Bioactive 30-noroleanane triterpenes from the pericarps of Akebia trifoliata.
Bioactive 30-noroleanane triterpenes from the pericarps of Akebia trifoliata.
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三叶木通果皮中具有生物活性的 30-Noroleanane 三萜
DOI：
10.3390/molecules19044301
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发表时间：
2014-04-04
期刊：
影响因子：
--
通讯作者：
Tan JW
中科院分区：
文献类型：
--
作者：
Wang J;Xu QL;Zheng MF;Ren H;Lei T;Wu P;Zhou ZY;Wei XY;Tan JW
从三叶木通（Akebia trifoliata）果皮中分离得到2个新的30-noroleanane三萜化合物，2α，3 β，20 α-trihydroxy-30-noroleana-12-en-28-oic acid（1），2α，3 β-dihydroxy-23-oxo-30-noroleana-12，20（29）-dien-28-oic acid（2），以及4个已知化合物，3β-akebonoic acid（3），2α，3 β-dihydroxy-30-noroleana-12，20（29）-二烯-28-酸（4）、3α-酮酸（5）和奎尼酸（6）。它们的结构均为从苦皮藤果皮中分离得到。三叶草第一次化合物3 - 6对四种测定的革兰氏阳性细菌菌株显示出体外抑菌活性。特别是3显示出对MRSA的抗菌活性，MIC值为25 μg/mL，比卡那霉素（MIC 125 μg/mL）更有效。没有化合物显示出对测试的三种革兰氏阴性细菌的抗菌活性。化合物4和5对人肿瘤A549和HeLa细胞株显示了有趣的体外生长抑制活性，IC 50值分别为8.8和5.6 μM。化合物1、2、5和6进一步显示出显著的体外α-葡萄糖苷酶抑制活性，IC 50值为0.035至0.367 mM，其比参比化合物阿卡波糖（IC 50 0.409 mM）更有效。
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).
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影响因子：
3.8
作者：
IKUTA, A;ITOKAWA, H
通讯作者：
ITOKAWA, H
影响因子：
2
作者：
Guan, Shu-hong;Xia, Jia-meng;Guo, De-an
通讯作者：
Guo, De-an
影响因子：
8.8
作者：
Ieyama, Tomohiro;Gunawan-Puteri, Maria D. P. T.;Kawabata, Jun
通讯作者：
Kawabata, Jun
影响因子：
3.8
作者：
IKUTA, A;ITOKAWA, H
通讯作者：
ITOKAWA, H
影响因子：
1.7
作者：
Mimaki, Y;Kuroda, M;Sashida, Y
通讯作者：
Sashida, Y