Pharmacological activities investigation of crude extracts and fractions from Qualea grandiflora Mart

This study investigates pharmacological activities of crude hydroalcoholic extract and fractions of Qualea grandiflora Mart. leaves employing different experimental models using mice. The treatment with crude hydroalcoholic extract (EH) in a dose of 500 mg/kg, i.p. caused: signs of central nervous system depressant action in the Hippocratic screening test, confirmed by the potentiation of sodium pentobarbital sleeping time. Increasing in the latency time of hot plate assay that indicate an analgesic effect; significantly delaying of the onset of clonic PTZ convulsions, increasing in the time for death, suppressing of the tonic PTZ convulsion, and decreasing of severity and number of convulsions. The median lethal dose of EH was 1.321 mg/kg. The convulsions induced by PTZ, ethyl ether fraction (300 mg/kg, i.p.) was more active in increasing the latency time for first convulsion, moreover, the hexane fraction, at the same dose, was more active in increasing the time for death and/or avoiding the death. Both did not cause disturbance in motor coordination at the dose of 500 mg/kg, assessed by rotarod test. These results suggest that the crude extract of leaves of Qualea grandiflora Mart. has a central nervous system depressant action, an analgesic effect and behave as a potential anticonvulsant.     

Anti-inflammatory and analgesic properties of the leaf extracts and essential oil of Lavandula angustifolia Mill

Extracts obtained from the leaves of Lavandula angustifolia Mill. (Lamiaceae) are used in Iranian folk medicine as remedies for the treatment of various inflammatory diseases. For evaluation of its probable analgesic and anti-inflammatory effects, hydroalcoholic extract, polyphenolic fraction and essential oil of the leaves of the herb were prepared and their analgesic effects were studied in mice using formalin and acetic acid-induced writhing tests. Carrageenan test in rats was used for assessment of anti-inflammatory activity of above-mentioned fractions. Results showed that while the hydroalcoholic extract (400-1600 mg/kg, p.o.) inhibited only the second phase of formalin test, the polyphenolic fraction (800 and 1600 mg/kg, p.o.) and essential oil (100 and 200 mg/kg, p.o.) suppressed both phases. In acetic acid-induced writhing test, polyphenolic fraction (400 and 800 mg/kg, p.o.) and essential oil (100 and 200 mg/kg, p.o.) reduced the number of abdominal constrictions. Essential oil at a dose of 200mg/kg also inhibited carrageenan-induced paw edema. Results of the present study confirm the traditional use of Lavandula angustifolia for the treatment of painful and inflammatory conditions and calls for further investigations to determine the active chemical constituent(s).     

木香降血糖有效部位及有效成分研究

目的筛选木香中降血糖活性部位及主要成分。方法制备木香乙醇提取物,乙醇提取物醋酸乙酯部位、正丁醇部位和水提取部位;用HepG2细胞消耗葡萄糖模型和四氧嘧啶致糖尿病小鼠模型测定各提取物的降血糖活性;降血糖活性强的醋酸乙酯部位用柱色谱法继续分离、精制,得2个化合物,经NMR等鉴定化合物结构;并对2个化合物进行降血糖活性研究。结果木香醋酸乙酯部位有较强的降血糖作用,从木香醋酸乙酯部位中分离得到木香烃内酯和去氢木香内酯,且两者均可降低四氧嘧啶所致糖尿病小鼠的血糖,并显示很好的抗氧化作用。结论木香烃内酯和去氢木香内酯可能是木香的降血糖活性成分,抑制氧化应激从而减轻胰岛素抵抗可能是其降血糖机制。     

The hypoglycaemic activity of Swertia japonica extract in streptozotocin induced hyperglycaemic rats

The hypoglycaemic activity of an aqueous ethanolic extract of Swertia japonica and its ethyl acetate, n-butanol, water soluble fractions, together with ether soluble and insoluble fractions of ethyl acetate soluble fraction was observed in streptozotocin (STZ) induced hyperglycaemic rats. It was found that an aqueous ethanolic extract was more effective than a mixture of tolbutamide and buformine, and an ethanolic extract of another species of this plant, S. chirayita in lowering the blood glucose level under similar experimental conditions. Furthermore, an ethyl acetate soluble fraction of S. japonica and its ether insoluble fraction showed a potent hypoglycaemic activity.     

Antiulcer action of the hydroalcoholic extract and fractions of Davilla rugosa Poiret in the rat

Davilla rugosa Poiret ("Cipó- Caboclo") is commonly used in Brazilian folk medicine. The hydroalcoholic extract of the stems (HE) was fractionated with chloroform (CF), chloroform/ethyl acetate (CAF), ethyl acetate (AF), ethyl acetate/ethanol (AEF), ethanol (EF), and ethanol/water (EWF). The hydroalcoholic extract (HE) and fractions of the stems of D. rugosa Poiret were investigated for possible anti gastric ulcer properties. These extracts were shown to protect rats from developing gastric ulcers induced by two acute models: HCl/ethanol (400 mg/kg i.p.) and immersion-restraint stress (15 and 30 mg/kg of the HE and 15 mg/kg either of the ethanol or the ethanol/water fractions, p.o.). The daily oral dose of 800 mg/kg of HE for 30 consecutive days was tested for possible toxic effects. There were no modifications in body weight, water or food intake or in the external aspect of kidneys, spleen, lungs and liver. The only difference observed was a decrease of liver weight. These results suggest that the D. rugosa Poiret HE has an antiulcer activity in rats and the active components are in the two more polar fractions.     

Antinociceptive and anti-inflammatory effects of Satureja hortensis L. extracts and essential oil

Satureja hortensis L. (Lamiaceae) is a medicinal plant used in Iranian folk medicine as muscle and bone pain reliever. In the present study, hydroalcoholic extract, polyphenolic fraction and essential oil of the aerial parts of the herb were prepared and evaluated for the analgesic activity using light tail flick, formalin and acetic acid-induced writhing in mice. Also, the anti-inflammatory effects of the above-mentioned preparations were assessed using carrageenan-induced paw edema in rats. Results showed that in the light tail flick test neither the essential oil nor the extracts could exert any significant effect. The hydroalcoholic extract (2000 mg/kg, p.o.) and the essential oil (200 mg/kg, p.o.) inhibited the mice writhing responses caused by acetic acid. In formalin test, hydroalcoholic extract (500-2000 mg/kg, p.o.), polyphenolic fraction (250-1000 mg/kg, p.o.) and the essential oil (50-200 mg/kg, p.o.) showed analgesic activity and pretreatment with naloxone (1 mg/kg, i.p.) or caffeine (20 mg/kg, i.p.) failed to reverse this antinociceptive activity. Polyphenolic fraction (1000 mg/kg, p.o.) and the essential oil (200 mg/kg) reduced edema caused by carrageenan. These results suggest that S. hortensis L. has antinociceptive and anti-inflammatory effects and probably mechanism(s) other than involvement of opioid and adenosine receptors mediate(s) the antinociception.     

Central effects of isolated fractions from the root of Petiveria alliacea L. (tipi) in mice

Ethnopharmacological relevance

Petiveria alliacea L. (tipi) a shrub from Phytolaccaceae family is popularly used in folk medicine for treating a wide variety of disorders in South and Central America.

Aim of the study

To investigate the neuropharmacological properties on experimental animals.

Materials and methods

The acetate (FA), hexanic (FH), hydroalcoholic (FHA) and precipitated hydroalcoholic (FHAppt) fractions from the root of tipi were studied to investigate its pharmacological properties in the classical behavioral models (open-field, elevated plus maze-EPM, rotarod, barbiturate-induced sleeping time, forced swimming and pentylenetetrazole (PTZ)-induced convulsions tests) using mice. These fractions were administered intraperitoneally and orally to female mice at single doses of 100 and 200 mg/kg.

Results

All these fractions decreased the locomotor activity, rearing and grooming in the open-field test, suggesting a possible central depressant action. No significant effect was evident on motor coordination of the animals in the rotarod test. On EPM, all the fractions of tipi presented a significant reduction on the time of permanence in the open arms, indicating an absence of anxiolytic-like effect. In addition, the fractions increased the immobility time in the forced swimming test and potentiated pentobarbital-induced sleeping time in mice, confirmed a probable sedative and central depressant effect. Furthermore, the fractions increased the latency to the first convulsion and the lethal time of the PTZ-induced convulsions test in the animals, confirmed its popular use as anticonvulsant.

Conclusion

Our results suggest that the fractions of P. alliacea L. contains biologically active substance(s) that might be acting in the CNS and have significant depressant and anticonvulsant potentials, supporting folk medicine use of this plant.     

Anticonvulsive activity of Albizzia lebbeck, Hibiscus rosa sinesis and Butea monosperma in experimental animals

The ethanolic extracts of leaves of Albizzia lebbeck and flowers of Hibiscus rosa sinesis and the petroleum ether extract of flowers of Butea monosperma exhibited anticonvulsant activity. The bioassay guided fractionation indicated that the anticonvulsant activity lies in the methanolic fraction of chloroform soluble part of ethanolic extract of the leaves of A. lebbeck, acetone soluble part of ethanolic extract of H. rosa sinesis flowers and acetone soluble part of petroleum ether extract of B. monosperma flowers. The fractions protected animals from maximum electro shock, electrical kindling and pentylenetetrazole-induced convulsions in mice. The fractions also inhibited convulsions induced by lithium-pilocarpine and electrical kindling. However, they failed to protect animals from strychnine-induced convulsions. The fractions antagonised the behavioral effects of D-amphetamine and potentiated the pentobarbitone-induced sleep. The fractions raised brain contents of gamma-aminobutyric acid (GABA) and serotonin. These fractions were found to be anxiogenic and general depressant of central nervous system.     

Topical anti-inflammatory activity of Serjania erecta Radlk (Sapindaceae) extracts

Serjania erecta Radlk (Sapindaceae), commonly called cinco-folhas or cipó-cinco-folhas in Brazil, is thought to be effective for treating several inflammatory diseases. In order to verify the topical anti-inflammatory effect of Serjania erecta, hydroalcoholic extract and fractions were obtained by extraction in solvents of increasing polarity and were tested in mouse models using croton-oil-induced inflammation. Our findings showed that topical application of Serjania erecta hydroalcoholic extract (0.01-3.0 mg/ear), and the dichloromethane (0.03-1.0 mg/ear), ethyl acetate (0.03-1.0 mg/ear), and hexane (0.003-1.0 mg/ear) fractions revealed significant activity, causing a dose-dependent reduction of croton-oil ear edema (ID(50)=0.14 mg/ear, 0.23 mg/ear, 0.14 mg/ear, 0.04 mg/ear, respectively). The extract and all tested fractions also decreased tissue myeloperoxidase activity (indicative of polymorphonuclear leukocytes influx) in mouse-ears treated with croton oil with a maximum inhibition of 72% at 3.0 mg/ear for the hydroalcoholic extract and 81%, 78%, and 83% at 1.0mg/ear for dichloromethane, ethyl acetate and hexane fractions, respectively. As expected, dexamethasone (0.05 mg/ear) was effective in inhibiting both edema and myeloperoxidase activity (99% and 82%, respectively). In conclusion, our results indicate a topical anti-inflammatory effect for the species of Serjania studied.     

白及不同提取部位抗耐甲氧西林金黄色葡萄球菌的体内外活性

目的:研究白及对“超级细菌”——耐甲氧西林金黄色葡萄球菌(MRSA)的抑菌作用及活性部位.方法:规范提取白及乙酸乙酯部位、正丁醇部位、萃取后水部位、醇提后水煎液部位等4个部位,采用琼脂平板二倍稀释法测定以上4个部位对金黄色葡萄球菌(MSSA)及MRSA共6株病原菌的MIC;用白及乙酸乙酯部位以两种给药方式对小鼠进行预防给药,测定白及对MRSA感染SPF小鼠的保护力.结果:乙酸乙酯部位和正丁醇部位对受试病原菌均具明显抑菌活性,4个部位中尤以乙酸乙醇部位的抑菌活性最强,其MIC为0.065 ～0.26 g·L-1;且白及乙酸乙酯部位对MRSA感染小鼠有很强的保护作用,其中尤以ip0.5 g·kg-1的保护达到100％.结论:白及对MSSA和MRSA有明显的抑菌作用,乙酸乙酯部位是其主要的活性部位.     

Antidiabetic potential of unripe Carissa carandas Linn. fruit extract

Ethnopharmacological relevance

Carissa carandas commonly known as Karanda have a long history of use in traditional system of medicine. It is used by tribal healers of Western Ghat region of Karnataka as hepatoprotective and antihyperglycemic. However, no scientific data is available to validate the folklore claim. The present study has been designed to evaluate its unripe fruit for the antidiabetic activity.

Aim

In the present study, methanol extract of unripe fruits and its fractions were studied for its antidiabetic potential.

Materials and methods

The methanol extract and its fractions were screened for antidiabetic activity in alloxan induced diabetic rats. The polyphenolic, flavonoid and flavanone contents of methanolic extract and its fractions were also determined and correlated with its antidiabetic activity.

Results

The experimental data indicated that the methanol extract and its ethyl acetate soluble fraction has significantly lowered the elevated blood glucose levels by 48% (p < 0.001) and 64.5% (p < 0.001) respectively at dose level of 400 mg/kg per oral after 24 h as compared to diabetic control. In order to assess the role of polyphenolic components in the relevant activity, polyphenolic and flavonoid contents were determined. The polyphenolic and flavonoid content of methanol extract and its ethyl acetate soluble fraction were found to be 15.8 ± 1.2 mg and 18.55 ± 0.34 mg (gallic acid equivalent/g extract) and flavonoid content 2.92 ± 0.03 mg and 1.534 ± 0.30 mg (rutin equivalent/g extract) respectively.

Conclusion

The increased antidiabetic potential of ethyl acetate fraction over methanol extract is due to its partial purification achieved by fractionation which resulted in increase in degree of polymerization and segregation of secondary metabolites.     

Procyanidin-rich fractions from Parkia biglobosa (Mimosaceae) leaves cause redox-sensitive endothelium-dependent relaxation involving NO and EDHF in porcine coronary artery

Aim of the study

Parkia biglobosa leaves are traditionally used as an antihypertensive agent in Benin. The present study assessed the vasorelaxant activity of different Parkia biglobosa leaf extracts using isolated porcine coronary artery rings.

Materials and methods

A hydroalcoholic leaf extract was submitted to a multi-step liquid-liquid fractionation with solvents of increasing polarity and the polyphenolic content of the different fractions was analyzed. Vascular reactivity of the different extracts was assessed using porcine coronary artery rings, in the presence or absence of specific pharmacological inhibitors.

Results

The hydroalcoholic, ethyl acetate and butanolic extracts contained mainly procyanidins and monomeric flavonoids. Parkia biglobosa leaf crude extract induced a redox-sensitive endothelium-dependent relaxation mediated by both nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF). The fractionation of the butanolic extract generated 6 fractions, two of which induced stronger vasorelaxation than the original extract and they had a higher phenolic content.

Conclusions

Parkia biglobosa leaf extract is able to induce endothelium-dependent NO- and EDHF-mediated relaxation in porcine coronary artery rings. The vasorelaxant activity is dependent on their phenolic content and appears to involve mainly procyanidins.     

Antioxidant and Anti‐α‐glucosidase Compounds from the Rhizome of Peltiphyllum peltatum (Torr.) Engl

The antioxidant, anti‐α‐glucosidase and anticholinesterase effects of the alcohol extract of fresh underground rhizomes of Peltiphyllum peltatum were studied. A potent antioxidant activity accompanied by a selective α‐glucosidase effect was observed for the crude extract. Further activity‐guided fractionation (petroleum ether, chloroform, ethyl acetate, n‐butanol and water) resulted in the identification of the ethyl acetate fraction with the highest antioxidant effect. Gallic acid, methyl‐3‐O‐methyl gallate, catechin, gallocatechin, bergenin and 11‐O‐galloylbergenin were isolated from the ethyl acetate fraction. While all the isolated compounds did show a variable degree of radical scavenging effect, 11‐O‐galloylbergenin was identified as the selective α‐glucosidase inhibitor. The isolation, structural elucidation and biological effects of these compounds are discussed. Copyright © 2012 John Wiley & Sons, Ltd.     

茜草炭不同极性部位化学成分组成及保护氧化损伤活性比较

采用氧化低密度脂蛋白(ox-LDL)诱导的人脐静脉内皮细胞(HUVECs)损伤模型,MTT比色法测定细胞活力,评价茜草炭不同极性部位提取物的抗氧化损伤活性,同时采用超高效液相色谱与串联四级杆飞行时间质谱联用技术(UPLC-QTOF-MS)对各极性部位化学成分进行定性研究。结果显示,乙酸乙酯部位与正丁醇部位均可显著提高细胞活力(P0.01),石油醚部位对细胞活力影响不大,水提取部位对损伤的HUVECs有一定的抑制作用。UPLC-Q-TOF-MS分析结果显示,从茜草炭4个极性部位提取物中共鉴定化合物32种,包括31种醌类及其糖苷类和1个烯萜(茜草哌唑嗪C),石油醚部位、乙酸乙酯部位、正丁醇部位、水提取部位分别鉴定出化合物23,32,26,15种。关联体外细胞实验结果表明,乙酸乙酯部位和正丁醇部位为茜草炭抑制ox-LDL诱导HUVECs损伤的有效部位,为阐明茜草炭的药效物质基础提供科学依据,为茜草炭功效-物质相关性研究奠定基础。     

Pharmacological basis for use of Lychnophora trichocarpha in gouty arthritis: anti-hyperuricemic and anti-inflammatory effects of its extract, fraction and constituents

Ethnopharmacological relevance

The ethanolic extract of Lychnophora trichocarpha Spreng. is used in Brazilian folk medicine to treat bruise, pain and inflammatory diseases.

Aim of the study

The present study aimed at investigating whether ethanolic extract of L. trichocarpha, its ethyl acetate fraction and its main bioactive compounds could be useful to treat gouty arthritis by countering hyperuricemia and inflammation.

Materials and methods

L. trichocarpha ethanolic extract (LTE), ethyl acetate fraction from ethanolic extract (LTA) and isolated compounds were evaluated for urate-lowering activity and liver xanthine oxidase (XOD) inhibition in oxonate-induced hyperuricemic mice. Anti-inflammatory activity in monosodium urate crystal-induced paw oedema, an experimental model of gouty arthritis, was also investigated.

Results

Crude ethanolic extract and its ethyl acetate fraction showed significant urate-lowering effects. LTE was also able to significantly inhibit liver xantine oxidase (XOD) activity in vivo at the dose of 250 mg/kg. Luteolin, apigenin, lupeol, lychnopholide and eremantholide C showed the anti-hyperuricemic activities among tested compounds. Apigenin also showed XOD inhibitory activity in vivo. Luteolin, lychnopholide, lupeol and eremantholide C, in turn, did not shown significant inhibitory activity towards this enzyme, indicating that this mechanism is not likely to be involved in urate-lowering effects of those compounds. LTE, LTA, lupeol, β-sitosterol, lychnopholide, eremantholide, luteolin and apigenin were also found to inhibit monosodium urate crystals-induced paw oedema in mice.

Conclusions

Ethanolic extract of Lychnophora trichocarpha and some of its bioactive compounds may be promising agents for the treatment of gouty arthritis since they possesses both anti-hiperuricemic and anti-inflammatory properties.     

甘草中-葡α萄糖苷酶抑制剂的初步研究

目的：从甘草中提取分离α-葡萄糖苷酶抑制剂。方法：将甘草水提取物依次用石油醚、乙酸乙酯、正丁醇萃取，然后测定各部分的酶抑制活性，对活性最强的部分进行酶抑制动力学研究。结果：石油醚部分、乙酸乙酯部分、正丁醇部分与剩余水提物部分的酶活性抑制率分别为68．93％、83．02％、32．17％和10．79％，与综合水提取物的酶活性抑制率69．77％相比，乙酸乙酯部分的活性最强，而且乙酸乙酯部分表现为一种快速的剂量依赖性的竞争性抑制类型，其Ki=34μg／ml。结论：乙酸乙酯部分存在较强的α-葡萄糖苷酶抑制活性成分，对其作进一步分离可望得到α-葡萄糖苷酶抑制单体成分。     

青葙子提取物降血糖活性的研究

 目的研究青葙子提取物对四氧嘧啶糖尿病小鼠降血糖作用。方法采用体积分数95%乙醇和水连续浸提青葙子获得醇提(A)和水提浸膏(B)。醇提浸膏用石油醚、醋酸乙酯、正丁醇连续萃取,获得不同部分。水提物采用3倍乙醇沉淀分为醇溶部分和粗多糖。尾静脉注射四氧嘧啶建立小鼠糖尿病模型,给予青葙子提取物灌胃,1 g·kg^-1或800 mg·kg^-1,连续3周, 测定血糖、血清中胰岛素含量及饮水量和耗食量,测定小鼠肝、肾、脾和胰腺重量指数。结果青葙子醇提物和水提物均有一定降血糖活性,其中醇提物的正丁醇部分(A-c)和水提物中粗多糖部分(B-b)具有显著降血糖活性,粗多糖部分具有明显促进胰岛素分泌作用,效果优于格列本脲(2 mg·kg^-1)。A-c和B-b能使四氧嘧啶引起的糖尿病小鼠肾脏和肝脏的肿胀恢复接近正常。结论青葙子提取物时四氧嘧啶糖尿病小鼠具有降血糖作用。     

淡豆豉抗菌活性及化学成分分析

目的:研究传统发酵中药淡豆豉的抗菌活性及化学成分。方法:淡豆豉80%乙醇提取物用适量蒸馏水混悬,依次用石油醚、乙酸乙酯及水饱和正丁醇萃取,得石油醚、乙酸乙酯、正丁醇萃取部分及水层,利用体外抗菌法筛选和追踪抗菌活性部分,采用硅胶柱色谱等方法及制备HPLC对抗菌活性最强部分进行分离纯化,得单体化合物,并根据化合物的理化性质和1H-NMR,13C-NMR,MS等波谱数据鉴定其结构。结果:淡豆豉80%乙醇提取物的乙酸乙酯萃取部分显示最强的抗菌活性,该有效部分对呼吸道致病菌及其他常见致病菌均显示较强的抗菌活性,正丁醇萃取部分和石油醚萃取部分次之。从乙酸乙酯萃取部分分离得到18个化合物,鉴定了其中11个化合物的化学结构,分别为大豆素(1),大豆苷(2),染料木素(3),染料木苷(4),黄豆黄素(5),黄豆黄苷(6),胡萝卜苷(7),胸腺嘧啶(8),腺嘌呤(9),尿嘧啶(10),尿苷(11)。结论:淡豆豉80%乙醇提取物的乙酸乙酯萃取部分抗菌效果明显。化合物1～6为异黄酮类;化合物7～11为首次从该药材中分离得到。     

栀子降尿酸有效部位研究

目的:确定栀子降尿酸作用有效部位.方法:用系统溶剂法提取分离得到4个部位,分别为石油醚部位、乙酸乙酯部位、正丁醇部位和水液部位,采用氧嗪酸钾盐诱导的小鼠急性高尿酸血症模型,研究栀子总提物和4个部位对高尿酸血症小鼠血清尿酸水平和肝脏黄嘌呤氧化酶的影响.结果:栀子总提物组、乙酸乙酯组和水组具有较好的降尿酸作用,栀子总提物组、石油醚组和水组能够较好的抑制黄嘌呤氧化酶的活性.栀子总提取物和各部位提取物对正常小鼠血清尿酸水平没有显著影响.结论:栀子乙酸乙酯提取部位和水液部位为降尿酸活性部位,其降尿酸作用部分机制是通过抑制黄嘌呤氧化酶的活性.     

Evaluation of the analgesic action of different fractions from the methanol extract of Teucrium buxifolium L

Different fractions (F-2, F-3, F-5) of the methanol extract from Teucrium buxifolium L. have been tested for their analgesic activity in mice. All of them exhibited peripheral analgesic activity except F-3. Fraction F-5 had the strongest effect and was subjected to a second re-extraction. The subfractions obtained (F-5/3 and F-5/8) exhibited a similar activity to that observed with the whole fraction. Copyright © 1998 John Wiley & Sons, Ltd.