罗米肽 A 和 B，两种从 Chromobacterium violaceum No.968 中分离得到的新型罗米司汀衍生物及其体外抗肿瘤活性。
Romipeptides A and B, two new romidepsin derivatives isolated from Chromobacterium violaceum No.968 and their antitumor activities in vitro.
机构信息
State Key Lab of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai 200000, China.
State Key Lab of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai 200000, China.
出版信息
Chin J Nat Med. 2019 Feb;17(2):155-160. doi: 10.1016/S1875-5364(19)30018-4.
Romipeptides A and B (1 and 2), two new romidepsin derivatives, and three known compounds, chromopeptide A (3), romidepsin (4) and valine-leucine dipeptide (5) were isolated from the fermentation broth of Chromobacterium violaceum No. 968. Their structures were elucidated by interpretation of their UV, HR-ESI-MS and NMR spectra. The absolute configuration of compound 1 and 2 were established by single crystal X-ray diffraction analysis. Compounds 1-5 were evaluated for their anti-proliferative activities against three human cancer cell lines, SW620, HL60, and A549. The results showed most of these compounds exhibited antitumor activities in vitro, in which compound 2 displayed potent cytotoxicity to SW620, HL60 and A549 cell lines, with IC of 12.5, 6.7 and 5.7 nmol·L, respectively.
从紫色色杆菌 No.968 的发酵液中分离得到了两个新的罗米肽衍生物罗米肽 A 和 B（1 和 2）以及三个已知化合物，色肽 A（3）、罗米肽（4）和缬氨酸-亮氨酸二肽（5）。通过对其 UV、HR-ESI-MS 和 NMR 谱的解析，确定了它们的结构。通过单晶 X 射线衍射分析确定了化合物 1 和 2 的绝对构型。对化合物 1-5 进行了抗增殖活性评价，针对三种人癌细胞系 SW620、HL60 和 A549。结果表明，这些化合物大多数在体外均具有抗肿瘤活性，其中化合物 2 对 SW620、HL60 和 A549 细胞系显示出较强的细胞毒性，IC 分别为 12.5、6.7 和 5.7 nmol·L。
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