Antifungals
Antifungals (also known as antimycotics) are a pharmacologically diverse group of compounds used to treat mycoses (fungal infections) in humans and animals. They may also be used in cell culture to prevent contamination. Most antimycotic products act by interfering with the integrity of the fungal cell membrane or cell wall.
| Cat. No. | Product Name / Activity |
|---|---|
| 6930 | Amphotericin B |
| Antifungal; binds ergosterol in fungal cell membranes | |
| 6384 | Ciclopirox |
| Antifungal; pan-histone demethylase inhibitor | |
| 4096 | Clotrimazole |
| Imidazole antimycotic and cytochrome P450 inhibitor | |
| 0970 | Cycloheximide |
| Antifungal antibiotic; preferentially inhibits protein synthesis in eukaryotes | |
| 6250 | Filipin III |
| Polyene antibiotic; binds sterols in fungal membranes. | |
| 3764 | Fluconazole |
| Triazole antifungal agent | |
| 5981 | Itraconazole |
| Azole antifungal; also SMO antagonist | |
| 3197 | Polygodial |
| Exhibits antifungal activity via inhibition of mitochondrial ATPase; also TRPA1 channel activator | |
| 1589 | Radicicol |
| Antifungal antibiotic | |
| 2395 | Sertraline hydrochloride |
| Exhibits antifungal activity against Candida auris in vitro; 5-HT reuptake inhibitor | |
| 6484 | Terbinafine hydrochloride |
| Antifungal; inhibits fungal sterol biosynthesis | |
| 5270 | Toyocamycin |
| Antifungal antibiotic; adenosine analog | |
| 3760 | Voriconazole |
| Triazole antifungal agent |
Antimycotic Mechanism of Action
The majority of antimycotic compounds, including the azole antifungals such as Fluconazole, the polyene antibiotics such as Amphotericin B, and the allylamine, Terbinafine, exert their effects via disruption of the fungal cell membrane. Azoles are inhibitors of sterol 14α-demethylase, a fungal cytochrome P450 (CYP)-dependent enzyme, which results in depletion of cell membrane ergosterol and impaired membrane fluidity, leading to accumulation of toxic 14α-methylated sterols and eventual fungal cell death. Terbinafine also inhibits ergosterol synthesis, but by a different route, the inhibition of squalene monooxygenase. Amphotericin B, on the other hand directly binds to ergosterol, forming complexes that intercalate the cell membrane and form pores.
Ciclopirox, another antimycotic, is a non-selective histone demethylase inhibitor. Among other types of antimycotics, the echinocandins act by disrupting cell wall synthesis, while compounds such as griseofulvin and flucytosine, affect mitosis.
Mycosis
Mycoses, or fungal infections, can be classified according to the site and extent of infection, as local (superficial, cutaneous or subcutaneous) or systemic, and range from common benign infections, such as athlete's foot (tinea pedis), to the life threatening, such as Aspergillosis or cryptococcal meningitis. Mycoses can occur as a result of inhalation of fungal spores, cutaneous exposure or percutaneous inoculation. In addition, mycoses can result from an endogenous process such as reactivation of an infection or from abnormal activation of normally harmless flora. An example of this is tinea versicolor, which is caused by a normally benign fungus, Malassezia furfur, that lives on human skin; heat and humidity or a compromised immune system can lead to this infection causing skin symptoms consisting of skin discoloration and flaking, usually on the trunk, abdomen and neck. Individuals with compromised immune systems, such cancer patients undergoing chemotherapy, patients with HIV/AIDS, or those receiving steroids are at greatest risk of developing serious, opportunistic, invasive fungal infections.