Topic
Acacetin
About: Acacetin is a research topic. Over the lifetime, 442 publications have been published within this topic receiving 10458 citations. The topic is also known as: 5,7-Dihydroxy-2-(4-methoxyphenyl)-4-benzopyrone & Linarigenin.
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TL;DR: Wang et al. as discussed by the authors showed that Chuju is an ideal source of natural flavonoids with significant antioxidant and anti-inflammatory effects, and is worthy of further development as health-promoting food or supplement.
Abstract: Chuju, the flower of Chrysanthemum morifolim cv. Chuju, is a traditional medicine-food material used in China. Bioassay-guided chemical investigation on Chuju led the isolation of 16 flavonoids ( 1-16 ) characterized as quercetin ( 1 ), isorhamnetin 3- O -β-D-glucoside ( 2 ), eriodictyol ( 3 ), pyracanthoside ( 4 ), apigenin ( 5 ), apigetrin ( 6 ), acacetin ( 7 ), acacipetalin ( 8 ), luteolin ( 9 ), diosmetin ( 10 ), spinacetin ( 11 ), axillarin ( 12 ), bonanzin ( 13 ), cirsiliol ( 14 ), chrysosplenol D ( 15 ) and artemetin ( 16 ). Among them, compounds (11-16) were first reported from the Chrysanthemum species. Chuju flavonoids displayed strong antioxidant in DPPH (1, 1-diphenyl-2- picrylhydrazyl) radical scavenging assay, and high anti-inflammatory activity by inhibiting NO production in LPS-induced RAW 264.7 cells. These findings suggests that Chuju is an ideal source of natural flavonoids with significant antioxidant and anti-inflammatory effects, and is worthy of further development as health-promoting food or supplement.
21 citations
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TL;DR: It is found that acacetin inhibits p38 and JNK phosphorylation and reduces M MP‐1, MMP‐3 and MMP-13 expression in interleukin‐1β‐induced FLSs, suggesting that ac acetin has antiarthritic effects in FLSS.
Abstract: It is well known that rheumatoid arthritis (RA) is an autoimmune joint disease in which fibroblast-like synoviocytes (FLSs) play a pivotal role. In this study, we investigated the anti-arthritic properties of acacetin in FLSs. The expression of matrix metalloproteinase (MMP)-1, MMP-3 and MMP-13 were investigated by quantitative RT-PCR and western blot at gene and protein levels. At the same time, the phosphorylation of mitogen-activated protein kinases (MAPK) was investigated. The DNA-binding activity of NF-κB was investigated by electrophoretic mobility shift assay. We found that acacetin inhibits p38 and JNK phosphorylation and reduces MMP-1, MMP-3 and MMP-13 expression in interleukin-1β-induced FLSs. Our results suggest that acacetin has antiarthritic effects in FLSs. Thus, acacetin should be further studied for the treatment of arthritis.
21 citations
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TL;DR: In this article, the efficiency of three different solvents (H2O, acidified H2O and 70% Methanol) for metabolites extraction from the leaves of sugar beet (Beta vulgaris subsp. rubra) was investigated along with their inhibitory activity on pancreatic α-amylase and lipase for obesity management.
20 citations
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TL;DR: The preclinical study indicates that the synthesized acacetin prodrug is highly water-soluble and safe; it effectively terminates experimental AF in beagle dogs and therefore may be a promising drug candidate for clinical trial to treat patients with acute AF.
Abstract: We previously reported that duodenal administration of the natural flavone acacetin can effectively prevent the induction of experimental atrial fibrillation (AF) in canines; however, it may not be used intravenously to terminate AF due to its poor water-solubility. The present study was to design a water-soluble prodrug of acacetin and investigate its anti-AF effect in beagle dogs. Acacetin prodrug was synthesized by a three-step procedure. Aqueous solubility, bioconversion and anti-AF efficacy of acacetin prodrug were determined with different methodologies. Our results demonstrated that the synthesized phosphate sodium salt of acacetin prodrug had a remarkable increase of aqueous solubility in H2O and clinically acceptable solution (5% glucose or 0.9% NaCl). The acacetin prodrug was effectively converted into acacetin in ex vivo rat plasma and liver microsome and in vivo beagle dogs. Intravenous infusion of acacetin prodrug (3, 6 and 12 mg/kg) terminated experimental AF without increasing ECG QTc interval in beagle dogs. The intravenous LD50 of acacetin prodrug was 721 mg/kg in mice. Our preclinical study indicates that the synthesized acacetin prodrug is highly water-soluble and safe; it effectively terminates experimental AF in beagle dogs and therefore may be a promising drug candidate for clinical trial to treat patients with acute AF.
20 citations
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TL;DR: The results from the present study provide further information about the flavonoids as taxonomic marker of the genus Chromolaena, and the chemotaxonomic significance of these compounds were also summarized.
20 citations