The aim of this study was to compare classical Balke and Bruce protocols with our modification of Balke protocol in pediatric cardiorespiratory diagnostics. The modification of Balke consists of nine stages per 1 min at a constant velocity of 5.6 km x h(-1) and increasing elevation from 6% to 22% in 2% increments. Sixty healthy children (mean age = 13.3+/-0.2 years; BMI = 18.8+/-0.6 kg x m(-2); mean +/- 95% CI), divided into three groups of 20 children each, matched by age, height and BMI performed integrative cardiopulmonary exercise testing using one of the treadmill protocols mentioned. At the end of each exercise increment and throughout the recovery period the children were asked to rate the perceived exertion (RPE) using the Borg Category Ratio scale--CR-10. Exercise results showed that Balke protocol had the longest duration (21.7+/-0.6 min.) and the lowest values for VO2/kg (34.2+/-1.8 ml x min(-1) x kg(-1)) due to the minimal workload increments. Bruce protocol had intermediate duration (14.9+/-1.1 min.) and children achieved the highest VO2/kg (48.6+/-2.7 ml x min(-1) x kg(-1)) but the test is symptom-limited which is ethically unacceptable in childhood. Exercise data revealed that our modification of the classical Balke protocol had an optimal duration (11 min.) and yielded peak VO2/kg values (39.4+/-2.3 ml x min(-1) x kg(-1)) adequate for evaluation of children's exercise capacity. Children's ratings of perceived exertion were highest in Bruce protocol (6.5+/-0.4) and lowest in the original Balke protocol (4.5+/-0.8). In conclusion, the modification of Balke protocol is suitable and reliable for screening and clinical testing in pediatric age group.
本研究的目的是比较经典的Balke和Bruce方案与我们修改的Balke方案在儿科心肺诊断中的应用。Balke的改进包括每1分钟以5.6 km x h(-1)的恒定速度进行9个阶段,并以2%的增量将海拔从6%增加到22%。60名健康儿童(平均年龄= 13.3±0.2岁;BMI = 18.8+/-0.6 kg × m(-2);平均+/- 95% CI),分为三组,每组20名儿童,根据年龄、身高和BMI进行匹配,使用上述一种跑步机方案进行综合心肺运动测试。在每个运动增量结束时和整个恢复期,要求儿童使用博格分类比率量表(CR-10)对感知运动(RPE)进行评分。运动结果显示,由于工作量增量最小,Balke方案持续时间最长(21.7+/-0.6 min), VO2/kg值最低(34.2+/-1.8 ml x min(-1) x kg(-1))。布鲁斯方案的持续时间中等(14.9+/-1.1分钟),儿童达到最高的VO2/kg (48.6+/-2.7 ml x min(-1) x kg(-1)),但该试验是症状有限的,这在儿童时期在伦理上是不可接受的。运动数据显示,我们对经典Balke方案的修改具有最佳持续时间(11分钟),并产生峰值VO2/kg值(39.4+/-2.3 ml x min(-1) x kg(-1)),足以评估儿童的运动能力。布鲁斯方案中儿童感知运动强度评分最高(6.5+/-0.4),原始Balke方案中儿童感知运动强度评分最低(4.5+/-0.8)。综上所述,Balke方案的修改适用于儿童年龄组的筛查和临床检测。
{"title":"Modified treadmill protocol for evaluation of physical fitness in pediatric age group--comparison with Bruce and Balke protocols.","authors":"B Marinov, S Kostianev, T Turnovska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of this study was to compare classical Balke and Bruce protocols with our modification of Balke protocol in pediatric cardiorespiratory diagnostics. The modification of Balke consists of nine stages per 1 min at a constant velocity of 5.6 km x h(-1) and increasing elevation from 6% to 22% in 2% increments. Sixty healthy children (mean age = 13.3+/-0.2 years; BMI = 18.8+/-0.6 kg x m(-2); mean +/- 95% CI), divided into three groups of 20 children each, matched by age, height and BMI performed integrative cardiopulmonary exercise testing using one of the treadmill protocols mentioned. At the end of each exercise increment and throughout the recovery period the children were asked to rate the perceived exertion (RPE) using the Borg Category Ratio scale--CR-10. Exercise results showed that Balke protocol had the longest duration (21.7+/-0.6 min.) and the lowest values for VO2/kg (34.2+/-1.8 ml x min(-1) x kg(-1)) due to the minimal workload increments. Bruce protocol had intermediate duration (14.9+/-1.1 min.) and children achieved the highest VO2/kg (48.6+/-2.7 ml x min(-1) x kg(-1)) but the test is symptom-limited which is ethically unacceptable in childhood. Exercise data revealed that our modification of the classical Balke protocol had an optimal duration (11 min.) and yielded peak VO2/kg values (39.4+/-2.3 ml x min(-1) x kg(-1)) adequate for evaluation of children's exercise capacity. Children's ratings of perceived exertion were highest in Bruce protocol (6.5+/-0.4) and lowest in the original Balke protocol (4.5+/-0.8). In conclusion, the modification of Balke protocol is suitable and reliable for screening and clinical testing in pediatric age group.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"27 2-3","pages":"47-51"},"PeriodicalIF":0.0,"publicationDate":"2003-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24037406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The age-related differences in the synapses of the paraventricular hypothalamic nucleus (PVN) were studied with transmission electron microscopy in young (3-month-old) and senescent (25-month-old) Wistar rats. The changes in the axodendritic (ADS) and axospinous (ASS) synapses in the PVN neuropil were determined by morphometry. The majority of synapses were of the ADS type. In senescent rats the density of both ADS and ASS was diminished. The mean area of the ASS presynaptic boutons in aged rats was more enlarged than of the boutons in the ADS. The parameters characterising synaptic vesicles (SV) were diminished in aging rats. The number of SV per synaptic bouton decline was not significantly different. The changes in the length of synaptic contact zone (SCZ) were not significant with the exception of the total SCZ length per 1000 microm2 and the total area of the SCZ per 1000 microm3 in the ADS. The decrease of the number of dendritic spines (DS) per 1000 microm2 in the neuropil was significantly age-related diminished. Moreover, the mean area of the DS was significantly enlarged.
{"title":"Aging and synaptic changes in the paraventricular hypothalamic nucleus of the rat.","authors":"D E Itzev, S R Lolov, K G Usunoff","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The age-related differences in the synapses of the paraventricular hypothalamic nucleus (PVN) were studied with transmission electron microscopy in young (3-month-old) and senescent (25-month-old) Wistar rats. The changes in the axodendritic (ADS) and axospinous (ASS) synapses in the PVN neuropil were determined by morphometry. The majority of synapses were of the ADS type. In senescent rats the density of both ADS and ASS was diminished. The mean area of the ASS presynaptic boutons in aged rats was more enlarged than of the boutons in the ADS. The parameters characterising synaptic vesicles (SV) were diminished in aging rats. The number of SV per synaptic bouton decline was not significantly different. The changes in the length of synaptic contact zone (SCZ) were not significant with the exception of the total SCZ length per 1000 microm2 and the total area of the SCZ per 1000 microm3 in the ADS. The decrease of the number of dendritic spines (DS) per 1000 microm2 in the neuropil was significantly age-related diminished. Moreover, the mean area of the DS was significantly enlarged.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"27 2-3","pages":"75-82"},"PeriodicalIF":0.0,"publicationDate":"2003-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24037813","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Physical activity has a beneficial effect on the serum lipid profile in adolescent and mature humans. The aim of the study was to compare the basic serum lipid parameters of pubescent athletes practicing different sports with those of untrained boys and girls and to investigate the relationship between the variations of the values of these variables and the respective type of sport practiced. 876 highly trained athletes (559 boys and 317 girls) were included in this study. Their mean (+/- SD) age, weight and duration of training were: 14.01 +/- 1.78 years; 56.24 +/- 15.39 kg, and 3.52 +/- 2.07 years. The control group consisted of 357 untrained subjects (171 boys and 186 girls) with mean (+/- SD) age and weight 14.58 +/- 1.70 years and 57.75 +/- 12.66 kg. The group of athletes was divided into seven subgroups according to the sport practiced: athletics (n = 105), swimming (n = 107), rowing (n = 233), wrestling, box and judo (n = 225), weight lifting (n = 47), various team sports (n = 92), and other sports (n = 67). Venous blood samples were drawn from the cubital vein and the concentrations of serum total cholesterol (CHOL), HDL-cholesterol (HDL-C), and triglycerides (TG) were measured. Statistical indices were computed for each group and for each variable, and analysis of variance factorial analysis was performed to evaluate the statistical significance of the differences detected. The CHOL in highly trained group was found lower than in the control group (3.93 +/- 0.89 vs. 4.31 +/- 0.76 mmol/l, p < 0.001), and in highly trained boys the CHOL was lower than in highly trained girls (3.88 +/- 0.71 vs. 4.02 +/- 0.89 mmol/l, p < 0.01). The HDL-C was lower in the trained group in comparison with the control one (1.43 +/- 0.59 vs. 1.60 +/- 0.57 mmol/l, p < 0.001). No differences were found in HDL-C between boys and girls in both trained and control group. Serum TG were higher in highly trained group than in controls (1.01 +/- 0.59 vs. 0.89 +/- 0.38 mmol/l, p < 0.001). The results of the study indicate that (a) trained pubescents have lower serum total cholesterol than untrained boys and girls of the same age; (b) trained pubescent boys have lower serum total cholesterol than trained pubescent girls; (c) the level of serum TG is not relevant to the type of physical exercise in pubescence; (d) long-term sport practicing is not able to decrease serum HDL-C levels in both sexes; (e) sport affects serum total cholesterol to a greater degree than does sex in pubescence.
体力活动对青少年和成年人的血脂有有益的影响。本研究的目的是比较不同运动训练的青少年运动员与未训练的男孩和女孩的基本血脂参数,并探讨这些变量值的变化与各自运动类型之间的关系。876名训练有素的运动员(559名男生和317名女生)被纳入本研究。他们的平均(+/- SD)年龄、体重和训练时间为:14.01 +/- 1.78岁;56.24 +/- 15.39千克,3.52 +/- 2.07年。对照组包括357名未经训练的受试者(171名男生和186名女生),平均(+/- SD)年龄和体重分别为14.58 +/- 1.70岁和57.75 +/- 12.66 kg。按运动员所从事的运动项目分为7个亚组:田径(105)、游泳(107)、赛艇(233)、摔跤、拳击和柔道(225)、举重(47)、各种团体项目(92)和其他项目(67)。取肘静脉静脉血,测定血清总胆固醇(CHOL)、高密度脂蛋白胆固醇(HDL-C)、甘油三酯(TG)浓度。计算各组、各变量的统计指标,并进行方差析因分析,评价差异的统计学意义。高训练组CHOL低于对照组(3.93 +/- 0.89比4.31 +/- 0.76 mmol/l, p < 0.001),高训练组男生CHOL低于高训练组女生CHOL(3.88 +/- 0.71比4.02 +/- 0.89 mmol/l, p < 0.01)。与对照组相比,训练组HDL-C较低(1.43 +/- 0.59 vs 1.60 +/- 0.57 mmol/l, p < 0.001)。在训练组和对照组的男孩和女孩之间没有发现HDL-C的差异。高训练组血清TG高于对照组(1.01 +/- 0.59 vs. 0.89 +/- 0.38 mmol/l, p < 0.001)。研究结果表明:(a)受过训练的青少年血清总胆固醇低于未受过训练的同龄男孩和女孩;(b)受过训练的青春期男孩血清总胆固醇低于受过训练的青春期女孩;(c)血清TG水平与青春期体育锻炼类型无关;(d)长期运动不能降低男女血清HDL-C水平;(e)运动对青春期血清总胆固醇的影响大于性行为。
{"title":"Serum lipid profile in pubescent athletes.","authors":"Z Taralov, N Boyadjiev, K Georgieva","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Physical activity has a beneficial effect on the serum lipid profile in adolescent and mature humans. The aim of the study was to compare the basic serum lipid parameters of pubescent athletes practicing different sports with those of untrained boys and girls and to investigate the relationship between the variations of the values of these variables and the respective type of sport practiced. 876 highly trained athletes (559 boys and 317 girls) were included in this study. Their mean (+/- SD) age, weight and duration of training were: 14.01 +/- 1.78 years; 56.24 +/- 15.39 kg, and 3.52 +/- 2.07 years. The control group consisted of 357 untrained subjects (171 boys and 186 girls) with mean (+/- SD) age and weight 14.58 +/- 1.70 years and 57.75 +/- 12.66 kg. The group of athletes was divided into seven subgroups according to the sport practiced: athletics (n = 105), swimming (n = 107), rowing (n = 233), wrestling, box and judo (n = 225), weight lifting (n = 47), various team sports (n = 92), and other sports (n = 67). Venous blood samples were drawn from the cubital vein and the concentrations of serum total cholesterol (CHOL), HDL-cholesterol (HDL-C), and triglycerides (TG) were measured. Statistical indices were computed for each group and for each variable, and analysis of variance factorial analysis was performed to evaluate the statistical significance of the differences detected. The CHOL in highly trained group was found lower than in the control group (3.93 +/- 0.89 vs. 4.31 +/- 0.76 mmol/l, p < 0.001), and in highly trained boys the CHOL was lower than in highly trained girls (3.88 +/- 0.71 vs. 4.02 +/- 0.89 mmol/l, p < 0.01). The HDL-C was lower in the trained group in comparison with the control one (1.43 +/- 0.59 vs. 1.60 +/- 0.57 mmol/l, p < 0.001). No differences were found in HDL-C between boys and girls in both trained and control group. Serum TG were higher in highly trained group than in controls (1.01 +/- 0.59 vs. 0.89 +/- 0.38 mmol/l, p < 0.001). The results of the study indicate that (a) trained pubescents have lower serum total cholesterol than untrained boys and girls of the same age; (b) trained pubescent boys have lower serum total cholesterol than trained pubescent girls; (c) the level of serum TG is not relevant to the type of physical exercise in pubescence; (d) long-term sport practicing is not able to decrease serum HDL-C levels in both sexes; (e) sport affects serum total cholesterol to a greater degree than does sex in pubescence.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 1","pages":"3-8"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21961198","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dietary copper- and iron restriction was achieved by application of the whole milk diet to growing rats in the course of 50 days. Three distinct responses of cytosolic and mitochondrial aconitases as well as of antioxidant defense system (CuZnSOD, MnSOD, catalase and GSH) to the dietary copper- and iron deficiency were established in liver, kidney and heart from experimental rats. The results were discussed with a view to the participation of ROS-generating processes in copper- and iron-deficient state. Differences in oxidative stability of cytosolic and mitochondrial aconitase activity of both control and experimental rats were also found. The in vitro increased aconitase activity of cytosol and the unchanged one of mitochondria from liver upon exposure of preparations to air were proved in vivo upon dietary copper- and iron restriction. This finding was interpreted to suggest the existence of putative aconitase activity.
{"title":"Effect of dietary copper and iron restriction on aconitase activity and antioxidant capacity of liver, kidney and heart from growing rats.","authors":"S G Konstantinova, N G Jordanova, E M Russanov","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Dietary copper- and iron restriction was achieved by application of the whole milk diet to growing rats in the course of 50 days. Three distinct responses of cytosolic and mitochondrial aconitases as well as of antioxidant defense system (CuZnSOD, MnSOD, catalase and GSH) to the dietary copper- and iron deficiency were established in liver, kidney and heart from experimental rats. The results were discussed with a view to the participation of ROS-generating processes in copper- and iron-deficient state. Differences in oxidative stability of cytosolic and mitochondrial aconitase activity of both control and experimental rats were also found. The in vitro increased aconitase activity of cytosol and the unchanged one of mitochondria from liver upon exposure of preparations to air were proved in vivo upon dietary copper- and iron restriction. This finding was interpreted to suggest the existence of putative aconitase activity.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 2","pages":"33-42"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21963156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The mediators of non-adrenergic non-cholinergic (NANC) relaxation of cat gastric fundus were examined in vitro. Electrical field stimulation (EFS, 10 pulses train and 10 s train) induced tetrodotoxin (TTX) sensitive relaxations in the presence of atropine and guanethidine. Relaxation induced by vasoactive intestinal polypeptide (VIP) was abolished by alpha-chymotrypsin (alpha-CT). N omega-nitro-L-arginine (L-NNA) completely inhibited relaxation induced by EFS of 10 pulses train at all frequencies. L-NNA completely inhibited the relaxation induced by EFS of 10 s train at low frequencies but partly that at high frequencies; alpha-CT had an additive to L-NNA inhibitory effect on the relaxation. The results suggest a nitrergic nature of NANC relaxation in cat gastric fundus upon EFS of 10 pulses, and a nitrergic and peptidergic (VIP) nature of relaxations upon EFS of 10 s train.
{"title":"Nitrergic and peptidergic components of NANC relaxations of cat gastric fundus.","authors":"L Chernaeva","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The mediators of non-adrenergic non-cholinergic (NANC) relaxation of cat gastric fundus were examined in vitro. Electrical field stimulation (EFS, 10 pulses train and 10 s train) induced tetrodotoxin (TTX) sensitive relaxations in the presence of atropine and guanethidine. Relaxation induced by vasoactive intestinal polypeptide (VIP) was abolished by alpha-chymotrypsin (alpha-CT). N omega-nitro-L-arginine (L-NNA) completely inhibited relaxation induced by EFS of 10 pulses train at all frequencies. L-NNA completely inhibited the relaxation induced by EFS of 10 s train at low frequencies but partly that at high frequencies; alpha-CT had an additive to L-NNA inhibitory effect on the relaxation. The results suggest a nitrergic nature of NANC relaxation in cat gastric fundus upon EFS of 10 pulses, and a nitrergic and peptidergic (VIP) nature of relaxations upon EFS of 10 s train.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 1","pages":"27-31"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21961197","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Heme oxygenase (HO) is a microsomal enzyme involved in the degradation of heme and biliverdin and carbon monoxide, the former being subsequently converted to bilirubin by the cytosolic biliverdin reductase. Two isoenzymes transcribed from separate genes have been characterized. The HO-2 isoform is constitutively expressed and is present in high concentration in the brain and testes. In contrast, the HO-1 isoform is ubiquitous, found in large quantities in liver and spleen and can be induced by its own substrate, heme and by a variety of stress-associated agents. Both HO-1 and HO-2 mRNA and protein have been detected in endothelial and smooth muscle cells of arterial and venous blood vessels. Carbon monoxide (CO) from HO catalysis has been identified as an endogenous biological messenger and recent studies suggest its important role in the circulation. Similarly to nitric oxide (NO), CO inhibits platelet aggregation and relaxes blood vessels by activating soluble guanylyl cyclase (sGC) and elevating intracellular levels of cyclic guanosine-3',5'-monophosphate (cGMP). CO is a powerful vasodilator and together with NO may serve as an important modulator of vascular cell function.
{"title":"Heme oxygenase--carbon monoxide signalling pathway as a physiological regulator of vascular smooth muscle cells.","authors":"T Christova, Z Diankova, M Setchenska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Heme oxygenase (HO) is a microsomal enzyme involved in the degradation of heme and biliverdin and carbon monoxide, the former being subsequently converted to bilirubin by the cytosolic biliverdin reductase. Two isoenzymes transcribed from separate genes have been characterized. The HO-2 isoform is constitutively expressed and is present in high concentration in the brain and testes. In contrast, the HO-1 isoform is ubiquitous, found in large quantities in liver and spleen and can be induced by its own substrate, heme and by a variety of stress-associated agents. Both HO-1 and HO-2 mRNA and protein have been detected in endothelial and smooth muscle cells of arterial and venous blood vessels. Carbon monoxide (CO) from HO catalysis has been identified as an endogenous biological messenger and recent studies suggest its important role in the circulation. Similarly to nitric oxide (NO), CO inhibits platelet aggregation and relaxes blood vessels by activating soluble guanylyl cyclase (sGC) and elevating intracellular levels of cyclic guanosine-3',5'-monophosphate (cGMP). CO is a powerful vasodilator and together with NO may serve as an important modulator of vascular cell function.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 1","pages":"9-17"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21961199","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
R Bakalova, M Mileva, C Kutsev, G Zlateva, S Ribarov
The aim of the present work was to determine the pharmacodynamics of antioxidant effect of alpha-tocopherol and its derivatives (alpha-tocopheryl esters and chromanols with different chain-length) in the animal tissues, as well as the role of cytochrome P-450 in biotransformation of these compounds. Alpha-tocopherol and its derivatives were injected intraperitoneally in rats or mice in a single dose of 100 mmol per kg b.w. The animals were sacrificed at different time intervals (0, 1, 2, 4, 8, 12, 24, 36 hours) and the liver, heart, brain and skeletal muscles were removed, homogenized and incubated with lipid peroxidation (LPO) inducers (Fe2+ + ascorbate). LPO was evidenced by the generated malone dialdehyde (MDA). Data were expressed as percentage of LPO inhibition by alpha-tocopherol or its derivatives as compared to control group. The kinetic curves of the inhibitory action of alpha-tocopherol and its derivatives on LPO were characterized by three phases: a phase of increasing antioxidant activity, a phase of maximal antioxidant activity (about 60-95% LPO inhibition), and a phase of decreasing antioxidant activity. Alpha-tocopheryl esters possessed dynamics of antioxidant action the same as alpha-tocopherol. Therefore the hydrolysis of alpha-tocopheryl esters in animal organism is not a limiting factor for their antioxidant effect. The alpha-tocopherol derivatives with short chain-length (C1, C6) had a shorter half-life in animal tissues as compared to alpha-tocopherol or its esters. In vitro experiments showed that C1 and C6 are substrates of cytochrome P-450. In contrast, alpha-tocopherol and its esters did not bind to cytochrome P-450 even at concentrations as high as 10 mmol/l. Apparently, C1 and C6 underwent biotransformation and were excreeted more quickly from the organism.
{"title":"Pharmacodynamic of the antioxidant action of alpha-tocopherol and its derivatives in liver, brain, heart and skeletal muscles.","authors":"R Bakalova, M Mileva, C Kutsev, G Zlateva, S Ribarov","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of the present work was to determine the pharmacodynamics of antioxidant effect of alpha-tocopherol and its derivatives (alpha-tocopheryl esters and chromanols with different chain-length) in the animal tissues, as well as the role of cytochrome P-450 in biotransformation of these compounds. Alpha-tocopherol and its derivatives were injected intraperitoneally in rats or mice in a single dose of 100 mmol per kg b.w. The animals were sacrificed at different time intervals (0, 1, 2, 4, 8, 12, 24, 36 hours) and the liver, heart, brain and skeletal muscles were removed, homogenized and incubated with lipid peroxidation (LPO) inducers (Fe2+ + ascorbate). LPO was evidenced by the generated malone dialdehyde (MDA). Data were expressed as percentage of LPO inhibition by alpha-tocopherol or its derivatives as compared to control group. The kinetic curves of the inhibitory action of alpha-tocopherol and its derivatives on LPO were characterized by three phases: a phase of increasing antioxidant activity, a phase of maximal antioxidant activity (about 60-95% LPO inhibition), and a phase of decreasing antioxidant activity. Alpha-tocopheryl esters possessed dynamics of antioxidant action the same as alpha-tocopherol. Therefore the hydrolysis of alpha-tocopheryl esters in animal organism is not a limiting factor for their antioxidant effect. The alpha-tocopherol derivatives with short chain-length (C1, C6) had a shorter half-life in animal tissues as compared to alpha-tocopherol or its esters. In vitro experiments showed that C1 and C6 are substrates of cytochrome P-450. In contrast, alpha-tocopherol and its esters did not bind to cytochrome P-450 even at concentrations as high as 10 mmol/l. Apparently, C1 and C6 underwent biotransformation and were excreeted more quickly from the organism.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 1","pages":"19-26"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21961196","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The effects of i.c.v. administered peptide and nonpeptide ANG II-receptor ligands (losartan, EXP 3174, saralasin and sarmesin) on monoamine oxidase A (MAO-A) and MAO-B activities in the frontal cortex, striatum, hypothalamus and hippocampus of water-repleted rats were investigated. Alterations in MAO-A and MAO-B activities were found in different rat brain regions after ANG II which depended on the isoenzyme type and brain structure. MAO-A activity significantly increased in the frontal cortex and hypothalamus, brain regions containing AT1 receptors, mainly. MAO-A and MAO-B activities were affected differently by all studied ANG II-receptor ligands, which in most cases antagonized the effect of ANG II (losartan, an AT1-nonpeptide receptor antagonist being the most effective). There was no clearcut relationship between the inhibition of ANG II-induced water intake and the changes of MAO-A and MAO-B activities under the effect of the ANG II-receptor antagonists studied.
{"title":"The effects of peptide and nonpeptide angiotensin II-receptor ligands on the activity of brain monoamine oxidase in water-repleted rats.","authors":"S Stancheva, L Alova, V Georgiev","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The effects of i.c.v. administered peptide and nonpeptide ANG II-receptor ligands (losartan, EXP 3174, saralasin and sarmesin) on monoamine oxidase A (MAO-A) and MAO-B activities in the frontal cortex, striatum, hypothalamus and hippocampus of water-repleted rats were investigated. Alterations in MAO-A and MAO-B activities were found in different rat brain regions after ANG II which depended on the isoenzyme type and brain structure. MAO-A activity significantly increased in the frontal cortex and hypothalamus, brain regions containing AT1 receptors, mainly. MAO-A and MAO-B activities were affected differently by all studied ANG II-receptor ligands, which in most cases antagonized the effect of ANG II (losartan, an AT1-nonpeptide receptor antagonist being the most effective). There was no clearcut relationship between the inhibition of ANG II-induced water intake and the changes of MAO-A and MAO-B activities under the effect of the ANG II-receptor antagonists studied.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 2","pages":"51-6"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21963158","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Short (up to 60 s) supramaximal (about 400 W on the average) exercise is accompanied by specific biochemical processes in the working muscles and by a general increase in energy metabolism. Outwardly, this is manifested by an excess post-exercise oxygen consumption (EPOC). Since its actual measurement is time consuming and associated sometimes with difficulties, we propose a fixed 3-min test for EPOC prediction. The measured volumes of oxygen consumption are related to the corresponding periods in a coordinate system as reciprocal values. The linear equation, whose parameters were calculated by the method of least squares or were determined graphically, provided for prediction of the EPOC volume with satisfactory accuracy and precision. The obtained increase of the predicted values over the actually measured values was below 5%, and the correlation coefficient r = 0.98. Other parameters of the recovery process were also calculated, such as tau (half-time) of EPOC and the rate constant k.
{"title":"Prediction method for the volume of the excess post-exercise oxygen consumption (EPOC) following supramaximal exercise.","authors":"D Stefanova","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Short (up to 60 s) supramaximal (about 400 W on the average) exercise is accompanied by specific biochemical processes in the working muscles and by a general increase in energy metabolism. Outwardly, this is manifested by an excess post-exercise oxygen consumption (EPOC). Since its actual measurement is time consuming and associated sometimes with difficulties, we propose a fixed 3-min test for EPOC prediction. The measured volumes of oxygen consumption are related to the corresponding periods in a coordinate system as reciprocal values. The linear equation, whose parameters were calculated by the method of least squares or were determined graphically, provided for prediction of the EPOC volume with satisfactory accuracy and precision. The obtained increase of the predicted values over the actually measured values was below 5%, and the correlation coefficient r = 0.98. Other parameters of the recovery process were also calculated, such as tau (half-time) of EPOC and the rate constant k.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 2","pages":"63-8"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21963160","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
V D Petkov, E Konstantinova, V V Petkov, S Belcheva, R Kehayov, J Vaglenova
In experiments on Wistar and Long Evans rats, using behavioral methods for passive (step-down and step-through) and active (shuttle-box two-way avoidance with punishment reinforcement) the newly synthesized diphenyl-methyl-piperazine derivative with Ca2+ and 5-HT antagonistic action dotarizine (DOT) administered repeatedly at oral doses of 50 and 10 mg/kg in some cases improve memory process. Under the same experimental conditions the chemically related to dotarizine Ca2+ antagonist flunarizine significantly facilitated retention. In old (Long Evans and Wistar) rats DOT in large dose decreases values of learning criterion. Probably this is a manifestation of the inherent to drugs with nootropic action "therapeutic window". Earlier investigations of the same and other authors suggest the participation of serotonergic neurotransmission in the mechanism of the memory effects of the drug DOT.
{"title":"Memory effects of the Ca2+ and 5-HT antagonists dotarizine and flunarizine.","authors":"V D Petkov, E Konstantinova, V V Petkov, S Belcheva, R Kehayov, J Vaglenova","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In experiments on Wistar and Long Evans rats, using behavioral methods for passive (step-down and step-through) and active (shuttle-box two-way avoidance with punishment reinforcement) the newly synthesized diphenyl-methyl-piperazine derivative with Ca2+ and 5-HT antagonistic action dotarizine (DOT) administered repeatedly at oral doses of 50 and 10 mg/kg in some cases improve memory process. Under the same experimental conditions the chemically related to dotarizine Ca2+ antagonist flunarizine significantly facilitated retention. In old (Long Evans and Wistar) rats DOT in large dose decreases values of learning criterion. Probably this is a manifestation of the inherent to drugs with nootropic action \"therapeutic window\". Earlier investigations of the same and other authors suggest the participation of serotonergic neurotransmission in the mechanism of the memory effects of the drug DOT.</p>","PeriodicalId":7035,"journal":{"name":"Acta physiologica et pharmacologica Bulgarica","volume":"25 2","pages":"43-50"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21963157","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}