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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 observe the effect of 5 sesquiterpenes (1) dehydrocostus lactone, 2santamarine, 3-cyclocostunolide, 4α-hydroxy-4β-methyldihydrocostol and 5α-hydroxyl-artemisinic acid on the growth of 5 cancer cells. Antitumor activity of sesquiterpenoids and their structure-activity relationship. Methods: Human gastric cancer cells MGC-803, human oral epithelial cancer cells KB, human hepatocellular carcinoma cells HepG-2, human lung cancer cells NCI-H460 and human colon cancer cells HT-29 were studied. Terpenoid on these five cancer cell growth inhibition. Results: Compound 1-3 showed obvious inhibitory effects on the growth of human gastric cancer cells MGC-803, human oral epithelial cancer cells KB, human lung cancer cells NCI-H460 and human colon cancer cells HT-29 (IC50 <10.0 mg / mL ) Inhibited the growth of HepG-2 cells (IC50: 16.3, 48.7 and 16.1 mg / mL, respectively); while compounds 4 and 5 showed no inhibitory effect on the growth of these 5 cell lines (IC50 > 100.0 mg / mL). CONCLUSION: The five-membered lactone ring may be one of the active groups that sesquiterpenoids inhibit the growth of cancer cells from the perspective of structure.