F0206 | Lipid metabolism

Compound Dose Time Species Model Method Action Result Positive criterion Reference
Tamoxifen affect Positive 227
amphotericin B 2.5mg/ml Aspergillus fumigatus the formation of MDAs by antifungal drug-derived ROS in A. fumigatus was determined using the thiobarbituric acid (TBA) assay. induce Positive 304
Terbinafine 4mg/ml Aspergillus fumigatus lipid peroxidation using the thiobarbituric acid assay induce Positive 304
itraconazole 4mg/ml Aspergillus fumigatus lipid peroxidation using the thiobarbituric acid assay induce Positive 304
amphotericin B 2.5mg/ml Aspergillus fumigatus mitochondrion-specific lipid peroxidation probe MitoPerOx induce Positive 304
Terbinafine 4mg/ml 3min, 5min, 15min Aspergillus fumigatus mitochondrion-specific lipid peroxidation probe MitoPerOx induce Positive 304
itraconazole 4mg/ml Aspergillus fumigatus mitochondrion-specific lipid peroxidation probe MitoPerOx induce Positive 304
Perhexiline 100 μM 5 minutes preincubation; 10 minutes mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of beta oxidation decrease Positive p < 0.01 193
Perhexiline 100 μM 5 minutes preincubation; 10 minutes mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of beta oxidation decrease Positive p < 0.01 193
Perhexiline 1200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 400 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 800 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 400 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 800 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1600 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Saquinavir Interfere Positive 307
Perhexiline 400 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.05 193
Perhexiline 800 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 1600 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline decrease Positive 16
Perhexiline decrease Positive 16
Perhexiline decrease Positive 17
Perhexiline decrease Positive 17
Trimetazidine decrease Positive 17
ranolazine decrease Positive 17
Salicylic acid decrease Positive 35
tetracyclines mouse liver mitochondria affect Positive 236
5-Hydroxydecanoate 100 μm decrease Positive 189
5-Hydroxydecanoate K1/2 values 45-75 microM heart and liver mitochondria from rat decrease Positive 190
Ibuprofen affect Positive 239
Perhexiline 77 μmol/L rat cardiac mitochondria CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, affect Positive IC50 240
Amiodarone affect Positive 227
Perhexiline 148 μmol/L rat hepatic mitochondria CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, affect Positive IC50 240
Amiodarone 228 μmol/L rat cardiac and hepatic mitochondria CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine, affect Positive IC50 240
FOX-988 decrease Positive 28
Acetaminophen >400μM >400 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Sdz-51641 decrease Positive 28
Carbamazepine >400μM 341 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Salicylic acid decrease Positive 32
Tamoxifen affect Positive 227
Diclofenac 47μM 11* mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Ibuprofen 287μM 80* mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Irinotecan 6μM 10 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Methotrexate 44μM 42 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Flufenamic Acid 146 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Troglitazone affect Positive 227
Valproic Acid affect Positive 227
Amiodarone 20 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Amiodarone 50 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Amiodarone 80 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Amiodarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzarone 20 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzarone 50 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzbromarone 2 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.05 4
benzbromarone 5 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzbromarone 10 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
benzbromarone 50 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Mefenamic acid 161 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Meloxicam > 500 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Sudoxicam > 500 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Piroxicam 728 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Diflunisal 68 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Diclofenac 122 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Sulindac sulfide 78 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Nimesulide 29 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
2‐Butylbenzofuran 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive p < 0.01 4
Amiodarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 28% inhibition 4
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 33% inhibition 4
benzbromarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 34% inhibition 4
2‐Butylbenzofuran 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of acyl‐CoA dehydrogenase activity decrease Positive 22% inhibition 4
benzarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of β‐ketothiolase activity decrease Positive 11% inhibition 4
benzbromarone 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of β‐ketothiolase activity decrease Positive 25% inhibition 4
Salicylic acid >400μM >400 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Tamoxifen 4μM 11 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Oxfenicine >100 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
oxfenicine metabolite 25.8 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
Perhexiline rat hepatocytes affect Positive 238
RO-25-0187 1.5 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
Zidovudine 79μM 83 mice Lean mice vs Ob/ob mice Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform Positive EC20 227
Tolfenamic Acid 83.1 24hr rat hepatocytes LipidTox, for neutral lipid accumulation, to evaluate lipid content. accumulation Positive AC50 (μM) 40
Acetaminophen affect Positive 227
Etomoxir decrease Positive 35
amineptine decrease Positive 54
pirprofen decrease Positive 59
Amiodarone 34 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive IC50 4
Propofol Positive 197
Salicylic acid affect Positive 227
Chlorpyrifos 30–50 μM PC12 cell line we measured the concentration malondialdehyde (MDA) to indicate formation of lipid peroxides Positive 242
Paraquat 10 mg/kg/week intraperitoneal (i.p.) 3weeks C57BL/6 mice Positive 242
Aluminium 100 mg/kg in drinking water daily for six weeks Wistar rats Positive 242
benzarone 34 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive IC50 4
Ibuprofen affect Positive 227
benzbromarone 2 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive IC50 4
buprenorphine 100 μM rat liver mitochondria the mitochondrial membrane potential assessed by the fluorescence of safranine. affect Positive 235
2‐Butylbenzofuran 100 μmol/L rat; Sprague–Dawley liver mitochondria Measurement of beta oxidation and ketone body formation decrease Positive 28% inhibition 4
Troglitazone 10 µM ZDF fa/fa rat vs ZDF lean rat isolated mitochondria Oxidation of mitochondrial phospholipids was measured by HPLC analysis. Peak area ratio (235/206 nm) shows relative peroxidative phospholipid content. Peak areas at 206 nm and 235 nm analyze non-peroxidative and peroxidative phospholipid. peroxidation Positive significantly different from ZDF lean rats (p < 0.05) 225
Tianeptine 0.0625 mmol/kg i.p. mouse in vivo affect Positive 237
TDGA 0.31 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
Dronedarone 10µM 24hr isolated rat liver mitochondria, and the human hepatoma cell line HepG2 inhibit Positive 271
Amiodarone 20µM 24hr isolated rat liver mitochondria, and the human hepatoma cell line HepG2 inhibit Positive 271
POCA 59.7 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
Etomoxir 2.76 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
DET 5.6 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
aminocarnitine 0.97 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
palmitoylaminocarnitine 0.11 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
ST1326 1.1 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
ST2425 0.21 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
Perhexiline 25 μM 24 hours rat; Sprague-Dawley Crl:CD-1 (ICR) BR hepatocytes Measurement of beta oxidation decrease Positive p < 0.05 193
Trimetazidine 47.1 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
Perhexiline 14.8 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
Amiodarone 16.6 Wistar rat hepatocytes ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) inhibition Positive IC50 (μM) 333
ranolazine 25μM 24hr T47D cells quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion stimulate Positive Student’s two-tail t-test, where p < 0.05 273
Trimetazidine 100 μM 24hr T47D cells quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion stimulate Positive Student’s two-tail t-test, where p < 0.05 273
Etomoxir 0.1 to 50 μM 24hr MCF-7 and T47D cells quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion inhibition Positive Student’s two-tail t-test, where p < 0.05 273
Oxfenicine 1.5 to 4.5mM 24hr T47D cells quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion inhibition Positive Student’s two-tail t-test, where p < 0.05 273
Carnitine 0.5mM 24hr U-937, MCF-7, and T47D quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion stimulate Positive 273
AICAR 1mM 24hr U-937, MCF-7, and T47D quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion stimulate Positive 273
AICAR stimulate Positive 273
TDGA <0.05/0.04 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
POCA 10.4/95.9 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Etomoxir 0.29/0.34 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
DET 1.8/4.4 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
aminocarnitine −/− human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
palmitoylaminocarnitine 2.8/0.27 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
ST1326 4.0/0.98 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
ST2425 0.73/0.03 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Trimetazidine 20.5/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Perhexiline 22.4/21.4 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Amiodarone 28.5/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Oxfenicine >100/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
oxfenicine metabolite 33.3/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
RO-25-0187 25.5/>100 human/rat hepatocytes Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate inhibition Positive IC50 (μM) 333
Hypoglycin A Positive 232
4-Pentenoic acid Positive 232
2-bromooctanoic acid Positive 232
2-tetradecylglycidic acid Positive 232
2-bromopalmitic acid Positive 232
Palmitoylcarnitine Positive 232
Perhexiline decrease Positive 35
Perhexiline 200 μM mouse; Crl/CD-l(1CR)BR Swiss liver mitochondria Measurement of activities of acyl-CoA dehydrogenases decrease Positive p < 0.01 193
Perhexiline 5 μM 72 hours rat; Sprague-Dawley Crl:CD-1 (ICR) BR hepatocytes Measurement of beta oxidation decrease Positive p < 0.05 193