Multi-targeting drug discovery research has been driven, medically, commercially and intellectually; this need has often been equated with the identification and exploitation of novel targets. Glycolipids present both potentials and problems, their biological relevance has been recognized, but problems in procuring lipids rendered them a difficult class of compounds to handle in drug discovery efforts. Sulfoquinovosylacylglycerols (SQAGs), which are one of the abundant sulfur-containing glycerolipids in the biotic world, isolated from different phototrophic organisms, particularly plants and algae, have already been identified as bioactive compounds. In addition to their antiviral activity, their influence on the immune response in mammalian cells is the focus of many studies shown to have an important role in several biological activities. The purpose of this contest is to spotlight the longtime untouched topics of availability, historical background synthesis and recent findings of SQAG's as mammalian DNA polymerase inhibitor, antiangiogenesis, radiosensitizer, immunosuppressive quality, HIV-reverse transcriptase inhibitor, not only for optimizing the treatment of cancer but also for developing the therapeutic approaches for various diseases. This is definitely the beginning of the revolution in the biotic world.