• Toxicological Research
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• v.2 no.1
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• pp.31-36
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• 1986

The present work was undertaken to investigate the effect of glycyrrhetinic acid on pyridine toxicity. When glycyrrhetinic acid was pretreated, pyridine-induced CNS depression and mortality were decreased. A striking enhancement of serum transaminase activities after pyridine administration was markedly decreased by glycyrrhetinic acid pretreatment. It was also observed that the hepatic microsomal aniline hydroxylase activity, which is concerned with pyridine metabolism, was significantly increased in glycyrrhetinic acid pretreated mice.

• YAKHAK HOEJI
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• v.31 no.5
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• pp.315-321
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• 1987

A high performance liquid chromatographic method was developed for the determination of glycyrrhetinic acid contained in licorice powder. Glycyrrhetinic acid which is hydrolysate of glycyrrhizin extracted from licorice powder, was determined with good result by HPLC using 2-bromoacetyltriphenylene labeling reagent. The glycyrrhetinic acids were labeled with 2-bromoacetyltriphenylene in acetonitrile using 18-crown-6-ether and KOH as a catalyst. Derivatized glycyrrhetinic acids were separated from the extracted licorice powder on a reversed-phase column (chemopak $C_{18}$) using 100% acetonitrile as a mobile phase and monitored by an UV-detector at 268nm. Linearity of calibration curve was obtained between 5 ng and 20 ng, and the lower limit of detection was 2 ng. The recovery of glycyrrhetinic acid to licorice powder was about 99.3%. This method was sensitive, reliable and useful for, determination of glycyrrhetinic acid.

• Journal of Periodontal and Implant Science
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• v.24 no.3
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• pp.513-528
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• 1994

배양한 치은섬유아세포와 3T3 세포에서, glycyrrhetinic acid가 cyclosporin A를 처리 세포의 활성에 미치는 영향을 알아보기 위해서 MTT 방법을 이용하여 측정하였다. Cyclosporin A는 $1{\sim}10ng/ml$의 농도에서 인체 치은 섬유아세포와 마우스 3T3 세포 활성을 증가시켰으며, glycyrrhetinic acid는 농도와 비례하게 마우스 3T3 세포의 성장을 억제시켰다. 특히 $25{\mu}g/ml$ 이상의 농도에서는 현저하게 억제시킴을 관찰할 수 있었다. 반면, 인체 치은 섬유아세포에서는 $50{\mu}g/ml$ 이상의 농도에서 조차도 성장을 억제 시키지 않았다. 또한, 마우스 3T3와 인체 치은 섬유아세포에서 일정한 cyclosporin A 농도에 $1-100{\mu}g/ml$의 다양한 농도로 glycyrrhetinic acid를 첨가하였을 때, cyclosporin A 단독으로 처리한 세포에 비하여 유의성 있게 세포의 활성을 억제시켰으며, 특히, $100{\mu}g/ml$의 glycyrrhetinic acid를 첨가하였을 경우 세포활성을 현저하게 억제시켰다. 3T3 세포에 cyclosporin A와 $50{\mu}g/ml$의 glycyrrhetinic acid를 함께 처리한 경우 glycyrrhetinic acid단독처리한 군에 비하여 세포활성에 첨가 효과를 보였으며, 인체 치은 섬유아세포 에서는 같이 처리한 경우 glycyrrhetinic acid단독 처리에 비하여 뚜렷한 억제 효과를 나타내었다. 이러한 상승효과는 1ng/ml 의 cyclosporin A와 $50{\mu}g/ml$ glycyrrhetinic acid를 같이 처리한 군에서 가장 뚜렷하게 관찰되었다. 이러한 결과로, 인체 치은 섬유아세포에 cyclosporin A와 glycyrrhetinic acid를 동에 처리하였을 경우 세포의 활성에 상승 효과가 있음을 알 수 있다.

• YAKHAK HOEJI
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• v.32 no.6
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• pp.377-385
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• 1988

The biologically active component of licoris(Glycyrrhizae Radix L.) is considered to be glycyrrhetinic acid, an aglycone of glycyrrhizin, on the basis of chemical and pharmacological studies. The present study was undertaken to investigate the effect of glycyrrhetinic acid on the hepatic morphine-6-dehydrogenase activity, which catalize morphine to morphinone. Morphine-6-dehydrogenase was further purified by centrifugation, $(NH_4)_2SO_4$ fractionation, sephadex G-100, hydroxyapatite column. Hepatic morphine-6-dehydrogenase activity was significantly decreased by the treatment of glycyrrhetinic acid. When effect of glycyrrhetinic acid on the hepatic morphine-6-dehydrogenase was investigated in vitro, it was powerfully inhibited the enzyme activity with dose-dependent manner. From the above results, glycyrrhetinic acid inhibits hepatic morphine-6-dehydrogenase activity and decreases the morphine induced harmful side effects.

• Journal of Periodontal and Implant Science
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• v.24 no.2
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• pp.238-254
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• 1994

Cyclosporine A is an immunosuppressant commonly used for patients receiving organ transplants. Gingival overgrowth is an adverse side-effect seen in about 8-26% of patients taking cyclosporine A which have been shown to increase the DNA synthesis of gingival fibroblast at the concentration of $10^{-9}g/ml$ in vitro. Glycyrrhetinic acid is the active pharmacological ingredients of licorice which exerts steroid-like action and anti-viral activity. Oleanolic acid, which were isolated from Glechoma hederacea, has been shown to act as inhibitors of tumor promotion in vivo and to be less cytotoxic retinoic acid. This study has been performed to evaluate the effects of glycyrrhetinic acid and oleanolic acid on cyclosporine A induced cell activity in vitro. Human gingival fibroblasts were isolated from explant cultures of healthy gingiva of orthodontic patients. Gingival fibroblasts were trypsinized and transferred to the walls of microtest plates. Fibroblasts were cultured in growth medium added $10^{-9}g/ml$ cyclosporineA and $50{\mu}l/ml$ lipopolysaccharides. Cells between the 4th and 6th transfer in culture were used for this study. The morphology of gingival fibroblst were examined by inverted microscope. The effects of cyclosporine A on the time course of DNA sythesis by human gingival fibroblasts were assessed by $[^3H]-thymidine$ uptake assays. Cyclosporine A was found to stimulate DNA synthesis of human gingival fibroblast at a concentration of $10^{-9}g/ml$. In the presence of lipopolysaccharide derived from Fusobacterium nucleatum, addition of cyclosporine A results in reversal of inhibition at the concentration which normally inhibits gingival fibroblast proliferation. The cell acitivities in the presence of glycyrrhetinic acid and oleanolic acid were decreased, and increased cell acitivities by cyclosporine A were decreased by glycyrrhetinic acid and oleanolic acid at the concentration of $200{\mu}g/ml$. These results suggested that the increased cell activities by cyclosporine A modulated by glycyrrhetinic acid and oleanolic acid.

• Journal of Periodontal and Implant Science
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• v.23 no.2
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• pp.228-242
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• 1993

Some therapeutic agents and medicaments may lead to pathologic changes in the gingival tissue, especially on the cultured human gingival fibroblasts. The purpose of this study was to investigate on the effect of diphenylhydantoin, retinoic acid to the human gingival fibroblast. Human gingival fibroblasts were cultured from the healthy gingiva of patients with orthodontic patients. Gingival fibroblasts were trypsinized and transferred to the wells of 96 well microtest plates. Next day, the medium was removed, fibroblasts were washed with HBSS, and the washed cells were cultured in growth medium added 5 or $10{\mu}g/ml$ of diphenylhydantoin, $10^{-5}M$, $10^{-6}M$ and $10^{-7}M$ of retinoic acid and glycyrrhetinic acid. The passage number of cultured fibroblasts were fifth and eighth. The cell morphology was examined by inverted microscope, the cell number was counted by hemocytometer, and cell activity was measured by the growth and proliferatiton assay using MTT assay. The fifth experiments were performed and statistical significance was measured by ANOVA. The cell morphology in the presence of retinoic acid was round irrespective of the presence of diphenylhydantoin and glycyrrhetinic acid(Fig 2-6). The proliferation of cells was not changed by diphenylhydantoin(Table 1). The cell activity showed the tendency to increase at the concentration of $10{\mu}$'/, of diphenylhydantoin (Table 2). The cell activity in the presence of retinoic acid glycyrrhetinic acid was decreased, and the increased cell activity by diphenylhydantoin was decreased by retinoic acid and glycyrrhetinic acid at the concentration of $10^{-7}M$(Table 3-5). These results suggested that the increased cell activity by diphenylhydantoin might be modulated by retinoic acid and glycyrrhetinic acid.

• Archives of Pharmacal Research
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• v.27 no.1
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• pp.57-60
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• 2004

Glycyrrhizin (18$\beta$-glycyrrhetinic acid-3-O-$\beta$-D-glucuronopyranosyl-(1$\rightarrow2)-\beta$-D-glucuronide, GL) was transformed to 18$\beta$-glycyrrhetinic acid-3-O-$\beta$-D-glucuronide (GAMG) by Streptococcus LJ-22. The antiallergic activities of GL and GAMG was measured using a RBL cell assay system and contact hypersensitivity model mice. GAMG exhibited anti-allergic activity with $IC_{50}$ values of 0.28 mM. GAMG, which is sweeter than GL, and 18$\beta$-glycyrrhetinic acid, which is a GAMG metabolite by human intestinal bacteria, also inhibited the passive cutaneous anaphylaxis and skin contact inflammation. In conclusion, GAMG may be useful as a new sweet food additive and an anti-allergic agent.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.36-40
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• 1996

The effect of glycyrrhetinic acid(18.betha.-glycyrrhetinic acid, GA) on histamine synthesis and release was investigated in cocultured mast cells with Swiss 3T3 fibroblasts. GA has strong dose dependent inhibitory activity for histamine synthesis and release in cocultured mast cells. GA(50 .mu.M) inhibited about 85% of histidine decarboxylase (HDC) activity. The appearance of cells staining positively with berberine sulface was also decreased in the presence of GA. It indicates that transdifferentiation of cultured mas cells (CMCs) was also inhibited.

• Journal of Microbiology and Biotechnology
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• v.28 no.11
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• pp.1876-1882
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• 2018

A series of pentacyclic triterpenoids similar to glycyrrhetinic acid were designed and synthesized via the combination of chemical modification and microbial catalysis. All products were screened for the glycogen phosphorylases inhibitory activities in vitro. Within this series of derivatives, compound 5 displayed good inhibitory activities with $IC_{50}$ value of $27.7{\mu}M$, which is better than that of the other derivatives and glycyrrhetinic acid. Structure-activity relationship (SAR) analysis of these inhibitors was also discussed.

• Proceedings of the Korean Society of Toxicology Conference
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• 2002.05a
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• pp.86-86
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• 2002

Glycyrrhizin, a triterpenoid saponin fraction of licorice, is reported to have anti-viral and anti-tumor activities and is metabolized to 18$\beta$-glycyrrhetinic acid (GA) in the intestine by intestinal bacteria. However, the mechanism underlying its effects is poorly understood.(omitted)