雷米芬太尼与芬太尼在小儿扁桃体摘除手术中的临床观察

目的:探讨雷米芬太尼在小儿扁桃体摘除术中的有效性和安全性.方法:将30例患儿随机分为雷米芬太尼组(R组)和芬太尼组(F组).R组给药:氯胺酮2 mg·kg-1、丙泊酚1 mg·kg-1、雷米芬太尼1 μg·kg-1和岁库溴铵0.5 μg·kg-1诱导插管,维持以输液泵泵入丙泊酚4～10 mg·kg-1·h-1和雷米芬太尼0.25～0.5 μg·kg-1·min-1;F组给药:氯胺酮2 mg·kg-1、丙泊酚1 mg·kg-1、芬太尼3 μg·kg-1和罗库溴铵0.5 mg·kg-1静脉推注诱导插管维持以输液泵泵入丙泊酚4～10 mg·kg-1·h-1,间断静脉推入芬太尼1 μg·k-1·h-1.分别记录患儿麻醉前、插管前1 min、插管后1 min的SBP、DBP、HR;术毕停药后患儿自主呼吸恢复时间、呼唤睁眼时间、拔管时间;术后24 h恶心、呕吐情况.结果:R组患儿术后呼吸恢复时间、呼唤睁眼时间、拔管时间与F组相比差异有统计学意义(P<0.05);麻醉诱导前两组血流动力学相似,插管前1 min R组HR慢于F组(P<0.05);插管后1 min R组SBP低于F组(P<0.05);术后恶心、呕吐的发生率及患儿年龄、性别、体重、手术时间等一般情况无统计学意义.结论:雷米芬太尼对血压、心率等血流动力学有良好的可控性,其麻醉镇痛效果好,诱导和苏醒迅速,术中平稳,不良反应小,值得临床推广.     

丙泊酚分别联合氯胺酮、芬太尼在无痛人流中麻醉效果比较

目的 比较丙泊酚分别联合氯胺酮、芬太尼的麻醉效果,探讨门诊病人在无痛人流时麻醉药物的配伍.方法 120 例需要无痛人流的病人随机分两组,分别静脉注射丙泊酚(1.5～2mg·kg-1) 氯胺酮(0.2～0.4mg·kg-1)和丙泊酚(1.5～2mg·kg-1) 芬太尼(0.5～1μg·kg-1),观察两组呼吸循环有关参数的变化和镇静镇痛效果.结果 两组药物配伍的镇静镇痛效果无明显差别,两泊酚 芬太尼组对病人的呼吸和循环的抑制作用较丙泊酚 氯胺酮显著(P＞0.05),但丙泊酚 氯胺酮组的定向恢复时间延长.结论 两组药物均可用于门诊病人无痛人流的麻醉,术中注意对病人呼吸循环等指标的监测,应用氯胺酮时适当廷长病人的在院时间,确认病人完全清醒后方可离院.     

Application of anesthesia using pentobarbital intraperitoneal combined with local lidocaine infiltration in establishing rat model of knee osteoarthritis

目的 观察戊巴比妥钠腹腔注射复合利多卡因局部浸润麻醉在制作大鼠膝关节骨关节炎(OA)模型的效果.方法 将20只雄性SD大鼠随机均分为两组,采用前交叉韧带切断术制作大鼠膝关节OA模型.联合麻醉组采用戊巴比妥腹腔注射及局部利多卡因浸润;腹腔麻醉组采用单纯腹腔注射戊巴比妥钠方式麻醉.观察两组术中戊巴比妥用量及手术时间.结果 联合麻醉组戊巴比妥用量(29.3±5.9) mg/kg,明显小于腹腔麻醉组的(37.0±8.9)mg/kg(P＜0.05);手术时间(44.9±7.4) min,也明显短于联合麻醉组的(52.1±7.4) min(P＜0.05).结论 联合麻醉可减少麻醉药物用量,改善麻醉效果,有利于大鼠膝关节OA模型的顺利制作.     

硫喷妥钠静注引起静脉炎7例的观察

硫喷妥钠 (Thiopental Soldium,戊硫巴比妥钠 )为超短时作用的巴比妥类药物 ,常用于静脉麻醉、诱导麻醉、基础麻醉、抗惊厥以及复合麻醉等。小剂量静注即引起镇静、嗜睡 ,稍大剂量 (3～ 5 mg· kg- 1 )于 10～ 2 0 s内意识消失。对中枢神经系统有起效快 ,作用时间短的特点。我院自 2 0 0 1年 3月至 2 0 0 2年 9月开展现代 ECT治疗 (即无抽搐电休克 ) 10 3例中 ,用硫喷妥钠配合琥珀胆碱作静脉麻醉 ,现将其中出现不同程度静脉炎 7例的观察及治疗报告如下。1　临床资料1.1　观察对象　 10 3例现代 ECT治疗者中出现不同程度静脉炎 7例 ,其中…     

麻醉前应用戊乙奎醚对冠脉搭桥术患者血流动力学和脑电双频指数的影响

目的观察冠脉搭桥术麻醉前应用戊乙奎醚对麻醉诱导前后患者血流动力学和脑电双频指数(BIS)的影响。方法择期全麻下行冠脉搭桥术患者40例,随机分为2组,每组20例。戊乙奎醚组麻醉诱导前肌内注射(肌注)戊乙奎醚0.01 mg.kg-1,东莨菪碱组肌注东莨菪碱0.006 mg.kg-1。观察比较2组麻醉诱导前后心率、血压、心率收缩压乘积(RPP)和BIS值。结果东莨菪碱组用药后收缩压和RPP无明显变化,用药后20 min患者心率有所上升,用药后10、20 min BIS值有所下降,但高于戊乙奎醚组(P<0.05)。戊乙奎醚组用药后10、20 min,患者心率、血压、RPP和BIS值均降低(P<0.05)。气管插管前后戊乙奎醚组心率、收缩压、RPP和BIS值多低于东莨菪碱组。2组均未见明显不良反应。结论应用戊乙奎醚作为冠脉搭桥术前用药,可降低心肌耗氧量,有利于患者血流动力学平稳和镇静。     

戊巴比妥钠腹腔注射复合利多卡因局部浸润麻醉在大鼠膝关节骨关节炎模型制作中的应用

目的观察戊巴比妥钠腹腔注射复合利多卡因局部浸润麻醉在制作大鼠膝关节骨关节炎(OA)模型的效果。方法将20只雄性SD大鼠随机均分为两组,采用前交叉韧带切断术制作大鼠膝关节OA模型。联合麻醉组采用戊巴比妥腹腔注射及局部利多卡因浸润;腹腔麻醉组采用单纯腹腔注射戊巴比妥钠方式麻醉。观察两组术中戊巴比妥用量及手术时间。结果联合麻醉组戊巴比妥用量(29.3±5.9)mg/kg,明显小于腹腔麻醉组的(37.0±8.9)mg/kg(P<0.05);手术时间(44.9±7.4)min,也明显短于联合麻醉组的(52.1±7.4)min(P<0.05)。结论联合麻醉可减少麻醉药物用量,改善麻醉效果,有利于大鼠膝关节OA模型的顺利制作。     

氯胺酮-丙泊酚复合应用在儿童静脉麻醉中的作用

目的 观察如何减轻氯胺酮在儿童静脉麻醉中对血流动力学变化的影响及其副作用.方法 41例学龄儿童随机分为两组(甲组17例,乙组24例).甲组以氯胺酮1mg/kg静脉慢注为诱导,然后用微量泵持续静注氯胺酮2mg·kg-1·h-1;乙组以丙泊酚1mg/kg、氯胺酮0.5mg/kg静脉慢注为诱导,然后用微量泵持续静注氯胺酮1mg·kg-1·h-1,丙泊酚5mg·kg-1·h-1维持.观察记录麻醉前(T0)、麻醉诱导后5分钟(T1)、维持麻醉后5分钟(T2)、维持麻醉切皮后5分钟(T3)、手术开始后15分钟(T4)的收缩压、舒张压、心率和SpO2及神志恢复时间和恢复期有无精神症状.结果 甲乙两组麻醉后各段时间内的收缩压、舒张压、心率与麻醉前相比较P均<0.05,其中甲组切皮后与麻醉前收缩压、舒张压相比较(T1、T2、T3与T0相比,P<0.01),乙组平均神志恢复时间和麻醉期低氧血症、恢复期精神症状发生率明显低于甲组.结论 丙泊酚可以有效地减少及减轻氯胺酮在心血管、精神症状、低氧血症及苏醒期长等方面的副作用,其复合应用是儿童麻醉的较为理想的方法.     

丙泊酚配伍芬太尼用于小儿眼科急诊手术麻醉的临床观察

目的观察丙泊酚配伍太尼用于小儿眼科急诊手术的麻醉效果,以及在用药期间的收缩压(SBP)、舒张压(DBP)、心率(HR)、血氧饱和度(SpO2)的变化,术毕的苏醒情况,与传统使用氯胺酮复合羟丁酸钠麻醉效果比较,是否更具有优越性.方法 40例眼外伤急诊手术的患儿,随机分为丙泊酚芬太尼组(Ⅰ组)和氯胺酮羟丁酸钠组(Ⅱ组),Ⅰ组先静注芬太尼2ug.kg-1、丙泊酚2～3mg·kg-1、阿曲库铵0.5mg·kg-1诱导插管,然后微泵持续注射丙泊酚6～8mg.kg-1·h-1维持,30～45min间断静注阿曲库铵0.25～0.5mg·kg-1.Ⅱ组肌注氯胺酮6mg·kg-1,待患儿入睡后抱入室,静注氯胺酮1～1.5mg·kg-1、羟丁酸钠80mg·kg-1、阿曲库铵0.5mg·kg-1作诱导插管,用微量泵0.8～1.2mg.kg-1·h-1速率输注氯胺酮维持,酌情追加羟丁酸钠60mg·kg-1,相隔35～45分钟追加阿曲库铵0.25-0.5mg.kg-1.结果Ⅰ组病例麻醉效果良好,但诱导后SBP、DBP、MAP、HR稍降低.而Ⅱ组用药后HR增快,术中肢体有不自主的躁动现象,苏醒时间及拨管时间明显延长.结论丙泊酚伍芬太尼用于小儿眼科急诊手术,诱导起效快,麻醉平稳,恢复迅速,与氯胺酮羟丁酸钠相比,麻醉效果确切,副作用少,可控性强.     

异丙酚用于结肠镜检查麻醉的临床研究

目的　研究不同剂量异丙酚用于结肠镜检查镇静镇痛作用及其对呼吸循环的影响。方法　选择12 0例结肠镜检查的患者 (ASA ～ ) ,随机分成 4组 ,每组 30例。C组不用药作为对照 ,P1、P2、P3组静脉注射异丙酚 1mg/ kg后接微量泵分别输注异丙酚 4mg· kg- 1 · h- 1 、6 mg· kg- 1 · h- 1 、8mg· kg- 1 · h- 1 。过结肠脾曲肝曲前分别追加异丙酚 0 .6 mg/ kg。观察术中镇静分级 ,术中症状 ,记忆 ,心率 ,血压及血氧饱和度变化。结果　与对照组比 ,用药组对肠镜检查安静无痛苦 ,其中 P2组镇静、镇痛程度 ,记忆缺失程度及对呼吸循环影响明显优于其他组。呼吸循环抑制无临床意义。结论　异丙酚 1mg/ kg诱导 ,6 mg· kg- 1 · h- 1 静脉维持用于肠镜检查麻醉是安全有效剂量。     

肝胆两益汤镇静促眠作用研究

目的探究《辨证录》·肝胆两益汤的镇静促眠作用,为研发镇静促眠新药提供实验依据。方法小鼠分别灌胃给予肝胆两益汤(水提冻干粉)2500,1250和625 mg·kg-1.d-1,连续灌胃给药1周,用小鼠自主活动仪观察其对小鼠自主活动的影响;以腹腔注射戊巴比妥钠方法,观察肝胆两益汤对阈剂量戊巴比妥钠致小鼠入睡潜伏期和睡眠持续时间的影响及其对戊巴比妥钠阈下剂量致小鼠入睡率的影响。结果与正常组相比,肝胆两益汤2500 mg·kg-1.d-1和1250 mg·kg-1.d-1均可显著减少小鼠自主活动次数(P<0.01)并且能够显著缩短阈剂量戊巴比妥钠致小鼠入睡潜伏期(P<0.01)和显著延长小鼠睡眠持续时间(P<0.05,P<0.01),阈下剂量戊巴比妥钠试验显示,1250 mg·kg-1.d-1组可明显提高阈下剂量戊巴比妥钠致小鼠入睡率(P<0.01)。结论肝胆两益汤2500 mg·kg-1.d-1和1250 mg·kg-1.d-1剂量对小鼠具有显著的镇静促眠作用。     

小鼠周边活动累积数据比率法评价药物镇静效应

目的建立一种基于累积周边活动时间/周边时间的比值(accumulate peripheral active time percent,APATP)的行为学评价模型。方法利用视频跟踪系统检测戊巴比妥钠和地西泮诱导小鼠自发活动并提取相应数据,并计算得到APATP。采用DAS软件对数据进行处理,得到小鼠活动趋稳半衰期((T_1/2)α)、对数曲线下面积(lgAUC0-60)和对数尾点回归值(lgPmin)进行统计学分析。结果各组小鼠的APATP随时间的延长而逐步下降,均符合方程P=Ae-αt+Be-βt。与正常组比较,PB5mg.kg-1组T12α、lgAUC0-60和lgPmin略有下降,而PB10mg.kg-1组(均为P<0.01)和PB15mg.kg-1组(P<0.01,P<0.01和P>0.05)均能不同程度的抑制3参数;与PB10mg.kg-1组比较,PB15mg.kg-1组3参数有所回升(P>0.05,P<0.05和P<0.05)。本模型参数lgAUC0-60和lgPmin与总路程具有较好的一致性(r2=1.0000和r2=0.9995,均为P<0.01)。应用地西泮进一步证实了模型的可行性,具有类似的特点;与正常组比较,地西泮2、4mg.kg-1组3参数均下降(均为P<0.01),认为两组的镇静效应与正常等同;与PB10mg.kg-1比较,地西泮2、4mg.kg-1组的3参数差异均无显著性,认为两组地西泮镇静作用与之等同。结论ICR小鼠累积周边活动时间占比模型可用于评价小鼠自发活动及药物干预效果。     

靶控输注维库溴铵在口腔颌面手术的应用

目的 探讨靶控输注(TCI)维库溴胺在口腔颌面外科手术中的应用.方法 择期手术患者60例,随机分为维库溴铵靶控输注(TCI)(Ⅰ组)和常速输注(Ⅱ组),每组30例.静脉推注咪唑安定、芬太尼、丙泊酚后,Ⅰ组维库溴铵起始血浆靶控浓度0.14 μg/ml;Ⅱ组0.1 mg/kg静脉推注维库溴铵.气管插管后,Ⅰ组维库溴铵继续TCI输注,调整靶浓度每次增加0.01 μg/ml,直至T1消失.Ⅱ组50 μg·kg~(-1)·h~(-1)静脉持续泵入,调整泵速至T1消失.临近手术结束时停用维库溴铵,术毕不用肌松拮抗药.记录肌松起效时间、维库溴铵用量和肌张力恢复时间.结果 Ⅰ组肌松起效时间(291.0±728.48)s,显著长于Ⅱ组的(244.87±26.03)S(P<0.01);Ⅰ组维库溴铵平均用药量(57.47±4.77)μg·kg~(-1)·h~(-1),明显少于Ⅱ组的(80.30±8.08)μg·kg~(-1)·h~(-1)(P<0.01);Ⅰ组肌张力恢复时间(16.85±1.94)min,明显短于Ⅱ组的(21.00±1.48)min(P<0.01).结论 与常速输注方法比较,维库溴铵TCI能减少药物用量,利于肌张力恢复,更适用于长时间手术.     

两性霉素B脂质体药代动力学及组织分布研究

目的：测定血浆及组织中两性霉素B的浓度,并比较受试与参比两性霉素B脂质体在犬体内药代动力学性质及大鼠主要组织分布特性。方法：6只犬静脉随机、交叉给予受试及参比药物,剂量为5 mg/kg,在不同时间点采集血浆样品;大鼠同样剂量静脉给予受试及参比药物,在给药后不同时间点取组织样品。用HPLC法测定生物样品中两性霉素B浓度,并用DAS 2.0软件拟合求算药代动力学参数。结果：犬i.v.给药两性霉素B脂质体后血药浓度-时间曲线符合二室模型,主要药代动力学参数为,受试药物：t1/2β（53.6±2.2）h,AUC（18.7±3.2）mg·L^-1.h,CL（0.23±0.05）L·h^-1·kg^-1,V1（11.6±2.8）L/kg;参比药物：t1/2β（52.8±0.9）h,AUC（19.6±2.2）mg·L^-1.h,CL（0.22±0.03）L·h^-1·kg^-1,V1（10.6±2.9）L/kg。结论：对上述参数以SAS统计软件进行双侧t检验,结果表明给予受试及参比药物后犬主要药代动力学参数差异无统计学意义（P〉0.05）。对各时间点主要脏器的药物浓度进行比较,差异无统计学意义（P〉0.05）。     

枯草芽孢杆菌纤溶酶的生物分析方法及其在猕猴体内的药动学研究

目的：研究猕猴单次静脉滴注注射用枯草芽孢杆菌纤溶酶（BSFE）的药动学。方法：6只猕猴静脉滴注BSFE2.5mg/kg,采用ELISA法测定动物的血药浓度,实验数据用DAS2.0药动程序拟合并计算药动参数。结果：6只猕猴静脉滴注2.5mg/kg的BSFE,浓度-时间数据经药代动力学参数计算,表明药物消除符合二房室模型。6只猕猴的达峰时间（tmax）均为0.5h,峰浓度（Cmax）均值为（592.3±150.9）μg/L;平均消除t1/2β为（5.78±1.19）h;平均清除率（CL）为（4.42±1.19）L.h^-1.kg^-1;药时AUC0-24.5h均值为（557.1±211.1）μg.L^-1.h。结论：本试验所建立的双抗体夹心ELISA法,灵敏度高、特异性强、操作简便,适于BFSE的药代动力学研究。     

注射用尼莫地平脂质体对麻醉犬脑循环的影响

目的:研究注射用尼莫地平脂质体对麻醉犬脑循环的影响。方法:36只犬随机分为6组,分别为对照组、溶媒组、尼莫地平脂质体0.3、0.15、0.075mg·kg~(-1)组和尼莫地平0.15mg·kg~(-1)组,静脉滴注给药,观察不同时间点脑血流量(CBF)、脑血管阻力(CVR)、平均动脉压(MAP)、心率(HR)和心电图(ECG)的变化。结果:尼莫地平脂质体各剂量组均可明显增加麻醉犬CBF,降低CVR(P<0.01);0.3、0.15mg·kg~(-1)可引起麻醉犬MAP和HR下降,QT间期延长(P<0.05);等剂量(0.15mg·kg~(-1))的尼莫地平脂质体与尼莫地平相比,增加CBF作用相当,降低CVR的作用更强(P<0.01)。结论:尼莫地平脂质体能增加CBF,降低CVR和MAP;剂量大时有减慢HR、延长QT间期的作用。     

加入不同吸收促进剂的盐酸氯胺酮鼻黏膜给药处方药效学研究

目的:以吸收促进剂为主要因素筛选具有良好麻醉效果的盐酸氯胺酮鼻黏膜给药处方。方法:以盐酸氯胺酮注射液为基本处方,添加各种鼻黏膜吸收促进剂/增黏剂(包括0.5%、1%、2%月桂氮酮,乙二胺四乙酸二钠,卡波姆,2-羟丙基-β-环糊精,羧甲基纤维素)配成不同处方滴鼻剂,对家兔进行鼻腔给药,以麻醉诱导期表现以及各项麻醉指标作为评价指标,对其麻醉效果进行比较。结果:以10mg·kg-1给药剂量的盐酸氯胺酮注射液加入1%月桂氮酮的处方麻醉效果较好,具有较长的麻醉时间,肌肉松弛时长(21.4±7.1)min,眼睑反射消失时长(11.4±4.6)min,痛觉消失时长(15.6±5.7)min,翻正反射消失时长(12.0±4.8)min。结论:以1%月桂氮酮作为吸收促进剂的盐酸氯胺酮鼻黏膜处方较好。     

苏芬太尼复合氯胺酮用于静脉自控镇痛最佳剂量的研究

目的观察不同剂量苏芬太尼复合小剂量氯胺酮在术后静脉自控镇痛中的效果,寻找苏芬太尼较为理想的配伍剂量。方法年龄30～60岁,ASAI-Ⅱ级,在静吸复合全麻下择期行子宫全切术的患者90例,随机分为三组（n=30）,A组苏芬太尼1．5μg／kg、B组苏芬太尼2．0μg／kg、C组苏芬太尼2．5μg／kg,所有镇痛泵均加入氯胺酮4mg／kg和止吐药托烷司琼4mg并用0．9％氯化钠注射液稀释至100ml。记录术后4h、12h、24h、48h视觉模拟评分（VAS）、镇静评分（SS）及不良反应。结果A组VAS评分显著高于B、C组（P〈0．05）,而C组SS评分显著高于A、B组（P〈0．05）;C组恶心呕吐发生率高于A、B组（P〈0．05）,余不良反应三组间差异无统计学意义（P〉0．05）。结论B组配伍在妇科术后静脉自控镇痛具有较好效果,不良反应少。     

Ginsenoside Rb1 attenuates adjuvant-induced arthritis in rats through inactivation of NF-κB signaling pathway

OBJECTIVE To investigate the anti-arthritic effect and mechanism of action of ginsenoside Rb1 on adjuvant-induced arthritis(AIA) in rats. METHODS Male SD rats were received 0.1 m L injections of FCA(10 g·L~(-1)) emulsion into the right hind metatarsal foot pad for arthritis induction. After that, rats were randomly divided into six groups, namely control group, untreated group, dexamethasone(DEX, 2.5 mg·kg~(-1)) group, low(5 mg·kg~(-1)), medium(10 mg·kg~(-1)) and high(20 mg·kg~(-1))doses of ginsenoside Rb1 groups, and treated intraperitoneally at the above dosage once a day for2 weeks. After treatment, paw swelling and arthritis indexes were evaluated, the thymus and spleen index were calculated as well. HE staining were used to observe the joint histopathology in rats. Rat ELISA kits were used to determinate the TNF-α, IL~(-1)β and IL-6 levels. Western blotting were used to detect the related protein expression of NF-κB signaling pathway in the tissues of inflamed joints. RESULTS Rb1 significantly decreased the paw swelling and arthritis index,Compared with AIA group. HE staining results revealed that medium and high doses of Rb1 significantly reduced synovial inflammatory cell infiltration, synovial lining hyperplasia and bone destruction, compared with AIA group. Elisa results showed that Rb1 significantly decreased the TNF-α, IL~(-1)β and IL-6 levels(P<0.05, P<0.01). Western blotting results revealed that the expression of p-IκB and p-P65 were significantly reduced in 20 mg·kg~(-1) of Rb1 group, compared with AIA group(P<0.05, P<0.01). CONCIUSION Rb1 manifests therapeutic anti-inflammatory effects on rats with AIA, potential y through a mechanism of inhibiting activation of the NF-κB.     

By regulating IP3/PKC/TRPV4 pathway hyperoside induces endothelium-dependent vasodilatation in rat basilar artery following four vessel occlusion ischemia reperfusion

OBJECTIVE To investigate regulatory effects of hyperoside(Hyp) on IP3/PKC/TRPV4 pathway in rat cerebral basilar artery(CBA) subjected to global cerebral ischemia-reperfusion(I/R). METHODS The model of global cerebral I/R in rats was established by four-vessel occlusions methods. The treated rats were administrated with Hyp(50 mg·kg~(-1)) group, Hyp(50 mg·kg~(-1))+HC-067047(10 mg·kg~(-1)), Hyp(50 mg·kg~(-1))+2 APB(2 mg·kg~(-1)), Hyp(50 mg·kg~(-1))+Bis I(2.5 mg·kg~(-1)), Hyp(50 mg·kg~(-1))+ 2 APB(2 mg·kg~(-1))+Bis I(2.5 mg·kg~(-1)). Hematoxylin-eosin(HE) and Nissl staining were performed and the contents of methane dicarboxylic aldehyde(MDA), neuron-specific enolase(NSE), S100β and the activity of lactic dehydrogenase(LDH) in serum were measured by enzyme-linked immunosorbnent assay(ELISA).The specific blocker N-nitro-L-arginine-methyl-ester(L-NAME) and indomethacin(Indo) were used to delete the prostacyclin(PGI2) and nitric oxide(NO) dependent relaxation. The protein expression level of TRPV4 was detected by Western blotting.Ca~(2+) intensity in vascular smooth muscle cells was measured by confocal laser scanning microscope and flow cytometry was performed to observe the apoptosis of CBA endothelial cells after in vivo administration. RESULTS Hyp induced a dose-dependent relaxation of CBA in IR rats via a PGI2 and NO independent manner, as evidenced by alleviated pathological changes and up-regulated expression of TRPV4 protein in the endothelial cells from cerebral vessels. Hyp significantly reduced the contents of MDA, NSE, S100β and the activity of LDH in serum and decreased the fluorescence intensity of Ca~(2+) in cerebral vascular smooth muscle cells by in vivo administration. The apoptotic rate of endothelial cells in Hyp treated group was significantly less than that in IR group. CONCLUSION Hyp does in fact ameliorate I/R injury by regulating IP3/PKC/TRPV4 pathway.     

Ethno-medicinal study of Artemisia ordosica Krasch.(traditional Chinese/Mongolian medicine) extracts for treatment of allergic rhinitis and nasosinusitis

OBJECTIVE To evaluate the in vivo anti-inflammatory and allergic rhinitis(AR) alleviating effect as well as in vitro antimicrobial activities of Artemisia ordosica Krasch.(AOK) extracts to verify its ethno-medicinal claims.METHODS Crude extracts(methanol/95%-ethanol/ethyl acetate) of AOK root/stem/leaf and fractions(petroleum ether/ethyl acetate/n-butanol/aqueous) of AOK root extractwere prepared. Xylene-induced ear swelling model in mouse and ovalbumin(OVA)-induced AR model in guinea pig were established. Ear swelling degrees of mice were measured. The numbers of rubbing movement and sneezes of guinea pigs were counted to evaluate the symptoms of AR. The serum levels of histamine, INF-γ, IL-2/4/10, and VCAM-1 were measured by ELISA assay. The histological changes of nasal mucosa were investigated by light microscope after H&E staining. Antimicrobial activities of AOK extracts were also tested.LC-MS/MS analysis was performed to characterize the constituents of active extract and molecular docking was conducted to predict the biological mechanism. RESULTS In ear-swelling model, extract(100.00 mg·kg~(-1)) from the ethyl acetate layer of 95% ethanol(100.00 mg·kg~(-1)) showed better swelling inhibition in mice than positive control(dexamethasone,191.91 mg·kg~(-1)). In AR model, extract from the ethyl acetate layer of 95% ethanol significantly alleviated the AR symptoms in guinea pigs, decreased the serum levels of histamine, INF-γ, IL-2/4/10, and VCAM-1, and reduced the infiltration of eosinophil in nasal mucosa. For Staphylococcus aureus, the ethyl acetate extract of AOK stem showed the highest inhibition(MIC=1.25 g·L~(-1)), for Escherichia coli, n-butanol layer of 95% ethanol extract of AOK root showed the highest inhibition(MIC=15.00 g·L~(-1)), for Candida glabrata, 95%-ethanol extract of AOK stem showed the best inhibition(MIC=0.064 g·L~(-1)),while ethyl acetate and n-butanol layers showed similar inhibition on MRSA(MIC=7.50 g·L~(-1)). LC-MS/MS characterization showed that dicaffeoylquinic acids account for more than 30% of ethyl acetate layer of AOK extract. Dicaffeoylquinic acids bind with histamine-1 receptor with high affinities and interesting modes. CONCLUSION Extracts from AOK had interesting anti-inflammatory activity in mice, alleviating effect against OVA-induced AR in guinea pigs, and antimicrobial activities in vitro, which support the ethno-medicinal use of it. The main constituents in ethyl acetate layer of AOK root extract are dicaffeoylquinic acids and could bind with histamine-1 receptor well. These findings highlighted the importance of natural product chemistry study of AOK.