Wang Jing, Xu Qiao-Lin, Zheng Meng-Fei, Ren Hui, Lei Ting, Wu Ping, Zhou Zhong-Yu, Wei Xiao-Yi, Tan Jian-Wen
Key Laboratory of Plant Resources Conservation and Sustainable Utilization, South China Botanical Garden, Chinese Academy of Sciences, Guangzhou 510650, China.
Biotechnology Division, Guangdong Academy of Forestry, Guangzhou 510520, China.
Molecules. 2014 Apr 4;19(4):4301-12. doi: 10.3390/molecules19044301.
Two new 30-noroleanane triterpenes, 2α,3β,20α-trihydroxy-30-norolean-12-en-28-oic acid (1), 2α,3β-dihydroxy-23-oxo-30-norolean-12,20(29)-dien-28-oic acid (2), were isolated from the pericarps of Akebia trifoliata, together with four known ones, 3β-akebonoic acid (3), 2α,3β-dihydroxy-30-noroleana-12,20(29)-dien-28-oic acid (4), 3α-akebonoic acid (5) and quinatic acid (6). Their structures were established on the basis of detailed spectroscopic analysis, and they were all isolated from the pericarps of A. trifoliata for the first time. Compounds 3-6 showed in vitro bacteriostatic activity against four assayed Gram-positive bacterial strains. In particular 3 showed antibacterial activity toward MRSA with a MIC value 25 μg/mL, which was more potent than kanamycin (MIC 125 μg/mL). No compounds showed antibacterial activity toward the three Gram-negative bacteria tested. Compounds 4 and 5 showed interesting in vitro growth inhibitory activity against human tumor A549 and HeLa cell lines, with IC50 values ranging from 8.8 and 5.6 μM, respectively. Compounds 1, 2, 5 and 6 were further revealed to show significant in vitro α-glucosidase inhibitory activity with IC50 values from 0.035 to 0.367 mM, which were more potent than the reference compound acarbose (IC50 0.409 mM).
从三叶木通果皮中分离得到两个新的30-降齐墩果烷型三萜，2α,3β,20α-三羟基-30-降齐墩果-12-烯-28-酸（1）、2α,3β-二羟基-23-氧代-30-降齐墩果-12,20(29)-二烯-28-酸（2），以及四个已知化合物，3β-木通酸（3）、2α,3β-二羟基-30-降齐墩果-12,20(29)-二烯-28-酸（4）、3α-木通酸（5）和齐墩果酸（6）。通过详细的光谱分析确定了它们的结构，且均为首次从三叶木通果皮中分离得到。化合物3-6对四种受试革兰氏阳性菌菌株表现出体外抑菌活性。特别是化合物3对耐甲氧西林金黄色葡萄球菌（MRSA）具有抗菌活性，最低抑菌浓度（MIC）值为25 μg/mL，比卡那霉素（MIC 125 μg/mL）更有效。没有化合物对三种受试革兰氏阴性菌表现出抗菌活性。化合物4和5对人肿瘤A549和HeLa细胞系表现出有趣的体外生长抑制活性，IC50值分别为8.8和5.6 μM。进一步研究发现化合物1、2、5和6具有显著的体外α-葡萄糖苷酶抑制活性，IC50值为0.035至0.367 mM，比参考化合物阿卡波糖（IC50 0.409 mM）更有效。
