Due to its pharmacological properties, α-Mangostin, mainly found in () L. (Mangosteen, queen of fruits), treats wounds, skin infections, and many other disorders. In fact, α-Mangostin and other xanthonoid, including β-Mangostin and γ-Mangostin, are found in , which have various advantages, namely neuroprotective, anti-proliferative, antinociceptive, antioxidant, pro-apoptotic, anti-obesity, anti-inflammatory, and hypoglycemic through multiple signaling mechanisms, for instance, extracellular signal-regulated kinase1/2 (ERK 1/2), mitogenactivated Protein kinase (MAPK), nuclear factor-kappa B (NF-kB), transforming growth factor beta1 (TGF-β1) and AMP-activated protein kinase (AMPK). This review presents comprehensive information on Mangosteen's pharmacological and antitoxic aspects and its xanthones against various natural and chemical toxins. Because of the insufficient clinical study, we hope the current research can benefit from performing clinical and preclinical studies against different toxic agents.