含碘白杨素衍生物的合成及其抗癌活性研究-药理学专业论文.docxVIP

PAGE PAGE 10 Synthesis and Anticancer Activities of Iodo-Chrysin Derivatives Abstract Objective: Chrysin, one kind of widely distributed flavonoids in nature, has been reported to have anticancer activity. However, the anticancer activity of chrysin was low because it was not or little absorbed in intestines. In order to search for anticancer substances with high efficacy, low toxicity and minimum side effects. We were interested in the synthesis and anticancer effect of iodo-chrysin derivatives. Methods: 6-iodo, 8-iodo and 6,8-di-iodo-chrysin derivatives were prepared by the reaction of ICl and I2 with the corresponding chrysin. 3-iodo-chrysin derivatives were synthesized from 3-iodo-4-methoxy-benzaldehyde. We tested their anticancer activities against leucocythemia (HL-60), colorectal adenocarcinoma (HT-29)and human gastric adenocarcinoma (SGC-7901) cells lines by MTT-Based Assay. Results: We have synthesized a series of iodo-chrysin derivatives , and these derivatives were tested for their in vitro anti-cancer activities against HL-60, HT-29 and SGC-7901 cell lines by MTT-Based Assay. It indicated that these closely related molecules displayed remarkable differences in cytotoxicity. Conclusion: Structure-activity relationships demonstrated that iodo-chrysin derivatives which introduced the iodine into A-ring or B-ring had stronger activity than chrysin against HL-60 tumor cells. However, the B-iodo-chrysin derivatives showed weaker activity than chrysin in rejecting HT-29 and SGC-7901 tumor cells. Key words: chrysin; iodonated; derivatives; anticancer activity Yi Liu Directed by Associate Prof. Xing Zheng Institute of Pharmacy and Pharmacology University of South China Hengyang, 421001 前 言 癌症是严重危害人类健康及生命的常见病，目前主要采用手术、化疗、放疗、 生物治疗等综合措施，但其疗效难以令人满意。因此，从不同途径寻找高效低毒 的抗癌药仍然是当务之急。随着对癌症研究的深入，天然产物在肿瘤治疗方面已 得到广泛的应用。从植物中寻找新型高效、低毒、不良反应少的抗癌药物或者以 天然活性成分为先导化合物，进行结构修饰或者结构改造，旨在合成生物利用率 高、生物活性强、毒性较低的靶分子已经成为当今新药研制的热点。据统计，在 1981 年至 2002 年进入市场的所有抗癌药物中，来源于天然产物的抗癌药物占 74%[1]。 黄酮类化合物广泛存