About: Pectolinarin is a research topic. Over the lifetime, 79 publications have been published within this topic receiving 1363 citations. The topic is also known as: 5-Hydroxy-6-methoxy-2-(4-methoxyphenyl)-7-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxymethyl]oxan-2-yl]oxychromen-4-one.
TL;DR: This study suggests important scaffolds to design 3CLpro inhibitors to develop antiviral agents or health-foods and dietary supplements to cope with SARS-CoV-2.
Abstract: Coronavirus disease 2019 (COVID-19) has been a pandemic disease of which the termination is not yet predictable. Currently, researches to develop vaccines and treatments is going on globally to cope with this disastrous disease. Main protease (3CLpro) from severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is one of the good targets to find antiviral agents before vaccines are available. Some flavonoids are known to inhibit 3CLpro from SARS-CoV which causes SARS. Since their sequence identity is 96%, a similar approach was performed with a flavonoid library. Baicalin, herbacetin, and pectolinarin have been discovered to block the proteolytic activity of SARS-CoV-2 3CLpro. An in silico docking study showed that the binding modes of herbacetin and pectolinarin are similar to those obtained from the catalytic domain of SARS-CoV 3CLpro. However, their binding affinities are different due to the usage of whole SARS-CoV-2 3CLpro in this study. Baicalin showed an effective inhibitory activity against SARS-CoV-2 3CLpro and its docking mode is different from those of herbacetin and pectolinarin. This study suggests important scaffolds to design 3CLpro inhibitors to develop antiviral agents or health-foods and dietary supplements to cope with SARS-CoV-2.
TL;DR: Administration of the main flavonoid glycoside component, pectolinarin, and its aglycone, pECTolinarigenin, for 2 weeks significantly decreased the activity levels of AST, ALT, ALP and LDH, indicating that the two compounds have hepatoprotective activity.
Abstract: To identify the hepatoprotective component from the leaves of Cirsium setidens (Compositae), the methanolic extract was divided into two fractions, chloroform and butanol fractions, and their hepatoprotective efficacy was evaluated in a rat model of hepatic injury caused by D-galactosamine (GalN). Hepatoprotective activity was measured by the activity of serum aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), and lactate dehydrogenase (LDH). Glutathione metabolism was measured via biochemical parameters such as glutathione (GSH), glutathione reductase (GR), γ-glutamylcysteine synthetase (GCS), glutathione S-transferase (GST), and superoxide dismutase (SOD) levels. We subjected the butanol fraction, which had higher activity, to column chromatography to yield pectolinarin, which was further hydrolyzed to yield pectolinarigenin. Administration (10, 20 mg/kg, p.o.) of the main flavonoid glycoside component, pectolinarin, and its aglycone, pectolinarigenin, for 2 weeks significantly decreased the activity levels of AST, ALT, ALP and LDH, indicating that the two compounds have hepatoprotective activity. Pectolinarin and pectolinarigenin also increased activity levels of GSH, GR, GCS, and GST, as well as SOD. The significant effect was only seen in SOD activity. This suggests that the two components exhibit hepatoprotective activity mainly via SOD antioxidant mechanism.
TL;DR: It is indicated that the flavones improved adiponectin expression, accompanied by restoring of the dysregulated activities of the glucose metabolism-related enzymes, ultimately resulting in well improved glucose and lipid homeostasis, suggesting the potential benefit of the Cirsium japonicum DC as an alternative in treating diabetes mellitus.
Abstract: Cirsium japonicum DC is a traditional Chinese herb used along with other herbs to treat hypertension, traumatic hemorrhage, inflammation, and renal cellular injury. Here, we isolated two flavones from Cirsium japonicum DC, pectolinarin and 5,7-dihydroxy-6,4′-dimethoxy flavone (DDMF), and investigated their antidiabetic effect in diabetic rats established by intravenous injection with streptozotocin followed by feeding with high-carbohydrate/high-fat diet. Both pectolinarin and DDMF showed antidiabetic effect in diabetic rats. However, FECJ, a mixture of pectolinarin and DDMF, is more effective than pectolinarin and DDMF in improving the plasma glucose, cholesterol and triglycerides levels in diabetic rats. The altered activities of glucose metabolism-related enzymes in diabetic rats were well reversed after flavone treatment. The plasma adiponectin level was greatly increased in diabetic rats treated with FECJ, while no obvious effect of the flavones on the dysregulated plasma insulin level and expressions of leptin and glucose transporter 4 (GLUT4) was observed. Our data indicated that the flavones improved adiponectin expression, accompanied by restoring of the dysregulated activities of the glucose metabolism-related enzymes, ultimately resulting in well improved glucose and lipid homeostasis. Thus, an antidiabetic effect of Cirsium japonicum DC was revealed in diabetic rats, suggesting the potential benefit of the Cirsium japonicum DC as an alternative in treating diabetes mellitus.
TL;DR: This is the first research on the pharmacokinetic study of bioactive components in rat plasma after oral administration of Cirsium japonicum DC, and the results provided a meaningful basis for better understanding the absorption mechanism of this herb medicine.