Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham.

Q1 Pharmacology, Toxicology and Pharmaceutics Advances in Pharmacological Sciences Pub Date : 2019-06-02 eCollection Date: 2019-01-01 DOI:10.1155/2019/2573965

Prapaporn Chaniad, Teeratad Sudsai, Abdi Wira Septama, Arnon Chukaew, Supinya Tewtrakul

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引用次数: 13

Abstract

Betula alnoides is a medicinal plant in Thai traditional longevity preparations. The crude extracts of this plant possess various biological activities. However, the isolated compounds from this plant have no reports of anti-HIV-1 integrase (IN) activity. Therefore, the present study aims to investigate the anti-HIV-1 integrase and anti-inflammatory effects of isolated compounds from this plant and predict the interaction of compounds with integrase active sites. From the bioassay-guided fractionation of the ethanol extract of B. alnoides stems using chromatographic techniques, five pentacyclic triterpenoid compounds were obtained. They are betulinic acid (1), betulin (2), lupeol (3), oleanolic acid (4), and ursolic acid (5). Compound 2 exhibited the most potent inhibitory activity against HIV-1 IN, with an IC₅₀ value of 17.7 μM. Potential interactions of compounds with IN active sites were investigated using computational docking. The results indicated that active compounds interacted with Asp64, a residue participating in 3'-processing, and Thr66, His67, and Lys159, residues participating in strand-transfer reactions of the integration process. Regarding anti-inflammatory activity, all compounds exerted significant inhibitory effects on LPS-induced nitric oxide production (IC₅₀ < 68.7 μM). Thus, this research provides additional scientific support for the use of B. alnoides in traditional medicine for the treatment of HIV patients.

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白桦抗hiv -1整合酶及抗炎活性评价

白桦是泰国传统长寿制剂中的药用植物。这种植物的粗提物具有多种生物活性。然而，从这种植物中分离的化合物没有抗hiv -1整合酶(IN)活性的报道。因此，本研究旨在研究从该植物中分离的化合物的抗hiv -1整合酶和抗炎作用，并预测化合物与整合酶活性位点的相互作用。利用色谱技术对苦参茎乙醇提取物进行生物测定分离，得到5个五环三萜化合物。它们分别是白桦酸(1)、白桦素(2)、鹿皮醇(3)、齐墩果酸(4)和熊果酸(5)。化合物2对HIV-1 IN的抑制活性最强，IC50值为17.7 μM。利用计算对接的方法研究了化合物与IN活性位点的潜在相互作用。结果表明，活性化合物与参与3'加工的Asp64残基以及参与整合过程链转移反应的Thr66、His67和Lys159残基相互作用。在抗炎活性方面，所有化合物均对lps诱导的一氧化氮生成(IC50 μM)有显著抑制作用。因此，本研究为在传统医学中使用B. alinode治疗HIV患者提供了额外的科学支持。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Advances in Pharmacological Sciences PHARMACOLOGY & PHARMACY-

CiteScore

6.40

自引率

0.00%

发文量

审稿时长

14 weeks

期刊介绍： Advances in Pharmacological and Pharmaceutical Sciences is a peer-reviewed, Open Access journal that publishes original research articles, review articles, and clinical studies in all areas of experimental and clinical pharmacology, pharmaceutics, medicinal chemistry and drug delivery. Topics covered by the journal include, but are not limited to: -Biochemical pharmacology, drug mechanism of action, pharmacodynamics, pharmacogenetics, pharmacokinetics, and toxicology. -The design and preparation of new drugs, and their safety and efficacy in humans, including descriptions of drug dosage forms. -All areas of medicinal chemistry, such as drug discovery, design and synthesis. -Basic biology of drug and gene delivery through to application and development of these principles, through therapeutic delivery and targeting. Areas covered include bioavailability, controlled release, microcapsules, novel drug delivery systems, personalized drug delivery, and techniques for passing biological barriers.