G2-M arrest and antimitotic activity mediated by casticin, a flavonoid isolated from Viticis Fructus (Vitex rotundifolia Linne fil.)

G2-M arrest and antimitotic activity mediated by casticin, a flavonoid isolated from Viticis Fructus (Vitex rotundifolia Linne fil.)
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DOI:
10.1016/j.canlet.2004.01.012
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发表时间:
2004-05-10
期刊:
影响因子:
9.7
通讯作者:
Matsukawa, Y
Matsukawa, Y
中科院分区:
医学1区
文献类型:
--
作者:
Kobayakawa, J;Sato-Nishimori, F;Matsukawa, Y

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黄酮类化合物分布在许多植物中。我们研究了从蔓荆子中分离出的黄酮类化合物、牡荆素、青蒿素、槲皮素和 5,3'-二羟基-6,7,4'-三甲氧基黄烷酮的抗肿瘤作用。与测试的其他黄酮类化合物(IC50 = 15.3-18.6 muM)相比,Casticin 显着抑制 KB 细胞的生长(IC50 = 0.23 muM)。相比之下,与正常细胞系、3T3 Swiss Albino 和 TIG-103 相似,牡蛎素不会抑制 A431 细胞的增殖。流式细胞术分析表明,KB 细胞暴露于牡蛎素会导致 G2-M 期显着停滞。在 KB 细胞的免疫染色中,casticin 破坏了有丝分裂纺锤体。这些结果表明,casticin 的 G2-M 阻滞可能与其抗有丝分裂活性有关,尽管选择性生长抑制的机制尚不清楚。还需要进一步的检查来确认casticin是一种针对特定癌症的低毒性抗肿瘤药物。 (C) 2004 Elsevier Ireland Ltd. 保留所有权利。
Flavonoids are distributed in many plants. We studied the antitumor effects of flavonoids isolated from Viticis Fructus, casticin, artemetin, quercetagetin and 5,3'-dihydroxy-6,7,4' -trimethoxyflavanone. Casticin inhibited the growth of KB cells markedly (IC50 = 0.23 muM), compared with the other flavonoids tested (IC50 = 15.3-18.6 muM). In contrast, casticin did not inhibit the proliferation of A431 cells similar to normal cell lines, 3T3 Swiss Albino and TIG-103. Flow cytometric analyses revealed that the exposure of KB cells to casticin led to significant arrest at G2-M. In immunostaining of KB cells, casticin disrupted mitotic spindles.These results suggest that G2-M arrest by casticin may be relevant to its antimitotic activity, although the mechanism of selective growth inhibition has been unknown. Further examinations are required to confirm that casticin is an antitumor drug for specific cancers with low toxicity. (C) 2004 Elsevier Ireland Ltd. All rights reserved.