• Biomolecules & Therapeutics
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• v.22 no.2
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• pp.155-160
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• 2014

Thelephoric acid is an antioxidant produced by the hydrolysis of polyozellin, which is isolated from Polyozellus multiplex. In the present study, the inhibitory effects of polyozellin and thelephoric acid on 9 cytochrome P450 (CYP) family members (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4) were examined in pooled human liver microsomes (HLMs) using a cocktail probe assay. Polyozellin exhibited weak inhibitory effects on the activities of all 9 CYPs examined, whereas thelephoric acid exhibited dose- and time-dependent inhibition of all 9 CYP isoforms ($IC_{50}$ values, $3.2-33.7{\mu}M$). Dixon plots of CYP inhibition indicated that thelephoric acid was a competitive inhibitor of CYP1A2 and CYP3A4. In contrast, thelephoric acid was a noncompetitive inhibitor of CYP2D6. Our findings indicate that thelephoric acid may be a novel, non-specific CYP inhibitor, suggesting that it could replace SKF-525A in inhibitory studies designed to investigate the effects of CYP enzymes on the metabolism of given compounds.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.6
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• pp.2307-2312
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• 2015

Curcumol is a sesquiterpene originally isolated from curcuma rhizomes, a component of herbal remedies commonly used in oriental medicine. Its beneficial pharmacological activities have attract significant interest recently. In this study, anti-cancer activity of curcumol was examined with both in vitro and in vivo models. It was found that curcumol exhibited time- and concentration-dependent anti-proliferative effects in SPC-A-1 human lung adenocarcinoma cells with cell cycle arrest in the G0/G1 phase while apoptosis-induction was also confirmed with flow cytometry and morphological analyses. Interestingly, curcumol did not display growth inhibition in MRC-5 human embryonic lung fibroblasts, suggesting the anti-proliferative effects of curcumol were specific to cancer cells. Anti-neoplastic effects of curcumol were also confirmed in tumor bearing mice. Curcumol (60 mg/ kg daily) significantly reduced tumor size without causing notable toxicity. In conclusion, curcumol appears a favorable anti-cancer candidate for further development.

• Journal of Ginseng Research
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• v.43 no.4
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• pp.550-561
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• 2019

Background: Gastric ulcer (GU) is a common gastrointestinal disease that can be induced by many factors. Finding an effective treatment method that contains fewer side effects is important. 20 (S)-ginsenoside Rg3 is a kind of protopanaxadiol and has shown superior antiinflammatory and antioxidant effects in many studies, especially cancer studies. In this study, we examined the treatment efficacy of 20 (S)-ginsenoside Rg3 on GU. Methods: Three kinds of GU models, including an alcohol GU model, a pylorus-ligated GU model, and an acetic acid GU model, were used. Mouse endothelin-1 (ET-1) and nitric oxide (NO) levels in blood and epidermal growth factor (EGF), superoxide dismutase, and NO levels in gastric mucosa were evaluated. Hematoxylin and eosin staining of gastric mucosa and immunohistochemical staining of ET-1, inducible nitric oxide synthase (NOS2), and epidermal growth factor receptors were studied. Ulcer index (UI) scores and UI ratios were also analyzed to demonstrate the GU conditions in different groups. Furthermore, Glide XP from $Schr{\ddot{o}}dinger$ was used for molecular docking to clarify the interactions between 20 (S)-ginsenoside Rg3 and EGF and NOS2. Results: 20 (S)-ginsenoside Rg3 significantly decreased the UI scores and UI ratios in all the three GU models, and it demonstrated antiulcer effects by decreasing the ET-1 and NOS2 levels and increasing the NO, superoxide dismutase, EGF, and epidermal growth factor receptor levels. In addition, high-dose 20 (S)-ginsenoside Rg3 showed satisfactory gastric mucosa protection effects. Conclusion: 20 (S)-ginsenoside Rg3 can inhibit the formation of GU and may be a potential therapeutic agent for GU.

• Archives of Pharmacal Research
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• v.4 no.2
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• pp.91-98
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• 1981

The substituent effects on the fluorescence of 2-(substituted anilino)benzoic acids and their aluminum chelate compounds were examined and satisfactory linear relationships between Hammett substitute constants, .sigma. and the lowest excited singlet energy levels were obtained. But fluorescence intensity only made a qualitative relationship with .sigma. values of substituent groups. Effects of solvents and metal ions on the native and metal chelate fluorescence of the above derivatives were also investigated.

• Archives of Pharmacal Research
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• v.11 no.2
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• pp.166-168
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• 1988

The effects of aglycones moring and quercetin and their corresponding glycosides quercitrin and rutin were studied on the blood glucose levels of rats. Quercetin and quercetrin caused hypoglycaemia in rats while rutin and morin showed almost no difference. Quercetin, which showed 50% pronounced hypoglycaemic effects, reduced significantly the blood glucose level of alloxan diabetic rats.

• Archives of Pharmacal Research
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• v.29 no.11
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• pp.963-968
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• 2006

Seven phenolic compounds (1-7) were isolated from the tubers of Gastrodia elata. Their structures were elucidated on the basis of MS and NMR spectral data. p-Ethoxymethyl phenyl-O-${\beta}$-D-glucoside (1) was proved to be a new compound, with N-(p-hydroxybenzyl)-adenosine (7) isolated from this plant for the first time. In this study, the protective effects of the six constituents (1-6) on PC12 cells against the cytotoxicity induced by KCI and glutamate were also investigated. The viability of the PC12 cells was significantly enhanced by pretreatment with the six phenolic constituents.

• Advances in Traditional Medicine
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• v.8 no.2
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• pp.196-203
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• 2008

The methanol extract of the root of Artanema sesamoides Family Scrophuilariaceae (MEAS) was investigated for possible analgesic and anti-inflammatory effects in animals. Three models were used to study the extract effects on nociception, which were acetic acid-induced writhing response, hot-plate method and the tail flick test in mice. The antiinflammatory effects were evaluated using carrageenan, dextran, histamine and serotonin induced rat paw oedema (acute) and cotton pellet induced granuloma (chronic) models in rats. Results of the study revealed that the extract exhibited significant (P < 0.001) analgesic effect at a dose of 50, 100 and 200 mg/kg b.w p.o in mice in all the models. In acute model, the MEAS also exhibited significant (P < 0.001) antiinflammatory effect in all the above mentioned doses. In chronic model (cotton pellet induced granuloma) the MEAS 200 mg/kg and indomethacin 10 mg/kg showed that inhibition of granuloma formation 25.0% and 47.7% respectively (P < 0.001). The MEAS and indomethacin were effectively preventing the transudation of the fluid. Thus, the present study revealed that the methanol extract of the root of Artanema sesamoides exhibited significant analgesic and antiinflammatory activity.

• Korean Journal of Pharmacognosy
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• v.35 no.1 s.136
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• pp.22-27
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• 2004

Scutellaria baicalensis Georgi is one of most important medicinal herbs in traditional chinese medicine. The object of this study was to determine the effects of the water extracts of Scutellaria baicalensis (SB) on the anxiolytic-like activities in the elevated plus-maze (EPM) test. The watεr extracts of SB (100, 200, or 400 mg/kg) were orally administered to male SD rats for 3 days, and behavioral tests for the anxiolytic activity were performed. SB (100, 200, or 400 mg/kg) significantly increased in time-spent and arm entries into the open arms of the EPM compared with the control group. Futhermore, those anxiolytic-like activities of SB were antagonized by flumazenil (a $GABA_A$ antagonist, 3 mg/kg), but not by pindolol (a $5-HT_{1A}$ antagonist, 10 mg/kg). SB did not cause myorelaxant effects in the horizontal wire test at any dosage regimen. Therefore, these findings suggest that SB promote the anxiolytic-like activity mediated by GABAergic nervous system in rats.

• Korean Journal of Clinical Pharmacy
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• v.29 no.1
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• pp.9-17
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• 2019

Objective: The objective of the present study was to evaluate the effects of implementing a systematic Drug Utilization Review (DUR) system on contraindicated drug use and pharmaceutical expenditures in Korea. Methods: A literature search was conducted using search engines such as PubMed, EMBASE, NDSL, and RISS for relevant systematic studies. The database search was performed and updated in April 2018. Two independent reviewers evaluated the abstracts to find potentially eligible articles. Results: In total, 1433 potentially eligible studies were selected, and 11 articles were eventually shortlisted for inclusion in the present review system. The outcome showed that contraindicated drug use decreased after implementation of the DUR system in Korea. The analysis also showed that the DUR system contributed to a reduction in pharmaceutical expenditures. Conclusions: Our study showed that implementing the DUR system reduced both contraindicated drug use and pharmaceutical expenditures in Korea.

• Archives of Pharmacal Research
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• v.21 no.1
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• pp.67-69
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• 1998

Three TNF-$\alpha$inhibitory lignans were isolated from the flower buds of Magnolia fargesii through bioassay-guided isolation. They were identified as eudesmin, magnolin and lirioresinol-B dimethylether on the basis of their spectroscopic data. All three lignans showed inhibitory effects on TNF-$\alpha$ production in LPS-stimulated murine macrophage cell line, RAW264.7 and eudesmin showed the strongest activity ($IC_{50}=51{\mu}M)$.