Background: Vitis vinifera has been long used as herbal medicine, dietary supplement, and functional food due to its hydrophilic and lipophilic constituents. Vitis vinifera is commonly known as the grape vine, and many species of Vitris vinifera have been profusely found in the region of Mediterranean, Europe and many areas of Asia including Morocco, and Portugal. Objectives: The objective of this review was to summarize the pharmacological activities of Grape Seed Oil (GSO) by analyzing various effects including anti-inflammatory, neuroprotective, anti-hyperlipidemic, anti-hepatotoxic, wound-healing effect, as antioxidant, radio-protective and hepato-protective effects. Methodology: The literature was searched using Google Scholar. Initially, 53 relevant reports were shortlisted for the detailed analysis. After compiling and summarizing, 40 full-length articles were reviewed and summarized in this review. Results: On basis of thorough review of 40 articles, it was found that GSO has high potential uses as nutraceutical due to its antioxidant property, total phenol and other minor constituents. Grape polyphenols have high antioxidant action; providing key role in fetus protection, while another constituent like pro-anthocyanidins have strong ability of prevention of stress-triggered abortion and resveratrol with an action on inhibition of uterine contractions. Conclusion: It was concluded that GSO has numerous pharmacological activities and a very strong potential as antioxidant, anti-in?ammatory, antimicrobial, neuroprotective, antihyperlipidemia, antihepatotoxic, wound-healing, radio protective and hepatoprotective. It is suggested that GSO can successfully be used as herbal medicine due to its high antioxidant potential, and due to its phenolic compounds, grape seed oil is effective in peptic ulcer and other diseases.