摘要
目的制备甘草次酸、11-脱氧甘草次酸的钠盐,并研究甘草次酸钠、11-脱氧甘草次酸钠的抗炎作用及其可能的机制。方法在无水乙醇条件下,与氢氧化钠反应分别得到相应的钠盐。并通过二甲苯致小鼠耳肿胀、纸片致小鼠慢性肉芽肿及气囊性滑膜炎3个模型观察甘草次酸钠、11-脱氧甘草次酸钠的抗炎作用,并测定小鼠血清和炎症液中前列腺素E2(PGE2)的含量和一氧化氮合酶(NOS)活性。结果所得钠盐通过熔点、红外、紫外等表征其结构。10、20、40 mg/kg的11-脱氧甘草次酸钠能明显抑制二甲苯致小鼠耳片肿胀,也可显著抑制滤纸片所致小鼠慢性肉芽肿,可使血清中PGE2含量减少。10、40 mg/kg的11-脱氧甘草次酸钠能使炎症液中的PGE2含量减少。在血清和炎症液中,10 mg/kg的11-脱氧甘草次酸钠可使NOS活性和NO的含量显著下降。结论甘草次酸、11-脱氧甘草次酸的钠盐从一定程度上提高了这类化合物的水溶性、吸收性,改善了相应的药理作用。其中11-脱氧甘草次酸钠有较好的抗炎活性。其机制可能与抑制PGE2和NO合成及抗脂质过氧化有关。
Objective To prepare the sodium salt of glycyrrhetinic acid and 11-deoxyglycyrrhetinic acid, and to study the anti-inflammatory effect and possible mechanisms of 11-sodium deoxyglycyrrhetinic acid. Methods The corresponding sodium salt was obtained by the reaction of these compounds with sodium hydroxide, under the condition of absolute ethyl alcohol. The anti-inflammatory effects of 11-sodium deoxyglycyrrhetinic acid were observed by 3 models.-xylene-induced mice ear swelling, chronic granuloma by filter paper method, air sac synovltis. The prostaglandin E2（PGE2） in serum and activity of nitric oxide synthase （NOS） were determined. Results The obtained sodium salt were characterized by melting point, IR and ultraviolet spectrophotometry, etc. 11-sodium deoxyglycyrrhetinic acid of 10, 20, 40 mg/ kg could inhibit xylene-induced mice ear swelling as well as chronic granuloma by filter paper method obviously, and decreased PGE2 level in serum, ll-sodium deoxyglycyrrhetinic acid of 10, 40 mg/kg could decrease PGE2 level and also reduce the activity of NOS and the level of NO significantly. Conelusion The water solubility of these pentacyclic triterpenoids increased to a certain extent, and the corresponding pharmacological actions can be improved accordingly. 11- sodium deoxyglycyrrhetinic acid has a certain anti-inflammatory effect, and it may be related to the inhibitory effects of the synthesis of PGE2 and NO, besides the inhibitory effect of lipid peroxidation.
出处
《实用药物与临床》
CAS
2008年第3期182-184,共3页
Practical Pharmacy and Clinical Remedies
