Enhanced anti-wrinkle activity of adlay bran fermented with Lactobacillus brevis MJM60390.

OBJECTIVES: The aim of this study was to screen the lactic acid bacteria for fermentation of adlay bran and evaluate the anti-wrinkle effect of fermented and non-fermented adlay bran. METHODS: Adlay bran was fermented with candidate LAB and extracted with 70% ethanol. The extracts from LAB-fermented adlay bran and non-fermented adlay bran were evaluated for the anti-wrinkle effects by measuring the hyaluronan, collagen, and elastin production in cells using ELISA kit. The molecular anti-wrinkle mechanism was investigated by RT-qPCR. Furthermore, the antioxidant activity, total phenolic and flavonoid content were also determined. RESULTS: Among the tested LAB, Lactobacillus brevis MJM60390 was selected for the highest glycosidase activity. Both extracts from adlay bran (NFAB) and L. brevis MJM60390-fermented adlay bran (LBFAB) showed anti-wrinkle effect, and LBFAB showed higher activity. Compared with control, hyaluronan production was increased by 24.73% and 59.38%, collagen production was increased by -13.08% and 34.19%, and the elastin production was increased by 29.78% and 53.73% by NFAB and LBFAB treatment, respectively. Investigation on the mRNA expression showed that LBFAB upregulated the expression of Has 2 and Has 3 and downregulate HYAL1 and HYAL2. LBFAB also upregulated the mRNA expression of COL1A1, COL1A2, ELN and inhibited the expression of collagenase and elastase. However, not all of these genes were regulated by NFAB. Furthermore, the antioxidant activity was significantly increased after fermentation, and the content of the phenolic and flavonoid compounds also increased in the LBFAB. CONCLUSIONS: In this study, we demonstrated that fermentation of adlay bran with L. brevis MJM60390 enhanced the anti-wrinkle activity through increasing the hyaluronan synthesis in keratinocytes and improving collagen and elastin production in dermal fibroblasts.

The additive memory and healthspan enhancement effects by the combined treatment of mature silkworm powders and Korean angelica extracts.

ETHNOPHARMACOLOGICAL RELEVANCE: Silkworm (Bombyx mori) and Korean angelica (KoAg; Angelica gigas Nakai) have been widely used as traditional oriental medicines in Korea, China, and Japan to treat various diseases such as anemia, cold, diabetes, palsy, stroke, etc. Steamed and freeze-dried mature silkworm powder, also known as HongJam (HJ), and extracts of KoAg root (KoAgE) are currently sold in Korea as functional foods to improve memory, cognition, and liver functions. However, the molecular and pharmacological basis for the improvement of brain functions of HJ and KoAgE has not yet been elucidated. AIM OF STUDY: This study aimed to elucidate the molecular basis underlying the memory-enhancing effects of HJ and KoAgE and determine whether administration of HJ and KoAgE complexes (HJ+KoAgC) has additive memory and healthspan-enhancing effects. MATERIALS AND METHODS: The MCI mouse models generated by intraperitoneal injection of Scopolamine (Sco-IP) were orally administered with HJ and KoAgE alone or as complexes. Their memory-enhancing effects were examined on spatial, fear-aggravated, and social memories and compared with control or Donepezil (Dp) treatment. The activities of mitochondria complex (MitoCom) I-IV and acetylcholinesterase (AChE) and the amounts of ATP in the mouse brains were examined. The Drosophila model was used to investigate lifespan- and healthspan-promoting effects of HJ+KoAgC. RESULTS: Administration of HJ+KoAgC produced more memory-enhancing effects than administration of HJ or KoAgE alone or Dp. The increase in MitoCom I-IV activities and ATP amounts and the decrease in AChE activities in the mouse brains were the molecular basis for the memory enhancement. The greatest improvement in memory and mitochondrial function was observed when the mice were administered the 1:0.8 ratio of HJ+KoAgC. Administration of HJ+KoAgC to Drosophila prolonged the lifespan and the healthspan and increased the amounts of ATP. CONCLUSION: HJ+KoAgC had superior effects on memory improvement and healthspan extension by increasing mitochondrial activities and ATP amounts in treated animal models.

Synergistic Neuroprotective Effects of Mature Silkworm and Angelica gigas Against Scopolamine-Induced Mild Cognitive Impairment in Mice and H2O2-Induced Cell Death in HT22 Mouse Hippocampal Neuronal Cells.

We previously reported that mature Bombyx mori silkworm (SW) ameliorated scopolamine (Sco)-induced amnesia, and Angelica gigas (AG) prevented cognitive impairment. SW is known for its gastroprotective effects such as improving liver function and alleviating the effects of Parkinson's disease. AG is known for its neuroprotective effects and for lowering the effects of low-density lipoprotein cholesterol. However, the neuroprotective effect of combined SW and AG (SWA-1) treatment and the underlying molecular mechanism by which SWA-1 regulates neurodegenerative diseases remains unclear. We evaluated the neuroprotective effect of SWA-1 against Sco-induced mild cognitive impairment in mice and H2O2-induced cell death in HT22 mouse hippocampal neuronal cells and elucidated the underlying molecular mechanism. Morris water maze and Y-maze tests were performed to examine the learning and memory abilities of mice. The underlying molecular mechanism was investigated by using western blotting. We demonstrated that SWA-1 significantly protects against H2O2-induced cell death in HT22 mouse hippocampal neuronal cells. SWA-1 also significantly reversed Sco-induced spatial learning and memory impairment. Specifically, SWA-1 upregulates the protein levels of phosphorylated extracellular signal-related kinase (Erk1/2) and phosphorylated p38 MAP kinase (p38). SWA-1 remarkably decreased the apoptotic index Bax/Bcl2 expression in the hippocampus of Sco-treated mice. Our results suggest that SWA-1 may be administered as alternative therapy for cognitive impairment and neurodegenerative diseases and should be studied further in human trials.

Effect of ACG-1, an Extract Blend of Angelica gigas, Cynanchum wilfordii, and Ginkgo biloba, on Blood Circulation Improvement Via Antiplatelet Aggregation and Antihyperlipidemia.

Thrombosis causes poor blood circulation, which may lead to several cardiovascular disorders. Antiplatelet aggregation and antihyperlipidemia are the key processes that improve blood circulation. The antiplatelet aggregation and antihyperlipidemic effects of ACG-1, a mixture of Angelica gigas, Cynanchum wilfordii, and Ginkgo biloba extracts, were investigated in this study. The antiplatelet aggregation activity of ACG-1 was determined by studying its effects on collagen-induced platelet aggregation in human platelet-rich plasma (PRP). In addition, the effects of ACG-1 were investigated in a thromboembolism mouse model. The high-fat diet (HFD)-fed mouse model was used to investigate the antihyperlipidemic effects of ACG-1 and western blotting assay was performed to elucidate its mechanism of action. It was observed that ACG-1 significantly inhibited platelet aggregation in human PRP. Furthermore, ACG-1 showed protective effects in a thromboembolism mouse model induced by administering a mixed collagen and epinephrine intravenous injection. Oral administration of ACG-1 also significantly ameliorated blood lipid profiles in the HFD-fed mouse model. In conclusion, ACG-1 should be considered a powerful functional food to improve blood circulation.

Ixeris dentata and Lactobacillus gasseri Extracts Improve Salivary Secretion Capability in Diabetes-Associated Dry Mouth Rat Model.

Dry mouth, hyposalivation, or xerostomia is a significant problem in diabetic patients; however, there has been no way to relieve these symptoms. This study's aim was to evaluate the effects of Ixeris dentata (IXD) in combination with lactobacillus extract on the salivation rate in diabetes-induced dry mouth, and its mechanism was also investigated. In the streptozotocin (STZ)-induced diabetes model, the dry mouth condition was established as a model. Here, rats were treated with water or IXD through the sublingual spray, and subsequently treated with or without a spray of lactobacillus extract. In diabetes condition, the salivary flow rate, amylase activity, and aquaporin-5 and Na+/H+ exchanger (NHE-1) expressions were markedly decreased, whereas they were more significantly recovered in the sequential treatment of IXD-lactobacillus extract than in each single treatment. Furthermore, oxidative stress and its related ER stress response were especially regulated in the IXD/lactobacillus extract condition, where the following anti-oxidative enzymes, glutathione assay (GSH: GSSG) ratio, superoxide dismutase (SOD), and glutathione peroxidase (GPx), were involved. This study suggests that the combination of IXD and lactobacillus would be a potential alternative medicine against diabetes-induced hyposalivation and xerostomia.

Strategies in anti-Mycobacterium tuberculosis drug discovery based on phenotypic screening.

The rise of multi- and extensively drug-resistant Mycobacterium tuberculosis (M. tb) strains and co-infection with human immunodeficiency virus has escalated the need for new anti-M. tb drugs. Numerous challenges associated with the M. tb, in particular slow growth and pathogenicity level 3, discouraged use of this organism in past primary screening efforts. From current knowledge of the physiology and drug susceptibility of mycobacteria in general and M. tb specifically, it can be assumed that many potentially useful drug leads were missed by failing to screen directly against this pathogen. This review discusses recent high-throughput phenotypic screening strategies for anti-M. tb drug discovery. Emphasis is placed on prioritization of hits, including their extensive biological and chemical profiling, as well as the development status of promising drug candidates discovered with phenotypic screening.

Preventive effects of a novel herbal mixture on atopic dermatitis-like skin lesions in BALB/C mice.

BACKGROUND: A combination of parts of Cornus officinalis, Rosa multiflora, Lespedeza bicolor, Platycladus orientalis, and Castanea crenata is commonly used for alleviating inflammatory skin disorders. Therefore, this study was carried out to evaluate the in vitro and in vivo preventive effects of a novel herbal formula made from the five plants (C2RLP) against atopic dermatitis in BALB/C mice. METHODS: Mice were allocated into five groups (n = 8) including, control (Normal, petrolatum, and betamethasone treated) and treatment groups (treated with 2.5 and 5% C2RLP ointment). Atopic lesion was induced by applying 1-Chloro-2, 4-dinitrobenzene to the dorsal thoracic area of mice. Macroscopical and histological evaluations were performed to determine the effects of treatment on the progress of the skin lesions. The effects of treatment on the production and release of interleukins, interferon -ϒ, nitrite, prostaglandin E2, thymus and activation-receptor chemokine, and ß-hexosaminidase were evaluated and comparisons were made between groups. In addition, the chemical compounds present in C2RLP were identified by Liquid Chromatography-Mass Spectrometry. RESULTS: Topical application of C2RLP reduced the dermatitis score and suppressed histopathological changes in mice. Treatment significantly reduced (P < 0.05) plasma IL-4 level, the production of nitrite, prostaglandin E2, and thymus and activation-receptor chemokine production. The lipopolysaccharide-induced iNOS-mRNA expression in RAW 264.7 cells was also suppressed by high concentrations of C2RLP. In addition, C2RLP showed an inhibitory effect against DPPH free radical (IC50 = 147.5 µg/ml) and ß-hexosaminidase release (IC50 = 179.5 µg/ml). Liquid Chromatography-Mass Spectrometry analysis revealed the presence of various compounds, including loganin, ellagic acid, and kaempferol 3-glucoside. CONCLUSION: Down-regulation of T- helper 2 cellular responses and suppression of inflammatory mediators contributed to the protective effects of C2RLP from atopic dermatitis in BALB/C mice.

Evaluating the Memory Enhancing Effects of Angelica gigas in Mouse Models of Mild Cognitive Impairments.

(1) Background: By 2050, it is estimated that 130 million people will be diagnosed with dementia, and currently approved medicines only slow the progression. So preventive intervention is important to treat dementia. Mild cognitive impairment is a condition characterized by some deterioration in cognitive function and increased risk of progressing to dementia. Therefore, the treatment of mild cognitive impairment (MCI) is a possible way to prevent dementia. Angelica gigas reduces neuroinflammation, improves circulation, and inhibits cholinesterase, which can be effective in the prevention of Alzheimer's disease and vascular dementia and the progression of mild cognitive impairment. (2) Methods: Angelica gigas (AG) extract 1 mg/kg was administered to mildly cognitive impaired mice, models based on mild traumatic brain injury and chronic mild stress. Then, spatial, working, and object recognition and fear memory were measured. (3) Result: Angelica gigas improved spatial learning, working memory, and suppressed fear memory in the mild traumatic brain injury model. It also improved spatial learning and suppressed cued fear memory in the chronic mild stress model animals. (4) Conclusions: Angelica gigas can improve cognitive symptoms in mild cognitive impairment model mice.

Woohwangcheongsimwon Prevents High-Fat Diet-Induced Memory Deficits and Induces SIRT1 in Mice.

Woohwangcheongsimwon (WHC) is a mixture of herbal medicines that is widely prescribed in Korean traditional medicine. SIRT1 is known for its regulatory roles in energy metabolism, oxidative stress, and circadian rhythms. This study was designed to determine whether WHC can increase and mimic the biological reactions of SIRT1 activation. Ten-month-old male mice were divided into four groups: nontreated normal diet (ND), nontreated high-fat diet (HFD), WHC-treated ND, and WHC-treated HFD. Body weight and cognitive functions were evaluated after treatment. The hippocampal expressions of SIRT1 and PGC-1α were also measured. The components of WHC were identified by liquid chromatography. High-fat diet-fed mice gained more weight and demonstrated greater deficits in short-term and long-term cognitive functions. WHC suppressed the deleterious effects of a HFD on weight gain and cognitive decline, but showed no prominent effects on animals fed NDs. The herbal treatment also increased the expression of SIRT1 and PGC-1α in the hippocampus. Despite the induction of hippocampal SIRT1 expression by WHC, resveratrol was not present among the natural compounds identified. This expression might have contributed to the suppression of high-fat diet-induced memory deficits in mice treated with the herbal mixture.

A new in vitro hemagglutinin inhibitor screening system based on a single-vesicle fusion assay.

Hemagglutinin (HA) from the influenza virus plays a pivotal role in the infection of host mammalian cells and is, therefore, a druggable target, similar to neuraminidase. However, research involving the influenza virus must be conducted in facilities certified at or above Biosafety Level 2 because of the potential threat of the contagiousness of this virus. To develop a new HA inhibitor screening system without intact influenza virus, we conceived a single-vesicle fusion assay using full-length recombinant HA. In this study, we first showed that full-length recombinant HA can mediate membrane fusion in ensemble and single-vesicle fusion assays. The fluorescence resonance energy transfer (FRET) frequency pattern of single-vesicle complexes completely differed when the inhibitors targeted the HA1 or HA2 domain of HA. This result indicates that analysing the FRET patterns in this assay can provide information regarding the domains of HA inhibited by compounds and compounds' inhibitory activities. Therefore, our results suggest that the assay developed here is a promising tool for the discovery of anti-influenza virus drug candidates as a new in vitro inhibitor screening system against HA from the influenza virus.

Microbial bioconversion and processing methods enhance the phenolic acid and flavonoids and the radical scavenging capacity of Smilax china L. leaf.

BACKGROUND: It has been reported that Smilax china L. leaf (SCL) provided various biological functions owing to polyphenols. The objective of the current study was to assess the enhancing effect of processing methods and microbial conversions on phenolic acid and flavonoid content and radical scavenging capacity of SCL for potential applications of diverse food products. RESULTS: Targeted phenolic acid (chlorogenic acid) and flavonoids (piceid and quercetin) were identified in fresh SCL using liquid chromatography-mass spectrometry. The total amount of identified phenolic acid and flavonoids was highest in steamed SCL (12.70 ± 0.12 mg g(-1) on a dry matter basis, dmb). A substantial amount of chlorogenic acid (5.81 ± 0.16 mg g(-1) dmb), piceid (3.96 ± 0.04 mg g(-1) dmb) and quercetin (6.06 ± 0.12 mg g(-1) dmb) were quantified in SCL fermented by Bacillus species, roasted and steamed, respectively (P < 0.05). The oxygen radical absorbance capacity (ORAC) value was greater in microbial fermented SCL than in others, with the exception of Saccharomyces cerevisiae and Aspergillus oryzae. However, vitamin C equivalent antioxidant capacity (VCEAC) was highest in SCL fermented by Aspergillus oryzae. CONCLUSION: Results from our study suggest that the microbial fermentation processing method could improve accessibility to extraction of phenolic acids and flavonoid content and radical scavenging capacity.

Modulation of quorum sensing-controlled virulence factors by Nymphaea tetragona (water lily) extract.

ETHNOPHARMACOLOGICAL RELEVANCE: Nymphaea tetragona is a widely distributed ornamental species with ethnomedicinal uses in the treatment of diarrhea, dysentery, eruptive fevers, and infections. The anti-infectious activities of this herb have already been assessed to clarify its traditional use as a medicine. AIM OF STUDY: In this study, we aimed to verify the inhibitory effects of N. tetragona 50% methanol extract (NTME) on quorum sensing (QS)-controlled virulence factors of bacteria since QS and its virulence factors are novel targets for antimicrobial therapy. MATERIALS AND METHODS: The antibacterial activity of this extract was evaluated against Chromobacterium violaceum and Pseudomonas aeruginosa. The inhibition of the violacein pigment of C. violaceum by NTME was determined qualitative and quantitative using standard methods. The effects of NTME on swarming motility, biofilm viability, pyocyanin production, and LasA protease activity were evaluated using P. aeruginosa. Finally, the in vitro and in vivo cytotoxicity of NTME were verified by MTT assay and oral administration to rats, respectively. RESULTS: The extract had concentration-dependent antibacterial activity against gram-negative bacteria. NTME at 1/2× minimum inhibitory concentration (MIC), 1× MIC and 2× MIC significantly lowered the levels of violacein of C. violaceum compared to that of the control. The swarming motility of P. aeruginosa was inhibited by ≥70% by treatment with 1/2× MIC of NTME. There were remarkable reductions in pyocyanin production and LasA protease activity in the overnight culture supernatant of P. aeruginosa supplemented with NTME when compared with that of the untreated control. The confocal micrographs of 24h biofilms of P. aeruginosa exposed to NTME exhibited a lower number of live cells than the control. No toxic effect was observed in in vitro and in vivo cytotoxicity assays of NTME. CONCLUSIONS: NTME was demonstrated to have significant concentration-dependent inhibitory effects on quorum sensing-mediated virulence factors of bacteria with non-toxic properties, and could thus be a prospective quorum sensing inhibitor.

In vitro probiotic characterization of Lactobacillus strains from fermented radish and their anti-adherence activity against enteric pathogens.

In this study, we evaluated the probiotic properties of Lactobacillus plantarum, Lactobacillus pentosus, and Lactobacillus fermentum strains isolated from fermented radish. All the strains survived the simulated oro-gastrointestinal transit condition and showed significantly higher adherence to Caco-2 cells compared with the probiotic strain Lactobacillus rhamnosus GG. The strains showed broad-spectrum antimicrobial activity, autoaggregation, and coaggregation capacity with pathogens. Furthermore, the Lactobacillus strains inhibited the adherence of Yersinia enterocolitica subsp. enterocolitica, Shigella boydii, and Salmonella choleraesuis to the Caco-2 cell line. The strains possessed bile salt hydrolase activity and their cholesterol-lowering activity in vitro was above 50% in the presence of bile. Strains of L. plantarum and L. pentosus possessed the plantaricin-encoding plnEF gene. In addition, the Lactobacillus strains maintained about 80% cell viability after freeze-drying in the presence of a combination of 5% skim milk and 5% maltodextrin as cryoprotectant, and 70% recovery of cell viability was observed in the absence of any cryoprotectant.

A polymethoxy flavonoids-rich Citrus aurantium extract ameliorates ethanol-induced liver injury through modulation of AMPK and Nrf2-related signals in a binge drinking mouse model.

Nobiletin and tangeretin are polymethoxy flavonoids (PMFs), found in rich quantities in the peel of citrus fruits. In the present study, we assessed the biological effect of the PMFs on liver damage using a mouse model of binge drinking. First, we extracted PMFs from the peels of Citrus aurantium to make Citrus aurantium extract (CAE). Male C57BL/6 mice were orally treated with silymarin and CAE (50, 100, and 200 mg/kg) for 3 days prior to ethanol (5 g/kg, total of 3 doses) oral gavage. Liver injury was observed in the ethanol alone group, as evidenced by increases in serum hepatic enzymes and histopathologic alteration, as well as by hepatic oxidative status disruption. CAE improved serum marker and hepatic structure and restored oxidative status by enhancing antioxidant enzyme levels and by reducing lipid peroxidation levels. In addition, CAE evidently suppressed inflammation and apoptosis in the livers of mice administered with ethanol, by 85% (tumor necrosis factor-α) and 44% compared to the control group, respectively. Furthermore, CAE activated lipid metabolism related signals and enhanced phosphorylation of AMP-activated protein kinase (AMPK) and nuclear factor E2-related factor 2 (Nrf2) with several cytoprotective proteins including heme oxygenase-1, NAD(P)H quinone oxidoreductase 1, and γ-glutamylcysteine synthetase. Taken together, the present study demonstrated that, CAE possesses antioxidant, anti-inflammatory, and antiapoptotic activity against ethanol-induced liver injury.

Expression of potato S-adenosyl-L-methionine synthase (SbSAMS) gene altered developmental characteristics and stress responses in transgenic Arabidopsis plants.

S-adenosyl-L-methionine (SAM) synthase (SAMS) catalyze the biosynthesis of SAM, which is a precursor for ethylene and polyamines, and a methyl donor for a number of biomolecules. A full-length cDNA of SAMS from Solanum brevidens was expressed in Arabidopsis thaliana to study its physiological function. RT-PCR analysis showed that SbSAMS expression was enhanced significantly in S. brevidens leaves upon treatment with salt, mannitol, ethephon, IAA and ABA. The transgenic SbSAMS overexpression lines accumulated higher levels S-adenosyl homocysteine (SAHC) and ethylene concomitantly with increased SAM level. Expression levels of genes related to ethylene biosynthesis such as ACC synthase, but not polyamine biosynthesis genes were enhanced in SbSAMS overexpressing Arabidopsis lines. In addition, ABA responsive, wound and pathogen-inducible genes were upregulated in SbSAMS transgenic Arabidopsis plants. Transgenic Arabidopsis lines exhibited higher salt and drought stress tolerance compared to those of vector control. Based on these results we conclude that SbSAMS is expressed under abiotic stress to produce SAM as a broad-spectrum signal molecule to upregulate stress-related genes including ethylene and ABA biosynthetic pathway genes responsible for ABA, pathogen and wound responses.

Soyasaponins Aa and Ab exert an anti-obesity effect in 3T3-L1 adipocytes through downregulation of PPARγ.

Saponins are a diverse group of biologically functional products in plants. Soyasaponins are usually glycosylated, which give rise to a wide diversity of structures and functions. In this study, we investigated the effects and molecular mechanism of soyasaponins Aa and Ab in regulating adipocyte differentiation and expression of adipogenic marker genes in 3T3-L1 adipocytes. Soyasaponins Aa and Ab dose-dependently inhibited the accumulation of lipids and the expression of adiponectin, adipocyte determination and differentiation factor 1/sterol regulatory element binding protein 1c, adipocyte fatty acid-binding protein 2, fatty acid synthase, and resistin in 3T3-L1 adipocytes. In addition, soyasaponins Aa and Ab suppressed the transcriptional activity of peroxisome proliferator-activated receptor γ (PPARγ) in HEK 293T cells. Furthermore, we confirmed that the expression of PPARγ and of CCAAT-enhancer-binding protein α (C/EBPα) was suppressed at both the mRNA and protein levels in 3T3-L1 adipocytes by treatment with soyasaponins Aa and Ab. Taken together, these findings indicate that soyasaponin Aa and Ab markedly inhibit adipocyte differentiation and expression of various adipogenic marker genes through the downregulation of the adipogenesis-related transcription factors PPARγ and C/EBPα in 3T3-L1 adipocytes.

The cyclic peptide ecumicin targeting ClpC1 is active against Mycobacterium tuberculosis in vivo.

Drug-resistant tuberculosis (TB) has lent urgency to finding new drug leads with novel modes of action. A high-throughput screening campaign of >65,000 actinomycete extracts for inhibition of Mycobacterium tuberculosis viability identified ecumicin, a macrocyclic tridecapeptide that exerts potent, selective bactericidal activity against M. tuberculosis in vitro, including nonreplicating cells. Ecumicin retains activity against isolated multiple-drug-resistant (MDR) and extensively drug-resistant (XDR) strains of M. tuberculosis. The subcutaneous administration to mice of ecumicin in a micellar formulation at 20 mg/kg body weight resulted in plasma and lung exposures exceeding the MIC. Complete inhibition of M. tuberculosis growth in the lungs of mice was achieved following 12 doses at 20 or 32 mg/kg. Genome mining of lab-generated, spontaneous ecumicin-resistant M. tuberculosis strains identified the ClpC1 ATPase complex as the putative target, and this was confirmed by a drug affinity response test. ClpC1 functions in protein breakdown with the ClpP1P2 protease complex. Ecumicin markedly enhanced the ATPase activity of wild-type (WT) ClpC1 but prevented activation of proteolysis by ClpC1. Less stimulation was observed with ClpC1 from ecumicin-resistant mutants. Thus, ClpC1 is a valid drug target against M. tuberculosis, and ecumicin may serve as a lead compound for anti-TB drug development.

Ameliorative effects of Monascus pilosus-fermented black soybean (Glycine max L. Merrill) on high-fat diet-induced obesity.

The purpose of this study was to examine the antiobesity effects of Monascus pilosus-fermented black soybean (F-BS) in C57BL/6 mice with high-fat diet (HFD)-induced obesity. F-BS (oral, 0.5 and 1.0 g/kg per body weight, twice per day) ameliorated obesity by reducing body and liver weight increases, and regulating blood glucose and cholesterol levels in C57BL/6 mice fed a control or HFD with oral administration of F-BS for 12 weeks. F-BS suppressed the growth of epididymal, retroperitoneal, and perirenal fat pads by preventing increases in the adipocyte size. Moreover, the levels of blood glucose, total cholesterol, and leptin were significantly lowered by F-BS administration in a dose-dependent manner. These results indicated that F-BS is a beneficial food supplement for preventing obesity, controlling blood glucose, and lowering cholesterol. Future research strategies should address the mechanisms that selectively regulate obesity, including hyperglycemia and hypercholesterolemia.

Synergistic effect and antiquorum sensing activity of Nymphaea tetragona (water lily) extract.

Salmonellosis is a common and widely distributed food borne disease where Salmonella typhimurium is one of the most important etiologic agents. The purpose of this study was to investigate the antimicrobial activity of Nymphaea tetragona alone and in combination with antibiotics against S. typhimurium. It also aimed to assess the plant for quorum sensing inhibition (QSI) activity and to identify the bioactive compounds. The antibacterial activities of the extract were assessed using broth microdilution method. Disk agar diffusion method was employed to determine the QSI and bioactive compounds were identified by GC-MS analysis. Ethyl acetate fraction of N. tetragona extract (EFNTE) demonstrated good antimicrobial activity (MIC 781 µg/mL) against 4 strains out of 5. FIC index ranged from 0.375 to 1.031 between EFNTE/tylosin and 0.515 to 1.250 between EFNTE/streptomycin against S. typhimurium. Among all extracts, EFNTE and butanol fraction more significantly inhibited pigment production of C. violaceum. Polyphenols were identified as major compound of EFNTE and butanol fraction. These results indicate that combination among N. tetragona extract and antibiotics could be useful to combat drug-resistance Salmonella infections and polyphenols are promising new components from N. tetragona that warrant further investigation as a candidate anti-Salmonella agent and quorum sensing inhibitor.

Dichlormethane extract of the jelly ear mushroom Auricularia auricula-judae (higher Basidiomycetes) inhibits tumor cell growth in vitro.

In this study, a dichloromethane fraction (DCMF) from 70% Auricularia auricula-judae ethanol extract showed the highest level of antitumor activity compared to other solvent fractions (ethyl acetate, butanol, and water). The DCMF was found to have more potent antitumor activity against broncheoalveolar cancer (half maximal inhibitory concentration = 57.2 µg/mL) and gastric cancer cells (half maximal inhibitory concentration = 73.2 µg/mL) compared to the other solvent fractions, although all fractions inhibited the proliferation of the tumor cells in a dose-dependent manner. We further analyzed the DCMF composition by gas chromatography-coupled mass spectroscopy. Based on the results of this analysis, an antitumor active component (diazane) was identified in the DCMF. However, we found that diazane alone had a lower level of antitumor activity than the DCMF. These findings indicate that other unknown components of the DCMF also are responsible for the cytotoxic effects of DCMF against tumor cells. Semiquantitative reverse transcription polymerase chain reaction analysis demonstrated that DCMF induced cytotoxicity or tumor cell apoptosis as a result of the downregulation of Bcl-2 expression and p53 overexpression. Taken together, our study results demonstrated that the DCMF may be used as a functional additive for enhancing antioxidant activities and suppressing tumor growth in the body.