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1.

Ethnopharmacological relevance

Aerial parts of Acanthospermum hispidum D.C. are often used by traditional healers in Benin for various diseases and especially for malaria.

Aim of the study

To identify active compounds from extracts of Acanthospermum hispidum D.CV. leaves previously shown to possess antimalarial properties and analyse in vivo activity and toxicity of crude extracts.

Materials and methods

Compounds were isolated from aerial part of Acanthospermum hispidum D.C. and structurally elucidated using extensive spectroscopic analysis. Antiplasmodial activity was evaluated in vitro against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity and in vivo against Plasmodium berghei berghei by the 4-day suppressive test. Selectivity of extract and purified compounds on Plasmodium parasites were evaluated by using MTT test on J774 macrophage like murine cells and WI38 human normal fibroblasts and also against two other parasites: Trypanosoma brucei brucei and Leishmania mexicana mexicana. Acute and sub-acute toxicities of a crude extract were evaluated on mice.

Results

Two known sesquiterpenic lactones were isolated: 1 (15-acetoxy-8β-[(2-methylbutyryloxy)]-14-oxo-4,5-cis-acanthospermolide) and 2 (9α-acetoxy-15-hydroxy-8β-(2-methylbutyryloxy)-14-oxo-4,5-trans-acanthospermolide). 1 and 2 showed in vitro antiplasmodial activity against the chloroquine-sensitive strain (3D7) with IC50 of 2.9 ± 0.5 and 2.23 ± 0.09 μM respectively. Only 2 showed a high selectivity index (SI: 18.4) on Plasmodium compared to cytotoxicity against human fibroblasts cell line (WI38). 1 and 2 also showed interesting antiparasitic activities in vitro against Trypanosoma brucei brucei (IC50 of 2.45 ± 0.49 and 6.36 ± 1.42 μM respectively) and Leishmania mexicana mexicana (IC50 of 0.94 ± 0.05 and 2.54 ± 0.19 μM respectively). Furthermore, crude acidic water extract and fractions containing one of the two isolated compounds displayed a weak in vivo antimalarial activity against Plasmodium berghei berghei with a long half-life causing a delayed effect. In vivo acute (2000 mg/kg) and sub-acute (1000 mg/kg) toxicity tests on the crude acidic water extract did not show toxicity.

Conclusion

Crude acidic water extract, fractions and pure isolated compounds from Acanthospermum hispidum showed promising in vitro antiplasmodial activity. Despite our study did not show in vivo acute and subacute toxicities of the crude acidic water extract, its weak in vivo antimalarial activity and the in vitro cytotoxicity of pure compounds and enriched extracts containing 1 and 2 indicate that the aerial parts of Acanthospermum hispidum should be used with caution for malaria treatments.  相似文献   

2.

Ethnopharmacological relevance

Our previous work has demonstrated that several plants in the Piperaceae family are commonly used by the Q’eqchi Maya of Livingston, Guatemala to treat amenorrhea, dysmenorrhea, and pain. Extracts of Piper hispidum Swingle (Piperaceae), bound to the estrogen (ER) and serotonin (5-HT7) receptors.

Aim of the study

To investigate the estrogenic and serotonergic activities of Piper hispidum extracts in functionalized assays, identify the active chemical constituents in the leaf extract, and test these compounds as agonists or antagonists of ER and 5-HT7.

Materials and methods

The effects of the Piper hispidum leaf extracts were investigated in estrogen reporter gene and endogenous gene assays in MCF-7 cells to determine if the extracts acted as an estrogen agonist or antagonist. In addition, the active compounds were isolated using ER- and 5-HT7 receptor bioassay-guided fractionation. The structures of the purified compounds were identified using high-resolution LC–MS and NMR spectroscopic methods. The ER- and 5-HT7-agonist effects of the purified chemical constituents were tested in a 2ERE-reporter gene assay in MCF-7 cells and in serotonin binding and functionalized assays.

Results

Three butenolides including one new compound (1) were isolated from the leaves of Piper hispidum, and their structures were determined. Compound 1 bound to the serotonin receptor 5-HT7 with IC50 values of 16.1 and 8.3 μM, respectively, and using GTP shift assays, Compound 1 was found to be a partial agonist of the 5-HT7 receptor. The Piper hispidum leaf extracts, as well as Compounds 2 and 3 enhanced the expression of estrogen responsive reporter and endogenous genes in MCF-7 cells, demonstrating estrogen agonist effects.

Conclusions

Extracts of Piper hispidum act as agonists of the ER and 5-HT7 receptors. Compound 1, a new natural product, identified as 9,10-methylenedioxy-5,6-Z-fadyenolide, was isolated as the 5-HT7 agonist. Compounds 2 and 3 are reported for the first time in Piper hispidum, and identified as the estrogen agonists. No inhibition of CYP450 was observed for any of these compounds in concentrations up to 1 μM. These activities are consistent with the Q’eqchi traditional use of the plant for the treatment of disorders associated with the female reproductive cycle.  相似文献   

3.

Aim of the study

The aim of the study was to evaluate the in vitro antiplasmodial activity of crude extracts of 12 plant species traditionally used in Benin for the treatment of malaria in order to validate their use.

Materials and methods

For each species, dichloromethane, methanol and total aqueous extracts were tested. The antiplasmodial activity of extracts was evaluated using the measurement of the plasmodial lactate dehydrogenase activity on chloroquine-sensitive (3D7) and resistant (W2) strains of Plasmodium falciparum. The selectivity of the different extracts was evaluated using the MTT test on J774 macrophage-like murine cells and WI38 human normal fibroblasts.

Results

The best growth inhibition of both strains of Plasmodium falciparum was observed with the dichloromethane extracts of Acanthospermum hispidum DC. (Asteraceae) (IC50 = 7.5 μg/ml on 3D7 and 4.8 μg/ml on W2), Keetia leucantha (K. Krause) Bridson (syn. Plectronia leucantha Krause) (Rubiaceae) leaves and twigs (IC50 = 13.8 and 11.3 μg/ml on 3D7 and IC50 = 26.5 and 15.8 μg/ml on W2, respectively), Carpolobia lutea G.Don. (Polygalaceae) (IC50 = 19.4 μg/ml on 3D7 and 8.1 μg/ml on W2) and Strychnos spinosa Lam. (Loganiaceae) leaves (IC50 = 15.6 μg/ml on 3D7 and 8.9 μg/ml on W2). All these extracts had a low cytotoxicity.

Conclusion

Our study gives some justifications for the traditional uses of some investigated plants.  相似文献   

4.

Ethnopharmacological relevance

Eulophia nuda L. (Orchidaceae) is a medicinally important terrestrial orchid used for the treatment of tumours and various health problems by the local healers throughout the Western Ghats region in Maharashtra (India).

Aim of the study

To isolate the active molecule from Eulophia nuda and to study its cytotoxic potential against human cancer cells.

Materials and methods

The crude methanolic extract of Eulophia nuda tubers was fractionated by stepwise gradient of the solvents—chloroform–methanol to isolate the pure compound. Isolated pure compound was assessed for its cytotoxic potential against human breast cancer cell lines, MCF-7 and MDA-MB-231 using MTT assay. Structure elucidation of the isolated active compound was carried out by extensive spectroscopic analysis including 1H NMR, 13C NMR, NOESY, COSY, LC–MS and IR.

Results

The isolated active molecule was identified as phenanthrene derivative 9,10-dihydro-2,5-dimethoxyphenanthrene-1,7-diol. This compound showed good antiproliferative activity against human breast cancer cell lines MCF-7 (91%) and MDA-MB-231 (85%) at 1000 μg/ml concentration.

Conclusion

9,10-Dihydro-2,5-dimethoxyphenanthrene-1,7-diol from Eulophia nuda tubers showed good growth suppressive effect against human cancer cell lines MCF-7 and MDA-MB-231 making it a potential biomolecule against human cancer.  相似文献   

5.

Ethnopharmacological relevance

Balanites aegyptiaca (Balantiaceae), mainly the fruit, is used by traditional healers and herbalists for treating many diseases in Africa and Asia.

Aim of the study

Investigation of fixed oil composition of fruits and evaluation of its biological activity.

Materials and methods

Oil content was identified using GC and GC/MS. In vitro examination of the oil biological activity (including cytotoxicity, antimutagenicity, antiparasitic, antiviral and antimicrobial activities) was performed.

Results

The oil contained 54.53% unsaturated fatty acids and 1.14% sterols. The oil exhibited anticancer activity against lung, liver and brain human carcinoma cell lines. It also had antimutagenic activity against Fasciola gigantica induced mutagenicity besides anthelmintic activity against hepatic worms (Schistosoma mansoni and Fasciola gigantica). Preliminary screening showed that the oil had antiviral activity against Herpes simplex virus. It also had antimicrobial activity against selected strains of Gram-positive bacteria, Gram-negative bacteria and Candida.

Conclusion

The results showed remarkable biological activity of Balanites aegyptiaca fixed oil and proved its importance as natural bioactive source.  相似文献   

6.

Ethnopharmacological relevance

Plants have been used in folk medicine by Mayan ancient people from the Yucatan Peninsula, Mexico, to treat some diseases considered as cancer diseases such as chronic wounds or tumors.

Aim of the study

We collected a selection of nine plants in order to investigate their cytotoxic activity against cancer cell lines.

Materials and methods

Methanolic extracts were tested for their cytotoxicity using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay on four cancer cell lines; nasopharynx carcinoma (KB), laryngeal carcinoma (Hep-2), cervix adenocarcinoma (HeLa), and cervix squamous carcinoma cells (SiHa) and one normal cell line; canine kidney (MDCK).

Results

All species exhibited some degree of cytotoxic activity. The root bark extract of Hamelia patens exhibited the highest cytotoxic activity on HeLa cells with a CC50 of 13 μg/mL and selectivity index of 13.3, higher than docetaxel. Gossypium schottii and Dioon spinulosum showed similar good cytotoxic activity and selectivity index on HeLa and Hep-2 cells, respectively.

Conclusions

Hamelia patens, Dioon spinulosum and Gossypium schottii demonstrated promising cytotoxic activity and have been selected for future bio-guided fractionation and isolation of active cytotoxic compounds.  相似文献   

7.

Ethnopharmacological relevance

Maharashtra is the third largest state in India with a large tribal population. Documentation of traditional knowledge through ethnobotanical studies is important for conservation and utilization of indigenous knowledge. Diarrhoeal diseases are the second largest cause of morbidity in rural India. Medicinal plants given by the traditional healers of Parinche in Pune district, Maharashtra are known to be efficacious for many common ailments, including diarrhoeal diseases.

Aim of the study

Ethnobotanical survey of antidiarrhoeal plants from Parinche valley towards the documentation and conservation of traditional knowledge.

Materials and methods

Interviews and inquiries were conducted amongst traditional healers, indigenous communities and village elders.

Results

One hundred and eighty two plants used by tribes and natives for different ailments were documented of which 28 flowering plants were for diarrhoea. Leaf was the most preferred plant part. Amongst the 28 plants, antidiarrhoeal activity of five plants viz., Caesalpinia sepiaria, Dioscorea pentaphylla, Launaea pinnatifida, Syzygium rubicundum and Ziziphus jujuba has not been reported previously. Two species viz., Ziziphus xylopyra and Syzygium rubicundum are endemic to India.

Conclusion

Parinche valley is an ethnobotanically rich area with abundant availability and knowledge of medicinal plants that can serve as a model for low cost health care.  相似文献   

8.

Aims of the study

Wounds represent a major health burden and drain on healthcare resources in the world including Ghana and Africa. The majority of the people of Ghana and Africa still patronize traditional medicine for their health needs including various forms of wounds. The aim of this study is the identification of medicinal plants, type of wounds, dosage forms and collection methods used traditionally in treating wounds in the Bosomtwi-Atwima-Kwanwoma district, Ghana. In vitro screening of selected extracts from these plants on cell physiology of human dermal fibroblasts and keratinocytes was to be performed.

Materials and methods

Validated questionnaires were administered to 78 traditional healers in 54 communities of the district. Interviews and structured conversations were used to administer the questionnaires. Selected herbal material dominantly used by the healers was collected, identified and aqueous and ethanolic extracts were investigated in vitro on influence on cell physiology of keratinocytes and dermal fibroblasts (MTT-, BrdU-, LDH-assay). Antioxidant activities of ethanolic extracts were determined by free radical scavenging activity. Antiadhesive activity against Helicobacter pylori on human stomach cells was investigated for extracts reported to be used for stomach ulcer treatment.

Results

The ethnopharmacological survey revealed 104 plants species belonging to 47 families. The detailed use of these plants is documented. Aqueous extracts of Phyllanthus muellerianus, Pycnanthus angolensis and Combretum smeathmanni influenced the mitochondrial activity and proliferation of dermal fibroblasts and keratinocytes significantly. Ethanolic extracts of selected plants exhibited strong antioxidant activities comparable to α-tocopherol. For Spathodea campanulata, Hoslundia opposita and Pycnanthus angolensis, which were reported by the healers to be used also for wound healing in case of stomach ulcers, strong antiadhesive activity against Helicobacter pylori was demonstrated, while the extracts did not exhibit any direct cytotoxicity against the bacterium.

Conclusions

Traditional use of many wound-healing plants from Ghana can be well rationalized by the in vitro investigation of aqueous extracts. E.g. extracts of Phyllanthus muellerianus, Pycnanthus angolensis and Combretum smeathmanni exhibited significant influence on the cell viability and proliferation of keratinocytes and dermal fibroblasts.  相似文献   

9.

Aim of the study

Lindera strychnifolia (LS) is widely used in traditional Chinese medicine. In the present study, we investigated cytotoxicity and antibacterial activity of essential oils and various fractions of ethanol extract of LS to explore the active components of LS and their pharmacological effects.

Materials and methods

The in vitro cytotoxicities of essential oils and various solvent fractions of LS on three human cancer cell lines (A549, HeLa and Hep G2) and a non-cancerous cell line (HUVEC) were examined using a modified MTT assay. And by using agar disc diffusion and broth microdilution methods, the antibacterial activity of these samples was evaluated against 10 bacteria including 5 clinically isolated strains. The compositions of the essential oils from the leaves and roots of LS were also analyzed by GC and GC–MS.

Results

The leaf oil showed the strongest cytotoxicity on the cancer cell lines tested with the IC50 values ranged from 22 to 24 μg/ml after 24 h of treatment. The most sensitive microbial strain to all the samples was Staphylococcus aureus ATCC 25923.

Conclusions

Our results showed that the essential oils of LS exhibited greater cytotoxicity and antibacterial activity than the solvent fractions of ethanol extract of LS.  相似文献   

10.

Introduction

The plant, Ficus exasperata is popularly used in Nigeria and in several parts of Africa for a variety of ailments.

Aim of study

This study was thus mapped out to investigate the toxicity profile of the aqueous leaf extract (AET) on haematological parameters, body weight and body temperature in mice.

Methodology

In the present study, AET was evaluated for acute toxicity over 24 h and 14-day periods. The LD50 was assessed via oral and intraperitoneal administration.

Results

The LD50 was indeterminable via the oral route but was determined to be 0.54 g/kg i.p. In the 24 h and 14 days single dose study, oral administration of 2.5, 5, 10 and 20 g/kg of AET produced neither mortality nor changes in behavior or any other physiological activity in mice. Body weights and body temperatures were not significantly altered. Haematological analysis showed no marked differences in any of the parameters examined (WBC count, platelet and haemoglobin estimation) in either the control or treated groups. However, the 14 days daily dose study showed significant increase in body temperature (p < 0.05) and a significant decrease in the red blood cell count, haemoglobin count and haematocrit values (p < 0.05), while other parameters remained unchanged.

Conclusion

In summary, AET was found to be relatively safe on short-term oral administration. However, chronic toxicity studies are required for the support of the safe use of this plant.  相似文献   

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