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 investi...
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| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Wiley
2019-01-01
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| Series: | Advances in Pharmacological Sciences |
| Online Access: | http://dx.doi.org/10.1155/2019/2573965 |
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| author | Prapaporn Chaniad Teeratad Sudsai Abdi Wira Septama Arnon Chukaew Supinya Tewtrakul |
| author_facet | Prapaporn Chaniad Teeratad Sudsai Abdi Wira Septama Arnon Chukaew Supinya Tewtrakul |
| author_sort | Prapaporn Chaniad |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-91bd899e011148f6a38dff3162080b20 |
| institution | Kabale University |
| issn | 1687-6334 1687-6342 |
| language | English |
| publishDate | 2019-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Advances in Pharmacological Sciences |
| spelling | doaj-art-91bd899e011148f6a38dff3162080b202025-02-03T06:12:28ZengWileyAdvances in Pharmacological Sciences1687-63341687-63422019-01-01201910.1155/2019/25739652573965Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-HamPrapaporn Chaniad0Teeratad Sudsai1Abdi Wira Septama2Arnon Chukaew3Supinya Tewtrakul4School of Medicine, Walailak University, Nakhon Si Thammarat 80160, ThailandSchool of Medicine, Walailak University, Nakhon Si Thammarat 80160, ThailandResearch Center for Chemistry, Indonesian Institute of Sciences, Kawasan Puspitek Serpong, Tangerang Selatan, Banten 15314, IndonesiaChemistry Department, Faculty of Science and Technology, Suratthani Rajabhat University, Surat Thani 84100, ThailandFaculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, ThailandBetula 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.http://dx.doi.org/10.1155/2019/2573965 |
| spellingShingle | Prapaporn Chaniad Teeratad Sudsai Abdi Wira Septama Arnon Chukaew Supinya Tewtrakul Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham Advances in Pharmacological Sciences |
| title | Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham |
| title_full | Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham |
| title_fullStr | Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham |
| title_full_unstemmed | Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham |
| title_short | Evaluation of Anti-HIV-1 Integrase and Anti-Inflammatory Activities of Compounds from Betula alnoides Buch-Ham |
| title_sort | evaluation of anti hiv 1 integrase and anti inflammatory activities of compounds from betula alnoides buch ham |
| url | http://dx.doi.org/10.1155/2019/2573965 |
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