Journal
ANTIOXIDANTS
Volume 11, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/antiox11102058
Keywords
lyso-DGTS; paraoxonase 1; docking; structure-activity relationship; antioxidant activities; LDL oxidation
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This study examined the effects of lipids on PON1 enzyme activity and LDL oxidation using structure-activity relationship methods. The results showed that certain lipids significantly increased PON1 activity and inhibited LDL oxidation.
Paraoxonase 1 (PON1) plays a role in regulating reverse cholesterol transport and has antioxidative, anti-inflammatory, antiapoptotic, vasodilative, and antithrombotic activities. Scientists are currently focused on the modulation of PON1 expression using different pharmacological, nutritional, and lifestyle approaches. We previously isolated a novel active compound from Nannochloropsis microalgae-lyso-diacylglyceryltrimethylhomoserine (lyso-DGTS)-which increased PON1 activity, HDL-cholesterol efflux, and endothelial nitric oxide release. Here, to explore this important lipid moiety's effect on PON1 activities, we examined the effect of synthesized lipid derivatives and endogenous analogs of lyso-DGTS on PON1 lactonase and arylesterase activities and LDL oxidation using structure-activity relationship (SAR) methods. Six lipids significantly elevated recombinant PON1 (rePON1) lactonase activity in a dose-dependent manner, and four lipids significantly increased rePON1 arylesterase activity. Using tryptophan fluorescence-quenching assay and a molecular docking method, lipid-PON1 interactions were characterized. An inverse correlation was obtained between the lactonase activity of PON1 and the docking energy of the lipid-PON1 complex. Furthermore, five of the lipids increased the LDL oxidation lag time and inhibited its propagation. Our findings suggest a beneficial effect of lyso-DGTS or lyso-DGTS derivatives through increased PON1 activity and prevention of LDL oxidation.
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