Kim, Seung-Hyun;Lee, Chang-Hoon;Lee, Jin-Moo;Cho, Jung-Hoon;Jang, Jun-Bock;Lee, Kyung-Sub
The Journal of Korean Obstetrics and Gynecology
/
v.22
no.1
/
pp.1-14
/
2009
Purpose: Oxidative stress was thought to play a critical role in neurodegenerative disease. Many in vivo and in vitro reports explained the possible pathway of human aging. But in therapeutic aspects, there was no clear answers to prevent aging associated with neural diseases. In this study, we investigated the antioxidant and neuroprotective effects of the Insamyangyung-tang (IYT). Methods: To estimate the antioxidant effects, we carried out 1.1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, 2,2'-azinobis-(3- ethylbenzothiazoline-6- sulfonic acid (ABTS) radical cation decolorization assay, and measurement of total polyphenolic content. To evaluate neuroprotective effect of IYT in vitro. We performed thiazolyl blue tetrazolium bromide (MTT) assay, reactive oxygen species (ROS) creation in SH-SY5Y. Tyrosine hydroxylase (TH) immunocytochemistry, nitric oxide (NO) assay, and TNF-${\alpha}$ assay in primary rat mesencephalic dopaminergic neurons. Results: The $IC_{50}$ values were $571.6{\mu}g/m{\ell}$ and $202.3{\mu}g/m{\ell}$ in DPPH and ABTS assay respectively. Total polyphenolic content was 1.05%. In SH-SY5Y culture, IYT significantly increased the decreased cell viability by 6-OHDA at the concentrations of $10{\mu}g/m{\ell}$ in pre-treatment group, $10-100{\mu}g/m{\ell}$ in post-treatment group, and $100{\mu}g/m{\ell}$ in co-treatment group. The production of ROS induced by 6-OHDA was significantly inhibited in IYT treated group. In mesencephalic dopaminergic cell culture, the IYT group reduced the dopaminergic cell loss against 6-OHDA toxicity and the production of No and TNF-${\alpha}$ at the concentration of $0.2{\mu}g/m{\ell}$. Conclusion: These results showed that IYT has antioxidant and neuroprotectctive effects in the dopaminergic cells through decreasing the production of ROS, NO and TNF-${\alpha}$ which can cause many neurodegenerative changes in brain cell.
Transmembrane protein TMEM16A, which encodes calcium-activated chloride channel has been implicated in tumorigenesis. Overexpression of TMEM16A is associated with poor prognosis and low overall survival in multiple cancers including lung adenocarcinoma, making it a promising biomarker and therapeutic target. In this study, three structure-related sesquiterpene lactones (mecheliolide, costunolide and dehydrocostus lactone) were extracted from the traditional Chinese medicine Aucklandiae Radix and identified as novel TMEM16A inhibitors with comparable inhibitory effects. Their effects on the proliferation and migration of lung adenocarcinoma cells were examined. Whole-cell patch clamp experiments showed that these sesquiterpene lactones potently inhibited recombinant TMEM16A currents in a concentration-dependent manner. The half-maximal concentration (IC50) values for three tested sesquiterpene lactones were 29.9 ± 1.1 µM, 19.7 ± 0.4 µM, and 24.5 ± 2.1 µM, while the maximal effect (Emax) values were 100.0% ± 2.8%, 85.8% ± 0.9%, and 88.3% ± 4.6%, respectively. These sesquiterpene lactones also significantly inhibited the endogenous TMEM16A currents and proliferation, and migration of LA795 lung cancer cells. These results demonstrate that mecheliolide, costunolide and dehydrocostus lactone are novel TMEM16A inhibitors and potential candidates for lung adenocarcinoma therapy.
Sun Lee;Seong-Ho Jo;Ji-Hyun An;Seong-man Jeong;Dong-Shin Kim;Sang Suk Kim;Suk Man Park;Su Hyun Yun;Seung-Gab Han;Hyun-Jin Kim
Food Science and Preservation
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v.30
no.2
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pp.235-246
/
2023
Yellowball (Citrus hybrid cv. Yellowball ) is a new citrus hybrid between Haruka (C. tamurana × natsudaidai ) and Kiyomi (C. unshiu × sinensis) and is known to possess strong antioxidant activity. However, detailed information on the antioxidant components of its peel has not yet been reported. This study evaluated the antioxidant activity of the peel and identified the antioxidant components by fractionating a methanolic extract of Yellowball peels using liquid-liquid extraction with n-hexane, ethyl ether (ether), ethyl acetate (EA), butanol, and water. The phenolic contents and antioxidant activities of the n-hexane, ether, and EA fractions were higher than those of the other fractions, and these fractions were further separated by semi-preparative high-performance liquid chromatography (HPLC). Four antioxidant peaks, EA1, EA2, EA3, and He1, were isolated and analyzed using ultra-performance liquid chromatography-quadrupole-time- of-flight mass spectrometry (UPLC-Q-TOF MS). Sinapoyl glucoside and hesperidin were identified in EA2 and EA3, respectively, and a polymethoxylated flavone (PMF) complex (5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone, natsudaidain, tetrameth- oxyflavone, and tangeretin) was identified in He1. A compound in EA1 with m/z 223.0246 [M-H] could not be identified and was named unknown2. The antioxidant activity of unknown2 (IC50=69.17 ㎍/mL) was similar to that of Trolox, which was noted as a major antioxidant in Yellowball peel. Further studies on the antioxidant capacity of Yellowball peel are required; however, these results provide a foundation for using Yellowball peel as an antioxidant.
Bo Min Kang;Dongbum Kim;Jinsoo Kim;Kyeongbin Baek;Sangkyu Park;Ha-Eun Shin;Myeong-Heon Lee;Minyoung Kim;Suyeon Kim;Younghee Lee;Hyung-Joo Kwon
Biomolecules & Therapeutics
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v.32
no.4
/
pp.481-491
/
2024
Paxlovid is the first approved oral treatment for coronavirus disease 2019 and includes nirmatrelvir, a protease inhibitor targeting the main protease (Mpro) of SARS-CoV-2, as one of the key components. While some specific mutations emerged in Mpro were revealed to significantly reduce viral susceptibility to nirmatrelvir in vitro, there is no report regarding resistance to nirmatrelvir in patients and animal models for SARS-CoV-2 infection yet. We recently developed xenograft tumors derived from Calu-3 cells in immunodeficient mice and demonstrated extended replication of SARS-CoV-2 in the tumors. In this study, we investigated the effect of nirmatrelvir administration on SARS-CoV-2 replication. Treatment with nirmatrelvir after virus infection significantly reduced the replication of the parental SARS-CoV-2 and SARS-CoV-2 Omicron at 5 days post-infection (dpi). However, the virus titers were completely recovered at the time points of 15 and 30 dpi. The virus genomes in the tumors at 30 dpi were analyzed to investigate whether nirmatrelvir-resistant mutant viruses had emerged during the extended replication of SARS-CoV-2. Various mutations in several genes including ORF1ab, ORF3a, ORF7a, ORF7b, ORF8, and N occurred in the SARS-CoV-2 genome; however, no mutations were induced in the Mpro sequence by a single round of nirmatrelvir treatment, and none were observed even after two rounds of treatment. The parental SARS-CoV-2 and its sublineage isolates showed similar IC50 values of nirmatrelvir in Vero E6 cells. Therefore, it is probable that inducing viral resistance to nirmatrelvir in vivo is challenging differently from in vitro passage.
Park, Jin Ju;Yang, Hye Jeong;Han, Kyu-Jai;Lim, Jeong-Ho
Food Science and Preservation
/
v.22
no.2
/
pp.232-240
/
2015
This study investigated the microbiological and nutritional characteristics of bimonthly radish sprouts purchased at a local market. The total bacteria and coliform measurements were highest in summer (June and August) and lowest in winter (February and December). The total phenol content was $16.82{\pm}0.69GAEmg/g$, and it did not significantly differ during the investigation period. The total carotenoid contents were highest in February (about $12.81{\pm}0.49$${\beta}$-carotene mg/g) and lowest in April (about $8.09{\pm}1.01$${\beta}$-carotene mg/g). However although total glucosinolates content differ between the total crude glucosinolate and the sum of the individual glucosinolates, it was highest in December. The individual glucosinolates were found to have been gucoraphenin, glucoerucin, glucobrassicin and gluconasturtiin in radish sprouts via HPLC analysis. The purchasing time of the glucoraphenin content did not significantly differ. The measured glucoerucin was highest in February and lowest in October. The gucobrassicin and gluconasturtiin were higher in summer than in winter, but did not significantly differ. The antioxidant activity (i.e., the $IC_{50}$ values of the DPPH radical scavenging) was highest in February. In conclusion, the microbial contamination, total carotenoids, and antioxidant activity changed according to the purchasing season, but the total phenolic compounds and total glucosinolates were maintained regardless of the time in the radish sprouts.
Choi, Kyeong-Hee;Oh, Hyun Jeong;Jeong, Young Jae;Lim, Eun Jeong;Han, Jin Soo;Kim, Ji Hyun;Kim, Oh Young;Lee, Hyun-Sun
Journal of the Korean Society of Food Science and Nutrition
/
v.44
no.8
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pp.1165-1171
/
2015
In this study, we examined the effects of cultivation adaptability and product quality of aronia (fruit of Aronia melanocarpa) cultivated in various domestic regions. Extracts of aronia cultivated in various domestic regions and Poland were measured for their total sugar contents, acidities, total polyphenol contents, anthocyanin contents, and antioxidant activities using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) assays. Our results showed that aronia extracts from the two countries had similar sugar contents, acidities, and anthocyanin contents. Anthocyanin is an important functional component of Aronia melanocarpa. Extracts of aronia from the two countries contained cyanidin-3-galactoside (65.5~69.1%) as the major anthocyanin compound. Aronia cultivated in C region showed higher polyphenol content (121.5%) than Poland aronia and we measured of antioxidant activities by DPPH ($IC_{50}$) and FRAP assay. Aronia cultivated in C region showed the highest antioxidant activity and polyphenol contents. Cultivation conditions of C region had sufficient sunshine and soil with pH of 6.5. From the above results, Korean aronia had similar activities with Poland aronia, which suggests that it can be a new potential development source and high technological foods.
Potentilla supina (Rosaceae) has traditionally been used to treat disorders of hemostasis, dysentery, malaria, bloody discharge and arthritis, and it has antinociceptive and anti-inflammatory properties. However, validity of the anti-inflammatory activity has not been scientifically investigated so far. Therefore, the aim of this study was to investigate the anti-inflammatory potential of P. supina using the ethanolic extract of P. supina and its sub-fractions. To evaluate the anti-inflammatory effects of P. supina, we examined the inflammatory mediators such as nitric oxide (NO), inducible nitric oxide synthase (iNOS) and prostaglandin $E_2$ ($PGE_2$) in RAW 264.7 cells. Our results indicated that ethyl acetate fraction significantly inhibited LPS-induced NO, iNOS and $PGE_2$ production in RAW 264.7 cells. This result showed that ethyl acetate fraction of P. supina is expected to be a good candidate for development into a source of anti-inflammatory agents.
Chloride($Cl^-$) channels play critical roles in cell homeostasis and its specific functions such as volume regulation, differentiation, secretion, and membrane stabilization. The presence of these channels have been reported in all kinds of cells and even in frog oocytes. These essential role of $Cl^-$ channels in cell homeostasis possibly play any role in egg homeostasis and in the early stage of development, however, there has been no report about the presence of $Cl^-$ channel in the mammalian oocyte. This study was performed to elucidate the presence of $Cl^-$ channels in hamster eggs. When allowing only $Cl^-$ to pass through the channel of the egg membrane by using impermeant cation such as N-methyl-D-glucamine(NMDG), single channel currents were recorded. These channel currents showed typical long-lasted openings interrupted by rapid flickering. Mean open $time({\tau}o)$ was 43${\pm}$10.14 ms(n=9, at 50 mV). The open probability(Po) was decrease with depolarization. The current-voltage relation showed outward rectification. Outward slop conductance(32${\pm}$5.4 pS, n=22) was steeper than the inward slop conductance(10${\pm}$1.3 pS). Under the condition of symmetrical 140 mM NaCl, single channel currents were reversed at 0 mV(n=4). This reversal potential(Erev) was shifted from 0 mV at 140 mM concentration of internal NaCl(140 mM [Na+]i) to 9.8${\pm}$0.5 mV(n=4) at 70 mM [Na+]i and 11.5${\pm}$1.9 mV at 280 mM [Na+]i(n=4) respectively, strongly suggesting that these are single $Cl^-$ channel currents. To examine further whether this channel has pharmacological property of the $Cl^-$ channel, specific Cl channel blockers, IAA-94(Indanyloxyacetic acid-94) and DIDS(4, 4'-diisothiocyan ostillben- 2-2'disulfonic acid) were applied. IAA-94 inhibited the channel current in a dose-dependent manner and revealed a rapid and flickering block. From these electrophysiological and pharmacological resluts, we found the novel $Cl^-$ channel present in the hamster oocyte membrane. The first identification of $Cl^-$ channel in the hamster oocyte may give a clue for the further study on the function of $Cl^-$ channel in the fertilization and cell differentiation.
Journal of the Korean Society of Food Science and Nutrition
/
v.40
no.10
/
pp.1353-1360
/
2011
This study was performed to investigate the antimicrobial effects against food-borne pathogens and antioxidant activity of Rhododendron brachycarpum ethanol-extract. The antimicrobial activity of the extract was determined using a paper disc-diffusion method, and the diameter of the clear zone was measured. The diameter of the clear zone in the presence of 10 mg of extract was maximal against Bacillus cereus among the three tested Gram-positive bacteria and against Escherichia coli O157:H7 among the five tested Gram-negative bacteria. Analysis of the minimum inhibitory concentration (MIC) showed that the extract exhibited a similar efficacy as that of sorbic acid, a well-known chemical preservative. The growth inhibitory effects of the extract at concentrations of 250, 500, 1,000, and 2,000 mg/L on food-borne pathogens were determined against Staphylococcus aureus, Listeria monocytogenes, Salmonella Typhimurium, and Escherichia coli O157:H7. Growth of the microorganisms was not affected by the extract at concentrations up to 250 mg/L, but it was significantly (p<0.05) inhibited by the extract at concentrations higher than 1,000 mg/L. The antioxidant effects of the extract were examined via measurement of DPPH radical scavenging activity, inhibition of reactive oxygen species (ROS) generation using fluorescent dichlorofluorescien (DCF) assay, and prevention of peroxyl radical- and hydroxyl radical-induced supercoiled DNA breakage. The $IC_{50}$ of the extract for DPPH radical scavenging activity was about half that of ${\alpha}$-tocopherol, which was used as a positive control. DCF fluorescence intensity decreased as the concentration of the extract increased, demonstrating that ROS generation was inhibited in a concentration-dependent manner. The ROS inhibitory effect of the extract was higher than that of ascorbic acid. The extract prevented supercoiled DNA strand breakage induced by peroxyl radical and hydroxyl radical. Thus, the results of the present study demonstrate that the extract exhibits antimicrobial effects against food-borne pathogens as well as potent antioxidant capacity, suggesting that R. brachycarpum could be used as a natural antibacterial agent and effective antioxidant in food.
The objective of this study is to investigate the physical and chemical properties for environmental assessment of water system affected by acid mine drainage (AMD) from coal mining activities in the Youngwol, Jungseon and Pyungchang areas in Korea. During November 2000 to July 2002, 6 times of water samples were collected season-ally from acid mine drainage and nearby streams at 13 coal mines in the study area. The physical and chemical properties including pH, Eh, TDS, salinity, bicarbonates and DO were measured in the field. Eighteen cations includ-ing Al, Ca, Fe, Mg, Mn and Zn, and 6 anions including nitrates and sulfates were also analyzed by ICP-AES and If, respectively. Acid water from the Jungam coal mine has typical characteristics of AMD with very low pH(3∼4) and high TDS(1,000∼5,000 mg/1). Relatively high concentrations(mg/kg) of heavy meals, especially for Al(380), Fe(80), Mn(44) and Zn(8), were found in water samples from the Jungam coal mine area. Water samples from the Seojin, Sebang and Sungjin coal mines also contained over 50 mg/l of Al, >100 mg/1 of Fe and )10 mg/1 of Mn. In addition to anioins, over 1,000 mg/l of sulfate was found in several water samples. Seasonally, the concentrations of metals and sulfates varied; wet season samples were relatively higher in metals and sulfates than dry season samples. It is needed to establish the proper remediation and environmental monitoring of the AMD continuously.
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