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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。
Aim To determine the effects of two new photosensitizers, 5-amino-1-pentanesulfonic acid, substituted for hypocrellin B derivative (PENSHB) and 15-deacetyl 13-amino-1-propanesulfonic acid The cytotoxicity and photodynamic killing effect of DPROHB were compared with that of its parental hypocrellin B (HB). Preliminary understanding of two new photosensitizers photodynamic effect. Methods The three photosensitizers were incubated with human gastric adenocarcinoma BGC-823 cells respectively. The photodynamic therapy group was irradiated with KTP laser at a wavelength of 532 nm and a power density of 20 mW / cm2 for 1000 s. Photosensitizer group: Incubate only for 24 h. MTT assay was used to determine the survival rate of cancer cells under different concentrations of photosensitizer in each group. The cytotoxic and cytotoxic effects of the drugs on the cells were plotted separately. The curve equations were fitted to calculate the concentration of 50% inhibition concentration (IC50-PDT) and the 50% inhibition concentration IC50-DT). And thus calculate the safety factor of the photosensitizer. Results The IC50-PDT of PENSHB, DPROHB and HB were 26.22,28.14 and 48.03 nM, respectively. The IC50-PDT of PENSHB and DPROHB was significantly different from that of HB-IC50-PDT (P < 0.01). There was no significant difference between IC50-PDT of PENSHB and IC50-PDT of DPROHB. Photosensitizer group PENSHB, DPROHB and HB half the concentration (IC50-DT), respectively 3.42,4.20 and 4.48μM, the three was no significant difference (P> 0.05). The safety factors of PENSHB, DPROHB and HB are 130,173,93. Conclusion The PDT killing effect of PENSHB and DPROHBP on BGC-823 cell line was not significantly different, but both were stronger than HB. The three photosensitizers had similar cytotoxicity to PDT, and the safety of PENSHB and DPROHBP to HB was improved.