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1.
Ethnopharmacological relevance
AT Ш, a sesquiterpenoid, is the major component of Atractylodes japonica Koidz that has been used as a traditional oriental medicine.Aim of the study
We investigated the anti-allergic activity of AT Ш and its mechanism of action.Materials and methods
The released amount of β-hexosaminidase in mast cells, a key parameter of degranulation, was measured. Anti-allergic potential of AT Ш was evaluated using passive cutaneous anaphylaxis in vivo. The anti-allergic mechanism of AT Ш was investigated by immunoblotting analysis, RT-PCR and measurement of [Ca2+]i in mast cells.Results
AT Ш significantly inhibited IgE/Ag-mediated degranulation with an IC50 value (36±4 μM) in RBL-2H3 cells without affecting cell viability. It also suppressed IgE/Ag-mediated passive cutaneous anaphylaxis (PCA) response with an ED50 value (65±41 mg/kg) in vivo. AT Ш suppressed the production of interleukin (IL-4) and tumor necrosis factor (TNF)-alpha mRNAs more potent than the Src-family kinase inhibitor PP2 in RBL-2H3 cells at all concentrations. In order to elucidate the anti-allergic mechanisms of AT Ш in mast cells, we examined the activated levels of signaling molecules. AT Ш inhibited the phosphorylation of Lyn, Fyn, Syk, LAT, PLCγ, Gab2, Akt, p38, and JNK kinases expression. IgE/Ag-mediated [Ca2+]i elevation was significantly inhibited by AT Ш.Conclusions
Our study suggests that AT Ш might be used as a therapeutic agent for allergic diseases. 相似文献2.
Aim of the study
The aim of this study is to examine the effects of andrographolide on intestinal enzyme cytochrome P450 3A4 (CYP3A4) and predict whether oral administration of andrographolide-containing remedy leads to herb–drug interaction.Materials and methods
Caco-2 cells are treated with 1α, 25-dihydroxyvitamin D3 for 3 wks to induce the expression of CYP3A4, and then andrographolide (1, 10, 100 μM) is added and treated for 72 h. Upon the further 4-h testosterone (250 μM) or nifedipine (200 μM) treatment, the basolateral medium samples and the Caco-2 monolayers are collected for analyses.Results
Andrographolide (1, 10, 100 μM) significantly down-regulates the mRNA level and protein level of CYP3A4, and inhibits nifedipine oxidation and testosterone 6β-hydroxylation.Conclusion
Oral administration of andrographolide likely leads to reduction of the metabolic activity of intestinal CYP3A4, therefore herb preparations containing andrographolide may result to herb–drug interactions in combination therapy. 相似文献3.
Aim of this study
Many cartilage protective agents have been developed from natural products, and they have resulted in the development of treatments for osteoarthritis. In this study, we determined the osteoarthritic efficacy and mechanism of butanol fraction from the bark of Betula platyphylla var. japonica (BFBP) in collagenase-induced rabbit model of osteoarthritis (CIA).Materials and methods
The right knees of rabbits were injected intra-articularly with collagenase, and rabbits were orally administrated with distilled water (vehicle), BFBP (50, 100 and 200 mg/kg) or celecoxib (100 mg/kg) once a day for 28 days after the initiation of the CIA.Results
Oral administration of BFBP dose-dependently suppressed the stiffness and global histologic score. Proteoglycan intensity was considerably increased in a dose-dependent manner. As well, the mRNA expression of MMP-1, and MMP-3 was decreased. On the contrary, the level of TIMP-1 in the synovial fluids was significantly increased in the BFBP treated group. The pathologic inflammatory molecules such as PGE2 and COX-2 were inhibited by BFBP, but COX-1 expression not affected.Conclusion
We suggest that BFBP has shown the protective effect on cartilage alternations through balance of MMPs/TIMP-1 and regulates inflammatory-related molecules in vivo model of osteoarthritis, and great candidate for development of osteoarthritis treatment. 相似文献4.
Balekar N Katkam NG Nakpheng T Jehtae K Srichana T 《Journal of ethnopharmacology》2012,141(3):817-824
Ethnopharmacological relevance
Wedelia trilobata (L.) Hitchc (Asteraceae) leaves are used in the treatment of wounds by traditional healers. Despite the use of this plant in wound healing, there is a scarcity of scientific data to support its therapeutic application.Aim of the study
To investigate the wound healing potential of Wedelia trilobata (L.) leaves commonly employed by traditional healers and to clarify its traditional use in a scientific investigation.Materials and methods
An ethanolic extract of Wedelia trilobata leaves was subjected to column chromatography. Hexane, ethyl acetate (WEA) and chloroform:methanol (50:50) (WCM) fractions were obtained. The fractions were tested using relevant in vitro wound healing assays. Antioxidant activity was measured by the DPPH assay. The fibroblast proliferation, oxidative stress using hydrogen peroxide, an in vitro scratch assay, and increasing collagen content was determined using fibroblast L929. Minimum inhibitory concentrations (MICs) were determined against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, and Pseudomonas aeruginosa.Results
WEA (3 μg/mL) promoted fibroblast L929 survivability up to more than 90% before and more than 85% after hydrogen peroxide induced oxidative stress. WEA (3 μg/mL) induced a 70% migration rate in the in vitro scratch assay and the collagen content was increased to 261 μg/mL compared to the control (57.5 μg/mL). WCM exhibited a scavenging activity for DPPH with an IC50 value of 179.5 μg/mL comparable to BHT (139.3 μg/mL). WEA was active against Gram positive bacteria Staphylococcus aureus, Staphylococcus epidermidis with MIC values of 62.5 and 31.25 μg/mL, respectively.Conclusion
These scientific findings of wound healing activity supports the traditional claims for Wedelia trilobata (L.) leaves. The WEA displayed antibacterial and fibroblast stimulatory activities while WCM exhibited antioxidant to indicate its potential wound healing properties. However further studies to isolate the antibacterial, antioxidant and fibroblast stimulatory compounds that contribute to the wound healing properties of this plant are needed. 相似文献5.
Ethnopharmacological relevance
Carum roxburghianum is traditionally used in hyperactive gastrointestinal and respiratory disorders. The present study was carried out to investigate the possible gut and airways relaxant potential of Carum roxburghianum to rationalize its folk uses.Materials and methods
Crude extract of Carum roxburghianum (Cr.Cr) was studied in in vivo and in vitro techniques.Results
Cr.Cr exhibited protective effect against castor oil-induced diarrhea in mice at 100–1000 mg/kg. In rabbit jejunum preparations, Cr.Cr (0.03–3.0 mg/mL) caused relaxation of spontaneous and K+ (80 mM)-induced contractions at similar concentrations, like papaverine. Pretreatment of tissues with Cr.Cr (0.1–1.0 mg/mL) shifted Ca++ concentration–response curves (CRCs) to right, like verapamil. Cr.Cr (0.03 and 0.1 mg/mL) caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In isolated guinea-pig ileum, Cr.Cr (0.01 and 0.03 mg/mL) produced rightward parallel shift of acetylcholine-curves, like atropine. Cr.Cr (1.0–30 mg/kg) caused suppression of carbachol (CCh, 100 μg/kg)-induced increase in inspiratory pressure of anaesthetized rats. In guinea-pig trachea, Cr.Cr (0.03–1.0 mg/mL) relaxed CCh and high K+-induced contractions, shifted isoprenaline-induced inhibitory CRCs to left at 0.1 and 0.3 mg/mL and CCh-curves parallel to right (0.01 and 0.03 mg/mL). Cr.Cr did not cause any mortality of mice up to 10 g/kg dose.Conclusion
These results indicate that Carum roxburghianum possess combination of antidiarrheal, antispasmodic and bronchodilatory effects, which provides pharmacological basis to its traditional use in the disorders of gut and airways hyperactivity, like diarrhea, colic and asthma. 相似文献6.
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7.
Antinociceptive activity of Mirabilis jalapa in mice 总被引:1,自引:0,他引:1
Walker CI Trevisan G Rossato MF Franciscato C Pereira ME Ferreira J Manfron MP 《Journal of ethnopharmacology》2008,120(2):169-175
Ethnopharmacological relevance
The infusion or decoction of Mirabilis jalapa leaves is used in traditional medicine in Brazil to treat inflammatory and painful diseases.Aim of the study
The present study examined the antinociceptive effect of Mirabilis jalapa extracts from leaves and stems in models of pain in mice.Materials, methods and results
The crude hydroethanolic extract from leaves (CrdL) was more potent than the crude extract from stems (CrdS) to inhibit abdominal constrictions induced by acetic acid, with ID50 values of 5.5 (2.3–13.1) and 18.0 (11.3–28.5) mg/kg, respectively. Among the fractions tested, the Eta fraction from leaves (Eta) was more effective (maximal inhibition of 83 ± 8%) and potent (ID50 of 1.1 (0.6–2.1) mg/kg) to induce antinociception. Eta and CrdL also possessed an antinociceptive effect in the tail-flick test. Pre-treatment with naloxone did not modify the antinociceptive effect of Eta, but co-administration with atropine completely prevented it. This suggests that the antinociceptive effect might depend on the cholinergic system. Instead, Eta was not able to alter the acetylcholinesterase activity in blood or spinal cord. Concerning side effects, Eta did not alter locomotor activity, body temperature, gastrointestinal transit and did not produce gastric lesions.Conclusion
Our results demonstrate that Mirabilis jalapa presents antinociceptive activity in mice, which supports its folkloric use as an analgesic. 相似文献8.
Ethnopharmacological relevance
Barleria prionitis Linn. (Family: Acanthaceae), one of the important Ayurvedic medicinal plant in India, has long been used to treat variety of ailments including swellings, gout, arthritic and rheumatic disorders, nervine and skin diseases, and also acts as immunorestorative.Aim of the study
The present study was aimed to explore in vitro and in vivo immunomodulatory activities of the iridoids fraction i.e. n-butanol fraction of methanol extract from Barleria prionitis aerial parts (IFBp).Materials and methods
IFBp was studied for in vitro [nitroblue tetrazolium (NBT) test and neutrophils candidacidal assay] and in vivo immunomodulatory activity on cellular and humoral immune responses to the antigenic challenge by sheep red blood cells (SRBCs) and by neutrophil adhesion test, phagocytic activity and cyclophosphamide-induced myelosuppression. The study comprised the preliminary phytochemical screening, HPTLC standardization and maximum tolerable dose determination of IFBp.Results
IFBp (50, 100 and 200 μg/ml) significantly (P ≤ 0.01) increased the intracellular killing activity of stimulated neutrophils assayed by in vitro NBT reduction test and neutrophils candidacidal assay. Pretreatment of IFBp (100 and 200 mg/kg; p.o.) evoked a significant increase in percent neutrophils and neutrophils adhesion to nylon fibres. Oral administration of IFBp augmented the humoral immune response to SRBCs, evidenced by increase in antibody titres and dose dependently potentiated the delayed-type hypersensitivity reaction induced by SRBCs in mice. IFBp potentiated significantly (P ≤ 0.01) the macrophage phagocytic activity and ameliorated the red blood cells, total white blood cells and platelets count and haemoglobin concentration, and also restored the myelosuppressive effects induced by cyclophosphamide. The content (% w/w; mean ± SD, n = 3) of main iridoids i.e. shanzhiside methyl ester and barlerin was found to be 21.55 ± 2.40 and 10.03 ± 1.69 in IFBp of BP, respectively.Conclusion
The present investigation reveals that IFBp is a potent immunostimulant, stimulating both the specific and non-specific immune mechanisms. 相似文献9.
Ethnopharmacological relevance
The dried root of Sophora flavescens Aiton (Sophorae radix, SR) has long been used in traditional medicine for the treatment of fever and swelling in eastern countries.Materials and methods
The present study investigated the anti-allergic and anti-inflammatory effects of SR using 1-fluoro-2,4-dinitrofluorobenzene (DNFB)-induced contact dermatitis mouse model and in vitro using RBL-2H3 cells.Results
In mice, the topical application of 10 mg/mL of SR effectively inhibited enlargement of ear thickness and weight induced by repeated painting with DNFB. Topical application of SR also inhibited hyperplasia, edema, spongiosis and infiltration of mononuclear cells in ear tissue. In addition, production levels of interferon-gamma and tumor necrosis factor-alpha were decreased by SR in vivo. Finally, the release of histamine and β-hexosaminidase, and migration were inhibited by treatment with SR.Conclusions
These data indicate the potential of SR in treating patients with allergic skin diseases and also suggest that related mechanisms are involved in anti-inflammatory action on the Th 1 skewing reaction and inhibition against recruitment and degranulation of mast cells. 相似文献10.
11.
Taehun Lee Sooryun Lee Kyeong Ho Kim Ki-Bong Oh Jongheon Shin Woongchon Mar 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
Laurus nobilis L. (Lauraceae) has been used for folk medicines in the Mediterranean area and Europe to treat various disorders including skin inflammation (dermatitis) and asthma.Aim of the study
Our aim was to investigate the scientific evaluation of the compounds from Laurus nobilis L. on immuniglobulin E (IgE)-mediated type I hypersensitivity responses in vitro such as atopic dermatitis and asthma.Methods and materials
Seven compounds were isolated and examined for the mast cell stabilizing effect on IgE-sensitized RBL-2H3 mast cells by measuring the β-hexosaminidase activity. In addition, the effects on interleukin (IL)-4 production and IL-5-dependent Y16 early B cell proliferation were investigated as well as their cytotoxic effects on RBL-2H3 cells.Results
Among the seven isolated compounds, magnolialide attenuated the release of β-hexosaminidase from RBL-2H3 cells with an IC50 value of 20.2 μM, while the other compounds revealed no significant effects at concentrations tested. Furthermore, magnolialide significantly inhibited the IL-4 release with an IC50 value of 18.1 μM and IL-4 mRNA expression with an IC50 value of 15.7 μM in IgE-sensitized RBL-2H3 cells. In addition, the inhibition of IL-5-dependent proliferation of early B cells (Y16 cells) by magnolialide was demonstrated with an IC50 value of 18.4 μM.Conclusion
These results suggest that the magnolialide might be a candidate for the treatment of IgE-mediated hypersensitivity responses such as atopic dermatitis and asthma by inhibiting mast cell degranulation, the IL-4 production, and IL-5-dependent early B cell proliferation, key factors in the development and amplification of type I hypersensitivity reactions. 相似文献12.
Zampini IC Villena J Salva S Herrera M Isla MI Alvarez S 《Journal of ethnopharmacology》2012,140(2):287-292
Ethnopharmacological relevance
Zuccagnia punctata Cav. (Fabaceae) is a monotypic species distributed in western Argentina and is traditionally used for the treatment of bacterial and fungal infections. The aim of this study was to demonstrated the antibacterial activity of the Zuccagnia punctata standardized extract and the structurally related non-methoxylated flavonoids with similar pattern of substitution and differences in ring C present in this plant species: 7-hydroxyflavanone (HF), 2′,4′-dihydroxychalcone (DHC) and 3,7-dihydroxyflavone (DHF), against Streptococcus pneumoniae clinical isolates using in vitro and in vivo models.Materials and Methods
MIC values of natural products were determined by agar macrodilution method. In vivo activities were investigated in a Streptococcus pneumoniae infection model in mice. Lung and blood samples were obtained for bacterial cell counts. The serum was used by biochemical analysis (alanine transaminase, aspartate transaminase, urea and creatinine) in order to evaluate the toxicity of natural products.Results
All samples showed antimicrobial activity in vitro with MIC values between 50 and 500 μg/ml. Zuccagnia punctata extract (1 mg/mice) and HF (1 mg/mice) significantly reduced the number of viable Streptococcus pneumoniae in lung (p < 0.01) while lower quantities has not effect. Therefore, the present study has shown that intake once or twice a day of 1 mg of Zuccagnia punctata extract or HF for seven days did not result in toxicity.Conclusions
Our results showed that Zuccagnia punctata extract as well as one of its isolated flavonoids, 7-hydroxyflavanone, could be useful for the development of a novel respiratory infections treatment. 相似文献13.
Musuyu Muganza D Fruth BI Nzunzu Lami J Mesia GK Kambu OK Tona GL Cimanga Kanyanga R Cos P Maes L Apers S Pieters L 《Journal of ethnopharmacology》2012,141(1):301-308
Ethnopharmacological relevance
The antiprotozoal and cytotoxic activity of the aqueous extracts from 33 medicinal plants, used by traditional healers for the treatment of various parasitic diseases and collected after an ethnopharmacological inventory conducted in the Bolongo area, Bandundu province in DR Congo, was evaluated.Materials and methods
Decoctions were prepared, lyophilized and evaluated for in vitro antiprotozoal activity against Trypanosoma b. brucei, Trypanosoma cruzi, Leishmania infantum, and the chloroquine- and pyrimethamine-resistant K1 strain of Plasmodium falciparum. Cytotoxicity against MRC-5 cells was included to assess selectivity of activity.Results
Most of the tested extracts exhibited pronounced (IC50 ≤ 5 μg/ml) or good (5 < IC50 ≤ 10 μg/ml) antiprotozoal activity against one or more of the selected protozoa. A total of 19 plant extracts inhibited Trypanosoma b. brucei, especially the extract from Isolona hexaloba stem bark (IC50 = 1.95 μg/ml, SI = 16.5); 8 plant extracts were active against Trypanosoma cruzi, the extracts from Enanatia chlorantha stem bark and Quassia africana root bark being the most active with IC50 values of 1.87 and 1.88 μg/ml, respectively (SI = 3.0 and 3.3, respectively); 8 plant extracts showed activity against Leishmania infantum, with extracts from Napoleona vogelii stem bark and Quassia africana root bark as the most active with IC50 values of 5.66 and 5.04 μg/ml (SI = 11.3 and 1.2). Finally, 9 plant extracts inhibited Plasmodium falciparum K1 with the extracts from Quassia africana (root bark and stem bark) being the most active ones with IC50 values of 0.46 and 1.27 μg/ml (SI = 13.7 and 13.6). Extracts from Enantia chlorantha stem bark, Piptadeniastrum africanum stem bark and Quassia africana root bark were cytotoxic for MRC-5 cells (CC50 < 10 μg/ml).Conclusions
These results can partly support and justify the traditional use of some of these plant species for the treatment of parasitic diseases. 相似文献14.
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15.
Lima DK Ballico LJ Rocha Lapa F Gonçalves HP de Souza LM Iacomini M Werner MF Baggio CH Pereira IT da Silva LM Facundo VA Santos AR 《Journal of ethnopharmacology》2012,142(1):274-282
Ethnopharmacological relevance
Piper aleyreanum is a small tree that is widely distributed in tropical and subtropical regions, mostly in North and South America, and is used as an immunomodulator, analgesic and antidepressant in folk medicine.Aim of the study
This study was designed to investigate the antinociceptive, anti-inflammatory and gastric antiulcer activities of the essential oils from the aerial parts of Piper aleyreanum (EOPa) in rodents.Materials and methods
The antinociceptive and anti-inflammatory effects of orally administered EOPa were evaluated in mice subjected to the formalin and pleurisy models, respectively. We also pretreated the rats with EOPa before acute ethanol-induced gastric lesions and measured gastric lesion extension and mucus and glutathione (GSH) levels in the gastric mucosa. Finally, we performed a phytochemical analysis of EOPa.Results
The chemical composition of EOPa was analyzed by gas chromatography and mass spectrometry (GC/MS), which identified 35 compounds, representing 81.7% of total oil compounds. Caryophyllene oxide (11.5%), β-pinene (9%), spathulenol (6.7%), camphene (5.2%), β-elemene (4.7%), myrtenal (4.2%), verbenone (3.3%) and pinocarvone (3.1%) were the major oil constituents. The oral administration of EOPa (10–1000 mg/kg) significantly inhibited the neurogenic and inflammatory phases of formalin-induced licking, with ID50 values of 281.2 and 70.5 mg/kg, respectively. The antinociception caused by EOPa (100 mg/kg, p.o.) was not reversed by naloxone (1 or 5 mg/kg, i.p.) in the formalin test. EOPa (100–300 mg/kg, p.o.) did not affect animal motor coordination in an open-field model. In carrageenan-induced pleurisy, EOPa (1–100 mg/kg, p.o.) significantly decreased the total cell count, neutrophils and mononuclear cells with mean ID50 values of 53.6, 21.7 and 43.5 mg/kg, respectively. In addition, EOPa (1–30 mg/kg, p.o.) protected the rats against ethanol-induced gastric lesions with an ID50 value of 1.7 mg/kg and increased the mucus and GSH levels of the gastric mucosa to levels similar to those of the non-lesioned group.Conclusions
These data show for the first time that EOPa has significant antinociceptive and anti-inflammatory actions, which do not appear to be related to the opioid system. EOPa also has interesting gastroprotective effects related to the maintenance of protective factors, such as mucus production and GSH. These results support the widespread use of Piper aleyreanum in popular medicine and demonstrate that this plant has therapeutic potential for the development of phytomedicines with antinociceptive, anti-inflammatory and gastroprotective properties. 相似文献16.
Toyang NJ Wabo HK Ateh EN Davis H Tane P Kimbu SF Sondengam LB Bryant J 《Journal of ethnopharmacology》2012,141(3):866-871
Ethnopharmacological relevance
Prostate cancer is a major problem worldwide and affects most men above the age of forty-five. Vernonia guineensis Benth. (Asteraceae) root decoction is used in folk medicine in Cameroon to treat a number of ailments including prostate cancer. The aim of this study was to provide a preliminary validation of the use of Vernonia guineensis Benth. extracts to treat prostate cancer by evaluating the in vitro activity of its crude extracts and isolated molecules on prostate cancer cells lines and effect on angiogenesis which is essential for growth and metastases of prostate cancer.Materials and methods
Aqueous, dichloromethane and methanol extracts of Vernonia guineensis Benth. tubers were tested for activity against three prostate cancer cell lines (PC-3, DU-145 and AT3B-1). The dichloromethane extract was subjected to bioactivity guided fractionation. Anti-proliferation, clonogenic and antiangiogenic activity of the crude extracts and isolated compound were tested. The WST-1 assay was used for the anti-proliferation activity meanwhile the standard clonogenic test and the rat ring aorta assay were carried out to determine the clonogenic and antiangiogenic activity of tested products respectively.Results
The aqueous and methanol extracts of Vernonia guineensis Benth. demonstrated weak activity against prostate cancer cell lines in vitro with IC50 > 100 μg/mL. The dichloromethane extract was more potent with IC50 of 56.233 ± 3.630 μg/ml and 67.316 ± 2.452 μg/ml against the DU-145 and PC-3 cell lines respectively. Activity guided fractionation of this extract yielded a Pentaisovalerylsucrose (1) isolated for the first time from a natural source to the best of our knowledge. Compound 1 demonstrated in vitro activity against the human prostate cancer cell lines PC-3 and DU-145 with IC50 of 5.701 ± 0.142 μM and 4.275 ± 0.710 μM, respectively. The IC50 of the compound was 5.763 ± 0.425 μM against AT3B-1, a rat prostate cancer cell line expressing P-glycoprotein which is linked to drug resistance in most metastatic cancers. Compared to compound 1, Paclitaxel and Docetaxel were active against AT3B-1 at 2.641 ± 1.253 μM and 0.613 ± 0.251 μM. Paclitaxel showed IC50 values of 0.004 ± 0.002 μM and 0.003 ± 0.001 μM against DU-145 and PC-3 prostate cancer cell lines respectively. Docetaxel showed IC50 values of 0.002 ± 0.001 μM and 0.004 ± 0.001 μM against DU-145 and PC-3 prostate cancer cell lines respectively.Conclusion
The in vitro anti-prostate cancer and the antiangiogenic activity of Vernonia guineensis Benth. extracts and isolated compound support the use of the tubers of this plant for the treatment of prostate cancer. 相似文献17.
Alonso-Castro AJ Ortiz-Sánchez E Domínguez F López-Toledo G Chávez M Ortiz-Tello Ade J García-Carrancá A 《Journal of ethnopharmacology》2012,140(2):438-442
Ethnopharmagological relevance
Medicinal plants are an important source of antitumor compounds. This study evaluated the acute toxicity in mice, as well as the cytotoxic and antitumoral effects of methanolic extracts of Croton lechleri leaves (CLE).Materials and methods
The cytotoxicity of CLE on human cancer cell lines and human non-cancerous cells was evaluated using the MTT and apoptosis assays. Apoptosis induced by CLE on human cancer cell lines was determined using flow cytometry with annexin-Alexa 488/propidium iodide. The acute toxicity in mice was performed according to the Lorke procedure. Different doses of CLE were injected intraperitoneally daily into athymic mice bearing tumor during 18 days. The growth and weight of tumors was measured.Results
CLE showed low IC50 values on HeLa (17 μg/ml) cells but lack toxic effects against human normal cells. Induction of cell death in HeLa cells by CLE was confirmed by an increase of apoptosis (Annexin/PI) by 30% compared to untreated cells. The LD50 was 356 mg/kg by intraperitoneal route (i.p.) and 500 mg/kg by oral route. CLE administrated at 1, 10 and 50 mg/kg i.p. inhibited the tumor growth by 38%, 48% and 59%, respectively, in mice bearing HeLa tumor.Conclusion
Croton lechleri shows moderate toxic effects in vivo, exerts cytotoxic effects on HeLa cells and has antitumor effects in mice bearing HeLa tumor. 相似文献18.
Saragusti AC Bustos PS Pierosan L Cabrera JL Chiabrando GA Santos AR Ortega MG 《Journal of ethnopharmacology》2012,140(1):117-122
Ethnopharmacological relevance
Prosopis strombulifera (Lam.) Benth. is a rhizomatous shrub that grows in the north and central zone of Argentina. In folk medicine, the fruits of this plant have been used as an astringent, anti-inflammatory and odontalgic agent and anti-diarrheic.Aim of the study
To investigate the antinociceptive effect of ethanol (EE), chloroform (CE) and ethyl acetate (EtOAcE) extracts of Prosopis strombulifera fruits and the involvement of the l-arginine-nitric oxide pathway in this effect.Materials and methods
The antinociceptive effects of the EE, CE and EtOAcE of Prosopis strombulifera fruits were evaluated in vivo using the formalin-induced pain test in mice with aspirin and morphine as reference antinociceptive compounds. The participation of the l-arginine-nitric oxide pathway in the antinociceptive effect was investigated in the same animal model using l-arginine as a nitric oxide (NO) precursor. The in vitro inhibitory effect of the extracts on LPS-induced nitric oxide production and iNOS expression was investigated in a J774A.1 macrophage-derived cell line.Results
CE (300 mg/kg), in contrast to EE and EtOAcE, caused significant inhibition (p < 0.05) of the in vivo nociceptive response. Moreover, CE (100–1000 mg/kg, p.o.) produced a dose-dependent inhibition of the neurogenic and the inflammatory phases of the formalin test with inhibition values (at 600 mg/kg) of 42 ± 7% and 62 ± 7%, respectively. CE inhibition was more potent in the inflammatory phase, with an ID50 of 400.1 (252.2–634.8) mg/kg. The antinociception caused by CE (600 mg/kg, p.o.) was significantly attenuated (p < 0.05) by i.p. treatment of mice with l-arginine (600 mg/kg). In addition, CE (100 μg/mL) produced significant in vitro inhibition (p < 0.001) of LPS-induced NO production, which was not observed with EE and EtOAcE at the same concentration. The inhibition of NO production by CE (10–100 μg/mL) was dose-dependent, with an IC50 of 39.8 (34.4–46.1) μg/mL, and CE significantly inhibited LPS-induced iNOS expression in J774A.1 cells.Conclusions
This study supports, in part, the ethnomedical use of Prosopis strombulifera fruits by showing that its CE produces moderate antinociception in vivo. The findings also provide scientific information for understanding the molecular mechanism involved in the analgesic effect of this plant. 相似文献19.
Moreira CG Horinouchi CD Souza-Filho CS Campos FR Barison A Cabrini DA Otuki MF 《Journal of ethnopharmacology》2012,141(3):1005-1011
Ethnopharmacological relevance
Pyrostegia venusta is a native Brazilian plant which has a variety of uses in traditional folk medicine including the treatment of vitiligo. However, its effectiveness on melanogenesis is not yet elucidated.Aim of the study
This study aimed to investigate the melanogenic activity of hydroalcoholic extracts from the leaves and flowers of P. venusta on murine B16F10 melanoma cells.Materials and methods
Different concentrations of the hydroalcoholic extracts of flowers and leaves of P. venusta were evaluated in trials of spontaneous melanin content (4 days), and cell viability by the MTT assay in murine B16F10 cells, and in the mushroom tyrosinase activity in vitro.Results
Both extracts, leaves (0.1; 0.3; 1 and 3 μg/mL) and flowers (0.03 and 0.1 μg/mL) increased the melanin content in a concentration dependent manner after 4 days of incubation on melanoma cells. Leaves extract promoted enhancement of melanogenesis with maximum effect of 33.3 ± 3% (3 μg/mL), and the flower extract increased in 23.4 ± 3% (0.1 μg/mL). The cell viability test using MTT showed that in the same tested concentrations of both extracts no cell death was detected. Actually, either extract was not able to cause any change in the tyrosinase activity. HPLC analysis of P. venusta extracts found 0.09% and 1.08% of allantoin on leaves and flowers extracts, respectively.Conclusions
The leaves and flowers extracts of P. venusta stimulates B16F10 melanogenesis at very low concentrations. These findings support the folk medicinal use of P. venusta on the treatment of hypopigmentation diseases, such as vitiligo. 相似文献20.
Senejoux F Girard C Aisa HA Bakri M Kerram P Berthelot A Bévalot F Demougeot C 《Journal of ethnopharmacology》2012,141(2):629-634