• Title/Summary/Keyword: clotrimazole

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Application of in situ gelling mucoadhesive delivery system for plasmid DNA as a macromolecule

  • Park, Jeong-Sook;Oh, Yu-Kyoung;Kim, Chong-Kook
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.236.1-236.1
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    • 2002
  • Mucosal administration of drug or therapeutic gene is emerging as a new route of delivery for systemic and local therapeutics. Previously. in situ gelling system has been applied to chemical drug such as acetaminophen. insulin. prostaglandin E1. and clotrimazole. Plasmid DNA has not been delivered in form of in situ gelling vehicles. To improve the intranasal absorption of plasmid DNA. we designed delivery systems composed of provide of in 냐셔 gelling and mucoadhesive polymers. (omitted)

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Progesterone Effects on Microsomal Epoxide Hydrolase and Glutathione S-transferease mRNA Levels in Rats (랫드 간 Epoxide Hydrolase와 Glutathione S-Transferase 유전자 발현에 미치는 Progesterone의 효과)

  • Cho, Joo-Youn;Kim, Sang-Geon
    • The Korean Journal of Pharmacology
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    • v.32 no.2
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    • pp.233-241
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    • 1996
  • Previous studies have shown that glucocorticoid suppresses microsomal epoxide hydrolase(EH) gene expression and that EH expression is altered during pregnancy. The effects of progesterone on the expression of rat EH and certain glutathione S-transferase(GST) genes were examined in this study. Northern RNA blot analysis revealed that progesterone was effective in increasing hepatic EH mRNA levels at 12 h to 48 h after treatment with a maximal 9-fold increase being noted at 12 h time point. Nonetheless, multiple daily treatment with progesterone rather caused minimal relative increases in EH mRNA levels. GST Ya and Yb1/2 mRNA levels were also transiently elevated at 12 h after progesterone treatment, followed by gradual decreases from the maximal Increases at day 1, 2 and 5 post-treatment. These changes in EH and GST mRNA levels were noted only at a relatively high dose of progesterone. Furthermore, immunoblot analyses showed that rats treated with progesterone for 5 days failed to show EH or GST induction, indicating that progesterone-induced alterations in EH and GST mRNA levels do not reflect bona fide induction of the detoxifying enzymes. Concomitant progesterone treatment of rats with the known EH inducers including ketoconazole and clotrimazole failed to additively nor antagonistically alter EH mRNA levels. In contrast, dexamethasone substantially reduced ketoconazole- or clotrimazole-inducible EH expression. These results showed that progesterone stimulates the EH, GST Ya and Yb1/2 gene expression at early times followed by marked reduction in the RNA levels from the maximum after multiple treatment and that the changes in mRNA do not necessarily reflect induction of the proteins.

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Design, Synthesis, and Antimicrobial Activity, of New 1,4-disubstituted Octahydroquinoxaline-2,3-dione Derivatives

  • Hussein, Mostafa A.
    • Bulletin of the Korean Chemical Society
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    • v.32 no.5
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    • pp.1511-1518
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    • 2011
  • A series of 1,4-disubstituted octahydroquinoxaline-2,3-dione derivatives was prepared through two steps reaction. The latter involves the formation of N,N-disubstituted cyclohexane-1,2-diamine derivatives (la-j) through reductive alkylation of 1,2-cyclohexanediamine with different aldehydes in presence of sodium cyanoborohydride. Fusion of compounds (1a-j) with diethyl oxalate affording the target compounds (2a-j). Elucidation of structures of compounds (2a-j) was based upon different spectral data as well as the elemental methods of analyses. In addition, mass spectrometry and X-ray diffraction analyses were carried out. Moreover, the lipophilicity of the target compounds as expressed from the Clog P. Most of the test compounds (2a-j) showed weak to moderate antibacterial and antifungal activities against most of the used bacterial and fungal strains in comparison to chloramphenicol and clotrimazole as reference drugs respectively.

Wicaltin, a New Protein Toxin Secreted by the Yeast Williopsis californica and Its Broad-Spectrum Antimycotic Potential

  • Theisen, Simone;Molkenau, Elisabeth;Schmitt, Manfred J.
    • Journal of Microbiology and Biotechnology
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    • v.10 no.4
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    • pp.547-550
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    • 2000
  • The yeast Williopsis californica was shown to secrete a unique broad-spectrum killer toxin (Wicaltin) with antifungal activity against 14 yeast genera, including yeast-like and mycelial forms of the human pathogens Candida albicans and Sporothrix schenkii. Agar diffusion bioassays indicated that its activity was more pronounced than the antifungal potential of frequently used antimycotics; 0.07 pmol Wicaltin showed the same toxicity as 0.2 pmol miconazole and 29 pmol clotrimazole. Since the toxin's primary target would appear to be the yeast cell wall, Wicaltin may be attractive in combatting clinically relevant yeast and fungal infections.

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Yeast Flora of the Human Vagina and Effects of Antifungal Agents on its Growth in vitro

  • Haridy, Mamdouh S.A.;Moustafa, A
    • The Korean Journal of Mycology
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    • v.21 no.2
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    • pp.140-145
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    • 1993
  • Yeast strains were isolated from healthy women(36 isolates), infertile women(15 isolates) and women suffering from local morbidity(82 isolates). On the basis of 37 different physiological and morphological characteristics, the isolated 133 yeast strains were assigned to 10 species belonging to 5 genera. Four pathogenic species were identified. They were Candida albicans, Candida parapsilosis, Candida tropicalis and Trichosporon beigelii. Candida albicans was the dominant species, whereas Saccharomyces cerevisiae prevailed among the saprophytic species. The percentage occurrence as well as the pattern of yeast species differed in the diagnostic groups. It was higher in the women suffering from local morbidity than in the healthy and infertile women. Moreover, a wider spectrum of species was isolated from this group. Women with intrauterine contraceptive devices showed the highest percentage of yeast occurrence which reached 50% of those tested. Five different antifungal agents were tested fro their effects on the growth of the isolated yeast species in vitro. Nystatin was the most effective against the isolated yeast species, followed by pyrithion zink and ciclopiroxolamine, whereas micronazole and clotrimazole, showed a lesser effect.

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Influence of Inhibitors on the Corrosion of Al and Al-composites in Chloride-containing Solutions - A Review

  • Kumar, Neeraj;Srivastava, Ashok K.;Gautam, Prabhat;Manoj, M.K.
    • Korean Journal of Materials Research
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    • v.32 no.5
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    • pp.280-286
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    • 2022
  • Corrosion is a natural, inevitable process, and is one of the world's most serious problems. Losses incurred due to corrosion are extremely expensive for society. Several technological strategies have been explored and implemented to address these losses. The use of inhibitors to prevent corrosion is a common and efficient method to reduce corrosion losses. This review covers Al and Al-composite corrosion inhibitors in chloride-containing solutions, because of their popularity in a broad array of industrial applications. A vast number of studies in the literature detail the common tendency of Al and Al-composites with reinforcements to deteriorate. Accordingly, it is worthwhile to employ inhibitors to protect them, as discussed in the present work. The emphasis is on selecting the smartest corrosion inhibitor and evaluating its performance. According to the study, the most commonly used corrosion inhibitors are 1,4-naphthoquinone (NQ), 1,5-naphthalene diol, 3-amino-1,2,4-triazole-5-thiol (ATAT), ammonium tetrathiotungstate, clotrimazole, amoxicillin, antimicrobial and antifungal drugs. Electrochemical impedance spectroscopy (EIS), potentiodynamic (PDP), and weight loss were among the most commonly used modern electrochemical technologies to test inhibitors' efficacy under environmental conditions.

Dust particles-induced intracellular Ca2+ signaling and reactive oxygen species in lung fibroblast cell line MRC5

  • Lee, Dong Un;Ji, Min Jeong;Kang, Jung Yun;Kyung, Sun Young;Hong, Jeong Hee
    • The Korean Journal of Physiology and Pharmacology
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    • v.21 no.3
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    • pp.327-334
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    • 2017
  • Epidemiologic interest in particulate matter (PM) is growing particularly because of its impact of respiratory health. It has been elucidated that PM evoked inflammatory signal in pulmonary epithelia. However, it has not been established $Ca^{2+}$ signaling mechanisms involved in acute PM-derived signaling in pulmonary fibroblasts. In the present study, we explored dust particles PM modulated intracellular $Ca^{2+}$ signaling and sought to provide a therapeutic strategy by antagonizing PM-induced intracellular $Ca^{2+}$ signaling in human lung fibroblasts MRC5 cells. We demonstrated that PM10, less than $10{\mu}m$, induced intracellular $Ca^{2+}$ signaling, which was mediated by extracellular $Ca^{2+}$. The PM10-mediated intracellular $Ca^{2+}$ signaling was attenuated by antioxidants, phospholipase blockers, polyADPR polymerase 1 inhibitor, and transient receptor potential melastatin 2 (TRPM2) inhibitors. In addition, PM-mediated increases in reactive oxygen species were attenuated by TRPM2 blockers, clotrimazole (CLZ) and N-(p-amylcinnamoyl) anthranilic acid (ACA). Our results showed that PM10 enhanced reactive oxygen species signal by measuring DCF fluorescence and the DCF signal attenuated by both TRPM2 blockers CLZ and ACA. Here, we suggest functional inhibition of TRPM2 channels as a potential therapeutic strategy for modulation of dust particle-mediated signaling and oxidative stress accompanying lung diseases.

Mechanism of the relaxant action of Trazodone in isolated rat aorta (흰쥐 대동맥에서 Trazodone의 혈관이완 작용기전)

  • Kim, Shang-jin;Kim, Jeong-gon;Kim, Jin-shang
    • Korean Journal of Veterinary Research
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    • v.43 no.4
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    • pp.587-595
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    • 2003
  • The aim of this study was to investigate trazodone's effect on vasorelaxation and blood pressure lowering and to examine its underlying mechanism of action in isolated thoracic aorta and anesthesized rats. Precontracted aortic rings with high KCl were relaxed with trazodone, at concentrations of $50{\mu}M$ or greater. However, precontracted rings with phenylephrine (PE) were relaxed with trazodone, at concentrations of $0.03{\mu}M$ or greater, in a concentration-dependent manner. These relaxant effects of trazodone on endothelium intact rat aortic rings were significantly greater than those on denuded rings. The trazodone-induced relaxations were suppressed by nitric oxide synthase (NOS) inhibitors, N(G)-nitro-L-arginine (L-NNA) and N(omega)-nitro-L-arginine methyl ester (L-NAME), guanylate cyclase inhibitors, methylene blue and 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), a $Ca^{2+}$-activated $K^+$ channel blocker, tetrabutylammonium (TBA), a $Ca^{2+}$ channel blocker, nifedipine, $Na^+$ channel blockers, lidocaine and procaine, and removal of extracellular $Na^+$, but not by aminoguanidine, 2-nitro-4-carboxyphenyl-n, n-diphenylcarbamate (NCDC), indomethacin, glibenclamide and clotrimazole. In vivo, infusion of trazodone elicited significant decrease in arterial blood pressure. Trazodone-induced decrease in blood pressure was markedly inhibited by pretreatment of intravenous injection of saponin, L-NNA, methylene blue, TBA, lidocaine or nifedipine. These findings suggest that the endothelium-dependent relaxation and decrease in blood pressure induced by trazodone is mediated by release of NO from the endothelium, activation of TBA-sensitive $Ca^{2+}$-activated $K^+$ channels or inhibition of $Ca^{2+}$ entry through voltage-gated channel.