Allyl-isothiocyanate (AITC) is an organosulfur phytochemical found in abundance in common cruciferous vegetables such as mustard, wasabi, and cabbage. Although AITC is metabolized primarily through the mercapturic acid pathway, its exact pharmacokinetics remains undefined and the biological function of AITC metabolites is still largely unknown. In this study, we evaluated the inhibitory effects of AITC metabolites on lipid accumulation in vitro and elucidated the pharmacokinetics and tissue distribution of AITC metabolites in rats. We found that AITC metabolites generally conjugate with glutathione (GSH) or N-acetylcysteine (NAC) and are distributed in most organs and tissues. Pharmacokinetic analysis showed a rapid uptake and complete metabolism of AITC following oral administration to rats. Although AITC has been reported to exhibit anti-tumor activity in bladder cancer, the potential bioactivity of its metabolites has not been explored. We found that GSH-AITC and NAC-AITC effectively inhibit adipogenic differentiation of 3T3-L1 preadipocytes and suppress expression of PPAR-γ, C/EBPα, and FAS, which are up-regulated during adipogenesis. GSH-AITC and NAC-AITC also suppressed oleic acid-induced lipid accumulation and lipogenesis in hepatocytes. Our findings suggest that AITC is almost completely metabolized in the liver and rapidly excreted in urine through the mercapturic acid pathway following administration in rats. AITC metabolites may exert anti-obesity effects through suppression of adipogenesis or lipogenesis.

We evaluated whether Monascus-fermented soybean extracts (MFSE) enriched with bioactive mevinolins (natural statins) and aglycone isoflavones (daidzein, glycitein, and genistein) perform an additive hypolipidemic effect in hyperlipidemic rats than unfermented soybean extracts (UFSE), which have a higher level of glucoside isoflavones (daidzin, glycitin, and genistin) without mevinolin. The oral administration of MFSE (200 and 400 mg kg(-1) body weight) significantly lowered the serum total cholesterol, triglyceride, and low-density lipoprotein cholesterol (LDL-C) levels (p < 0.01) and raised high-density lipoprotein cholesterol (HDL-C) levels (p < 0.05) in hyperlipidemic rats. The MFSE group had a significantly lower 3-hydroxyl-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity and higher atherogenic index (calculated as HDL-C/LDL-C) when compared with the UFSE group (400 mg kg(-1) body weight) (p < 0.05). Treatment with both MFSE200 and MFSE400 groups for 40 days significantly reduced the activities of serum aspartate aminotransferase and alanine aminotransferase by averages of 35.6 and 43.2%, respectively, as compared to the high-fat diet group (p < 0.01). The results indicate that MFSE performs a more potent hypolipidemic action via improvement of the lipid profiles and down-regulated HMG-CoA reductase activity than UFSE in hyperlipidemic rats.

This study aimed to investigate the anti-obesity effects of yogurt fermented by Lactobacillus plantarum Q180 in diet-induced obese rats. To examine the effects, male Sprague-Dawley rats were fed on six different diets, as follows: Group A was fed an ND and orally administrated saline solution; Group B, an HFD and orally administrated saline solution; Group C, an HFD and orally administrated yogurt fermented by ABT-3 and L. plantarum Q180; Group D, an HFD and orally administrated yogurt with added Garcinia cambogia extract, fermented by ABT-3 and L. plantarum Q180; Group E, an HFD and orally administrated yogurt fermented by L. plantarum Q180; and Group F, an HFD and orally administrated yogurt with added Garcinia cambogia extract, fermented by L. plantarum Q180 for eight weeks. After eight weeks, the rate of increase in bodyweight was 5.14%, 6.5%, 3.35% and 10.81% lower in groups C, D, E and F, respectively, compared with group B; the epididymal fat weight of groups E and F was significantly lower than that of group B; and the level of triglyceride and leptin was significantly reduced in groups C, D, E and F compared to group B. In addition, the level of AST was reduced in group C compared to the other groups. To examine the effects of yogurt on the reduction of adipocyte size, the adipocyte sizes were measured. The number of large-size adipose tissue was less distributed in groups A, C, D, E and F than in group B.

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