Structure-activity relationships and the cytotoxic effects of novel diterpenoid alkaloid derivatives against A549 human lung carcinoma cells.
Structure-activity relationships and the cytotoxic effects of novel diterpenoid alkaloid derivatives against A549 human lung carcinoma cells.
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DOI：
10.1007/s11418-010-0452-3
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发表时间：
2011-01
影响因子：
3.3
通讯作者：
Kashiwakura I
中科院分区：
文献类型：
--
作者：
Wada K;Hazawa M;Takahashi K;Mori T;Kawahara N;Kashiwakura I
The cytotoxicity of three alkaloids from the roots of Aconitum yesoense var. macroyesoense as well as 36 semi-synthetic C20-diterpenoid atisine-type alkaloid derivatives against A549 human lung carcinoma cells was examined. Ten acylated alkaloid derivatives, pseudokobusine 11-veratroate (9), 11-anisoate (12), 6,11-dianisoate (14), 11-p-nitrobenzoate (18), 11,15-di-p-nitrobenzoate (22), 11-cinnamate (25) and 11-m-trifluoromethylbenzoate (27), and kobusine 11-p-trifluoromethylbenzoate (35), 11-m-trifluoromethylbenzoate (36) and 11,15-di-p-nitrobenzoate (39), exhibited cytotoxic activity, and 11,15-dianisoylpseudokobusine (16) was found to be the most potent cytotoxic agent. Their IC50 values against A549 cells ranged from 1.72 to 5.44 μM. In the occurrence of cytotoxic effects of atisine-type alkaloids, replacement by an acyl group at both C-11 and C-15 resulted in the enhancement of activity of the parent alkaloids compared to that from having hydroxy groups at this position, and the presence of a hydroxy group at the C-6 position was required for the cytotoxic effects. These acylated alkaloid derivatives inhibit cell growth through G1 arrest.
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影响因子：
2
作者：
Lee, Jong-Won;Min, Hye-Young;Lee, Sang Kook
通讯作者：
Lee, Sang Kook
影响因子：
2
作者：
Wada, K;Ishizuki, S;Kawahara, N
通讯作者：
Kawahara, N
影响因子：
3.4
作者：
Hazawa, Masaharu;Takahashi, Kenji;Kashiwakura, Ikuo
通讯作者：
Kashiwakura, Ikuo
影响因子：
2
作者：
Wada, K;Ishizuki, S;Kawahara, N
通讯作者：
Kawahara, N
影响因子：
5.6
作者：
Ogura, Hirotsugu;Tsukumo, Yoshinori;Kataoka, Takao
通讯作者：
Kataoka, Takao