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Isolation and characterisation of the active phyto-pharmaceutical ingredient from Lobostemon trigonus for use in the development of a microbicide

The HIV-1 pandemic affects millions of people worldwide with approximately 70% of those affected residing in sub-Saharan Africa (SSA) relying on traditional medicines for treatment. The key aim of the study was to isolate and characterise an active phyto-pharmaceutical ingredient (API) from L. trigonus for use as a vaginal microbicide.
The aerial parts of L. trigonus were oven-dried at 80°C, ground and then extracted with boiling water for 30 minutes. Aqueous extracts were screened using an HIV-1 neutralization assay in TZM bl cells. Chromatographic and spectroscopic techniques were used to purify, isolate and identify the API.
The API (BP36-117-26464C) was identified as a polymeric macromolecule with IC50 = 0.04 μg/ml against HIV-1 HXB 2 subtype B. This activity is comparable to the ARV drug, enfuvirtide (IC50 = 0.02 μg/ml). The API consists of galacturonic acid polymer and a mixture of seven compounds. Its mode of action may involve inhibiting virus attachment.
The activity of this precipitate (BP36-117-26464C) tested against HIV-1 subtype C pseudovirions and shown to compare favorably with that of enfuvirtide (T20). The water-soluble nature of this API and its mode of action identified it as a potential microbicide. In the current form, the precipitate (API) would be difficult to develop as an oral treatment for HIV, as high-molecular weight agents often have poor bioavailability following oral administration. However, large molecules with potent anti-HIV activity are ideal for topical use and potent development as a microbicide. / Life and Consumer Sciences / M.Sc (Life Sciences)

Identiferoai:union.ndltd.org:netd.ac.za/oai:union.ndltd.org:unisa/oai:uir.unisa.ac.za:10500/19567
Date01 1900
CreatorsMbobela, Phindiwe Felicia
ContributorsDewar, John, Kenyon, Colin, Pillay, Pamisha
Source SetsSouth African National ETD Portal
LanguageEnglish
Detected LanguageEnglish
TypeDissertation
Format1 online resource (xix, 110 leaves), illustrations (some color)

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