Lovastatin, a HMG-CoA reductase inhibitor, is a cholesterol-lowering drug.

Lovastatin is an inactive lactone prodrug that must be chemically or enzymatically converted to its dihydroxy open-acid form in order to elicit inhibitory activity. Lovastatin in its hydroxy acid form is an exceptionally potent competitive inhibitor of liver HMG CoA reductase^[1]. Lovastatin, other than its anticholesterol property, has diverse applications in the field of osteoporosis, neuro-degeneration, rheumatoid arthritis, antifungals and also is reported to reduce proliferation of lung cancer cells, breast cancer (MCF-7), liver cancer (HepG2). Lovastatin treatments show significant dose dependent cytotoxic effect on HeLa cells with IC₅₀ value of 160 μg/mL. Lovastatin is effective to accelerate hydroxyl radical scavenging activity (54.06%) at an IC₅₀ of 3601 μg/mL^[2].

Lovastatin is an inactive lactone that is hydrolyzed in the liver to an active f3-hydroxyacid form. This principal metabolite is the inhibitor of the enzyme HMG-CoA reductase. The K_i is 1 nM. Lovastatin and its β-hydroxyacid metabolite are highly bound to human plasma proteins. Lovastatin crosses the blood-brain and placental barriers^[3]. Lovastatin produces a profound reduction of apolipoprotein-B-containing lipoproteins, especially LDL cholesterol and, to a lesser extent, plasma triglycerides, and a small increase in HDL cholesterol^[4].

• [1]. Alberts AW, et al. Discovery, biochemistry and biology of lovastatin. Am J Cardiol. 1988 Nov 11;62(15):10J-15J.

  [2]. Bhargavi S, et al. Purification of Lovastatin from Aspergillus terreus (KM017963) and Evaluation of its Anticancer and Antioxidant Properties. Asian Pac J Cancer Prev. 2016;17(8):3797-803.

  [3]. Frishman WH, et al. Lovastatin: an HMG-CoA reductase inhibitor for lowering cholesterol. Med Clin North Am. 1989 Mar;73(2):437-48.

  [4]. Tobert JA, et al. Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26.

Hela cells are treated with lovastatin (0, 5, 10, 20, 40, 80, 160, 320 μg/mL) for 24 h. Cells treated with culture medium serves as a negative control. cell viability is measured using the MTT based colorimetric assay ^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Alberts AW, et al. Discovery, biochemistry and biology of lovastatin. Am J Cardiol. 1988 Nov 11;62(15):10J-15J.

  [2]. Bhargavi S, et al. Purification of Lovastatin from Aspergillus terreus (KM017963) and Evaluation of its Anticancer and Antioxidant Properties. Asian Pac J Cancer Prev. 2016;17(8):3797-803.

  [3]. Frishman WH, et al. Lovastatin: an HMG-CoA reductase inhibitor for lowering cholesterol. Med Clin North Am. 1989 Mar;73(2):437-48.

  [4]. Tobert JA, et al. Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26.

404.54

C₂₄H₃₆O₅

75330-75-5

Room temperature in continental US; may vary elsewhere

DMSO: ≥ 215 mg/mL

* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">