Synthesis and &lt;i&gt;in vivo&lt;/i&gt; anti-hyperlipidemic activity of novel n-benzoylphenyl-2-furamide derivatives in Wistar rats

Hikmat, Suhair; Al-Qirim, Tariq; Alkabbani, Dania; Shattat, Ghassan; Sheikha, Ghassan Abu; Sabbah, Dima A.; Khalaf, Reema Abu; Al‐Hiari, Yusuf

doi:10.4314/tjpr.v16i1.26

Cited by 6 publications

(15 citation statements)

References 21 publications

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“…As reported in the literature, the maximum plasma TC and TG levels were reached after 20 h. of Triton WR-1339 treatment followed by a decline to the standard values. In our study, the results of tested compounds were analyzed after 18 h. of treatment and Triton WR-1339 model gave similar pattern in lipid profile changes compared to published data [21][22][23] ( Table 1).…”

Section: Discussionsupporting

confidence: 70%

Synthesis and <i>in Vivo</i> Lipid-Lowering Activity of Novel Imidazoles-5-carboxamide Derivatives in Triton-WR-1339-Induced Hyperlipidemic Wistar Rats

Jasim

Sheikha

Abuzaid

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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A new series of imidazole-5-carboxamide derivatives were prepared and tested for their anti-hyperlipidemic activity in Triton-WR-1339-induced hyperlipidemic Wistar rats. The purpose of this research was to improve benzophenone carboxamides water solubility maintaining at the same time the antihyperlipidemic activity. Compounds 4, 6, 10, and 11 were synthesized through a coupling reaction between imidazoles-5-carbonyl chloride and amino benzophenones. The tested animals (n 48) were divided into six groups: the first group (hyperlipidemic control group; HCG) received an intraperitoneal injection (i.p.) of (300 mg/kg) Triton WR-1339. The second group received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of bezafibrate (100 mg/kg) (bezafibrate; BF). The third, fourth, fifth, and sixth groups received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of (30 mg/kg) of compounds 4, 6, 10, and 11, respectively. At a dose of 30 mg/kg body weight compounds 4, 6, 10, and 11 significantly (p<0.0001) decreased the plasma level of triglyceride (TG), low-density lipoprotein (LDL) and total cholesterol (TC) levels after 18 h of treatment. Additionally, compounds 4, 6, 11 and bezafibrate (100 mg/kg) significantly (p<0.0001) increased the plasma level of high-density lipoprotein (HDL) levels, which is known for its preventive role against atherogenesis. These results demonstrate the possibility of pharmacokinetic properties improvement maintaining the biological and pharmacological profile of these compounds.

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Section: Discussionsupporting

confidence: 70%

Synthesis and <i>in Vivo</i> Lipid-Lowering Activity of Novel Imidazoles-5-carboxamide Derivatives in Triton-WR-1339-Induced Hyperlipidemic Wistar Rats

Jasim

Sheikha

Abuzaid

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Epidemiological studies have demonstrated that hyperlipidaemia is the most prevalent indicator of susceptibility to atherosclerosis and coronary heart diseases (CHD). Therefore, decreasing plasma lipids play a major role in the treatment and prevention of CHD ( 6 ). Furthermore, hyperlipidaemia and hypercholesterolemia are not only secondary metabolic dysregulations associated with diabetes but also represent increased risk factors for its development ( 27 ).…”

Section: Discussionmentioning

confidence: 99%

“…The side effects of statins and fibrates are well documented ( 4 , 5 ). For this reason, many studies have been conducted to evaluate the potential lipid-lowering activity of synthetic and natural compounds ( 6 ). It has been suggested that herbal remedies are among the best existing alternative therapies and have been used since ancient times ( 7 ) and they have contributed to the development of important drugs used currently in modern medicine ( 8 ).…”

Section: Introductionmentioning

confidence: 99%

Hypolipidaemic and Insulin Secretagogue Activities of (R)-(−)-Carvone

Abbas

Oriquat

Al-Najjar

et al. 2020

MJMS

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Background: Dyslipidaemias are common in patients with diabetes mellitus. A high prevalence of type 2 diabetes in hyperlipidaemic patients also exists. The aim of this study was to find a treatment that lowers both blood glucose and lipid levels simultaneously. Methods: The hypolipidaemic effect of (R)-(−)-carvone was investigated in a tyloxapol- induced hyperlipidaemia mice model. Furthermore, its effect on insulin secretion and proliferation of 1.1E7 human pancreatic β-cells was studied. In addition, using molecular docking, the binding affinity of (R)-(−)-carvone against 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG- CoA) reductase was estimated. Results: (R)-(−)-carvone (100 mg/kg) decreased plasma triglyceride, total cholesterol, low-density lipoprotein cholesterol (LDL-C) levels and atherogenic index by 90.6%, 49.3%, 56.6% and 70.3%, respectively, but it had no effect on high-density lipoprotein cholesterol (HDL-C). Furthermore, it increased hepatic triglyceride level and catalase activity by 79.6% and 59.6%, respectively. In-vitro, 500 μM (R)-(−)-carvone increased insulin secretion by 454.4% and proliferation of 1.1E7 cells with no cytotoxic effects up to a concentration of 100 μM. Molecular docking simulation demonstrated a good binding affinity with –5.03 Kcal/mol of (R)-(−)-carvone to HMG-CoA reductase. Conclusion: The hypolipidaemic effect of (R)-(−)-carvone is comparable to that of fenofibrate. (R)-(−)-carvone has the advantage over fenofibrate of not producing hypoglycaemia in animals. Furthermore, (R)-(−)-carvone increased proliferation and insulin secretion of human pancreatic β-cells.

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“…Recently, in 2017, they further studied the antihyperlipidemic activities of a few more furamide derivatives containing benzophenone. 112 Compound 76 was found to be the most active. The observations of the authors suggested that the presence of a lipophilic moiety (benzophenone), a carboxamide linkage and a furan ring (which can form hydrogen bonds) are three important requirements for the activity of the synthesized molecules.…”

Section: Antihyperlipidemic Activitymentioning

confidence: 95%

Benzophenone: a ubiquitous scaffold in medicinal chemistry

Surana¹,

Chaudhary²,

Diwaker³

et al. 2018

Med. Chem. Commun.

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Synthesis and <i>in vivo</i> anti-hyperlipidemic activity of novel n-benzoylphenyl-2-furamide derivatives in Wistar rats

Abstract: Purpose: To synthesize and evaluate the anti-hyperlipidemic activity of a novel series of N-(benzoylphenyl)-2-furamides

Cited by 6 publications

References 21 publications

Synthesis and <i>in Vivo</i> Lipid-Lowering Activity of Novel Imidazoles-5-carboxamide Derivatives in Triton-WR-1339-Induced Hyperlipidemic Wistar Rats

Synthesis and <i>in Vivo</i> Lipid-Lowering Activity of Novel Imidazoles-5-carboxamide Derivatives in Triton-WR-1339-Induced Hyperlipidemic Wistar Rats

Hypolipidaemic and Insulin Secretagogue Activities of (R)-(−)-Carvone

Benzophenone: a ubiquitous scaffold in medicinal chemistry

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