Rosmarinic acid extract with potent biological activities was successfully isolated by supramolecular technique and solvent extraction from Perilla leaves. By the supramolecular complex which was formed from flavocommelin and Perilla leaf extract as initial materials, the supernatant containing rosmarinic acid was isolated. Rosmarinic acid extract (62.9 ± 4.5% purity) was partly purified by partitioning ethyl acetate and water. Rosmarinic acid extract exhibited high total phenolic content of 433.9 ± 58.6 μg/mg of gallic acid equivalent, effective DPPH radical scavenging activity (SC50 of 5.5 ± 0.2 μg/mL), antiallergic activity (IC50 of 52.9 ± 6.7 μg/mL), and α-glucosidase inhibitory activity (IC50 of 0.23 ± 0.01 mg/mL). Rosmarinic acid extract shows high potential for diabetes mellitus and allergy treatments by inhibiting α-glucosidase activity and measuring β-hexosaminidase, related to life-style disease.