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Characterization Of Three Piperine Analogs Of Dipeptidyl Boronic Acid

593 words - 3 pages

In the present study three piperine analogs of dipeptidyl boronic acid (1 to 3) were synthesized. Structures of the synthesized compounds were characterized by spectral studies. All the compounds were screened for their antineoplastic activity against three cancer cell lines and antimicrobial activity against seven bacterial and five fungal species. In vitro results showed that most of the compounds displayed moderate to good inhibitory activitiy on the tested cancer cell lines, among them compound 1 showed excelent antitumor activity where as Compound 3 was found to be potent antimicrobial agent against Asperigillus fumigates at a concentration of 62 µg/mL than other tested compounds and the parent molecule piperine. All the compounds were subjected to molecular docking studies for Leucyl-tRNA synthase as well as for 20S proteasome inhibition. The in silico molecular docking study results showed that, all compounds have minimum binding energy toward the active pocket and thus they will act as a good Leucyl- tRNA synthase inhibitor, this is in concordance with our in vitro results.

Keywords: Piperine, piperic acid, Boronic acids, HeLa, MCF-7, antibacterial activity.
Boronic acids have been illustrious in the literature back in 1860[ ], developing over the years into a wide studied area of chemistry. After the approval of Velcade® as proteasome inhibitor, boronic acids have emerged as a unique lead for several malignant tumors, as β-lactamase inhibitors, NS3 protease inhibitors, amino-acyl tRNA synthase inhibitors, and anticoagulants. Boronic acids and its derivatives have gained outstanding importance as a result of their wide-spread biological activity and their use in synthetic chemistry. Piperine, alkaloid from piper nigrum L found to display an ample spectrum of pharmacologic activities, together with antimicrobial[ ] and antineoplastic properties[ , ]. Despite the acclaimed potential of piperine, up to now there are few reports available for piperine based antimicrobial and antineoplastic...

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