Helicocerin - General Information
Helicocerin is an antifungal antibiotic that inhibits sterol and fatty acid biosynthesis. In fatty acid synthesis, reported to bind in equimolar ratio to b-keto-acyl-ACP synthase. In sterol synthesis, inhibits HMG-CoA synthetase activity. It is also shown to inhibit feeding and induce dramatic weight loss in mice. It is found naturally in the Cephalosporium caerulensfungus. [Wikipedia]
Pharmacology of Helicocerin
Helicocerin is an antifungal antibiotic isolated from Cephalosporium caerulens. It interrupts fungal growth by inhibiting the biosynthesis of sterols and fatty acids (inhibits bacterial fatty acid synthesis). It also inhibits HMG-CoA synthetase activity. Helicocerin produces metabolic effects similar to effects of leptin, but through mechanisms that are independent of, or down-stream from, both leptin and melanocortin receptors.
Additional information about Helicocerin
Helicocerin Indication: For use as a biochemical tool, Helicocerin is shown to cause dramatic weight loss in animals
Mechanism Of Action: Irreversibly binds to fatty acid synthase, specifically b-ketoacyl-acyl carrier protein synthase (FabH, FabB and FabF condensation enzymes). A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FAS). Inhibition of FAS by cerulenin leads to cytotoxicity and apoptosis in human cancer cell lines, an effect believed to be mediated by the accumulation of malonyl-coenzyme A in cells with an upregulated FAS pathway.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Cerulenin
Synonyms: Not Available
Drug Category: Antibiotics, Antifungal
Drug Type: Small Molecule; Approved
Absorption: Not Available
Toxicity (Overdose): Oral, mouse LD50: 547 mg/kg. Symptoms of overexposure include moderate to severe erythema (redness) and moderate edema (raised skin), nausea, vomiting, and headache.
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Helicocerin: Not Available
Chemical IUPAC Name: (2R,3S)-3-nona-4,7-dienoyloxirane-2-carboxamide
Chemical Formula: C12H17NO3
Cerulenin on Wikipedia: https://en.wikipedia.org/wiki/Cerulenin
Organisms Affected: Humans and other mammals; Fungi; Bacteria