2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway

IMR OpenIR

	2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway
其他题名	2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway
	Liang Rongmei 1; Cao Yongbing 1; Fan Kaihua 2; Xu Yi 1; Gao Pinghui 1; Zhou Youjun 3; Dai Baodi 4; Tan Yonghong 2; Wang Shihua 2; Tang Hui 3; Liu Hongtao 5; Jiang Yuanying 1
	2009
发表期刊	ACTA PHARMACOLOGICA SINICA
ISSN	1671-4083
卷号	30 期号:12 页码:1709-1716
摘要	Aim: To investigate the action mechanism of a novel chemical structural aminotetralin derivate, 2-Amino-Nonyl-6-Methoxyl-Tetralin Muriate (10b), against Candida albicans (C albicans) in the ergosterol biosynthetic pathway.
其他摘要	Aim: To investigate the action mechanism of a novel chemical structural aminotetralin derivate, 2-Amino-Nonyl-6-Methoxyl-Tetralin Muriate (10b), against Candida albicans ( C albicans ) in the ergosterol biosynthetic pathway. Methods: Antifungal susceptibility test of 10b was carried out using broth microdilution method, the action mechanism of 10b against C albicans was investigated by GC-MS spectrometry and real-time RT-PCR assay, and cytotoxicity of 10b in vitro was assessed by MTS Results: 10b reduced the ergosterol content markedly, and the 50% ergosterol content inhibitory concentration (ECIC 50 value) was 0.08 μg erg24 strain, the content of ergosta-8,14,22-trienol in 10b-grown cells was much higher than that in erg24 strain. Real-time RT-PCR assay revealed a global upregulation of sterol metabolism genes. In addition, the 50% inhibitory concentration (IC 50 value) of 10b was 11.30 μg Conclusion: 10b possessed a mode of action different from that of azoles and morpholines, whose targets were sterol C-14 reductase (encoded by ERG24 gene) and sterol C-5 desaturase (encoded by ERG3 ) related enzyme. Although 10b seemed to reduce MTS 50 value for mammalian cells was much higher than 50% minimum inhibitory concentration (MIC 50 ) value for C albicans . This indicates that the formulation is preliminarily safe and warrants further study for possible human applications.
关键词	CANDIDA-ALBICANS AMPHOTERICIN-B LANOSTEROL 14-ALPHA-DEMETHYLASE ANTIFUNGAL ACTIVITIES MOLECULAR DOCKING IN-VITRO FLUCONAZOLE RESISTANCE SYSTEMS DUBLINIENSIS Candida albicans sterol C-14 reducase ergosterol 2-amino-nonyl-6-methoxyl-tetralin muriate
收录类别	CSCD
语种	英语
资助项目	[National Natural Science Foundation of China]
CSCD记录号	CSCD:3798143
引用统计	被引频次：1[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/157917
专题	中国科学院金属研究所
作者单位	1.安徽肥东花生原种场 2.Gen Hosp Chengdu Mil Command Reg, Department Pharm, Chengdu 610083, Peoples R China 3.Second Mil Med University, Sch Pharm, Dept Med Chem, Shanghai 200433, Peoples R China 4.中国科学院金属研究所 5.Capital Med University, Beijing Stomatol Hosp, Dept Pharm, Beijing 100050, Peoples R China
推荐引用方式 GB/T 7714	Liang Rongmei,Cao Yongbing,Fan Kaihua,et al. 2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway[J]. ACTA PHARMACOLOGICA SINICA,2009,30(12):1709-1716.
APA	Liang Rongmei.,Cao Yongbing.,Fan Kaihua.,Xu Yi.,Gao Pinghui.,...&Jiang Yuanying.(2009).2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway.ACTA PHARMACOLOGICA SINICA,30(12),1709-1716.
MLA	Liang Rongmei,et al."2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway".ACTA PHARMACOLOGICA SINICA 30.12(2009):1709-1716.