Zinchenko V P, Kim Iu A, Tarakhovskiĭ Iu S, Bronnikov G E
Biofizika. 2011 May-Jun;56(3):433-8.
The biological properties of dihydroquercetin (DHO) modified by including it into the ring of beta-cyclodextrin (beta-CD) to give it more water-soluble properties have been investigated. It was shown that the peroral administration of the DHQ/beta-CD complex provides a long increase of DHQ concentration in rat blood (up to 7.5 h), and, unlike pure DHQ, the complex does not accumulate in the liver. As DHQ is released from the complex, it penetrates into liposome membranes, changing their thermodynamic characteristics. DHQ decreases the specific heat absorption, enthalpies, and temperature maximum of lipid melting and increases the transition half-width. This property is used to estimate the stability of the DHQ/beta-CD complex. It was shown that complex DHQ/beta-CD is not stable, and DHQ molecules slowly leave the complex in water environment. Seven and a half hours after the peroral injection of drugs, DHQ was found in the blood plasma of rats to which water-soluble complex DHQ/betaCD was injected and in the liver of rats to which free DHQ was injected. Thus, DHQ/betaCD not only is a more water-soluble complex but also it slowly releases DHQ, supporting long a low concentration of the free form of DHQ and providing the penetration of DHQ into the blood stream. After several weeks of feeding old mice with antioxidants, the activity of mitochondrial enzymes was restored to the level observed in young animals.
研究了将二氢槲皮素(DHO)包合到β-环糊精(β-CD)环中以使其具有更高水溶性后其生物学特性。结果表明,口服DHQ/β-CD复合物可使大鼠血液中DHQ浓度长时间升高(长达7.5小时),并且与纯DHQ不同,该复合物不会在肝脏中蓄积。当DHQ从复合物中释放出来时,它会渗透到脂质体膜中,改变其热力学特性。DHQ降低了脂质熔化的比热吸收、焓和最高温度,并增加了转变半峰宽。这一特性被用于评估DHQ/β-CD复合物的稳定性。结果表明,复合物DHQ/β-CD不稳定, DHQ分子在水环境中会缓慢地从复合物中释放出来。口服注射药物7.5小时后,在注射了水溶性复合物DHQ/β-CD的大鼠血浆中以及注射了游离DHQ的大鼠肝脏中均发现了DHQ。因此,DHQ/β-CD不仅是一种水溶性更高的复合物,而且它还能缓慢释放DHQ,长时间维持低浓度的游离形式DHQ,并使DHQ渗透到血流中。用抗氧化剂喂养老年小鼠数周后,线粒体酶的活性恢复到了在年轻动物中观察到的水平。