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1.
Aim of the study
Antinociceptive activity of Rhoifoline A (RA), a benzophenanthridine alkaloid obtained from the ethanol extract of Zanthoxylum nitidum, was evaluated in mice using chemical and thermal models of nociception.Materials and methods
RA was evaluated on anti-nociceptive activity in mice using chemical and thermal models of nociception.Results
RA administered intraperitoneally at doses of 10, 20, 40 and 80 mg/kg exhibited significant inhibitions on chemical nociception induced by intraperitoneal acetic acid and subplantar formalin, and on thermal nociception in the tail-flick test and the hot plate test. RA neither significantly impaired motor coordination in the rotarod test nor did spontaneous locomotion in the open-field test. RA did not enhance the pentobarbital sodium induced sleep time. These results indicated that the observed antinociceptive activity of RA was unrelated to sedation or motor abnormality. Core body temperature measurement showed that RA did not affect temperature during a 2-hour period. Furthermore, RA-induced antinociception in the hot plate test was insensitive to naloxone or glibenclamide but significantly antagonized by L-NAME, methylene blue and nimodipine.Conclusions
Therefore, it is reasonable that the analgesic mechanism of RA possibly involved the NO-cGMP signaling pathway and L-type Ca2+ channels. 相似文献2.
Victor Kuete Frédéric Nana Bathélémy Ngameni Armelle Tsafack Mbaveng Félix Keumedjio Bonaventure Tchaleu Ngadjui 《Journal of ethnopharmacology》2009
Aim of the study
This study was designed to investigate the antimicrobial activities of the methanol extracts from the stem bark of Ficus ovata (FOB), fractions (FOB1–6) and compounds isolated following bio-guided fractionation [3-friedelanone (1), taraxeryl acetate (2), betulinic acid (3), oleanoïc acid (4), 2-hydroxyisoprunetin (5), 6,7-(2-isopropenyl furo)-5,2,4-trihydroxyisoflavone (6), Cajanin (7) and protocatechuic acid (8)].Materials and Methods
The micro-dilution method was used for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC) against fungi (two species), Gram-positive (three species) and Gram-negative bacteria (five species).Results
The results of the MIC determinations indicated that the crude extract (FOB), fractions FOB2 and FOB4 as well as compound 5 were active on the entire studied organisms. Other samples showed selective activity, fractions FOB1, FOB3 and FOB5 being active against 50% of the tested microbial species while FOB6 was active on 40%. Compounds 8, 6, 2 and 7 prevented the growth of 80%, 70%, 50% and 20% of the organisms respectively. The lowest MIC value (156g/ml) observed with the crude extract was recorded on Streptococcus faecalis, Candida albicans and Microsporum audouinii. The corresponding value for fractions (39 μg/ml) was noted with FOB4 against Staphylococcus aureus, while that of the tested compounds (10 μg/ml) was observed with compound 8 on Microsporum audouinii. The results of the MMC determination suggested that the cidal effect of most of the tested samples on the studied microorganisms could be expected.Conclusions
The overall results provided evidence that the studied plant extract, as well as some of the isolated compounds might be potential sources of new antimicrobial drug. 相似文献3.
Brice Ayissi Owona Nico Frederic Njayou Stefan Laufer Paul Fewou Moundipa Hermann J. Schluesener 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Entada africana is a plant used in African traditional medicine for the treatment of stomachache, fever, liver related diseases, wound healing, cataract and dysentery.Aims of the study
This study aimed at evaluating the anti-inflammatory activity of fractions of the stem bark extract of the plant using lipopolysaccharide (LPS)-induced inflammation in RAW 264.7 macrophages model.Materials and methods
The crude extract was prepared using the mixture CH2Cl2/MeOH (1:1, v/v) and fractionated by flash chromatography using solvents of increasing polarity to obtain five different fractions. The effects of the fractions on the cells viability were studied by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and their inhibitory activity against LPS-induced nitric oxide (NO) production screened by Griess test. The most active fraction was further investigated for its effects on reactive oxygen species (ROS) production using flux cytometry, the expression of inducible nitric oxide synthase (iNOS), pro-and anti-inflammatory cytokines (IL1β, TNFα, IL6, IL10 and IL13) by RT-PCR, and the activity of the enzyme p38 MAPK kinase by enzyme-linked immunosorbent assay (ELISA).Results
The fractions presented no significant effect on the viability of macrophages at 100 μg/ml after 24 h incubation. The CH2Cl2/MeOH 5% (Ea5) fraction was found to be the most potent in inhibiting NO production with a half inhibition concentration (IC50)=18.36 μg/ml, and showed the highest inhibition percentage (89.068%) in comparison with Baicalin (63.34%), an external standard at 50 μg/ml. Ea5, as well as Baicalin significantly (P<0.05) inhibited the expression of TNFα, IL6 and IL1β mRNA, attenuated mRNA expression of inducible NO synthase in a concentration-dependent manner, stimulated the expression of anti-inflammatory cytokines (IL10 and IL13), and showed a 30% inhibition of the activity of p38 MAPK kinase.Conclusion
The results of the present study indicate that the fraction Ea5 of Entada africana possesses most potent in vitro anti-inflammatory activity and may contain compounds useful as a therapeutic agent in the treatment of inflammatory related diseases cause by over-activation of macrophages. 相似文献4.
Deliorman Orhan D Hartevioğlu A Küpeli E Yesilada E 《Journal of ethnopharmacology》2007,112(2):394-400
The aqueous and ethanol extracts of Rosa canina L. (Rosaceae) fruits and the fractions prepared from the latter were investigated for their anti-inflammatory and antinociceptive activities in several in vivo experimental models. The ethanolic extract was shown to possess significant inhibitory activity against inflammatory models (i.e., carrageenan-induced and PGE(1)-induced hind paw edema models, as well as on acetic acid-induced increase in a capillary permeability model) and on a pain model based on the inhibition of p-benzoquinone-induced writhing in mice. Hexane, chloroform, ethylacetate, n-butanol and the remaining water fractions were obtained through bioassay-guided fractionation. Ethylacetate and n-butanol fractions displayed potent anti-inflammatory and antinociceptive activities at a dose of 919 mg/kg without inducing acute toxicity. Further attempts to isolate and define the active constituent(s) were inconclusive, possibly due to the synergistic interaction of components in the extract. 相似文献
5.
S.L. Lumpu C.M. Kikueta M.E. Tshodi A.P. Mbenza O.K. Kambu B.M. Mbamu P. Cos L. Maes S. Apers L. Pieters R.K. Cimanga 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
To evaluate the antiprotozoal activity and cytotoxicity of extracts and fractions from the leaves, root bark and stem bark of Alstonia congensis (Apocynaceae), used in traditional medicine against parasitic diseases.Materials and methods
The aqueous and 80% MeOH extracts, and a series of fractions and subfractions from the leaves, stem and root bark of Alstonia congensis were tested in vitro for their antiprotozoal activity against Trypanosoma brucei brucei, Trypanosoma cruzi, Lesihamania infantum and the chloroquine and pyrimethamine-resistant K1 strain of Plasmodium falciparum. Their cytotoxicity on MRC-5 cells (human lung fibroblasts) was evaluated as well.Results
The aqueous and 80% MeOH extracts and a series of subfractions of each plant part exhibited pronounced antiprotozoal activity against the K1 strain of Plasmodium falciparum with IC50 values ranging from 2 to 5 µg/ml, and good activity against Trypanosoma brucei brucei and Trypanosoma cruzi with IC50 values ranging between 5 and 10 µg/ml. The residual 80% MeOH extract from the leaves, and the total alkaloid extract from stem and root bark were the only subfractions active against Leishmania infantum with IC50 values <10 µg/ml. None of the samples from the root bark was cytotoxic against MRC-cell lines (CC50>64 µg/ml). In general, the aqueous extract (traditional decoction) showed the highest selectivity, especially against Plasmodium falciparum.Conclusion
These results can partly support and justify the traditional use of these plant parts of Alstonina congensis as raw materials for the preparation of traditional remedies to treat parasitic diseases such as malaria and trypanosomiasis. 相似文献6.
Hao-Shu Wu Di-Feng Zhu Chang-Xin Zhou Chu-Rui Feng Yi-Jia Lou Bo Yang Qiao-Jun He 《Journal of ethnopharmacology》2009
Acorus calamus L. (AC), family Araceae, have been used in the Indian and Chinese systems of medicine for hundreds of years. The radix of AC is widely used in the therapy of diabetes in traditional folk medicine of America and Indonesia. 相似文献
7.
Rde C Da Silva S Crestani P de Souza AA Boligon ML Athayde AR Santos MC Marques CA Kassuya JE Da Silva-Santos 《Journal of ethnopharmacology》2012,141(3):997-1004
Ethnopharmacological relevance
Scutia buxifolia has been widely used in Brazilian folk medicine as an anti-hypertensive agent.We evaluated the vascular effects and mechanism involved in the relaxation of aorta induced by an n-butanolic fraction (BuOH) from Scutia buxifolia.Materials and Methods
Rat aortic rings precontracted by phenylephrine (1 μM) were exposed to cumulative concentrations (3–3000 μg/ml) of crude extracts or fractions obtained from bark or leaves of Scutia buxifolia. Classical receptor antagonists, channel and enzymatic inhibitors were used to check the mechanisms involved.Results
The crude extracts of both leaves and bark of Scutia buxifolia, as well as several fractions, were able to induce partial or total relaxation of rat aortic rings. The BuOH fraction of bark of Scutia buxifolia was the most potent in endothelium-intact (E+) preparations, and also induced a partial, but very significant relaxation in endothelium-denuded (E−) vessels. The non-selective nitric oxide synthase inhibitor L-NAME, as well as the soluble guanylate cyclase inhibitor ODQ, vanished the relaxation in E+. In E− preparations, K+ channel blockers, such as tetraethylammonium, glibenclamide, 4-aminopyridine, and the large-conductance calcium-activated K+ channel blocker iberiotoxin, were able to significantly reduce the maximum relaxation elicited by BuOH fraction.Conclusion
Our results demonstrated that BuOH fraction obtained from barks of Scutia buxifolia induced both endothelium-dependent and -independent relaxation in rat aortic rings. The endothelium-dependent relaxation is fully dependent on NO/cGMP system, while direct activation of K+ channels may explain, at least in part, the endothelium-independent relaxation induced by BuOH fraction of Scutia buxifolia. 相似文献8.
Kuete V Wabo GF Ngameni B Mbaveng AT Metuno R Etoa FX Ngadjui BT Beng VP Meyer JJ Lall N 《Journal of ethnopharmacology》2007,114(1):54-60
The antimicrobial activity of the methanolic extract from the stem bark of Irvingia gabonensis (IGM), fractions and compounds isolated from IGM [3-friedelanone (1), betulinic acid (2), oleanolic acid (3), 3,3',4'-tri-O-methylellagic acid (4), 3,4-di-O-methylellagic acid (5) and hardwickiic acid (6)] was evaluated against Gram-positive bacteria (6 species), Gram-negative bacteria (13 species) and three Candida species using dilution methods for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC). From the obtained results, IGM prevented the growth of all the species of microorganisms tested at a concentration limit of 312.50 microg/ml. Compounds 4-6 also inhibited the growth of all the tested microbial species while compounds 1-3 showed selective activities. The lowest MIC values (78.12 microg/ml) were obtained with IGM on 13 of the 22 microorganisms tested. The corresponding value of 1.22 microg/ml (4.26 microM) for compounds was recorded with compound 6 on Neisseria gonorrhoeae. The obtained results confirmed the use of Irvingia gabonensis in the treatment of bacterial and fungal infections. 相似文献
9.
Ethnopharmacological relevance
The leaf of Elaeagnus pungens thunb. (Family Elaeagnaceae) has been documented as an effective herb for the treatment of asthma and chronic bronchitis in traditional Chinese medicine. In the past years, only a few of preliminary studies reported the chemical constituents and pharmacology effects of the herb, but their action on the tracheal relaxation has not been investigated.Aim of the study
To investigate the relaxing effect and mechanism of the extracts from Elaeagnus pungens leaves on guinea pig tracheal smooth muscle and bronchi smooth muscle cells.Materials and methods
Four fractions of different polarities from Elaeagnus pungens leaves were tested to the tracheal strips on the resting tension or pre-contracted by histamine (20 μM) and acetylcholine (20 μM). Inhibitory effects of the 1-butanol fraction (400 mg/ml) on cumulative histamine and acetylcholine (0.2–20 μM) induced contraction were measured. In order to determine the mediators on the 1-butanol fraction effect, the relaxing effect of the 1-butanol fraction was evaluated in the absence and presence of β-adrenoceptor antagonists (1 μM propranolol), K+ channels-blockers (4-aminopyridine (2 mM), tetraethylammonium chloride (5 mM) or glibenclamide (10 μM)), the cyclooxygenase inhibitor (indomethacin, 10 μM), nitric oxide synthase inhibitor (Nω-nitro-l-arginine methyl ester, 100 μM) or l-type Ca2+ channel inhibitor (nifedipine, 1 μM). Moreover, [Ca2+]i in bronchi smooth muscle cells was analyzed by measuring the fluorescence intensity with confocal system.Results
1-Butanol fraction induced the highest relaxant effect among four fractions of different polarities from Elaeagnus pungens leaves, and significantly relaxed the tracheal strip in the concentration-dependent manner on the resting tension and pre-contracted by histamine phosphate and acetylcholine. It also produced an unparallel rightward shift of the cumulative concentration-response curve of histamine or acetylcholine. Furthermore, the relaxant effect of 1-butanol fraction was not affected by propranolol, glibenclamide, tetraethylammonium chloride, 4-aminopyridine, indomethacin and Nω-nitro-l-arginine methyl ester. However, 1-butanol fraction-induced relaxation decreased after adding nifedipine. It also concentration-dependently inhibited CaCl2-induced contraction in the Ca2+-free, 60 mM K+-containing solution. Additionally, [Ca2+]i in the BSMCs significantly reduced after administration of the 1-butanol fraction.Conclusions
The 1-butanol fraction from Elaeagnus pungens leaves resulted in a relaxation in the non-precontracted and pre-contracted tracheal strips. The relaxant effect was not related to K+ channels, NO, cGMP or β-adrenoceptors, but related to the inhibition of Ca2+ influx through l-type Ca2+ channels. 相似文献10.
Hai-Tao Xiao Siu-Wai Tsang Hong-Yan Qin Franky F.K. Choi Zhi-Jun Yang Quan-Bin Han Hu-Biao Chen Hong-Xi Xu Hong Shen Ai-Ping Lu Zhao-Xiang Bian 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Polygonum chinense Linn., a folk medicine, has long been used for the treatment of diarrhea and enteritis in southwestern China. However, the components responsible for its anti-diarrheal activity are still poorly understood.Aim of the study
To determine anti-diarrheal activities of Polygonum chinense L. and to identify its active components through bioactivity-guided isolation technique.Materials and methods
Animals were orally administered with the extract of Polygonum chinense L. The anti-diarrheal effects of 75% ethanol extract, four fractions with different polarities from 75% ethanol extract, different eluates collected from Diaion HP-20 macroporous resin chromatography, ellagic acid and corilagin, were examined based on mouse models of castor oil- and magnesium sulfate-induced diarrhea.Results
The results showed that the 75% ethanol extract of Polygonum chinense L. exhibited significant anti-diarrheal activities in a dose-dependent manner in two mouse models. Through in vivo bioactivity-guided fractionation processes, n-butanol and aqueous fractions were found to exhibit prominent anti-diarrheal activities, and two major compounds, ellagic acid and corilagin, from these active fractions were found to possess anti-diarrheal effects.Conclusion
Present study provides evidence of the utilization of Polygonum chinense L. for diarrhea, and ellagic acid and corilagin are two components contributing to the anti-diarrheal effect. 相似文献11.
Ethnopharmacological relevance
Lentinus polychrous is a Thai local edible mushroom, traditionally used for the treatments of fever and inflammation due to snake or scorpion envenomation.Aim of study
The present study aimed to investigate an anti-inflammatory effect of Lentinus polychrous mycelial extract (LPME) both in vitro and in vivo.Materials and methods
The cytotoxicity and suppressive effects of LPME on nitric oxide production, intracellular O2− production, pro-inflammatory mediator expression, TNF-α production were determined by using LPS-activated RAW 264.7 cells. In addition, Anti-inflammatory effect of LPME was evaluated by using carageenan-induced paw edema in rats.Results
The LPME exhibited cytotoxicity with 50% inhibitory concentration (IC50) of 280.25±10.10 μg/ml and significantly suppressed the productions of NO and intracellular O2− with dose-dependent manner. LPME decreased the expressions of iNOS, IL-1β, IL-6, TNF-α and COX-2 and significantly decreased the TNF-α production in LPS-activated macrophage with dose-dependent manners. Moreover, LPME showed significant suppressive effect on paw edema in rats.Conclusion
The results clearly revealed that the LPME inhibited NO and pro-inflammatory productions by down-regulating the gene expressions of pro-inflammatory mediators leading to the decrease paw edema in rat which support the traditional use. 相似文献12.
Aroke S. Ahmed Esameldin E. Elgorashi Nivan Moodley Lyndy J. McGaw Vinasan Naidoo Jacobus N. Eloff 《Journal of ethnopharmacology》2012
Ethnopharmacological importance
Many Bauhinia species, including those indigenous to South Africa, are used in traditional medicine across the world for treating ailments such as gastrointestinal tract (GIT) disorders, diabetes, infectious diseases and inflammation.Aims
Several relevant aspects of different fractions of leaf extracts of Bauhinia bowkeri (BAB), Bauhinia galpinii (BAG), Bauhinia petersiana (BAP), and Bauhinia variegata (BAV) used in South African traditional medicine to alleviate diarrhoea related symptoms were evaluated.Materials and Methods
The antioxidative activities of the extracts were determined using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH), 2, 2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS+) radical scavenging and ferric reducing antioxidant power (FRAP) methods. In vitro antimicrobial activities of the extracts were determined against bacterial strains (Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Enterococcus faecalis) and clinical isolates of the opportunistic fungal strains (Aspergillus fumigatus, Candida albicans, and Cryptococcus neoformans) using a serial dilution microplate method. The polyphenolic contents were quantified using standard methods, and anti-inflammatory activities of the crude extracts were determined using the cyclooxygenase and soybean 15-lipoxygenase enzyme inhibitory assays. The safety of the extracts was evaluated by determining the cytotoxicity against Vero cell lines.Results
The acidified 70% acetone crude extract and their fractions had good antiradical potency against the DPPH and ABTS radicals. The methanol soluble portions of the butanol fractions were more potent (EC50 ranges from 0.64±0.05 to 1.51±0.07 and 0.88±0.18 to 1.49±0.09 μg/ml against DPPH and ABTS radical respectively) compared to the standard, trolox and ascorbic acid (EC50 ranges from 1.47±0.24 to 1.70±0.27 μg/ml) for both DPPH and ABTS. The crude extracts contained variable quantities of phenolic content. The crude extracts and their fractions had weak to good antimicrobial activities, inhibiting the growth of the organisms at concentrations ranging from 39 to 2500 μg/ml. The BAG crude extract and its fractions were the most active against the fungi (MICs ranging from 39 to 625 μg/ml) while the BAB extract and its fractions were the least active with the MICs ranging between 39 and 2500 μg/ml. Aspergillus fumigatus was the least susceptible fungus while Cryptococcus neoformans was the most susceptible.The phenolic-rich crude extracts of BAB, BAG, and BAP had moderate to good dose-dependent cyclooxygenase-1 enzyme inhibitory activity with inhibitions between 22.8% and 71.4%. The extracts were however, inactive against cyclooxygenase-2. The extracts had some level of cytotoxicity towards Vero cell lines, reducing cell viability to less than 10% at concentrations more than 50 μg/ml.Conclusion
The biological activities observed in Bauhinia species provide a scientific basis for the use of the plants in traditional medicines to treat diseases with multi-factorial pathogenesis such as diarrhoea, with each aspect of activity contributing to the ultimate therapeutic benefit of the plants. However, the use of the phenolic-rich extracts of these plants to treat diarrhoea or any other ailments in traditional medicine needs to be monitored closely because of potential toxic effects and selective inhibition of COX-1 with the associated GIT injury. 相似文献13.
Monteiro FS Silva AC Martins IR Correia AC Basílio IJ Agra MF Bhattacharyya J Silva BA 《Journal of ethnopharmacology》2012,141(3):895-900
Ethnopharmacological relevance
Solanum paludosum Moric. (jurubeba-roxa) is commonly used to treat hypertension as a substitute for Solanum paniculatum L. (jurubeba verdadeira). The total ethanolic extract from the root bark of Solanum paludosum have been found to cause hypotension in rats.Aim of the study
To investigate the mechanism by which the total alkaloid fraction obtained from the root bark of Solanum paludosum (FAT-SP) acts as a vasorelaxant agent on rat thoracic aorta.Materials and methods
Rings of rat aorta were suspended in organ bath containing Krebs solution at 37 °C, bubbled with carbogen mixture (95% O2 and 5% CO2) under a resting tension of 1 g. Isometric contractions were measured using a force transducer coupled to an amplifier and a microcomputer.Results
FAT-SP has been found cause relaxation of the aortic rings pre-contracted with phenylephrine (Phe) in a concentration-dependent manner, in the presence and absence of endothelium. This effect was more potent on the endothelium-intact aorta. In the presence of endothelium, neither indomethacin (non-selective cyclooxygenase inhibitor) nor atropine (non-selective muscarinic receptor antagonist), produced significant changes on the relaxation response. On the other hand, in the presence of calmidazolium (a calmodulin inhibitor), N-nitro-l-arginine methyl ester (l-NAME, nitric oxide synthase inhibitor), hydroxocobalamin (HDX) (scavenger of free-radical nitric oxide), 1-H-[1,2,4]-oxadiazolo-[4,3a]-quinoxalin-1-one (ODQ, selective blocker of soluble guanylate cyclase), Rp-8-bromo-β-phenyl-1,N2-ethenoguanosine 3′:5′-cyclic monophosphorothioate sodium salt hydrate (Rp-8-Br-PET-cGMPS, competitive inhibitor of cGMP-dependent protein kinase G) or TEA+ (tetraethylammonium, nonselective potassium channel blocker), the vasorelaxant effect was significantly reduced, suggesting the involvement of NO/sCG/PKG pathway and potassium channel opening in vasorelaxant action of the FAT-SP.Conclusion
The mechanism of vasorelaxant activity of the FAT-SP on rat aorta involves both NO/sCG/PKG pathway and potassium channels. 相似文献14.
Xiang Li Hye Yoom KimHao Zhen Cui Kyung Woo ChoDae Gill Kang Ho Sub Lee 《Journal of ethnopharmacology》2010
Aim of the study
The aim of the present study was to define the effects of extracts of leaves of Zanthoxylum piperitum (ZP) on the vascular tension and its mechanisms responsible in rat thoracic aortic rings.Materials and methods
Methanol extract of ZP and aqueous fraction of the methanol extract (AZP) were examined for their vascular relaxant effects in isolated phenylephrine-precontracted aortic rings.Results
Methanol extract of ZP and aqueous fraction of the methanol extract (AZP) induced relaxation of the phenylephrine-precontracted aortic rings in a concentration-dependent manner. Endothelium-denudation abolished the AZP-induced vasorelaxation. Pretreatment of the endothelium-intact aortic rings with NG-nitro-l-arginine methylester (L-NAME) and 1H-[1,2,4]-oxadiazolo-[4,3-α]-quinoxalin-1-one (ODQ) inhibited the AZP-induced vasorelaxation. Inhibition of Ca2+ entry via L-type Ca2+ channels failed to block the AZP-induced vasorelaxation. Extracellular Ca2+ depletion slightly but significantly attenuated the AZP-induced vasorelaxation. Thapsigargin significantly attenuated the AZP-induced vasorelaxation. Further, Gd3+ and 2-aminoethyl diphenylborinate (2-APB), inhibitors of store-operated Ca2+ entry (SOCE), markedly attenuated the AZP-induced vasorelaxation. Also, wortmannin, an inhibitor of Akt, an upstream signaling molecule of eNOS, attenuated the AZP-induced vasorelaxation. AZP increased cGMP levels of the aortic rings in a concentration-dependent manner and the effect was blocked by L-NAME, ODQ, thapsigargin, Gd3+, 2-APB, and wortmannin. K+ channel inhibition with glibenclamide and tetraethylammonium, cyclooxygenase inhibition with indomethacin, and adrenergic and muscarinic receptors blockade had no effects on the AZP-induced vasorelaxation.Conclusion
Taken together, the present study suggests that AZP relaxes vascular smooth muscle via endothelium-dependent activation of NO-cGMP signaling through the Akt- and SOCE-eNOS pathways. 相似文献15.
Maira Conceição Jerônimo de Souza Lima Mariana Angélica Oliveira Bitencourt Allanny Alves Furtado Hugo Alexandre Oliveira Rocha Ruth Medeiros Oliveira Arnóbio Antônio da Silva-Júnior Eryvaldo Sócrates Tabosa do Egito Denise Vilarinho Tambourgi Silvana Maria Zucolotto Matheus de Freitas Fernandes-Pedrosa 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
Envenoming caused by scorpion sting is a serious public health problem. In Brazil, 13,038 accidents caused by venomous animals have been reported. Of this total, 53% of the cases and 14 deaths were caused by scorpions. Furthermore, Tityus serrulatus (Buthidae) is the most dangerous scorpion due to the high toxicity of its venom. The treatment is the common supportive therapy and the serum therapy, but some people do not have access to both therapies and seek healing through the use of medical plants.Aim of the study
This study evaluated the ability of the crude extract and fractions from the leaves of Ipomoea asarifolia in neutralizing the main biological effects caused by Tityus serrulatus envenoming in mice.Materials and methods
BALB/c mice were pretreated (i.v.) with 100 μλ of aqueous extracts and fractions dichloromethane, ethyl acetate, and n-butanol (CH2Cl2, EtOAc, and n-BuOH, respectively) of Ipomoea asarifolia, rutin or saline. Then, the animals received 100 μλ (i.p.) of venom of Tityus serrulatus (0.8 mg/kg). After six hours, the peritoneal lavage was performed with PBS and the number cells were determined using a Neubauer chamber. The supernatants were collected for determination of cytokines, such as IL-6, IL-12, and IL-1β.Results
The aqueous extract, fractions and rutin, at all doses, significantly reduced cell migration, which was endorsed by the reduction of the levels of certain cytokines.Conclusion
This is the first study that demonstrated the potential effect of Ipomoea asarifolia against inflammation caused by Tityus serrulatus venom, suggesting that these extracts and/or their bioactive molecules, especially the flavonoid rutin, have potential use in the therapy of this envenomation. 相似文献16.
Aim of the study
The aim of the present study was to define the effect of Xanthoceras sorbifolia extracts (XS) on vascular tension and responsible mechanisms in rat thoracic aortic rings.Materials and methods
Ethanol extract of the leaves of XS (EXS) was examined for their vascular relaxant effects in isolated phenylephrine-precontracted rat thoracic aorta.Results
EXS (0.1-100 μg/ml) induced relaxation of the phenylephrine-precontracted aortic rings in a concentration-dependent manner. Endothelium-denudation abolished EXS-induced vasorelaxation. Pretreatment of the endothelium-intact aortic rings with NG-nitro-l-arginine methylester (l-NAME) and 1H-[1,2,4]-oxadiazolo-[4,3-α]-quinoxalin-1-one (ODQ) inhibited EXS-induced vasorelaxation. Inhibition of Ca2+ entry via l-type Ca2+ channels failed to block the EXS-induced vasorelaxation. Extracellular Ca2+ depletion significantly attenuated EXS-induced vasorelaxation. Modulators of the store-operated Ca2+ entry (SOCE), thapsigargin, 2-aminoethyl diphenylborinate (2-APB) and Gd3+, and an inhibitor of Akt, wortmannin, markedly attenuated the EXS-induced vasorelaxation. EXS increased cGMP levels of the aortic rings in a concentration-dependent manner and the effect was blocked by l-NAME, ODQ, thapsigargin, Gd3+, 2-APB, and wortmannin. Further, EXS-induced vasorelaxation was significantly attenuated by tetraethylammonium, a non-selective Kca channels blocker, but not by glibenclamide, an ATP-sensitive K+ channels inhibitor. Inhibition of cyclooxygenase with indomethacin, and adrenergic and muscarinic receptors blockade had no effects on EXS-induced vasorelaxation.Conclusions
The present study suggests that EXS relaxes vascular smooth muscle via endothelium-dependent NO-cGMP signaling through activation of the Akt- and SOCE-eNOS-sGC pathways, which may, at least in part, be related to the function of K+ channels. 相似文献17.
S. Schmidt M. Jakab S. Jav D. Streif A. Pitschmann M. Zehl S. Purevsuren S. Glasl M. Ritter 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Traditional Mongolian medicine (TMM) uses preparations from herbs as one form of medication for the treatment of a diversity of diseases including diabetes mellitus (DM). We evaluated the effect of extracts from the plant Leonurus sibiricus L. (LS), used in TMM to treat typical symptoms of type 2 DM, on insulin secretion, electrophysiological properties, intracellular calcium concentration and cell proliferation of INS-1E insulinoma cells under standard cell culture conditions (SCC; 11.1 mM glucose).Materials and methods
Insulin secretion was measured by ELISA, electrical properties were assessed by whole cell patch clamping, intracellular calcium concentration (Cai) by Fluo-4 time lapse imaging, insulin receptor expression was verified by RT-PCR and cell proliferation assessed by CellTiter-Glo® cell viability assay.Results
Insulin released from INS-1E cells into the culture medium over 24 h was significantly increased in presence of 500 mg/L aqueous LS extract (LS OWE) as well as methanolic LS extract (LS MeOH/H2O) but not in the presence of the butanol-soluble extract (LS MeOH/BuOH). Acute application of LS OWE resulted in a depolarization of the cell membrane potential paralleled by an initial increase and subsequent decline and silencing of action potential frequency, by KATP channel inhibition, persisting depolarization and an increase in Cai. The electrophysiological effects were comparable to those of 100 μM tolbutamide, which, however failed to elevate insulin secretion under SCC. Furthermore all LS extracts stimulated INS-1E cell proliferation.Conclusions
The finding that extracts from Leonurus sibiricus L. enhance insulin secretion and/or foster cell proliferation may provide possible explanations for the underlying therapeutic principles in the empirical use of LS-containing formulations in DM and DM-related disorders as applied in TMM. 相似文献18.
Aim of the study
This study aimed to evaluate in vivo hepatoprotective activity of the aqueous extract of Artemisia absinthium L. (AEAA), which has been used for the treatment of liver disorders in Traditional Uighur Medicine.Materials and methods
Qualitative and quantitative phytochemical analysis of the AEAA was performed by means of thin layer chromatography and spectrophometric assays. Aqueous extract (50, 100 or 200 mg/kg body weight/day) was administered orally to experimental mice. Liver injury was induced chemically, by a single CCl4 administration (0.1% in olive oil, 10 ml/kg, i.v.), or immunologically, by injection of endotoxin (LPS, 10 μg, i.v.) in BCG-primed mice. The levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), tumor necrosis factor-α (TNF-α) and interleukin-1 (IL-1) in mouse sera, as well as superoxide dismutase (SOD), glutathione peroxidase (GPx) and malondialdehyde (MDA) in mouse liver tissues were measured. The biochemical observations were supplemented by histopathological examination.Results
Obtained results demonstrated that the pretreatment with AEAA significantly (P < 0.001) and dose-dependently prevented chemically or immunologically induced increase in serum levels of hepatic enzymes. Furthermore, AEAA significantly (P < 0.05) reduced the lipid peroxidation in the liver tissue and restored activities of defense antioxidant enzymes SOD and GPx towards normal levels. In the BCG/LPS model, increase of the levels of important pro-inflammatory mediators TNF-α and IL-1 was significantly (P < 0.01) suppressed by AEAA pretreatment. Histopathology of the liver tissue showed that AEAA attenuated the hepatocellular necrosis and led to reduction of inflammatory cells infiltration. Phytochemical analyses revealed the presence of sesquiterpene lactones, flavonoids, phenolic acids and tannins in the AEAA.Conclusions
The results of this study strongly indicate the protective efect of AEAA against acute liver injury which may be attributed to its antioxidative and/or immunomodulatory activity, and thereby scientifically support its traditional use. 相似文献19.
Romina E. D’Almeida María I. Isla Elina de L. Vildoza Cristina Quispe Guillermo Schmeda-Hirschmann María R. Alberto 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Parastrephia lucida (Meyen) Cabrera is used in the traditional medicine of Argentinean highlands as an antiseptic and anti-inflammatory medicinal plant. To give scientific support to the ethnopharmacological claim of Parastrephia lucida as an anti-inflammatory crude drug the effect of Parastrephia lucida extracts and fractions was assessed on key enzymes of the biosynthesis of pro-inflammatory eicosanoids mediators from arachidonic acid (AA).Materials and methods
A bio-guided fractionation of the plant extract was carried out to find out the compounds or mixtures responsible for the anti-inflammatory effect. The extracts and fractions were tested in vitro for their ability to inhibit the enzymes cyclooxygenase (COX)-1 and COX-2, lipoxygenase (LOX) and phospholipase (sPLA2). Fractions were analyzed by HPLC–MS, HPLC–ESI-MS/MS and NMR to relate the effect with groups of secondary metabolites.Results
Parastrephia lucida was more effective inhibiting COX and sPLA2 than LOX. Assay-guided isolation led to the active fractions C and F which showed different effect on the selected enzymes. The fraction C was more effective inhibiting LOX while fraction F showed better activity against sPLA2 and COX-2. Both fractions were further worked-up following the isolation of the anti-inflammatory agents with the selected enzyme assays. The main compounds identified in the most active fractions were 5,4′-dihydroxi-7-methoxyflavanone, apigenin, apigenin methyl ether and apigenin trimethyl ether, methyl and dimethyl ethers from quercetin, kaempferol and luteolin methyl ether, ferulic acid esters, cinnamic acid and vanillin.Conclusions
Parastrephia lucida extract inhibit AA metabolism via several enzymes. The results give support to the traditional use of this plant for the treatment of inflammatory disorders. 相似文献20.
Amit S Choudhari Prerna Raina Manasi M Deshpande Ashok G Wali Anand Zanwar Subhash L Bodhankar Ruchika Kaul-Ghanekar 《Journal of ethnopharmacology》2013