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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 IC 50  value of 17.7  μ 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 50  < 68.7  μ M). Thus, this research provides additional scientific support for the use of  B. alnoides  in traditional medicine for the treatment of HIV patients.

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