Three new compounds, ocimumosides A (1) and B (2) and ocimarin (3), were isolated from an extract of the leaves of holy basil (Ocimum sanctum), together with eight known substances, apigenin, apigenin-7-O--D-glucopyranoside, apigenin-7-O--D-glucuronic acid (4), apigenin-7-O--D-glucuronic acid 6′′-methyl ester, luteolin-7-O--D-glucuronic acid 6′′-methyl ester, luteolin-7-O--D-glucopyranoside, luteolin-5-O--D-glucopyranoside, and 4-allyl-1-O--Dglucopyronosyl-2-hydroxybenzene (5), and two known cerebrosides. The structures of the new compounds were determined on the basis of extensive 1D and 2D NMR spectroscopic analysis. The new compounds (1–3) and the known compounds 4 and 5 were screened at a dose of 40 mg/kg body weight for acute stress-induced biochemical changes in male Sprague–Dawley rats. Compound 1 displayed promising antistress effects by normalizing hyperglycemia, plasma corticosterone, plasma creatine kinase, and adrenal hypertrophy. Compounds 2 and 5 were also effective in normalizing most of these stress parameters. In contrast, compounds 3 and 4 were ineffective in normalizing any of these effects.