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甘遂根中的二萜类化合物及其对非洲爪蟾细胞分裂的体外作用(第2部分)

Diterpenes from the roots of Euphorbia kansui and their in vitro effects on the cell division of Xenopus (part 2).

作者信息

Wang Li-Yan, Wang Nai-Li, Yao Xin-Sheng, Miyata Syohei, Kitanaka Susumu

机构信息

Department of Natural Products Chemistry, Shenyang Pharmaceutical Universit, Shenhe District, Shenyang 110016, People's Republic of China.

出版信息

Chem Pharm Bull (Tokyo). 2003 Aug;51(8):935-41. doi: 10.1248/cpb.51.935.

Abstract

Four new ingenane-type diterpenes, 3-O-(2,3-dimethylbutanoyl)-13-O-dodecanoyl-20-O-acetylingenol (1), 3-O-(2,3-dimethylbutanoyl)-13-O-dodecanoyl-20-deoxyingenol (2), 3-O-(2E,4Z-decadienoyl)-20-deoxyingenol (3), and 3-O-(2E,4E-decadienoyl)-20-deoxyingenol (4), two new jatrophane-type diterpenes, kansuinins D (9) and E (10), and four known ingenane-type diterpenes were isolated from the root of Euphorbia kansui. Their structures were elucidated by spectroscopic and chemical analysis, and individual Xenopus cells at the blastular stage were cultured with the diterpenes to test for biological activity. 20-Deoxyingenol diterpenes 3 and 4 induced the greatest cell cleavage arrest (0.5 micro g/ml of each compound resulted in >75% cleavage arrest), but cell cleavage inhibitory activity became weak when C-16 had an acyl residue. In contrast, the jatrophane diterpene kansuinin D (9) showed no activity.

摘要

从甘遂根部分离得到4个新的瑞香烷型二萜,3 - O -(2,3 - 二甲基丁酰基)- 13 - O - 十二烷酰基 - 20 - O - 乙酰基瑞香毒素(1)、3 - O -(2,3 - 二甲基丁酰基)- 13 - O - 十二烷酰基 - 20 - 脱氧瑞香毒素(2)、3 - O -(2E,4Z - 癸二烯酰基)- 20 - 脱氧瑞香毒素(3)和3 - O -(2E,4E - 癸二烯酰基)- 20 - 脱氧瑞香毒素(4),2个新的麻风树烷型二萜,甘遂素D(9)和甘遂素E(10),以及4个已知的瑞香烷型二萜。通过光谱和化学分析阐明了它们的结构,并用这些二萜培养囊胚期的非洲爪蟾单个细胞以测试其生物活性。20 - 脱氧瑞香毒素二萜3和4诱导的细胞分裂停滞作用最强(每种化合物0.5μg/ml导致>75%的分裂停滞),但当C - 16有酰基残基时,细胞分裂抑制活性变弱。相比之下,麻风树烷二萜甘遂素D(9)没有活性。

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