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Troxerutin (TRX), a semi-synthetic bioflavonoid derived from rutin, has been reported to exert several pharmacological
effects including antioxidant, anti-inflammatory, antihyperlipidemic, and nephroprotective. However, the related molecular details
and its mechanisms remain poorly understood. In the present review, we presented evidences from the diversity in vitro and in vivo
studies on the therapeutic potential of TRX against neurodegenerative, diabetes, cancer and cardiovascular diseases with the purpose
to find molecular pathways related to the treatment efficacy. TRX has a beneficial role in many diseases through multiple mechanisms including, increasing antioxidant enzymes and reducing oxidative damage, decreasing in proapoptotic proteins (APAF-1, BAX,
caspases-9 and-3) and increasing the antiapoptotic BCL-2, increasing nuclear translocation of nuclear factor erythroid 2-related factor
2 (Nrf2) and downregulating the nuclear factor κB (NFκ). TRX also reduces acetylcholinesterase activity and upregulates phosphoinositide 3-kinase/Akt signaling pathway in Alzheimer’s disease models. Natural products such as TRX may develop numerous and
intracellular pathways at several steps in the treatment of many diseases. Molecular mechanisms of action are revealing novel, possible combinational beneficial approaches to treat multiple pathological conditions.