放线菌素A新型磺酸衍生物的体内活性

In vivo activity of novel sulphonic derivatives of distamycin A.

作者信息

Sola F, Biasoli G, Pesenti E, Farao M, Della Torre P, Mongelli N, Grandi M

机构信息

Farmitalia Carlo Erba, Erbamont Group, Research and Development Center, Nerviano, Italy.

出版信息

EXS. 1992;61:459-62. doi: 10.1007/978-3-0348-7001-6_77.

DOI:10.1007/978-3-0348-7001-6_77

PMID:1377572

Abstract

Solid tumor growth can be modulated through inhibition of vascularization elicited by angiogenic factors. With the objective to complex these factors, new derivatives of distamycin A were synthesized and evaluated in vitro [1] and in vivo for their ability, after i.v. administration, to inhibit bFGF-induced vascularization and the growth of M5076 murine reticulosarcoma implanted i.m. The tested compounds were able to block angiogenesis with inhibition values ranging between 70-100%. Moreover, they were found to be capable of inducing tumor inhibition with values ranging between 40% and 95% at non-toxic doses.

摘要

实体瘤的生长可通过抑制血管生成因子引发的血管生成来调节。为了综合这些因子，合成了新的放线菌素A衍生物，并在体外[1]和体内评估了它们在静脉给药后抑制碱性成纤维细胞生长因子诱导的血管生成以及抑制皮下植入的M5076小鼠网状细胞肉瘤生长的能力。测试的化合物能够阻断血管生成，抑制率在70%-100%之间。此外，发现在无毒剂量下，它们能够诱导肿瘤抑制，抑制率在40%至95%之间。