竹红菌乙素及其衍生物对人胃腺癌细胞光动力杀伤效应的比较

Comparative Study on Hypocrellin B and Hypocrellin B-derivatives Induced Photodynamic Effects to Gastric Adenocarcinoma Cell Line

目的测定两种新型光敏剂5-氨基-1-戊磺酸取代竹红菌乙素衍生物(PENSHB)和15位脱乙酰基13位3-氨基-1-丙磺酸取代的竹红菌乙素衍生物(DPROHB)的细胞毒性及其光动力杀伤效应,并与其母体竹红菌乙素(hypocrellin B,HB)的细胞毒性、光动力杀伤效应进行比较。初步了解两种新型光敏剂的光动力作用效果。方法三种光敏剂分别孵育人胃腺癌BGC-823细胞,光动力组:采用波长532 nm、功率密度20 mW/cm2 KTP激光照射1 000 s。光敏剂组:仅孵育24 h。用MTT法分别测定各组不同光敏剂浓度下的癌细胞存活率。分别绘制药物对细胞光毒及暗毒的杀伤曲线,并拟合曲线方程,计算光动力组半数杀伤浓度(50%inhibition concentration,IC50-PDT)及光敏剂组半数杀伤浓度(50%inhibition concentration,IC50-DT)。并由此计算光敏剂的安全系数。结果 PENSHB、DPROHB及HB对BGC-823细胞的半数杀伤浓度(IC50-PDT)分别为26.22、28.14和48.03 nM;PENSHB、DPROHB的IC50-PDT与HB的IC50-PDT比较差异有显著意义(P<0.01)。PENSHB的IC50-PDT与DPROHB的IC50-PDT比较差异无显著意义。光敏剂组PENSHB、DPROHB及HB半数杀伤浓度(IC50-DT),分别为3.42、4.20和4.48μM,三者比较差异无显著意义(P>0.05)。PENSHB、DPROHB及HB的安全系数依次为130,173,93。结论 PENSHB和DPROHBP对BGC-823细胞株的PDT杀伤效应无明显区别,但均强于HB,三种光敏剂对细胞暗毒性相当,PENSHB和DPROHBP较HB安全性有所提高。

Objective The photodynamic therapy（PDT） effects and cytotoxicity per se of 17-5-amino-1-pentane-sulfonicacid-hypocrellin B（PENSHB）and 15-deacetyl-13-3-amino-1-propane-sulfonic acid-hypocrellin B（DPROHB）have been studied and compared with the parent hypocrellin B（HB）.The PDT effects of these two new photosensitizers have been evaluated. Methods The BGC-823 cells were incubated with PENSHB,DPROHB or HB in different concentrations.Light-dependent cytotoxicity： cells were irradiated by KTP laser under wavelength 532nm with power density of 20mW/cm2 for 1000s.The cytotoxicity per se： cells were incubated as above without irradiation.Cell survival rates were measured by MTT assay respectively.Cell survival relationship with concentrations based on photosensitisers was plotted and polynomial curved.Light-induced cytotoxicity IC50（50% inhibition concentration） of each photosensitizer was derived.The safety coefficient for the photosensitizers was calculated based on the dark and light-induced cytotoxicity. Results Light-dependent cytotoxicity IC50 of PENSHB,DPROHB and HB was 26.22,28.14 and 48.03 nM,respectively.The statistical difference existed between HB and its derivatives,whereas no such difference was observed between PENSHB and DPROHB.The cytotoxicity per se IC50 of three photosensitizers was 3.42、4.20 and 4.48 μM,respectively,without statistical difference between each other.The safety coefficients of the individual photosensitizer were 130,173 and 93. Conclusions PENSHB and DPROHBP were better in PDT effect on BGC-823 cells and safer than HB.The cytotoxicity perse of three photosensitizers has no difference.