Abstract
Dihydropyranocoumarins (DPCs) were isolated from Peucedanum japonicum Thunb as anti-obesity compounds in 3T3-L1 adipocytes assay; however, it is uncertain whether DPC exerts anti-obesity activity in vivo. Therefore, this study evaluated the oral intake of pure DPCs in mice fed a high-fat diet, and also attempted to enhance its activity by nanoparticulation. Increases in body weight gain and fat accumulation in white adipose tissues were significantly suppressed by the dietary intake of DPCs (1.943 mg/mouse/day). DPCs intake also significantly decreased the mean size of adipocytes and upregulated mRNA levels of thermogenesis-related genes. Nanoparticulation of DPCs with polylactic-co-glycolic acid (PLGA) dramatically increased its activity almost 100-fold over that of a non-nanoparticulated form. Thus, our findings clearly demonstrated the anti-obesity activity of DPCs in vivo and suggested that PLGA nanoparticle encapsulation was useful to enhance the anti-obesity activity of DPCs with the aim to develop natural and safe anti-obesity agents.
Highlights
IntroductionThe nutritional value of food can be improved by adding bioactive compounds; most of their positive effects are impaired by their poor bioavailability, limited water solubility, and metabolic transformations [3]
Obesity is well known as a major global health issue and several therapeutic agents have been developed for treating this condition by reducing nutrient absorption or by enhancing thermogenesis and lipid turnover [1,2]; considering the safety of these agents and their adverse side effects, medicinal plants and their active compounds merit investigation for the development of more natural and safer anti-obesity agents.The nutritional value of food can be improved by adding bioactive compounds; most of their positive effects are impaired by their poor bioavailability, limited water solubility, and metabolic transformations [3]
high performance liquid chromatography (HPLC) analyses showed that purified DPC extract has two major peaks, peucedanocoumarin III (PCIII) (41.7%, v/v) and PTX (57.3%, v/v) (Figure S1)
Summary
The nutritional value of food can be improved by adding bioactive compounds; most of their positive effects are impaired by their poor bioavailability, limited water solubility, and metabolic transformations [3]. One strategy for reducing these limitations is to integrate these bioactive compounds into nanoparticles. Delivery systems using nanoparticles have been investigated as a possible approach to markedly improve the bioavailability of drug and food bioactives [3,4]. Carrier systems of biodegradable particulates are of interest as a potential means to orally delivery compounds to improve their bioavailability [5].
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