This study aimed to examine whether Ocimum gratissimum (OG) has the Angiotensin-converting enzyme (ACE) inhibitory activity in vitro and in spontaneously hypertensive rats (SHRs). OG water extract exhibited an in vitro ACE-inhibition activity, with the 50% inhibition concentration (IC50) value being 56.3 mu g/mL, which is higher than rutin's 43.08 mu g/mL. The main phenolic compound found in OG extract was rutin, according to the HPLC fractionation profile. The anti-hypertension effect in vivo was tested with SHRs. SHRs were fed orally with a distilled water, 100 or 500 mg/kg BW OG extract for 8 weeks. Systolic blood pressure, ACE levels in plasma and lung, and plasma endothelin-1 were significantly lower in the 500 mg/kg OG group compared with the SHRs group. These results suggested that OG extract has the ACE inhibition activity in vitro and also in SHRs, which may be due to its main component of phenolic compound, rutin. (C) 2017 Elsevier Ltd. All rights reserved.