BackgroundCompounds with the ability to scavenge reactive oxygen species (ROS) and inhibit tyrosinase may be useful for the treatment and prevention from ROS-related diseases. The number and location of phenolic hydroxyl of the flavonoids will significantly influence the inhibition of tyrosinase activity. Phenolic hydroxyl is indispensable to the antioxidant activity of flavonoids. Isoeugenol, shikonin, baicalein, rosmarinic acid, and dihydromyricetin have respectively one, two, three, four, or five phenolic hydroxyls. The different molecular structures with the similar structure to l-3,4-dihydroxyphenylalanine (l-DOPA) were expected to the different antityrosinase and antioxidant activities.MethodsThis investigation tested the antityrosinase activity, the inhibition constant, and inhibition type of isoeugenol, shikonin, baicalein, rosmarinic acid, and dihydromyricetin. Molecular docking was examined by the Discovery Studio 2.5 (CDOCKER Dock, Dassault Systemes BIOVIA, USA). This experiment also examined the antioxidant effects of the five compounds on supercoiled pBR322 plasmid DNA, lipid peroxidation in rat liver mitochondria in vitro, and DPPH, ABTS, hydroxyl, or superoxide free radical scavenging activity in vitro.ResultsThe compounds exhibited good antityrosinase activities. Molecular docking results implied that the compounds could interact with the amino acid residues in the active site center of antityrosinase. These compounds also exhibited antioxidant effects on DPPH, ABTS, hydroxyl, or superoxide free radical scavenging activity in vitro, lipid peroxidation in rat liver mitochondria induced by Fe2+/vitamin C system in vitro, and supercoiled pBR322 plasmid DNA. The activity order is isoeugenol < shikonin < baicalein < rosmarinic acid < dihydromyricetin. The results showed the compounds with more phenolic hydroxyls have more antioxidant and antityrosinase activities.ConclusionThis was the first study of molecular docking for modeling the antityrosinase activity of compounds. This was also the first study of the protective effects of compounds on supercoiled pBR322 plasmid DNA, the lipid peroxidation inhibition activity in liver mitochondria. These results suggest that the compounds exhibited antityrosinase and antioxidant activities may be useful in skin pigmentation and food additives.Electronic supplementary materialThe online version of this article (10.1186/s13020-018-0206-9) contains supplementary material, which is available to authorized users.
To the best of our knowledge, this was the first study of the hepatoprotective effects of phloretin and PIH on D-GalN-induced acute liver damage in Kunming mice as well as the possible mechanisms. This was also the first study of the lipid peroxidation inhibition activity of phloretin and PIH in liver mitochondria induced by the Fe(2+)/vitamin C (Vc) system in vitro, the protective effects on supercoiled pBR322 plasmid DNA, and the antityrosinase activity of phloretin and PIH.
Aims Here, regulatory effects of Xiaoyaosan polysaccharide on entire intestinal flora and butyrate-producing bacteria were investigated to reveal their pharmacological mechanism serving as bacterial-derived carbon sources for regulating intestinal microecology during the treatment of chronic unpredictable mild stress (CUMS)-induced depression in rats. Methods and results The effects were measured by analyzing depression-like behavior, intestinal flora, butyrate-producing bacteria diversity, and fecal butyrate content. After intervention, CUMS rats exhibited alleviated depression and increased body weight, sugar water consumption rate, and performance index in the open-field test. The abundance of dominant phyla, such as Firmicutes and Bacteroidetes, and dominant genera, such as Lactobacillus and Muribaculaceae, was regulated to restore the diversity and abundance of the entire intestinal flora to a healthy level. The polysaccharide enriched the diversity of butyrate-producing bacteria, increased the abundance of the butyrate-producing bacteria Roseburia sp. and Eubacterium sp., reduced the abundance of Clostridium sp., increased the distribution of Anaerostipes sp., Mediterraneibacter sp., and Flavonifractor sp., and subsequently increased the content of butyrate in the intestine. Conclusions These findings suggest that the Xiaoyaosan polysaccharide alleviates unpredictable mild stress-induced depression-like chronic behavior in rats by regulating the composition and abundance of the entire intestinal flora, restoring the diversity of butyrate-producing bacteria, and increasing the butyrate levels.
Significance and Impact of the Study: This is a significant study examining the regulatory mechanisms of traditional Chinese medicine on the intestinal flora of depressed rats based on functional groups. The present study investigated whether Xiaoyaosan, a traditional Chinese medicine, can improve depression-like behaviour in rats by regulating intestinal butyrate-producing bacteria, thus providing new insights into the targeted regulation of intestinal flora to treat depression.
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