抗菌新药替米考星在兽医临床应用简介

替米考星（Tilmicosin）化学名为4A-O-脱（2，6-二去氧-3-C-甲基-L-核糖-吡喃已基）-20-脱氧-20-（3，5-二甲基-1-哌啶基）泰乐菌素，又名20-去氧-20-（3，5-二甲基-1-哌啶基）脱碳霉糖泰乐菌素，是一种以泰乐菌素为前体半合成的大环内酯类畜禽专用抗生素，二十世纪八十年代由英国Elanco动物保健品公司首先开发成功。     

变温培养对泰乐菌素发酵的影响

在泰乐菌素发酵过程中的不同阶段采用不同的培养温度,通过实验考察其对泰乐菌素发酵的影响。实验结果表明,变温培养的发酵水平要高于其它恒温培养的发酵水平。     

白僵菌对大黄酸的葡萄糖基化作用研究

目的：利用白僵菌的生物转化功能，生物合成大黄酸的葡萄糖基化衍生物。方法：在白僵菌培养液中加入大黄酸底物，利用生长细胞对其进行生物转化。结果：确定大黄酸的糖基化衍生物为：3-羟甲基-β-D-葡萄糖，芦茎大黄素醇苷。结论：白僵菌对大黄酸具有时羰基的还原以及葡萄糖基化生物转化作用，合成的3-羟甲基-β-D-葡萄糖-芦荟大黄素醇苷为新的大黄酸衍生物。     

雷公藤内酯及蟾毒配基类化合物的生物转化研究进展

生物转化(biotransformation)是利用生物体系或其产生的酶对外源性化合物进行结构修饰的生物化学过程,其本质为酶催化反应[1,2].生物转化反应具有选择性强,催化效率高,反应条件温和,反应类型多,以及环境污染小等特点,且往往可用于催化有机合成方法难以完成的化学反应,易于得到结构新颖的化合物.因此,生物转化技术作为合成方法的有力补充,已成为有机化学家的重要研究工具之一.目前采用生物转化技术已获得了大量新颖的化学结构,包括很多天然产物衍生物,为新药的研制与开发提供了极有价值的先导化合物.有的生物转化反应还达到了工业化生产的规模,创造了巨大的经济效益[3].     

几种蒽醌衍生物的合成

对靶向抗生素中的蒽环抗生素进行了介绍,简明阐述了其作用机理及研究价值,并且合成了几种蒽醌衍生物.     

富勒烯功能高分子材料的制备与性能研究

对富勒烯功能高分子材料的制备、表征及其性能研究已成为光前国际上的前沿领域之一。从合成角度考虑,以不同的方法对Ｃ６０进行高分子修饰可得到结构、性质各异的富勒烯高分子衍生物,对于研究如何更好地控制Ｃ６０高分子衍生物的结构,探讨了有Ｃ６０参与的聚合反应的机理以及Ｃ６０在高分子衍生物中的作用无疑是很有帮助的。从应用角度考虑,Ｃ６０引入高分子中必将导致新型聚合物的产生。这些新型聚合物表现出许多独特而极具应用     

用微生物转化法合成4-孕甾-3,20-二酮的羟基类衍生物

目的:合成具有潜在活性的4-孕甾-3,20-二酮的羟基类衍生物.方法和结果:利用本中心筛选的总枝状毛霉(Maeor racemosus)进行微生物转化,得到的产物经熔点、红外、核磁和质谱分析,确定为预期产物14β-羟基-孕甾-3,20-二酮和7β,14β二羟基-孕甾-3,20-二酮.结论:用微生物转化法可以制备甾体的羟基类衍生物.     

新型抗菌药吡啶酮酸类的临床药理研究进展

概述抗菌药应用范围广泛,是临床最常用药物之一,目前,仍以磺胺类和抗生素构成抗菌药的两大支柱。自1962年美国 Ste-rling—Winthrop 研究所 Lesher 发现第一个吡啶酮酸类抗菌药萘啶酸以来,这一领域的研究异常活跃,进展较快,到目前为止已有数百种该系列化合物合成,其中有20余种抗菌活性强的衍生物已用于临床或进入临床药理研究阶段,形成了有别于磺胺类和抗生素的一个新分支。根据     

卡介菌素与结核菌纯蛋白衍生物在新生儿12周阳转比较

目的在新生儿12周阳转结素试验中比较卡介菌素与结核菌纯蛋白衍生物。方法比较卡介菌素与结核菌纯蛋白衍生物12周阳转中结素反应平均直径的频率分布图。结果卡介菌素与结核菌纯蛋白衍生物12周阳转中结素反应平均直径的频率分布图都是单峰正态分布,卡介菌素峰值幅度更高,更集中。结论卡介菌素可以替代结核菌纯蛋白衍生物用于12周阳转来监测卡介苗的接种质量。     

固定化酶催化合成头孢克洛与产物的分离纯化

应用来源于粪产碱杆菌的青霉素G酰化酶催化合成头孢克洛,并对生物转化反应过程进行了研究。在反应条件：pH 7.0、25 ℃、磷酸钠缓冲体系、加酶量3 U/mL和底物浓度60 mmol/L时,转化率达到85%,表明粪产碱杆菌青霉素G酰化酶具有较高的催化活力。研究了新型分离纯化方法,经过树脂分离的产物纯度超过95%,主要杂质含量小于0.5%,可以达到药典要求,为生物法合成头孢抗生素走向产业化奠定了基础。     

前交叉韧带残端结节：可能引起伸膝受限的因素 王健 敖英芳

背景：前交叉韧带残端形成结节引起伸膝受限的研究较少,多见于个案报道,没有系统分析前交叉韧带残端结节的研究报道。本研究目的是综合分析研究前交叉韧带损伤后前交叉韧带残端结节引起伸膝受限的临床特点。方法: 回顾性研究2008年6月至2011年12月1012例前交叉韧带损伤拟重建手术患者,通过重建术中关节镜观察前交叉韧带残端结节形成情况,同时观察患者伸膝受限情况及伴随的病史、体征、核磁共振（MRI）及病理结果。结果:1012例患者中有24例存在前交叉韧带残端结节,其中19例（男13例,女6例）因前交叉韧带残端结节卡压引起伸膝受限。平均受限角度为9.1°（5°～20°）,所有伴有伸膝受限的病例发现时间平均在伤后8.9周（3周到26周）。术前15例伴有伸膝受限的患者MRI可以看到残端迂曲成团存在于髁间窝,术中观察断裂位置均位于上止点附近,病理显示病变为排列紊乱的纤维增生结缔组织和韧带成分。结论：关节镜下观察发现1024例前交叉韧带损伤患者中24例存在前交叉韧带残端结节,19例伴有伸膝受限。作为可能引起伸膝受限的因素前交叉韧带残端结节应予重视。     

Determination of sensitivity of Mycoplasma hyosynoviae to tylosin and selected antibacterial drugs by a microtiter technique.

A microtiter technique was used for determination of the sensitivity of Mycoplasma hyosynoviae to antibiotics and other drugs. Use of a biphasic agar-broth medium in microtiter plates allowed direct visualization of growth. Results were more reproducible with this system than when broth alone was used and evaluation based on color change was required. Attempts to adapt the test for use with Mycoplasma hyorhinis were not successful. Minimal inhibitory concentrations of 12 drugs and drug combinations for 12 strains of M. hyosynoviae are presented. Drugs with the lowest minimal inhibitory concentrations were tylosin (0.37 mcg/ml)and lincomycin (0.88 mcg/ml), both of which have been used for treatment and control of M. hyosynoviae arthritis. Comparison of the minimal inhibitory concentrations of tylosin for 43 isolates of M. hyosynoviae obtained in 1959 and 1960 and from 1966 through 1971 indicated the possibilty of decreasing sensitivity to the drug although differences between recent isolates and earlier ones were not statistically significant.     

The action of certain antibiotics and ether on swine enzootic pneumonia

The susceptibility of Mycoplasma hyopneumoniae to the action of three antibiotics and diethyl ether was determined. Infected swine were used in an in vivo sensitivity detection system. The parameter of susceptibility was lesion prophylaxis. In vivo, Mycoplasma hyopneumoniae appeared to be resistant to diethyl ether, tylosin tartrate, and erythromycin, but was susceptible to the action of chlortetracycline. Chlortetracycline was effective in preventing the development of lesions when given at levels which would be practical in commercial swine operations.     

硅胶封闭感染性起搏电极残端法的疗效及安全性随访与评价

目的评价硅胶封闭感染性起搏电极残端的疗效、远期预后及安全性.方法选择1998年以来因起搏器残留电极感染,经反复局部换药和全身抗感染治疗无效而实施硅胶封闭感染性起搏电极残端的12例住院患者进行疗效总结和随访资料分析.结果11例接受长期随访的患者未发现局部再感染、渗漏或心内膜炎等,患侧上肢活动自如,生活质量明显改善.结论硅胶封闭是治疗起搏电极残端引起囊袋感染、破溃的简便实用技术,具有良好的应用及推广前景.     

大肠早期癌变息肉的内镜诊治及随访

通过详细的病理学检查，从4000例内镜切除的息肉病人中发现121例病人为早期癌变息肉，根据癌组织侵润的深度和切缘是否有癌细胞残留决定行内科保守治疗或补做外科根治术，所有病人每年一次内镜检查，结果显示：33例m癌病人，27例切缘无癌细胞残留而且未做手术的sm1癌病人和38例补做根治术的sm2癌病人均未出现复发，1例切缘有癌细胞残留的sm1癌和3例sm2癌因未做根治术出现复发。     

Experimental control of Mycoplasma meleagridis in turkeys by the dipping of eggs in tylosin and spiramycin

As a result of temperature differential dipping of turkey eggs in 715 p.p.m. of tylosin or 1000 p.p.m. spiramycin in tap water, air sac lesions caused by M. meleagridis were reduced 87% and 72%, and the M. meleagridis isolations were reduced 85% and 84% respectively.Mean weights at six weeks of age showed that poults hatched from eggs dipped in tylosin and spiramycin were 128 and 130 grams heavier than control birds. This difference in mean weights was apparent at two weeks of age.DIPPING OF EGGS IN SPIROMYCIN APPARENTLY PRODUCED A DETRIMENTAL EFFECT ON THE POULTS ONE TO SEVEN DAYS OF AGE, RESULTING IN: increased mortality of 62.4% vs. 12.5% for control and 14.7% for those dipped in tylosin, and a mean weight depression of -3.6 grams and -4.4 grams below those dipped in control or tylosin solutions, although no detrimental effect of the antibiotic introduction was apparent at hatching time.     

Genetic defects in lipoprotein metabolism. Elevation of atherogenic lipoproteins caused by impaired catabolism.

Certain proteins (called apolipoproteins B and E) on the surface of lipoprotein particles are responsible for mediating the binding of cholesterol-rich particles to specific lipoprotein receptors on the surface of cells and represent a major pathway controlling blood cholesterol levels. Three important disorders of lipoprotein metabolism, which provide insights into the molecular mechanisms responsible for the elevation of specific atherogenic lipoproteins, are the following: (1) Type III hyperlipoproteinemia results from specific mutations in apolipoprotein E that prevent the normal binding of chylomicron remnants and very-low-density lipoprotein remnants to lipoprotein receptors. Patients with this disorder who have elevated levels of these remnant lipoproteins develop atherosclerosis. (2) Familial defective apolipoprotein B-100 results from a single amino acid substitution in apolipoprotein B that prevents low-density lipoprotein from binding normally to the low-density lipoprotein receptor and elevates plasma cholesterol levels. (3) Familial hypercholesterolemia, which results in elevated levels of plasma low-density lipoprotein and premature atherosclerosis, is caused by a variety of mutations in the low-density lipoprotein receptor that interfere with the normal binding of lipoproteins to this receptor. These observations not only provide insights into the mechanisms responsible for normal lipoprotein metabolism, but also highlight the potential role of specific lipoproteins in atherogenesis.     

关节镜下同时保留股骨及胫骨残端重建前交叉韧带的临床疗效评估

目的 探讨关节镜下采取同时保留股骨及胫骨残端方式重建前交叉韧带的技术应用并观察其效果.方法 选取安徽医科大学第一附属医院2014年1月至2016年1月收住的前交叉韧带(ACL)损伤患者52例,术前依据随机数字表法分为同时保留胫骨及股骨韧带残端重建ACL组(保残组)与不保留任何韧带残端重建ACL组(对照组)并按照单束重建ACL方法完成手术,每组26例.采用Lysholm膝关节功能评分评估客观功能及行为能力,采用国际膝关节文献委员会(IKDC)主观评分评估主观运动能力及生活质量,比较两组患者术前、术后18个月上述评分标准评估的患者膝关节功能.所有患者于术后6个月复查磁共振,观察移植肌腱与骨隧道的愈合情况及有无其他关节异常信号.结果 保残组患者膝关节术前Lysholm评分和IKDC评分均低于术后[(57.21±5.05)分vs(89.43±4.12)分;(52.18±7.61)分vs(91.43±4.52)分],差异有统计学意义(P<0.05).对照组患者术前Lysholm评分和IKDC评分均低于术后[(54.72±4.06)分vs(86.21±3.89)分;(56.24±6.59)分vs(83.56±5.02)分],差异有统计学意义(P<0.05).术后IKDC主观评分保残组优于对照组[(91.43±4.52)分vs(83.56±5.02)分],且差异有统计学意义(P<0.05).所有患者术后未发生严重并发症.结论 关节镜下同时保留胫骨及股骨侧残端重建前交叉韧带术术后效果良好,无不良并发症,有利于前交叉韧带重建术后膝关节功能的恢复.     

Two cases of cancer in the remnant stomach derived from gastritis cystica polyposa

We have recently encountered two patients with early gastric cancer in the remnant stomach which resulted from gastritis cystica polyposa at the anastomosis site. The remnant stomach, which had been reconstructed with the Billroth II method, contained an elevated sessile lesion at the anastomosis site. One patient was a 73-year-old woman who had undergone gastrectomy for a gastric ulcer at 30 years earlier, cancer type I + IIa of the remnant stomach was diagnosed, and total remnant gastrectomy was performed. The other patient was a 59-year-old man who had undergone gastrectomy for a duodenal ulcer at 31 years earlier, cancer type I + IIa of the remnant stomach was diagnosed, and subtotal remnant gastrectomy was performed. Histological examination in each case showed that moderately differentiated adenocarcinoma had developed from gastritis cystica polyposa. These results suggested that this cancer has a close relationship with gastritis cystica polyposa.     

双氢克尿噻对分化型甲状腺癌术后残留甲状腺摄碘功能及辐射吸收剂量的影响

目的　探讨双氢克尿噻 (双克 )提高分化型甲状腺癌 (DTC)术后残留甲状腺摄碘功能及增强 1 31 I辐射吸收剂量的作用。方法　将 30例 DTC术后患者随机分为双克组与对照组 ,双克组给予双克 2 5 m g tid,连用 4 d,对照组给予安慰剂。两组均分别在给药前后测定 2 4 h甲状腺摄碘率、1 31 I有效半衰期 (Teff)、甲状腺激素水平及促甲状腺激素 (TSH)水平。结果　双克组用药后同用药前相比 ,2 4 h摄碘率提高至原来的 (1 .36± 0 .5 8)倍 ,辐射吸收剂量增强至原来的 (1 .35± 0 .5 4 )倍 ,Teff改变不明显 ,与对照组比较 ,2 4 h摄碘率显著提高 ,辐射吸收剂量显著增强。结论　双克有明显提高 DTC术后残留甲状腺摄碘功能、增强残留甲状腺 1 31 I辐射吸收剂量的作用