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Atopic dermatitis (AD) is a long-term allergic skin disorder that occurs most frequently in children. Currently, the common treatment of AD is corticosteroids; however, the drugs cause serious side effects. Therefore, there are many patients who seek complementary and alternative treatments such as healthy food. We report that fucoidan from Cladosiphon okamuranus (COP) exhibit exceptional immuno-modulatory effects significantly improving atopic dermatitis (AD) at both in vitro and in vivo levels: First, we performed the P815 cell degranulation assay, of which the results revealed that COP possesses anti-degranulation activity suggesting COP is very conducive to relieving allergic reactions of AD. Next, we performed the animal model examination, of which AD was significantly improved, suggesting COP can focally and globally modulate the immune systems of animals. The systemic improvements were manifested clearly by decreased epidermal hyperplasia, reduced infiltration of eosinophils, and decreased expression of AD-associated cytokines. Notably, COP reduced epidermal hyperplasia by downregulating the expression of IL-22. COP displayed therapeutic effects, which is comparable to corticosteroids but lack corticosteroid side effects, such as weight loss in our animal study. COP is multitudinous immunomodulatory abilities to serve as a healthy food supplement at the current stage, not least beneficial to atopic dermatitis.

The modulatory activity of water extracts from fresh roots of Polygonum multiflorum (WRP) on oxidative stress in two liver cell lines was investigated for the first time. WRP increased antioxidant enzyme activities in Clone 9 cells, including catalase (CAT), glutathione-S-transferase (GST), glutathione reductase (GR), and glutathione peroxidase (GPx). The intracellular glutathione (GSH) level was also increased in the Clone 9 cells owing to antioxidase activity elevating effect by WRP treatment for 24 h. On the other hand, reactive oxygen species (ROS) were generated in abundance upon WRP treatment in Hep G2 cells, resulting in the suppression of cell proliferation. Apoptosis was increased to 78% and 77% after WRP (1000 μg/mL) treatment for 24 and 48 h, respectively. Moreover, WRP stimulated the activation of caspase-8, caspase-9, and ultimately caspase-3. Hep G2 cell growth suppression and caspase induction by WRP were greater than that by emodin-like substances (WRPE), a major active compound. These results indicated that phytochemicals present in extracts of P. multiflorum root act synergistically to promote apoptosis, suggesting the possible use of these extracts for hepatoprotection.

Monascus purpureus is a fungus used in rice fermentation. Monascus-fermented rice is called red-mold rice (RMR) in Taiwan since the fermentation products contain a considerable amount of red pigments. The protective effects of RMR on oxidative stress in the testis and sperm were evaluated in this study. Zn deficiency was induced in rats by feeding them with a Zn-deficient diet for 12 weeks while the control rats were fed with a normal diet. The Zn-deficient rats were then divided into 6 groups, designated as Zn-deficient (ZD). Zn-compensated (ZC), IR (151 mg RMR/kg), 5R (755 mg RMR/kg), 1R+ZC (1RZ), and 5R+ZC (5RZ). The animals were administered with the mentioned diet (RMR/Zn) for 8 weeks. In the ZD rats, no spermatid cell formation was observed in the seminiferous tubular epithelia, and testis necrosis/atrophy was apparent. However, 5R and 5RZ administration improved testicular antioxidant enzyme activity, elevated serum testosterone levels, and increased sperm number in ZD rats; this treatment also exhibited inhibitory effects on caspase activities and reactive oxygen species (ROS) levels in the ZD rats, suggesting that RMR attenuated ZD-induced oxidative stress and testis apoptosis. The preventive activity against ZD-induced reproductive damage was more apparent in the 1RZ and 5RZ groups than in the ZC group, suggesting that RMR can serve as a supplement in adjuvant therapy for diseases associated with Zn deficiency.

Staphylococcus aureus is a common zoonotic bacterium for disease in pigs and human and causes health problem. The aim of the study is to investigate the potential of soluble pathogenic recognition protein pentraxin-3 (PTX3) on inhibiting proliferation, adhesion, and infection of S. aureus in porcine kidney epithelial PK15 cells (PK15 cells). PTX3 suppressed the growth of S. aureus and avoided it adhering to PK15 cells. PTX3 treatment also attenuated cell apoptosis induced by S. aureus in PK15 cells. The results suggest that PTX3 is able to interfere with the bacterial pathogenesis via inhibiting the growth of S. aureus and decreasing their adhesion to cells. Hence, PTX3 may replace the use of antibiotics and develop as a novel anti-microbial agent for disease prevention in piglets.

PT-peptide is derived from the anti-lipopolysaccharide factor of the swimming crab Portunus trituberculatus. The peptide, consisting of 34 amino acids, contains a lipopolysaccharide binding domain. In this study, we investigated the effect of PT-peptide encapsulated in raw milk-derived extracellular vesicles (EVs), designated as EVs-PT peptide, on immune regulation. The results showed that raw milk-derived EVs efficaciously delivered the PT-peptide into monocytes and elevated immune activity, including reactive oxygen species level, superoxide anion production, and phagocytosis. PT-peptide and EVs-PT peptide also elevated the secretion of cytokines, such as interferon-&gamma, interleukin-6, and tumor necrosis factor-&alpha, in human monocytic THP-1 cells. These results suggest that the PT-peptide could be developed as an immune stimulator.

Graptopetalum paraguayense was shown to exhibit antioxidant, hepatoprotective and anti-hepatocellular carcinoma activities in a recent study. In this work, fractions of the G. paraguayense aqueous solution were extracted using n-hexane, ethyl acetate (EF) and n-butanol, and its antioxidative and anti-glycative activities were evaluated. The EF extract exhibited the highest antioxidative activity, potently inhibited the formation of advanced glycation end products (AGEs) and reduced glycation-induced protein oxidation. Additionally, the EF extract protected Hep G2 cells against AGE-induced DNA damage. Five major components were isolated and identified in the EF fraction by semi-preparative high-performance liquid chromatography, liquid chromatography-tandem mass spectroscopy and nuclear magnetic resonance: gallic acid, isoquercitrin-6-(3-hydroxy-3-methylglutarate), astragalin-6-(3-hydroxy-3-methylglutarate), isoquercitrin-2-acetyl-6-(3-hydroxy-3-methylglutarate) and astragalin-2-acetyl-6-(3-hydroxy-3-methylglutarate). G. paraguayense exhibited antioxidant and anti-glycation activities, likely because of the presence of gallic acid. The findings indicate the potential for using G. paraguayense for development of novel treatments for diabetes. Practical Applications Herbal treatments for hyperlipidemia are relatively cheap and locally available. The results indicated that the extracts of Graptopetalum paraguayense may be developed as functional foods for antidiabetic treatment mediated by attenuations of advanced glycation end product oxidation.

Monascus has traditionally been used for the preparation of fermented products and as a food additive in Asia and is also a traditional Chinese medicine. The present review summarizes the underlying biochemical and molecular mechanisms that can explain anti-inflammation, antioxidation, hepatoprotection, inhibition of cancer cell invasion, and detoxification of dimerumic acid (DMA) isolated from Monascus-fermented products. DMA is an antioxidant that effectively inhibits liver damage and inflammation by attenuating oxidative stress in vitro and in vivo, which is stronger than silymarin, resveratrol, or curcumin. In addition, several lines of evidence have indicated that reactive oxygen species (ROS) promotes cancer cell invasion and suppress tumor development. DMA has been reported to attenuate ROS-induced invasion of SW620 (colorectal adenocarcinoma cells) greater than silymarin, resveratrol, and curcumin. These findings suggest that DMA has potential for development as a novel antioxidant for functional foods to act against several diseases-associated oxidative stress.

Miracle fruit (Synsepalum dulcificum) belongs to the Sapotaceae family. It can change flavors on taste buds, transforming acidic tastes to sweet. We evaluated various miracle fruit extracts, including water, butanol, ethyl acetate (EA), and hexane fractions, to determine its antioxidant effects. These extracts isolated from miracle fruit exerted potential for reduction of uric acid and inhibited xanthine oxidase activity in vitro and in monosodiumurate (MSU)-treated RAW264.7 macrophages. Moreover, we also found that the butanol extracts of miracle fruit attenuated oxonic acid potassium salt-induced hyperuricaemia in ICR mice by lowering serum uric acid levels and activating hepatic xanthine oxidase. These effects were equal to those of allopurinol, suggesting that the butanol extract of miracle fruit could be developed as a novel anti-hyperuricaemia agent or health food.

The role of inflammation-induced oxidative stress in the pathogenesis and progression of chronic inflammatory airways diseases has received increasing attention in recent years. Nuclear factor-erythroid 2 related factor 2 (Nrf-2) is the primary transcription factor that regulates the expression of antioxidant and detoxifying enzymes. In this study, yellow pigment ankaflavin (AK), derived from Monascus-fermented products, elevated nuclear Nrf-2 protein translocation in both the A549 lung cell line and the lungs of ovalbumin (OVA)-challenged mice. Furthermore, AK increased the mRNA expression of antioxidant enzymes regulated by Nrf-2, leading to a reduction in allergen-driven airway inflammation, mucus cell hyperplasia, and eosinophilia in OVA-challenged mice. Additionally, AK prevented T-cell infiltration and Th2 cytokines including interleukin (IL)-4, IL-5, and IL-13 generation in bronchial alveolar lavage fluid. The adhesion molecules ICAM-1, VCAM-1, and eotaxin were substantially reduced by AK treatment. Importantly, the inhibitory effect of AK on adhesion molecule production and immune cell infiltration was abolished by Nrf-2 small interfering RNA. This is the first study to illustrate that AK acts as a novel Nrf-2 activator for modulating the oxidative stress pathway to improve the lung injury and ameliorate the development of airway inflammation.

Polygonum multiflorum is known as a medicinal plant. It has been used as a folk medicine which showed antioxidative property.Protective effects of the water extracts (w/v:1/10) from fresh P. multiflorum (WEP) on carbon tetrachloride (CCl(4))-induced liver damage in rats were investigated.CCl(4) was used for inducing liver damage of SD rats, and WEP and emodin were fed for eight consecutive weeks.We found that emodin levels in fresh WEP was higher than that in ripening WEP. Rats were administered WEP and emodin, the main active compound, for 56 consecutive days. WEP significantly lowered the serum levels of hepatic enzyme markers, aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and reduced the generation of malonaldehyde. Treatment with WEP recovered glutathione S-transferase and catalase activity in rats as compared to treatment with CCl(4) alone. In addition, serum tumor necrosis factor-α, an inflammatory marker, was found to decrease in rats treated with WEP. In histopathological evaluation, fatty degeneration and necrosis were found to be significantly decreased in the CCl(4) plus WEP treatment group.WEP may be effective in attenuating liver damage by reducing lipid peroxidation as well as by positively modulating inflammation.

Gamma-aminobutyric acid (GABA) and angiotensin-converting enzyme inhibitor (ACEI) are compounds which can influence hypertension. The goal of this study is to optimize the culture condition for GABA and ACEI production by Lactobacillus plantarum NTU 102 fermented skim milk. In this study, we used 3-factor-3-level Box–Behnken design combining with response surface methodology, where the 3 factors represent the concentration of skim milk, the concentration of monosodium glutamate, and culture temperature. Best conditions for GABA and ACEI production differed. The results indicated that L. plantarum NTU 102 produced the highest combined levels of GABA and ACEI at 37 °C, in milk having 8% to 12% nonfat solids supplemented with 0.6% to 1% MSG. Agitation of the medium during fermentation had no effect on GABA or ACEI production but extended incubation (up to 6 d) increases levels of the bioactive compounds. L. plantarum NTU 102 fermented products may be a potential functional food source for regulating hypertension.

Monascus-fermented products offer valuable therapeutic benefits and have been extensively used for centuries in East Asia. Dioscorea has been proved to have anti-cancer effect. The aim of this study is to investigate the anti-tumor ability of the ethanol extract of red mold dioscorea (RMDE) on 7,12-dimethyl-1,2-benz[a]anthracene (DMBA)-induced hamster buccal pouch carcinogenesis. We induced oral squamous cell carcinoma (OSCC) in the buccal pouch of male Syrian golden hamsters by painting with 0.5% DMBA three times a week for 14 weeks. From 9 to 14 weeks, a dose of 50, 100, and 200 mg RMDE per kg body weight were painting with the hamsters for 6 weeks on days alternate to the DMBA application. The results demonstrated that RMDE decreased nitric oxide (NO), reactive oxygen species (ROS), and prostaglandin E2 (PGE2) overexpression in hamster buccal pouches in the DMBA treatment group and increased p53, serum tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β) to significantly stimulate caspase-8 and -3 activities, indicating that RMDE reduced oxidative damage causing by DMBA and induced apoptosis in oral cancer cells. Therefore, RMDE may have therapeutic potentials against OSCC.

BACKGROUND:Monascus-fermented products are among the most commonly used traditional food supplements. Dioscorea is known to exhibit anticancer properties. In this study the effects of the ethanol extract of red mold dioscorea (RMDE) on cell proliferation, cell cycle and apoptosis in human oral cancer cells were investigated. RESULTS: RMDE exercised growth inhibition on squamous cell carcinoma-25 (SCC-25) cells. RMDE-mediated G2/M phase arrest was associated with the down-regulation of NF-κB, resulting in the inhibition of cyclin B1 and CDK1 expression; this may be the mechanism by which RMDE inhibits cancer cells. Furthermore, the proapoptotic activity of RMDE was revealed by the Annexin V-FITC/PI double-staining assay. In addition, the proapoptotic effect of RMDE was evident by the inhibition of Bax expression in the mitochondria, resulting in the activation of caspase-9 and caspase-3 and subsequent triggering of the mitochondrial apoptotic pathway. RMDE also enhanced caspase-8 activity, indicating the involvement of the death receptor pathway in RMDE-mediated SCC-25 cell apoptosis. CONCLUSION: RMDE treatment inhibited the growth of SCC-25 cells by arresting cell cycle at the G2/M phase and induced apoptosis in a time- and dose-dependent manner. Therefore RMDE may be a good candidate for development as a dietary supplement against oral cancer. Copyright © 2010 Society of Chemical Industry

Zn deficiency is a common disease leading to memory impairment with increasing age. This study evaluated the protection effects of red mold rice (RMR) administration and Zn supplementation against memory and learning ability impairments from oxidative stress caused by Zn deficiency. Rats (4 weeks old) were induced to be Zn deficiency by a Zn-deficient diet for 12 weeks. After that, rats were administered Zn, 1xRMR, 5xRMR, and various dosages of RMR plus Zn, respectively. Decreases of antioxidant enzyme activities in the hippocampus and cortex were observed, and the levels of Ca, Fe, and Mg were increased in the hippocampus and cortex of Zn-deficient rats, leading to memory and learning ability injury. However, the administration of RMR (1- or 5-fold dosage) and with or without Zn significantly improved the antioxidase and neural activity to maintain cortex and hippocampus functions. This study demonstrates that RMR is a possible functional food for the prevention or cure of neural injury associated with Zn deficiency.

Methylglyoxal (MG) is a reactive dicarbonyl compound generated as an intermediate of glycolysis during the physical glycation in the diabetic condition. MG itself has been commonly implicated in the development of diabetic neuropathy. Several active compounds in Actinidia callosa have been found to inhibit glycation and MG-protein reaction.This study investigated the protective effects of A. callosa (kiwi fruits) peel ethanol extracts (ACE) on MG-induced Neuro-2A cell apoptosis.The Neuro-2A cells pre-treated by ACE (50-200 μg/mL) or allyl-isothiocyanate (AITC) (50 μM) for 6 h, in turn, the cells were treated with MG (250 μM) for 24 h.ACE or AITC treatment markedly inhibited the generation of reactive oxygen species (ROS) and the elevation of caspase-3 and capase-9 levels induced by MG in Neuro-2A cells. ACE and AITC elevated Bcl2 and inhibited Bax expressions in MG-induced Neuro-2A cells. ACE elevated Nrf2 transcriptional activity and nuclear translocation in MG-induced Neuro-2A cells. Nrf2 down-stream molecules including HO-1 and GCL were elevated by ACE or AITC treatment in MG-induced Neuro-2A cells. The protective effects of ACE on MG-induced Neuro-2A apoptosis were attenuated while Nrf2 knockdown.We established the first evidence that ACE might contribute to the prevention of the development of diabetic neuropathy by blocking the MG-mediated intracellular glycation system.

Yellow pigment monascin (MS) is a secondary metabolite isolated from Monascus -fermented products and has numerous physiological activities. However, the potential use of MS for immunomodulation remains unclear. We showed that MS and the synthetic peroxisome proliferator-activated receptor (PPAR)-γ ligand rosiglitazone (RG) significantly inhibited the production of Th2 cytokines, including IL-4, IL-5, and IL-13, in PMA/ionomycin-activated mouse EL-4 T cells. Moreover, we showed that this was due to cellular PPAR-γ translocation. These results indicate that MS and RG promote PPAR-γ-DNA interactions and suggest that the regulatory effects of MS and RG on Th2 cytokine production could be abolished with PPAR-γ antagonist treatment. MS and RG also suppressed Th2 transcription factor translocation (e.g., GATA-3 and nuclear factor of activated T cells) by preventing the phosphorylation of protein kinase C and signal transducer and activator of transcription 6.

This study was designed to evaluate the effects of dimerumic acid (DMA) on receptor for advanced glycation endproducts (RAGE) signal activation and THP-1 monocyte inflammation treated with S100b, a specific ligand of RAGE. We found that DMA inhibited inflammatory cytokine production via upregulation of nuclear factor-erythroid 2-related factor 2 (Nrf2) and alleviated oxidative stress through attenuation of p47phox translocation to the membrane of S100b-treated THP-1 monocytes. We found that DMA activated Nrf2 mediated by the p38 kinase pathway in THP-1 monocytes. However, anti-inflammatory activity of DMA was attenuated by Nrf2 siRNA treatment. In an animal model, methylglyoxal (MG; 200mg/kg bw) was chosen to induce diabetes in Balb/C mice (6 weeks) in this work. The in vivo verification of anti-inflammation in peripheral blood mononuclear cells by DMA treatment was confirmed by tumor necrosis factor-α and interleukin-1β measurements. Oral glucose tolerance test, insulin tolerance test, hyperinsulinemia, and hyperglycemia were improved in MG-treated mice by DMA treatment and these effects were greater than those of silymarin and N-acetylcysteine. Furthermore, DMA increased hepatic glyoxalase mRNA and glutathione mediated by Nrf2 activation to metabolize MG into d-lactic acid, thereby reducing serum and hepatic AGE levels and suppressing inflammatory factor generation in MG-treated mice. However, DMA did not exert the antiglycation activity in MG-bovine serum albumin incubation. Taken together, the results indicate that DMA is a novel antioxidant and Nrf2 activator that lowers AGE levels and may prove to be an effective treatment for diabetes.

Ankaflavin (AK) is an active compound having anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects. We have previously reported that AK acts as an antioxidant and antidiabetic drug; however, the mechanism by which AK prevents diabetes remains unknown. Hyperglycemia is associated with protein glycation, which produces advanced glycation end-products (AGEs). Methylglyoxal (MG)—a metabolite of carbohydrates—is believed to cause insulin resistance by inducing inflammation and pancreas damage. In this work, diabetes was induced in Wistar rats (4 weeks of age) by treating them with MG (600 mg/kg bw) for 4 weeks. We observed that AK (10 mg/kg bw) exerted peroxisome proliferator-activated receptor-γ (PPARγ) agonist activity, thereby enhancing insulin sensitivity (as indicated by hepatic GLUT2 translocation, PTP1B suppression, and glucose uptake) by downregulating blood glucose and upregulating pancreatic and duodenal homeobox-1 and Maf-A expression and increasing insulin production in MG-induced rats. However, these effects were abolished by the administration of GW9662 (PPARγ antagonist), but the expression of hepatic heme oxygenase-1 (HO-1) and glutamate–cysteine ligase (GCL) was not suppressed in MG-induced rats. Therefore, the nuclear factor erythroid-related factor-2 (Nrf2) activation was investigated. AK did not affect hepatic Nrf2 mRNA or protein expression but significantly increased Nrf2 phosphorylation (serine 40), which was accompanied by increased transcriptional activation of hepatic HO-1 and GCL. These data indicated that AK protected rats from oxidative stress resulting from MG-induced insulin resistance. In contrast, these effects were not detected when the rats were treated with the antidiabetic drug rosiglitazone (10 mg/kg bw). Moreover, we found that AK did not inhibit the generation of AGEs in vitro; however, the glutathione (GSH) levels in liver and pancreas of MG-induced rats were elevated in rats administered AK. Therefore, we believe that GSH may lower the MG level, which attenuates the formation of AGEs in the serum, kidney, liver, and pancreas of MG-induced rats. We also found that AK treatment reduced the production of inflammatory factors, such as tumor necrosis factor-α and interleukin-1β. Taken together, the results of our mechanistic study of MG-induced rats suggest that the protective effects of AK against diabetes are mediated by the upregulation of the signaling pathway of Nrf2, which enhances antioxidant activity and serves as a PPARγ agonist to enhance insulin sensitivity.

Previous studies have established that red mold rice can regulate blood pressure in spontaneously hypertensive rats (SHR) and that Monascus -fermented products, including monacolin K, ankaflavin (AF), and monascin (MS), can inhibit expression of adhesion factors such as E-selectin and endothelin-1 to prevent human acute monocytic leukemia cell line THP-1 monocytes from adhering to human aortic endothelial cells. However, it remains unknown whether AF and MS act directly on human umbilical endothelial cells (HUVECs) to enhance nitric oxide (NO) synthesis through the stimulation of endothelial NO synthase (eNOS) expression. To address this knowledge gap, this study investigated whether AF and MS directly regulate NO synthesis and attenuate adhesion factor expression induced by treatment with tumor necrosis factor-α (TNF-α) in HUVECs. The results revealed that both AF and MS (20 μM) treatments promoted increases in eNOS expression and decreases in vascular cell adhesion molecule-1 (VCAM-1), E-selectin, and endothelin-1 mRNA and protein expression resulting from 12 h of TNF-α treatment. These effects are attributed to the ability of AF and MS to inhibit extracellular signal-regulated protein kinase (ERK) phosphorylation and nuclear factor κB (NF-κB) translocation from the cytoplasm into the nucleus, thereby exerting antihypertensive activity.

Fermentation products of the fungus Monascus offer valuable therapeutic benefits and have been used extensively for centuries in Asia. The aim of this study is to investigate the inhibitory effect of the Monascus -fermented metabolite monascin (MS) on the molecular mechanism of ovalbumin (OVA)-induced inflammation in the human THP-1 monocyte cell line. We found that 1, 5, and 25 μM of MS significantly attenuated several proinflammatory mediators, including inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression as well as nitric oxide (NO) and prostaglandin E 2 (PGE 2 ) formation caused by OVA stimulation. Further, 5 and 25 μM of MS significantly reduced the generation of tumor necrosis factor-α (TNF-α) and interleukin 6 (IL-6) at both the protein and mRNA levels. MS (5 and 25 μM) decreased OVA-induced phosphorylation of mitogen-activated protein kinase (MAPK) c-Jun NH 2 -terminal kinase (JNK), but not that of extracellular signal-regulated kinase (ERK) or p38 kinase. We used the peroxisome proliferator activated receptor-γ (PPAR-γ) antagonist GW9662 to show that MS inhibit JNK phosphorylation through increased expression of PPAR-γ. Thus, the metabolites from Monascus fermentation may serve as a dietary source of anti-inflammatory agents.

BACKGROUND: Immunomodulation by probiotic microorganisms has become a topic of increasing interest in food microbiology. Polysaccharides are broadly used in the food industry as gelling, thickening, stabilizing, or emulsifying agents. Some probiotics such as lactic acid bacteria also produce exopolysaccharides that stimulate macrophage production of cytokines. The aim of this study was to characterize the effects of exopolysaccharides of Lactobacillus paracasei subsp. paracasei NTU 101 (101EP) and Lactobacillus plantarum NTU 102 (102EP) exopolysaccharides on antioxidant activity and immunomodulation in vitro. RESULTS: The sugar composition (including arabinose, galactose, glucose, fructose, mannose, and maltose) of 101EP and 102EP was quantified by high-performance anion-exchange chromatography. Cytokine production (including IL-6, TNF-α, and IL-1β) was induced by 101EP and 102EP in Raw 264.7 in a dose-dependent manner (5-500 µg mL−1). 101EP and 102EP also demonstrated potential antioxidant properties (1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, chelation of ferrous ions, inhibition of linoleic acid peroxidation, and reducing power) in vitro. CONCLUSION: 101EP and 102EP stimulate cell proliferation and may be useful as a mild immune modulator of macrophages. Copyright © 2011 Society of Chemical Industry

Buckwheat is a healthy food commonly eaten worldwide. The antitumor activity of buckwheat polysaccharides (BWPSs) has not yet been evaluated. In recent years, inducing differentiation of leukemic cells has become one of the most important therapeutic approaches for curing leukemia, and this strategy effectively inhibits leukemia cell proliferation and growth because the differentiation inducer changes leukemic cell morphology and cellular characters by inducing cellular maturity. The ability of BWPS to induce the differentiation of human leukemic THP-1 cells (monocyte [MNC]/macrophage-like cells) was investigated by both direct and indirect treatments in this study. In the indirect treatment, BWPS significantly stimulated cytokine secretion (differentiation inducer) in MNCs from peripheral blood mononuclear cells in MNC-conditioned medium (BWPS-MNC-CM) following a 24-hour treatment, and THP-1 cell differentiation and maturity were significantly increased after 5 days of treatment with the BWPS-MNC-CM. On the other hand, BWPS directly induced THP-1 cell differentiation and maturity following 3-day and 5-day treatments in a dose-dependent manner and exerted phagocytic activity and superoxide anion production in these mature cells. These findings indicate that BWPS has potential for differentiation therapy in leukemia.

Monascus -fermented products offer valuable therapeutic benefits and have been extensively used in East Asia. This study investigated the prevention of oral tumor formation and antioxidative ability of the ethanol extracts from red mold dioscorea (RMDE) on 7,12-dimethyl-1,2-benz[a]anthracene (DMBA)-induced hamster buccal pouch (HBP) carcinogenesis. The HBP was painted with DMBA three times per week for 14 weeks, and animals were painted with celecoxib, RMDE (50, 100, and 200 mg/kg of bw), and ethanol extracts from dioscorea (200 mg/kg of bw) on days alternate to the DMBA application. The results demonstrated that RMDE attenuated tumor formation by elevating the antioxidase activity and suppressing the overproduction of reactive oxygen species, nitric oxide, prostaglandin E(2), and pro-inflammatory cytokines in the HBP caused by DMBA induction. These results indicated that RMDE exerted anti-inflammatory and antioxidative activity to prevent oral cancer. Therefore, the metabolite from Monascus fermentation may serve as a possible functional edible substance for the prevention of oral cancer.

Monascus-fermented products offer valuable therapeutic benefits and have been extensively used in East Asia. However, the polysaccharide obtained from Monascus-fermented products has never been investigated. This study evaluated the effects of dioscorea polysaccharide (DPS) and red mold dioscorea polysaccharide (RMDPS) on differentiation of leukemic THP-1 cells. DPS and RMDPS inhibited THP-1 cells proliferation in dose- and time-dependent manners. The differentiation induction (macrophage-like cells) was observed when THP-1 cells were treated with DPS and RMDPS for 5 days. Superoxide anion production, phagocytic capacity, and cytokine secretion confirmed activity for differentiating THP-1 cells. Results indicated that RMDPS elevated reactive oxygen species production and immune activity, including phagocytosis, interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), and interferon-γ (IFN-γ) productions in THP-1 cells, which was greater than that seen with DPS. These results may be attributed to Monascus-fermentation altering the carbohydrate components and polysaccharide structure. RMDPS may serve as a novel material and functional ingredient to exert anticancer capacity.

Because of the high incidence of cardiovascular diseases in Asian countries, traditional fermented foods from Asia have been increasingly investigated for antiatherosclerotic effects. This study investigated the production of nattokinase, a serine fibrinolytic enzyme, in pigeon pea by Bacillus subtilis fermentation. B. subtilis 14714, B. subtilis 14715, B. subtilis 14716, and B. subtilis 14718 were employed to produce nattokinase. The highest nattokinase activity in pigeon pea was obtained using B. subtilis 14715 fermentation for 32 hours. In addition, the levels of antioxidants (phenolics and flavonoids) and angiotensin converting enzyme inhibitory activity were increased in B. subtilis 14715-fermented pigeon pea, compared with those in nonfermented pigeon pea. In an animal model, we found that both water extracts of pigeon pea (100 mg/kg body weight) and water extracts of B. subtilis-fermented pigeon pea (100 mg/kg body weight) significantly improved systolic blood pressure (21 mmHg) and diastolic blood pressure (30 mmHg) in spontaneously hypertensive rats. These results suggest that Bacillus-fermented pigeon pea has benefits for cardiovascular health and can be developed as a new dietary supplement or functional food that prevents hypertension.