Department of Biosciences, Jamia Millia Islamia, New Delhi, India.
Microb Pathog. 2010 Jan;48(1):35-41. doi: 10.1016/j.micpath.2009.10.001. Epub 2009 Oct 14.
Azoles target the ergosterol synthesizing enzyme lanosterol 14alpha-demethylase and are a widely applied class of antifungal agents. Unfortunately azoles are generally fungistatic, and resistance to fluconazole is emerging in several fungal pathogens. In contrast to the increasing number of agents for the treatment of invasive fungal infections, discoveries of new antifungal agents with therapeutic value in dermatomycoses are reported only rare. Attention has been drawn to the antimicrobial activity of plants and their active principles due to the challenge of growing incidences of drug-resistant pathogens. Eugenol and methyl eugenol were reported to possess antimycotic properties. To further explore the antifungal activity of these compounds, in vitro studies were conducted on various Candida isolates. Insight studies to mechanism suggested that both eugenol and methyl eugenol exerts their antifungal activity by targeting sterol biosynthesis. Furthermore, it was also observed that additional methyl group to eugenol increases its antifungal activity. The observed fungicidal characteristics of both eugenol and methyl eugenol indicate that both the compounds might be promising antifungal agents defining a new class of antimycotics.
唑类药物靶向麦角甾醇合成酶羊毛甾醇 14α-脱甲基酶，是一类广泛应用的抗真菌药物。不幸的是，唑类药物通常具有抑菌作用，并且几种真菌病原体对氟康唑的耐药性正在出现。与治疗侵袭性真菌感染的药物数量不断增加形成对比的是，在治疗皮肤真菌病方面具有治疗价值的新型抗真菌药物的发现却很少有报道。由于耐药病原体发病率不断上升的挑战，人们开始关注植物及其活性成分的抗菌活性。已报道丁香酚和甲基丁香酚具有抗真菌特性。为了进一步探索这些化合物的抗真菌活性，对各种念珠菌分离株进行了体外研究。对作用机制的深入研究表明，丁香酚和甲基丁香酚通过靶向甾醇生物合成发挥其抗真菌活性。此外，还观察到丁香酚中增加一个甲基会增加其抗真菌活性。丁香酚和甲基丁香酚的杀菌特性表明，这两种化合物都可能是有前途的抗真菌药物，定义了一类新的抗真菌药物。
