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

SÖYÜT H.

INTERNATIONAL JOURNAL OF PHARMACOLOGY, cilt.18, sa.3, ss.522-526, 2022 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 18 Sayı: 3
  • Basım Tarihi: 2022
  • Doi Numarası: 10.3923/ijp.2022.522.526
  • Dergi Adı: INTERNATIONAL JOURNAL OF PHARMACOLOGY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), BIOSIS, CAB Abstracts, EMBASE, Veterinary Science Database
  • Sayfa Sayıları: ss.522-526
  • Anahtar Kelimeler: Paraoxonase, carfilzomib, inhibition, anticancer drug, multiple myeloma, HDL, lymphoblastic lymphoma, OXIDATIVE STRESS, BLOOD-PRESSURE, PON1, MOUSE, PURIFICATION, EXPRESSION
  • Bursa Uludağ Üniversitesi Adresli: Evet

Özet

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.