Medicinal fungi, taken whole or as various forms of extracts, have been used to alleviate, cure or prevent human ailments since pre-historic times. In particular, Asian cultures have incorporated a variety of mushrooms into their medical practices. Chemically pure, bioactive metabolites from fungi have been a mainstay of modern pharmacological research and in addition to antibiotics, include anticancer agents, immunosuppressants, enzyme inhibitors, antagonist and agonists of hormones, and a variety of psychotropic substances. However, to date not many studies have focused on the possible health benefits of odorant volatile organic compounds (i.e., gas phase compounds). An analysis of these compounds for their health related effects will expand the range of compounds available for the treatment of chronic and acute diseases. This review highlights phenolic acids and monoterpenes from Asian medicinal mushrooms (AMMs), which not only produce pleasant odors but also have antioxidant and antibacterial effects. Odorant bioactive volatile phase compounds from medicinal mushrooms remain an essentially untapped source for future medicines, and AMMs remain a promising resource for future pharmacological research.