The synthetic approaches towards unique asparagusic acid and its analogues as well as its chemical use, the breadth of its biological properties and their relevant applications have been explored. The significance of the 1,2-dithiolane ring tension in dithiol-mediated uptake and its use for the intracellular transport of molecular cargoes is discussed alongside some of the challenges that arise from the fast thiolate-disulfide interchange. The short overview with the indication of the available literature on natural 1,2-dithiolanes synthesis and biological activities is also included. The general review structure is based on the time-line perspective of the application of asparagusic acid moiety as well as its primitive derivatives (4-amino-1,2-dithiolane-4-carboxylic acid and 4-methyl-1,2-dithiolane-4-carboxilic acid) used in clinics/cosmetics, focusing on the recent research in this area and including international patents applications.