UNAIR NEWS – Dr. Juni Ekowati, MSi., Apt., a lecturer of Faculty of Pharmacy UNAIR does various researches to study many useful things. This time, she tried to explore the potential of p-coumaric acid derivatives as antiplatelet.
Before reviewing the study further, Juni explained that thromboembolism is one of the main causes of death in patients with cardiovascular disease. Reports of aspirin resistance in patients with cardiovascular disease and side effects on the gastrointestinal tract encourage the search for new compounds for potential antithrombotic drugs, including antiplatelet.
“One of the phenolic compounds, namely p-coumaric acid, is known to have antiplatelet activity,” she said.
To increase its activity, continued June, the structural modification of the p-coumaric acid was carried out. Structural modification is carried out by esterification, alkylation, hydrogenation and hydrolysis of alkaline conditions.
“The purpose of the modification is to obtain more lipophilic derivatives and it is also intended to make interaction of the pharmacophore group with the cyclooxygenase-1 (COX-1) enzyme target more optimal. More lipophilic derivatives are expected to improve the absorption process in the digestive tract, ” she said.
Next, Juni and her team conducted various testing processes. The test results, she explained, showed that the blood clotting time of all synthesized products was significantly different from negative controls. It is in accordance with the prediction of the in silico test which stated that the synthesized product has an antiplatelet activity through COX-1 enzyme inhibition.
“P-coumaric methyl derivatives showed activity that was not significantly different from aspirin. But the change of unsaturated bonds to saturation reduces the antiplatelet activity, ” she explained.
In the end, she said that based on the results of the analysis, the relationship between the structure of p-coumaric acid derivatives and their activity, a linear relationship was known. Its lipophilic properties and affinity for COX-1 have an antiplatelet effect, especially in oral use. ” P-coumaric acid derivative compounds have the potential to be further developed, in a larger scale of laboratory synthesis and their use as an anti-platelet alternative,” she concluded.
Author: Nuri Hermawan
Editor: Khefti Al Mawalia
Details of research available at:
Juni Ekowati, Nuzul Wahyuning Diyah, Achmad Syahrani. 2019.
Synthesis and Antiplatelet Activites of Some Derivatives of p-Coumaric Acid.
Chemistry & Chemical Technology Vol. 13, No. 3, 2019. pp. 296–302 ISSN 1996-4196|