Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in Rodents
Abstract
:Introduction
Chemistry
Results
Compound | Ra- | Rb- | Rc- | Rd- |
---|---|---|---|---|
1 | H- | 4'-Cl-C6H4- | 4'-Cl-C6H4- | H3CH2COOC- |
2 | H- | C6H5- | 4'-Br-C6H4- | H3CH2COOC- |
3 | H- | C6H5- | 3'-Cl-C6H4- | H3CH2COOC- |
4 | H- | 4'-F-C6H4- | 4'-CH3-C6H4- | H3CH2COOC- |
5 | H- | 4'-Cl-C6H4- | 4'-CH3-C6H4- | H3CH2COOC- |
6 | H3C- | CH3CH2O- | H- | 4'-Cl-C6H4- |
7 | H- | 4'-F-C6H4- | 4'-F-C6H4- | H3CH2COOC- |
8 | H- | 4'-CH3O-C6H4- | 4'-Cl-C6H4- | H3CH2COOC- |
9 | H- | 4'-Cl-C6H4- | 4'-F-C6H4- | H3CH2COOC- |
10 | H- | 4'-CH3-C6H4- | 4'-CH3O-C6H4- | H3COOC- |
11 | H- | 4'-CH3O-C6H4- | 4'-CH3O-C6H4- | H3COOC- |
12 | H- | 4'-Cl-C6H4- | 4'-CH3O-C6H4- | H3COOC- |
13 | H- | 4'-CH3O-C6H4- | 4'-CH3O-C6H4- | 4'-CH3O-C6H4- |
14 | H- | CH3O- | 3',4'-(CH3O)2-C6H4- | 3',4'-(CH3O)2-C6H4- |
15 | H3C- | CH3CH2O- | 3',4'-(CH3O)2-C6H4- | 3',4'-(CH3O)2-C6H4- |
N=6 Compound | (g/rat/day) Food Consumption | Percent of Control (X±SD) | |||
Day 7 | Day 14 | ||||
Cholesterol | Triglycerides | Cholesterol | Triglycerides | ||
1 | 19.13 | 98±5 | 93±18 | 68±16* | 147±7* |
2 | 20.60 | 120±24 | 85±13 | 104±7 | 159±8* |
Atorvastatina | 19.03 | 110±14 | 92±28 | 69±6* | 119±5* |
Gemfibrozilb | 17.47 | 122±5 | 56±62* | 116±17 | 138±2* |
Controlc | 20.06 | 100±14d | 100±7e | 100±8f | 100±6g |
a Dosed at 8 mg/kg/day | e 94 mg/dL serum triglycerides | ||||
b Dosed at 90 mg/kg/day | f 46 mg/dL total serum cholesterol | ||||
c 1% CMC | g 56 mg/dL serum triglycerides |
N=6 | Percent of Control (X±SD) | |
Compound | Cholesterol | Triglycerides |
Liver | ||
1 | 187±19* | 106±20 |
2 | 197±19* | 100±40 |
Atorvastatina | 169±19* | 166±35 |
Gemfibrozilb | 107±18 | 96±16 |
Controlc | 100±24d | 100±35e |
Small intestine | ||
1 | 48±13 | 127±24 |
2 | 33±17 | 115±20 |
Atorvastatina | 49±15 | 55±18* |
Gemfibrozilb | 75±16 | 81±28 |
Controlc | 100±35f | 100±19g |
Aorta | ||
1 | 61±12* | 15±41* |
2 | 126±18 | 30±28* |
Atorvastatina | 105±17 | 56±23* |
Gemfibrozilb | 106±13 | 29±22* |
Controlc | 100±15h | 100±14i |
Feces | ||
1 | 123±18 | 84±20 |
2 | 94±10 | 92±16 |
Atorvastatina | 178±54 | 85±16 |
Gemfibrozilb | 106±13 | 98±23 |
Controlc | 100±22j | 100±24k |
a Dosed at 8 mg/kg/day | g 12.78 mg/g (wt) | |
b Dosed at 90 mg/kg/day | h 2.97 mg/dL (wt) | |
c 1% CMC | I 13.85 mg/dL (wt) | |
d 3.17 mg/g (wet tissue) | j 7.92 mg/dL (wt) | |
e 3.31 mg/dL (wt) | k 9.44 mg/dL (wt) |
Percent of Control (X±SD) | ||||
N=6 | Day 7 | Day14 | ||
Compound | Cholesterol | Triglycerides | Cholesterol | Triglycerides |
3 | 68±11* | 28±29* | 72±8* | 59±37 |
4 | 69±9* | 54±5* | 66±11* | 113±43 |
5 | 73±8* | 99±8 | 87±8 | 184±28 |
6 | 97±7 | 62±7* | 82±9* | 109±20 |
7 | 67±15* | 56±24* | 76±14 | 61±30* |
8 | 79±14* | 91±31 | 91±13 | 53±23* |
9 | 95±8 | 58±14* | 91±18 | 52±23* |
10 | 93±10 | 70±19 | 98±17 | 60±21* |
11 | 89±9 | 76±26 | 90±17 | 77±30 |
12 | 102±12* | 67±11* | 103±12 | 67±31 |
13 a | 80±13* | 49±17* | 76±8* | 65±28* |
14 a | 62±19* | 55±20* | 66±14* | 62±23* |
15 a | 75±9* | 83±14 | 89±3* | 76±24 |
Atorvastatinb | 77±6* | 66±11* | 81±17 | 84±33 |
Gemfibrozilc | 62±11* | 43±21* | 57±13* | 82±15 |
Niacind | 97±18 | 70±8 | 93±24 | 102±21 |
Controle | 100±14f | 100±7g | 100±8h | 100±6i |
a Dosed at 4 mg/kg/day, IP | f 188 mg/dL total serum cholesterol | |||
b Dosed at 8 mg/kg/day, IP | g 231 mg/dL serum triglycerides | |||
c Dosed at 90 mg/kg/day, IP | h 164 mg/dL total serum cholesterol | |||
d Dosed at 12.5 mg/kg/day, IP | i 179 mg/dL serum triglycerides |
Discussion
N=6 | Percent of Control (X±SD) | |
Compound | LDL-Cholesterol | HDL-Cholesterol |
3 | - | 102±20 |
4 | - | 112±24 |
5 | - | 109±21 |
6 | - | 130±12 |
7 | 47±21* | 63±53 |
8 | 65±40* | 56±38 |
9 | 53±31 | 283±10* |
10 | 106±5 | 46±31* |
11 | 47±15* | 96±63 |
12 | 47±25* | 203±21 |
13a | 39±34* | 82±31 |
14a | 114±21 | 148±4 |
15a | 156±17 | 250±11 |
Atorvastatinb | - | 178±34 |
Gemfibrozilc | - | 192±8* |
Niacind | - | 152±19 |
Controle | 100±15f | 100±14g |
a Dosed at 4 mg/kg/day, IP | e 1% CMC, PO | |
b Dosed at 8 mg/kg/day, IP | f 86 mg/dL LDL-Cholesterol | |
c Dosed at 90 mg/kg/day, IP | g 63 mg/dL HDL-Cholesterol |
Conclusions
Experimental
General:
Chemistry
Hypolipidemic Studies.
Statistical Analysis.
Acknowledgements
References
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Holub, J.M.; O'Toole-Colin, K.; Getzel, A.; Argenti, A.; Evans, M.A.; Smith, D.C.; Dalglish, G.A.; Rifat, S.; Wilson, D.L.; Taylor, B.M.; et al. Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in Rodents. Molecules 2004, 9, 134-157. https://doi.org/10.3390/90300134
Holub JM, O'Toole-Colin K, Getzel A, Argenti A, Evans MA, Smith DC, Dalglish GA, Rifat S, Wilson DL, Taylor BM, et al. Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in Rodents. Molecules. 2004; 9(3):134-157. https://doi.org/10.3390/90300134
Chicago/Turabian StyleHolub, Justin M., Kathy O'Toole-Colin, Adam Getzel, Anthony Argenti, Michael A. Evans, Daniel C. Smith, Gerard A. Dalglish, Shahzad Rifat, Donna L. Wilson, Brett M. Taylor, and et al. 2004. "Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in Rodents" Molecules 9, no. 3: 134-157. https://doi.org/10.3390/90300134