中国临床药理学与治疗学
中國臨床藥理學與治療學
중국림상약이학여치료학
CHINESE JOURNAL OF CLINICAL PHARMACOLOGY
2003年
5期
506-510
,共5页
张洪泉%许正新%葛晓群%李吉平%孙云%柳丽
張洪泉%許正新%葛曉群%李吉平%孫雲%柳麗
장홍천%허정신%갈효군%리길평%손운%류려
药理学%白介素-1%受体拮抗剂%豚鼠%组胺%乙酰胆碱%卵白蛋白%哮喘
藥理學%白介素-1%受體拮抗劑%豚鼠%組胺%乙酰膽堿%卵白蛋白%哮喘
약이학%백개소-1%수체길항제%돈서%조알%을선담감%란백단백%효천
pharmacology%interleukin-1%receptora tagonist%histamine%acetylcholine%asthma%contraction%guinea pigs
目的:观察白介素-1受体拮抗剂(IL-1ra)对致敏豚鼠的抗喘作用.方法:用卵白蛋白致敏豚鼠,用张力换能器和MedLab软件记录气道平滑肌的肌张力和收缩活动.结果:整体实验时,在0.33~9.0 mg@kg-1剂量范围内,IL-1ra能使组胺-乙酰胆碱及卵白蛋白诱发的致敏豚鼠哮喘的潜伏期延长,动物跌倒率降低.此作用具有剂量依赖性.其中,9.0 mg@kg-1剂量组的作用与异丙基肾上腺素相同;离体实验时,3×10-7 mol@L-1以上浓度的IL-1ra对气管平滑肌具有直接松弛作用,其EC50为5.88×10-7 mol@L-1;10-7 mol@L-1的IL-1ra能对抗卵白蛋白引起的气管平滑肌肌张力的增加:3×10-7 mol@L-1以上剂量组的IL-1ra预防给药则能使卵白蛋白诱发的气管平滑肌的收缩程度显著降低,其IC50为4.48×10-7 mol@L-1.结论:IL-1ra能直接松弛致敏豚鼠的气管平滑肌,拮抗多种抗原诱发的致敏豚鼠的哮喘发作.
目的:觀察白介素-1受體拮抗劑(IL-1ra)對緻敏豚鼠的抗喘作用.方法:用卵白蛋白緻敏豚鼠,用張力換能器和MedLab軟件記錄氣道平滑肌的肌張力和收縮活動.結果:整體實驗時,在0.33~9.0 mg@kg-1劑量範圍內,IL-1ra能使組胺-乙酰膽堿及卵白蛋白誘髮的緻敏豚鼠哮喘的潛伏期延長,動物跌倒率降低.此作用具有劑量依賴性.其中,9.0 mg@kg-1劑量組的作用與異丙基腎上腺素相同;離體實驗時,3×10-7 mol@L-1以上濃度的IL-1ra對氣管平滑肌具有直接鬆弛作用,其EC50為5.88×10-7 mol@L-1;10-7 mol@L-1的IL-1ra能對抗卵白蛋白引起的氣管平滑肌肌張力的增加:3×10-7 mol@L-1以上劑量組的IL-1ra預防給藥則能使卵白蛋白誘髮的氣管平滑肌的收縮程度顯著降低,其IC50為4.48×10-7 mol@L-1.結論:IL-1ra能直接鬆弛緻敏豚鼠的氣管平滑肌,拮抗多種抗原誘髮的緻敏豚鼠的哮喘髮作.
목적:관찰백개소-1수체길항제(IL-1ra)대치민돈서적항천작용.방법:용란백단백치민돈서,용장력환능기화MedLab연건기록기도평활기적기장력화수축활동.결과:정체실험시,재0.33~9.0 mg@kg-1제량범위내,IL-1ra능사조알-을선담감급란백단백유발적치민돈서효천적잠복기연장,동물질도솔강저.차작용구유제량의뢰성.기중,9.0 mg@kg-1제량조적작용여이병기신상선소상동;리체실험시,3×10-7 mol@L-1이상농도적IL-1ra대기관평활기구유직접송이작용,기EC50위5.88×10-7 mol@L-1;10-7 mol@L-1적IL-1ra능대항란백단백인기적기관평활기기장력적증가:3×10-7 mol@L-1이상제량조적IL-1ra예방급약칙능사란백단백유발적기관평활기적수축정도현저강저,기IC50위4.48×10-7 mol@L-1.결론:IL-1ra능직접송이치민돈서적기관평활기,길항다충항원유발적치민돈서적효천발작.
AIM: To observe the anti-asthmatic ef-fects of interleukin-1 receptor antagonist (IL-1ra) in sen-sitized guinea pigs. METHODS: Sensitized guinea pigswere made by ovalbumin, and the tension and contractionof tracheal smooth muscles were measured by force-dis-placement transducer and MedLab software. RESULTS:In the doses of 0.33 - 9.0 mg@ kg- 1, IL- 1 ra prolongedthe asthmatic incubation period and reduced animal tum-ble ratio in asthma guinea pigs induced by histamine-ace-tylcholine or ovalbumin. These effects were dose-depen-dent. In vitro, IL-1 ra could directly relax tracheal smoothmuscles up the dose of 3 × 10-7mol@L-1 and the EC50value was 5.88 × 10-7mol@L-1. IL-1ra antagonized theincrease of trachea tension stimulated by ovalbumin at thedose of 10-7mol@ L-1. Moreover, IL - 1ra prevented tra-cheal smooth muscle contraction induced by ovalbumin upthe dose of 3 × 10-7 mol@L-1, and the IC50 value was4.48 × 10-7mol@L-1. CONCLUSIONS: IL-1ra can di-rectly relax tracheal smooth muscles in sensitized guineapigs, and antagonize asthma caused by many kinds of antigens.