Saffron (Crocus sativus) aqueous extract and its constituent crocin reduces stress-induced anorexia in mice

In the present study, the effects of an ethanol and aqueous extract of saffron Crocus sativus and its constituents safranal and crocin on the stress‐induced reduction in food intake, weight gain and anorexic time in mice were investigated. Male albino mice (20–25 g) were irregularly exposed to a trial of electroshock stress for 7 days. Then, the anorexic time as well as the animal's food intake and weight were recorded. In addition, blood samples were obtained on days 1 and 7 for corticosterone determination. Intraperitoneal (i.p.) administration of the aqueous but not the ethanol extract (10, 50 and 100 mg/kg) significantly reduced the anorexic time. The results were similar for crocin (1, 5 and 10 mg/kg; i.p.). In addition, a reduction in weight gain was observed in the controls as well as in the groups that received alcohol extract or safranal. However, this was not observed in animals treated with aqueous extract or crocin. The plasma corticosterone level did not increase in the aqueous extract and crocin treated animals. It can be concluded that the saffron aqueous extract and its constituent crocin reduce side effects of electroshock stress in mice. Copyright © 2011 John Wiley & Sons, Ltd.     

Anxiolytic and hypnotic effect of Crocus sativus aqueous extract and its constituents,crocin and safranal,in mice

Saffron stigma (Crocus sativus L.) is used for insomnia and anxiety in traditional medicine. In this study, the anxiolytic and hypnotic effects of saffron aqueous extract and its constituents, crocin and safranal, were studied in mice. Agents were administered intraperitoneally in mice before the experiments for the evaluation of hypnotic activity (induced by sodium pentobarbital, 30 mg/kg, i.p.), anxiolytic activity (elevated plus maze test), locomotor activity (open field test) and motor coordination (Rotarod test). The aqueous extract reduced the locomotor activity dose dependently. At low doses, saffron showed a significant increase in the time on the open arms of the maze. When using the Rotarod method, the aqueous extract showed considerable effect on motor coordination of the mice. In the hypnotic test, only a dose of 0.56 g/kg of saffron increased the total sleep. Crocin showed no anxiolytic, hypnotic or myorelaxation effects. Safranal, in higher doses, 0.15 and 0.35 mL/kg, showed anxiolytic effects. Safranal increased the total sleep time dose dependently. This constituent at lower doses (0.05 and 0.15 mL/kg) decreased some locomotion activity parameters. Safranal demonstrated no effects on motor coordination. The results showed that saffron aqueous extract and safranal have anxiolytic and hypnotic effects. Copyright © 2009 John Wiley & Sons, Ltd.     

Effect of crocus sativus L. (saffron) stigma and its constituents,crocin and safranal,on morphine withdrawal syndrome in mice

Crocus sativus L. has been shown to interact with the opioid system. Thus, the effects of aqueous and ethanolic extracts of stigma and its constituents were evaluated on morphine‐withdrawal syndrome in mice. Dependence was induced using subcutaneous (s.c.) injections of morphine for 3 days. On day 4, morphine was injected 0.5 h prior the interaperitoneal (i.p.) injections of the extracts, crocin, safranal, clonidine (0.3 mg/kg) or normal saline. Naloxone was injected (5 mg/kg i.p.) 2 h after the final dose of morphine and the number of episodes of jumping during 30 mm was considered as the intensity of the withdrawal syndrome. Clonidine, the aqueous and ethanolic extracts of saffron reduced the jumping activity. Safranal was injected (s.c.) 30 mm prior and 1 and 2 h after the injection of morphine. It potentiated some signs of withdrawal syndrome. The aqueous extract decreased the movement in all of the doses (80, 160, 320 mg/kg) and the ethanolic extract decreased it in the dose of 800 mg/kg in open field test. But crocin and the dose of 400 mg/kg ethanolic extract showed no effect on activity in this test. It is concluded that the extracts and crocin may have interaction with the opioid system to reduce withdrawal syndrome. Copyright © 2009 John Wiley & Sons, Ltd.     

Effects of saffron (Crocus sativus L.) and its active constituent, crocin, on recognition and spatial memory after chronic cerebral hypoperfusion in rats

Cerebral ischemia produces brain damage and related behavioral deficits such as memory. In this study, a rat model of chronic cerebral hypoperfusion was used to determine whether saffron extract and crocin, which are potent antioxidants and free radical scavengers, can reduce vascular cognitive impairment. Male adult Wistar rats were administered different doses of an aqueous solution of crocin or hydroalcohol extract of saffron intraperitoneally (i.p.) 5 days after permanent occlusion of the common carotid arteries. Spatial learning and memory were assessed in training trials, 7–11 days after common carotid artery ligation using the Morris water maze. The results showed that the escape latency time was significantly reduced from 24.64 s in the control group to 8.77 and 10.47 s by crocin (25 mg/kg) and saffron extract (250 mg/kg). The traveled distance to find the platform was also changed from 772 cm in the control group to 251 and 294 cm in the crocin (25 mg/kg) and saffron extract (250 mg/kg) groups. The percentages of time spent in the target quadrant, in comparison with the control group (24.16%), increased to 34.25% in the crocin (25 mg/kg) and 34.85% in the saffron extract (250 mg/kg) group. This study suggests that saffron extract and crocin improve spatial cognitive abilities following chronic cerebral hypoperfusion and that these effects may be related to the antioxidant effects of these compounds. Copyright © 2011 John Wiley & Sons, Ltd.     

Hypotensive activity and toxicology of constituents from root bark of Polyalthia longifolia var. pendula

A defatted extract of Polyalthia longifolia var. pendula root bark (PRB) in 50% methanol showed a significant ability to reduce blood pressure. It caused a 22% and 47% fall in mean arterial blood pressure (MABP) in rats at doses of 3 mg/kg and 30 mg/kg, respectively. Compounds purified from this extract include kolavenic acid (3), clerodane (1) and its isomer (2), liriodenine (4), lysicamine (5) and bisclerodane imide (6) and its isomer (7). Of these, only kolavenic acid produced a 22% fall in MABP, at a dose of 30 mg/kg. PRB showed a decrease in blood pressure of normotensive and egg yolk induced hypertensive rats. The LD50 of PRB was determined as 100 mg/kg in mice.     

Saponins from the leaves of Musanga cecropioïdes (cecropiaceae) constitute a possible source of potent hypotensive principles

The aqueous leaf extract and saponins extracted from the aqueous leaf extract of Musanga cecropioïdes exhibited potent hypotensive effects in both normotensive and hypertensive rats. The intravenous administration (direct invasive blood pressure study technique) of 15–30 mg/kg body weight of the aqueous leaf extract produced a fall in blood pressure (BP) of 35%–57% in hypertensive rats and 27% in normotensive individuals. This BP fall was followed by a transient rise, while saponins extracted from the aqueous extract of the leaves of MC produced a fall in BP of 55% in hypertensive and 30% in normotensive rats. In the indirect (tail cuff) blood pressure study, the effect was also dose-dependent. The oral administration of 300 mg/kg body weight of the aqueous leaf extract produced a BP fall of over 30% by 12 h following extract administration while the saponins (0.02–0.8 mg/kg body weight) produced a fall of 10% to 53%.     

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.     

Germinated Buckwheat extract decreases blood pressure and nitrotyrosine immunoreactivity in aortic endothelial cells in spontaneously hypertensive rats

Thee present study analysed the quantification of rutin in raw buckwheat extract (RBE) and germinated buckwheat extract (GBE) by high performance liquid chromatography (HPLC), and examined changes in body weight, systolic blood pressure (SBP) and nitrotyrosine (a marker for peroxynitrite formation) immunoreactivity in aortic endothelial cells in spontaneously hypertensive rats (SHRs) and normotensive Wistar‐Kyoto (WKY) rats after treatment with RBE and GBE for 5 weeks. In the HPLC study, RBE and GBE contained a mean content of rutin of 1.52 ± 0.21 and 2.92 ± 0.88 mg/g, respectively. In the 600 mg/kg GBE‐treated group, SBP was lower than that in the 600 mg/kg RBE‐treated group. The treatment with RBE and/or GBE significantly reduced oxidative damage in aortic endothelial cells by lowering nitrotyrosine immunoreactivity. These results suggest that GBE has an antihypertensive effect and may protect arterial endothelial cells from oxidative stress. Copyright © 2009 John Wiley & Sons, Ltd.     

Antihypertensive effect of Lepidium sativum L. in spontaneously hypertensive rats

The antihypertensive and diuretic effects of the aqueous extract of Lepidium sativum L. (LS) were studied both in normotensive (WKY) and spontaneously hypertensive rats (SHR). Daily oral administration of the aqueous LS extract (20mg/kg for 3 weeks) exhibited a significant decrease in blood pressure (p<0.01) in SHR rats while in WKY rats, no significant change was noted during the period of treatment. The systolic blood pressure was decreased significantly from the 7th day (p<0.05) to the end of treatment (p<0.01) in SHR rats. The aqueous LS extract enhanced significantly the water excretion in WKY rats (p<0.001) but no statistically significant change was observed in SHR rats. Furthermore, oral administration of aqueous LS extract at a dose of 20mg/kg produced a significant increase of urinary excretion of sodium (p<0.05), potassium (p<0.01) and chlorides (p<0.01) in WKY rats. In spontaneously hypertensive rats, the aqueous LS extract administration induced a significant increase of urinary elimination of sodium (p<0.01), potassium (p<0.001) and chlorides (p<0.001). Glomerular filtration rate showed a significant increase after oral administration of LS in normal rats (p<0.001) while in SHR rats, no significant change was noted during the period of treatment. Furthermore, no significant changes were noted on heart rate after LS treatment in SHR as well as in WKY rats. Our results suggest that daily oral administration of aqueous LS extract for 3 weeks exhibited antihypertensive and diuretic activities.     

Experimental and clinical antihypertensive activity of Matricaria chamomilla extracts and their angiotensin‐converting enzyme inhibitory activity

Three different extracts of Matricaria chamomilla L. were evaluated for their antihypertensive activity, these extracts were total alcohol extract (Extract 1), oil extracted (Extract 2), and water lifted after oil extraction (Extract 3). Quantitative and Qualitative analyses were carried out for all extracts. The 3 extracts were proved to be safe for human use. A single oral administration of the plant extracts (200 mg/kg) decreases both systolic and diastolic blood pressure of normotensive rats after 1, 1.5, and 2 hr. Furthermore, groups treated with the evaluated extracts (100 & 200 mg/kg) or Captopril (20 mg/kg) showed a significant reduction in the elevated blood pressure and heart rate. Extract 3 showed the most antihypertensive activity. Serum biochemical parameters and lipid profile levels of treated groups were improved in comparison with induced‐hypertensive untreated rats. In evaluation of oxidative damage parameters Glutathione and superoxide dismutase ( SOD ) in some organs, the investigated extracts or captopril restored the amount of reduced Glutathione in tissues in addition to an increase in the activity of the SOD after a significant depletion of SOD activity. In the clinical study, there was a significant dose dependent decrease in Systolic blood pressure, Diastolic blood pressure, and heart rate compared with their basal values in both normotensive and hypertensive human volunteers after oral administration of Matricaria chamomilla beverages.     

Blood pressure lowering effect of the aqueous extract of the stem of Ipomoea acanthocarpa (convolvulaceae) in spontaneously and salt-loaded hypertensive rats

Spontaneously hypertensive (SHR) and salt-loaded hypertensive rats (SLHR) were submitted to a daily treatment by gavage of 2 mL/100 g body weight of the aqueous extract of the stem of Ipomoea acanthocarpa (30 mg/mL stock solution). A fall in blood pressure of nearly 13% was observed after two successive administrations of the aqueous extract. After 14 days of treatment, the blood pressure fell by more than 30±8%. The hypotensive effect might be due to a direct vascular smooth muscle effect or to its already observed high diuretic effects or might be acting by some other mechanism.     

Radical scavenging activity of Crocus sativus L. extract and its bioactive constituents

Radical scavenging activity is involved in aging processes, antiinflammatory, anticancer and wound healing activity. Hence, in the present study the DPPH radical scavenging activity of a natural product that possesses biological properties, an extract of Crocus sativus L. (saffron), grown in Crocos, Kozani (Greece), and some of its bioactive constituents (crocin, safranal) was studied.It was shown that a methanol extract of Crocus sativus exhibited high antioxidant activity, although it contains several active and inactive constituents. In trying to approximate a structure-activity relationship, two bioactive constituents of saffron extract were tested, namely crocin and safranal. Crocin showed high radical scavenging activity (50% and 65% for 500 and 1,000 ppm solution in methanol, respectively), followed by safranal (34% for 500 ppm solution). All the tested samples showed high radical scavenging activity, probably due to the ability to donate a hydrogen atom to the DPPH radical.Thus, saffron grown in Greece can be used promisingly in functional foods, drinks with antioxidant activity, in pharmaceutical and cosmetic preparations for their antioxidant activity and probably for their antiaging activity. Saffron can also be used internally in the form of powder or other pharmacotechnical formulae as a food supplement with antioxidant properties.     

西红花有效成分的神经药理学研究进展

名贵中药材西红花用于治疗多种疾病,历史悠久.西红花主要活性成分有西红花酸、西红花索、西红花醛等.近年来研究发现:西红花有效成分在中枢神经系统具有广泛的生物学活性,对脑缺血再灌注损伤、失眠、焦虑、抑郁症、学习记忆障碍、帕金森氏病、老年性痴呆等多种神经精神性疾病具有改善作用.文章综述西红花及活性成分的神经药理学研究进展.     

Hypotensive effect of Laurelia sempervirens (Monimiaceae) on normotensive rats

The leaves of Laurelia sempervirens (Monimiaceae), an endemic Chilean tree known as ‘Laurel’, were used by the Mapuche Amerindians for treating headache and as a diuretic. Intravenous administration of a hydroalcoholic L. sempervirens extract to rats, elicited a hypotensive response of ?27.0%±2.0% in the mean blood pressure of normotensive animals at a dose of 5 mg crude extract ± kg body weight. Bioassay-guided isolation of the active ‘Laurel’ metabolites led to the alkaloid laurotetanine as the main hypotensive principle of L. sempervirens leaves. At 1 mg/kg body weight, laurotetanine produced a hypotensive response of ?29.0%±2.1% in the mean blood pressure of normotensive rats, with a duration of 2 min, both comparable to those elicited by the crude extract at 5 mg/kg. In the acute oral toxicity study, ‘Laurel’ proved to be a very low toxicity crude drug at doses up to 3 g crude extract/kg body weight. The data obtained support the use of L. sempervirens in Mapuche traditional medicine.     

Fraxinus excelsior L. evokes a hypotensive action in normal and spontaneously hypertensive rats

The hypotensive effect of an aqueous extract of Fraxinus excelsior L. was investigated in both normotensive (WKY) and spontaneously hypertensive rats (SHR). Daily oral administration of Fraxinus excelsior (20 mg/kg) aqueous extract for 3 weeks produced a significant decrease in systolic blood pressure (SBP) with variation coefficient (Delta%) of 13.5% in SHR (p<0.01) and 9% in WKY rats (p<0.05). The aqueous extract of Fraxinus excelsior significantly enhanced the urination in both SHR (p<0.05 compared to control) and WKY (p<0.05 compared to control). Irbesartan (Avapro), an angiotensin II antagonist, was used as reference drug. Furthermore, oral administration of aqueous Fraxinus excelsior extract at a dose of 20 mg/kg produced a significant increase in urinary excretion of sodium (p<0.01 compared to control), potassium (p<0.001 compared to control) and chlorides (p<0.01) in SHR rats. In normal rats, the aqueous Fraxinus excelsior extract administration induced a significant increase of the urinary elimination of sodium (p<0.05 compared to control), chlorides (p<0.01 compared to control) and potassium (p<0.01 versus control). While there were no significant changes in heart rate (HR) after Fraxinus excelsior treatment in both SHR and WKY rats, glomerular filtration rate (GFR) showed a significant increase in SH rats (p<0.001) after Fraxinus excelsior treatment. These results suggest that oral administration of aqueous extract of Fraxinus excelsior exhibited hypotensive and diuretic actions.     

Avicenna's (Ibn Sina) the Canon of Medicine and Saffron (Crocus sativus): A Review

In this review, we introduce the traditional uses of saffron and its pharmacological activities as described by either Avicenna in Book II, Canon of Medicine (al‐Qanun fi al‐tib) or from recent scientific studies. Modern pharmacological findings on saffron are compared with those mentioned in Avicenna's monograph. A computerized search of published articles was performed using MEDLINE, Scopus and Web of Science databases as well as local references. The search terms used were saffron, Crocus sativus, crocin, crocetin, safranal, picrocrocin, Avicenna and ‘Ibn Sina’. Avicenna described various uses of saffron, including its use as an antidepressant, hypnotic, anti‐inflammatory, hepatoprotective, bronchodilatory, aphrodisiac, inducer of labour, emmenagogue and others. Most of these effects have been studied in modern pharmacology and are well documented. The pharmacological data on saffron and its constituents, including crocin, crocetin and safranal, are similar to those found in Avicenna's monograph. This review indicates that the evaluation of plants based on ethnobotanical information and ancient books may be a valuable approach to finding new biological activities and compounds. Copyright © 2012 John Wiley & Sons, Ltd.     

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.     

Hypotensive and diuretic effect of Equisetum bogotense and Fuchsia magellanica and micropropagation of E. bogotense

Equisetum bogotense (Equisetaceae) and Fuchsia magellanica (Onagraceae) were used by the Mapuche Amerindians as diuretics. Intravenous administration of hydroalcoholic extracts to rats elicited a hypotensive response of ?29.0% ±4.5% and ?24.2% ±0.5% respectively in the mean blood pressure of normotensive animals at a dose of 5 mg crude extract/kg body weight. The activity was found to be related with polar compounds. For Fuchsia, the active principles are related to tannins. A single oral dose of 500 mg/kg body weight Equisetum extract produced a significant increase (p < 0.05) in the urine output in rats, while in Fuchsia a reduction in diuresis was observed. The diuretic effect of the Equisetum extract was weak compared with hydrochlorothiazide at 25 mg/kg body weight. The data presented support the use of E. bogotense in Chilean traditional medicine. A micropropagation method for E. bogotense was established by culturing shoot tips in Murashige-Skoog medium with macro and micronutrients diluted 4-fold and containing 0.1 mg/L thiamine, 100 mg/L myoinositol, 1.0 mg/L NAA and 0.1 mg/L BAP.     

Pharmacological studies on hypotensive, diuretic and vasodilator activities of chrysin glucoside from Calycotome villosa in rats

The present study was undertaken in normotensive anaesthetized male rats that received a continuous perfusion of a chrysin glucoside isolated from the flowers and leaves of Calycotome villosa subsp intermedia at a dose of 2.5 mg/kg, or furosemide (control diuretic) at a dose of 0.5 mg/kg. Compared with the control rats receiving NaCl (0.9%), the urine flow, glomerular filtration and electrolyte excretion (Na+, K+) increased significantly in rats treated with chrysin glucoside (p < 0.001). A similar effect was observed in the rats perfused with furosemide. Intravenous injections of bolus doses (1-3 mg/kg) of the chrysin glucoside to anaesthetized rats elicited an immediate and dose-dependent decrease in mean arterial blood pressure (MABP). Pretreatment of the rats with the nitric oxide synthase inhibitor, l-NOArg (10 mg/kg), reduced partially, but significantly (p < 0.01), the maximal decrease in MABP elicited by chrysin glucoside. In the rat isolated aorta preparation, chrysin glucoside (10-100 microm) inhibited in a concentration-dependent manner the noradrenaline (1 microm) induced contractions (IC(50) = 52 microm). This relaxant activity of chrysin glucoside was significantly reduced by incubation of the endothelium-intact rings with l-NOArg (100 microm), (80 +/- 4.7% vs 48 +/- 5.06% in the absence of L-NOArg). In conclusion, these results demonstrate a diuretic and hypotensive action of a chrysin glucoside from Calycotome villosa in anaesthetized rats and indicating an action on renal function, and an active vascular relaxation mediated partially through nitric oxide release.     

Effects of three different doses of a fruit extract of Terminalia chebula on metabolic components of metabolic syndrome,in a rat model

There is documented evidence of the use of Terminalia chebula for various ailments in the Ayurvedic literature. The extract has been shown to possess glucose lowering activity and to improve insulin sensitivity in animal models of type 2 diabetes mellitus. The present study was carried out to study the dose response relationship of this extract in a rat model of metabolic syndrome. Six groups of rats were fed a high fructose diet (HFD) for a period of 20 days to induce metabolic syndrome. Three doses of fruit extract of T. chebula 50, 100 and 200 mg/kg were administered orally and pioglitazone 2.7 mg/kg was used as a positive control. Blood samples were collected at days 0, 20 and 40 from the tail vein. Systolic blood pressure (SBP) was measured using the tail cuff method and an oral glucose tolerance test (OGTT) was done on the day of blood collection. Administration of HFD for 20 days significantly increased fasting blood glucose (FBG), SBP and the area under the curve of OGTT. On day 40 the FBG in the 50, 100 and 200 mg/kg group was 97.33 ± 5.82 (NS), 86.83 ± 5.08 (p = 0.038) and 85.67 ± 6.74 (p = 0.15), respectively. These results show that the fruit extract of T. chebula exerts a significant and dose‐dependent glucose lowering effect in the rat model of metabolic syndrome. Copyright © 2009 John Wiley & Sons, Ltd.