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.     

Antispasmodic and hypotensive effects of Ferula asafoetida gum extract

The effects of Ferula asafoetida gum extract on the contractile responses of the isolated guinea-pig ileum induced by acetylcholine, histamine and KCl, and on the mean arterial blood pressure of rat were investigated. In the presence of extract (3 mg/ml), the average amplitude of spontaneous contractions of the isolated guinea-pig ileum was decreased to 54 +/- 7% of control. Exposure of the precontracted ileum by acetylcholine (10 microM) to Ferula asafoetida gum extract caused relaxation in a concentration-dependent manner. Similar relaxatory effect of the extract was observed on the precontracted ileum by histamine (10 microM) and KCl (28 mM). However, when the preparations were preincubated with indomethacin (100 nM) and different antagonists, such as propranolol (1 microM), atropine (100 nM), chlorpheniramine (25 nM) then were contracted with KCl, exposure to the extract (3 mg/ml) did not cause any relaxation. Furthermore, Ferula asafoetida gum extract (0.3-2.2 mg/100g body weight) significantly reduced the mean arterial blood pressure in anaesthetised rats. It might be concluded that the relaxant compounds in Ferula asafoetida gum extract interfere with a variety of muscarinic, adrenergic and histaminic receptor activities or with the mobilisation of calcium ions required for smooth muscle contraction non-specificly.     

The pharmacological effects of an aqueous extract from Acacia nilotica seeds

An aqueous extract of the seed of Acacia nilotica was investigated for its pharmacological profile. On the isolated guinea-pig ileum, the extract displayed sustained dose-related contractile activity. The contractions which were reduced by hexamethonium, promethazine or atropine were completely abolished by nifedipine. The intravenous (i.v.) administration of the extract (11, 22, 44, 55 microg/kg) to anaesthetized cats produced a dose-related significant elevation of blood pressure. The mechanisms of the spasmogenic and vasoconstrictor actions of the extract have not been determined, however, the results suggest the involvement of calcium.     

Pharmacology of an Indian-snuff obtained from Amazonian Maquira sclerophylla

The powdered bark of Maquira sclerophylla is consumed as snuff in north Brazil. Both the crude and the purified hydrosoluble extract (WP) injected i.p. in the dose range of 0.05-0.5 g/kg induced hyperexcitability, tremors, motor incoordination, ataxia, quietness and muscle relaxation in rats. The effects were progressive, dose-related and reversed after 30 min. Anesthetized rats, guinea-pigs and dogs injected with the purified extract (10-50 mg/kg, i.v.) showed a biphasic change of carotid blood pressure. The early and transient hypotension was blocked by atropine but not by vagotomy: the secondary hypertension was long lasting and sustained for over 30 min. The hypertension was shortened but not blocked after ganglionic blockade or reserpine treatment. Either pithing or alpha receptor blockade with yohimbine reduced both effects of the extract. Guinea-pigs and dogs were more responsive than rats and died by heart arrest. Incubation of WP (20 micrograms/ml) increased both the rate and force of contraction of isolated guinea-pig right atria by 2 and 5 times, respectively. Propranolol (4 micrograms/ml) blocked the chronotropic effect but did not decrease the inotropic effect. In electrically driven guinea-pig left atria, WP (10 micrograms/ml) increased the force of contraction by 80% and the maximum rate of force development by 60%, but did not change the time to peak tension, the time to 50% relaxation, or the rate of relaxation. These cardiovascular effects resemble those of digitalis-like drugs. Cardenolides were detected in WP by phytochemical screening.     

UpI: in vivo studies involving the potent cardiac stimulant and haemolysin from the sea anemone Urticina piscivora

UpI is a basic protein purified from the crude extract of the sea anemone Urticina piscivora. As a potent positive inotrope, it increases the force of contraction of the left atria of the heart of rat and guinea-pig with little or no increase in heart rate in vitro. It also elicited ileal contractions similar to acetylcholine and such action was inhibited by atropine. Intravenous administration (direct invasive blood pressure studies) of UpI (0.1–20 μg/kg body weight) produced a fall in blood pressure (BP) in normotensive rats. This fall in BP was further reduced by atropine (1 mg/kg) but not completely abolished. Postmortem findings of the internal organs revealed severe haemorrhage, oedema and necrosis to the lung and skin but to a lesser extent on the kidney and liver. No histological alteration was observed in the brain or heart. © 1997 John Wiley & Sons, Ltd.     

葶苈子水提物对狗左心室功能的作用

iv葶苈子水提物0.2ml/kg(含生药2g/ml),能增加犬的左心室心肌收缩性和泵血功能,并能增加冠脉流量,与iv异丙肾上腺素10μg/kg的作用相似,但葶苈子水提物对心率、动静脉氧分压差及动静脉氧溶解度无明显影响。说明葶苈子水提物具有显著强心和增加冠脉流量的作用且不增加心肌耗氧量。     

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.     

Effects of an n-butanol extract from the stem of Tinospora crispa on blood pressure and heart rate in anesthetized rats

Ethnopharmacological relevance

Tinospora crispa has been used in folkloric medicine for control of blood pressure, as an antipyretic, for cooling down the body temperature and for maintaining good health.

Aim of the study

To investigate the effects and mechanisms of action of an n-butanol extract from the stems of Tinospora crispa (T. crispa extract) on blood pressure and heart rate in anesthetized rats.

Materials and methods

Air-dried stems of T. crispa were extracted with water, followed by partitioned extract with chloroform, ethyl acetate, and finally by n-butanol. The n-butanol soluble part was evaporated under reduced pressure and lyophilization to obtain a crude dried powder (T. crispa extract). The effects and mechanisms of the T. crispa extract on blood pressure and heart rate were studied in anesthetized normal and reserpinized rats in vivo in the presence of different antagonists.

Results

T. crispa extract (1-100 mg/kg, i.v.) caused a decrease in mean arterial blood pressure (MAP) and this effect was inhibited by propranolol, phentolamine, atenolol and/or the β₂-antagonist ICI-118,551, but not by atropine or hexamethonium. In reserpinized rats, the T. crispa extract had a dual effect: reduction in hypotensive activity, followed by a small increase in blood pressure. The decrease in MAP in reserpinized rat was slightly potentiated by phentolamine, but inhibited by propranolol or ICI-118,551 only if atenolol and phentolamine were also present. The increase in MAP was potentiated by propranolol and ICI-118,551, but was inhibited by phentolamine. The T. crispa extract had a dual effect on heart rate in the normal rat: a small transient decrease, followed by an increase in heart rate. The positive chronotropic effect of T. crispa extract was inhibited by propranolol, phentolamine and atenolol, but not by ICI-118,551, atropine or hexamethonium. Reserpine potentiated the positive chronotropic effect of the T. crispa extract and this effect was inhibited by propranolol, atenolol and ICI-118,551, but not by phentolamine.

Conclusions

From these results we suggest that T. crispa extract possesses at least three different cardiovascular-active components that act directly via (1) β₂-adrenergic receptors to cause a decrease in blood pressure, and β₁- and β₂-adrenergic receptors to cause an increase in heart rate, (2) α-adrenergic receptors to cause an increase in blood pressure and heart rate, and (3) a non-adrenergic and non-cholinergic pathway to cause a decrease in MAP and heart rate. These findings provide scientific support for the tradition of using this plant to modify the actions of the human cardiovascular system.     

Isolation of hypotensive compounds from Solanum sisymbriifolium Lam

The crude hydroalcoholic root extract (CRE) of Solanum sisymbriifolium Lam. has formerly been shown to have hypotensive activity both in normo-and hypertensive rats. Hypotensive activity-guided fractionation of the CRE was performed in anaesthetized normotensive rats, which led to the isolation of the active principles. The intravenous (i.v.) and intraperitoneal (i.p.) values of the CRE in mice were found to be, respectively, 343 and 451 mg/kg, and 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 piloerection 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 transit was found using 0.1 g/kg, whereas at doses of 0.5 and 1 g/kg, no significant 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 isolated from the butanolic fraction induced a significant decrease of the blood pressure, HR, amplitude of the ECG 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 compounds were not influenced by pretreatment with atropine and propranolol; and the pressor response to noradrenaline was not affected by any of them which suggests that neither a direct muscarinic activity, β-adrenoceptor activation nor decrease of sympathetic vascular tone (sympatholitic activity) are probably involved in the mechanism of hypotension. The present study shows that the CRE of S. sisymbriifolium contains at least two hypotensive compounds whose characterization is under way.     

Cardiovascular effects of the South American medicinal plant Cecropia pachystachya (ambay) on rats

Cecropia pachystachya is used in South America for relieving cough and asthma. In Argentina it is known as "ambay" and grows in the neotropical forests (Ntr C.p.) and in temperate hilly regions (Tp C.p.). To evaluate their cardiovascular profile, the effect of extracts obtained from plants growing in the neotropical region as well as in temperate areas were compared by i.v. administration in normotensive rats. The following parameters were measured: blood pressure (BP) and heart rate (HR). The hypotensive effect was stronger for Ntr C.p., which aqueous extract decreased BP at doses between 90 and 300 mg lyophilised/kg until 46.2 +/- 12% of basal. The extract of Tp C.p. reduced BP to 86.1 +/- 11% of basal (p < 0.05 respect to Ntr C.p.) at 180 mg/kg, but increased HR at 90 and 180 mg/kg (until 133.6 +/- 10.8% of basal, p < 0.05) and produced death by respiratory paralysis at 320 mg/kg (about 3g dry leaves/kg). The hypotensive effects, but not the chronotropic ones, were attenuated by pretreatment with reserpine (5 mg/kg). The plant extracts had not diuretic activity by oral administration in conscious rats, nor produced vasodilation of perfused hindquarters arterial bed precontracted with high-[K] or 100 microM phenylephrine. The results suggest that neotropical ambay is more hypotensive than the one from the temperate hilly region. When it reaches plasma, it could produce hypotension (by central blockade of sympathic innervation of vessels) and tachycardia (by central cholinergic inhibition of heart), although it happens at doses higher than the oral ethnotherapeutic (about 340 mg dried leaves/kg).     

Anti-inflammatory and smooth muscle relaxant activities of the hydroalcoholic extract and chemical constituents from Amburana cearensis A C Smith

Amburana cearensis A. C. Smith, Fagaceae, is a medicinal plant commonly known as 'cumaru' and used in Northeast Brazil for the treatment of respiratory tract diseases. In the present work, we investigated the anti-inflammatory and smooth muscle relaxant activities of the hydroalcoholic extract (HAE), coumarin (Coum) and fl avonoid fraction (FF) isolated from the trunk barks of Amburana cearensis A. C. Smith. It was shown that HAE (200 and 400 mg/kg), Coum (20 and 40 mg/kg) and FF (40 mg/kg), administered orally, significantly inhibited both leukocyte and neutrophil migrations, in the carrageenan or N-formyl-methyl-leucyl-phenylalanine (fMLP)-induced migration in rat peritoneal cavity. The increase in cutaneous vascular permeability induced by serotonin in rats was significantly blocked by HAE (150 mg/kg, i.p.), Coum (5 mg/kg, i.p.) and FF (20 mg/kg, i.p.). However, only HAE blocked the histamine effect on Evans blue extravasation. In the guinea-pig trachea precontracted with carbachol (0.3 microM), histamine (0.1 microM) or KCl (0.1 M), the HAE, Coum and FF evoked a concentration-dependent relaxation in the presence of the three agonists. HAE (100-800 microg/ml) and Coum (4-32 microg/ml) also caused significant relaxation of the rat vas deferens previously contracted with adrenaline, acetylcholine or barium chloride. In addition, HAE, Coum and FF inhibited the histamine and serotonin-induced increase of cutaneous vascular permeability in rats.     

Hypotensive effect of crude root extract of Solanum sisymbriifolium (Solanaceae) in normo- and hypertensive rats

The hypotensive effect of the crude hydroalcoholic extract from root of Solanum sisymbriifolium Lam. (Solanaceae) was investigated both in normotensive and hypertensive rats. The intravenous administration of the extract (50 and 100 mg/kg) produced a significant decrease in blood pressure in anaesthetized hypertensive (adrenal regeneration hypertension + deoxycorticosterone acetate (ARH + DOCA)) rats. Oral administration of the extract (10, 50, 100 and 250 mg/kg) also produced a dose-dependent hypotensive effect in conscious hypertensive animals. In anaesthetized normotensive rats, the extract (50 and 100 mg/kg, i.v.) also induced hypotension in a dose-dependent manner. Lastly, no significant effect on blood pressure was produced by the extract when administered orally (10, 50, 100, 250, 500 and 1000 mg/kg) to conscious normotensive rats.     

Evaluation of in vivo antihypertensive and in vitro vasodepressor activities of the leaf extract of Syzygium guineense (Willd) D.C

The aim of this work was to evaluate the antihypertensive activity of the hydroalcohol extract of the leaves of Syzygium guineense (Willd) D.C. (Myrtaceae) in a 1-kidney-1-clip rat model and its vasorelaxant effect on isolated aorta. The extract reduced blood pressure in a dose and time dependent fashion. Following 3 days of treatment, single oral daily doses of 50, 100 and 150 mg/kg caused an overall reduction (p < 0.05) of systolic blood pressure by 6.9, 34.0 and 40.8 mmHg, respectively. The diastolic blood pressure was, however, significantly reduced (p < 0.05) by 100 mg/kg (10.3 mmHg) and 150 mg/kg (18.4 mmHg) doses only. The mean blood pressure was reduced by 5.0, 18.3 and 25.9 mmHg by the respective doses. The extract also caused a dose-dependent relaxation of aorta precontracted with KCl at a concentration of 5-70 mg/mL, with a maximum relaxation of 56.22% achieved at 70 mg/mL concentration. The relaxation mechanism was found to be independent of the endothelium system, muscarinic receptors, histamine receptors, ATP dependent K(+) channels, cyclooxygenase enzymes and cGMP/NO pathway. The findings suggest that the extract had an antihypertensive effect most likely caused by dilation of the blood vessels, a confirmation for the folkloric use of the plant.     

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.     

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.     

Autonomic nervous system mediates the cardiovascular effects of Rhodiola sacra radix in rats

ETHNOPHARMACOLOGICAL RELEVANCE: Rhodiola sacra (Crassulaceae) exhibits cardiovascular bioactivities and is used in Tibetan medicine for promoting circulation and preventing hypertension. However, the underlying mechanisms of its cardiovascular effects are poorly understood. AIM OF THE STUDY: The aim of this study was therefore to evaluate the cardiovascular activity of water-soluble fraction (WtF) and n-butanol-soluble fraction (BtF) of Rhodiola sacra radix and to explore its mechanism of action in propofol anesthetized Sprague-Dawley rats. MATERIALS AND METHODS: The changes of blood pressure, heart rate and cardiac contractility after systemic administration of the extracts (10-75mg/kg) were examined for at least 40min. Different antagonists were used to evaluate the mechanisms of cardiovascular effects of the extracts. RESULTS: Intravenous injection of the WtF (10, 25, 35, 50 or 75mg/kg) exhibited dose-dependent hypotension and increases in heart rate and cardiac contractility. In contrast, mild alterations in the same cardiovascular parameters were detected only at high dose (75mg/kg) BtF. The WtF-induced hypotensive, positive inotropic and chronotropic effects were significantly abolished by pretreatment with hexamethonium (30mg/kg, i.v.) or reserpine (5mg/kg, i.v.), whereas the hypotensive, but not the positive inotropic or chronotropic effect was potentiated by captopril (2.5mg/kg, i.v.). Pretreatment with methylatropine (1mg/kg, i.v.), on the other hand, reversed the positive inotropic and chronotropic but not the hypotensive effects of WtF. The WtF-induced cardiovascular responses were not affected in rats pretreated with N(G)-nitro-l-arginine methyl ester (20mg/kg, i.v.). CONCLUSIONS: We conclude that systemic administration of the WtF of Rhodiola sacra radix elicited a potent hypotensive effect that was mediated by the withdrawal of sympathetic vasomotor tone and interaction with the circulatory angiotensin system. The positive inotropic and chronotropic effects of WtF may result from a direct vagal inhibition on the heart.     

C-fiber-evoked autonomic cardiovascular effects after injection of Piper betle inflorescence extracts

Piper betle inflorescence extracts contain eugenol (6.2%) and safrole (78.9%). Intravenous injections of water extracts of P. betle inflorescence (PBE), eugenol, and safrole in rats induced hypotensive and bradycardiac effects, whereas both intraarterial and intrathecal injections of PBE, eugenol and safrole resulted in hypotensive and tachycardiac effects. Moreover, the effects of intravenous injections of PBE were reversed or inhibited by the pretreatment with bilateral vagotomy, atropine (1 mg/kg, i.p.) and capsaicin (100 mg/kg, s.c.). Effects of intraarterial injections of PBE on blood pressure were inhibited by the pretreatment with substance P (SP) antagonist (1 nmol, i.t.) and clonidine (2.5 μg, i.t.), while heart rate was only inhibited by the pretreatment with SP antagonist (1 nmol, i.t.). In addition, the tachycardia resulting from intrathecal injections of PBE was inhibited by pretreatment with propranolol (0.3 mg/kg, i.v.). Eugenol and safrole induced the same pattern on blood pressure and heart rate changes as PBE in rats after various treatments. This report suggests that acute administration of betel inflorescence extracts by different routes may activate C-fiber-evoked parasympathetic and sympathetic cardiovascular reflexes in rats.     

Activation of nitric oxide signaling pathway mediates hypotensive effect of Muntingia calabura L. (Tiliaceae) leaf extract

The cardiovascular effect of the crude methanol extract from the leaf of Muntingia calabura L. (Tiliaceae) was investigated in the anesthetized rats. The crude methanol extract was sequentially fractionated to obtain the water-soluble extract (WSE). Intravenous administration of the WSE (10, 25, 50, 75 or 100 mg/kg) produced an initial followed by a delayed decrease in systemic arterial pressure (SAP) in a dose-dependent manner. The M. calabura-induced initial hypotension lasted for 10 min and the delayed depressor effect commenced after 90 min and lasted for at least 180 min post-injection. The same treatment, on the other hand, had no appreciable effect on heart rate (HR) or the blood gas/electrolytes concentrations. Both the initial and delayed hypotensive effects of WSE (50 mg/kg, i.v.) were significantly blocked by pre-treatment with a nonselective nitric oxide (NO) synthase (NOS) inhibitor, N(G)-nitro-L-arginine methyl ester ((L)-NAME, 0.325 mg/kg/min for 5 min) or a soluble guanylate cyclase (sGC) inhibitor, 1H-[1,2,4]oxadiazole[4,3-alpha]quinoxalin-1-one (ODQ, 0.2 mg/kg/min for 5 min). Moreover, whereas the initial depressor effect of WSE was inhibited by pre-treatment with a selective endothelial NOS (eNOS) inhibitor, N5-(1-Iminoethyl)-L-ornithine ((L)-NIO, 1 mg/kg/min for 5 min), the delayed hypotension was attenuated by a selective inducible NOS (iNOS) inhibitor, S-methylisothiourea (SMT, 0.5 mg/kg/min for 5 min). Administration of WSE also produced an elevation in plasma nitrate/nitrite concentration, as well as an increase in the expression of iNOS protein in the heart and thoracic aorta. These results indicate that WSE from the leaf of M. calabura elicited both a transient and delayed hypotensive effect via the production of NO. Furthermore, activation of NO/sGC/cGMP signaling pathway may mediate the M. calabura-induced hypotension.     

Vasorelaxant effect of stilbenes from rhizome extract of rhubarb (Rheum undulatum) on the contractility of rat aorta

The vascular relaxant effect of the rhizome extract of Rheum undulatum was evaluated with isolated rat thoracic aorta preparations. The methanol extract of the rhizome induced a concentration-dependent relaxation of aortic preparations precontracted with 0.3 microm phenylephrine (EC50 value: 5.8 microg/mL). The activity-guided fractionation of the extract led to the isolation of seven hydroxystilbene components as active principles, i.e. piceatannol, resveratrol, desoxyrhapontigenin, rhapontigenin, piceid, rhaponticin and epsilon-viniferin. Of these, piceatannol, a tetrahydroxystilbene, exhibited the most potent vascular relaxant effect in rat aortic preparations (EC50 value 2.4 microm). The vasorelaxant effect of piceatannol on endothelium-intact aorta rings was diminished completely by the removal of functional endothelium or by pretreatment of the aortic tissues with N(G)-nitro-l-arginine methyl ester. These results suggest that piceatannol may be the major mediator responsible for the vasorelaxing properties of the rhizome extract of Rheum undulatum and the vasorelaxant effects of the piceatannol may be mediated via endothelium-dependent nitric oxide signaling pathway.     

Hypotensive Activity of Lannea coromandelica Bark Extract

An ethanol extract of Lannea coromandelica bark (ELC) showed hypotensive activity in anaesthetized dogs and rats. On intravenous administration (i.v.) at a dose range of 5–100 mg/kg in dogs and 1–25 mg/kg in rats it produced a mild to marked decrease in the arterial blood pressure in a dose dependent manner. The effect did not alter after cholingergic, histaminergic, adrenergic and ganglion receptor blockade. The hypotension was also unchanged in vagotomized and eviscerated dogs, whereas there was a slight increase in hypotension in the spinal preparation. It produced dose related decreases in heart rate, without any effect on respiratory rate.