The mechanism of biotransformation comprehensive studies has been made and used in the pharmaceutical industry for commercialization of pharmaceutical drugs. Biotransformation studies of β-methyldigitoxin to p-methyldigoxin in Digitalis lanata cells were performed. By using horseradish peroxidise and glucose oxidase in biotransformation studies, anhydrovinblastine was synthesized from vindoline. Two new compounds (eudesmane and guaiane) were synthesized from biotransformation of a-santonin in cell cultures of Catharanthus roseus. Cell culture studies demonstrate an extensive phytochemical potential for the production of secondary products via biotransformation. The biotransformation of bioactive principle such as dydrogesterone was incubated with Azadirachta indica cells, for synthesis of dydrogesterone. The process of biotransformation includes chemical reactions catalyzed by entrapped enzymes of regioselectivity and stereospecificity in immobilized plant cells. By this methodology, production of highly significant secondary metabolites was enhanced in plant cells or organs.