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洋甘比宁细胞毒性:一种从鸭脚樟(樟科)中提取的具有药理活性的木脂素。

Yangambin cytotoxicity: a pharmacologically active lignan obtained from Ocotea duckei vattimo (Lauraceae).

作者信息

Monte Neto Rubens L, Sousa Louisa M A, Dias Celidarque S, Filho José M Barbosa, Oliveira Márcia R

机构信息

Laboratório de Tecnologia Farmacêutica, Universidade Federal da Paraíba, 58051-970, João Pessoa, Paraíba, Brazil.

出版信息

Z Naturforsch C J Biosci. 2008 Sep-Oct;63(9-10):681-6. doi: 10.1515/znc-2008-9-1012.

DOI:10.1515/znc-2008-9-1012
PMID:19040107
Abstract

The in vitro cytotoxic potential of yangambin was evaluated. Yangambin is a pharmacologically active furofuran lignan obtained from the leaves of Ocotea duckei. It is the major compound from the lignoids fraction. Yangambin presented low cytotoxicity in all in vitro models analyzed. Its cytotoxicity to murine macrophages was measured by the Trypan blue dye exclusion test and MTT reduction assay, resulting in high CC50 values of 187.0 microg/mL (383.3 microM) and 246.7 microg/mL (504.3 microM), respectively. The difference obtained in the inhibitory concentrations aforementioned can be explained, at least in part, by the different principles of the methods. While the MTT reduction assay evaluates the ability of yangambin to inhibit the activity of the mitochondrial enzyme succinate dehydrogenase, the Trypan blue dye exclusion test evaluates possible damages to the integrity of the cytoplasmic membrane which result in cell death. The capacity of yangambin to inhibit the sea urchin embryonic development showed that it has low antimitotic and teratogenic potential, once continued exposure of embryos to concentrations up to 500 microg/mL (1.025 microM) did not result in an inhibitory effect on the first egg cleavages. Such low in vitro cytotoxicity is correlated with the low acute toxicity previously studied. All these data, together with the various therapeutic properties of yangambin, make this lignan a promising one for a new drug.

摘要

对洋甘菊素的体外细胞毒性潜力进行了评估。洋甘菊素是一种从杜克奥寇梯木(Ocotea duckei)叶子中提取的具有药理活性的呋喃呋喃型木脂素。它是木脂素类成分中的主要化合物。在所有分析的体外模型中,洋甘菊素均表现出低细胞毒性。通过台盼蓝染料排斥试验和MTT还原试验测定了其对小鼠巨噬细胞的细胞毒性,结果CC50值分别高达187.0微克/毫升(383.3微摩尔)和246.7微克/毫升(504.3微摩尔)。上述抑制浓度的差异至少部分可以通过方法的不同原理来解释。MTT还原试验评估洋甘菊素抑制线粒体酶琥珀酸脱氢酶活性的能力,而台盼蓝染料排斥试验评估对细胞质膜完整性可能造成的损害,这种损害会导致细胞死亡。洋甘菊素抑制海胆胚胎发育的能力表明其抗有丝分裂和致畸潜力较低,因为胚胎持续暴露于高达500微克/毫升(1.025微摩尔)的浓度下对首次卵裂没有抑制作用。这种低体外细胞毒性与先前研究的低急性毒性相关。所有这些数据,连同洋甘菊素的各种治疗特性,使这种木脂素成为一种有前途的新药。

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