HMG-CoA reductase (HMGCR) is a rate-limiting enzyme in cholesterol synthesis. Lovastatin is a potent inhibitor of HMGCR with an Ki value of 0.6 nM[3]. In human myeloid leukemia KBM-5 cells, treatment with 5 – 50 μM lovastatin for 12 hours effectively inhibited TNF-induced NF-κB activation at a dose-dependent manner. Incubation of KBM-5 cells with 5 μM lovastatin for 24 hours enhanced cytotoxicity induced by chemotherapeutic agents (i.e. paclitaxel, doxorubicin, and 5-fluorouracil). The same treatment also augmented chemotherapeutic agents-induced apoptotic effects in KBM-5 cells[4]. In rat primary astrocytes, 8h preincubation with 10 μM lovastatin led to 90% inhibition of LPS-induced NO production. Pretreatment with 5 or 10 μM lovastatin for 8 hours also significantly suppressed LPS-mediated induction of iNOS mRNA and protein. A combination of lovastatin (2 μM) and sodium phenylacetate (2 nM) almost completely inhibited LPS-induced NO production and iNOS expression. The addition of 10 μM lovastatin to rat primary astrocytes inhibited cholesterol synthesis by 73% and reduced NO production induced by different combinations of LPS and cytokines. Lovastatin (10 μM) also showed potent inhibitory effect on LPS-induced production of NO, TNF-a, IL-1b, and IL-6 in rat primary microglia and macrophages[5]. In nf1+/− mice, daily injection with lovastatin (10 mg/kg) for 4 days decreased the level of phosphorylated p44/42 MAPK compared to wild-type controls. Lovastatin treatment also resulted in an improvement in sensory gating deficits and long-term potentiation in nf1+/− mice[6].
Lovastatin 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
HEP G2 cells
Function assay
Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line), IC50=5e-05 μM
2153213
HEP G2 cells
Function assay
Tested for inhibition of cholesterol biosynthesis in HEP G2 cells, IC50=0.029 μM
7932551
HES 9 cell line
Function assay
Concentration required to inhibit HMG-CoA reductase by 50% was determined in HES 9 cell line, IC50=0.013 μM
1527791
human A549 cells
Cytotoxic assay
72 h
Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=11.4 μM
Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line), IC50=5e-05 μM
2153213
HEP G2 cells
Function assay
Tested for inhibition of cholesterol biosynthesis in HEP G2 cells, IC50=0.029 μM
7932551
HES 9 cell line
Function assay
Concentration required to inhibit HMG-CoA reductase by 50% was determined in HES 9 cell line, IC50=0.013 μM
1527791
human A549 cells
Cytotoxic assay
72 h
Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=11.4 μM
23570542
human AU565 cells
Growth inhibition assay
48 h
Growth inhibition of ER-negative, HER2-positive human AU565 cells after 48 hrs by WST-1 assay
24556504
human HepG2 cells
Function assay
6 h
Lipid lowering activity in human HepG2 cells assessed as decrease in oleic acid elicited lipid accumulation after 6 hrs by oil-red O staining method, IC50=8.3 μM
26169125
human HS68 cells
Cytotoxic assay
72 h
Cytotoxicity against human HS68 cells after 72 hrs by MTT assay, IC50=23.2 μM
23570542
human HT29 cells
Growth inhibition assay
96 h
Growth inhibition of human HT29 cells after 96 hrs by MTS assay, IC50=46.8 μM
17472962
human K562 cells
Function assay
48 h
Inhibition of GGTase1 in human K562 cells assessed as reduction of Rap1a protein geranylgeranylation after 48 hrs by Western blotting
20832326
human LS180 cells
20 μM
Function assay
Inhibition of survivin expression in parent human LS180 cells at 20 uM by immunoblot analysis
17472962
human MCF7 cells
Growth inhibition assay
48 h
Total growth inhibition of ER-positive, HER2-negative human MCF7 cells after 48 hrs by WST-1 assay
24556504
human MDA-MB-231 cells
Function assay
24 h
Induction of p21 expression in human PR, ER, HER2-negative human MDA-MB-231 cells at 1 to 10 uM after 24 hrs by western blot analysis
24556504
human MDA-MB-361 cells
Growth inhibition assay
48 h
Growth inhibition of ER-positive, HER2-positive human MDA-MB-361 cells after 48 hrs by WST-1 assay
24556504
human MDA-MB-468 cells
Function assay
48 h
Total growth inhibition of PR, ER, HER2-negative human MDA-MB-468 cells after 48 hrs by WST-1 assay
24556504
human RPMI8226 cells
20 μM
Apoptosis assay
48 h
Induction of apoptosis in human RPMI8226 cells assessed as increase in caspase-3 cleavage at 20 uM incubated for 48 hrs by immunoblot method
25935643
human SW480 cells
Growth inhibition assay
96 h
Growth inhibition of human SW480 cells after 96 hrs by MTS assay, IC50=7.1 μM
17472962
human SW480 cells
20 μM
Function assay
Inhibition of FBS-stimulated increase in Akt phosphorylation in human SW480 cells at 20 uM by immunoblot analysis
17472962
mouse MEF cells
Cytotoxic assay
72 h
Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay, IC50=35 μM
United States, California
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Terminated(Overall profile of ... 展开 >>the compound does not offer significant clinical advantage to patients over currently available lipid lowering agents) 收起 <<
Taiwan
... 展开 >> Research Site
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Canada, British Columbia
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Dept. of Anesthesiology, Pharmacology & Therapeutics (APT), University of British Columbia
Vancouver, British Columbia, Canada, V6T 1Z3 收起 <<
United States, Ohio
... 展开 >>
The Ohio State University Medical Center
Recruiting
Columbus, Ohio, United States, 43210
Principal Investigator: Joseph P Kitzmiller, MD PhD
Sub-Investigator: Wolfgang Sadee, Dr rer nat
Sub-Investigator: Mitch Phelps, PhD
Sub-Investigator: Rebecca Jackson, MD 收起 <<
United States, Oregon
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Atherosclerosis Research Unit, Division of Cardiovascular Medicine, Department of Medicine
Los Angeles, California, United States, 90033 收起 <<
Healthy Volunteers
... 展开 >> Drug Drug Interactions 收起 <<
Phase 1
Completed
-
United States, North Carolina
... 展开 >>
University of North Carolina, Clinical and Translational Research Center (CTRC)
Chapel Hill, North Carolina, United States, 27599 收起 <<
Irritable Bowel Syndrome With ... 展开 >>Constipation 收起 <<
Phase 2
Not yet recruiting
January 1, 2020
United States, California
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Cedars-Sinai Medical Center
Not yet recruiting
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Contact: Tahli Singer-Englar 310-423-3792 tahli.singerenglar@cshs.org 收起 <<
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University of California, Los Angeles Stroke Network
Los Angeles, California, United States, 90024
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Jackson Memorial Hospital
Miami, Florida, United States, 33136
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Miami, Florida, United States, 33136
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Birmingham, Alabama, United States, 35294
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Washington, District of Columbia, United States, 20010
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Boston, Massachusetts, United States, 02115
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Cincinnati, Ohio, United States, 45229
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Westmead, New South Wales, Australia, 2145 收起 <<
Precancerous Condition
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Stage I Melanoma
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Phase 2
Completed
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United States, California
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University of California Medical Center At Irvine-Orange Campus
Orange, California, United States, 92868
United States, Florida
H. Lee Moffitt Cancer Center and Research Institute
Tampa, Florida, United States, 33612
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Huntsman Cancer Institute
Salt Lake City, Utah, United States, 84112 收起 <<
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Birmingham, Alabama, United States, 35294
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San Francisco, California, United States, 94143
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University of Colorado
Aurora, Colorado, United States, 80095
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University of Chicago Medical Center
Chicago, Illinois, United States, 60637
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Justus J. Fiechtner, MD, PLLC
Lansing, Michigan, United States, 48910
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Feinstein Institute for Medical Research NS-LIJ Health System
Manhasset, New York, United States, 11030
University of Rochester
Rochester, New York, United States, 14642
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Carolina Bone and Joint
Charlotte, North Carolina, United States, 29425
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Durham, North Carolina, United States, 27710
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Oklahoma Medical Research Foundation
Oklahoma City, Oklahoma, United States, 73104
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Altoona Center for Clinical Research
Duncansville, Pennsylvania, United States, 16635
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Pittsburgh, Pennsylvania, United States, 15261
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Charleston, South Carolina, United States, 29425
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Dallas, Texas, United States, 75231
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Richmond, Virginia, United States, 23249
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Richmond, Virginia, United States, 23298
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