海洋小单孢菌产生的抗肿瘤新化合物rakicidin B1（英文）  

Rakicidin B1, a new rakicidin analogue with antitumor activities from marine Micromonospora sp.

作　　者：林风[1] 王传喜[1] 江宏磊[1] 周剑[1] 赵薇[1] 陈晓明[1] 方东升[1] 连云阳[1] 江红[1] 

机构地区：[1]福建省微生物研究所,福建省新药(微生物)筛选重点实验室,福州350007

出　　处：《中国抗生素杂志》2016年第7期510-515,共6页Chinese Journal of Antibiotics

基　　金：福建省化药技术重大研发平台项目(No.2014Y2001);973项目(No.2012CBA01303);福建省科技计划项目(No.2015R1009-1和No.2016R1009-1);福建省海洋高新项目(No.闽海洋高新[2015]32号);厦门南方海洋研究中心项目(No.厦海渔合[2015]26号)

摘　　要：从海洋小单孢菌FIM02-523的发酵液中分离到一个新的缩肽类化合物rakicidin B1(1)及两个已知化合物rakicidin A(2)和rakicidin B(3)。通过一维、二维核磁图谱、红外光谱、紫外光谱和高分辨质谱确定了3个化合物的结构。测定了3个化合物对HCT-8、MGC803、A549、A375、Hep G2和CASKI 5种人肿瘤细胞株的细胞毒活性,结果显示化合物1、2和3对这些肿瘤细胞株均具有显著的抑制活性(对这5个肿瘤细胞株,化合物1的IC50值分别为0.341,0.121,0.394,0.066和2.516μg/m L;化合物2的IC50值分别为0.731,0.991,0.226,0.040和0.576μg/m L;化合物3的IC_(50)值分别为0.347,0.104,0.216,0.041和2.239μg/m L),化合物1和3的抗肿瘤活性相当。A new depsipeptide, Rakicidin B1 （1）, together with two known rakicidin A （2） and rakicidin B （3）, were isolated from the fermentation broth of marine Micromonospora sp. FIM02-523. The structures of all the compounds were determined by extensive spectroscopic method such as 1D and 2D NMR, IR, UV, and HR-ESI-MS. All the compounds were tested for the antitumor activities against HCT-8, MGC803, A549, A375, HepG2 and CASKI human tumor cell lines. Results indicated that compound 1, 2 and 3 exhibited significant cytotoxicities to these tumor cell lines （To these 5 tumor cell lines, the IC50 values of compound 1 were 0.341, 0.121, 0.394, 0.066 and 2.516μg/mL, respectively; the IC50 values of compound 2 were 0.731, 0.991, 0.226, 0.040 and 0.576μg/mL, respectively; the IC50 values of compound 3 were 0.347, 0.104, 0.216, 0.041 and 2.239μg/mL, respectively）. Compound 1 and 3 showed similar antitumor activities.

关 键 词：小单孢菌 Rakicidins 缩肽 抗肿瘤 

分 类 号：R979.1[医药卫生—药品]