Abstract

Various drugs have been developed to treat obesity, but these have undesirable secondary effects, and an efficient but non-toxic anti-obesity drug from natural sources is desired. This study investigated the anti-obesity effects and mechanisms of action of acetylshikonin (AS)—which is used in traditional Chinese medicine—in rats on a high-fat diet (HFD). Rats were fed a normal diet or an HFD; the latter group was received no treatment or were treated with 100, 300, or 900 mg/kg AS extract by intragastric administration for 6 weeks. In addition, 3T3-L1 adipocytes were treated with AS and the effects on adipogenesis and lipolysis were evaluated by western blot analysis of adipogenic transcription factors and lipid-metabolizing enzyme levels and the phosphorylation status of protein kinase (PK) A and hormone-sensitive lipase (HSL). AS prevented HFD-induced obesity including reduction in body weight, white adipose tissue content, liver mass, and serum triglyceride and free fatty acid levels in rats. It also suppressed the expression of adipogenic differentiation transcription factors and decreased the expression of the adipocyte-specific proteins HSL and adipose triglyceride lipase (ATGL). Furthermore, AS treatment induced lipolysis, leading to the release of glycerol and increased in PKA and HSL phosphorylation. These findings demonstrate that AS has anti-obesity effects in a rat model and may be a safe treatment for obesity in humans.

Highlights

  • Obesity has become a global epidemic, especially in developed countries

  • The present study addressed this issue by evaluating the anti-obesity effect of AS and the associated mechanisms in a rat model of obesity induced by a high-fat diet (HFD)

  • The food efficiency ratio and body weight of the HFD model group were increased by 30.6% and 49.3%, respectively, relative to the normal controls (P < 0.05 and P < 0.01, respectively) (Fig 1)

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Summary

Introduction

Obesity has become a global epidemic, especially in developed countries. In 2013–2014, More than 42 million children under the age of 5 and more than 1.9 billion adults 18 years and older were overweight [1]. Obesity is a complex metabolic disorder linked to an increased risk of common and serious human diseases, including type 2 diabetes mellitus, coronary atherosclerotic heart disease, and cardiovascular diseases such as hypertension and hyperlipidemia [2, 3]. Obesity is defined as excessive fat mass and expansion of adipose tissue resulting from adipocyte hypertrophy and hyperplasia that lead to weight gain and a body mass index > 30 kg/m2.

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