Bioactive saponins and glycosides.: XXIII.: Triterpene saponins with gastroprotective effect from the seeds of Camellia sinensis -: Theasaponins E3, E4, E5, E6, and E7
Bioactive saponins and glycosides.: XXIII.: Triterpene saponins with gastroprotective effect from the seeds of Camellia sinensis -: Theasaponins E3, E4, E5, E6, and E7
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DOI：
10.1248/cpb.53.1559
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发表时间：
2005-12-01
影响因子：
1.7
通讯作者：
Matsuda, H
中科院分区：
文献类型：
--
作者：
Yoshikawa, M;Morikawa, T;Matsuda, H
茶树竖条茶（Camellia sinensis（L.））种子中的皂苷级分O. Kuntze（山茶科）垂直杆被发现表现出强大的保护作用，对乙醇和消炎痛诱导的大鼠胃粘膜损伤。从皂苷级分中分离得到五个新的三萜皂苷，即茶皂苷E-3（1）、E-4（2）、E-5（3）、E-6（4）和E-7（5）。化合物1-5的化学结构经理化分析鉴定。在分离的皂苷中，茶皂苷E-1（6）、E-2（7）和E-5（3）和阿萨姆皂苷C（10）在5.0 mg/kg，p.o.其活性均强于奥涅拉唑。关于茶皂苷的构效关系，提出了对乙醇诱导的胃损伤的保护作用的以下结构要求：1）21-和/或22-酰基是活性所必需的，2）16-羟基的乙酰化降低活性。
The saponin fraction from the seeds of the tea plant vertical bar Camellia sinensis (L.) O. Kuntze (Theaceae)vertical bar was found to exhibit potent protective effects on ethanol- and indomethacin-induced gastric mucosal lesions in rats. Five new triterpene saponins, theasaponins E-3 (1), E-4, (2), E-5 (3), E-6 (4), and E-7 (5), were isolated together with I I known saponins from the saponin fraction. The chemical structures of 1-5 were elucidated on the basis of chemical and physicochemical evidence. Among the isolated saponins, theasaponins E-1 (6), E-2 (7), and E-5 (3) and assamsaponin C (10) showed an inhibitory effect on ethanol-induced gastric mucosal lesions at a dose of 5.0 mg/kg, p.o. and their activities were stronger than that of onieplazole. With regard to the structure-activity relationships of theasaponins, the following structural requirements for a protective effect on ethanol-induced gastric lesions were suggested; 1) the 21- and/or 22-acyl groups are essential for the activity, 2) acetylation of the 16-hydroxyl group reduce the activity.