Obesity is a global health concern. Piceatannol (Pic), an analog of resveratrol (Res), has many reported biological activities. In this study, we investigated the anti-obesity effect of Pic in a high-fat diet (HFD)-induced obese animal model. The results showed that Pic significantly reduced mouse body weight in a dose-dependent manner without affecting food intake. Serum total cholesterol (TC), low-density lipoprotein (LDL), high-density lipoprotein (HDL) levels, and blood glucose (GLU) were significantly lowered in Pic-treated groups. Pic significantly decreased the weight of liver, spleen, perigonadal and retroperitoneal fat compared with the HFD group. Pic significantly reduced the adipocyte cell size of perigonadal fat and decreased the weight of liver. Pic-treated mice showed higher phosphorylated adenosine 5 -monophosphate-activated protein kinase (pAMPK) and phosphorylated acetyl-CoA carboxylase (pACC) protein levels and decreased protein levels of CCAAT/enhancer-binding protein C/EBPα, peroxisome proliferator-activated receptor PPARγ and fatty acid synthase (FAS), resulting in decreased lipid accumulation in adipocytes and the liver. Pic altered the composition of the gut microbiota by increasing Firmicutes and Lactobacillus and decreasing Bacteroidetes compared with the HFD group. Collectively, these results suggest that Pic may be a candidate for obesity treatment.

Adlay (Coix lachryma-jobi L. var. ma-yuen Stapf) seeds have long been used to treat warts, chapped skin, rheumatism, and neuralgia in traditional Chinese medicine (TCM). Recently, studies demonstrated its anti-inflammatory, antiproliferative, antitumor, and antiallergic activities. In the present study, we first report the gastroprotective effects of dehulled adlay (DA) seeds, which consist of bran (AB) and endosperm (AE). The DA ethanolic extract (DAE) was prepared, along with the AB and AE ethanolic extracts (ABE and AEE), and the inhibitory effects of these extracts were tested on the AGS gastric cancer cell line. Results indicated that the ABE showed better antiproliferative activity, and 19 compounds were purified from AB in a further phenolic-compound-guided separation. Among the isolated compounds, caffeic and chlorogenic acids significantly suppressed the growth of AGS cells. In addition, the antiulcer activity of DA was examined in an indomethacin-induced gastric lesion model. The ulcer index (UI) and oxidative biomarkers in animals decreased, while the non-protein sulfhydryl (NPSH) groups were elevated when given DA. This is the first investigation of antiulcer activity of adlay, and we demonstrated that the antioxidative-active phenolic acids in DA contribute to some portion of the gastroprotective effects.

Allergy is an immune dysfunction caused by degranulation from mast cells in the early phase and cytokine secretion in the late phase of the cell. The purpose of this study was to investigate the effects of adlay (Job's tears, Coix lachryma-jobi L. var. ma-yuen Stapf) testa against beta-hexosaminidase release as a marker of degranulation in rat basophilic leukemia (RBL)-2H3 cells. The ethyl acetate fraction from ethanolic extracts of adlay testa (ATE-EtOAc) exhibited potent inhibitory activity that suppressed degranulation from RBL-2H3 cells stimulated by 1 microM A23187. The 20%-80% EtOAc/Hex subfractions of ATE-EtOAc significantly inhibited histamine release with a IC(50) of 75-100 microg/mL. In addition, the ATE-EtOAc subfractions suppressed interleukin (IL)-4, IL-6, and tumor necrosis factor-alpha secretion in RBL-2H3 cells, indicating that adlay testa were able to inhibit cytokine secretion. In order to explore the inhibitory mechanism of adlay testa in mast cell degranulation, we examined the activation of intracellular signaling molecules. Adlay testa inhibited the phosphorylation ERK expression. Furthermore, the two major active compounds, 4-hydroxyacetophenone and p-coumaric acid, were isolated from the ATE-EtOAc subfractions. These results suggest that ATE had an inhibitory effect on allergic response via the ERK signaling transduction in RBL-2H3 cells.

In this study, the inhibitory effect of Ganoderma formosanum mycelium extracts on tyrosinase, the central regulatory enzyme being responsible for cutaneous pigmentation, was investigated in both cell-free and cellular enzymatic systems, as well as in phenotype-based zebrafish model. Bioassay-guided purification indicated that the ethyl acetate fraction of G. fromosanum mycelium ethanolic extract (GFE-EA) demonstrated the highest inhibition toward cell-free tyrosinase (IC50 = 118.26 ± 13.34 ppm). The secreted and intracellular melanin of B16-F10 cells were reduced by GFE-EA through suppression of tyrosinase activity (IC50 = 102.27 ± 9.49 ppm) and its protein expression. Moreover, GFE-EA decreased surface pigmentation level of zebrafish via down-regulation of tyrosinase activity. Most of all, there is no significant difference in morphology and mortality between control and GFE-EA treated groups. Not only does GFE-EA exhibit similar depigmenting efficacy to kojic acid with lower dosage (approximately one-seventh of dose), but show less toxicity to zebrafish. It is worth noting that GFE-EA is extracted from mycelium, which subverts the general concept that mycelium lacks certain bioactivities possessed by fruit bodies. Altogether, it would appear that GFE-EA has great potential for application in the cosmetics industry.