Developing of anti-HIV agents from natural resources(Chemical & Pharmacological study)
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概要
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Most drugs clinically used to suppress replication of HIV, the virus that causes AIDS, are nucleosides and their analogs, but their use is limited due to their severe toxicity, emerging drug resistance and cost. These challenges prompt the search for new anti-HIV-1 agents that are affordable for resource-poor countries and have fewer side effects. As an approach, traditional medicines from different places of the world were evaluated with a panel of in vitro bioassays [designed to monitor inhibition of HIV-1-induced cytopathic effect (CPE), and HIV essential enzymes; reverse transcriptase (RT), protease (PR), and integrase (IN)], and active leads were then isolated and identified. In this review, structurally diverse compounds that have potent anti-HIV activity were classified to CPE inhibitors (phorbol diterpenes), RT inhibitors (caffeic acid derivatives and polyphenols), PR-inhibitors (derivatives of oleanane, ursane and lupane type triterpenes). Other compounds included are IN inhibitors. Structural modification of the active compounds and conjugation with synthesized anti-HIV agents were carried out, which, hopefully, could help for developing novel and effective anti-HIV agents.
- 和漢医薬学会の論文
- 2005-00-00
和漢医薬学会 | 論文
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