| 李斌,连重福,刘学强,焦艳晓,彭游.化学通报,2021,84(7):732-737. |
| 4′-甲基-7-(2-萘磺酰基)大豆素的细胞吸收及代谢研究 |
| CellUptakeandMetabolismof4′-Methyl-7-(2-naphthalenesulfonyl)Daidzein |
| 投稿时间：2020-12-22 修订日期：2021-03-01 |
| DOI： |
| 中文关键词: 大豆素萘磺酸酯 主动脉血管平滑肌细胞 细胞吸收 体外代谢途径 |
| 英文关键词:Daidzein naphthalene sulfonate, HAVSMCs, Cellular uptake, Metabolic pathways in vitro |
| 基金项目:国家自然科学基金项目(81660541)、江西省自然科学基金项目(20202BABL203017)和江西省教育厅科技项目(GJJ201839)资助 |
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| 中文摘要: |
| 对新型大豆素萘磺酸酯衍生物（DD）的细胞吸收和代谢变化进行研究，并根据实验结果预测其可能存在的体外代谢途径。利用高效液相色谱法（HPLC）对衍生物DD在人主动脉血管平滑肌细胞（HAVSMCs）内的吸收和利用率进行研究，并利用液相色谱-质谱联用技术考察其细胞代谢变化。人主动脉血管平滑肌细胞对化合物DD的吸收率达到了74.3%，远远高于大豆素（DZ）的细胞吸收率。细胞代谢研究表明，化合物DD中4"-和7-位上的取代基影响其代谢途径和代谢产物。与4"-位的甲基相比，衍生物DD的7-位的萘磺酰基更容易水解。对药物分子进行适当的结构修饰和改造，可以增强药物分子的脂溶性，进而提高药物分子在细胞中的吸收利用率，说明药物的吸收利用率与其理化性质密切相关。 |
| 英文摘要: |
| The cellular absorption and metabolism of a novel derivative of daidzein naphthalene sulfonate (DD) were studied, and the possible metabolic pathway in vitro was predicted according to the experimental results. The absorption and utilization of DD in human aortic smooth muscle cells (HAVSMCs) were evaluated by high performance liquid chromatography (HPLC), and the metabolism of DD was investigated by liquid chromatography-mass spectrometry (LC-MS). The absorption rate of DD in HAVSMCs was 74.3%, which was much higher than that of DZ. The study of metabolism showed that the substituents at 4"- and 7-positions in DD affected its metabolic pathway and metabolites. The naphthalene sulfonyl group at 7-position of DD was easier to hydrolyze, compared with the methyl group at 4"- position. The liposolubilities of drug molecules were enhanced by appropriate modification and transformation in their structures, and then improved their absorption and utilization in cells. It showed that the absorption and utilization rate of drugs was closely related to their physical and chemical properties. |
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