新型细菌卟吩类衍生物的合成及抗肿瘤活性研究

Study on Synthesis and Antitumor Activity of Novel Bacteriochlorin Derivative

关键词:  细菌卟吩  合成  光动力治疗  抗肿瘤

Key words:  bacteriochlorin  synthesis  photodynamic therapy  antitumor

摘要:

目的 设计、合成新型细菌卟吩类衍生物，并研究其抗肿瘤效果。方法 以细菌卟吩类化合物为原料，经还原、溴化后与2-[4-(羟甲基)苯氧基]乙酸甲酯进行醚化，随后水解得到目标化合物。采用NCI-H460 BALB/c裸鼠移植瘤模型，检测药物在组织中的分布，利用光动力治疗法对目标化合物的抗肿瘤效果进行了研究。结果 合成了1个全新结构的细菌卟吩类衍生物，结构经¹H-NMR、¹³C-NMR、MS和UV确证，目标化合物具有较好的组织分布性，对肿瘤细胞的生长具有较好的抑制作用。结论 细菌卟吩类衍生物结构中引入亲水性基团后，组织选择性及抗肿瘤效果得到了改善，值得深入研究。

Abstract:

OBJECTIVE To design and synthesize a novel bacteriochlorin derivative and study its antitumor effect. METHODS The target compound was synthesized from bacteriochlorin derivative via reduction, bromination after reacted with methyl 2-[4-(hydroxymethyl)phenoxy]acetate via etherification and hydrolysis. NCI-H460 BALB/c nude mice model was used to detect the distribution of drugs in various tissues, the antitumor effect of the target compound was studied by photodynamic therapy. RESULTS A novel bacteriochlorin derivative was synthesized, and structure was characterized by ¹H-NMR, ¹³C-NMR, MS and UV. The target compound expressed fine distribution in tissues, and it had a great inhibit effect on the growth of tumor cells. CONCLUSION After introducing hydrophilic group into the structure of bacteriochlorin derivative, the tissue selectivity and antitumor effect has been improved, which is worthy of further study.