Balunas Marcy J, Su Bin, Riswan Soedarsono, Fong Harry H S, Brueggemeier Robert W, Pezzuto John M, Kinghorn A Douglas
Program for Collaborative Research in the Pharmaceutical Sciences, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois 60612.
Phytochem Lett. 2009 Feb 19;2(1):29-33. doi: 10.1016/j.phytol.2008.10.009.
The hexane- and ethyl acetate-soluble extracts of the leaves of Brassaiopsis glomerulata (Blume) Regel (Araliaceae), collected in Indonesia, were found to inhibit aromatase, the rate-limiting enzyme in the production of estrogens from androgens, in both enzyme- and cell-based aromatase inhibition (AI) assays. Bioassay-guided fractionation led to the isolation of six known compounds of the steroid and triterpenoid classes (1-6) from the hexane extract, of which 6β-hydroxystimasta-4-en-3-one (5), was moderately active in the cell-based AI assay. Fractionation of the ethyl acetate extract afforded seven pure isolates (7-13) of the modified peptide, fatty acid, monoterpenoid, and benzenoid types, including six known compounds and the new natural product, N-benzoyl-L-phenylalanine methyl ester (9). The absolute stereochemistry of 9 and the other two peptides, 7 and 8, was determined by Marfey's analysis. Linoleic acid (10) was found to be active in the enzyme-based AI assay, while 9 and (-)-dehydrololiolide (12) showed activity in the cell-based AI assay.
在印度尼西亚采集的球序鹅掌柴（五加科）叶片的正己烷和乙酸乙酯可溶提取物，在基于酶和细胞的芳香化酶抑制（AI）试验中，被发现能抑制芳香化酶，该酶是雄激素转化为雌激素过程中的限速酶。通过生物活性导向的分级分离，从正己烷提取物中分离出六种甾体和三萜类已知化合物（1 - 6），其中6β - 羟基豆甾 - 4 - 烯 - 3 - 酮（5）在基于细胞的AI试验中具有中等活性。乙酸乙酯提取物的分级分离得到了七种修饰肽、脂肪酸、单萜类和苯类的纯分离物（7 - 13），包括六种已知化合物和新的天然产物N - 苯甲酰 - L - 苯丙氨酸甲酯（9）。通过马尔菲分析法确定了9以及另外两种肽7和8的绝对立体化学结构。亚油酸（10）在基于酶的AI试验中具有活性，而9和（ - ） - 脱氢洛里醇内酯（12）在基于细胞的AI试验中显示出活性。
