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.

Radix Paeoniae Rubra (RPR), a traditional Chinese herb, has anti-inflammatory and immuno-regulatory properties. This study explored the effects of RPR on stimulation of osteoclast differentiation in RAW264.7 cells and peripheral blood mononuclear cells (PBMC)s. The mature osteoclasts were measured by bone resorption assays and TRAP staining. JNK, ERK, p38 and NF-κB inhibitors were used applied in order to verify their contribution in RPR-induced osteoclast differentiation. The NF-κB and MAPK pathways were evaluated by western blotting, RT-PCR and luciferase assay. RPR induced osteoclast differentiation in a dose-dependent manner and induced the resorption activity of osteoclasts differentiation of RAW264.7 cells and PBMCs. Western blotting showed that RPR treatment induced phosphorylation of JNK, ERK, and p38 in RAW 264.7 cells. Treatment of JNK, ERK, and p38 MAP kinase inhibitors verified the contribution of JNK, ERK and p38. RPR treatment induced c-Fos and NFATc1 protein expression; NF-κB inhibitor treatment and luciferase assay verified the contribution of the NF-κB pathway. This study demonstrated the interesting effect, in which RPR stimulated osteoclast differentiation in murine RAW264.7 cells and human monocytes.

The severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2-M^pro) plays an essential role in viral replication, transcription, maturation, and entry into host cells. Furthermore, its cleavage specificity for viruses, but not humans, makes it a promising drug target for the treatment of coronavirus disease 2019 (COVID-19). In this study, a fragment-based strategy including potential antiviral quinazolinone moiety and glutamine- or glutamate-derived peptidomimetic backbone and positioned nitro functional groups was used to synthesize putative M^pro inhibitors. Two compounds, G1 and G4, exhibited anti-M^pro enzymatic activity in a dose-dependent manner, with the calculated IC₅₀ values of 22.47 ± 8.93 μM and 24.04 ± 0.67 μM, respectively. The bio-layer interferometer measured real-time binding. The dissociation kinetics of G1/M^pro and G4/M^pro also showed similar equilibrium dissociation constants (K_D) of 2.60 × 10⁻⁵ M and 2.55 × 10⁻⁵ M, respectively, but exhibited distinct association/dissociation curves. Molecular docking of the two compounds revealed a similar binding cavity to the well-known M^pro inhibitor GC376, supporting a structure−function relationship. These findings may open a new avenue for developing new scaffolds for M^pro inhibition and advance anti-coronavirus drug research.

The aim of this study was to investigate the possible analgesic and anti-inflammatory mechanisms of the ethanolic extract ofA. morrisonensisHayata (AMEtOH). Two models were employed for evaluation of the analgesic effects: acetic acid-induced writhing response and formalin-induced paw licking. The results demonstrated thatAMEtOHdecreased writhing response for both the acetic acid assay and the licking time in the formalin test. The anti-inflammatory effect was evaluated by paw edema of mice induced byλ-carrageenan.AMEtOHsignificantly decreased induced paw edema three to four hours afterλ-carrageenan injection. Additionally, the results indicated that the anti-inflammatory mechanism ofAMEtOHmay be due to the declined levels of nitric oxide (NO) and malondialdehyde (MDA) in the edematous paw. Furthermore,AMEtOHdecreased the tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) levels, leading to the reduction of prostaglandins and subsequently alleviated edema. Isolation and purification of theAMEtOHextract determinedp-hydroxyacetophenone to be a major component at 130 mg/g of extract. No mortality was observed in the acute toxicity test given at the dose of 10 g/kg. This study demonstrated the possible mechanisms for the analgesic and anti-inflammatory effects ofAMEtOHfor mice and provided evidence for the ethnobotanical uses ofA. morrisonensisin treating inflammatory diseases.

High performance anion exchange chromatography-pulsed amperometric detection was employed in this study to conduct quantitative analysis of the inulin-related fructo-oligosaccharides present in Gynura divaricata subsp. formosana. Result obtained for the 1-kestose (GF₂), nystose (GF₃) and 1^F-β-fructofuranosyl-nystose (GF₄) contents were 146.60 ± 0.04, 24.70 ± 0.75 and 16.60 ± 0.91 μg/g, fresh weight, and 68.90 ± 0.02, 7.60 ± 1.34 and 149.30 ± 0.06 μg/g (mean ± RSD), dry weight, respectively. Using this method, the limit of quantitation was 20 μg/mL and the linear detectability between 0-250 μg/mL. The developed method provides a practical analysis for these low caloric value, prebiotic and non-digestible carbohydrates in the genus Gynura.