The relaxant responses induced by ethanol in the smooth muscle: role of extracellular and intracellular Ca2+ [Duz kasta etanol ile induklenen gevseme cevaplari: ekstraseluler ve intraseluler Ca2+un rolu]

Since worldwide alcohol consumption, the understanding the mechanism of action of ethanol is important in the gastrointestinal tract. In this study we aimed to clarify the role of extracellular and intracellular calcium (Ca2+) on relaxations induced by ethanol in isolated mouse gastric fundus. Mice (Swiss albino) of either sex were used in this study. After killing the mice by cervical dislocation the gastric fundal strips were prepared by longitudinal incision and mounted under 0.5 g tension in an organ bath filled with Tyrodes solution. The bath medium was maintained at 37 oC and gassed with %95O2 and 5%CO2. Experimental data were recorded by an isometric transducer. Ethanol (164 mM) caused reproducible relaxations in isolated mouse gastric fundal strips. These relaxations were significantly inhibited by verapamil (10-5-5x10-4 M), a blocker of L-type Ca2+ channels, and ruthenium red (10-5-10-4 M), a blocker of ryanodine receptors (intracellular Ca2+ channels) in a concentration dependent manner. On the other hand cyclopiasonic acid (CPA; 10-6-10-5 M), a blocker of Ca2+-ATPase, failed to affect the relaxations induced by ethanol. The results of experimental data suggest that extracellular Ca2+ influx and intracellular Ca2+ release may play a role on relaxations induced by ethanol in the isolated mouse gastric fundal smooth muscle. [Med-Science 2016; 5(4.000): 967-71

Düz kasta etanol ile indüklenen gevşeme cevapları: ekstraselüler ve intraselüler Ca2+'un rolü

Alkol dünyada yaygın olarak tüketildiğinden, etanolün gastrointestinal sistem üzerindeki etkisinin mekanizmasının anlaşılması önemlidir. Bu çalışmada, izole fare mide fundusunda etanol ile indüklenen gevşemeler üzerinde ekstraselüler ve intraselüler kalsiyum (Ca2+)'un rolünü araştırmayı amaçladık. Bu çalışmada her iki cinsten (Swiss albino) fare kullanıldı. Fareler servikal dislokasyon ile öldürüldükten sonra longitudinal insizyon suretiyle gastrik fundal stripler hazırlandı ve içinde Tyrode solusyonu olan organ banyosuna 0.5 g tansiyon altında asıldı. Banyo ortamı 37 oC'de sabit tutuldu ve %95 O2 ve %5 CO2 ile gazlandırıldı. Deneysel veriler izometrik transdusır ile kaydedildi. Etanol(164 mM) izole fare mide fundus şeritlerinde tekrarlanabilir gevşemelere neden oldu. Bu gevşemeler L-tipi Ca2+ kanal blokörü verapamil (10-5-5x10-4 M) ve ryanodin reseptör (intraselüler kalsiyum kanal)'lerinin spesifik blokörü rutenyum red (10-5-10-4M) ile istatistiksel olarak anlamlı bir şekilde azaldı. Buna karşılık Ca2+-ATPaz'ın spesifik inhibitörü siklopiazonik asit (CPA; 10-6-10-5 M) bu gevşemeleri etkilemedi. Deneysel bulgular, izole fare mide fundus şeritlerinde etanol (164 mM) ile oluşturulan gevşemelerde hem ekstraselüer hem de intraselüler Ca2+'un rolü olabileceğini telkin etmektedirSince worldwide alcohol consumption, the understanding the mechanism of action of ethanol is important in the gastrointestinal tract. In this study we aimed to clarify the role of extracellular and intracellular calcium (Ca2+) on relaxations induced by ethanol in isolated mouse gastric fundus. Mice (Swiss albino) of either sex were used in this study. After killing the mice by cervical dislocation the gastric fundal strips were prepared by longitudinal incision and mounted under 0.5 g tension in an organ bath filled with Tyrode's solution. The bath medium was maintained at 37 oC and gassed with %95O2 and 5%CO2. Experimental data were recorded by an isometric transducer. Ethanol (164 mM) caused reproducible relaxations in isolated mouse gastric fundal strips. These relaxations were significantly inhibited by verapamil (10-5-5x10-4 M), a blocker of L-type Ca2+ channels, and ruthenium red (10-5-10-4 M), a blocker of ryanodine receptors (intracellular Ca2+ channels) in a concentration dependent manner. On the other hand cyclopiasonic acid (CPA; 10-6-10-5 M), a blocker of Ca2+-ATPase, failed to affect the relaxations induced by ethanol. The results of experimental data suggest that extracellular Ca2+ influx and intracellular Ca2+release may play a role on relaxations induced by ethanol in the isolated mouse gastric fundal smooth muscl

The impact of extracellular and intracellular Ca2+ on ethanol-induced smooth muscle contraction

WOS: 000270733600006PubMed ID: 19749788Aim: To evaluate the impact of extracellular and intracellular Ca2+ on contractions induced by ethanol in smooth muscle. Methods: Longitudinal smooth muscle strips were prepared from the gastric fundi of mice. The contractions of smooth muscle strips were recorded with an isometric force displacement transducer. Results: Ethanol (164 mmol/L) produced reproducible contractions in isolated gastric fundal strips of mice. Although lidocaine (50 and 100 mu mol/L), a local anesthetic agent, and hexamethonium (100 and 500 mu mol/L), a ganglionic blocking agent, failed to affect these contractions, verapamil (1-50 mu mol/L) and nifedipine (1-50 mu mol/L), selective blockers of L-type Ca2+ channels, significantly inhibited the contractile responses of ethanol. Using a Ca2+-free medium nearly eliminated these contractions in the same tissue. Ryanodine (1-50 mu mol/L) and ruthenium red (10-100 mu mol/L), selective blockers of intracellular Ca2+ channels/ryanodine receptors; cyclopiazonic acid (CPA; 1-10 mu mol/L), a selective inhibitor of sarcoplasmic reticulum (SR) Ca2+-ATPase; and caffeine (0.5-5 mmol/L), a depleting agent of intracellular Ca2+ stores, significantly inhibited the contractile responses induced by ethanol. In addition, the combination of caffeine (5 mmol/L) plus CPA (10 mu mol/L), and ryanodine (10 mu mol/L) plus CPA (10 mu mol/L), caused further inhibition of contractions in response to ethanol. This inhibition was significantly different from those associated with caffeine, ryanodine or CPA. Furthermore the combination of caffeine (5 mmol/L), ryanodine (10 mu mol/L) and CPA(10 mu mol/L) eliminated the contractions induced by ethanol in isolated gastric fundal strips of mice. Conclusion: Both extracellular and intracellular Ca2+ may have important roles in regulating contractions induced by ethanol in the mouse gastric fundus.Scientific and Technical Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [SBAG-HD-244, 107S290]This study was supported by the Scientific and Technical Research Council of Turkey (TUBITAK) (SBAG-HD-244, 107S290). Part of this work was presented at VII National Congress of Neuroscience, Adana, Turkey, 2008

N-Benzoylthiourea-pyrrolidine carboxylic acid derivatives bearing an imidazole moiety: Synthesis, characterization, crystal structure, in vitro ChEs inhibition, and antituberculosis, antibacterial, antifungal studies

A series of novel N-benzoylthiourea-pyrrolidine carboxylic acid derivatives bearing an imidazole moiety has been prepared and their various biological activities are evaluated. The ability of forming intermolecular hydrogen-bonds of these molecules was pursued in the search of the best antimicrobial activity. The synthesized compounds were tested to search whether they had an enzyme inhibitory potency against AChE and BChE, which are the main targets for Alzheimer's disease. The prepared compounds were also screened for antituberculosis activity against M. tuberculosis H37Rv strain and the antibacterial activity against E. coli, A. baumannii, S. aureus, B. subtilis, A. hydrophila, bacteria. In addition, their antifungal activities are also evaluated against C. tropicalis, C. albicans, C. glabrata strains.This work is a part of Samet POYRAZ's Ph.D. thesis granted by Mersin University (Project no: 2019-1-TP3-3463) and (Project no: 2020-1 AP4-3982). We also gratefully acknowledge support from Çukurova University (Project no: TSA-2021-13814), Alicante University and Mersin University