Woerdenbag H J, Merfort I, Passreiter C M, Schmidt T J, Willuhn G, van Uden W, Pras N, Kampinga H H, Konings A W
Department of Pharmaceutical Biology, University Centre for Pharmacy, University of Groningen, The Netherlands.
Planta Med. 1994 Oct;60(5):434-7. doi: 10.1055/s-2006-959526.
The cytotoxicity of 21 flavonoids and 5 sesquiterpene lactones, as present in Arnica species, was studied in GLC4, a human small cell lung carcinoma cell line, and in COLO 320, a human colorectal cancer cell line, using the microculture tetrazolium (MTT) assay. Following continuous incubation, most flavonoids showed moderate to low cytotoxicity, as compared with the reference compound cisplatin (IC50 = 1.1 microM against GLC4 and 2.9 microM against COLO 320). Their IC50 values varied from 17 to > 200 microM. The most toxic compound was the flavone jaceosidin. Of the sesquiterpene lactones tested, helenalin, possessing both the reactive alpha-methylene-gamma-lactone moiety and a reactive alpha,beta-unsubstituted cyclopentenone ring, displayed the strongest cytotoxicity. For 2 h exposure, its IC50 value was 0.44 microM against GLC4 and 1.0 microM against COLO 320. COLO 320 was more sensitive than GLC4 for many flavonoids (especially for flavones), but more resistant to the cytotoxic effect of the sesquiterpene lactones bearing an exocylic methylene group fused to the lactone function.
利用微量培养四氮唑蓝（MTT）法，对山金车属植物中所含的21种黄酮类化合物和5种倍半萜内酯在人小细胞肺癌细胞系GLC4和人结肠癌细胞系COLO 320中的细胞毒性进行了研究。连续孵育后，与参考化合物顺铂（对GLC4的IC50 = 1.1 microM，对COLO 320的IC50 = 2.9 microM）相比，大多数黄酮类化合物表现出中度至低度细胞毒性。它们的IC50值在17至>200 microM之间变化。毒性最大的化合物是黄酮类化合物雅可西定。在所测试的倍半萜内酯中，海伦内酯同时具有反应性α-亚甲基-γ-内酯部分和反应性α,β-未取代的环戊烯酮环，表现出最强的细胞毒性。暴露2小时后，其对GLC4的IC50值为0.44 microM，对COLO 320的IC50值为1.0 microM。对于许多黄酮类化合物（尤其是黄酮），COLO 320比GLC4更敏感，但对带有与内酯功能稠合的环外亚甲基的倍半萜内酯的细胞毒性作用更具抗性。
