Non-competitive inhibition of acetylcholinesterase by jaboticaba (Myrciaria cauliflora) peel ethanolic extracts.

Specific anthocyanins and phenolic compounds exhibit acetylcholinesterase inhibitory (AChEi) activity. In this study, the AChEi activity of jaboticaba peel extracts were investigated based on their high phenol contents. Jaboticaba peel ethanolic extract (PEX) and aqueous extract (PAX) were prepared by extracting jaboticaba peel with 95% ethanol and boiling water, respectively. Through HPLC-MS/MS and HPLC-PDA analysis, gallic acid was identified in PAX with a concentration of 598.13 ± 42.43 mg/100 g extract, and ellagic acid in PEX with a concentration of 350.47 ± 8.53 mg/100 g extract. Both PEX and PAX showed dose-dependent inhibition against AChE activity, with IC50 values of 3.54 and 4.07 mg/mL, respectively. The mechanism of inhibition of PEX was determined to be non-competitive inhibition based on the decreasing V max and relatively constant K m with increasing PEX concentration, as determined using a Lineweaver-Burk plot.

The Association between Delayed Gut Microbiota Maturity in Pre-Term Infants and the Feeding Intolerance-A Pilot Study.

This study compared gut (fecal) microbiota profiles between pre-term and full-term infants, assuming that pre-term infants without feeding intolerance would have gut microbiota similar to those of full-term infants. A total of 13 pre-term infants (gestational age < 37 weeks, birthweight ≤ 2500 g) and 10 full-term infants were included. The pre-term infants were assigned to the feeding tolerance (FT) group (n = 7) if their daily intake exceeded 100 mL/kg/day at two weeks after birth, or the feeding intolerance (FI) group (n = 6). Microbial DNA from weekly fecal samples was analyzed. The microbiota profiles of the pre-term infants and full-term infants were significantly different (p = 0.0001), as well as the FT and FI groups (p = 0.0009). The full-term group had more diversity, with higher concentrations of facultative anaerobes such as Bifidobacteriaceae and Lactobacteriaceae. The FT group's gut microbiota matured over four weeks, with higher levels of digestion-related bacteria, while the FI group had more pathogens. In the FI group, a significant difference was observed between the first and second weeks, with no significant differences noted between the first week and the third or fourth weeks. The delay in the development of the pre-term infants' gut microbiota may be associated with the FI.

Antidiabetic, Antihyperlipidemic, and Antioxidant Activities of Mulberry Lees Fermented Products in Diabetic Mice.

Mulberry lees are the sediment in the bottom of the barrel, which can be obtained from the processing of mulberry wine, and they are considered as low-value byproducts. In this study, mulberry lees were extracted with ethanol, and then fermented with Monascus pilosus to obtain fermented products (M × M). Male ICR mice were diabetes induced by STZ, and then oral administration of fermented products. The results showed that fermented products could reduce 31.9% to 47.9% plasma glucose, 25.8% to 48.2% total cholesterol, and 16.7% to 25% triglyceride levels in diabetic mice, and it can greatly lower the malondialdehyde (MDA) content by 26.4% to 59.7% but raise antioxidant enzyme activity in the liver of the mice. Moreover, fermented products not only could reduce AST and ALT activity of the diabetic mice, thereby alleviating liver inflammation, but also lowered the urea nitrogen and creatinine levels, improved glomerulus volume, and reduced swelling and inflammation in the kidneys. It was concluded that mulberry lees fermented products could be served as a value-added resource for human health.

Red Bean Extract Inhibits Lipopolysaccharide-Induced Inflammation and H2O2-Induced Oxidative Stress in RAW 264.7 Macrophages.

Red bean (Phaseolus radiatus L. var. Aurea) is a leguminous seed and mainly used as one of the popular ingredients in oriental desserts. The objective of this study was to evaluate the anti-inflammatory activity of 50 g/kg ethanolic extract of red bean (RBE) by measuring lipopolysaccharide (LPS)-induced expressions of nitric oxide (NO), inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX-2), tumor necrosis factor-α (TNF-α), and interleukin-6 (IL-6) in RAW 264.7 macrophages. On the other hand, the antioxidant activity of RBE was determined by thiobarbituric acid reactive substances method and comet assay using H2O2-induced macrophages. The results showed that RBE at the concentrations of 50-200 µg/mL can significantly suppress the inflammatory responses in LPS-stimulated macrophages through the reduction of cellular NO and downregulation of the gene expressions of iNOS, COX-2, TNF-α, and IL-6 in a dose-dependent manner. Furthermore, RBE can diminish H2O2-induced oxidative damage in RAW 264.7 macrophage. Phenolic compounds and cyanidin-3-O-glucoside from BRE may have efficacy as overall in vitro anti-inflammatory and antioxidant agents. Red bean exerts an anti-inflammatory response and has potential as a health-promoting ingredient.

Effect of thermal treatments on anti-nutritional factors and antioxidant capabilities in yellow soybeans and green-cotyledon small black soybeans.

BACKGROUND: The effects of different thermal processes on the anti-nutritional factors (tannins, phytic acids and trypsin inhibitors) and antioxidant capacity of yellow soybeans (YS) and green-cotyledon small black soybeans (GCSBS) were investigated. The soybean samples were subjected to roasting, microwaving and boiling as the thermal treatments. RESULTS: Sixty-minute boiling was most effective for eliminating the tannins in both YS and GCSBS, and also resulted in the maximal reduction of phytic acids. Trypsin inhibitors were most effectively reduced (76.92-97.91%) by microwaving, and boiling was least favourable for retaining total phenolic content. The total flavonoid content was significantly (P < 0.05) decreased by all thermal processes, and particularly by employing 60-min boiling. The total anthocyanin content of GCSBS was higher than that of YS, but significantly declined upon boiling (P < 0.05). Roasting did not significantly affect the DPPH free radical scavenging activity of GCSBS (P > 0.05). Microwaving increased the FRAP (ferric reducing antioxidant power) of GCSBS up to 6.07%. CONCLUSION: Our raw GCSBS possesses much better antioxidant capacity than raw YS. Microwaving resulted in a substantial reduction of the trypsin inhibitors of our soybean samples. Dry thermal treatments caused slight increase of FRAP in GCSBS.

Influence of preheating on antioxidant activity of the water extract from black soybean and color and sensory properties of black soybean decoction.

BACKGROUND: Our previous study indicated that black soybean (BS) tea (BST) made from preheated BS showed a significant protective effect against CCl4 -induced liver damage in Sprague Dawley rats due to BS's antioxidant activity. In this study, we investigated three different preheating methods on the antioxidant activity of water extract from BS (WBS) (Glycine max (L.) Merrill), as well as on the color and sensory properties of BST. RESULTS: WBS baked at 130 °C for 5 min showed high total phenol, flavonoid and anthocyanin contents among three preheating methods, as well as high DPPH radical-scavenging activity, ferrous ion chelating ability and reducing power. BST baked at 130 °C for 5 min had higher polyphenol oxidase activity and L*, a* and b* values but lower peroxidase activity then BST made from unheated BS. Sensory evaluation indicated that BST made from baked BS produced better aroma and flavor than the tea made from unheated BS or a commercial preheated BS. CONCLUSION: An appropriate preheating process improved the amount of extractable antioxidant and the antioxidant activity in WBS. BST baked at 130 °C for 5 min had good flavor properties, as well as high amount of antioxidant.

Improving antioxidant status in aged mice by 50% ethanol extract from red bean fermented by Bacillus subtilis.

BACKGROUND: The purpose of this study was to investigate the effects of 50% ethanol extracts from red bean non-fermented (RBE) and fermented by Bacillus subtilis (RBNE) on the antioxidant status of aged ICR mouse. RESULTS: Compared to 2-month-old ICR mouse, the plasma total antioxidant status (TAS) in 12-month-old ICR mouse decreased about 57%, while malondialdehyde (MDA) levels in the liver and brain of 12-month-old ICR mouse increased 56% and 30%, respectively. Orally administration of RBE or RBNE could completely recover the changes of MDA and plasma TAS levels due to the aging process. Vitamin E contents declined 88% in the liver and 74% in the brain of aged ICR mouse. At a level of 0.3 or 0.6 g kg(-1) body weight, RBNE raised vitamin E content in the liver and brain; however, RBE showed no significant influence. All antioxidant enzymes activities in the liver and brain of aged ICR mouse decreased compared to those activities in 2-month-old ICR mouse. RBNE could significantly enhance the superoxide dismutase activity in the brain of aged ICR mouse. CONCLUSION: Oral administration of RBE or RBNE could improve antioxidant status in aged ICR mouse. Fermentation by Bacillus subtilis could enhance the antioxidant properties of red bean.

Crude ethanol extracts from grape seeds and peels exhibit anti-tyrosinase activity.

This study aimed to evaluate the anti-tyrosinase activities of ethanol extracts from the peels and the seeds of Kyoho grapes and Red Globe grapes (KG-PEE, KG-SEE, RGG-PEE, and RGG-SEE). The total phenolic content in KG-SEE and RGG-SEE was 400 +/- 11 and 339 +/- 7 mg gallic acid equivalent/g, respectively, about 22 times and 13 times that in KG-PEE and RGG-PEE, respectively. Both seed extracts showed significantly higher anti-tyrosinase activity than the peel extracts due to their high total phenolic content. The gallic acid content in RGG-SEE was twice that in KG-SEE, and gallic acid showed high anti-tyrosinase activity; thus, RGG-SEE had higher anti-tyrosinase activity than KG-SEE. Lineweaver-Burk plots revealed that the inhibitory mechanism of the ethanol extracts from the grapes was a mix-type inhibition. Grape seed has a greater total phenolic content and has potential as a skin-lighting agent.

Solanum lyratum extract inhibits Helicobacter pylori-mediated apoptosis in human gastric epithelial cells.

Helicobacter pylori infection is associated with chronic gastritis, peptic ulcers, and gastric cancer. The effects of Solanum lyratum extract (SLE) on anti-H. pylori activity and H. pylori-induced apoptosis were investigated. SLE showed a moderate ability in inhibiting growth of H. pylori and also in interrupting the association of bacteria with host cells. SLE was also able to suppress H. pylori-induced apoptosis. SLE inhibited caspase-8 activation, thereby preventing the release of cytochrome c from mitochondria and activation of the subsequent downstream apoptotic pathway. Thus, SLE may offer a new approach for the treatment of H. pylori by down-regulation of apoptosis in the H. pylori infected gastric epithelium. As it does not directly target bacteria, SLE treatment might not cause development of resistant strains.

Solanum lyratum extract affected immune response in normal and leukemia murine animal in vivo.

Solanum lyratum Thunberg (Solanaceae) has been used as a folk medicine for treating liver, lung and esophagus in the Chinese population. Our previous studies have shown that the crude extract of S. lyratum Thunberg (SLE) induced apoptosis in colo 205 human colon adenocarcinoma cells; however, there is no report to show SLE affect immune responses in vivo. In this study, the in vivo effects of SLE on leukemia WEHI-3 cells and immune responses such as phagocytosis and natural killer (NK) cell activity in normal and leukemia mice were investigated. The SLE treatment decreases surface markers of CD3 and Mac-3 in normal and leukemia mice but promoted the cell markers of CD19 and CD11b in normal mice and CD11b in leukemia mice indicating that the precursors of T cells was inhibited and B cells and macrophage were promoted. The SLE treatment promoted the activity of macrophage phagocytosis in the peripheral blood mononuclear cells (PBMC) and peritoneal cells from normal and leukemia mice. The results also showed that NK cells from the normal and leukemia mice after treatment with SLE can kill the YAC-1 target cells. Therefore, the SLE treatment increased macrophage and NK cell activities. These consistent results indicate SLE could be a potent immune responses agent.

Apoptotic effects of protocatechuic acid in human breast, lung, liver, cervix, and prostate cancer cells: potential mechanisms of action.

Apoptotic effects of protocatechuic acid (PCA) at 1, 2, 4, 8 micromol/L on human breast cancer MCF7 cell, lung cancer A549 cell, HepG2 cell, cervix HeLa cell, and prostate cancer LNCaP cell were examined. Results showed that PCA concentration-dependently decreased cell viability, increased lactate dehydrogenase leakage, enhanced DNA fragmentation, reduced mitochondrial membrane potential, and lowered Na(+)-K(+)-ATPase activity for these cancer cells (P < 0.05). PCA also concentration-dependently elevated caspase-3 activity in five cancer cells (P < 0.05), but this agent at 2-8 micromol/L significantly increased caspase-8 activity (P < 0.05). PCA concentration-dependently decreased intercellular adhesion molecule level in test cancer cells (P < 0.05) but significantly inhibited cell adhesion at 2-8 micromol/L (P < 0.05). PCA also concentration-dependently lowered the levels of interleukin (IL)-6 and IL-8 in five cancer cells (P < 0.05), but this agent at 2-8 micromol/L significantly suppressed vascular endothelial growth factor production (P < 0.05). These findings suggest that PCA is a potent anticancer agent to cause apoptosis or retard invasion and metastasis in these five cancer cells.

Rhein induced apoptosis through the endoplasmic reticulum stress, caspase- and mitochondria-dependent pathways in SCC-4 human tongue squamous cancer cells.

Rhein, an anthraquinone compound, can be found in the rhizome of rhubarb, a traditional Chinese medicine herb showing antitumor activity. In this study, it was observed that rhein induced S-phase arrest through the inhibition of p53, cyclin A and E and it induced apoptosis through the endoplasmic reticulum stress by the production of reactive oxygen species (ROS) and Ca2+ release, mitochondrial dysfunction, and caspase-8, -9 and -3 activation in human tongue cancer cell line (SCC-4). The most efficient induction of apoptosis was observed at 30 microM for 24 h. Mechanistic analysis demonstrated that rhein induced changes in the ratio of Bax/Bcl-2 based on the decrease of Bcl-2 levels, the loss of mitochondrial membrane potential, cytochrome c release from the mitochondria and the activation of caspase-9 and -3. The data demonstrated that rhein induces apoptosis in SCC-4 cells via caspase, ROS and mitochondrial death pathways.

Improving the antioxidant activity of buckwheat (Fagopyrum tataricm Gaertn) sprout with trace element water.

Trace element water (TEW) (100, 200, 300, 400 and 500ppm) was used to grow buckwheat (Fagopyrum tataricm Gaertn) to evaluate whether the beneficial effects of trace elements on the antioxidant activity could be accomplished with the supplement of TEW. At 300ppm, TEW significantly increased the Cu, Zn and Fe contents in buckwheat sprout, but not the Se and Mn contents. The levels of rutin, quercitrin and quercetin did not differ between buckwheat sprouts grown in TEW and de-ionized water (DIW). The ethanolic extract from buckwheat sprout grown in 300ppm TEW showed higher DPPH radical scavenging activity, ferrous ion chelating activity, superoxide anion scavenging activity and inhibitory activity toward lipid peroxidation than that grown in DIW. The extract of the TEW group also enhanced intracellular superoxide dismutase activity and resulted in lower level of reactive oxygen species in human Hep G2 cells.

Trace element water improves the antioxidant activity of buckwheat (Fagopyrum esculentum Moench) sprouts.

Buckwheat (Fagopyrum esculentum Moench) was grown in trace element water (TEW) (100, 200, 300, 400, and 500 ppm) and deionized water (DIW) to evaluate whether the beneficial effects of trace elements on the antioxidant activity could be accomplished with the supplement of TEW. At 300 ppm, TEW significantly increased the Cu, Zn, Mn, and Fe contents in buckwheat sprout but not the Se content. However, the levels of rutin, isoorientin, vitexin, and isovitexin did not differ between buckwheat sprouts grown in TEW and DIW. The ethanolic extract from buckwheat sprout grown in 300 ppm of TEW showed higher ferrous ion chelating activity and inhibitory activity toward lipid peroxidation than that grown in DIW. The extract in the TEW group also enhanced intracellular superoxide dismutase activity and lowered reactive oxygen species and superoxide anion in the human Hep G2 cell. It was concluded that TEW could increase the antioxidant activities of buckwheat sprouts.

Beneficial effect of Toona sinensis Roemor on improving cognitive performance and brain degeneration in senescence-accelerated mice.

The purpose of the present study was to examine the effects of Toona sinensis Roemor extracts on antioxidative activities, brain morphological changes and cognitive ability. In an in vitro study, the antioxidant capacities of water extracts from Toona sinensis Roemor leaf (TSL), root (TSR) and bark (TSB) were evaluated by an alpha,alpha-diphenyl-beta-pricryl-hydrazyl radical-scavenging test. The results showed that the scavenging activities of all Toona sinensis Roemor extracts were over 80% at a concentration of 0.625 mg/ml. In an in vivo study, 3-month-old male senescence-accelerated-prone 8 mice were used as the tested subjects and fed four different diets: casein diet or casein diet supplemented with 1% TSL, TSR or TSB extract for 12 weeks. The results showed that the mice supplemented with Toona sinensis Roemor extracts demonstrated significantly less amyloid beta-protein deposition and lower levels of thiobarbituric acid-reactive substances than the control group. All Toona sinensis Roemor diet groups also showed better active shuttle avoidance responses, and higher superoxide dismutase, catalase and glutathione peroxidase activities, than the control group. It can thus be concluded that supplementation with either TSL, TSR or TSB extract could not only reduce the incidence of ss-amyloid plaques, but also improve learning and memory ability in senescence-accelerated-prone 8 mice. This might be due to the beneficial effects of Toona sinensis Roemor extracts on promoting the antioxidative defence system.

Xylooligosaccharides and fructooligosaccharides affect the intestinal microbiota and precancerous colonic lesion development in rats.

Certain nondigestible oligosaccharides can be selectively utilized by probiotics and reduce the risk of colon cancer. However, the inhibitory effects of xylooligosaccharides (XOS) on colon cancer are not well documented. This study evaluated the effects of xylooligosaccharides and fructooligosaccharides (FOS) on the alteration of cecal microbiota, cecal pH, cecal weight, and serum lipid levels, and also their inhibitory effect on precancerous colon lesions in male Sprague-Dawley rats. The rats were randomly assigned to 4 groups: control, treatment with 1,2-dimethylhydrazine (DMH) [15 mg/(kg body wt.wk) for 2 wk], treatment with DMH + 60 g XOS/kg diet, and treatment with DMH + 60 g FOS/kg diet. Rats were fed the experimental diets for 35 d, beginning 1 wk after the second dose of DMH. Both XOS and FOS markedly decreased the cecal pH and serum triglyceride concentration, and increased the total cecal weight and bifidobacteria population. XOS had a greater effect on the bacterial population than did FOS. Moreover, both XOS and FOS markedly reduced the number of aberrant crypt foci in the colon of DMH-treated rats. These results suggest that XOS and FOS dietary supplementation may be beneficial to gastrointestinal health, and indicate that XOS is more effective than FOS.