双极关节腔内脉冲射频联合臭氧注射治疗膝骨性关节炎的临床疗效

目的 观察双极关节腔内脉冲射频(IAPRF)联合臭氧注射治疗膝骨性关节炎(KOA)的临床疗效.方法 140例KOA患者随机分为两组,每组70例.联合组予以双极IAPRF联合臭氧注射治疗,对照组仅予以双极IAPRF治疗.分别于治疗前及治疗后1周、6个月和12个月比较两组患者VAS疼痛评分和骨关节炎指数(WOMAC)评分的差异.结果 两组治疗前VAS疼痛评分和WOMAC评分差异均无统计学意义(P＞0.05).两组治疗后1周、6个月和12个月VAS疼痛评分和WOMAC评分均低于治疗前,且联合组优于对照组(P＜0.05).结论 与双极IAPRF治疗比较,双极IAPRF联合臭氧注射治疗更能减轻KOA患者疼痛,改善膝关节功能.     

单极和双极关节内脉冲射频治疗膝骨性关节炎的疗效

目的 观察单极和双极关节内脉冲射频治疗膝骨性关节炎(KOA)患者的临床疗效.方法 120例KOA患者随机均分为单极组和双极组,分别采用单极和双极关节内脉冲射频治疗,于治疗前以及治疗后1周、1个月和6个月比较VAS疼痛评分和骨关节炎指数(WOMAC)评分的变化.结果 治疗后1周、1个月和6个月,两组VAS疼痛评分和WOMAC评分均低于治疗前(P＜0.05),并且双极组VAS疼痛评分和WOMAC评分均低于单极组(P＜0.05).结论 单极和双极关节内脉冲射频治疗均能有效缓解KOA患者疼痛症状,改善膝关节功能,且双极关节内脉冲射频优于单极.     

关节腔内注射富血小板血浆或玻璃酸钠联合体外冲击波治疗膝骨关节炎的疗效

目的 比较关节腔内注射自体富血小板血浆(PRP)或玻璃酸钠联合体外冲击波(ESWT)治疗膝骨关节炎(KOA)的临床疗效。方法 37例KOA患者随机分为玻璃酸钠组(19例)和PRP组(18例)。两组患者均给予常规康复训练、行为干预和ESWT治疗。玻璃酸钠组予膝关节腔内注射玻璃酸钠20 mg,每周1次，连续4周；PRP组予膝关节腔内注射自体PRP 5 mL,每2周1次，连续4周。治疗前(T1)、治疗结束时(T2)、治疗后3个月(T3)和6个月(T4)时分别采用西安大略和麦克马斯特大学骨关节炎指数(WOMAC)评估两组膝关节功能，并记录不良事件发生情况。结果 两组患者均顺利完成治疗，无明显不良事件发生。两组T1时WOMAC各评分比较均无统计学差异(P>0.05)。与T1时比较，两组T2～T4时WOMAC各评分均下降(P<0.01)。与玻璃酸钠组比较，PRP组T3、T4时WOMAC关节疼痛评分和T4时关节功能评分均下降(P<0.05)。结论关节腔内注射自体PRP或玻璃酸钠联合ESWT均能有效缓解KOA患者膝关节疼痛，改善膝关节功能，自体PRP的疗效更好。     

盐酸氨基葡萄糖联合Mulligan动态关节松动术对膝关节骨性关节炎的影响

目的:研究盐酸氨基葡萄糖联合Mulligan动态关节松动术治疗膝关节骨性关节炎(knee osteoarthritis,KOA)患者的临床疗效.方法:将60例KOA患者随机分为盐酸氨基葡萄糖联合Mulligan动态关节松动术治疗组(观察组)和对照组,每组各30例.对照组只进行常规康复治疗(包括超短波、低强度脉冲超声及运动疗法,共90 min/d).观察组在常规康复治疗基础上还同时服用盐酸氨基葡萄糖,并且进行Mulligan动态关节松动术(20 min/次).两组均治疗6次/周,共6周.所有患者在治疗前及治疗6周后采用疼痛VAS评分、WOMAC关节炎指数、LKSS膝关节评分量表来评估对患者受累膝关节的治疗效果.结果:治疗6周后,两组患者VAS评分、WOMAC评分、LKSS评分均较治疗前有不同程度的改善,评分比均较治疗前明显提高(P<0.05);观察组的VAS评分、WOMAC评分、LKSS评分与对照组比较均具有显著性差异(P<0.05).结论:应用盐酸氨基葡萄糖联合Mulligan动态关节松动术治疗,能更好地改善KOA患者的膝关节疼痛、僵硬、日常生活状态和健康状态等方面,建议在临床上进一步推广应用.     

水针刀联合玻璃酸钠治疗膝骨性关节炎的WOMAC评分和VAS评分比较

目的 对比分析水针刀联合关节腔内玻璃酸钠注射治疗膝骨性关节炎的疗效.方法 2012年10月至2013年2月广东省中医院门诊治疗膝骨性关节炎患者共80例,随机分为治疗组(n=43)与对照组(n=37).治疗组给予水针刀联合关节内注射玻璃酸钠,对照组单纯给予玻璃酸钠治疗,评价临床疗效.结果 两组患者入院治疗前的国际膝骨关节炎WOMAC评分和疼痛视觉模拟VAS评分比较差异无统计学意义(p＞0.05).治疗后1个月和3个月两组患者的WOMAC评分和VAS评分均较前降低,且3个月上述评分比1个月进一步减少,组内比较差异有统计学意义(P＜0.05).组间比较治疗组1个月和3个月的WOMAC评分和VAS评分均比对照组显著降低(P＜0.05).结论 水针刀联合关节内注射玻璃酸钠治疗膝骨性关节炎可进一步提高疗效.     

补肾散寒通络汤联合艾灸及塞来昔布治疗膝骨关节炎的临床观察

目的:观察补肾散寒通络汤联合艾灸及塞来昔布治疗膝骨关节炎(KOA)的临床疗效及安全性。方法:选取2014年5月-2015年12月在重庆康华医院就诊的KOA患者70例,按照就诊单双号顺序分为对照组和观察组,各35例。对照组患者给予塞来昔布胶囊0.2 g,qd;观察组患者在对照组基础上加用补肾散寒通络汤(每日1剂,水煎取汁300 mL,分早、中、晚3次服用)及艾灸治疗。两组患者均以4周为1个疗程,连续治疗2个疗程。比较两组患者的临床疗效,治疗前后的中医证候积分、视觉模拟评分法(VAS)评分、西安大略和麦克马斯特大学量表(WOMAC)评分、实验室检查指标、关节情况,以及不良反应发生情况。结果:观察组患者的总有效率(85.71%)显著高于对照组(68.57%),差异有统计学意义(P<0.05)。治疗前,两组患者的上述指标比较,差异均无统计学意义(P>0.05)。治疗后,两组患者的中医证候积分、VAS评分、WOMAC评分、红细胞沉降率、C反应蛋白水平和膝关节肿胀积分均较治疗前显著降低,且观察组各指标水平显著低于对照组,差异均有统计学意义(P<0.05);两组患者治疗前后骨摩擦音关节个数比较,差异均无统计学意义(P>0.05)。两组患者不良反应发生率比较(5.71%vs.2.86%),差异无统计学意义(P>0.05)。结论:补肾散寒通络汤联合艾灸及塞来昔布能改善KOA患者临床症状,缓解关节疼痛,减轻关节炎症和肿胀,且用药较安全。     

关节腔内注射帕瑞昔布在早期膝骨关节炎治疗中的临床疗效

目的:探讨关节腔内注射帕瑞昔布在早期膝骨关节炎(KOA)治疗中的临床疗效及对血清学指标水平的影响.方法:选取2018年1月—2019年12月我院收治的早期KOA患者110例为研究对象,随机分为相同例数的两组:对照组和研究组,每组各有患者55例.对照组患者膝关节腔内注射玻璃酸钠注射液+口服盐酸氨基葡萄糖胶囊治疗,研究组膝关节腔内注射帕瑞昔布+口服盐酸氨基葡萄糖胶囊治疗.观察比较两组患者的临床疗效,采用WOMAC评分评价治疗前后膝关节功能,采用视觉模拟评分法(VAS)评价膝关节疼痛程度,检测比较治疗前后血清基质金属蛋白酶(MMP)-3;白细胞介素(IL)-1β、肿瘤坏死因子-α(TNF-α)水平变化.结果:研究组患者临床治疗总有效率方面较对照组患者的显著提高(92.73％VS 78.18％,P<0.05).两组治疗后WOMAC评分均低于治疗前(P<0.05).治疗后,研究组WOMAC评分均低于对照组(P<0.05).治疗后,两组血清MMP-3、IL-1β、TNF-α水平均降低(P<0.05).治疗组治疗后上述血清学指标水平均低于对照组(P<0.05).结论:关节腔内注射帕瑞昔布可以改善早期KOA患者膝关节功能,降低患者疼痛程度,取得理想的治疗效果,考虑治疗机制与降低机体炎症反应有关.     

膝骨性关节炎联合应用玻璃酸钠及复方倍他米松注射液治疗的临床研究

目的:观察分析膝骨性关节炎患者联合应用玻璃酸钠及复方倍他米松注射液治疗的临床疗效.方法:选择我院2017年11月—2019年11月收治的110例膝骨性关节炎患者为观察对象,按照入院顺序单双号分为两组:治疗组(n=55)、对照组(n=55).对照组患者采用玻璃酸钠关节腔内注射,治疗组患者玻璃酸钠与复方倍他米松注射液联合应用关节腔内注射.比较两组患者的临床疗效,采用视觉模拟评估法(VAS)、Lvsholm关节功能评分、WOMAC的疼痛量表评价两组疼痛程度及膝关节功能,检测比较两组治疗前后关节液基质金属蛋白酶-3(MMP-3)、MMP-9及白细胞介素1β(IL-1β)水平.结果:治疗组患者的治疗总有效率较对照组的显著提高(92.73％VS 78.18％,P<0.05).两组治疗后VAS、Lvsholm及WOMAC评分均降低,关节液MMP-3、MMP-9及IL-1β水平均降低(P<0.05).治疗组治疗后VAS、Lvsholm及WOMAC评分低于对照组,治疗后关节液MMP-3、MMP-9及IL-1β水平低于对照组(P<0.05).结论:玻璃酸钠与复方倍他米松注射液联合应用关节腔内注射治疗膝骨性关节炎可以取得满意效果,患者关节局部疼痛程度及膝关节功能明显改善,考虑作用机制可能与降低关节液MMP-3、MMP-9及IL-1β的水平有关.     

“针”“灸”“药”并举综合疗法治疗膝骨关节炎的疗效观察

目的观察雷火灸联合刃针并口服骨龙胶囊治疗膝骨关节炎(KOA)的临床疗效。方法 60例膝骨关节炎患者,采用随机数字表法分为治疗组和对照组,每组30例。治疗组采用雷火灸联合刃针并口服骨龙胶囊治疗,对照组采用口服非甾体抗炎药美洛昔康治疗。比较两组患者治疗前后西安大略和麦克马期特大学骨关节炎指数(WOMAC)评分、视觉模拟评分法(VAS)评分及临床疗效。结果治疗前,两组患者WOMAC评分、VAS评分比较差异无统计学意义(P>0.05);治疗4周后,两组患者WOMAC评分、VAS评分均较本组治疗前降低,且治疗组WOMAC评分(36.4±10.3)分、VAS评分(3.6±1.3)分均低于对照组的(46.5±13.6)、(5.5±1.4)分,差异具有统计学意义(P<0.05)。治疗组患者显效率为56.67%、总有效率为90.00%,明显高于对照组的30.00%、66.67%,差异具有统计学意义(P<0.05)。结论雷火灸联合刃针并口服骨龙胶囊的"针""灸""药"并举综合疗法治疗膝骨关节炎疗效确切。     

仙灵骨葆联合玻璃酸钠治疗膝骨性关节炎46例

目的 观察仙灵骨葆联合玻璃酸钠关节腔内注射治疗膝骨性关节炎(KOA)的临床疗效。方法 将92例KOA患者随机分为治疗组和对照组,各46例,对照组给予双氯芬酸钠缓释胶囊治疗,治疗组口服仙灵骨葆联合玻璃酸钠关节腔内注射治疗。治疗5周后比较两组患者的疗效。结果 两组患者的疼痛视觉模拟评分法(VAS)评分、Lysholm总评分比较,差异均有统计学意义(P<0.05);治疗组疗效优良率为84.78%,明显高于对照组的67.39%(P<0.05)。结论 仙灵骨葆联合玻璃酸钠关节腔内注射治疗KOA,可明显缓解患者的临床症状,改善关节功能,疗效显著,值得临床推广。     

alpha-glucosidase (CHO) (Genzyme)

Genzyme General is developing recombinant human alpha-glucosidase, produced in mammalian cell culture, as a potential treatment for Pompe disease. By July 2004, enrollment was completed in two clinical trials and an observational study in adults. Genzyme was planning to file for regulatory approval in Europe during 2004, followed by filings in the US and Japan in mid-2005.     

(S)-oxybutynin (Sepracor)

Sepracor is developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.     

Allosteric interaction of zinc with recombinant alpha(1)beta(2)gamma(2) and alpha(1)beta(2) GABA(A) receptors

In a recent study we have provided evidence that inhibition of native GABA(A) receptors by zinc depends primarily on the allosteric modulation of receptor gating. Both the kinetics and the sensitivity of the GABA(A) receptor to zinc depend on subunit composition, especially on the presence of the gamma(2) subunit. To analyze the mechanism of action of zinc its effects have been tested on recombinant alpha(1)beta(2)gamma(2) and alpha(1)beta(2) receptors expressed in HEK 293 cells. The currents produced by ultrafast application of GABA have been measured to assess the impact of zinc ions on GABA(A) receptor gating with resolution corresponding to the time scale of synaptic currents. While, as expected, zinc markedly reduced the peak amplitude of alpha(1)beta(2)-mediated currents, its effect on kinetics was significantly different from that observed for alpha(1)beta(2)gamma(2). In particular, unlike alpha(1)beta(2)gamma(2), zinc did not affect the onset of alpha(1)beta(2)-mediated responses. Moreover, zinc increased the extent of desensitisation of alpha(1)beta(2)gamma(2) receptors and reduced desensitisation of alpha(1)beta(2) ones. Quantitative analysis suggests that zinc exerts an allosteric modulation on both alpha(1)beta(2)gamma(2) and alpha(1)beta(2) receptors. Zinc effects on alpha(1)beta(2)gamma(2) were qualitatively similar to those reported for native receptors.     

Di(isononyl) phthalate (DINP) and di(isodecyl) phthalate (DIDP) are not mutagenic

Recently there have been reports of liver and kidney tumors in rodents following long-term exposure to di(isononyl) phthalate (DINP). Mechanistic studies suggested that the liver tumors were a consequence of peroxisomal proliferation, whereas the kidney tumors (found only in male rats) were associated with induction of alpha(2u)-globulin. Because both peroxisomal proliferation and alpha(2u)-globulin are considered to be non-genotoxic carcinogenic processes, it seemed appropriate to investigate the genotoxic potential of DINP. Additional studies were also conducted on di(isodecyl) phthalate (DIDP), a structurally related substance that also induces peroxisomal proliferation, although it has not been tested in a carcinogenicity bioassay. The DINP was tested in Salmonella, in vitro cytogenetics and mouse micronucleus assays, whereas DIDP was evaluated in a mouse micronucleus test. All of these tests produced negative results, i.e. neither phthalate was mutagenic in any of the test systems. These data are consistent with results of other published and unpublished genotoxicity tests and provide support for the hypothesis that the liver and kidney tumors induced by DINP were the result of non-genotoxic processes.     

Developmental toxicity of di-(C(7)-C(9) alkyl) phthalate and di-(C(9)-C(11) alkyl) phthalate in the rat

Two phthalate esters, di-(C(7)-C(9) alkyl) phthalate (D79P) and di-(C(9)-C(11) alkyl) phthalate (D911P), have been assessed for their potential to cause developmental toxicity in the rat. Groups of 22 timed-mated Sprague-Dawley rats were administered 250, 500, or 1000 mg/kg D79P or D911P daily by oral gavage (5 ml/kg) between gestation days (GD) 1 and 19. Control animals received the vehicle (olive oil) alone. On GD20, the animals were sacrificed and the fetuses examined. Treatment resulted in no signs of maternal toxicity, as assessed by adjusted maternal bodyweight gain throughout gestation and clinical examinations, and no effects upon litter size, fetal survival or bodyweight. Pups of the high dose D79P and intermediate and high dose D911P groups showed increased incidences of supernumerary lumbar ribs. There was a significant increase in dilated renal pelves in pups of the low dose D79P and high dose D911P groups, but only for D911P was there a significant trend. Consequently, the no observed adverse effect level (NOAEL) for maternal toxicity for both D79P and D911P is 1000 mg/kg/day. The NOAEL values for developmental toxicity are 500 mg/kg/day D79P and 250 mg/kg/day D911P.     

1,2-环己二胺柠檬酸铂(Ⅱ)及异柠檬酸铂(Ⅱ)的合成和抗癌活性

报道了1,2-环己二胺异柠檬酸铂(Ⅱ)及1,2-环己二胺柠檬酸铂(Ⅱ)的合成及鉴定方法。抗癌试验表明前者在40及80mg/kg 剂量下对小鼠 L1210、P388及S180均有明显的抑瘤作用,且有部分动物可治愈;后者对 L1210也有明显的抑瘤作用,但较前者为弱。     

Two-generation reproduction toxicity studies of di-(C(7)-C(9) alkyl) phthalate and di-(C(9)-C(11) alkyl) phthalate in the rat

Di-(C(7)-C(9) alkyl) phthalate (D79P) and di-(C(9)-C(11) alkyl) phthalate (D911P), based on high-normality linear oxo-alcohols, have been assessed for their impact upon reproductive performance in Sprague-Dawley rats. Rats were continuously exposed to either D79P or D911P at dietary levels of 0%, 0.1%, 0.5%, or 1.0% over two generations. Selected F(0) offspring (F(1) generation) were exposed to the same dietary concentration of D79P or D911P as the respective F(0) animals, and were mated to produce F(1) offspring. Both D79P and D911P markedly reduced body weight gain in F(0) and F(1) adult males at the highest dose, but females were affected to a lesser extent. There was no impairment of fertility, fecundity, or development in either generation, but body weights of offspring in the 1.0% D79P and 1.0% D911P groups were slightly and transiently reduced over the weaning period. Although decreases in the weight of several organs were accounted for by depressed body weight, ovary weights were reduced in both generations exposed to 1.0% D79P, and epididymidal weights were slightly reduced in adults of both generations exposed to 1.0% D911P. However, ovarian function-assessed by the oestrus cycle and mating behaviour-and epididymidal sperm concentration, motility, and morphology were unaffected by either substance. Treatment resulted in liver changes, particularly in males, characterised by increased liver weight in young animals, histopathologic changes and reduced organ weight in mature animals, and an increase in palmitoyl CoA oxidase activity. In conclusion, neither D79P nor D911P impaired reproductive function in rats when administered in the diet at levels that induce systemic toxicity, and the NOAEL for effects on reproduction in the rat is 0.5% for both D79P and D911P.     

4（R）—（6—氨基—9H—嘌呤—9—基）—2（R）—（羟甲基）四氢呋喃—3（R）—醇的合成

为寻找抗HIV化合物,我们以D－核糖为原料,经甲基化、硅烷基化、还原裂解反应制得重要中间体1－脱氧核糖（5）,再通过形成环状亚砜化合物,与NaN3发生反应后,经过还原、缩合、环合、氨化、脱保护基反应制得异脱氧腺嘌呤核苷（1）,各步反应收率均超过70％。其抗HIV活性测定尚在进行中。     

Serotonin(7) receptors (5-HT(7)Rs) and their ligands

Serotonin (5-HT) is involved in various physiological and pathological processes by interaction with 14 distinct receptor subtypes, grouped in seven classes of receptors (5-HT(1-7)) on the basis of amino acid sequence, pharmacology, and signal transduction pathways. The 5-HT(7)R is a G-protein coupled receptor with seven transmembrane domains. It was found by the application of molecular cloning and has been identified in rat, mouse, human, pig, and guinea pig. Although the biological functions of the 5-HT(7)Rs are poorly understood, preliminary evidence suggests that it may be involved in depression, control of circadian rhythms, and relaxation of vascular smooth muscles. For these reasons, the 5-HT(7)R has become a target for the development of novel drugs. This review will give a brief introduction of the pharmacology of 5-HT(7)R (molecular structure, distribution of 5-HT(7)R mRNA, localization of the 5-HT(7)R protein, functional correlates, and therapeutic potential) and a detailed survey of the 5-HT(7)R ligands, which have appeared in the literature in both papers and patents. Structure-activity relationships (SAR) of these ligands will also be described.