Natural products/ phytochemicals continue to serve as preventive and therapeutic agents formany pharmaceutical or cosmetic industries in finding new therapeutic agents against widerange of diseases. Tetrahydrocurcumin is a major colourless metabolite of curcuminoidsisolated from Curcuma longa. Despite wider therapeutic applications of tetrahydrocurcumin,the low aqueous solubility and bioavailability of the compound in humans, impairs its use inbiological and pharmacological activities. The object of the study is to synthesizetetrahydrocurcumin-di-P-glycoside and to evaluate its biological and pharmacological activity.The maximum plasma concentration of tetrahydrocurcumin-di-P-glycoside (2%) onsubcutaneous absorption was 4.35 ig/ml after two hours of the compound application, whichwas higher concentration than other curcuminoids studied. The present study demonstratedpromising antioxidant, antimicrobial and efficient tyrosinase enzyme inhibition activities. Theaccelerated wound-healing process with non toxic, non- irritant and non staining propertiesrender this multi-functional compound tetrahydrocurcumin-di-P-glucoside as a usefulingredient in achromatic food and cosmetic applications.