Lovastatin, a HMG-CoA reductase inhibitor, is a cholesterol-lowering drug.
Description
Lovastatin, a HMG-CoA reductase inhibitor, is a cholesterol-lowering drug.
In Vitro
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].
In Vivo
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 Ki 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].
Clinical Trial
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References
[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.
Preparing Stock Solutions
ConcentrationVolumeMass
1 mg
5 mg
10 mg
1 mM
2.4719 mL
12.3597 mL
24.7194 mL
5 mM
0.4944 mL
2.4719 mL
4.9439 mL
10 mM
0.2472 mL
1.2360 mL
2.4719 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]
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.
References
[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.
Molecular Weight
404.54
Formula
C₂₄H₃₆O₅
CAS No.
75330-75-5
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Shipping
Room temperature in continental US; may vary elsewhere
[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.
