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从[植物名称未给出]中鉴定出的植物成分作为与感染性心内膜炎相关的HIV-1逆转录酶的潜在治疗剂:[研究方法未给出]和[研究方法未给出]方法。

Identification of phytoconstituents from as potential therapeutics against HIV-1 reverse transcriptase associated with infective endocarditis: and approaches.

作者信息

Al-Masri Abeer A

机构信息

Department of Physiology, College of Medicine, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

Saudi J Biol Sci. 2023 Sep;30(9):103751. doi: 10.1016/j.sjbs.2023.103751. Epub 2023 Jul 28.

Abstract

Acquired immune deficiency syndrome (AIDS) is an unadorned disease affected the human immunodeficiency virus (HIV), which has become the most infectious diseases worldwide. HIV-1 RT has been shown to be present in the cardiac tissue of patients with HIV-associated infective endocarditis, and to be associated with the development of valvular lesions and other cardiac abnormalities. The use of anti-retroviral therapies has helped to control the virus and reduce the incidence of HIV-1 associated infective endocarditis. Though, these treatments have several adjacent effects, and the improvement of drug-resistant stresses of the virus has become a significant challenge in HIV treatment. This study is to identify phytoconstituents with HIV-1 RT inhibitory activity for potential therapeutic use against HIV-1 RT associated with infective endocarditis. We performed and screening of natural cardiovascular phytoconstituents from , a medicinal plant that has been traditionally used for the management of numerous diseases. The results showed that all three compounds (geraldone, luteolin, and isookanin) exhibited affinities of solid binidng to the active amino acids of HIV-1 RT's DNA-polymerase (DNA-p) and Ribonuclease-H (RNA-H) active positions, suggesting their potential as HIV-1 RT inhibitors. assessment of the three compounds at a concentration of 1 mg/mL revealed that Geraldone exhibited the most effective inhibitory consequence on HIV-1 RT activity (83.45%), followed by Isookanin (75.88%) and Luteolin (66.36%). These findings suggest that these compounds have the potential to inhibit HIV-1 RT associated with infective endocarditis and could assist as main compounds for emerging unique anti-HIV-1 agents. Further studies are needed to confirm the and efficacy of these molecules and assess their safety and efficiency as anti-HIV-1 drugs.

摘要

获得性免疫缺陷综合征(艾滋病)是一种由人类免疫缺陷病毒(HIV)感染引起的疾病,它已成为全球最具传染性的疾病。已证明HIV-1逆转录酶存在于HIV相关感染性心内膜炎患者的心脏组织中,并与瓣膜病变和其他心脏异常的发生有关。抗逆转录病毒疗法的使用有助于控制病毒并降低HIV-1相关感染性心内膜炎的发病率。然而,这些治疗有一些副作用,并且病毒耐药性的提高已成为HIV治疗中的一项重大挑战。本研究旨在鉴定具有HIV-1逆转录酶抑制活性的植物成分,以用于针对与感染性心内膜炎相关的HIV-1逆转录酶的潜在治疗用途。我们对一种传统上用于治疗多种疾病的药用植物——[植物名称未给出]中的天然心血管植物成分进行了筛选。结果表明,所有三种化合物(杰拉尔多酮、木犀草素和异奥卡宁)对HIV-1逆转录酶的DNA聚合酶(DNA-p)和核糖核酸酶H(RNA-H)活性位点的活性氨基酸都表现出紧密结合的亲和力,表明它们具有作为HIV-1逆转录酶抑制剂的潜力。在浓度为1mg/mL时对这三种化合物的评估显示,杰拉尔多酮对HIV-1逆转录酶活性表现出最有效的抑制作用(83.45%),其次是异奥卡宁(75.88%)和木犀草素(66.36%)。这些发现表明,这些化合物有可能抑制与感染性心内膜炎相关的HIV-1逆转录酶,并可作为新型独特抗HIV-1药物的主要成分。需要进一步研究来证实这些分子的体外和体内疗效,并评估它们作为抗HIV-1药物的安全性和有效性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6615/10428122/ddd7b3bbdba1/gr1.jpg

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