Novel, soluble, FluXoro functional substituted zinc phthalocyanines; synthesis, characterization and photophysicochemical properties
- Erdoğmuş, Ali, Nyokong, Tebello
- Authors: Erdoğmuş, Ali , Nyokong, Tebello
- Date: 2010
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/261258 , vital:53378 , xlink:href="https://doi.org/10.1016/j.dyepig.2010.01.001"
- Description: Three novel phthalonitriles and the respective, peripheral tetrakis zinc phthalocyanines were synthesized and characterized using elemental analysis, IR, 1H NMR, mass spectra and electronic spectroscopy. The phthalocyanines displayed good solubility in organic solvents such as CHCl3, DCM, DMSO, DMF, THF and toluene. The presence of a long chain fluorine substitituent was found to result in reduced aggregation. The singlet oxygen, photodegradation, fluorescence quantum yield, triplet quantum yield and triplet life time of the complexes in toluene were determined. The effect of fluoro-functional groups on the photophysical and photochemical parameters of the zinc(II) phthalocyanines are also reported. Fluorescence quantum yields for the complexes ranged from 0.021 to 0.041.
- Full Text:
- Date Issued: 2010
- Authors: Erdoğmuş, Ali , Nyokong, Tebello
- Date: 2010
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/261258 , vital:53378 , xlink:href="https://doi.org/10.1016/j.dyepig.2010.01.001"
- Description: Three novel phthalonitriles and the respective, peripheral tetrakis zinc phthalocyanines were synthesized and characterized using elemental analysis, IR, 1H NMR, mass spectra and electronic spectroscopy. The phthalocyanines displayed good solubility in organic solvents such as CHCl3, DCM, DMSO, DMF, THF and toluene. The presence of a long chain fluorine substitituent was found to result in reduced aggregation. The singlet oxygen, photodegradation, fluorescence quantum yield, triplet quantum yield and triplet life time of the complexes in toluene were determined. The effect of fluoro-functional groups on the photophysical and photochemical parameters of the zinc(II) phthalocyanines are also reported. Fluorescence quantum yields for the complexes ranged from 0.021 to 0.041.
- Full Text:
- Date Issued: 2010
New thiazolidine-2,4-dione derivatives combined with organometallic ferrocene: Synthesis, structure and antiparasitic activity
- Oderinlo, Ogunyemi O, Tukulula, Matshawandile, Isaacs, Michelle, Taylor, Dale, Smith, Vincent J, Khanye, Setshaba D, Hoppe, Heinrich C
- Authors: Oderinlo, Ogunyemi O , Tukulula, Matshawandile , Isaacs, Michelle , Taylor, Dale , Smith, Vincent J , Khanye, Setshaba D , Hoppe, Heinrich C
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/122978 , vital:35382 , https://doi.org/10.1002/aoc.4385
- Description: Favourable physicochemical properties of an organometallic ferrocene and antiplasmodial potency of compounds containing the thiazolidine‐2,4‐dione framework (TZD‐4) prompted us to explore compounds containing both the thiazolidine‐2,4‐dione core and the ferrocenyl unit with the primary aim of identifying compounds with promising antiprotozoal activities. Thus, a new series of rationally designed ferrocene‐based thiazolidine‐2,4‐dione derivatives, containing a selection of secondary cyclic amines, was synthesised and fully characterised using standard spectroscopic techniques. The resulting compounds were screened for their antiplasmodial and antitrypanosomal activities against both the chloroquine‐resistant (Dd2) strain of Plasmodium falciparum and the Nagana Trypanosoma brucei brucei 427. The general trend that emerged indicated that the target compounds were more selective towards T. b. brucei compared to the P. falciparum parasite. Moreover, the analogues bearing methylpiperazine (8a) and piperidine (8b) rings were more active against T. b. brucei compared to hit compound TZD‐4. Except compound 8b, which appeared promising, none of the synthesised compounds showed better activity than TZD‐4 against the P. falciparum parasite. All the synthesised compounds were non‐toxic and often showed >90% viability of the HeLa cell line screened.
- Full Text:
- Date Issued: 2018
- Authors: Oderinlo, Ogunyemi O , Tukulula, Matshawandile , Isaacs, Michelle , Taylor, Dale , Smith, Vincent J , Khanye, Setshaba D , Hoppe, Heinrich C
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/122978 , vital:35382 , https://doi.org/10.1002/aoc.4385
- Description: Favourable physicochemical properties of an organometallic ferrocene and antiplasmodial potency of compounds containing the thiazolidine‐2,4‐dione framework (TZD‐4) prompted us to explore compounds containing both the thiazolidine‐2,4‐dione core and the ferrocenyl unit with the primary aim of identifying compounds with promising antiprotozoal activities. Thus, a new series of rationally designed ferrocene‐based thiazolidine‐2,4‐dione derivatives, containing a selection of secondary cyclic amines, was synthesised and fully characterised using standard spectroscopic techniques. The resulting compounds were screened for their antiplasmodial and antitrypanosomal activities against both the chloroquine‐resistant (Dd2) strain of Plasmodium falciparum and the Nagana Trypanosoma brucei brucei 427. The general trend that emerged indicated that the target compounds were more selective towards T. b. brucei compared to the P. falciparum parasite. Moreover, the analogues bearing methylpiperazine (8a) and piperidine (8b) rings were more active against T. b. brucei compared to hit compound TZD‐4. Except compound 8b, which appeared promising, none of the synthesised compounds showed better activity than TZD‐4 against the P. falciparum parasite. All the synthesised compounds were non‐toxic and often showed >90% viability of the HeLa cell line screened.
- Full Text:
- Date Issued: 2018
Cordidepsine is A Potential New Anti-HIV Depsidone from Cordia millenii
- Zeukang, Rostanie D, Siwe-Noundou, Xavier, Fotsing, Maurice T, Mbafor, Joseph T, Krause, Rui W M, Choudhary, Muhammad I, Atchade, Alex de Theodore
- Authors: Zeukang, Rostanie D , Siwe-Noundou, Xavier , Fotsing, Maurice T , Mbafor, Joseph T , Krause, Rui W M , Choudhary, Muhammad I , Atchade, Alex de Theodore
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193988 , vital:45413 , xlink:href="https://doi.org/10.3390/molecules24173202"
- Description: Chemical investigation of Cordia millenii, Baker resulted in the isolation of a new depsidone, cordidepsine (1), along with twelve known compounds including cyclooctasulfur (2), lup-20(29)-en-3-triacontanoate (3), 1-(26-hydroxyhexacosanoyl)glycerol (4), glyceryl-1-hexacosanoate (5) betulinic acid (6), lupenone (7), β-amyrone (8), lupeol (9), β-amyrin (10), allantoin (11), 2′-(4-hydroxyphenyl)ethylpropanoate (12) and stigmasterol glycoside (13). Hemi-synthetic reactions were carried out on two isolated compounds (5 and 6) to afford two new derivatives, that is, cordicerol A (14) and cordicerol B (15), respectively. The chemical structures of all the compounds were established based on analysis and interpretation of spectroscopic data such as electron ionization mass spectrometry (EI–MS), high resolution electrospray ionization mass spectrometry (HR-ESI–MS), fast atom bombardment mass spectrometry (FAB–MS), one dimension and two dimension nuclear magnetic resonance (1D and 2D-NMR) spectral data as well as X-ray crystallography (XRC). Lupeol ester derivatives [Lup-20(29)-en-3-triacontanoate (3)], monoglycerol derivatives [1-(26-hydroxyhexacosanoyl)glycerol (4) and glyceryl-1 hexacosanoate (5)] were isolated for the first time from Cordia genus while sulfur allotrope [cyclooctasulfur (2)] was isolated for the first time from plant origin. Biological assays cordidepsine (1) exhibited significant anti-HIV integrase activity with IC50 = 4.65 μM; EtOAc extract of stem barks, EtOAc fraction of roots and leaves were not toxic against 3T3 cells.
- Full Text:
- Date Issued: 2019
- Authors: Zeukang, Rostanie D , Siwe-Noundou, Xavier , Fotsing, Maurice T , Mbafor, Joseph T , Krause, Rui W M , Choudhary, Muhammad I , Atchade, Alex de Theodore
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193988 , vital:45413 , xlink:href="https://doi.org/10.3390/molecules24173202"
- Description: Chemical investigation of Cordia millenii, Baker resulted in the isolation of a new depsidone, cordidepsine (1), along with twelve known compounds including cyclooctasulfur (2), lup-20(29)-en-3-triacontanoate (3), 1-(26-hydroxyhexacosanoyl)glycerol (4), glyceryl-1-hexacosanoate (5) betulinic acid (6), lupenone (7), β-amyrone (8), lupeol (9), β-amyrin (10), allantoin (11), 2′-(4-hydroxyphenyl)ethylpropanoate (12) and stigmasterol glycoside (13). Hemi-synthetic reactions were carried out on two isolated compounds (5 and 6) to afford two new derivatives, that is, cordicerol A (14) and cordicerol B (15), respectively. The chemical structures of all the compounds were established based on analysis and interpretation of spectroscopic data such as electron ionization mass spectrometry (EI–MS), high resolution electrospray ionization mass spectrometry (HR-ESI–MS), fast atom bombardment mass spectrometry (FAB–MS), one dimension and two dimension nuclear magnetic resonance (1D and 2D-NMR) spectral data as well as X-ray crystallography (XRC). Lupeol ester derivatives [Lup-20(29)-en-3-triacontanoate (3)], monoglycerol derivatives [1-(26-hydroxyhexacosanoyl)glycerol (4) and glyceryl-1 hexacosanoate (5)] were isolated for the first time from Cordia genus while sulfur allotrope [cyclooctasulfur (2)] was isolated for the first time from plant origin. Biological assays cordidepsine (1) exhibited significant anti-HIV integrase activity with IC50 = 4.65 μM; EtOAc extract of stem barks, EtOAc fraction of roots and leaves were not toxic against 3T3 cells.
- Full Text:
- Date Issued: 2019
Synthesis, characterization and biological activity of some Dithiourea Derivatives:
- Odame, Felix, Hosten, Eric, Krause, Jason, Isaacs, Michelle, Hoppe, Heinrich C, Khanye, Setshaba D, Sayed, Yasien, Frost, Carminita, Lobb, Kevin A, Tshentu, Zenixole
- Authors: Odame, Felix , Hosten, Eric , Krause, Jason , Isaacs, Michelle , Hoppe, Heinrich C , Khanye, Setshaba D , Sayed, Yasien , Frost, Carminita , Lobb, Kevin A , Tshentu, Zenixole
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/163046 , vital:41007 , DOI: 10.17344/acsi.2019.5689
- Description: Novel dithiourea derivatives have been designed as HIV-1 protease inhibitors using Autodock 4.2, synthesized and characterized by spectroscopic methods and microanalysis.
- Full Text:
- Date Issued: 2020
- Authors: Odame, Felix , Hosten, Eric , Krause, Jason , Isaacs, Michelle , Hoppe, Heinrich C , Khanye, Setshaba D , Sayed, Yasien , Frost, Carminita , Lobb, Kevin A , Tshentu, Zenixole
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/163046 , vital:41007 , DOI: 10.17344/acsi.2019.5689
- Description: Novel dithiourea derivatives have been designed as HIV-1 protease inhibitors using Autodock 4.2, synthesized and characterized by spectroscopic methods and microanalysis.
- Full Text:
- Date Issued: 2020
Secondary metabolites from Tetracera potatoria stem bark with anti-mycobacterial activity.
- Fomogne-Fodjo, M C Y, Ndinteh, Derek T, Olivier, D K, Krause, Rui W M, Kempgens, Pierre, Van Vuuren, S
- Authors: Fomogne-Fodjo, M C Y , Ndinteh, Derek T , Olivier, D K , Krause, Rui W M , Kempgens, Pierre , Van Vuuren, S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125556 , vital:35795 , https://doi.org/10.1016/j.jep.2016.11.027
- Description: Ethnopharmacological relevance Tetracera potatoria Afzel. Exg. Don (Dilleniaceae) is a medicinal plant used traditionally in Africa for the treatment of tuberculosis related ailments and respiratory infections. The antibacterial activity of the medium polar extracts of T. potatoria leaves and stem bark was recently reported against Mycobacterium smegmatis (MIC 25 µg/mL) and M. aurum (65 µg/mL), two fast-growing Mycobacterium strains used as model micro-organisms for the more pathogenic strain Mycobacterium tuberculosis (Fomogne-Fodjo et al., 2014). The aim of this study was consequently to isolate the compounds possibly contributing to this activity, and which may therefore be promising precursors to be used for the development of novel anti-TB drugs.
- Full Text:
- Date Issued: 2017
- Authors: Fomogne-Fodjo, M C Y , Ndinteh, Derek T , Olivier, D K , Krause, Rui W M , Kempgens, Pierre , Van Vuuren, S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125556 , vital:35795 , https://doi.org/10.1016/j.jep.2016.11.027
- Description: Ethnopharmacological relevance Tetracera potatoria Afzel. Exg. Don (Dilleniaceae) is a medicinal plant used traditionally in Africa for the treatment of tuberculosis related ailments and respiratory infections. The antibacterial activity of the medium polar extracts of T. potatoria leaves and stem bark was recently reported against Mycobacterium smegmatis (MIC 25 µg/mL) and M. aurum (65 µg/mL), two fast-growing Mycobacterium strains used as model micro-organisms for the more pathogenic strain Mycobacterium tuberculosis (Fomogne-Fodjo et al., 2014). The aim of this study was consequently to isolate the compounds possibly contributing to this activity, and which may therefore be promising precursors to be used for the development of novel anti-TB drugs.
- Full Text:
- Date Issued: 2017
Photolytic changes in the morphology of porphyrin-phthalocyanine nanostructures (P-PcNs) in the presence of platinum and gold salts
- George, Reama C, D'Souza, Sarah, Durmus, Mahmut, Nyokong, Tebello
- Authors: George, Reama C , D'Souza, Sarah , Durmus, Mahmut , Nyokong, Tebello
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/190416 , vital:44992 , xlink:href="https://doi.org/10.1080/24701556.2017.1284085"
- Description: Porphyrin-phthalocyanine nanostructures (P-PcNs) have been fabricated by electrostatic self-assembly of two oppositely charged molecules. The negatively charged molecule, meso-tetra-(4-phenylsulphonate)porphyrin (HT) and the positively charged species; {1,(4)-tetrakis-[(N-methyl(3-pyridyloxy) phthlocyaninato] chloro gallium(III)} sulphate, {2,(3)-tetrakis-[(N-methyl{(2-mercaptopyridine) phthalocyaninato} hydroxy manganese(III)} sulphate, {1,(4)-tetrakis-[(N-methyl-(3-pyridyloxy) phthalocyaninato] chloro indium(III)} sulphate, {2,3-octakis-{[(N-methyl-2-mercaptopyridine) phthalocyaninato] acetato manganese(III)} sulphate, {2,(3)-tetrakis-[(N-methyl(3-pyridyloxy) phthlocyaninato] choro gallium(III)} sulphate, {2,3-octakis-[(N-methy-3-pyridyloxy) phthalocyaninato] chloro indium(III)} sulphate, and {2,(3)-tetrakis-[(N-methyl (3-pyridyloxy) phthalocyaninato] chloro indium(III)} sulphate. Transmission electron microscopic (TEM) images showed that the formed nanostructures ranged from nanosheets to nanorods and nanotubes. The UV-Vis spectra confirmed that the molecules formed J-aggregates. The P-PcNs were exposed to incandescence light in the presence of platinum and gold salts. It was observed that the presence of platinum salts resulted in the destruction of the P-PcNs with possible formation of a Pt-Pc complex. While with the gold salt, the structures of P-PcNs were not only retained but were also enhanced to longer nanorods and nanofibers with the formation of gold nanoparticles.
- Full Text:
- Date Issued: 2017
- Authors: George, Reama C , D'Souza, Sarah , Durmus, Mahmut , Nyokong, Tebello
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/190416 , vital:44992 , xlink:href="https://doi.org/10.1080/24701556.2017.1284085"
- Description: Porphyrin-phthalocyanine nanostructures (P-PcNs) have been fabricated by electrostatic self-assembly of two oppositely charged molecules. The negatively charged molecule, meso-tetra-(4-phenylsulphonate)porphyrin (HT) and the positively charged species; {1,(4)-tetrakis-[(N-methyl(3-pyridyloxy) phthlocyaninato] chloro gallium(III)} sulphate, {2,(3)-tetrakis-[(N-methyl{(2-mercaptopyridine) phthalocyaninato} hydroxy manganese(III)} sulphate, {1,(4)-tetrakis-[(N-methyl-(3-pyridyloxy) phthalocyaninato] chloro indium(III)} sulphate, {2,3-octakis-{[(N-methyl-2-mercaptopyridine) phthalocyaninato] acetato manganese(III)} sulphate, {2,(3)-tetrakis-[(N-methyl(3-pyridyloxy) phthlocyaninato] choro gallium(III)} sulphate, {2,3-octakis-[(N-methy-3-pyridyloxy) phthalocyaninato] chloro indium(III)} sulphate, and {2,(3)-tetrakis-[(N-methyl (3-pyridyloxy) phthalocyaninato] chloro indium(III)} sulphate. Transmission electron microscopic (TEM) images showed that the formed nanostructures ranged from nanosheets to nanorods and nanotubes. The UV-Vis spectra confirmed that the molecules formed J-aggregates. The P-PcNs were exposed to incandescence light in the presence of platinum and gold salts. It was observed that the presence of platinum salts resulted in the destruction of the P-PcNs with possible formation of a Pt-Pc complex. While with the gold salt, the structures of P-PcNs were not only retained but were also enhanced to longer nanorods and nanofibers with the formation of gold nanoparticles.
- Full Text:
- Date Issued: 2017
Semi-synthesis and evaluation of sargahydroquinoic acid derivatives as potential antimalarial agents:
- Munedzimwe, Tatenda C, van Zyl, Rovyn L, Heslop, Donovan C, Edkins, Adrienne L, Beukes, Denzil R
- Authors: Munedzimwe, Tatenda C , van Zyl, Rovyn L , Heslop, Donovan C , Edkins, Adrienne L , Beukes, Denzil R
- Date: 2019
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/163456 , vital:41040 , DOI: 10.3390/medicines6020047
- Description: Malaria continues to present a major health problem, especially in developing countries. The development of new antimalarial drugs to counter drug resistance and ensure a steady supply of new treatment options is therefore an important area of research. Meroditerpenes have previously been shown to exhibit antiplasmodial activity against a chloroquinone sensitive strain of Plasmodium falciparum (D10). In this study we explored the antiplasmodial activity of several semi-synthetic analogs of sargahydroquinoic acid.
- Full Text:
- Date Issued: 2019
- Authors: Munedzimwe, Tatenda C , van Zyl, Rovyn L , Heslop, Donovan C , Edkins, Adrienne L , Beukes, Denzil R
- Date: 2019
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/163456 , vital:41040 , DOI: 10.3390/medicines6020047
- Description: Malaria continues to present a major health problem, especially in developing countries. The development of new antimalarial drugs to counter drug resistance and ensure a steady supply of new treatment options is therefore an important area of research. Meroditerpenes have previously been shown to exhibit antiplasmodial activity against a chloroquinone sensitive strain of Plasmodium falciparum (D10). In this study we explored the antiplasmodial activity of several semi-synthetic analogs of sargahydroquinoic acid.
- Full Text:
- Date Issued: 2019
Three new pentacyclic triterpenoids from twigs of Manniophyton fulvum (Euphorbiaceae)
- Mbeunkeu, Ahri B D, Noundou, Xavier S, Krause, Rui W M, Teinkela, Jean E M, Laatsch, Hartmut, Azebaze, Anatole G B, Vardamides, Juliette C, Tala, Michel F
- Authors: Mbeunkeu, Ahri B D , Noundou, Xavier S , Krause, Rui W M , Teinkela, Jean E M , Laatsch, Hartmut , Azebaze, Anatole G B , Vardamides, Juliette C , Tala, Michel F
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126782 , vital:35922 , https://doi.org/10.1016/j.phytol.2018.06.019
- Description: Phytochemical investigation of the methanol extracts of the twigs of Manniophyton fulvum has led to the isolation and characterization of three new pentacyclic triterpenoids, designated as 3α,28-dihydroxyfriedelan-1-one (1), manniotaraxerol A (3) and manniotaraxerol B (4), along with fourteen known compounds, 3α-hydroxy-1-oxofriedelane (2), betulinic acid (5), friedelin (S1), taraxerol (S2), a mixture of stigmasterol (S3) and β-sitosterol (S4), herranone (S5), docosanoic acid (S6), ursolic acid (S7), nasutin B (S8), bergenin (S9), stigmasterol-3-O-β-Dglucopyranoside (S10), 1,2-di-O-palmitoyl-3-O-(6-sulfo-α-D-quinovopyranosyl)glycerol (S11), and aridanin (S12). The structures of all compounds were determined by comprehensive spectroscopic analyses (1D and 2D NMR, EI and ESI-MS). 3α,28-Dihydroxyfriedelan-1-one (1), 3α-hydroxy-1-oxofriedelane (2), manniotaraxerol A (3), manniotaraxerol B (4), and betulinic acid (5) were evaluated against HeLa (human cervix adenocarcinoma) cancer cells. Manniotaraxerol A (3) showed weak in vitro cytotoxicity with a cell viability value of 49.3%. Betulinic acid (5) also showed significant cytotoxicity against HeLa cell with a cell viability value of 4.0%; the other compounds were inactive in this test.
- Full Text:
- Date Issued: 2018
- Authors: Mbeunkeu, Ahri B D , Noundou, Xavier S , Krause, Rui W M , Teinkela, Jean E M , Laatsch, Hartmut , Azebaze, Anatole G B , Vardamides, Juliette C , Tala, Michel F
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126782 , vital:35922 , https://doi.org/10.1016/j.phytol.2018.06.019
- Description: Phytochemical investigation of the methanol extracts of the twigs of Manniophyton fulvum has led to the isolation and characterization of three new pentacyclic triterpenoids, designated as 3α,28-dihydroxyfriedelan-1-one (1), manniotaraxerol A (3) and manniotaraxerol B (4), along with fourteen known compounds, 3α-hydroxy-1-oxofriedelane (2), betulinic acid (5), friedelin (S1), taraxerol (S2), a mixture of stigmasterol (S3) and β-sitosterol (S4), herranone (S5), docosanoic acid (S6), ursolic acid (S7), nasutin B (S8), bergenin (S9), stigmasterol-3-O-β-Dglucopyranoside (S10), 1,2-di-O-palmitoyl-3-O-(6-sulfo-α-D-quinovopyranosyl)glycerol (S11), and aridanin (S12). The structures of all compounds were determined by comprehensive spectroscopic analyses (1D and 2D NMR, EI and ESI-MS). 3α,28-Dihydroxyfriedelan-1-one (1), 3α-hydroxy-1-oxofriedelane (2), manniotaraxerol A (3), manniotaraxerol B (4), and betulinic acid (5) were evaluated against HeLa (human cervix adenocarcinoma) cancer cells. Manniotaraxerol A (3) showed weak in vitro cytotoxicity with a cell viability value of 49.3%. Betulinic acid (5) also showed significant cytotoxicity against HeLa cell with a cell viability value of 4.0%; the other compounds were inactive in this test.
- Full Text:
- Date Issued: 2018
Synthesis, in vitro cytotoxicity and trypanocidal evaluation of novel 1, 3, 6-substituted non-fluoroquinolones
- Beteck, Richard M, Isaacs, Michelle, Khanye, Setshaba D, Hoppe, Heinrich C
- Authors: Beteck, Richard M , Isaacs, Michelle , Khanye, Setshaba D , Hoppe, Heinrich C
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123140 , vital:35409 , https://doi.org/10.17159/0379-4350/2018/v71a25
- Description: Sleeping sickness (trypanosomiasis) is a neglected tropical disease that affects mostly the poorest communities in sub-Saharan Africa. Toxic side effects associated with the use of current anti-trypanosomal drugs, which in some cases kill faster than the disease itself, necessitate the search for new drugs with better safety margins. To this effect, a small library bearing different substituents at position -1, -3, and -6 of the quinolone nucleus were synthesized and evaluated in vitro against HeLa cell lines and Trypanosoma brucei brucei for cytotoxicity and trypanocidal potentials, respectively. While most of these compounds showed no cytotoxic effect, they exhibited moderate to weak anti-trypanosomal activities. The SAR studies of this series provide new information worth considering in future exploration of the quinolone scaffold in search ofmore potent and safe trypanocidal agents.
- Full Text:
- Date Issued: 2018
- Authors: Beteck, Richard M , Isaacs, Michelle , Khanye, Setshaba D , Hoppe, Heinrich C
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123140 , vital:35409 , https://doi.org/10.17159/0379-4350/2018/v71a25
- Description: Sleeping sickness (trypanosomiasis) is a neglected tropical disease that affects mostly the poorest communities in sub-Saharan Africa. Toxic side effects associated with the use of current anti-trypanosomal drugs, which in some cases kill faster than the disease itself, necessitate the search for new drugs with better safety margins. To this effect, a small library bearing different substituents at position -1, -3, and -6 of the quinolone nucleus were synthesized and evaluated in vitro against HeLa cell lines and Trypanosoma brucei brucei for cytotoxicity and trypanocidal potentials, respectively. While most of these compounds showed no cytotoxic effect, they exhibited moderate to weak anti-trypanosomal activities. The SAR studies of this series provide new information worth considering in future exploration of the quinolone scaffold in search ofmore potent and safe trypanocidal agents.
- Full Text:
- Date Issued: 2018
Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives
- Waleguele, Christine C, Mba'ning, Brice M, Awantu, Angelbert F, Bankeu, Jean J, Fongang, Yannick S F, Ngouela, Augustin S, Tsamo, Etienne, Sewald, Norbert, Lenta, Bruno N, Krause, Rui W M
- Authors: Waleguele, Christine C , Mba'ning, Brice M , Awantu, Angelbert F , Bankeu, Jean J , Fongang, Yannick S F , Ngouela, Augustin S , Tsamo, Etienne , Sewald, Norbert , Lenta, Bruno N , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193364 , vital:45325 , xlink:href="https://doi.org/10.3390/molecules25122862"
- Description: The MeOH/CH2Cl2 (1:1) extracts of the roots and leaves of Beilschmiedia louisii and B. obscura showed potent antitrypanosomal activity during preliminary screening on Trypanosoma brucei brucei. Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B (1) and beilschmiedol C (2), and one new phenylalkene obscurene A (3) together with twelve known compounds (4–15). In addition, four new derivatives (11a–11d) were synthesized from compound 11. Their structures were elucidated based on their NMR and MS data. Compounds 5, 6, and 7 were isolated for the first time from the Beilschmiedia genus. Additionally, the NMR data of compound 4 are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against Tb brucei and the Plasmodium falciparum chloroquine-resistant strain Pf3D7 in vitro, respectively. From the tested compounds, the mixture of new compounds 1 and 2 exhibited the most potent antitrypanosomal activity in vitro with IC50 value of 4.91 μM.
- Full Text:
- Date Issued: 2020
- Authors: Waleguele, Christine C , Mba'ning, Brice M , Awantu, Angelbert F , Bankeu, Jean J , Fongang, Yannick S F , Ngouela, Augustin S , Tsamo, Etienne , Sewald, Norbert , Lenta, Bruno N , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193364 , vital:45325 , xlink:href="https://doi.org/10.3390/molecules25122862"
- Description: The MeOH/CH2Cl2 (1:1) extracts of the roots and leaves of Beilschmiedia louisii and B. obscura showed potent antitrypanosomal activity during preliminary screening on Trypanosoma brucei brucei. Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B (1) and beilschmiedol C (2), and one new phenylalkene obscurene A (3) together with twelve known compounds (4–15). In addition, four new derivatives (11a–11d) were synthesized from compound 11. Their structures were elucidated based on their NMR and MS data. Compounds 5, 6, and 7 were isolated for the first time from the Beilschmiedia genus. Additionally, the NMR data of compound 4 are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against Tb brucei and the Plasmodium falciparum chloroquine-resistant strain Pf3D7 in vitro, respectively. From the tested compounds, the mixture of new compounds 1 and 2 exhibited the most potent antitrypanosomal activity in vitro with IC50 value of 4.91 μM.
- Full Text:
- Date Issued: 2020
Photodynamic therapy activities of phthalocyanine-based macromolecular photosensitizers on MCF-7 breast cancer cells
- Ahmetali, Erem, Sen, Pinar, Süer, N Ceren, Nyokong, Tebello, Erin, Tarik, Sener, M Kasim
- Authors: Ahmetali, Erem , Sen, Pinar , Süer, N Ceren , Nyokong, Tebello , Erin, Tarik , Sener, M Kasim
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/185655 , vital:44407 , xlink:href="https://doi.org/10.1080/10601325.2021.1934012"
- Description: Poly(oxanorbornene)s with zinc(II) phthalocyanine side chains have been synthesized by ring-opening metathesis polymerization. The incorporation of zinc(II) phthalocyanine into cationic polymer has given poly(oxanorbornene)s noteworthy photophysicochemical properties and the capacity to generate singlet oxygen under light irradiation. To investigate photosensitizer’s properties of the newly synthesized polymers P6 and P7: fluorescence (ΦF), singlet oxygen (ΦΔ) and triplet (ΦT) quantum yields of polymers have been measured in dimethyl sulfoxide and aqueous medium. Singlet oxygen quantum yields of P6 and P7 have been found to be 0.22 and 0.20 in dimethyl sulfoxide, respectively. Then, photodynamic therapy activities of polymers (P1-P7) against human breast adenocarcinoma cell line (MCF-7 cells) have been investigated. The copolymer P5 bearing pendant zinc(II) phthalocyanine and triethyl phosphonium functionalities has showed enhanced PDT activity with less than 10% viable cells at 60 μg/mL.
- Full Text:
- Date Issued: 2021
- Authors: Ahmetali, Erem , Sen, Pinar , Süer, N Ceren , Nyokong, Tebello , Erin, Tarik , Sener, M Kasim
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/185655 , vital:44407 , xlink:href="https://doi.org/10.1080/10601325.2021.1934012"
- Description: Poly(oxanorbornene)s with zinc(II) phthalocyanine side chains have been synthesized by ring-opening metathesis polymerization. The incorporation of zinc(II) phthalocyanine into cationic polymer has given poly(oxanorbornene)s noteworthy photophysicochemical properties and the capacity to generate singlet oxygen under light irradiation. To investigate photosensitizer’s properties of the newly synthesized polymers P6 and P7: fluorescence (ΦF), singlet oxygen (ΦΔ) and triplet (ΦT) quantum yields of polymers have been measured in dimethyl sulfoxide and aqueous medium. Singlet oxygen quantum yields of P6 and P7 have been found to be 0.22 and 0.20 in dimethyl sulfoxide, respectively. Then, photodynamic therapy activities of polymers (P1-P7) against human breast adenocarcinoma cell line (MCF-7 cells) have been investigated. The copolymer P5 bearing pendant zinc(II) phthalocyanine and triethyl phosphonium functionalities has showed enhanced PDT activity with less than 10% viable cells at 60 μg/mL.
- Full Text:
- Date Issued: 2021
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
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
A New Synthetic Method for Tetraazatricyclic Derivatives and Evaluation of Their Biological Properties
- Odame, Felix, Betz, Richard, Hosten, Eric C, Krause, Jason, Isaacs, Michelle, Hoppe, Heinrich C, Khanye, Setshaba D, Sayed, Yasien, Frost, P Carminita, Lobb, Kevin A, Tshentu, Zenixole
- Authors: Odame, Felix , Betz, Richard , Hosten, Eric C , Krause, Jason , Isaacs, Michelle , Hoppe, Heinrich C , Khanye, Setshaba D , Sayed, Yasien , Frost, P Carminita , Lobb, Kevin A , Tshentu, Zenixole
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123189 , vital:35413 , https://doi.org/10.1002/slct.201802930
- Description: Herein, we propose novel quinolones incorporating an INH moiety as potential drug templates against TB. The quinolone-based compounds bearing an INH moiety attached via a hydrazide–hydrazone bond were synthesised and evaluated against Mycobacterium tuberculosis H37Rv (MTB). The compounds were also evaluated for cytotoxicity against HeLa cell lines. These compounds showed significant activity (MIC90) against MTB in the range of 0.2–8 μM without any cytotoxic effects. Compounds 10 (MIC90; 0.9 μM), 11 (MIC90; 0.2 μM), 12 (MIC90; 0.8 μM) and compound 15 (MIC90; 0.8 μM), the most active compounds in this series, demonstrate activities on par with INH and superior to those reported for the fluoroquinolones. The SAR analysis suggests that the nature of substituents at positions −1 and −3 of the quinolone nucleus influences anti-MTB activity. Aqueous solubility evaluation and in vitro metabolic stability of compound 12 highlights favourable drug-like properties for this compound class.
- Full Text:
- Date Issued: 2018
- Authors: Odame, Felix , Betz, Richard , Hosten, Eric C , Krause, Jason , Isaacs, Michelle , Hoppe, Heinrich C , Khanye, Setshaba D , Sayed, Yasien , Frost, P Carminita , Lobb, Kevin A , Tshentu, Zenixole
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123189 , vital:35413 , https://doi.org/10.1002/slct.201802930
- Description: Herein, we propose novel quinolones incorporating an INH moiety as potential drug templates against TB. The quinolone-based compounds bearing an INH moiety attached via a hydrazide–hydrazone bond were synthesised and evaluated against Mycobacterium tuberculosis H37Rv (MTB). The compounds were also evaluated for cytotoxicity against HeLa cell lines. These compounds showed significant activity (MIC90) against MTB in the range of 0.2–8 μM without any cytotoxic effects. Compounds 10 (MIC90; 0.9 μM), 11 (MIC90; 0.2 μM), 12 (MIC90; 0.8 μM) and compound 15 (MIC90; 0.8 μM), the most active compounds in this series, demonstrate activities on par with INH and superior to those reported for the fluoroquinolones. The SAR analysis suggests that the nature of substituents at positions −1 and −3 of the quinolone nucleus influences anti-MTB activity. Aqueous solubility evaluation and in vitro metabolic stability of compound 12 highlights favourable drug-like properties for this compound class.
- Full Text:
- Date Issued: 2018
Optimal template removal from molecularly imprinted polymers by pressurized hot water extraction
- Batlokwa, Bareki Shima, Mokgadi, Janes, Nyokong, Tebello, Torto, Nelson
- Authors: Batlokwa, Bareki Shima , Mokgadi, Janes , Nyokong, Tebello , Torto, Nelson
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/247813 , vital:51620 , xlink:href="https://doi.org/10.1007/s10337-010-1884-3"
- Description: An optimal extraction method for the removal of templates from molecularly imprinted polymers (MIPs) is presented. The extraction method is based on pressurized hot water extraction (PHWE). PHWE was evaluated by application to three distinctly colored MIPs for chlorophyll (green), quercetin (yellow) and phthalocynine (dark blue) with subsequent monitoring of template removal and template bleeding by an ultraviolet spectrophotometer. The templates were washed-off and the extraction efficiency (EE) was compared to that of soxhlet and ultrasonic extraction methods. PHWE employed hot water at an optimal temperature of 220 °C, pressure of 50 bars and flow rate of 2 mL min−1 to thoroughly wash-off the respective templates from their MIPs. The EE evaluated for PHWE was over 99.6% for all the MIPs with no subsequent or minimal template bleeding (more than 0.01%). The washing procedure was simple and relatively fast as it was achieved in 70 min at the most. At 95% confidence level (n = 3), soxhlet and ultrasonic recorded EE that was not significantly different (more than 94.5% in all cases) from that of PHWE (less than 99.6% in all cases). Soxhlet and ultrasonic had washing procedures that were slower (over 18 h) and employed large quantities (400 mL) of organic solvents modified with acids. The percentage relative standard deviations (%RSD) for the EE and recovery results were less than 2.3% in all cases indicating the high reproducibility of the method. Overall, the three methods performed comparably in extracting templates. PHWE seems to be the method of choice as it employed water which poses no environmental threat.
- Full Text:
- Date Issued: 2011
- Authors: Batlokwa, Bareki Shima , Mokgadi, Janes , Nyokong, Tebello , Torto, Nelson
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/247813 , vital:51620 , xlink:href="https://doi.org/10.1007/s10337-010-1884-3"
- Description: An optimal extraction method for the removal of templates from molecularly imprinted polymers (MIPs) is presented. The extraction method is based on pressurized hot water extraction (PHWE). PHWE was evaluated by application to three distinctly colored MIPs for chlorophyll (green), quercetin (yellow) and phthalocynine (dark blue) with subsequent monitoring of template removal and template bleeding by an ultraviolet spectrophotometer. The templates were washed-off and the extraction efficiency (EE) was compared to that of soxhlet and ultrasonic extraction methods. PHWE employed hot water at an optimal temperature of 220 °C, pressure of 50 bars and flow rate of 2 mL min−1 to thoroughly wash-off the respective templates from their MIPs. The EE evaluated for PHWE was over 99.6% for all the MIPs with no subsequent or minimal template bleeding (more than 0.01%). The washing procedure was simple and relatively fast as it was achieved in 70 min at the most. At 95% confidence level (n = 3), soxhlet and ultrasonic recorded EE that was not significantly different (more than 94.5% in all cases) from that of PHWE (less than 99.6% in all cases). Soxhlet and ultrasonic had washing procedures that were slower (over 18 h) and employed large quantities (400 mL) of organic solvents modified with acids. The percentage relative standard deviations (%RSD) for the EE and recovery results were less than 2.3% in all cases indicating the high reproducibility of the method. Overall, the three methods performed comparably in extracting templates. PHWE seems to be the method of choice as it employed water which poses no environmental threat.
- Full Text:
- Date Issued: 2011
A comparative study of the dosimetric features of α-Al2O3: C, Mg and α-Al2O3: C
- Kalita, Jitumani M, Chithambo, Makaiko L
- Authors: Kalita, Jitumani M , Chithambo, Makaiko L
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/113058 , vital:33694 , https://doi.org/10.1093/rpd/ncx039
- Description: A comparative study of the dosimetric features of α-Al2O3:C,Mg and α-Al2O3:C relevant to thermoluminescence dosimetry is reported. A glow curve of α-Al2O3:C,Mg measured at 1°C/s after beta irradiation to 1 Gy shows two subsidiary peaks at 42°C (labelled as I) and 72°C (II) and the main peak at 161°C (III) whereas a glow curve of α-Al2O3:C measured under the same conditions shows the main peak at 178°C (II′) and a lower intensity peak at 48°C (I′). Apart from these ones, there are several other peaks at temperatures beyond that of the main peak in both α-Al2O3:C,Mg and α-Al2O3:C. However, the latter are not included in this study. We report a comparative quantitative analysis of dose response and fading of peaks I, II and III of α-Al2O3:C,Mg and peaks I′ and II′ of α-Al2O3:C. Analysis shows that the dose response of peaks I and III is sublinear within 1–10 Gy whereas that of peak II is superlinear within 1–4 Gy followed by a sublinear region within 4–10 Gy. In comparison, the dose response of peak I′ is superlinear within 1–4 Gy followed by a sublinear region within 4–10 Gy whereas that of peak II′ is sublinear within 1–4 Gy followed by a superlinear region within 4–10 Gy. As regards to fading corresponding to 1 Gy, peak I is very unstable and fades within 300 s, peak II is more stable and takes up to 43200 s to fade. In comparison, peak III fades down to 30% of its initial intensity within 2400 s. Interestingly, between 2400 and 800 s, the intensity fades by 17% only. Regarding fading in α-Al2O3:C, peak I′ fades within 600 s whereas peak II′ shows an inverse fading behaviour up to 64800 s. The rate of fading for peaks I, II and III in α-Al2O3:C,Mg was found to decrease with increase in dose. However, no such behaviour was observed in α-Al2O3:C. The fading in both samples is discussed on the basis of a charge hopping mechanism.
- Full Text:
- Date Issued: 2017
- Authors: Kalita, Jitumani M , Chithambo, Makaiko L
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/113058 , vital:33694 , https://doi.org/10.1093/rpd/ncx039
- Description: A comparative study of the dosimetric features of α-Al2O3:C,Mg and α-Al2O3:C relevant to thermoluminescence dosimetry is reported. A glow curve of α-Al2O3:C,Mg measured at 1°C/s after beta irradiation to 1 Gy shows two subsidiary peaks at 42°C (labelled as I) and 72°C (II) and the main peak at 161°C (III) whereas a glow curve of α-Al2O3:C measured under the same conditions shows the main peak at 178°C (II′) and a lower intensity peak at 48°C (I′). Apart from these ones, there are several other peaks at temperatures beyond that of the main peak in both α-Al2O3:C,Mg and α-Al2O3:C. However, the latter are not included in this study. We report a comparative quantitative analysis of dose response and fading of peaks I, II and III of α-Al2O3:C,Mg and peaks I′ and II′ of α-Al2O3:C. Analysis shows that the dose response of peaks I and III is sublinear within 1–10 Gy whereas that of peak II is superlinear within 1–4 Gy followed by a sublinear region within 4–10 Gy. In comparison, the dose response of peak I′ is superlinear within 1–4 Gy followed by a sublinear region within 4–10 Gy whereas that of peak II′ is sublinear within 1–4 Gy followed by a superlinear region within 4–10 Gy. As regards to fading corresponding to 1 Gy, peak I is very unstable and fades within 300 s, peak II is more stable and takes up to 43200 s to fade. In comparison, peak III fades down to 30% of its initial intensity within 2400 s. Interestingly, between 2400 and 800 s, the intensity fades by 17% only. Regarding fading in α-Al2O3:C, peak I′ fades within 600 s whereas peak II′ shows an inverse fading behaviour up to 64800 s. The rate of fading for peaks I, II and III in α-Al2O3:C,Mg was found to decrease with increase in dose. However, no such behaviour was observed in α-Al2O3:C. The fading in both samples is discussed on the basis of a charge hopping mechanism.
- Full Text:
- Date Issued: 2017
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
Isolation, characterization and antiproliferative activity of new metabolites from the South African endemic red algal species Laurencia alfredensis
- Dziwornu, Godwin A, Caira, Mino R, de la Mare, Jo-Anne, Edkins, Adrienne L, Bolton, John J, Beukes, Denzil R, Sunassee, Suthananda N
- Authors: Dziwornu, Godwin A , Caira, Mino R , de la Mare, Jo-Anne , Edkins, Adrienne L , Bolton, John J , Beukes, Denzil R , Sunassee, Suthananda N
- Date: 2017
- Language: English
- Type: article , text
- Identifier: http://hdl.handle.net/10962/59963 , vital:27715 , https://doi:10.3390/molecules22040513
- Description: The marine red algae of the genus Laurencia have been widely studied for their structurally diverse and biologically active secondary metabolites. We report here the natural product investigation of the organic extract of a newly identified South African endemic species, Laurencia alfredensis. A sequence of column chromatography, preparative TLC and normal phase HPLC resulted in the isolation of eleven compounds comprising three labdane-type diterpenes (1-3), four polyether triterpenes (4-7), three cholestane-type ecdysteroids (8-10) and a glycolipid (11). Compounds 1-3, 5-8 and 10 have not previously been reported, while compound 9 is reported here for the first time from a natural source and the known compound 11 isolated for the first time from the genus Laurencia. The structural elucidation and the relative configuration assignments of the compounds were accomplished by extensive use of ID- and 2D-NMR, HR-ESI-MS, UV and IR spectroscopic techniques, while the absolute configuration of compound 1 was determined by single-crystal X-ray diffraction analysis. All compounds were evaluated against the MDA-MB-231 breast and HeLa cervical cancer cell lines. Compound 2 exhibited low micromolar antiproliferative activity (IC50 = 9.3 gM) against the triple negative breast carcinoma and compound 7 was similarly active (IC50 = 8.8 gM) against the cervical cancer cell line.
- Full Text:
- Date Issued: 2017
- Authors: Dziwornu, Godwin A , Caira, Mino R , de la Mare, Jo-Anne , Edkins, Adrienne L , Bolton, John J , Beukes, Denzil R , Sunassee, Suthananda N
- Date: 2017
- Language: English
- Type: article , text
- Identifier: http://hdl.handle.net/10962/59963 , vital:27715 , https://doi:10.3390/molecules22040513
- Description: The marine red algae of the genus Laurencia have been widely studied for their structurally diverse and biologically active secondary metabolites. We report here the natural product investigation of the organic extract of a newly identified South African endemic species, Laurencia alfredensis. A sequence of column chromatography, preparative TLC and normal phase HPLC resulted in the isolation of eleven compounds comprising three labdane-type diterpenes (1-3), four polyether triterpenes (4-7), three cholestane-type ecdysteroids (8-10) and a glycolipid (11). Compounds 1-3, 5-8 and 10 have not previously been reported, while compound 9 is reported here for the first time from a natural source and the known compound 11 isolated for the first time from the genus Laurencia. The structural elucidation and the relative configuration assignments of the compounds were accomplished by extensive use of ID- and 2D-NMR, HR-ESI-MS, UV and IR spectroscopic techniques, while the absolute configuration of compound 1 was determined by single-crystal X-ray diffraction analysis. All compounds were evaluated against the MDA-MB-231 breast and HeLa cervical cancer cell lines. Compound 2 exhibited low micromolar antiproliferative activity (IC50 = 9.3 gM) against the triple negative breast carcinoma and compound 7 was similarly active (IC50 = 8.8 gM) against the cervical cancer cell line.
- Full Text:
- Date Issued: 2017
Anti-malarial synergy of secondary metabolites from Morinda lucida Benth.
- Lakkakula, Jaya R, Matshaya, Thabo, Krause, Rui W M
- Authors: Lakkakula, Jaya R , Matshaya, Thabo , Krause, Rui W M
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125609 , vital:35800 , https://doi.org/10.1016/j.msec.2016.08.073
- Description: Ethnopharmacological relevance The roots, stem and leaves of Morinda lucida are used in some African countries as treatment against different types of fevers including yellow fever, malaria, trypanosomiasis and feverish conditions during child birth. Aim of the study To determine the in vitro cell toxicity and anti-malarial activity of the extracts of stem bark of M. lucida and to identify the secondary metabolites in the extract that may be responsible for this activity. Materials and methods The cell toxicity studies of crude extract [dichloromethane (DCM): Methanol (MeOH) in a ratio of1:1 (v/v)] as well as compounds isolated from the same extract were carried out using human cervix adenocarcinoma cells (HeLa cells); while the anti-malarial activities of the same samples were performed against Plasmodium falciparum strain 3D7 using the parasite lactate dehydrogenase (pLDH) assay. The isolation of the active compounds was carried out using chromatographic techniques (column and thin layer chromatography) where as mass spectrometry (MS), Fourier transform infrared spectroscopy (FTIR) as well as 1D- and 2D- nuclear magnetic resonance (NMR) analyses were employed in the characterisation and identification of the isolated secondary metabolites. Results The pLDH and cell toxicity assays for the crude extract and the fractions of M. lucida indicated that some fractions reduced the malaria parasite viability by approximately 50% at 100 μg/mL and they were not significantly cytotoxic. An IC50 done on the crude extract gave a value of 25 μg/mL. The % cell viability for the crude extract in cell toxicity assay remained at 100%. Seven chemical constituents i.e. asperuloside (1), asperulosidic acid (2), stigmasterol (3a), β-sitosterol (3b), cycloartenol (3c), campesterol (3d) and 5,15-O-dimethylmorindol (4) were isolated from the DCM-MeOH extract of stem bark. The isolated compounds tested were not that active by themselves individually at 20 μM but their activities were increased when the isolated compounds were combined. As seen when compounds 2, 3 and 4 (% viability: 93, 123 and 101 respectively) were combined yielding an IC50 value of 17 μM. Furthermore, this is the first report of compounds 1, 2, 3c, 3d and 4 isolated from M. lucida. Conclusion The crude extract completely suppressed the growth of P. falciparum. This indicates that the crude extract contains many compounds that might be acting in synergy. The observed activity of the crude extract and the samples containing a mixture of different compounds support the traditional use of M. lucida for the treatment of malaria.
- Full Text:
- Date Issued: 2017
- Authors: Lakkakula, Jaya R , Matshaya, Thabo , Krause, Rui W M
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125609 , vital:35800 , https://doi.org/10.1016/j.msec.2016.08.073
- Description: Ethnopharmacological relevance The roots, stem and leaves of Morinda lucida are used in some African countries as treatment against different types of fevers including yellow fever, malaria, trypanosomiasis and feverish conditions during child birth. Aim of the study To determine the in vitro cell toxicity and anti-malarial activity of the extracts of stem bark of M. lucida and to identify the secondary metabolites in the extract that may be responsible for this activity. Materials and methods The cell toxicity studies of crude extract [dichloromethane (DCM): Methanol (MeOH) in a ratio of1:1 (v/v)] as well as compounds isolated from the same extract were carried out using human cervix adenocarcinoma cells (HeLa cells); while the anti-malarial activities of the same samples were performed against Plasmodium falciparum strain 3D7 using the parasite lactate dehydrogenase (pLDH) assay. The isolation of the active compounds was carried out using chromatographic techniques (column and thin layer chromatography) where as mass spectrometry (MS), Fourier transform infrared spectroscopy (FTIR) as well as 1D- and 2D- nuclear magnetic resonance (NMR) analyses were employed in the characterisation and identification of the isolated secondary metabolites. Results The pLDH and cell toxicity assays for the crude extract and the fractions of M. lucida indicated that some fractions reduced the malaria parasite viability by approximately 50% at 100 μg/mL and they were not significantly cytotoxic. An IC50 done on the crude extract gave a value of 25 μg/mL. The % cell viability for the crude extract in cell toxicity assay remained at 100%. Seven chemical constituents i.e. asperuloside (1), asperulosidic acid (2), stigmasterol (3a), β-sitosterol (3b), cycloartenol (3c), campesterol (3d) and 5,15-O-dimethylmorindol (4) were isolated from the DCM-MeOH extract of stem bark. The isolated compounds tested were not that active by themselves individually at 20 μM but their activities were increased when the isolated compounds were combined. As seen when compounds 2, 3 and 4 (% viability: 93, 123 and 101 respectively) were combined yielding an IC50 value of 17 μM. Furthermore, this is the first report of compounds 1, 2, 3c, 3d and 4 isolated from M. lucida. Conclusion The crude extract completely suppressed the growth of P. falciparum. This indicates that the crude extract contains many compounds that might be acting in synergy. The observed activity of the crude extract and the samples containing a mixture of different compounds support the traditional use of M. lucida for the treatment of malaria.
- Full Text:
- Date Issued: 2017
In Vitro Studies on Antioxidant and AntiParasitic Activities of Compounds Isolated from Rauvolfia caffra Sond
- Tlhapi, Dorcas B, Ramaite, Isaiah D, Anokwuru, Chinedu P, van Ree, Teunis, Hoppe, Heinrich C
- Authors: Tlhapi, Dorcas B , Ramaite, Isaiah D , Anokwuru, Chinedu P , van Ree, Teunis , Hoppe, Heinrich C
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/425993 , vital:72305 , xlink:href="https://doi.org/10.3390/molecules25173781"
- Description: As part of an ongoing study of natural products from local medicinal plants, the methanol extract of stem bark of Rauvolfia caffra Sond was investigated for biological activity. Column chromatography and preparative thin-layer chromatography were used to isolate lupeol (1), raucaffricine (2), N-methylsarpagine (3), and spegatrine (4). The crude extract, fractions and isolated compounds were tested for anti-oxidant, antitrypanosomal and anti-proliferation activities. Two fractions displayed high DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity and reducing power with IC50 (The half maximal inhibitory concentration) and IC0.5 values of 0.022 ± 0.003 mg/mL and 0.036 ± 0.007 mg/mL, and 0.518 ± 0.044 mg/mL and 1.076 ± 0.136 mg/mL, respectively. Spegatrine (4) was identified as the main antioxidant compound in R. caffra with IC50 and IC0.5 values of 0.119 ± 0.067 mg/mL and 0.712 ± 0 mg/mL, respectively. One fraction displayed high antitrypanosomal activity with an IC50 value of 18.50 μg/mL. However, the major constituent of this fraction, raucaffricine (2), was not active. The crude extract, fractions and pure compounds did not display any cytotoxic effect at a concentration of 50 μg/mL against HeLa cells. This study shows directions for further in vitro studies on the antioxidant and antitrypanosomal activities of Rauvolfia caffra Sond.
- Full Text:
- Date Issued: 2020
- Authors: Tlhapi, Dorcas B , Ramaite, Isaiah D , Anokwuru, Chinedu P , van Ree, Teunis , Hoppe, Heinrich C
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/425993 , vital:72305 , xlink:href="https://doi.org/10.3390/molecules25173781"
- Description: As part of an ongoing study of natural products from local medicinal plants, the methanol extract of stem bark of Rauvolfia caffra Sond was investigated for biological activity. Column chromatography and preparative thin-layer chromatography were used to isolate lupeol (1), raucaffricine (2), N-methylsarpagine (3), and spegatrine (4). The crude extract, fractions and isolated compounds were tested for anti-oxidant, antitrypanosomal and anti-proliferation activities. Two fractions displayed high DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity and reducing power with IC50 (The half maximal inhibitory concentration) and IC0.5 values of 0.022 ± 0.003 mg/mL and 0.036 ± 0.007 mg/mL, and 0.518 ± 0.044 mg/mL and 1.076 ± 0.136 mg/mL, respectively. Spegatrine (4) was identified as the main antioxidant compound in R. caffra with IC50 and IC0.5 values of 0.119 ± 0.067 mg/mL and 0.712 ± 0 mg/mL, respectively. One fraction displayed high antitrypanosomal activity with an IC50 value of 18.50 μg/mL. However, the major constituent of this fraction, raucaffricine (2), was not active. The crude extract, fractions and pure compounds did not display any cytotoxic effect at a concentration of 50 μg/mL against HeLa cells. This study shows directions for further in vitro studies on the antioxidant and antitrypanosomal activities of Rauvolfia caffra Sond.
- Full Text:
- Date Issued: 2020