Nakayama O, Yagi M, Tanaka M, Kiyoto S, Uchida I, Hashimoto M, Okuhara M, Kohsaka M
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
J Antibiot (Tokyo). 1990 Nov;43(11):1394-402. doi: 10.7164/antibiotics.43.1394.
WS-7528, produced by Streptomyces sp. No. 7528, was extracted from cultured broth, purified by solvent extraction followed by chromatography on silica gel and then isolated as pale yellow powder (C16H14O5, mp 95-98 degrees C). WS-7528 inhibited estrogen binding to its receptor protein in rat uterine cytosol. The IC50 value of WS-7528 for partially purified rat uterine cytosol receptor was 5.7 x 10(-8) M. This compound was found to induce the growth of the estrogen dependent cell line MCF-7. WS-7528 was tested orally and subcutaneously in immature rats to confirm its effect on the growth of the uterus. WS-7528 has also weak anti-inflammatory activity on the carrageenin paw edema of the rat model.
WS - 7528由链霉菌7528号菌株产生，从培养液中提取，经溶剂萃取后用硅胶柱色谱法纯化，然后分离得到淡黄色粉末（C16H14O5，熔点95 - 98摄氏度）。WS - 7528可抑制雌激素与大鼠子宫胞质溶胶中其受体蛋白的结合。WS - 7528对部分纯化的大鼠子宫胞质溶胶受体的IC50值为5.7×10（-8）M。发现该化合物可诱导雌激素依赖性细胞系MCF - 7生长。对未成熟大鼠进行了WS - 7528的口服和皮下试验，以确认其对子宫生长的影响。WS - 7528对大鼠角叉菜胶足肿胀模型也有微弱的抗炎活性。
