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In the present study, the antioxidant activities and immunostimulatory ability of a polysaccharide extracted from Chinese Sesbania cannabina , which was identified to be a galactomannan in our previous study, were investigated. The extracted polysaccharide exhibited strong DPPH, ABTS and hydroxyl radical scavenging activities and ferrous ion chelating activity in a concentration-dependent manner. The immune-enhancing effect of our polysaccharide on RAW 264.7 macrophage cells was investigated by determining the cell viability, phagocytic activity, NO and intracellular ROS production and mRNA expression of cytokines. The results indicated that the polysaccharide could increase the production of NO and intracellular ROS, as well as effectively trigger transcriptional activation of TLR-2/4, NF-κB, IL-10/1β/6, IFN-γ, Ik-Bα, iNOS, COX-2 and TNF-α. These findings provide useful information for potential application of the polysaccharide extracted from Chinese Sesbania cannabina in the food industry.

Estrogen deficiency in menopausal women is the main cause of osteoporosis. Phytoestrogen could be a suitable candidate for treatment of post-menopausal osteoporosis. Recent studies showed that S. chinensis contains several lignans, which may be phytoestrogen. In this study, we investigated the ameliorative effects of S. chinensis on post-menopausal osteoporosis. 30% ethanol extract of S. chinensis (SC) was administered orally for 6 weeks after 7 weeks of ovariectomized-induced osteoporosis. Bone mineral density was significantly increased following increased serum osteocalcin levels by SC treatment. Histological analysis showed that SC reduced the increased growth plate of the epiphyseal plate in femur. In addition, pores within bone marrow cells filling the lateral and medial epicondyle were decreased. Serum estradiol concentration was significantly increased in the SC-treated group. The expressions of estrogen receptor-α and -β were increased in uterus and MCF-7 breast cancer cells by SC treatment. And two transcriptions of proto-oncogenes, c-fos and c-Jun, were suppressed by treatment of SC. From these data, we propose that S. chinensis attenuates post-menopausal osteoporosis with its phytoestrogenic effects. S. chinensis may have the potential to be used as an alternative for treatment of osteoporosis.

Inflammatory cytokine tumor necrosis factor-α (TNFα) has been demonstrated to accelerate the progression and metastasis of various carcinomas. In this study, we investigated the effect of amentoflavone on inhibiting the migration and invasion of TNFα-induced breast cancer cells. Results showed that amentoflavone significantly blocked the cellular migration and invasion of MCF10DCIS.com and MDA-MB-231 cells at a concentration of 10 μM but did not affect the cell viability. The mRNA and protein levels of matrix metalloproteinase (MMP)-9, significantly activated by TNFα, were reversed by amentoflavone treatment in a dose-dependent manner in MCF10DCIS.com cells. Congruent with the protein level, the activity of MMP-9 was significantly suppressed by amentoflavone treatment. Additionally, we found that amentoflavone dampened Gli1-dependent noncanonical hedgehog signaling, which is a key factor in the regulation of migration and invasion in TNFα-induced human breast cancer cells. Further study elucidated that TNFα enhanced Gli1 through the activation of the AKT/mTOR/S6K1 cascade, whereas it receded after amentoflavone treatment in human breast cancer cells. In summary, amentoflavone abrogated Gli1 activation in TNFα-induced mammary tumor cells, resulting in a decrease of invasiveness in human breast cancer cells via mediating AKT/mTOR/S6K1 signaling. Amentoflavone should be considered as a potent food ingredient for the retardation of mammary tumorigenesis.

Bian-Que Triple-Bean Soup ( Bian-Que San Dou Yin in Chinese) is a folk remedy which has been used for thousands of years in the practices of traditional Chinese medicine. The objectives of the current study were aimed to determine in vitro anti-diabetic effects and to find out the optimal cooking time for retaining active substances. α-Glycosidase in vitro inhibitory capacities and DPPH free radical scavenging capacities, and contents of active substances including total phenolics, saponin , tannin and monomeric anthocyanin , were determined with colorimetric methods. The results revealed that Bian-Que Triple-Bean Soup boiled for 30 min has the most effective impact on α-glycosidase inhibition. n -Butanol-soluble and water extract fractions showed relatively higher α-glycosidase inhibitory activity (17.4% and 11.2%, respectively) than that (2.56% and 5.32%, respectively) of hexane-soluble and dichloromethane-soluble fractions. Degradation was observed for those thermally unstable substances (TPC, tannin , and anthocyanin ) by extending the boiling time; however, there were no obvious changes for thermo-stable substances ( saponin ).

Cadmium (Cd) induces hepatocyte injury by oxidative stress. Albicanol is a sesquiterpenoid extracted from the medicinal plant Dryopteris fragrans that has previously been shown to exhibit anti-aging and antioxidant activity. In this study, we explored the mechanism of albicanol inhibition of the Cd-induced apoptosis of chicken hepatoma cells (LMH) by treating these cells with CdCl 2 (25 μM) and/or albicanol (2.5 × 10 ?5 μg mL ?1 ) for 24 h. Under Cd treatment, the research results showed that the apoptosis rate markedly increased in LMH cells. In addition, the iNOS activity and NO content increased significantly, which promoted the expressions of genes associated with the mitochondrial apoptosis pathway (Bax, CytC, Caspase-3 and Caspase-9) and inhibited the expression of Bcl-2 in this pathway. However, Cd + albicanol co-treatment significantly reduced the apoptosis rate and the expressions of iNOS and genes associated with the mitochondrial apoptosis pathway (Bax, CytC, Caspase-3 and Caspase-9), and promoted the expression of Bcl-2 in this pathway. In addition, molecular docking supported a link between the albicanol ligand and the iNOS receptor. These results indicated that albicanol can inhibit Cd-induced apoptosis by regulating the NO/iNOS-mediated mitochondrial pathway.

Aloe, the leaf juice of Aloe vera , is a popular functional food worldwide. The major constituents of aloe are polyphenolic anthranoids such as aloin, aloe-emodin and rhein. Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a probe substrate of P-glycoprotein (P-gp), an efflux pump, and CYP 3A4. This study first investigated the serum kinetics of aloe, then evaluated the modulation effects of aloe on P-gp and CYP 3A through an aloe–CSP interaction study in rats. The serum kinetic study showed that aloe-emodin glucuronides (G) and rhein sulfates/glucuronides (S/G) were major molecules in the bloodstream. The aloe–CSP interaction study showed that the systemic exposure to CSP was significantly decreased by either a single dose or multiple doses of aloe. The results of in vitro studies indicated that aloe activated P-gp and aloe metabolites activated CYP 3A4. In conclusion, aloe ingestion activated the functions of P-gp and CYP 3A in rats.

Epidemiological and clinical studies suggest that grapes and grape-derived products may reduce the risk for chronic disease. Grape seed extract specifically has been gaining interest due to its reported ability to prevent weight gain, moderate hyperglycemia, and reduce inflammation. The purpose of this study was to examine the long-term effects of two doses of grape seed extract (10 and 100 mg kg ?1 body wt per d in mice) on markers of metabolic syndrome in the context of a moderately high-fat diet. After 12 weeks, the lower dose of grape seed extract was more effective at inhibiting fat gain and improving glucose tolerance and insulin sensitivity. Neither the high fat diet nor grape seed extract altered skeletal muscle substrate metabolism. Most interestingly, when examining the profile of metabolically active microbiota in the mucosa of the small intestine, cecum, and colonic tissue, grape seed extract seemed to have the most dramatic effect on small intestinal tissue, where the population of Firmicutes was lower compared to control groups. This effect was not observed in the cecal or colonic tissues, suggesting that the main alterations to gut microbiota due to flavan-3-ol supplementation occur in the small intestine, which has not been reported previously. These findings suggest that grape seed extract can prevent early changes in glucose tolerance and alter small intestinal gut microbiota, prior to the onset of skeletal muscle metabolic derangements, when grape seed extract is consumed at a low dose in the context of a moderately high fat diet.

Betaine is a methyl donor utilized in regeneration of methionine from homocysteine in a metabolic reaction catalyzed by betaine-homocysteine methyltransferase (BHMT), an enzyme mostly localized in the liver. However, we recently showed that the metabolism of sulfur-containing amino acids in the kidney was also influenced by betaine, which is attributable to elevation of renal methionine availability resulting from an increase in its supply through blood. In this study we investigated the change in pulmonary sulfur-containing amino acid metabolism by betaine and its potential beneficial effect on paraquat (PQ)-induced lung injury. Male rats were provided with betaine for 2 weeks prior to an intratracheal instillation of PQ (0.3 mg/500 μl kg ?1 ). Two weeks after PQ exposure, histopathological assessment revealed severe fibrotic lesions accompanied with elevation of 4-hydroxyproline in the lung, which were all prevented effectively by betaine supplementation. PQ-induced DNA fragmentation in lymphocytes, reduction of oxidant scavenging capacity, expression of heme oxygenase 1 and inducible nitric oxide synthase in the lung, and elevation of serum transforming growth factor beta 1 were also inhibited. PQ instillation increased cysteine, but depleted glutathione in the lung. Betaine supplementation before PQ exposure suppressed the cysteine accumulation and increased the glutathione synthesis. The polyamine synthesis, which requires decarboxylated S -adenosylmethionine as a substrate, was also increased significantly. The results suggest that betaine may enhance pulmonary antioxidant capacity by modulating the metabolism of sulfur-containing amino acids and related substances despite the lack of BHMT in the lung.

As a dihydrochalcone, phloretin was reported to effectively attenuate palmitic acid (PA)-induced oxidative stress in endothelial cells. In the present study, we further investigated the antioxidant capacity of phloretin via restoring the activity of MnSOD through deacetylation in vitro and in vivo . The results revealed that phloretin (50 μM) treatment significantly increased the activity of MnSOD in the HUVECs and mouse aortas, and then obviously reduced the accumulation of mitochondrial ROS. Immunoprecipitation assay and Western blot analysis indicated that phloretin could decrease the lysine acetylation of MnSOD and restore its activity by promoting the expression of Sirt3 by increasing the phosphorylation of AMPK (Thr172). These findings provide a novel profile to explain the antioxidant activity of phloretin by reducing the acetylation level of MnSOD via an AMPK/Sirt3 signaling pathway.

Acylated anthocyanins are more stable than monomeric anthocyanins, but little is known about their physiological effects. We evaluated the hemodynamic effects of single intragastric doses of purple carrot ( Daucus carota L.) anthocyanin (PCA) and two monomeric anthocyanins, cyanidin 3- O -glycoside (C3G) and delphinidin 3- O -ruthenoside (D3R). PCA, C3G, or D3R was administered orally to rat and blood flow in the cremaster artery was measured for 60 min using a laser Doppler blood flow meter. After measurements, the aorta of the animal was removed and the extent of phosphorylation of aortic epithelial nitric oxide synthase (eNOS) and Akt were determined by western blotting. PCA (10 mg kg ?1 ) or C3G (1 mg kg ?1 ) significantly increased rat cremaster arteriole blood flow and phosphorylation of eNOS and Akt; D3G (1 mg kg ?1 ) only slightly altered cremaster arteriole blood flow and did not affect the phosphorylation of eNOS and Akt in the aorta. These results suggest that hemodynamic alterations depend more on the chemical structure of anthocyanins, particularly the aglycon, than on the glycoside. In addition, increase of blood flow by a single oral dose of PCA was practically reduced with treatment of carvedilol (CR), a non-specific adrenaline blocker. Blood concentrations of cyanidin or its glycoside 15, 30, or 60 min after the administration of 10 mg kg ?1 PCA were below the limit of detection. These hemodynamic changes may have been associated with an indirect adrenergic action induced following a single dose of PCA.