SERIES ON LIVER-PROTECTIVE DRUGS .25. ANTIHEPATOTOXIC ACTIONS OF GINGEROLS AND DIARYLHEPTANOIDS
SERIES ON LIVER-PROTECTIVE DRUGS .25. ANTIHEPATOTOXIC ACTIONS OF GINGEROLS AND DIARYLHEPTANOIDS
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DOI：
10.1016/0378-8741(85)90025-x
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发表时间：
1985-01-01
影响因子：
5.4
通讯作者：
SANKAWA, U
中科院分区：
文献类型：
--
作者：
HIKINO, H;KISO, Y;SANKAWA, U
利用四氯化碳和半乳糖胺诱导的原代培养大鼠肝细胞毒性，对姜辣素、姜酚、二芳基庚烷及相关类似物的抗肝毒作用进行了评估。大多数同系物在这些检测方法中表现出显著的作用。四氯化碳测定法似乎在确定构效关系方面最有用。姜辣素和姜辣素的抗肝毒活性与侧链的长度有关，其中[7]-和[8]-伴体的活性最强。姜辣素比相应的shogaol表现出更强烈的活动。在二芳基七烷类化合物中，苯基环上引入羟基基团导致活性增加；然而，羟基的位置和数量对活性的影响随碳骨架的不同而不同。
The antihepatotoxic effects of gingerols, shogaols, diarylheptanoids and related analogues were assessed utilizing carbon tetrachloride- and galactosamine-induced cytotoxicity in primary cultured rat hepatocytes. Most congeners exhibited significant actions in these assay methods. The carbon tetrachloride assay appeared to be most useful in defining structure-activity relationships. The antihepatotoxic activity of gingerols and shogaols was dependent on the length of the side chain with the [7]- and [8]- companions elicting the strongest activity. The gingerols exerted more intense activity than the corresponding shogaols. In the diarylheptanoids, introduction of hydroxyl groupings on the phenyl rings caused increased activity; however, the effect of the positions and number of hydroxyls on activity was variable depending on the carbon skeleton.