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Silibinin binding and release activities moderated by interstices of trimesoyl, tridimethyl, and tridiethyl malonate first-tier dendrimers

机译:水飞蓟宾结合和释放活性由间苯二甲酰,三甲基和丙二酸丙二酸酯第一级树状聚合物的间隙调节

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Trimesoyl 1,3,5-tridimethyl malonate (TTDMM), trimesoyl 1,3,5-tridiethyl malonate (TTDEM), trimesoyl 1,3,5-tridipropyl malonate, trimesoyl 1,3,5-tridibutyl malonate, and trimesoyl 1,3,5-tridihexyl malonate first-generation dendrimers, a complete series of dialkyl malonate esters from methyl to hexyl, were synthesized by a divergent growth approach with about a 95% yield. TTDMM and TTDEM members of this series were characterized with 500-MHz NMR and Fourier transform infrared spectroscopy. The 7.469353 and 8.435395 m~2/g surface areas and 700.1907- and 792.6436-nm pore-average diameters of TTDMM and TTDEM, respectively, implied that they could be used as prospective drug binders. Alkyl chains from methyl to hexyl of dialkyl malonate esters had enhanced interstitial spaces to trap the drugs and toxic heavy metals for their distribution and bioremediation, respectively. Thus, the dendrimers, silibinin (SB) complexes in a 1:1 ratio with acetone, were prepared and studied with Fourier transform infrared spectroscopy, differential scanning calorimetry, dynamic light scattering, scanning electron microcopy, and atomic force microscopy. The ultraviolet-visible spectroscopy at a 330-nm lamda max (λ_(max)) showed about 5%/h SB released in phosphate buffered saline with 10% dimethyl sulfoxide. The objective was used to investigate the capacity of dialkyl malonate terminated dendrimers to encapsulate a maximum amount of SB and anticancer drugs and the in vitro releasing activity.
机译:1,3,5-三甲基丙二酸三甲酰基1,3,5-三丙二酸丙二酯(TTDEM),1,3,5-三丙二丙二酸三甲酰基,1,3,5-三丙二酸丙二酸酯和三甲酰基1, 3,5-三己二丙二酸丙二酸酯第一代树状大分子,从甲基到己基的完整系列的二烷基丙二酸酯,是通过发散生长法合成的,产率约为95%。该系列的TTDMM和TTDEM成员通过500 MHz NMR和傅里叶变换红外光谱进行了表征。 TTDMM和TTDEM分别具有7.469353和8.435395 m〜2 / g的表面积以及700.1907-nm和792.6436-nm的孔平均直径,暗示它们可以用作预期的药物粘合剂。丙二酸二烷基酯的甲基到己基之间的烷基链增强了间隙空间,分别捕获了药物和有毒重金属以进行分布和生物修复。因此,制备了树状聚合物,水飞蓟宾(SB)与丙酮的比例为1:1的复合物,并进行了傅里叶变换红外光谱,差示扫描量热,动态光散射,扫描电子显微镜和原子力显微镜研究。在330 nmλmax(λ_(max))下的紫外可见光谱表明,磷酸盐缓冲液中含10%的二甲亚砜释放了约5%/ h的SB。目的是研究丙二酸二烷基酯封端的树枝状聚合物包封最大量的SB和抗癌药的能力以及体外释放活性。

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