• Biomolecules & Therapeutics
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• v.3 no.1
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• pp.34-37
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• 1995

Non-steroidal anti-inflammatory drugs (NSAIDs) have been known as inhibitors of the folate-requiring enzymes. In the present work, we have expanded on these observations and have investigated the inhibitory effects of NSAIDs on Lactobacillus casei thymidylate synthase expressed in E. coli. NSAIDs including sulphasalizine, salicylic acid, indomethacin and mefenamic acid were found to be competitive inhibitors with respect to folate of Lactobacillus casei thymidylate synthase. In contrast, aspirin and the antipyretic-analgesic drugs acetaminophen and antipyrine were weak inhibitors of the enzyme. Structure-activity correlation suggests that an aromatic ring with a side chain containing a carboxylic acid is a requirement for competitive inhibition of the thymidylate synthase. The results are consistent with the hypothesis that the antifolate activity of NSAIDs, and hence cytostatic consequences, are important factors in producing anti-inflammatory activity and aspirin exerts its anti-inflammatory effects after its conversion into salicylic acid, which possesses greater antifolate activity than its parent compound.

• YAKHAK HOEJI
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• v.30 no.4
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• pp.180-184
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• 1986

Such carboxyl drugs as mefenamic acid, alclofenac, ketoprofen, cicloxilic acid and tolfenainic acid in rat plasma were determined by the gas chromatography flame photometric detector (GC-FPD). After methylthiomethyl (MTM) esterification with MTM-chloride in 1, 8-diazabicyclo [5.4.0] undec-7-ene (DBU) catalyst, determination of these drugs by this method was tried and compared with that by the GC-flame ionization detector (FID) method in respect to sensitivity and effect of inteferences. The results showed it was possible to analyze with accuracy by this method because of specificity of the FPD, although these drugs were not separated from interferences in plasma on GC column. The GC-FPD method was more sensitive than GC-FID method and the minimum detectable amount of monocarboxylic drugs on 3%, QF-1 column was about 15fmol/injection.

• Maxillofacial Plastic and Reconstructive Surgery
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• v.30 no.1
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• pp.30-40
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• 2008

The objectives of this study was to check up the effect of celecoxib, COX-2 inhibitor, on the pathogenesis of oral squamous cell carcinoma. After mefenamic acid, aspirin and celecoxib, COX-2 inhibitor, were inoculated to HN 22 cell line, the following results were obtained through tumor cell viability by wortmannin, growth curve of tumor cell line, apoptotic index, PGE2 synthesis, total RNA extraction, RT-PCR analysis and TEM features. 1. When wortmannin and celecoxib were given together, the survival rate of tumor cells was lowest about 47 %. So wortmannin had an effect on the decrease of survival rate of tumor cells. 2. In growth curve, the slowest growth was observed in celecoxib inoculated group. 3. The synthesis of PGE2 was decreased in all group and the obvious suppression and highest apoptotic index was observed in celecoxib inoculated group. 4. Suppression of expression of COX-2 mRNA was evident in celecoxib inoculated group. But that of COX-1,2 mRNA was observed in mefenamic acid inoculated group and aspirin inoculated group. 5. In celecoxib inoculated group, mRNA expression of AKT1 was decreased and that of PTEN & expression of caspase 3 and 9 was evidently increased. Depending on above results, when celecoxib was inoculated to oral squamous cell carcinoma cell line, an increase of mRNA expression of caspase 3,9 and PTEN is related to a decrease of mRNA expression of AKT1. Wortmannin had an effect on the decrease of survival rate of tumor cells. Celecoxib might induce apoptosis of tumor cell by suppression of AKT1 pathway and COX-2 inhibition. This results suggested that COX-2 inhibitor might be significantly effective in chemoprevention of oral squamous cell carcinoma.

• CELLMED
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• v.11 no.4
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• pp.19.1-19.8
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• 2021

Background: Dysmenorrhea is the most common menstrual complaint in young women with a prevalence as high as 90% and is responsible for substantial repeated short-term absenteeism from school and work in young women. The objective of this study was to compare the efficacy of Commiphora myrrha and honey with mefenamic acid in primary dysmenorrhea. Materials and Methods: This prospective standard controlled trial was conducted at Luqman Unani Medical College Hospital and Research Center Vijayapura, India where 40 diagnosed patients of primary dysmenorrhea were randomly assigned to receive test drug (powdered Commiphora myrrha gum resin10g with 30g honey in two divided doses) or active control drug (mefenamic acid 250mg TID) for first 3days of menstruationfor two consecutive cycles. The primary outcome measure was reduction in severity of pain assessed by numerical pain rating scale (NPRS), and secondary outcome measures were improvement in quality of life (QOL) assessed by SF-36 and reduction in perceived stress score (PSS). Results: During first cycle treatment no significant difference was found in NPRS score (p=0.085) between the groups however significant difference in NPRS score (p<0.001) was seen during 2^nd treatment cycle. Significant reduction (p=0.022) in the perceived stress score was noted and overall quality of life was markedly improved after treatment in both the groups. Conclusion: These data suggest that Commiphora myrrha gum resin with honey is an effective herb in reducing symptoms of primary dysmenorrhea. These results need to be confirmed by a properly designed trial with a larger sample size. Trial registration: Clinical Trial Registry India CTRI/2017/09/009596.

• YAKHAK HOEJI
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• v.43 no.6
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• pp.802-808
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• 1999

Vibrio vulnificus cytolysin has been incriminated as one of the important virulence determinants in V. vulnificus infection. In the present study, the effects of Vibrio vulnificus cytolysin on platelets were examined. Vibrio vulnificus cytolysin induced platelet aggregation and increased intracellular calcium concentration ($[Ca^{2+}]_i$) of rat platelets. These effects were abolished in $Ca^{2+}-free$ buffer (2 mM EGTA). Cytolysin also potentiated ADP-and collagen-induced platelet aggregation. Lanthanum (2 mM) inhibited cytolysin-diduced platelet aggregation. However, another $Ca^{2+}$ channel blockers, verapamil ($20{\;}{\mu}M$) or mefenamic acid ($20{\;}{\mu}M$) did not block cytolysin-induced platelet aggregation. Osmotic protectants, sucrose (50 mM) and raffinose (50 nM) suppressed platelet aggregation by 35.9% and 63.4%, respectively. V. vulnificus cytolysin increased membrane conductances of platelet membranes. These results suggest that cytolysin-induced platelet aggregation is mediated via lanthanum sensitive-calcium influx which resulted from the pore formation by V. vulnificus cytolysin.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.401.1-401.1
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• 2002

Potentiometric sensors are important and viable devices for use in pharmaceutical analysis. liquid polymeric membrane electrodes for many basic drugs and a few acidic drug were reported. The acidic drug-metal(Ⅱ)-triethylene tetramine ion pair complexes were prepared and used in poly(vinyl chloride) membrane electrodes to analyze anionic drugs such as mefenamic acid and ibuprofen. Metal ion used were Fe2＋. Co2＋. Ni2＋ and Cu2＋. Plasticizer used was o-nitrophenyl octyl ether.. (omitted)

• Journal of Environmental Health Sciences
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• v.35 no.1
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• pp.45-52
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• 2009

In recent years, pharmaceuticals in the aquatic environment have become a matter of increasing public concern. Environmental risk assessment (ERA), including an exposure assessment, is considered the best scientifically based approach for evaluating the potential effects of pharmaceuticals on ecosystems. Computerized exposure models constitute an important tool in predicting environmental exposures of pharmaceuticals. This paper presents the applicability of an exposure model by comparing measured data of selected pharmaceuticals with predicted environmental concentrations from an exposure model. $PhATE^{TM}$ (Pharmaceutical Assessment and Transport Evaluation) model developed by the Pharmaceutical Research and Manufacturers of America (PhRMA) was adapted to run simulations for the Keum River. A set of 7 pharmaceuticals of high production in Korea was modeled. The PECs generated by the $PhATE^{TM}$ model that were then compared to the measured concentrations. The $PhATE^{TM}$ model predicted concentrations for 7 pharmaceuticals including acetaminophen, acetylsalicylic acid, erythromycin, ibuprofen, lincomycin, mefenamic acid, and naproxen were in good agreement with actual measured concentrations, which demonstrated the utility of $PhATE^{TM}$ as a predictive tool. In conclusion, $PhATE^{TM}$, although it does not intend to accurately represent reality, could be utilized for rapid predictions of the environmental concentrations of pharmaceuticals.

• Journal of Korean Society of Environmental Engineers
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• v.35 no.1
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• pp.45-56
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• 2013

This study was suggested as fundamental data to control medical materials remained in Nakdong range gauge. The level of Iopromide detected in Nakdong mainstream was $0.0015{\sim}0.37{\mu}g/L$, Mefenamic acid $0.0087{\sim}0.056{\mu}g/L$, Diclofenac $N.D.{\sim}0.01{\mu}g/L$, Atenolol $N.D.{\sim}0.024{\mu}g/L$, Propranolol $N.D.{\sim}0.0038{\mu}g/L$, Lincomycin $0.0005{\sim}0.038{\mu}g/L$, and Trimethoprim $N.D.{\sim}0.0083{\mu}g/L$. At sewage disposal plant in the region, most of them were detected high levels of density. Especially, the level of Iopromide was found the highest up to $5.38{\mu}g/L$. At livestock wasted water disposal plant, the level of lincomycin was detected the highest figure of $477{\mu}g/L$. As a result, medical materials from Nakdong River mainstream got increasing the concentration due to inflow from sewage disposal plant in Gumi and River Geumho in Daegu, which affects residential and industrial areas significantly. Therefore, to control medical materials remained in Nakdong River efficiently, Geumho River and sewage disposal plants shall be continuously monitored and managed, which is recommendable.

• Advances in Traditional Medicine
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• v.4 no.2
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• pp.91-94
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• 2004

Water and chloroform/methanol extracts of the three local Malaysian snakehead fish, Channa striatus (striped snakehead), Channa micropeltes (giant snakehead) and Channa lucius (blotched snakehead) were evaluated for inhibitory activity in chronic inflammation, using cotton pellet granuloma test. Both water extracts of C. striatus and C. micropeltes showed marked inhibition of the transudative and proliferative components of chronic inflammation (42.9 and 31.2% respectively for C. striatus, 35.6 and 26.2% for C. micropeltes) when compared to those of mefenamic acid (25.1 and 21.3% respectively) and piroxicam (36.1 and 26.2% respectively). The chloroform/methanol extracts did not exhibit any anti-inflammatory effects. These results indicated that C. striatus has more anti-transudative and anti-proliferative activities than the extract of C. micropletes. C. lucius extract in contrast, did not inhibit these two components. This present study indicated the beneficial effects of the water extracts of C. striatus and C. micropeltes, but not C. lucius on chronic inflammation.

• Journal of the Korean Chemical Society
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• v.64 no.2
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• pp.79-83
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• 2020

A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC₅₀) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC₅₀), cytotoxicity concentration (CC₅₀) and in vitro efficacy index (iEI), 6 (IC₅₀ = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC₅₀ = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.