联吡啶硫醚及相关化合物的生物学特性。

Biological properties of dipyridyl sulphides and related compounds.

作者信息

Boduszek B, Wieczorek J S, Mordarski M, Wieczorek J

出版信息

Arch Immunol Ther Exp (Warsz). 1985;33(2):331-8.

Abstract

Antibacterial, antifungal and antitumor activity of 15 newly synthetized compounds were investigated in vitro. These compounds were mainly 1-[4-pyridyl]-pyridinium salts, dipyridyl sulphides and corresponding sulphones. Antitumor activity was evaluated in a model of leukemia L1210, P388, Sarcoma 180, Ehrlich carcinoma, NK-lymphoma and melanoma B16. None of the compounds investigated, even at the concentration of 100 micrograms/ml, appeared to influence Gram-negative bacteria. However, at the concentration as low as 1.0 microgram/ml, three of them (No. III, VI and VII) strongly inhibited the growth of Gram positive bacteria and fungi. The compounds did not prolong the survival time of Sarcoma 880 leukemia L1210 or P388--bearing mice. Few of the compounds examined exerted marked antitumor effect on Ehrlich carcinoma and NK-lymphoma--compounds No. I and XV inhibited the growth of these tumors by ca. 70%. The strongest inhibitory effect on melanoma B16 was observed with compound No. XV, the effect being dose-dependent.

摘要

对15种新合成化合物的抗菌、抗真菌和抗肿瘤活性进行了体外研究。这些化合物主要是1-[4-吡啶基]-吡啶鎓盐、二吡啶硫醚及相应的砜。在白血病L1210、P388、肉瘤180、艾氏癌、NK淋巴瘤和黑色素瘤B16模型中评估了抗肿瘤活性。所研究的化合物中，即使在浓度为100微克/毫升时，似乎也对革兰氏阴性菌没有影响。然而，在低至1.0微克/毫升的浓度下，其中三种化合物（III号、VI号和VII号）强烈抑制革兰氏阳性菌和真菌的生长。这些化合物并未延长荷肉瘤880、白血病L1210或P388小鼠的存活时间。所检测的化合物中很少有对艾氏癌和NK淋巴瘤有显著抗肿瘤作用的——I号和XV号化合物对这些肿瘤的生长抑制约70%。观察到XV号化合物对黑色素瘤B16的抑制作用最强，且该作用呈剂量依赖性。