Risk assessment traditionally are conducted on individual chemicals; however, humans are exposed to multiple chemicals in daily life. The organophosphorus (OP) pesticides are considered in a single risk assessment because they act by a common mechanism of toxicity, and there is likely to be expose to multiple OP pesticides simultaneously or sequentially. The OP pesticides act by inhibiting the enzyme acetylcholinesterasc (AChE) and have available extensive database. AChE is widely distributed throughout the body, most importantly in the nervous system. Inhibition of AChE results in accumulation of acetylcholine in the nervous system that results in clinical signs of cholinergic toxicity, including increased salivation and lacrimation, nausea and vomiting, muscle fasciculation, lethargy and fatigue, among others. To conduct an exposure assessment for pesticides in the diet, we need to know the food consumption patterns of the populations, and the pesticide residue levels in the foods that are consumed. This study was conducted to identify cumulative dietary risk due to multiple OP pesticides that can be exposed through various foods. Total 22 food samples including cereals, vegetables and fruits were collected randomly two times from food markets in several sites (4 cities). The subjected foods were selected by regarding of highly consumed foods to general Korean people. The 12 OP pesticides including Acephate, Azinphos-methyl, Chlorpyrifos, and Diazinon were monitored. For the exposure assessment, general adult group of 60 kg body weight was regarded as target population and food consumption data suggested by Lee et al. (2000) were used as consumed value of individual food. Analyses of samples for OP pesticides have been carried out according to the multiclass multiresidue analysis method and acephate and methamidophos analysis method of Korea Food Code. In general the levels of OP pesticides found in the food samples were very low or not detected.
This study investigated anti-obesity and antioxidant effects of dietary non-fermented soybean crud residue (SCR) and fermented SCR by Monascus pilosus (FSCR) in high-fat induced-obese mice. SCR and FSCR were supplemented with high-fat diet at 2% (wt/wt) dose for 8 weeks. Both SCR and FSCR significantly lowered body weight, epididymal fat weight and weight gain rate compared to high-fat diet control (HC) group and FSCR group showed lowest weight gain rate. In addition, it was observed that serum and hepatic lipid profiles including triglyceride, total cholesterol, LDL-cholesterol and HDL-cholesterol were significantly improved by supplementing SCR or FSCR. Furthermore, SCR and FSCR administration showed increase of glutathione content and decrease of hepatic lipid peroxide content, serum aminotransferase activity, and hepatic xanthine oxidase activity. On the other hand, activities of reactive oxygen species scavenging enzyme such as superoxide dismutase, glutathione S-transferase and glutathione peroxidase in two test groups were higher than those of HC. Lastly, in comparison with SCR, FSCR was more effective in restoring obesity-related biomarkers to normal level in high-diet induced obese mice. In conclusion, the present study indicates that FSCR could have not only anti-obese effects such as inhibition of abdominal fat accumulation, but also protective effects of cardiovascular disease such as atherosclerosis by decreasing serum and hepatic lipid contents. Furthermore, these results suggest that experimental diets in this study could alleviate hepatic damage caused by overproduction of reactive oxygen spices (ROS) due to obesity via inhibition of ROS generating activities and induction of ROS scavenging activities.
To develop an effective anti-hangover product, hot-water extracts of 25 medicinal herbs were screened for inhibition or activation of alcohol dehydrogenase(ADH) and acetaldehyde dehydrogenase(ALDH), and 12 herbs were selected for further study. Chosen medicinal herb extracts(CMHEs) were fermented by Lactobacillus delbruechii subspecies lactis for 10 days at $35^{\circ}C$ after saccharification with nuruk(malt inoculated by 5 types of microbs) for 72 hours at $35^{\circ}C$ and both CMHEs and fermented CMHEs(FCMHEs) were explored for anti-hangover effects in vitro. We found significant ADH inhibition by hot-water extracts of Pueraria thunbergiana, Hovenia dulcis Thunb, Lycium chinense, Glycyrrhiza uralensis, Acanthopanax sessiliflorus, Liriope platyphylla, and Ixeris dentata, and significant ALDH activation by extracts of Acanthopanax sessiliflorus, Lycium chinense, Ixeris dentata, and Polypori umbellati of the Polyporaceae. The ADH effects on CMHE and FCMHE were -20.22% and -62.63% of control values, and the ALDH effects 173.20% and 280.17%, respectively. In rats given 20%(v/v) alcohol(15 mL/kg), FCMHEs significantly decreased blood acetaldehyde concentrations on 3 hours after ethanol administration, in a dose-dependent manner(p<0.05). Notably, blood acetaldehyde concentrations were markedly reduced in animals given FCMHEs(400 mg/kg) compared to levels seen in rats receiving CADB(commercial alcohol detoxification beverage). Thus, anti-hangover effects were promoted by fermentation of certain medicinal herb extracts.
Lee, Eun Kyeong;Kim, Ju Hyun;Moon, Kyoung Mi;Ha, Sugyeong;Noh, Sang-Gyun;Kim, Dae Hyun;Lee, Bonggi;Kim, Do Hyun;Kim, Su Jeong;Ullah, Sultan;Moon, Hyung Ryong;Chung, Hae Young
Journal of Life Science
/
v.27
no.2
/
pp.139-148
/
2017
The inhibition of tyrosinase, a key enzyme in mammalian melanin synthesis, plays an important role in preventing skin pigmentation and melanoma. Therefore, tyrosinase inhibitors are very important in the fields of medicine and cosmetics. However, only a few tyrosinase inhibitors are currently available because of their toxic effects on skin or lack of selectivity and stability. Therefore, we synthesized a novel series of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one derivatives and evaluated their inhibitory effects on mushroom tyrosinase, with the aim of discovering a novel tyrosinase inhibitor. Among 19 derivatives, MHY3655 ($IC_{50}=0.1456{\mu}M$) showed the strongest inhibitory effect on tyrosinase activity compared to kojic acid ($IC_{50}=17.2{\mu}M$), a well-known tyrosinase inhibitor. In addition, MHY3655 showed competitive inhibition on Lineweaver-Burk plots. We confirmed that MHY3655 strongly interacts with mushroom tyrosinase residues through the docking simulation. Substitutions with a hydroxy group at both R2 and R4 in the phenyl ring indicated that these groups play a major role in the high binding affinity to tyrosinase. Further, MHY3655 did not show cytotoxicity at the concentrations tested in B16F10 melanoma cells. In conclusion, the novel compound MHY3655 potentially shows tyrosinase inhibitory activity, and it could be used as an ingredient in whitening cosmetics.
This study was carried out to investigate the physiological activities of the ethanol extract from Gymnopilus spectabilis mycelium (EGM) and of the supernatant obtained from fermentation broth (SGB). The contents of polysaccharides, phenol compounds and total ${\beta}-glucans$ of EGM were found to be 80.14%, 3.5 mg/ml and 5.91%, respectively and those for SGB were 78.68%, 3.32 mg/ml and 3.28%, respectively. Both EGM and SGB exhibited dose-dependent nitrate-scavenging abilities at pH 1.2. In addition, both EGM and SGB on the autoxidation rate of the linoleic acid demonstrated powerful antioxidant activities at 1 mg/ml level. With respect to fibrolytic activity, EGM showed 1,180 unit/g, which was the same activity as streptokinase, while SGB was 1,011 unit/g. The angiotensin converting enzyme inhibition activity of EMG determined by both the normal and pretreatment methods were estimated to be 8.2% and 10.2%, respectively. However, SGB showed no corresponding activity. The growth inhibitory effects of EGM on AGS, A549, HeLa and NCTC cells were over 58.88%, respectively. And the growth inhibitory effects of the SGB on HeLa and NCTC cells were 44.92 and 76.76%, respectively. Also, EGM and SGB activated the components of the alternative complement pathway from 51 and 62% at the concentration of 100 mg/ml, The xanthine oxidase inhibition activities of EGM and SGB (1 mg/ml) were 9.53 and 16.92%, respectively.
Sambucus sieboldiana var. miquelii (Nakai) Hara is distributed in Korea, China, and Japan, and has been used as an anti-rheumatic in folk medicine in oriental countries. The present study aims to investigate the potential use of this species in health functional foods, cosmetics, and food preservatives. Methanol extracts of leaves and branches from this plant were prepared to quantitatively analyze the total phenol and flavonoid contents, and to investigate the antioxidative and enzyme inhibitory activities, and the inhibition of nitric oxide (NO) production activity. The results showed that the total polyphenol and flavonoid contents of the crude extract were 1.52±0.1 mg/g and 1.73±0.1 mg/g, respectively. S. sieboldiana polyphenols exhibited potent scavenging activity shown by 2, 2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and 2, 2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation assay. The crude extract also exhibited significant α-glucosidase and tyrosinase inhibitory activity with IC50 values of 183.5 ㎍/ml and 323.9 ㎍/ ml, respectively. Additionally, the crude extract exhibited strong anti-inflammatory activity determined through the nitric oxide inhibition assay in a dose-dependent manner with an IC50 value of 36.7 ㎍/ml and no cytotoxic effect on the macrophages. Therefore, we demonstrated that the leaves and branches of S. sieboldiana extract possess antioxidant, anti-diabetic, depigmentation potential, and NO production inhibitory activities. According to recent research, S. sieboldiana has great potential as a source of the bioactive compound which could be used as food, cosmetics, and pharmaceutical agents.
In this study, three GRAS (generally recognized as safety) strain was isolated from Doenjang and Cheonggukjang and identified as a protease-producing microorganism, following the appearance of a clear zone around its colony when cultured on a medium containing skim milk. Based on an analysis of the nucleotide sequence of 16S ribosomal RNA, the strains wereas identified as Bacillus amyloliquefaciens and wereas therefore named Bacillus amyloliquefaciens CDD5, Bacillus amyloliquefaciens CPD4, and Bacillus amyloliquefaciens CGD3. Here, we analyzed the protease and ${\alpha}$-glucosidase inhibitory activities of the three B. amyloliquefaciens strains. Among the isolated strains, B. amyloliquefaciens CGD3 exhibited the highest protease activity (9.21 U/mL, 24 hr). The protease activities of B. amyloliquefaciens CDD5 and B. amyloliquefaciens CPD4 reached 1.14 U/mL and 8.02 U/mL, respectively, at 48 hr. The proteases from the three B. amyloliquefaciens strains showed the highest activities within a pH range of 8.0-9.0 at $50^{\circ}C$, and casein was found to be the preferred substrate on evaluating enzyme activity in the substrate specificity assay. The B. amyloliquefaciens strains exhibited maximal growth when the nutrient broth medium had an initial pH within the range of 5.0-10.0, 6-9% sodium chloride (NaCl), and 5% glucose. B. amyloliquefaciens CDD5 exhibited a low ${\alpha}$-glucosidase inhibition rate (5.32%), whereas B. amyloliquefaciens CPD4 and B. amyloliquefaciens CGD3 exhibited relatively higher inhibition rates of 96.89% and 97.55%, respectively.
Kim, Myung-Uk;Lee, Eun-Ho;Jung, Hee-Young;Lee, Seung-Yeol;Cho, Young-Je
Journal of Applied Biological Chemistry
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v.62
no.2
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pp.173-179
/
2019
The aim of this study is to investigate the biological activities of Hericium erinaceus. 1,1-Diphenyl-2-picrylhydrazyl radical scavenging activity of H. erinaceus extract was higher than positive control. The inhibitory activities of xanthin oxidase, ${\alpha}$-glucosidase, and hyaluronidase was measured as functional food activity, and inhibitory activities on collagenase, tyrosinase, and astringent effect as beauty food activity in water and ethanol extracts from H. erinaceus. In functional food activity, xanthin oxidase inhibitory activities at $50-200{\mu}g/mL$ phenolic concentration in ethanol extracts from H. erinaceus showed inhibitory activity in dose dependent manner. ${\alpha}$-Glucosidase inhibitory activities at $50{\mu}g/mL$ phenolic concentration showed high activity of higher than 80%. Inhibitory activities on hyaluronidase as anti-inflammation factor showed inhibition effect in dose dependent manner both in water and ethanol extracts. In beauty food activity, Inhibitory activities on collagenase at $200{\mu}g/mL$ phenolic concentration in water and ethanol extracts showed high activity to 65.09 and 58.38% dose dependently. Tyrosinase inhibitory activity in water extract showed 9.4-58.24%. Astringent activity as pore shrink effect in ethanol extracts also showed a very high activity of 18.94-100%. Antimicrobial activity on pathogenic bacteria was highly effective on Staphylococcus aureus, Salmonella enteritidis, Vibrio parahaemolyticus and Escherichia coli at 2.5 mg/mL or above. Therefore, the extracts from H. erinaceus can be used as a functional food and beauty food resources and natural antimicrobial agent on pathogenic bacteria in food.
Min Ji Kim;Si Eun Park;Geun soo Lee;Jin Hwa Kim;Sunwoo Kwon;Hyung Seo Hwang
Journal of Applied Biological Chemistry
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v.66
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pp.204-212
/
2023
Whitening is inhibitory activity of the melanin synthesis of melanocytes. Recently, whitening materials have been developed on natural materials because of its side effects on skin. Figs (Ficus Carica L.) is a fruit belonging to the Moraceae family and whitening activity was reported in focusing on the fig's stem and leaf components, but whitening activity of the figs fruit was not known. Thus, in this study, we tried to observe its anti-melanogenesis as well as antioxidant and anti-inflammation. The radical scavenging activity of figs fruits extract (FFE) was observed as the level of 34.52±1.98%/60.71±1.26% compared to the control in the its maximum concentration in the DPPH/ABTS assay. Cytotoxicity of FFE was observed at 10% concentration by CCK8 assay, so the maximum concentration was set at 5% and applied to all experiments. FFE concentration dependently decreased NO production associated with inducible nitric oxide synthase, cyclooxygenase-2, interleukin-6 and tumor necrosis factor-α gene expression, these strongly suggesting anti-inflammatory activity. In melanin contents assay, FFE significantly down-regulated melanin production in α-MSH-stimulated B16F10 cell as well as tyrosinase inhibition in vitro. In addition, FFE decreased the Microphthalmia-associated transcription factor (MITF) mRNA expression about 94.34% compared to the α-MSH treatment group in RT-PCR. Finally, FFE significantly reduced the MITF, cAMP response element-binding protein and tyrosinase protein expression in the α-MSH stimulated B16F10 cell. Through these results, we found that FFE can not only directly inhibit tyrosinase enzyme activity but also suppress melanogenesis through regulation of MITF gene expression in α-MSH signal transduction.
Journal of the korean academy of Pediatric Dentistry
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v.26
no.2
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pp.399-415
/
1999
From bacteria to mammalian cells, one of the most important mediators of intracellular signal transduction mechanisms which regulate a variety of intracellular processes is free calcium. In salivary acinar cells, elevation of intracellular calcium concentration ($[Ca^{2+}]_i$) is essential for the salivary secretion induced by parasympathetic stimulation. However, in addition to $[Ca^{2+}]_i$, gap junctions which couple individual cells electrically and chemically have also been reported to regulate enzyme secretion in pancreatic acinar cells. Since the plasma membrane of salivary acinar cells has a high density of gap junctions, and these cells are electrically and chemically coupled with each other, gap junctions may modulate the secretory function of salivary glands. In this respect, I planned to investigate the role of gap junctions in the modulation of salivary secretion and $[Ca^{2+}]_i$, using mandibular salivary glands of rats. In order to measure the salivary flow rate, fluid was collected from the cannulated duct of the isolated perfused rat mandibular glands at 2 min intervals. $[Ca^{2+}]_i$, was measured from the cells loaded with fura-2 by spectrofluorometry. The results obtained were as follows: 1. CCh-induced salivary secretion was reversibly inhibited by 1 mM octanol, a gap junction blocker. 2. CCh-induced increase in $[Ca^{2+}]_i$, was also reversed by the application of 1 mM octanol. 3. Octanol did not block the initial increase in $[Ca^{2+}]_i$ caused by CCh, which suggested that the reduction of $[Ca^{2+}]_i$, caused by gap junction blockade was not resulted from the inhibition of $Ca^{2+}$ release from intracellular $Ca^{2+}$ stores. 4. Addition of octanol during stimulation with $1{\mu}M$ thapsigargin, a potent microsomal ATPase inhibitor, reduced $[Ca^{2+}]_i$, to the basal level. This suggested that inhibition of gap junction permeability closed plasma membrane $Ca^{2+}$ channels. 5. 2,5-di-tert-butyl-1,4-benzohydroquinone (TBQ) generated $[Ca^{2+}]_i$ oscillations resulting from periodic influx of $Ca^{2+}$ via plasma membrane. The TBQ-induced $[Ca^{2+}]_i$ oscillations were stopped by the application of 1mM octanol which implicated that gap junctions modulate the permeability of plasma membrane $Ca^{2+}$ channels. 6. Glycyrrhetinic acid, another well known gap junction blocker, also inhibited CCh-induced salivary secretion from rat mandibular glands. These results suggested that gap junctions play an important role in the modulation of fluid secretion from the rat mandibular glands and this was probably due to the inhibition of $Ca^{2+}$ influx through the plasma membrane $Ca^{2+}$ channels.
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