Evolution of ergosterol biosynthesis inhibitors as fungicidal against Candida. 2010

Aijaz Ahmad, and Amber Khan, and Nikhat Manzoor, and Luqman A Khan
Department of Biosciences, Jamia Millia Islamia, New Delhi, India.

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.

UI MeSH Term Description Entries
D002175 Candida A genus of yeast-like mitosporic Saccharomycetales fungi characterized by producing yeast cells, mycelia, pseudomycelia, and blastophores. It is commonly part of the normal flora of the skin, mouth, intestinal tract, and vagina, but can cause a variety of infections, including CANDIDIASIS; ONYCHOMYCOSIS; VULVOVAGINAL CANDIDIASIS; and CANDIDIASIS, ORAL (THRUSH). Candida guilliermondii var. nitratophila,Candida utilis,Cyberlindnera jadinii,Hansenula jadinii,Lindnera jadinii,Monilia,Pichia jadinii,Saccharomyces jadinii,Torula utilis,Torulopsis utilis,Monilias
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D004875 Ergosterol A steroid occurring in FUNGI. Irradiation with ULTRAVIOLET RAYS results in formation of ERGOCALCIFEROL (vitamin D2). Lumisterol,Pro-Vitamin D2,Provitamin D 2,D2, Pro-Vitamin,Pro Vitamin D2
D005054 Eugenol A cinnamate derivative of the shikimate pathway found in CLOVE OIL and other PLANTS. Phenol, 2-methoxy-4-(2-propenyl)-
D000935 Antifungal Agents Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues. Anti-Fungal Agents,Antifungal Agent,Fungicides, Therapeutic,Antibiotics, Antifungal,Therapeutic Fungicides,Agent, Antifungal,Anti Fungal Agents,Antifungal Antibiotics
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D050296 Microbial Viability Ability of a microbe to survive under given conditions. This can also be related to a colony's ability to replicate. Bacterial Viability,Virus Viability,Bacteria Viability,Microbial Inactivation,Inactivation, Microbial,Viability, Bacteria,Viability, Bacterial,Viability, Microbial,Viability, Virus

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