Simultaneous characterization and quantification of flavonoids in Morus australis root as potential hepatoprotective nutraceutical.

Morus australis distributed widely in China has high value in food and agriculture. Twelve phenolic compounds were isolated and identified as major constituents of M. australis root from Shaanxi province, China, while the protective effect of M. australis root on liver injury has never been determined in detail. In this study, the hepatoprotective ability of M. australis root was investigated in vivo and in vitro. The ethanol-water extract prepared from M. australis root showed protection on alcohol-induced liver damage in mice by decreasing the levels of serum alanine aminotransferase, aspartate transaminase, triacylglycerol and malondialdehyde, and by increasing glutathione contents. Furthermore, among 12 major constituents of M. australis root, 10 flavonoids (especially 1) showed protection against carbon tetrachloride (CCl4 )-intoxicated HepG2 cell lines by decreased lactic dehydrogenase levels. In addition a validated HPLC-DAD method was established for the quantitative analysis of 10 flavonoids in the bioactive extract. PRACTICAL APPLICATIONS: Our results showed that M. australis root extract significantly alleviated the liver damage in mice. Ten flavonoids from the root of this plant exhibited protection on CCl4 -intoxicated HepG2 cell lines. This study suggests that Morus australis root has hepatoprotective potential as a promising supplement for the prevention and treatment of liver diseases.

Chemical characterization of the main bioactive polyphenols from the roots of Morus australis (mulberry).

Morus species, commonly known as mulberry, is widely distributed in China. The mulberry tree is a high-value plant in agriculture. Morus australis is one of the major Morus species growing in Northern China. However, the biological properties of the main constituents of M. australis roots were not well studied. In the present study, through extensive chromatographic and spectral analysis, 12 phenolic compounds were isolated and identified from the M. australis roots. Compounds 1, 2, 8, 9 and 12 were isolated from M. australis roots for the first time. Antitumor activities of these polyphenols were studied on the A549 cell line. Compounds 1, 5 and 6 exhibited cytotoxicity on A549 cells and induced apoptosis in A549 cells via the intrinsic mitochondrial pathway. They also mediated inhibition of autophagic flux contributed cell death via the PI3k/Akt/mTOR pathway. In order to explore more potential bioactivities of these isolates, α-glucosidase, acetylcholinesterase and tyrosinase inhibitory activities were studied, and the results demonstrated that the inhibitory activity of these polyphenols on enzymes was not defined by their basic structural skeletons, but by the substituted position.