An in vitro Study: Inhibitory Effect of Carfilzomib on Human Serum Paraoxonase-1 (hPON1)


INTERNATIONAL JOURNAL OF PHARMACOLOGY, vol.18, no.3, pp.522-526, 2022 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 18 Issue: 3
  • Publication Date: 2022
  • Doi Number: 10.3923/ijp.2022.522.526
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), BIOSIS, CAB Abstracts, EMBASE, Veterinary Science Database
  • Page Numbers: pp.522-526
  • Keywords: Paraoxonase, carfilzomib, inhibition, anticancer drug, multiple myeloma, HDL, lymphoblastic lymphoma, OXIDATIVE STRESS, BLOOD-PRESSURE, PON1, MOUSE, PURIFICATION, EXPRESSION
  • Bursa Uludag University Affiliated: Yes


Background and Objective: hPON1 is an HDL-related lactonase that can inhibit LDL. It is considered atheroprotective. hPON1 contributes to the antioxidant function of HDL. It is believed that a decrease in PON1 activity may promote atherosclerosis. This article was aimed to investigate the inhibitory effect of carfilzomib on hPON1. Materials and Methods: In this study, we detect the inhibition between hPON1 and carfilzomib used in the treatment of myeloma. Results: We determined that carfilzomib showed very strong inhibitory properties for human serum PON1, with an IC50 value of 43.31 mu M and a mean K-i value of 44.37 mu M. We determined that carfilzomib showed competitive inhibition. Conclusion: The use of carfilzomib, which has a very strong inhibitory effect, in the treatment of multiple myeloma can be very harmful.