首页> 美国卫生研究院文献>Biomolecules >Therapeutic Efficacy of Nyctanthes arbor-tristis Flowers to Inhibit Proliferation of Acute and Chronic Primary Human Leukemia Cells with Adipocyte Differentiation and in Silico Analysis of Interactions between Survivin Protein and Selected Secondary Metabolites
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Therapeutic Efficacy of Nyctanthes arbor-tristis Flowers to Inhibit Proliferation of Acute and Chronic Primary Human Leukemia Cells with Adipocyte Differentiation and in Silico Analysis of Interactions between Survivin Protein and Selected Secondary Metabolites

机译:菊苣花对抑制急性和慢性原发性人类白血病细胞增殖的治疗作用脂肪细胞分化和存活蛋白与某些次生代谢物相互作用的计算机模拟分析

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摘要

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 α-amylase enzyme and glucose uptake by yeast cells. The percentage glucose uptake and α-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.
机译:尽管已经报道了花朵的抗糖尿病功效,但抗增生和抗肥胖活性尚待探索。我们首次使用3T3-L1细胞,从健康人和成年急性髓细胞中分离的原代外周血单核细胞(PBMC),首次检查了花提取物不同部分(己烷,氯仿,乙酸乙酯,甲醇)的不同部位的抗肥胖和抗增殖能力(AML)和慢性淋巴细胞性白血病(CLL)患者,重组Jurkat T细胞和MCF7细胞系。使用抑制α-淀粉酶和酵母细胞摄取葡萄糖来评估体外降血糖活性。原油和被测馏分(己烷和乙酸乙酯)中葡萄糖的摄取百分比和α-淀粉酶抑制活性呈剂量依赖性。在乙酸乙酯和氯仿馏分中观察到3T3-L1细胞分化的抑制,然后在己烷馏分中观察到。抗增殖分析显示,它对抗AML和抗CLL PBMC细胞具有很高的比活性,尤其是通过己烷和乙酸乙酯馏分。气相色谱/质谱分析表明存在1-庚二十烷醇(己烷馏分),1-十八碳烯(己烷和氯仿馏分)和其他有机化合物。分子对接表明,苯酚,2,5-双(1,1-二甲基乙基)和4-羟基吡啶一氧化物化合物对survivin蛋白具有特异性,表明开发抗白血病新药的可行性。

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