Abstract: There is provided a pharmaceutical composition for preventing or treating human immunodeficiency virus, and more particularly, to a pharmaceutical composition and health functional food for preventing or treating/improving human immunodeficiency virus, the pharmaceutical composition and health functional food including a new compound with chitooligosaccharides conjugated amino acids or dipeptides as an effective component. The new compound has an excellent anti-HIV effect through an activity of inhibiting a HIV initial infection by interrupting an interaction between host-virus membranes, and also activities of inhibiting reverse transcriptase and protease of HIV. The compound according to the present invention is a conjugate synthesized through conjugating chitooligosaccharides derived from a natural material with amino acids or dipeptides. The compound is stable without cytotoxicity.