Caveolins are integral membrane proteins which consist of caveolae, present in plasma membrane. Many researchers have reported the role of caveolae in major physiological conduits of the mammalian cells, including cholesterol homeostasis, transcytosis and endocytosis. Caveolin also play a role in ischemic preconditioning of heart, postmenopausal women, brain microvessels, cancer progression and Alzheimer’s disease. Attenuation of myocardial protection in diabetic heart may be due to decrease in the ischemic preconditioning mediated release of nitric oxide, upregulation of caveolin and consequently decrease in activity of endothelial nitric oxide synthase (eNOS). Caveolin alogwith integral membrane proteins overexpress in a huge range of tumor entities, while hormonal changes cause variation in caveolin expression. Under ovariectomy conditions, eNOS inhibitory action occurs because of interaction between eNOS and caveolin. Some new concepts explain that multiple proteins, including caveolin-1 alter trans-membrane flux of fatty acid and play role in fatty acid uptake. Caveolin can be useful in the controlling of cardiovascular system (CVS) and brain disease using various predicaments. New intermediate steps have been discovered which correlate various mechanisms of ischemic preconditioning, cardiopotection and eNOS in the field of cardiovascular research.