.2018.08.010
- Description: This study was designed to assess the cytotoxicity, anti-HIV and antibacterial efficacy of various solvent extracts of roots, stem and leaves of Alchornea laxiflora, as well as five compounds isolated from its methanolic stem extract viz.; ellagic acid (1); 3-O-methyl-ellagic acid (2), 3-O-β-d-glucopyranosyl-β-sitosterol (3), 3-O-acetyl-oleanolic acid (4) and 3-O-acetyl-ursolic acid (5). The tested crude extracts were prepared from several solvent polarities including: hexane (Hex), chloroform (CHCl3), ethyl acetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O). The anti-HIV properties were assessed on HIV-1 subtype C integrase while the cytotoxicity was tested against Hela cells. The antibacterial activity was studied on a panel of pathogens including gastrointestinal, skin, respiratory and urinary-tract infection causing Gram positive bacteria viz.; Bacillus cereus (ATCC 11778), Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 25923) and Staphylococcus saprophyticus (ATCC 15305)] and Gram-negative bacteria, i.e., Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 13883), Moraxella catarrhalis (ATCC 23246). All the tested samples were determined to be non-toxic due to the low inhibitions observed. The most potent anti-HIV activity was observed for the methanolic extract of A. laxiflora root (ALR4) with an IC50 value of 0.21 ng/ml, which was more active than chicoric acid used as reference drug (6.82 nM). Roots, stem and leaves of A. laxiflora extracts exhibited antibacterial activities against most of the Gram-positive bacteria with the minimum inhibitory concentrations (MIC) ranging between 50 and 63 μg/ml. Compounds 1–5 displayed antibacterial activities against S. saprophyticus with MIC values as low as 4 μg/ml. The results inferred from this study demonstrate the potential of A. laxiflora root as a source for new anti-HIV drugs and scientifically validate the traditional use of A. laxiflora in the treatment of gastrointestinal, skin, respiratory and urinary tract related infections. These results reaffirm the ethnopharmacological significance of African traditional medicines.
- Full Text:
- Date Issued: 2018
Phytochemical, anti-inflammatory and anti-trypanosomal properties of Anthocleista vogelii Planch (Loganiaceae) stem bark
- Eze, Fabian I, Siwe-Noundou, Xavier, Osadebe, Patience, Krause, Rui W M
- Authors: Eze, Fabian I , Siwe-Noundou, Xavier , Osadebe, Patience , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194059 , vital:45419 , xlink:href="https://doi.org/10.1016/j.jep.2019.111851"
- Description: Ethnopharmacological relevance: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. Aim of the study: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. Materials and methods: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced rat paw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. Results: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 μg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p less than 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. Conclusion: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.
- Full Text:
- Date Issued: 2019
- Authors: Eze, Fabian I , Siwe-Noundou, Xavier , Osadebe, Patience , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194059 , vital:45419 , xlink:href="https://doi.org/10.1016/j.jep.2019.111851"
- Description: Ethnopharmacological relevance: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. Aim of the study: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. Materials and methods: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced rat paw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. Results: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 μg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p less than 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. Conclusion: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.
- Full Text:
- Date Issued: 2019