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铜绿假单胞菌弹性蛋白酶特异性抑制剂2-巯基乙酰-L-苯丙氨酰-L-亮氨酸对兔眼实验性铜绿假单胞菌角膜炎的影响。

The effect of 2-mercaptoacetyl-L-phenylalanyl-L-leucine, a specific inhibitor of Pseudomonas aeruginosa elastase, on experimental Pseudomonas keratitis in rabbit eyes.

作者信息

Spierer A, Kessler E

出版信息

Curr Eye Res. 1984 Apr;3(4):645-50. doi: 10.3109/02713688409003066.

Abstract

The compound 2-mercaptoacetyl-L-phenylalanyl-L-leucine (HS-Ac-Phe-Leu) is a potent and specific inhibitor of Pseudomonas aeruginosa elastase, effectively inhibiting the elastase activity both, in vitro and within the rabbit cornea. This inhibitor was therefore evaluated as an adjunct to antibiotics (gentamicin) treatment in experimentally induced Pseudomonas keratitis in rabbits. Twenty eight hours after infection, the eyes that received both, gentamicin and HS-Ac-Phe-Leu showed significantly less corneal melting than those treated with the antibiotics alone, demonstrating the beneficial effect of the inhibitor. Forty eight hours after infection, the difference in clinical appearance between the two treatment groups diminished and was statistically insignificant. No adverse effects were noted in the eyes that received the inhibitor in spite of its frequent application. The protective effect of HS-Ac-Phe-Leu, seen on the first day of the experiment suggests further exploration of the therapeutic potential of this or other, similarly structured, specific and potent inhibitors of Pseudomonas elastase.

摘要

化合物2-巯基乙酰基-L-苯丙氨酰-L-亮氨酸(HS-Ac-Phe-Leu)是铜绿假单胞菌弹性蛋白酶的一种强效特异性抑制剂,在体外和兔角膜内均能有效抑制弹性蛋白酶的活性。因此,该抑制剂被评估为兔实验性铜绿假单胞菌角膜炎抗生素(庆大霉素)治疗的辅助药物。感染28小时后,同时接受庆大霉素和HS-Ac-Phe-Leu治疗的眼睛角膜融化程度明显低于单独使用抗生素治疗的眼睛,表明该抑制剂具有有益作用。感染48小时后,两个治疗组的临床外观差异减小且无统计学意义。尽管频繁应用该抑制剂,但在接受治疗的眼睛中未观察到不良反应。实验第一天观察到的HS-Ac-Phe-Leu的保护作用表明,需要进一步探索该抑制剂或其他结构类似、特异性强且强效的铜绿假单胞菌弹性蛋白酶抑制剂的治疗潜力。

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