党参多糖口服液抗应激及抗炎作用的研究

为研究党参多糖口服液的抗应激与抗炎作用,给小鼠灌服不同剂量（每kg体重灌服9、7、5 g生药）的党参多糖口服液后,通过测定小鼠负重游泳时间、常压耐缺氧时间来评价其应激性作用;观察党参多糖口服液对小鼠耳廓二甲苯致炎的影响,考察其抗炎作用.结果显示,党参多糖口服液能显著（P＜0.01）延长小鼠的游泳时间和常压缺氧条件下的存活时间,对二甲苯所致小鼠耳廓炎症具有不同程度的抑制作用.因此,党参多糖口服液具有抗应激、抗炎作用,该试验可为党参多糖口服液的临床应用提供参考.     

Oxygenated Polyketides from Plakinastrella mamillaris as a New Chemotype of PXR Agonists

Further purification of the apolar extracts of the sponge Plakinastrella mamillaris, afforded a new oxygenated polyketide named gracilioether K, together with the previously isolated gracilioethers E–G and gracilioethers I and J. The structure of the new compound has been elucidated by extensive NMR (¹H and ¹³C, COSY, HSQC, HMBC, and ROESY) and ESI-MS analysis. With the exception of gracilioether F, all compounds are endowed with potent pregnane-X-receptor (PXR) agonistic activity and therefore represent a new chemotype of potential anti-inflammatory leads. Docking calculations suggested theoretical binding modes of the identified compounds, compatible with an agonistic activity on hPXR, and clarified the molecular basis of their biological activities.     

Antioxidant and Anti-Inflammatory Activities of Barettin

In this paper, we present novel bioactivity for barettin isolated from the marine sponge Geodia barretti. We found that barettin showed strong antioxidant activity in biochemical assays as well as in a lipid peroxidation cell assay. A de-brominated synthetic analogue of barettin did not show the same activity in the antioxidant cell assay, indicating that bromine is important for cellular activity. Barettin was also able to inhibit the secretion of the inflammatory cytokines IL-1β and TNFα from LPS-stimulated THP-1 cells. This combination of anti-inflammatory and antioxidant activities could indicate that barettin has an atheroprotective effect and may therefore be an interesting product to prevent development of atherosclerosis.     

中药“炎痈饮”抗炎镇痛活性研究

该文旨在研究中药“炎痈饮”对小鼠急性炎症的抗炎镇痛效果.试验采用小鼠耳廓肿胀和足趾肿胀研究中药“炎痈饮”的抗炎效果及其对醋酸扭体反应的镇痛效果.结果表明:中药“炎痈饮”各剂量组均能不同程度地抑制小鼠耳廓肿胀,其中中剂量组与对照组差异显著(p＜0.05),效果优于地塞米松组和中药高、低剂量组;“炎痈饮”高、中、低剂量组在注射蛋清后4h足趾肿胀率显著低于对照组,差异极显著(p＜0.01);中药各剂量组均能降低醋酸致小鼠扭体反应次数,“炎痈饮”中剂量组效果更佳,与对照组差异显著(p＜0.05).研究结果显示中药复方“炎痈饮”对急性炎症抗炎效果显著,且具有一定程度的镇痛作用.     

紫花地丁水提物急性毒性试验及其抗炎镇痛作用研究

采用二甲苯致小鼠耳肿胀法和鸡蛋清致小鼠足肿胀法研究紫花地丁(Viola philippica)水提物高、中、低剂量(9.0、6.0、3.0 g/kg)抗炎作用,采用热板致痛法和醋酸致扭体反应法研究其镇痛作用,并测定紫花地丁水提物的小鼠最大耐受量(MTD).结果表明,紫花地丁水提物对小鼠灌胃给药MTD为480 g/(kg·d).与空白组比较,紫花地丁水提物各剂量组对二甲苯致小鼠耳肿胀及鸡蛋清致小鼠足肿胀均有显著的抑制作用(P＜0.05～P＜0.01),并能显著减少醋酸致小鼠扭体反应次数(P＜0.05～P＜0.01),显著提高热板致痛小鼠痛阈值(P＜0.05).表明紫花地丁水提物毒性较低,具有较强的抗炎镇痛作用.     

兽用非甾体抗炎药的应用现状

动物疼痛和炎症可影响其健康状况、养殖场经济效益等,预防和治疗动物疼痛、炎症具有重要意义。非甾体抗炎药可以减少动物疼痛和炎症的发生。近几年对非甾体抗炎药在动物中的应用研究越来越多,同时非甾体抗炎药的一些新功能被发现。论文对兽医常用非甾体抗炎药物的应用研究进展做一综述,以期为非甾体抗炎药在动物中的合理使用以及进一步研究提供参考。     

Pharmacokinetics of tolfenamic acid in Hawksbill turtles (Eretmochelys imbricata) after single intravenous and intramuscular administration

To the best of our knowledge, limited pharmacokinetic information to establish suitable therapeutic plans is available for Hawksbill turtles. Therefore, the present study aimed to assess the pharmacokinetic features of tolfenamic acid (TA) in Hawksbill turtles, Eretmochelys imbricata, after single intravenous (i.v.) and intramuscular (i.m.) administration at dosage 4 mg/kg body weight (b.w.). The study (parallel design) used 10 Hawksbill turtles randomly divided into equal groups. Blood samples were collected at assigned times up to 144 hr. The concentrations of TA in plasma were quantified by a validated liquid chromatography tandem mass spectrometry (LC-ESI-MS/MS). The concentration of TA in the experimental turtles with respect to time was pharmacokinetically analyzed using a noncompartment model. The C_max values of TA were 89.33 ± 6.99 µg/ml following i.m. administration. The elimination half-life values were 38.92 ± 6.31 hr and 41.09 ± 9.32 hr after i.v. and i.m. administration, respectively. The absolute i.m. bioavailability was 94.46%, and the average binding percentage of TA to plasma protein was 31.39%. TA demonstrated a long half-life and high bioavailability following i.m. administration. Therefore, the i.m. administration is recommended for use in clinical practice because it is both easier to perform and provides similar plasma concentrations to the i.v. administration. However, further studies are needed to determine the clinical efficacy of TA for treatment of inflammatory disease after single and multiple dosages.     

仔猪痢清口服液的急性毒性和抗炎活性研究

为了考察仔猪痢清口服液的急性毒性和抗炎活性,根据《兽药试验技术规范汇编》的要求选用小白鼠进行了急性毒性试验和抗炎试验。采用灌胃和腹腔注射给药进行急性毒性试验。结果表明仔猪痢清口服液实际无毒;用小鼠耳廓肿胀法观察了仔猪痢清口服液的抗炎效果,结果表明仔猪痢清口服液对二甲苯所致的小鼠急性耳廓肿胀有一定的抑制作用。