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抗 HIV 天然产物的构效关系及作用机制研究进展。

Structure-Activity-Relationship and Mechanistic Insights for Anti-HIV Natural Products.

机构信息

Sri Sai College of Pharmacy, Manawala, Amritsar 143001, India.

Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, India.

出版信息

Molecules. 2020 Apr 29;25(9):2070. doi: 10.3390/molecules25092070.

DOI:10.3390/molecules25092070
PMID:32365518
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7249135/
Abstract

Acquired Immunodeficiency Syndrome (AIDS), which chiefly originatesfroma retrovirus named Human Immunodeficiency Virus (HIV), has impacted about 70 million people worldwide. Even though several advances have been made in the field of antiretroviral combination therapy, HIV is still responsible for a considerable number of deaths in Africa. The current antiretroviral therapies have achieved success in providing instant HIV suppression but with countless undesirable adverse effects. Presently, the biodiversity of the plant kingdom is being explored by several researchers for the discovery of potent anti-HIV drugs with different mechanisms of action. The primary challenge is to afford a treatment that is free from any sort of risk of drug resistance and serious side effects. Hence, there is a strong demand to evaluate drugs derived from plants as well as their derivatives. Several plants, such as , , , , , and others have displayed significant anti-HIV activity. Here, weattempt to summarize the main results, which focus on the structures of most potent plant-based natural products having anti-HIV activity along with their mechanisms of action and IC values, structure-activity-relationships and important key findings.

摘要

获得性免疫缺陷综合征(AIDS)主要源自一种名为人类免疫缺陷病毒(HIV)的逆转录病毒,已在全球范围内影响了约 7000 万人。尽管在抗逆转录病毒联合疗法领域取得了一些进展,但 HIV 仍然是非洲大量死亡的罪魁祸首。目前的抗逆转录病毒疗法在提供即时 HIV 抑制方面取得了成功,但也带来了无数不良的副作用。目前,许多研究人员正在探索植物王国的生物多样性,以发现具有不同作用机制的强效抗 HIV 药物。主要的挑战是提供一种没有任何耐药风险和严重副作用的治疗方法。因此,需要评估植物来源的药物及其衍生物。一些植物,如 、 、 、 、 等,已经显示出显著的抗 HIV 活性。在这里,我们试图总结主要的结果,重点是具有抗 HIV 活性的最有效植物天然产物的结构及其作用机制和 IC 值、构效关系和重要关键发现。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/4ef2b50ae9b0/molecules-25-02070-g018.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/43ad6f3b960a/molecules-25-02070-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/2964c626c302/molecules-25-02070-g007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/0581b90b28bf/molecules-25-02070-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/f705f001a69e/molecules-25-02070-g010.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/d475b5d0afcd/molecules-25-02070-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/67b6f40b1874/molecules-25-02070-g017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/4ef2b50ae9b0/molecules-25-02070-g018.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/43ad6f3b960a/molecules-25-02070-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/6aeb752bca6c/molecules-25-02070-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/c80f1f1694c2/molecules-25-02070-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/b4e8b348c741/molecules-25-02070-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/5cfa6118b6b4/molecules-25-02070-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/3030ba9b0d9c/molecules-25-02070-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/2964c626c302/molecules-25-02070-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/8e9457d51a73/molecules-25-02070-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/0581b90b28bf/molecules-25-02070-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/f705f001a69e/molecules-25-02070-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/2b45eb0698be/molecules-25-02070-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/295ae2866401/molecules-25-02070-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/f537409caa08/molecules-25-02070-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/75fab302620f/molecules-25-02070-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/c20166542e95/molecules-25-02070-g015.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/d475b5d0afcd/molecules-25-02070-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/67b6f40b1874/molecules-25-02070-g017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a2f/7249135/4ef2b50ae9b0/molecules-25-02070-g018.jpg

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