Agnuside (AGN), an iridoid glycoside, is the principle active phytoconstituent and a chemotaxonomic marker of the genus Vitex. It is isolated from V. agnus castus, V. negundo, and V. cymosa and composed of aucubin and p-hydroxy benzoic acid (PHBA). Agnuside has exhibited estrogen-like activity which might be the reason for its use in premenstrual syndrome problems in women of fertile age as well as in menopause. It has also been reported to possess anti-arthritic activity in the polyarthritis rats which was associated with significant suppression of the inflammatory mediators and T-cell mediated cytokinines. Recently, Agnuside has shown higher hepatoprotective potential in rats in comparison to silymarin, a commercially available herbal hepatoprotective agent. In addition, Agnuside has shown an inhibitory effect on P-glycoprotein (P-gp) ATPase activity. The diversified therapeutic indications of AGN with a profoundly high medicinal value have created great curiosity among researchers for its further investigation as a medicinal agent.