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The HIV-1 entry inhibition capabilities of Isoflavones
Dissertation (MSc (Biochemistry))--University of Pretoria, 2023.
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| Format: | Thesis |
| Language: | English |
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University of Pretoria
2023
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| _version_ | 1867613449212657664 |
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| access_status_str | Open Access |
| author2 | Gama, Ntombenhle Hlengiwe |
| author_browse | Gama, Ntombenhle Hlengiwe |
| author_facet | Gama, Ntombenhle Hlengiwe |
| collection | Thesis |
| dc_rights_str_mv | © 2023 University of Pretoria. All rights reserved. The copyright in this work vests in the University of Pretoria. No part of this work may be reproduced or transmitted in any form or by any means, without the prior written permission of the University of Pretoria. |
| description | Dissertation (MSc (Biochemistry))--University of Pretoria, 2023. |
| format | Thesis |
| id | oai:repository.up.ac.za:2263/93769 |
| institution | University of Pretoria (South Africa) |
| language | English |
| last_indexed | 2026-06-10T12:36:19.431Z |
| license_str | Other — see source repository |
| provenance_str_mv | Harvested via OAI-PMH from UPSpace — University of Pretoria Institutional Repository |
| publishDate | 2023 |
| publishDateRange | 2023 |
| publishDateSort | 2023 |
| publisher | University of Pretoria |
| publisherStr | University of Pretoria |
| record_format | dspace |
| source_str | UPSpace — University of Pretoria Institutional Repository |
| spelling | oai:repository.up.ac.za:2263/93769 The HIV-1 entry inhibition capabilities of Isoflavones Gama, Ntombenhle Hlengiwe stevengregoryr@gmail.com Raubenheimer, Steven UCTD Biochemistry Human immunodeficiency virus (HIV) Drug discovery Entry inhibitors Drug design Isoflavones Flavonoids Gp120 Sustainable development goals (SDGs) SDG-03: Good health and well-being Natural and agricultural sciences theses SDG-03 Dissertation (MSc (Biochemistry))--University of Pretoria, 2023. The availability of treatment for HIV infection has resulted in a drastic increase in the life expectancy of infected individuals. However, the current therapeutics fall short in many areas. A considerable 60% of treated individuals will show minor cognitive disorders due to infection, immune reconstruction inflammatory syndrome occurs in a high number of individuals of African descent as a treatment side-effect, and treatment resistance occurs commonly both with long-term infected individuals and newly infected individuals. This all highlights the need for continued research into combating the HIV pandemic. This research investigated the anti-HIV activity of five novel Isoflavones. Isoflavones and similar compounds have been extensively researched for their ability to hinder HIV reproduction through multiple routes of antagonism in the HIV life cycle but with little research in HIV entry inhibition. In this study, the anti-HIV activity of the isoflavones was quantified through the generation of IC50 values using a luciferase reporter assay. Evidence for potential entry-inhibiting activity was generated through time-of-addition studies and the potential drug targets were hypothesised using computational docking studies. All the Isoflavones were shown to inhibit HIV replication in the lower micromolar regions with IC50 values ranging from 6.2 to 10.6 μM. Two of the isoflavones, B and C, were shown to possess significant entry inhibitory activity of HIV-1 through time-of-addition studies (0.041 and 0.007, respectively ). Docking studies illustrate the potential for these compounds to act through gp120 antagonism and provide the framework for future drug development using these compounds as gp120 anchoring regions. NRF Thuthuka Grant. Biochemistry MSc (Biochemistry) Unrestricted Faculty of Natural and Agricultural Sciences 2023-12-07T08:53:37Z 2023-12-07T08:53:37Z 2024-04 2023 Dissertation * A2024 http://hdl.handle.net/2263/93769 DOI: https://doi.org/10.25403/UPresearchdata.24650211.v1 https://doi.org/10.25403/UPresearchdata.24650211 en © 2023 University of Pretoria. All rights reserved. The copyright in this work vests in the University of Pretoria. No part of this work may be reproduced or transmitted in any form or by any means, without the prior written permission of the University of Pretoria. application/pdf University of Pretoria |
| spellingShingle | UCTD Biochemistry Human immunodeficiency virus (HIV) Drug discovery Entry inhibitors Drug design Isoflavones Flavonoids Gp120 Sustainable development goals (SDGs) SDG-03: Good health and well-being Natural and agricultural sciences theses SDG-03 The HIV-1 entry inhibition capabilities of Isoflavones |
| title | The HIV-1 entry inhibition capabilities of Isoflavones |
| title_full | The HIV-1 entry inhibition capabilities of Isoflavones |
| title_fullStr | The HIV-1 entry inhibition capabilities of Isoflavones |
| title_full_unstemmed | The HIV-1 entry inhibition capabilities of Isoflavones |
| title_short | The HIV-1 entry inhibition capabilities of Isoflavones |
| title_sort | hiv 1 entry inhibition capabilities of isoflavones |
| topic | UCTD Biochemistry Human immunodeficiency virus (HIV) Drug discovery Entry inhibitors Drug design Isoflavones Flavonoids Gp120 Sustainable development goals (SDGs) SDG-03: Good health and well-being Natural and agricultural sciences theses SDG-03 |
| url | http://hdl.handle.net/2263/93769 https://doi.org/10.25403/UPresearchdata.24650211 |