中国临床药理学杂志
中國臨床藥理學雜誌
중국림상약이학잡지
THE CHINESE JOURNAL OF CLINICAL PHARMACOLOGY
2015年
8期
635-639
,共5页
贾诩%李茂星%陶锐%傅仲学
賈詡%李茂星%陶銳%傅仲學
가후%리무성%도예%부중학
环烯醚萜苷%8-去羟基山栀子苷%镇痛%抗炎
環烯醚萜苷%8-去羥基山梔子苷%鎮痛%抗炎
배희미첩감%8-거간기산치자감%진통%항염
iri doid glycosides%8-deoxyshanzhiside%analgesic%anti-inflammatory
目的:比较独一味中环烯醚萜苷化合物在小鼠体内的镇痛与抗炎活性。方法5种环烯醚萜苷化合物:8-乙酰氧基山栀子苷甲酯(Ⅰ)、8-去羟基山栀子苷(Ⅱ)、sesamoside (Ⅲ)、7,8-dehydro -penstemoside (Ⅳ)、山栀子苷甲酯(Ⅴ),均在小鼠尾静脉一次注射给药200 mg? kg-1,阳性对照组给予吗啡5 mg? kg-1,空白对照组给予0.9%氯化钠。用经典的动物实验模型,评价其体内镇痛、抗炎作用。结果给药后5种单体化合物均显示了一定的镇痛抗炎活性,其中Ⅰ和Ⅱ都能显著减少小鼠扭体次数,抑制二甲苯引起的小鼠耳肿胀,抑制足部注射福尔马林所致第二阶段疼痛反应,抑制角叉菜胶诱导小鼠足肿胀,降低醋酸诱导的腹腔通透性的增加,减少腹腔内伊文思蓝含量和腹腔白细胞游走。但不能延长小鼠热板痛阈值,不能减少福尔马林致疼痛第一阶段舔足次数。结论藏药独一味中的5种环烯醚萜苷单体,尤其是8-乙酰氧基山栀子苷甲酯和8-去羟基山栀子苷具有较好的体内镇痛、抗炎作用。
目的:比較獨一味中環烯醚萜苷化閤物在小鼠體內的鎮痛與抗炎活性。方法5種環烯醚萜苷化閤物:8-乙酰氧基山梔子苷甲酯(Ⅰ)、8-去羥基山梔子苷(Ⅱ)、sesamoside (Ⅲ)、7,8-dehydro -penstemoside (Ⅳ)、山梔子苷甲酯(Ⅴ),均在小鼠尾靜脈一次註射給藥200 mg? kg-1,暘性對照組給予嗎啡5 mg? kg-1,空白對照組給予0.9%氯化鈉。用經典的動物實驗模型,評價其體內鎮痛、抗炎作用。結果給藥後5種單體化閤物均顯示瞭一定的鎮痛抗炎活性,其中Ⅰ和Ⅱ都能顯著減少小鼠扭體次數,抑製二甲苯引起的小鼠耳腫脹,抑製足部註射福爾馬林所緻第二階段疼痛反應,抑製角扠菜膠誘導小鼠足腫脹,降低醋痠誘導的腹腔通透性的增加,減少腹腔內伊文思藍含量和腹腔白細胞遊走。但不能延長小鼠熱闆痛閾值,不能減少福爾馬林緻疼痛第一階段舔足次數。結論藏藥獨一味中的5種環烯醚萜苷單體,尤其是8-乙酰氧基山梔子苷甲酯和8-去羥基山梔子苷具有較好的體內鎮痛、抗炎作用。
목적:비교독일미중배희미첩감화합물재소서체내적진통여항염활성。방법5충배희미첩감화합물:8-을선양기산치자감갑지(Ⅰ)、8-거간기산치자감(Ⅱ)、sesamoside (Ⅲ)、7,8-dehydro -penstemoside (Ⅳ)、산치자감갑지(Ⅴ),균재소서미정맥일차주사급약200 mg? kg-1,양성대조조급여마배5 mg? kg-1,공백대조조급여0.9%록화납。용경전적동물실험모형,평개기체내진통、항염작용。결과급약후5충단체화합물균현시료일정적진통항염활성,기중Ⅰ화Ⅱ도능현저감소소서뉴체차수,억제이갑분인기적소서이종창,억제족부주사복이마림소치제이계단동통반응,억제각차채효유도소서족종창,강저작산유도적복강통투성적증가,감소복강내이문사람함량화복강백세포유주。단불능연장소서열판통역치,불능감소복이마림치동통제일계단첨족차수。결론장약독일미중적5충배희미첩감단체,우기시8-을선양기산치자감갑지화8-거간기산치자감구유교호적체내진통、항염작용。
Objective To study the analgesic and anti -inflammatory ac-tivities of iridoid glycoside from Lamiophlomis rotata in mice . Methods After one dose of iridoid glycosides ( 200 mg? kg -1 ) , 8 -O-acetylshanzhiside methylester , 8 -deoxyshanzhiside , sesamoside , 7 ,8-dehydropenstemoside , and shanzhiside methylester , were adminis-tered by tail vein injection .Morphine ( 5 mg? kg -1 ) and aspirin ( 100 mg? kg-1 ) were used as positive controls , and 0.9% NaCl as negative control.The hot plate test , acetic-acid induced writhing test , formalin test , carrageenan -induced paw edema test and xylene -induced ear swelling test , peritoneal capillary permeability test on mice were used to test the analgesic and anti-inflammatory activities.Results Compared with blank group , these five iridoid glycosides could remarkably induce the number of writhing reaction with the inhibition ratio were 43.96%, 47.81%, 25.96%, 37.70%, and 26.23% ( P <0.01 , P <0.01 , P<0.05 , P<0.01 , and P<0.05 );could inhibit the xylene -induced ear swelling were 0.79%( P<0.05 ) , 43.07% ( P<0.01 ) , 7.90%, 14.25%, and 5.59%; exhibited significant analgesic activities on the second period of formalin test by 8 -O -acetylshanzhiside methylester and 8-deoxyshanzhiside ( P<0.01 ) .All compounds exhibited effects on paw edema induced by carrageenan in 1 hour, but only 8-O-acetylshanzhiside methylester and 8-deoxy-shanzhiside were effective in 3 hours with inhibition ratio were 32.84%and 40.36%, respectively.They also reduced permeability of ab-dominal capillaries and inflammatory peritoneal exudation induced by acetic acid , especial for 8-O-acetylshanzhiside methylester, 8-deoxyshanzhiside and sesamoside.On the other hand, these iridoid glycosides couldn′t prolong the leg-licking time in hot plate test and the first period of formalin test .Conclusion The five iridoid glycosides , espicially 8-O-acetylshanzhiside methylester and 8-deoxyshanzhiside exhibited significant analgesic and anti -inflammatory activities.