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Tizanidine对胶质瘤细胞U251增殖、迁移及凋亡的影响
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作者 刘冰 霍会永 +5 位作者 冯社军 曹凌 赵现 曹妍 王如科 李军涛 《中国医药导报》 CAS 2018年第2期27-31,共5页
目的探究Tizanidine对胶质瘤细胞U251的增殖、迁移及凋亡的影响,并尝试探讨其作用机制。方法将U251细胞分为两组,一组用Tizanidine(20μmol/L)处理24 h;另一组用DMSO处理为对照组。采用CCK8实验检测细胞增殖情况;采用Transwell实验检测... 目的探究Tizanidine对胶质瘤细胞U251的增殖、迁移及凋亡的影响,并尝试探讨其作用机制。方法将U251细胞分为两组,一组用Tizanidine(20μmol/L)处理24 h;另一组用DMSO处理为对照组。采用CCK8实验检测细胞增殖情况;采用Transwell实验检测细胞的迁移和侵袭情况;采用细胞流式检测细胞凋亡情况,采用Western blot检测PI3K-AKT信号通路相关蛋白及凋亡相关蛋白的表达量的变化。结果 CCK8增殖实验表明Tizanidine可以抑制脑胶质瘤细胞U251的增殖(P<0.05);Transwell结果说明Tizanidine可以抑制脑胶质瘤细胞U251的迁移和侵袭(P<0.05);流式凋亡结果分析显示经无血清凋亡诱导后,经Tizanidine处理的细胞凋亡明显增多(P<0.05),Western blot结果显示经过Tizanidine处理的U251细胞,细胞的抗凋亡蛋白B淋巴细胞瘤-2(BCL-2)的表达量显著下调(P<0.05),促凋亡蛋白Bcl-2相关X蛋白(BAX)和Active Caspase3表达量则显著上调(P<0.05),AKT和mTOR的磷酸化水平均受到了显著抑制(P<0.05),PI3K/AKT信号通路的下游蛋白P70、Cyclin D1的表达也相应下调(P<0.05)。结论 Tizanidine抑制胶质瘤细胞U251的增殖、迁移和侵袭,诱导其凋亡,这有可能是通过抑制PI3K/AKT信号通路的激活实现的。 展开更多
关键词 tizanidine U251 PI3K/AKT信号通路
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Comparison of Baclofen and Tizanidine in Reducing Spasticity in Cerebral Palsy: A Randomized Control Trial 被引量:1
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作者 Nazmul Haque Narayan Saha +3 位作者 Tahmina Ahmed Bithi Debnath Abid Hossain Mollah Ekhlasur Rahman 《Open Journal of Pediatrics》 2020年第4期617-625,共9页
<strong>Background:</strong><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;"> Cerebral palsy is the m... <strong>Background:</strong><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;"> Cerebral palsy is the most common chronic motor disability that begins in childhood with the predominant motor abnormality</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;"> that</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;"> is spasticity</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">.</span></span></span><span><span><span style="font-family:""> <b><span style="font-family:Verdana;">Objective:</span></b><span style="font-family:Verdana;"> The purpose of the present study was to compare the efficacy of oral baclofen and oral tizanidine in reducing spasticity in cerebral palsy patients. </span><b><span style="font-family:Verdana;">Methodology: </span></b><span style="font-family:Verdana;">This randomized controlled trial was conducted from January 2010 to December 2011 and it was carried out in the Out Patient Department (OPD) of Pediatrics at Dhaka Medical College Hospital (DMCH), Dhaka, Bangladesh and Center for Neurodevelopment and Autism in Children (CNAC) of Bangabandhu Sheikh Mujib Medical University (BSMMU), Dhaka, Bangladesh. </span><b><span style="font-family:Verdana;">Results</span></b><span style="font-family:Verdana;">: A total number of 70 cerebral palsy children were recruited for this study of which 35 patients were in </span><span style="font-family:Verdana;">Tizanidine</span><span style="font-family:Verdana;"> group and 35 patients were in </span><span style="font-family:Verdana;">baclofen</span><span style="font-family:Verdana;"> group. </span><span style="font-family:Verdana;">Furthermore</span></span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">,</span></span></span><span><span><span style="font-family:""><span style="font-family:Verdana;"> 70 cerebral palsy children were taken as control who were treated with </span><span style="font-family:Verdana;">placebo</span><span style="font-family:Verdana;">. Tizanidine had superior efficacy in reducing tone in spastic cerebral palsy over baclofen measured by using </span><span style="font-family:Verdana;">Modified</span><span style="font-family:Verdana;"> Ashworth scale in </span><span style="font-family:Verdana;">different</span> <span style="font-family:Verdana;">time period</span></span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">s</span></span></span><span><span><span style="font-family:""><span style="font-family:Verdana;"> from AS score-3 to score-2 (p < 0.05). Tizanidine was also superior in joint angle improvement in spastic cerebral palsy measured by </span><span style="font-family:Verdana;">physician</span><span style="font-family:Verdana;"> rating scale from AS score-3 to score-2 (crouch p < 0.0001) and foot contact from AS score-3 to score-2 (p < 0.0001);but no statistically significant improvement in gross motor function. </span><span style="font-family:Verdana;">Adverse</span><span style="font-family:Verdana;"> effect </span><span style="font-family:Verdana;">w</span></span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">as</span></span></span><span><span><span style="font-family:""><span style="font-family:Verdana;"> more in </span><span style="font-family:Verdana;">baclofen</span><span style="font-family:Verdana;"> group. </span><b><span style="font-family:Verdana;">Conclusion</span></b><span style="font-family:Verdana;">: For reducing generalized spasticity with regards to muscle tone, joint angle </span><span style="font-family:Verdana;">and</span><span style="font-family:Verdana;"> improvement in gait in cerebral palsy patients, tizanidine has superior efficacy and less adverse effects than baclofen.</span></span></span></span> 展开更多
关键词 Cerebral Palsy SPASTICITY BACLOFEN tizanidine
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Formulation and evaluation of a bioadhesive patch for buccal delivery of tizanidine 被引量:2
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作者 Mohamed S.Pendekal Pramod K.Tegginamat 《Acta Pharmaceutica Sinica B》 SCIE CAS 2012年第3期318-324,共7页
Tizanidine hydrochloride(THCl)is an antispasmodic agent which undergoes extensive first pass metabolism making it a possible candidate for buccal delivery.The aim of this study was to prepare a monolayered buccal patc... Tizanidine hydrochloride(THCl)is an antispasmodic agent which undergoes extensive first pass metabolism making it a possible candidate for buccal delivery.The aim of this study was to prepare a monolayered buccal patch containing THCl using the emulsification solvent evaporation method.Fourteen formulations were prepared using the polymers Eudragit■ RS 100 or EudragitB RL 100 and chitosan.Polymer solutions in acetone were combined with a THCl aqueous solution(in some cases containing chitosan)by homogenization at 9000 rpm for 2 min in the presence of triethyl citrate as plasticizer and cast in novel Teflon molds.Physicochemical properties such as film thickness,in vitro drug release and in vitro mucoadhesion were evaluated after which permeation across sheep buccal mucosa was examined in terms of flux and lag time.Formulations prepared using a Eudragit■polymer alone exhibited sa tisfactory physicomechanical properties but lacked a gradual in vitro drug release pattern.Incorporation of chitosan into formulations resulted in the formation of a porous structure which did exhibit gradual release of drug.In conclusion,THCl can be delivered by a buccal patch formulated as a blend of Eudragit■ and chitosan,the latter being necessary to achieve gradual drug release. 展开更多
关键词 tizanidine hydrochloride Buccal patch CHITOSAN Eudragits■RS 100 Eudragits■RL 100 In vitro drug release In vitro mucoadhesion
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