19-[(1'S,4'R)-4'-羟基-1'-甲氧基-2'-氧代戊基]格尔德霉素，一种来自吸水链霉菌 17997 的天然格尔德霉素类似物。
19-[(1'S,4'R)-4'-Hydroxy-1'-methoxy-2'-oxopentyl]geldanamycin, a natural geldanamycin analogue from Streptomyces hygroscopicus 17997.
机构信息
Key Laboratory of Biotechnology of Antibiotics of Ministry of Health, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, People's Republic of China.
出版信息
J Nat Prod. 2013 May 24;76(5):969-73. doi: 10.1021/np4000679. Epub 2013 May 8.
A novel natural geldanamycin analogue was discovered in Streptomyces hygroscopicus 17997. Its 4,5-dihydro form was also identified in the gdmP gene disruption mutant of Streptomyces hygroscopicus 17997. The structures of the two compounds were determined to be 19-[(1'S,4'R)-4'-hydroxy-1'-methoxy-2'-oxopentyl]geldanamycin (1) and 19-[(1'S,4'R)-4'-hydroxy-1'-methoxy-2'-oxopentyl]-4,5-dihydrogeldanamycin (2), respectively, by extensive spectroscopic data analysis, including 2D NMR, modified Mosher's method, and electronic circular dichroism. Compared to geldanamycin, 1 and 2 showed increased water solubility and decreased cytotoxicity against HepG2 cells.
在吸水链霉菌 17997 中发现了一种新型天然格尔德霉素类似物。在吸水链霉菌 17997 的 gdmP 基因敲除突变体中也鉴定出其 4,5-二氢形式。通过广泛的光谱数据分析，包括 2D NMR、改良的莫舍尔法和电子圆二色谱，确定这两种化合物的结构分别为 19-[(1'S,4'R)-4'-羟基-1'-甲氧基-2'-氧代戊基]格尔德霉素（1）和 19-[(1'S,4'R)-4'-羟基-1'-甲氧基-2'-氧代戊基]-4,5-二氢格尔德霉素（2）。与格尔德霉素相比，1 和 2 具有更高的水溶性和更低的对 HepG2 细胞的细胞毒性。
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