Schisandra chinensis and Its Main Constituent Schizandrin Attenuate Allergic Reactions by Down-Regulating Caspase-1 in Ovalbumin-Sensitized Mice.

Schisandra chinensis (SC) and its main constituent, schizandrin (SCH) exhibit anti-inflammatory and anti-allergic activities. Allergic and inflammatory reactions are aggravated via caspase-1 signaling pathway. However, the regulatory effects of SC and SCH on caspase-1 activation have not been clarified yet. In this study, we aimed to clarify the anti-allergic effects of SC and SCH using an ovalbumin (OVA)-sensitized mice and anti-CD3 and anti-CD28 antibodies-stimulated splenocytes. SC or SCH significantly inhibited the levels of immunoglobulin (Ig)E, IgG1, or interleukin (IL)-4 in serum of OVA-sensitized mice. SC or SCH significantly inhibited the levels of IL-6, tumor necrosis factor (TNF)-[Formula: see text], and IL-1[Formula: see text] in spleen of the OVA-sensitized mice. SC or SCH significantly suppressed the expression of caspase-1 and receptor-interacting protein (RIP)-2 in spleen of the OVA-sensitized mice. In activated splenocytes, SC or SCH significantly decreased the expression of caspase-1 and RIP-2 as well as the production of IL-6 and TNF-[Formula: see text]. We suggest that SC and SCH exert an anti-allergic effect by down-regulating caspase-1 signaling.

Improvement of depressive behavior by Sweetme Sweet Pumpkin™ and its active compound, ß-carotene.

AIMS: Sweetme Sweet Pumpkin™ (SSP, baked Cucurbita moschata Duch.) has been used to treat patients with depression in Korea. However, the role of SSP in improving depression has not been elucidated yet. Thus, we assessed the antidepressant-like effect of SSP and its active compound, ß-carotene, with the forced swimming test (FST). MAIN METHODS: SSP and ß-carotene were orally administered once a day for 28days. The levels of brain-derived neurotrophic factor (BDNF), phosphorylated extracellular signal-regulated kinase (pERK), and estrogen receptor-beta (ER-ß) were analyzed by Western blotting and quantitative real-time-polymerase chain reaction. KEY FINDINGS: After 28days, treatment with SSP and ß-carotene significantly decreased the immobility time during the FST. SSP significantly increased the levels of serotonin and norepinephrine in the brain. The levels of BDNF, pERK, and ER-ß were significantly increased in the SSP- and ß-carotene-administered groups compared with the control group. In addition, the groups treated with SSP and ß-carotene showed significantly reduced levels of tumor necrosis factor-alpha and interleukin-6 compared with the control group. SIGNIFICANCE: In conclusion, these findings suggest the potential of SSP and ß-carotene as a novel therapeutic agent for the treatment of depression.

The complete chloroplast genome of a medicinal plant Epimedium koreanum Nakai (Berberidaceae).

Epimedium koreanum is a perennial medicinal plant distributed in Eastern Asia. The complete chloroplast genome sequences of E. koreanum was obtained by de novo assembly using whole genome next-generation sequences. The chloroplast genome of E. koreanum was 157 218 bp in length and separated into four distinct regions such as large single copy region (89 600 bp), small single copy region (17 222 bp) and a pair of inverted repeat regions (25 198 bp). The genome contained a total of 112 genes including 78 protein-coding genes, 30 tRNA genes, and 4 rRNA genes. Phylogenetic analysis with the reported chloroplast genomes revealed that E. koreanum is most closely related to Berberis bealei, a traditional medicinal plant in the Berberidaceae family.

Antidepressant effect of Stillen.

Stillen has been used to treat patients with gastric mucosal ulcers and has an anti-inflammatory effect. It is well-known that neuro-inflammatory reactions are related to depression. Here we evaluated the antidepressant-like effect of Stillen on mice subjected to the forced swimming test (FST). Stillen and eupatilin (a major component of Stillen) significantly decreased immobility times compared with the FST control group. In the Stillen-administered group, increased levels of 5-hydroxytryptamine (serotonin) and brain-derived neurotrophic factor protein were observed in the hippocampus. Nissl bodies also increased in the hippocampus neuronal cytoplasm of the Stillen-administered group. Stillen decreased levels of interleukin (IL)-1ß, IL-6, and tumor necrosis factor-α (at the mRNA and protein levels) in the hippocampus and serum, compared with the control group. In addition, the mRNA expression of estrogen receptor-ß increased after Stillen administration in the hippocampus. These findings suggest that Stillen should be viewed as a candidate antidepressant.

Inhibition of IRAK-4 activity for rescuing endotoxin LPS-induced septic mortality in mice by lonicerae flos extract.

Lonicerae flos extract (HS-23) is a clinical candidate currently undergoing Phase I trial in lipopolysaccharide (LPS)-injected healthy human volunteers, but its molecular basis remains to be defined. Here, we investigated protective effects of HS-23 or its major constituents on Escherichia coli LPS-induced septic mortality in mice. Intravenous treatment with HS-23 rescued LPS-intoxicated C57BL/6J mice under septic conditions, and decreased the levels of cytokines such as tumor necrosis factor α (TNF-α), interleukin (IL)-1ß and high-mobility group box-1 (HMGB-1) in the blood. Chlorogenic acid (CGA) and its isomers were assigned as major constituents of HS-23 in the protection against endotoxemia. As a molecular mechanism, HS-23 or CGA isomers inhibited endotoxin LPS-induced autophosphorylation of the IL-1 receptor-associated kinase 4 (IRAK-4) in mouse peritoneal macrophages as well as the kinase activity of IRAK-4 in cell-free reactions. HS-23 consequently suppressed downstream pathways critical for LPS-induced activation of nuclear factor (NF)-κB or activating protein 1 (AP-1) in the peritoneal macrophages. HS-23 also inhibited various toll-like receptor agonists-induced nitric oxide (NO) production, and down-regulated LPS-induced expression of NF-κB/AP-1-target inflammatory genes in the cells. Taken together, HS-23 or CGA isomers exhibited anti-inflammatory therapy against LPS-induced septic mortality in mice, at least in part, mediated through the inhibition of IRAK-4.

Effect of water-soluble fraction of cherry tomatoes on the adhesion of probiotics and Salmonella to intestinal epithelial cells.

BACKGROUND: Tomato is one of the most consumed vegetables in the world and contains many valuable nutritional components. Here we investigate the prebiotic effects of cherry tomatoes for improving gut health. RESULTS: Water-soluble dietary fiber was prepared from fresh and processed (heat treatment at 80 °C for 15 min) cherry tomato samples, each with and without Viscozyme L treatment. In the adhesion assays, all water-soluble dietary fiber samples improved adhesion of probiotics (Lactobacillus rhamnosus and Bifidobacterium bifidum) to intestinal epithelial cells (Caco-2 cells). Heat treatment in the preparation of juice from cherry tomatoes showed no significant effect on the adhesion of probiotics to Caco-2 cells. The oligofructose content of samples affected the intestinal adhesion of probiotic bacteria, with higher oligosaccharide concentrations associated with greater adhesion of probiotics and more inhibition of the adhesion of pathogens to Caco-2 cells. CONCLUSION: The present results suggest that cherry tomato can act as a prebiotic, with oligofructose potentially being one of its major prebiotic components.

Evaluation of the antibacterial activity of rhapontigenin produced from rhapontin by biotransformation against Propionibacterium acnes.

Biotransformation is often used to improve chemical activity. We evaluated the antimicrobial activity of rhapontigenin, converted from rhapontin after treatment with Pectinex. Rhapontigenin showed 4-16 times higher antimicrobial activity than rhapontin. Activity was higher against Gram positive strains than Gram negative strains. Minimum inhibitory concentrations (MICs) of rhapontigenin, retinol, and five antibiotics were determined by microbroth dilution method for antibiotic-sensitive and -resistant Propionibacterium acnes. We also investigated the in vitro antibacterial activity of rhapontigenin in combination with antibiotic against antibiotic-resistant P. acnes. The antibiotic combination effect against resistant P. acnes was studied by checkerboard method. The combination formulations (rhapontigenin and clindamycin, retinol and clindamycin) showed synergic effects on the inhibition of the growth of clindamycin-resistant P. acnes. It is predictable that the combination of antibiotics with rhapontigenin is helpful to treat acne caused by antibiotic resistant P. acnes. The antibacterial activity of rhapontigenin was enhanced by biotransformation.

Obovatols, new chitin synthase 2 inhibitors of Saccharomyces cerevisiae from Magnolia obovata.

In the course of the search for inhibitors of ScCHS2 from natural sources, we have isolated a new type of chitin synthase 2 inhibitor, obovatol, which has a biphenol skeleton, from Magnolia obovata. Obovatol inhibited chitin synthase 2 activity of Saccharomyces cerevisiae with an IC(50) of 38 microM. Its derivative, tetrahydroobovatol, inhibited chitin synthase 2 activity under the same conditions with an IC(50) of 59 microM. These compounds exhibited no inhibitory activity for ScCHS3, and showed less inhibitory activity for chitin synthase 1 than for chitin synthase 2 (IC(50) > 1 mM). These results indicated that obovatol and tetrahydroobovatol are specific inhibitors of ScCHS2. They also inhibited CaCHS1, which is structurally and functionally analogous to ScCHS2, with similar IC(50)s to ScCHS2 (IC(50) 28 and 51 microM, respectively). The compounds exhibited mixed competitive inhibition with respect to UDP-N-acetyl-D-glucosamine as substrate [inhibition constant (K(i)) 21.8 microM for obovatol and 23.1 microM for tetrahydroobovatol]. Furthermore, they showed antifungal activities against various pathogenic fungi, with a particularly strong inhibitory activity against Cryptococcus neoformans (MIC 7.8 mg/L). The results indicate that obovatol and tetrahydroobovatol can potentially serve as antifungal agents.