Onoda T, Isshiki K, Takeuchi T, Tatsuta K, Umezawa K
Institute of Microbial Chemistry, Tokyo, Japan.
Drugs Exp Clin Res. 1990;16(6):249-53.
Lavendustin A is a novel microbial secondary metabolite that strongly inhibits tyrosine kinase in vitro. But, since it was found that it did not inhibit tyrosine kinase in situ, possibly because of its poor penetration into the cells, the authors therefore synthesized a methyl ester derivative of lavendustin A. Lavendustin A methyl ester inhibited autophosphorylation and internalization of epidermal growth factor receptor in cultured A431 cells. It also inhibited phosphatidylinositol kinase in vitro and phosphatidylinositol turnover in situ.
拉文达斯汀A是一种新型微生物次级代谢产物，在体外能强烈抑制酪氨酸激酶。但是，由于发现它在原位不能抑制酪氨酸激酶，可能是因为其细胞穿透性差，因此作者合成了拉文达斯汀A的甲酯衍生物。拉文达斯汀A甲酯在培养的A431细胞中抑制表皮生长因子受体的自磷酸化和内化。它在体外还能抑制磷脂酰肌醇激酶，并在原位抑制磷脂酰肌醇周转。
