Silva Kaltz V S, Lima Maria I O, Cardoso Gustavo N, Santos Aldeir S, Silva Gezaíldo S, Pereira Fillipe O
Laboratory of Biochemistry, Academic Unit of Health, Education and Health Center, Federal University of Campina Grande, Cuité, Brazil.
Mycoses. 2017 Jun;60(6):387-393. doi: 10.1111/myc.12606. Epub 2017 Feb 15.
In humans worldwide, Microsporum sp. is a frequent agent of dermatophytsosis. When considering the emergence of resistant fungi and the clinical relevance of dermatophytosis, terpene antifungal activity is of great interest. Linalool is a monoterpene alcohol with pharmacological properties. In this study, antifungal in vitro activity of linalool and ketoconazole (as a positive control) were evaluated against clinical isolates of M. canis and M. gypseum. The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of each drug were determined by broth microdilution. The effects of the drugs (1/2MIC, MIC, 2xMIC) on radial mycelial growth, conidial production and germination were analysed. The effect on the fungal cell membrane (release of intracellular material) was also investigated. Linalool (MIC: 128 μg/mL) and ketoconazole (MIC: 64 μg/mL) were effective in inhibiting all dermatophytes studied. The MFC values of linalool ranged between 128 and 256 μg/mL, whereas ketoconazole showed MFC values of from 64 to 256 μg/mL. Linalool (at MIC and 2xMIC) and ketoconazole (at 1/2MIC, MIC, 2xMIC) inhibited mycelial growth (P < 0.05). The drugs (1/2MIC, MIC, 2xMIC) were also active on conidiogenesis and conidia germination, causing complete inhibition (P < 0.05). Linalool caused leakage of intracellular material. Our study supports the use of linalool as a potential antifungal agent against M. canis and M. gypseum.
在全球范围内的人类中,小孢子菌属是皮肤癣菌病的常见病原体。考虑到耐药真菌的出现以及皮肤癣菌病的临床相关性,萜类化合物的抗真菌活性备受关注。芳樟醇是一种具有药理特性的单萜醇。在本研究中,评估了芳樟醇和酮康唑(作为阳性对照)对犬小孢子菌和石膏样小孢子菌临床分离株的体外抗真菌活性。通过肉汤微量稀释法测定每种药物的最低抑菌浓度(MIC)和最低杀菌浓度(MFC)。分析了药物(1/2MIC、MIC、2xMIC)对菌丝径向生长、分生孢子产生和萌发的影响。还研究了对真菌细胞膜的影响(细胞内物质的释放)。芳樟醇(MIC:128μg/mL)和酮康唑(MIC:64μg/mL)对所有研究的皮肤癣菌均有抑制作用。芳樟醇的MFC值在128至256μg/mL之间,而酮康唑的MFC值为64至256μg/mL。芳樟醇(在MIC和2xMIC浓度下)和酮康唑(在1/2MIC、MIC、2xMIC浓度下)均抑制菌丝生长(P<0.05)。这些药物(1/2MIC、MIC、2xMIC)对分生孢子形成和分生孢子萌发也有活性,导致完全抑制(P<0.05)。芳樟醇导致细胞内物质泄漏。我们的研究支持将芳樟醇用作针对犬小孢子菌和石膏样小孢子菌的潜在抗真菌剂。