Vitis vinifera, known as the grapevine, is native to southern Europe and Western Asia. Grape seed and skin contain several active components including flavonoids, polyphenols, anthocyanins, proanthocyanidins, procyanidines, and the stilbene derivative resveratrol. Grape seed extract in particular has been reported to possess a broad spectrum of pharmacological and therapeutic effects such as antioxidative, anti-inflammatory, and antimicrobial activities, as well as having cardioprotective, hepatoprotective, and neuroprotective effects. Thus, the present review attempts to give a short overview on the pharmacological, toxicological, and clinical studies of grape and its active components.