{"title":"白桦抗hiv -1整合酶及抗炎活性评价","authors":"Prapaporn Chaniad, Teeratad Sudsai, Abdi Wira Septama, Arnon Chukaew, Supinya Tewtrakul","doi":"10.1155/2019/2573965","DOIUrl":null,"url":null,"abstract":"<p><p><i>Betula alnoides</i> 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 <i>B. alnoides</i> stems using chromatographic techniques, five pentacyclic triterpenoid compounds were obtained. They are betulinic acid (<b>1</b>), betulin (<b>2</b>), lupeol (<b>3</b>), oleanolic acid (<b>4</b>), and ursolic acid (<b>5</b>). Compound <b>2</b> exhibited the most potent inhibitory activity against HIV-1 IN, with an IC<sub>50</sub> value of 17.7 <i>μ</i>M. 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 (IC<sub>50</sub> < 68.7 <i>μ</i>M). Thus, this research provides additional scientific support for the use of <i>B. alnoides</i> in traditional medicine for the treatment of HIV patients.</p>","PeriodicalId":7389,"journal":{"name":"Advances in Pharmacological Sciences","volume":"2019 ","pages":"2573965"},"PeriodicalIF":0.0000,"publicationDate":"2019-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2019/2573965","citationCount":"13","resultStr":"{\"title\":\"Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from <i>Betula alnoides</i> Buch-Ham.\",\"authors\":\"Prapaporn Chaniad, Teeratad Sudsai, Abdi Wira Septama, Arnon Chukaew, Supinya Tewtrakul\",\"doi\":\"10.1155/2019/2573965\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p><i>Betula alnoides</i> 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 <i>B. alnoides</i> stems using chromatographic techniques, five pentacyclic triterpenoid compounds were obtained. They are betulinic acid (<b>1</b>), betulin (<b>2</b>), lupeol (<b>3</b>), oleanolic acid (<b>4</b>), and ursolic acid (<b>5</b>). Compound <b>2</b> exhibited the most potent inhibitory activity against HIV-1 IN, with an IC<sub>50</sub> value of 17.7 <i>μ</i>M. 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 (IC<sub>50</sub> < 68.7 <i>μ</i>M). Thus, this research provides additional scientific support for the use of <i>B. alnoides</i> in traditional medicine for the treatment of HIV patients.</p>\",\"PeriodicalId\":7389,\"journal\":{\"name\":\"Advances in Pharmacological Sciences\",\"volume\":\"2019 \",\"pages\":\"2573965\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2019-06-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1155/2019/2573965\",\"citationCount\":\"13\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Advances in Pharmacological Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1155/2019/2573965\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2019/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q1\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Advances in Pharmacological Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1155/2019/2573965","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2019/1/1 0:00:00","PubModel":"eCollection","JCR":"Q1","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham.
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.
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.
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