摘要
目的从苏木提取物中寻找抗癌活性物质。方法采用不同溶剂从苏木中提取粗提物，液相色谱法测定各提取物中几种主要成分的含量；以人类膀胱癌T24细胞为靶细胞，采用锥虫蓝拒染法测定各提取物作用20、40、60、80、100min时对靶细胞的杀伤率；选择与杀伤率呈正相关性的主要组分，进行反复色谱层析，分离得到纯度达到98％以上的单体，采用核磁共振、质谱、红外等波谱学方法对该单体进行结构测定；以T24、人类卵巢癌SKOV3、小鼠肉瘤S180、小鼠肝癌H22细胞为靶细胞，以丝裂霉素、羟喜树碱为阳性对照药物，测定其对靶细胞抑制活性。结果粗提物中R12与细胞杀伤率呈正相关性（r100min=0．941，P〈0．001）；R12的主要成分是巴西木素，其在1．2mg／ml浓度下对T24、SKOV3、H22、5180细胞作用40min时的杀伤率分别达到90．89％、98．65％、99．82％和100．00％，杀伤作用明显优于阳性对照药物。结论巴西木素是苏木中主要抗癌活性物质之一。
Objective To search for the anticancer active substance from Caesalpinia sappan wood extractions. Methods Crude extracts were extracted from Caesalpinia sappan wood with different solvents. Liquid chromatography was applied to analyze the content of each essential component in the extraction fractions. Trypan blue exclusion test was performed to detect the growth suppression rate of human bladder carcinoma cell line T24 treated by the extraction fractions at different time course （20, 40, 60, 80, 100 min）.The main component positively correlated with the cell suppression rate was separated out using repeated chromatography, thus the anticancer active monomer was obtained, with purity over 98 %. The chemical constitution was determined using NMR （nuclear magnetic resonance）, mass spectrum and infrared spectrum methods. T24 cell line, human ovarian cancer cell line SKOV3, mice sarcoma S180 and hepatic carcinoma H22 cell were chosen as target subjects, with mitomycin, hydroxycamptothecin as positive control drug, the inhibitory activity of the monomer was tested by trypan blue chromophobia method. Results Among theextraction fractions, R12 has a positive correlation with the cell suppression rate （r100min=0.941, P〈0.001）. Brazilin is the key component in R12. The inhibition rate of brazilin could reach 90.89 %, 98.65 %, 99.82 % and 100.00 % on T24, SKOV3, S180 and H22 respectively in 40 rain at the concentration of 1.2 mg/ml, and its effect is much superior to that of the control drug mitomycin and hydroxycamptothecin. Conclusion Brazilin is one of the essential anticancer principles in Caesalpinia sappan wood.
出处
《肿瘤研究与临床》
CAS
2012年第3期157-160,共4页
Cancer Research and Clinic
关键词
苏木
抗癌
活性成分
巴西木素
Caesalpinia sappan
Anticancer
Active principle
Brazilin
