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从巴西红厚壳中分离出的香豆素的抗增殖、细胞毒性和抗肿瘤活性。

Antiproliferative, cytotoxic and antitumour activity of coumarins isolated from Calophyllum brasiliense.

作者信息

Ruiz-Marcial César, Reyes Chilpa Ricardo, Estrada Elizabeth, Reyes-Esparza Jorge, Fariña Germán Garrido, Rodríguez-Fragoso Lourdes

机构信息

Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, México.

出版信息

J Pharm Pharmacol. 2007 May;59(5):719-25. doi: 10.1211/jpp.59.5.0013.

DOI:10.1211/jpp.59.5.0013
PMID:17524238
Abstract

Among the eight Calophyllum species found on the American continent, Calophyllum brasiliense is the most widely distributed. Chemical analysis of this species has shown the presence of xanthones with cancer chemopreventive properties and antifungal activity. Recently, three new coumarins with antineoplastic properties have been found. In this study, we have evaluated the biological effects of the antiproliferative activity of coumarins isolated from C. brasiliense on the survival, cell cycle and apoptosis of cells in-vitro and their antitumour effects in mice. The cytological study showed that coumarins from C. brasiliense reduce the survival of BMK cells (baby mouse kidney cells) by inducing apoptosis and, to a lesser degree, necrosis. The cell cycle was arrested in S-phase and the division of BMK cells was inhibited. Coumarins had caused a reduction of experimental tumours in 83% of animals by the end of the treatment. Therefore, coumarins have the potential to be used alone or in combination with other antineoplastic drugs, and they might increase the effectiveness of other treatments for cancer.

摘要

在美洲大陆发现的8种红厚壳属植物中,巴西红厚壳分布最为广泛。对该物种的化学分析表明,其含有具有癌症化学预防特性和抗真菌活性的氧杂蒽酮。最近,又发现了三种具有抗肿瘤特性的新香豆素。在本研究中,我们评估了从巴西红厚壳中分离出的香豆素的抗增殖活性对体外细胞存活、细胞周期和凋亡的生物学效应,以及它们对小鼠的抗肿瘤作用。细胞学研究表明,巴西红厚壳中的香豆素通过诱导凋亡以及程度较轻的坏死来降低BMK细胞(幼鼠肾细胞)的存活率。细胞周期停滞在S期,BMK细胞的分裂受到抑制。到治疗结束时,香豆素使83%的动物实验性肿瘤体积减小。因此,香豆素有可能单独使用或与其他抗肿瘤药物联合使用,并且它们可能会提高其他癌症治疗方法的有效性。

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