Key Laboratory of Plant Resources and Beijing Botanical Garden, Institute of Botany, Chinese Academy of Sciences, Beijing 100093, China.
School of Kinesiology and Health, Capital University of Physical Education and Sports, No. 11 Beisanhuanxi Road, Beijing 100191, China.
Molecules. 2022 Feb 16;27(4):1324. doi: 10.3390/molecules27041324.
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 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 (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 (IC) 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.
麻疯树在全世界范围内广泛种植。脂肪酸合酶（FAS）是治疗肥胖症和癌症的潜在靶点。目前仅报道了少数几种 FAS 抑制剂。本研究采用 FAS 活性测定和酶动力学研究，考察了种皮（ESA）对 FAS 的抑制作用及抑制机制。采用 UPLC-MS/MS 分析了 ESA 的主要化学成分。采用油红 O 染色法研究了 ESA 对 3T3-L1 脂肪细胞分化和脂质积累的影响。首先从麻疯树种子种皮 50%乙醇提取物中鉴定出 7 种主要化合物（奎宁酸、苹果酸、龙胆酸、原花青素二聚体、原花青素三聚体、儿茶素和槲皮素），发现其在 50μg/mL 浓度下可抑制 3T3-L1 脂肪细胞分化。ESA 明显减少可见的甘油三酯滴积累，在较高浓度下明显减少脂肪细胞数量。表明这些作用是由于 ESA 抑制 FAS 所致；ESA 以 0.57μg/mL 的半抑制浓度（IC）抑制 FAS 活性，低于经典的 FAS 抑制剂。同时，ESA 对 FAS 的抑制表现出不同的动力学和反应部位。这些结果为开发新型肥胖症治疗产品提供了新线索，并为充分利用植物油未来工业生产的副产物提供了科学依据。
