The crude hydroalcoholic root extract (CRE) of Solanum sisymbriifolium Lam.
has formerly been shown to have hypotensive activity both in normo-and hyp
ertensive rats. Hypotensive activity-guided fractionation of the CRE was pe
rformed in anaesthetized normotensive rats, which led to the isolation of t
he active principles. The intravenous (i.v.) and intraperitoneal (i.p.) val
ues of the CRE in mice were found to be, respectively, 343 and 451 mg/kg, a
nd no lethal effect was caused by doses up to 5.0 g/kg when administered by
oral route. Depression of locomotion, increase of breathing rate and piloe
rection was observed in a general behavior test with doses up to 200 mg/kg
i.p., and 1000 mg/kg p.o., respectively. Increase in the gastrointestinal t
ransit was found using 0.1 g/kg, whereas at doses of 0.5 and 1 g/kg, no sig
nificant activity was observed in comparison with the control mice. Hexanic
and butanolic fractions induced a remarkable hypotension in anaesthetized
normotensive rats in doses of 1, 5, 7.5 and 10 mg/kg i.v. Two compounds iso
lated from the butanolic fraction induced a significant decrease of the blo
od pressure, HR, amplitude of the ECC and breathing rate when injected in a
dose of 1 mg/kg i.v; and both systofic and diastolic, blood pressures were
affected in a proportional mode. The hypotensive effect of the two compoun
ds were not influenced by pretreatment with atropine and propranolol; and t
he presser response to noradrenaline was not affected by any of them which
suggests that neither a direct muscarinic activity, beta-adrenoceptor activ
ation nor decrease of sympathetic vascular tone (sympatholitic activity) ar
e probably involved in the mechanism of hypotension. The present study show
s that the CRE of S. sisymbriifolium contains at least two hypotensive comp
ounds whose characterization is under way. (C) 2000 Elsevier Science Irelan
d Ltd. All rights reserved.