Restorative Dentistry today is increasingly moving away from passive replacement of lost dental tissues and more toward biologically active methods that will preserve the remaining dentin structure, control the cariogenic biofilm, stabilize the dentin matrix and enhance restoration longevity. Of the interest in plant derived bioactive compounds, some phytochemicals have antimicrobial, antioxidant, anti-inflammatory, collagen-cross-linking, matrix metalloproteinase-inhibitory and remineralizing properties. Potential restorative molecules like proanthocyanidins, epigallocatechin-3-gallate, quercetin, resveratrol, curcumin, genipin, hesperidin and naturally occurring photosensitizing and cross-linking molecules have been tested for such use. Experimental studies suggest that these compounds can strengthen demineralized dentin, inhibit collagen degradation, decrease the activity of cariogenic biofilm, enhance the stability of resin-dentin interface, create a more favorable environment for mineral deposition [1-6]. Recently, the inclusion of phytochemicals in dental adhesives, and as polymerizable derivatives in composite materials, has provided an opportunity for the development of multifunctional restorative materials [7-11]. However, for the time being these are hampered by concentration-dependent effects, chemical instability, possible interference with resin polymerization, discoloration, and the absence of standardization of the formulations and limited clinical evidence over a long period. In this review, the biological basis, key phytochemical constituents, mechanism of action, therapeutic uses of phytochemicals in modern restorative dentistry are discussed, along with limitations and future prospects.