BACKGROUND: Numerous studies suggest that morellic acid (MOR), highly available in Garcinia plants, has different physiological activities, including anti-cancer, anti-oxidant, and anti-microbial activity. AIM: In this investigation, we aimed to demonstrate the anxiolytic activity, along with the mechanism behind this activity of MOR, using in vivo and in silico studies. METHODS: For this, we used different doses of MOR (5 and 10 mg/kg) and administered this drug intraperitoneally to Swiss albino mice (male and female). Diazepam (DZP), a positive allosteric modulator of the GABA RESULTS: This investigation revealed that MOR remarkably reduced the locomotor activity of mice in a dose-dependent manner and produced calming behaviors like DZP. However, the findings showed that the combination of MOR and DZP synergistically reduced the locomotion of mice compared to the single therapy. On the other hand, from the computational study, the result demonstrated that MOR exhibited the highest binding scores (-9.2 kcal/mol) towards the GABA CONCLUSION: However, it is recommended that more precise and comprehensive preclinical investigations be required to demonstrate the exact mechanism behind the anxiolytic effects and conduct clinical trials to determine efficacy and safety.