Single-Step Isolation of Phyllacanthone from Cnidoscolus Quercifolius Using Centrifugal Partition Chromatography.

Sovannychloé Nai,Christiane Adrielly Alves Ferraz，Raphaël Grougnet,Raimundo Gonçalves de Oliveira Junior

Journal Of Separation Science（2025）SCI 3区

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Abstract

Favelines, benzocycloheptene diterpenes exclusively found in Cnidoscolus quercifolius, have shown promising anticancer properties, particularly phyllacanthone. Nevertheless, the isolation of these compounds remains challenging due to their similar polarity. The use of centrifugal partition chromatography (CPC) has enabled the quick and efficient purification of phyllacanthone from C. quercifolius crude extract with a yield of 4.5% (w/w) and a purity of 83%. Favelines-enriched fractions were also obtained and purified by preparative HPLC, resulting in the isolation of faveline, isofavelol, and deoxofaveline. In addition, phyllacanthone B, a previously unreported derivative, was identified and characterized. Pharmacological evaluations revealed the significant anti-melanoma activity of purified metabolites, with distinct structure-activity relationships. These results shed light on the mechanism of action of favelines, suggesting their potential as hits for the development of novel anticancer agents.

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【要点】：本文通过离心分配色谱法实现了一步法从Cnidoscolus quercifolius中分离得到具有抗肿瘤活性的phyllacanthone及其衍生物，并发现了新的衍生物phyllacanthone B。

【方法】：采用离心分配色谱法（CPC）进行快速高效分离，随后通过制备高效液相色谱（HPLC）进一步纯化得到目标化合物。

【实验】：实验中使用了Cnidoscolus quercifolius粗提物，通过CPC分离得到phyllacanthone，产率为4.5%（w/w），纯度为83%。Favelines富集的组分通过HPLC进一步纯化，得到了faveline、isofavelol和deoxofaveline，以及新发现的衍生物phyllacanthone B。药理学评价显示，这些纯化的代谢物具有显著的抗黑色素瘤活性。