Helicocerin: Full Drug Profile

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.

Generic Name

Cerulenin

Drug Category

Antibiotics, Antifungal

Drug Type

Small Molecule; Approved

Other Brand Names containing Cerulenin

Helicocerin;

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.

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