Description |
Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
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Target |
HMG-CoA reductase[1]
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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].
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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].
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Cell Assay |
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].
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Density | 1.1±0.1 g/cm3 |
Boiling Point | 559.2±50.0 °C at 760 mmHg |
Flash Point | 185.3±23.6 °C |
Exact Mass | 404.256287 |
PSA | 72.83000 |
LogP | 4.07 |
Vapour Pressure | 0.0±3.4 mmHg at 25°C |
Storage condition | 2-8°C |