Hui Ge, Zhao Yu, Zhang Wei, Xie Yun-fei, Yang Jing-xiu, Zhao Da-qing, Zhao Bing
State Key Laboratory of Supramolecular Structure and Materials, Jilin University, Changchun 130012, China.
Guang Pu Xue Yu Guang Pu Fen Xi. 2010 Sep;30(9):2393-6.
In the present work, the authors studied the interaction of ginsenoside Rh1 with lipid bilayers composed of DPPC using Raman spectroscopy. The conformational changes of DPPC molecule were further revealed by analyzing its vibrational modes such as the C--N stretching mode in the polar head-group region (650-850 cm(-1)), C--C stretching (1000-1200 cm(-1)), and C--H stretching (2750-3000 cm(-1)). The results indicated that there was little influence of Rb1 on the conformation of O--C--C--N+ backbone in the choline group of DPPC bilayers. The polar head group is still extending parallel to the bilayer sur face. The intensity ratios I1096/I1126 and I1096/I1062 represent the gauche/trans ratio. Both of them increased with adding the concentration of Rb1 to DPPC bilayers. The increment of gauche/trans ratio indicates that the disorder/order proportion of the alkyl chains arises. The ordering conformations in lipid chains decreased while the interchain disorder increased. The intensity ratio I2848/I2880 in the region of hydrocarbon chain C--H stretching mode reflects phase transition and has been demonstrated as a sensitive parameter of both inter-chain and intra-chain disorder/order intensity ratio in bilayer alkyl chains. The higher the ratio, the more disordered the hydrocarbon chains. Therefore, the increasing ratio I2848/I2880 with increasing amount of Rb1 indicates that this drug decreases the intermolecular ordering of the lipid lattice, and simultaneously increases the membrane lipid fluidity. In addition, previous study showed that an electrostatic interaction exists between sphingomyelin bilayers and drugs like scopolamine and anisodamine. Compared with those results, the action mode of ginsenoside Rb1 on DPPC bilayers may be because of hydrogen bonds that can be easily formed for the sugar moieties and the hydroxyls in Rb1 molecule. Therefore, the mechanism of drug action on DPPC bilayers may be resulting from the intra or inter hydrogen bonds and the head-group hydrophilic region of the DPPC membrane.
在本研究中,作者使用拉曼光谱研究了人参皂苷Rh1与由二棕榈酰磷脂酰胆碱(DPPC)组成的脂质双层的相互作用。通过分析DPPC分子的振动模式,如极性头部基团区域的C-N伸缩模式(650 - 850 cm⁻¹)、C-C伸缩(1000 - 1200 cm⁻¹)和C-H伸缩(2750 - 3000 cm⁻¹),进一步揭示了DPPC分子的构象变化。结果表明,Rb1对DPPC双层胆碱基团中O-C-C-N⁺主链的构象影响很小。极性头部基团仍平行于双层表面延伸。强度比I1096/I1126和I1096/I1062代表gauche/trans比。随着向DPPC双层中添加Rb1浓度的增加,它们都增加。gauche/trans比的增加表明烷基链的无序/有序比例增加。脂质链中的有序构象减少,而链间无序增加。烃链C-H伸缩模式区域的强度比I2848/I2880反映相变,并且已被证明是双层烷基链中链间和链内无序/有序强度比的敏感参数。该比值越高,烃链越无序。因此,随着Rb1量的增加,I2848/I2880比值增加表明该药物降低了脂质晶格的分子间有序性,同时增加了膜脂流动性。此外,先前的研究表明,鞘磷脂双层与东莨菪碱和山莨菪碱等药物之间存在静电相互作用。与这些结果相比,人参皂苷Rb1对DPPC双层的作用模式可能是由于Rb1分子中的糖部分和羟基容易形成氢键。因此,药物对DPPC双层的作用机制可能源于DPPC膜的内部或分子间氢键以及头部基团亲水区。