Evaluation of diuretic and laxative activity of hydro-alcoholic extract of Desmostachya bipinnata (L.) Stapf in rats

ObjectiveIn continuation to the growing evidence for therapeutical potential of Desmostachya bipinnata (Linn) Stapf, the current pharmacological study was carried out to evaluate the diuretic and laxative activity of its hydro-alcoholic extract in rats.MethodsThe hydro-alcoholic extract of D. bipinnata whole plant was prepared by using Soxhlet extractor and subjected to analysis by standard preliminary phytochemical tests. Evaluation of both diuretic and laxative activity was carried out using standard methods as reported earlier. Frusemide (20 mg/kg) was served as positive control for diuretic activity and sennosides (10 mg/kg) served as negative control for laxative activity.ResultsThe hydro-alcoholic extract showed significant diuretic activity and was found to be the most potent in increasing the urinary output at 500 mg/kg when the effect was compared with that of the standard frusemide (P<0.01). Moreover, this extract was found to be most effective in increasing urinary electrolyte concentration (Na⁺, K⁺, and Cl⁻) at both doses tested. Whereas the results for laxative activity showed minimal increase of feces output at the dose of 500 mg/kg and the increase was negligible when compared with that of the standard drug sennosides.ConclusionAltogether, the above significant findings validate and support its folkloric diuretic use and lend pharmacological credence to the ethno-medical use of this plant in traditional system of medicine, which demands further studies to investigate its active constituents, as well as its use and safety.     

Calcium channel blocking activity of Mentha longifolia L. explains its medicinal use in diarrhoea and gut spasm

Mentha longifolia has a reputation in traditional medicine in the indications of diarrhoea and gut spasm. This study was carried out to provide a possible pharmacological basis for its medicinal use in hyperactive gut disorders. In a castor oil induced diarrhoeal model, the crude extract of Mentha longifolia (Ml.Cr), at doses of 100–1000 mg/kg, provided 31–80% protection, similar to loperamide. In isolated rabbit jejunum preparations, Ml.Cr caused inhibition of spontaneous and high K⁺‐induced contractions, with respective EC₅₀ values of 1.80 (1.34–2.24; n = 6–8) and 0.60 mg/mL (0.37–0.85; n = 6–8), which suggests spasmolytic activity, mediated possibly through calcium channel blockade (CCB). The CCB activity was further confirmed when pretreatment of the tissue with Ml.Cr (0.3–1 mg/mL) caused a rightward shift in the Ca⁺⁺ concentration–response curves (CRCs), similar to verapamil. Loperamide also inhibited spontaneous and high K⁺‐induced contractions and shifted the Ca⁺⁺ CRCs to the right. Activity‐directed fractionation revealed that the petroleum spirit fraction was more potent than the parent crude extract and aqueous fraction. These data indicate that the antidiarrhoeal and spasmolytic effects of the crude extract of Mentha longifolia are mediated through the presence of CCB‐like constituent(s), concentrated in the petroleum spirit fraction and this study provides indirect evidence for its medicinal use in diarrhoea and spasm. Copyright © 2010 John Wiley & Sons, Ltd.     

Presence of cholinergic and calcium antagonist constituents in Saussurea lappa explains its use in constipation and spasm

This study was carried out to provide a scientific basis for the traditional use of Saussurea lappa, in constipation and spasms. Isolated tissue preparations were used to see if the aqueous-methanol crude extract of the S. lappa root (Sl.Cr) contains gut stimulatory and inhibitory constituents. In isolated guinea-pig ileum, a quiescent preparation, Sl.Cr caused a concentration-dependent (0.3-5.0 mg/mL) spasmogenic effect, with the maximum effect reaching 91% of the acetylcholine maximum. A further increase in concentration caused a declining effect, indicating the presence of spasmolytic constituent(s). The spasmolytic effect was more marked in the spontaneously contracting rabbit jejunum and in the atropinized preparations. The spasmolytic effect was mediated through calcium channel blocking (CCB) activity, as evident by its inhibitory effect against high K(+) (80 mm)-induced contraction and displacement of the Ca(++) concentration-response curves to the right. These data indicate that the crude extract of Sl.Cr contains gut stimulatory constituent(s) of cholinergic-type providing a scientific basis for its use in constipation. The presence of spasmolytic constituents of CCB-type more evident in the spontaneous contracting gut preparation may explain its use in spasms.     

灯盏花素对大鼠全脑缺血再灌注后海马神经元L型钙通道的影响

目的观察灯盏花素对大鼠全脑缺血再灌注后海马神经元L型钙通道平均开放概率和开放时间的影响。方法制作全脑缺血大鼠模型,再灌注1．5 h、3．0 h、4．5 h和6．0 h,急性分离海马CA1区神经元,采用膜片钳技术细胞贴附式方法记录神经细胞膜上单通道Ca~(2 )电流,分析L型钙通道平均开放概率和开放时间,在此基础上观察灯盏花素对其影响。结果不同浓度的灯盏花素能降低海马神经元L型钙通道的平均开放概率和开放时间,且在缺血再灌注3．0 h内作用明显。结论灯盏花素对脑缺血再灌注脑损伤有一定的保护作用。     

黄芪对感染病毒大鼠心肌细胞L型钙通道的效应

目的:了解黄芪对感染柯萨奇病毒心肌细胞 L 型钙通道的影响,以探讨黄芪用于心肌炎治疗的作用机制。方法:以柯萨奇 B_3病毒感染急性分离的成年大鼠心肌细胞,利用膜片钳技术记录 L 型钙通道电流。结果:黄芪不影响正常心肌细胞 L 型钙通道电流的幅度,但可减缓 L 型钙通道电流的衰减。病毒感染增加心肌细胞 L 型钙通道电流的幅度,并改变其电压依赖性而使电流电压曲线向左下偏移。黄芪可抑制病毒感染细胞 L 型钙通道电流的增加。结论:黄芪通过抑制感染细胞经 L 型钙通道的跨膜钙内流和稳定 L 型钙通道的作用,可防止病毒感染可能导致的细胞内钙超载和异常电活动,从而对感染细胞起到保护作用     

芎归鼻用喷雾剂的制备及其体外释药与在体吸收特性评析

目的:制备芎归鼻用喷雾剂,并研究其体外释药及在体鼻黏膜吸收特性。方法:采用正交设计对芎归鼻用喷雾剂进行处方筛选;通过动态透析法考察其在Ringer液中的释药特性;通过在体大鼠鼻黏膜吸收试验考察其在体吸收特性。结果:最优处方为Pemulen TR-1 0.35%,EDTA 0.2%,PEG400 1%,黄原胶0.2%,三乙醇胺适量(调处方pH 7.0)。其体外释药及在体吸收均符合Higuchi分布模型。结论:芎归鼻用喷雾剂的制备工艺基本可行,其体外释药与在体吸收有良好的相关性。     

Estimation of naphthaquinones from Arnebia hispidissima (Lehm.) DC. In vivo and in vitro. I. Anti-inflammatory screening

The hexane extract of Arnebia hispidissima yielded a mixture of naphthaquinones: arnebin-1, arnebin-7, tiglic acid (ester of dihydroxy alkannin), alkannin, arnebinol and cycloarnebin-7. To evaluate the anti-inflammatory activities of hexane extract and isolated naphthaquinones, models with carrageenan-induced acute arthritis and complete Freund's adjuvant (CFA)-induced chronic arthritis in rats were conducted. The observed results indicated that pretreatment with cycloarnebin-7 significantly inhibited the carrageenan-induced acute arthritis. Moreover, arnebin-1, significantly suppressed the development of chronic arthritis induced by CFA. The present study deals with the quantification of naphthaquinones from in vivo and in vitro cell cultures of plant species and isolated compounds from intact plant tested for their swelling inhibitory potency. It has been reported that arnebin-1 was the major naphthaquinone both in vivo (0.62%) and in vitro (0.27%) cell cultures.     

生物降解型左炔诺孕酮微球的体内外释药特性研究

 目的对左炔诺孕酮(LNG)微球的体内释药特性进行研究和评价。方法用放射免疫法测定生物降解型PLGA(9∶1)LNG微球在大鼠的药代动力学,进行了体内外释药试验。结果该微球具有相似的体内外释药特性：存在双峰现象,双峰之间有一较为平稳的释药区域,约占整个释药过程的70%。LNG微球在大鼠的MRT约为对照组LNG微晶的6.6倍。结论该微球有比较好的控释作用。依据微球体内外释药的两个特点可对该生物降解型控释微球的质量进行初步控制。     

芦荟多糖的纯化工艺与体外抗肿瘤活性

目的:研究芦荟多糖的提取、纯化工艺及体外抗肿瘤活性,为芦荟的产业化开发提供实验依据。方法:采用水提醇沉,三氯乙酸法除蛋白,DEAE-52离子交换色谱分离。用Sephacryl S-400凝胶柱层析纯化并确定芦荟多糖的相对分子量,HPLC法检测纯度,GC法鉴别单糖组成及分子摩尔比。以MTT法观察其体外抗肿瘤活性等。结果:从中华芦荟(Aloe vera L.var. chinesis(Haw.)Berger.)凝胶冻干粉中提取分离得到纯多糖AVP,经HPLC检测为单一对称峰,相对分子量为86000,由甘露糖和葡萄糖组成,摩尔比为10.3∶1.0。AVP对人肝癌细胞(SMMC-7721)、人胃癌细胞(BGC-823)及人肺癌细胞(A549)的增殖均有抑制作用。结论:该法分离的芦荟多糖AVP纯度好,收率高达3.6%,可用于进一步的研究和开发,提高芦荟的资源利用率。     

In vitro antileukaemic activity of extracts from chokeberry (Aronia melanocarpa [Michx] Elliott) and mulberry (Morus alba L.) leaves against sensitive and multidrug resistant HL60 cells

The aim of the present study was to determine in vitro antileukaemic activities of extracts obtained from chokeberry (Aronia melanocarpa [Michx] Elliot) and mulberry (Morus alba L.) leaves against promyelocytic HL60 cell line and its multidrug resistant sublines exhibiting two different MDR phenotypes: HL60/VINC (overexpressing P-glycoprotein) and HL60/DOX (overexpressing MRP1 protein). It was found that the extracts from chokeberry and mulberry leaves were active against the sensitive leukaemic cell line HL60 and retained the in vitro activity against multidrug resistant sublines (HL60/VINC and HL60/DOX). The values of resistance factor (RF) found for these extracts were very low lying in the range 1.2-1.6.     

Genotoxic and Antigenotoxic Activity of Acerola (Malpighia glabra L.) Extract in Relation to the Geographic Origin

Malpighia glabra L, popularly known as acerola, is considered a functional fruit and therefore is taken to prevent disease or as adjuvant to treatment strategies, since the fruit is an undeniable source of vitamin C, carotenoids, and flavonoids. Acerola is a natural source of vitamin C, flavonoids, and carotenoids. Its chemical composition is affected by genetic uniformity of the orchards and environmental factors. Considering the extensive growth of the culture of acerola in Brazil as well as its widespread use, this study evaluates the genotoxic and antigenotoxic activity of acerola in relation to geographical origin using the comet assay in mice blood cells in vitro. No acerola samples showed potential to induce DNA damage, independently of origin. Also, for antigenotoxicity activity, only the acerola sample from São Paulo reduced DNA damage induced by hydrogen peroxide (by about 56%). The sample from Ceará showed good antioxidant activity by the 2,2‐diphenyl‐1‐picrylhydrazyl assay, in agreement with its higher rutin, quercetin, and vitamin C levels. Additional studies with other treatment regimens are necessary to better understand the impact of the complex mixture of acerola on genomic stability. Copyright © 2012 John Wiley & Sons, Ltd.     

川白芷离体培养与多倍体诱导过程中的形态组织学观察

目的：探索川白芷离体培养过程中的形态变化与组织发生的关系,为其多倍体诱变寻找最佳处理时期。方法：对离体培养的外植体采取不定期取材固定,作切片观察;当其分化出不定芽时,用秋水仙液作诱变处理。结果：不定芽主要为外起源,最适宜作诱变处理;培养３８ ｄ 左右为诱变的最佳处理期;此种处理方法证明是有效的。结论：对组织培养中产生的不定芽作诱变处理,是一种行之有效的生物技术方法。     

Jasmine absolute (Jasminum grandiflora L.) and its mode of action on guinea-pig ileum in vitro

Jasmine (Jasminum grandiflorum L.) is used in aromatherapy as a holistic treatment for apathy, hysteria, uterine disorders and childbirth, muscle relaxation and coughs. Its stimulant nature, on inhalation, has been shown both in animals and man. Jasmine has a spasmolytic activity on guinea-pig ileum and rat uterus in vitro. The mechanism of action of the spasmolytic activity, studied in vitro using a guinea-pig ileum smooth muscle preparation, was postsynaptic and not atropine-like. The spasmolytic effect of jasmine absolute was most likely to be mediated through cAMP, and not through cGMP. The mode of action in vitro resembled that of geranium, lavender and peppermint oils. The contradictory effect in vitro and in vivo is probably due to the solely physiological effects of jasmine absolute in vitro (producing a relaxation) compared with that in vivo, where it has a strong psychological input, producing a stimulant effect in man and enhanced movement in animals.     

二至天癸颗粒对体外受精-胚胎移植患者卵泡液代谢组学及Ca~(2+)浓度的影响

目的从人卵泡液代谢组学及Ca~(2+)浓度,探讨二至天癸颗粒提高卵细胞质量的机制。探讨体外受精-胚胎移植(in vitro fertilization and embryo transfer,IVF-ET)周期人卵泡液代谢组学及钙离子(Ca~(2+))浓度、胆碱脂酶(ChE)、肌酐(Cr)对卵细胞质量及妊娠结局的影响。方法57例IVF-ET患者随机分为试验组(二至天癸颗粒加IVF-ET常规用药组,27例)和对照组(六味地黄颗粒合IVF-ET常规用药组,30例)。观察患者取卵日肾阴虚证候较垂体降调节后的改善情况,比较两组患者卵泡液Ca~(2+)浓度、胆碱脂酶、肌酐的差异及两组卵泡液代谢组学的变化,取卵数、受精率、卵裂率、优质胚胎率和妊娠率的差异。结果试验组治疗后肾阴虚证候积分为8.30±1.46,受精率0.82±0.09,卵裂率0.97±0.07,优质胚胎率0.51±0.18,对照组分别为9.16±1.15,0.74±0.18,0.91±0.10,0.41±0.09,试验组优于对照组(P0.05)。主成分分析法分析两组卵泡液代谢组学,试验组主要分布在Ⅰ区;对照组主要分布在Ⅱ区。两组卵泡液代谢组学有明显差异。妊娠组卵泡液主要分布在Ⅰ区。试验组Ca~(2+)浓度显著高于对照组(P0.05)。ChE、Cr高于对照组,但差异无统计学意义。结论在调节卵泡液代谢组学和Ca~(2+)浓度,提高卵细胞、胚胎质量,提高IVF-ET妊娠率方面,二至天癸颗粒优于六味地黄颗粒。     

莪术对大鼠在体子宫肌电活动的影响及其机制研究

目的 :观察莪术水煎剂对未孕大鼠在体子宫肌电活动的影响并探讨其机制。方法 :在一侧子宫浆膜面上埋植一对Ag-AgCl双极电极并联机记录 ,分别进行 5种阻断剂使用前后莪术对子宫肌电活动影响的慢性实验。结果 :莪术水煎剂可显著增加子宫肌电爆发波的峰面积、持续时间和爆发波的个数 ,且与剂量相关。腹腔注射阻断剂后 ,阿托品或酚妥拉明均明显减弱莪术对子宫肌电的兴奋效应 ,而其它 3种阻断剂则无影响。结论 :莪术对大鼠子宫肌电具有明显的兴奋作用 ,其兴奋作用与M受体和α受体有关。     

Evaluation of the Antinociceptive Activity of Ocimum gratissimum L. (Lamiaceae) Essential Oil and its isolated Active Principles in Mice

Ocimum gratissimum is used in popular medicine to treat painful diseases. The antinociceptive properties of O. gratissimum essential oil (OgEO) and two of its active principles (eugenol and myrcene) were tested in classic models of pain (hot plate test and formalin test). Adult male C57BL/6 J mice acutely received corn oil (control group, p.o.), morphine (positive control group, 5 mg/kg, i.p.), OgEO (10, 20, or 40 mg/kg, p.o.), eugenol or myrcene (both at 1, 5, or 10 mg/kg, p.o.). The highest doses of all tested drugs significantly increased the latency to lick the paw(s) in the hot plate test compared with the control group. OgEO at a dose of 40 mg/kg and eugenol and myrcene at a dose of 10 mg/kg were effective in minimizing animal pain in the first and second phases of the formalin test. The antinociceptive effect shown by all drugs tested in hot plate test was reverted by naloxone administration (1 mg/kg), indicating opiod system participation. These results demonstrate the beneficial effects of OgEO and its active principles against neurogenic and inflammatory pain. Our findings demonstrate that OgEO and its isolated active principles exhibited antinociceptive activity in murine pain models. Copyright © 2012 John Wiley & Sons, Ltd.     

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.     

Role of oil extract of garlic (Allium sativum Linn.) on intestinal transference of calcium and its possible correlation with preservation of skeletal health in an ovariectomized rat model of osteoporosis

The present study was undertaken to examine the effects of an oil extract of garlic on the in vivo intestinal transference of calcium, and also to verify its role in maintaining the bone mineral content and bone tensile strength in an ovariectomized rat model of osteoporosis. The results suggest that, in this experimental model, oil extract of garlic promotes intestinal transference of calcium by modulating the activities of both intestinal alkaline phosphatase and Ca(2+) activated ATPase. Also the observed low bone mineral content and low bone tensile strength in these rats were significantly restored by garlic oil supplementation. Further, garlic oil supplementation was able to revive partially the bilateral ovariectomy-induced decrease in the serum estrogen titer. The serum parathyroid hormone level, however, was found unaltered in these rats. The garlic oil supplemented partial recovery in serum estrogen titer in bilaterally ovariectomized rat was found to be persistently associated with enhanced calcium transference and better preservation of bone mineral content. The results of this study propose that the phytoestrogenic efficacy of an oil extract of garlic prevents ovarian hormone deficiency induced bone mineral loss possibly by promoting intestinal transference of calcium through the partial revival of the serum estrogen titer.     

Effect of American ginseng (Panax quinquefolius L.) on arterial stiffness in subjects with type-2 diabetes and concomitant hypertension

Ethnopharmacological relevance

Substantial pre-clinical and some clinical data are available showing that Asian ginseng (Panax ginseng C.A. Meyer) varieties or its particular ginsenosides exert a vasodilatating effect, thus may modulate vascular function. However, the clinical evidence for American ginseng (Panax quinquefolius L.) is scarce. Therefore, this study evaluates the effect of American ginseng (AG) on arterial stiffness, as measured by augmentation index (AI), and blood pressure (BP), in type 2 diabetes patients with concomitant hypertension.

Materials and methods

Using a double-blind, placebo-controlled, parallel design, each participant was randomized to either the selected AG extract or placebo at daily dose of 3 g for 12 weeks as an adjunct to their usual antihypertensive and anti-diabetic therapy (diet and/or medications). AI and BP were measured by applanation tonometry at baseline and after 12 weeks of treatment.

Results

A total of 64 individuals with well-controlled essential hypertension and type 2 diabetes (gender: 22 M:42 F, age:63±9.3 years, BP: 145±10.8/84±8.0 mmHg, HbA1c: 7.0±1.3%, fasting blood glucose (FBG): 8.1±2.3 mmol/L) completed the study. Compared to placebo, 3 g of AG significantly lowered radial AI by 5.3% (P=0.041) and systolic BP by 11.7% (P<0.001) at 12 weeks. No effect was observed with diastolic BP.

Conclusions

Addition of AG extract to conventional therapy in diabetes with concomitant hypertension improved arterial stiffness and attenuated systolic BP, thus warrants further investigation on long-term endothelial parameters before recommended as an adjunct treatment.     

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.