Department of Biomedical Sciences, British College of Applied Studies, BCAS City Campus, Colombo 00600, Sri Lanka.
Department of Zoology, Faculty of Applied Sciences (Center for Biotechnology), University of Sri Jayewardenepura, Nugegoda 10250, Sri Lanka.
Biomolecules. 2020 Jan 21;10(2):165. doi: 10.3390/biom10020165.
Although the antidiabetic efficacy of flowers has been reported, antiproliferative and anti-obesity activities are yet to be explored. We examined the anti-obesity and antiproliferative potentials of different fractions (hexane, chloroform, ethyl acetate, methanol) of flower extract for the first time using 3T3-L1 cells, primary peripheral blood mononuclear cells (PBMC) isolated from healthy and adult acute myeloid (AML) and chronic lymphocytic leukemia (CLL) patients, recombinant Jurkat T cells, and MCF7 cell lines. The in vitro hypoglycemic activity was evaluated using the inhibition of -amylase enzyme and glucose uptake by yeast cells. The percentage glucose uptake and -amylase inhibitory activity increased in a dose-dependent manner in the crude and the tested fractions (hexane and ethyl acetate). Inhibition of the 3T3-L1 cells' differentiation was observed in the ethyl acetate and chloroform fractions, followed by the hexane fraction. Antiproliferative analyses revealed that exerted a high specific activity against anti-AML and anti-CLL PBMC cells, especially by the hexane and ethyl acetate fractions. The gas chromatography/mass spectrometry analysis indicated the presence of 1-heptacosanol (hexane fraction), 1-octadecene (hexane and chloroform fractions), and other organic compounds. Molecular docking demonstrated that phenol,2,5-bis(1,1-dimethylethyl) and 4-hydroxypyridine 1-oxide compounds showed specificity toward survivin protein, indicating the feasibility of in developing new drug leads against leukemia.
虽然花的抗糖尿病功效已被报道,但抗增殖和抗肥胖活性尚未得到探索。我们首次使用 3T3-L1 细胞、从健康和成人急性髓系白血病(AML)和慢性淋巴细胞白血病(CLL)患者分离的外周血单核细胞(PBMC)、重组 Jurkat T 细胞和 MCF7 细胞系,研究了花提取物的不同馏分(己烷、氯仿、乙酸乙酯、甲醇)的抗肥胖和抗增殖潜力。使用酵母细胞抑制 -淀粉酶酶和葡萄糖摄取来评估体外降血糖活性。粗提物和测试馏分(己烷和乙酸乙酯)的葡萄糖摄取百分比和 -淀粉酶抑制活性均呈剂量依赖性增加。在乙酸乙酯和氯仿馏分中观察到 3T3-L1 细胞分化的抑制,随后是己烷馏分。抗增殖分析表明,对 AML 和 CLL PBMC 细胞具有高特异性的活性,尤其是己烷和乙酸乙酯馏分。气相色谱/质谱分析表明存在 1-二十七烷醇(己烷馏分)、1-十八烯(己烷和氯仿馏分)和其他有机化合物。分子对接表明,酚、2,5-二叔丁基-4-羟基吡啶 1-氧化物化合物对survivin 蛋白具有特异性,表明在开发针对白血病的新药方面具有可行性。