- Title
- Isolation of bioactive metabolites with activity against HIV-1 target proteins from extracts of Sutherlandia frutescens and Lobostemon trigonus
- Creator
- Dambuza, Ntokozo Shirley
- Subject
- Medicinal plants -- Africa, Southern
- Subject
- HIV infections -- Alternative treatment -- Africa, Southern
- Subject
- Plant bioactive compounds
- Date Issued
- 2007
- Date
- 2007
- Type
- Thesis
- Type
- Masters
- Type
- MSc
- Identifier
- vital:10335
- Identifier
- http://hdl.handle.net/10948/492
- Identifier
- http://hdl.handle.net/10948/d1012003
- Identifier
- Medicinal plants -- Africa, Southern
- Identifier
- HIV infections -- Alternative treatment -- Africa, Southern
- Identifier
- Plant bioactive compounds
- Description
- Acquired Immunodeficiency Syndrome (AIDS) is a human disease caused by the human immunodeficiency virus type 1 (HIV-1) and it is one of the biggest social, economic and health challenges in the world. The Joint United Nations Programme on HIV/AIDS (UNAIDS) and World Health Organization (WHO) estimated that between 33.4 to 46.0 million people around the world were living with HIV/AIDS in December 2005 and the highest estimates are in the Sub-Saharan Africa (around 25 million). In more developed countries a combined antiretroviral therapy called highly active antiretroviral therapy (HAART) is used, which results in reduced progression to AIDS in most patients. Despite the beneficial effects of HAART, significant side effects are experienced by treated patients. In addition, most infected people live in countries where the treatment is very expensive or, in many cases, not available at all. These people therefore rely on medicinal plants for health care. In this study, aqueous extracts from Sutherlandia frutescens and Lobostemon trigonus were screened for potential anti-HIV activities in a series of in vitro enzymatic assays, including reverse transcriptase, HIV-1 protease and glycohydrolases. Two extracts of Sutherlandia leaves (SFL-1 and SFL-2) were prepared that inhibited HIV reverse transcriptase and a Lobostemon leaf extract (LTL) was shown to also inhibit this enzyme. All extracts were assayed at 1.25mg/ml. Tannin content was determined for all active extracts using a tannic acid assay. SFL-1 and SFL-2 were found to contain about 6 percent and 7 percent tannins, respectively, and LTL contained 31% tannins by weight. Tannins were removed using polyamide columns and three fractions were collected for each. The extracts were also fractionated with Sephadex G-25, Amberlite IR 120 and Dowex 1-X8 as size exclusion, cation exchange and anion exchange, respectively. Extracts were also fractionated by preparative thin layer chromatography where two compounds were separated from S. frutescens extract with high activity against reverse transcriptase while showing insignificant inhibition towards other enzymes tested. SFL-BFW-10 and SFL-WEF-7 inhibited reverse transcriptase by almost 100 percent and the IC50 values calculated for these compounds were 0.34 and 0.23mg/ml, respectively. Cytotoxicity of these compounds was evaluated on Chang liver cells and peripheral blood mononuclear cells (PBMCs). None of these compounds showed any significant inhibition of cell proliferation. The purity of these compounds could not be confirmed because there was insufficient material to use in the techniques required to show purity and identification. Therefore, TLC was used to determine the nature of these compounds. SFL-BFW-10 was identified as an organic acid and SFL-WEF-7 was identified as flavonoid.
- Format
- xii, 124 leaves
- Format
- Publisher
- Nelson Mandela Metropolitan University
- Publisher
- Faculty of Science
- Language
- English
- Rights
- Nelson Mandela Metropolitan University
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NMMU School of BioMolecular and Chemical Sciences
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