Inhibitory Effects of Bendamustine on Human Serum Paraoxonase-1 (hPON1)

Abstract

hPON1 is an ester hydrolase associated with HDL and having a molecular mass of 43-45 kDa. It is synthesized in the liver. It hydrolyzes organophosphate agents and nerve gases. It plays a protective role against oxidation of LDL and formation of lipid peroxides and bacterial endotoxins. The fact that oxidation of LDL constitutes the initial stage of the atherosclerosis process demonstrates the importance of hPON1 antioxidant properties. Many epidemiological studies have shown an inverse relationship between HDL cholesterol levels and cardiovascular events. It is known that high serum HDL-cholesterol and low LDL-cholesterol levels are protective against the development of coronary heart disease and atherosclerosis. Therefore, hPON1 is a component of HDL, thus contributing to the protective role of HDL in coronary artery disease. In this research, we investigated the inhibition effects of bendamustine on hPON1 enzyme activity in the human serum in vitro conditions.

Keywords

• bendamustine
• inhibition
• Paraoxonase

İnsan Serum Paraoksonaz-1 (hPON1) Üzerine Bendamustin İnhibisyon Etkisi

Abstract

hPON1, HDL ile ilişkili ve 43-45 kDa'lık bir moleküler kütleye sahip olan bir ester hidrolazdır. Karaciğerde sentezlenir. Organofosfat ajanlarını ve sinir gazlarını hidrolize eder. LDL'nin oksidasyonuna ve lipit peroksitlerin ve bakteriyel endotoksinlerin oluşumuna karşı koruyucu bir rol oynar. LDL'nin oksidasyonunun ateroskleroz sürecinin başlangıç aşamasını oluşturması, hPON1 antioksidan özelliklerinin önemini göstermektedir. Birçok epidemiyolojik çalışma HDL kolesterol düzeyleri ile kardiyovasküler olaylar arasında ters bir ilişki olduğunu göstermiştir. Yüksek serum HDL-kolesterol ve düşük LDL-kolesterol seviyelerinin koroner kalp hastalığı ve ateroskleroz gelişimine karşı koruyucu olduğu bilinmektedir. Bu nedenle, hPON1 bir HDL bileşenidir, bu nedenle koroner arter hastalığında HDL'nin koruyucu rolüne katkıda bulunur. Bu araştırmada, in vitro koşullarda insan serumunda hPON1 enzim aktivitesi üzerine bendamustin kemoterapik ilacının inhibisyon etkisini araştırdık.

Keywords

• Paraoksanaz
• inhibisyon
• bendamustin

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