Effects of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall on caecal amoebiasis in mice

The anti-amoebic effects of crude methanol extracts of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall against Entamoeba histolytica infecting the caecum of mice were studied. Caecal amoebiasis in mice was induced by injection of Entamoeba histolytica trophozoites directly into the caecum. The mice were then treated orally with the extract, a standard drug (metronidazole), or vehicle p.o. for five consecutive days, beginning 24 h after the infection and were examined on the sixth day. At a dose of 1000 mg/kg per day, the extracts of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall had a curative rate of 100, 40 and 26%, respectively. At a concentration of 500 and 250 mg/kg/day, extract from Piper longum fruit was still effective in 93 and 46% of the cases, respectively, while extract from Piper sarmentosum root at a dose of less than 1000 mg/kg per day did not cure any mice from amoebiasis. Extract of Quercus infectoria nut gall at a concentration of 500 and of 250 mg/kg per day cured 26 and 13% of mice, respectively. Metronidazole at a concentration of 125 and of 62.5 mg/kg per day had a curative rate of 100 and 60%, respectively. The severity of caecal wall ulceration was reduced in mice which received the extract and metronidazole as compared to the control animals.     

Antiamoebic activity of Piper longum fruits against Entamoeba histolytica in vitro and in vivo

The fruits of Piper longum used in traditional remedies against intestinal distress have been tested for their efficacy against experimental caecal amoebiasis of rats. The ethanolic extract, hexane fraction, n-butanol soluble fraction exerted in vitro amoebicidal action at 1000 μg/ml and the chloroform fraction at 500 μg/ml. The ethanolic extract and piperine, a pure compound, from this plant material cured 90% and 40% of rats with caecal amoebiasis, respectively.     

The antiamoebic effect of a crude drug formulation of herbal extracts against Entamoeba histolytica in vitro and in vivo

The antiamoebic effect of a crude drug formulation against Entamoeba histolytica was studied. In the traditional system of medicine in India, the formulation has been prescribed for intestinal disorders. It comprises of five medicinal herbs, namely, Boerhavia diffusa, Berberis aristata, Tinospora cordifolia, Terminalia chebula and Zingiber officinale. The dried and pulverized plants were extracted in ethanol together and individually. In vitro amoebicidal activity was studied to determine the minimal inhibitory concentration (MIC) values of all the constituent extracts as well as the whole formulation. The formulation had a MIC of 1000 μg/ml as compared with 10 μg/ml for metronidazole. In experimental caecal amoebiasis in rats the formulation had a curative rate of 89% with the average degree of infection (ADI) reduced to 0.4 in a group dosed with 500 mg/kg per day as compared with ADI of 3.8 for the sham-treated control group of rats. Metronidazole had a cure rate of 89% (ADI = 0.4) at a dose of 100 mg/kg per day and cured the infection completely (ADI = 0) when the dosage was doubled to 200 mg/kg per day. There were varying degrees of inhibition of the following enzyme activities of crude extracts of axenically cultured amoebae: DNase, RNase, aldolase, alkaline phosphatase, acid phosphatase, α-amylase and protease.     

Cytotoxicity and in vitro susceptibility of Entamoeba histolytica to Morinda morindoides leaf extracts and its isolated constituents

An aqueous decotion (dried extract), an 80% MeOH extract from Morinda morindoides leaves, and 10 flavonoids and 4 iridoids isolated from the 80% MeOH extract were evaluated in vitro for their potential antiamoebic activity and their cytotoxic effect against MT-4 cells. Results indicated that the aqueous decoction and the 80% MeOH extract exhibited an interesting antiamoebic activity with IC(50) values of 3.1 +/- 1.7 and 1.7 +/- 0.6 microg/ml, respectively. Apigenin-7-O-glucoside and luteolin-7-O-glucoside exhibited a moderate antiamoebic activity with IC(50) values of 22.3 +/- 3.2 and 37.4 +/- 2.7 microg/ml, respectively. Kaempferol (IC(50) = 10.3 +/- 2.3 microg/ml), apigenin (IC(50) = 12.7 +/- 4.3 microg/ml), and luteolin (IC(50) = 17.8 +/- 4.3 microg/ml) showed a more pronounced activity than their corresponding glycosides. All tested iridoids displayed a very good activity with IC(50) values less than 10 microg/ml. The most active iridoids were epoxygaertneroside (IC(50) = 1.3 +/- 0.4 microg/ml) and methoxygaertneroside (IC(50) = 2.3. +/- 0.7), followed by gaertneroside and gaertneric acid with IC(50) values of 4.3 +/- 1.8 and 7.1 +/- 1.4 microg/ml, respectively. Except quercetin and quercetin-7,4'-dimethylether which have shown a cytotoxic effect with IC(50) ranging from 14 to 22 microg/ml. No correlation could be deduced between the observed antiamoebic and cytotoxic activity of these tested samples. A structure-activity relationship for isolated compounds is discussed. These findings support the medicinal report for the traditional use of Morinda morindoides leaves for the treatment of amoebiasis.     

Antigiardial and immunostimulatory effect of Piper longum on giardiasis due to Giardia lamblia.

Piper longum fruit, used in traditional remedies as well as in the Ayurvedic system of medicine against intestinal disorders, was tested for its efficacy against experimental infection of Giardia lamblia in mice. On in vitro test, an aqueous extract of P. longum fruit powder (PF) at 250 microg/mL and its ethanol extract at 125 microg/mL showed 100% giardicidal activity. A low order activity was found in the n-butanol extract. Further fractionation in hexane and chloroform resulted in a total loss of activity. The survival of-trophozoites in mice at 900 mg/kg body weight was 11.12 in PF, 8. 54 in aqueous extract, 5.81 in ethanol extract. The antigiardial activity of PF in hexane, chloroform and n-butanol soluble fractions was comparable to the drug-untreated control (47.63). Piper longum possessed a demonstrable immunostimulatory activity, both specific and nonspecific, as evident from the standard test parameters such as haemagglutination titre (HA), plaque forming cell (PFC) counts, macrophage migration index (MMI) and phagocytic index (PI). A maximum effect was found at 225 mg/kg body weight in mice. The effect was marginally reduced at higher doses of 450 and 900 mg/kg or the lower dose of 112.5 mg/kg.     

A review of plant species assessed in vitro for antiamoebic activity or both antiamoebic and antiplasmodial properties

The resurgence of the protozoal diseases amoebiasis and malaria has been known to occur, from time to time, in endemic and epidemic proportions all over the world. Furthermore, the import of these individual pathogens to other areas from tropical regions encourages these protozoal diseases to occur on a global scale with considerable associated mortality and morbidity. From time immemorial, the cure of these diseases has been attempted with the use of traditional plant products, derived from such species as are available within local habitats and ecosystems, and dependent on their host community for their conservation. Scientific validation and in vitro investigation, continues to be an important requirement for drug development, particularly with the emergence of resistance and cross resistance to some standard drugs used in such protozoal diseases. This paper provides a comparative compilation of the various studies reported between 1982 and 1999, on plants with antiamoebic activities and those which possess both antiamoebic and antiplasmodial activities. The results suggest that it is advisable to increase efforts towards the conservation of such plants, in order to retain their economic and therapeutic significance.     

Overview for various aspects of the health benefits of Piper longum linn. fruit

Herbal remedies have become popular, due in part to the lower risk of adverse reactions. Thousands of plants have been used traditionally to treat various diseases. Among them, species of the genus Piper are important medicinal plants used in various systems of medicine. The Piper longum fruit has been used in traditional medicine, including the Ayurvedic system of medicine. Although there are numerous indications for its use, controlled trials are needed to determine its efficacy. The primary constituents isolated from various parts of P. longum are piperine, piperlongumine, sylvatin, sesamin, diaeudesmin piperlonguminine, pipermonaline, and piperundecalidine. It is most commonly used to treat chronic bronchitis, asthma, constipation, gonorrhea, paralysis of the tongue, diarrhea, cholera, chronic malaria, viral hepatitis, respiratory infections, stomachache, bronchitis, diseases of the spleen, cough, and tumors. This study provides detailed information about the P. longum fruit, including phytochemistry, pharmacological profile and safety profile. In view of the commercial, economic, and medicinal importance of the P. longum plant, it is useful for researchers to study the plant in detail.     

Additional antiprotozoal constituents from Cuphea pinetorum, a plant used in Mayan traditional medicine to treat diarrhoea

In addition to kaempferol and quercetin already found in the roots from Cuphea pinetorum, bioassay-guided fractionation of the crude extract of the aerial part of this species gave four flavonoid glycosides, quercetin-3-O-alpha-rhamnopyranoside, luteolin-7-O-beta-D-glucopyranoside, apigenin-7-O-alpha-L-rhamnopyranoside and apigenin-7-O-beta-D-glucopyranoside, as well as squalen and beta-sitosterol. In vitro antiamoebic and antigiardial activities of isolated compounds indicated that kaempferol is the principal antiprotozoal agent in C. pinetorum. Based on finding this antiprotozoal inhibitor, flavonoids were studied in order to elucidate structure-activity relationships. These data suggest that kaempferol may play an important role in antidiarrhoeal activity of C. pinetorum.     

荜茇根化学成分及其抗肿瘤活性

目的 研究荜茇PiperlongumL.根的化学成分及其抗肿瘤活性.方法 荜茇干燥根茎95％乙醇提取物采用硅胶、Sephadex LH-20、重结晶进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构.MTT法测定其中2种典型生物碱的抗肿瘤活性.结果 从中分离得到10个化合物,分别鉴定为β.谷甾醇(1)、胡萝卜苷(...     

Anti-inflammatory and antinociceptive activity assessment of plants used as remedy in Turkish folk medicine

Ethanolic and aqueous extracts from seven plant species used in Turkish traditional medicine were evaluated for in vivo anti-inflammatory and antinociceptive activities; Helleborus orientalis Lam. roots and herbs, Juglans regia L. leaves, Laurocerasus officinalis Roemer leaves, Nerium oleander L. dried and fresh flowers and leaves, Rhododendron ponticum L. leaves, Rubus hirtus Walds. et Kit aerial parts and Rubus sanctus Schreber aerial parts and roots. All the plant extracts, except the aqueous extract of Rubus hirtus, were shown to possess significant antinociceptive activity in varying degrees against p-benzoquinone-induced abdominal contractions in mice. However, only the ethanolic extracts of Helleborus orientalis roots, Juglans regia leaves, Laurocerasus officinalis leaves, Nerium oleander dried and fresh flowers, and Rhododendron ponticum leaves exhibited potent anti-inflammatory activity against carrageenan-induced hind paw edema model in mice without inducing any gastric damage. Results of the present study confirmed the folkloric claim that all the selected materials to possess potent antinociceptive and anti-inflammatory activity.     

人参生长季根中几种氧化还原酶的活力变化研究

目的:研究人参根在生长季的不同时期几种氧化还原酶的活力变化。方法:以五年生人参根为供试材料,采用中性磷酸缓冲溶液提取粗酶液。应用紫外分光光度法分别测定过氧化物酶(POD)、过氧化氢酶(CAT)、多酚氧化酶(PPO)和抗坏血酸过氧化物酶(APX)的活力。结果:POD和PPO活力在果后参根生长期之前维持在较低水平,随后快速上升,并于果后参根生长期达到整个生长季的最高值。CAT和APX分别在展叶期和果后参根生长期出现活力高峰。结论:人参根在展叶期和果后参根生长期活性氧代谢水平最高。     

胡椒、荜茇对正常大鼠肝脏能量代谢因子的影响

目的:探讨热性中药胡椒、荜茇对正常大鼠肝脏能量代谢的影响,研究热性中药对大鼠生理活动的影响,为中药药性理论研究打下基础。方法:将30只大鼠随机分为3组,空白组给予生理盐水,胡椒组给予胡椒水提取液,荜茇组给予荜茇水提液,按10 mL·kg-1的量连续灌胃30 d,分别测定肝脏能量代谢相关酶类的变化。结果:与空白组比较,胡椒组、荜茇组能显著升高Ca2+-ATP酶、Ca2+-Mg2+-ATP酶以及LDH酶的活性,同时明显降低肝糖原含量,能够明显升高大鼠单位体重摄入能、消化能和可代谢能;胡椒组与荜茇组间结果比较无明显差异。结论:热性中药胡椒、荜茇能促进肝糖原的分解,增加LDH酶、Ca2+-ATP酶、Ca2+-Mg2+-ATP酶的活性,从而增加ATP酶的消耗,同时升高大鼠单位体重摄入能、消化能和可代谢能,进而促进大鼠肝脏能量代谢。     

Embryotoxicity and teratogenicity studies of an ayurvedic contraceptive--pippaliyadi vati

An ayurvedic contraceptive--pippaliyadi vati, containing equal parts of powdered seeds or fruit berries of Embelia ribes, fruit of Piper longum and borax powder was fed orally to two groups of pregnant rats: 2.5 times to one and five times to the other; the recommended dose for humans. The foetuses of mothers fed with pippaliyadi had low birth weights and were smaller in length. The mothers gained less weight during gestation. Developmental defects of soft tissues and skeletons were analyzed. There were instances of herniation of the intestines into the umbilical cord in foetuses of mothers who were administered pippaliyadi. The control and the gum acacia groups did not show such herniation.     

Antiplasmodial and antiamoebic activities of medicinal plants from Sierra Leone

Crude ethanol extracts of 18 medicinal plants from Sierra Leone, West Africa were examined for antiplasmodial activity against Plasmodium falciparum, using an in vitro microtest. Eleven of these extracts were also screened for in vitro antiamoebic activity against Entamoeba histolytica. Only one plant extract, Triclisia patens (Menispermaceae) showed significant antiplasmodial activity (IC(50) = 8 microg/mL). None of the plant extracts was effective against Entamoeba histolytica.     

荜拔酰胺的结构修饰与生物活性研究进展

荜拔酰胺为叔胺型酰胺类生物碱,该成分主要存在于胡椒科植物长柄胡椒以及瘤突变胡椒等的根中。荜拔酰胺具有抗血小板聚集、抗炎和抗肿瘤等多种药理活性,其衍生物也具有多种多样的活性。笔者综述了荜拔酰胺的结构修饰及其生物活性的研究进展,为荜拔酰胺类化合物的进一步研究提供参考。     

荜茇水提取物对小鼠胃排空和肠推进的影响

目的:研究荜茇水提取物对小鼠肠推进和胃排空的影响。方法:荜茇水提取物灌胃给药6天,采用小肠炭末推进实验观察荜茇水提取物对正常小鼠小肠运动及硫酸阿托品所致小鼠小肠抑制模型的影响,采用甲基橙胃残留率的方法观察荜茇水提取物对正常小鼠胃排空的影响。结果:荜茇水提取物20g/kg和10g/kg可促进正常小鼠小肠运动,并能明显拮抗硫酸阿托品所致小鼠小肠抑制作用,荜茇水提取物20g生药/kg和10g生药/kg可促进正常小鼠胃排空。结论:荜茇水提取物对正常小鼠小肠运动及硫酸阿托品所致小鼠小肠抑制均有明显促进作用,并对正常小鼠胃排空有促进作用,其机制可能与M胆碱受体有关。     

Plants as sources of antimalarial drugs, Part 4: Activity of Brucea javanica fruits against chloroquine-resistant Plasmodium falciparum in vitro and against Plasmodium berghei in vivo

Extracts of Brucea javanica fruit have been prepared and monitored for their in vitro and in vivo antiplasmodial activities. The antimalarial activity of the fruit was found to be attributable to its quassinoid constituents. Nine of the quassinoids possessed in vitro IC50 values between 0.046-0.0008 microgram/ml against the chloroquine resistant Plasmodium falciparum strain (Kl) tested. The two quassinoid glycosides tested were considerably less active in vitro than the aglycones. Four quassinoids were found to possess activity in vivo against Plasmodium berghei infections in mice after oral dosing. All five quassinoids tested in vivo showed some toxicity.     

Antiamoebic and Antigiardial Activity of Clerodane Diterpenes from Mexican Salvia Species Used for the Treatment of Diarrhea

Terpenoids from Salvia species have been identified to possess biological properties as antiprotozoal agents. Here, we evaluated the antiamoebic and antigiardial activities of 14 known clerodane and modified clerodane‐type diterpenes isolated from five Mexican Salvia species against Entamoeba histolytica and Giardia lamblia, and analyzed the effects of the functionalities in decalin ring or in the whole clerodane framework to visualize the structural requirements necessary to produce an antiprotozoal activity. Among these, linearolactone was the most active clerodane diterpene against both protozoa with IC₅₀ values of 22.9 μM for E. histolytica and of 28.2 μM in the case of G. lamblia. In this context it may be a lead compound for the development of novel therapeutic agent for the treatment of diarrhea and dysentery. The remaining diterpenes assayed showed moderate to weak activity against both protozoa. These findings give support to the use of Salvia species in the traditional medicine from México for the treatment of diarrhea. Copyright © 2015 John Wiley & Sons, Ltd.     

Effect of Trimeric Myricetin Rhamnoside (TMR) in Carrageenan‐induced Inflammation and Caecal Ligation and Puncture‐induced Lung Oxidative Stress in Mice

The Eugenia jambolana is used in folklore medicine. Leaves of E. jambolana contain flavonoids as their active constituents which possess in vitro antiinflammatory, antioxidant and the antimicrobial activity. The aim of the present study was to investigate the antiinflammatory and antioxidant effects of a flavonoid glucoside, trimeric myricetin rhamnoside (TMR) isolated from leaves of E. jambolana. TMR was studied for antiinflammatory activity in carrageenan‐induced hind paw oedema and antioxidant activity in lung by caecal ligation and puncture (CLP)‐induced sepsis in mice. Results of the present study indicated that TMR significantly attenuated the oedema, myeloperoxidase (MPO), cytokines and prostaglandin levels in the paw after 5 h of carrageenan injection as compared to vehicle control. It also reduced the lung MPO, lipid peroxides, and serum nitrite plus nitrate levels and increased lung reduced glutathione levels 20 h of CLP as compared to vehicle control. Thus the results of this study concluded that the TMR appears to have potential benefits in diseases that are mediated by both inflammation and oxidative stress and support the pharmacological basis of use of E. jambolana plant as traditional herbal medicine for the treatment of inflammatory diseases. Copyright © 2015 John Wiley & Sons, Ltd.     

Effect of an indigenous herbal compound preparation 'Trikatu' on the lipid profiles of atherogenic diet and standard diet fed Rattus norvegicus

Combating heart disease is one of the challenging problems of biomedical science today. Towards this goal an indigenous preparation 'Trikatu' (a herbal combination containing Piper longum (fruit), Piper nigrum (fruit) and Zingiber officinale (rhizome) dry powder) was fed to normal and cholesterol fed male Rattus norvegicus to ascertain its efficacy as a hypolipidaemic agent. Its effects on body weight, blood and tissue (aortic, cardiac and hepatic) lipids--total, free and esterified cholesterol, low density lipoprotein(LDL) and high density lipoprotein(HDL) cholesterol, triglycerides and phospholipids--and the atherogenic index were measured. It was found that 'Trikatu' by virtue of its ability to reduce triglycerides and LDL cholesterol and to increase HDL cholesterol can reduce the risk of hyperlipidaemia and atherosclerosis. Hence 'Trikatu' can be used as a potent hypolipidaemic agent and it can reduce the atherosclerosis associated with a high fat diet.