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کاربرد نوع شرط:
- جایگاه : پژوهشی
- مجله: Iranian Journal of Basic Medical Sciences
- نوع مقاله: Journal Article
- کلمات کلیدی: Isoprenaline,Cilostamide,Inotropic activity,PDE inhibitor,Rat atria
- چکیده:
- چکیده انگلیسی: Objective(s): Recently, we showed that some new synthetic compounds structurally related to cilostamide (4-(1,2-dihydro-2-oxoquinolin-6-hydroxy)- N-cyclohexyl-N-methylbutanamide), a selective phosphodiesterase 3 (PDE3) inhibitor, produce inotropic effect comparable to that of IBMX (3-isobutyl-1-methylxanthine), a non-selective PDE inhibitor, but with differential chronotropic effect. In this investigation, we compared the pharmacological effects of these compounds as potential cardiotonic agents using the spontaneously beating atria model.
Materials and Methods: In each experiment, rats were treated with reserpine. The atrium was isolated and mounted in an organ bath. We assessed chronotropic and inotropic effects using cumulativelogconcentration-response curves of isoprenaline alone or in combination of each test-compound.
Results: Majority of test compounds augment atria contraction force (ACF) significantly but with different potencies on atrium contraction rate. Cilostamide, MCPIP ([4-(4-methyl piperazin-1-yl)-4-oxobutoxy)-4-methylquinolin-2(1H)-one]), methyl carbostyril compounds- (mc1), mc2 and mc5 increased the isoprenaline effect on ACF synergistically. But, mc6 failed to potentiate the effect of isoprenalin; mc3 and mc4 did not increase ACF, which may be because of their higher hydrophilic nature. It was interesting that mc2, alone or in combination with isoprenaline, produced the highest inotropic effect while it did not affect the basal contraction rate and almost blocked the isoprenaline chronotropic effect.
Conclusion: Combination of mc2 with isoprenaline had synergistic effect on inotropic effect, but this combination reduced isoprenaline chronotropic effect; therefore, these effects cannot be related to reducing B-adrenergic receptors activity. These compounds showed different effects; probably all of them were not mediated via PDE3 inhibition and other mechanisms are involving.- انتشار مقاله: 13-03-1396
- نویسندگان: Azar Hosseini,Reza Shafiee-Nick,Hamid Sadeghian,Heydar Parsaee
- مشاهده
- جایگاه : پژوهشی
- مجله: Iranian Journal of Basic Medical Sciences
- نوع مقاله: Journal Article
- کلمات کلیدی: Insulin,Glycogen,Cilostamide,IBMX (3-isobutyl-1-methyl xanthine),Milrinone
- چکیده:
- چکیده انگلیسی: Objective(s) PDE3 has a functional role in insulin secretion and action. We investigated the metabolic effects of new synthetic PDE3 inhibitors (mc1, mc2, mc5 and mc6), on mice and hyperglycemic rat. Materials and Methods The test compound or solvent was injected subcutaneously to mice, for 7 days. On day 8, blood and liver samples were obtained. In hyperglycemic rat, 0.5 g/kg glucose with or without test compounds was injected, and followed with infusion of 1.5 g/kg/hr glucose. Blood samples were collected in mentioned intervals and liver was dissected. Results In hyperglycemic rat, all test compounds decreased blood glucose and the effect of milrinone was potentiated by glybenclamide. Milrinone or IBMX did not change plasma insulin levels, but it was augmented by combination of milrinone and glybenclamide. In both species, liver glycogen storage was decreased by IBMX, mc5, mc6 or MCPIP, increased by mc2 (liver glycogen, rat, control=56±2, mc2=70±3 P< 0.01, mice, control=33±0.7, mc2=42±2.3 P< 0.01) and was not changed in the presence of mc1. Milrinone did not change the glycogen storage in rats though increased it in mice (control= 33±0.7, milrinone= 40±1 P< 0.05). Conclusion Increasing plasma insulin levels by combination of milrinone and glybenclamide confirmed that in hyperglycemic rat, the hypoglycemic effect was correlated with increasing insulin secretion. Variations of plasma insulin were obscured by the pulsative characteristic of pancreatic insulin release. Decreasing glycogen storage reflected inhibition of liver PDE activity. The reasons for ineffectiveness of mc1, anabolic effect of mc2, and differential effects of milrinone were not clear.
- انتشار مقاله: 25-06-1394
- نویسندگان: Azar Hosseini,Reza Shafiee-Nick,Nasser Pour Ali Behzad,Hamid Sadeghian
- مشاهده
- جایگاه : پژوهشی
- مجله: Avicenna Journal of Phytomedicine
- نوع مقاله: Journal Article
- کلمات کلیدی: Insulin,Rat,Ganoderma lucidum,Isolated islets
- چکیده:
- چکیده انگلیسی: Objective: Ganoderma Lucidum (G. Lucidum) has been suggested to increase serum insulin level.This study was undertaken to investigateits direct effect on the islets of Langerhans. Material and Methods: Male albino Wistar rats were anesthetized and the islets were isolated after digestion of the pancreas with collagenase. The islets were incubated for 60 min in Krebs bicarbonate buffer containing 3 or 10 mM glucose in the presence of hydroalcoholic extract of G. Lucidum (1 mg/ml), 3-isobutyl-1-methylxanthine (IBMX, 100 µM) or vehicle. Results: Exposure of islets to the extract increased insulin secretion at basal (3 mM) glucose concentration. Increase of glucose concentration to 10 mM resulted in a significant increase in the rate of insulin secretion. While the IBMX could augment insulin release evoked by 10 mM glucose, the extract failed to modify it. Conclusion: Our results demonstrate that G. lucidum acts directly on the Langerhans islets to increase basal insulin release.
- انتشار مقاله: 30-10-1391
- نویسندگان: Reza Shafiee-Nick,Seyyed Mohammad Reza Parizadeh,Nona Zokaei,Ahmad Ghorbani
- مشاهده