Immunomodulatory and immunostimulatory effects of some bisbenzoxazole derivatives on lipopolysaccharide stimulated mammalian macrophages

Abstract

Benzoxazoles and their derivatives have exerted anti-cancer and anti-inflammatory (immunomodulatory)potential due to their anti-proliferative effect on the cells. These molecules are DNA basebioisosteres, therefore, theirmechanism of action could be by mimicking the structures of the DNA bases and halting the DNA polymerizationprocesses. Based on their anti-proliferative effect, in our study we aimed to decipher the potential anti-inflammatoryactivities of unique bisbenzoxazole derivatives in vitro on mammalian macrophages. Being able to manipulate theinflammatory function of macrophages would enable the regulation of the immune response against danger stimuli.This would enable us better prognosis against different types of the diseases ranging from autoimmune disorders tocancer. Our results support the stark anti-inflammatory potential of bisbenzoxazole derivatives RHE 241 and RHE 248in vitro on the LPS activated mammalian macrophages. After further delineation of their mechanism of action in vitroand their in vivo potency, these molecules could be utilized as potent anti-inflammatory medicines.