Triterpenoids with α-glucosidase inhibitory activity and cytotoxic activity from the leaves of Akebia trifoliata.
Triterpenoids with α-glucosidase inhibitory activity and cytotoxic activity from the leaves of Akebia trifoliata.
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三叶木通叶中具有α-葡萄糖苷酶抑制活性和细胞毒活性的三萜类化合物
DOI：
10.1039/c8ra08894b
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发表时间：
2018-11-28
期刊：
影响因子：
3.9
通讯作者：
Tan, Jian-Wen
中科院分区：
文献类型：
--
作者：
Ouyang, Jin-Kui;Dong, Li-Mei;Xu, Qiao-Lin;Wang, Jing;Liu, Shao-Bo;Qian, Tao;Yuan, Yun-Fei;Tan, Jian-Wen
从三叶木通（Akebia trifoliata）叶中分离得到10个五环三萜化合物，其中包括一个新的多花烷三萜酸2α，3 β，23-三羟基多花-7-烯-28-酸（1）和一个新的羽扇烷三萜单糖苷Akebiaoside C（2）。它们的结构经波谱分析鉴定，均为从苦马豆叶中分离得到。三叶草第一次除化合物4和化合物5外，其余化合物的体外α-葡萄糖苷酶抑制活性均强于阿卡波糖。特别地，2、3、6、8和10显示出体外α-葡萄糖苷酶抑制活性，IC 50值为0.004至0.081 mM，其接近或甚至比科罗索酸（IC 50 0.06 mM）更强。三萜类化合物1、8和10对人肿瘤A549、HeLa和HepG 2细胞系显示出中等的体外细胞毒活性，IC 50值范围为26.5 - 51.9 μM。化合物9对HeLa和HepG 2细胞系显示出选择性的体外细胞毒性，IC 50值分别为81.49和73.47 μM。这些结果为A.三叶草是具有生物活性的三萜类化合物的丰富来源，具有很高的药用开发价值。从三叶木通（Akebia trifoliata）叶中分离得到10个五环三萜化合物，其中包括一个新的多花烷三萜酸2α，3 β，23-三羟基多花-7-烯-28-酸（1）和一个新的羽扇烷三萜单糖苷Akebiaoside C（2）。
Ten pentacyclic triterpenoids including a new multiflorane triterpene acid, 2α,3β,23-trihydroxymultiflor-7-en-28-oic acid (1), and a new lupane triterpene monoglucoside named akebiaoside C (2), were obtained from the leaves of Akebia trifoliata. Their structures were elucidated by extensive spectroscopic analysis, and they were all isolated from the leaves of A. trifoliata for the first time. These compounds, except 4 and 5, showed in vitro α-glucosidase inhibitory activity much stronger than acarbose. Especially, 2, 3, 6, 8 and 10 displayed in vitro α-glucosidase inhibitory activity with IC50 values from 0.004 to 0.081 mM, which were close or even more potent than corosolic acid (IC50 0.06 mM). Triterpenoids 1, 8 and 10 were further revealed to show moderate in vitro cytotoxic activity against human tumor A549, HeLa and HepG2 cell lines, with IC50 values ranging from 26.5 to 51.9 μM. Compound 9 selectively showed in vitro cytotoxicity toward HeLa and HepG2 cell lines, with IC50 values of 81.49 and 73.47 μM, respectively. These findings provided new data to support that the leaves of A. trifoliata are a rich source in bioactive triterpenoids highly valuable to be developed for medicinal usage. Ten pentacyclic triterpenoids including a new multiflorane triterpene acid, 2α,3β,23-trihydroxymultiflor-7-en-28-oic acid (1), and a new lupane triterpene monoglucoside named akebiaoside C (2), were obtained from the leaves of Akebia trifoliata.
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DOI：
10.3390/molecules21070962
发表时间：
2016-07-22
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Xu QL;Wang J;Dong LM;Zhang Q;Luo B;Jia YX;Wang HF;Tan JW
通讯作者：
Tan JW
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：
3.5
作者：
Luo, Han-Guang;Ma, Li;Kong, Ling-Yi
通讯作者：
Kong, Ling-Yi