Macrosphelide, a novel inhibitor of cell-cell adhesion molecule .1. Taxonomy, fermentation, isolation and biological activities
Macrosphelide, a novel inhibitor of cell-cell adhesion molecule .1. Taxonomy, fermentation, isolation and biological activities
复制标题
DOI：
10.7164/antibiotics.48.1435
复制
发表时间：
1995-12-01
影响因子：
3.3
通讯作者：
Omura, S
中科院分区：
文献类型：
--
作者：
Hayashi, M;Kim, YP;Omura, S
微生物菌株FO-5050的发酵液具有较强的抗黏附活性。分离得到两个活性化合物，命名为大环螺内酯A和大环螺内酯B，确定其结构为16元大环内酯类抗生素，环结构中含有3个酯键。Macrosphelide A剂量依赖性地抑制HL-60细胞与脂多糖激活的HUVEC单层的黏附(IC50，3.5mM)，Macrosphelide B也抑制HL-60细胞的黏附，但程度较小(IC50，36mU M)。大环内酯A在1000mU g/m l和100 m u g/m l浓度下均未表现出抑菌和杀细胞活性。
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 mu M); macrosphelide B also inhibited HL-60 adhesion but to a lesser extent (IC50, 36 mu M). Macrosphelide A did not show any antimicrobial and cytocidal activities at the concentration of 1000 mu g/ml and 100 mu g/ml, respectively.