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β-柠檬醛异构体对白色念珠菌的抗真菌活性及其潜在靶标 ERG6。

Antifungal Activities of - Citral Isomers against with ERG6 as a Potential Target.

机构信息

College of Animal Science, Guizhou University, Guiyang 550025, China.

College of Animal Science and Veterinary Medicine, Henan Agricultural University, Zhengzhou 450002, China.

出版信息

Molecules. 2021 Jul 14;26(14):4263. doi: 10.3390/molecules26144263.

Abstract

causes ringworm worldwide. Citral (CIT), extracted from plants, is a monoterpene and naturally composed of geometric isomers neral (-citral) and geranial (-citral). CIT has promising antifungal activities and ergosterol biosynthesis inhibition effects against several pathogenic fungi. However, no study has focused on neral and geranial against , which hinders the clinical application of CIT. This study aimed to compare antifungal activities of neral and geranial and preliminarily elucidate their ergosterol biosynthesis inhibition mechanism against . Herein, the disc diffusion assays, cellular leakage measurement, flow cytometry, SEM/TEM observation, sterol quantification, and sterol pattern change analyses were employed. The results showed geranial exhibited larger inhibition zones ( < 0.01 or 0.05), higher cellular leakage rates ( < 0.01), increased conidia with damaged membranes ( < 0.01) within 24 h, more distinct shriveled mycelium in SEM, prominent cellular material leakage, membrane damage, and morphological changes in TEM. Furthermore, geranial possessed more promising ergosterol biosynthesis inhibition effects than neral, and both induced the synthesis of 7-Dehydrodesmosterol and Cholesta-5,7,22,24-tetraen-3β-ol, which represented marker sterols when ERG6 was affected. These results suggest geranial is more potent than neral against , and both inhibit ergosterol biosynthesis by affecting ERG6.

摘要

导致世界各地的癣病。柠檬醛(CIT)从植物中提取,是一种单萜烯,由几何异构体橙花醛(-CIT)和香叶醛(-CIT)组成。CIT 具有有前途的抗真菌活性和抑制麦角固醇生物合成的作用,对几种致病性真菌有效。然而,目前还没有研究集中在橙花醛和香叶醛对 ,这阻碍了 CIT 的临床应用。本研究旨在比较橙花醛和香叶醛的抗真菌活性,并初步阐明它们对 的麦角固醇生物合成抑制机制。在此,采用了圆盘扩散试验、细胞渗漏测量、流式细胞术、SEM/TEM 观察、甾醇定量和甾醇模式变化分析。结果表明,香叶醛在 24 小时内表现出更大的抑制区(<0.01 或 0.05)、更高的细胞渗漏率(<0.01)、更多细胞膜受损的分生孢子(<0.01)、在 SEM 中更明显的皱缩菌丝体、明显的细胞物质渗漏、膜损伤和 TEM 中的形态变化。此外,香叶醛比橙花醛具有更有前途的麦角固醇生物合成抑制作用,两者都诱导 7-去氢胆固醇和胆甾-5,7,22,24-四烯-3β-醇的合成,当 ERG6 受到影响时,这两种物质是标记甾醇。这些结果表明,香叶醛比橙花醛对 更有效,两者通过影响 ERG6 抑制麦角固醇生物合成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9c7/8304469/8b317cd43e3e/molecules-26-04263-g001.jpg

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