The antihypertensive and vasodilator effects of aqueous extract from Berberis vulgaris fruit on hypertensive rats

The aqueous extract from Berberis vulgaris fruit (B.V.) was tested to evaluate its antihypertensive effects on DOCA-induced hypertension in the rats. Hypertension was induced in male Sprague-Dawley rats (200-250 g) by DOCA-salt injection (20 mg/kg, twice weekly, for 5 weeks, s.c.) plus NaCl (1%) which was added to the animals' drinking water. Then 5 weeks later, the rats were anaesthetized with thiopental (30 mg/kg, i.p.) and the arterial blood pressure was measured. The mean arterial blood pressure and heart rate were 231 +/- 6.4 (mmHg) and 506 +/- 12 (beats/min), respectively. Administration of B.V. extracts significantly reduced the rat arterial blood pressure. In in vitro studies, rings of descending aorta were cut and mounted for isometric tension recording in an organ chamber containing Krebs solution. Mesenteric beds were also removed and perfused with Krebs solution. After 1 h of stabilization, preparations (aortic rings or mesenteric beds) were precontracted with phenylephrine (10(-5) M), then different concentrations of B.V. (0.4, 2 and 4 mg/mL) were added which caused a relaxation in these vessels. To investigate the mechanism of action of the extract, the tissues were incubated with either L-NAME (10(-5) M) or indomethacin (10(-5) M) for 20 min. In the aortic rings L-NAME pretreatment could only reduce the vasodilatory effects of a low concentration of B.V. (0.4 mg/mL), but indomethacin was without effect. In isolated perfused mesenteric beds preincubation with either L-NAME or indomethacin did not modify the vasodilator effects of the aqueous extract from B.V. fruit. The present results suggest that the antihypertensive and vasodilatory effects of B.V. fruit extract are mainly endothelial-independent and it may be used to treat hypertension, a status with endothelial dysfunction.     

Blood pressure depression by the fruit juice of Carica papaya (L.) in renal and DOCA-induced hypertension in the rat

A crude ethanol extract was prepared from the unripened fruit of Carica papaya. Lethality studies showed a dose-mortality relationship with an LD(50) of 325.2 mg/kg in mice administered i.p. Male albino Wistar rats were randomly divided into three batches (15 rats per batch)-renal, DOCA-salt hypertensives and normotensives. Each batch was further divided into three groups-the untreated, hydrallazine and extract treated groups. The mean arterial blood pressure (MAP) and the heart rate were measured in all groups. From the results, the basal (control) MAP were 93.8 +/- 4.5, 175.2 +/- 5. 1 and 181.3 +/- 6.2 mmHg in the normotensive, renal and DOCA-salt hypertensives, respectively. Both hydrallazine (200 microg/100 g i. v) and extract (20 mg/kg.i.v) produced a significant depression of MAP in all groups (p < 0.01 vs controls), but the extract produced about 28% more depression of MAP than hydrallazine in the hypertensive groups. In another group of rats, the extract failed to depress the MAP in rats pretreated with propranolol, but atropine and noradrenaline pretreatment did not prevent the action of the extract on blood pressure. In vitro studies using isolated rabbit arterial (aorta, renal and vertebral) strips showed that the extract (10 microg/mL) produced relaxation of vascular muscle tone which was, however, attenuated by phentolamine (0.5-1.5 microg/mL). It is concluded that the fruit juice of C. papaya probably contains antihypertensive agent(s) which exhibits mainly alpha-adrenoceptor activity.     

The hypotensive mechanisms for the aqueous stem bark extract of Musanga cecropioides in Sprague-Dawley rats

The present study was designed to evaluate the hypotensive properties and the mechanisms of action of the stem bark aqueous extract of Musanga cecropioides R.Br. Apud Tedlie (MCW) in anesthetized rats of Sprague-Dawley strain, through an invasive direct blood pressure measuring procedure. Thirty adult rats, weighing 150-230 g, were grouped into five groups of six rats each. The effects of the intravenous graded doses (0.0005-0.05 mg/kg) of the extract on the blood pressure indices were investigated. Its underlying mechanisms were also studied using additional five groups of rats. The results showed that the extract caused a dose dependent fall in the systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure and heart rate of the rats. Bilateral carotid artery occlusion (BCO) caused a reflex increase in mean arterial pressure and heart rate which were significantly attenuated by the extract injection. Angiotensin Converting Enzyme (ACE) blockade with 5 mg/kg of Captopril and cholinergic blockade with 0.2 mg/kg of atropine significantly attenuated the hypotensive response to MCW. However, the pattern of MAP fall in rats pretreated with a combination of Promethazine (1 mg/kg) and Cimetidine (15 mg/kg) was not significant. The results of the study was able to demonstrate dose dependent hypotensive effect of MCW and that its vasorelaxant effects may be through inhibition of sympathetic, cholinergic control of the arterial pressure and most significantly through ACE blockade. However, the phytochemical, elemental and toxicological studies of this potential antihypertensive still needed to be investigated.     

Hypotensive effect of aqueous saffron extract (Crocus sativus L.) and its constituents,safranal and crocin,in normotensive and hypertensive rats

In this study, the effects of saffron (Crocus sativus) stigma aqueous extract and two active constituents, crocin and safranal, were investigated on blood pressure of normotensive and desoxycorticosterone acetate‐induced hypertensive rats. Three doses of crocin (50, 100 and 200 mg/kg), safranal (0.25, 0.5 and 1 mg/kg) and the aqueous extract (2.5, 5 and 10 mg/kg) were administered intravenously in different groups of normotensive and hypertensive animals and their effects on mean arterial blood pressure (MABP) and heart rate (HR) were evaluated. The aqueous extract of saffron stigma, safranal and crocin reduced the MABP in normotensive and hypertensive anaesthetized rats in a dose‐dependent manner. For example, administrations of 10 mg/kg of aqueous extract, 1 mg/kg of safranal and 200 mg/kg of crocin caused 60 ± 8.7, 50 ± 5.2 and 51 ± 3.8 mmHg reductions in MABP, respectively. It can be concluded that the aqueous extract of saffron stigma has hypotensive properties which appear to be attributable, in part, to the actions of two major constitutes of this plant, crocin and safranal. It seems that safranal is more important than crocin for lowering down blood pressure of rats. Copyright © 2009 John Wiley & Sons, Ltd.     

Relaxant effects of the neutral extract of the leaves of Bidens pilosa Linn on isolated rat vascular smooth muscle

The long-lasting antihypertensive effect of a neutral extract of Bidens pilosa has been suggested to be due to vasodilation. The present work was undertaken to assess this hypothesis. The vasorelaxant effect of a neutral extract (NBp) of the leaves of B. pilosa was evaluated in vitro on isolated rat aorta contracted with KCl or norepinephrine. NBp induced a concentration-dependent vasorelaxation of the rat aorta precontracted with KCl (60 mM) by 25%-105% at the respective concentrations of 0.25-1.5 mg/mL. The maximal concentration of 1.5 mg/mL provoked 88% relaxation of norepinephrine-induced contractions. There were no significant differences between the effects of the extract on the aorta strips with or without endothelium. In the presence of indomethacin or pyrilamine maleate, the relaxant response induced by the plant extract was significantly inhibited at the lower concentrations. The plant extract was able to reduce the aorta resting tone, inhibit the KCl-induced contractions (90% at 1.5 mg/mL) and the CaCl2-induced contractions by 95% at a concentration of 0.75 mg/mL. These results demonstrate the vasodilating properties of the neutral extract of Bidens pilosa and indicate that it may act as a calcium antagonist.     

Antihypertensive, vasorelaxant and inotropic effects of an ethanolic extract of the roots of Saururus chinensis

AIM OF THE STUDY: The present study was performed to evaluate the cardiovascular effects of ethanolic extract of the roots of Saururus chinensis (EERSC) in rats. MATERIALS AND METHODS: The effects of EERSC on the vascular responses of isolated rat aorta, the cardiac functions in isolated rat heart, and the antihypertensive effects in spontaneously hypertensive rats (SHRs) were evaluated. RESULTS: In isolated rat aortic preparations, EERSC exhibited a potent vasorelaxant effect with EC(50) value of 9.1 microg/ml. This relaxation was significantly inhibited by denudation of endothelial layer or by pretreatment with N(G)-nitro-l-arginine methyl ester. In addition, the raising extracellular K(+) (45 mM), or pretreatment with tetraethylammonium (10 mM) significantly inhibited EERSC-induced vasorelaxation in endothelium-denuded aortic rings. In isolated rat hearts, EERSC significantly reduced cardiac functions such as left ventricle pressure and heart rate. In an antihypertensive study with SHRs, long-term oral administrations of EERSC decreased blood pressure of SHRs (approximately 20 mmHg). CONCLUSIONS: These results suggest that chronic treatment with EERSC exerts an antihypertensive effect in SHRs, and its direct vasorelaxant properties and negative inotropic actions may contribute to reduce the elevated blood pressure.     

Vasoconstrictor and cardiotonic actions of Haloxylon recurvum extract

Intravenous administration of an ethanolic extract of Haloxylon recurvum (30–300 μg/kg) caused a rise in arterial blood pressure in normotensive anaesthetized rats. Pretreatment of animals with phentolamine (1 mg/kg) abolished the vasoconstrictor response of the plant extract in a way similar to that of norepinephrine (NE). In an isolated rabbit aorta preparation, both plant extract and NE produced contractile responses which were blocked by phentolamine (0.3 μg/mL). In isolated guinea-pig atria, the plant extract caused positive inotropic and chronotropic responses similar to that of NE and was blocked by propranolol (0.3 μg/mL). These results suggest that vasoconstrictor and cardiac stimulatory effects of the plant extract are mediated through mechanisms similar to those of NE (stimulation of α-adrenergic receptors in the blood vessels and cardiac β-receptors respectively) and hence this plant contains sympathomimetic constituent(s).     

Cardiovascular effects of an extract from the roots of a shrub Elaeophorbia drupifera.

A crude extract was prepared from the roots of E. drupifera. Lethality studies in mice showed a dose-mortality relationship with an LD(50) of 145 mg/kg mice i.p. The extract (2-260 microg/kg. i.v.) was tested in graded doses on the blood pressure and heart rate of urethane anaesthetized rats. The results showed that the extract decreased both the blood pressure and heart rate in a dose-dependent manner. The maximum decrease in blood pressure (control, 78.3 +/- 6. 5 mmHg) and heart rate (control, 120.2 +/- 5.5 beats/min) produced by the extract was about 46.2% and 41.7% (% control), respectively. Blocking the beta adrenoceptors with propranolol (0.5 microg/kg. i.v. ) did not prevent the action of the extract on both the blood pressure and heart rate, suggesting that the extract was acting at a different site. This view was supported by the observation that the extract significantly depressed the increase in blood pressure and heart rate caused by bilateral occlusion of the common carotid artery. Also, the extract was found to prolong ACh-induced hypotension in the rats. In animals pretreated with atropine sulphate (0.2 mg/kg. i.v), the extract was less effective in depressing the blood pressure. However, this atropine antagonism was surmounted by raising the concentration of the extract. Finally, in vitro studies using isolated arterial strips revealed that the extract also had a relaxant effect on vascular smooth muscle. This relaxant effect was dose-dependent and was attenuated and/or abolished by phentolamine (0.5 microg/mL). Also, the extract relaxed aortic strips precontracted with noradrenaline (1 x 10(-7) mol L(-1)) but failed to relax strips precontracted with KCl (50 mmol/L). We conclude that the crude extract from the roots of E. drupifera probably contains acetylcholine-like agent(s) which interferes with the cholinergic mechanism, as well as catecholamine-like agent(s) exhibiting mainly alpha-adrenoceptor activity.     

Presence of blood‐pressure lowering and spasmolytic constituents in Buddleja crispa

This aim of this study was to investigate the crude extract of Buddleja crispa (Bc.Cr) and its active constituent(s) for their antihypertensive and antispasmodic activities. The Bc.Cr caused a dose‐dependent (3–10 mg/kg) fall in mean arterial pressure in rats under anesthesia. In rabbit aorta preparations, Bc.Cr (0.03–1 mg/mL) caused inhibition of high K⁺ (80 mM) precontractions. The Bc.Cr (0.03–1 mg/mL) also inhibited spontaneous and high K⁺ precontractions in rabbit jejunum preparations, suggestive of calcium channel blocking (CCB) activity. CCB activity was further confirmed when pretreatment of the tissues with Bc.Cr (0.03–0.10 mg/mL) caused a rightward shift in Ca⁺⁺ concentration response curves, similar to verapamil. Among the pure compounds, BdI‐H3 was more potent against the high K⁺ than spontaneous contractions and was around eight times more potent than Bc.Cr against the spontaneous contractions while the other two compounds, BdI‐2 and BH‐3 were inactive. Activity‐directed fractionation revealed that the hexane fraction was more potent against K⁺ precontractions. These data indicate that Bc.Cr possesses a blood‐pressure lowering effect, mediated possibly through CCB, though additional mechanism(s) cannot be ruled out. Among the pure compounds, Bdl‐H3 is likely to be the active compound involved in the spasmolytic and possibly BP lowering effect of the parent crude extract. Copyright © 2008 John Wiley & Sons, Ltd.     

Studies on the hypoglycaemic activity of Punica granatum seed in streptozotocin induced diabetic rats.

The hypoglycaemic activity of Punica granatum Linn. (Family Punicaceae) seed extract on rats made diabetic by streptozotocin (STZ) was investigated. The methanol extract of the seed at doses of 300 and 600 mg/kg, and chlorpropamide 200 mg/kg was administered to STZ diabetic rats. The seed extract (150, 300 and 600 mg/kg, orally) caused a significant reduction of blood glucose levels in STZ induced diabetic rats by 47% and 52%, respectively, at the end of 12 h.     

Cardiovascular effects of oblongine chloride,an alkaloid from Leontice leontopetalum,in the anaesthetized guinea-pig

The effects of (?)oblongine chloride, a quaternary alkaloid from Leontice leontopetalum on blood pressure, heart rate and blood flow of the anaesthetized guinea-pig were studied. At doses ranging from 0.5 mg/kg to 30 mg/kg, i.v., oblongine chloride caused a dose-dependent reduction of systolic and diastolic blood pressure. These doses were associated with an increase in heart rate. Propranolol (5 mg/kg) failed to block the effects of oblongine chloride on systolic and diastolic blood pressure but significantly reduced the increase in heart rate observed with low doses (0.5–6 mg/kg) of oblongine chloride. In doses ranging from 0.05 mg/kg to 0.5 mg/kg, oblongine chloride caused a small increase in blood flow. Larger doses (1.5, 4.5, 15 and 30 mg/kg) caused an initial decrease followed by an increase of blood flow. The net effect of cumulative doses was an increase in blood flow over the control value. These observations suggest that oblongine chloride may have potential haemodynamic effects and that these effects are not mediated by β-adrenergic receptor stimulation.     

Studies on the antihypertensive, antispasmodic, bronchodilator and hepatoprotective activities of the Carum copticum seed extract

This study describes the antihypertensive, antispasmodic, bronchodilator and hepatoprotective activities of the aqueous-methanolic extract of Carum copticum Benth. seeds (CSE) to rationalize some of its traditional uses. CSE (3-100 mg/kg) caused a dose-dependent fall in arterial blood pressure in anaesthetized rats. In isolated rabbit aorta and jejunum preparations, CSE (0.1-3.0 mg/ml) caused an inhibitory effect on the K+-induced contractions. The calcium channel blocking (CCB) effect was confirmed when CSE shifted the Ca2+ dose-response curves (DRCs) to right similar to verapamil. In isolated guinea-pig tracheal preparations, it caused inhibition of carbachol and K+-induced bronchoconstriction at 0.1-1.0 mg/ml as well as shifted the dose-response curves (DRCs) of carbachol and histamine to the right with suppression of maximum response suggestive of non-specific bronchodilator effect mediated possibly through CCB. Pretreatment of rats with CSE (500 mg/kg orally for 2 days at 12 h intervals) prevented paracetamol (640 mg/kg) and CCl4 (150 ml/kg)-induced rise in serum alkaline phosphatase (ALP) and aminotransferases (AST and ALT). The same dose of CSE was able to prevent the CCl4-induced prolongation in pentobarbital-induced sleeping time in mice confirming its hepatoprotectivity. These results indicate the presence of calcium antagonist(s) in Carum copticum seeds and thus provides sound mechanistic basis for some of their folkloric uses.     

Antihypertensive and vasodilator effects of methanolic and aqueous extracts of Tribulus terrestris in rats

The effects of methanolic and aqueous extracts of Tribulus terrestris on rat blood pressure (BP) and the perfused mesenteric vascular bed were investigated. The extracts dose-dependently reduced BP in spontaneously hypertensive rats (SHRs) with the aqueous fraction being more potent than the methanolic fraction at all doses tested. In vitro, the methanolic but not aqueous extract produced a dose-dependent increase in perfusion pressure of the mesenteric vascular bed. When perfusion pressure was raised with phenylephrine (10(-5) M), the aqueous extract produced a dose-dependent reduction in perfusion pressure at all doses. A low dose of the methanolic extract produced a vasoconstrictor effect while higher doses produced dose-dependent reduction in perfusion pressure. L-NAME (10(-4) M) significantly reduced but did not abolish vasodilation induced by the extracts. Vasodilator responses to aqueous and methanolic fractions were significantly reduced in preparations where perfusion pressure was raised with KCl (60 mM). A combination of KCl and L-NAME abolished the vasodilator responses induced by the extracts. It was concluded that methanolic and aqueous extracts of Tribulus terrestris possess significant antihypertensive activity in spontaneously hypertensive rats. The antihypertensive effects appeared to result from a direct arterial smooth muscle relaxation possibly involving nitric oxide release and membrane hyperpolarization.     

Anti-hypertensive effects of the methanol/methylene chloride stem bark extract of Mammea africana in l-NAME-induced hypertensive rats

AIM OF THE STUDY: The methanol/methylene chloride (CH(3)OH/CH(2)Cl(2)) extract from the stem bark of Mammea africana was showed to possess vasodilating effect in the presence and the absence of N(omega)-nitro-l-arginine methyl ester (l-NAME). The present study was designed to evaluate the effects of the methanol/methylene chloride from the stem bark of Mammea africana. MATERIALS AND METHODS: The extract (200 mg/(kg day)) was administered orally in rats treated concurrently with l-NAME (40 mg/(kg day)). l-Arginine (100 mg/(kg day)) and captopril (20 mg/(kg day))were used as positive controls. Bodyweight, systolic arterial blood pressure and heart rate were measured weekly throughout the experiment period (28 days). At the end of treatment, animals were killed and the cardiac mass index evaluated. The aorta was used to evaluate the endothelium-dependant relaxation to carbachol. The aorta contraction induced by noradrenalin was also examined and expressed as a percentage of that induced by KCl. RESULTS: The extract neither affected the body weight nor the heart rate. The extract as captopril completely prevented the development of arterial hypertension. Both the substances failed to restore the endothelium-dependent vascular relaxation and increased the vascular contraction to norepinephrine in relation to KCl contraction. They also significantly reduced the left ventricular hypertrophy induced by l-NAME. CONCLUSION: These findings are in agreement with the traditional use of Mammea africana in the treatment of arterial hypertension and indicate that it may have a beneficial effect in patients with NO deficiency but will be unable to improve their endothelium-dependent vasorelaxation.     

Antihypertensive activities of the aqueous extract of Kalanchoe pinnata (Crassulaceae) in high salt-loaded rats

Ethnopharmacological relevance

The leaves of Kalanchoe pinnata (Crassulaceae) are used in Cameroon folk medicine to manage many diseases such as cardiovascular dysfunctions. In this work, we aimed to evaluate the activities of aqueous leaf extract of Kalanchoe pinnata on the blood pressure of normotensive rat (NTR) and salt hypertensive rats (SHR), as well as its antioxidant properties.

Materials and methods

Hypertension was induced in rats by oral administration of 18% NaCl for 4 weeks. For the preventive study, three groups of rats received 18% NaCl solution and the plant extract at 25 mg/kg/day, 50 mg/kg/day or 100 mg/kg/day by gavage. Two positive control groups received 18% NaCl solution and either spironolactone (0.71 mg/kg/day) or eupressyl (0.86 mg/kg/day) by gavage for 4 weeks. At the end of this experimental period, systolic arterial pressure (SAP), diastolic arterial pressure (DAP) and heart rate (HR) were measured by the invasive method. Some oxidative stress biomarkers (reduced glutathione (GSH), superoxide dismutase (SOD), nitric monoxide (NO) were evaluated in heart, aorta, liver and kidney. NO level was indirectly evaluated by measuring nitrite concentration.

Results

Kalanchoe pinnata extract prevented significantly the increase of systolic and diastolic arterial pressures in high salt-loaded rats (SHR). In SHR, concomitant administration of Kalanchoe pinnata at 25, 50 and 100 mg/kg/day significantly prevented the increase in blood pressure by 32%, 24% and 47% (for SAP); 35%, 33% and 56% (for DAP), respectively. No significant change was recorded in heart rate of those rats. The plant extract improved antioxidant status in various organs, but more potently in aorta. Thus, antioxidant and modulatory effects of Kalanchoe pinnata at the vasculature might be of preponderant contribution to its overall antihypertensive activity.

Conclusion

The work demonstrated that the concomitant administration of high-salt and the aqueous extract of Kalanchoe pinnata elicits prevention of salt-induced hypertension in rat. This antihypertensive activity is associated with an improvement of antioxidant status. Overall, results justify and support the use of Kalanchoe pinnata as antihypertensive medicine.     

Hypotensive and vasorelaxant effects of the procyanidin fraction from Guazuma ulmifolia bark in normotensive and hypertensive rats

THE AIM OF THE STUDY: was to investigate the in vivo and in vitro cardiovascular activity of a procyanidin fraction (PCF) obtained from acetone extract of Guazuma ulmifolia bark which has traditionally been used as an antihypertensive agent. RESULTS: 10 mg/kg PCF doses orally administered to sugar-fed hypertensive rats decreased both the systolic arterial pressure and the heart rate, whereas the same doses intravenously administered induced arterial hypotension which was attenuated by NG-nitro-L-arginine methylester (L-NAME 31 mg/kg) pretreatment. In these experiments we employed carbachol as a positive control test. The PCF reduced the contraction induced by norepinephrine (1x10(-7) M) in isolated aortic rings of normotensive (IC50=35.3+/-12.4 ng/mL) and sugar-fed hypertensive (IC50=101.3+/-57.2 ng/mL) rats. This relaxant activity was inhibited by either vascular endothelium removal or L-NAME (30 microM) pretreatment, while indomethacin (10 microM) or atropine (10 microM) had no effect. Preliminary analysis of the PCF by HPLC-DAD-MS and FAB+ mass spectrometry allowed the detection of the main components such as the complex of procyanidin oligomers consisting mainly of tetramers and trimers. CONCLUSIONS: Guazuma ulmifolia bark possesses long-lasting antihypertensive and vasorelaxing properties linked to the endothelium related factors, where nitric oxide is involved.     

Effect of a diterpenoid from Salvia cinnabarina on arterial blood pressure in rats

The effect of a diterpenoid isolated from Salvia cinnabarina, 3,4-seicosopimar-4(18),7,15-triene-3-oic acid (SCB), on arterial blood pressure was evaluated in anaesthetized rats. Male Wistar rats, anaesthetized with urethane (sol. 10% p/v; 10 mL/kg), underwent surgery for continuous monitoring of arterial blood pressure. After preliminary experiments to evaluate the dose response (3, 10 and 30 mg/kg i.v.) of SCB, a dose of 3 mg/kg was chosen for all successive experiments. On different groups of rats treated with the ganglion-blocking agent chlorisondamine (2.5 mg/kg i.p.) the effect of SCB (3 mg/kg i.v.) was evaluated before and following an infusion of the nitric oxide synthase inhibitor L-NAME (0.3 mg/kg/min i.v.). Intravenous administration of SCB at doses of 3, 10 and 30 mg/kg led to a fall in mean arterial blood pressure (MABP) of 14.75 +/- 1.44 mmHg, 36.60 +/- 31.40 mmHg and 31.40 +/- 6.28 mmHg, respectively (n = 4-5), that was not modified by treatment of the rat with chlorisondamine nor with L-NAME. The results demonstrate a hypotensive effect of SCB - due to a peripheral mechanism but independent of endothelial nitric oxide release.     

Studies on antihypertensive and antispasmodic activities of methanol extract of Acacia nilotica pods

A methanol extract of Acacia nilotica pods (AN) caused a dose-dependent (3-30 mg/kg) fall in arterial blood pressure. Treatment of animals with atropine abolished the vasodilator response of acetylcholine (ACh), whereas the antihypertensive effect of the plant extract remained unaltered. Phentolamine (an alpha-adrenergic blocker) abolished the vasoconstrictor effect of norepinephrine (NE), whereas pretreatment of the animal with AN, did not modify the NE response. These results indicate that the antihypertensive effect of plant extract is independent of muscarinic receptor stimulation or adrenoceptor blockade. In the in vitro studies, AN produced a dose-dependent (0.3-3.0 mg/mL) inhibitory effect on force and rate of spontaneous contractions in guinea-pig paired atria. Similarly, it inhibited the spontaneous contraction of rabbit jejunum in a concentration-dependent (0.1-3.0 mg/mL) manner. AN also inhibited K(+)-induced contractions in rabbit jejunum at a similar concentration range, which suggests that the antispasmodic action of AN is mediated through calcium channel blockade, and this may also be responsible for the blood pressure lowering effect of AN, observed in the in vivo studies.     

From the vasodilator and hypotensive effects of an extract fraction from Agelanthus dodoneifolius (DC) Danser (Loranthaceae) to the active compound dodoneine

Aim of the study

Effects of the different fractions obtained by partition of ethanolic extract (EE) of Agelanthus dodoneifolius through column chromatography were investigated on rat blood pressure and aortic relaxation and compared to those observed in the presence of crude EE.

Materials and methods

The acute hypotensive activity of EE, fractions and dodoneine, administrated intravenously, was evaluated in anaesthetized rats using the invasive method of blood pressure recording. Bioassay-guided fractionation using rat aorta pre-contracted by norepinephrine to monitor the relaxant activity led to the isolation of dodoneine.

Results

In normotensive rats, injection of EE (0.01-10 mg/kg) produced a dose-dependent decrease in both systolic and diastolic blood pressure without any significant change in heart rate. In a similar way, the EE (0.001-3 mg/mL) caused relaxation of rat pre-contracted aorta in a concentration-dependent manner. Fractionation of the EE afforded 14 fractions, F1-F14, that were tested on rat precontracted aortic rings. At the concentration level of 1 mg/mL, a maximum relaxation effect was observed for fractions F2-F5. F4 was the most effective to elicit a concentration-dependent relaxation effect with an ED₅₀ = 160 ± 1.1 μg/mL (n = 5) and to decreased systolic and diastolic control pressure by 56.9% and 81.6% respectively. F4 contains most of the dihydropyranone dodoneine, with 93% of the sample mass. Dodoneine separated from this fraction was also able to decrease both systolic and diastolic arterial pressure by 32.5% and 38.7% at 100 μg/kg, respectively.

Conclusion

For the first time, this study demonstrates the hypotensive property of the dodoneine present in Agelanthus dodoneifolius.     

Hypotensive and spasmolytic activities of ethanolic extract of Capparis cartilaginea

An ethanolic extract of Capparis cartilaginea (CC) at a dose of 1–10 mg/kg caused a dose-dependent fall in blood pressure and heart rate in anaesthetized rats. These effects were not blocked by atropine (1 mg/kg) and pretreatment with CC did not alter the pressor response to norepinephrine, indicating that the cardiovascular effects of CC are independent of cholinergic or adrenergic receptor involvement. In spontaneously beating guinea-pig atria, CC induced a concentration-dependent (0.1–1 mg/mL) decrease in force and rate of atrial contractions. In rabbit thoracic aorta, CC caused inhibition of norepinephrine or K⁺-induced contractions. In guinea-pig ileum, CC (1 mg/mL) inhibited submaximal contractions induced by acetylcholine, histamine or 5-HT. Spontaneous contractions of rat uterus were also abolished when CC was added to the tissue bath at similar concentrations. These results suggest that the direct relaxant action of CC on myocardium and blood vessels may be responsible for its hypotensive and bradycardiac effects observed in the in vivo studies. Moreover, CC exhibits general spasmolytic activity in different smooth muscle preparations.