谷氨酰胺的抗疲劳生化机制研究

用两批各 48只小鼠分 4组 (n =12 )每天分别灌喂生理盐水和 3 4mmol·kg-1的谷氨酰胺、谷氨酸和天冬酰胺 ,连续 10d。结果显示 ,三者都可提高小鼠血清、肝和骨骼肌中的肌酸磷酸激酶活性 ,降低乳酸脱氢酶活性 ,并显著增加肝、骨骼肌糖原积累。其中有相同碳架结构的谷氨酰胺、谷氨酸能极显著提高小鼠的游泳耐力 ,但与谷氨酰胺有相等酰胺氮的天冬酰胺作用不强。结果提示 ,谷氨酰胺提高机体抗疲劳作用与其碳架结构有关     

Hypoglycemic effect of lupin seed γ-conglutin in experimental animals and healthy human subjects

A lupin seed γ-conglutin-enriched preparation was tested in a glucose overload trial with both murine models and adult healthy volunteers. The results with rats showed a dose-dependent significant decrease of blood glucose concentration, which confirmed previous findings obtained with the purified protein. Moreover, three test-product doses equivalent to 630, 315, and 157.5 mg γ-conglutin, orally administered 30 min before the carbohydrate supply, showed a relevant hypoglycemic effect in human trials. Insulin concentrations were not significantly affected. The general hematic parameters did not change at all.This is the first report on the glucose-lowering effect of lupin γ-conglutin in human subjects.     

恩诺沙星缓释溶液在猪体内的药物动力学及生物利用度

选用18头健康猪进行恩诺沙星普通溶液静脉注射、肌肉注射和恩诺沙星缓释溶液肌肉注射的药物动力学研究,比较了2种溶液在猪体内的药物动力学特征和生物利用度。结果表明:静脉注射给药的药时数据适合无吸收二室开放模型,主要药物动力学参数为t1/2α=0 726±0 164h,t1/2β=9 083±1 121h,Vd=4 364±0 565L/kg,ClB=0 336±0 053L/(kg·h),AUC=30 397±4 895mg·h/L。肌肉注射恩诺沙星缓释溶液和普通溶液的药时数据均符合一级吸收二室模型,其主要药物动力学参数分别为:t1/2ka=0 468±0 114h和t1/2α=0 415±0 195h;t1/2β=25 818±6 528h和t1/2β=9 460±2 946h(P<0 01);Tmax=1 498±0 194h和Tmax=1 347±0 393h;Cmax=2 206±0 555μg/mL和Cmax=2 561±0 152μg/mL;AUC=23 715±3 528mg·h/L和AUC=18 397±1 808mg·h/L(P<0 01);F=(78 02±11 61)%和F=(60 52±5 95)%。肌肉注射恩诺沙星缓释溶液和普通溶液的主要药物动力学参数t1/2β和AUC有显著性差异,其他指标均无显著性差异。恩诺沙星缓释溶液既有速释部分(与普通溶液相比吸收半衰期不变),又有缓释部分(消除半衰期延长),应用于临床其有速效和长效双重作用。     

奶牛慢性子宫内膜炎的治疗试验

选用乳酸环丙沙星、中药“孕宝”制剂两种药物对134头患有慢性子宫内膜炎的奶牛进行治疗对比试验。结果表明，乳酸环丙沙星治疗慢性卡他性子宫内膜炎、慢性卡他性脓性子宫内膜炎、隐性子宫内膜炎的治愈率分别为79．17％、72．73％、71．43％；“孕宝”治疗此3种慢性子宫内膜炎的治愈率分别为93．10％、72．73％、83．33％。乳酸环丙沙星治疗慢性卡他性脓性子宫内膜炎的效果优于“孕宝”，“孕宝”治疗慢性卡他性子宫内膜炎和隐性子宫内膜炎的效果则高于乳酸环丙沙星。     

恩诺沙星微胶囊的制备及其抗紫外、热稳定性的研究

采用冷冻干燥法，分别以羧甲基纤维素和淀粉为壁材，制备恩诺沙星微胶囊制剂。抗紫外和热稳定性试验表明：以羧甲基纤维素和淀粉为壁材的恩诺沙星微胶囊均有抗紫外和热稳定性能。其中，羧甲基纤维素与恩诺沙星、淀粉与恩诺沙星包埋质量比为1：1、1：2时，微胶囊表现出显著的抗紫外作用（P〈0．05）；羧甲基纤维素与恩诺沙星、淀粉与恩诺沙星包埋质量比为2：1、1：1、1：2时，微胶囊表现出极显著的热稳定性（P〈0．01）。羧甲基纤维素的抗紫外和热稳定性均优于淀粉，但差异不显著。     

高精料条件下延胡索酸对山羊瘤胃微生物体外发酵的影响

通过山羊瘤胃液的体外批次培养,研究延胡索酸对瘤胃混合细菌体外发酵的影响。瘤胃液在含底物(玉米粉、豆粕和黑麦草)和延胡索酸(0、4、8和12 mmol.L-1)条件下发酵24 h。结果表明,在整个发酵期内,不同浓度的延胡索酸均显著提高了累积产气量,同时显著影响总挥发性脂肪酸(TVFA)浓度及其组成,降低乙酸的浓度及比例,增加丙酸的浓度及比例。其中4 mmol.L-1延胡索酸在12~24 h提高了TVFA浓度和丙酸浓度(P<0.05),8 mmol.L-1组和12 mmol.L-1组的TVFA浓度和丙酸浓度在16 h和24 h也有显著提高(P<0.05)。在12、16、20和24 h时,3个添加组乙酸比例均显著低于对照组(P<0.05),而丙酸比例则明显提高(P<0.01),乙酸和丙酸的比值显著降低(P<0.05)。4 mmol.L-1延胡索酸添加组的乳酸浓度在12、16、20和24 h均极显著低于对照组(P<0.01)。结果提示,延胡索酸能显著提高瘤胃微生物体外发酵液中TVFA及丙酸比例,其中4 mmol.L-1延胡索酸对于调控瘤胃微生物体外发酵效果最佳。     

Clinical evaluation of serum alcohol dehydrogenase activity in horses with acute intestinal obstruction

Objectives – To measure serum alcohol dehydrogenase (ADH) activity in horses with acute intestinal obstruction and to determine the diagnostic and prognostic utility of this analyte. Design – Prospective observational study. Setting – University Veterinary Hospital. Animals – Thirty healthy horses (control group) and 77 horses with acute intestinal obstruction, including 36 horses with nonstrangulating obstruction (23 with left ventral colon impaction and 13 with left dorsal displacement [G1], 22 with small intestinal strangulation [G2], and 19 with colon torsion [G3]). Interventions – Serum ADH activity was assayed spectrophotometerically in all horses. Serum lactate concentration and hepatic enzyme (aspartate aminotransferase, gamma‐glutamyl transferase, glutamate dehydrogenase) activities were measured using an automatic analyzer. Measurements and Main Results – The median [interquartile range] serum ADH activity in healthy horses was 10.5 [8.7 – 11 U/L]. ADH activity was significantly increased (P<0.05) in G1=16.5 [13.8 – 18 U/L], G2=40 [20 – 74.9 U/L], and G3=63.2 [40 – 78 U/L] compared with healthy controls. Aspartate aminotransferase and glutamate dehydrogenase activities were also significantly increased in G3 in comparison with controls. ADH activity was correlated with serum lactate concentration in G1 and G3, respectively (P<0.01, r=0.55 and 0.8). Other liver enzymes did not show any significant correlation with lactate. ADH activity was directly related to the probability of strangulation; odds ratio=1.11. ADH activity >20 U/L had 80.6% specificity and 80.5% sensitivity for discriminating horses with strangulating obstruction. Twelve horses euthanized before surgery were excluded from the outcome analysis. Increasing ADH activity was associated with nonsurvival; odds ratio=1.03. ADH activity <80 U/L had 94.44% specificity and 66.67% sensitivity for survival. Conclusion – Serum ADH activity may be a useful clinical parameter in detecting intestinal strangulation in horses and may provide some prognostic value in horses with acute intestinal obstruction.     

恩诺沙星混悬液在猪体内残留消除规律研究

采用高效液相色谱法研究恩诺沙星(口服)混悬液在猪体内各组织中的残留消除规律.恩诺沙星(口服)混悬液,按每头猪10 mg/kg体重的剂量灌服给药,连续使用3 d之后,宰杀猪,取组织.组织样品经磷酸盐缓冲液提取,C18固相萃取柱净化,过膜,用流动相0.05 mol/L磷酸溶液/三乙胺一乙腈(82+18)溶解,微孔过滤,进行...     

兽用微囊制剂的研究进展

微囊技术是一种利用天然的或合成的高分子成膜材料把液体或固体药物包嵌形成直径1μm-500μm微小胶囊的技术。微囊具有良好的溶解分散、缓释、抗外界干扰等性能,被广泛应用于医药、化工、生物、食品和饲料等众多领域。从20世纪90年代开始,微囊化技术逐步应用到动保行业中,如恩诺沙星微囊制剂、替米考星微囊制剂、吉他霉素微囊制剂等。     

Hepatoprotective activity of angiotensin-converting enzyme (ACE) inhibitors, captopril and enalapril, against paraquat toxicity

Paraquat is a highly toxic herbicide that is used in most countries without restriction. The cytotoxic action of paraquat is mediated by reactive radicals that are products of its metabolic reduction in cells. It has already been hypothesized that some angiotensin-converting enzyme inhibitors (e.g., captopril and enalapril) could show antioxidant and radical scavenging activity through their structural thiol groups, increasing antioxidant enzymes production or nitric oxide synthesis. In this study the hepatoprotective effect of captopril and enalapril against paraquat induced oxidative stress cytotoxicity was evaluated in isolated rat hepatocyte. Subtoxic concentrations of captopril (0.2 mM) and enalapril (0.2 mM) significantly (p < 0.05) protected the hepatocytes against paraquat (2 mM) induced oxidative stress cytotoxicity markers including: cell lysis, reactive oxygen species (ROS) generation, lipid peroxidation, glutathione depletion, mitochondrial membrane potential decrease, lysosomal membrane oxidative damage and cellular proteolysis. Moreover, we showed that non-thiol enalapril acts as well as thiol containing captopril at inhibiting oxidative stress cytotoxicity markers. Finally, our results support the hypothesis that it is the increase in nitric oxide synthesis and not the presence of the thiol group that accounts for the antioxidant activity of ACE inhibitors.