• Title/Summary/Keyword: glycyrrhetinic acid

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Ginseng Saponin as an Antagonist for Gap Junctional Channels

  • Rhee, Seung-Keun
    • Journal of Ginseng Research
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    • v.30 no.2
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    • pp.64-69
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    • 2006
  • Gap junctional channels, allowing rapid intercellular communication and synchronization of coupled cell activities, play crucial roles in many signaling processes, including a variety of cell activities. Consequently, a modulation of the gap junctional intercellular communication (GJIC) should be a potential pharmacological target. In the present, the GJIC of a epithelial-derived rat mammary cells (BICR-M1Rk) was assessed in the presence of ginseng saponin, by using an established method of scrape-loading dye transfer assay. The transfer of Lucifer yellow (diameter: 1.2 nm) among the neighboring BICR-M1Rk cells, in which connexin43 (Cx43) is a major gap junction channel-forming protein, was significantly retarded at a concentration of $10{\mu}g/ml$ ginseng saponin. By using both methods of RT-PCR and Western blotting, it was demonstrated that ginseng saponin modulated neither the mRNA synthesis of Cx43 nor the translational process of Cx43. This ginseng saponin-induced modification of GJIC was a similar phenomenon observed under the $\beta$-glycyrrhetinic acid treatment, a well-known gap junction channel blocker. Taken together, it is reasonable to conclude that the ginseng saponin inhibits GJIC only by modulating the gating property of gap junction channels.

Estimation of Impurities from Commercially Available Glycyrrhizin Standards by the HPLC/ESI-MS (HPLC/ESI-MS에 의한 글리시리진 표준품의 불순물 추정)

  • Myung, Seung-Woon;Min, Hye-Ki;Kim, Myungsoo;Kim, Young Lim;Park, Seong-Soo;Cho, Jung Hee;Lee, Jong-Chul;Cho, Hyun-Woo;Kim, Taek-Jae
    • Analytical Science and Technology
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    • v.13 no.4
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    • pp.504-510
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    • 2000
  • The impurity profiles from the raw materials of glycyrrhizin were performed by the high performance liquid chromatography (HPLC)/electrospray ionization (ESI)- mass spectrometry (MS). For the HPLC experiment, a $C_{18}$($3.9{\times}300mm$, $10{\mu}m$) column was used and the mobile phase was acetic acid/$H_2O$ (1:10):acetonitrile=3:2 with a flow rate of 0.8 ml/min. The effluent was splitted into the ratio of 50:1 and went into the ESI-MS. Three to six impurities were found and informed of the identification of the structure of the impurities by ESI-MS. And the structures of impurities were suggested to a hydroxy-glycyrrhizin which is added with hydroxy group (-OH) in the glycyrrhetic acid moiety and a reduced-glycyrrhizin which the position of 12 of the glycyrrhetic acid moiety is reduced. The purities of the standard materials were about 90%.

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Induction of Growth Hormone Release by Glycyrrhizae Radix on Rat

  • Lee, Ho-Young;Jung, Dae-Young;Ha, Hye-Kyung;Kang, Sam-Sik;Kim, Ju-Sun;Kim, Chung-Sook
    • BMB Reports
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    • v.40 no.6
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    • pp.979-985
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    • 2007
  • Induction of growth hormone (GH) by Glycyrrhizae Radix (GR), one of the most popular herbal medicine, and its major ingredients were studied in rat pituitary cells in vitro and in vivo assay. The MeOH extract and the n-hexane (HX) fraction of GR induced rat GH (rGH) release up to 1.89 times ($0.34{\pm}0.04 nM$) and 4.59 times ($0.83{\pm}0.03 nM$), compared to the basal level (p < 0.05). Among many ingredients isolated and purified from GR both glycyrrhetinic acid and glycyrrhizin induced significantly rGH release compared to the control (p < 0.05). After an intravenous injection of rat growth hormone releasing hormone (rGHRH) ($10{\mu}g$/kg) as positive control, in SD rats, $T_{max}$ of plasma rGH level was 10 min, $C_{max}$ was $3.84{\pm}0.01 nM$ (n = 3), and enhanced plasma rGH level returned to the baseline in 90 min. Both $AUC_{0-90}$ (area under the curve) of plasma rGH level after HX fraction and that after rGHRH administration were increased significantly from the basal level, respectively (p < 0.01). In conclusions, HX fraction is the most active fraction of MeOH extract of GR in rGH induction.

Role of Gap Junction in the Regulation of Renin Release and Intracellular Calcium in As 4.1 Cell Line

  • Han, Jeong-Hee;Hong, Bing-Zhe;Kwak, Young-Geun;Yuan, Kui-Chang;Park, Woo-Hyun;Kim, Sung-Zoo;Kim, Suhn-Hee
    • The Korean Journal of Physiology and Pharmacology
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    • v.11 no.3
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    • pp.107-112
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    • 2007
  • Gap junction protein, connexin, is expressed in endothelial cells of vessels, glomerulus, and renin secreting cells of the kidney. The purpose of this study was to investigate the role of gap junction in renin secretion and its underlying mechanisms using As 4.1 cell line, a renin-expressing clonal cell line. Renin release was increased proportionately to incubation time. The specific gap junction inhibitor, 18-beta glycyrrhetinic acid (GA) increased renin release in dose-dependent and time-dependent manners. Heptanol and octanol, gap junction blockers, also increased renin release, which were less potent than GA. GA-stimulated renin release was attenuated by pretreatment of the cells with amiloride, nifedipine, ryanodine, and thapsigargin. GA dose-dependently increased intracellular $Ca^{2+}$ concentration, which was attenuated by nifedipine, nimodipine, ryanodine, and thapsigargin. However, RP-cAMP, chelerythrine, tyrphostin A23, or phenylarsine oxide did not induced any significant change in GA-stimulated increase of intracellular $Ca^{2+}$ concentration. These results suggest that gap junction plays an important role on the regulation of renin release and intracellular $Ca^{2+}$ concentration in As 4.1 cells.

Effect of glycyrrhetinic acid on the viability of human gingival fibroblasts (감초산이 인체 치은 섬유모 세포에 미치는 영향)

  • Yoo, Soo-Kyoung;Kim, Ki-Young;You, Yong-Ouk;Jang, Seon-Il;Kim, Kang-Ju;Park, Jong-Keun;Chung, Chong-Pyoung;Kurihara, Hidemi
    • Journal of Periodontal and Implant Science
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    • v.28 no.3
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    • pp.453-465
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    • 1998
  • 감초산이 인체 치은 섬유모세포에 미치는 영향을 세포의 성장과 증식, 총 교원질 합성 및 인체 치은 섬유모세포 핵내 acridine orange 결합으로 추적조사하였다. 조절이 되지 않는 성장을 해결하기 위하여 세포분화인자인 감초산이 배양 치은 섬유모세포의 활성에 미치는 효과를 검색하였다. 감초산 존재하의 배양 인체 섬유모세포의 세포성장 및 증식, 교원질 합성 및 세포 핵내 acridine orange 결합을 각각 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT)법, 4-hydroxyproline, 유식세포분석기를 이용한 acridine orange 결합으로 검색하였다. 형태학적으로 $100\;{\mu}g/ml$의 감초산으로 처리한 섬유모세포는 모양이 둥글게 되었다. 감초산은 $50\;{\mu}g/ml$ 이상의 농도에서 치은 섬유모세포의 성장과 증식을 억제하였다. 감초산 존재 시에 세포내 총 교원질 양이 감소하였고, 세포외배지내의 교원질 총 양이 증가하였다. 인체 치은 섬유모 세포를 $100\;{\mu}g/ml$의 감초산과 함께 24 시간동안 배양하였을 때, 80 채널 이상의 평균형광을 갖는 diploid 세포가 감소하였고, 80 채널 이하의 형광을 갖는 acridine orange결합이 증가하였다. 이러한 연구 결과 감초산은 인체 섬유모세포에서 세포성장 및 증식, 교원질합성 및 DNA 분절화를 유도함이 제시하였다.

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EFFECT OF OCTANOL, THE GAP JUNCTION BLOCKER, ON THE REGULATION OF FLUID SECRETION AND INTRACELLULAR CALCIUM CONCENTRATION IN SALIVARY ACINAR CELLS (흰쥐 악하선 세포에서 gap junction 봉쇄제인 octanol이 타액분비 및 세포내 $Ca^{2+}$ 농도 조절에 미치는 영향)

  • Lee, Ju-Seok;Seo, Jeong-Taeg;Lee, Syng-Il;Lee, Jong-Gap;Sohn, Heung-Kyu
    • Journal of the korean academy of Pediatric Dentistry
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    • v.26 no.2
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    • pp.399-415
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    • 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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INHIBITORY EFFECT OF Er:YAG LASER ON THE GROWTH OF STREPTOCOCCUS MUTANS (Er:YAG 레이저 조사가 Streptococcus mutans의 증식억제에 미치는 효과)

  • Song, Gwang-Chul;Lee, Chang-Seop;Lee, Sang-Ho;Lee, Nan-Young
    • Journal of the korean academy of Pediatric Dentistry
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    • v.30 no.1
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    • pp.15-24
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    • 2003
  • The purpose of this study is to investigate the sterilization effect of Er:YAG laser against the intraoral acid producing bacterium, S. mutans, by irradiating the culture solution containing S. mutans KCTC 3065 with Er:YAG laser having a $650{\mu}m$ diameter beam through the non-contact method. We obtained the following results after examining the temperature changes of the culture solution, numbers of bacterial colonies, and acid-producing ability and attaching ability on teeth by measuring the amount of extracellular polysaccharide produced by S. mutans. The number of bacterial colony was decreased in $10{\mu}l$ culture solution irradiated with laser in overall compared to the control solution. The number decreased as the irradiation intensity and pulse repetition rate were larger and as the exposure time was increased. However, it did not change significantly in $100{\mu}l$ culture solution compared to the control solution. Although the acid-producing ability of S. mutans was inhibited for a certain duration after laser irradiation in 10r1 bacterial culture solution, it did not change in $100{\mu}m$ solution compared with the control solution. The amount of extracellular polysaccharide synthesized by S. mutans was partially decreased through laser irradiation in $10{\mu}m$ culture solution but did not change in $100{\mu}m$ culture solution. Based on these findings, we concluded that Er:YAG laser has an sterilization effect on S. mutans in which we presume that the mechanism is through the heat effect rather than the mechanical effect from development of ultrasound.

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Anti-carcinogenic effects of non-polar components containing licochalcone A in roasted licorice root

  • Park, So Young;Kim, Eun Ji;Choi, Hyun Ju;Seon, Mi Ra;Lim, Soon Sung;Kang, Young-Hee;Choi, Myung-Sook;Lee, Ki Won;Yoon Park, Jung Han
    • Nutrition Research and Practice
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    • v.8 no.3
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    • pp.257-266
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    • 2014
  • BACKGROUND/OBJECTIVE: Licorice has been shown to possess cancer chemopreventive effects. However, glycyrrhizin, a major component in licorice, was found to interfere with steroid metabolism and cause edema and hypertension. The roasting process of licorice modifies the chemical composition and converts glycyrrhizin to glycyrrhetinic acid. The purpose of this study was to examine the anti-carcinogenic effects of the ethanol extract of roasted licorice (EERL) and to identify the active compound in EERL. MATERIALS/METHODS: Ethanol and aqueous extracts of roasted and un-roasted licorice were prepared. The active fraction was separated from the methylene chloride (MC)-soluble fraction of EERL and the structure of the purified compound was determined by nuclear magnetic resonance spectroscopy. The anti-carcinogenic effects of licorice extracts and licochalcone A was evaluated using a MTT assay, Western blot, flow cytometry, and two-stage skin carcinogenesis model. RESULTS: EERL was determined to be more potent and efficacious than the ethanol extract of un-roasted licorice in inhibiting the growth of DU145 and MLL prostate cancer cells, as well as HT-29 colon cancer cells. The aqueous extracts of un-roasted and roasted licorice showed minimal effects on cell growth. EERL potently inhibited growth of MCF-7 and MDA-MB-231 breast, B16-F10 melanoma, and A375 and A2058 skin cancer cells, whereas EERL slightly stimulated the growth of normal IEC-6 intestinal epithelial cells and CCD118SK fibroblasts. The MC-soluble fraction was more efficacious than EERL in inhibiting DU145 cell growth. Licochalcone A was isolated from the MC fraction and identified as the active compound of EERL. Both EERL and licochalcone A induced apoptosis of DU145 cells. EERL potently inhibited chemically-induced skin papilloma formation in mice. CONCLUSIONS: Non-polar compounds in EERL exert potent anti-carcinogenic effects, and that roasted rather than un-roasted licorice should be favored as a cancer preventive agent, whether being used as an additive to food or medicine preparations.

Effects of Toothpaste Containing Several Natural Medicines on Periodontal Disease (수 종의 생약제제가 함유된 치약이 치주질환에 미치는 영향)

  • You, Seung-Han;Hong, Sung-Woo;Kim, Tak;Park, Young-Chae;Kim, Heung-Shik;Yu, Yong-Uk;Yu, Hyeong-Geun;Shin, Hyung-Shik
    • Journal of Periodontal and Implant Science
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    • v.29 no.4
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    • pp.737-749
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    • 1999
  • Recently many researches on plaque removal effect and therapeutic effect of toothpaste containing natural medicines are being studied in early periodontal diseases. The purpose of this study is to examine the clinical and microbiological effect of toothpaste containing natural medicines such as camomile, rhatany, myrrh,sage oil, glycyrrhetinic acid and vitamin E. Sixty three subjects with gingivitis were divided into an experimental group which performed normal oral hygiene procedure with toothpaste containing natural medicines and vitamine E and a control group which also performed normal oral hygiene procedure with Syrinmed? toothpaste without containing herbal extracts and vitamine E. At the baseline, 2 weeks, and 4 weeks, subjects were analyzed for clinical study and microbiological study. After 2 weeks and 4 weeks use of their respective toothpastes, statistically significant decreases of gingival index, plaque index, and bleeding index were shown in both the control and the experimental group. The degree of decrease was more significant in the experimental group than the control group. A statistically significant decrease of pocket depth, and gingival crevicular fluid were shown in both the control and lie experimental group. A statistically significant increase of cocci was shown in both the control and the experimental group, the degree of increase was more significant in the experimental group than control group. A statistically significant decrease ofnon-motile rods, and motile rods were shown in both the control and the experimental group, the degree of decrease was more significant in the experimental group than the control group. Spirochetes increased weakly in both the control and the experimental group but a statistic significance was not shown. A statistically significant decrease of anaerobic bacteria, aerobic bacteria, and black pigmented Bacteroides were shown in both the control and the experimental group. These results indicate that the use of toothpaste containing natural medicines is effective in the prevention and the treatment of periodontal diseases.

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Biological Activities of Licorice F1 Lines and Content Analysis of Phytochemical Constituents

  • Park, Chun-Geon;Lee, Ah Young;Lee, Jeong Hoon;Lee, Jeong Min;Park, Jun Yeon;Lee, Sang-Hoon;Choi, Ae Jin;Park, Chung Berm;Cho, Eun Ju;Lee, Sanghyun
    • Natural Product Sciences
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    • v.20 no.3
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    • pp.137-145
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    • 2014
  • The biological activities of licorice F1 (Glycyrrhiza glabra ${\times}$ G. uralensis) lines (G) were investigated, revealing strong radical scavenging activity targeting 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl (${\cdot}OH$) radicals. At a concentration of $100{\mu}g/mL$, most of the licorice F1 lines scavenged DPPH and ${\cdot}OH$ by more than 80%. Gs-1, -2, and -6 can be considered good scavengers of DPPH radical and G-7 have higher antioxidant activity against ${\cdot}OH$ radical. In addition, licorice F1 lines exerted effective anti-microbial activities against Escherichia coli (Gs-12, -17, and -18) and Staphylococcus aureus (Gs-3, -4, -5, -21, and -26). Moreover, Gs-2, - 20, -31, and -32 effectively inhibited the growth of Helicobacter pylori. Among licorice F1 lines, Gs-25 exhibited high anti-inflammatory effects on nitric oxide produced by lipopolysaccharide- and interferon-${\gamma}$-activated RAW 264.7 cells. Furthermore, Gs-1, -12, and -20 inhibited the growth of AGS human gastric adenocarcinoma cells by more than 60% at a concentration of $100{\mu}g/mL$ and Gs-5, -11, -19, and -32 showed inhibitory effects against rat lens aldose reductase ($IC_{50}$ values, 1.69, 6.07, 6.12, and $4.54{\mu}g/mL$, respectively). The total content of glycyrrhizin (1), glycyrrhetinic acid (2), glabridin (3), and isoliquiritigenin (4) in licorice F1 lines was high in Gs-11, -15, and -30. The present study therefore indicated that Gs-2, -26, -31, and -32 of licorice F1 possessing strong anti-oxidative, anti-microbial, anti-inflammatory, anti-cancer, and aldose reductase inhibitory effects may be used as a possible source material for natural health supplements in the future.