ABSTRACT
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 .
ABSTRACT
Danshensu is one of the main water soluble active ingredients of Salvia miltiorrhiza ,which has many phar-macological activities ,especially in cardiovascular system .T he cardiovascular pharmacological mechanism of Danshensu and its derivatives from the view of anti-apoptosis ,antioxidant ,inhibiting calcium overload and role in the inflammatory reaction path-ways etc .were summarized in this article .