S-烯丙基-L-半胱氨酸衍生物对内质网应激诱导的细胞毒性的神经保护作用与钙蛋白酶抑制无关。

Neuroprotective effect of S-allyl-l-cysteine derivatives against endoplasmic reticulum stress-induced cytotoxicity is independent of calpain inhibition.

作者信息

Imai Toru, Kosuge Yasuhiro, Saito Hiroaki, Uchiyama Taketo, Wada Taira, Shimba Shigeki, Ishige Kumiko, Miyairi Shinichi, Makishima Makoto, Ito Yoshihisa

机构信息

Laboratory of Pharmacology, School of Pharmacy, Nihon University, 7-7-1 Narashinodai, Funabashi-shi, Chiba 274-8555, Japan.

Laboratory of Bio-organic Chemistry, School of Pharmacy, Nihon University, 7-7-1, Narashinodai, Funabashi, Chiba 274-8555, Japan.

出版信息

J Pharmacol Sci. 2016 Mar;130(3):185-8. doi: 10.1016/j.jphs.2016.03.004. Epub 2016 Mar 14.

DOI:10.1016/j.jphs.2016.03.004

PMID:27032909

Abstract

S-allyl-l-cysteine (SAC) is known to have neuroprotective properties. We synthesized various SAC derivatives and tested their effects on endoplasmic reticulum stress-induced neurotoxicity in cultured hippocampal neurons (HPNs). Among the compounds tested, S-propyl-l-cysteine (SPC) exhibited the strongest neuroprotective activity in HPNs, followed by S-ethyl-l-cysteine (SEC) and S-methyl-l-cysteine (SMC). Unlike SAC and SMC, SPC and SEC did not have inhibitory activity on μ-calpain, suggesting that the mechanism underlying the protective activity of SPC and SEC differs from that of SAC.

摘要

已知S-烯丙基-L-半胱氨酸（SAC）具有神经保护特性。我们合成了各种SAC衍生物，并测试了它们对培养的海马神经元（HPNs）内质网应激诱导的神经毒性的影响。在所测试的化合物中，S-丙基-L-半胱氨酸（SPC）在HPNs中表现出最强的神经保护活性，其次是S-乙基-L-半胱氨酸（SEC）和S-甲基-L-半胱氨酸（SMC）。与SAC和SMC不同，SPC和SEC对μ-钙蛋白酶没有抑制活性，这表明SPC和SEC的保护活性机制与SAC不同。