While currently marketed antiplatelet drugs are undoubtedly efficient, all of them have some clinical limitations. It has also been reported that high reactive oxygen species (ROS) levels contribute to platelet activation and play a causal role in CVDs. Cyclooxygenase 1 (COX-1), constitutively expressed in all tissues, is a key regulator of platelet activation. Platelets represent a key element in this due to their crucial role in the coagulation cascade, and antiplatelet therapies are of fundamental importance in the treatment of cardiovascular and in cerebrovascular pathologies. Many factors are implicated in CVDs’ development and progression, including an imbalance between haemostasis and thrombosis. Compound 5 was identified as the most potent antioxidant that is also promising for use in the central nervous system (CNS).Ĭardiovascular diseases (CVDs) represent a leading cause of death worldwide, with approximately 17.9 million deaths every year, according to the World Health Organisation (WHO) reports. 6-Shogaol ( 2) was identified as the best overall antiplatelet lead, along with compounds 3 and 11 and the new compound 17, which require formulation to optimize their water solubility. The investigated 6-gingerol derivatives were also characterised by in silico and experimental physicochemical and blood–brain barrier-related parameters for lead and preclinical candidate selection. In silico docking of selected compounds to h-COX-1 enzyme revealed favourable interactions. In this study, we synthesised fourteen 6-gingerol derivatives, including eight new compounds, and studied their antiplatelet, COX-1 inhibitor, and antioxidant activities. Different pathways were suggested to contribute to these effects, like the inhibition of platelet aggregation. Many bioactivities have been reported for its extracts and the isolated compounds, including cardiovascular protective effects. Ginger ( Zingiber officinale) is widely used as a spice and a traditional medicine.
0 Comments
Leave a Reply. |