黄连解毒汤中黄酮成分逆转 K562/ADM多药耐药的实验观察

目的:观察黄连解毒汤中黄酮成分逆转肿瘤多药耐药的作用,探讨本方逆转肿瘤多药耐药的物质基础。方法:以人慢性粒细胞白血病红白血病细胞株K562的耐阿霉素(adriamycin,ADM)细胞株(K562/ADM)为细胞系,通过MTT实验观察黄芩苷、京尼平苷对K562/ADM细胞ADM的敏感性的影响,计算细胞增殖抑制率、半数抑制浓度(IC50)及耐药逆转倍数,并对细胞内ADM浓度变化进行测定。结果:黄芩苷、京尼平苷均能部分逆转K562/ADM细胞。黄芩苷、京尼平苷的IC50值分别为5.06,6.74 mg.L-1。黄芩苷、京尼平苷的耐药逆转倍数分别为1.95,1.46倍。与相应的对照组相比,K562/ADM细胞经黄芩苷(50 mg.L-1)、京尼平苷(100 mg.L-1)作用后,细胞内ADM的荧光强度高于对照组,其中黄芩苷组提高到3.6%,京尼平苷组提高到1.7%。结论:黄连解毒汤逆转肿瘤多药耐药的物质基础可能与其含有的黄芩苷、京尼平苷有关。

Study on the Flavonoid of Huanglian Jiedu Decoction in Reversing MDR of K562/ADM

Objective:To observe the effect on the flavoniod of Huanglian Jiedu decoction, and discuss its material base in reversing multiple-drug resistance(MDR) of cancer so as to provide the theory basis for Huanglian Jiedu decoction in clinical practices. Method: MTT assay was adopted to test the sensitivity of baicalin and geniposide to adriamycin(ADM) of K562/ADM, the inhibitory rate was calculated, the value of 50% inhibition concentration(IC₅₀) and the multiple of the reversal of drug resistance as well as the change of the concentration of the intracellular ADM were assayed by using ADM K562/ADM of human chronic myelogenous leukemia(CML) erythroleukemia K562 as cell line. Result: Both baicalin and geniposide could partly reverse K562/ADM cell. The value of IC₅₀ of baicalin and geniposide was 5.06 mg·L^-1and 6.74 mg·L^-1 respectively.The multiple of the reversal of drug resistance of baicalin and geniposide was 1.95 times and 1.46 times.The fluorescence intensity of the intracellular K562/ADM was higher than the control group, and the fluorescence intensity in the group of baicalin rised to 3.6%, The fluorescence intensity of the group of geniposide rise to 1.7%. Conclusion: The material base of the Huanglian Jiedu decoction in reversing MDR of cancer is probably related to its components baicalin and geniposide.