In Vitro/In Vivo Hepatoprotective and Antioxidant Effects of Defatted Extract and a Phenolic Fraction Obtained from Phlomis Tuberosa.

An in vitro/in vivo hepatotoxicity and hepatoprotection evaluation of a defatted extract and a phenolic fraction from Phlomis tuberosa, administered alone and in a carbon tetrachloride (CCl4)-induced metabolic bioactivation model, was performed. The extract and the phenolic fraction were analysed by high performance liquid chromatography (HPLC) to determine the total flavonoid content, to identify flavonoids and to quantify verbascoside. In addition, total polyphenolics in the samples were expressed as gallic acid equivalents. Applied alone, the extract and the fraction (5, 10 and 50 µg/mL) did not show a statistically significant hepatotoxic effect on isolated rat hepatocytes in vitro. In a CCl4-induced hepatotoxicity model, the samples exhibited a concentration-dependent, statistically significant hepatoprotective effect, which was most pronounced at 50 µg/mL for both. The phenolic fraction exhibited a more pronounced hepatoprotective effect compared to the extract. Data from the in vitro study on the effects of the extract were also confirmed in the in vivo experiment conducted in a CCl4-induced hepatotoxicity model in rats. A histopathological study showed that the animals treated with CCl4 and the extract had an unaltered histoarchitecture of the liver. The effects of the extract were the same as those of silymarin.

Beneficial effects of the fructus Sophorae extract on experimentally induced osteoporosis in New Zealand white rabbits.

Sophora japonica is a source of several flavonol, flavone and isoflavone glycosides that are reported to positively affect menopausal symptoms including osteoporotic complications. In the present study fructus Sophorae extract (FSE) was administered orally for three months at a dose of 200 mg kg-1 in ovariectomized (OVX) New Zealand rabbits. 3D computed tomography scans and histopathological images revealed microstructural disturbances in the bones of the castrated animals. FSE recovered most of the affected parameters in bones in a manner similar to zoledronic acid (ZA) used as a positive control. The aglycones of the main active compounds of FSE, daidzin, and genistin, were docked into the alpha and beta estrogen receptors and stable complexes were found. The findings of this study provide an insight into the effects of FSE on bone tissue loss and suggest that it could be further developed as a potential candidate for the prevention of postmenopausal osteoporotic complications.

Antiproliferative and antitumour activity of saponins from Astragalus glycyphyllos on myeloid Graffi tumour.

ETHNOPHARMACOLOGICAL RELEVANCE: Astragalus glycyphyllos L. has been extensively used in Bulgarian folk medicine as an antihypertensive, diuretic, anti-inflammatory, anti-tumour, in cases of cardiac insufficiency, renal inflammation, calculosis, etc. AIM OF THE STUDY: To evaluate the possible in vitro/in vivo anti-proliferative/anti-tumour activity of a purified saponins' mixture (PSM) obtained from the plant. MATERIALS AND METHODS: Viability and proliferative activity of the Graffi myeloid tumour cells was assessed by MTT test. The morphological alterations were visualized and analysed by fluorescent microscopy after intravital double staining. An in vivo model of Graffi tumour bearing hamsters was used to examine the influence of PSM on transplantability, tumour growth, survival and mortality as well as to observe pathomorphological changes. RESULTS: Graffi tumour cells were sensitive to purified saponins' mixture after 24 and 48 h treatment. The treatment induced a statistically significant decrease of the viability/proliferation of the Graffi tumour cells. These effects were concentration- and time-dependent. Fluorescent microscopy studies showed that these antiproliferative effects were connected to the induction of apoptosis. The in vivo study showed the presence of a stromal component, single mononuclear cells in the stroma. Multiple incorrect mitotic figures were observed in the tumour tissue from the control group. Well-formed stroma with accumulation of mononuclear cells and mitotic cells were found in the group, treated with PSM. The tumour weight was decreased in the group, treated with PMS. CONCLUSION: The results indicate that PSM exhibited in vitro/in vivo antiproliferative/anti-tumour effects.