• Title/Summary/Keyword: ${\alpha}-D-glucopyranoside$

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Comparison of on Rat Intestinal Digestive Enzyme Inhibitory Activity and Antioxidant Enzyme Activity of Korean and Chinese Schizandra chinensis

  • Chae Hee-Jun;Hwang Hyun-Ik;Lee In-Soon;Moon Hae-Yeon
    • Biomedical Science Letters
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    • v.11 no.4
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    • pp.517-523
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    • 2005
  • The purpose of this study was to determine the effect of rat intestinal a-glucosidase inhibitor; methanol $(80\%)$, ethanol $(80\%)$ and water extract of Schizandra chinensis in Korea (KS: Schizandra chinensis in Korea) and China (CS: Schizandra chinensis in China). When the final concentration was 1 mg/ml for each sample (KS and CS), methanol extract of KS ($IC_{50}$ 1.62 mg/ml) showed $46.8\%$, ethanol extract of KS ($IC_{50}$ 1.48 mg/ml) showed $47.4\%$, water extract of KS ($IC_{50}$ 1.72 mg/ml) showed $46.3\%$ and methanol extract of CS ($IC_{50}$ 8.35 mg/ml) showed $13.3\%$, ethanol extract of CS ($IC_{50}$ 8.05 mg/lml) showed $16\%$, water extract of CS ($IC_{50}$ 8.37 mg/ml) showed $11.54\%$ of inhibitor for p-nitrophenyl $\alpha-D-glucopyranoside$ (pNPG) $\alpha-glcosidase$ activity, respectively. And the contents of total phenol, flavonoid of Schizandra chinensis were measured. When the final concentration was 1mg/ml for each sample (KS and CS), total phenol and flavonoid in KS were higher than CS, respectively. The order superoxide dismutase (SOD) activity $IC_{50}$ values of each solvent extracts of KS were: 2.006 mg/ml methanol extract, 2.304 mg/ml ethanol extract and 2.5 mg/ml water extract, which were higher than that of each solvent extracts CS as: 2.881 mg/ml methanol extract, 3.085 mg/ml ethanol extract and 3.190 mg/ml water extract.

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Antioxidant Constituents from the Leaves of Cedrela sinensis A. Juss

  • Lee, Ik-Soo;Wei, Chun-Hua;Thoung, Phuong Thien;Song, Kyung-Sik;Seong, Yeon-Hee;Bae, Ki-Hwan
    • Korean Journal of Medicinal Crop Science
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    • v.14 no.5
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    • pp.267-272
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    • 2006
  • Phytochemical study on the EtOAc fraction from the MeOH extract of the leaves of Cedrela sinensis led to the isolation of five known phenolic compounds (1-5), whose structures were identified as (+)-catechin (1), $kaempferol-3-0-{\alpha}- L-rhamnopyranoside$ (2), quercetin (3), $quercetin-3-O-{\alpha}-L-rhamnopyranoside$ (4), and $quercetin-3-O-{\beta}-D-glucopyranoside$ (5), respectively, by comparing their spectral $(uv,\;JR,\;IH\;and\;^{13}C-NMR,\;and\;ESI-MS)$ and physicochemical data with those reported in the literature. Among the isolated compounds (1-5), compounds 1 and 3-5 exhibited significant DPPH radical scavenging effects with $IC{_50}$ values ranging from $21.3{\pm}1.4\;to\;38.1{\pm}3.2 {\mu}M$ as well as superoxide anion radical scavenging effects with $IC{_50}$ values ranging from $9.4{\pm}0.7\;to\;21.2{\pm}3.6 {\mu}M$. Furthermore, compounds 1 and 3-5 also exhibited considerable inhibitory effects on LDL peroxidation induced by either $CU^{2+}$ or AAPH with $IC{_50}$ values ranging from $1.4{\pm}0.4\;to\;11.9{\pm}1.4\;{\mu}M$. These results indicated that flavonoids are the major constituents of C. sinensis and considered to be antioxidant principles of this plant.

Antioxidant Activity of the Extractives from the Needles of Picea abies Karsten (독일가문비(Picea abies Karsten) 잎 추출성분의 항산화 활성)

  • Lee, Sang-Keug;Bae, Young-Soo
    • Journal of Korean Society of Forest Science
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    • v.95 no.4
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    • pp.429-434
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    • 2006
  • The dried needles (1.5 kg) of Picea abies Karsten were ground, extracted with acetone-$H_2O$ (7:3, v/v), concentrated, and fractionated with a series of n-hexane, methylene chloride, ethyl acetate and water on a separatory funnel. Each fraction was freeze dried, then a portion of ethyl acetate soluble powder was chromatographed on a Sephadex LH-20 column using a series of aqueous methanol and ethanol-n-hexane mixture as eluents. The isolated compounds were identified by cellulose TLC, $^1H$-, $^{13}C$-NMR, FAB and EI-MS. (+)-catechin (compound I), (-)-epicatechin (compound II), kaempferol-3-O-${\beta}$-D-glucopyranoside (compound III), 4-hydroxyacetophenone (compound IV) were isolated from the ethyl acetate soluble fraction and (+)-catechin (compound I), protocatechuic acid (compound V) were isolated from the $H_2O$ soluble fraction of P. abies needle. The antioxidative activities of each fraction and the isolated compounds were tested by DPPH radical scavenging method, and EtOAc soluble fraction, (+)-catechin and (-)-epicatechin showed similar values to ${\alpha}$-tocopherol and BHT as controls.

Effects of high glucose concentration on IGF-I binding and glucose transporters in renal proximal tubule cells (신장 근위세뇨관세포에서 고포도당이 IGF-I 결합과 포도당운반계에 미치는 영향)

  • Han, Ho-jae;Park, Kwon-moo;Son, Chang-ho;Yoon, Yong-dal
    • Korean Journal of Veterinary Research
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    • v.37 no.2
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    • pp.301-310
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    • 1997
  • Diabetes mellitus is associated with a wide range of pathophysiological in the kidney. This study was designed to examine the effects of high glucose concentration on IGF-I binding and glucose transporters in renal proximal tubule cells. The results were as follows : The binding of $^{125}I-IGF-I$ reached the peak at the 30 minutes and gradually decreased by the time dependent manner. The binding of $^{125}I-IGF-I$ was inhibited by the unlabelled IGF-I($10^{-14}{\sim}10^{-8}M$) in a concentration dependent manner. The relative affinity of IGF-I receptor for IGF-I, IGF-II and insulin exhibited typical type 1 binding(IGF-I > insulin > IGF-II). However IGF-II did not compete for the cultured cell membrane $^{125}I-IGF-I$ binding site at $10^{-14}{\sim}10^{-8}M$. Under optimal conditions, IGF-I binding to the membranes from 5mM and 20mM glucose treated cells was analyzed. It was found that 20mM glucose treated cells exhibited higher binding activity for IGF-I. In order to further substantiate this increase in IGF-I binding sites, we performed affinity-labelling studies. The cross-linked cell membrane subjected to SDS-PAGE; labelled material was detected by autoradiography. 20mM glucose treated cells exhibited higher levels. The initial rate of $methyl-{\alpha}-D-glucopyranoside({\alpha}-MG)$ uptake was significantly lower($74.41{\pm}6.71%$) in monolayers treated with 20mM glucose than those of 5mM glucose. However, 3-O-methyl-D-glucose(3-O-MG) uptake was not affected by glucose concentration in culture media. IGF-I significantly increased ${\alpha}-MG$ uptake in both 5mM and 20mM glucose treated cells. However, 3-O-MG uptake was not affected by IGF-I in both conditions. In conclusion, 20mM glucose increased binding sites of $^{125}I-IGF-I$, inhibited Na/glucose cotransporter activity. But 20mM glucose did not change facilitated glucose transporter.

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Development of Quality Control Method for a Novel Herbal Medicine, HPL-1 using UHPLC (UHPLC를 이용한 새로운 한약제제 HPL-1의 품질관리법 개발)

  • Kim, Se-Gun;Lamichhane, Ramakanta;Lee, Kyung-Hee;Jung, Hyun-Ju
    • The Korea Journal of Herbology
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    • v.30 no.3
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    • pp.19-24
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    • 2015
  • Objectives : HPL-1, a novel herbal medicine which is composed of five herbs such as Kalopanacis Cortex, Chaenomelis Fructus, Raphani Semen, Atractylodis Rhizoma and Pulvis Aconiti Tuberis Purificatum, was developed for treatment of osteoarthritis. This study is aimed to develop analytical method for consistent quality control of HPL-1 and validate chromatographic method. Methods : Chromatographic analysis was performed using ultra-high performance liquid chromatography - diode array detector (UHPLC-DAD) equipped with RP-amide column, column oven, and auto sampler. Marker compounds [protocatechuic acid, chlorogenic acid, liriodendrin, 3,5-dicaffeoylquinic acid, ${\beta}$-D-(3-O-sinapoyl)-fructofuranosyl-$\alpha$-D-(6-O-sinapoyl)glucopyranoside and benzoylmesaconine] were separated by step gradient elution of acetonitrile and 0.1% phosphoric acid/water. The method validation was evaluated by quantitative validation parameters of linearity, accuracy, precision, limit of detection (LOD) and limit of quantification (LOQ) according to KFDA guideline.Results : An optimized method for six marker compounds in HPL-1 was established by UHPLC-DAD. The correlation coefficient (R2) with each calibration curve was greater than 0.99. The LOD and LOQ were within the range of 0.008-0.090 and $0.023-0.274{\mu}g/mL$, respectively. The relative standard deviation (RSD) of intra- and inter-day variability were less than 4.0%. The result of recovery test was range from 93.3-106.3% with RSD < 4.0%.Conclusions : These results suggest that the quantitative UHPLC method is precise, accurate, effective for quality evaluation of HPL-1. The method may also contribute to improve quality of crude drug preparations used for treatment of various diseases.

Isolation and Structural Determination of Free Radical Scavenging Compounds from Korean Fermented Red Pepper Paste (Kochujang)

  • Chung, Jin-Ho;Shin, Heung-Chule;Cho, Jeong-Yong;Kang, Seong-Koo;Lee, Hyoung-Jae;Shin, Soo-Cheol;Park, Keun-Hyung;Moon, Jae-Hak
    • Food Science and Biotechnology
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    • v.18 no.2
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    • pp.463-470
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    • 2009
  • Sixteen antioxidative active compounds isolated from the EtOAc layer of MeOH extracts of kochujang, Korean fermented red pepper paste, were structurally elucidated as fumaric acid, methyl succinate, succinic acid furan-2-yl ester methyl ester (gochujangate, a novel compound), 2-hydroxy-3-phenylpropanoic acid, 3,4-dihydroxybenzoic acid, 2,3-dihydroxybenzoic acid, 2,4-dihydroxybenzoic acid, 6,7-dihydroxy-2H-chromen-2-one (esculetin), caffeic acid, cis-p-coumaric acid, trans-p-coumaric acid, daidzin, genistin, apigenin 7-O-$\beta$-D-apiofuranosyl($1{\rightarrow}2$)-$\beta$-D-glucopyranoside, apigenin 7-O-$\beta$-Dglucopyranoside, and quercetin 3-O-$\alpha$-L-rhamnopyranoside by mass spectrometry (MS) and nuclear magnetic resonance (NMR) experiments. These compounds were analyzed for the first time as antioxidants from kochujang.

Biological Activities and Bioactive Compounds in the Extract of Acer tegmentosum Maxim. Stem (산겨릅나무 줄기추출물의 생리활성 및 유효성분 분리)

  • Hong, Bo-Kyong;Eom, Seok-Hyun;Lee, Chan-Ok;Lee, Ji-Won;Jeong, Jong-Hyun;Kim, Jae-Kwang;Cho, Dong-Ha;Yu, Chang-Yeon;Kwon, Yong-Soo;Kim, Myong-Jo
    • Korean Journal of Medicinal Crop Science
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    • v.15 no.4
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    • pp.296-303
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    • 2007
  • Acer tegmentosum (Acereaceae) has been used a source of traditional medicines for the treatment of hepatic disorders in Korea. This research was conducted to determine biofunctional activities of A. tegmentosum stem extract and to identify its bioactive components. Methanolic extract from A. tegmentosum stem was partitioned by using organic solvents, including n-hexane, ethyl acetate, n-butanol, and water. Two compounds were isolated by using an ODS column chromatography from ethyl acetate soluble fraction shown to the strongest antioxidant activity ($RC_{50}=3.15\;{\mu}g/m{\ell}$) among the fractions. The isolated compounds were analyzed by $^1H$ and $^{13}C$ NMR, IR, UV/VIS, MS spectrum data and identified as catechin, ${\rho}-Hydroxyphenethyl$ alcohol $1-O-{\beta}-_D-(6'-O-galloyl)-glucopyranoside$. The compounds have shown strong antioxidant activity, with similar activity to BHA ($RC_{50}=2\;{\mu}g/m{\ell}$). Especially, ${\rho}-Hydroxyphenethyl$ alcohol 1-O-{\beta}-_D-(6'-O-galloyl)-glucopyranoside$ was shown strong anti-lipid peroxidative activity. However, the compounds were not shown antimicrobial activities. In antimicrobial activity assays, ethyl acetate soluble fraction was effective to bacterial inhibition, such as Escherichia coli and Klebsiella pneumonia, with minimum inhibitory concentrations in $125\;{\mu}g/m{\ell}$. Otherwise, antifungal activity against Candida albicans was shown in n-hexane soluble fraction exhibiting $63\;{\mu}g/m{\ell}$ of minimum inhibitory concentration. In anticomplementary activity assays, water soluble fraction was the most effective exhibiting 24% inhibitory activity.

Neuroprotective effects of antioxidant constituents isolated from Opuntia ficus-indica var. saboten Makino

  • K.J. Jung;Lee, E.H.;Kim, H.J.;Lee, J.Y.;Y.S. Song;Lee, Y.H.;J. Cho;Park, M.;Park, H.
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.63-63
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    • 2003
  • Opuntia ficus-indicavar. saboten Makino (Cactaceae) is a tropical or subtropical plant that has been widely used as folk medicine for the treatment of diabetes, asthma, burn, edema and gastritis. The purposes of the present study were to identify antioxidant constituents from fruits and stems of the plant cultivated in Cheju island, Korea, and examine their in vitro neuroprotective activities. Using a chromatographic fractionation method, ten chemical constituents were isolated from ethyl acetate extracts. By means of chemical and spectroscopic methods, those were identified as eight flavonoids such as kaempherol (a), quercetin (b), kaempferol 3-methyl ether (c), quercetin 3-methyl ether (d), narcissin (e), dihydrokaernpferol (f), dihydroquercetin (g) and erioclictyol (h), and two terpenoids such as 3-oxo-${\alpha}$-ionol-${\beta}$-d-glucopyranoside (i) and roseoside (j). Among the isolated compounds, comrounds c~e and h~j were those reported for the first titre from the plant. Compounds b, d and g showed DPPH free radical scavenging activities with IC$\sub$50/ values of 28, 19 and 31, ${\mu}$M respectively. Compounds d and g also inhibited iron-dependent lipid peroxidation with IC$\sub$50/ values of 2.4 and 3.5 ${\mu}$M. In a primary rat cortical neuronal cell culture system, compounds b, d and g inhibited xanthine/xanthine oxidase-induced (IC$\sub$50/ values of 18.2, 2.1 and 54.6 ${\mu}$M) and H$_2$O$_2$-induced (IC$\sub$50/ values of 13.6, 1.9 and 25.7 ${\mu}$M) cytotoxicities. In addition, compounds d and g inhibited NMDA-induced excitotoxicity by 21 and 33%, and only compound d inhibited growth factor withdrawal-induced apoptosis by 31% at a tested concentration of 3 ${\mu}$M. The results suggest that the antioxidant constituents with in vitroneuroprotective activities may serve as lead chemicals for the development of neuroprotective agent.

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Studies on Biological Activity of Wood Extractives(VII) - Antimicrobial and Antioxidation Activities of Extractives from the Heartwood of Prunus sargentii - (수목추출물의 생리활성에 관한 연구(VII) - 산벚나무 심재 추출성분의 항균 및 항산화활성 -)

  • Lee, Sung-Suk;Lee, Hak-Ju;Choi, Don-Ha
    • Journal of the Korean Wood Science and Technology
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    • v.29 no.2
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    • pp.140-145
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    • 2001
  • Antimicrobial and antioxidative activities on heartwood extractives of domestic species were investigated to develop a natural fungicide or preservative. Six flavanones including pinostrobin, eriodictyol, naringenin, pinocembrin, taxifolin and verecundin were isolated from Prunus sargentii which has been selected due to its high antimicrobial and antioxidative activities among the tested species. According to the results of antifungal test, pinocembrin was evaluated as the highest antifungal compound among the test compounds, which showed 80% of hyphal growth inhibition rate. Antifungal activity of pinocembrin was similar to hinokitiol(${\beta}$-thujaplicin), strong antimicrobial compound isolated from Thujopsis dolabrata. Naringenin followed pinocembrin in its antifungal activity. However, verecundin did not show any antifungal activity. No compound was effective in antibacterial activities. As a result of the measurement of free radical scavenging activity, antioxidative activities of taxifolin and eriodictyol were 2 times that of ${\alpha}$-tocopherol, and antioxidative index of these compounds were even superior to that of ${\alpha}$-tocopherol. In this regard, it could inferred that high antifungal and antioxidative activities of extractives of P. sargentii were derived from pinocembrin, taxifolin and eriodictyol, respectively.

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Effect of Cisplatin on Sodium-Dependent Hexose Transport in LLC-$PK_1$ Renal Epithelial Cells

  • Lee, Suk-Kyu;Kim, Jee-Yeun;Yu, Tai-Hyun;Kim, Kyoung-Ryong;Kim, Kwang-Hyuk;Park, Yang-Saeng
    • The Korean Journal of Physiology and Pharmacology
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    • v.1 no.1
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    • pp.35-43
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    • 1997
  • Cis-dichlorodiammine platin${\mu}M$II (Cisplatin), an effective chemotherapeutic agent, induces acute renal failure by unknown mechanisms. To investigate direct toxic effects of cisplatin on the renal proximal tubular transport system, LLC-$PK_1$ cell line was selected as a cell model and the sugar transport activity was evaluated during a course of cisplatin treatment. Cells grown to confluence were treated with cisplatin for 60 min, washed, and then incubated for up to 5 days. At appropriate intervals, cells were tested for sugar transport activity using ${\alpha}-methyl-D-[^{14}C]glucopyranoside$ (AMG) as a model substrate. In cells treated with 100 ${\mu}M$ cisplatin, the AMG uptake was progressively impaired after 3 days. The viability of cells was not substantially changed with cisplatin of less than 100 ${\mu}M$, but it decreased markedly with 150 and 200 ${\mu}M$. In cisplatin-treated cells, the $Na^+$ -dependent AMG uptake was drastically inhibited with no change in the $Na^+$ -independent uptake. Kinetic analysis indicated that Vmax was suppressed, but Km was not altered. The $Na^+$ -dependent phlorizin binding was also decreased in cisplatin-treated cells. However, the AMG efflux from preloaded cells was not apparently retarded by cisplatin treatment. These data indicate that the cisplatin treatment impairs $Na^+$ -hexose cotransporters in LLC-$PK_1$ cells and suggest strongly that defects in transporter function at the luminal plasma membrane of the proximal tubular cells constitute an important pathogenic mechanism of cisplatin nephrotoxicity.

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