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兰卡杀菌素类抗生素的抗肿瘤和免疫抑制活性:构效关系

Antitumor and immunosuppressive activities of lankacidin-group antibiotics: structure-activity relationships.

作者信息

Oostu K, Matsumoto T, Harada S, Kishi T

出版信息

Cancer Chemother Rep. 1975 Sep-Oct;59(5):919-28.

PMID:1148
Abstract

The antitumor and immunosuppressive activities of the lankacidin-group antibiotics were studied in mice. Seventeen of 29 newly prepared lankacidin-group antibiotics, including 14-derivatives of lankacidin C, lankacidinol, isolankacidinol, and lankacidinol 14-acetate, possessed considerable antitumor activity against ascites 6C3HED/OG lymphosarcoma. Comparative studies on the antitumor activity of lankacidin C and eight of its derivatives against L1210 leukemia and solid 6C3HED/OG lymphosarcoma demonstrated that replacement of the hydroxyl group at position 8 or 14 of lankacidin C by an acyloxy group potentiated antitumor activity. However, these modifications of lankacidin C resulted in reduction of the immunosuppressive activity.

摘要

在小鼠中研究了兰卡杀菌素类抗生素的抗肿瘤和免疫抑制活性。新制备的29种兰卡杀菌素类抗生素中的17种,包括兰卡杀菌素C的14种衍生物、兰卡杀菌醇、异兰卡杀菌醇和兰卡杀菌醇14 - 乙酸酯,对腹水型6C3HED/OG淋巴肉瘤具有相当的抗肿瘤活性。对兰卡杀菌素C及其8种衍生物对L1210白血病和实体6C3HED/OG淋巴肉瘤的抗肿瘤活性的比较研究表明,用酰氧基取代兰卡杀菌素C第8位或第14位的羟基可增强抗肿瘤活性。然而,兰卡杀菌素C的这些修饰导致免疫抑制活性降低。

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