CAJ | 학술논문

目的：通过对丹参素进行结构改造，以改善其稳定性和药理活性。方法以中药提取的丹参素钠为起始化合物，经酯化反应、甲氧基保护酚羟基、硝化反应等合成新型的丹参素衍生物。建立心肌细胞缺氧模型，用MTT方法检测丹参素及其衍生物对缺氧 H9c2细胞的保护作用。结果合成了15个全新的丹参素衍生物，并对其进行结构验证；药理活性实验显示，只有少数目标化合物在浓度为5μmol／L时表现出强于丹参素的活性。结论多数化合物的最大药理活性未显现在所选浓度范围内，其活性未必低于丹参素，尚需做进一步探讨。
목적：통과대단삼소진행결구개조，이개선기은정성화약리활성。방법이중약제취적단삼소납위기시화합물，경지화반응、갑양기보호분간기、초화반응등합성신형적단삼소연생물。건립심기세포결양모형，용MTT방법검측단삼소급기연생물대결양 H9c2세포적보호작용。결과합성료15개전신적단삼소연생물，병대기진행결구험증；약리활성실험현시，지유소수목표화합물재농도위5μmol／L시표현출강우단삼소적활성。결론다수화합물적최대약리활성미현현재소선농도범위내，기활성미필저우단삼소，상수주진일보탐토。
Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia .Methods Novel Danshensu derivatives were synthesized chiefly viaesterification , methoxy phenol hydroxyl protection ,nitration and amine solution reaction .All the target compounds were evaluated their bio-logical effects on anti-myocardial ischemia with H9c2 cells in vitro .Results 15 compounds were synthesized and further con-firmed by 1 H NMR and MS .Pharmacological studies showed that few synthetic derivatives at 5μmol/L performed a higher bi-ological effect than Danshensu .Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done .