Um panorama atual da química e da farmacologia de naftoquinonas, com ênfase na beta-lapachona e derivados

Química Nova

Milton N. Da Silva¹  Vítor F. Ferreira¹  Maria Cecília B. V. De Souza¹ 

[1] ,Universidade Federal Fluminense Instituto de Química Departamento de Química OrgânicaNiterói RJ

关键词: beta-Lapachone;    naphthoquinone;    pyranaphthoquinone;    apoptosis;   

DOI  :  10.1590/S0100-40422003000300019

来源: SciELO

【 摘 要 】

Naphthoquinones have been extensively studied due to their activity as topoisomerase inhibitors. These enzymes are critical to DNA replication in cells. In addition, naphthoquinones have been shown to induce what are known as "reactive oxygen species" that can cause damage to cells. beta-Lapachone is a very important pyranaphthoquinone obtained from the heartwood of the lapacho tree, Tabebuia avellanedae Lorentz ex. Griseb. (Bignoniaceae), and other Tabebuia trees native to Central and South America and chemically from lapachol. beta-Lapachone has a diversity of useful biological activities against various cancer cell lines such as human ovarian and prostate tumors and, at lower doses is a radiosensitizer of several human cancer cell lines. It gives rise to a variety of effects in vitro including the inhibition or activation of topoisomerase I an II in a distinct manner from that of other topoisomerase inhibitors. This review intend to discuss some details of the mechanisms of quinone-induced cell damage and death, and we also summarize results of the literature indicating that b-Lapachone may take part in quinone-elicited apoptosis despite the fact that its mechanism of action in vivo and its targets are still unknown.

【 授权许可】

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