Biological Evaluation of Chalcones and Analogues as Hypolipidemic Agents

Santos, Lorena dos; Pedrosa, Rozangela Curi; Corrêa, Rogério; Filho, Valdir Cechinel; Nunes, Ricardo José; Yunes, Rosendo A.

doi:10.1002/ardp.200600034

Cited by 21 publications

(10 citation statements)

References 18 publications

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“…In support of this, Santos et al reported that chalcone compounds had significant anti-lipidemic activity. 55) In summary, the present study demonstrated that S. flavescens and its components, kurarinol and kuraridinol, had hypolipidemic effects in poloxamer 407-induced hyperlipidemic rats, where the compounds significantly lowered serum TC, TG, and LDL-C concentrations, elevated HDL-C levels, and decreased serum A.I. values.…”

Section: Discussionsupporting

confidence: 53%

Hypolipidemic Effects of Sophora flavescens and Its Constituents in Poloxamer 407-Induced Hyperlipidemic and Cholesterol-Fed Rats

Kim

Jeong

Jung

et al. 2008

Biological & Pharmaceutical Bulletin

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In this study, we investigated the hypolipidemic effects of Sophora flavescens in poloxamer 407-induced hyperlipidemic and cholesterol-fed rats. The MeOH extract and 4 fractions of S. flavescens were administered at doses of 250 and 100 mg/kg body weight, respectively, once a day for 3 d to the poloxamer 407-induced hyperlipidemic rats. Serum lipid levels such as total cholesterol (TC), triglycerides (TG), and low-density lipoprotein-cholesterol (LDL-C) were markedly elevated in the poloxamer 407-induced hyperlipidemic control rats, while lipid levels were significantly decreased in the rats administered the MeOH extract or 4 fractions of S. flavescens. In addition, serum high-density lipoprotein-cholesterol (HDL-C) was reduced in the poloxamer 407-induced hyperlipidemic control rats. However, oral administration of both the MeOH extract and 4 fractions significantly increased HDL-C levels. Of the tested fractions, the EtOAc fraction showed the strongest lipid-lowering effect, as well as a high antiatherogenic potential with atherogenic index (A.I.) values of less than 1.92. We also investigated the hypolipidemic effects of the main compounds of the EtOAc fraction, kurarinol and kuraridinol, using the hyperlipidemic and hypercholesterolemic animal models. Here, elevated TC, TG, and LDL-C levels in the poloxamer 407-induced hyperlipidemic and cholesterol-fed rats were significantly reduced after oral administration of the compounds, and HDL-C levels had a significant increase. Furthermore, A.I. values were lowered by administering kurarinol and kuraridinol. In particular, kuraridinol exhibited stronger protective activities against hyperlipidemia than kurarinol. These results suggest that S. flavescens and its constituents may be effective cholesterol-lowering agents and useful for preventing hypercholesterolemic atherosclerosis.

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Section: Discussionsupporting

confidence: 53%

Hypolipidemic Effects of Sophora flavescens and Its Constituents in Poloxamer 407-Induced Hyperlipidemic and Cholesterol-Fed Rats

Kim

Jeong

Jung

et al. 2008

Biological & Pharmaceutical Bulletin

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“…Fluvastatin ( 25 ), compound with indole moiety, was the first synthetic 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor (statin) and is used in the management of dyslipidemia in the primary and secondary prevention of cardiovascular disease [ 69 , 70 ]. In addition, a recent literature survey revealed that chalcone derivatives, such as 4′,4-dichlorochalcone ( 26 ), exhibited potential hypolipidemic activities [ 71 ]. Fibrates are selective agonists of the peroxisome proliferator-activated receptor gamma (PPARγ).…”

Section: Design Of New Chalcone Derivativesmentioning

confidence: 99%

Chalcone Derivatives: Promising Starting Points for Drug Design

et al. 2017

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Medicinal chemists continue to be fascinated by chalcone derivatives because of their simple chemistry, ease of hydrogen atom manipulation, straightforward synthesis, and a variety of promising biological activities. However, chalcones have still not garnered deserved attention, especially considering their high potential as chemical sources for designing and developing new effective drugs. In this review, we summarize current methodological developments towards the design and synthesis of new chalcone derivatives and state-of-the-art medicinal chemistry strategies (bioisosterism, molecular hybridization, and pro-drug design). We also highlight the applicability of computer-assisted drug design approaches to chalcones and address how this may contribute to optimizing research outputs and lead to more successful and cost-effective drug discovery endeavors. Lastly, we present successful examples of the use of chalcones and suggest possible solutions to existing limitations.

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“…An increase of triglycerides was observed in free chalcone-treated animals, while the encapsulation of R13 and R15 avoided these effects. Chalcones also induced a decrease in total cholesterol that could be related to a hypolipidemic effect of chalcones, as demonstrated in another study [ 36 ].…”

Section: Resultsmentioning

confidence: 62%

In vitro and in vivo Effects of Free and Chalcones-Loaded Nanoemulsions: Insights and Challenges in Targeted Cancer Chemotherapies

Winter

Pizzol

Locatelli

et al. 2014

IJERPH

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Several obstacles are encountered in conventional chemotherapy, such as drug toxicity and poor stability. Nanotechnology is envisioned as a strategy to overcome these effects and to improve anticancer therapy. Nanoemulsions comprise submicron emulsions composed of biocompatible lipids, and present a large surface area revealing interesting physical properties. Chalcones are flavonoid precursors, and have been studied as cytotoxic drugs for leukemia cells that induce cell death by different apoptosis pathways. In this study, we encapsulated chalcones in a nanoemulsion and compared their effect with the respective free compounds in leukemia and in non-tumoral cell lines, as well as in an in vivo model. Free and loaded-nanoemulsion chalcones induced a similar anti-leukemic effect. Free chalcones induced higher toxicity in VERO cells than chalcones-loaded nanoemulsions. Similar results were observed in vivo. Free chalcones induced a reduction in weight gain and liver injuries, evidenced by oxidative stress, as well as an inflammatory response. Considering the high toxicity and the side effects induced generally by all cancer chemotherapies, nanotechnology provides some options for improving patients’ life quality and/or increasing survival rates.

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Biological Evaluation of Chalcones and Analogues as Hypolipidemic Agents

Cited by 21 publications

References 18 publications

Hypolipidemic Effects of Sophora flavescens and Its Constituents in Poloxamer 407-Induced Hyperlipidemic and Cholesterol-Fed Rats

Hypolipidemic Effects of Sophora flavescens and Its Constituents in Poloxamer 407-Induced Hyperlipidemic and Cholesterol-Fed Rats

Chalcone Derivatives: Promising Starting Points for Drug Design

In vitro and in vivo Effects of Free and Chalcones-Loaded Nanoemulsions: Insights and Challenges in Targeted Cancer Chemotherapies

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