A review: Inhibitors and activators for paraoxonase 1

Abstract： Paraoxonase 1 (PON1) is a calcium-dependent hydrolase with many physiological functions. The decrease of PON1 activity is related to many diseases. The research about PON1 is a hot topic, and its activators and inhibitors are expected to help in our diets and in choose of drugs. The papers about PON1 activators and inhibitors were collected and classified. The PON1 activators and inhibitors are grouped into four categories: in-vivo activators, in-vitro activators, in-vivo inhibitors and in-vitro inhibitors. For each activator or inhibitor, the activating effect or inhibiting effect along with the methods used was reviewed. Up to now, we found from literatures that there were 16 samples demonstrating activating effects on PON1 in-vivo and 5 compounds showed in-vitro activation. Of the 16 in-vivo activators there were 4 plant extracts and 12 pure components. Seven in-vivo inhibitors and 71 in-vitro inhibitors have been reported in publications. Additionally, smoking, drinking and treatment with exogenous gonadotropins induced decrease of PON1 activity. The summary of the activators and inhibitors are beneficial to reveal the structure-activity relationship, and also it provides convenience to look up the activating or inhibiting effects of the compounds on PON1 at a glance.