RESUMO
OBJECTIVE: To investigate the lipid metabolic effect and mechanism of water extract of lotus leaves(Traditional Chinese Medicine). METHODS: Isolated SD rat lipid tissues were suspended in organ baths containing Krebs solution, and the effect of lotus leaf water extract on free fatty acids (FFA) release was observed; The experimental obesity rat model was established by feeding them high glucose and fat diets, then the changes of body weight and blood lipid were measured in the model rats after intragastric administration with water extract of lotus leaves for four weeks, and the expressions of peroxisome proliferator-activated receptor gamma (PPAR-γ) and leptin were examined by RT-PCR and immunohistochemical. RESULTS: The ex vivo experiment showed that water extract of lotus leaves effectively promoted the FFA release from isolated lipid tissues. In vivo experiment, similarly to Orlistat, water extract of lotus leaves(60 mg/kg)markedly decreased the body weight and blood lipid of experimental obesity rats(P<0.05), and obviously reduced the expressions of PPAR-γ and leptin(P<0.05). CONCLUSIONS: Water extract of lotus leaves greatly improves the expression of PPAR-γ and leptin, which can promote the lipid mobilization and dissolution, reduce the body weight and blood lipid of adult rats with experimental obesity, therefore is expected to be developed into lipid-lowering diet pills.
Assuntos
Metabolismo dos Lipídeos/efeitos dos fármacos , Lotus/química , Obesidade , Extratos Vegetais/farmacologia , Animais , Leptina/metabolismo , PPAR gama/metabolismo , Folhas de Planta/química , Ratos , Ratos Sprague-Dawley , ÁguaRESUMO
Phytoestrogens, a group of plant-derived non-steroidal compounds that can behave as estrogens by binding to estrogen receptors, have drawn great attention for their potentially beneficial effects on human health. However, there are few studies investigating the potential side effects of phytoestrogens on the reproductive system. The present study was to elucidate the effects of 17ß-estradiol (E2), progesterone (P4), and phytoestrogens genistein (Gen), resveratrol (Res), and phloretin (Phl) on eosinophilic infiltration of the ovariectomized rat uterus and endometrial vascular permeability, and to analyze the underlying mechanisms. The ovariectomized rats received daily subcutaneous injections of E2, E2+P4, P4, Gen, Res, Phl, or an equivalent volume of vehicle for 21 days, and sham-operated animals (Sham rats) were used as the controls. Hematoxylin-eosin staining revealed a marked increase in uterine eosinophilic infiltrations in ovariectomized rats treated with E2, E2+P4 or P4, which was associated with increased expression of vascular endothelial growth factor (VEGF), nuclear factor-κB (NF-κB), and tumor necrosis factor-α (TNF-α) proteins as determined by immunohistochemical and Western blot analysis. However, all three phytoestrogens had no markedly effect on the uterine eosinophilic infiltration and the expressions of VEGF, NF-κB, and TNF-α in the uterus of ovariectomized rats. Our data demonstrate that E2 alone or in combination with P4 increases uterine eosinophilic infiltration which is related with vascular hyperpermeability caused by VEGF, NF-κB and TNF-α, whereas phytoestrogens Gen, Res, and Phl, have no such an effect.
Assuntos
Endotélio Vascular/efeitos dos fármacos , Estrogênios/farmacologia , Fitoestrógenos/farmacologia , Útero/efeitos dos fármacos , Animais , Eosinófilos/citologia , Estradiol/farmacologia , Feminino , Genisteína/farmacologia , NF-kappa B/metabolismo , Ovariectomia , Permeabilidade , Floretina/farmacologia , Progesterona/farmacologia , Ratos , Resveratrol , Estilbenos/farmacologia , Fator de Necrose Tumoral alfa/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismoRESUMO
AIM: To observe and compare the effects of phytoestrogen genistein, resveratrol and 17beta-estradiol on the tonic contraction and the phasic contraction of isolated gallbladder muscle strips and to study the underlying mechanisms. METHODS: Isolated strips of gallbladder muscle from guinea pigs were suspended in organ baths containing Kreb's solution, and the contractilities of strips were measured before and after incubation with genistein, resveratrol and 17beta-estradiol respectively. RESULTS: Similar to 17beta-estradiol, genistein and resveratrol could dose-dependently inhibit the phasic contractile activities, they decreased the mean contractile amplitude and the contractile frequencies of gallbladder muscle strips, and also produced a marked reduction in resting tone. The blocker of estrogen receptor ICI 182780 failed to alter the inhibitory effects induced by genistein and resveratrol, but potassium bisperoxo (1, 10 phenanthroline) oxovanadate bpV (phen), a potent protein tyrosine phosphatase inhibitor, markedly attenuated the inhibitory effects induced by genistein and resveratrol. In calcium-free Kreb's solution containing 0.01 mmol/L egtazic acid (EGTA), genistein and resveratrol inhibited the first phasic contraction induced by acetylcholine (ACh), but did not affect the second contraction induced by CaCl(2). In addition, genistein, resveratrol and 17beta-estradiol also could reduce the contractile responses of ACh and KCl, and shift their cumulative concentration-response curves rightward. CONCLUSION: Phytoestrogen genistein and resveratrol can directly inhibit the contractile activity of isolated gallbladder muscle both at rest and in response to stimulation. The mechanisms responsible for the inhibitory effects probably due mainly to inhibition of tyrosine kinase, Ca(2+) influx through potential-dependent calcium channels (PDCs) and Ca(2+) release from sarcoplasmic reticulum (SR), but were not related to the estrogen receptors.
Assuntos
Estradiol/farmacologia , Vesícula Biliar/efeitos dos fármacos , Genisteína/farmacologia , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Fitoestrógenos/farmacologia , Estilbenos/farmacologia , Acetilcolina/farmacologia , Animais , Cloreto de Cálcio/farmacologia , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/farmacologia , Estradiol/análogos & derivados , Antagonistas de Estrogênios/farmacologia , Feminino , Fulvestranto , Vesícula Biliar/enzimologia , Cobaias , Técnicas In Vitro , Masculino , Músculo Liso/enzimologia , Compostos Organometálicos/farmacologia , Fenantrolinas/farmacologia , Cloreto de Potássio/farmacologia , Proteínas Tirosina Fosfatases/antagonistas & inibidores , Proteínas Tirosina Fosfatases/metabolismo , ResveratrolRESUMO
To study the effects of different reactive oxygen species (ROS) on the resting tension of porcine coronary artery rings and to identify the effects of genistein (GEN), resveratrol (RES) and 17beta-estradiol (EST) on ROS-elicited vasoconstriction, porcine coronary rings were prepared and mounted in an organ bath and, after an equilibration period, the changes induced by the drugs were observed. Rings with intact endothelium showed an obvious but slow contraction after treatment with xanthine (100 microM)/xanthine oxidase (20 mU x mL(-1)) (X/XO) whereas endothelium-denuded rings showed no effects. H2O2 (200 microM) induced a fast and transient contraction in endothelium-denuded rings and failed to do so in intact-endothelium rings. Like superoxide dismutase (SOD, 200 U x mL(-1)), GEN (1 microM) and RES (1 microM) significantly inhibited contractile response evoked by X/XO, however in contrast to GEN and RES, EST (1 microM) had no obvious effect. GEN (30 microM) and RES (30 microM), like catalase (CAT, 800 U x mL(-1)), markedly attenuated the contraction elicited by H2O2. The results demonstrate that GEN and RES have distinct inhibitory effects on vasoconstriction induced by O2*- generated by X/XO and H2O2, and their actions are clearly greater than to that of EST.