Diterpenes from the roots of Euphorbia kansui and their in vitro effects on the cell division of Xenopus
Diterpenes from the roots of Euphorbia kansui and their in vitro effects on the cell division of Xenopus
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DOI：
10.1021/np0200921
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发表时间：
2002-09-01
影响因子：
5.1
通讯作者：
Kitanaka, S
中科院分区：
文献类型：
--
作者：
Wang, LY;Wang, NL;Kitanaka, S
从甘遂根中分离得到12个多环二萜化合物。其中9个化合物均鉴定为吲哚骨架，分别为20-O-(2‘E，4’E-十碳二烯基)吲哚(1)，20-O-(2‘E，4’Z-十碳二烯基)吲哚(2)，3-O-(2‘E，4’Z-十碳二烯基)吲哚(3)，3-O-(2‘E，4’E-十碳二烯基)吲哚(4)，3-O-(2‘E，4’Z-十碳二烯基)-5-O-乙酰基(5)，3-O-(2‘E，4’E-十碳二烯基)3-O-(2‘E，4’E-十碳二烯基)-20-O-乙酰二烯醇(6)，3-O-(2‘E，4’E-十碳二烯基)-20-O-乙酰二烯醇(7)，20-O-(癸二酰基)橙皮醇(8)和5-O-(2‘E，4’E-十碳二烯基)橙皮醇(9)，以及三个具有黄腐烷骨架的化合物，甘草素A(12)，B(11)和C(10)。化合物1、2、5、9和12为新化合物，而化合物4和7被指定为新的几何构型。通过波谱和化学分析确定了它们的结构。体外培养的非洲爪哇胚胎期单个细胞被1-9个卵裂停滞剂处理(每种化合物0.5个/毫升，卵裂停滞率为75%)。在3个麻疯烷二萜(10-12)中，只有甘遂素B(11)显示出任何活性，当浓度为50µg/m L时，切割停滞率为87%。
Twelve polycyclic diterpenes have been isolated from the roots of Euphorbia kansui. Nine were assigned with an ingenol skeleton, 20-O-(2'E,4'E-decadienoyl)ingenol (1), 20-O-(2'E,4'Z-decadienoyl)ingenol (2), 3-O-(2'E,4'Z-decadienoyl)ingenol (3), 3-O-(2'E,4'E-decadienoyl)ingenol (4), 3-O-(2'E,4'Z-decadienoyl)-5-O-acetylingenol (5), 3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol (6), 3-O-(2'E,4'E-decadienoyl)-20-O-acetylingenol (7), 20-O-(decanoyl)ingenol (8), and 5-O-(2'E,4'E-decadienoyl)ingenol (9), and three with a jatrophane skeleton, kansuinins A (12), B (11), and C (10). Compounds 1, 2, 5, 9, and 12 are new compounds, while 4 and 7 were assigned with new geometric configurations. Their structures were elucidated by spectroscopic and chemical analysis. In vitro treatment of cultured individual Xenopus cells at the blastular stage with 1-9 arrested cleavage significantly (0.5 mug/mL of each compound resulted in >75% cleavage arrest). Of the three jatrophane diterpenes (10-12), only kansuinin B (11) showed any activity, resulting in 87% cleavage arrest at 50 mug/mL.