黄连解毒汤中黄酮成分逆转K562/ADM多药耐药的实验观察

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

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。

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 ICs0of 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 intraeellular 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.