Abstract
Acer truncatum Bunge is now widely cultivated throughout the world. Fatty acid synthase (FAS) is a potential target in the treatment of both obesity and cancer. Only a few FAS inhibitors have been reported. In this study, the inhibitory effect of A. truncatum seed coat (ESA) on FAS and the inhibition mechanisms were investigated using a FAS activity assay and an enzyme kinetics study. The main chemicals of ESA were analyzed with UPLC-MS/MS. The effects of ESA on 3T3-L1 adipocyte differentiation and lipid accumulation were investigated using Oil red O staining. We first identified seven main compounds (quinic acid, malic acid, gentisic acid, procyanidin dimer, procyanidin trimer, catechin, and quercetin) from 50% ethanol extracts of seed coats of A. truncatum (ESAs), which were then found to inhibit 3T3-L1 adipocyte differentiation at the concentration of 50 μg/mL. ESA obviously reduced the visible triglyceride droplets accumulation, and dramatically decreased the number of the adipocytes at a comparatively high concentration. It is suggested that the effects are due to the inhibition of FAS by ESA; FAS activity is inhibited by ESA at a half inhibition concentration (IC50) of 0.57 μg/mL, which is lower than that of classically known FAS inhibitors. Meanwhile, ESA displayed different inhibition kinetics and reacting sites for FAS. These results provide new clues for the development of novel products for obesity treatment and a scientific basis for the full use of byproducts for future industrial production of vegetable oil.
Highlights
Obesity is prevailing at an alarming rate in the developed countries but the developing countries
We report that the extracts of seed coat of A. truncatum (ESA) effectively inhibit differentiation of 3T3-L1 adipocytes by reducing the size and number of these cells
We found that ESA had high inhibitory activity on Fatty acid synthase (FAS) activity, with an IC50 value of 0.57 μg/mL, which is lower than that of EGCG and cerulenin [5]
Summary
Obesity is prevailing at an alarming rate in the developed countries but the developing countries. Many diseases are considered to be related to obesity, such as cardiovascular disease [1], type 2 diabetes [2] and cancer [3]. Novel treatments for obesity are valuable to reduce obesity-related health problems. Adipose tissue is often considered the core of obesity. Increase in adipose tissue mass is related to both the size and number of adipocytes (hypertrophy and hyperplasia), which all rely on the differentiation from preadipocytes into adipocytes. It has been reported that FAS gene expression in adipocytes is associated with obesity and diabetes [4]
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