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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 To investigate two novel photosensitizers, 5-amino-1-pentosesulfobetaine (PENSHB) and 15-deacetyl 13-amino-l-propanesulfonate derivatives. (DPROHB) Absorption in human gastric adenocarcinoma BGC-823 cells. Methods Human gastric adenocarcinoma BGC-823 cells were incubated with PENSHB and DPROHB at a concentration of 4 μM for 0, 0.5, 1, 2, 4 and 8 h, respectively. Fluorescence assay was used to determine the content of photosensitizer in the cells and the standard curve of concentration-fluorescence intensity was measured. Converted to photosensitizer concentration, plot the incubation time-cell content for each photosensitizer. The BGC-823 cells were incubated with two photosensitizers with concentrations of 0.5, 1, 2, 4 and 8 μM for 4 h. Then the intracellular fluorescence intensity was measured and the incubation concentration-cell content curve of the photosensitizer was plotted. Results The uptake of PENSHB and DPROHB in BGC-823 cells increased with the incubation time, and the changes were similar. The content of the two new photosensitizers increased rapidly in 1 h after incubation and reached the plateau at 4 h. In the concentration range of this experiment, the cell uptake of PENSHB and DPROHB increased with the increase of the incubation concentration. The linear relationship was basically linear and the uptrend was similar. The intracellular absorption of both depends on the incubation time and incubation concentration. Conclusion Both PENSHB and DPROHB derivatives of the new type of hypothallicin can improve the water solubility and photodynamic effect, and have good cell absorption properties. It is a new type of photosensitizer with potential applications.