Arborinine is an acridone alkaloids obtained from different natural sources including in the majority bark, seed, leaves of plants species of Rutaceae family among which Teclea gerrardii, Zanthoxylum leprieurii and Teclea trichocarpa, Erthela bahiensis, Ruta angustifolia,, Ruta suavolenses.. This alkaloid is extensively studied due to its great pharmacological potential, which includes anticancer, antimicrobial, antiparasitic, antifeedant and antioxidant activities among others. Arborinine block heme-mediated protein oxidation and degradation markers for heme-induced oxidative stress; was predicted virtually for a critical evaluation by In silico target fishing for rationalized ligand discovery by inhibiting acetylchlolinesterase with IC50 value 34.7 ± 71µM; displayed potent in vitro activities against chloroquine sensitive HB3 cell line and chloroquine resistance K1 cell line with IC50 value 3.85 ± 0.11μM and 9.34 ± 0.37 μM; showed the good anticancer activity on three human cancer line viz human colon cancer COLO-205, human ovarian cancer OVCAR-3, Human cervical cancer human breast cancer and T-47D line with GI50 value ˂10μg/ml and presented antimicrobial activities against resistant microbial strains. The overall synthesis of Arborinine has been done and the key stapes are the Ullmann condensation followed by the cyclisation with Eaton’s reagent. It undergoes a few structural modification reactions such as selective methylation and demethylation, electrophilic substitution. Acetylation, benzoylation. This review present the chemistry and the biological properties of Arborinine: methods of isolation from plant crude extract, its characterization as well as their derivatives obtained by structural modification including structure activity relationship are also described.