Constituents of the essential oil of Achillea wilhelmsii from Iran

Constituents of the essential oil of Achillea wilhelmsii L. growing wild in Kerman-Iran were studied by TLC, GC, and GC/MS methods. The main components of the monoterpene fraction of the oil were camphor, borneol, linalool, 1,8-cineole, chrysanthenol acetate, and carvacrol. The percentage of the identified sesquiterpenoid components was relatively high and constituted 29% of the oil.     

Protective effects of Iranian Achillea wilhelmsii essential oil on acetaminophen-induced oxidative stress in rat liver

Abstract

Context: Achillea wilhelmsii C. Koch (Asteraceae) is widely used in Iranian traditional medicine.

Objective: This in vivo study evaluates the hepatoprotective role of Iranian A. wilhelmsii oils against acetaminophen-induced oxidative damages in rats.

Materials and methods: The animals were divided into five groups: in negative control and control groups, the DMSO and 500?mg/kg acetaminophen were i.p. injected, respectively. In treatment groups, 100 and 200?mg/kg oils and 10?mg/kg BHT were given i.p. immediately after acetaminophen administration. Then, the hepatic oxidative/antioxidant parameters such as lipid peroxidation (LP), glutathione (GSH), superoxide dismutase (SOD), catalase (CAT), and ferric reducing ability of plasma (FRAP) were measured in time intervals (2, 4, 8, 16, and 24?h) after administrations confirmed by histophatological consideration at 24?h.

Results: The results indicated that acetaminophen caused a significant elevation in SOD activity (8–24?h) and LP and FRAP levels (4?h) paralleled with significant decline in GSH level (4 and 8?h). The apparent oxidative injury was associated with evident hepatic necrosis confirmed in histological examination. The presences of A. wilhelmsii oils (100 and 200?mg/kg) with acetaminophen mitigated significantly the rise in SOD, LP, and FRAP levels and restored the GSH compared with the group treated with acetaminophen. These were confirmed by histological examination indicating the hepatic necrosis reversal by the oils.

Discussion and conclusion: It can be concluded that concomitant administration of A. wilhelmsii oils with acetaminophen may be useful in reversing the drug hepatotoxicity.     

Investigation of optimal extraction,antioxidant, and antimicrobial activities of Achillea biebersteinii and A. wilhelmsii

Objective: Achillea species are endowed with multiple biological activities including antioxidant properties. However, no study has yet investigated the impact of extraction method and pH on the biological activities of these plants. The present study aimed to investigate the antioxidant and antimicrobial effects of methanol extracts from the aerial parts of the species Achillea biebersteinii Afan and Achillea wilhelmsii C. Koch (Asteraceae). In addition, the impact of extraction method and pH on these biological activities was evaluated.

Materials and methods: Methanol extracts of A. biebersteinii and A. wilhelmsii were prepared using classical maceration and high-intensity ultrasound methods. Ultrasound-assisted extraction was performed at three different pH values: 5.7, 6.3 and 6.9.

Results: Total phenolic compounds (range: 20.16–108.54 vs. 17.18–59.61 mg gallic acid equivalent/g sample in A. biebersteinii and A. wilhelmsii, respectively), total flavonoids (range: 8.33–12.97 vs. 7.79–9.41 mg catechin equivalent/g sample), 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (IC₅₀: 40.63–346.34 vs. 84.02–462.41) and reducing power (IC₅₀: 504.44–4406.67 vs. 1710.00–5501.67) were significantly higher in A. biebersteinii vs. A. wilhelmsii and ultrasound-assisted vs. classical maceration extracts of both species. The aforementioned items were higher at pH = 6.3, followed by pHs of 6.9 and 5.7, respectively. Overall, A. biebersteinii extracts were more active against all of the tested microorganisms than A. wilhelmsii. Sensitivities of Gram-positive bacteria were higher for both Achillea extracts than the Gram-negative bacteria. No observable inhibitory activity was found from different extracts against Aspergillus niger.

Conclusion: The findings of the present study suggest that methanol extracts of A. biebersteinii and A. wilhelmsii possess antioxidant and antimicrobial activity, being higher in the former. Ultrasound-assisted extraction and pH of 6.3 have significant augmenting impact on the total phenolic and flavonoid content as well as antioxidant activities of both species.     

Investigation of optimal extraction, antioxidant, and antimicrobial activities of Achillea biebersteinii and A. wilhelmsii

Objective: Achillea species are endowed with multiple biological activities including antioxidant properties. However, no study has yet investigated the impact of extraction method and pH on the biological activities of these plants. The present study aimed to investigate the antioxidant and antimicrobial effects of methanol extracts from the aerial parts of the species Achillea biebersteinii Afan and Achillea wilhelmsii C. Koch (Asteraceae). In addition, the impact of extraction method and pH on these biological activities was evaluated. Materials and methods: Methanol extracts of A. biebersteinii and A. wilhelmsii were prepared using classical maceration and high-intensity ultrasound methods. Ultrasound-assisted extraction was performed at three different pH values: 5.7, 6.3 and 6.9. Results: Total phenolic compounds (range: 20.16-108.54 vs. 17.18-59.61 mg gallic acid equivalent/g sample in A. biebersteinii and A. wilhelmsii, respectively), total flavonoids (range: 8.33-12.97 vs. 7.79-9.41 mg catechin equivalent/g sample), 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (IC(50): 40.63-346.34 vs. 84.02-462.41) and reducing power (IC(50): 504.44-4406.67 vs. 1710.00-5501.67) were significantly higher in A. biebersteinii vs. A. wilhelmsii and ultrasound-assisted vs. classical maceration extracts of both species. The aforementioned items were higher at pH = 6.3, followed by pHs of 6.9 and 5.7, respectively. Overall, A. biebersteinii extracts were more active against all of the tested microorganisms than A. wilhelmsii. Sensitivities of Gram-positive bacteria were higher for both Achillea extracts than the Gram-negative bacteria. No observable inhibitory activity was found from different extracts against Aspergillus niger. Conclusion: The findings of the present study suggest that methanol extracts of A. biebersteinii and A. wilhelmsii possess antioxidant and antimicrobial activity, being higher in the former. Ultrasound-assisted extraction and pH of 6.3 have significant augmenting impact on the total phenolic and flavonoid content as well as antioxidant activities of both species.     

乙酰泽泻醇B与洛伐他汀对大鼠降血脂作用的比较

目的 观察乙酰泽泻醇B和洛伐他汀对高血脂模型大鼠的影响.方法 给予大鼠高脂饲料15 d,造成高血脂大鼠模型,测定灌服乙酰泽泻醇B和洛伐他汀后高脂模型大鼠甘油三酯(TG)、总胆固醇(TC)、高密度脂蛋白(HDL-C)、低密度脂蛋白(LDL-C)等指标.结果 乙酰泽泻醇B能极显著地降低大鼠血清中的TC、LDL-C.结论 乙...     

槲皮素的降压作用及其机制研究

槲皮素是一种天然多酚黄酮类化合物,富含于苹果、洋葱、浆果等食物中,与心血管疾病负相关。最近动物和人类试验均表明,槲皮可以降低高血压个体的血压,机制可能涉及抗氧化应激、抑制血管紧张素转化酶(ACE)活性,以内皮依赖性和非依赖性方式改善血管内皮功能等。本综述将系统阐述槲皮素的降压作用及其相关机制。     

Antihypertensive and renal effects of nicardipine

Both the acute blood pressure lowering and renal effects of the calcium antagonist nicardipine and those after 1 week's treatment were investigated in 10 normotensive volunteers and in 10 patients with mild to moderate essential hypertension. After 1 week of placebo, nicardipine was administered orally for 1 week (20 mg three times daily), Investigations, done on the first and last day of nicardipine treatment were compared with those on the last day of placebo. During water loading, nicardipine increased urinary volume and urinary excretion of sodium significantly after 1 week nicardipine treatment. In the normotensive group the natriuretic effect was caused by a decrease of fractional proximal and distal reabsorption of sodium. In the hypertensive group the natriuresis was achieved mainly by an increase of the rate of glomerular filtration (GFR) and also by a slight distal effect. Our results show that nicardipine had natriuretic effects. There were trends suggesting that the renal effects may differ between patients with essential hypertension and normotensive volunteers, but the findings might also be related to differences in age between the groups.     

美托洛尔治疗高血压病的疗效及其耐受性

原发性高血压患者425例(男252,女173;年龄60±s12a)采用美托洛尔100mg,po,每晨1次,4wk为一个疗程。总有效率82.4％,治疗2wk后血压继续下降,心率并不继续减慢。不良反应主要为心率减慢后的症状及神经系症状,停药率6.4％。60a以上的患者总有效率及停药率与中、青年患者无明显区别。故美托洛尔同样适用于老年人。     

Antihypertensive and metabolic effects of tiapamil

Tiapamil, a new calcium antagonist, was evaluated for its antihypertensive and metabolic effects in a long-term (58 weeks) drug trial in 20 adult outpatient mild to moderately hypertensive subjects. Baseline systolic and diastolic blood pressure dropped after initiation of treatment and was significantly reduced after 4 weeks of treatment, further improving until the termination of the study. There was no impairment of renal and hepatic functions. Electrolytes, plasma aldosterone, plasma renin activity, as well as plasma lipids were not significantly altered during the course of therapy. Fasting blood sugar determinations and oral glucose tolerance test showed significant reductions from the baseline level as a result of the drug treatment. In conclusion, tiapamil is a metabolically safe and effective antihypertensive drug for long-term use.     

Antihyperglycemic and antihyperlipidemic effects of Salvadora persica in streptozotocin-induced diabetic rats

Context: Many synthetic antidiabetic components show toxic and/or mutagenic effects. Hence, attention has been given to naturally occurring antidiabetic components. Identification of effective antidiabetic components from plants origin is an ideal strategy for new drug development. The fresh root, bark, and leaves of Salvadora persica L. (Salvadoraceae) have been used in folk medicine for the treatment of a wide range of medical problems such as cough, asthma, scurvy, piles, rheumatism, leprosy, and gonorrhea disorders.

Objective: The S. persica root extract was investigated for the reduction of the risk of diabetes in diabetic rats.

Material and methods: The hydro-alcoholic root extract, 200 and 400?mg/kg, was fed to streptozotocin-induced diabetic rats for 21?d. Blood serum glucose, lipid profile, body weight, and food intake were monitored at 0, 7, 14, and 21?d after induction of diabetes.

Results: S. persica hydro-alcoholic root extract was not toxic at doses up to 1200?mg/kg. Significant reduction of blood glucose and lipid profile in diabetic rats treated with 400?mg/kg hydro-alcoholic root extract after 21?d versus diabetic control and glibenclamide-treated rats. The glibenclamide and root extract-treated group’s peak values of blood glucose significantly decreased from 281.50 to 106?mg/dL and 285.50 to 150.25?mg/dL, respectively. Hence, in this study, observations showed that root hydro-alcoholic reduced the blood glucose level in diabetic rats but values did not return to normal controls.

Conclusion: The research suggests that the root extract was significantly effective when compared with control and standard in the treatment of hyperlipidemia and hyperglycemia in diabetic rats. Therefore, it may be beneficial to diabetic patients.     

姜黄素与辛伐他汀降血脂及抗氧化作用比较

目的:以高脂血症大鼠为模型比较姜黄素、姜黄素固体分散体、辛伐他汀降血脂及抗氧化作用。方法:雄性SD大鼠灌胃给予高脂肪乳剂制备高脂血症大鼠模型。造模的同时,给予姜黄素、姜黄素固体分散体、辛伐他汀,连续给药6周后测定总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)、丙二醛(MDA)的含量,超氧化物歧化酶(SOD)的活性。结果:姜黄素与姜黄素固体分散体在降低血清中甘油三酯(TG)的作用明显优于辛伐他汀(P<0.05);而辛伐他汀降低血清中总胆固醇的作用明显优于姜黄素(P<0.01);姜黄素与姜黄素固体分散体能提高血清及肝匀浆中SOD活性,降低MDA含量,姜黄素抗氧化作用明显优于辛伐他汀(P<0.01);姜黄素固体分散体的降血脂及抗氧化能力明显优于姜黄素(P<0.01)。结论:姜黄素固体分散体对高脂血症模型大鼠具有降低血脂及抗氧化的双重作用。     

Antihypertensive and noradrenaline-depleting effects of guanethidine metabolites

The antihypertensive and myocardial noradrenaline-depleting activities of the three identified guanethidine metabolites were compared with those of guanethidine itself. Metabolite A (guanethidine-N-oxide) and Metabolite B [2-(6-carboxylamino)ethylguanidine] both showed approximately 1/30th of the antihypertensive effect of guanethidine in rats. Metabolite A, but not Metabolite B, caused a depletion of cardiac noradrenaline stores. The intensity of this effect was between 1/10th and 1/30th that of guanethidine. Metabolite C [(6-carboxyhexyl)-2-iminoimidazolidine] was inactive on both parameters. [³H]Noradrenaline uptake into isolated bovine nerve granules was not impaired by either guanethidine or its metabolites. It is concluded that the antihypertensive and myocardial noradrenaline depleting effects of guanethidine are produced by the unchanged drug rather than by one of the identified metabolites.     

Antihypertensive effects of the flavonoid quercetin

The blood pressure lowering effect of a fruit and vegetable-rich diet is a necessary dietary lifestyle measure now included the guidelines for the management of arterial hypertension. Furthermore, flavonoids represent a major class of plant polyphenolics. The present review addresses the antihypertensive effect of quercetin, one of the most abundant flavonoids present in fruits and vegetables, and probably the best studied flavonoid because of its high biological activity. Quercetin has been shown to induce a progressive, dose-dependent and sustained reduction in blood pressure when given chronically in several rat models of hypertension, including spontaneously hypertensive rats, L-NAME-treated rats, DOCA-salt hypertensive rats, two-kidney one-clip Goldblatt rats, rats with aortic constriction and Dahl salt-sensitive hypertensive rats. Quercetin was also effective in reducing blood pressure in rat models of metabolic syndrome, including the obese Zucker rats as well as rats treated with a high-sucrose, high-fat diet. Quercetin also prevented morphological and functional changes in the heart, vessels and kidney, while increasing production of reactive oxygen species associated with hypertension. A high dose of quercetin also reduced blood pressure in stage 1 hypertensive patients in a randomized, double-blind, placebo-controlled, crossover study. Since raised blood pressure is the major cause of stroke as well as an important risk factor for ischemic heart disease, we propose that the blood pressure-lowering effect of quercetin could be an important mechanism contributing to the reduced risk of myocardial infarction and stroke observed with fruit and vegetables-rich diets, and possibly with flavonoid-rich diets.     

Antihypertensive and renal effects of orally administered verapamil

Summary In 12 in-patients with moderate uncomplicated hypertension, maintained on constant sodium intake for 15 days, single-blind oral administration of verapamil 80–160 mg t. i. d. for 10 days had a significant antihypertensive effect: in the supine position systolic blood pressure decreased from 177±5 to 150±3 mmHg, and diastolic pressure from 111±3 to 96±2 mmHg; standing values were similarly lowered from 171±7 to 143±4 mmHg, systolic, and from 118±4 to 97±2 mmHg, diastolic. The heart rate did not show any significant change (from 79±3 to 77±2 beats/min, supine, and from 92±3 to 87±3 beats/min, upright). The antihypertensive effect was uniform throughout the day, being similar 2, 3, 6 and 8 h after administration of a dose. Dynamic exercise (75–100 watts on a cycle-ergometer) caused identical increases in arterial pressure and heart rate on the last day of placebo and again on the last day with verapamil, but the peak levels of systolic pressure reached during exercise were lower after verapamil than with placebo, because of the lower blood pressure before exercise. Reduction of arterial pressure by verapamil was not accompanied by increased plasma renin activity, or by renal retention of sodium and water: there was a small increase in sodium excretion, at least during the first days of verapamil administration (from 107±15 to 113±15 mEq Na⁺/day), and a slight significant reduction in body weight (from 74.2±3.7 to 73.5±3.7 kg). It is concluded that oral administration of verapamil significantly lowers blood pressure without simultaneously inducing cardiac stimulation, renin secretion or salt and water retention.     

Antihypertensive and neuroprotective effects of astaxanthin in experimental animals

Astaxanthin is a natural antioxidant carotenoid that occurs in a wide variety of living organisms. We investigated, for the first time, antihypertensive effects of astaxanthin (ASX-O) in spontaneously hypertensive rats (SHR). Oral administration of ASX-O for 14 d induced a significant reduction in the arterial blood pressure (BP) in SHR but not in normotensive Wistar Kyoto (WKY) strain. The long-term administration of ASX-O (50 mg/kg) for 5 weeks in stroke prone SHR (SHR-SP) induced a significant reduction in the BP. It also delayed the incidence of stroke in the SHR-SP. To investigate the action mechanism of ASX-O, the effects on PGF(2alpha)-induced contractions of rat aorta treated with NG-nitro-L-arginine methyl ester (L-NAME) were studied in vitro. ASX-O (1 to 10 microM) induced vasorelaxation mediated by nitric oxide (NO). The results suggest that the antihypertensive effect of ASX-O may be due to a NO-related mechanism. ASX-O also showed significant neuroprotective effects in ischemic mice, presumably due to its antioxidant potential. Pretreatment of the mice with ASX-O significantly shortened the latency of escaping onto the platform in the Morris water maze learning performance test. In conclusion, these results indicate that astaxanthin can exert beneficial effects in protection against hypertension and stroke and in improving memory in vascular dementia.     

Antidiabetic and antihyperlipidemic effects of Thespesia populnea fruit pulp extracts on alloxan-induced diabetic rats

Present study was carried to find out the antihyperglycemic and antihyperlipidemic activity of ethanol and aqueous extract of Thespesia populnea fruit pulp on alloxan-induced diabetic rats. Diabetes was induced in rats by administration of alloxan (150 mg/kg, i.p.). After the successful induction of experimental diabetes, the rats were divided into five groups each comprising a minimum of six rats. Phytochemical analysis and acute toxicity study of extracts was also done. The effects of extracts and metformin on fasting blood glucose and plasma lipid were examined for 28 days. Statistical analysis was carried out by using analysis of variance followed by Dunnet''s multiple comparison test and paired t-test were done as the test of significance using GraphPad Prism. P≤0.05 was considered as the minimal level of statistical significance. Therapeutic dose of extract was found to be 200 mg/kg on the basis of acute toxicity study. Aqueous and alcoholic extract showed a significant reduction in blood glucose levels as well as a lipid profile of diabetic rats at the end of 28^th day of treatment. However, in groups treated with plant extract the reduction in the blood glucose and improvement in lipid profile was slightly less than that achieved with the standard group (metformin). From this study, it can be concluded that ethanol and aqueous extract of Thespesia populnea exhibited significant antihyperglycemic and antihyperlipidemic effects on alloxan-induced diabetic rats.     

降脂药物临床疗效评价

<正>降低血脂治疗方法包括两大类:非药物性降脂治疗和药物性降脂治疗。前者包括饮食控制、血浆净化、外科手术和基因治疗等。采用药物使过高的血脂降至正常,效果肯定,患者易于接受。目前,临床上常用的降脂药物大体上可分为5大类。 1 三羟基三甲基戊二酰辅酶A(HMG-CoA)还原酶抑制剂(他汀类) 这类药物是细胞内胆固醇合成限速酶即 HMG-CoA还原酶的抑制剂,是目前临床上应用最广泛的一类调脂药,由于这类药物的英文名称均含有“statin”,故常简称为他汀类。他汀类通过抑制     

Antihypertensive therapy with ketanserin: metabolic and hemodynamic effects

Ketanserin, a serotonin-2-receptor antagonist, was administered to 12 subjects with mild to moderate hypertension in a randomized, double-blind, placebo-controlled crossover trial. After 6 weeks of ketanserin (40 mg every 12 h), blood pressures measured 12 h after dosing were not significantly different from those obtained during the placebo period. However, 2 h after ketanserin administration, supine systolic and diastolic blood pressures declined 11 +/- 10 mm Hg (p less than 0.01) and 6 +/- 5 mm Hg (p less than 0.005) from predose values, whereas placebo caused no change in either systolic or diastolic blood pressure. At the time of peak antihypertensive activity, plasma renin activity, aldosterone, growth hormone, and prolactin levels were unchanged. Prolactin levels decreased slightly (4.1 +/- 3.0 vs. 3.7 +/- 2.9 ng/ml, p less than 0.05) during ketanserin therapy when measured 12 h after dosing. Other pituitary hormones, serum testosterone, plasma catecholamines, and plasma lipids showed no changes. Heart rate was also unchanged. Stroke volume, measured 2 h after dosing, increased (70 +/- 22 vs. 85 +/- 31 ml, p less than 0.05) with ketanserin therapy, but cardiac output did not change significantly. Ketanserin has a moderate antihypertensive effect and neutral metabolic-hormonal profile when used as monotherapy for the treatment of hypertension. However, further studies are needed to define the frequency of dosing that will provide 24-h antihypertensive activity.