Abstract

Pancreatic lipase is considered an important target for the control of hyperlipidemia. Several plants, especially those rich in phenolic metabolites, have been shown to have anti-hyperlipidemic activity and are considered a good alternative for obesity prevention. Extracts of the stem bark of Endopleura uchi (Huber) Cuatrec (Humiriaceae) were evaluated for the inhibitory activity on the pancreatic lipase enzyme, as well as their antioxidant potential were verified in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) test. In addition, the total phenolics (TPC) and flavonoids contents (TFC) were estimated. In general way, the acetonic and ethanolic extracts showed better results than aqueous extract. At the concentration of 1 mg/mL, both acetonic and ethanolic extracts inhibited the activity of pancreatic lipase by 49.33 and 36.88%, representing 135.26 and 102.75 of inhibited lipase activity per gram of extract (ILA/g). On the other hand, the aqueous extract inhibited lipase by 47.54% at the concentration of 2 mg/mL, which means 213.84 ILA/g. The highest antioxidant activity was observed for the acetonic extract with a 50% effective concentration (EC50) of 7.9 µg/mL, followed by the ethanolic extract with EC50 of 9.7 µg/mL and the aqueous extract with EC50 of 12.4 µg/mL. TPC in gallic acid equivalent per gram of sample (GAE/g) were 0.52, 0.51 and 0.35 respectively for the ethanolic, acetonic and aqueous extracts. In turn, TFC in quercetin equivalent per gram of sample (QE/g) were 2.13, 1.89 and 1.35 for the acetonic, ethanolic and aqueous extracts, respectively. Positive and strong correlations (r Pearson > 9.0) between TPC and antioxidant activity were found for all 3 extracts. These results suggest that both pancreatic lipase inhibition and antioxidant activity were distinguished by organic solvents and water extraction. Furthermore, organic extracts (acetone and ethanol) showed to be richer in phenolic metabolites. These metabolites may be related to the biological activities that were found, indicating the stem bark extracts of E. uchi as possible candidates for the development of strategies in the prevention of obesity and hyperlipidemia. Key words: Antioxidant activity, pancreatic lipase activity, Endopleura uchi extracts.

Highlights

  • A possible imbalance between consumption of high calorie diet and lipids, body weight and lipoproteins in the body (Sharma et al, 2005; Nguyen et al, 2012) can influence the susceptibility of the organism to disorders and changes in lipid metabolism, increasing reserves fat (Montoya et al, 2002; Coelho et al, 2011), with subsequent accumulation of adipose tissue and abdominal fat, causing weight gain (Daniels, 2006; de Oliveira et al Barbieri, 2012). These disorders can be accompanied by changes in the lipid profile - increased serum triglycerides, total cholesterol, high density lipoproteins (LDL) cholesterol and free fatty acids and decreased high density lipoproteins (HDL) (Bertolami et al, 2004; Wilborn et al, 2005), causing rising prevalence of dyslipidemias (Pozzan et al, 2004; Grillo et al, 2005), pro-inflammatory conditions, oxidative stress - lipid peroxidation of low density lipoproteins (LDL) (Bevilacqua et al, 2007; Singh et al, 2011) and atherosclerosis (Sorace et al, 2006; Peluso et al, 2012)

  • Inhibition of the pancreatic lipase, an enzyme essential for the metabolism of fats (Yun, 2010; Sukhdev and Singh, 2013) and formation of the lipoproteins: LDL, intermediate-density lipoprotein (IDL), LDL and very-lowdensity lipoprotein (VLDL) in the body (Sharma et al, 2005; Klop et al, 2013), has become a valuable therapeutic alternative for the treatment of dyslipidemia resulting from excess weight and obesity induced by a hyperlipidemic diet (Zhang et al, 2008; Lee et al, 2010; Lewis et al, 2012)

  • Aqueous solutions containing organic solvent ranging from 50 to 80%, tend to modulate the polarity of the solvent mixture (Do et al, 2014) and the variety of polyphenolic constituents, unlike a pure aqueous solvent (Mazandarani et al, 2012). This may explain the higher values for both total flavonoids and total phenolics (p

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Summary

Introduction

These disorders can be accompanied by changes in the lipid profile - increased serum triglycerides, total cholesterol, high density lipoproteins (LDL) cholesterol and free fatty acids and decreased high density lipoproteins (HDL) (Bertolami et al, 2004; Wilborn et al, 2005), causing rising prevalence of dyslipidemias (Pozzan et al, 2004; Grillo et al, 2005), pro-inflammatory conditions, oxidative stress - lipid peroxidation of low density lipoproteins (LDL) (Bevilacqua et al, 2007; Singh et al, 2011) and atherosclerosis (Sorace et al, 2006; Peluso et al, 2012). It is popularly known as ‘uxi amarelo’ (Gaia and Shanley, 2004)

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