新型三唑类抗真菌药物依氟康唑的作用机制。
Mechanism of action of efinaconazole, a novel triazole antifungal agent.
机构信息
Central Research Laboratories, Kaken Pharmaceutical Co, Ltd, Kyoto, Japan.
出版信息
Antimicrob Agents Chemother. 2013 May;57(5):2405-9. doi: 10.1128/AAC.02063-12. Epub 2013 Mar 4.
Abstract
The mechanism of action of efinaconazole, a new triazole antifungal, was investigated with Trichophyton mentagrophytes and Candida albicans. Efinaconazole dose-dependently decreased ergosterol production and accumulated 4,4-dimethylsterols and 4α-methylsterols at concentrations below its MICs. Efinaconazole induced morphological and ultrastructural changes in T. mentagrophytes hyphae that became more prominent with increasing drug concentrations. In conclusion, the primary mechanism of action of efinaconazole is blockage of ergosterol biosynthesis, presumably through sterol 14α-demethylase inhibition, leading to secondary degenerative changes.
摘要
新型三唑类抗真菌药依氟康唑的作用机制通过须毛癣菌和白色念珠菌进行了研究。依氟康唑剂量依赖性地降低麦角固醇的产生，并在低于 MIC 的浓度下积累 4,4-二甲基固醇和 4α-甲基固醇。依氟康唑诱导须毛癣菌菌丝的形态和超微结构发生变化，随着药物浓度的增加，变化更加明显。总之，依氟康唑的主要作用机制是阻断麦角固醇生物合成，可能通过抑制甾醇 14α-去甲基酶，导致次级退行性变化。
相似文献
1
Mechanism of action of efinaconazole, a novel triazole antifungal agent.新型三唑类抗真菌药物依氟康唑的作用机制。
Antimicrob Agents Chemother. 2013 May;57(5):2405-9. doi: 10.1128/AAC.02063-12. Epub 2013 Mar 4.
2
Biochemical changes associated with the antifungal action of the triazole ICI 153,066 on Candida albicans and Trichophyton quinckeanum.
FEMS Microbiol Lett. 1991 Apr 15;63(2-3):127-31. doi: 10.1016/0378-1097(91)90074-k.
3
A new triazole, voriconazole (UK-109,496), blocks sterol biosynthesis in Candida albicans and Candida krusei.一种新型三唑类药物伏立康唑（UK-109,496）可阻断白色念珠菌和克鲁斯念珠菌中的甾醇生物合成。
Antimicrob Agents Chemother. 1997 Nov;41(11):2492-6. doi: 10.1128/AAC.41.11.2492.
4
Biochemical mode of action and enantiomeric selectivity of SDZ 89-485, a new triazole antimycotic.新型三唑类抗真菌药SDZ 89 - 485的生化作用模式及对映体选择性
J Med Vet Mycol. 1990;28(5):385-94. doi: 10.1080/02681219080000491.
5
The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis.新型唑类药物R126638是白色念珠菌、毛癣菌属和犬小孢子菌中麦角甾醇合成的选择性抑制剂。
Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8. doi: 10.1128/AAC.48.9.3272-3278.2004.
6
Evaluation of drug susceptibility test for Efinaconazole compared with conventional antifungal agents.棘白菌素类药物敏感性试验与传统抗真菌药物的比较评估。
Mycoses. 2019 Mar;62(3):291-297. doi: 10.1111/myc.12870. Epub 2018 Dec 17.
7
Dodonaea viscosa var angustifolia derived 5,6,8-trihydroxy-7,4' dimethoxy flavone inhibits ergosterol synthesis and the production of hyphae and biofilm in Candida albicans.窄叶黄麻来源的 5,6,8-三羟基-7,4'-二甲氧基黄酮抑制白念珠菌麦角固醇合成及菌丝和生物膜形成。
J Ethnopharmacol. 2020 Sep 15;259:112965. doi: 10.1016/j.jep.2020.112965. Epub 2020 May 13.
8
Efinaconazole (Jublia) for the treatment of onychomycosis.依氟鸟氨酸（Jublia）治疗甲真菌病。
Expert Rev Anti Infect Ther. 2014 Jul;12(7):743-52. doi: 10.1586/14787210.2014.919852. Epub 2014 May 22.
9
Inhibitory effect of a new mycotic agent, piritetrate on ergosterol biosynthesis in pathogenic fungi.新型抗真菌药吡立四环素对致病真菌麦角固醇生物合成的抑制作用
J Med Vet Mycol. 1989;27(1):17-25. doi: 10.1080/02681218980000031.
10
Comparison of in vitro antifungal activities of efinaconazole and currently available antifungal agents against a variety of pathogenic fungi associated with onychomycosis.比较依氟康唑与目前可用的抗真菌药物对各种与甲真菌病相关的致病性真菌的体外抗真菌活性。
Antimicrob Agents Chemother. 2013 Apr;57(4):1610-6. doi: 10.1128/AAC.02056-12. Epub 2013 Jan 14.
引用本文的文献
1
Antifungal Selection for the Treatment of Onychomycosis: Patient Considerations and Outcomes.治疗甲癣的抗真菌药物选择：患者考量与治疗结果
Infect Drug Resist. 2024 Mar 4;17:819-843. doi: 10.2147/IDR.S431526. eCollection 2024.
2
Evaluation of the antidermatophytic activity of potassium salts of N-acylhydrazinecarbodithioates and their aminotriazole-thione derivatives.评价 N-酰基腙二硫代羧酸酯及其氨基三唑硫酮衍生物的抗真菌活性。
Sci Rep. 2024 Feb 12;14(1):3521. doi: 10.1038/s41598-024-54025-9.
3
The Plant Defensin Ppdef1 Is a Novel Topical Treatment for Onychomycosis.植物防御素Ppdef1是一种治疗甲癣的新型局部用药。
J Fungi (Basel). 2023 Nov 17;9(11):1111. doi: 10.3390/jof9111111.
4
Evaluation of Inhibitory Effect and Mechanism of Euphorbia Factor L against .评价飞扬草因子 L 的抑制作用及机制
Molecules. 2023 Mar 26;28(7):2958. doi: 10.3390/molecules28072958.
5
Sphingosine as a New Antifungal Agent against and spp.鞘氨醇作为一种新型抗真菌剂，可对抗 和 。
Int J Mol Sci. 2022 Dec 7;23(24):15510. doi: 10.3390/ijms232415510.
6
The Tricalbin-Family Endoplasmic Reticulum-Plasma Membrane Tethering Proteins Attenuate ROS-Involved Caspofungin Sensitivity in Candida albicans.三钙结合蛋白家族内质网-质膜连接蛋白降低白念珠菌中活性氧（ROS）相关卡泊芬净敏感性。
Microbiol Spectr. 2022 Dec 21;10(6):e0207922. doi: 10.1128/spectrum.02079-22. Epub 2022 Nov 29.
7
Effect of Topical Antifungal Luliconazole on Hyphal Morphology of Trichophyton mentagrophytes Grown on in vitro Onychomycosis Model.外用抗真菌药物卢立康唑对体外甲真菌病模型中生长的须癣毛癣菌菌丝形态的影响。
Mycopathologia. 2022 Dec;187(5-6):491-496. doi: 10.1007/s11046-022-00661-6. Epub 2022 Sep 3.
8
Novel 1, 2, 4-Triazoles as Antifungal Agents.新型 1,2,4-三唑类抗真菌剂。
Biomed Res Int. 2022 Mar 22;2022:4584846. doi: 10.1155/2022/4584846. eCollection 2022.
9
Triazole Fungicide Residues and Their Inhibitory Effect on Some Trichothecenes Mycotoxin Excretion in Wheat Grains.三唑类杀菌剂残留及其对小麦中部分单端孢霉烯族毒素排泄的抑制作用。
Molecules. 2021 Mar 22;26(6):1784. doi: 10.3390/molecules26061784.
10
Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations.渗透促进剂对水醇制剂中依氟康唑经趾甲给药的影响。
Molecules. 2021 Mar 16;26(6):1650. doi: 10.3390/molecules26061650.
本文引用的文献
1
Comparison of in vitro antifungal activities of efinaconazole and currently available antifungal agents against a variety of pathogenic fungi associated with onychomycosis.比较依氟康唑与目前可用的抗真菌药物对各种与甲真菌病相关的致病性真菌的体外抗真菌活性。
Antimicrob Agents Chemother. 2013 Apr;57(4):1610-6. doi: 10.1128/AAC.02056-12. Epub 2013 Jan 14.
2
Efinaconazole 10% solution in the treatment of toenail onychomycosis: Two phase III multicenter, randomized, double-blind studies.依氟康唑 10% 溶液治疗趾甲甲真菌病：两项 III 期多中心、随机、双盲研究。
J Am Acad Dermatol. 2013 Apr;68(4):600-608. doi: 10.1016/j.jaad.2012.10.013. Epub 2012 Nov 20.
3
Impact of pH on the antifungal susceptibility of vaginal Candida albicans.pH 值对阴道白色念珠菌抗真菌敏感性的影响。
Int J Gynaecol Obstet. 2011 Sep;114(3):278-80. doi: 10.1016/j.ijgo.2011.03.016. Epub 2011 Jun 21.
4
Effects of micafungin on the morphology of Aspergillus fumigatus.米卡芬净对烟曲霉形态的影响。
J Electron Microsc (Tokyo). 2005 Jan;54(1):67-77. doi: 10.1093/jmicro/dfh100.
5
The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis.新型唑类药物R126638是白色念珠菌、毛癣菌属和犬小孢子菌中麦角甾醇合成的选择性抑制剂。
Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8. doi: 10.1128/AAC.48.9.3272-3278.2004.
6
History of the development of azole derivatives.唑类衍生物的发展历程。
Clin Microbiol Infect. 2004 Mar;10 Suppl 1:1-10. doi: 10.1111/j.1470-9465.2004.00841.x.
7
Therapeutic efficacy of topically applied KP-103 against experimental tinea unguium in guinea pigs in comparison with amorolfine and terbinafine.与阿莫罗芬和特比萘芬相比，局部应用KP-103对豚鼠实验性甲癣的治疗效果。
Antimicrob Agents Chemother. 2002 Dec;46(12):3797-801. doi: 10.1128/AAC.46.12.3797-3801.2002.
8
In vitro antifungal activity of KP-103, a novel triazole derivative, and its therapeutic efficacy against experimental plantar tinea pedis and cutaneous candidiasis in guinea pigs.新型三唑衍生物KP-103的体外抗真菌活性及其对豚鼠实验性足跖部足癣和皮肤念珠菌病的治疗效果。
Antimicrob Agents Chemother. 2001 May;45(5):1493-9. doi: 10.1128/AAC.45.5.1493-1499.2001.
9
Current and emerging azole antifungal agents.当前及新出现的唑类抗真菌药物。
Clin Microbiol Rev. 1999 Jan;12(1):40-79. doi: 10.1128/CMR.12.1.40.
10
Two mechanisms of butenafine action in Candida albicans.布替萘芬作用于白色念珠菌的两种机制。
Antimicrob Agents Chemother. 1993 Apr;37(4):785-8. doi: 10.1128/AAC.37.4.785.
Zotero 插件