Abstract

Due to the side effects of obesity medications, many studies have focused on the natural products used in the daily diet to control weight. Moringa seed pods and leaves are widely used as vegetables or diet supplements due to the high nutrition value. However, no bioactivity-guided anti-adipogenic study was previously conducted. Therefore, a preadipocyte cell line was adopted as the bioactivity assay to identify the anti-adipogenic compounds in the peeled Moringa seed. Two known sulphur-containing compounds (1 and 2) were isolated and identified. Compound 2, 4-(α-l-rhamnosyloxy) benzyl isothiocyanate, showed a great anti-adipogneic effect with an IC50 value of 9.2 μg/mL. The isothiocyanate (ITC) group in compound 2 could be responsible for the inhibitory activity. In addition, a series of compounds with the ITC group were used to further investigate the structure-activity relationship, indicating foods containing ITC derivatives have the potential of being used to control weight.

Highlights

  • Obesity is characterised by increased mass in the adipose tissue

  • Five anti-obesity medications have been approved by the Food and Drug Administration (FDA), but studies have demonstrated the side effects of these medications [3]

  • The only difference was the presence of an isothiocyanate group in compound 2, which played a vital role in the anti-adipogenic effect towards 3T3-L1 cells

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Summary

Introduction

Obesity is characterised by increased mass in the adipose tissue. In addition to the cosmetic concern, the most serious problem is the increased risk of other diseases, such as cardiovascular disease, type 2 diabetes, and cancers, etc. [1]. Extracts from the leaves or seeds were reported to show health benefits such as cholesterol-lowering, anti-diabetic, anti-hypertensive, Molecules 2020, 25, 2504; doi:10.3390/molecules25112504 www.mdpi.com/journal/molecules. Molecules 2020, 25, 2504 leaves or seeds were reported to show health benefits such as cholesterol-lowering, anti-diabetic, anti-hypertensive, anti-inflammatory, antioxidant, and anti-hyperlipidaemic effects. In the of the Moringa with composition the anti-adipogenic activity. 3T3-L1 cell line, which has the fibroblast-like morphology, has been cell line,study, whichthe haspre-adipocyte the fibroblast-like morphology, has been employed as a bioactivity-guided model employed as a bioactivity-guided model combined with analytical techniques (i.e., NMR and combined with analytical techniques (i.e., NMR and LC-MS) to isolate and identify anti-adipogenic. The hypothesis of this study is that some compounds in the Moringa seed are able to inhibit lipid in the Moringafrom seedpreventing are able toadipogenesis, inhibit lipid accumulation fromchemical preventing adipogenesis, and some accumulation and some specific groups could influence the specific chemicalactivity.

Bioactivity-Guided
Structure Elucidation of Compounds 1 and 2 from Moringa Seeds
Anti-Adipogenic Effects of Purified Compounds
Structure-Activity
Effects
Materialsand Methods
LC-MS Analysis
Purification of Compounds 1 and 2
Anti-Adipogenic Activity Assay
Cytotoxicity Assay
Conclusions
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