Discipline of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia.
Tropical Medicine Research Institute (TMRI), National Centre for Research (NCR), Khartoum, Sudan.
Planta Med. 2020 Apr;86(6):387-394. doi: 10.1055/a-1129-7026. Epub 2020 Mar 13.
rhizomes are traditionally used for the treatment of numerous human ailments. The present study was carried out to investigate the inhibitory activity of the crude extract, chromatographic fractions, and purified compounds from rhizomes on the migration of MDA-MB-231 cells. The effect of the extract on cell migration was investigated by a scratch assay, which showed significant inhibition in a concentration-dependent manner. Vacuum liquid chromatography on silica gel afforded four fractions (Frs. 1 - 4), which were tested on cell migration in the scratch assay. Frs. 1 and 2 showed the most significant inhibition of MDA-MB-231 cell migration. The effect of the most potent fraction (Fr. 2) was further confirmed in a transwell migration assay. The study of Frs. 1 and 2 by gelatin zymography showed significant inhibition of MMP-9 enzyme activity. Chromatographic separation of Frs. 1 and 2 afforded buddledone A (1: ), zerumbone (2: ), (2,9)-6-methoxy-2,9-humuradien-8-one (3: ), zerumbone epoxide (4: ), stigmasterol (5: ), and daucosterol (6: ). In a cell viability assay, compounds 1: - 4: inhibited the viability of MDA-MB-231 cells in a concentration-dependent manner. The study of buddledone A (1: ) and zerumbone epoxide (4: ) on cell migration revealed that 4: significantly inhibited the migration of MDA-MB-231 cells in both scratch and transwell migration assays. The results of the present study may lead to further molecular studies behind the inhibitory activity of zerumbone epoxide (4: ) on cell migration and support the traditional use of rhizomes for the treatment of cancer.
块茎传统上被用于治疗许多人类疾病。本研究旨在研究从块茎中提取的粗提取物、色谱馏分和纯化化合物对 MDA-MB-231 细胞迁移的抑制活性。通过划痕实验研究了提取物对细胞迁移的影响，结果表明提取物在浓度依赖性方式下具有显著的抑制作用。硅胶真空液相色谱分离得到四个馏分（Fr. 1-4），并在划痕实验中测试了它们对细胞迁移的抑制作用。馏分 1 和 2 对 MDA-MB-231 细胞迁移的抑制作用最为显著。最有效馏分（Fr. 2）的作用在 Transwell 迁移实验中得到进一步证实。Fr. 1 和 2 的研究通过明胶酶谱法显示对 MMP-9 酶活性的显著抑制作用。Fr. 1 和 2 的色谱分离得到了块茎酮 A（1：）、菖蒲酮（2：）、（2,9）-6-甲氧基-2,9-胡麻二烯-8-酮（3：）、菖蒲酮环氧化物（4：）、豆甾醇（5：）和胡萝卜甾醇（6：）。在细胞活力测定中，化合物 1：-4：以浓度依赖性方式抑制 MDA-MB-231 细胞的活力。对块茎酮 A（1：）和菖蒲酮环氧化物（4：）对细胞迁移的研究表明，4：在划痕和 Transwell 迁移实验中均显著抑制 MDA-MB-231 细胞的迁移。本研究的结果可能导致对菖蒲酮环氧化物（4：）抑制细胞迁移的抑制活性的进一步分子研究，并支持块茎传统上用于治疗癌症的用途。
