The present invention conveys a fractionation method to isolate different bioactive Phytocannabinoids by solid phase extraction using HP-20 resins and one step method to synthesize C- and O-β-D-glycoside derivatives of Cannabinoid by using a β-D-glucose donor (O-Glycosyl trichloroacetimidate donor) to obtain glycosidic derivatives. The novel C-glycosides of Cannabinoids displayed significant anti-proliferative properties against wide range of human cancer cell lines as compared to their respective parent molecules. Furthermore, the C- and O glycosides of Cannabinoids also showed anti-invasive and anti-migratory activities against metastatic cancer cells of breast and pancreatic origin. When applied in combination with DNA damaging agent (5-Fluorouracil) to colorectal cancer cells, the C- and O-glycosides of Cannabinoids potentiate DNA damaging property and thus augment apoptosis resulting in an increment in the efficacy of DNA damaging drugs.