STRUCTURE-RELATED INHIBITING ACTIVITY OF SOME TOBACCO CEMBRANOIDS ON THE PROSTAGLANDIN SYNTHESIS IN-VITRO

STRUCTURE-RELATED INHIBITING ACTIVITY OF SOME TOBACCO CEMBRANOIDS ON THE PROSTAGLANDIN SYNTHESIS IN-VITRO
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DOI:
10.1055/s-2006-959684
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发表时间:
1993-08-01
期刊:
影响因子:
2.7
通讯作者:
WAHLBERG, I
WAHLBERG, I
中科院分区:
医学3区
文献类型:
--
作者:
OLSSON, E;HOLTH, A;WAHLBERG, I

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已检测到西松烷类的 8 种二萜化合物对体外前列腺素合成具有结构相关的抑制作用 (1-8)。 4,6-二醇 1 和 2 是所研究的西松烷内酯中活性最强的,其 IC50 值分别为 0. 36 和 0. 39 mM,而乙酰水杨酸的 IC50 值为 1.4。发现11,12双键(5-8)处发生氧化的西松烷酯活性较低,而4-羟基-6-氧西松烷酯3和4的效果低于1和2,但高于5-8。
Structure-related inhibitory effects on the prostaglandin synthesis in vitro have been detected among eight diterpenoids of the cembrane class (1-8). The 4,6-diols 1 and 2 are the most active of the cembranoids studied with IC50 values of 0. 36 and 0. 39 mM, respectively, as compared with an IC50 value of 1.4 for acetylsalicylic acid. Lower activities are found for cembranoids having undergone oxidation of/at the 11,12 double bond (5-8), while the 4-hydroxy-6-oxocembranoids 3 and 4 exhibit effects lower than those of 1 and 2 but higher than those of 5-8.