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首页> 外文期刊>DNA and Cell Biology >DNA-Binding Cytotoxic Alkaloids: Comparative Study of the Energetics of Binding of Berberine, Palmatine, and Coralyne
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DNA-Binding Cytotoxic Alkaloids: Comparative Study of the Energetics of Binding of Berberine, Palmatine, and Coralyne

机译：DNA结合细胞毒性生物碱：小Ber碱，Palmatine和Coralyne结合能的比较研究。

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摘要

Deoxyribonucleic acid is the site of storage and retrieval of genetic information through interaction with proteins and other small molecules. In the present study, the interaction of two natural cytotoxic protoberberine plant alkaloids, berberine and palmatine, and a synthetic derivative, coralyne, with mammalian herring testis DNA was investigated using a combination of isothermal titration calorimetry, differential scanning calorimetry, and optical melting experiments to characterize the energetics of their binding. The binding constants of these alkaloids to DNA under identical conditions were evaluated from the UV melting data, and the enthalpy of binding was elucidated from isothermal titration studies. The binding constants of berberine, palmatine, and coralyne to DNA were found to be 1.15 x 10(4), 2.84 x 10(4), and 3.5 x 10(6) M(-1) at 20 degrees C in buffer of 20 mM [Na(+)]. Parsing of the free energy change of the interaction observed into polyelectrolytic and nonpolyelectrolytic components suggested that although these alkaloids are charged, the major contributor of about 75% of the binding free energy arises from the nonpolyelectrolytic forces. The binding in case of palmatine and coralyne was predominantly enthalpy driven with favoring smaller entropy terms, while that of berberine was favored by both negative enthalpy and positive entropy changes. Temperature dependence of the binding enthalpies determined from ITC studies in the range 20-40 degrees C was used to calculate the binding-induced change in heat capacity (DeltaC(o)(p)) values as -117, -135, and -157 cal/mol K, respectively, for berberine, palmatine, and coralyne. Taken together, the results suggest that the DNA binding of the planar synthetic coralyne is stronger and thermodynamically more favored compared to the buckled natural berberine and palmatine.
机译：脱氧核糖核酸是通过与蛋白质和其他小分子相互作用来存储和检索遗传信息的场所。在本研究中，使用等温滴定量热法，差示扫描量热法和光学熔融实验相结合，研究了两种天然的细胞毒性原小ber碱植物生物碱小ber碱和棕榈酸，以及合成衍生物珊瑚虫与哺乳动物鲱鱼睾丸DNA的相互作用。表征其绑定的能量。从紫外熔融数据评估了这些生物碱在相同条件下与DNA的结合常数，并通过等温滴定研究阐明了结合焓。在20℃的缓冲液中，在20摄氏度下，小coral碱，棕榈碱和科宁与DNA的结合常数分别为1.15 x 10（4），2.84 x 10（4）和3.5 x 10（6）M（-1）。 mM [Na（+）]。将观察到的相互作用的自由能变化解析为聚电解和非聚电解成分表明，尽管这些生物碱带电，但约75％的结合自由能的主要贡献者来自非聚电解力。在棕榈蛋白和珊瑚素的情况下，结合主要是由焓驱动，有利于较小的熵项，而小ber碱的结合受负焓和正熵变化的影响。由ITC研究确定的在20-40摄氏度范围内的结合焓的温度依赖性用于计算结合诱导的热容变化（DeltaC（o）（p））值为-117，-135和-157 cal / mol K，分别用于小碱，巴马汀和coralyne。两者合计，结果表明，与带扣的天然小ber碱和巴马汀相比，平面合成珊瑚虫的DNA结合更强，热力学更受青睐。

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