School of Chinese Medicine, Hong Kong Baptist University , Kowloon Tong, Hong Kong SAR, People's Republic of China.
J Nat Prod. 2014 Mar 28;77(3):663-7. doi: 10.1021/np400779v. Epub 2014 Jan 9.
A new lignan, vitexkarinol (1), as well as a known lignan, neopaulownin (2), a known chalcone, 3-(4-hydroxyphenyl)-1-(2,4,6-trimethoxyphenyl)-2-propen-1-one (3), two known dehydroflavones, tsugafolin (4) and alpinetin (5), two known dipeptides, aurantiamide and aurantiamide acetate, a known sesquiterpene, vemopolyanthofuran, and five known carotenoid metabolites, vomifoliol, dihydrovomifoliol, dehydrovomifoliol, loliolide, and isololiolide, were isolated from the leaves and twigs of Vitex leptobotrys through bioassay-guided fractionation. The chalcone (3) was found to inhibit HIV-1 replication by 77% at 15.9 μM, and the two dehydroflavones (4 and 5) showed weak anti-HIV activity with IC50 values of 118 and 130 μM, respectively, while being devoid of cytotoxicity at 150 μM. A chlorophyll-enriched fraction of V. leptobotrys, containing pheophorbide a, was found to inhibit the replication of HIV-1 by 80% at a concentration of 10 μg/mL. Compounds 1 and 3 were further selected to be evaluated against 21 viral targets available at NIAID (National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD, USA).
从牡荆属植物的叶和小枝中，通过生物测定指导的分离，分离得到了一种新的木脂素，荜澄茄素（1），以及一种已知的木脂素，新厚朴酚（2），一种已知的查尔酮，3-（4-羟基苯基）-1-（2,4,6-三甲氧基苯基）-2-丙烯-1-酮（3），两种已知的去氢黄酮，穗花杉双黄酮（4）和白杨素（5），两种已知的二肽，橙皮酰胺和橙皮酰胺醋酸盐，一种已知的倍半萜，vemopolyanthofuran，以及五种已知的类胡萝卜素代谢物，vomifoliol，二氢vomifoliol，脱氢vomifoliol，loliolide 和 isololiolide。查尔酮（3）在 15.9 μM 时被发现抑制 HIV-1 复制 77%，两种去氢黄酮（4 和 5）表现出弱的抗 HIV 活性，IC50 值分别为 118 和 130 μM，而在 150 μM 时无细胞毒性。牡荆属植物的叶绿素富集部分，含有原卟啉 a，在浓度为 10 μg/mL 时被发现抑制 HIV-1 的复制 80%。化合物 1 和 3 进一步被选择用于评估 NIAID（国家过敏和传染病研究所，美国国立卫生研究院，马里兰州贝塞斯达）提供的 21 种病毒靶标。
