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首页> 外文期刊>Life sciences >Antiproliferative efficacy of lipophilic soy isoflavone phytoestrogens delivered by low density lipoprotein particles into cultured U937 cells
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Antiproliferative efficacy of lipophilic soy isoflavone phytoestrogens delivered by low density lipoprotein particles into cultured U937 cells

机译：低密度脂蛋白颗粒将脂溶性大豆异黄酮植物雌激素释放到培养的U937细胞中的抗增殖作用

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摘要

Some fat-soluble bioactive substances incorporated into low density lipoprotein (LDL) may be delivered into cells via LDL receptor pathway influencing cellular functions. In this study, we synthesized a number of fat-soluble isoflavone esters and investigated their incorporation into LDL as well as their delivery into U937 cells. Using an artificial transfer system (Celite dispersion), genistein and daidzein oleates and daidzein dilinoleate were efficiently incorporated into LDL with concentrations ranging between 2.7 to 16.9 isoflavone molecules/LDL particle, while much smaller amounts of unesterified isoflavones and genistein stearates were transferred into LDL. LDL containing 7-oleates or 4',7-dioleates of genistein and daidzein significantly reduced U937 cell proliferation by 36-43%. The strongest inhibitory effect was shown by daidzein 4',7-dilinoleate with 93% reduction of cell proliferation. Neither of the 4'-oleates of genistein and daidzein contained in LDLs exhibited antiproliferative effects although they were incorporated into LDL. In summary, we demonstrated that isoflavones made fat-soluble by esterification can be incorporated into LDL in vitro and delivered into cultured U937 cells via the LDL-receptor pathway, reducing the cell proliferation.
机译：掺入低密度脂蛋白（LDL）的某些脂溶性生物活性物质可能会通过影响细胞功能的LDL受体途径进入细胞。在这项研究中，我们合成了许多脂溶性异黄酮酯，并研究了它们在LDL中的掺入以及它们在U937细胞中的递送。使用人工转移系统（Celite分散体），染料木黄酮和黄豆苷元油酸酯和大豆黄酮二亚油酸酯被有效地掺入LDL中，浓度范围为2.7至16.9个异黄酮分子/ LDL颗粒，同时将少量的未酯化的异黄酮和染料木黄酮硬脂酸酯转移到LDL中。含有染料木黄酮和黄豆苷元的7-油酸酯或4'，7-二醇酸酯的LDL可将U937细胞增殖显着降低36-43％。大豆黄酮4'，7-二亚油酸酯显示出最强的抑制作用，细胞增殖减少了93％。尽管LDL中含有染料木黄酮和黄豆苷元的4'-油酸酯，但它们均未显示出抗增殖作用。总之，我们证明了通过酯化作用制成脂溶性的异黄酮可以体外掺入LDL中，并通过LDL受体途径传递到培养的U937细胞中，从而减少细胞增殖。

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