Abstract
Pancreatic lipase is the enzyme responsible for digestion and absorption of triglycerides, being its inhibition one of the widest studied methods used to determine the potential activity of natural products to inhibit dietary fat absorption. Decrease of energy intake from dietary fat through inhibition of this enzyme may be an excellent strategy to prevent and treat obesity. The inhibitory activity on pancreatic lipase enzyme of Diospyros kaki fruit and Citrus unshiu peel mixture extract (PCM) was evaluated in vitro and its antiobesity effects were studied based on the serum lipid parameters analysis from high-fat diet- (HFD-) fed mice in vivo. PCM was orally administered at a dose of 50 and 200 mg/kg body weight for 6 weeks. In addition, the activity of pancreatic lipase was assessed using orlistat (positive control). PCM exhibited inhibitory effect on lipase activity with IC50 value of 507.01 μg/mL. Moreover, serum triacylglycerol, total cholesterol levels, and visceral fat weight were significantly reduced compared to HFD control mice in PCM 200 mg/kg-treated mice (p < 0.05). These results suggest that PCM administration may be a novel potential antiobesity agent for reduction of fat absorption via inhibition of pancreatic lipase.
Highlights
Obesity results from an energy imbalance and is considered a serious and global health risk by the World Health Organization (WHO). It is associated with health problems like dyslipidemia, hypertension, fatty liver disease, diabetes mellitus, cancers, osteoarthritis, and asthma [1, 2]
WHO predicted that this number will be elevated to approximately 3.3 billion by 2030 [4]
The obtained result showed that PCM inhibited pancreatic lipase activity with IC50 of 507.01 μg/mL compared to orlistat with IC50 of 0.218 μg/mL (Figure 2)
Summary
Obesity results from an energy imbalance and is considered a serious and global health risk by the World Health Organization (WHO). Orlistat (Xenical) approved by FDA, relatively effective drug for long-term treatment of obesity, exerts the drug efficacy through inhibition of pancreatic lipase enzyme and prevents the absorption of approximately 30% of dietary fat [5]. It is limited in its use due to severe gastrointestinal side effects. The biological and multiple compounds of two herbs, Diospyros kaki fruit or Citrus unshiu peel, performed a pharmacological effect such as hypocholesterolemic [19], antiadipogenic [20], anti-inflammatory [21], antioxidant [22], antitumor [13] effects. The present study aims to investigate the inhibition property on porcine pancreatic lipase in vivo and changes in body weight and serum lipid parameters and visceral fat weight on an experimental model of obesity
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