In vitro and in silico toxicity evaluation of bioactive 4'-aminochalcone derivatives.

The 4'-aminochalcones compounds are open-chain flavonoids structures which have shown a known array of pharmacological activities, such as antibacterial, antifungal, anti-inflammatory and antitumor effects. There is little toxicological information available about these compounds in the literature. Therefore, the investigation of toxic effects of three 4'-aminochalcone derivatives was performed using in silico and in vitro assays. In silico provided results that indicated the occurrence of mutagenic and genotoxic effects. In vitro tests, using Cellular Proliferation and Viability, Micronucleus, and DNA damage by Comet assay, showed that the compounds studied also present mutagenic and genotoxic effects, which confirm the result determined by the in silico analysis. The use of experimental and computational models is complementary to each other and the results determined for 4'-aminochalones suggest that the chalcones should also be carefully considered since they show some risks to cause toxic effects to human cells.

14 Days of supplementation with blueberry extract shows anti-atherogenic properties and improves oxidative parameters in hypercholesterolemic rats model.

The effects of supplementation with blueberry (BE) extract (Vaccinium ashei Reade) for 14 consecutive days on biochemical, hematological, histopathological and oxidative parameters in hypercholesterolemic rats were investigated. After supplementation with lyophilized extract of BE, the levels of total cholesterol, low-density lipoprotein cholesterol and triglycerides were decreased. Histopathological analysis showed significant decrease (p < 0.05) of aortic lesions in hypercholesterolemic rats. Oxidative parameters showed significant reductions (p < 0.05) in oxidative damage to lipids and proteins and an increase in activities of antioxidant enzymes such as catalase, superoxide dismutase and glutathione peroxidase. The BE extract showed an important cardioprotective effect by the improvements in the serum lipid profile, antioxidant system, particularly in reducing oxidative stress associated with hypercholesterolemia and anti-atherogenic effect in rats.

Preliminary in vitro assessment of the potential toxicity and antioxidant activity of Ceiba speciosa (A. St.-Hill) Ravenna (Paineira)

ABSTRACT The bark tea of Ceiba speciosa, a tropical tree of the Malvaceae family, is used in the Northwestern Region of Rio Grande do Sul state, Brazil, to reduce blood cholesterol levels. However, there are no scientific data on the efficacy and safety of this plant. The aim of the present study was to evaluate the in vitro antioxidant and toxic potential of bark extracts of C. speciosa. We performed a preliminary phytochemical analysis by high-performance liquid chromatography-diode array detection (HPLC-DAD) and evaluated the oxidative damage to proteins and lipids, the radical scavenging effect, and genotoxicity of the lyophilized aqueous extract (LAECs) and the precipitate obtained from the raw ethanol extract (Cs1). The phytochemical profile demonstrated the presence of phenolic and flavonoid compounds. The LAECs and Cs1 prevented damage to lipids and proteins at concentrations of 50 and 10 µg/mL. They also showed a scavenging effect on 2,2-diphenyl-1-pricril-hydrazyl (DPPH) radicals in a concentration-dependent manner. Furthermore, no genotoxic effect was observed at concentrations of 10, 5 and 2 µg/mL in the Comet assay. The present study is the first evaluation regarding the characterization of C. speciosa and its safety, and the results demonstrate its antioxidant potential and suggest that its therapeutic use may be relatively safe.