Terminalia arjuna,an ayurvedic cardiotonic,increases contractile force of rat isolated atria

The direct effects of aqueous, ethanolic, chloroform and petroleum ether extracts of Terminalia arjuna (family: Combretaceae) bark, an ayurvedic remedy for cardiovascular disorders, were studied on isolated atria of rats. The aqueous extract produced a substantial positive inotropic effect (EC₅₀ = 0.25 mg/mL) but no change in the rate. The ethanol, chloroform and petroleum ether extracts all decreased the rate of contraction. A slight increase in force was seen with ethanol and chloroform extracts. Higher concentrations of the chloroform extract had a negative inotropic effect. The ethanol extract decreased the maximum following frequency of the left atria. It is concluded that Terminalia arjuna has a significant positive inotropic property on rat atria in vitro which could contribute to its efficacy in treating cardiovascular disorders.     

Studies of biological properties of Uncaria tomentosa extracts on human blood mononuclear cells

Ethnopharmacological relevance

Uncaria tomentosa (Willd.) DC is a lignified climbing plant from South and Central America, which (under the name of “vilcacora” or “cat's claw”) has become highly popular in many countries due to its proven immunostimmulatory and anti-inflammatory activities and also with respect to its anticancer and antioxidative effects. There are insufficient data on the mechanism of U. tomentosa action on normal blood mononuclear cells.

Aim of the study

The aim of the study was to analyze the impact of ethanol and aqueous extracts from bark and leaves of Uncaria tomentosa on the structure and function of human mononuclear cells and to find out whether the kind of extractant used modulates biological activity of the extracts studied.

Materials and methods

Plant material consisted of four different extracts: (1) ethanol extract from leaves, (2) aqueous extract from leaves, (3) ethanol extract from bark and (4) aqueous extract from bark. The effect of these extracts on protein damage as well as on free-radical formation in human peripheral blood mononuclear cells was analyzed. Moreover, changes in viability, size, and granularity as well as apoptotic alterations in human blood mononuclear cells exposed to U. tomentosa extracts were investigated.

Results

The oxidative changes were observed in mononuclear blood cells exposed to both ethanol and aqueous extracts obtained from bark and leaves. Moreover, in the cells studied the extracts from U. tomentosa induced apoptosis and a decrease in viability of mononuclear blood cells, with the exception of aqueous extract from leaves. Additionally, no statistically significant changes in the cell size were observed both for aqueous extracts from leaves and bark. Changes in the blood mononuclear cell granularity were observed at 250 μg/mL for all extracts examined. The strongest changes were observed for the ethanol extract of the bark, which increased cell granularity at 50 μg/mL and changed cell size at 100 μg/mL.

Conclusion

The conducted research showed differences in biological activity between aqueous and ethanol extracts. It was observed that ethanol extracts exhibited stronger negative effects on mononuclear blood cells. The kind of extractant used had a significant influence of the chemical composition of the tested extracts. The ethanol extract from bark containing a high amount of polyphenols and alkaloids revealed the highest pro-apoptotic effect.     

Experimental evaluation of Myracrodruon urundeuva bark extract for antidiarrhoeal activity

The bark of M. urundeuva (Anacardiaceae) used in popular medicine as an antidiarrhoeal agent has been investigated for its effects on castor oil-induced diarrhoea and on intestinal motility. In rats, the ethanol extract of stem bark significantly inhibited the castor oil-induced diarrhoea, small intestinal transit and accumulation of fluid volume at an oral dose of 400 mg/kg. Furthermore, the plant extract caused marked inhibition of the contractile responses evoked by acetylcholine and histamine on guinea-pig ileum in vitro. These results point to a possible antidiarrhoeic effect of M. urundeuva bark extract since inhibition of intestinal motility and secretion can greatly control clinical diarrhoea. Copyright © 1998 John Wiley & Sons, Ltd.     

山核桃树皮中槲皮苷的提取工艺优选及含量测定

目的:优选山核桃树皮中槲皮苷的提取工艺,并建立其含量测定方法。方法:采用乙醇回流法提取山核桃树皮,经聚酰胺吸附去杂、多次析晶得槲皮苷,采用核磁共振波谱法(NMR)确证其结构,HPLC测定其含量。通过正交试验考察乙醇体积分数、提取时间和提取次数对槲皮苷得率的影响。结果:经NMR确证产物为槲皮苷,HPLC表明其在4.8～91.2 mg·L-1呈良好线性关系,山核桃树皮中槲皮苷含量高达8.37%。最佳提取工艺为10倍量60%乙醇回流提取2次,每次1 h,提取率>90%。结论:建立的山核桃中槲皮苷含量测定方法简单精确,优选的提取工艺稳定可行。     

Analgesic and anti-inflammatory effects of Cassia siamea Lam. stem bark extracts

Aim of the study

The present study was carried out to investigate analgesic and anti-inflammatory activities of Cassia siamea Lam stem bark extracts. We have also determined the cytotoxicity of each extract.

Materials and methods

C. siamea, a widespread medicinal plant traditionally used in sub-Saharan Africa, was collected in Congo Brazzaville. Stem bark was extracted with petroleum ether (CSE1), chloroform (CSE2), ethanol (CSE3) and water (CSE4). Analgesic, anti-inflammatory and antipyretic activities of these extracts were assessed in rats with hot plate test, paw pressure and carrageenan induced paw oedema. Cytotoxicity was assessed against KB and Vero cells.

Results

At the doses used (100, 200, and 400 mg/kg) ethanol and water extracts showed significant and dose-dependent analgesic and anti-inflammatory effects. None of the extracts had cytotoxic activity on KB and Vero cell lines and the most active extracts (CSE3 and CSE4) had no acute toxicity.

Conclusions

The study highlighted the analgesic and anti-inflammatory of C. siamea stem bark. Four major families of compounds present in the plant may explain these activities: triterpenes (lupeol, oleanolic acid, ursolic acid, friedelin, betulin), flavonoids (apigenin, kaempferol, luteolin), anthraquinones (emodin), phytosterols (stigmasterol, beta-sitosterol).     

山核桃树皮中槲皮苷的提取工艺及含量测定研究

[摘要] 目的：对山核桃树皮中槲皮苷的提取工艺进行研究,建立其含量测定方法。方法：采用乙醇回流法提取山核桃树皮,经聚酰胺吸附去杂、多次析晶得槲皮苷,采用核磁共振波谱法（NMR）确证其结构,HPLC法测定其含量,并通过正交实验考查乙醇浓度、提取时间和提取次数对槲皮苷得率的影响。结果：经NMR确证产物为槲皮苷,HPLC法表明其在4.8~91.2µg•mL-1的范围内线性关系良好,山核桃树皮中其含量高达8.37%。最佳的提取工艺为10倍树皮重量的60%乙醇回流提取2次,每次1h,可以获得超过90%的提取率。结论：建立了山核桃中槲皮苷最佳的提取工艺和含量测定的方法,所建立的体系精确可靠。     

飞龙掌血根皮的生药学鉴别与止血活性考察

目的:开展飞龙掌血根皮的组织切片、粉末显微方面的生药学鉴别研究,以及其止血活性与样品制备方法研究。方法:通过制作飞龙掌血全根横切片,飞龙掌血根皮与根心各自粉末的水装片、透化片、染色片,运用生药学传统鉴别手段完善飞龙掌血全根的组织切片特征,寻找飞龙掌血根皮与根心之间的粉末显微特征。采用小鼠断尾法、毛细玻管法,以出血时间、出血量、凝血时间为指标,考察不同提取方法、不同极性部位对飞龙掌血根皮止血活性的影响。结果:飞龙掌血根皮含有大量石细胞、草酸钙方晶、木栓细胞、油细胞等,飞龙掌血根心含木纤维、草酸钙方晶、网纹纹孔导管等。95%乙醇冷浸提取与50%乙醇回流提取都适合于飞龙掌血根皮提取;冷浸浸膏乙酸乙酯部位止血活性优于石油醚部位和正丁醇部位,冷浸浸膏乙酸乙酯部位按剂量1.50 g·kg-1给药,平均出血时间、出血量、凝血时间依次为(59.67±12.31)s,(4.42±1.67)mg,(79.67±5.57)s。结论:石细胞、木栓细胞、油细胞是飞龙掌血根皮的显微鉴别项目,木纤维是飞龙掌血根心的专有鉴别项目。飞龙掌血根皮的提取应结合乙醇冷浸法和回流法,飞龙掌血根皮具有良好的止血凝血效果,以冷浸提取乙酸乙酯部位止血效果最好。     

Ethanol Extract of Magnolia officinalis Prevents Lipopolysaccharide‐Induced Memory Deficiency via Its Antineuroinflammatory and Antiamyloidogenic Effects

Magnolia bark contains several compounds such as magnolol, honokiol, 4‐O‐methylhonokiol, obovatol, and other neolignan compounds. These compounds have been reported to have various beneficial effects in various diseases. There is sufficient possibility that ethanol extract of Magnolia officinalis is more effective in amyloidogenesis via synergism of these ingredients. Neuroinflammation has been known to play a critical role in the pathogenesis of Alzheimer's disease (AD). We investigated whether the ethanol extract of M. officinalis (10 mg/ kg in 0.05% ethanol) prevents memory dysfunction and amyloidogenesis in AD mouse model by intraperitoneal lipopolysaccharide (LPS, 250 µg/ kg/day for seven times) injection. We found that ethanol extract of M. officinalis prevented LPS‐induced memory deficiency as well as inhibited the LPS‐induced elevation of inflammatory proteins, such as inducible nitric oxide synthase and cyclooxygenase 2, and activation of astrocytes and microglia. In particular, administration of M. officinalis ethanol extract inhibited LPS‐induced amyloidogenesis, which resulted in the inhibition of amyloid precursor protein, beta‐site amyloid‐precursor‐protein‐cleaving enzyme 1 and C99. Thus, this study shows that ethanol extract of M. officinalis prevents LPS‐induced memory impairment as well as amyloidogenesis via inhibition of neuroinflammation and suggests that ethanol extract of M. officinalis might be a useful intervention for neuroinflammation‐associated diseases such as AD. Copyright © 2012 John Wiley & Sons, Ltd.     

Effects of aqueous extracts from Quercus ilex L. root bark, Punica granatum L. fruit peel and Artemisia herba-alba Asso leaves on ethanol-induced gastric damage in rats

The gastroprotective effect of tannic acid and the aqueous extract of Quercus ilex L. root bark, Punica granatum L. fruit peel and Artemisia herba-alba Asso leaves was investigated in the rat against ethanol-induced damage. Tannic acid, Q. ilex and P. granatum extracts gave 100% precipitation of ovine haemoglobin in vitro, whereas A. herba-alba extract was devoid of any protein-binding property. Oral administration of these plant extracts or tannic acid induced a significant decrease in gastric lesions (47.7%-76%). The observed protection was more pronounced when the test solution was given at the same time with ethanol, except for Q. ilex extract. The acid content of the stomach was significantly increased by P. granatum (368%) and A. herba-alba (251%) extracts prepared in ethanol. It is suggested that monomeric and polymeric polyphenols can strengthen the gastric mucosal barrier.     

Investigation of CYP3A4 and CYP2D6 Interactions of Withania somnifera and Centella asiatica in Human Liver Microsomes

Withania somnifera is commonly used as a rejuvenator, whereas Centella asiatica is well known for its anxiolytic and nootropic effects. The present study aims at investigating the effect of crude extracts and principal phytoconstituents of both the medicinal plants with CYP3A4 and CYP2D6 enzyme activity in human liver microsomes (HLM). Phytoconstituents were quantified in the crude extracts of both the medicinal plants using reverse phase HPLC. Crude extracts and phytoconstituents of W. somnifera showed no significant interaction with both CYP3A4 and CYP2D6 enzymes in HLM. Of the crude extracts of C. asiatica screened in vitro, methanolic extract showed potent noncompetitive inhibition of only CYP3A4 enzyme (Ki—64.36 ± 1.82 µg/mL), whereas ethanol solution extract showed potent noncompetitive inhibition of only CYP2D6 enzyme (Ki—36.3 ± 0.44 µg/mL). The flavonoids, quercetin, and kaempferol showed potent (IC₅₀ values less than 100 μM) inhibition of CYP3A4 activity, whereas quercetin alone showed potent inhibition of CYP2D6 activity in HLM. Because methanolic extract of C. asiatica showed a relatively high percentage content of quercetin and kaempferol than ethanol solution extract, the inhibitory effect of methanolic extract on CYP3A4 enzyme activity could be attributed to the flavonoids. Thus, co‐administration of the alcoholic extracts of C. asiatica with drugs that are substrates of CYP3A4 and CYP2D6 enzymes may lead to undesirable herb‐drug interactions in humans. Copyright © 2015 John Wiley & Sons, Ltd.     

白花蛇舌草中熊果酸的透皮吸收试验

目的:考察白花蛇舌草中熊果酸的透皮吸收特性.方法:采用HPLC测定熊果酸含量.选择SD大鼠背部皮肤,通过Franz垂直扩散池考察熊果酸的透皮性能,并考察氮酮(azone)、桉叶油、冰片、白花蛇舌草水提取物和醇提取物对熊果酸透皮吸收的影响.结果:熊果酸很难透过皮肤,需加入透皮吸收促进剂才能有效地透过皮肤.不同质量分数促进剂对熊果酸促透作用顺序为5％醇提物＞5％醇提物+2％冰片＞5％水提物＞ 2％ azone+ 10％丙二醇(PG)＞2％桉叶油＞4％ azone ＞3％桉叶油＞ 2％ azone＞ 1％ azone.结论:Azone和桉叶油是白花蛇舌草中熊果酸的良好促透剂,复方水提取物和醇提物具有协同促透的作用.     

Antioxidant/Antibacterial Activities of a Topical Phytopharmaceutical Formulation Containing a Standardized Extract of Baccharis incarum,an Extremophile Plant Species from Argentine Puna

The antimicrobial and antioxidant activities of standardized extracts of Baccharis incarum in 60° and 80° ethanol and of a phytopharmaceutical formulation obtained from them were measured. Baccharis tinctures showed antimicrobial activity against clinically isolated antibiotic resistant Staphylococcus aureus and Enterococcus faecalis, with MIC values of 40–80 µg GAE/mL. Both tinctures exhibited ABTS^●+ scavenging activity with SC₅₀ values between 1.6 and 4.0 µg GAE/mL. The tinctures were not genotoxic in the Salmonella assay. For this reason, the tincture in 60° ethanol was incorporated into a topical pharmaceutical formulation (Hydrogel/ Carbopol® 934). The phytopharmaceutical formulation also showed antibacterial and antioxidant activities in the in vitro assays. The hydrogel showed microbiological, chemical, physical and functional stability during storage at room temperature. Studies that measure drug release as a determination of bioavailability were also carried out using the Franz diffusion cell (FC). The results demonstrated the release of two bioactive compounds (chlorogenic acid and 4′,5‐dihydroxy‐3′,3,6,7,8‐pentamethoxyflavone) from the phytotherapic preparation in HPLC studies of FC receptor solution. In consequence, the phytopreparation applied topically could be used to treat skin and soft tissue infection produced by methicillin‐resistant Staphylococcus aureus (MRSA) or Enterococcus faecalis and opens new opportunities for the use of active natural ingredients in the cosmeceutical field as antiacne and antioxidant. Copyright © 2012 John Wiley & Sons, Ltd.     

Effect of alcohol extract of Annona muricata on cold immobilization stress induced tissue lipid peroxidation

Administration of an ethanol extract of the stem bark of Annona muricata significantly inhibited cold immobilization stress-induced increase in lipid peroxidation in the liver and brain of albino rats. © 1997 John Wiley & Sons, Ltd.     

泽泻降血尿酸乙醇提取物的提取工艺研究

目的:筛选泽泻降血尿酸乙醇提取物的最佳提取工艺。方法:采用正交试验设计,以泽泻所含泽泻醇B23-乙酸酯为指标,考察乙醇浓度、提取时间、提取次数和乙醇用量等4种因素对提取结果的影响。泽泻醇B23-乙酸酯和血尿酸的含量均用HPLC法测定。结果:只有提取次数对泽泻乙醇提取物的泽泻醇B23-乙酸酯含量有显著影响。结论:泽泻降血尿酸乙醇提取物的最佳制备工艺为7倍药材量的70%乙醇提取2次,每次提取1 h。该提取工艺合理、可行。     

D101大孔树脂对丹酚酸B分离工艺的优化

 目的探讨D101树脂对丹酚酸B分离的最佳工艺。方法丹参提取液经过D101树脂吸附后,以不同乙醇浓度溶液洗脱,采用HPLC测定丹酚酸B的含量。一次正交试验考察丹参提取液浓度、树脂用量、时间等对树脂吸附的影响;二次正交试验考察乙醇浓度、洗脱液用量、流速等对树脂解吸的影响;并绘制丹酚酸B的洗脱曲线。结果树脂用量对丹酚酸B吸附量影响显著,最佳吸附条件为:药材树脂比1:3、色谱柱径高比1:5、药液浓度为原液、上样时间24 h;最佳解吸条件根据考察指标有所不同,以得率为指标时最佳条件为:乙醇浓度70%、洗脱速度2 mL·min^-1、洗脱液用量12倍柱体积;以纯度为指标时最佳条件为:乙醇浓度70%、洗脱速率0.5 mL·min^-1、洗脱液用量8倍柱体积;提高乙醇浓度有利于解吸。结论D101树脂可作为分离丹酚酸B较好分离材料,优化的分离工艺是可行的。     

姜黄不同提取部位对姜黄素的稳定作用

目的：研究了中药姜黄不同提取部位对纯姜黄素稳定性的影响,揭示中药姜黄中存在着对姜黄素产生稳定作用的物质。方法：将姜黄的水、乙醇、丙酮、乙醚、醋酸乙酯、石油醚等不同部位的提取物,定量加入到纯姜黄素溶液中,高效液相色谱法测定姜黄素浓度的变化,采用动力学方法建立姜黄素降解速率方程。结果：姜黄的乙醇、丙酮、乙醚、醋酸乙酯等提取部位均能降低姜黄素的降解速率。80%的乙醇提取物对姜黄素的稳定作用最强。结论：在制备姜黄素制剂时,选用姜黄的醇提物,在相同的条件下与纯姜黄素比较,可增加姜黄素的稳定性。     

Gastroprotective effect of aqueous stem bark extract of Ziziphus jujuba L.against HCl/Ethanol-induced gastric mucosal injury in rats

OBJECTIVE: To evaluated the gastroprotective effects of standardized aqueous extract of Ziziphus jujuba(Z. jujuba) stem bark against acidified ethanol-induced gastric ulcers as well as anti helicobacter pylori activity of the plant extract in rats.METHODS: Five groups of rats were orally pre-treated with normal saline(0.9%) as ulcer group, 150 mg/kg of ranitidine as positive control group, 100, 200 and 400 mg of standardized extract solution as the experimental groups. Two hours later, acidified ethanol solution was given by gavages in order to induce of gastric ulcer. The antibacterial effect of extract against clinical strains of Helicobacter pylori(H. pylori) was evaluated through disc diffusion test.RESULTS: The ulcer group exhibited significantly severe mucosal injury as compared with ranitidine or extract group which shows significant protective action against gastric mucosal injury. The extract showed no effect on H. pylori.CONCLUSION: The present study indicates that Z.jujuba stem bark extract had a potential antiulcer activity which might be due to its protective activity, providing a direct, protective effect on the gastric mucosa. Our study showed that anti-H. pylori activity was not among gastroprotective mechanism of Z. jujuba. Further pre-clinical and clinical investigations for evaluating natural active agents and efficacy of this plant are recommended.     

An In Vitro and Molecular Informatics Study to Evaluate the Antioxidative and β‐hydroxy‐β‐methylglutaryl‐CoA Reductase Inhibitory Property of Ficus virens Ait

The present study is initially intended to evaluate antioxidant and β‐hydroxy‐β‐methylglutaryl‐CoA reductase (HMGR) inhibitory property of Ficus virens Ait., first by in vitro analyses followed by a corroboratory molecular informatics study. Our results show that of all the sequentially extracted fraction of F. virens bark and leaves extract, F. virens bark methanol extract exhibits strong radical scavenging, antioxidant and oxidative DNA damage protective activity, which is well correlated with its total phenolic content. In addition, F. virens bark methanol extract, which is non‐cytotoxic, significantly and non‐covalently inhibit the HMGR activity (IC₅₀ = 3.45 ± 0.45 µg/ml) in comparison with other extracts. The mechanistic aspect of this inhibition activity is authenticated by molecular docking study of bioactive compounds as revealed from gas chromatography–mass spectrometry data, with HMGR. The analysis for the first time indicates that quinic acid (ΔG: ?8.11 kcal/mol) and paravastatin (ΔG: ?8.22 kcal/mol) exhibit almost same binding energy, while other compounds also showed good binding energy, suggesting that quinic acid alone or in combination with other major bioactive compound is probably responsible for HMGR inhibitory property of the extract and plausibly can be used in in vivo system for the management, prevention, and alleviation of hypercholesterolemia as well as hypercholesterolemia‐induced oxidative stress. Copyright © 2013 John Wiley & Sons, Ltd.     

土茯苓降血尿酸乙醇提取物的提取工艺研究

目的:筛选土茯苓降血尿酸乙醇提取物的最佳提取工艺。方法:采用正交试验设计,以土茯苓所含落新妇苷为指标,考察乙醇浓度、提取时间、提取次数和乙醇用量的4种因素对提取结果的影响。落新妇苷和血尿酸含量均采用HPLC法测定。结果:提取次数、提取时间和乙醇浓度对以落新妇苷为指标的提取率都有显著的影响。结论:土茯苓降血尿酸乙醇提取物的最佳工艺是7倍药材量的90%乙醇提取2次,每次2.0h。该提取工艺合理、可行。     

Extract from Ceratonia siliqua Exhibits Depigmentation Properties

Skin hyper‐pigmentation is a condition initiated by the overproduction of melanin existing in the melanocytes. Melanin pigment is responsible for the colour of skin in humans. It is formed through a series of oxidative reactions involving the amino acid tyrosine in the presence of the key enzyme tyrosinase. In continuation with our efforts to identify tyrosinase inhibitors from plants sources, the methanol extract from leaf, bark and fruit of Ceratonia siliqua were screened for tyrosinase inhibition and diphenolase activity. The bark extract exhibited significant inhibition on mushroom tyrosinase using L‐tyrosine as a substrate and showed diphenolase activity. The extract further significantly lowered tyrosinase mRNA levels in B16‐F10 mouse melanocytes. Bioassay‐guided fractionation led to the isolation of six compounds. Compounds (?)‐epicatechin‐3‐O‐gallate, 1,2,3,6‐tetra‐O‐galloyl‐ß‐D‐glucose and gallocatechin‐3‐O‐gallate showed tyrosinase inhibitions with the IC₅₀ values of 27.52, 83.30 and 28.30 µg/mL, respectively. These compounds also exhibited L‐DOPA activities with IC₅₀ values of >200, 150 and 200 µg/mL, respectively. A clinical study was conducted using 20 volunteers in a patch testing trial for irritancy potential and skin depigmentation. The clinical results showed the sample to be non‐irritant with irritancy potential of ?34.21 and depigmentation trial showed an improvement in the even skin tone of UV induced pigmentation at 3% after 28 days of application. Copyright © 2015 John Wiley & Sons, Ltd.