Marcela Rosas-Nexticapa

Evaluation of activity exerted by a steroid derivative on injury by ischaemia/reperfusion

There are reports which indicate that some steroid derivatives have activity atcardiovascular level; nevertheless, there is scarce information about the effects exerted by the progesterone derivatives on cardiac injury caused by ischemia/reperfusion. In this study, a new steroid (progesterone derivative) was synthetized with the objective of evaluating its activity on ischemia/reperfusion injury. The Langendorff technique was used to evaluate the effect of progesterone derivative on ischemia/reperfusion injury. Additionally, molecular mechanism involved in the activity exerted by the progesterone derivative on perfusion pressure and coronary resistance was evaluated by measuring left ventricular pressure in absence or presence of following compounds; mifepristone, prazosin, metoprolol, indomethacin and nifedipine. The results showed that the progesterone derivative reduces infarct size compared with control. Other results showed that the progesterone derivative significantly increase (p = 0.05) the perfusion pressure and coronary resistance in isolated heart. Other data indicate that the progesterone derivative increase left ventricular pressure in a dose-dependent manner (0.001 to 100 nM); however, this phenomenon was significantly inhibited by nifedipine at a dose of 1 nM (p = 0.05). In conclusion, these data suggest that progesterone derivative exert acardioprotective effect via the calcium channels activation and consequently induces changes in the left ventricular pressure levels. This phenomenon results in decrease of myocardial necrosis after ischemia and reperfusion. Key words: Steroid, progesterone, left ventricular pressure, indomethacin.

Biological activity exerted by omega-3 fatty acids on body mass index, glucose, total cholesterol and blood pressure in obese children

Background: Obesity is risk factor to development cardiovascular diseases. There are several studies which indicate that fatty acids can exert changes in body fat in children. However, the results found relatively are few and have generally been conducted over short time periods with small sample sizes, making it difficult to draw definitive conclusions. Objective: In this study the effect induced by omega-3 fatty acids on some biological parameters such as glucose, total cholesterol and body mass index levels in obese children were evaluated. Methods: A dietary intake of gummies with omega-3 fatty acids at dose (100-350 mg) was administered to obese children. Then, glucose, total cholesterol and body mass index levels were determinate using an apparatus (accutrend pluss) and enzyme-immunoassay techniques. Results: The results showed that dietary intake of gummies with omega-3 fatty acids induces significantly changes on total cholesterol and body mass index levels in obese girls compared with obese boys. Conclusions: All these data suggest that dietary intakes of omega-3 fatty acids could be used for the treatment of degree of obesity in obese girls. However, it is important to mention that it is also necessary to evaluate the beneficial effect of omega-3 fatty acids on other biological parameters involved in the degree of obesity as well as the possible toxicity involved in its administration. great controversy about the effect exerted by intake dietary of omega-3 fatty acids against obesity. Therefore, in this study the effect produced by omega-3 fatty acids on some factors associated with obesity such as glucose, body mass index, total cholesterol, and blood pressure levels was evaluated on obese children. Material and Methods Fifth and sixth graders (n=300) in two San Francisco de Campeche Mexico schools were invited to participate in a dietary intake gummy with omega-3 fatty acids at dose of 100 to 350 mg. The parents were informed about the nature and the purpose of this study, and a consent form was signed by parents. In addition, the protocol of this research was previously approved by the ethical committee at the University Autonomous of Campeche. Correspondence to: Lauro Figueroa-Valverde, Laboratory of PharmacoChemistry at the Faculty of Chemical Biological Sciences of the University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México, E-mail: lauro_1999@yahoo.com Received: January 31, 2018; Accepted: February 28, 2018; Published: March 05, 2018 García-Cervera E (2018) Biological activity exerted by omega-3 fatty acids on body mass index, glucose, total cholesterol and blood pressure in obese children Integr Obesity Diabetes, 2018 doi: 10.15761/IOD.1000199 Volume 4(1): 2-4 Anthropometric measures Body mass index. Subjects were weighed without shoes. Standing height was measured without shoes to the nearest 0.5 cm with the use of a commercial stadiometer. Body mass index (BMI) was calculated by dividing weight (kg) by height squared (m2). Blood Parameters Measured. A fasting blood sample was obtained for determination of glucose, triglyceride and total cholesterol concentrations were determined using Accutrend Pluss (Hoffmann-La Roche, Grenzach-Wyhlen, Germany) [19]. Evaluation of insulin levels. Insulin assay was performed by enzyme-immunoassay (Human Insulin ELISA kit, Sigma-Aldrich company) according to the manufacturer’s instruction [20]. Statistical analysis The obtained values are expressed as average ± SE [21]. Results Evaluation of Body Mass Index Body Mass Index (BMI) differences in BMI levels for obese boys after of a dietary intake from gummies with omega-3 fatty acids at a dose of 100 mg (31.00 ± 1.2 Kg/m2), 150 mg (30.04 ± 1.2 Kg/m2), 200 mg (29.00 ± 1.2 Kg/m2), 210 mg (29.29 ± 1.2 Kg/m2), 280 (28.13 ± 1.2 Kg/m2) and 350 mg (25.00 ± 1.7 Kg/m2) in comparison with control (31.48 ± 1.7 Kg/m2). Other results indicate that an intake from gummies with omega-3 fatty acids in obese girls at different doses 100 mg (29.00 ± 1.2 Kg/m2), 150 mg (28.50 ± 1.2 Kg/m2), 200 mg (28.00 ± 1.2 Kg/m2), 210 mg (28.71 ± 1.2 Kg/m2), 280 (27.57 ± 1.2 Kg/m2) and 350 mg (24.00 ± 1.7 Kg/m2) exert changes on BMI levels compared with control (30.40 ± 1.8 Kg/m2). Determination of Glucose levels Administration of dietary intake from gummies with omega-3 fatty acids to obese boys at dose of 100 (102.00 ± 1.7 dg/ml), 150 (110.00 ± 1.7 dg/ml), 200 (115.02 ± 1.7 dg/ml), 210 mg (98.04 ± 1.7 dg/ml), 280 mg (102.00 ± 1.3 dg/ml) and 350 mg (108.00 ± 1.4 dg/ml) was no significant differences. Also, the dietary intake with omega-3 fatty acids in obese girls at dose of 100 (98.00 ± 1.6 dg/ml), 150 (100.00 ± 1.4 dg/ ml), 200 (104.02 ± 1.5 dg/ml), 210 mg (110.00 ± 1.6), 280 mg (107.00 ± 1.3) and 350 mg(102.16 ± 1.2 ) was no significantly changes in the glucose levels compared control conditions (100 .02 ± 1.6). Evaluation of insulin levels The data found showed that insulin levels was not significantly difference in obese boys after of a dietary intake of gummies with omega-3 fatty acids at dose of 100 (14.00 ± 1.5 μU/L), 150 (14.40 ± 1.4 μU/L), 200 (14.60 ± 1.5 μU/L), 2 10 mg (14.80 ± 1.2 μU/L), 280 mg (14.88 ± 1.3 μU/L) and 350 mg (14.08 ± 1.2 μU/L) compared with conditions control (14.0800 ± 1.4 μU/L). Additionally, other results showed that dietary intake of gummies with omega-3 fatty acids in obese girls at doses of 100 (14.50 ± 1.4 μU/L), 150 (14.88 ± 1.3 μU/L), 200 (14.00 ± 1.5 μU/L), 210 mg (13.98 ± 1.1 μU/L), 280 mg (14.20 ± 1.5 μU/L) and 350 mg (14.88 ± 1.4 μU/L) was no significant differences compared with control (13.88 ± 1.5 μU/L). Cholesterol total The results showed significantly variations in cholesterol total levels for obese boys after of a dietary intake of gummies with omega-3 fatty acids at dose of 100 (202.00 ± 1.6 mg/dl), 150 (194 ± 1.5 mg/dl), 200 (190.00 ± 1.7 mg/dl), 210 mg (188.14 ± 1.6 mg/dl), 280 mg (172.12 ± 1.8 mg/dl) and 350 mg (152.10 ± 1.9 mg/dl) in comparison with obese boys without treatment. Other data showed in the Figure 2 indicated that dietary intake with omega-3 fatty acids in obese girls at dose of 100 (186.00 ± 1.6 mg/dl), 150 (182.00 ± 1.5 mg/dl), 200 (180.00 ± 1.7 mg/dl), 210 mg (176.00 ± 1.6 mg/dl), 280 mg (170.00 ± 1.6 mg/dl) and 350 mg (144.10 ± 1.9 mg/dl) exert changes on cholesterol total levels compared with conditions control (188.75 ± 1.5 mg/dl). Blood pressure On the other hand, other results from a dietary intake of gummies with omega-3 fatty acids in obese boys showed significant changes on blood pressure at dose of 100 mg (114.00 mg/dl ± 12.0), 150 mg (108.00 mg/dl ± 14.0), 200 mg (116.00 mg/dl ± 17.0) 210 mg (114.20 mg/dl ± 15.0), 280 mg (118.02 mg/dl ± 13.0) and 350 mg (110.200 mg/dl ± 14.0) with relation to control (116.00 mg/dl ± 13.0). Finally, other data showed that dietary intake with omega-3 fatty acids in obese girls at dose of 100 (106.00 ± 1.4 mg/dl), 150 (104.00 ± 1.4 mg/dl), 200 (102.00 ± 1.7 mg/dl), 210 mg (99.00 ± 1.4 mg/dl), 280 mg (102.00 ± 1.5 mg/dl) and 350 mg (102.04 ± 1.6 mg/dl) produce changes on blood pressure compared with conditions control (112.02 ± 1.4 mg/dl). Discussion There are some reports which indicate that obesity is a factor risks to development several cardiovascular diseases [2,3]. To reduce this clinical pathology some strategies have been used; for example, an intake dietary with high-fiber [22], fruit and vegetable [23] or use of drugs such as Orlistat, sibutiramine, rimonabant and others; however, some of these treatment may produce some adverse effects [24]. Evaluation of effect produced by omega-3 fatty acids on Body Mass Index (BMI) In the search of some therapeutic alternative to reduce the obesity, the effect exerted by a dietary intake of gummies with omega-3 fatty acids on some parameters clinical such as body mass index glucose, cholesterol and blood pressure in an obese children population was evaluated. The results showed that effect produced by a dietary intake of gummies with omega-3 fatty acids decreased BMI levels in obese girls compared to obese boys and control (obese girls without treatment) at different doses (Figure 1); these data are supported by some studies previously reported [25], which indicate that administration of omega-3 fatty acids decreased the BMI in obese girls. Determination of biological activity exerted by omega-3 fatty acids on Cholesterol total concentration Analyzing the data above mentioned and other studies which suggest that intake diet of n-3 polyunsaturated fatty acids can produce changes on total cholesterol levels [26], in this study, the effect exerted by omega-3 fatty acids on total cholesterol concentration in obese children was evaluated. The results found indicated that omega-3 fatty acids significantly reduce the total cholesterol concentration in obese girls compared with obese boys and controls (Figure 2). However, it is noteworthy that some studies indicate that omega-3 fatty acids, in addition of alterations of total cholesterol also may exert changes in blood pressure levels [27]. Evaluation of effect produced by omega-3 fatty acids on Blood Pressure In this study, the biological activity of by dietary intake of gummies with omega-3 fatty acids on blood pressure in obese children was García-Cervera E (2018) Biological activity exerted by omega-3 fatty acids on body mass index, glucose, total cholesterol and blood pressure in obese children Integr Obesity Diabetes, 2018 doi: 10.15761/IOD.1000199 Volume 4(1): 3-4 evaluated. The results showed (Figure 3) that omega-3 fatty acids decreased the blood pressure in a dependent-dose manner compared with obese boys and controls (obese children, without treatment). These data are similar to other studies that indicate that omega-3 fatty acids can induce changes in blood pressure in hypertensive patients [28]. It is important to mention that this phenomenon also may also be conditioned by changes

Design and synthesis of a new steroid-macrocyclic derivative with biological activity

The aims of this study were to evaluate the positive inotropic effect of a new macrocyclic derivative (compound 11) and characterize the molecular mechanism involved in its biological activity. The first step was achieved by synthesis of a macrocyclic derivative involving a series of reactions for the preparation of several steroid derivatives such as (a) steroid-pyrimidinone (3 and 4), (b) steroid-amino (5), (c) steroid-imino (6), (d) ester-steroid (7 and 8), and (e) amido-steroid (9 and 10). Finally, 11 was prepared by removing the tert-butyldimethylsilane fragment of 10. The biological activity of compounds on perfusion pressure and vascular resistance was evaluated on isolated rat heart using the Langendorff model. The inotropic activity of 11 was evaluated in presence of prazosin, metoprolol, indomethacin, nifedipine, and flutamide to characterize its molecular mechanism. Theoretical experiments were carried out with a Docking model, to assess potential interactions of androgen receptor with 11. The results showed that only this macrocyclic derivative exerts changes on perfusion pressure and vascular resistance translated as the positive inotropic effect, and this effect was blocked with flutamide; these data indicate that the positive inotropic activity induced by this macrocyclic derivative was via androgen receptor activation. The theoretical results indicated that the interaction of the macrocyclic derivative with the androgen receptor involves several amino acid residues such as Leu704, Asn705, Met780, Cys784, Met749, Leu762, Phe764, Ser778, and Met787. In conclusion, all these data suggest that the positive inotropic activity of the macrocyclic derivative may depend on its chemical structure.

Experimental, theoretical and biological activity of a triazonine-derivative on left ventricular pressure.

BACKGROUND There are data indicating that several azonine-derivatives may exert effects on some biological systems; however, there is very low information on the biological activity induced by these compounds on left ventricular pressure. OBJECTIVE The aim of this study was to synthesize and evaluate the biological activity of new triazoninederivative on left ventricular pressure. MATERIAL AND METHODS The first stage involved: 1) preparation of two azepine-benzamide derivatives (Z or E) by reaction of the nitrobenzoyl azide with adrenosterone; and 2) reaction of (Z)-azepine-benzamide derivative with ethylenediamine to form the triazonine derivative. The structure of compounds was confirmed by spectroscopy and spectrometry data. The second stage involved the biologic activity on left ventricular pressure was evaluated in a model of rat heart isolated. In addition, some physicochemical parameters were evaluated to characterize the possible molecules involved in its effect. RESULTS The results showed that only the triazonine increased left ventricular pressure via androgen receptor. CONCLUSIONS In conclusion, this phenomenon is conditioned by the functional groups involved in the chemical structure of triazonine derivative and their interaction with residues of amino acids involved on the androgen receptor surface.