Medicinal plants have played a key role in world health. Today, science has isolated the medicinal properties of a large number of botanicals, and their healing components have been extracted and analyzed. Many plant components are now synthesized in large laboratories for use in pharmaceutical preparations. However, the potential of many plants species as source for new drugs is still largely unexplored. Premna esculenta Roxb. belonging to the family of Lamiaceae, is one of a covered shrub used traditionally by tribal people of Bangladesh for the treatment of various inflammatory conditions. Considering the vast area of potentiality of plants as sources for drugs and taking into account the local traditional uses, a systematic investigation was undertaken to screen the phytochemical and pharmacological activity of different fractions of Premna esculenta. The plant was extracted with solvents to obtain ethanolic, chloroform and pet-ether fractions, which were then subjected to phytochemical screenings and various pharmacological studies. The study showed the plant contains effective active compounds that can be a potential source of biologically important drug candidates.