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2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway
Alternative Title2-Amino-nonyl-6-methoxyl-tetralin muriate inhibits sterol C-14 reductase in the ergosterol biosynthetic pathway
Liang Rongmei1; Cao Yongbing1; Fan Kaihua2; Xu Yi1; Gao Pinghui1; Zhou Youjun3; Dai Baodi4; Tan Yonghong2; Wang Shihua2; Tang Hui3; Liu Hongtao5; Jiang Yuanying1
2009
Source PublicationACTA PHARMACOLOGICA SINICA
ISSN1671-4083
Volume30Issue:12Pages:1709-1716
AbstractAim: 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.
Other AbstractAim: 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.
KeywordCANDIDA-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
Indexed ByCSCD
Language英语
Funding Project[National Natural Science Foundation of China]
CSCD IDCSCD:3798143
Citation statistics
Cited Times:1[CSCD]   [CSCD Record]
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/157917
Collection中国科学院金属研究所
Affiliation1.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
Recommended Citation
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.
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