Study South Africa
- International Education Association of South Africa (IEASA), Jooste, Nico
- Authors: International Education Association of South Africa (IEASA) , Jooste, Nico
- Date: 2012
- Subjects: Education, Higher -- South Africa , Universities and colleges -- South Africa , Technical Institutes -- South Africa , Vocational guidance -- South Africa
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/64928 , vital:28637 , ISBN 9780620542661
- Description: [Extract from article by Ms Merle Hodges]: A recent article points to the feeling of alienation that students feel when studying away from home. It seeks to address the problem by establishing a range of fora where foreign students can feel more ‘at home’. It encourages host students to be more willing to accommodate these ‘outsiders’ in order to boost the reputation of the institution. Most of these initiatives are slightly patronising, but obviously well-meant. The overriding sense behind the article is that international students, within higher education institutions, are a benevolent burden. International students should be looked after, because universities are generally maternal (they are someone’s alma mater after all), places of kindness (they literally give away knowledge) and generally care for others (community outreach is fundamental to most universities). More importantly, international students – in places like the USA and UK – generate additional funding in an environment where government and federal funding is drying up. But what if four out of every ten students in the world who graduated were from China and India? In the next eight years? That genial inconvenience now becomes an imperative. These are the predictions by such august organisations as The British Council and the education branch of the OECD. It is also anticipated that these countries will not be in a position to educate this number of students internally. Which, in turn, suggests that there will be mass outflows at the undergraduate level and, by sheer dint of numbers, also means that internationalisation is heading towards a compounding acceleration in numbers. Where then does internationalisation stand? It will no longer be an altruistic add-on, but core business to the lifeblood of the universities across the globe. As far back as 1994, Jane Knight understood internationalisation as a phenomenon that would have a profound impact on the functions and structures of the university. “Internationalization,” she points out, “is the process of integrating an international, intercultural, global outlook into the major functions of a university – teaching, SRC, and service functions.” Over the past year arguments have been made that suggest that global shifts in student demographics are not the ‘province’ of South African higher education and that our obligation is to focus internally, on poverty alleviation and job creation. This argument misses the point. The free flow of academics and students – especially the large number of postgraduate students from other countries already at our institutions – are working with our academics on solving exactly these kinds of problems. IEASA is no longer only about the 60 000 students who migrate to our shores annually. It’s about what they learn and the diverse experiences that they will go through; experiences that will change them for life and will inevitably bring them to a different understanding of the world that we, collectively, are presently fashioning. , 12th Edition
- Full Text:
- Date Issued: 2012
- Authors: International Education Association of South Africa (IEASA) , Jooste, Nico
- Date: 2012
- Subjects: Education, Higher -- South Africa , Universities and colleges -- South Africa , Technical Institutes -- South Africa , Vocational guidance -- South Africa
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/64928 , vital:28637 , ISBN 9780620542661
- Description: [Extract from article by Ms Merle Hodges]: A recent article points to the feeling of alienation that students feel when studying away from home. It seeks to address the problem by establishing a range of fora where foreign students can feel more ‘at home’. It encourages host students to be more willing to accommodate these ‘outsiders’ in order to boost the reputation of the institution. Most of these initiatives are slightly patronising, but obviously well-meant. The overriding sense behind the article is that international students, within higher education institutions, are a benevolent burden. International students should be looked after, because universities are generally maternal (they are someone’s alma mater after all), places of kindness (they literally give away knowledge) and generally care for others (community outreach is fundamental to most universities). More importantly, international students – in places like the USA and UK – generate additional funding in an environment where government and federal funding is drying up. But what if four out of every ten students in the world who graduated were from China and India? In the next eight years? That genial inconvenience now becomes an imperative. These are the predictions by such august organisations as The British Council and the education branch of the OECD. It is also anticipated that these countries will not be in a position to educate this number of students internally. Which, in turn, suggests that there will be mass outflows at the undergraduate level and, by sheer dint of numbers, also means that internationalisation is heading towards a compounding acceleration in numbers. Where then does internationalisation stand? It will no longer be an altruistic add-on, but core business to the lifeblood of the universities across the globe. As far back as 1994, Jane Knight understood internationalisation as a phenomenon that would have a profound impact on the functions and structures of the university. “Internationalization,” she points out, “is the process of integrating an international, intercultural, global outlook into the major functions of a university – teaching, SRC, and service functions.” Over the past year arguments have been made that suggest that global shifts in student demographics are not the ‘province’ of South African higher education and that our obligation is to focus internally, on poverty alleviation and job creation. This argument misses the point. The free flow of academics and students – especially the large number of postgraduate students from other countries already at our institutions – are working with our academics on solving exactly these kinds of problems. IEASA is no longer only about the 60 000 students who migrate to our shores annually. It’s about what they learn and the diverse experiences that they will go through; experiences that will change them for life and will inevitably bring them to a different understanding of the world that we, collectively, are presently fashioning. , 12th Edition
- Full Text:
- Date Issued: 2012
Submission to Press Freedom Commission (PFC) on Media Self-regulation, Co-regulation or Statutory regulation in South Africa:
- Wasserman, Herman, Steenveld, Lynette N, Strelitz, Larry N, Amner, Roderick J, Boshoff, Priscilla A, Mathurine, Jude, Garman, Anthea
- Authors: Wasserman, Herman , Steenveld, Lynette N , Strelitz, Larry N , Amner, Roderick J , Boshoff, Priscilla A , Mathurine, Jude , Garman, Anthea
- Date: 2012
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/143571 , vital:38263 , ISBN , https://www.ru.ac.za/media/rhodesuniversity/content/ruhome/documents/JMS Submission to Press Freedom Commission.pdf
- Description: Prof Duncan has outlined the relative merits and demerits of self-regulation, co-regulation and deregulation, with which we are in broad agreement. She has also ably dealt with the three functions of regulatory bodies, namely the setting of ground rules for the industry to ensure best practice; enforcement of these; and adjudication of claims and counter claims re journalistic practice (Duncan 2012, p17). Finally, she has also taken up the issue of the necessity of accepting Third Party Complaints as one of the fundamental mechanisms by which citizens can make complaints on the basis of principle, rather than being personally aggrieved. While we are in broad agreement with her on these issues, we would like to highlight some further points for consideration.
- Full Text:
- Date Issued: 2012
- Authors: Wasserman, Herman , Steenveld, Lynette N , Strelitz, Larry N , Amner, Roderick J , Boshoff, Priscilla A , Mathurine, Jude , Garman, Anthea
- Date: 2012
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/143571 , vital:38263 , ISBN , https://www.ru.ac.za/media/rhodesuniversity/content/ruhome/documents/JMS Submission to Press Freedom Commission.pdf
- Description: Prof Duncan has outlined the relative merits and demerits of self-regulation, co-regulation and deregulation, with which we are in broad agreement. She has also ably dealt with the three functions of regulatory bodies, namely the setting of ground rules for the industry to ensure best practice; enforcement of these; and adjudication of claims and counter claims re journalistic practice (Duncan 2012, p17). Finally, she has also taken up the issue of the necessity of accepting Third Party Complaints as one of the fundamental mechanisms by which citizens can make complaints on the basis of principle, rather than being personally aggrieved. While we are in broad agreement with her on these issues, we would like to highlight some further points for consideration.
- Full Text:
- Date Issued: 2012
Substantive second-level reasoning and experiential learning in legal ethics
- Authors: Kruuse, Helen
- Date: 2012
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/68983 , vital:29345 , https://hdl.handle.net/10520/EJC127082
- Description: Publisher version , This article takes a critical look at law teaching in South Africa and seeks to consider how the application of experiential learning theory may assist law students in gaining a deeper understanding of the law in general, and the complexities of real life practice in particular. While clinical legal education is often seen as the locus of experiential learning in law, the author proposes that well-structured simulations in class can achieve similar goals. The article comprises a description of the nature of experiential learning and a further description of the application of the principles of experiential learning in a particular simulation exercise in a Legal Ethics course (using the US case of Wash St Phys Ins Exch v Fisons Corp 858 P2d 1054 (Wash 1993) as a basis). The author posits that the so-called experiential learning "cycle" or "process" enables a process of learning which draws out the students' beliefs and ideas about a topic so that it can be examined, tested and integrated with new, more refined ideas. This notion is then in keeping with the expectation that students who emerge from higher education institutions have developed meta-cognitive skills. Essentially then, it is hoped that, by using the methods proposed in this article, students can then manage their own development and learning throughout life.
- Full Text: false
- Date Issued: 2012
- Authors: Kruuse, Helen
- Date: 2012
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/68983 , vital:29345 , https://hdl.handle.net/10520/EJC127082
- Description: Publisher version , This article takes a critical look at law teaching in South Africa and seeks to consider how the application of experiential learning theory may assist law students in gaining a deeper understanding of the law in general, and the complexities of real life practice in particular. While clinical legal education is often seen as the locus of experiential learning in law, the author proposes that well-structured simulations in class can achieve similar goals. The article comprises a description of the nature of experiential learning and a further description of the application of the principles of experiential learning in a particular simulation exercise in a Legal Ethics course (using the US case of Wash St Phys Ins Exch v Fisons Corp 858 P2d 1054 (Wash 1993) as a basis). The author posits that the so-called experiential learning "cycle" or "process" enables a process of learning which draws out the students' beliefs and ideas about a topic so that it can be examined, tested and integrated with new, more refined ideas. This notion is then in keeping with the expectation that students who emerge from higher education institutions have developed meta-cognitive skills. Essentially then, it is hoped that, by using the methods proposed in this article, students can then manage their own development and learning throughout life.
- Full Text: false
- Date Issued: 2012
Suicide - a global overview and focus on the South African situation
- Authors: Alonso-Betancourt, O
- Date: 2012
- Subjects: Suicide and Epilepsy Suicide -- South Africa Suicide -- Assessment -- Prevention
- Language: English
- Type: text , Lectures
- Identifier: http://hdl.handle.net/11260/1067 , vital:30560
- Description: As a medical doctor you learn how to deal with death and you feel that your duty is to encourage people to fight against illness for their lives but, when you face suicide, you feel defenseless because it is the person him or herself who chooses to die. Another reason for choosing this topic is that I’m advocating the development and implementation of a Suicide Prevention Program in South Africa and this could be a good forum to talk about this important issue.
- Full Text:
- Date Issued: 2012
- Authors: Alonso-Betancourt, O
- Date: 2012
- Subjects: Suicide and Epilepsy Suicide -- South Africa Suicide -- Assessment -- Prevention
- Language: English
- Type: text , Lectures
- Identifier: http://hdl.handle.net/11260/1067 , vital:30560
- Description: As a medical doctor you learn how to deal with death and you feel that your duty is to encourage people to fight against illness for their lives but, when you face suicide, you feel defenseless because it is the person him or herself who chooses to die. Another reason for choosing this topic is that I’m advocating the development and implementation of a Suicide Prevention Program in South Africa and this could be a good forum to talk about this important issue.
- Full Text:
- Date Issued: 2012
Syntheses, protonation constants and antimicrobial activity of 2-substituted N-alkylimidazole derivatives
- Kleyi, Phumelele, Walmsley, Ryan S, Gundhla, Isaac Z, Walmsley, Tara A, Jauka, Tembisa I, Dames, Joanna F, Walker, Roderick B, Torto, Nelson, Tshentu, Zenixole R
- Authors: Kleyi, Phumelele , Walmsley, Ryan S , Gundhla, Isaac Z , Walmsley, Tara A , Jauka, Tembisa I , Dames, Joanna F , Walker, Roderick B , Torto, Nelson , Tshentu, Zenixole R
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184066 , vital:44165 , xlink:href="https://www.ajol.info/index.php/sajc/article/view/123858"
- Description: A series of N-alkylimidazole-2-carboxylic acid, N-alkylimidazole-2-carboxaldehyde and N-alkylimidazole-2-methanol derivatives [alkyl = benzyl, methyl, ethyl, propyl, butyl, heptyl, octyl and decyl] have been synthesized and the protonation constants determined. The antimicrobial properties of the compounds were tested against Gram-negative (Escherichi coli), Gram-positive (Staphylococcus aureus and Bacillus subtilis subsp. spizizenii) bacterial strains and yeast (C. albicans). Both the disk diffusion and broth microdilution methods for testing the antimicrobial activity showed that N-alkylation of imidazole with longer alkyl chains and the substitution with low pKa group at 2-position resulted in enhanced antimicrobial activity. Particularly, the N-alkylimidazole-2-carboxylic acids exhibited the best antimicrobial activity due to the low pKa of the carboxylic acid moiety. Generally, all the N-alkylimidazole derivatives were most active against the Gram-positive bacteria [S. aureus (MIC = 5–160 µg mL–1) and B. subtilis subsp. spizizenii (5–20 µg mL–1)], with the latter more susceptible. All the compounds showed poor antimicrobial activity against both Gram-negative (E. coli, MIC = 0.15 to >2500 µg mL–1) bacteria and all the compounds were inactive against the yeast (Candida albicans).
- Full Text:
- Date Issued: 2012
- Authors: Kleyi, Phumelele , Walmsley, Ryan S , Gundhla, Isaac Z , Walmsley, Tara A , Jauka, Tembisa I , Dames, Joanna F , Walker, Roderick B , Torto, Nelson , Tshentu, Zenixole R
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184066 , vital:44165 , xlink:href="https://www.ajol.info/index.php/sajc/article/view/123858"
- Description: A series of N-alkylimidazole-2-carboxylic acid, N-alkylimidazole-2-carboxaldehyde and N-alkylimidazole-2-methanol derivatives [alkyl = benzyl, methyl, ethyl, propyl, butyl, heptyl, octyl and decyl] have been synthesized and the protonation constants determined. The antimicrobial properties of the compounds were tested against Gram-negative (Escherichi coli), Gram-positive (Staphylococcus aureus and Bacillus subtilis subsp. spizizenii) bacterial strains and yeast (C. albicans). Both the disk diffusion and broth microdilution methods for testing the antimicrobial activity showed that N-alkylation of imidazole with longer alkyl chains and the substitution with low pKa group at 2-position resulted in enhanced antimicrobial activity. Particularly, the N-alkylimidazole-2-carboxylic acids exhibited the best antimicrobial activity due to the low pKa of the carboxylic acid moiety. Generally, all the N-alkylimidazole derivatives were most active against the Gram-positive bacteria [S. aureus (MIC = 5–160 µg mL–1) and B. subtilis subsp. spizizenii (5–20 µg mL–1)], with the latter more susceptible. All the compounds showed poor antimicrobial activity against both Gram-negative (E. coli, MIC = 0.15 to >2500 µg mL–1) bacteria and all the compounds were inactive against the yeast (Candida albicans).
- Full Text:
- Date Issued: 2012
Synthesis and photophysical behavior of a novel zinc phthalocyanine containing a single carboxylic acid and three phenylthio substituents
- Forteath, Shaun, Antunes, Edith M, Chidawanyika, Wadzanai J U, Nyokong, Tebello
- Authors: Forteath, Shaun , Antunes, Edith M , Chidawanyika, Wadzanai J U , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/243207 , vital:51127 , xlink:href="https://doi.org/10.1016/j.jlumin.2012.03.050"
- Description: Zinc 2, (3)-tri-(phenylthio)-2, (3)-carboxy phthalocyanine (ZnPc(COOH)(SPh)3), zinc 2, (3)-tetra-(phenylthio) phthalocyanine (ZnPc(SPh)4) and 2, (3)-tetra-(phenylthio) phthalocyanine (H2Pc(SPh)4) were synthesized and their photophysical behavior were compared with those of a number of zinc phthalocyanine (ZnPc) derivatives. ZnPc(COOH)(SPh)3 and ZnPc(SPh)4 had similar fluorescence (ΦF=0.14) and triplet state (ΦT=0.65) quantum yields in dimethylsulfoxide, hence showing no effects of the replacement of one of the phenylthio groups with a carboxylic acid group. ZnPc(COOH)(SPh)3 displayed a slightly shorter triplet lifetime (τT=331 μs) than ZnPc (τT=350 μs) in DMSO, but within the range of ZnPc derivatives. The triplet lifetime for ZnPc(COOH)(SPh)3 is much longer than for the symmetrical derivative (ZnPc(SPh)4) with τT=149 μs in DMSO.
- Full Text:
- Date Issued: 2012
- Authors: Forteath, Shaun , Antunes, Edith M , Chidawanyika, Wadzanai J U , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/243207 , vital:51127 , xlink:href="https://doi.org/10.1016/j.jlumin.2012.03.050"
- Description: Zinc 2, (3)-tri-(phenylthio)-2, (3)-carboxy phthalocyanine (ZnPc(COOH)(SPh)3), zinc 2, (3)-tetra-(phenylthio) phthalocyanine (ZnPc(SPh)4) and 2, (3)-tetra-(phenylthio) phthalocyanine (H2Pc(SPh)4) were synthesized and their photophysical behavior were compared with those of a number of zinc phthalocyanine (ZnPc) derivatives. ZnPc(COOH)(SPh)3 and ZnPc(SPh)4 had similar fluorescence (ΦF=0.14) and triplet state (ΦT=0.65) quantum yields in dimethylsulfoxide, hence showing no effects of the replacement of one of the phenylthio groups with a carboxylic acid group. ZnPc(COOH)(SPh)3 displayed a slightly shorter triplet lifetime (τT=331 μs) than ZnPc (τT=350 μs) in DMSO, but within the range of ZnPc derivatives. The triplet lifetime for ZnPc(COOH)(SPh)3 is much longer than for the symmetrical derivative (ZnPc(SPh)4) with τT=149 μs in DMSO.
- Full Text:
- Date Issued: 2012
Synthesis and photophysical properties of covalent conjugates of aqua platinum (II) and octacarboxy-substituted zinc phthalocyanine
- Bulgakov, Roman A, Kuznetsova, Nina A, Dolotova, Olga V, Solovieva, Ludmila I, Mack, John, Chidawanyika, Wadzanai J U, Kaliya, Oleg L, Nyokong, Tebello
- Authors: Bulgakov, Roman A , Kuznetsova, Nina A , Dolotova, Olga V , Solovieva, Ludmila I , Mack, John , Chidawanyika, Wadzanai J U , Kaliya, Oleg L , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242726 , vital:51073 , xlink:href="https://doi.org/10.1142/S1088424612501209"
- Description: New covalent conjugates of aqua platinum(II) and octacarboxy-substituted zinc phthalocyanine, bearing one, two, three and four aqua platinum moieties on the periphery of the Pc ligand have been synthesized and characterized. The effect of the stepwise introduction of the aqua platinums on the photophysical and photochemical properties of these compounds has been investigated in dimethylsulfoxide solution. It has been found that aqua platinum moieties have only a limited effect on the dynamics of the singlet and triplet excited states, on the ability to sensitize singlet oxygen formation and on the photostability. Each conjugate has a high singlet oxygen quantum yield (ΦΔ 0.51–0.62) and thus retains potential for use as a dual action anticancer drugs by acting as a sensitizer for PDT in addition to the likely chemotherapeutic effects of the Pt(II) complexes.
- Full Text:
- Date Issued: 2012
- Authors: Bulgakov, Roman A , Kuznetsova, Nina A , Dolotova, Olga V , Solovieva, Ludmila I , Mack, John , Chidawanyika, Wadzanai J U , Kaliya, Oleg L , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242726 , vital:51073 , xlink:href="https://doi.org/10.1142/S1088424612501209"
- Description: New covalent conjugates of aqua platinum(II) and octacarboxy-substituted zinc phthalocyanine, bearing one, two, three and four aqua platinum moieties on the periphery of the Pc ligand have been synthesized and characterized. The effect of the stepwise introduction of the aqua platinums on the photophysical and photochemical properties of these compounds has been investigated in dimethylsulfoxide solution. It has been found that aqua platinum moieties have only a limited effect on the dynamics of the singlet and triplet excited states, on the ability to sensitize singlet oxygen formation and on the photostability. Each conjugate has a high singlet oxygen quantum yield (ΦΔ 0.51–0.62) and thus retains potential for use as a dual action anticancer drugs by acting as a sensitizer for PDT in addition to the likely chemotherapeutic effects of the Pt(II) complexes.
- Full Text:
- Date Issued: 2012
Synthesis and photophysical properties of peripherally and non-peripherally mercaptopyridine substituted metal free, Mg (II) and Al (III) phthalocyanines
- Arslanoğlu, Yasin, Idowu, Mopelela, Nyokong, Tebello
- Authors: Arslanoğlu, Yasin , Idowu, Mopelela , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/243248 , vital:51131 , xlink:href="https://doi.org/10.1016/j.saa.2012.04.004"
- Description: The syntheses and photophysical properties of metallophthalocyanines containing Mg2+ and Al3+ as central metal ions and their unmetallated derivative (complexes 3–8) tetra- substituted at the non-peripheral (α) and peripheral (β) positions with 2-mercaptopyridine are reported. The trends in triplet and fluorescence quantum yields are described for these compounds. The complexes exhibited relatively high triplet quantum yields (ΦT) ranging from 0.33 to 0.54 and fluorescence quantum yields (ΦF) ranging from 0.02 to 0.29. Triplet state lifetimes of the complexes were long ranging from 120 to 460 μs, indicating a potential use of these complexes as photosensitizers.
- Full Text:
- Date Issued: 2012
- Authors: Arslanoğlu, Yasin , Idowu, Mopelela , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/243248 , vital:51131 , xlink:href="https://doi.org/10.1016/j.saa.2012.04.004"
- Description: The syntheses and photophysical properties of metallophthalocyanines containing Mg2+ and Al3+ as central metal ions and their unmetallated derivative (complexes 3–8) tetra- substituted at the non-peripheral (α) and peripheral (β) positions with 2-mercaptopyridine are reported. The trends in triplet and fluorescence quantum yields are described for these compounds. The complexes exhibited relatively high triplet quantum yields (ΦT) ranging from 0.33 to 0.54 and fluorescence quantum yields (ΦF) ranging from 0.02 to 0.29. Triplet state lifetimes of the complexes were long ranging from 120 to 460 μs, indicating a potential use of these complexes as photosensitizers.
- Full Text:
- Date Issued: 2012
Synthesis and photophysicochemical properties of novel zinc phthalocyanines mono substituted with carboxyl containing functional groups
- Rapulenyane, Nomasonto, Antunes, Edith M, Masilela, Nkosiphile, Nyokong, Tebello
- Authors: Rapulenyane, Nomasonto , Antunes, Edith M , Masilela, Nkosiphile , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242389 , vital:51037 , xlink:href="https://doi.org/10.1016/j.jphotochem.2012.09.007"
- Description: This work reports on the synthesis and the physicochemical properties of novel unsymmetrically substituted zinc phthalocyanines (complexes 8, 10 and 11) and their symmetrically substituted counterparts (complexes 9, 12 and 13). The new complexes and their counterparts were successfully structurally characterized by IR, NMR, mass spectral and elemental analyses. Low fluorescence quantum yields (0.032) and lifetimes (0.91 ns) were obtained for the symmetrical ZnOTPc (complex 9) compared to the higher fluorescence quantum yields (0.15, 0.13, 0.10, 0.09 and 0.29) and lifetimes (4.4, 1.69, 1.69, 2.16 and 3.23 ns) obtained for ZnMPCPc (8), ZnTDTPc (12), ZnMCapPc (10), ZnMCafPc (11) and ZnTCPPc (13), respectively. All the complexes showed the ability to produce singlet oxygen with the highest triplet quantum yields obtained for 8 and 10 (0.80 and 0.65 respectively). High triplet lifetimes (109–286 μs) were obtained for all complexes. Complex 8 showed the longest triplet and fluorescence lifetimes as well the largest triplet state and singlet oxygen quantum yields.
- Full Text:
- Date Issued: 2012
- Authors: Rapulenyane, Nomasonto , Antunes, Edith M , Masilela, Nkosiphile , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242389 , vital:51037 , xlink:href="https://doi.org/10.1016/j.jphotochem.2012.09.007"
- Description: This work reports on the synthesis and the physicochemical properties of novel unsymmetrically substituted zinc phthalocyanines (complexes 8, 10 and 11) and their symmetrically substituted counterparts (complexes 9, 12 and 13). The new complexes and their counterparts were successfully structurally characterized by IR, NMR, mass spectral and elemental analyses. Low fluorescence quantum yields (0.032) and lifetimes (0.91 ns) were obtained for the symmetrical ZnOTPc (complex 9) compared to the higher fluorescence quantum yields (0.15, 0.13, 0.10, 0.09 and 0.29) and lifetimes (4.4, 1.69, 1.69, 2.16 and 3.23 ns) obtained for ZnMPCPc (8), ZnTDTPc (12), ZnMCapPc (10), ZnMCafPc (11) and ZnTCPPc (13), respectively. All the complexes showed the ability to produce singlet oxygen with the highest triplet quantum yields obtained for 8 and 10 (0.80 and 0.65 respectively). High triplet lifetimes (109–286 μs) were obtained for all complexes. Complex 8 showed the longest triplet and fluorescence lifetimes as well the largest triplet state and singlet oxygen quantum yields.
- Full Text:
- Date Issued: 2012
Synthesis and physicochemical behavior of new low symmetry Ge, Ti and Sn phthalocyanines
- Masilela, Nkosiphile, Nyokong, Tebello
- Authors: Masilela, Nkosiphile , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242421 , vital:51040 , xlink:href="https://doi.org/10.1016/j.synthmet.2012.07.028"
- Description: The synthesis and photophysicochemical properties of new low symmetrically Ge, Sn and Ti phthalocyanines substituted with one carboxy containing group are reported. Broading and splitting in the absorption spectra were observed for some of the complexes in particular for both the titanium Pcs due to loss of symmetry. Higher fluorescence quantum yields and lifetimes were obtained for the Pcs substituted with three benzyloxy (5–7) compared to their corresponding counterparts substituted with six 2-diethylaminoethylthiol groups (9–11). The germanium Pc complexes gave the highest triplet and singlet oxygen quantum yields compared to all the other complexes studied in DMF. All the complexes showed reasonable ability to generate singlet oxygen with quantum yields ranging from 0.54 to 0.69.
- Full Text:
- Date Issued: 2012
- Authors: Masilela, Nkosiphile , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242421 , vital:51040 , xlink:href="https://doi.org/10.1016/j.synthmet.2012.07.028"
- Description: The synthesis and photophysicochemical properties of new low symmetrically Ge, Sn and Ti phthalocyanines substituted with one carboxy containing group are reported. Broading and splitting in the absorption spectra were observed for some of the complexes in particular for both the titanium Pcs due to loss of symmetry. Higher fluorescence quantum yields and lifetimes were obtained for the Pcs substituted with three benzyloxy (5–7) compared to their corresponding counterparts substituted with six 2-diethylaminoethylthiol groups (9–11). The germanium Pc complexes gave the highest triplet and singlet oxygen quantum yields compared to all the other complexes studied in DMF. All the complexes showed reasonable ability to generate singlet oxygen with quantum yields ranging from 0.54 to 0.69.
- Full Text:
- Date Issued: 2012
Synthesis and physicochemical behaviour of aluminium trikis and tetrakis (diaquaplatinum) octacarboxyphthalocynine
- Malinga, Nduduzo, Dolotova, Olga, Bulgakov, Roman, Antunes, Edith M, Nyokong, Tebello
- Authors: Malinga, Nduduzo , Dolotova, Olga , Bulgakov, Roman , Antunes, Edith M , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242687 , vital:51068 , xlink:href="https://doi.org/10.1016/j.dyepig.2012.05.011"
- Description: The combination of chemotherapy and photodynamic therapy was investigated by the synthesis and characterisation of phthalocyanine conjugates with Pt complexes. The complexes synthesized are: hydroxoaluminum trikis(diaquaplatinum) octacarboxyphthalocyanine (OHAlOCPc(Pt)3) and hydroxoaluminum tetrakis(diaquaplatinum) octacarboxyphthalocyanine (OHAlOCPc(Pt)4). The platinated phthalocyanine complexes gave long triplet lifetimes of 577 and 526 μs for OHAlOCPc(Pt)3 and OHAlOCPc(Pt)4, respectively. The triplet quantum yields were found to be 0.45 for OHAlOCPc(Pt)3 and 0.57 OHAlOCPc(Pt)4 while the singlet oxygen quantum yields were found to be 0.38 and 0.48, respectively.
- Full Text:
- Date Issued: 2012
- Authors: Malinga, Nduduzo , Dolotova, Olga , Bulgakov, Roman , Antunes, Edith M , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/242687 , vital:51068 , xlink:href="https://doi.org/10.1016/j.dyepig.2012.05.011"
- Description: The combination of chemotherapy and photodynamic therapy was investigated by the synthesis and characterisation of phthalocyanine conjugates with Pt complexes. The complexes synthesized are: hydroxoaluminum trikis(diaquaplatinum) octacarboxyphthalocyanine (OHAlOCPc(Pt)3) and hydroxoaluminum tetrakis(diaquaplatinum) octacarboxyphthalocyanine (OHAlOCPc(Pt)4). The platinated phthalocyanine complexes gave long triplet lifetimes of 577 and 526 μs for OHAlOCPc(Pt)3 and OHAlOCPc(Pt)4, respectively. The triplet quantum yields were found to be 0.45 for OHAlOCPc(Pt)3 and 0.57 OHAlOCPc(Pt)4 while the singlet oxygen quantum yields were found to be 0.38 and 0.48, respectively.
- Full Text:
- Date Issued: 2012
Synthesis of phthalocyanine conjugates with gold nanoparticles and liposomes for photodynamic therapy
- Nombona, Nolwazi, Maduray, Kaminee, Antunes, Edith M, Karsten, Aletta, Nyokong, Tebello
- Authors: Nombona, Nolwazi , Maduray, Kaminee , Antunes, Edith M , Karsten, Aletta , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/245798 , vital:51406 , xlink:href="https://doi.org/10.1016/j.jphotobiol.2011.11.007"
- Description: The efficiency of [2,9,17,23-tetrakis-(1,6-hexanedithiol)phthalocyaninato]zinc(II) as a photodynamic therapy (PDT) agent was investigated. This compound belongs to the second generation of photosensitizers currently tested for the cellular photo-damage of cancer cells. The production of reactive oxygen species (ROS) and phototoxicity of the photosensitizer were assessed. Healthy fibroblast cells and breast cancer (MCF-7) cells were treated with either free phthalocyanine or phthalocyanine bound to either gold nanoparticles or encapsulated in liposomes. Cell viability studies showed the optimum phototoxic effect on non-malignant cells to be 4.5 J cm−2. The PDT effect of the liposome bound phthalocyanine showed extensive damage of the breast cancer cells. Gold nanoparticles only showed a modest improvement in PDT activity.
- Full Text:
- Date Issued: 2012
- Authors: Nombona, Nolwazi , Maduray, Kaminee , Antunes, Edith M , Karsten, Aletta , Nyokong, Tebello
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/245798 , vital:51406 , xlink:href="https://doi.org/10.1016/j.jphotobiol.2011.11.007"
- Description: The efficiency of [2,9,17,23-tetrakis-(1,6-hexanedithiol)phthalocyaninato]zinc(II) as a photodynamic therapy (PDT) agent was investigated. This compound belongs to the second generation of photosensitizers currently tested for the cellular photo-damage of cancer cells. The production of reactive oxygen species (ROS) and phototoxicity of the photosensitizer were assessed. Healthy fibroblast cells and breast cancer (MCF-7) cells were treated with either free phthalocyanine or phthalocyanine bound to either gold nanoparticles or encapsulated in liposomes. Cell viability studies showed the optimum phototoxic effect on non-malignant cells to be 4.5 J cm−2. The PDT effect of the liposome bound phthalocyanine showed extensive damage of the breast cancer cells. Gold nanoparticles only showed a modest improvement in PDT activity.
- Full Text:
- Date Issued: 2012
Synthesis, density functional theory, molecular dynamics and electrochemical studies of 3-thiopheneacetic acid-capped gold nanoparticles
- Sosibo, Ndabenhle M, Mdluli, Phumlane S, Mashazi, Philani N, Dyan, Busiswa, Revaprasadu, Neerish, Nyokong, Tebello, Tshikhudo, Robert T, Skepu, Amanda, Van Der Lingen, Elma
- Authors: Sosibo, Ndabenhle M , Mdluli, Phumlane S , Mashazi, Philani N , Dyan, Busiswa , Revaprasadu, Neerish , Nyokong, Tebello , Tshikhudo, Robert T , Skepu, Amanda , Van Der Lingen, Elma
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/246446 , vital:51477 , xlink:href="https://doi.org/10.1016/j.molstruc.2011.09.057"
- Description: Gold nanoparticles capped with a bifunctional ligand, 3-thiopheneacetic acid (3-TAA) were synthesised by borohydride reduction at room temperature. The transmission electron microscopy (TEM) analysis showed that the particle aggregates and had semi-linear partial linkages that could be attributed to multi-modal binding of the ligand with various gold nanoparticles through the terminal thiolether (–S–) group and oxygen of the carboxylic (–COOH) group. This bimodal interaction led to limited stability of the resultant nanoparticles when tested using highly electrolytic media. To investigate further, density functional theory (DFT) quantum chemical and molecular dynamic calculations were conducted. The energetically favorable binding modes of the ligand to gold nanoparticle surfaces using the Gaussian program were studied. The DFT results showed kinetic stability of Au–3-TAA–Au interactions leading to inter-particle coupling or aggregation. Electrochemical analysis of the resultant nature of the capping agent revealed that 3-thiopheneacetic acid did not form a polymer during the preparation of Au–3-TAA. The cyclic voltammograms of Au–3-TAA nanoparticles coated glassy carbon electrode showed a typical gold character with the oxidation and reduction peaks at 1.4 V and 0.9 V, respectively.
- Full Text:
- Date Issued: 2012
- Authors: Sosibo, Ndabenhle M , Mdluli, Phumlane S , Mashazi, Philani N , Dyan, Busiswa , Revaprasadu, Neerish , Nyokong, Tebello , Tshikhudo, Robert T , Skepu, Amanda , Van Der Lingen, Elma
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/246446 , vital:51477 , xlink:href="https://doi.org/10.1016/j.molstruc.2011.09.057"
- Description: Gold nanoparticles capped with a bifunctional ligand, 3-thiopheneacetic acid (3-TAA) were synthesised by borohydride reduction at room temperature. The transmission electron microscopy (TEM) analysis showed that the particle aggregates and had semi-linear partial linkages that could be attributed to multi-modal binding of the ligand with various gold nanoparticles through the terminal thiolether (–S–) group and oxygen of the carboxylic (–COOH) group. This bimodal interaction led to limited stability of the resultant nanoparticles when tested using highly electrolytic media. To investigate further, density functional theory (DFT) quantum chemical and molecular dynamic calculations were conducted. The energetically favorable binding modes of the ligand to gold nanoparticle surfaces using the Gaussian program were studied. The DFT results showed kinetic stability of Au–3-TAA–Au interactions leading to inter-particle coupling or aggregation. Electrochemical analysis of the resultant nature of the capping agent revealed that 3-thiopheneacetic acid did not form a polymer during the preparation of Au–3-TAA. The cyclic voltammograms of Au–3-TAA nanoparticles coated glassy carbon electrode showed a typical gold character with the oxidation and reduction peaks at 1.4 V and 0.9 V, respectively.
- Full Text:
- Date Issued: 2012
Targeting conserved pathways as a strategy for novel drug development: disabling the cellular stress response:
- Edkins, Adrienne L, Blatch, Gregory L
- Authors: Edkins, Adrienne L , Blatch, Gregory L
- Date: 2012
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/165129 , vital:41211 , ISBN 978-3-642-28174-7 , DOI: 10.1007/978-3-642-28175-4_4
- Description: The ability to respond to and cope with stress at a molecular level is essential for cell survival. The stress response is conserved across organisms by the expression of a group of molecular chaperones known as heat shock proteins (HSP). HSP are ubiquitous and highly conserved proteins that regulate cellular protein homeostasis and trafficking under physiological and stressful conditions, including diseases such as cancer and malaria. HSP are good drug targets for the treatment of human diseases, as the significant functional and structural data available suggest that they are essential for cell survival and that, despite conservation across species, there are biophysical and biochemical differences between HSP in normal and disease states that allow HSP to be selectively targeted. In this chapter, we review the international status of this area of research and highlight progress by us and other African researchers towards the characterisation and targeting of HSP from humans and parasites from Plasmodium and Trypanosoma as drug targets.
- Full Text:
- Date Issued: 2012
- Authors: Edkins, Adrienne L , Blatch, Gregory L
- Date: 2012
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/165129 , vital:41211 , ISBN 978-3-642-28174-7 , DOI: 10.1007/978-3-642-28175-4_4
- Description: The ability to respond to and cope with stress at a molecular level is essential for cell survival. The stress response is conserved across organisms by the expression of a group of molecular chaperones known as heat shock proteins (HSP). HSP are ubiquitous and highly conserved proteins that regulate cellular protein homeostasis and trafficking under physiological and stressful conditions, including diseases such as cancer and malaria. HSP are good drug targets for the treatment of human diseases, as the significant functional and structural data available suggest that they are essential for cell survival and that, despite conservation across species, there are biophysical and biochemical differences between HSP in normal and disease states that allow HSP to be selectively targeted. In this chapter, we review the international status of this area of research and highlight progress by us and other African researchers towards the characterisation and targeting of HSP from humans and parasites from Plasmodium and Trypanosoma as drug targets.
- Full Text:
- Date Issued: 2012
Teacher education in post-apartheid South Africa: navigating a way through competing state and global imperatives for change
- Schäfer, Marc, Wilmot, P Dianne
- Authors: Schäfer, Marc , Wilmot, P Dianne
- Date: 2012
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/140905 , vital:37928 , DOI: 10.1007/s11125-012-9220-3
- Description: This article focuses on teacher education in post-apartheid South Africa. It argues that the restructuring and reorganization of teacher education is at the nexus of the axes of tension created by national and global imperatives for change. Along with the dismantling of apartheid and the transition to a free and democratic state in 1994 came the urgent need for social reconstruction, democratization, redress, social justice, and equity. At the same time, and as part of a global context, the country needed global competitiveness, human capital development, global skills, international standards, and accountability. These competing modernist discourses have informed the design and orientation of the National Qualifications Framework and national curriculum that took place in parallel with, and simultaneous to, the restructuring and reform of teacher education. This article reviews literature pertinent to understanding the post-apartheid transformation in South African education in general and teacher education in particular. It concludes that policy makers have managed to navigate a way through the axis of tension created by opposed orientations to transformation. A more equitable and improved system of teacher education has been achieved but critical issues of teacher quality and quantity have emerged which urgently need resolution.
- Full Text:
- Date Issued: 2012
- Authors: Schäfer, Marc , Wilmot, P Dianne
- Date: 2012
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/140905 , vital:37928 , DOI: 10.1007/s11125-012-9220-3
- Description: This article focuses on teacher education in post-apartheid South Africa. It argues that the restructuring and reorganization of teacher education is at the nexus of the axes of tension created by national and global imperatives for change. Along with the dismantling of apartheid and the transition to a free and democratic state in 1994 came the urgent need for social reconstruction, democratization, redress, social justice, and equity. At the same time, and as part of a global context, the country needed global competitiveness, human capital development, global skills, international standards, and accountability. These competing modernist discourses have informed the design and orientation of the National Qualifications Framework and national curriculum that took place in parallel with, and simultaneous to, the restructuring and reform of teacher education. This article reviews literature pertinent to understanding the post-apartheid transformation in South African education in general and teacher education in particular. It concludes that policy makers have managed to navigate a way through the axis of tension created by opposed orientations to transformation. A more equitable and improved system of teacher education has been achieved but critical issues of teacher quality and quantity have emerged which urgently need resolution.
- Full Text:
- Date Issued: 2012
Technauriture: Multimedia Research and Documentation of African Oral Performance
- Authors: Kaschula, Russell H
- Date: 2012
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/175223 , vital:42554 , ISBN 9783643901309
- Description: This paper seeks to assess the contribution of technology to the preservation and popularizing of oral performance in Southern Africa. An example will be provided which looks at the oral poetry, izibongo, produced by Xhosa oral poet Bongani Sitole (both in book and technological form). It will trace this poetry from the moment it was orally produced, through to the technologising and publication of this poetry in book form and on a website. A number of websites will also be analysed. The initial part of the paper provides a contextual analysis of selected poetry. This genre will also be compared (in terms of technological influence) with more contemporary Southern African performers such as the story-teller, Gcina Mhlophe as well as Lebo Mashile and Botsotso, spoken word artists and the oral poet Zolani Mkiva. The latter part of the article concentrates on issues related to technology and its relationship to the oral and written word.
- Full Text:
- Date Issued: 2012
- Authors: Kaschula, Russell H
- Date: 2012
- Language: English
- Type: text , book
- Identifier: http://hdl.handle.net/10962/175223 , vital:42554 , ISBN 9783643901309
- Description: This paper seeks to assess the contribution of technology to the preservation and popularizing of oral performance in Southern Africa. An example will be provided which looks at the oral poetry, izibongo, produced by Xhosa oral poet Bongani Sitole (both in book and technological form). It will trace this poetry from the moment it was orally produced, through to the technologising and publication of this poetry in book form and on a website. A number of websites will also be analysed. The initial part of the paper provides a contextual analysis of selected poetry. This genre will also be compared (in terms of technological influence) with more contemporary Southern African performers such as the story-teller, Gcina Mhlophe as well as Lebo Mashile and Botsotso, spoken word artists and the oral poet Zolani Mkiva. The latter part of the article concentrates on issues related to technology and its relationship to the oral and written word.
- Full Text:
- Date Issued: 2012
Tetra and octa (2, 6-di-iso-propylphenoxy)-substituted phthalocyanines
- Tuhl, Ahmad, Chidawanayika, Wadzanai, Ibrahim, Hamada Mohamed, Al-Awadi, Nouria, Litwinski, Christian, Nyokong, Tebello, Behbehani, Haider, Manaa, Hacene, Makhseed, Saad
- Authors: Tuhl, Ahmad , Chidawanayika, Wadzanai , Ibrahim, Hamada Mohamed , Al-Awadi, Nouria , Litwinski, Christian , Nyokong, Tebello , Behbehani, Haider , Manaa, Hacene , Makhseed, Saad
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/245855 , vital:51411 , xlink:href="https://doi.org/10.1142/S1088424612004495"
- Description: This work reports on the synthesis of novel metal free, zinc, aluminum, gallium and indium tetra and octa (2,6-di-iso-propylphenoxy)-substituted phthalocyanine derivatives. UV-visible and 1H NMR analyses confirm that a non-planar conformation, adapted by the phenoxy substituents due to steric interaction in both derivative series, perfectly discourage cofacial aggregation. Fluorescence quantum yields vary as a function of the number of substituents on the ring periphery, while the fluorescence lifetimes display no distinct trend. Triplet quantum yields are significantly larger for the tetra 2,6-di-iso-propylphenoxy- substituted derivatives relative to their corresponding octa-substituted species. However there was no overall trend in the triplet lifetime values. For almost all of the phthalocyanine derivatives, singlet oxygen was produced with relatively good quantum yields. This study explores the possibility of fine-tuning their physicochemical properties by simple structural modification.
- Full Text:
- Date Issued: 2012
- Authors: Tuhl, Ahmad , Chidawanayika, Wadzanai , Ibrahim, Hamada Mohamed , Al-Awadi, Nouria , Litwinski, Christian , Nyokong, Tebello , Behbehani, Haider , Manaa, Hacene , Makhseed, Saad
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/245855 , vital:51411 , xlink:href="https://doi.org/10.1142/S1088424612004495"
- Description: This work reports on the synthesis of novel metal free, zinc, aluminum, gallium and indium tetra and octa (2,6-di-iso-propylphenoxy)-substituted phthalocyanine derivatives. UV-visible and 1H NMR analyses confirm that a non-planar conformation, adapted by the phenoxy substituents due to steric interaction in both derivative series, perfectly discourage cofacial aggregation. Fluorescence quantum yields vary as a function of the number of substituents on the ring periphery, while the fluorescence lifetimes display no distinct trend. Triplet quantum yields are significantly larger for the tetra 2,6-di-iso-propylphenoxy- substituted derivatives relative to their corresponding octa-substituted species. However there was no overall trend in the triplet lifetime values. For almost all of the phthalocyanine derivatives, singlet oxygen was produced with relatively good quantum yields. This study explores the possibility of fine-tuning their physicochemical properties by simple structural modification.
- Full Text:
- Date Issued: 2012
The art of dying
- Authors: Jones, Ward E
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/275722 , vital:55073 , xlink:href="https://doi.org/10.1080/05568641.2012.743217"
- Description: In this paper, I explore what Jean Améry calls the ‘aesthetic view of death’. I address the following three questions. To what extent, and how, do we take an aesthetic view of death? Why do we take an aesthetic view of death? Third, for those whose deaths are impending and have some choice over how they die—most prominently the elderly and the terminally ill—what would it mean for them to take an aesthetic view of their own impending deaths, and, in particular, what would it mean for them to act in the light of such a view?
- Full Text:
- Date Issued: 2012
- Authors: Jones, Ward E
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/275722 , vital:55073 , xlink:href="https://doi.org/10.1080/05568641.2012.743217"
- Description: In this paper, I explore what Jean Améry calls the ‘aesthetic view of death’. I address the following three questions. To what extent, and how, do we take an aesthetic view of death? Why do we take an aesthetic view of death? Third, for those whose deaths are impending and have some choice over how they die—most prominently the elderly and the terminally ill—what would it mean for them to take an aesthetic view of their own impending deaths, and, in particular, what would it mean for them to act in the light of such a view?
- Full Text:
- Date Issued: 2012
The design, synthesis and antiplasmodial activity of a series of halogenated fosmidomycin analogues and hybrid drugs
- Authors: Afolayan, Anthonia Folake
- Date: 2012
- Subjects: Uncatalogued
- Language: English
- Type: text , Thesis , Doctoral , PhD
- Identifier: http://hdl.handle.net/10962/64370 , vital:28538
- Description: Malaria continues to be a devastating disease and a major cause of death in sub-Saharan Africa. With resistance against most of the available antimalarial drugs, there is a need for ongoing research and development of antimalarial agents. Fosmidomycin and its acetyl analogue FR900098 have been identified as potent inhibitors of Plasmodium falciparum, the causative agent of the most deadly form of malaria. Clinical trials of these agents have revealed poor absorption due to their high hydrophilicity. In the present studies the effect of halogenation of the acyl chain as well as the biological effect of extending the acyl sidechain was explored. This provided the basis on which fosmidomycin hybrids were designed to investigate the feasibility of hybrid extending into NADPH binding pocket. Synthesis of a series of halogenated FR900098 analogues was carried out in three stages. This included i) The introduction of the phosphonate group by reaction with 1,3dibromopropane in an Arbuzov reaction, ii) The introduction of a hydroxamate group by reaction of the propyl phosphonate by means of a nucleophilic substitution reaction with BocNHOBn and iii) The introduction of a halogenated acyl side chain on a protected fosmidomycin backbone. The synthesis of fosmidomycin-hybrids for which chloroquinefosmidomycin hybrids were used as the prototype, involved convergence of the two separately constructed moieties i.e. fosmidomycin and the quinoline moieties in a covalent linkage. The quinoline moiety was easily synthesized from the reaction of 4,7dichloroquinoline with 1,2-diamino ethane. The aminoquinoline so formed resulted in chloroquine-fosmidomycin hybrids 3.8 and 3.9 when reacted with halogenated FR900098 analogues. Antiplasmodial assays were conducted on the chloroquine-fosmidomycin hybrids and the halogenated fosmidomycin derivatives against the chloroquine resistant Gambian FCR-3 strain of P. falciparum. The most potent iodoacetyl fosmidomycin analogues 2.21 gave an IC50 value of 5.54 µM which is eight times more potent than the known antiplasmodial FR900098 which gave an IC50 value of 41.67 µM. All the halogenated FR900098 analogues showed better antiplasmodial activity than their non-halogenated derivatives. This indicated that the presence of halogens in the FR900098 analogues contributes to their biological Chapter 1 Literature review activity. The acetyl and propyl linked hybrids 3.8 and 3.9 showed potent antiplasmodial activity with IC50 values of 0.18 and 0.82 µM respectively. These were by far the most potent hybrids synthesized and provided leads for a new class of promising antimalarial agents. Preliminary E. coli DXR enzyme inhibition assays were carried out on the halogenated fosmidomycin analogues. The results showed good inhibition of the enzyme by the phosphonic acids of the chloroacetyl and chloropropyl analogues 2.1 and 2.2 respectively. Molecular modelling of the compounds on E. coli (PDB code: 2EGH) and P. falciparum (PDB code: 3AUA) DXR showed strong binding of the halogenated fosmidomycin analogues while the hybrids in the absence of docked NADPH showed minimum binding to the enzymes.
- Full Text:
- Date Issued: 2012
- Authors: Afolayan, Anthonia Folake
- Date: 2012
- Subjects: Uncatalogued
- Language: English
- Type: text , Thesis , Doctoral , PhD
- Identifier: http://hdl.handle.net/10962/64370 , vital:28538
- Description: Malaria continues to be a devastating disease and a major cause of death in sub-Saharan Africa. With resistance against most of the available antimalarial drugs, there is a need for ongoing research and development of antimalarial agents. Fosmidomycin and its acetyl analogue FR900098 have been identified as potent inhibitors of Plasmodium falciparum, the causative agent of the most deadly form of malaria. Clinical trials of these agents have revealed poor absorption due to their high hydrophilicity. In the present studies the effect of halogenation of the acyl chain as well as the biological effect of extending the acyl sidechain was explored. This provided the basis on which fosmidomycin hybrids were designed to investigate the feasibility of hybrid extending into NADPH binding pocket. Synthesis of a series of halogenated FR900098 analogues was carried out in three stages. This included i) The introduction of the phosphonate group by reaction with 1,3dibromopropane in an Arbuzov reaction, ii) The introduction of a hydroxamate group by reaction of the propyl phosphonate by means of a nucleophilic substitution reaction with BocNHOBn and iii) The introduction of a halogenated acyl side chain on a protected fosmidomycin backbone. The synthesis of fosmidomycin-hybrids for which chloroquinefosmidomycin hybrids were used as the prototype, involved convergence of the two separately constructed moieties i.e. fosmidomycin and the quinoline moieties in a covalent linkage. The quinoline moiety was easily synthesized from the reaction of 4,7dichloroquinoline with 1,2-diamino ethane. The aminoquinoline so formed resulted in chloroquine-fosmidomycin hybrids 3.8 and 3.9 when reacted with halogenated FR900098 analogues. Antiplasmodial assays were conducted on the chloroquine-fosmidomycin hybrids and the halogenated fosmidomycin derivatives against the chloroquine resistant Gambian FCR-3 strain of P. falciparum. The most potent iodoacetyl fosmidomycin analogues 2.21 gave an IC50 value of 5.54 µM which is eight times more potent than the known antiplasmodial FR900098 which gave an IC50 value of 41.67 µM. All the halogenated FR900098 analogues showed better antiplasmodial activity than their non-halogenated derivatives. This indicated that the presence of halogens in the FR900098 analogues contributes to their biological Chapter 1 Literature review activity. The acetyl and propyl linked hybrids 3.8 and 3.9 showed potent antiplasmodial activity with IC50 values of 0.18 and 0.82 µM respectively. These were by far the most potent hybrids synthesized and provided leads for a new class of promising antimalarial agents. Preliminary E. coli DXR enzyme inhibition assays were carried out on the halogenated fosmidomycin analogues. The results showed good inhibition of the enzyme by the phosphonic acids of the chloroacetyl and chloropropyl analogues 2.1 and 2.2 respectively. Molecular modelling of the compounds on E. coli (PDB code: 2EGH) and P. falciparum (PDB code: 3AUA) DXR showed strong binding of the halogenated fosmidomycin analogues while the hybrids in the absence of docked NADPH showed minimum binding to the enzymes.
- Full Text:
- Date Issued: 2012
The direct use value of municipal commonage goods and services to urban households in the Eastern Cape, South Africa
- Davenport, Nicholas A, Shackleton, Charlie M, Gambiza, James
- Authors: Davenport, Nicholas A , Shackleton, Charlie M , Gambiza, James
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/181071 , vital:43696 , xlink:href="https://doi.org/10.1016/j.landusepol.2011.09.008"
- Description: To redress past racial discrepancies in ownership and tenure, the ANC government of South Africa initiated programmes to make land accessible to the previously disadvantaged. A key component of the national land reform programme was the provision of commonage lands to urban municipalities for use by the urban poor. However, there has been no assessment of the contribution that urban commonage makes to previously disadvantaged households. This study assessed the economic benefits of the commonage programme to local households, through an in-depth survey of 90 households across three small towns in the Eastern Cape of South Africa. We examined the marketed and non-marketed consumptive direct-use values of land-based livelihoods on commonage, calculated via the ‘own reported values’ approach. The results indicate that a proportion of South Africa's urban population rely to some degree on municipal commonage for part of their livelihoods. Commonage contributions to total livelihood incomes ranged between 14 and 20%. If the contributions from commonage were excluded, the incomes of over 10% of households in each study town would drop below the poverty line. Overall, the value of harvests from commonage was worth over R1 000 (US$ 142) per hectare per year and over R4.7 million (US$ 0.68 million) per commonage per year. However, the extent and nature of use and reliance was not uniform among households, so that we developed a typology of commonage users, with four types being identified. However, rapidly growing urban populations and high levels of poverty potentially threaten the sustainability of commonage resource use. Yet the national land reform programme focuses largely on the transfer of land to municipalities and not on sustainable management. Municipalities, in turn, invest relatively little in commonage management, and the little they do is focussed on livestock production. Non-timber forest products are not considered at all, even though this study shows that they are a vital resource for the urban poor, notably for energy and construction materials.
- Full Text:
- Date Issued: 2012
- Authors: Davenport, Nicholas A , Shackleton, Charlie M , Gambiza, James
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/181071 , vital:43696 , xlink:href="https://doi.org/10.1016/j.landusepol.2011.09.008"
- Description: To redress past racial discrepancies in ownership and tenure, the ANC government of South Africa initiated programmes to make land accessible to the previously disadvantaged. A key component of the national land reform programme was the provision of commonage lands to urban municipalities for use by the urban poor. However, there has been no assessment of the contribution that urban commonage makes to previously disadvantaged households. This study assessed the economic benefits of the commonage programme to local households, through an in-depth survey of 90 households across three small towns in the Eastern Cape of South Africa. We examined the marketed and non-marketed consumptive direct-use values of land-based livelihoods on commonage, calculated via the ‘own reported values’ approach. The results indicate that a proportion of South Africa's urban population rely to some degree on municipal commonage for part of their livelihoods. Commonage contributions to total livelihood incomes ranged between 14 and 20%. If the contributions from commonage were excluded, the incomes of over 10% of households in each study town would drop below the poverty line. Overall, the value of harvests from commonage was worth over R1 000 (US$ 142) per hectare per year and over R4.7 million (US$ 0.68 million) per commonage per year. However, the extent and nature of use and reliance was not uniform among households, so that we developed a typology of commonage users, with four types being identified. However, rapidly growing urban populations and high levels of poverty potentially threaten the sustainability of commonage resource use. Yet the national land reform programme focuses largely on the transfer of land to municipalities and not on sustainable management. Municipalities, in turn, invest relatively little in commonage management, and the little they do is focussed on livestock production. Non-timber forest products are not considered at all, even though this study shows that they are a vital resource for the urban poor, notably for energy and construction materials.
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- Date Issued: 2012