The hydroalcoholic extract of Cassia alata (Linn.) leaves and its major compound rhein exhibits antiallergic activity via mast cell stabilization and lipoxygenase inhibition

Ethnopharmacological relevance

Leaves of Cassia alata (family: Caesalpiniaceae) are ethnomedically claimed as anti-asthmatic. In the current study we aimed to investigate the anti-allergic activities of hydro-methanolic extract of Cassia alata (Linn.) and its constituents rhein and kaempferol on triple antigen/sheep serum-induced mast-cell degranulation in rats.

Materials and methods

Antiallergic activity of hydroalcoholic extract of Cassia alata along with its two components rhein and kaempferol was evaluated using in vivo mast cell stabilization assay. Inhibitory effect on lipoxygenase (LOX) enzyme was also evaluated in vitro. Further chemical standardization of Cassia alata extract was done using rhein and kaempferol by HPTLC-densitometric method.

Results

The hydroalcoholic extract of Cassia alata significantly inhibited mast cell degranulation at 200 mg/kg dose. Both chemical constituents rhein and kaempferol also showed potent (>76%) inhibition of mast-cell degranulation at 5 mg/kg. Extract and rhein inhibited LOX enzyme with IC₅₀ values of 90.2 and 3.9 μg/mL, respectively, whereas kaempferol was inactive.

Conclusion

Our results suggest that Cassia alata exhibit anti-allergic activity through mast cell stabilization and LOX inhibition. Thus, Cassia alata or its active constituents could be potential alternative treatment for allergic diseases.     

Some pharmacological effects of the ethanol extract of leaves of Annona diversifolia on the central nervous system in mice

In the present study we investigated some neuropharmacological effects of the ethanol extract of the leaves of Annona diversifolia (Annonaceae). Intraperitoneal administration of the extract delayed the onset of clonic seizures induced by pentylenetetrazole and delayed the time in the ‘rota-rod’ and ‘swimming’ test. In addition, the extract augmented the duration of sleeping time induced by sodium pentobarbital. These results indicate that the ethanol extract of the leaves of A. diversifolia has depressant activity on the central nervous system. Copyright © 1998 John Wiley & Sons, Ltd.     

Assessment of Sedative Effects of Passiflora edulis f. flavicarpa and Passiflora alata Extracts in Mice,Measured by Telemetry

Several Passiflora species have been used widely as a folk medicine due to their sedative and anxiolytic activities. In Brazil, a number of native plants of the genus Passiflora exist, but only Passiflora edulis f. flavicarpa (PE) and Passiflora alata (PA) are of commercial value. Thus, the aim of the present study was to investigate the sedative effects of aqueous extracts obtained from the pericarp as well as from the leaves of PE and PA in mice using radiotelemetry. Aqueous extracts from PE and PA were tested for effects on locomotion over 180 min in 300 mg/kg, 600 mg/kg and 1200 mg/kg, in male C57BL/6J mice after oral administration. For validation of the telemetry system, caffeine (negative control) and midazolam (positive control) were used. All tested extracts decreased locomotor activity in a dose‐dependent manner in comparison to the control group. The two lower concentrations of each extract showed the highest decrease in locomotion after 24 min, while 1200 mg/kg had a significant sedative effect already after 18 min. Interestingly, aqueous extracts of PA were more active in comparison to aqueous extracts of PE and the pericarp extracts of both plants showed more pronounced effects on locomotor activity if compared to leaf extracts. In conclusion, the present study represents an innovative, objective approach to measure sedative effects of plant extracts with minimized handling‐related stress and remote data collection. Copyright © 2013 John Wiley & Sons, Ltd.     

Antiprotozoal activity of Senna racemosa

Methanol extracts of leaves, roots and bark of Senna racemosa (Mill.) H.S. Irwin & Barneby (syn. Cassia racemosa Mill.) were tested for antiprotozooal activity against Giardia intestinalis and Entamoeba histolytica. All of the tested extracts showed good activity against both protozoa species. Extracts from stem bark and leaves were most active, with an IC(50) of 2.10 microg/mL for Giardia intestinalis and 3.87 microg/mL for Entamoeba histolytica. Of the previously isolated compounds from Senna racemosa, the piperidine alkaloid cassine had greater activity against Giardia intestinalis with an IC(50) of 3.28 microg/mL and chrysophanol, a 1,8-dihydroxy-anthraquinone, was the most active agent against Entamoeba histolytica, with an IC(50) of 6.21 microg/mL.     

丹参茎叶酚酮有效部位的提取纯化工艺研究

目的对丹参茎叶酚酮有效部位提取纯化工艺进行优选。方法采用超高效液相色谱仪检测,以丹参茎叶中酚酸类(丹参素、原儿茶酸、原儿茶醛、咖啡酸、丹酚酸B、迷迭香酸、紫草酸)及黄酮类成分(芦丁、异槲皮苷、山柰酚-3-O-芸香糖苷、紫云英苷)二者提取量、总提取量及浸膏得率为评价指标,通过单因素及正交试验考察提取方法、提取溶剂、料液比、提取时间及提取次数对丹参茎叶提取工艺的影响;采用大孔吸附树脂纯化丹参茎叶提取物并对纯化工艺参数进行考察,确定最佳纯化工艺。结果以50%乙醇8倍量回流提取3次,每次提取1.0 h为最佳提取工艺;以AB-8型大孔吸附树脂纯化,1.0 g/m L药液上样,上样量为每10克干树脂上样1.5 g干燥提取物,40%乙醇洗脱,洗脱用量3 BV为最佳纯化工艺,酚酸类及黄酮类成分总纯度可达到41.83%。结论优选的提取工艺稳定可行,适用于丹参茎叶酚酮有效部位的提取纯化,可为丹参茎叶的进一步开发提供参考。     

银杏叶中双黄酮成分的提取与测定

目的分离纯化银杏Ginkgo biloba叶中的双黄酮类成分,考察银杏叶变黄前后黄酮类成分质量分数的变化。方法从自然脱落的银杏叶中提取分离双黄酮类成分,对其乙醇提取物的二氯甲烷部位进行了分离,通过硅胶柱色谱和半制备液相方法对目标成分进行制备,采用HPLC法对银杏叶中的双黄酮进行了测定。结果分离的4个化合物分别为去甲银杏双黄酮、银杏双黄酮、异银杏双黄酮和金松双黄酮。对变黄前后银杏叶中4种双黄酮进行测定,结果表明,自然黄叶前3周内,银杏叶中双黄酮量逐渐降低,质量分数差别达30%左右。结论 HPLC法可用作银杏叶中双黄酮的测定,方法简便、可靠,能用于银杏叶的质量控制。同时,制备条件可对快速制备双黄酮对照品提供依据。     

辣木叶提取物对便秘小鼠润肠通便的作用及机制研究

目的探究辣木叶Moringaoleifera醇提物和水提物对便秘小鼠的通便作用及机制。方法昆明种小鼠随机分为对照组、模型组、酚酞(0.05 g/kg)组以及辣木叶醇提物低、中、高剂量(0.5、1.0、2.0 g/kg)组和辣木叶水提物低、中、高剂量(0.5、1.0、2.0g/kg)组,每组10只。通过失水燥结法建立小鼠便秘模型,给予药物进行干预,考察辣木叶醇提物和水提物对便秘小鼠首次排便时间、粪便含水率、6 h内排便数量、胃排空率、小肠内容物推进率的影响;采用苏木素-伊红(HE)染色考察辣木叶醇提物和水提物对便秘小鼠小肠组织病理变化的影响;采用ELISA试剂盒考察辣木叶醇提物和水提物对便秘小鼠血清中胃泌素、胃动素、内皮素和一氧化氮水平的影响;采用免疫组化法考察辣木叶醇提物和水提物对便秘小鼠小肠组织中胃泌素、胃动素、内皮素和一氧化氮蛋白表达的影响。结果辣木叶醇提物和水提物均能明显缩短小鼠首次排便时间(P0.01),提高粪便含水率(P0.05),增加6 h内排便数量(P0.05),提高小鼠胃排空率和小肠内容物推进率(P0.05、0.01),上调小鼠血清和小肠组织胃泌素、胃动素、内皮素分泌及表达(P0.05、0.01),下调血清和小肠组织一氧化氮分泌及表达(P0.05、0.01),减轻小肠绒毛损伤。结论辣木叶醇提物和水提物能够改善小鼠便秘,达到润肠通便的效果,其作用机制可能与调节小鼠胃肠激素水平、促进肠蠕动有关。     

In vivo and in vitro anti-inflammatory properties of Achyrocline alata (Kunth) DC

Ethnopharmacological relevance

Achyrocline alata is a locally marketed (Mato Grosso do Sul/ Brazil) herb used in folk medicine as an anti-inflammatory and a sedative. Evaluate the anti-inflammatory properties of Achyrocline alata in both in vivo and in vitro models.

Materials and methods

A hydroethanolic extract from inflorescences of Achyrocline alata (HEAa) was characterized by HPLC-DAD and compared to standards (chlorogenic acid; isoquercetrin; quercetin; 4,2?,4?-trihydroxy-6?-methoxychalcone; gnaphalin; 3-O-methyl-quercetin; 3,5-dicaffeoyl-quinic acid and 4,5-dicaffeoyl-quinic acid). The in vivo anti-inflammatory properties of the HEAa (4, 20 and 100 mg/kg, per os) were evaluated using the following animal models: carrageenan-induced paw edema in rats, carrageenan-induced vascular permeability and peritonitis in mice and an acetic acid-induced writhing model to test antihyperalgesic activity in mice. In vitro assays were performed to study the effects of the HEAa (0.16, 0.8 and 4 mg/ml) on the cell viability, cell spreading and production of NO and H₂O₂ in stimulated macrophages.

Results

The A. alata extract inhibited the development of edema and vascular permeability, reduced polymorphonuclear cell recruitment in the acute peritonitis assay and decreased the amount of writhing induced by acetic acid. The HEAa did not increase NO/H₂O₂ production, while it did inhibit production when the macrophages were stimulated by LPS or PMA at all tested concentrations. In the presence of HEAa, macrophage spreading did not increase even after stimulation with LPS. Additionally, the HEAa was nontoxic to macrophages at all tested concentrations.

Conclusions

The HEAa displayed anti-inflammatory and antihyperalgesic effects, which supports the use of this plant in folk medicine. These effects might be due to the flavonoids and phenylpropanoids derivatives present in the HEAa.     

Effect of aqueous leaf extract of Cassia alata (Linn.) on some haematological indices in albino rats

The effect of an aqueous leaf extract of Cassia alata (Linn.) on haematological indices in albino rats was studied. Increasing doses (10, 50, 100 and 150 mg/kg body weight) of the extract were administered orally to different groups of rats daily for a period of 14 days. Significant dose-dependent decreases in the levels of haemoglobin (Hb) and erythrocyte count (p < 0.05) were observed. In addition, increased packed cell volume (PCV) mean corpuscular volume (MCV), and mean corpuscular haemoglobin concentration (MCHC) were also observed. However, mean corpuscular haemoglobin (MCH) did not show any change. Clinical symptoms of loss of appetite, emaciation and loss of weight in the treated rats indicated toxicity. The observed symptoms of toxicity have been discussed in relation to the saponin content of the plant extract. © 1998 John Wiley & Sons, Ltd.     

决明毛状根化学成分研究

目的：研究决明毛状根的化学成分。方法：用发根农杆菌Agrobacterium rhizogenes 9402菌株从决明子叶外植体上诱导产生毛状根,在MS0液体培养基中大量培养获得。并采用色谱技术和波谱手段对毛状根的化学成分进行分离鉴定。结果：从决明毛状根95%乙醇提取物的醋酸乙酯部分分离鉴定了8个化合物,分别是白桦酯酸、大黄酚、大黄素甲醚、豆甾醇、1-羟基-7-甲氧基-3-甲基蒽醌、大黄酚-8-甲醚、大黄酚-1-甲醚和芦荟大黄素。其中芦荟大黄素是首次从决明毛状根中分得。结论：决明毛状根能合成与原植物相似的化学成分。     

The effects of Baphia nitida Lodd (leguminosae) extract on the gastrointestinal tract of rats and mice

The constituents from the leaves of Baphia nitida were extracted using methanol and acetone as solvents. The extract did not demonstrate any acute toxic effects in mice within the dose range used during this study. The extract inhibited gastric emptying time in rats and intestinal motility in mice, both effects were manifested in a dose-related fashion. These effects were similar but less pronounced than those produced by atropine sulphate. The extract did not induce gastric ulceration in rats and failed to protect against acetyl salicylic acid-induced gastric ulcer in rats or histamine-induced duodenal ulcer in guinea-pigs.     

Contractile effect of some extracts from the leaves of Musanga cecropioides (Cecropiaceae) on uterine smooth muscle of the rat

Portions of the hot water extract, chloroform and n-butanol fractions of the leaves of Musanga cecropioïdes were used to challenge uterine strips from nonpregnant and early stage pregnant (3–8 days) female Wistar rats. Uterine strips were obtained from oestrogenized females. The aqueous and n-butanol extracts (10 mg/L showed very marked uterotonic effects which were more pronounced in the pregnant females. These contractile effects were dose-dependent and comparable to oxytocin and acetylcholine (100 μg/mL) but were all antagonized by ethanol, a potent Ca^2t channel antagonist. These effects may account for the abortifacient properties of the extracts observed in previous in vivo trials.     

木豆叶提取物对心肌缺血再灌注损伤大鼠的保护作用

目的研究木豆叶提取物对大鼠心肌缺血再灌注损伤的保护作用。方法采用结扎冠状动脉前降支方法制备大鼠心肌缺血再灌注损伤模型,缺血前10 min大鼠ig给予不同剂量木豆叶提取物(125、200、500 mg/kg),复方丹参滴丸为阳性对照,再灌注30 min后以II导联心电图监测各组大鼠心律失常出现和持续时间,进行心律失常评分;再灌注90 min后测定心肌梗死范围,HE染色观察心肌形态学变化。结果模型组大鼠心律失常出现较早,持续时间较长,室性早搏、室速、室颤等发生率较高,且心律失常在缺血再灌注损伤末期仍非常明显。与模型组相比,木豆叶提取物能够降低大鼠缺血性心律失常的严重程度和发生率,明显缩小心肌梗死范围,减轻心肌细胞肿胀和炎性细胞浸润。结论木豆叶提取物对心肌缺血再灌注损伤大鼠有一定的保护作用。     

Evaluation of Alstonia scholaris leaves for broncho-vasodilatory activity

The present study demonstrates that the ethanol extract of Alstonia scholaris (Apocynaceae) leaves induced pronounced bronchodilatory activity in anaesthetized rats with the probable involvement of prostaglandins. However, in vitro preparations of guinea-pig trachea did not confirm this property, indicating that bronchodilation is not due to the direct tracheal smooth muscle relaxation. The vasodilatory activity of the extract was independent of adrenergic or muscarinic receptors or prostaglandins but was mainly via endothelial-derived relaxing factor, nitric oxide. The extract inhibited the spontaneous movements of rabbit jejunum and contractile effects of acetylcholine and histamine on guinea-pig ileum. Additionally, the extract caused marked reduction of barium chloride-, potassium chloride- and calcium chloride-induced contraction on guinea-pig ileum and pulmonary artery, implying a direct interference of plant extract with the influx of calcium ions into cells. However, the extract has no detectable effect on mobilization of intracellular calcium. These results coupled with the in vivo effects of ethanol extract reveal that the Alstonia scholaris leaves possess broncho-vasodilatory activity mediated presumably by prostaglandins, calcium antagonism and endothelium-derived relaxing factor(s).     

In vitro antimicrobial activity of ethanol and water extracts of Cassia alata

Crude ethanol and water extract of leaves and barks from Cassia alata were tested in vitro against fungi, (Aspergillus fumigatus and Microsporum canis), yeast (Candida albicans) and bacteria (Staphylococcus aereus and Escherichia coli). C. albicans showed concentration-dependent susceptibility towards both the ethanol and water extracts from the barks, but resistant towards the extracts of leaves. The degree of susceptibility varied, the water extract from barks showed bigger inhibition zone than the ethanol extracts (12-16 and 10-14 mm, diameter respectively). The growth of Aspergillus fumigatus and Microsporum canis were not affected by all types of the plant extracts. Results were comparable to standard antifungal drug Tioconazole (18 mm diameter) at equivalent concentration. The anti-bacterial activity of C. alata extracts on S. aureus was detected with only the leaves extracts using water and ethanol. The water extract exhibited higher antibacterial activity than the ethanol extract from leaves (inhibition zones of 11-14 and 9-11 mm, respectively). E. coli showed resistance to all types of extracts. Based on the current findings, it can be concluded that this plant has antimicrobial activity, which is as potent as standard antimicrobial drugs against certain microorganisms.     

Antiviral activity of panamanian plant extracts

Panamanian tropical forest plants are potential sources of useful medicinal compounds including some with antiviral activities. Extracts prepared from the leaves of seven plants (Alseis blackiana Hemsl., Aspidosperma megalocarpon Muell, Arg., Hybanthus prunifolius (Humb. & Bonpl.) G. K. Schulze, Ouratea lucens Engl., Piper cordulatum C. DC., Trichilia cipo C. DC. and Tetragastris panamensis Kuntze) were screened for antiviral activity using three separate assay methods. The more polar (aqueous and ethanol) extracts of all plants demonstrated antiviral and virucidal activities. Good activities were found in the Ouratea lucens and Trichilia cipo ethanol and aqueous extracts which were further characterized for antiviral activity and cytotoxic effects. These extracts had direct virucidal activity as well as intracellular antiviral activity against both DNA and RNA viruses. Antiviral activity was achieved with extract concentrations significantly lower than those necessary to produce cytotoxic effects. Additionally, extracts were less toxic to normal cells than to the tumour cells tested.     

The toxicity of extracts of plant parts of Moringa stenopetala in HEPG2 cells in vitro

The cytotoxicity of extracts from a widely used species of plant, Moringa stenopetala, was assessed in HEPG2 cells, by measuring the leakage of lactate dehydrogenase (LDH) and cell viability. The functional integrity of extract-exposed cells was determined by measuring intracellular levels of ATP and glutathione (GSH). The ethanol extracts of leaves and seeds increased significantly (p < 0.01) LDH leakage in a dose- and time-dependent manner. The water extract of leaves and the ethanol extract of the root did not increase LDH leakage. A highly significant (p < 0.001) decrease in HEPG2 viability was found after incubating the cells with the highest concentration (500 microg/mL) of the ethanol leaf and seed extracts. At a concentration of 500 microg/mL, the water extract of leaves increased (p < 0.01), while the ethanol extract of the same plant part decreased (p < 0.01), ATP levels. The root and seed extracts had no significant effect on ATP levels. The ethanol leaf extract decreased GSH levels at a concentration of 500 microg/mL (p < 0.01), as did the ethanol extract of the seeds at 250 microg/mL and 500 microg/mL (p < 0.05). The water extract of the leaves did not alter GSH or LDH levels or affect cell viability, suggesting that it may be non-toxic, and is consistent with its use as a vegetable. The data obtained from the studies with the ethanol extract of the leaves and seeds from Moringa stenopetala show that they contain toxic substances that are extractable with organic solvents or are formed during the process of extraction with these solvents. The significant depletion of ATP and GSH only occurred at concentrations of extract that caused leakage of LDH. Further investigation with this plant in order to identify the constituents extracted and their individual toxic effects both in vivo and in vitro is warranted. This study also illustrates the utility of cell culture for screening plant extracts for potential toxicity.     

Cytotoxic activity of marine macro‐algae on Artemia salina (Brine shrimp)

A total of 22 ethanol extracts of seaweed species (13 brown, 6 green and 3 red) collected from the Karachi coast were investigated for brine shrimp cytotoxicity. Of all the species, only six namely Stoechospermum marginatum, Sargassum swartzii, S. binderi, Spatoglossum asperum, Stokeyia indica (brown) and Caulerpa racemosa (green) showed significant activity. n‐Hexane‐soluble fractions of the ethanol extract of S. marginatum and S. swartzii were found to be responsible for the activity, whereas the methanol‐soluble fractions of S. asperum and S. binderi were most active. The water extract of S. indica and C. racemosa exhibited the most prominent activity (LC₅₀ value below 70 µg/mL) when compared with the ethanol extracts and their fractions. Cytotoxic activity may be due to the compounds differing in polarity. Copyright© 1999 John Wiley & Sons, Ltd.     

Repeated administration of an aqueous spray-dried extract of the leaves of Passiflora alata Curtis (Passifloraceae) inhibits body weight gain without altering mice behavior

Ethnopharmacological relevance

Passiflora alata is a Southern American species that constitutes many traditional remedies as well as phytomedicines used for sedative and anxiolytic purposes in Brazil. However studies on repeated treatment effects are scarce.

Aim of the study

To evaluate behavioral, physiological and biochemical effects of the repeated treatment with an aqueous spray-dried extract of Passiflora alata leaves containing 2.5% (w/v) of flavonoids (PA) in mice.

Material and methods

Male adult CF1 mice were treated (p.o.) for 14 days with PA (2.5; 25 or 250 mg/kg). The feeding behavior was evaluated at the beginning (1 h after the first administration) and at the end of the treatment (15th day). The body weight gain and food consumption were monitored along the days. On day 15 mice were evaluated on plus maze, spontaneous locomotor activity, catalepsy and barbiturate sleeping time tests. Serum glucose, lipids, ALT and AST enzymes were determined. Liver, kidney, perirenal fat, epididymal and peritoneal fat were analyzed.

Results

The repeated treatment with the highest dose tested (250 mg/kg) did not alter the mice behavior on open field, elevated plus maze, catalepsy and barbiturate sleeping time tests. Repeated administration of PA 250 decreased mice feeding behavior and weight gain. PA 25 and PA 250 reduced mice relative liver weight and caused mild hepatic hydropic degeneration as well as a decrease in alanine aminotransferase (ALT) serum level.

Conclusions

These results indicate that Passiflora alata does not present central cumulative effects and point to the needs of further studies searching for its hepatotoxicity as well as potential anorexigenic.     

Antiulcerogenic activity of Lantana camara leaves on gastric and duodenal ulcers in experimental rats

Ethnopharmacological relevance

Lantana camara L. (Verbenaceae), a widely growing shrub has been used in the traditional medicine for treating many ailments. The objective of the present study was to evaluate the effects of methanolic extract of Lantana camara leaves on gastric and duodenal ulcers.

Materials and methods

The antiulcerogenic effect of methanolic extract of Lantana camara was evaluated in aspirin induced gastric ulcerogenesis in pyloric ligated rats, ethanol induced gastric ulcer, and cysteamine induced duodenal ulcer models. The extract was administered orally at two different doses of 250 mg/kg and 500 mg/kg. The lipid peroxidation, reduced glutathione levels of ethanol induced gastric ulcer model and inhibition zone in diameter against Helicobacter pylori also determined.

Results

The L. camara extract significantly (P < 0.01) reduced ulcer index, total acidity and significantly (P < 0.01) increased the gastric pH of aspirin + pylorus-ligation induced ulcerogenesis and ethanol induced gastric ulcer models. The extract also significantly (P < 0.01) reduced the ulcer index of cysteamine induced duodenal ulcer. The L. camara showed significant (P < 0.01) reduction in lipid peroxidation and increase in reduced glutathione levels. The inhibition zone in diameter of extract against H. pylori was 20 mm.

Conclusion

The methanolic extract of Lantana camara leaves shown healing of gastric ulcers and also prevents development of duodenal ulcers in rats.