Rhodiola crenulate is the edible medicinal herbal medicine widely used for altitude sickness in China. Interestingly, our previous work has found that R. crenulate extract (RCE) could significantly improve the pathology associated with dextran sulfate sodium-induced colitis. Thus, the current research aims to reveal the pharmacodynamic material basis of RCE, as well as its mechanism against colitis. The chemical characterization of RCE was performed by UHPLC-HR-MS, through which a total of 88 constituents were identified. Meanwhile, our results also found 29 constituents absorbed into blood and 8 metabolized absorbable compounds. The decreased flavonoids prototype and the elevated sulfated products of phenols were observed under pathophysiological conditions of colitis. The metabolomics study revealed that colitis caused the alternation of fatty acid metabolism, steroid hormone biosynthesis and bile acid metabolism. Correspondingly, RCE could prevent colitis by improving fatty acid metabolism and secondary bile acid metabolism.
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Dietary flavonoids are abundant in natural plants and possess multiple pharmacological and nutritional activities. In this study, apigenin, luteolin, and baicalein were chosen to evaluate their anti-diabetic effect in high-glucose and dexamethasone induced insulin-resistant (IR) HepG2 cells. All flavonoids improves the glucose consumption and glycogen synthesis abilities in IR-HepG2 cells via activating glucose transporter protein 4 (GLUT4) and phosphor-glycogen synthase kinase (GSK-3β). These flavonoids significantly inhibited the production of reactive oxygen species (ROS) and advanced glycation end-products (AGEs), which were closely related to the suppression of the phosphorylation form of NF-κB and P65. The expression levels of insulin receptor substrate-1 (IRS-1), insulin receptor substrate-2 (IRS-2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) pathway in IR-HepG2 cells were all partially activated by the flavonoids, with variable effects. Furthermore, the intracellular metabolic conditions of the flavonoids were also evaluated.
The present study aimed to evaluate the effects of chrysoeriol from Cardiospermum halicacabum in streptozotocin induced Wistar rats. Thirty rats were categorized as control, diabetic control supplemented with 0, 20 mg/kg chrysoeriol and 600 μg/kg BW of glibenclamide for 45-day trial period. Our results indicated that the inclusion of chrysoeriol (20 mg/kg), showed a significant reduction in plasma glucose, hemoglobin and glycosylated hemoglobin level with a rising of plasma insulin sensitivity. Further, downregulated enzymes including glucose 6-phosphatase, fructose 1,6-bisphosphatase, and glycogen phosphorylase as well upregulated enzymes such as hexokinase, glucose-6-phosphate dehydrogenase, pyruvate kinase, and hepatic glycogen content. There was a diminish action found in liver glycogen synthase of tested rat with a rise in gamma-glutamyl transpeptidase, towards normal levels upon treatment with chrysoeriol. The histopathological study confirmed that renewal of the beta cells of pancreatic of chrysoeriol and glibenclamide treated rats. In addition, the molecular docking of chrysoeriol against glycolytic enzymes including hexokinase, glucose-6-phosphate dehydrogenase, pyruvate kinase, using Argus software shows chrysoeriol had greatest ligand binding energy as equivalent to glibenclamide, as a standard drug. Thus, chrysoeriol found to be non-toxic with potential regulation on glycemic control and upregulation of the carbohydrate metabolic enzymes.
This study investigated the effects of domestic cooking process on the variations of soybean isoflavones, aiming at understanding the conversion of β-glucosides and aglycones isoflavones during the process and the relation with antioxidant activity. It was found that β-glucosides isoflavones was significantly increased from 223.01 (raw) to 727.29 mg/g (frying at 160 ℃ for 2 min), but boiling showed only a slight increase to 258.14 mg/g. The process for the mixed cooking of soybeans with vegetables was also evaluated, which is quite common in home cuisine. The results showed all bioactive ingredients were aggressively destroyed by over processing, but interestingly, green pepper and kelp exhibited isoflavones generation potentials for soybean. In addition, cooking from 60 to 160 ℃ for 2 or 5 min, showed a significantly decrease on FRAP. However, in the case of fried soybeans which treated at 120 ℃ or 160 ℃, when extending the heating time to 5 min, their FRAP activity got a significant increase. The present study may provide a practical guidance for healthy soybean cooking, by using frying around 120 ℃ for 5 min and mixed with some vegetables such as green peppers or kelp.