Background: Leucas cephalotes has been used by many tribes to treat variety of diseases and known to have many essential secondary metabolites. To the best of our knowledge, it is the first comparative analysis of total fatty acid (FA) composition and α-amylase inhibition activity of L. cephalotes. Objective: The present study is carried out to explore the antihyperglycemic activity and FA contents of all parts of L. cephalotes. Material and Method: Fruits, leaves, stems, and roots part of L. cephalotes have been extracted in ethanol. Simultaneously, all plant parts have been extracted in hexane with Soxhlet extraction. Ethanolic extracts have been evaluated for antihyperglycemic activity and hexane extract have been analyzed for FA identification. Result: The present study indicated that ethanolic extract of fruit and leaves have shown significant α-amylase inhibitory activity with IC50 value of 92.86 ± 0.89 and 98.09 ± 0.69 μg/mL, respectively. FA composition of all the parts of L. cephalotes was analyzed by GC/MS. Nineteen FAs have been identified in all parts of L. cephalotes in which palmitic acid, oleic acid, linolenic acid, and linoleic acid were major FAs. Conclusion: The study indicates that L. cephalotes has significant potential to inhibit α-amylase enzyme and it is a rich source of essential FAs.