MARINE BIOACTIVE COMPOUNDS - STEREOSPECIFIC ANTIINFLAMMATORY ACTIVITY OF NATURAL AND SYNTHETIC CORDIACHROMENE-A

MARINE BIOACTIVE COMPOUNDS - STEREOSPECIFIC ANTIINFLAMMATORY ACTIVITY OF NATURAL AND SYNTHETIC CORDIACHROMENE-A
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DOI:
10.1002/j.1552-4604.1992.tb03785.x
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发表时间:
1992-01-01
影响因子:
2.9
通讯作者:
BRION, JD
BRION, JD
中科院分区:
医学4区
文献类型:
--
作者:
BENSLIMANE, AF;POUCHUS, YF;BRION, JD

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提出了一种新的合成方法,用外消旋混合物的方法合成了海鞘中的生物活性成分紫草烯A(CCA)。以角叉菜胶致大鼠足肿胀为模型,对天然提取物和化学合成的CCA的抗炎活性进行了体内评价。用高岭土诱导的大鼠肉芽肿实验证实了人工合成CCA的活性。两种CCA都有很强的活性,但第一次测试的结果比较表明,只有天然的光学活性异构体具有抗炎作用。CCA对角叉菜胶致大鼠足肿胀的作用与消炎痛相似,是苯丁酮的10倍。
A new synthesis is proposed for cordiachromene A (CCA), a bioactive component of the ascidian Aplidium antillense Gravier, using a method producing a racemic mixture. The anti-inflammatory activities of a natural extract and a chemically synthetic form of CCA were assessed in vivo by carrageenan-induced rat-paw edema. The activity of synthetic CCA was confirmed by a test on kaolin-induced granuloma in the rat. Strong activities were measured for both CCA, but comparison of results of the first test suggests that only the natural optically active isomer has an anti-inflammatory effect. CCA is similar to indomethacin in its effect on carrageenan-induced rat-paw edema and ten times as active as phenylbutazone.