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从斜叶厚皮香的叶子和小枝中提取到抗 HIV-1 的二萜。

Anti-HIV-1 diterpenoids from leaves and twigs of Polyalthia sclerophylla.

机构信息

Department of Chemistry and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Mahidol University, Bangkok 10400, Thailand.

出版信息

Planta Med. 2010 May;76(7):721-5. doi: 10.1055/s-0029-1240683. Epub 2009 Dec 14.

DOI:10.1055/s-0029-1240683
PMID:20013639
Abstract

Bioassay-guided fractionation and purification of the anti-HIV-1-active MeOH extract from the leaves and twigs of Polyalthia sclerophylla led to the isolation of two new compounds, ENT-kaur-sclerodimer ( 1) and cyclotucanol 3-palmitate ( 2), along with the known ENT-kaur-16-en-19-oic acid ( 3), 15 beta-hydroxy- ENT-kaur-16-en-19-oic acid ( 4), 15 beta-acetoxy- ENT-kaur-16-en-19-oic acid ( 5), 15-oxo- ENT-kaur-16-en-19-oic acid ( 6), 16 alpha,17-dihydroxy- ENT-kauran-19-oic acid ( 7), 16 alpha-hydroxy- ENT-kauran-19-oic acid (xylopic acid) ( 8), a pseudodimer (15 alpha-hydroxy- ENT-kaur-16-en-19-oic acid/17-hydroxy- ENT-kaur-15-en-19-oic acid) ( 9), ermanin, nicotiflorin, and allantoin. Among these isolates, compound 3 was the most active in both anti-syncytium (EC (50) 13.7 microg/mL and selectivity index 3.1) and HIV-1 reverse transcriptase (IC (50) 34.1 microg/mL) assays.

摘要

从轮叶蒲桃的叶和小枝的抗 HIV-1 活性的甲醇提取物进行生物测定指导的分离和纯化,导致了两种新化合物的分离,ENT-贝壳杉二聚体(1)和环土豆醇 3-棕榈酸酯(2),以及已知的 ENT-贝壳杉-16-烯-19-酸(3),15β-羟基-ENT-贝壳杉-16-烯-19-酸(4),15β-乙酰氧基-ENT-贝壳杉-16-烯-19-酸(5),15-氧代-ENT-贝壳杉-16-烯-19-酸(6),16α,17-二羟基-ENT-贝壳杉-19-酸(7),16α-羟基-ENT-贝壳杉-19-酸(木糖醇酸)(8),假二聚体(15α-羟基-ENT-贝壳杉-16-烯-19-酸/17-羟基-ENT-贝壳杉-15-烯-19-酸)(9),埃曼宁,烟碱酸,和尿囊素。在这些分离物中,化合物 3 在抗合胞体(EC(50)13.7μg/mL 和选择性指数 3.1)和 HIV-1 逆转录酶(IC(50)34.1μg/mL)测定中最活跃。

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