• 제목/요약/키워드: Glycyrrhizin acid

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SB-31의 Glycyrrhizin을 지표로 한 Rat과 Rabbit에서의 약물동태 및 심혈관계에 대한 효과 연구 (Pharmacokinetics of Anticancer Agent SB-31 in Rats & Rabbits and the Cardiovascular Effect on the Isolated Perfused Rat Heart & Blood Coagulation)

  • 강원구;박용순;이동흠;권광일
    • 한국임상약학회지
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    • 제8권2호
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    • pp.122-132
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    • 1998
  • SB-31 which contains Pursatilla, Licoris and Ginseng extracts was recently proved as an anticancer agent. In a preclinical effort to be applied this drug to human, pharmacokinetics of SB-31 was carried out in rats and rabbits. Glycyrrhizin(GZ), a saponin of Licoris was used as a standard ingradient for the pharmacokinetics of SB-31. The rat's blood, bile and urine samples were serially collected in femoral vein, common bile duct and bladder, respectively, after bolus i.v. injection at a dose of 1 or 1/5 ampul/rat and rabbit's blood samples from the marginal ear vein at a dose of 1 or 3 amp./rabbit. GZ and glycyrrhetic acid(GA), a major metabolite of GZ in the physiological samples were analysed by HPLC with UV detection. The decline of GZ in plasma concentration was generally biexponential at each dose. GZ was almost completely recovered in bile within 18 hour. GA wasn't detected in the samples with UV detector. In the rat, Vss and Kel at a dose of 1 and 1/5 ampul of SB-31 were $98.06\pm6.07\;ml,\;0.33\pm0.05\;hr^{-1}\;and\;65.46\pm11.19\;ml,\;0.68\pm0.25\;hr^{-1}$, respectively. Those in rabbits at a dose of 3 and 1 ampul of SB-31 were $235.24\pm30.72\;ml,\;0.13\pm0.36\;hr^{-1}\;and\;341.32\pm28.58\;ml,\;0.27\pm0.04\;hr^{-1}$, respectively. 'WinNonlin' was utilized for the compartmental analysis. A two-compartment model was chosen as the most appropriate pbarmaco-kinetic model. The data were best described by using a weighting factor of $1/y^2$. To evaluate the effect of SB-31 on cardiovascular system, serially diluted SB-31 was directly injected into coronary artery in the isolated perfused rat heart and the effect of PSF, PSH, saponins of Pursatilla, and SB-31 on PT, APTT of healthy human plasma was examined. Except the positive inotropic effect of ten times diluted solution of SB-31, there was no significant effect on LVDP, (- dp/dt)/(+dp/dt), heart rate and coronary flow in comparision with that of vehicle. SB-31 had no effect on PT but slightly delayed APTT about $6.9{\sim}11.5\%$. There was no significant effect of PSF and PSH on PT & APTT. Conclusively, SB-31 did not show any notable toxic effects on cardiovascular system.

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Pharmacognostical Evaluation and Phytochemical Standardization of Abrus precatorius L. Seeds

  • Verma, Durgesh;Tiwari, Shashi Shankar;Srivastava, Sharad;Rawat, A.K.S.
    • Natural Product Sciences
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    • 제17권1호
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    • pp.51-57
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    • 2011
  • The seeds of Abrus precatorius L. (Family- Fabaceae) constitute the drugs Abrus, Gunja, or Ratti in commerce. In the Indian System of Medicine, the seeds are used for sciatica, paralysis, headache, dysentery, diarrhoea, leprosy, ulcer, nervous disorders, alopecia, as well as anti-inflammatory, antidiabetic, antibacterial, antitumor, sexual stimulant and abortifacient. Seeds are poisonous and therefore are used after mitigation. The protein abrin is responsible for the highly toxic properties of seeds. Quantitative HPTLC analysis of the methanolic extract of seeds determined the presence of 0.4018% gallic acid and 0.4009% glycyrrhizin. The present study was undertaken to develop an HPTLC method, as well as ascertain the physico-chemical, morphological and histological parameters to establish the authenticity of A. precatorius seeds.

구미강활탕의 성분 분석 및 LDL 산화억제 효능 연구 (Simultaneous Determination of Gumiganghwal-tang and Its Anti-atherosclerotic Effect)

  • 김온순;서창섭;신현규
    • 대한예방한의학회지
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    • 제17권3호
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    • pp.165-176
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    • 2013
  • Objective : The purpose of this study was to establish the simultaneous analysis for six compounds in Gumiganghwal-tang (GMGHT, Jiuweiqianghuo-tang) and to investigate the anti-atherosclerotic effects of GMGHT in vitro. Methods : The column for separation of six compounds was used Luna $C_{18}$ column and maintained at $40^{\circ}C$. The mobile phase for gradient elution consisted of two solvent systems, 1.0% acetic acid in water and 1.0% acetic acid in acetonitrile. The analysis was carried out at a flow rate of 1.0 mL/min with pothodiode array (PDA) detection at 254, 280, and 320 nm. The injection volume was 10 ${\mu}L$. The antioxidant activities of GMGHT were evaluated by measuring free radical scavenging activities on 2,2'-Azinobis-3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) and 1-1-diphenyl-2-picrylhydrazyl (DPPH). The inhibitory effects on low-density lipoprotein (LDL) oxidation were evaluated by the formation of thiobarbituric acid relative substances (TBARS), relative electrophoretic mobility (REM), and fragmentation of apolipoprotein B (ApoB)-100. Results : Calibration curves were acquired with $r^2{\geq}0.9998$. The contents of liquiritin, ferulic acid, baicalin, baicalein, glycyrrhizin, and wogonin in GMGHT were 1.784, 1.693, 37.899, 0.258, 1.869, and 0.034 mg/g, respectively. The GMGHT showed the radical scavenging activity in a dose-dependent manner. The concentration required for 50% reduction ($RC_{50}$) against ABTS and DPPH radicals were 72.51 ${\mu}g/mL$ and 128.49 ${\mu}g/mL$. Furthermore, GMGHT reduced the oxidation properties of LDL induced by $CuSO_4$. Conclusion : HPLC-PDA is considered as an available and convenient method for quality control and standardization of GMGH and GMGHT has potentials on anti-atherosclerosis by anti-oxidative effect and suppressive effect on LDL oxidation.

18α-Glycyrrhetinic acid의 위암 세포 사멸 효과에 관한 연구 (18α-Glycyrrhetinic acid induces apoptosis of AGS human gastric cancer cells)

  • 김정남;김병주
    • 대한한의학방제학회지
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    • 제28권1호
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    • pp.63-70
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    • 2020
  • Objectives : The purpose of this study was to investigate the anti-cancer effects of 18α-Glycyrrhetinic acid (18α-GA), a hydrolyzed metabolite of glycyrrhizin, in AGS human gastric adenocarcinoma cells. Methods : We used human gastric adenocarcinoma cell line, AGS cells. We examined cell death by MTT assay and caspase 3 and 9 assay with 18α-GA. To examine the inhibitory effects of 18α-GA, sub-G1 analysis was done the AGS cells after 24 hours with 18α-GA. Also, to investigate the inhibitory mechanisms of 18α-GA, mitogen-activated protein kinase pathways and reactive oxygen species (ROS) generation were examined. Results : 1. 18α-GA inhibited the growth of AGS cells in a dose-dependent fashion. 2. Sub-G1 fractions were significantly and dose-dependently increased by 18α-GA. 3. 18α-GA increased the caspase 3 and 9 activities in AGS cells. 4. 18α-GA inhibited proliferation of AGS cells via the modulation of c‑Jun N‑terminal kinase (JNK) signaling pathways, which results in the induction of apoptosis. 5. 18α-GA enhanced ROS accumulation in AGS cells. Conclusions : Our findings provide insight into unraveling the effects of 18α-GA in human gastric adenocarcinoma cells and developing therapeutic agents against gastric cancer.

LC-MS/MS를 이용한 향소산 중 15종 성분의 정량분석 (Quantitative Analysis of the Fifteen Constituents in Hyangso-San by LC-MS/MS)

  • 서창섭;신현규
    • 생약학회지
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    • 제47권4호
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    • pp.381-388
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    • 2016
  • Hyangso-san is a traditional herbal medicine that consists of the seven herbal medicines, Cyperi Rhizoma, Perillae Folium, Atractylodis Rhizoma, Citri Unshius Pericarpium, Glycyrrhizae Radix et Rhizoma, Zingiberis Rhizoma Crudus, and Allii Fistulosi Bulbus. Hyangso-san has long been clinically used to treat the influenza, including headache, ferver, chills, and pantalgia. In this study, we were performed the simultaneous analysis of the 15 marker compounds (liquiritin apioside, liquiritin, ferulic acid, naringin, hesperidin, rosmarinic acid, liquiritigenin, kaempferol, glycyrrhizin, nobiletin, 6-gingerol, elemicin, atractylenolide III, nootkatone, and atractylenolide I) in Hyangso-san using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS/MS). Column for the separation of the 15 ingredients was used a Waters Acquity UPLC BEH $C_{18}$ analytical column ($2.1{\times}100mm$, $1.7{\mu}m$) at $45^{\circ}C$ by using a mobile phase of 0.1% (v/v) formic acid in water and acetonitrile with gradient condition. Identifications of all analytes were performed using a Waters ACQUITY TQD LC-MS/MS system. The flow rate and injection volume were 0.3 mL/min and $2.0{\mu}L$, respectively. Correlation coefficient of the calibration curve was ${\geq}0.9958$. The values of limits of detection and quantification of the 15 components were 0.002-4.29 and 0.01-12.88 ng/mL, respectively. The result of an analysis using the established LC-MS/MS method, kaempferol and atractylenolide I were not detected, while other 13 compounds were 0.08-56.87 mg/g in lyophilized Hyangso-san sample.

HPLC-PDA을 이용한 이진탕 중 6종 성분의 동시분석 (Simultaneous Analysis of Six Compounds in Yijin-tang by HPLC-PDA)

  • 김성실;김정훈;신현규;서창섭
    • 대한한의학방제학회지
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    • 제21권1호
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    • pp.71-79
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    • 2013
  • Objectives : Yijin-tang has been used in the treatment of gastrointestinal diseases such as irritable bowel syndrome, gastritis, and gastric ulcer. In this study, a high-performance liquid chromatography (HPLC) method was established for simultaneous analysis of six compounds, liquiritin, glycyrrhizin, hesperidin, 6-gingerol, homogentisic acid, and 3,4-dihydroxybenzaldehyde in Yijin-tang, a traditional Korean herbal medicinal preparation. Methods : A Gemini C18 column was used for the separation of six constituents at $40^{\circ}C$. The mobile phase using gradient elution consist of two solvent systems, 1.0% acetic acid in water (A) and 1.0% acetic acid in acetonitrile (B). The flow-rate was 1.0 mL/min and injection volume was $10{\mu}g$. The detector was a photodiode array (PDA) detector set at 254 nm and 280 nm. Results : The calibration curves of six compounds showed good linearity in various concentration ranges ($R^2{\geq}0.9997$). The limits of detection (LOD) and limits of quantification (LOQ) were 0.028-$0.192{\mu}g/mL$ and 0.093-$0.540{\mu}g/mL$, respectively. The RSD (%) of the intra and inter day validations were 0.03-0.84% and 0.05 -1.00%, respectively. Recovery was 96.14-01.90% and RSD (%) was less than 1.5%. Conclusions : The established simultaneous analysis methods will help management to improve the quality of Yijin-tang.

LC-ESI-MS/MS를 이용한 계지탕 중 주요 성분 분석 (Quantitative Determination of the Bioactive Marker Components in Gyeji-tang Using LC-ESI-MS/MS)

  • 서창섭;하혜경
    • 생약학회지
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    • 제49권1호
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    • pp.76-83
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    • 2018
  • A traditional herbal formula, Gyeji-tang has been used to treat the early colds, headache, chills, and fever in Asian countries. In this study, we were performed simultaneous determination of the 14 bioactive marker compounds, gallic acid, spinosin, paeoniflorin, albiflorin, liquiritin apioside, liquiritin, 6'''-feruloylspinosin, liquilitigenin, coumarin, cinnmamic acid, benzoylpaeoniflorin, cinnamaldehyde, glycyrrhizin, and 6-gingerol in Gyeji-tang using an ultra-performance liquid chromatography-electrospray ionization-mass spectrometry (UPLC-ESI-MS/MS). Analytical column was used a Waters Acquity UPLC BEH $C_{18}$ analytical column ($2.1{\times}100mm$, $1.7{\mu}m$) and maintained at $45^{\circ}C$ with a flow rate of 0.3 mL/min. The mobile phase consists of 0.1% (v/v) formic acid in water and acetonitrile with gradient elution. The MS analysis was conducted using multiple reaction monitoring in the positive and negative modes by a Waters ACQUITY TQD LC-MS/MS system. The calibration curves of 14 bioactive marker compounds showed linearity with correlation coefficients ${\geq}0.9798$. The limits of detection and quantification values were in the range of 0.11-6.66 ng/mL and 0.34-19.99 ng/mL, respectively. As a result of the analysis using the established LC-MS/MS method, the amounts of tested 14 compounds in the lyophilized Gyeji-tang sample were detected up to $85.7{\mu}g/g$. These results may be useful for quality assessment of a traditional herbal formulas.

오약순기산 발효물의 성분 분석 및 뇌세포 보호 활성 (Neuroprotective Activity of Fermented Oyaksungisan)

  • 원진배;마진열;양혜진;마충제
    • 생약학회지
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    • 제42권1호
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    • pp.22-26
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    • 2011
  • Korean traditional prescription, Oyaksungisan was usually used to treat rheumatoid arthritis, paralysis. In this study, we compared the contents of five major components, ephedrine HCl, ferulic acid, hesperidin, 6-gingerol, glycyrrhizin and various unknown compounds in Ohyaksungisan (OY) with fermented Ohyaksungisan (FOY) by established HPLC-DAD method. The neuroprotective activity against glutamate-induced cytotoxicity in HT22 cell of OY and FOY was investigated by MTT assay. And anti-oxidative activity of OY and FOY was measured by DPPH radical, hydrogen peroxide and hydroxyl radical scavenging activity. After fermentation, contents of five major components and some unknown compounds (1), (2), (3) and (4) were increased in FOY. Also, FOY showed more potent neuroprotective activity. Furthermore, anti-oxidative activity of FOY was increased. In conclusion, the fermentation of OY could change contents various compounds and improved its neuroprotective activity.

장기보존시험에 따른 쌍화탕의 유통기한 설정 (Establishment of Shelf-life of Ssanghwa-tang by Long-term Storage Test)

  • 서창섭;김정훈;임순희;신현규
    • 생약학회지
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    • 제43권3호
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    • pp.257-264
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    • 2012
  • The purpose of this study was to estimate the shelf-life of Ssanghwa-tang by long-term storage test. Experiments were conducted to evaluate the stability such as the selected physicochemical, pH, identification, heavy metal, microbiological experiment under a long-term storage test of Ssanghwa-tang. The significant change was not showed in pH, heavy metal, microbiological, identification test and quantitative analysis based on long-term storage test. The contents of albiflorin, paeoniflorin, cinnamic acid, liquiritin, and glycyrrhizin in long-term storage test were 66.8-93.1 ${\mu}g/mL$, 429.0-495.0 ${\mu}g/mL$, 3.8-4.4 ${\mu}g/mL$, 32.0-38.1 ${\mu}g/mL$, and 66.8-71.7 ${\mu}g/mL$, respectively. Shelf-lifes by 5 compounds about 3 lots at room temperature were predicted 21-37, 14-21, and 16-72 months, respectively. The suggested shelf-life would be helpful on the storage and distribution of herbal medicine.

Compositional Differences of Ojeok-san (Wuji-san) Decoctions Using Pressurized or Non-pressurized Methods for Variable Extraction Times

  • Kim, Jung-Hoon;Seo, Chang-Seob;Kim, Seong-Sil;Shin, Hyeun-Kyoo
    • 대한약침학회지
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    • 제15권2호
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    • pp.24-30
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    • 2012
  • This study compared Ojeok-san (Wuji-san in Chinese) decoctions produced using different extraction methods for variable times. Decoctions were extracted in pressurized or non-pressurized conditions for 60, 120, and 180 mins. We investigated the Ojeok-san extract yield, the total soluble solid content, the hydrogen ion concentration (pH), and the reference compound content. The extract yield and the total soluble solid content were higher in decoctions produced by non-pressurized extraction; both were proportional to the extraction time. The pH tended to decrease as the extraction time was increased in decoctions produced using both methods. After 60 and 180 mins, the levels of albiflorin, paeoniflorin, nodakenin, naringin, and neohesperidin were significantly higher in decoctions extracted using the non-pressurized method compared with those extracted using the pressurized method. After 120 mins, only cinnamaldehyde was extracted in a greater amount in pressurized decoctions compared with non-pressurized decoctions. The levels of paeoniflorin, ferulic acid, nodakenin, naringin, hesperidin, neohesperidin, and glycyrrhizin increased with time in non-pressurized decoctions. This study showed that the use of pressurized and non-pressurized extraction methods for different times affected the composition of Ojeoksan (Wuji-san) decoctions.