喹噁啉类药物对醛固酮合成和分泌影响的研究进展

喹噁啉类药物的肾上腺毒性作用主要表现为对醛固酮合成和分泌的影响。随着喹噁啉类药物作为抗菌促生长剂在畜牧业中的广泛应用,其肾上腺毒性逐渐受到关注。本文从醛固酮合成过程和肾素-血管紧张素-醛固酮系统这两方面,综述了近年来该类药物对醛固酮影响的研究进展,旨在为后期进一步揭示喹噁啉类药物的肾上腺毒性做出贡献。     

规模养鸡场分离的大肠杆菌和金黄色葡萄球菌的药敏试验

通过对规模养鸡场的环境和鸡的口腔、泄殖腔采样,培养分离出大肠杆菌和金黄色葡萄球菌,进行常见15种抗菌药物的药敏试验,发现规模养鸡场分离的大肠杆菌对庆大霉素、妥布霉素、头孢拉定、头孢曲松、卡拉霉素、林可霉素等较敏感,而对土霉素、青霉素、头孢唑啉、头孢氨苄、磺胺异噁唑等耐药;金黄色葡萄球菌对氟苯尼考、头孢拉定、头孢唑啉、头孢曲松、卡拉霉素等较敏感,而对于青霉素、氨苄西林、红霉素、林可霉素、土霉素、庆大霉素、妥布霉素、恩诺沙星、磺胺异噁唑等耐药。通过实验也了解到规模养殖场养殖年限和环境内细菌的耐药性存在着正相关关系,而与鸡体内的细菌耐药性关系不大。     

新型异噁唑啉类化合物氟雷拉纳研究应用现状

异噁唑啉类是一类新型抗寄生虫药物,氟雷拉纳（fluralaner）作为异噁唑啉类的成员,对节肢动物γ–氨基丁酸和L–谷氨酸门控氯通道具有选择性抑制作用,目前广泛用于治疗犬和猫的体外寄生虫。与其他类杀虫剂相比,氟雷拉纳具有操作简单、易吸收、安全、高效、长效以及良好的耐受性等特点。本文围绕氟雷拉纳的作用机制与药代动力学特征、临床研究现状以及临床安全性展开充分的总结与归纳。以期为氟雷拉纳在科研、消费以及应用范围等方面,提供有价值参考。     

禁抗前后规模鸡场环境中金黄色葡萄球菌和大肠杆菌对15种抗菌药的敏感性比较

为了解规模鸡场两种环境细菌在禁抗前后耐药性的变化,以评估使用抗菌药对养殖场用药的影响,通过对禁抗前以及禁抗6个月后规模鸡场的环境进行采样,培养分离大肠杆菌和金黄色葡萄球菌(金葡菌),然后针对15种常见抗菌药物开展药敏试验,并对敏感性进行比对。结果显示:禁抗前规模鸡场分离的大肠杆菌对妥布霉素、林可霉素、头孢拉定、卡拉霉素等较敏感,而对磺胺异噁唑、土霉素、头孢唑林和青霉素等耐药;金葡菌对头孢曲松、卡拉霉素、头孢唑啉、氟苯尼考等较敏感,而对土霉素、磺胺异噁唑、庆大霉素、妥布霉素等耐药。禁抗6个月后,两种细菌对大部分抗菌药的敏感性都有不同程度的增加,但对土霉素、磺胺异噁唑、氟苯尼考、青霉素等的敏感性增加不多甚至有降低。结果表明禁抗总体上可以增强鸡场环境中两种细菌对抗菌药的敏感性,降低耐药性。本文为指导规模鸡场禁用和科学使用抗菌药物提供了数据支持。     

高效液相色谱法测定鹅肉中磺胺类药物的残留

建立了一种快速、准确测定鹅肉中磺胺类药物残留量的检测方法。采用高效液相色谱法测定鹅肉中磺胺类药物的残留,以Cloversil C18色谱柱,甲醇-1%乙酸水溶液作为流动相进行梯度洗脱。柱温30℃,进样量5μL,流速0.6 mL/min,240-280nm波长紫外检测。经测定,鹅肉中含有磺胺嘧啶、磺胺甲基异噁唑、磺胺噻唑、磺胺二甲嘧啶和磺胺喹噁啉等磺胺类物质。     

氟喹诺酮类药物粉剂中非法添加四种喹噁啉类药物的UPLC检测方法研究

建立了超高效液相色谱法测定氟喹诺酮类药物粉剂中非法添加喹乙醇、乙酰甲喹、卡巴氧及喹烯酮的方法。采用purospher RP-18色谱柱(2.1 mm×100 mm,粒径2.0μm)分离四种喹噁啉类药物,以磷酸溶液和甲醇-乙腈(7.5∶7.0)为流动相进行梯度洗脱,流速0.3 m L/min,二极管阵列检测器检测,采集波长范围为200~400 nm,分辨率为1.2 nm,记录光谱图和365 nm波长处的色谱图。结果显示,四种喹噁啉类药物的浓度在0.2~100μg/m L范围内的线性良好,相关系数r均为0.9999,回收率在98.0%~100.2%范围内,RSD在0.27%~0.89%之间,检测限200 mg/kg。本方法快速、准确,可用于氟喹诺酮类粉剂中非法添加喹噁啉类药物的定性和定量检测。     

喹噁啉类药物抗肿瘤与抗菌活性的研究进展

喹噁啉类药物是畜牧生产中大量使用的抗菌促生长添加剂,同时在医药领域也进行着大量的研究,在国际上得到广泛的重视。主要介绍了目前国内外在喹噁啉类药物在抗肿瘤和抗菌生物活性方面作用的研究进展,并且探讨了其作用的机理。     

新型抗球虫药预防盲肠球虫病的效果实验

为了解鸡球虫对新型合成化学物敏感性程度,开发新型抗球虫药物提供科学依据,本试验选择了4种新型合成化学物,分别为磺胺喹噁啉钠溶液,复方磺胺喹噁啉钠溶液A,复方磺胺喹噁啉钠溶液B,黑球粉(6%癸氧喹酯),并以抗球虫指数ACI为指标考察了以上4种新型合成化学物防治鸡球虫病的作用效果。     

HPLC法同时测定禽肉中氯羟吡啶和多种磺胺类药物残留

建立了用于禽肉中氯羟吡啶和磺胺嘧啶、磺胺甲基嘧啶、磺胺二甲基嘧啶、磺胺甲氧嘧啶、磺胺-6-甲氧嘧啶、磺胺甲基异噁唑、磺胺二甲氧嘧啶、磺胺喹噁啉等残留测定的高效液相色谱法。样品以乙腈-氯仿提取,正己烷脱脂净化,以Symmetry C18 5μm(4.6 mm×150 mm)色谱柱进行分离,二极管阵列检测器检测,梯度洗脱测定氯羟吡啶和8种磺胺。回收率在71.7%~99.7%,相对标准偏差为1.5%~3.8%,最低检测限除磺胺二甲氧嘧啶、磺胺喹噁啉为0.02 mg/kg外,其余都可达到0.01 mg/kg。该方法已成功应用于禽类样品多兽药残留的检测。     

喹噁啉类药物致HepG2细胞DNA损伤与修复

喹噁啉类药物是一类人工合成的、含有喹噁啉-1,4-二氧化物基本结构的抗菌促生长剂.这类药物具有提高饲料转化率、促进动物生长和广谱的抗菌作用,因而在国内外被广泛应用.但本类早期产品喹乙醇和卡巴氧由于对人和动物有不同程度的毒副作用已经被禁止或严格限制使用[1].     

匹莫苯丹的合成工艺研究进展

匹莫苯丹是国家二类新兽药。但由于该药的原料药成本较高,不易合成,反应步骤多而限制了该药物的临床普遍应用。因此,进行了对匹莫苯丹合成工艺的调查,概述了近年来国内外关于匹莫苯丹的10个合成方法。主要包括以氯苯、乙酰苯胺、对氯苯甲醛、3-(4-乙酰胺基苯甲酰基)-丁腈、邻苯二乙酸二铵和5-(2-溴代丙酰基)-1,3-2H-苯丙[d]咪唑-2-酮为起始原料合成制备匹莫苯丹,并分析了这些合成方法中存在的问题,还考察了匹莫苯丹副产物的产生和解决办法,为其工业化合成研究提供参考。     

7-氨基头孢烷酸分子印迹聚合物的制备及结合性能评价

以头孢类药物的母核7-氨基头孢烷酸为模板分子、4-乙烯基吡啶为功能单体在一定条件下合成7-氨基头孢烷酸分子印迹聚合物,用平衡结合实验研究了聚合物的结合性能。并研究了7-氨基头孢烷酸分子印迹聚合物对头孢类药物的选择性。结果表明,7-氨基头孢烷酸分子印迹聚合物对头孢类药物有很好的选择性,能够作为畜禽食品中头孢类药物萃取净化的分离材料。     

Potential interactions between non-steroidal anti-inflammatory drugs and other drugs

Objective: The objective of this review is to summarize what is known in human and veterinary patients regarding the potential interactions of non‐steroidal anti‐inflammatory drugs (NSAIDs) with clinically important drugs. Data sources: Relevant articles as identified through searches of Medline, 1985 to present. Human data synthesis: Hemodynamic drug interactions are most likely to cause clinically relevant problems in humans, in which NSAIDs blunt the response to anti‐hypertensive agents and diuretics in patients with cardiovascular disease, or cause renal decompensation in patients with hypovolemia. In addition, NSAIDs enhance the ulcerogenic effects of glucocorticoids or other recently administered NSAIDs, and can increase bleeding from anti‐coagulant drugs or from herbs with platelet inhibitory activities. Veterinary data synthesis: Although there are numerous studies examining the safety and efficacy of various NSAIDs in healthy or arthritic dogs, there are very few studies that address the safety of these agents in veterinary patients receiving medication for other acute or chronic conditions. Conclusions: Based upon what is known in humans, more studies are needed in veterinary patients to assess the safety of NSAIDs in those animals being treated with anti‐hypertensive, diuretic or anti‐coagulant drugs.     

氟喹诺酮类药物残留检测方法研究进展

药物残留直接危害人体健康,近年来畜产品中药物残留问题倍受关注.氟喹诺酮类药物残留检测的方法较多,同时也获得了大量的试验数据.常用的方法有微生物法、免疫分析测定法、免疫亲和色谱-液相色谱法、高效液相色谱法、高效毛细管电泳法、液相色谱-质谱-质谱法、薄层色谱法、荧光分光光度法等.文章对这些检测方法从定性(筛选)和定量两个方面进行综述.     

Nonsteroidal antiinflammatory drugs: a review

The increasing use of nonsteroidal antiinflammatory drugs (NSAIDs) in small animals has resulted in the development of new and innovative additions to this class of drugs. Examples of NSAIDs now available for use in small animals include aspirin, etodolac, carprofen, ketoprofen, meloxicam, deracoxib, and tepoxalin. The purposes of this article are to review the pathophysiology of prostaglandin synthesis and inhibition, the mechanisms of action, pharmacokinetics, pharmacological effects, and potential adverse reactions of aspirin and the newly released NSAIDs.     

Applications of equine models of acute inflammation. The Ciba-Geigy Prize for Research in Animal Health

The development of reproducible models of acute inflammation in which inflammatory heat is easily quantified and from which inflammatory exudate is readily harvested has facilitated studies in the horse of the actions of steroids and non-steroidal anti-inflammatory drugs (NSAIDS). Blockade of the synthesis of eicosanoids and suppression of inflammatory heat by clinical dose rates of NSAIDS suggests a causal link between the two events and provides further evidence for a role of these compounds in acute equine inflammation. The tendency for enolic and carboxylic acids NSAIDS to accumulate in inflammatory exudate may account for the duration of action of these compounds in inhibiting exudate eicosanoid synthesis and the data confirm clinical experiences with these drugs. A novel NSAID which inhibits both cyclo-oxygenase and lipoxygenase pathways of arachidonic acid metabolism, BW540C, and two anti-inflammatory steroids, betamethasone and dexamethasone, have been evaluated in the models of equine inflammation with some interesting and unexpected findings. This paper emphasises the interrelationships between the inflammatory process and the actions and fate of anti-inflammatory drugs.     

动物抗寄生虫药物作用机理研究进展

动物抗寄生虫药物主要用于防制动物寄生虫病,是保障畜牧业健康发展和公共卫生安全的有效手段。抗寄生虫药物的药效建立在药物分子与寄生虫或动物机体不同靶组织、靶细胞间相互作用的基础上。由于抗寄生虫药物种类多样,抗寄生虫机理复杂。随着新抗寄生虫药物的开发和科学研究的深入,尤其是化学合成和生物制药技术的发展,抗寄生虫药物的品种和数量都在不断的增加,新的药物结构和作用靶标不断发现,作用机理研究也不断深入。作者主要对抗寄生虫药物的作用机理研究进展进行综述。     

Research Progress on Action Mechanism of Animal Anti-parasitical Drugs

Animal anti-parasitical drugs are mainly used to prevent and control animal parasitosis, and also an effective way to protect the healthy development of animal husbandry and public health security.The efficacy of anti-parasitical drugs depends on the interaction between drug molecular and different target tissues and target cells of parasite or animal.Because of the variety of anti-parasitical drugs, the anti-parasitical mechanisms are complex.With the development of new anti-parasitical drugs and the depth of scientific research, especially the development of chemical synthesis and biological pharmaceutical technology, the variety and quantity of anti-parasitical drugs constantly increase.With the discovery of new drug structure and its action target, the study on the mechanism is constantly deep.The author mainly summarized the research progress on action mechanism of anti-parasitical drugs.     

Effects of three antiarthritic drugs on fibronectin and keratan sulfate synthesis by cultured canine articular cartilage chondrocytes.

Because articular chondrocytes are a target for drugs that can influence the integrity of cartilage, we investigated the effects of 3 antiarthritic drugs, glycosaminoglycan polysulfate, diclofenac-Na, and S-adenosylmethionine sulfate p-toluenesulfonate on total protein, fibronectin, and DNA synthesis, as well as on extradomain-A fibronectin and keratan sulfate content. Glycosaminoglycan polysulfate stimulated dose-dependent incorporation of [35S]methionine into protein and fibronectin, whereas incorporation of [3H]thymidine into DNA was unaffected. Total fibronectin, extradomain-A fibronectin, and keratan sulfate content were high in chondrocyte cultures treated with glycosaminoglycan polysulfate. In contrast, fibronectin and DNA synthesis, as well as extradomain-A fibronectin and keratan sulfate content were unaffected by diclofenac-Na. S-Adenosyl-methionine decreased dose-dependently the synthesis of fibronectin, as well as the content of fibronectin and keratan sulfate. At the highest concentration of S-adenosyl-methionine tested, findings suggest that cell viability was impaired as assessed by the release of lactate dehydrogenase into the media.