The present invention relates to agent for suppressing infection and proliferation of human immunodeficiency syndrome virus (HIV-1), which infects immunocompetent cells such as macrophage or dendritic cell and causes destruction of immune system, and use of known compounds, macrolide derivatives for suppression of infection and proliferation of human immunodeficiency syndrome virus in M type macrophage derived from human monocytes. The present invention is useful for treatment of patients with HIV-1 infection by low cost chemotherapeutic agents, and in addition, is clinically used as supplement agent in HAART.