The pharmacological effects of novel 5-fluoro-N-(9,10-dihydro-9,10-dioxoanthracen-8-yl)-1H-indole-2-carboxamide derivatives on plasma lipid profile of Triton-WR-1339-induced Wistar rats.
A novel series of 5-fluoro-N-(9,10-dihydro-9,10-dioxoanthracen-8-yl)-1H-indole-2-carboxamides (3c-3g) were synthesized. The present study was undertaken to investigate the possible antihyperlipidemic effect of these novel compounds on hyperlipidemic rats. Hyperlipidemia was induced by a single intraperitoneal injection of Triton WR-1339 (300 mg/kg). The tested animals were divided into normal control (NCG), hyperlipidemic control (HCG), compounds 3c-, 3d-, 3e-, 3f-, 3g- and bezafibrate (BF)-treated groups. At a dose of 15 mg/kg, compounds 3c-3g and BF (100 mg/kg) significantly (p < 0.0001) reduced elevated plasma triglycerides levels after 12 and 24 h compared to the hyperlipidemic control group. However, only compounds 3e and 3g obviously showed a significant (p < 0.0001) reduction in plasma total cholesterol levels after 12 and 24 h. Moreover, high-density lipoprotein cholesterol levels were significantly increased in all treated groups. The current study demonstrates that 5-fluoro-N-(9,10-dihydro-9,10-dioxoanthracen-8-yl)-1H-indole-2-carboxamides (3c-3g) have a definite antihyperlipidemic potential and these beneficial activities may contribute to their cardioprotective and antiatherosclerotic role.
Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan. gassan10@yahoo.com
Ghassan
G
Shattat
Tariq
T
Al-Qirim
Ghassan Abu
GA
Sheikha
Yusuf
Y
Al-Hiari
Kamal
K
Sweidan
Rania
R
Al-Qirim
Suhair
S
Hikmat
Lama
L
Hamadneh
Sameer
S
Al-Kouz
D000818:Animals; D000880:Anthraquinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006949:Hyperlipidemias / Q000139:chemically induced / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008055:Lipids / Q000097:blood; D008297:Male; D015394:Molecular Structure; D011092:Polyethylene Glycols; D051381:Rats; D017208:Rats, Wistar
D000880:Anthraquinones; D000960:Hypolipidemic Agents; D007211:Indoles; D008055:Lipids; D011092:Polyethylene Glycols; C016811:tyloxapol