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1.
J Reprod Immunol ; 160: 104154, 2023 12.
Artigo em Inglês | MEDLINE | ID: mdl-37774536

RESUMO

Pelvic inflammatory disease (PID) is commonly encountered in gynecological practice. Kangfuxiaomi suppository, made from the compound extract of Periplaneta Americana, is a Traditional Chinese Medicine remedy widely used for the treatment of gynecological disorders. This study aimed to preliminarily explore the therapeutic effect of Kangfuxiaomi suppository in a rat model of PID established by chemical injury and pathogen infection. The key parameters assessed were vulvar inflammation score, vaginal + uterine organ index, and serum levels of interleukin (IL)- 8; tumor necrosis factor (TNF)-α; C-reactive protein (CRP); superoxide dismutase (SOD); and malondialdehyde (MDA). In addition, levels of IL-6, cyclooxygenase (COX)- 2, and IL-2 in cervical tissues as well as that of IL-1ß and prostaglandin E-2 (PGE2) in uterine tissues were measured. The expression levels of nuclear factor-kappa B (NF-κB) p65 and Toll-like receptor 4 (TLR4) in uterine tissues were detected by immunohistochemical method. After Kangfuxiaomi suppository treatment, the vulva inflammation score and histopathological score of PID rats showed a tendency to decrease. Serum IL-8, TNF-α, CRP, and MDA levels were reduced, while SOD levels were significantly increased. Levels of IL-6, IL-2, and COX-2 in cervical tissues were somewhat decreased, and PGE2 and IL-1ß levels in uterine tissue were significantly decreased. Moreover, the levels of NF-κB p65 and TLR4 protein expression were also decreased. These findings demonstrated the therapeutic effect of Kangfuxiaomi suppository in PID rats. The underlying mechanism may involve enhanced antioxidant capacity and decreased secretion of proinflammatory factors via the NF-κB/TLR4 signaling pathway.


Assuntos
NF-kappa B , Doença Inflamatória Pélvica , Humanos , Feminino , Ratos , Animais , NF-kappa B/metabolismo , Receptor 4 Toll-Like/metabolismo , Doença Inflamatória Pélvica/tratamento farmacológico , Interleucina-6 , Dinoprostona , Interleucina-2 , Fator de Necrose Tumoral alfa/metabolismo , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Superóxido Dismutase/uso terapêutico
2.
ACS Omega ; 8(32): 29735-29745, 2023 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-37599957

RESUMO

Nonalcoholic fatty liver disease (NAFLD) is a prevalent global condition and a common precursor to liver cancer, yet there is currently no specific medication available for its treatment. Ginseng, renowned for its medicinal and dietary properties, has been utilized in NAFLD management, although the precise underlying mechanism remains elusive. To investigate the effectiveness of ginsenoside Rd, we employed mouse and cell models to induce NAFLD using high-fat diets, oleic acid, and palmitic acid. We explored and confirmed the specific mechanism of ginsenoside Rd-induced hepatic steatosis through experiments involving mice with a liver-specific knockout of SIRT6, a crucial protein involved in metabolic regulation. Our findings revealed that administration of ginsenoside Rd significantly reduced the inflammatory response, reactive oxygen species (ROS) levels, lipid peroxide levels, and mitochondrial stress induced by oleic acid and palmitic acid in primary hepatocytes, thereby mitigating excessive lipid accumulation. Moreover, ginsenoside Rd administration effectively enhanced the mRNA content of key proteins involved in fatty acid oxidation, with a particular emphasis on SIRT6 and its target proteins. We further validated that ginsenoside Rd directly binds to SIRT6, augmenting its deacetylase activity. Notably, we made a significant observation that the protective effect of ginsenoside Rd against hepatic disorders induced by a fatty diet was almost entirely reversed in mice with a liver-specific SIRT6 knockout. Our findings highlight the potential therapeutic impact of Ginsenoside Rd in NAFLD treatment by activating SIRT6. These results warrant further investigation into the development of Ginsenoside Rd as a promising agent for managing this prevalent liver disease.

3.
Pharm Biol ; 61(1): 949-962, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37334466

RESUMO

CONTEXT: Periplaneta americana L. (Blattariae) is used as a treatment for ulcerative colitis (UC) in Chinese traditional medicine. OBJECTIVE: To evaluate the antioxidative activity of P. americana whole body ethanol extract (PAE) on UC mice and whether glycine and proline could be used for quality control and identification of active PAE components. MATERIALS AND METHODS: NCM460 cells were pre-incubated in PAE, AA-L, AA-M, and AA-H (low, high and medium doses of proline and glycine), then treated with recombinant human TNF-α. The glutathione (GSH), malondialdehyde (MDA), superoxide dismutase (SOD) and reactive oxygen (ROS) levels were determined. UC mice were fed with water containing 2.5% dextran sulfate sodium (w/v) after pre-treatment with different doses of PAE once a day for 7 days. ELISA was used to detect the concentrations of inflammation-related factors. Colon tissues of mice were used to detect the activity of myeloperoxidase (MPO), GSH, MDA, and SOD. Histological changes were observed using H&E staining. The expression of target proteins was determined by western blotting. RESULTS: In vivo, PAE treatment reduced the DAI score more than in the model group, restoring the weight and colonic length. It also reduced the severity of colitis, and inflammatory and oxidative stress intensity. Additionally, western blotting showed that the Nrf2 pathway was activated by PAE. In vitro PAE significantly alleviated TNF-α-induced cell damage and oxidative stress, which is relevant to the activation of the Nrf2 pathway. CONCLUSIONS: PAE may relieve oxidative stress through the Nrf2 signaling pathway, and proline and glycine may be used as active components of its antioxidative stress activity.


Assuntos
Colite Ulcerativa , Periplaneta , Camundongos , Humanos , Animais , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/metabolismo , Antioxidantes/uso terapêutico , Periplaneta/metabolismo , Sulfato de Dextrana/toxicidade , Fator 2 Relacionado a NF-E2/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Colo , Superóxido Dismutase/metabolismo , Modelos Animais de Doenças
4.
Inflammopharmacology ; 30(3): 907-918, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35303235

RESUMO

Ulcerative colitis (UC) is a chronic inflammatory bowel disease (IBD) with a low cure rate. Periplaneta americana is a traditional American Cockroach and reportedly has potential therapeutic roles for UC treatment; however, its mechanisms remain unclear. To address this, we investigated the therapeutic effects and underlying molecular mechanisms of Ento-A, a Periplaneta americana extract, in a dextran sulfate sodium (DSS)-induced chronic and recurrent UC mouse model. Ento-A treatment decreased pro-inflammatory cytokine secretion, disease activity index (DAI), colon mucosa damage index (CMDI), histopathological scores (HS), and increased colon length. Additionally, Ento-A effectively increased interleukin-4 (IL-4), and forkhead transcription factor protein 3 (Foxp3) expression levels, while it abated interferon-γ (IFN-γ) and IL-17 levels in spleen lymphocytes. Conversely, in mesenteric lymph nodes, IL-4 and Foxp3 expression were decreased, while IFN-γ and IL-17 expression was increased. Furthermore, Ento-A blocked p-PI3K, p-AKT,*and p-NF-κB activation. In conclusion, Ento-A improved UC symptoms and exerted therapeutic effects by regulating immune responses and inhibiting PI3K/AKT/NF-κB signaling.


Assuntos
Colite Ulcerativa , Colite , Periplaneta , Animais , Colite/tratamento farmacológico , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/patologia , Colo , Sulfato de Dextrana/farmacologia , Modelos Animais de Doenças , Fatores de Transcrição Forkhead/metabolismo , Imunidade , Interleucina-17/metabolismo , Interleucina-4/metabolismo , Camundongos , NF-kappa B/metabolismo , Periplaneta/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais
5.
Med Sci Monit Basic Res ; 27: e930887, 2021 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-33972493

RESUMO

BACKGROUND The aim of this study was to determine the effect of kangfuxin liquid (KFXL) on inflammatory response, and its underlying mechanism in treating acute ulcerative colitis (UC) in mice induced by dextran sulfate sodium (DSS). MATERIAL AND METHODS Mice were provided drinking water containing DSS (3%) for 7 days to induce acute enteritis. The mice were divided into 6 groups: a control group, a DSS-induced (vehicle) group, a sulfasalazine (SASP) group, and low-, medium-, and high-dose kangfuxin liquid groups. Disease activity index (DAI), colon mucosa damage index (CMDI), histopathological score (HS), and organ index were monitored daily. The levels of interleukin-1ß (IL-1ß), interleukin-10 (IL-10) in serum and interleukin-17 (IL-17) and epidermal growth factor (EGF) in colon tissue were assessed by enzyme-linked immunosorbent assay (ELISA). Flow cytometry was used to assess the changes of T lymphocyte subsets in spleens of mice to evaluate the therapeutic effect of drugs on acute UC in mice. RESULTS Different doses of kangfuxin liquid reduced the DAI, CMDI, and HS scores (P<0.01 or P<0.05) of acute UC mice, reduced the level of IL-1ß and IL-17 in serum, increased the expression of IL-10 in serum and EGF in colon tissue, increased the number of CD3⁺ T cells, and decreased the level of CD4⁺ T cells and the ratio of CD4⁺/CD8⁺. CONCLUSIONS Kangfuxin liquid has a therapeutic effect on DSS-induced acute UC in mice, and its mechanism of action may be associated with regulating immune function and reducing intestinal inflammatory response.


Assuntos
Colite Ulcerativa , Sulfato de Dextrana/toxicidade , Materia Medica/farmacologia , Substâncias Protetoras/farmacologia , Animais , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Modelos Animais de Doenças , Fator de Crescimento Epidérmico , Imunidade , Inflamação , Interleucina-10 , Interleucina-17 , Materia Medica/uso terapêutico , Camundongos , Substâncias Protetoras/uso terapêutico , Transdução de Sinais
6.
Acta Cir Bras ; 35(10): e202001002, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33237174

RESUMO

PURPOSE: To investigate the mechanism of Periplaneta americana extract promoting intestinal mucosal repair of OXZ-induced colitis in rat. METHODS: All experiments used an equal number of male and female SD rats (n=48). We injected OXZ into the colon to induce UC rat model. To determine the optimal concentration of P. Americana's extract (PA-40), it was classified into low (L), medium (M), and high (H) doses. After OXZ treatment, each drug was administered by enema for 7 consecutive days. Rats were divided into the following 6 groups: (1) Saline treatment group (NC), (2) OXZ treatment UC model group (MC), (3) OXZ + budesonide group (BUN), (4) OXZ + PA-40 L group, (5) OXZ + PA-40 M group, (6) OXZ + PA-40 H group. Disease activity index (DAI) scores, colon length, histopathological score, serum cytokine level (IL-4, IL-10, iNOS, tNOS), and amount of MPO, EGF, IL-13 in colonic mucosa were measured. RESULTS: PA treatment had a significant healing effect on the OXZ-colitis model and significantly reduced the lesioned area, especially in the PA-40H groups. PA treatment did not alter the expression of IL-10 and MPO level, but increased EGF (epidermal growth factor) and decrease IL-13 in the colonic tissue. PA inhibited the rise of NOSs (nitric oxide synthase) and decreased the serum IL-4 level. CONCLUSIONS: The data suggest that Periplaneta americana extract may be a potential compound for the treatment of colonic lesions. The mechanism may be related to inhibiting the secretion of IL-13 and promoting the formation of EGF.


Assuntos
Colite Ulcerativa , Periplaneta , Animais , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Colo , Feminino , Mucosa Intestinal , Masculino , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Sprague-Dawley
7.
Acta cir. bras ; 35(10): e202001002, 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1130615

RESUMO

Abstract Purpose: To investigate the mechanism of Periplaneta americana extract promoting intestinal mucosal repair of OXZ-induced colitis in rat. Methods: All experiments used an equal number of male and female SD rats (n=48). We injected OXZ into the colon to induce UC rat model. To determine the optimal concentration of P. Americana's extract (PA-40), it was classified into low (L), medium (M), and high (H) doses. After OXZ treatment, each drug was administered by enema for 7 consecutive days. Rats were divided into the following 6 groups: (1) Saline treatment group (NC), (2) OXZ treatment UC model group (MC), (3) OXZ + budesonide group (BUN), (4) OXZ + PA-40 L group, (5) OXZ + PA-40 M group, (6) OXZ + PA-40 H group. Disease activity index (DAI) scores, colon length, histopathological score, serum cytokine level (IL-4, IL-10, iNOS, tNOS), and amount of MPO, EGF, IL-13 in colonic mucosa were measured. Results: PA treatment had a significant healing effect on the OXZ-colitis model and significantly reduced the lesioned area, especially in the PA-40H groups. PA treatment did not alter the expression of IL-10 and MPO level, but increased EGF (epidermal growth factor) and decrease IL-13 in the colonic tissue. PA inhibited the rise of NOSs (nitric oxide synthase) and decreased the serum IL-4 level. Conclusions: The data suggest that Periplaneta americana extract may be a potential compound for the treatment of colonic lesions. The mechanism may be related to inhibiting the secretion of IL-13 and promoting the formation of EGF.


Assuntos
Animais , Masculino , Feminino , Ratos , Periplaneta , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Extratos Vegetais/farmacologia , Ratos Sprague-Dawley , Colo , Mucosa Intestinal
8.
Fitoterapia ; 139: 104389, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31669963

RESUMO

A new heterodimer, rynchopeterine F (1), a new natural product, rynchopeterine G (2), and eleven known phenolics were isolated from Blap rynchopetera Fairmaire, a kind of medicinal insect utilized by the Yi and Bai Nationality in Yunnan Province of China. Their structures were established on the basis of extensive spectroscopic analyses (1D and 2D NMR, HR-MS) along with calculated electronic circular dichroism method. Rynchopeterine F was a unusual heterodimer of a 3,4-dihudroxy phenylethanol unit fused to a 3,4-dihudroxy phenylacetyl group through two ester bonds with lactic acid, and rynchopeterine G was a 3,4-dihudroxy phenylethanyl monoester succinate. Attributed to the adjacent dihydroxyl grops, compounds 1 and 2 exhibited significant anti-radical activity with an IC50 value of 3.52 and 7.83 µg/mL for DPPH radical-scavenging, similar with that of the positive controls, vitamin C, 6.92 µg/mL and rutin, 8.28 µg/mL.


Assuntos
Besouros/química , Sequestradores de Radicais Livres/farmacologia , Fenóis/farmacologia , Animais , China , Sequestradores de Radicais Livres/isolamento & purificação , Ácido Láctico/química , Estrutura Molecular , Fenóis/isolamento & purificação , Álcool Feniletílico/química
9.
BMC Complement Altern Med ; 18(1): 309, 2018 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-30477490

RESUMO

BACKGROUNDS: Although the physical and mental enhancement effect of essential oils have been proved, the beneficial effect of essential oil in central fatigue remains unclear. In this study, we extracted essential oils from nine aromatic plants to make a compound essential oil, and detected the therapeutic effect of central fatigue by daily aerial diffusion. METHODS: Thirty-three rats were randomly and equally divided into control group, chronic sleep deprivation group, and compound essential oil inhalation group. Central fatigue was generated by chronic sleep deprivation. RESULTS: After 21-day various interferences, it is found that the sleep deprivation rats showed an evident decrease in physical endurance, negative emotion, and cognitive dysfunction compared with the control group, and the group that treated with the compound essential oil behaved significantly better than central fatigue group. CONCLUSION: We concluded that this formula of essential oils could alleviate central fatigue on rats, and our study provides a new direction of application of aromatic therapy, which could be expanded to insomnia, depression and other healthy issue in the further research.


Assuntos
Fadiga/tratamento farmacológico , Óleos Voláteis/administração & dosagem , Óleos de Plantas/administração & dosagem , Administração por Inalação , Animais , Fadiga/fisiopatologia , Humanos , Masculino , Óleos Voláteis/química , Óleos de Plantas/química , Ratos , Ratos Wistar , Sono , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico , Distúrbios do Início e da Manutenção do Sono/fisiopatologia
10.
Artigo em Inglês | MEDLINE | ID: mdl-30151021

RESUMO

The traditional Chinese medicine (TCM) decoction Si-Ni-San (SNS) has been utilised for millennia to improve physiological coordination of the functions of the liver and spleen, which are regarded as the main pathological organs of central fatigue in TCM. This study evaluates the effect of a modified SNS (MSNS) formula on central fatigue in rats and explores molecular changes associated with hippocampal mitochondrial biogenesis. Central fatigue was induced through a 21-day sleep deprivation protocol. We assessed MSNS's effects on behaviour, blood and liver biomarkers, and mitochondrial ultrastructure. We found that MSNS could reverse various signs of central fatigue such as its effects on hippocampal gene and protein expression levels of sirtuin 1 (SIRT1), peroxisome proliferator-activated receptor gamma coactivator-1α (PGC-1α), and nuclear respiratory factor 1 (NRF1). We also observed evidence of MSNS decreasing central fatigue, such as decreasing creatine kinase activity, decreasing levels of malondialdehyde and blood urea nitrogen, increasing lactate dehydrogenase and superoxide dismutase activities, increasing mitochondrial DNA copy number, and reversing mitochondrial ultrastructure changes. These findings suggest that MSNS can ameliorate central fatigue and that its molecular mechanism involves mitochondrial biogenesis enhancement mediated by hippocampal SIRT1, PGC-1α, and NRF1.

11.
Molecules ; 23(1)2017 Dec 21.
Artigo em Inglês | MEDLINE | ID: mdl-29267186

RESUMO

Blaps rynchopetera Fairmaire has long been used as a folk medicine by the Yi and Bai ethnic groups in China to treat fever, cough, gastritis, boils, and tumors. In the present study, the cytotoxicity of the defensive secretion (TDS) of B. rynchopetera against AGS Caco-2, HepG2 U251 and Bel-7402 was tested, and the results revealed that TDS had potent cytotoxicity against testing cells with IC50 values of 45.8, 17.4, 53.6, 98.4 and 23.4 µg/mL, respectively. Gas chromatography-mass spectrometry (GC-MS) analysis was employed to clarify the cytotoxic constituents in TDS of B. rynchopetera and five volatile compounds, including 2-ethyl-2,5-cyclohexadiene-1,4-dione (3, 31.00%), 1-tridecene (5, 28.02%), 2-methyl-2,5-cyclohexadiene-1,4-dione (2, 22.86%), hydroquinone (4, 1.33%), and p-benzoquinone (1, 1.01%), were identified. Chemical constituent investigation on TDS further supported the presence of 5 above compounds. A cytotoxic assay indicated that compounds 1, 2, 3 and 4 exhibited significant cytotoxicity against the testing cell lines, implying that benzoquinones and hydroquinone played important roles in the cytotoxicity of TDS of B. rynchopetera. TDS is a cytotoxic natural material and further studies investigating mechanisms and inhibitory activities on other cell lines is warranted.


Assuntos
Antineoplásicos/química , Secreções Corporais/química , Compostos Orgânicos Voláteis/química , Alcenos/química , Alcenos/farmacologia , Animais , Antineoplásicos/farmacologia , Benzoquinonas/química , Benzoquinonas/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular , Besouros , Cicloexenos/química , Cicloexenos/farmacologia , Humanos , Hidroquinonas/química , Hidroquinonas/farmacologia , Estrutura Molecular , Compostos Orgânicos Voláteis/farmacologia
12.
Zhongguo Zhong Yao Za Zhi ; 37(2): 158-64, 2012 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-22737843

RESUMO

The recent research progress of the utilization of natural drugs for the treatment of liver fibrosis in China and other countries was reviewed. Forty reported remedies were summarized and classified into 3 categories, that is, the single herbal drugs (rhizome, leaf, fruit, bark, peel, flower, whole plants, and oil), traditional Chinese medicine prescriptions and animal drugs. The future directions of the R&D of new natural drugs against liver fibrosis were discussed and some suggestions were provided.


Assuntos
Produtos Biológicos/uso terapêutico , Pesquisa Biomédica/métodos , Cirrose Hepática/tratamento farmacológico , Medicina Tradicional Chinesa/métodos , Animais , Pesquisa Biomédica/tendências , China , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Medicina Tradicional Chinesa/tendências , Fitoterapia
13.
Fitoterapia ; 83(3): 568-85, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22248534

RESUMO

Twenty-nine phenolic compounds were isolated from the root bark of fresh (Yunnan) ginger and their structures fully characterized. Selected compounds were divided into structural categories and twelve compounds subjected to in-vitro assays including DPPH radical scavenging, xanthine-oxidase inhibition, monoamine oxidase inhibition, rat-brain homogenate lipid peroxidation, and rat pheochromocytoma PC12 cell and primary liver cell viability to determine their antioxidant and cytoprotective properties. Isolated compounds were also tested against nine human tumor cell lines to characterize anticancer potency. Several diarylheptanoids and epoxidic diarylheptanoids were effective DPPH radical scavengers and moderately effective at inhibiting xanthine oxidase. An enone-dione analog of 6-shogaol (compound 2) was isolated and identified to be most effective at protecting PC12 cells from H2O2-induced damage. Almost all tested compounds inhibited lipid peroxidation. Three compounds, 6-shogaol, 10-gingerol and an enone-diarylheptanoid analog of curcumin (compound 6) were identified to be cytotoxic in cell lines tested, with KB and HL60 cells most susceptible to 6-shogaol and the curcumin analog with IC50<10 µM. QSAR analysis revealed cytotoxicity was related to compound lipophilicity and chemical reactivity. In conclusion, we observed distinct compounds in fresh ginger to have biological activities relevant in diseases associated with reactive oxygen species.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Catecóis/farmacologia , Neoplasias/tratamento farmacológico , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Zingiber officinale/química , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/isolamento & purificação , Antioxidantes/uso terapêutico , Compostos de Bifenilo/metabolismo , Catecóis/isolamento & purificação , Catecóis/uso terapêutico , Curcumina/isolamento & purificação , Curcumina/farmacologia , Curcumina/uso terapêutico , Citoproteção , Álcoois Graxos/isolamento & purificação , Álcoois Graxos/farmacologia , Álcoois Graxos/uso terapêutico , Células HL-60 , Humanos , Peróxido de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Células KB , Peroxidação de Lipídeos/efeitos dos fármacos , Células PC12 , Fenóis/isolamento & purificação , Fenóis/uso terapêutico , Fitoterapia , Picratos/metabolismo , Casca de Planta , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Raízes de Plantas , Ratos , Xantina Oxidase/metabolismo
14.
Integr Cancer Ther ; 10(3): NP12-23, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21733985

RESUMO

The organic extract of Periplaneta americana L. (Dictyoptera; Blattidae) has been traditionally used in southwestern China as an alternative medicine against disorders such as hepatitis, trauma, gastric ulcers, burns, and heart disease. The present study describes bioassay-guided purification and chemotherapeutic evaluation of the 60% ethanolic fraction of P americana organic extracts (PAE60). The most effective cytotoxic fraction was determined by way of repeated in vitro screenings against 12 distinct cultured human carcinoma cell lines: Eca 109, BGC823, HO8910, LS174T, CNE, HeLa, K562, PC-3, A549, BEL 7404, HL-60, and KB, followed by in vivo antitumor assays of the lead fraction (PAE60). The complexity of enriched active fraction was qualitatively evaluated using thin layer chromatography. Reconstituted PAE60 was effective at inhibiting HL-60, KB, CNE, and BGC823 cell growth with IC(50) values <20 µg mL-(1). PAE60 reduced tumor growth in S180-bearing immunocompetent mice by 72.62% after 10 days following oral doses of 500 mg kg d-(1) compared with 78.75% inhibition following 40 mg kg d-(1) of cyclophosphamide (CTX). Thymus and spleen indices of S180-bearing mice treated with PAE60 were significantly greater (P < .05) than CTX treatment groups, suggesting potential immunomodulation of antitumor host defenses by PAE60. Antiviral activity was also investigated and PAE60 inhibited herpes simplex type-2 replication (IC(50) = 4.11 ± 0.64 µg mL-(1)) with a selectivity index (CC(50) to IC(50) ratio) of 64.84 in Vero cells but was less effective on type-1 virus (IC(50) of 25.6 ± 3.16 µg mL-(1)). These results support future clinical trials on P. americana as an alternative or complementary medicinal agent.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Periplaneta/química , Extratos de Tecidos/química , Extratos de Tecidos/farmacologia , Animais , Antivirais/química , Antivirais/farmacologia , Linhagem Celular Tumoral , Chlorocebus aethiops , Ciclofosfamida/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Células HeLa , Herpesvirus Humano 1/efeitos dos fármacos , Herpesvirus Humano 2/efeitos dos fármacos , Humanos , Células K562 , Células KB , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos ICR , Distribuição Aleatória , Células Vero
15.
J Ethnopharmacol ; 126(1): 50-6, 2009 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-19703545

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Laggera alata, as a traditional Chinese herbal medicine, has been widely used to ameliorate some ailments associated with inflammation including hepatitis in folk. AIM OF THE STUDY: Based on anti-inflammatory activity of total phenolics from Laggera alata (TPLA), to further validate the remarkable curative effect Laggera alata in hepatitis, hepatoprotective effect of TPLA was examined. MATERIALS AND METHODS: TPLA was prepared and its principle components were quantificationally analyzed. The hepatoprotective effects of TPLA were studied using a CCl(4)-induced injury model in primary cultured neonatal rat hepatocytes, and a CCl(4)-induced acute and chronic damage model in vivo. RESULTS: TPLA significantly reduced cellular leakage of hepatocyte aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and improved cell viability in vitro. TPLA markedly decreased the serum AST and ALT levels of the mice, the levels of AST, ALT, total protein, albumin, and sialic acid in rat serum, and the hydroxyproline level in rat liver. Meanwhile, severe hepatic lesions induced by CCl(4) in mice/rats were remarkably improved by the administration of TPLA. CONCLUSIONS: This investigation verifies the hepatoprotective effect of TPLA in vitro/in vivo and clarifies its active components dicaffeoylquinic acids responsible for hepatoprotective potential.


Assuntos
Asteraceae/química , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Hepatócitos/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/uso terapêutico , Ácido Quínico/análogos & derivados , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Proteínas Sanguíneas/efeitos dos fármacos , Tetracloreto de Carbono , Sobrevivência Celular/efeitos dos fármacos , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Medicamentos de Ervas Chinesas/uso terapêutico , Hepatócitos/metabolismo , Hepatócitos/patologia , Hidroxiprolina/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Ácido N-Acetilneuramínico/sangue , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Albumina Sérica/efeitos dos fármacos
16.
Chem Biodivers ; 6(7): 1053-65, 2009 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-19623551

RESUMO

A phytochemical investigation of the roots of Ligularia atroviolacea resulted in the isolation of 24 compounds including seven new eremophilanoids named eremophila-3,7(11),8-triene-12,8;14,6alpha-diolide (1), 3beta-(angeloyloxy)eremophil-7(11)-en-12,8beta-olid-14-oic acid (2), 1alpha-chloro-10beta-hydroxy-6beta-(2-methylpropanoyloxy)-9-oxo-7,8-furoeremophilane (3), (10betaH)-8-oxoeremophila-3(4),6(7)-diene-12,14-dioic acid (4), (10alphaH)-8-oxoeremophila-3(4),6(7)-diene-12,14-dioic acid (5), 8beta-[eremophila-3',7'(11')-diene-12',8'alpha;14',6'alpha-diolide]eremophila-3,7(11)-diene-12,8alpha;14,6alpha-diolide (6), and ligulatrovine A (7), eleven known eremophilanoids, 8-18, four steroids, one glucose derivative, and one fatty acid. The structures of these compounds were elucidated by spectroscopic methods including 2D-NMR experiments. The structure of 3 was also established by an X-ray diffraction study. The in vitro cytotoxicity evaluation of selected compounds was performed on seven cultured tumor cell lines, i.e., KB, BEL-7404, A549, HL-60, HeLa, CNE, and P-388D1. The preliminary taxonomy of this species was also discussed, and the possible biogenesis of a dimer possessing a new noreremophilanoid type skeleton, 7, is presented in a preliminary form.


Assuntos
Antineoplásicos Fitogênicos/toxicidade , Asteraceae/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Conformação Molecular , Compostos Orgânicos/química , Compostos Orgânicos/isolamento & purificação , Compostos Orgânicos/toxicidade , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Raízes de Plantas/química , Plantas Medicinais/química
17.
Food Chem Toxicol ; 45(8): 1349-55, 2007 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-17329003

RESUMO

Although Laggera pterodonta as a folk medicine has been widely used for several centuries to ameliorate some inflammatory ailments as hepatitis in China, there have been no studies of the hepatoprotective and antioxidative effects of this plant. In this paper, the hepatoprotective effect of total phenolics from L. pterodonta (TPLP) against CCI4-, D-GalN-, TAA-, and t-BHP-induced injury was examined in primary cultured neonatal rat hepatocytes. TPLP inhibited the cellular leakage of two enzymes, hepatocyte ASAT and ALAT, caused by these chemicals and improved cell viability. Moreover, TPLP afforded much stronger protection than the reference drug silibinin. Meanwhile, DPPH and superoxide radicals scavenging activities of TPLP were also determined. The present investigation is the first to report chemical-induced injury model in primary cultured neonatal rat hepatocytes and provide evidence for the hepatoprotective and antioxidative effects of L. pterodonta. Neutralizing reactive oxygen species by nonenzymatic mechanisms may be one of main mechanisms of TPLP against chemical-induced hepatocyte injury. Furthermore, The total phenolic content of L. pterodonta and its main component type were quantified, and its principle components isochlorogenic acids were isolated and authenticated. These data support the folkloric uses of L. pterodonta in the treatment of hepatitis.


Assuntos
Asteraceae/química , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Medicamentos de Ervas Chinesas/farmacologia , Ácido Quínico/análogos & derivados , Alanina Transaminase/metabolismo , Animais , Animais Recém-Nascidos , Antioxidantes/química , Antioxidantes/farmacologia , Aspartato Aminotransferases/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/enzimologia , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Ácido Clorogênico/análogos & derivados , Ácido Clorogênico/química , Ácido Clorogênico/farmacologia , Medicamentos de Ervas Chinesas/química , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Hepatócitos/efeitos dos fármacos , Concentração Inibidora 50 , Monossacarídeos/química , Monossacarídeos/farmacologia , Ácido Quínico/química , Ácido Quínico/farmacologia , Ratos , Ratos Sprague-Dawley , Superóxidos/metabolismo , Xenobióticos/toxicidade
18.
J Enzyme Inhib Med Chem ; 21(4): 399-404, 2006 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-17059172

RESUMO

In this work, we evaluated the antioxidant properties of the eight novel silybin analogues for their capacity to scavenge free radicals including superoxide anion radicals and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals in vitro. Compound 7d demonstrated an excellent antioxidant effect in scavenging superoxide anion free radical with an IC50 value of 26.5 microM, while the IC50 of quercetin (the reference compound) was 38.1 microM. Compounds 7b, 7e, 7h showed certain scavenging activities for both types of free radicals.


Assuntos
Antioxidantes/farmacologia , Compostos de Bifenilo/química , Sequestradores de Radicais Livres/síntese química , Hidrazinas/química , Quercetina/química , Ânions , Antioxidantes/química , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Sequestradores de Radicais Livres/química , Concentração Inibidora 50 , Modelos Químicos , Picratos , Silibina , Silimarina/química , Espectrofotometria , Superóxidos/química
19.
J Ethnopharmacol ; 108(2): 243-50, 2006 Nov 24.
Artigo em Inglês | MEDLINE | ID: mdl-16814499

RESUMO

The anti-inflammatory effect of total phenolics from Laggera alata (TPLA) was evaluated with various in vivo models of both acute and chronic inflammations. In the acute inflammation tests, TPLA inhibited significantly xylene-induced mouse ear oedema, carrageenan-induced rat paw oedema and acetic acid-induced mouse vascular permeability. In the carrageenan-induced rat pleurisy model, TPLA significantly suppressed inflammatory exudate and leukocyte migration, reduced the serum levels of lysozyme (LZM) and malondialdehyde (MDA), increased the serum levels of superoxide dismutase (SOD) and glutathione peroxidase (GSH-PX), and also decreased the contents of total protein, nitric oxide (NO) and prostaglandin E(2) (PGE(2)) in the pleural exudates. In the chronic inflammation experiment, TPLA inhibited significantly cotton pellet-induced rat granuloma. These results indicated that TPLA possesses potent anti-inflammatory activity on acute and chronic inflammation models. Its anti-inflammatory mechanisms are probably associated with the inhibition of prostaglandin formation, the influence on the antioxidant systems, and the suppression of LZM release. Furthermore, the total phenolic content of Laggera alata and its main component type was quantified, and its principle components were isolated and authenticated. Acute toxicity studies revealed that TPLA up to an oral dose of 8.5 g/kg body weight was almost nontoxic in mice.


Assuntos
Asteraceae/química , Inflamação/prevenção & controle , Ácido Quínico/análogos & derivados , Doença Aguda , Animais , Permeabilidade Capilar/efeitos dos fármacos , Carragenina , Doença Crônica , Dexametasona/uso terapêutico , Orelha Externa/efeitos dos fármacos , Orelha Externa/patologia , Edema/induzido quimicamente , Edema/prevenção & controle , Glutationa Peroxidase/sangue , Inflamação/induzido quimicamente , Inflamação/metabolismo , Masculino , Malondialdeído/sangue , Camundongos , Camundongos Endogâmicos ICR , Muramidase/sangue , Óxido Nítrico/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Pleurisia/sangue , Pleurisia/induzido quimicamente , Pleurisia/prevenção & controle , Ácido Quínico/química , Ácido Quínico/isolamento & purificação , Ácido Quínico/uso terapêutico , Ratos , Ratos Sprague-Dawley , Superóxido Dismutase/sangue , Xilenos
20.
Phytother Res ; 20(7): 585-90, 2006 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-16673449

RESUMO

The antiinflammatory effect of the total flavonoids of Laggera pterodonta (TFLP) was evaluated with various in vivo models of both acute and chronic inflammation. In the acute inflammation tests, TFLP significantly inhibited xylene-induced mouse ear oedema, carrageenan-induced rat paw oedema and acetic acid-induced mouse vascular permeability. In the carrageenan-induced rat pleurisy model, TFLP efficiently suppressed inflammatory exudate and leukocyte migration, reduced the serum levels of lysozyme (LZM) and malondialdehyde (MDA), increased the activity of serum superoxide dismutase (SOD), and also decreased the contents of total protein, nitric oxide (NO) and prostaglandin E2 (PGE2) in the pleural exudates. No marked effect of TFLP on the activity of serum glutathione peroxidase (GSH-PX) was observed. In the chronic inflammation experiment, TFLP inhibited cotton pellet-induced rat granuloma. The antiinflammatory mechanisms of TFLP are probably associated with the inhibition of prostaglandin formation, influence on the antioxidant systems and the suppression of LZM release. The acute toxicity study revealed that TFLP was nontoxic in mice up to an oral dose of 7.5 g/kg body weight.


Assuntos
Anti-Inflamatórios/farmacologia , Asteraceae/química , Flavonoides/farmacologia , Inflamação/tratamento farmacológico , Doença Aguda , Animais , Anti-Inflamatórios/química , Carragenina/toxicidade , Doença Crônica , Relação Dose-Resposta a Droga , Flavonoides/química , Inflamação/induzido quimicamente , Masculino , Camundongos , Camundongos Endogâmicos ICR , Ratos , Ratos Sprague-Dawley , Xilenos/toxicidade
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