两种新型竹红菌乙素衍生物在人胃腺癌BGC-823细胞中吸收规律的研究

Absorption Characteristics of Two Novel Hypocrellin B Derivatives in BGC-823 Cell

目的探讨两种新型光敏剂5-氨基-1-戊磺酸竹红菌乙素衍生物(PENSHB)和15位脱乙酰基13位3-氨基-1-丙磺酸竹红菌乙素衍生物(DPROHB)在人胃腺癌BGC-823细胞中的吸收规律。方法以浓度为4μM的PENSHB、DPROHB对人胃腺癌BGC-823细胞分别孵育0、0.5、1、2、4和8 h,用荧光分析法测定细胞内光敏剂含量,通过浓度-荧光强度标准曲线换算成光敏剂浓度,绘制每种光敏剂的孵育时间-细胞含量的关系曲线。以浓度为0.5、1、2、4和8μM的两种光敏剂分别孵育BGC-823细胞4 h后,测定细胞内荧光强度,绘制光敏剂的孵育浓度-细胞含量关系曲线。结果 BGC-823细胞对PENSHB和DPROHB的吸收含量随孵育时间的延长而增加,两者变化趋势相近,孵育1 h内细胞吸两种新型光敏剂收含量增加较快,4 h达到平台。在本实验的浓度范围内PENSHB和DPROHB的细胞吸收量随孵育浓度的增高而增加,基本呈线性关系,上升趋势相似。两者在细胞内的吸收含量依赖孵育时间及孵育浓度。结论两种新型竹红菌乙素衍生物PENSHB和DPROHB在提高水溶性及光动力效应的同时,细胞吸收特性良好,是有潜在应用前景的新型光敏剂。

Objective The purpose of this study is to investigate the absorptive characteristics of 17-5-amino-1-pentane-sulfoicacid-hypocrellin B（PENSHB） and 15-Deacetyl-13-3-amino-propane-sulfonic acid-hypocrellin B（DPROHB）. Methods Human Gastric Adenocarcinoma Cells（BGC-823） were cultured,and PENSHB or DPROHB having a concentration of 4 μM was added to the culture medium.Then,they were incubated for different periods.Samples were measured with spectrofluorophotometer to get the curve of relationship between cell content and photosensitizer incubation period.The BGC-823 cells were incubated with PENSHB and DPROHB at different concentrations for 4 hours,then the relationship between the cell content and incubation concentration of the photosensitizers was plotted. Results he absorption curves of PENSHB and DPROHB by BGC-823 were similar.The absorption content increased rapidly in the first hour and the cells reached platform after 4 hours＇ incubation.Within the concentration range of this experiment,the cell uptake of PENSHB and DPROHB rose with the incubating concentration,revealing a linear relationship and similar rising trend.The content of PENSHB and DPROHB in BGC-823 was dose-dependent and time-dependent. Conclusions Besides better water solubility and photodynamic effects,the two novel hypocrellin derivatives,namely,PENSHB and DPROHB,perform well in cell absorption.They are new photosensitizers with the potential for clinical application.