Phytochemical analysis of the triterpenoids with cytotoxicity and QR inducing properties from the total tea seed saponin of Camellia sinensis
Phytochemical analysis of the triterpenoids with cytotoxicity and QR inducing properties from the total tea seed saponin of Camellia sinensis
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茶树总皂苷中具有细胞毒性和 QR 诱导特性的三萜类化合物的植物化学分析
DOI：
10.1016/j.fitote.2012.12.022
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发表时间：
2013-01-01
期刊：
影响因子：
3.4
通讯作者：
Li, Xian
中科院分区：
文献类型：
--
作者：
Li, Ning;Ma, Zhong-jun;Li, Xian
结果表明，茶籽三萜皂苷（TS）对荷瘤小鼠的体内抗肿瘤活性和对肝癌细胞hepa 1c 1c 7的QR诱导活性均优于茶籽总皂苷（TTS）、茶籽三萜皂苷水解物（TTS水解物）和茶籽黄酮苷（TF）。通过生物活性导向分离，从该属植物中分离得到7个主要成分，分别为茶皂苷E1（1）、茶皂苷E2（2）、茶皂苷C1（3）、茶皂苷C（4）、茶皂苷H1（5）、茶皂苷A9（6）和茶皂苷A8（7），其中化合物4和5为首次从该属植物中分离得到。抗肿瘤活性测定结果表明，化合物1、2和3对人肿瘤细胞株K562和HL 60具有潜在的抑制活性。此外，化合物1（质量含量超过1%的主要成分）显示出显著的QR诱导活性，在4 μ g/ml时IR值为4.2。因此，茶籽特别是化合物1（茶皂苷E1）可作为一种抗肿瘤剂和癌症的化学预防剂。初步探讨了茶皂苷抗肿瘤活性和QR诱导活性的构效关系。(c)2012爱思唯尔有限公司版权所有。
The tea seed triterpene saponin (TS) from Camellia sinensis was found to exhibit better antitumor activity in vivo in S180 implanted ICR mice and QR inducing activity for hepa 1c1c7 cells respectively compared with the total tea seed saponin (TTS), hydrolysate of the TTS and tea seed flavonoid glycosides (TF). By bioassay-guided isolation, the TS fraction was separated and seven major components were purified and identified as theasaponin El (1), theasaponin E2 (2), theasaponin C1 (3), assamsaponin C (4), theasaponin H1 (5), theasaponin A9 (6), and theasaponin A8 (7), among which compounds 4 and 5 were isolated from this genus for the first time. The antitumor bioassay of the isolated compounds showed that compounds 1, 2 and 3 exhibited potential activities against the human tumor cell lines K562 and HL60. Furthermore, compound 1 (the major constituent with a mass content of over 1%) showed significant QR inducing activity with an IR value of 4.2 at 4 mu g/ml. So it can be concluded that tea seed especially the compound 1 (theasaponin E1) could be used as an antitumor agent and a chemoprevention agent of cancer. The preliminary structure-activity relationship in the anti-tumor activity and QR inducing activity of tea saponins was discussed briefly. (c) 2012 Elsevier B.V. All rights reserved.