• 한국자원식물학회지
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• 제23권6호
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• pp.487-497
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• 2010

ROS have been associated with pathogenic processes including carcinogenesis through direct effect on DNA and play an important role in the pathogenesis of inflammation. Because of many types of phenolic acid derivatives and flavonoids, apples have been one of the human diet since ancient times and are one of the most commonly consumed fruits in worldwide. In this study, catechin, chlorogenic acid and phlorizin dihydrate were purified and identified by HPLC and GC/MS. The contents of catechin, chlorogenic acid and phlorizin dihydrate were 1.01 mg, 7.01 mg and 3.67 mg/ kg wet weight, respectively. Catechin and phlorizin dihydrate were found to significantly inhibit oxidative DNA damage, while chlorogenic did not affect. Also, catechin inhibits NO and $PGE_2$ production via suppressing iNOS and COX-2 expression. However, chlorogenic acid and phlorizin dihydrate did not affect. Our results show that catechin may be the most active phenolic compound in anti-oxidative damage and anti-inflammatory effect.

• Bulletin of the Korean Chemical Society
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• 제6권1호
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• pp.7-11
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• 1985

The crystal structure of phlorizin, a ${\beta}$ -D-glucopyranoside of a flavonoid dihydrochalcone phloretin, has been determined by single crystal diffraction methods using diffractometer data obtained by the ${\omega}-2{\theta}$ scan technique with Cu $K{\alpha}$ radiation from a crystal with space group symmetry $P2_12_12_1$ and unit cell parameters a = 4.9094 (2), b = 19.109 (1), c = 23.275 (4) $\AA$. The structure was solved by direct methods and refined by full-matrix least-squares to a final R = 0.047 for the 1697 observed reflections. The dihydrochalcone moiety is flat and fully extended. The glucose ring has the $^4C_1$ chair conformation and the conformation of the primary alcohol group is gauche-gauche. The crystal packing is dominated by an extensive hydrogen bonding pattern. There are one strong and two weak intramolecular hydrogen bonds in the phlorizin molecule.

• 한국식품영양학회지
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• 제34권5호
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• pp.477-486
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• 2021

To utilize Malus pruniforia Borkh. as a functional material, cold-water (CW), hot-water (HW), and 70% ethanol (EtOH) extracts were prepared, and their antioxidant and anti-inflammatory activities were compared. The antioxidant activity of the HW extract evaluated by ABTS and DPPH radical scavenging and FRAP activity was significantly effective. The total polyphenol content of the HW extract was also higher by 15.5±0.7 mg GAE/g extract compared to other extracts. The EtOH extract showed significantly decreased TNF-α (39.8%), IL-6 (65.5%), and NO (34.9%) levels in RAW 264.7 cells compared to the LPS-induced control group. The levels of IL-6 (21.1%) and IL-8 (19.3%) were significantly decreased by treatment of EtOH extract in HaCaT keratinocytes induced with TNF-α and IFN-γ. The UHPLC-MS results indicated that the EtOH extract might have chlorogenic acid and phlorizin as the major compounds. This was validated using HPLC-DAD, which showed that the EtOH extract had higher levels of chlorogenic acid and phlorizin (1,185±58 and 470±10 ㎍/g extract, respectively). In conclusion, the present study suggested that the anti-inflammatory activity of the EtOH extract was more effective than the CW and HW extracts, and chlorogenic acid and phlorizin could be used as indicator compounds and functional substances.

• The Korean Journal of Physiology and Pharmacology
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• 제1권1호
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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.

• 한국균학회지
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• 제15권4호
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• pp.224-230
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• 1987

표고버섯의 미토콘드리아는 설탕밀도 선형기울기 원심분리법으로 정제하여, 광감응성 mitochondrial ATPase의 유기물 효과, 광증감제 효과 및 파장 변화에 따른 $K^+$ 이온의 유입 효과를 실험하였다. 1. 이 효소는 10m mol dithiothreitol 및 0.1m mol quinacrine에 의하여 각각 139% 및 128%의 활성도를 증가시켰다. 2. $100\;{\mu}g$의 oligomycin과 1m mol phlorizin은 이 효소의 활성을 각각 48% 및 45% 억제시켰다. 3. 광증감제인 0.1m mol phenazine methosulfate는 이 효소의 활성도를 36% 촉진시켰다. 4. $K^+$ 이온 유입 효과의 최적 파장은 690nm였고, 이때의 최적 pH 및 최적 온도는 각각 7.2 및 $55^{\circ}C$였다.

• Preventive Nutrition and Food Science
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• 제16권2호
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• pp.135-141
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• 2011

Inhibition of intestinal glucose uptake is beneficial in reducing the blood glucose level for diabetes. To search for an effective intestinal glucose uptake inhibitor from natural sources, 70 native edible plants, fruits and vegetables were screened using Caco-2 cells and fluorescent D-glucose analog 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-D-glucose (2-NBDG). A compound that was able to inhibit glucose uptake was isolated from methanol extract of Punica granatum L. and called PG-1a. PG-1a appears to be a phthalic acid-diisononyl ester- like compound (PDE) with molecular weight of 418. The inhibitory effect of PG-1a on intestinal glucose uptake was dose-dependent with 89% inhibition at $100\;{\mu}g$/mL. Furthermore, the intestinal glucose uptake inhibitory effect of PG-1a was 1.2-fold higher than phlorizin, a well known glucose uptake inhibitor. This study suggests that PG-1a could play a role in controlling the dietary glucose absorption, and that PG-1a can effectively improve the diabetic condition, and may be used as an optional therapeutic and preventive agent.

• The Korean Journal of Physiology and Pharmacology
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• 제3권2호
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• pp.191-198
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• 1999

This study was undertaken to examine the effect of ethanol on $Na^+-dependent$ transport systems (glucose, phosphate, and dicarboxylate) in renal brush-border membrane vesicles (BBMV). Ethanol inhibited $Na^+-dependent$ uptakes of glucose, phosphate, and succinate in a dose-dependent manner, but not the uptakes of $Na^+-dependent.$ The $H^+/TEA$ antiport was reduced by 8% ethanol. Kinetic analysis showed that ethanol caused a decrease in $V_{max}$ of three transport systems, leaving $K_m$ values unchanged. Ethanol decreased phlorizin binding, which was closely correlated with the decrease in $V_{max}$ of $Na^+-glucose$ uptake. These results indicate that ethanol inhibits $Na^+-dependent$ uptakes of glucose, phosphate, and dicaboxylate and that the reduction in $V_{max}$ of $Na^+-glucose$ uptake is caused by a decrease in the number of active carrier proteins in the membrane.

• 동의생리병리학회지
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• 제19권5호
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• pp.1330-1336
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• 2005

This study was carried out to investigate the motor activity and glucose transport and metabolism of Gaewool-Whadam-Jian(GWJ) in rat gastro-intestinal tract. The motor activity of the rat gastro-intestinal tract has been investigated by means of measuring barium sulfate passage degrees. Atropine treatment significantly delayed barium sulfate transit, and GWJ pretreatment increased intestinal motor activity, but not significant. GWJ administration showed no toxicity to kidney and liver. Transport and metabolism of glucose were studied in everted sac of rat small intestine with incubation under several conditions. The transport and metabolism of glucose were greater at jejunum than ileum. So, everted jejunum of rat were used to study the effect of GWJ. When GWJ were treated, the concentration of glucose were higher than untreated group. This result was thought to be influenced by the glucose in GWJ. When 2, 4 dinitrophenol and phlorizin were treated, the transport and metabolism of glucose were decreased, but GWJ treated together, the concentration of glucose in serosal solution increased. Gastric juice secretion and total acidity significantly decreased by administration of GWJ through duodenum region. The mechanism of effect of GWJ was still unidentified, Dut through continuous investigation, the effect of GWJ should be investigated.

• 한국식품위생안전성학회지
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• 제8권4호
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• pp.195-204
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• 1993

Basolateral and brush border membrane (BLM and BBM) vesicles of renal proximal tubules were prepared from adult male New Zealand White rabbits to evaluate as a potential model for assessment of nephrotoxicity. PAH uptakes using BLMV, glucose and leucine uptakes using BBMV were measured in the rabbits treated cephaloridine. In addition, urinalysis and histopathological studies were performed to investigate the correlationship with membrane vesicle uptakes. The results were as follows: (1) the activite of Na+, K+ -ATPase was enriched 12.3-fold in vasolateral memvrane vesicles (BLMV) and the specific activity of alkaline phosphatase in purified brush border memvrane vesicles (BBMV) was enriched 10.1-fold compared with each of microsomal homogenate. (2) In the uptake experiments, cephaloridine decreased initial and probenecid-sensitive PAH uptakes in BLMV. (3) Cephaloridine tested decreased initial and phlorizin-sensitive glucose uptakes in BBMV. (4) Cephaloridine tested decreased initial and Na+-dependent leucine uptakes in BBMV. (5) Cephaloridine tested significantly increased the urinary excretion of glucose and activity of ${\gamma}$-GTP. (6) Cephaloridine tested caused moderate necrotic changes in renal tubular cells and formation of urinary cast in the lumina of Henle's loop and collecting tubules besides the swelling of renal tubules.

• 대한의생명과학회지
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• 제12권1호
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• pp.17-22
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• 2006

The baculovirus expression system is a powerful method for producing large amounts of the human erythrocyte-type glucose transport protein, heterologously. Characterization of the expressed protein is expected to show its ability to transport sugars directly. To achieve this, it is a prerequisite to know the properties of the endogenous sugar transport system in Spodoptera frugiperda Clone 21 (Sf21) cells, which are commonly employed as a host permissive cell line to support the baculovirus replication. The Sf21 cells can grow well on TC-100 medium that contains 0.1% D-glucose as the major carbon source, strongly suggesting the presence of endogenous glucose transport system. However, unlike the human glucose transport protein that has a broad substrate and inhibitor specificity, very little is known about the nature of the endogenous sugar transport system in Sf21 cells. In order to characterize further the inhibitor recognition properties of the Sf21 cell transporter, the ability of phloretin, cytochalasin B and D-fructose to inhibit 2-deoxy-D-glucose (2dGlc) transport was examined by measuring inhibition constants $(K_i)$. The $K_i's$ for reversible inhibitors were determined from plots of uptake versus inhibitor concentration. The 2dGlc transport in the Sf21 cells was very potently inhibited by phloretin, the aglucone of phlorizin with a $K_i$ similar to the value of about $2{\mu}M$ reported for inhibition of glucose transport in human erythrocytes. However, the Sf21 cell transport system was found to differ from the human transport protein in being much less sensitive to inhibition by cytochalasin B (apparent $K_i$ approximately $10\;{\mu}M$). In contrast, It is reported that the inhibitor binds the human erythrocyte counterpart with a $K_d$ of approximately $0.12\;{\mu}M$. Interestingly, the Sf21 glucose transport system also appeared to have high affinity for D-fructose with a $K_i$ of approximately 5mM, contrasting the reported $K_m$ of the human erythrocyte transport protein for the ketose of 1.5M.