Isolates of Alpinia officinarum Hance as COX-2 inhibitors: Evidence from anti-inflammatory,antioxidant and molecular docking studies

BackgroundInflammation triggered by oxidative stress can cause various ailments, such as cancer, rheumatoid arthritis, asthma, diabetes etc. In the last few years, there has been a renewed interest in studying the antioxidant and anti-inflammatory action of plant constituents such as flavonoids and diarylheptanoids.AimTo evaluate the antioxidant, anti-inflammatory activity and the total phenolic content of isolated compounds from Alpinia officinarum rhizomes. Furthermore, molecular docking was performed to study the binding mode of these compounds into the active site of cyclooxygenase-2 (COX-2).MethodsA. officinarum rhizomes were extracted by maceration, using methanol. This extract was further fractionated by partitioning with hexane, chloroform and ethyl acetate and these fractions on further purification resulted in isolation of five pure compounds. Characterization was carried out by using ¹H NMR, ¹³C NMR and MS. They were further evaluated for antioxidant and anti-inflammatory activity using carrageenan-induced paw edema model in rats. Molecular docking study was performed using Glide module integrated in Schrodinger molecular modeling software.ResultsThe compounds were identified as 1,7-diphenylhept-4-en-3-one (1), 5-hydroxy-1,7-diphenyl-3-heptanone (2), 3,5,7-trihydroxyflavone (Galangin, 3), 3,5,7-trihydroxy-4′-methoxyflavone (Kaempferide, 4) and 5-hydroxy-7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl-3-heptanone (5). The compound-3 and compound-5 (10 mg/kg) showed significant (p < 0.001) antioxidant and anti-inflammatory potential. Moreover, total phenolic content was detected as 72.96 mg and 51.18 mg gallic acid equivalent respectively. All the five isolates were found to be good binders with COX-2 (average docking score − 9.03).ConclusionsGalangin and 5-hydroxy-7-(4″-hydroxy-3″-methoxyphenyl)-1-phenyl-3-heptanone exhibited anti-inflammatory and in-vitro antioxidant activity which may be due to presence of phenolic content in it. The molecular docking study revealed that these compounds have affinity towards COX-2 active site which can further be explored as selective COX-2 inhibitors. The results obtained in this work justify the use of A. officinarum in the treatment of inflammatory disorders like rheumatoid arthritis and inflammatory bowel diseases.     

双侧子宫动脉氨甲喋呤灌注加栓塞治疗宫颈妊娠11例效果分析

目的探讨双侧子宫动脉氨甲喋呤灌注加栓塞对宫颈妊娠的治疗效果。方法临床确诊宫颈妊娠伴阴道出血患者11例,急诊治疗。双侧子宫动脉插管、造影,分别灌注氨甲喋呤(MTX),然后用明胶海绵微粒或明胶海绵微粒加少量丝线微粒栓塞。结果宫颈妊娠孕囊由子宫动脉供血,部分以一侧为主,8例见对比剂外溢。双侧子宫动脉栓塞完毕,阴道出血明显减少。术后血β-HCG进行性下降。9例胚胎自行排出。2例行宫颈搔刮术,术中出血量不多,刮出物为陈旧性胎盘组织。胚胎排出或刮出后阴道出血完全停止。结论双侧子宫动脉化疗栓塞治疗宫颈妊娠效果良好,达到了预防和终止阴道大出血、保留子宫的目的。     

固本延衰方对亚急性衰老模型小鼠IL-2及其受体表达的影响

目的:探讨固本延衰方延缓亚急性衰老模型小鼠衰老的机制。方法:将60只小鼠随机分为4组,除正常对照组外均皮下注射D-半乳糖造成衰老模型,并给予不同剂量的固本延衰方治疗,分别用放免法及流式法测定脾淋巴细胞白细胞介素2及其受体水平。结果:衰老模型组IL-2及其受体水平明显低于正常对照组(P<0.05),固本延衰方各剂量组IL-2及其受体水平明显高于衰老模型组(P<0.05,P<0.01)。结论:提示固本延衰方通过提高衰老机体淋巴细胞IL-2及其受体表达水平,从而调节机体免疫功能延缓衰老。     

腹腔镜胆总管切开取石后鼻胆管引流术

目的:探讨腹腔镜胆总管切开取石后鼻胆管引流的可行性及优越性。方法:随机将56例胆石症患者分为两组,28例行腹腔镜胆总管切开取石后胆总管一期缝合鼻胆管引流术(鼻胆管组),28例行常规腹腔镜胆总管切开取石T形管引流术(T形管组)。比较两组手术时间、拔引流管时间、术后住院时间及并发症等。结果:28例患者成功完成腹腔镜胆总管探查后胆总管一期缝合鼻胆管引流术,鼻胆管组拔管时间(7.6±1.8)d、术后住院时间(9.7±1.6)d,明显少于T形管组(28.6±10.3)d与(20.4±3.6)d,差异有统计学意义(P<0.05),手术时间及并发症的发生率无显著差异(P>0.05)。结论:腹腔镜胆总管切开取石后鼻胆管引流术既能避免Odd is括约肌痉挛引起的胆管压力增高,又能彻底消除拔T形管后引起的胆汁性腹膜炎等并发症,是在胆总管探查术后一种安全实用的引流的新方法。     

电针周围性面瘫患者地仓穴的fMRI研究

目的：采用功能性磁共振成像（fMRI）技术,研究电针周围性面瘫患者地仓穴对脑功能的影响。方法：筛选6例左侧周围性面瘫患者为研究对象,电针刺激,同时行全脑fMR I扫描,SPM软件进行图像后处理,t检验（P〈0.01）分析得出电针不同穴位的脑功能图像。结果：双侧中央前回、双侧中央后回等多个脑区信号发生变化。结论：电针刺激引起了多个脑区信号的变化,穴位治疗作用的发生可能是多个脑区互相联络,对信息进行分析、整合,共同作用的结果。     

小陷胸汤加味含药血清对人脐静脉内皮细胞分泌NO/ET-1的调节作用

目的:探讨小陷胸汤加味中药方对血管内皮细胞的保护作用。方港:建立ox-LDL损伤人脐静脉内皮细胞株(ECV-304)模型,用小陷胸汤加味含药血清处理模型,并用放免和硝酸酶还原法在药物干预6h和24h后检测细胞上清液中ET-1和NO含量。结果:100 μg/ml的ox-LDL可损伤血管内皮细胞并导致其分泌NO和ET-1功能失调,小陷胸汤加味含药血清通过影响NO/ET-1的分泌而明显改善此失调状态。结论:小陷胸汤加味中药通过调节NO/ET-1水平显著拮抗ox-LDL对血管内皮细胞损害,具有防治AS的作用。     

温阳活血方对大鼠阿霉素肾病模型的影响

目的：探讨不同治法治疗原发性肾病综合征高脂血症的疗效差异。方法：用阿霉素（ADR）诱导一种类似人类微小病变肾病模型,然后用中药温阳方、活血方及温阳活血方对模型进行治疗,并设空白、病理及强的松组对照。结果：温阳活血方组尿蛋白、血脂、脂蛋白及肾脏病理损害明显改善;温阳方及活血方组血脂、脂蛋白部分指标及肾脏病理损害有所改善。结论：温阳活血方对ADR肾病的治疗作用较全面,其疗效优于温阳法和活血法。     

薄层扫描法测定安神宁康胶囊中黄芪甲甙的含量

目的：建立测定安神宁康胶囊中黄芪甲甙含量的方法。方法：以氯仿——甲醇——水（65:35:10)的下层为展开剂,用双波长薄层扫描仪测定。结果：黄芪甲甙在1.049μg-5.245μg与峰面积积分值,呈良好的线性关系（r=0.9993,n=5),平均回收率为96.24%。结论：为控制安神宁康胶囊中黄芪甲甙的含量提供了方法。     

酒客乐对酒精性肝损伤大鼠血清微量元素含量的影响

目的 :观察酒客乐对酒精性肝损伤大鼠血清微量元素含量的影响。方法 :用白酒、吡唑、橄榄油的混合液制成酒精性肝损伤模型 ,酒客乐冲剂为防治用药 ,观察血清微量元素Cu、Zn、Se及Mn含量的变化。结果 :与正常组比较 ,肝损伤组血清Se、Cu、Zn含量下降 (P <0 0 1或P <0 0 5 ) ;而防治组血清Se、Cu、Zn含量得以回升 ,其中Zn含量升至 3 2± 0 2 4ug ml,明显高于损伤组 (P <0 0 1)。结论 :酒客乐可通过补充酒精性肝损伤大鼠某些血清微量元素含量间接发挥清除自由基 ,稳定生物膜的作用     

黄芪多糖对糖尿病大鼠微血管病变的作用及机制的研究

目的：探讨黄芪多糖（APS）对糖尿病大鼠微血管病变的影响以及对糖尿病的治疗作用及机制。方法：成年,健康SD大鼠40只,雌雄不限,分成四组：正常对照组,糖尿病组（腹腔注射四氧嘧啶200mg/kg),APS组（造模成功后用APS治疗）,优降糖组（造模成功后用优降糖治疗）。治疗两周时测一次血糖,四周后,测血糖;颈动脉取血测定血清胰素水平,NO和MDA含量。应用形态定量的方法比较各组的心肌病理变化。结果：腹腔注射alloxan(200mg/kg)后的SD大鼠血糖浓度显升高,血清NO,MDA,胰岛素水平明显改变。APS治疗四周后,血糖浓度明显下降,与优降糖治疗组无明显差异,血清NO较未治疗组明显升高（P＜0．01）,血清MDA较未治疗组明显减少（P＜0．01）,血清胰岛素水平升高（P＜0．05）,光镜下观察,糖尿病大鼠的心肌毛细血管数量减少,基底膜增厚,微血管与心肌纤维的比率显减低,这些改变都可被APS改善.结论：APS有降低血糖和保护血管内皮细胞的作用,这可能与APS减轻氧自由基的损伤,影响NO的产生以及促进胰岛B细胞的损伤的恢复有关。