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1.
Aim of the study
This study investigated the medicinal plant Siphonochilus aethiopicus (Zingiberaceae) for antiplasmodial activity.Materials and methods
The ethyl acetate extract of Siphonochilus aethiopicus rhizomes was fractionated using solid phase extraction (SPE) and purified by high performance liquid chromatography. Structure elucidation was performed with nuclear magnetic resonance and mass spectrometry. The in vitro cytotoxicity and antiplasmodial activity was determined. In vivo schizontocidal activity was performed in a malaria mouse-model. Additional in vitro testing was done against Staphylococcus aureus, Klebsiella pneumoniae and Mycobacterium tuberculosis.Results and discussion
The ethyl acetate extract showed in vitro activity against the chloroquine-sensitive (CQS) and chloroquine-resistant (CQR) strains of Plasmodium falciparum with IC50-values of 2.9 μg/ml and 1.4 μg/ml, respectively. Bioassay-guided fractionation led to the isolation of three novel furanoterpenoids with moderate in vitro antiplasmodial activity. The crude extract showed very good in vivo activity. The compounds and crude extract were more active against the CQR strain than the CQS strain of Plasmodium falciparum. The SPE fractions were more active than the isolated compounds. The compounds did not show good activity against the micro-organisms tested. No in vitro cytotoxicity was observed.Conclusion
This study provides evidence of antiplasmodial compounds present in Siphonochilus aethiopicus. 相似文献2.
Kamaraj C Kaushik NK Rahuman AA Mohanakrishnan D Bagavan A Elango G Zahir AA Santhoshkumar T Marimuthu S Jayaseelan C Kirthi AV Rajakumar G Velayutham K Sahal D 《Journal of ethnopharmacology》2012,141(3):796-802
Ethnopharmacological relevance
An ethnopharmacological investigation of medicinal plants traditionally used to treat diseases associated with fevers in Dharmapuri region of South India was undertaken. Twenty four plants were identified and evaluated for their in vitro activity against Plasmodium falciparum and assessed for cytotoxicity against HeLa cell line.Aim of the study
This antimalarial in vitro study was planned to correlate and validate the traditional usage of medicinal plants against malaria.Materials and methods
An ethnobotanical survey was made in Dharmapuri region, Tamil Nadu, India to identify plants used in traditional medicine against fevers. Selected plants were extracted with ethyl acetate and methanol and evaluated for antimalarial activity against erythrocytic stages of chloroquine (CQ)-sensitive 3D7 and CQ-resistant INDO strains of Plasmodium falciparum in culture using the fluorescence-based SYBR Green I assay. Cytotoxicity was determined against HeLa cells using MTT assay.Results
Promising antiplasmodial activity was found in Aegle marmelos [leaf methanol extract (ME) (IC50 = 7 μg/mL] and good activities were found in Lantana camara [leaf ethyl acetate extract (EAE) IC50 = 19 μg/mL], Leucas aspera (flower EAE IC50 = 12.5 μg/mL), Momordica charantia (leaf EAE IC50 = 17.5 μg/mL), Phyllanthus amarus (leaf ME IC50 = 15 μg/mL) and Piper nigrum (seed EAE IC50 = 12.5 μg/mL). The leaf ME of Aegle marmelos which showed the highest activity against Plasmodium falciparum elicited low cytotoxicity (therapeutic index > 13).Conclusion
These results provide validation for the traditional usage of some medicinal plants against malaria in Dharmapuri region, Tamil Nadu, India. 相似文献3.
Hussain Zeashan G. Amresh Satyawan Singh Chandana Venkateswara Rao 《Journal of ethnopharmacology》2009,125(2):364-366
Aim
50% ethanolic extract (ASE) of Amaranthus spinosus (whole plant) was evaluated for in vitro antioxidant and hepatoprotective activity.Methods
The total phenolics and reducing capacity of ASE was determined using standard curve of gallic acid (0–1.0 mg/ml) and butylated hydroxy anisole. In vitro antioxidant activity was determined by DPPH, superoxide, hydroxyl radicals, hydrogen peroxide and nitric oxide scavenging methods. The hepatoprotective activity of ASE was evaluated at 6, 7, 8, 9 and 10 μg/ml concentration against CCl4 (1%) induced toxicity in freshly isolated rat hepatocytes and HepG2 cells.Results
ASE was found to contain 336 ± 14.3 mg/g total polyphenolics expressed as gallic acid equivalent while the reducing capacity was 2.26 times of BHA. ASE showed significant antioxidant activity in DPPH assay (IC50 29 μg/ml), scavenges superoxide (IC50 ∼ 66–70 μg/ml), hydrogen peroxide (IC50 ∼120–125 μg/ml), hydroxyl radicals (IC50 ∼140–145 μg/ml) and nitric oxide (IC50 ∼ 135–140 μg/ml). ASE (6, 7, 8, 9 and 10 μg/ml) was able to normalise the levels of biochemical parameters in isolated rat hepatocytes intoxicated with CCl4. A dose dependent increase in percentage viability was observed in CCl4 intoxicated HepG2 cells.Conclusions
ASE possesses significant hepatoprotective activity which might be due to antioxidant defence factors and phenolics might be the main constituents responsible for activity. 相似文献4.
Ganfon H Bero J Tchinda AT Gbaguidi F Gbenou J Moudachirou M Frédérich M Quetin-Leclercq J 《Journal of ethnopharmacology》2012,141(1):411-417
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5.
Ali Mohamed Kaou Valérie Mahiou-Leddet Cécile Canlet Laurent Debrauwer Sébastien Hutter Michèle Laget Robert Faure Nadine Azas Evelyne Ollivier 《Journal of ethnopharmacology》2010
Aim of the study
In the Comoros Islands, the aerial parts of Flacourtia indica are used in traditional medicine to treat malaria. Because of the important use of this plant, the phytochemistry of the aerial parts was investigated.Materials and methods
Three compounds were isolated from the decoction of this plant material, Pyrocatechol, Homaloside D and Poliothrysoside. The in vitro antiplasmodial activity on the chloroquine-resistant strain (W2) of Plasmodium falciparum and the cytotoxicity on two complementary human cell lines (THP1, HepG2), of AcOEt extract obtained after liquid/liquid extraction of the decoction and pure compounds, were evaluated.Results
The Poliothrysoside isolated from the AcOEt extract presented a strong antiplasmodial activity (IC50 = 7.4 μM) and a good selectivity index (>28) similar to chloroquine.Conclusion
This study reports for the first time antiplasmodial activity for Flacourtia indica, for its AcOEt extract and the three major constituents and confirms its traditional use. 相似文献6.
Miranda Júnior RN Dolabela MF da Silva MN Póvoa MM Maia JG 《Journal of ethnopharmacology》2012,142(3):679-683
Ethnopharmacological relevance
From seeds of Carapa guianensis the Amazon native people extracts the andiroba oil, which is traditionally used as febrifuge, anti-malarial, insecticidal and repellant. The non-saponifiable fraction separated from the oil is rich in limonoids, which assigns its pharmacological effects.Materials and methods
The andiroba oil and its limonoid-rich fraction were submitted to in vitro antiplasmodial bioassay using W2 and Dd2 strains of Plasmodium falciparum. The acute toxicity of andiroba oil was evaluated. The limonoid-rich fraction was subjected to fractionation and identified its major constituents.Results
Andiroba oil and its limonoid-rich fraction inhibited the growth of W2 clone in 100%, between 24 and 72 h, at concentrations of 8.2 μg/mL and 3.1 μg/mL, respectively. Under the same conditions, the parasitaemia of Dd2 clone provoked by the andiroba oil showed inhibition of 31% (IC50 >82 μg/mL) with a time-dependent relationship of 24 h and inhibition of 88% (IC50 8.4 μg/mL) after 72 h, while for the limonoid-rich fraction the inhibition of Dd2 clone was 56% (IC50 2.8 μg/mL) at 24 h and 82% (IC50 0.4 μg/mL) after 72 h. Andiroba oil in acute toxicity test with a fixed dose (LD50 >2000 mg/kg) was not toxic The limonoids identified in the oil were gedunin, 6α-acetoxygedunin, 7-deacetoxy-7-oxogedunin, 7-deacetylgedunin, 1,2-dihydro-3β-hydroxy-7-deacetoxy-7-oxogedunin and andirobin. Gedunin and derivatives has been reputed as anti-malarials.Conclusion
The results support the traditional use of andiroba oil as antiplasmodial, which additionally proved not to be toxic in bioassays conducted with mice. 相似文献7.
Ethnopharmacological relevance
Medicinal plants traditionally used to treat malaria can provide quality leads towards identifying novel anti-malarial drugs. Here we combined this approach with target based drug discovery and explored Plasmodium specific lactate dehydrogenase (LDH) inhibitory activity of 8 Indian plants which are ethnically used to treat malaria.Methods
LDH from Indian Plasmodium falciparum and Plasmodium vivax strains, were cloned and expressed in Escherichia coli, followed by purification of recombinant enzymes (rPfLDH and rPvLDH respectively). Extracts of 8 plants in different organic and aqueous solvents, were screened for their inhibitory activity on rPfLDH, rPvLDH and mammalian LDHs. Phyllanthus amarus aqueous extract was further tested for in vitro parasiticidal activity.Results
Aqueous extract of Phyllanthus amarus Schum. and Thonn. and chloroform extract of Murraya koenigii (L.) Spreng. exhibited profound and exclusive inhibitory effect on Plasmodium falciparum LDH (IC50=11.2 μg/ml±0.4) and Plasmodium vivax LDH (IC50=6.0 μg/ml±0.6) respectively. Moreover, Phyllanthus amarus aqueous extract also demonstrated antiplasmodial activity in vitro, on Chloroquine sensitive and resistant strains of Plasmodium falciparum (IC50=7.1 μg/ml±0.5 and 6.9 μg/ml±0.7 respectively).Conclusion
Target specific screening of traditional herbs used in malaria treatment has proffered Phyllanthus amarus and Murraya koenigii extracts as hits which can optimistically provide novel antimalarial drugs. 相似文献8.
Ethnopharmacological relevance
Damiana (Turnera diffusa Willd. Ex Schult) has traditionally been used as an herbal aphrodisiac.Aim of the study
The study was aimed to investigate the anti-aromatse activity and the estrogenic activity of the constituents isolated from Turnera diffusa.Materials and methods
The methanolic extract and 24 compounds isolated from the leaves of Turnera diffusa were evaluated for aromatase activity by using a tritiated-water release assay and for estrogenic activity by using yeast estrogen screen (YES) assay.Results
The methanolic extract demonstrated a dose-dependent inhibitory activity of the aromatase enzyme with the IC50 value of 63.1 μg/ml. Among the 24 tested compounds, pinocembrin and acacetin showed the most potent inhibition with IC50 values of 10.8 and 18.7 μM, respectively. Estrogenic activity was also observed in the extract and three compounds including apigenin 7-glucoside, Z-echinacin and pinocembrin with EC50 values of 10, 20 and 67 μM, respectively.Conclusions
The extract of Turnera diffusa and two isolated compounds pinocembrin and acacetin could significantly suppress aromatase activity. Moreover, apigenin 7-glucoside, Z-echinacin and pinocembrin showed estrogenic activity. 相似文献9.
Olivia Jansen L. Angenot M. Tits J.P. Nicolas P. De Mol J.-B. Nikiéma M. Frédérich 《Journal of ethnopharmacology》2010
Aim of the study
The aim of this study was to evaluate the antiplasmodial properties of 13 plants used against malaria in traditional medicine in Burkina Faso.Materials and methods
In vitro antiplasmodial activity of dichloromethane, methanol and aqueous crude extracts obtained from vegetal samples collected in Burkina Faso was first evaluated on the Plasmodium falciparum 3D7 chloroquine-sensitive strain using a colorimetric method.Results
Thirteen extracts obtained from 8 different species were found to exhibit antiplasmodial activity (IC50 < 50 μg/ml). Five species demonstrated a moderate activity (15 μg/ml < IC50 < 50 μg/ml): Boswellia dalzielii (leaves), Waltheria indica (roots and aerial parts), Bergia suffruticosa (whole plant), Vitellaria paradoxa (bark) and Jatropha gossypiifolia (leaves). The best results were obtained with extracts from the Dicoma tomentosa whole plant, from Psorospermum senegalense leaves and from Gardenia sokotensis leaves. These extracts found to display promising antiplasmodial activity, with IC50 values ranging from 7.0 to 14.0 μg/ml.The most active plant extracts were then tested for in vitro activity on the Plasmodium falciparum W2 chloroquine-resistant strain and also for in vitro cytotoxicity on normal human fibroblasts (WI-38) in order to determine the selectivity index.Conclusions
Dicoma tomentosa (Asteraceae) and Psorospermum senegalense (Clusiaceae) appeared to be the best candidates for further investigation of their antiplasmodial properties, reported for the first time by this study. 相似文献10.
Graziose R Rojas-Silva P Rathinasabapathy T Dekock C Grace MH Poulev A Ann Lila M Smith P Raskin I 《Journal of ethnopharmacology》2012,142(2):456-461
Aim of the study
The objective of this study was to identify the antiplasmodial constituents from the bark of Cornus florida L., a plant traditionally used in North America for the treatment of malaria.Methods and materials
Dried and powdered bark was extracted with 95% ethanol. The resultant extract was subjected to in vitro antiplasmodial-guided fractionation against Plasmodium falciparum (D10 strain). Antiplasmodial IC50 values were calculated for pure compounds. Compounds were also assayed against Leishmania tarentolae, and rat skeletal myoblast L6 cells to assess antileishmanial activity and cytotoxicity, respectively.Results
Antiplasmodial-guided fractionation afforded 8 compounds: betulinic acid (1), ursolic acid (2), β-sitosterol (3), ergosta-4,6,8,22-tetraene-3-one (4), 3β-O-acetyl betulinic acid (5), 3-epideoxyflindissol (6), 3β-O-cis-coumaroyl betulinic acid (7), 3β-O-trans-coumaroyl betulinic acid (8), of which, (6) is for the first time here isolated from a natural product and (4), (7) and (8) are reported for the first time from this genus. In vitro IC50 values against P. falciparum for (4) (61.0 μM) (6) (128.0 μM), (7) (10.4 μM), (8) (15.3 μM) are reported for the first time. Antileishmanial IC50 values are reported here for the first time for (4) (11.5 μM), (6) (1.8 μM), (7) (8.3 μM) and (8) (2.2 μM). Cytotoxicity against L6 cells is reported for all compounds.Conclusions
The compounds isolated in this study, while displaying moderate in vitro antiplasmodial activity, do not fully support the historical importance of C. florida as an antimalarial remedy in North America. The traditional remedy may exert its well documented effects by mechanisms unrelated to direct antiplasmodial action. While not traditionally used to treat Leishmania, this work shows that several constituents of C. florida possess promising in vitro antileishmanial activity. 相似文献11.
Ethnopharmacological relevance
Seeds of Annona squamosa L. have been used in the south of China as a folk remedy to treat “malignant sores” (cancer).Aim of the study
To investigate the chemical constituents and the anti-tumor activity of the standardized A. squamosa seeds extract in vitro and in vivo.Materials and methods
Annonaceous acetogenin profiles of the standardized extract were determined by using Fourier transform infrared (FT-IR) and high performance liquid chromatography (HPLC) techniques. The anti-tumor activity of the extract was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) cytotoxicity in vitro and H22 hepatoma cells transplantation tumor model in vivo.Results
The FT-IR spectroscopy showed the presence of annonaceous acetogenin compounds in the extract. Two major annonaceous acetogenins: 12, 15-cis-squamostatin-A and bullatacin were identified and quantified by HPLC. The seed extract showed significant anti-tumor activity against four human tumor cell lines, especially for MCF-7 (IC50. 0.25 μg/ml) and Hep G2 (IC50. 0.36 μg/ml) cells in vitro. The extract inhibited the growth of H22 tumor cells in mice with a maximum inhibitory rate of 69.55% by oral administration.Conclusion
A. squamosa seed extract showed significant anti-tumor activities against human hepatoma cells in vitro and in vivo, indicating a potential for developing the extract as a novel anti-liver cancer drug. 相似文献12.
Lekana-Douki JB Bongui JB Oyegue Liabagui SL Zang Edou SE Zatra R Bisvigou U Druilhe P Lebibi J Toure Ndouo FS Kombila M 《Journal of ethnopharmacology》2011,133(3):1103-1108
Aim of the study
As part of a project to identify new compounds active on malarial parasites, we tested the in vitro antiplasmodial activity of nine plants traditionally used to treat malaria symptoms in Haut-Ogooué Province, South-East Gabon.Materials and methods
Dichloromethane and methanolic extracts of each plant were tested for their antiplasmodial activity on two chloroquine-resistant strains of Plasmodium falciparum (FCB and W2), based on lactate dehydrogenase activity. Cytotoxicity was assessed with the MTT test on MRC-5 human diploid embryonic lung cells.Results
The methanolic extract of Staudtia gabonensis and the dichloromethane extract of Adhatoda latibracteata showed high antiplasmodial activity (IC50 < 1 μg/ml) and low cytotoxicity, with selectivity indexes of about 58.25 and 16.43, respectively. The methanolic extract of Monodora myristica and the dichloromethane extract of Afromomum giganteum also showed promising activity (1 < IC50 < 10 μg/ml) and low cytotoxicity, with selectivity indexes about 15.70 and 12.48, respectively. Dichloromethane extracts of Monodora myristica and Leonotis Africana showed moderate activity (10 < IC50 < 40 μg/ml), with selectivity indexes about 6.07 and 28.89, respectively. Both extracts of Culcasia lancifolia had IC50 values of 10-40 μg/ml but high cytotoxicity (selectivity indexes <2.77). The methanolic extract of Dorstenia klaineana had moderate antiplasmodial activity (IC50 around 17 μg/ml) but strong cytotoxicity (0.43 μg/ml), giving a selectivity index of about 0.03.Conclusions
Most extracts of nine selected plants traditionally used to treat malaria in Gabon had interesting antiplasmodial activity in vitro. This supports continued investigations of traditional medicines in the search for new antimalarial agents. The compounds responsible for the observed antiplasmodial effects are under investigation. 相似文献13.
C.M. Kikueta O.K. Kambu A.P. Mbenza S.T. Mavinga B.M. Mbamu P. Cos L. Maes S. Apers L. Pieters R.K. Cimanga 《Journal of ethnopharmacology》2013
Ethnopharmacological Relevance
To evaluate the in vitro antiplasmodial activity and cytotoxicity, and the in vivo activity of extracts and fractions from the leaves, root-bark and stem-bark of Triclisia gilletii (De Wild) Staner (Menispermaceae), used in traditional medicine against malaria.Materials and Methods
The aqueous and 80% MeOH extracts, and a series of fractions and subfractions from the leaves, stem and root-bark of Triclisia gilletii were tested in vitro for their antiplasmodial activity against a Congolese-sensitive strain of Plasmodium falciparum, against the chloroquine and pyrimethamine-resistant K1 strain of Plasmodium falciparum, for cytotoxicity against MRC-5 cells, and in vivo in mice infected with Plasmodium berghei berghei.Results
Many samples from the three plant parts exhibited pronounced activity against the Congolese chloroquine-sensitive strain of Plasmodium falciparum with some IC50 values <0.02 µg/ml, and against the K1 strain, with some IC50 <0.25; the selectivity was higher against the Congolese strain. At oral doses of 200 and 400 mg/kg body weight in infected mice, the aqueous, 80% methanol and total alkaloid extracts from the three plant parts produced more than 65% and 75% chemosuppression, respectively. The antiplasmodial activity of these three plant parts of Triclisia gilletii can at least in part be attributed to bisbenzylisoquinoline alkaloids, and supports its use for the treatment of uncomplicated malaria in traditional medicine. 相似文献14.
Somayeh Esmaeili Farzaneh Naghibi Mahmoud Mosaddegh Shamim Sahranavard Saeideh Ghafari Noor Rain Abdullah 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
An investigation of plants was undertaken through interviews and literature surveys on plants used to treat malaria or cancer or microbial diseases in Iran.Aim of study
In vitro and in vivo antiplasmodial tests were carried out on selected plants traditionally used in Iran.Materials and methods
Thirty-two plants were extracted with methanol and tested for their in vitro (pLDH assay) activity against Plasmodium falciparum, in vivo activity against Plasmodium berghei and assessed for any cytotoxicity against the human cancer cell line MCF7 and the normal cell MDBK.Results
Extracts from four plants, Buxus hyrcana Pojark. (Buxaceae), Erodium oxyrrhnchum M. Bieb. (Geraniaceae), Glycyrrhiza glabra L. (Fabaceae) and Ferula oopoda (Boiss and Bushe) Boiss. (Apiaceae) were found to have significant antiplasmodial activity (IC50 ranging from 4.7 to 26.6 μg/ml). These findings lend support to the use of Buxus hyrcana and Glycyrrhiza glabra in traditional medicine. The chloroformic fraction also was active against K1 and 3D7 strains. The chloroformic fraction was studied at 10 mg per kg body weight mouse per day. This fraction reduced parasitaemia by 86.1% compared to untreated control mice.Conclusion
Glycyrrhiza glabra showed antiplasmodial activity and has selectivity for Plasmodium falciparum and Plasmodium berghei when tested on mammalian cells. This is the first report that mentioned in vitro and in vivo antiplasmodial activity of Glycyrrhiza glabra. 相似文献15.
Aim of the study
The present study is designed to explore the anti-inflammatory potential of Aegiceras corniculatum Linn. Blanco stems extracts and their mechanism of action against various pro-inflammatory mediators and to validate its traditional use against inflammatory diseases.Materials and methods
Rat paw edema and peritonitis models were employed for in vivo studies. For in vitro studies human platelets and rat neutrophils were stimulated with Ca2+-ionophore A23187 leading to the production of various pro-inflammatory metabolites, i.e., 12-HTT, 12-HETE and LTB4 and 5-HETE which were quantified by HPLC.Results
The highly polar methanol extract (100 mg/kg) caused ∼90% reduction in the carrageenan- and prostaglandin E2-induced paw edema in rats. It also caused the inhibition of cycloxygenase-1 metabolite, 12-HHT (IC50 41.1 ± 1.5 μg/ml) with a concomitant rise in 12-lipoxygenase metabolite, 12-HETE in A23187 stimulated human platelets. Conversely, the non-polar hexane extract attenuated (IC50 0.36 ± 0.12 μg/ml) 12-HETE formation with a parallel rise in 12-HHT, thereby displaying a selectivity towards 12-lipoxygenase. Non-polar hexane extract also antagonized the production of 5-lipoxygenase metabolites, i.e., leukotriene B4 and 5-HETE in the rat neutrophils. Furthermore, ethyl acetate extract inhibited both COX and 5-LOX with a marked decline in the production of 12-HHT (IC50 0.08 ± 0.002 μg/ml) and LTB4 (IC50 0.86 ± 0.03 μg/ml), respectively. The anti-inflammatory effect of hexane and ethyl acetate extracts was also reflected by the diminution of carrageenan-induced cell infiltration in rat peritoneum. Additionally, plant extracts caused ∼60% suppression in dextran-induced paw edema implying that they also ameliorate histamine and serotonin release.Conclusion
Hexane, ethyl acetate and methanol extracts derived from Aegiceras corniculatum possess significant anti-inflammatory activity via multiple mechanisms and validate their traditional use against inflammation-related diseases. 相似文献16.
P Wangchuk PA Keller SG Pyne AC Willis S Kamchonwongpaisan 《Journal of ethnopharmacology》2012,143(1):310-313
Ethnopharmacological relevance
Corydalis dubia is used in Bhutanese traditional medicine as a febrifuge and for treating infections in the blood, liver and bile which correlate to the signs and symptoms of malarial and microbial infections.Aim of the study
To validate the ethnopharmacological uses of the plant and to discover potential new therapeutic drug leads.Materials and methods
C. dubia was collected from Bhutan and the alkaloids were obtained using acid–base fractionation and separation by repeated column and preparative plate chromatography. The alkaloids were identified from analysis of their physiochemical and spectroscopic data and were tested for antiplasmodial, antimicrobial and cytotoxicity activities.Results
A systematic extraction and isolation protocol yielded one new natural product, dubiamine, and seven known isoquinoline alkaloids, scoulerine, cheilanthifoline, protopine, capnoidine, bicuculline, corydecumbine and hydrastine. Among the four alkaloids tested, scoulerine showed the best antiplasmodial activity with IC50 values of 5.4 μM and 3.1 μM against the antifolate sensitive and the multidrug resistant P. falciparum strains: TM4/8.2 and K1CB1, respectively. None of the alkaloids tested showed significant antimicrobial or cytotoxicity activities.Conclusions
The antiplasmodial test results, of the isolated alkaloid components, are commensurated with the ethnopharmacological uses of this plant. 相似文献17.
Aim of the study
Solanum fastigiatum is a medicinal plant widely distributed in the south of Brazil and has been used mainly to treat hepatitis, spleen disorders, uterine tumors, irritable bowel syndrome and chronic gastritis. The present research was aimed to evaluate the potential antioxidant and hepatoprotective activity of aqueous extracts of leaves using in vitro and in vivo models to validate the folkloric use of the plant.Materials and methods
Antioxidant activity was evaluated by different assays, including thiobarbituric acid reactive species (TBARS), total antioxidant, 2,2-diphenlyl-1-picrylhydrazyl (DPPH) radical and metal ion-chelating activities. The hepatoprotective activity of the aqueous extracts was studied on mice liver damage induced by paracetamol (250 mg/kg) by monitoring biochemical parameters.Results
The extract showed inhibition against TBARS, induced by 10 μM FeSO4 and 5 μM sodium nitroprusside in rat liver, brain and phospholipid homogenates from egg yolk. The plant exhibited strong antioxidant activity in the DPPH (IC50, 68.96 ± 1.25 μg/ml) assay. The aqueous extract also showed significant hepatoprotective activity that was evident by enzymatic examination and brought back the altered levels of TBARS, non-protein thiol and ascorbic acid to near the normal levels in a dose dependent manner. Acute toxicity studies revealed that the LD50 value of the extract is more than the dose 4 g/kg body weight of mice.Conclusions
The results indicate that this plant possesses potential antioxidant and hepatoprotective properties and has therapeutic potential for the treatment of liver diseases. 相似文献18.
Ethnopharmacological relevance
Jasminum officinale L. var. grandiflorum (JOG) is a folk medicine used for the treatment of hepatitis in south of China. Phytochemical studies showed that secoiridoid glycosides are the typical constituents of this plant.Aim of the study
The present study was undertaken to evaluate the effect of oleuropein (Ole) derived from the flowers of JOG on hepatitis B virus (HBV) replication in HepG2 2.2.15 cell line in vitro and duck hepatitis B virus (DHBV) replication in ducklings in vivo.Material and methods
The extracellular hepatitis B e antigen (HBeAg) and hepatitis B surface antigen (HBsAg) concentrations in cell culture medium were determined by ELISA. DHBV in duck serum was analyzed by dot blot.Results
Ole blocks effectively HBsAg secretion in HepG2 2.2.15 cells in a dose-dependent manner (IC50 = 23.2 μg/ml). Ole (80 mg/kg, intraperitoneally, twice daily) also reduced viremia in DHBV-infected ducks.Conclusion
Ole therefore warrants further investigation as a potential therapeutic agent for HBV infection. 相似文献19.
Phurpa Wangchuk John B. Bremner Samten Brian W. Skelton Allan H. White Roonglawan Rattanajak Sumalee Kamchonwongpaisan 《Journal of ethnopharmacology》2010
Ethnopharmacological relevance
The plant Aconitum orochryseum Stapf. (Ranunculaceae) is employed together with other plants in Bhutanese traditional medicine and is indicated for malaria-associated fever.Aim of the study
To study the in vitro antiplasmodial activity of atisinium chloride, the major alkaloid from Aconitum orochryseum.Materials and methods
Atisinium chloride was extracted and purified from aerial parts of Aconitum orochryseum and its structure and absolute configuration confirmed by single crystal X-ray crystallography. The crude methanol extract, crude alkaloid fraction, and atisinium chloride were tested for in vitro antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (TM4; wild type) and K1CB1 (K1; chloroquine and antifolate resistant).Results
The diterpenoid alkaloid atisinium chloride was shown to have moderate antiplasmodial activities with IC50 values of 4 μM and 3.6 μM, respectively against the TM4 strain and the K1 strain of Plasmodium falciparum.Conclusions
Our studies provide the first evidence in support of one of the indicated treatments with Aconitum orochryseum in Bhutanese traditional medicine. This alkaloid also represents a potential new antimalarial structural lead. 相似文献20.
Joanne Bero Habib Ganfon Marie-Caroline Jonville Michel Frédérich Fernand Gbaguidi Patrick DeMol Mansourou Moudachirou Joëlle Quetin-Leclercq 《Journal of ethnopharmacology》2009