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The hepatoprotective potential of saponarin, isolated from Gypsophila trichotoma, was evaluated in vitro/in vivo using a hepatotoxicity model of paracetamol-induced liver injury. In freshly isolated rat hepatocytes, paracetamol (100 μmol) led to a significant decrease in cell viability, increased LDH leakage, decreased levels of cellular GSH, and elevated MDA quantity. Saponarin (60–0.006 μg/mL) preincubation, however, significantly ameliorated paracetamol-induced hepatotoxicity in a concentration-dependent manner. The beneficial effect of saponarin was also observed in vivo. Rats were challenged with paracetamol alone (600 mg/kg, i.p.) and after 7-day pretreatment with saponarin (80 mg/kg, oral gavage). Paracetamol toxicity was evidenced by increase in MDA quantity and decrease in cell GSH levels and antioxidant defence system. No changes in phase I enzyme activities of AH and EMND and cytochrome P 450 quantity were detected. Saponarin pretreatment resulted in significant increase in cell antioxidant defence system and GSH levels and decrease in lipid peroxidation. The biochemical changes are in good correlation with the histopathological data. Protective activity of saponarin was similar to the activity of positive control silymarin. On the basis of these results, it can be concluded that saponarin exerts antioxidant and hepatoprotective activity against paracetamol liver injury in vitro/in vivo.

A new flavonol tetraglycoside, quercetin-3-O-[α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-galactopyranosyl]-7-O-β-D-glucopyranoside (1), and two new flavonol alkaloids, N-(8-methylquercetin-3-O-[α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-galactopyranosyl])-3-hydroxypiperidin-2-one (2) and N-(8-methylkaempferol-3-O-[α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-galactopyranosyl])-3-hydroxypiperidin-2-one (3), were isolated from the aerial parts of Astragalus monspessulanus ssp. monspessulanus. Two rare flavonoids with an unusual 3-hydroxy-3-methylglutaric acid moiety, quercetin-3-O-α-L-rhamnopyranosyl-(1→2)-[6-O-(3-hydroxy-3-methylglutaryl)-β-D-galactopyranoside (4) and kaempferol-3-O-α-L-rhamnopyranosyl-(1→2)-[6-O-(3-hydroxy-3-methylglutaryl)-β-D-galactopyranoside (5), were isolated from the aerial parts of A. monspessulanus ssp. illyricus. In addition, the eight known flavonoids alangiflavoside (6), alcesefoliside (7), mauritianin (8), quercetin-3-β-robinobioside (9), cosmosine (10), apigenin-4'-O-glucoside (11), trifolin (12), and rutin (13) were isolated from aerial parts of A. monspessulanus ssp. monspessulanus. Their structures were elucidated via NMR and HRESIMS data. In a model that tested t-BuOOH-induced oxidative stress on isolated rat hepatocytes, flavonoids 1-13 had statistically significant cytoprotective activity similar to that of silymarin, tested at 60 μg/mL. The most prominent effects were observed for flavonoids 1, 4, 7, and 12.

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Flavonoids, the most common plant polyphenols are widely distributed in every species and possess a broad range of pharmacological activities. The genus Astragalus is the largest in the Fabaceae family with more than 2,500 species spread. They are known to contain different metabolites such as flavonoids, saponins, and polysaccharides. Plants from the genus have been used in the traditional medicine of many countries for centuries. This paper is focused on the large group of flavonoid compounds. Details on structure as well as information about the pharmacological properties of flavonoids, isolated from Astragalus species have been discussed. This review is based on publications until the first half of 2014 and includes also the results from our phytochemical investigations of the genus.

Recebido em 10/11/06; aceito em 25/5/07; publicado na web em 19/12/07 Nine flavonoids were identified in aerial parts of Astragalus corniculatus Bieb. (Fabaceae) by liquid chromatography coupled with ionspray mass spectrometry in the tandem mode (LC/MS/MS) with negative ion detection. Vitexin, orientin and eriodictyol-7-Oglucoside are obtained for the first time in genus Astragalus L, and isorhamnetin-3-O-glucoside in the species.

A purified mixture containing mostly saponins (PMS) from Astragalus corniculatus Bieb. was used in an in vivo model to demonstrate its protective effect against myeloid Graffi tumour in hamsters. Survivability, tumour growth and tumour transplantability were followed. Comparative studies revealed that the intraperitoneal administration of PMS: (i) decreased the tumour transplantability; (ii) inhibited tumour growth in the early stages of tumour progression; (iii) increased the mean survival time; (iv) reduced the percentage mortality. These results suggest that appropriate use of PMS could outline a promising strategy for the treatment of myeloid Graffi tumour.

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