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LIGAND OF PERIPHERAL IMIDAZOLINE RECEPTORS BASED ON AMIDES OF HETEROCYCLIC ACIDS C7070: EFFECT ON ISHEMIZED TISSUES

Introduction: In this regard, the study of pleiotropic hepatoprotective properties of the agonist of peripheral imidazoline receptors C7070 seems interesting from an applied point of view.

Materials and Methods: Models of a skin flap on a feeding leg, ischemia-reperfusion of the liver and rat heart isolated from Langendorff (ischemia-reperfusion and doxorubicin cardiomyopathy) were used.

Results and Discussion: The I2 agonist C7070 at a dose of 10 mg/kg 4.5-fold prevents the increase in ALT and AST (332.56 ± 22.05/825.49 ± 22.46 ALT/AST 526.90 ± 17.97/1045.16 ± 80.02 units/l in control) and 2.5 times reduces the areas of ischmeic damage and necrosis (0.058 ± 0.029/0.046 ± 0.013 mm2) in the modeling of 15-minute ischemia liver. Moxonidine and metformin had a hepatoprotective effect: 44.99 and 36.88 for moxonidine (ALT and AST) and 34.20 / 21.02 for metformin (ALT / AST). The coefficients of histological hepatoprotective activity: 72.33 and 38.96 (moxonidine and metformin).

C7070 (10.0 mg/kg) has a pronounced dermatoprotective activity and prevents the formation of necrosis on days 3 and 7 of the pathology by 40%. The dermatoprotective activity of metformin (50 mg/kg) from 3 to 10 days decreases from 81% to 92%. The dermatoprotective activity of moxonidine (1 μg/kg) was maximal on the 7th day and was 76%.

In the isolated rat heart, the C7070 showed a protective effect in ischemia-reperfusion and on the model of doxorubicin cardiomyopathy. The STTi index: 8.3, 1.5; 7.9 and 7.8 U. in control, C7070, moxonidine and metformin.

Иллюстрации

Table 1. THE influence of C7070 (10 mg/kg), moxonidine (20 µg/kg) and metformin (50 mg/kg) at the degree of skin flap necrosis at rats. (%) (M±m)

Table 2. The influence of C7070 (10 mg/kg), moxonidine (20 µg/kg) and metformin (50 mg/kg) at the mean values of ALT and AST in blood of experimental animals (U/ml) (M±m)

Table 3.  The influence of C7070 (10 mg/kg), moxonidine (20 µg/kg) and metformine (50 mg/kg) to the hepatic damage area, mm2 (M±m)

Table 4. The influence of C7070 (10 mg/kg), moxonidine (20 µg/kg) and metformine (50 mg/kg) to the heart function measures (M±m, n=10)

Fig. 1. The coefficient STTi for C7070 (10 mg/kg), moxonidine (20 µg/kg) and metformine (50 mg/kg) in modeling of doxorubicine (20 mg/kg) cardiomyopathy

Fig. 2. The differences between C7070 and moxonidine mechanisms of action

DOI: 10.18413/2313-8971-2017-3-4-78-88
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