Abstract：
BACKGROUND: Antiproliferative and apoptotic activities have been attributed to the phytosteroid diosgenin ((25R)-spirost-5-en-3β-ol; 1). It is known that combining glucose with two rhamnoses (the chacotrioside framework) linked to diosgenin increases its apoptotic activity. However, the effects of diosgenin glucosamine glycosides on different cancer cell types and cell death have not been entirely explored.
RESULTS: This study reports the antiproliferative, cytotoxic, and apoptotic activities of diosgenin and its glycosylated derivative ((25R)-spirost-5-en-3β-yl β-D-glucopyranoside; 2). It also explores the effects of two diosgenin glucosamine derivates, diosgenin 2-acetamido-2-deoxy-β-D-glucopyranoside (3), and diosgenin 2-amino-2-deoxy-β-D-glucopyranoside hydrochloride (4), on different cancer cell lines. We found that all the compounds affected proliferative activity with minimal toxicity. In addition, all cancer cell lines showed morphological and biochemical characteristics corresponding to an apoptotic process. Apoptotic cell death was higher in all cell lines treated with compounds 2, 3 and 4 than in those treated with diosgenin. Moreover, compounds 3 and 4 induced apoptosis better than compounds 1 and 2. These results suggest that combining glucosamine with modified glucosamine attached to diosgenin has a greater apoptotic effect than diosgenin or its glycosylated derivative (compound 2). Furthermore, diosgenin and the abovementioned glycosides had a selective effect on tumour cells since the proliferative capacity of human lymphocytes, keratinocytes (HaCaT) and epithelial cells (CCD841) was not significantly affected.
CONCLUSIONS: Altogether, these results demonstrate that diosgenin glucosamine compounds exert an antiproliferative effect on cancer cell lines and induce apoptotic effects more efficiently than diosgenin alone without affecting non-tumour cells.
CONCLUSIONS: This study evidences the pro-apoptotic and selective activities of diosgenyl glucosamine compounds in cancer cell lines.
RESULTS: This study reports the antiproliferative, cytotoxic, and apoptotic activities of diosgenin and its glycosylated derivative ((25R)-spirost-5-en-3β-yl β-D-glucopyranoside; 2). It also explores the effects of two diosgenin glucosamine derivates, diosgenin 2-acetamido-2-deoxy-β-D-glucopyranoside (3), and diosgenin 2-amino-2-deoxy-β-D-glucopyranoside hydrochloride (4), on different cancer cell lines. We found that all the compounds affected proliferative activity with minimal toxicity. In addition, all cancer cell lines showed morphological and biochemical characteristics corresponding to an apoptotic process. Apoptotic cell death was higher in all cell lines treated with compounds 2, 3 and 4 than in those treated with diosgenin. Moreover, compounds 3 and 4 induced apoptosis better than compounds 1 and 2. These results suggest that combining glucosamine with modified glucosamine attached to diosgenin has a greater apoptotic effect than diosgenin or its glycosylated derivative (compound 2). Furthermore, diosgenin and the abovementioned glycosides had a selective effect on tumour cells since the proliferative capacity of human lymphocytes, keratinocytes (HaCaT) and epithelial cells (CCD841) was not significantly affected.
CONCLUSIONS: Altogether, these results demonstrate that diosgenin glucosamine compounds exert an antiproliferative effect on cancer cell lines and induce apoptotic effects more efficiently than diosgenin alone without affecting non-tumour cells.
CONCLUSIONS: This study evidences the pro-apoptotic and selective activities of diosgenyl glucosamine compounds in cancer cell lines.
摘要：
背景:抗增殖和凋亡活性已归因于植物类固醇薯白皂苷元((25R)-螺旋体-5-烯-3β-醇;1)。已知将葡萄糖与两种鼠李糖(chacotrioside框架)结合,所述鼠李糖结合至皂苷元增加其凋亡活性。然而,皂苷元葡糖胺苷对不同癌细胞类型和细胞死亡的影响尚未完全研究。
结果：本研究报告了抗增殖，细胞毒性，皂苷元及其糖基化衍生物（（25R）-螺旋藻-5-en-3β-ylβ-D-吡喃葡萄糖苷；2）的凋亡活性。它还探讨了两种皂苷元葡糖胺衍生物的作用，皂苷元2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖苷(3)，和薯白皂苷元2-氨基-2-脱氧-β-D-吡喃葡萄糖苷盐酸盐(4)，在不同的癌细胞系上。我们发现所有化合物都以最小的毒性影响增殖活性。此外,所有癌细胞系都表现出与凋亡过程相对应的形态学和生化特征.在用化合物2、3和4处理的所有细胞系中，凋亡细胞死亡均高于用皂苷元处理的细胞系。此外，化合物3和4诱导细胞凋亡的效果优于化合物1和2。这些结果表明,将葡糖胺与连接至皂苷元的修饰的葡糖胺组合比皂苷元或其糖基化衍生物(化合物2)具有更大的凋亡作用。此外，皂苷元和上述糖苷对肿瘤细胞具有选择性作用，因为人类淋巴细胞的增殖能力，角质形成细胞（HaCaT）和上皮细胞（CCD841）没有显着影响。
结论：总而言之，这些结果证明,皂苷元葡糖胺化合物对癌细胞系发挥抗增殖作用,并且比单独使用皂苷元更有效地诱导凋亡作用,而不影响非肿瘤细胞.
结论：本研究证明了二烯酮基葡糖胺化合物在癌细胞系中的促凋亡和选择性活性。
结果：本研究报告了抗增殖，细胞毒性，皂苷元及其糖基化衍生物（（25R）-螺旋藻-5-en-3β-ylβ-D-吡喃葡萄糖苷；2）的凋亡活性。它还探讨了两种皂苷元葡糖胺衍生物的作用，皂苷元2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖苷(3)，和薯白皂苷元2-氨基-2-脱氧-β-D-吡喃葡萄糖苷盐酸盐(4)，在不同的癌细胞系上。我们发现所有化合物都以最小的毒性影响增殖活性。此外,所有癌细胞系都表现出与凋亡过程相对应的形态学和生化特征.在用化合物2、3和4处理的所有细胞系中，凋亡细胞死亡均高于用皂苷元处理的细胞系。此外，化合物3和4诱导细胞凋亡的效果优于化合物1和2。这些结果表明,将葡糖胺与连接至皂苷元的修饰的葡糖胺组合比皂苷元或其糖基化衍生物(化合物2)具有更大的凋亡作用。此外，皂苷元和上述糖苷对肿瘤细胞具有选择性作用，因为人类淋巴细胞的增殖能力，角质形成细胞（HaCaT）和上皮细胞（CCD841）没有显着影响。
结论：总而言之，这些结果证明,皂苷元葡糖胺化合物对癌细胞系发挥抗增殖作用,并且比单独使用皂苷元更有效地诱导凋亡作用,而不影响非肿瘤细胞.
结论：本研究证明了二烯酮基葡糖胺化合物在癌细胞系中的促凋亡和选择性活性。
