Avato Pinarosa, Migoni Danilo, Argentieri Mariapia, Fanizzi Francesco P, Tava Aldo
Dipartimento di Farmacia- Scienze del Farmaco, Via Orabona 4, 70125 Bari, Italy.
DISTEBA, Universita del Salento, Via Monteroni, 73100 Lecce, Italy.
Anticancer Agents Med Chem. 2017 Nov 24;17(11):1508-1518. doi: 10.2174/1871520617666170727152805.
Saponins from Medicago species display several biological activities, among them apoptotic effects against plant cells have been evidenced. In contrast, their cytotoxic and antitumor activity against animal cells have not been studied in great details.
To explore the cytotoxic properties of saponin from Medicago species against animal cells and their effect in combination with the antitumoral drug cisplatin.
Cytotoxic activity of saponin mixtures from M. arabica (tops and roots), M. arborea (tops) and M. sativa (tops, roots and seeds) and related prosapogenins from M. arborea and M. sativa (tops) against HeLa and MCF-7 cell lines is described. In addition, cytotoxicity of soyasaponin I and purified saponins (1-8) of hederagenin, medicagenic and zanhic acid is also presented. Combination experiments with cisplatin have been also conducted.
Saponins from M. arabica tops and roots (mainly monodesmosides of hederagenin and bayogenin) were the most effective to reduce proliferation of HeLa and MCF-7 cell lines. Among the purified saponins, the most cytotoxic was saponin 1, 3-O-ß-D-glucopyranosyl(1→2)-α-L-arabinopyranosyl hederagenin. When saponins, derived prosapogenins and pure saponins were used in combination with cisplatin, they all, to different extent, were able to potentiate cisplatin activity against HeLa cells but not against MCF-7 cell lines. Moreover uptake of cisplatin in these cell lines was significantly reduced.
Overall results showed that specific molecular types of saponins (hederagenin glycosides) have potential as anti-cancer agents or as leads for anti-cancer agents. Moreover saponins from Medicago species have evidenced interesting properties to mediate cisplatin effects in tumor cell lines.
来自苜蓿属植物的皂苷具有多种生物活性，其中对植物细胞的凋亡作用已得到证实。相比之下，它们对动物细胞的细胞毒性和抗肿瘤活性尚未得到详细研究。
探讨苜蓿属植物皂苷对动物细胞的细胞毒性特性及其与抗肿瘤药物顺铂联合使用的效果。
描述了来自阿拉伯苜蓿（地上部分和根部）、乔木状苜蓿（地上部分）和紫花苜蓿（地上部分、根部和种子）的皂苷混合物以及来自乔木状苜蓿和紫花苜蓿（地上部分）的相关前皂苷元对HeLa和MCF-7细胞系的细胞毒性活性。此外，还介绍了大豆皂苷I以及常春藤皂苷元、苜蓿皂苷元和赞尼酸的纯化皂苷（1-8）的细胞毒性。还进行了与顺铂的联合实验。
阿拉伯苜蓿地上部分和根部的皂苷（主要是常春藤皂苷元和贝约皂苷元的单糖苷）对HeLa和MCF-7细胞系增殖的抑制效果最为显著。在纯化的皂苷中，细胞毒性最强的是皂苷1，即3-O-β-D-吡喃葡萄糖基（1→2）-α-L-阿拉伯吡喃糖基常春藤皂苷元。当皂苷、衍生的前皂苷元和纯皂苷与顺铂联合使用时，它们都能在不同程度上增强顺铂对HeLa细胞的活性，但对MCF-7细胞系无效。此外，这些细胞系中顺铂的摄取量显著降低。
总体结果表明，特定分子类型的皂苷（常春藤皂苷元糖苷）具有作为抗癌剂或抗癌剂先导物的潜力。此外，苜蓿属植物的皂苷在介导肿瘤细胞系中顺铂的作用方面表现出有趣的特性。
