Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Saud University, Riyadh, Saudi Arabia.
Research and Laboratories Sector, National Drug and Cosmetic Control Laboratories (NDCCL), Saudi Food and Drug Authority, Riyadh, Saudi Arabia.
Sci Rep. 2021 Mar 8;11(1):5390. doi: 10.1038/s41598-021-84717-5.
Propolis, is a gummy material produced by honey bees from different parts of plants and is enriched with varied biological active compounds like flavonoids, phenolics and phenolic acids with wide applicability in the food, pharmaceutical and cosmetics industries. The current report is focused on the characterisation of propolis collected from Asir region, South-west of Saudi Arabia and its effect on Trypanosoma brucei (the causative organism of African sleeping sickness) and cytotoxic effect against U937 human leukemia cells. The Chemical composition and spectral characteristics of Saudi propolis was studied by Liquid Chromatography Mass Spectrometry (LC-MS) and High-performance liquid chromatography-evaporative light scattering detector (HPLC-ELSD).The two main active compounds isolated from Saudi propolis via column chromatography and size exclusion chromatography were fisetinidol and ferulic acid. High resolution electrospray ionization-mass spectrophotometer (HRESI-MS) and nuclear magnetic resonance (NMR) were used to elucidate the structures of the isolated compounds. All crudes extracts, fractions as well as isolated compounds were subjected for biological testing against Trypanosoma brucei (S427 WT), and their cytotoxicity against U937 human leukemia cells. Amongst the various samples investigated, S-6 fraction demonstrated highest anti-trypanosomal activity at 2.4 µg/ml MIC followed by fisetinidol at 4.7 µg/ml reflecting that the anti-trypanosomal activity is attributable to the presence of fisetinidol in the fraction. Similarly, all the tested samples exhibited cytotoxicity with an IC50 > 60 µg/ml. S-6 fractions exhibited highest cytotoxic activity against U937 cells with an IC50 of 58.7 µg/ml followed by ferulic acid with an IC50 87.7 µg/ml indicating that the cytotoxic effect of propolis might be due to the presence of ferulic acid. In conclusion, the biological activity of propolis could be attributed to the synergistic action of the two active compounds-ferulic acid and fisetinidol. The data obtained in the study is thus indicative of the role of propolis as potential anti-trypanosomal and anticancer agent for effective cancer therapy.
蜂胶是由蜜蜂从植物的不同部位采集的粘性物质，富含多种生物活性化合物，如类黄酮、酚类和酚酸，在食品、制药和化妆品行业有广泛的应用。本报告重点介绍了从沙特阿拉伯西南部阿西尔地区采集的蜂胶的特性，及其对布氏锥虫（非洲昏睡病的病原体）的影响，以及对 U937 人白血病细胞的细胞毒性作用。采用液相色谱-质谱联用（LC-MS）和高效液相色谱-蒸发光散射检测器（HPLC-ELSD）对沙特蜂胶的化学成分和光谱特征进行了研究。通过柱色谱和分子筛层析从沙特蜂胶中分离得到的两种主要活性化合物为非瑟酮醇和阿魏酸。高分辨电喷雾电离质谱（HRESI-MS）和核磁共振（NMR）用于阐明分离化合物的结构。所有粗提物提取物、馏分以及分离化合物均进行了针对布氏锥虫（S427 WT）的生物测试及其对 U937 人白血病细胞的细胞毒性测试。在所研究的各种样品中，S-6 馏分在 2.4µg/ml MIC 下表现出最高的抗锥虫活性，其次是非瑟酮醇在 4.7µg/ml 下，表明抗锥虫活性归因于该馏分中存在非瑟酮醇。同样，所有测试的样品均表现出细胞毒性，IC50>60µg/ml。S-6 馏分对 U937 细胞的细胞毒性活性最高，IC50 为 58.7µg/ml，其次是阿魏酸，IC50 为 87.7µg/ml，表明蜂胶的细胞毒性可能是由于阿魏酸的存在。总之，蜂胶的生物活性可能归因于两种活性化合物-阿魏酸和非瑟酮醇的协同作用。因此，研究中获得的数据表明，蜂胶具有作为潜在抗锥虫和抗癌药物的作用，可用于有效的癌症治疗。
