羧甲基壳聚糖的骨髓细胞染色体畸变试验

羧甲基壳聚糖(CMC)是甲壳糖的水溶性衍生物,是一种新兴的海洋类药物,其来源广泛,价格低廉,有可能替代价格昂贵的透明质酸(HA)关节腔注射治疗骨关节炎(Osteoarthritis,OA).     

患者退变软骨及滑膜组织中一氧化氮的表达及意义

目的骨关节炎是一种常见疾病,一氧化氮(NO)是关节炎病因的一种重要介质,NO的表达影响滑膜和关节软骨细胞的功能并导致滑膜充血而诱发关节炎。本文综述了近年来骨关节炎NO表达研究进展以及通过抑制NO含量对骨关节炎进行治疗临床应用。     

二氟尼柳治疗类风湿性关节炎和退行性骨关节炎的临床研究

目的：评价二氟尼柳治疗类风湿性关节炎和退行性骨关节炎的临床疗效和安全性。方法：采用随机对照试验,选用各芬作为对照药。试验组共９４例,其中类风湿性关节炎５５例,退行性骨关节炎３９例。对照组共５８例,其中类风湿性关节炎３７例,退行性骨关节炎均有效,但二氟尼柳的疗效略优于布洛芬,治疗类风湿性关节炎总有效率分别为８７．２７％和８６．４９％,退行性骨关节炎总有效率分别为９４．８７％和７６．１９％,试验组和对     

美洛昔康治疗类风湿关节炎与骨关节炎的疗效及安全性Meta分析

目的:系统评价美洛昔康治疗类风湿关节炎与骨关节炎的临床疗效和安全性。方法:检索并选取国内公开发表的有关美洛昔康治疗类风湿关节炎和骨关节炎随机对照试验文献,应用Jadad评分法进行质量评价,运用Meta分析方法进行统计。结果:共有15项研究符合纳入标准。与对照组比较,美洛昔康治疗类风湿关节炎疗效的合并效应量OR值为1.07(95%CI为0.82～1.40);美洛昔康治疗骨关节炎疗效的合并效应量OR值为1.25(95%CI为0.86～1.82);安全性的合并效应量OR值为0.75(95%CI为0.61～0.92)。结论:美洛昔康治疗类风湿关节炎和骨关节炎的临床疗效总体上与对照组相当,而不良反应发生率总体上低于对照组。     

影响膝骨关节炎患者疼痛VAS评分的因素分析

<正>骨关节炎又称退行性关节炎、增生性关节炎、老年性关节炎等其患病率随着年龄增长而增加,女性比男性多见。世界卫生组织统计,50岁以上人群中,骨关节炎的患病率为50%,55岁以上的人群中,患病率为80%[1,2]。到目前为止,普遍的观点认为骨关节炎不可根治,骨关节炎临床治疗的首要目标是缓解临床症状,减轻疼痛对患者生活、工作能力的影响[3,4]。本研究分别于出院和入院时对膝骨关节炎患者进行疼痛VAS评分调查。报告如下。     

关节镜清理术结合透明质酸钠治疗膝骨关节炎的疗效

骨关节炎是临床常见的疾病,为退行性关节炎、肥大性关节、增生性关节炎,是临床导致膝关节疼痛的主要原因。流行病学调查统计．膝骨关节炎是导致膝关节疼痛的主要原因．且为最常见的三大老年疾病,50％以上的55岁老年人有此疾病。本文研究分析膝关节镜清理手术联合透明质酸治疗膝骨关节炎,报告如下。     

膝骨关节炎的中医疗法与研究

膝骨关节炎是骨科中的常见病,又被称为膝关节骨关节病、退行性膝关节炎等,多见于老年人群体。主要研究了膝骨关节炎行中医治疗的方法与护理,旨在为今后该病的治疗提供临床借鉴意义。     

补肾活血中药治疗膝骨关节炎80例的临床疗效观察

目的：研究补肾活血方在膝骨关节炎临床治疗中的作用。方法：选择80例膝骨性关节炎患者,将其随机分为研究组和对照组,每组各40例,研究组给予补肾活血方治疗加西药治疗,对照组仅给予西药治疗。观察治疗前后两组患者膝关节活动功能的变化情况及临床疗效。结果：补肾活血中药可明显缓解膝关节骨性关节炎的临床症状、体征及膝关节活动功能,达到与西药治疗相类似的临床疗效,且不良反应发生率低。结论：补肾活血方在膝骨关节炎临床治疗中疗效肯定,值得临床推广应用。     

氯诺昔康应用于围术期镇痛的药理学基础

氯诺昔康是一种新型非甾体类抗炎镇痛药（nonsteroidal anti—inflmmatory drugs,NSAIDs）,系噻嗪类衍生物。现在临床上使用的氯诺昔康有注射剂和口服片剂两种,可以单独使用,也可与临床常用的大部分镇痛药合用。注射剂主要用于急性中度手术后疼痛以及急性腰、坐骨神经相关的疼痛。片剂主要用于各种外伤引起的急性轻中度疼痛,晚期癌痛,骨关节炎,类风湿关节炎和强直性脊柱炎的治疗。     

帕歌斯治疗关节炎60例

目的：观察帕歌斯治疗关节炎的疗效。方法：120例患者分成两组，治疗组口服帕歌斯，每次2片(每片410 mg)，tid，疗程4周，对照组口服双氯芬酸钠，每次25 mg，tid，疗程4周。结果：治疗组治疗骨关节炎总有效率90.0%，治疗类风湿性关节炎总有效率76.7%。无胃肠道不良反应。对照组治疗骨关节炎总有效率86.7%，治疗类风湿性关节炎总有效率63.3%。结论：帕歌斯治疗关节炎疗效肯定，无明显不良反应，值得临床应用。     

亚甲蓝类似物的合成及其与牛血清白蛋白相互作用的研究

目的 合成3种亚甲蓝类似物3,7-二(二正丙胺基)-吩噻嗪-5-鎓碘化物、3,7-二(二正丁胺基)-吩噻嗪-5-鎓碘化物和3,7-二(二正戊胺基)-吩噻嗪-5-鎓碘化物,并研究模拟生理条件下这3种亚甲蓝类似物与牛血清白蛋白的相互作用.方法 通过1H-NMR及MS对这3种亚甲蓝类似物进行结构表征,应用荧光光谱法研究了模拟生理条件下这3种亚甲蓝类似物与牛血清白蛋白的相互作用.结果 3种亚甲蓝类似物和BSA相互作用形成了蛋白质-药物复合物并猝灭其固有荧光,亚甲蓝类似物与BSA相互作用过程的ΔG0<0,亚甲蓝类似物与BSA荧光残基间的距离r均小于7 nm.结论 亚甲蓝类似物和BSA相互作用的猝灭机制为静态猝灭,二者之间的反应是自发进行的.非辐射能量转移理论表明BSA与亚甲蓝类似物之间存在非辐射能量转移.同步荧光光谱和三维荧光光谱的研究结果表明,亚甲蓝类似物与BSA的相互作用导致BSA构象发生变化.     

Efficacy study of two novel hyaluronic acid-based formulations for viscosupplementation therapy in an early osteoarthrosic rabbit model

Viscosupplementation (VS) is a therapy for osteoarthrosis (OA) consisting of repetitive intra-articular injections of hyaluronic acid (HA). It is known to be clinically effective in relieving pain and increasing joint mobility by restoring joint homeostasis. In this study, the effects of two novel HA-based VS hydrogel formulations were assessed and challenged against a pure HA commercial formulation for the first time and this in a rabbit model of early OA induced by anterior cruciate ligament transection (ACLT). The first formulation tested was a hybrid hydrogel composed of HA and reacetylated chitosan, a biopolymer considered to be chondroprotective, assembled thanks to an ionic shielding. The second formulation consisted of a novel HA polymer grafted with antioxidant molecules (HA-4AR) aiming at decreasing OA oxidative stress and increasing HA retention time in the articulation.ACLT was performed on rabbits in order to cause structural changes comparable to traumatic osteoarthrosis. The protective effects of the different formulations were observed on the early phase of the pathology in a full randomized and blinded manner. The cartilage, synovial membrane, and subchondral bone were evaluated by complementary investigation techniques such as gross morphological scoring, scanning electron microscopy, histological scoring, and micro-computed tomography were used.In this study, ACLT was proven to successfully reproduce early OA articular characteristics found in humans. HA and HA-4AR hydrogels were found to be moderately protective for cartilage as highlighted by μCT. The HA-4AR was the only formulation able to decrease synovial membrane hypertrophy occurring in OA. Finally, the hybrid HA-reacetylated chitosan hydrogel surprisingly led to increased subchondral bone remodeling and cartilage defect formation. This study shows significant effects of two innovative HA modification strategies in an OA rabbit model, which warrant further studies toward more effective viscosupplementation formulations.     

D-奎尼酸研究进展

D-奎尼酸是一种具有极高价值的精细化工产品和医药中间体,在医药、食品、化工等行业均有广泛的应用价值。其部分衍生物已被证实有多种重要的药理作用。本文综述了D-奎尼酸来源、衍生物的药理活性及其在手性合成中的应用。     

Growth factors in asymptomatic osteoarthritis - insulin,insulin-like growth factor-1, growth hormone

An association of growth hormone (GH) and chronic arthritis has been demonstrated in patients with primary osteoarthritis (OA), in patients with acromegaly and in animals with experimental arthritis. We investigated a possible role for the growth factors, insulin-like growth factor-1 (IGF-1), insulin and GH in the aetiopathogenesis of OA by measuring serum levels in OA patients with symptoms and in OA patients without symptoms. Quantification was by standardized radioimmunoassays. Symptomatic OA patients with pain and characteristic radiological changes, joint-space narrowing and bony overgrowth had elevated GH and insulin levels and reduced IGF-1 levels. Asymptomatic OA patients with only characteristic radiographic changes had normal levels of these growth factors. These data suggest that growth factors may have a role in symptomatic OA, with GH acting as an inciting factor. Treatment should include correction of these metabolic perturbations.     

Treatment decisions,side-effect liability and cost-effectiveness in osteoarthritis

Cost-benefit ratios emphasize benefits as much as they do risks but the consequences of not treating also figure in the equation. For osteoarthritis (OA), most drugs designed to alter the progression have either been found wanting or have been withdrawn. That leaves palliation of symptoms as the search for pharmacological intervention to replace the very effective surgery continues. Guidelines to aid in the search succeed in defining alternatives to amelioration but less satisfactority define disease modifiers. Much of this derives from a misunderstanding: OA is not a disease, though it often provokes symptoms, but rather is the final common pathway of all events at a joint. Treatment can therefore be offered only when OA produces symptoms, and that is too late to reverse the process. If prediction were possible, more effective prophylaxis might be developed. The interferences with life content, life space and life span lead to the therapeutic decisions and their cost-effectiveness. Because symptoms in OA often result from secondary inflammation, anti-inflammatory drugs remain appropriate choices, even though simple analgesics suffice in the short term for pain relief alone. That inflammation may also underlie the inception of the process that leads to OA is self-evident and more effective initial treatment might slow the progression, but the symptoms of established OA are a secondary event, long after the historically elusive primary insult, and warrant careful appraisal of cost-effectivness of interventions as part of risk assessment.     

Animal Models of Osteoarthritis: Challenges of Model Selection and Analysis

Osteoarthritis (OA) is the most common musculoskeletal disease, affecting millions of individuals worldwide. New treatment approaches require an understanding of the pathophysiology of OA and its biomechanical, inflammatory, genetic, and environmental risk factors. The purpose of animal models of OA is to reproduce the pattern and progression of degenerative damage in a controlled fashion, so that opportunities to monitor and modulate symptoms and disease progression can be identified and new therapies developed. This review discusses the features, strengths, and weaknesses of the common animal models of OA; considerations to be taken when choosing a method for experimental induction of joint degeneration; and the challenges of measuring of OA progression and symptoms in these models.     

Investigational drugs for the treatment of osteoarthritis,an update on recent developments

ABSTRACT

Introduction: Osteoarthritis (OA) is the leading cause of pain, loss of function, and disability among elderly, with the knee the most affected joint. It is a heterogeneous condition characterized by complex and multifactorial etiologies which contribute to the broad variation in symptoms presentation and treatment responses that OA patients present. This poses a challenge for the development of effective treatment on OA.

Areas covered: This review will discuss recent development of agents for the treatment of OA, updating our previous narrative review published in 2015. They include drugs for controlling local and systemic inflammation, regulating articular cartilage, targeting subchondral bone, and relieving pain.

Expert opinion: Although new OA drugs such as monoclonal antibodies have shown marked effects and favorable tolerance, current treatment options for OA remain limited. The authors believe there is no miracle drug that can be used for all OA patients’; treatment and disease stage is crucial for the effectiveness of drugs. Therefore, early diagnosis, phenotyping OA patients and precise therapy would expedite the development of investigational drugs targeting at symptoms and disease progression of OA.     

The pathobiology of osteoarthritis and the rationale for using the chondroitin sulfate for its treatment

Structure-modifying osteoarthritis (OA) drugs are agents that reverse, retard, or stabilize the pathology of OA, thereby providing symptomatic relief in the long-term treatment. The objective of this review is to evaluate the literature on chondroitin sulfate (CS) with respect to the pathobiology of OA to ascertain whether this agent should be classified as a symptomatic slow-acting drug (SYSADOA), a compound that has a slow onset of action and improve OA symptoms after a couple of weeks. CS exhibits a wide range of biological activities and from a pharmacological point of view it produces a slow but gradual decrease of the clinical symptoms of OA and these benefits last for a long period after the end of treatment. Many literature data show that CS could have an anti-inflammatory activity and a chondroprotective action by modifying the structure of cartilage. These properties are also related to the oral adsorption of this molecule as high-molecular mass compounds having clusters of sulfate groups and high charge density capable of exert their chondroprotective activity in vivo.     

Investigation of the distribution and excretion of okadaic acid in mice using immunostaining method.

This paper describes the distribution and excretion of okadaic acid (OA) administered orally to mice and examined by immunostaining method. Five min after administration, OA was systemically distributed, being detected in the lung, liver, heart, kidney, and small and large intestine. The swollen small intestinal villi contained OA, causing the separation of epithelial cells from villi and erosion, which developed within 1h. Bleeding and edema in the lung were also found, and the distribution of OA coincided with these injuries. Although a considerable amount of OA was accumulated in the liver, no symptoms, such as bleeding, were observed. The detection of OA continued for 2 weeks in the liver and blood vessels. Excretion from kidney, cecum and large intestine began even after 5 min of the administration, and the excretion from intestine continued for 4 weeks.     

大蒜素/有机凹凸棒黏土/海藻酸钠/壳聚糖复合微球的制备及其性能

目的制备大蒜素/有机凹凸棒黏土/海藻酸钠/壳聚糖复合微球(ASCM),并研究其载药性能。方法采用复凝聚法制备了ASCM,以复合微球的载药量和包封率为指标,以大蒜素(DATS)为模型药物,考察了有机凹土(OA)/海藻酸钠(SA)质量比、药物含量、复合温度对微球载药性能的影响,并比较了OA加入前后微球的溶胀性能和缓释性能。结果加入OA后,当复合微球中OA:SA为1:3,OA:DATS为1:1时,其载药量和包封率由原来的12.3%和42.3%分别提高到16.8%和66.5%,而在pH 6.8的磷酸盐缓冲溶液中累积释放率降低。结论复合微球可以作为药物的缓释载体。