Polyene antifungals bind to ergosterol, the main sterol in the fungal cell membrane, and cause depolarization of the membrane. This increases the membrane permeability and leads to cell death. They are not absorbed when given orally, so are used to treat fungal infections of the gastrointestinal tract, such as oral thrush .

Polyene antimycotics, sometimes referred to as polyene antibiotics, are a class of antimicrobial polyene compounds that target fungi. [1] These polyene antimycotics are typically obtained from certain species of Streptomyces bacteria.

2023年3月7日 · Polyene antifungals (e.g., amphotericin B) bind to ergosterol, a steroid-alcohol unique to Fungi. The polyene-ergosterol complex creates pores in the fungal cell membrane, ultimately leading to electrolyte leakage, cell lysis, and cell death.

Polyene Antifungal Drugs. Amphotericin, nystatin, and pimaricin interact with sterols in the cell membrane (ergosterol in fungi, cholesterol in humans) to form channels through which small molecules leak from the inside of the fungal cell to the outside.

Polyene antifungal agents include amphotericin B and its various formulations, and nystatin. Amhptericin B is primarily used to treat deep-seated fungal infections while nystatin is used to treat localized oral candidial infections.

Antifungals can be grouped into three classes based on their site of action: azoles, which inhibit the synthesis of ergosterol (the main fungal sterol); polyenes, which interact with fungal membrane sterols physicochemically; and 5-fluorocytosine, …

2020年12月1日 · Polyenes represent the oldest class of systemic antifungal agents comprising over 200 polyene macrolides, which are mainly derived from the Streptomyces spp. [23]. They are amphipathic in nature, mainly comprising of a hydrophobic polyene chain linked to a hydrophilic polyhydroxyl chain.

2024年8月14日 · Polyene antifungal drugs are a class of antimicrobial compounds known for their potential effect in treating fungal infections. Over two hundred polyene compounds have been discovered and shown to be the first antifungal antibiotics.

2024年8月14日 · Polyenes are a class of organic compounds well known for their potent antifungal properties. They are effective due to their ability to target and disrupt fungal cell membranes by binding to ergosterol and forming pores.

Antifungal agents • A history of pharmaceutical neglect: –Rare – Difficult to devise – Difficult to test in vitro – Not renumerative • Escalating pace of research but • Old gold standard Available classes • Polyenes (cell membrane synthesis • Azoles (cell membrane synthesis) • Echinocandins (cell wall synthesis)(cell wall ...