Inhibitory effects of selected cannabinoids against dipeptidyl peptidase IV, an enzyme linked to type 2 diabetes
- Mkabayi, Lithalethu, Viljoen, Zenobia, Krause, Rui W M, Lobb, Kevin A, Pletschke, Brett I, Frost, Carminita L
- Authors: Mkabayi, Lithalethu , Viljoen, Zenobia , Krause, Rui W M , Lobb, Kevin A , Pletschke, Brett I , Frost, Carminita L
- Date: 2024
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/452760 , vital:75168 , xlink:href="https://doi.org/10.1016/j.heliyon.2023.e23289"
- Description: Ethnopharmacological relevance: In recent times the decriminalisation of cannabis globally has increased its use as an alternative medication. Where it has been used in modern medicinal practises since the 1800s, there is limited scientific investigation to understand the biological activities of this plant. Aim of the study: Dipeptidyl peptidase IV (DPP-IV) plays a key role in regulating glucose homeostasis, and inhibition of this enzyme has been used as a therapeutic approach to treat type 2 diabetes. However, some of the synthetic inhibitors for this enzyme available on the market may cause undesirable side effects. Therefore, it is important to identify new inhibitors of DPP-IV and to understand their interaction with this enzyme.
- Full Text:
- Date Issued: 2024
- Authors: Mkabayi, Lithalethu , Viljoen, Zenobia , Krause, Rui W M , Lobb, Kevin A , Pletschke, Brett I , Frost, Carminita L
- Date: 2024
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/452760 , vital:75168 , xlink:href="https://doi.org/10.1016/j.heliyon.2023.e23289"
- Description: Ethnopharmacological relevance: In recent times the decriminalisation of cannabis globally has increased its use as an alternative medication. Where it has been used in modern medicinal practises since the 1800s, there is limited scientific investigation to understand the biological activities of this plant. Aim of the study: Dipeptidyl peptidase IV (DPP-IV) plays a key role in regulating glucose homeostasis, and inhibition of this enzyme has been used as a therapeutic approach to treat type 2 diabetes. However, some of the synthetic inhibitors for this enzyme available on the market may cause undesirable side effects. Therefore, it is important to identify new inhibitors of DPP-IV and to understand their interaction with this enzyme.
- Full Text:
- Date Issued: 2024
Inclusion complexation and liposomal encapsulation of an isoniazid hydrazone derivative in cyclodextrin for pH-dependent controlled release
- Safari, Justin B, Mona, Lamine B, Sekaleli, Bafokeng T, Avudi, Bénite K, Isamura, Bienfait K, Mukubwa, Grady K, Salami, Sodeeq A, Mbinze, Jérémie K, Lobb, Kevin A, Krause, Rui W M, Nkanga, Christian I
- Authors: Safari, Justin B , Mona, Lamine B , Sekaleli, Bafokeng T , Avudi, Bénite K , Isamura, Bienfait K , Mukubwa, Grady K , Salami, Sodeeq A , Mbinze, Jérémie K , Lobb, Kevin A , Krause, Rui W M , Nkanga, Christian I
- Date: 2023
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/452727 , vital:75166 , xlink:href="https://doi.org/10.1016/j.jddst.2023.104302"
- Description: Tuberculosis, a predominantly pulmonary pathology, is currently the deadliest infection worldwide. Its treatment is based on combination therapy involving selected antimicrobials including Isoniazid. However, physicochemical properties of isoniazid negatively affect the clinical performance of current tuberculosis regimens, causing drug resistance development and increasing mortality rates. Liposomal encapsulation improves antituberculosis drug delivery; however, nano-formulation of isoniazid remains challenging due to its small molecular size and high hydrophilicity. Therefore, this study aimed to derivatize isoniazid and formulate a controlled delivery system using the concept of drug-in-cyclodextrins-in-liposomes to enhance drug biopharmaceutical properties. A prodrug of isoniazid was synthesized and screened for its ability to form stable complexes with α, β, and γ cyclodextrins. A selected inclusion complex with β-cyclodextrin was encapsulated in liposomes and assessed for controlled release of isoniazid. Successful formation of a 1:1 complex was established and characterized, followed by molecular modeling studies to demonstrate strength of the interactions within the complex and predicted complex structure. The inclusion complex was successfully encapsulated in liposomes using the thin film hydration method and the ethanol injection ultrasonic dispersion, with the latter giving the best results. These findings demonstrate the potential.
- Full Text:
- Date Issued: 2023
- Authors: Safari, Justin B , Mona, Lamine B , Sekaleli, Bafokeng T , Avudi, Bénite K , Isamura, Bienfait K , Mukubwa, Grady K , Salami, Sodeeq A , Mbinze, Jérémie K , Lobb, Kevin A , Krause, Rui W M , Nkanga, Christian I
- Date: 2023
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/452727 , vital:75166 , xlink:href="https://doi.org/10.1016/j.jddst.2023.104302"
- Description: Tuberculosis, a predominantly pulmonary pathology, is currently the deadliest infection worldwide. Its treatment is based on combination therapy involving selected antimicrobials including Isoniazid. However, physicochemical properties of isoniazid negatively affect the clinical performance of current tuberculosis regimens, causing drug resistance development and increasing mortality rates. Liposomal encapsulation improves antituberculosis drug delivery; however, nano-formulation of isoniazid remains challenging due to its small molecular size and high hydrophilicity. Therefore, this study aimed to derivatize isoniazid and formulate a controlled delivery system using the concept of drug-in-cyclodextrins-in-liposomes to enhance drug biopharmaceutical properties. A prodrug of isoniazid was synthesized and screened for its ability to form stable complexes with α, β, and γ cyclodextrins. A selected inclusion complex with β-cyclodextrin was encapsulated in liposomes and assessed for controlled release of isoniazid. Successful formation of a 1:1 complex was established and characterized, followed by molecular modeling studies to demonstrate strength of the interactions within the complex and predicted complex structure. The inclusion complex was successfully encapsulated in liposomes using the thin film hydration method and the ethanol injection ultrasonic dispersion, with the latter giving the best results. These findings demonstrate the potential.
- Full Text:
- Date Issued: 2023
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 cytotoxic effects of chemical constituents of Euphorbia grandicornis Blanc against breast cancer cells
- Kemboi, Douglas, Peter, Xolani, Langat, Moses K, Mhlanga, Richwell, Vukea, Nyeleti, de la Mare, Jo-Anne, Siwe-Noundou, Xavier, Krause, Rui W M, Tembu, Vuyelwa J
- Authors: Kemboi, Douglas , Peter, Xolani , Langat, Moses K , Mhlanga, Richwell , Vukea, Nyeleti , de la Mare, Jo-Anne , Siwe-Noundou, Xavier , Krause, Rui W M , Tembu, Vuyelwa J
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191747 , vital:45160 , xlink:href="https://doi.org/10.1016/j.sciaf.2021.e01002"
- Description: Euphorbia grandicornis Blanc is widely utilized in traditional medicine for a variety of ailments including body pains associated with skin irritations, inflammation, and snake or scorpion bites. Compounds from E. grandicornis were characterized using spectroscopic techniques, NMR, IR, MS, and melting points and alongside the extracts were evaluated for in vitro anticancer activity against several cancer cell lines. The root extract afforded known, β-glutinol (1), β-amyrin (2), 24-methylenetirucalla-8-en-3β-ol (3), tirucalla-8,25-diene-3β,24R-diol (4), stigmasterol (5), sitosterol (6), and hexyl (E)-3-(4-hydroxy-3-methoxyphenyl)-2-propenoate (7) based on their NMR spectroscopic data for the first report in E. grandicornis. The extracts and isolated compounds were evaluated for anticancer activities against hormone receptor-positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12A) cell lines. The CH2Cl2 extract exhibited potent, cytotoxicity against MCF-7, HCC70, and MCF-12A cells. The aerial extract exhibited IC50 values of 1.03, 0.301, and 1.68 µg/mL, and root extract displayed IC50 values of 0.83, 0.83 and 3.98 µg/mL against MCF-7, HCC70, and MCF-12A cells respectively. The root extract thus showed selectivity for the cancer cell lines over the non-cancerous control cell line (SI = 4.80). Hexyl (E)-3-(4-hydroxy-3-methoxyphenyl)-2-propenoate (7) showed significant activity with IC50 values of 23.41, 29.45 and 27.01 µM against MCF-7, HCC70 and MCF-12A cells respectively, suggesting non-specific cytotoxicity.
- Full Text:
- Date Issued: 2021
- Authors: Kemboi, Douglas , Peter, Xolani , Langat, Moses K , Mhlanga, Richwell , Vukea, Nyeleti , de la Mare, Jo-Anne , Siwe-Noundou, Xavier , Krause, Rui W M , Tembu, Vuyelwa J
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191747 , vital:45160 , xlink:href="https://doi.org/10.1016/j.sciaf.2021.e01002"
- Description: Euphorbia grandicornis Blanc is widely utilized in traditional medicine for a variety of ailments including body pains associated with skin irritations, inflammation, and snake or scorpion bites. Compounds from E. grandicornis were characterized using spectroscopic techniques, NMR, IR, MS, and melting points and alongside the extracts were evaluated for in vitro anticancer activity against several cancer cell lines. The root extract afforded known, β-glutinol (1), β-amyrin (2), 24-methylenetirucalla-8-en-3β-ol (3), tirucalla-8,25-diene-3β,24R-diol (4), stigmasterol (5), sitosterol (6), and hexyl (E)-3-(4-hydroxy-3-methoxyphenyl)-2-propenoate (7) based on their NMR spectroscopic data for the first report in E. grandicornis. The extracts and isolated compounds were evaluated for anticancer activities against hormone receptor-positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12A) cell lines. The CH2Cl2 extract exhibited potent, cytotoxicity against MCF-7, HCC70, and MCF-12A cells. The aerial extract exhibited IC50 values of 1.03, 0.301, and 1.68 µg/mL, and root extract displayed IC50 values of 0.83, 0.83 and 3.98 µg/mL against MCF-7, HCC70, and MCF-12A cells respectively. The root extract thus showed selectivity for the cancer cell lines over the non-cancerous control cell line (SI = 4.80). Hexyl (E)-3-(4-hydroxy-3-methoxyphenyl)-2-propenoate (7) showed significant activity with IC50 values of 23.41, 29.45 and 27.01 µM against MCF-7, HCC70 and MCF-12A cells respectively, suggesting non-specific cytotoxicity.
- Full Text:
- Date Issued: 2021
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
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
Electronic and nonlinear optical properties of 3-(((2-substituted-4-nitrophenyl) 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/10962/193408 , vital:45329 , xlink:href="https://doi.org/10.1016/j.comptc.2020.113050"
- Description: This work entails the study of electronic and nonlinear optical (NLO) properties of two synthesized Schiff bases namely 3-(((2-methyl-4-nitrophenyl)imino)methyl)phenol (MMP) and 3-(((2,4-dinitrophenyl)imino)methyl)phenol (DMP). Electronic absorption properties studied using UV–Visible spectrophotometry in ethanol reveal low-energy absorption indicating a low band gap. Time-dependent density functional calculations on their excited state properties with ωB97X-D/6-311++G(d,p) method show comparable transition energies and intensities with the experimental results. Energy gaps (ΔE) and NLO properties were evaluated from the frontier orbitals and hyperpolarizabilities (βtot and γ) in gas, cyclohexane and ethanol. Low ΔE obtained shows the potentials of the systems as organic semiconductor with remarkable band gap stabilization in ethanol. Higher βtot and γ than urea imply that the Schiff bases possess potentials for NLO applications. The solvatochromic shift in transition energies and perturbation of electronic properties reveal the solvent dependence of the electronic and optical properties of MMP and DMP due to solute-solvent interactions.
- 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/10962/193408 , vital:45329 , xlink:href="https://doi.org/10.1016/j.comptc.2020.113050"
- Description: This work entails the study of electronic and nonlinear optical (NLO) properties of two synthesized Schiff bases namely 3-(((2-methyl-4-nitrophenyl)imino)methyl)phenol (MMP) and 3-(((2,4-dinitrophenyl)imino)methyl)phenol (DMP). Electronic absorption properties studied using UV–Visible spectrophotometry in ethanol reveal low-energy absorption indicating a low band gap. Time-dependent density functional calculations on their excited state properties with ωB97X-D/6-311++G(d,p) method show comparable transition energies and intensities with the experimental results. Energy gaps (ΔE) and NLO properties were evaluated from the frontier orbitals and hyperpolarizabilities (βtot and γ) in gas, cyclohexane and ethanol. Low ΔE obtained shows the potentials of the systems as organic semiconductor with remarkable band gap stabilization in ethanol. Higher βtot and γ than urea imply that the Schiff bases possess potentials for NLO applications. The solvatochromic shift in transition energies and perturbation of electronic properties reveal the solvent dependence of the electronic and optical properties of MMP and DMP due to solute-solvent interactions.
- Full Text:
- Date Issued: 2020
Green synthesis of antimicrobial silver nanoparticles using aqueous leaf extracts from three Congolese plant species (Brillantaisia patula, Crossopteryx febrifuga and Senna siamea)
- Kambale, Espoir K, Nkanga, Christian I, Mutonkole, Blaise-Pascal I, Bapolisi, Alain M, Tassa, Daniel O, Liesse, Jean-Marie I, Krause, Rui W M, Memvanga, Patrick B
- Authors: Kambale, Espoir K , Nkanga, Christian I , Mutonkole, Blaise-Pascal I , Bapolisi, Alain M , Tassa, Daniel O , Liesse, Jean-Marie I , Krause, Rui W M , Memvanga, Patrick B
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193419 , vital:45330 , xlink:href="https://doi.org/10.1016/j.heliyon.2020.e04493"
- Description: In the present study, silver nanoparticles (AgNPs) were synthesized using aqueous leaf extracts of three Congolese plant species, namely Brillantaisia patula (BR-PA), Crossopteryx febrifuga (CR-FE) and Senna siamea (SE-SI). The obtained AgNPs were studied for their optical, structural, surface morphological and antibacterial properties. The prepared AgNPs were characterized by using UV-Visible spectra, Transmission Electron Microscopy (TEM), Fourier Transform Infrared Spectroscopy (FTIR), X-ray spectroscopy (EDX) and X-ray diffractometer (XRD). The synthesized nanoparticles were spherical shaped and well-dispersed with average sizes ranging from 45 to 110 nm. The AgNPs derived from BR-PA, CR-FE and SE-SI exhibited higher antibacterial activity against three bacterial pathogens of the human skin compared to their respective crude extracts and AgNO3. This indicated that the biomolecules covering the nanoparticles may enhance the biological activity of metal nanoparticles. Hence, our results support that biogenic synthesis of AgNPs from Congolese plants constitutes a potential area of interest for the therapeutic management of microbial diseases such as infectious skin diseases.
- Full Text:
- Date Issued: 2020
- Authors: Kambale, Espoir K , Nkanga, Christian I , Mutonkole, Blaise-Pascal I , Bapolisi, Alain M , Tassa, Daniel O , Liesse, Jean-Marie I , Krause, Rui W M , Memvanga, Patrick B
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193419 , vital:45330 , xlink:href="https://doi.org/10.1016/j.heliyon.2020.e04493"
- Description: In the present study, silver nanoparticles (AgNPs) were synthesized using aqueous leaf extracts of three Congolese plant species, namely Brillantaisia patula (BR-PA), Crossopteryx febrifuga (CR-FE) and Senna siamea (SE-SI). The obtained AgNPs were studied for their optical, structural, surface morphological and antibacterial properties. The prepared AgNPs were characterized by using UV-Visible spectra, Transmission Electron Microscopy (TEM), Fourier Transform Infrared Spectroscopy (FTIR), X-ray spectroscopy (EDX) and X-ray diffractometer (XRD). The synthesized nanoparticles were spherical shaped and well-dispersed with average sizes ranging from 45 to 110 nm. The AgNPs derived from BR-PA, CR-FE and SE-SI exhibited higher antibacterial activity against three bacterial pathogens of the human skin compared to their respective crude extracts and AgNO3. This indicated that the biomolecules covering the nanoparticles may enhance the biological activity of metal nanoparticles. Hence, our results support that biogenic synthesis of AgNPs from Congolese plants constitutes a potential area of interest for the therapeutic management of microbial diseases such as infectious skin diseases.
- Full Text:
- Date Issued: 2020
Synthesis and biological evaluation of bis-N2, N2′-(4-hydroxycoumarin-3-yl) ethylidene]-2, 3-dihydroxysuccinodihydrazides
- Manyeruke, Meloddy H, Tshiwawa, Tendamudzimu, Hoppe, Heinrich C, Isaacs, Michelle, Seldon, Ronnett, Warner, Digby F, Krause, Rui W M, Kaye, Perry T
- Authors: Manyeruke, Meloddy H , Tshiwawa, Tendamudzimu , Hoppe, Heinrich C , Isaacs, Michelle , Seldon, Ronnett , Warner, Digby F , Krause, Rui W M , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193430 , vital:45331 , xlink:href="https://doi.org/10.1016/j.bmcl.2019.126911"
- Description: A series of N2,N2′-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Full Text:
- Date Issued: 2020
- Authors: Manyeruke, Meloddy H , Tshiwawa, Tendamudzimu , Hoppe, Heinrich C , Isaacs, Michelle , Seldon, Ronnett , Warner, Digby F , Krause, Rui W M , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193430 , vital:45331 , xlink:href="https://doi.org/10.1016/j.bmcl.2019.126911"
- Description: A series of N2,N2′-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Full Text:
- Date Issued: 2020
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 C, 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 C , 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 C , 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
Nano-enabled liposomal mucoadhesive films for enhanced efavirenz buccal drug delivery
- Okafor, Nnamadi I, Ngoepe, Mpho, Siwe-Noundou, Xavier, Krause, Rui W M
- Authors: Okafor, Nnamadi I , Ngoepe, Mpho , Siwe-Noundou, Xavier , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194032 , vital:45417 , xlink:href="https://doi.org/10.1016/j.jddst.2019.101312"
- Description: Buccal films (BFs) were prepared using a solvent casting method using the liposomal suspension as the dispersing medium. Optimization of some physical properties of the films containing different amounts of polymers was done using digital Vernier calliper and digital weighing balance. The physiochemical properties of the best optimized properties were characterized using Differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transfer infrared spectroscopy (FTIR), Transmission Electron Microscopy (TEM), Energy dispersive X-ray spectroscopy (EDS), and Scanning Electron Microscopy (SEM). Permeation study of the BFs composed of Carbopol (CP) alone and CP to Pluronic 127 (PF127) demonstrated better bio-adhesive properties than the films made of other polymers such as HPMC (hydroxyl propyl methyl cellulose) and HPMC-PF127. These CP based BFs (without and with PF127) exhibited good film thickness 0.88 ± 0.10 and 0.76 ± 0.14 mm, with weight uniformity 68.22 ± 1.04 and 86.28 ± 2.16 mg, satisfactory flexibility values 258 and 321, and slightly acidic pH 6.43 ± 0.76 and 6.32 ± 0.01. The swelling percentage was found to be 50% for CP and 78% for CP-PF127. The cumulative amount of drug that permeated through the buccal epithelium after 24 h was about 66% from CP and 75% from CP-PF127.
- Full Text:
- Date Issued: 2019
- Authors: Okafor, Nnamadi I , Ngoepe, Mpho , Siwe-Noundou, Xavier , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194032 , vital:45417 , xlink:href="https://doi.org/10.1016/j.jddst.2019.101312"
- Description: Buccal films (BFs) were prepared using a solvent casting method using the liposomal suspension as the dispersing medium. Optimization of some physical properties of the films containing different amounts of polymers was done using digital Vernier calliper and digital weighing balance. The physiochemical properties of the best optimized properties were characterized using Differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transfer infrared spectroscopy (FTIR), Transmission Electron Microscopy (TEM), Energy dispersive X-ray spectroscopy (EDS), and Scanning Electron Microscopy (SEM). Permeation study of the BFs composed of Carbopol (CP) alone and CP to Pluronic 127 (PF127) demonstrated better bio-adhesive properties than the films made of other polymers such as HPMC (hydroxyl propyl methyl cellulose) and HPMC-PF127. These CP based BFs (without and with PF127) exhibited good film thickness 0.88 ± 0.10 and 0.76 ± 0.14 mm, with weight uniformity 68.22 ± 1.04 and 86.28 ± 2.16 mg, satisfactory flexibility values 258 and 321, and slightly acidic pH 6.43 ± 0.76 and 6.32 ± 0.01. The swelling percentage was found to be 50% for CP and 78% for CP-PF127. The cumulative amount of drug that permeated through the buccal epithelium after 24 h was about 66% from CP and 75% from CP-PF127.
- Full Text:
- Date Issued: 2019
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
Purification and biochemical characterisation of a putative sodium channel agonist secreted from the South African Knobbly sea anemone Bunodosoma capense
- van Losenoord, Wynand, Krause, Jason, Parker-Nance, Shirley, Krause, Rui W M, Stoychey, Stoyan, Frost, Carminita L
- Authors: van Losenoord, Wynand , Krause, Jason , Parker-Nance, Shirley , Krause, Rui W M , Stoychey, Stoyan , Frost, Carminita L
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194082 , vital:45421 , xlink:href="https://doi.org/10.1016/j.toxicon.2019.06.222"
- Description: Voltage gated ion channels have become a subject of investigation as possible pharmaceutical targets. Research has linked the activity of ion channels directly to anti-inflammatory pathways, energy homeostasis, cancer proliferation and painful diabetic neuropathy. Sea anemones secrete a diverse array of bioactive compounds including potassium and sodium channel toxins. A putative novel sodium channel agonist (molecular mass of 4619.7 Da) with a predicted sequence: CLCNSDGPSV RGNTLSGILW LAGCPSGWHN CKKHKPTIGW CCK was isolated from Bunodosoma capense using a modified stimulation technique to induce the secretion of the neurotoxin rich mucus confirmed by an Artemia nauplii bio-assay. The peptide purification combined size-exclusion and reverse-phase high performance liquid chromatography. A thallium-based ion flux assay confirmed the presence of a sodium channel agonist/inhibitor and purity was determined using a modified tricine SDS-PAGE system. The peptide isolated indicated the presence of multiple disulfide bonds in a tight β-defensin cystine conformation. An IC50 value of 26 nM was determined for total channel inhibition on MCF-7 cells. The unique putative sodium channel agonist initiating with a cystine bond indicates a divergent evolution to those previously isolated from Bunodosoma species.
- Full Text:
- Date Issued: 2019
- Authors: van Losenoord, Wynand , Krause, Jason , Parker-Nance, Shirley , Krause, Rui W M , Stoychey, Stoyan , Frost, Carminita L
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194082 , vital:45421 , xlink:href="https://doi.org/10.1016/j.toxicon.2019.06.222"
- Description: Voltage gated ion channels have become a subject of investigation as possible pharmaceutical targets. Research has linked the activity of ion channels directly to anti-inflammatory pathways, energy homeostasis, cancer proliferation and painful diabetic neuropathy. Sea anemones secrete a diverse array of bioactive compounds including potassium and sodium channel toxins. A putative novel sodium channel agonist (molecular mass of 4619.7 Da) with a predicted sequence: CLCNSDGPSV RGNTLSGILW LAGCPSGWHN CKKHKPTIGW CCK was isolated from Bunodosoma capense using a modified stimulation technique to induce the secretion of the neurotoxin rich mucus confirmed by an Artemia nauplii bio-assay. The peptide purification combined size-exclusion and reverse-phase high performance liquid chromatography. A thallium-based ion flux assay confirmed the presence of a sodium channel agonist/inhibitor and purity was determined using a modified tricine SDS-PAGE system. The peptide isolated indicated the presence of multiple disulfide bonds in a tight β-defensin cystine conformation. An IC50 value of 26 nM was determined for total channel inhibition on MCF-7 cells. The unique putative sodium channel agonist initiating with a cystine bond indicates a divergent evolution to those previously isolated from Bunodosoma species.
- Full Text:
- Date Issued: 2019
Antibacterial effects of Alchornea cordifolia (Schumach. and Thonn.) Müll. Arg extracts and compounds on gastrointestinal, skin, respiratory and urinary tract pathogens
- Siwe-Noundou, Xavier, Krause, Rui W M, van Vuuren, Sandy, Tantoh Ndinteh, Derek, Olivier, Denise K
- Authors: Siwe-Noundou, Xavier , Krause, Rui W M , van Vuuren, Sandy , Tantoh Ndinteh, Derek , Olivier, Denise K
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195418 , vital:45563 , xlink:href="https://doi.org/10.1016/j.jep.2015.12.043"
- Description: Ethnopharmacological relevance:The leaves, stems and roots ofAlchornea cordifolia(Schumach. andThonn.) Müll. Arg. are used as traditional medicine in many African countries for the management ofgastrointestinal, respiratory and urinary tract infections as well as for the treatment of wounds.Aim of the study:To determine the in vitro antibacterial activity of the crude extracts of leaves and stemsofA. cordifoliaon gastrointestinal, skin, respiratory and urinary tract pathogens and to identify thecompounds in the extracts that may be responsible for this activity.Materials and methods:The antibacterial activities of crude extracts [hexane, chloroform (CHCl3), ethylacetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O)] as well as pure compounds isolatedfrom these extracts were evaluated by means of the micro-dilution assay against four Gram-positivebacteria, i.e.Bacillus cereusATCC 11778,Enterococcus faecalisATCC 29212, Staphylococcus aureusATCC25923 andS. saprophyticusATCC 15305,as well as four Gram-negative bacterial strains, i.e.EscherichiacoliATCC 25922, Klebsiella pneumoniaeATCC 13883, Moraxella catarrhalisATCC 23246 andProteus mir-abilisATCC 43071. The isolation of the active constituents was undertaken by bio-autographic assays inconjunction with chromatographic techniques. The identification and characterisation of the isolatedcompounds were done using mass spectrometry (MS) and Fourier transformed infrared spectrometry(FTIR) as well as 1D- and 2D- nuclear magnetic resonance (NMR) analyses.Results:The leaves and stems ofA. cordifoliaexhibited varied antibacterial activity against all eight pa-thogens. Most of the MIC values ranged between 63 and 2000mg/ml. The highest activities for the crudeextracts (63mg/ml) were observed againstS. saprophyticus[stem (EtOAc, CHCl3and hexane), leaves(MeOH, EtOH, EtOAc and CHCl3)],E. coli[stem (MeOH and EtOH), leaves (MeOH, EtOH, EtOAc andCHCl3)],M. catarrhalis[leaves (EtOAc and CHCl3)],K. pneumoniae[stem (CHCl3), leaves (CHCl3)] andS.aureus[leaves (CHCl3)]. Seven constituents [stigmasterol (1), stigmasta-4,22-dien-3-one (2), friedelin (3),friedelane-3-one-28-al (4), 3-O-acetyl-aleuritolic acid (5), 3-O-acetyl-erythrodiol (6) and methyl-3,4,5-trihydroxybenzoate (methyl gallate) (7)] were isolated from the stem MeOH extract. All these com-pounds displayed some antibacterial activity against the eight pathogens with highest activity againstS.saprophyticus(2mg/ml). Furthermore, this is thefirst report of compounds1,2,3,4,6and7isolated fromA. cordifoliaand where a complete set of 2D-NMR data for fridelane-3-one-28-al (4) is presented.Conclusion:The study demonstrated that the antibacterial activities ofA. cordifoliaextracts may be dueto the presence of the seven isolated compounds, where compounds3–6showed the best activity. Theobserved activity against gastrointestinal, skin, respiratory and urinary tract pathogens supports thetraditional use for the treatment of such ailments.
- Full Text:
- Date Issued: 2016
- Authors: Siwe-Noundou, Xavier , Krause, Rui W M , van Vuuren, Sandy , Tantoh Ndinteh, Derek , Olivier, Denise K
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195418 , vital:45563 , xlink:href="https://doi.org/10.1016/j.jep.2015.12.043"
- Description: Ethnopharmacological relevance:The leaves, stems and roots ofAlchornea cordifolia(Schumach. andThonn.) Müll. Arg. are used as traditional medicine in many African countries for the management ofgastrointestinal, respiratory and urinary tract infections as well as for the treatment of wounds.Aim of the study:To determine the in vitro antibacterial activity of the crude extracts of leaves and stemsofA. cordifoliaon gastrointestinal, skin, respiratory and urinary tract pathogens and to identify thecompounds in the extracts that may be responsible for this activity.Materials and methods:The antibacterial activities of crude extracts [hexane, chloroform (CHCl3), ethylacetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O)] as well as pure compounds isolatedfrom these extracts were evaluated by means of the micro-dilution assay against four Gram-positivebacteria, i.e.Bacillus cereusATCC 11778,Enterococcus faecalisATCC 29212, Staphylococcus aureusATCC25923 andS. saprophyticusATCC 15305,as well as four Gram-negative bacterial strains, i.e.EscherichiacoliATCC 25922, Klebsiella pneumoniaeATCC 13883, Moraxella catarrhalisATCC 23246 andProteus mir-abilisATCC 43071. The isolation of the active constituents was undertaken by bio-autographic assays inconjunction with chromatographic techniques. The identification and characterisation of the isolatedcompounds were done using mass spectrometry (MS) and Fourier transformed infrared spectrometry(FTIR) as well as 1D- and 2D- nuclear magnetic resonance (NMR) analyses.Results:The leaves and stems ofA. cordifoliaexhibited varied antibacterial activity against all eight pa-thogens. Most of the MIC values ranged between 63 and 2000mg/ml. The highest activities for the crudeextracts (63mg/ml) were observed againstS. saprophyticus[stem (EtOAc, CHCl3and hexane), leaves(MeOH, EtOH, EtOAc and CHCl3)],E. coli[stem (MeOH and EtOH), leaves (MeOH, EtOH, EtOAc andCHCl3)],M. catarrhalis[leaves (EtOAc and CHCl3)],K. pneumoniae[stem (CHCl3), leaves (CHCl3)] andS.aureus[leaves (CHCl3)]. Seven constituents [stigmasterol (1), stigmasta-4,22-dien-3-one (2), friedelin (3),friedelane-3-one-28-al (4), 3-O-acetyl-aleuritolic acid (5), 3-O-acetyl-erythrodiol (6) and methyl-3,4,5-trihydroxybenzoate (methyl gallate) (7)] were isolated from the stem MeOH extract. All these com-pounds displayed some antibacterial activity against the eight pathogens with highest activity againstS.saprophyticus(2mg/ml). Furthermore, this is thefirst report of compounds1,2,3,4,6and7isolated fromA. cordifoliaand where a complete set of 2D-NMR data for fridelane-3-one-28-al (4) is presented.Conclusion:The study demonstrated that the antibacterial activities ofA. cordifoliaextracts may be dueto the presence of the seven isolated compounds, where compounds3–6showed the best activity. Theobserved activity against gastrointestinal, skin, respiratory and urinary tract pathogens supports thetraditional use for the treatment of such ailments.
- Full Text:
- Date Issued: 2016
A colorimetric probe for dopamine based on gold nanoparticles-electrospun nanofibre composite
- Ngomane, Nokuthula, Torto, Nelson, Krause, Rui W M, Vilakazi, Sibulelo
- Authors: Ngomane, Nokuthula , Torto, Nelson , Krause, Rui W M , Vilakazi, Sibulelo
- Date: 2015
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195407 , vital:45562 , xlink:href="https://doi.org/10.1016/j.matpr.2015.08.036"
- Description: An easily prepared solid state colorimetric probe for detecting the neurotransmitter dopamine (DA) was developed. The probe, in the form of an electrospun Nylon−6 (N6) nanofibre with embedded un−functionalized gold nanoparticles (UF−AuNPs) produces a clear colour change in the presence of a DA that is detectable by the naked eye. Characterisation of the nanofibre using UV/vis spectroscopy and electron microscopy (TEM) confirmed the formation of the AuNPs in the polymer solution, and that the AuNPs were completely encapsulated within the composite nanofibres before exposure to the analytes. The probe exhibited very high sensitivity towards DA resulting in colour change of the composite fibres from purple to navy blue/black even under low concentrations of DA. The probe was also selective to DA since the colour remained unchanged in the presence of commonly encountered interfering species such as ascorbic acid, uric acid, catechol, epinephrine and norepinephrine. Moreover, the colour change was observed rapid, occurring either immediately on contact with higher concentrations (5 x10−4 M) or within about 3−5 min for the lower concentrations (e.g. 5 x10−7 M). Since this probe does not require the use of any instruments, and is both rapid and stable over time, it can be applied in the field by an inexperienced person.
- Full Text:
- Date Issued: 2015
- Authors: Ngomane, Nokuthula , Torto, Nelson , Krause, Rui W M , Vilakazi, Sibulelo
- Date: 2015
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195407 , vital:45562 , xlink:href="https://doi.org/10.1016/j.matpr.2015.08.036"
- Description: An easily prepared solid state colorimetric probe for detecting the neurotransmitter dopamine (DA) was developed. The probe, in the form of an electrospun Nylon−6 (N6) nanofibre with embedded un−functionalized gold nanoparticles (UF−AuNPs) produces a clear colour change in the presence of a DA that is detectable by the naked eye. Characterisation of the nanofibre using UV/vis spectroscopy and electron microscopy (TEM) confirmed the formation of the AuNPs in the polymer solution, and that the AuNPs were completely encapsulated within the composite nanofibres before exposure to the analytes. The probe exhibited very high sensitivity towards DA resulting in colour change of the composite fibres from purple to navy blue/black even under low concentrations of DA. The probe was also selective to DA since the colour remained unchanged in the presence of commonly encountered interfering species such as ascorbic acid, uric acid, catechol, epinephrine and norepinephrine. Moreover, the colour change was observed rapid, occurring either immediately on contact with higher concentrations (5 x10−4 M) or within about 3−5 min for the lower concentrations (e.g. 5 x10−7 M). Since this probe does not require the use of any instruments, and is both rapid and stable over time, it can be applied in the field by an inexperienced person.
- Full Text:
- Date Issued: 2015
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