水黄皮种子中查尔酮对HIV p24和逆转录酶的结合特性

Binding property of HIV p24 and Reverse transcriptase by chalcones from Pongamia pinnata seeds.

作者信息

Mathaiyan Manikannan, Suresh Arumugam, Balamurugan Rangasamy

机构信息

Centre for Drug Discovery and Development, Sathyabama Institute of Science and Technology, Chennai-600 119.

Central Research Laboratory, Sri Manakula Vinayagar Medical College & Hospital, Madagadipet, Puducherry- 605107.

出版信息

Bioinformation. 2018 Jun 30;14(6):279-284. doi: 10.6026/97320630014279. eCollection 2018.

DOI:10.6026/97320630014279

PMID:30237673

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6137571/

Abstract

HIV remains a challenging life threatening viral agent for humans despite available anti HIV drugs. The known effective drug named HAART clears the circulating viruses but not the intracellular viruses. Therefore, it is of interest to identify molecules with improved anti-HIV activity from natural plant sources. Hence, we studied the anti-HIV potency of an Indian medicinal plant named Pongamia pinnata. Aqueous extracts were made from leaf, seed and roots of Pongmia pinnata and screened for anti HIV-1 activity using HIV-1 p24 and reverse transcriptase (RT) inhibition assays. Further, the active chalcone derivatives namely, P24 protein and RT enzymes showed promising binding score against Glabarachalcone and Karanijin. Among these extracts, P. pinnta aqueous seed extracts have shown HIV-1 p24 inhibition at 66.9 ± 4.4 percentage. However, RT inhibition assay showed only 36.8%. Hence, the HIV-1 p24 inhibition infers either the prevention of virus entry or inhibits other enzymes and or interferes with virion assembly.

摘要

尽管有抗艾滋病毒药物，但艾滋病毒对人类来说仍然是一种具有挑战性的、危及生命的病毒制剂。已知的有效药物高效抗逆转录病毒疗法（HAART）能清除循环中的病毒，但不能清除细胞内的病毒。因此，从天然植物来源中鉴定出具有更强抗艾滋病毒活性的分子具有重要意义。于是，我们研究了一种名为印度水黄皮的印度药用植物的抗艾滋病毒效力。从印度水黄皮的叶、种子和根中制备了水提取物，并使用艾滋病毒-1 p24和逆转录酶（RT）抑制试验筛选其抗艾滋病毒-1活性。此外，活性查尔酮衍生物，即P24蛋白和RT酶，对格拉巴查尔酮和卡拉尼金显示出有前景的结合分数。在这些提取物中，印度水黄皮种子水提取物对艾滋病毒-1 p24的抑制率为66.9±4.4%。然而，RT抑制试验仅显示36.8%。因此，艾滋病毒-1 p24抑制可能意味着预防病毒进入或抑制其他酶和/或干扰病毒体组装。