Diversity in Pyracantha fortuneana fruits maturity stages enables discrepancy in the phenolic compounds, antioxidant activity, and tyrosinase inhibitory activity.

Pyracantha fortuneana (P. fortuneana) fruit is a wild fruit that is popular because of its delicious taste and numerous nutrients, and phenolic compounds are considered to be the main bioactive components in P. fortuneana fruits. However, the relationship between phenolic compounds and their antioxidant and tyrosinase (TYR) inhibitory activities during the ripening process is still unclear. The study compared the influence of the five developmental stages on the accumulation of phenolic compounds, antioxidant activity, and TYR inhibitory activity in the fruits of P. fortuneana. The compounds were identified by offline two-dimensional liquid chromatography-electrochemical detection (2D-LC-ECD) combined with liquid chromatography-tandem mass spectrometry, and the main active ingredients were quantified. The results showed that stage II had higher total phenolic and flavonoid content, as well as higher antioxidant and TYR inhibitory activity, but the total anthocyanin content was lowest at this stage. A total of 30 compounds were identified by 2D-LC-ECD. Orthogonal partial least squares discriminant analysis screened out six major potential markers, including phenolic acids, procyanidins, and flavonoids. In addition, it was found that caffeoylquinic acids, procyanidins, and flavonoids were higher in stage II than in stages I, III, IV, and V, whereas anthocyanins accumulated gradually from stages III to V. Therefore, this study suggests that the changes in antioxidant and TYR inhibitory activities of P. fortuneana during the five developmental stages may be due to the transformation of procyanidins, caffeoylquinic acids, and phenolic glycosides into other forms during the fruit maturation process. Practical Application: Differences in chemical constituents, antioxidant, and tyrosinase inhibitory activities in fruit maturity stages of P. fortuneana were elucidated to provide reference for rational harvesting and utilization of the fruits and their bioactive components. These findings are expected to provide a comprehensive assessment of the bioactive profile and guide the food industrial production.

Biosorption of a common micropollutant (methylene blue) from a water environment by chemically activated biomass of a widely available plant species (Pyracantha coccinea M. J. Roemer).

Recently, to protect the health of aquatic life and, indirectly, all living things, biomass-based substances have been increasingly applied as biosorbent materials to remove micropollutant agents from an aquatic environment. However, these studies are under development, and the search for more successful materials continues. Here, the biosorption of a common micropollutant, methylene blue, from an aquatic environment was investigated using the chemically activated biomass of a widely available plant species, Pyracantha coccinea M. J. Roemer. The biosorption efficiency of the biosorbent material was improved by optimizing the experimental conditions, including the contact time, micropollutant load, pH, and biosorbent material amount, and the highest performance was observed at t = 360 mins, C0 = 15 mg L-1, pH = 8 and m = 10 mg. The pseudo-second-order kinetics model and Freundlich isotherm model were in good agreement with the experimentally obtained results. The thermodynamic study suggested that the micropollutant biosorption was a favorable, spontaneous, and physical process. The micropollutant-biosorbent interaction mechanism was presented using SEM and FTIR studies. The maximum Langmuir biosorption capacity of the biosorbent was determined to be 156.674 mg g-1. The activation operation more than doubled the biosorption potential of the biosorbent material. Thus, the present study showed that the chemically activated plant biomass-based material could be a promising biosorbent for the effective removal of the micropollutant from water environment.

The biosorption of a common micropollutant, methylene blue, from a water environment was studied using chemically activated biomass of Pyracantha coccinea M. J. Roemer. The activation operation more than doubled the biosorption potential of the biosorbent material. It exhibited higher micropollutant biosorption performance compared to most other biosorbents. These results indicated that the chemically activated biomaterial could be a very effective biosorbent for the micropollutant biosorption from an aqueous medium.

LC-ESI-QTOF-MS/MS characterization of phenolic compounds from Pyracantha coccinea M.Roem. and their antioxidant capacity.

Pyracantha coccinea M.Roem. is considered as an important medicinal plant contributing remarkably to health and medicinal benefits. This is attributed to the presence of abundant polyphenols with powerful antioxidant properties. However, little research has been studied on the comprehensive identification and characterization of the phenolic compounds in areal parts of P. coccinea.  This study aimed to investigate, characterize, and quantify the phenolic profiles of P. coccinea through liquid chromatography electrospray ionization quadrupole time-of-flight mass spectrometry (LC-ESI-QTOF-MS/MS) and high-performance liquid chromatography-photodiode array (HPLC-PDA. Further, it showed a significantly higher value in total phenolic content (TPC) than that of total flavonoids (TFC) and tannins (TTC). As for antioxidant capacities, P. coccinea presented the highest activity in ABTS (7.12 ± 0.25 mg AAE/g dw) compared with DPPH, FRAP, and TAC assays. The LC-ESI-QTOF-MS/MS analysis detected 28 phenolic compounds, including phenolic acids (12), flavonoids (13), other polyphenols (2), and lignans (1) in P. coccinea samples. The results from HPLC-PDA indicated the chlorogenic acid (11.49 ± 1.89 mg/g) was the most abundant phenolic acid, while kaempferol (14.67 ± 2.17 mg/g) was the predominant flavonoid in P. coccinea. This research confirms the benefits of the P. coccinea plant as a potential source of natural antioxidants for the food and pharmaceutical industries.

High-performance thin-layer chromatography fingerprinting and anti-inflammatory and antinociceptive activities of Pyracantha coccinea M.Roem.: A laboratory-based study.

This study aimed to investigate the high-performance thin-layer chromatography (HPTLC) fingerprinting and in-vivo anti-inflammatory and antinociceptive activities of different leaf extracts (ethanolic extract, n-hexane, chloroform, and ethyl acetate) of Pyracantha coccinea M.Roem. plant. A total of one hundred and twenty-four Wistar rats for anti-inflammatory and antinociceptive tests (carrageenan and formalin tests, respectively) were treated with two doses of the ethanolic extract (100 and 300 mg/kg), two doses of other plant fractions (30 and 100 mg/kg), Diclofenac (25 mg/kg) as the positive control, and normal saline as the negative control group, by oral gavage route. HPTLC fingerprinting is used for assay of terpenoids, flavonoids, alkaloids, and antioxidant activity. Treatment of the animal with the ethanolic extract at doses of 100 and 300 mg/kg, both ethyl acetate and chloroform fractions at the dose of 30 mg/kg and 100 mg/kg decreased the pain score in the formalin test and paw edema caused by carrageenan relative to control group significantly. Moreover, these extracts reported the highest amounts of flavonoid contents. In conclusion, phytochemicals present in Pyracantha coccinea M.Roem. leaves have anti-inflammatory and antinociceptive activities. Future studies are needed to identify the compounds with the anti-inflammatory and antinociceptive potential present in the plant.

Production of Pyracantha Polysaccharide-Iron(III) Complex and Its Biologic Activity.

In this study, the optimum synthetic process of the Pyracantha polysaccharide-iron (PPI) complex was studied via response surface methodology (RSM). Its antioxidant and anti-cancer activities were also investigated. It was demonstrated that the optimal conditions for the synthetic process of the complex were as follows: a pH of 8.9, a reaction temperature of 70 °C and a trisodium citrate:polysaccharide ratio of 1:2. PPI were analysis by UV, FTIR, SEM, CD, XRD, TGA and NMR. PPI was able to scavenge the metal ion, ABTS and free radicals of the superoxide anion, demonstrating its potential antioxidant activity. PPI was found to display cytotoxicity to Skov3 cells, as shown by its ability to induce apoptosis and alter gene expression in Skov3 cells. These findings show than PPI may represent a novel antioxidant and chemotherapeutic drug.

Biological activities and health-promoting effects of Pyracantha genus: a key approach to the phytochemical's potential.

Pyracantha spp. are commonly called firethorn, and attract human attention due to their colorful berries. These berries are eaten globally as a traditional remedy for treating different stomach abnormalities, and as a cooking ingredient for folk diets. The present review aims to provide an overview on Pyracantha genus' geographical distribution and botanical description, traditional uses, phytochemical composition, biological activities and safety issues. Several biological activities have been reported to Pyracantha species, namely antioxidant, anti-inflammatory, antimicrobial, larvicidal and cytotoxic properties, most of them attributed to the use of their fruits. Pyracantha species phytochemical composition reveal the presence of interesting bioactive molecules, such as pyracrenic acid and fortuneanosides. The currently reported biological activities to these plants derive from in vitro and in vivo studies, so that clinical trials are needed to confirm these preclinical results. Nonetheless, Pyracantha species can be suggested as a safe herb useful to develop future drug formulations and functional foods.

A Theoretical Study of the Adsorption Process of B-aflatoxins Using Pyracanthakoidzumii (Hayata) Rehder Biomasses.

Employing theoretical calculations with density functional theory (DFT) using the B3LYP/6-311++G(d,p) functional and basis set, the interaction of the aflatoxin B1 (AFB1) molecule and the functional groups present in the Pyracantha koidzumii biosorbent was investigated. Dissociation free energy and acidity equilibrium constant values were obtained theoretically both in solution (water) and gas phases. Additionally, the molecular electrostatic potential for the protonated molecules was calculated to verify the reactivity. Thus, methanol (hydroxyl group), methylammonium ion (amino group), acetate ion (carboxyl group), and acetone (carbonyl group), were used as representatives of the substrates present in the biomass; these references were considered using the corresponding protonated or unprotonated forms at a pH value of 5. The experimental infrared spectrophotometric data suggested the participation of these functional groups in the AFB1 biosorption process, indicating that the mechanism was dominated by electrostatic interactions between the charged functional groups and the positively charged AFB1 molecule. The theoretical determination indicated that the carboxylate ion provided the highest interaction energy with the AFB1 molecule. Consequently, an enriched biosorbent with compounds containing carboxyl groups could improve the yield of the AFB1 adsorption when using in vitro and in vivo trials.

Polysaccharides from Pyracantha fortuneana and its biological activity.

This study used response surface methodology to determine the optimal conditions for extraction of polysaccharides from Pyracantha. fortuneana (PSPF), and studied the mechanism of PSPF-inducing apoptosis in human ovarian carcinoma Skov3 cells. Response surface methodology (RSM) were adopted to extract PSPF. The maximum value of polysaccharide yield was obtained under these optimal conditions. PSPF had good potential as an antioxidant. Exposure of cells to PSPF resulted in cytotoxicity through the induction of apoptosis, and the reactive oxygen species were increased, mitochondrial membrane potential decreased, DNA damage (detected as γ- H2AX and RAD51 foci) was observed in Skov3 cells. In addition, PSPF could induce apoptosis of cancer cells. Therefore, PSPF should be explored as novel potential antioxidants and an anti-tumor drug in a clinical setting.

Extraction optimization of polyphenols from fruits of Pyracantha fortuneana (Maxim.) Li by ultrasonic assistant method and their antibacterial activity.

The present study was designed to utilise ultrasound assistance technology to optimize the extraction conditions of polyphenols, and identify their antibacterial activity from fruits of Pyracantha fortuneana (Maxim.) Li, facilitated by the use of orthogonal experiment methodology. A four factors and three levels of orthogonal design was carried out to elucidate the effect of ethanol concentration, solvent-to-solid ratio, ultrasonic temperature and time on the yields of the polyphenols. The results showed that the optimal conditions were as follows: ethanol concentration 70%, solvent-to-solid ratio 70:1, ultrasonic temperature 30°C, and ultrasonic time 40 min, the maximum polyphenol yield was 5.58mg/g under the optimum extraction condition. The extracted hydro-alcohol polyphenols showed the excellent antibacterial potential to both Staphylococcus aureus and Escherichia coli with the minimum inhibitory concentration (MIC) 10 mg/ml and 20 mg/ml, and the corresponding diameter of inhibition zone (DIZ) was 7.4 and 6.8 mm, respectively. The results indicated the ability of ultrasound assistance technology to obtain polyphenols from fruits. Furthermore, present results highlighted that fruits of Pyracantha fortuneana (Maxim.) Li are a potential natural source of bioactive compounds with strong antibacterial activity. These compounds could be considered for potential application in nutraceutical and functional foods ingredient or pharmaceutical applications.

Protective roles of Pyracantha fortuneana extract on acute renal toxicity induced by cadmium chloride in rats.

PURPOSE: To investigate the protective roles of pyracantha fortune fruit extract (PFE) on acute renal toxicity induced by cadmium chloride (CdCl2) in rats. METHODS: Rats were pretreated with PFE and consecutively injected with CdCl2 (6.5 mg/kg) for 5 days. RESULTS: The concentration of Cd, kidney weight, malondialdehyde (MDA), and nitric oxide (NO) production were remarkably increased in CdCl2 group as well as the levels of plasma uric acid, urea, and creatinine (P < 0.001). However, the body weight and glutathione (GSH), superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and glutathione peroxidase (GR) levels were markedly reduced by CdCl2 treatment (P < 0.001). Histological manifestations of renal tissue showed severely adverse changes. Moreover, CdCl2 treatment significantly decreased the B-cell lymphoma-2 (Bcl-2) expression while increased the Bcl-2-Associated X Protein (Bax), tumor necrosis factor-α (TNF-α) expression (P < 0.001). Additionally, the expression of Nrf2/Keap 1 related proteins Keap-1 gained a significant increase (P < 0.001), whereas the Nrf2, HO-1, γ-GCS, GSH-Px and NQO1 expression decreased by CdCl2 treatment (P < 0.05). These rats were pretreated with PFE to improve the changes caused by CdCl2 treatment. CONCLUSION: PFE could protect the kidney against acute renal toxicity induced by CdCl2.

The ameliorative effect of the Pyracantha fortuneana (Maxim.) H. L. Li extract on intestinal barrier dysfunction through modulating glycolipid digestion and gut microbiota in high fat diet-fed rats.

Pyracantha fortuneana fruits are consumed as a dietary supplement in China and attenuate obesity and metabolic disorders. Obesity is known to be associated with intestinal barrier dysfunction driven by hyperglycemia and gut dysbiosis. However, whether the health benefits of P. fortuneana fruits are linked with the intestinal barrier function (IBF) remains unknown. This study aimed to evaluate the restorative effects of P. fortuneana fruit extract (PFE) on the IBF. Sprague Dawley rats were fed with a chow, a high-fat diet (HFD), or a PFE-supplemented diet for 8 weeks. Results showed that PFE intervention ameliorated HFD-induced intestinal barrier dysfunction by attenuating impaired structural integrity, reducing the elevated lactulose/mannitol ratio, and improving the mRNA and protein expression levels of tight junction proteins in HFD-fed rats. The ameliorations were associated with a beneficial effect on glycolipid homeostasis, as evidenced from the PFE decreasing intestinal absorptive capacity based on the d-xylose excretory rate, lowering the expression of GLUT2 and inhibiting digestive enzyme activities. The proanthocyanidins in the PFE showed greater in vitro inhibition on α-amylase, α-glucosidase, and lipase compared with triterpenoid saponins. Furthermore, the ameliorations on the IBF were also associated with effects on the microbial composition based on 16S rRNA gene sequence analysis. Several bacterial groups, which were linked with gut barrier integrity, were modulated after PFE administration, that is, Actinobacteria, Bacteroidaceae, Corynebacteriaceae, Lactobacillaceae, and S24-7 were elevated and the HFD-induced increase in Clostridia, Ruminococcaceae, Oscillospira, and Flexispira was restored. These data provide evidence for the ameliorative effect of the PFE on diet-induced intestinal barrier functional alternations in association with its capacity to modulate glycolipid digestion and gut microbiota in HFD-fed obese rats.

HPLC-QTOF-MS/MS profiling, antioxidant, and α-glucosidase inhibitory activities of Pyracantha fortuneana fruit extracts.

This study was carried out to optimize the solvent for extracting the antioxidants and α-glucosidase inhibitors (AGIs) from Pyracantha fortuneana fruit (PFF) and the major chemical components were characterized by HPLC-QTOF-MS/MS. The results showed that 50% and 70% acetone (v/v, ml/ml) gave the best extraction efficiency on phenolics and total flavonoids, while 70% acetone and 50% methanol possess better recovery on protein and polysaccharides, respectively. In addition, the 50% and 70% acetone extracts gave the strongest radical scavenging ability and α-glucosidase inhibitory activity (p > 0.05), but the Fe3+ reducing power of the 50% acetone extract was higher than that of 70% acetone. Correlation analysis indicated that phenolic acids and flavonoids were connected to the antioxidant activity and α-glucosidase inhibitory activity closely. Moreover, 25 compounds including 7 flavonoids, 6 phenolic acids, 7 organic acids, 3 tannins, 1 terpene, and 1 alkaloid were identified or tentatively identified in the 50% acetone extract. Overall, 50% acetone can be a proper solvent for extracting antioxidants and AGIs from PFF. PRACTICAL APPLICATIONS: Imbalance between production and clearance of reactive oxygen species (ROS) in the body could induce various chronic diseases. PFF is an edible fruit beneficial to human health; it is reported to be capable of optimizing blood glucose levels and may prevent premature aging. In the present study, PFF was found to be excellent in antioxidant activities and α-glucosidase inhibitory ability; 50% acetone was found to be the best extraction solvent. In addition, the predominant phytochemical components of the 50% acetone extract were characterized. This study can promote further research of Pyracantha fortuneana in natural functional products, especially in the prevention of type II diabetes and its complication.

Protective roles of Pyracantha fortuneana extract on acute renal toxicity induced by cadmium chloride in rats

Abstract Purpose: To investigate the protective roles of pyracantha fortune fruit extract (PFE) on acute renal toxicity induced by cadmium chloride (CdCl2) in rats. Methods: Rats were pretreated with PFE and consecutively injected with CdCl2 (6.5 mg/kg) for 5 days. Results: The concentration of Cd, kidney weight, malondialdehyde (MDA), and nitric oxide (NO) production were remarkably increased in CdCl2 group as well as the levels of plasma uric acid, urea, and creatinine (P < 0.001). However, the body weight and glutathione (GSH), superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and glutathione peroxidase (GR) levels were markedly reduced by CdCl2 treatment (P < 0.001). Histological manifestations of renal tissue showed severely adverse changes. Moreover, CdCl2 treatment significantly decreased the B-cell lymphoma-2 (Bcl-2) expression while increased the Bcl-2-Associated X Protein (Bax), tumor necrosis factor-α (TNF-α) expression (P < 0.001). Additionally, the expression of Nrf2/Keap 1 related proteins Keap-1 gained a significant increase (P < 0.001), whereas the Nrf2, HO-1, γ-GCS, GSH-Px and NQO1 expression decreased by CdCl2 treatment (P < 0.05). These rats were pretreated with PFE to improve the changes caused by CdCl2 treatment. Conclusion: PFE could protect the kidney against acute renal toxicity induced by CdCl2.

Novel Insights into the Inhibitory Effect and Mechanism of Proanthocyanidins from Pyracantha fortuneana Fruit on α-Glucosidase.

Proanthocyanidins were extracted from Pyracantha fortuneana fruit (PFF), and their structures were investigated through 13 C nuclear magnetic resonance (13 C NMR), high performance liquid chromatography (HPLC) and high resolution mass spectrometry (HRMS). The results showed that these compounds were predominantly constituted of procyanidin with A-type and B-type linkage and coexistence of procyanidins glucoside. Spectroscopy methods were used to analyze the inhibitory activity of proanthocyanidins on α-glucosidase. The results demonstrated that these compounds exhibited excellent inhibitory effect on α-glucosidase with the IC50 value of 0.15 ± 0.01 µg/mL, and they reversibly inhibited α-glucosidase in a non-competitive type. The fluorescence quenching analysis revealed that proanthocyanidins statically quenched the fluorescence spectra by forming an inhibitor-α-glucosidase complex. Molecular docking results further indicated that the driving powers of the interaction between proanthocyanidins and α-glucosidase were hydrogen bonds and hydrophobic force. The main inhibitory mechanism of proanthocyanidins on α-glucosidase may be due to the insertion of proanthocyanidins into the pocket of the enzyme altering the catalytic configuration of the active site in a manner, thus reducing substrate binding affinity. The findings of this work provided a new perspective that proanthocyanidins from PFF with a possibility to be used as novel natural anti-diabetic agents in functional food industries. PRACTICAL APPLICATION: In this study, Pyracantha fortuneana fruit proanthocyanidins with a yield of 3.05% were identified for the first time as predominantly constituted of procyanidin with A-type and B-type linkage and coexistence of procyanidins glucoside. Proanthocyanidins from P. fortuneana fruit had higher anti-α-glucosidase activity value compared with positive control acarbose, which indicated that P. fortuneana fruit proanthocyanidins with a possibility to be used as novel natural antidiabetic agents in functional food industries.

Antimutagenic Effects of Selenium-Enriched Polysaccharides from Pyracantha fortuneana through Suppression of Cytochrome P450 1A Subfamily in the Mouse Liver.

Both selenium (Se) and polysaccharides from Pyracantha fortuneana (Maxim.) Li (PFPs) (P. fortuneana) have been reported to possess antioxidative and immuno-protective activities. Whether or not Se-containing polysaccharides (Se-PFPs) have synergistic effect of Se and polysaccharides on enhancing the antioxidant and immune activities remains to be determined. We previously reported that polysaccharides isolated from Se-enriched P. fortuneana (Se-PFPs) possessed hepatoprotective effects. However, it is not clear whether or not they have anti-mutagenic effects. In the present study, we compared and evaluated anti-mutagenic effects of Se-PFPs at three concentrations (1.35, 2.7 and 5.4 g/kg body weight) with those of PFPs, Se alone or Se + PFPs in mice using micronucleus assay in bone marrow and peripheral blood as well as mitomycin C-induced chromosomal aberrations in mouse testicular cells. We also elucidated the underlying mechanism. Our results demonstrated that Se-PFPs inhibited cyclophosphamide (CP)-induced micronucleus formation in both bone marrow and peripheral blood, enhanced the activities of superoxide dismutase (SOD) and glutathione peroxidase (GPx) in mouse liver, and reduced the activity and expression of cytochrome P450 1A (CYP4501A) in mouse liver in a dose-dependent manner. In addition, we found that the anti-mutagenic potential of Se-PFPs was higher than those of PFPs, Se alone or Se + PFPs at the same level. These results suggest that the anti-mutagenic potential of Se-PFPs may be mediated through the inhibition of the activity and expression of CYP4501A. This study indicates that application of Se-PFPs may provide an alternative strategy for cancer therapy by targeting CYP1A family.

Inhibition on the growth of human MDA-MB-231 breast cancer cells in vitro and tumor growth in a mouse xenograft model by Se-containing polysaccharides from Pyracantha fortuneana.

Breast cancer is the second cause of cancer-related death among Women. Current therapies for breast cancer have adverse side-effects. Selenium (Se)-containing polysaccharides have multiple health benefits to humans. Pyracantha fortuneana (P. fortuneana) contains rich Se polysaccharides. We hypothesized that Se-containing polysaccharides from P. fortuneana possess anticancer activity on breast cancer via inhibiting growth and inducing apoptosis. This study aimed to assess the anticancer effect of Se-containing polysaccharides from P. fortuneana and the underlying mechanisms. Se-containing polysaccharides were purified. Their properties and monosaccharide compositions were analyzed. Their effects on cell growth, expression of cycle proteins, apoptosis and apoptosis-related protein, and tumor growth in mouse xenograft model were examined. This extract contained 93.7% (w/w) of carbohydrate, 2.1% (w/w) of uronic acid and 3.7µg/g of Se, and was considered as Se-conjugated polysaccharides (Se-PFPs). In vitro studies showed that treatment of triple negative breast cancer (TNBC) MDA-MB-231 cells with Se-PFPs (1) inhibited cell growth dose-dependently by arresting cells at G2 phase via inhibiting CDC25C-CyclinB1/CDC2 pathway; (2) caused apoptosis associated with increased p53, Bax, Puma and Noxa, decreased Bcl2, increased Bax/Bcl2 ratio and increased activities of caspases 3/9, suggesting its effect on p53-mediated cytochrome c-caspase pathway. Treatment of nude mice bearing MDA-MB-231-derived xenograft tumors with Se-PFPs significantly reduced tumor growth without altering body weight, confirming its antitumor activity without toxic side effects. Se-PFPs enhanced doxorubicin cytotoxic effects. It is concluded that Se-containing polysaccharides from P. fortuneana potently inhibit the growth and induce apoptosis of TNBC cells and can be potential anticancer agent for TNBC.

New Whitening Constituents from Taiwan-Native Pyracantha koidzumii: Structures and Tyrosinase Inhibitory Analysis in Human Epidermal Melanocytes.

Nontoxic natural products useful in skin care cosmetics are of considerable interest. Tyrosinase is a rate-limiting enzyme for which its inhibitor is useful in developing whitening cosmetics. Pyracantha koidzumii (Hayata) Rehder is an endemic species in Taiwan that exhibits tyrosinase-inhibitory activity. To find new active natural compounds from P. koidzumii, we performed bioguided isolation and studied the related activity in human epidermal melanocytes. In total, 13 compounds were identified from P. koidzumii in the present study, including two new compounds, 3,6-dihydroxy-2,4-dimethoxy-dibenzofuran (9) and 3,4-dihydroxy-5-methoxybiphenyl-2'-O-ß-d-glucopyranoside (13), as well as 11 known compounds. The new compound 13 exhibited maximum potency in inhibiting cellular tyrosinase activity, the protein expression of cellular tyrosinase and tyrosinase-related protein-2, as well as the mRNA expression of Paired box 3 and microphthalmia-associated transcription factor in a concentration-dependent manner. In the enzyme kinetic assay, the new compound 13 acted as an uncompetitive mixed-type inhibitor against the substrate l-3,4-dihydroxyphenylalanine and had a Km value against this substrate of 0.262 mM, as calculated using the Lineweaver-Burk plots. Taken together, our findings show compound 13 exhibits tyrosinase inhibition in human melanocytes and compound 13 may be a potential candidate for use in cosmetics.

Combination of selenium-enriched green tea polysaccharides and Huo-ji polysaccharides synergistically enhances antioxidant and immune activity in mice.

BACKGROUND: The aim of this study was to investigate the influence of a combination of selenium-enriched green tea polysaccharides (Se-GTP) and Huo-ji polysaccharides (HJP) on the immune function and antioxidant activity in mice. RESULTS: The results showed that the indices of spleen and thymus were markedly increased, and the activity of natural killer (NK) cell was promoted in mice treated with the combination of Se-GTP and HJP. The combined treatment of Se-GTP and HJP also reduced the content of tumour necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in splenocytes. In addition, the activities of glutathione peroxidase (GPx) and superoxide dismutase (SOD) were remarkably enhanced, and malondialdehyde (MDA) levels were significantly reduced in mice treated with combination of Se-GTP and HJP. Furthermore, the combined treatment of Se-GTP and HJP increased nuclear factor erythroid 2-related factor (Nrf2) expression at mRNA and protein levels in splenocytes. The effects of the combination treatment of Se-GTP and HJP in mice were stronger than with Se-GTP or HJP treatment alone. CONCLUSION: Our study suggests that the combined administration of Se-GTP and HJP can synergistically improve immune function and decrease the oxidative stress by enhancing the mechanisms involved in the clearance of free radicals.

Effects of polysaccharides from selenium-enriched Pyracantha fortuneana on mice liver injury.

We have previously reported that polysaccharides extracted from Pyracantha fortuneana (Maxim.) Li (P. fortuneana) lowered the oxidative stress and inhibited the inflammatory responses in mice. Our present study aims to determine the effects of Selenium enriched P. fortuneana polysaccharides (Se-PFPs) against carbon tetrachloride (CCl4)-induced liver injury in a mouse model. Our results displayed that CCl4 remarkably elevated the levels of alanine transferase (ALT), aspartate transaminase (AST), lactic dehydrogenase (LDH), cholesterol, triglycerides in serum. However, similar to BP treatment, supplementation of mice with Se-PFPs resulted in reversal of ALT, AST, LDH, cholesterol, triglycerides in serum. Contrary to CCl4, supplementation of mice with Se-PFPs elevated the activities of superoxide dismutase (SOD), glutathione peroxidase (GPx) and levels of glutathione (GSH) in liver. Furthermore, Se-PFPs treatment increased the expression of GPx and catalase (CAT) at mRNA and protein levels in liver which were decreased in CCl4 group. Contrary to CCl4, Se-PFPs supplement decreased the levels of thiobarbituric acid reactive substances (TBAR) and H2O2, which served as lipid peroxidation biomarker. Our study indicates that Se-PFPs administration is effective in attenuating CCl4-induced liver injury. The mechanism underlying this effect may be attributed to the reduction of oxidative stress and inflammation in the liver by Se-PFPs through up-regulation of the antioxidant system. Our study suggests that Se-PFPs might be a potential dietary agent in the prevention of hepatic damage.

Characterisation of water-soluble proanthocyanidins of Pyracantha fortuneana fruit and their improvement in cell bioavailable antioxidant activity of quercetin.

Proanthocyanidins (PCs) with poor bioavailability were argued for their health benefits. In this study, water-soluble polymeric polyphenolic PCs fractions from Pyracanthafortuneana fruit were used to investigate whether the presence of PCs is correlated with the increased cell antioxidant activities (CAA) of quercetin (Q). The results indicated that the most decrement in the values of EC50, which Q inhibited peroxyl radical-induced DCFH oxidation effective in the HepG2 cells, was observed to be 2.91 (vs. control 5.97) in the present of the fraction with 15.8 of the average degree of polymerisation of PCs (ADP). Also, the order of efficacy was the same with the ADP of PCs. Further, this effect is associated with the improvement of the solubility and stability of Q after the addition of the PCs. Our current study suggests that the additive effects of PCs on small molecular polyphenols may be responsible for their antioxidant benefits in vivo.