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硫内酯霉素,一种新型抗生素。IV. 小鼠体内的生物学特性及化疗活性

Thiolactomycin, a new antibiotic. IV. Biological properties and chemotherapeutic activity in mice.

作者信息

Miyakawa S, Suzuki K, Noto T, Harada Y, Okazaki H

出版信息

J Antibiot (Tokyo). 1982 Apr;35(4):411-9. doi: 10.7164/antibiotics.35.411.

Abstract

The new thiolactone antibiotic, thiolactomycin, is rapidly absorbed in rats when administered either orally or by intramuscular injection. A peak in concentration of the drug is reached in the blood and in various visceral organs within 15 minutes after administration. The concentration decreases rather rapidly and about 51-69% of the drug is excreted in urine during the first 24 hours. Though the in vitro effect of thiolactomycin is moderate, it effectively protected mice challenged intraperitoneally with several strains of S. marcescens and K. pneumoniae and more effective than carbenicillin in treating experimental acute urinary tracts infected with S. marcescens. Also, in mice whom immunodefense was decreased by treatment with cyclophosphamide, thiolactomycin was more effective than carbenicillin against S. marcescens challenge.

摘要

新型硫内酯抗生素硫乳霉素,经口服或肌肉注射给药后,在大鼠体内吸收迅速。给药后15分钟内,血液和各内脏器官中药物浓度达到峰值。浓度下降相当迅速,在最初24小时内约51 - 69%的药物经尿液排出。尽管硫乳霉素的体外作用中等,但它能有效保护经腹腔注射几种粘质沙雷氏菌和肺炎克雷伯菌菌株攻击的小鼠,在治疗实验性急性粘质沙雷氏菌感染的尿道方面比羧苄青霉素更有效。此外,在用环磷酰胺治疗使免疫防御能力下降的小鼠中,硫乳霉素在抵抗粘质沙雷氏菌攻击方面比羧苄青霉素更有效。

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