四个新的Angucycline类抗生素的研究.pdfVIP

四个新的Angucycline 类抗生素的研究 * 任晓，路新华 ，可爱兵，郑智慧，林洁，朱京童，范玉玲，丁彦博，蒋沁，张华 （微生物 药物国家研究工程中心,华北制药股份公司新药研究开发中心，石家庄，河北050015） 摘要：目的 筛选新的具有抗癌活性的抗生素。方法 在体外利用 MTT 比色法筛选其代谢产物对结肠癌细 胞系SW620 具有增殖抑制活性的菌株。活性菌株的发酵产物进行分离纯化获得活性化合物, 通过对它们的 综合光谱数据分析确定其化学结构。并且对活性化合物进行进一步的抗癌活性评价。结果 从活性菌株 Streptomyces sp. N05WA963 的发酵产物中分离得到 4 个 Angucycline 类的新结构化合物, 命名为 N05WA963A(1) 、B(2) 、C(3) 和 D(4), 它们均对结肠癌细胞系 SW620 、白血病细胞系 K-562 和乳癌细胞 系MDA-MB-231 显示较强的增殖抑制活性。 结论 发现了N05WA963A(1) 、B(2) 、C(3) 和 D(4)共4 个新 结构化合物，它们在体外对一系列癌细胞具有较强的细胞毒活性。 关键词: angucycline 类抗生素; 链霉菌 sp.N05WA963; 结构解析; 抗癌 Studies on four novel members of angucycline group antibiotics * REN Xiao, LU Xin-hua , KE Ai-bing, ZHENG Zhi-hui, LIN Jie, Zhu Jing-tong, FAN Yu-ling, DING Yan-bo, Jiang Qin, ZHANG Hua (National Microbial Medicine Engineering and Research Center, New Drug Research and Development Center of North China Pharmaceutical Co. Ltd, Shijiazhuang ,Hebei 050015, China) ABSTRACT: OBJECTIVE To screen novel anticancer antibiotics. METHODS In vitro the MTT colorimetry was used to pick out the strain whose metabolites exhibited antiproliferative effect on colon cancer cell line SW620. The culture broth of the strain with active principle was purified to get active compounds. The structures of the compounds were elucidated on the basis of comprehensive spectral data analysis. In the sequel more anticancer activity evaluations on the compounds were investigated. RESULTS From the culture broth of Streptomyces sp. N05WA963, the active strain, four novel members of angucycline family named N05WA963A(1), B(2), C(3) and D(4) were isolated. All these compounds showed significant antiproliferative effect on colon cancer cell line SW620, leu