Siriwan D, Miyawaki C, Miyamoto T, Naruse T, Okazaki K, Tamura H
The United Graduate School of Agricultural Sciences, Ehime University, 3-5-7 Tarumi, Matsuyama 790-8566, Japan.
Pak J Biol Sci. 2011 May 15;14(10):605-9. doi: 10.3923/pjbs.2011.605.609.
Yacon is a medicinal plant used as a traditional medicine by the natives in South America. In Japan, it becomes popular as a health food. Sesquiterpene Lactones (SLs) from yacon leaves were investigated and the active SLs such as enhydrin, uvedalin and sonchifolin, bearing alpha-methylene-gamma-lactone and epoxides as the active functional groups, were identified by 1H-6000 MHz-NMR. Chemopreventive and cytotoxic activities were determined using different primary screening methods. In this study, all tested SLs strongly inhibited TPA-induced deformed of Raji cells. The IC50 values of yacon SLs from anti-deforming assay were 0.04-0.4 microM. Interestingly, yacon SLs showed more potential of chemo preventive activity than both curcumin and parthenolide. However, the cytotoxicity on Raji cells was observed at high concentration of yacon SLs. The degree of anti-deformation was ranked in order: enhydrin >uvedalin >sonchifolin >parthenolide >curcumin. As according to structure-activity relationship, the high activities of enhydrin, uvedalin and sonchifolin may be due to the 2-methyl-2-butenoate and its epoxide moiety.
雪莲果是一种药用植物，被南美洲当地人用作传统药物。在日本，它作为一种健康食品而受到欢迎。对雪莲果叶中的倍半萜内酯（SLs）进行了研究，并通过1H - 6000 MHz - NMR鉴定出了具有活性的SLs，如安海苷、乌韦苷和苦苣菜苷，它们带有α - 亚甲基 - γ - 内酯和环氧化物作为活性官能团。使用不同的初步筛选方法测定了化学预防和细胞毒性活性。在本研究中，所有测试的SLs均强烈抑制佛波酯诱导的Raji细胞变形。抗变形试验中雪莲果SLs的IC50值为0.04 - 0.4 microM。有趣的是，雪莲果SLs显示出比姜黄素和小白菊内酯更强的化学预防活性潜力。然而，在高浓度的雪莲果SLs下观察到对Raji细胞的细胞毒性。抗变形程度排序为：安海苷＞乌韦苷＞苦苣菜苷＞小白菊内酯＞姜黄素。根据构效关系，安海苷、乌韦苷和苦苣菜苷的高活性可能归因于2 - 甲基 - 2 - 丁烯酸酯及其环氧化物部分。
