The extraction of medicinal or functional compounds from herbal plants is an important unit operation in food and bio-industries. The target compounds are generally present inter- or intra-cellularly in an intricate microstructure formed by cells, intercellular spaces, capillaries, and pores. The major resistance of molecular diffusion in materials of plant origin always comes from the intact cell walls and adhering membranes. Therefore, increasing the permeability of cell walls and membranes plays a very important role to increase extraction yield and/or extraction rate. Important pretreatment methods to modify the cellular structures and increase the permeability of cell walls or membranes are discussed in this paper. They include physical, biologic, and chemical treatments. In physical methods, mechanical disruption, high-pressure (HP) process, pulsed electric field (PEF) application, ultrasonic treatment, and freeze-thaw, and so on were applied. In biologic methods, different cell wall-degrading enzymes were applied to break-down cell walls or membranes and to diminish the overall internal resistance for transporting bioactive compounds from internal matrix to the external solution. In chemical methods, various chemicals for increasing the inner- or outer-membrane permeabilization were introduced. The principles of the technologies, examples of improvements, and advantages and disadvantages of the pretreatment methods are critically reviewed in this paper.