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目的:研究短葶山麦冬水提物((Lm-a)、总皂苷(Lm-s)及主要成分Lm-3的抗炎活性,为其临床应用于治疗炎性疾病提供药理学依据。方法:采用二甲苯诱导小鼠耳廓肿胀和角叉菜胶或组胺诱导小鼠足跖肿胀模型,评价Lm-a,Lm-s和Lm-3灌胃给药的体内抗炎活性;采用肿瘤坏死因子(TNF-α)或佛波酯(PMA)诱导的髓样白血病细胞(HL-60)与人脐静脉内皮细胞(ECV304)黏附模型,考察Lm-3的体外抗炎活性。结果:单次灌胃给予Lm-a(336和672mg.kg-1)明显抑制二甲苯致小鼠耳廓肿胀和角叉菜胶致小鼠足跖肿胀;Lm-s和Lm-3(23.2和4.6mg.kg-1,相当于Lm-a672mg.kg-1)对上述炎症模型显示相似的抗炎活性;相当于短亭山麦冬4g.kg-1生药量的Lm-a、Lm-s及Lm-3均明显抑制组胺致小鼠足跖肿胀;Lm-3(0.01、0.1和1μmol.L-1)体外显著抑制TNF-α或PMA诱导的HL-60与ECV304细胞的粘附作用,提示其抗炎机制可能与调节蛋白激酶C通路等有关。结论:短葶山麦冬具有显著体内外抗炎活性,其主要活性部位和成分为总皂苷和Lm-3,为其临床应用于治疗炎性疾病提供药理学依据。
OBJECTIVE: To study the anti-inflammatory activity of aqueous extracts of Lonicera mandshurica (Lm-a), total saponins (Lm-s) and Lm-3, and to provide pharmacological evidences for its clinical application in the treatment of inflammatory diseases. Methods: Xylol was used to induce mouse auricles swelling and carrageenan or histamine-induced mouse paw edema model to evaluate the anti-inflammatory activity of Lm-a, Lm-s and Lm-3 administered intragastrically. 3 anti-inflammatory activity of Lm-3 in vitro.Methods: The myeloid leukemia cells (HL-60) and human umbilical vein endothelial cells (ECV304) induced by tumor necrosis factor (TNF- Single oral administration of Lm-a (336 and 672 mg.kg-1) significantly inhibited xylene-induced auricle swelling and carrageenan-induced paw edema in mice; Lm-s and Lm-3 mg.kg-1, which corresponds to Lm-a672mg.kg-1) showed similar anti-inflammatory activity to the above inflammatory model; Lm-a, Lm-s corresponding to 4g.kg- Lm-3 significantly inhibited the paw swelling of mice induced by histamine; Lm-3 (0.01,0.1 and 1μmol.L-1) significantly inhibited the adhesion of HL-60 and ECV304 cells induced by TNF- Suggesting that its anti-inflammatory mechanism may be related to the regulation of protein kinase C pathway, etc. Conclusion: short Liriope has significant in vivo anti-inflammatory activity, the active site of the main ingredient and total saponins and Lm-3, offering pharmacology clinical application for the treatment of inflammatory diseases.