文献类型：期刊文献

中文题名：异海松基水杨酰腙的合成及细胞毒性评价

英文题名：Synthesis and Cytotoxicity of Isopimaric-based Salicyloylhydrazone

作者：刘娟娟[1,2,3,4] 卢言菊[1,2,3,4,5] 陈玉湘[1,2,3,4,5] 赵振东[1,2,3,4,5]

第一作者：刘娟娟

机构：[1]中国林业科学研究院林产化学工业研究所;[2]生物质化学利用国家工程实验室;[3]国家林业局林产化学工程重点开放性实验室;[4]江苏省生物质能源与材料重点实验室;[5]中国林业科学研究院林业新技术研究所

年份：2017

卷号：37

期号：4

起止页码：35-39

中文期刊名：林产化学与工业

外文期刊名：Chemistry and Industry of Forest Products

收录：CSTPCD;;Scopus;北大核心:【北大核心2014】；CSCD:【CSCD2017_2018】；

基金：中国林科院中央级公益性科研院所基本科研业务费专项资金(CAFYBB2017QA018);国家自然科学基金资助项目(31370575)

语种：中文

中文关键词：酰腙;异海松酸;异海松基水杨酰腙;细胞毒性

外文关键词：acylhydrazone; isopimaric acid; isopimaric-based salicyloylhydrazone; cytotoxic

分类号：TQ351

摘要：以水杨醛和异海松酸为原料,合成了异海松基水杨酰腙,通过IR,~1H NMR和HR-TOF-MS对产物结构进行了鉴定,采用噻唑蓝(MTT)比色法研究了目标化合物对癌细胞及正常细胞的细胞毒性,并进一步对比了其与阳性药物紫杉醇的细胞毒性。结果表明:异海松基水杨酰腙对人体肝癌细胞HepG-2和前列腺癌细胞PC-3具有显著的细胞毒性,半数抑制浓度(IC_(50))值分别为6.50和9.25μmol/L,高于或接近于对照物紫杉醇(IC_(50)12.14和6.48μmol/L)的细胞毒性,同时异海松基水杨酰腙对人体正常的肝细胞L-02具有较低的细胞毒性,IC_(50)值为68.01μmol/L,远远低于对照品紫杉醇(IC_(50)4.02μmol/L)。抑制率和细胞形态变化分析表明,异海松基水杨酰腙对细胞增殖的抑制活性与剂量有关。
Isopimaric-based salicylhydrazone was synthesized by the reaction of isopimaric acid （IPA） and salicylaldehyde, and characterized by IR, JH NMR and HRMS. The cytotoxicities of target compound were evaluated against two human cancer cells （hepatoma cell HepG-2 and prostatic carcinoma cell PC-3） and a human normal liver cell L-02 in vitro using MTY method, which were compared with that of the positive drug taxol. The results showed that cytotoxic activity of isopimaric-based salieylhydrazone was similar or higher than that of taxol （IC50, 12. 14 and 6. 48 μmol/L） against HepG-2 and PC-3 cell lines, with ICs0 values 6. 50 and 9. 25 μmol/L, respectively. Moreover, isopimaric-based salicylhydrazone displayed hypotoxicity to L-02 cell, with IC50 value 68. 01 μmol/L, which was much lower than that of taxol （IC50, 4. 02 μmol/L）. The inhibitory rates and cell morphological changes showed that isopimaric-based salicylhydrazone significantly inhibited the cell proliferation in a dose-dependent manner.