The present invention relates to a pharmaceutical composition to prevent or treat human immunodeficiency virus (HIV) and, more specifically, to a pharmaceutical composition and a health functional food to prevent or treat human immunodeficiency virus, comprising as an active ingredient, a novel compound in which chitosan oligosaccharide is linked to amino acid. The novel compound of the present invention does not only suppress early HIV infection by inhibiting the interaction between a host cell membrane and a viral membrane, but also have excellent anti-HIV effect through activity to inhibit HIV reverse transcriptase and protease. Therefore, the composition of the present invention comprising the novel compound as an active ingredient can exhibit excellent effects in the prevention or treatment/amelioration of HIV, and thus is useful as a functional medicinal composition and food composition. In particular, the novel compound of the present invention is complex synthesized by linking amino acid or dipeptide to naturally occurring chitosan oligosaccharide and has stability without cytotoxicity, and thus the composition of the present invention comprising the novel compound as an active ingredient has an advantage of being stable despite long-term usage.COPYRIGHT KIPO 2014