木香中倍半萜类化合物体外抗癌活性评价研究

Inhibitory effects of sesquiterpenes from Common Aucklandia Root on proliferation of five kinds cultured cancer cells in vitro

目的:通过观察木香中5个倍半萜类化合物①dehydrocostus lactone,②santamarine,③β-cyclocostunolide,④4α-hydroxy-4β-methyldihydrocostol,⑤10α-hydroxyl-artemisinic acid对5株癌细胞生长的影响,探讨这5个倍半萜类化合物的抗癌作用及各化合物结构与活性之间的构效关系。方法:以人胃癌细胞MGC-803、人口腔上皮癌细胞KB、人肝癌细胞HepG-2、人肺癌细胞NCI-H460和人结肠癌细胞HT-29为研究对象,采用MTT法检测5个倍半萜类化合对这5株癌细胞生长的抑制率。结果:化合物1-3对人胃癌细胞MGC-803、人口腔上皮癌细胞KB、人肺癌细胞NCI-H460和人结肠癌细胞HT-29的生长均显示明显的抑制作用(IC50<10.0mg/mL),对人肝癌细胞HepG-2的生长抑制作用较弱(IC50分别为16.3、48.7,16.1mg/mL);而化合物4和5对这5种癌细胞株的生长均未显示抑制作用(IC50>100.0mg/mL)。结论:从结构上分析,五元内酯环可能是木香中倍半萜类化合物抑制癌细胞生长的活性基团之一。

Objective：To study the effects of five sesquiterpenes including dehydrocostus lactone（1）,santamarine （2）,β-cyclocostunolide（3）,4α-hydroxy-4β-methyldihydrocostol（4）,and 10α-hydroxyl-artemisinic acid（5）from Common Aucklandia Root on inhibited proliferation of five cultured cancer cells in vitro.Methods：MTT was used to observe the effects of inhibiting proliferation of human stomach cancer cells MGC-803,human pharyngeal cancer cells KB,human liver cancer cells HepG-2,human lung cancer cells NCI-H460,and human colon cancer cells HT-29 cultured in vitro for72 h.Results：It was found that compounds 1-3 showed obvious effects on inhibited proliferation of human stomach cancer cells MGC-803,human pharyngeal cancer cells KB,human lung cancer cells NCI-H460,and human colon cancer cells HT-29 cultured for 72 h（IC5010.0 mg/ml）,and had weak effects on inhibiting proliferation of human liver cancer cells HepG-2 cultured for 72 h（IC50=16.3,48.7,and 16.1 mg/ml,respectively）.However,compounds 4 and 5 showed no effects on inhibiting proliferation of the five kinds of cancer cell lines cultured for 72 h（IC50100.0 mg/ml）.Conclusion：Five-membered lactone ring may be one of the essential parts of sesquiterpenes from A.lappa for inhibiting proliferation of cancer cells.