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1.
Albert Wulari Mbaya Umar Isah Ibrahim Onyiche Thank God Sanya Ladi 《Journal of ethnopharmacology》2010
Aim of the study
To determine the toxicity and anti-trypanosomal activity of the ethanolic extract of Azadirachta indica (Maliacea) stem bark, through in vivo and in vitro approach using Trypanosoma brucei brucei.Materials and methods
Graded concentrations (100, 200, 400, 800, 1600 and 3200 mg/kg) of the crude stem bark ethanolic extract of Azadirachta indica, Hochst ex. A. Dc. (Maliacea) was tested for acute toxicity in 35 out bred Swiss (Wister) adult albino rats of both sexes. Secondly, the in vitro activity in test tubes and in vivo activity of the extract in 30 out bred Swiss (Wister) adult albino rats against Trypanosoma brucei brucei strain NITR/14 (Federe) was evaluated in a graded dose manner.Results
The calculated intra-peritoneal LD50 of the extract was 870 mg/kg and produced toxicity at high doses (>800 mg/kg). Graded concentrations of the ethanolic extract produced remarkable in vitro activity against Trypanosoma brucei brucei within seconds of inoculation. It also suppressed the establishment of parasitaemia at 100 mg/kg when administered simultaneously with infection in vivo. Similarly, at 200 and 400 mg/kg, the extract administered at the onset of parasitaemia for 4 consecutive days reduced parasitaemia, modulated declined packed volume (PCV) changes by day 48 post-infection in vivo.Conclusion
The results confirm that the folkloric medicinal application of the extract of Azadirachta indica (Maliacea) has a pharmacological basis. Further investigation is however, needed to optimize the effectiveness of the extract. 相似文献2.
Ethnopharmacological relevance
The stem of Marsdenia tenacissima (Roxb.) Wight et Arn. is mainly produced in Yunnan China and has long been used as a medicine to treat cancer in China. Xiao-Ai-Ping injection, the water-soluble part of the stem of Marsdenia tenacissima, is administrated as an anti-cancer agent in clinics for decades. Our previous study showed that Marsdenia tenacissima extract (MTE) restored gefitinib sensitivity in gefitinib-resistant non-small cell lung cancer (NSCLC) cells, but the mechanism involved is unknown. Gefitinib undergoes hepatic metabolism predominantly through human cytochrome P450 (CYP) 3A4 and CYP2D6 enzymes. This study aims to evaluate whether MTE interferes with gefitinib metabolism via human hepatic P450 enzymes.Material and methods
A cocktail-substrate assay was used to test the effect of MTE on major CYP enzyme activities by incubation of pooled human liver microsomes with specific substrate probes of CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 in the absence and presence of MTE. Recombinant human CYP450 enzymes were used to predict in vitro gefitinib metabolic clearance in the absence and presence of MTE. The metabolites of the substrate probes and gefitinib were detected by high-performance liquid chromatographic tandem mass spectrometry (HPLC-MS/MS). Human hepatoma HepG2 cells were used to investigate the effect of gefitinib alone or in combination with MTE on CYP3A4 and CYP2D6 mRNA and protein expression.Results
The cocktail-substrate assay showed that MTE inhibited CYP450 activities in human liver microsomes with the inhibition rate of 3A4>2C9>2C19>1A2>2D6. The co-administration of MTE with gefitinib significantly decreased the in vitro intrinsic clearance (Clint) of gefitinib by 2.6 and 4.0-fold for CYP2D6 and CYP3A4, respectively, but did not affect other CYP450s. CYP2D6 and CYP3A4 mRNA and protein expression in human hepatoma HepG2 cells were greatly reduced in the combined gefitinib and MTE treatment.Conclusion
We demonstrate that MTE inhibits gefitinib metabolism by interfering with CYP3A4 and CYP2D6. Meanwhile, MTE combined with gefitinib down-regulates the mRNA and protein expression of CYP3A4 and CYP2D6 in the HepG2 cells. Thus, these data suggest that MTE is a promising herbal medicine to enhance gefitinib efficacy through improving its metabolic stability. 相似文献3.
Zahra Hajializadeh Sima Nasri Ayat Kaeidi Vahid Sheibani Bahram Rasoulian Saeed Esmaeili-Mahani 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
Since Thymus caramanicus Jalas is used as a folk medicine for the treatment of rheumatism, skin disorders, bacterial infections and diabetes and it contain antioxidant agents, we decided to investigate the possible effects of Thymus caramanicus Jalas (TCJ) extract on in vitro and in vivo models of diabetic neuropathy.Materials and methods
The high glucose-induced cell injury in Pheochromocytoma (PC12) cells and streptozotocin-induced diabetic rats were used. Tail-flick and rotarod treadmill assessments were used to determine nociceptive threshold and motor coordination. Cell viability was determined by MTT assay test. Western blotting was performed to measurement of apoptosis markers.Results
The data showed that elevation of glucose consecutively increases functional cell injury and apoptosis. Furthermore, diabetic rats developed thermal hyperalgesia and motor deficit. Activated caspase 3, cytochrome c release and Bax/Bcl-2 ratio were significantly increased in high glucose-treated PC12 cells and in spinal cord of diabetic animals. TCJ extract (60 and 80 µg/ml) attenuates high glucose-induced PC12 cells damage and apoptosis. In diabetic animals, TCJ extract at daily doses of 100 and 150 mg/kg ameliorated hyperalgesia and suppressed spinal apoptosis.Conclusion
The data indicate that TCJ extract has neuroprotective effects against high glucose-induced neural damage. These protective effects are mediated, at least in part, through attenuation of neural apoptosis and suggest therapeutic potential of TCJ extract in amelioration of diabetic neuropathy. 相似文献4.
Ethnopharmacological relevance
Meconopsis integrifolia (Maxim.) Franch is a high mountain endemic species used as a traditional Tibetan and Mongolian herb to treat hepatitis, pneumonia, and edema. This study aims to investigate the hepatoprotective and antioxidant effects of Meconopsis integrifolia ethanolic extract (MIE) in vitro and in vivo.Materials and methods
The in vitro antioxidant property of MIE was investigated by employing various established systems. Rats with carbon tetrachloride (CCl4)-induced liver injury were used to assess the hepatoprotective and antioxidant effect of MIE in vivo. The level or activity of alkaline phosphatase (ALP), glutamate pyruvate transaminase (ALT), aspartate aminotransferase (AST), and total bilirubin (TB) in the blood serum and thiobarbituric acid reactive substances (TBARS), superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) in the liver and kidney of the rats were assayed using standard procedures.Results
MIE exhibited strong antioxidant ability in vitro. In the rats with CCl4-induced liver injury, the groups treated with MIE and silymarin showed significantly lower levels of ALT, AST, ALP, and TB. MIE demonstrated good antioxidant activities in both the liver and kidney of the rats in vivo.Conclusions
MIE exhibits excellent hepatoprotective effects and antioxidant activities in vitro and in vivo, supporting the traditional use of Meconopsis integrifolia in the treatment of hepatitis. 相似文献5.
Lang Linghu Haixia Fan Yijie Hu Yanling Zou Panpan Yang Xiaozhong Lan Zhihua Liao Min Chen 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
The roots of Mirabilis himalaica have been used in Tibetan folk medicine for treatment of uterine cancer, nephritis edematous, renal calculus and arthrodynia. In our previous work, the ethanol extract of roots had shown potent cytotoxicity against human cancer cells. However, no information is available on the antitumor effect of Mirabilis himalaica. The aim of the present study was to investigate the active constituents guided by bioassay and evaluate the related antitumor efficacy in vitro and in vivo.Materials and methods
The active subextract (ethyl acetate) was subjected to successive chemical separation using a combination of silica gel, LH-20 chromatography and semi-preparative HPLC. The structures were determined by spectroscopic analysis techniques such as nuclear magnetic resonance (NMR) and mass spectrometry. Three human cancer cell lines, A549, HepG2 and HeLa were used for in vitro cytotoxicity evaluation of all isolated compounds by MTT-assay. Then, the potent and novel compound mirabijalone E was employed to the mechanism study againstA549 cells. BrdU immunofluorescence, soft agar assay and cell cycle analysis were employed to detect the cell proliferation effects. Annexin V-FITC/PI staining assay was used for examining apoptotic effects. Expression levels of apoptosis-related proteins were determined by western blot assay. in vivo tumorigenic assay was used to evaluate the xenograft tumor growth treated with mirabijalone E.Results
One new rotenoid compound, mirabijalone E, together with eight known rotenoids was isolated from Mirabilis himalaica. Mirabijalone E, 9-O-methyl-inone B, boeravinone C and boeravinone H exhibited cytotoxicity against A 549 and HeLa cells. Further study on mirabijalone E was carried out in vitro and in vivo. Mirabijalone E inhibited A549 cells growth in a time and dose-dependent manner, which arrested cell cycle in S phase. Mechanistically, mirabijalone E treatment resulted in the increase of Bax expression level, the decrease of Bcl-2 level and the activation of caspase-3, which suggested the activation of apoptosis cascades. Consequently, the xenograft treated with mirabijalone E showed markedly suppressed tumor growth.Conclusions
The result suggested that mirabijalone E, together with active compounds, 9-O-methyl-4-hydroxyboeravinone B, boeravinone C and boeravinone H could be a promising candidate for cancer therapy. 相似文献6.
You-Cheng Hseu Chuan-Chen Lee Yung-Chang Chen K.J. Senthil Kumar Chee-Shan Chen Yu-Chi Huang Li-Sung Hsu Hui-Chi Huang Hsin-Ling Yang 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
The medicinal mushroom Antrodia salmonea has been used as a traditional Chinese medicine and has demonstrated antioxidant and anti-inflammatory effects.Materials and methods
In the present study, we examined the anti-tumor activity of the fermented culture broth of Antrodia salmonea (AS) in vitro and in vivo and revealed its underlying molecular mechanism of action.Results
Treatment of human promyelocytic leukemia (HL-60) cells with AS (50–150 μg/mL) significantly reduced cell viability and caused G1 arrest via the inhibition of cell-cycle regulatory proteins, including cyclin D1, CDK4, cyclin E, cyclin A, and phosphorylated retinoblastoma protein (p-Rb). Furthermore, AS treatment induced apoptosis, which was associated with DNA fragmentation, followed by a sequence of events, including intracellular ROS generation; mitochondrial dysfunction; Fas ligand activation; cytochrome c release; caspase-3, -8, -9, and PARP activation; and Bcl-2/Bax dysregulation. The results of the in vitro study suggested that AS-induced apoptosis in HL-60 cells was mediated by both the mitochondrial and death receptor pathways. Furthermore, we found that AS treatment was effective in delaying tumor incidence in HL-60 xenografted nude mice and reducing tumor burden.Conclusions
To the best of our knowledge, this is the first report confirming the anti-tumor activity of this potentially beneficial mushroom against human promyelocytic leukemia. 相似文献7.
Hafiz Allah Bachaya Zafar Iqbal Muhammad Nisar Khan Zia-ud-Din Sindhu Abdul Jabbar 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
Ziziphus nummularia (Rhamnaceae) and Acacia nilotica (Fabaceae) are being used as anthelmintics in ethnoveterinary medicinal system of Pakistan.Aim of the study
Present study was conducted to determine the anthelmintic activity of Ziziphus nummularia (bark) and Acacia nilotica (fruit) in order to justify their traditional use in veterinary medicine.Materials and methods
In vitro anthelmintic activity of crude methanolic extract (CME) of both the plants was determined against Haemonchus contortus by the adult motility assay, the egg hatch test and the larval development assay. In vivo anthelmintic activity was evaluated in sheep naturally infected with gastrointestinal nematodes by administering increasing doses of crude powder (CP) and CME (1.0–3.0 g/kg).Results
Both the plants exhibited dose- and time-dependent anthelmintic effects by causing mortality of worms, and inhibiting egg hatching and larval development. Acacia nilotica (LC50 = 512.86 and 194.98 μg/ml) was found to be more potent than Ziziphus nummularia (LC50 = 676.08 and 398.11 μg/ml) in egg hatch test and larval development assay, respectively. In vivo, maximum fecal egg count reduction (84.7%) was recorded on day 13 post-treatment in sheep treated with Ziziphus nummularia CME (3.0 g/kg) followed by 78.5% on same day with Acacia nilotica CME (3.0 g/kg).Conclusions
These data show that both Ziziphus nummularia and Acacia nilotica possess anthelmintic activity in vitro and in vivo, justifying their use in traditional veterinary medicine in Pakistan. 相似文献8.
Xin-Hong Zhu Shu-Ji Li Hong-Hai HuLi-Rong Sun Manas DasTian-Ming Gao 《Journal of ethnopharmacology》2010
Ethnopharmacological relevance
Xiao-Xu-Ming decoction (XXMD) has long been employed clinically to treat stroke in traditional Chinese Medicine.Aim of the study
To investigate the neuroprotective effects of XXMD in vivo and in vitro stroke models and determine involved mechanisms.Materials and methods
Two models (four-vessel occlusion in adult Wistar rats and oxygen–glucose deprivation primary cultured neurons) were employed to mimic ischemia-reperfusion damage, in vivo and in vitro, respectively. The effects of XXMD were investigated with respect to neuronal damage, activity of caspase-3 and expression of Bcl-2 in CA1 region of hippocampus after ischemia. The cognitive ability was measured 7 days after ischemia/reperfusion by using Morris water maze.Results
Oral administration of XXMD significantly increased the density of neurons that survived in the CA1 region of hippocampus on the 3rd and 7th day after transient global ischemia was induced in a dose-dependent manner. XXMD ameliorated severe deficiencies in spatial cognitive performance induced by transient global ischemia. Inhibition of caspase-3 activity and up-regulation of Bcl-2 expression were induced in the high dose of XXMD-treated rats after ischemia. In oxygen–glucose deprivation model, both XXMD extract and drug-containing serum prepared from blood of high dose of XXMD-treated rats inhibited apoptotic neuronal death at 24 h after reoxygenation.Conclusions
Our results clearly demonstrated that XXMD is neuroprotective and appears to influence deleterious pathological processes that are activated after the onset of ischemia. 相似文献9.
Min Hye Yang Kee Dong Yoon Young-Won Chin Ju Hyun Park Seung Hyun Kim Young Choong Kim Jinwoong Kim 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
Plants belong to the genus Dioscorea have long been used as edible tuber crops in many tropical and subtropical areas and as a traditional herbal medicine in oriental countries including China, Japan and Korea.Aim of the study
In this study, in vivo and in vitro tests were carried out to evaluate the cognitive enhancing effects of CHCl3-soluble extract from Dioscorea opposita against scopolamine-induced amnesic mice and glutamate- and H2O2-treated cortical neurons of rats.Materials, methods and results
Acute treatment (200 mg/kg body weight, p.o.) and 10 days’ daily administration (50 mg/kg body weight, p.o.) of CHCl3-soluble extract showed significant spatial learning and memory improvement on mice. Furthermore, the neuroprotective effects on glutamate- and H2O2-induced neurotoxicity in primary cultured cortical neurons of rats were assessed. Pretreatment with the extract was found to impart significant protection against neurotoxicity.Conclusions
These in vivo and in vitro results suggest that the Dioscorea opposita has neuroprotective effects on memory impairment related neurodegenerative diseases. 相似文献10.
Jaw-Chyun Chen Tin-Yun Ho Yuan-Shiun Chang Shih-Lu Wu Chia-Cheng Li Chien-Yun Hsiang 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
Glycyrrhiza uralensis has been used for the treatment of gastrointestinal disorders, such as diarrhea, in several ancient cultures. Glycyrrhizin is the principal component of liquorice and lots of pharmacological effects have been demonstrated.Aim of the study
Heat-labile enterotoxin (LT), the virulence factor of enterotoxigenic Escherichia coli, induces diarrhea by initially binding to the GM1 on the surfaces of intestinal epithelial cells and consequently leading to the massive loss of fluid and ions from cells. Therefore, we evaluated the inhibitory effects of traditional medicinal herbs (TMH) on the B subunit of LT (LTB) and GM1 interaction.Materials and methods
The inhibitory effects of TMH on LTB-GM1 interaction were evaluated by GM1-enzyme-linked immunosorbent assay (ELISA). The likely active phytochemicals of these TMH were then predicted by in silico model (docking) and analyzed by in vitro (GM1-ELISA) and in vivo (patent mouse gut assay) models.Results
We found that various TMH, which have been ethnomedically used for the treatment of diarrhea, inhibited the LTB-GM1 interaction. Docking data showed that triterpenoids were the most active phytochemicals and the oleanane-type triterpenoids presented better LTB-binding abilities than other types of triterpenoids. Moreover, by in vitro and in vivo models, we demonstrated that glycyrrhizin was the most effective oleanane-type triterpenoid that significantly suppressed both the LTB-binding ability (IC50 = 3.26 ± 0.17 mM) and the LT-induced fluid accumulation in mice.Conclusions
We found an LT inhibitor, glycyrrhizin, from TMH by in silico, in vitro, and in vivo analyses. 相似文献11.
Abbas Azadmehr Afshin Afshari Behzad Baradaran Reza Hajiaghaee Shamsali Rezazadeh Hamidreza Monsef-Esfahani 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
Scrophularia striata (Scrophulariaceae), a traditional Iranian medicine, has been used for the treatment of allergy, rheumatics and chronic inflammatory disorders.Aim of the study
In the present study, we investigated the in vitro and ex vivo suppressive effects of Scrophularia striata ethanolic extract on nitric oxide production in mouse peritoneal macrophages.Materials and methods
Peritoneal macrophages were harvested by lavaging with ice cold phosphate buffer saline. Macrophages obtained from mice not treated were cultured with 10 μg/mL lipopolysaccaride (LPS), 20 U/mL interferon-γ (IFN-γ), and various concentrations of Scrophularia striata extract for the in vitro experiments and those obtained from mice treated with different doses of the extract for 7 days were cultured with 10 μg/mL LPS, 20 U/mL IFN-γ for the in vivo experiments. Nitrit levels were measured by using the diazotization method based on the Griess reaction, which is an indirect assay for NO production.Results
In vitro exposure of mouse peritoneal macrophages with various concentrations of Scrophularia striata extract (10, 50 and 100 μg/mL) significantly suppressed NO production in a dose-dependent manner. In vivo administration of Scrophularia striata extract (50 and 100 mg/kg) to Balb/c mice inhibited LPS and IFN-γ induced production of NO in the isolated mouse peritoneal macrophages ex vivo in a dose-dependent manner. Exposure to Scrophularia striata extract had no effect on cell viability.Conclusion
The results of the study demonstrated that the Scrophularia striata extract inhibit NO production in activated murine macrophages and we suggest that Scrophularia striata may be used in treating the inflammatory diseases. 相似文献12.
Ethnopharmacological relevance
Alocasia macrorrhiza has been used as a folk medicine for cancer treatment in the Southwest of China.Aim of the study
The purpose of this study is to confirm the anticancer activity of aqueous extract of alocasia macrorrhiza against hepatic cancer and to elucidate its mechanism of action.Materials and methods
Human normal liver cells and hepatocellular carcinoma cells were tested in vitro for cytotoxicity, colony formation inhibition, EdU incorporation, AO/EB staining apoptotic cells, apoptotic DNA fragmentation, and cell cycle distribution in response to alocasia macrorrhiza extract. The mRNA and protein expressions of PPARγ, Cyclin D1, Rb, P21, Bax, Bcl-2 and caspase-3 were detected through RT-PCR and Western blotting; the tumor growth inhibition in vivo was tested by oral administration of the extract.Results
Alocasia macrorrhiza aqueous extract exhibited proliferation inhibition and apoptosis effects on human hepatocellular carcinoma cells in vitro, inhibited hepatoma growth in vivo.Conclusion
Alocasia macrorrhiza extract has potential cytotoxic and apoptotic effect on human hepatocellular carcinoma cells and inhibits hepatoma growth in vivo, its mechanism of action might be associated with the inhibition of DNA synthesis, cell cycle (G0/G1) arrest, apoptosis induction through up-regulation the mRNA and protein expressions of PPARγ, Rb, Bax and capase-3genes and down-regulation of the expressions of Cyclin D1 and Bcl-2 genes. 相似文献13.
Yan-Wei Hu Chun-Yu Liu Chong-Min Du Jian Zhang Wen-Qian Wu Zhen-Lun Gu 《Journal of ethnopharmacology》2009
Aim of the study
Flavonoids extracted from the seeds of Astragalus complanatus R.Br. reduce the proliferation of many cancer cells. The present study was carried out to evaluate the effects of these flavonoids from Astragalus complanatus (FAC) on human hepatocarcinoma cell viability and apoptosis and to investigate its mechanisms of action in SMMC-7721 cells.Materials and methods
Cell viability was measured using the MTT assay. To detect apoptotic cells, SMMC-7721 cells treated with FAC were stained with Hoechst 33258 and subjected to agarose gel electrophoresis. Quantitative detection of apoptotic cells was performed by flow cytometry. The effects of FAC on apoptosis and cell cycle regulatory genes and proteins in SMMC-7721 cells were examined using an S series apoptosis and cell cycle gene array and Western blot analysis.Results
The growth of SMMC-7721 and HepG2 cells was inhibited by treatment with FAC. Cell death induced by FAC was characterized by nuclear condensation and DNA fragmentation. Moreover, the cell cycle was arrested in the G0/G1 and S phases in FAC-treated SMMC-7721 cells. A sub-G1 peak with reduced DNA content was also formed. The activity of caspase-3 was significantly increased following FAC treatment. Microarray data indicated that the expression levels of 76 genes were changed in SMMC-7721 cells treated with FAC: 35 genes were up-regulated and 41 were down-regulated. Western blot analysis showed that caspase-3, caspase-8, Bax, P21, and P27 protein levels in SMMC-7721 cells were increased after 48 h of FAC treatment, while cyclinB1, cyclinD1, CDK1, and CDK4 protein levels were decreased.Conclusions
These results suggest that FAC may play an important role in tumor growth suppression by inducing apoptosis in human hepatocarcinoma cells via mitochondria-dependent and death receptor-dependent apoptotic pathways. 相似文献14.
Anti-inflammatory and antinociceptive activities of the ethanolic extract of Bougainvillea xbuttiana
A.L. Alvarez Perez Gil L. Barbosa Navarro M. Patipo Vera V.L. Petricevich 《Journal of ethnopharmacology》2012
Ethnopharmacological relevance
Bougainvillea xbuttiana is widely distributed in Mexico and it is used as an analgesic in folk medicine.Aim of the study
In the present study the in vivo antinociceptive and anti-inflammatory effects of the Bougainvillea xbuttiana ethanolic extract have been studied in mice.Materials and methods
The phytochemical analysis was performed. Antinociceptive activity was evaluated through writhing and formalin test in mice. The anti-inflammatory activity was determined with the carrageenan-induced mice paw oedema model. IL-6, IL-10 and IFN-γ levels were determined by enzyme-like immunosorbent assay, whereas TNF and nitrite levels were detected by standard assay with L929 cells and colorimetric Griess reactive, respectively.Results
The results showed that the ethanolic extract of the Bougainvillea xbuttiana has significant anti-inflammatory and antinociceptive activities, by inhibition of nociception induced by acetic acid and paw oedema. This extract also induced a decrease in TNF levels and an increase of IL-6, IFN-γ and NO levels that we observed up to 2 h. The highest levels of IL-10 were observed up to 4 h. The ratios of pro-/anti-inflammatory cytokines in sera from mice injected with the ethanolic extract, may be manifesting an anti-inflammatory status.Conclusions
The present study provides convincing evidences that Bougainvillea xbuttiana extract possesses significant anti-nociceptive and anti-inflammatory effects. 相似文献15.
Maria do Carmo Souza Angela Márcia Selhorst Beserra Dely Cristina Martins Vânia Villa Real Rogério Alexandre Nunes dos Santos Vietla Satyanarayana Rao Regilane Matos da Silva Domingos Tabajara de Oliveira Martins 《Journal of ethnopharmacology》2009
Aims of the study
Calophyllum brasiliense (Camb.) is a medicinal tree that grows particularly in the hilly and forested regions of Brazil. Preparations from its stem bark are popular remedies for the treatment of chronic ulcers. Since earlier investigations on bark extracts evidenced gastroprotective and gastric acid inhibitory properties, this study evaluated the effects of hydroethanolic extract (HEECb) and the dichloromethanic fraction (DCMF), from Calophyllum brasiliense stem bark, against Helicobacter pylori, in vitro and in vivo.Materials and methods
The in vitro assays were performed using the disk diffusion and broth microdilution methods to determine the minimum inhibitory concentration (MIC) values. The test substances were evaluated in vivo taking into account the delay in the gastric ulcer healing in Wistar rats, infected with Helicobacter pylori.Results
DCMF appeared the most active and potent in vitro against Helicobacter pylori growth with an MIC of 31 μg/mL. In the in vivo assays, rats ulcerated by acetic acid, and inoculated with Helicobacter pylori showed a marked delay in ulcer healing. Treatment with HEECb (50, 100 and 200 mg/kg) and DCMF (100 and 200 mg/kg) reduced the ulcerated area in a dose-dependent manner. While DCMF, at 200 mg/kg, increased the prostaglandin E2 (PGE2) level, both HEECb and DCMF decreased the number of urease-positive animals, as confirmed by the reduction of Helicobacter pylori presence in histopathological analysis.Conclusion
The results suggest that the antiulcer activity of Calophyllum brasiliense is due, in part, to its anti-Helicobacter pylori action, validating the popular use of this species. 相似文献16.
Seetharaman Rajasekar Da Jung Park Cheol Park Sejin Park Young Hoon Park Sun Tae Kim Yung Hyun Choi Young Whan Choi 《Journal of ethnopharmacology》2012
Ethnopharmacological relevance
Lithospermum erythrorhizon has long been used in traditional Asian medicine for the treatment of diseases including skin cancer. In this study, hexane extract from the roots of Lithospermum erythrorhizon (LEH) was chemically characterized and its anticancer activity was tested against the most aggressive form of skin cancer.Materials and methods
The in vitro anticancer studies viz. cell growth, cell cycle and apoptosis, and the expression of tumor regulating proteins were analyzed against B16F10 melanoma cells. In addition, C57BL/6 mice models were used to evaluate the in vivo anticancer potential of LEH. Mice were intraperitoneally injected with LEH at doses of 0.1 and 10 mg/kg every 3 days. The tumor inhibition ratio was determined after 21 days of treatment and the histopathological analyses of the tumor tissues were compared. Further, LEH was purified and its active compounds were structurally elucidated and identified by NMR spectra and quantified by HPLC analyses.Results
LEH effectively inhibits the growth of melanoma cells with an IC50 of 2.73 μg/ml. Cell cycle analysis revealed that LEH increased the percentage of cells in sub-G1 phase by dose dependent manner. LEH exhibited down regulation of anti-apoptotic Bcl-2 family proteins and up regulation of apoptotic Bax protein expression. Importantly, LEH induced cleavage of poly (ADP-ribose) polymerase (PARP) and activated the caspase cascade (caspase 3) with this cleavage mediating the apoptosis of B16F10 cells. LEH treatment at a dose of 10 mg/kg for 21 days in experimental mice implanted with tumors resulted in significant reduction of the tumor growth (43%) and weight (36%). Histopathology analysis of LEH treated tumor tissues showed evidence of increased necrotic cells in a concentration dependent manner. Meanwhile, five naphthoquinone compounds [Shikonin (1); Deoxyshikonin (2); β-Hydroxyisovalerylshikonin (3); Acetylshikonin (4) and Isobutyrylshikonin (5)] were purified from LEH and responsible for its anticancer activity.Conclusion
LEH induced apoptosis in B16F10 cells by activation of caspase 3 and inducing sub-G1 cell cycle arrest. LEH exhibited both in vitro and in vivo anticancer activity. Shikonin derivatives in the LEH are responsible for the anticancer activity. 相似文献17.
Daniela Rigano Carmen Formisano Felice Senatore Sonia Piacente Ester Pagano Raffaele Capasso Francesca Borrelli Angelo A. Izzo 《Journal of ethnopharmacology》2013
Ethnopharmacological relevance
In the Mediterranean Area, the flowers of Helichrysum italicum ssp. italicum are a traditional remedy for the treatment of intestinal complaints and are used as herbal tea for curing digestive, stomachic and intestinal diseases. In order to find scientific evidence for the traditional utilization of this plant, the effect of an ethanolic extract of Helichrysum italicum was investigated by using in vivo and in vitro experimental models. Then, through bioassay-guided fractionation procedures, active component(s) were identified.Material and methods
Contractility in vitro was evaluated by stimulating the isolated ileum, in an organ bath, with acetylcholine and barium chloride; motility in vivo was evaluated by measuring upper gastrointestinal transit, both in control mice and in mice with experimental intestinal inflammation induced by croton oil. Chromatographic separation techniques such as HPLC and silica gel columns have yielded the active principles of Helichrysum italicum.Results
We found that the ethanolic extract of Helichrysum italicum ssp. italicum flowers elicited antispasmodic actions in the isolated mouse ileum and inhibited transit preferentially in the inflamed gut. A bioassay guided fractionation of the extract yielded the known compounds 12-acetoxytremetone (1) and 2,3-dihydro-2-[1-(hydroxymethyl)ethenyl]-5-benzofuranyl]-ethanone (2).Conclusion
Present study supported the traditional use of Helichrysum italicum ssp. italicum flowers for intestinal complaints and through bioassay-guided fractionation procedures from the crude extract we showed that 12-acetoxytremetone (1) and 2,3-dihydro-2-[1-(hydroxymethyl)ethenyl]-5-benzofuranyl]-ethanone (2) acted in a synergistic way to produce an intestinal antispasmodic effect. 相似文献18.
Myung-Ja Youn Jin-Kyung Kim Seong-yeol Park Yunha Kim Channy Park Eun Sook Kim Kie-In Park Hong Seob So Raekil Park 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
Inonotus obliquus (Chaga mushroom), one of the widely known medicinal mushrooms, has been used to treat various cancers in Russia and most of Baltic countries for many centuries.Aim of the study
To examine the anti-proliferative effects of Inonotus obliquus extract on melanoma B16-F10 cells. Furthermore, to assess the anti-tumor effect of Inonotus obliquus extract in vivo in Balb/c mice.Materials and methods
The water extract of Inonotus obliquus was studied for anti-proliferative effects on the growth and morphology of B16-F10 melanoma cells and for anti-tumor effect using in vivo in Balb/c mice.Results
Inonotus obliquus extract not only inhibited the growth of B16-F10 cells by causing cell cycle arrest at G0/G1 phase and apoptosis, but also induced cell differentiation. These effects were associated with the down-regulation of pRb, p53 and p27 expression levels, and further showed that Inonotus obliquus extract resulted in a G0/G1 cell cycle arrest with reduction of cyclin E/D1 and Cdk 2/4 expression levels. Furthermore, the anti-tumor effect of Inonotus obliquus extract was assessed in vivo in Balb/c mice. Intraperitoneal administration of Inonotus obliquus extract significantly inhibited the growth of tumor mass in B16-F10 cells implanted mice, resulting in a 3-fold (relative to the positive control, *p < 0.05) inhibit at dose of 20 mg/kg/day for 10 days.Conclusion
This study showed that the water extract of Inonotus obliquus mushroom exhibited a potential anticancer activity against B16-F10 melanoma cells in vitro and in vivo through the inhibition of proliferation and induction of differentiation and apoptosis of cancer cells. 相似文献19.
Qijin Shu Minhe Shen Binbin Wang Qingli Cui Xiaoying Zhou Luming Zhu 《Journal of traditional Chinese medicine》2014
Objective
To explore the anticancer mechanism of aqueous extract of Taxus Chinensis (Pilger) Rehd (AETC).Methods
The serum pharmacological method was used to avoid interference from administration of the crude medicinal herbs. Eight purebred New Zealand rabbits were used for preparation of serum containing various concentrations of AETC. Forty-eight Balb/c-nu mice were used for in vivo experiments. The effects of serum containing AETC on the proliferation of A549 cells and expression levels of the epidermal growth factor receptor/mitogen-activated protein kinase (EGFR/MAPK) pathway-related proteins in vitro were investigated. Additionally, the effects on the growth of A549 xenografts in nude mice, and expression levels of the EGFR/MAPK pathway-related proteins in the xenografts, were investigated.Results
3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay revealed that the serum containing AETC significantly decreased the viability of A549 cells in a dose-dependent manner. Western blot showed that the serum containing various concentrations of AETC strongly reduced the levels of phospho-Jun N-terminal kinase (p-JNK) and phospho-extracellular signal-regulated kinasel/2 (ERK1/2) while it increased the level of p-p38. However, no significant effects on the expression levels of JNK, ERK1/2, and p38 MAPK were found. In addition, an anticancer effect from AETC was observed in vivo in the Balb/c-nu mice bearing A549 xenografts.Conclusion
AETC has significant effects on the growth of A549 xenografts and on the activity of the EGFR/MAPK pathway. Therefore, AETC may be beneficial in lung carcinoma treatment. 相似文献20.
Sandeep Kataria Dilsher Kaur Shaival Kamalaksha Rao Ravi K. Khajuria 《Journal of ethnopharmacology》2013