Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata

Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata
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DOI:
10.1016/j.bmcl.2004.12.026
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发表时间:
2005-02-15
影响因子:
2.7
通讯作者:
Kobayashi, J
Kobayashi, J
中科院分区:
医学4区
文献类型:
--
作者:
Morita, H;Koyama, K;Kobayashi, J

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8个二苯乙烯类化合物,1-(p-hydroxybenzyl)-4,8-dimethoxyphenanthrene-2,7-diol(1),2,7-dihydroxy-1,3-bis(p-hydroxybenzyl)4-methoxy-9,10-dihydrophenanthrene(2),4,7-dihydroxy-1-(p-hydroxybenzyl)-2-methoxy-9,10-dihydrophenanthrene(3),3,3‘-dihydroxy-2’,6‘-bis(p-hydroxybenzyl)-5-methoxybibenzyl(4),3’,5-dihydroxy-2-(p-hydroxybenzyl)-3-methoxybibenzyl(5),blestrienes B(6)和C(7),在抑制微管蛋白聚合作用的指导下,从白头翁块茎中分离得到白藜芦醇A(8)。其中,双苄基4和5分别在IC50为10um时抑制微管蛋白的聚合。此外,双苯并[4]可增强SN-38对BCRP转导的K562(K562/BCRP)细胞的细胞毒作用。(C)2004爱思唯尔有限公司。保留所有权利。
Eight stilbenoids, 1-(p-hydroxybenzyl)-4,8-dimethoxyphenanthrene-2,7-diol (1), 2,7-dihydroxy-1,3-bis(p-hydroxybenzyl)4-methoxy-9,10-dihydrophenanthrene (2), 4,7-dihydroxy-1-(p-hydroxybenzyl)-2-methoxy-9,10-dihydrophenanthrene (3), 3,3'-dihydroxy-2',6'-bis(p-hydroxybenzyl)-5-methoxybibenzyl (4), 3',5-dihydroxy-2-(p-hydroxybenzyl)-3-methoxybibenzyl (5), blestriarenes B (6) and C (7), and blestrianol A (8) have been isolated by the guidance of inhibitory effect of tubulin polymerization from the tubers of Bletilla striata (Orchidaceae). Among them, both of bisbenzyls 4 and 5 inhibited the polymerization of tubulin at IC50 10 muM, respectively. Furthermore bisbenzy] 4 potentiated the cytotoxicity of SN-38 in BCRP-transduced K562 (K562/BCRP) cells. (C) 2004 Elsevier Ltd. All rights reserved.