Spatholobus sinensis is a plant of the Spatholobus genus (Leguminosae family). Its caulis are used as "ji-xue-teng" regionally. However, to our knowledge, no phytochemical investigation on S. sinensis has been reported to date. In this study, eight compounds were isolated from the ethanol extract of the caulis of S. sinensis, by solvents extraction and column chromatography methods. By analysis of their physic-chemical constants and spectral data, the structures of 8 compounds were identified as spatholosineside A (1), 2',4',5,7-tetrahydroxyisoflavone (2), isoliquiritigenin (3), lupinalbin A (4), coumestrol (5), naringenin (6), protocatechuic acid (7), leonuriside A (8). Compound 1 is a new compound.
Chalcones ; chemistry ; isolation & purification ; Coumestrol ; chemistry ; isolation & purification ; Fabaceae ; chemistry ; Flavanones ; chemistry ; isolation & purification ; Glycosides ; chemistry ; isolation & purification ; Molecular Structure ; Plant Stems ; chemistry ; Plants, Medicinal ; chemistry

OBJECTIVETo observe effects of phytoestrogens quercetin (QC), Genistein (GEN), coumestrol (COM), and enterolactone (ENL) on gap junctional intercellular communication (GJIC) in HaCaT cells.

METHODSHaCaT cells were exposed to QC, GEN, COM, and ENL at 0.1, 1.0, 10.0 and 100.0 micromol/L for 24 hours. The effects of phytoestrogens on GJIC were determined by fluorescence redistribution after photobleaching (FRAP) technique of using a laser scanning confocal microscope (LSCM).

RESULTSQC did not affect the GJIC at 0.1-10.0 micromol/L, whereas, GEN, COM, and ENL exhibited inhibition on the GJIC in some extent at 0.1-10.0 micromol/L without showing significant cytotoxicity. The ratio of fluorescence recovery were between 31.77% to 37.06%, which were significantly decreased compared the vehicle control (44.74%).

CONCLUSIONThe phytoestrogens GEN, COM, and ENL, but not QC, could inhibit the GJIC function in HaCaT cells at concentrations could be reached in human serum in some instance, indicating they could, under certain conditions, be cancer promoters. Therefore, it should be prudent to use these chemicals as pharmaceuticals or dietary supplements.

Cell Communication ; drug effects ; physiology ; Cell Line ; Coumestrol ; pharmacology ; Dose-Response Relationship, Drug ; Gap Junctions ; drug effects ; physiology ; Genistein ; pharmacology ; Humans ; Microscopy, Confocal ; Phytoestrogens ; pharmacology ; Quercetin ; pharmacology

This study was conducted to evaluate the antihyperglycemic effects of three phytoestrogens, genistein, coumestrol, and enterolactone, in type 2 diabetic animals. Forty male C57BL/KsOlaHsd-db/db mice were used as a diabetic animal model. The animals were divided into four groups and fed a phytoestrogen-free AIN-76 diet (control), or one of three phytoestrogen-supplemented (3.75 mg/100 g diet) AIN-76 diets for six weeks. During the experimental period, fasting blood glucose levels were measured on week 0, 2, 5, and 6 of the experiment, and oral glucose tolerance tests were performed on the 5th week. After the experimental period, blood concentrations of HbA1c, insulin, and glucagon were measured, and hepatic glycogen content and glucose regulating enzyme activities were analyzed. Fasting blood glucose, HbA1c level, and the area under the blood glucose curve in the oral glucose tolerance test were significantly lower in all of the phytoestrogen-supplemented groups compared to the control group. Plasma glucagon levels were also significantly lower in all of the phytoestrogen-supplemented groups compared to the control group. Hepatic glycogen level was significantly higher in the coumestrol-supplemented group compared to the other groups. However, there were no significant differences in the activities of glucokinase and glucose-6-phosphatase between the groups. These results suggest that all of the three major phytoestrogens tested in the present study were effective in lowering blood glucose levels in type 2 diabetic animals. However, further studies need to be conducted to elucidate the exact mechanism for the hypoglycemic effects of phytoestrogens.
4-Butyrolactone ; Animals ; Blood Glucose ; Coumestrol ; Diet ; Fasting ; Genistein ; Glucagon ; Glucokinase ; Glucose ; Glucose Tolerance Test ; Glucose-6-Phosphatase ; Humans ; Hypoglycemic Agents ; Insulin ; Lignans ; Liver Glycogen ; Male ; Mice ; Models, Animal ; Phytoestrogens ; Plasma