In this study, a novel photosensitizer meso-tetra (3-pyrrolidinomethyl-4-methoxyphenyl) chlorin (TPMC) was reported. It displays a characteristic long wavelength absorption peak at 656 nm and it shows a singlet oxygen quantum yield of 0.48. After light irradiation with 650 nm laser, it can kill Eca-109 and SMMC-7721 cells in vitro (25mW/cm², 1.2 to 3.6 J/cm²) and destroy Eca-109 tumor in nude mice (50mW/cm², 90 J/cm²). It has the perspective to be developed as a new anti-tumor drug in photodynamic therapy (PDT) photodiagnosis, and deserves further investigation.

Photodynamic therapy (PDT) represents a promising method for treatment of cancerous tumors. The chemical and physical properties of used photosensitizer (PS) play key roles in the treatment e±cacy. In this study, a novel PS, 5,10,15,20-tetrakis((5-dipropylamino)pentyl)-chlorin (TDPC) which displayed a characteristic long wavelength absorption peak at 650 nm were synthesized. It also shows a singlet oxygen generation rate of 4.257 min^-1. Generally, TDPC is localized in mitochondria and nucleus of cell. After light irradiation with 650 nm laser, it can kill many types of cell, in addition, TDPC–PDT can destroy ECA-109 tumor in nude mice and a necrotic scab was formed eventually. The expression levels of many genes which regulated cell growth and apoptosis were determined by RT-PCR following TDPC–PDT. The results showed that it either increased or decreased, among which, the expression level of TNFSF13, a member of tumor necrosis factor superfamily, increased significantly. In general, TDPC is an effective antitumor PS in vitro and in vivo and is worthy of further study as a new drug candidate. TNFSF13 will be an important molecular target for the discovery of new PSs.

研究了二氢卟吩e6-C15单甲酯在不同溶剂体系中的荧光光谱特性, 据此建立了检测血浆中二氢卟吩e6-C15单甲酯的荧光分析法。 首先, 通过比较分析二氢卟吩e6-C15单甲酯在甲醇、 乙醇、 丙酮、 乙腈、 磷酸盐缓冲液和水六种不同溶剂体系中的荧光光谱特征, 考察了溶剂体系对二氢卟吩e6-C15单甲酯荧光光谱特性的影响, 结果发现甲醇和乙腈是比较理想的溶剂体系, 而磷酸盐缓冲液优于水溶液。 通过进一步考察有机溶剂含量和溶液pH对二氢卟吩e6-C15单甲酯发射波长和荧光强度的影响, 结果表明pH 7.2 磷酸盐缓冲液-乙腈(3∶7)混合溶液中二氢卟吩e6-C15单甲酯荧光强度大、 性质稳定。 采用pH 7.2 磷酸盐缓冲液-乙腈(3∶7)混合溶液沉淀SD大鼠血浆蛋白, 选择498.00和664.05 nm作为激发波长和发射波长, 建立的SD大鼠血浆样品中二氢卟吩e6-C15单甲酯荧光分析法专属性好, 灵敏度高, 线性范围为0.50～50.00 μg·mL-1(R2≥ 0.999), 批内和批间精密度RSD均小于10%, 提取回收率大于90%。 该方法简便、 快速、 可靠, 成功地应用于二氢卟吩e6-C15单甲酯在SD大鼠体内的药代动力学研究。