Hayashi M, Kim Y P, Hiraoka H, Natori M, Takamatsu S, Kawakubo T, Masuma R, Komiyama K, Omura S
The Kitasato Institute, Tokyo, Japan.
J Antibiot (Tokyo). 1995 Dec;48(12):1435-9. doi: 10.7164/antibiotics.48.1435.
Potent anti-adherent activity was detected in fermentation extracts of microbial strain FO-5050. Active compounds designated macrosphelide A and B were isolated and the structure was determined to be 16-membered macrolide antibiotics possessing three ester bonds in the ring structure. Macrosphelide A dose-dependently inhibited the adhesion of HL-60 cells to LPS-activated HUVEC monolayer (IC50, 3.5 microM); macrophelide B also inhibited HL-60 adhesion but to a lesser extent (IL50, 36 microM). Macrosphelide A did not show any antimicrobial and cytocidal activities at the concentration of 1000 micrograms/ml and 100 micrograms/ml, respectively.
在微生物菌株FO - 5050的发酵提取物中检测到了强大的抗黏附活性。分离出了名为大环球霉素A和B的活性化合物，其结构被确定为在环结构中具有三个酯键的16元大环内酯类抗生素。大环球霉素A剂量依赖性地抑制HL - 60细胞与LPS激活的人脐静脉内皮细胞单层的黏附（IC50为3.5微摩尔）；大环球霉素B也抑制HL - 60细胞黏附，但程度较小（IL50为36微摩尔）。大环球霉素A在浓度分别为1000微克/毫升和100微克/毫升时未表现出任何抗菌和杀细胞活性。
