Lovastatin (Syn: mevinolin) is a secondary metabolite isolated from fungi hyphae that is often used as a statin prodrug commonly used to diminish endogenous LDL cholesterol synthesis and reduce hypercholesterolemia. Lovastatin inhibits 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase), an enzyme involved in the cholesterol synthesis pathway. Lovastatin is a natural product first isolated by Monascus sp. by the Japanese professor Akira Endo in 1979. Cholesterol itself is biosynthesized in a series of more than 25 separate enzymatic reactions.
Inactive in its native form, which is a gamma-lactone closed ring form, Lovastatin is hydrolyzed in vivo to the β-hydroxy acid open ring form which is considered the active form.
In addition to its anti-inflammatory and neuroprotective effects, Lovastatin has anti-cancer properties.
Lovastatin is practically insoluble in aqueous solution.
| Mechanism of Action | Lovastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonate. |
| Source | Monascus species. Lovastatin is also naturally produced by certain higher fungi such as oyster mushrooms (Pleurotus ostreatus) and other closely related Pleurotus species. |
| Cancer Applications |
Research has shown that statins like Lovastatin have been able to inhibit melanoma cell growth at high concentrations. Lovastatin can regulate the proliferation, apoptosis and drug resistance in different types of cancer cells such as breast, liver, lung, colon, stomach etc. (Xie, 2021). |
| References |
Eustace AJ et al (2008) The 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors, simvastatin, Lovastatin and mevastatin inhibit proliferation and invasion of melanoma cells. BMC Cancer 8:9 Alberts AW (1988) Discovery, biochemistry and biology of lovastatin. Am J Cardiol. 62(15):10J-15J. PMID 3055919 Xie L (2021) An overview on the biological activity and anti-cancer mechanism of Lovastatin. Cell. Sig. 87:110122 |
