良性前列腺增生与前列腺慢性炎症的相关性研究进展

良性前列腺增生（BPH）是老年男性常见的泌尿系统疾病，其发病与前列腺慢性炎症之间存在显著相关。感染因子、尿液返流、代谢综合征、衰老过程和自身免疫应答在内的几种刺激，通过相应分子途径引起前列腺免疫细胞的组织定位和组成成分发生广泛改变，从而导致免疫系统失调，之后引发的组织损伤和缓慢愈合，导致了BPH发生和进展。本文通过总结良性前列腺增生与前列腺慢性炎症的相关性的临床研究结果，前列腺免疫细胞在病理生理机制层面与前两者之间的内在联系，以及抗炎药物对BPH-LUTS的干预作用，以其为BPH-LUTS的药物研发提供参考。     

Novel β-Coronavirus (SARS-CoV-2): Current and future aspects of pharmacological treatments

The novel coronavirus outbreak has reported to be rapidly spreading across the countries and becomes a foremost community health alarm. At present, no vaccine or specific drug is on hand for the treatment of this infectious disease. This review investigates the drugs, which are being evaluated and found to be effective against nCOVID-19 infection. A thorough literature search was performedon the recently published research papers in between January 2020 to May 2020, through various databases like “Science Direct”, “Google Scholar”, “PubMed”,“Medline”, “Web of Science”, and “World Health Organization (WHO)”. We reviewed and documented the information related with the current and future aspects for the management and cure of COVID-19. As of 21st July 2020 a total of 14,562,550 confirmed cases of coronavirus and 607,781 deaths have been reported world-wide. The main clinical feature of COVID-19 ranges from asymptomatic disease to mild lower respiratory tract illness to severe pneumonia, acute lung injury, acute respiratory distress syndrome (ARDS), multiple organ dysfunction, and death. The drugs at present used in COVID-19 patients and ongoing clinical trials focusing on drug repurposing of various therapeutic classes of drug e.g. antiviral, anti-inflammatory and/or immunomodulatory drugs along with adjuvant/supportive care. Many drugs on clinical trials shows effective results on preliminary scale and now used currently in patients. Adjuvant/supportive care therapy are used in patients to get the best results in order to minimize the short and long-term complications. However, further studies and clinical trials are needed on large scale of population to reach any firm conclusion in terms of its efficacy and safety.     

The effect of indomethacin and metamizole on ureteral motility and urine flow in sheep

Summary The objective of this study was to evaluate the effect of two non-steroid anti-inflammatory drugs, indomethacin and metamizole, on ureteral peristalsis during acute occlusion similar to the situation in renal colic. In 12 pentobarbital anesthetized sheep, both ureters were cannulated and the frequency of ureteral contractions, urine flow, mean ureteral pressure and blood pressure were recorded during 10-min control and i.v. drug administration periods. Both indomethacin (1–2 mg/kg) and metamizole (60–120 mg/kg) showed a dose dependent reduction in peristaltic frequency without reduction of the mean pressure. In addition, the pressure amplitude of the peristaltic waves was also lowered, particularly with indomethacin. Only indomethacin reduced the urine flow. Arterial blood pressure was elevated by both drugs, particularly after the first dose of indomethacin. It can be concluded that indomethacin and metamizole reduce ureteral peristaltic frequency, probably blocking the impulse transmission at the ureteropelvic junction.For the partial fulfillment of a Master's degree in Pharmacology     

鱼腥草止咳口服液治疗难治性肺炎的临床观察

目的:观察鱼腥草止咳口服液对难治性肺炎患者的临床疗效,并探讨其作用机理。方法:65例患者随机分成两组,治疗组35例,对照组30例。对照组采用西医常规治疗,治疗组在同对照组治疗基础上加用鱼腥草止咳口服液口服,观察两组患者症状及体征的改善情况,并检测治疗前后外周血IL-2和TNF-α的变化。结果:治疗后总有效率:治疗组为94.3%,对照组为83.3%,组间比较有显著性差异(P<0.05);治疗组在增加外周血IL-2及降低TNF-α水平方面明显优于对照组。结论:鱼腥草止咳口服液治疗难治性肺炎具有显著疗效,尤其在镇咳、平喘、抗炎、退热及促进排痰、肺部啰音和炎症消失、毒副作用等方面具有明显优势。     

Anti-inflammatory,analgesic, antipyretic and related properties of meloxicam,a new non-steroidal anti-inflammatory agent with favourable gastrointestinal tolerance

The anti-inflammatory, analgesic and antipyretic properties of the new non-steroidal anti-inflammatory agent, meloxicam, were investigated in a variety of animal models and compared with the properties of piroxicam, diclofenac, indomethacin and several other NSAIDs.With respect to the total effect of a single oral dose, the anti-exudative effect of meloxicam on carrageenaninduced oedema in the rat exceeded that of all the NSAIDs included in the comparison. Additionally, meloxicam showed the greatest potency of all the compounds examined with respect to adjuvant-induced arthritis in the rat, the granuloma pouch model and the cotton pellet test in the rat. Unlike indomethacin, in the carrageenan pleurisy model in the rat, meloxicam caused both a dose-dependent reduction in exudate volume and also inhibition of leucocyte migration.Meloxicam showed a strong and lasting effect on inflammatory pain in the rat. Like other NSAIDs, but unlike dipyrone, meloxicam had no effect in the hot plate and tail clamp tests, which are used to identify weak central analgesic effects. Unlike dipyrone and like indomethacin, meloxicam had no effect in a model of visceral distention pain.In common with other NSAIDs, meloxicam had no influence on the body temperature of normothermic rats in the anti-inflammatory dose range, but did reduce yeastinduced fever in the rat in a dose-dependent manner. Like piroxicam, meloxicam had a uricosuric effect on rats treated with oxonic acid.Low-dose meloxicam inhibited both bradykinin-induced and PAF-induced bronchospasm in the guinea-pig, but had no effect on acetylcholine-induced bronchospasm.Piroxicam had greater ulcerogenic effects in the rat stomach than meloxicam.The therapeutic range of meloxicam in the rat, with regard to inhibition of adjuvant arthritis, was several times greater than that of piroxicam, indomethacin, diclofenac and naproxen.     

金茵利胆胶囊的体外抗炎活性评价及其谱效关系研究

目的 评价金茵利胆胶囊的体外抗炎活性,并研究其抗炎谱效关系。方法 建立LPS诱导的RAW264.7细胞炎症模型,通过检测细胞上清中NO、TNF-α和IL-6等指标的含量来评价金茵利胆胶囊的抗炎活性。在此基础上,采用均匀设计法制备金茵利胆胶囊组成饮片的不同配伍样本,采用高效液相法建立均匀设计样品的指纹图谱,对均匀设计样品进行抗炎活性测定;以细胞上清液中NO、TNF-α和IL-6的抑制率为药效指标,与共有峰峰面积经灰色关联分析构建抗炎谱效关系。结果 金茵利胆胶囊提取物（0.25~1.00 mg/mL）能显著降低LPS诱导的RAW264.7细胞分泌NO、TNF-α和IL-6。经对照品比对指认出其中7个色谱峰,分别为新绿原酸（9号峰）、绿原酸（13号峰）、隐绿原酸（14号峰）、1, 3-二咖啡酰奎宁酸（16号峰）、对羟基苯乙酮（17 号峰）、柚皮苷（21 号峰）、新橙皮苷（23 号峰）。抗炎谱效关系结果表明,共有峰均具有一定的抗炎贡献度,其中共有峰峰21（柚皮苷）、峰23（新橙皮苷）与3个细胞炎症指标的关联度均大于0.74。结论：金茵利胆胶囊发挥抗炎作用是多种成分共同作用的结果,为金茵利胆胶囊抗炎药效物质基础及其质量控制提升提供参考。     

Inhibitory activity of a series of coumarins on leukocyte eicosanoid generation

Sixteen plant-derived or synthetic coumarins with different patterns of substitution were tested for their capacity to modify A23187-induced synthesis of leukotriene B₄ and thromboxane B₂ via the 5-lipoxygenase and cyclooxygenase pathways of arachidonate metabolism in rat peritoneal exudate leukocytes. Five of the 16 coumarins inhibited LTB₄ production: all containortho-dihydroxy substitutions (approximate IC₅₀ values 8–100 M). The mechanism is likely to depend upon a combination of the coumarins' iron-chelating and iron ion-reducing abilities, properties which also confer beneficial activities of these compounds as scavengers of reactive oxygen species (Payá et al., Biochem. Pharmacol.44, 205–214 (1992)). Inhibition of the cyclooxygenase pathway was only demonstrated by one compound, 5,7-dihydroxy-4-methylcoumarin, which did not inhibit 5-lipoxygenase, indicating that the cyclooxygenase inhibitory mechanism is different. Similar effects of the active coumarins were obtained using arachidonic acid as substrate for rat leukocyte eicosanoid generation, confirming that they act at the 5-lipoxygenase/cyclooxygenase level. The same profile of activity was also shown when the coumarins were tested against 5-lipoxygenase in human polymorphonuclear neutrophils. Taken together, these antioxidant and anti-eicosanoid properties of coumarins could be exploited for the design of potentially valuable non-toxic anti-inflammatory agents for treating diseases in which eicosanoid generation and the production of reactive oxygen species are involved.     

急性肺血栓栓塞症兔TNF-α、IL-8、IL-10水平及地塞米松的影响

目的:探讨兔急性肺血栓栓塞症(PTE)时血浆及支气管肺泡灌洗液(BALF)中TNF-α,IL-8、IL-10的水平和地塞米松(Dex)的影响。方法:采用自体血栓回输法建立兔急性PTF模型。36只兔随机分为对照组、Dex治疗组和PTE模型组。用ELISA方法检测上述细胞因子(CK)水平,术毕肺组织行病理观察。结果:栓塞后上述CK均有升高,治疗后TNF-α、IL-8均有下降,IL-10变化不明显。组织病理学可见栓塞后肺动脉内血栓形成,肺组织萎缩、出血、炎性反应明显,Dex治疗后肺组织病理改变明显减轻。结论:PTE后促炎性CK在引起肺部炎性反应和肺组织及肺动脉病损中起了重要作用,抗炎治疗可以明显减轻CK引起的这种损伤。抗炎治疗能降低PTE急性期病死率,改善远期预后,CK可能起了很重要的作用。