Hori Y, Abe Y, Ezaki M, Goto T, Okuhara M, Kohsaka M
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
J Antibiot (Tokyo). 1993 Jul;46(7):1055-62. doi: 10.7164/antibiotics.46.1055.
New non-steroidal estrogen-receptor antagonists, R1128 A, B, C and D, were isolated from the cultured broth of Streptomyces sp. No. 1128 by solvent extraction, silica gel chromatography, reverse phase chromatography and preparative HPLC. These compounds inhibited estrogen binding to its receptor. The IC50 values of R1128 A, B, C and D for partially purified rat uterine cytosol receptor were 1.1 x 10(-7) M, 1.2 x 10(-7) M, 2.6 x 10(-7) M and 2.7 x 10(-7) M, respectively.
新型非甾体雌激素受体拮抗剂R1128 A、B、C和D是从链霉菌属1128号菌株的培养液中，通过溶剂萃取、硅胶柱色谱、反相色谱和制备型高效液相色谱法分离得到的。这些化合物能抑制雌激素与其受体的结合。R1128 A、B、C和D对部分纯化的大鼠子宫胞质溶胶受体的半数抑制浓度（IC50）值分别为1.1×10⁻⁷ M、1.2×10⁻⁷ M、2.6×10⁻⁷ M和2.7×10⁻⁷ M。
