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1.
Curr Neurovasc Res ; 19(3): 275-281, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35996236

RESUMO

OBJECTIVE: This study aimed to explore and analyze the effect of acupuncture on improving the enteral nutrition level and gastrointestinal dynamics in patients who had suffered a severe stroke. METHODS: A total of 122 patients who experienced a severe stroke who were treated in the intensive care unit of the Affiliated Hospital of Hebei University (China) between September 2021 and March 2022 were randomly divided into two groups as follows: 1) the observation group, the participants of which received acupuncture combined with early enteral nutrition (61 cases); 2) the control group, the participants of which received early enteral nutrition (61 cases). Following treatment, the hemoglobin, neutrophil count, blood glucose, albumin, pre-albumin, immediate postprandial antral area, antral contraction frequency (at 2 min), and antral motility index on days 1 and 7 of treatment were compared between the two groups. RESULTS: The total clinical effective rate was 96.72% in the observation group and 77.05% in the control group. The curative effect comparison between the two groups after seven days of treatment showed a lower probability of gastrointestinal bleeding, faster recovery of gastrointestinal motility, and a higher level of nutrient absorption in the observation group. Serum albumin, pre-albumin, hemoglobin, total lymphocyte count, immediate postprandial maximum (max) and minimum (mix) area of the gastric antrum, antral contraction frequency (at 2 min), and antral motility index were higher in the observation group than in the control group (P < 0.05). The difference in blood glucose levels between the two groups was not statistically significant (P > 0.05). CONCLUSION: Acupuncture improved the enteral nutrition status of patients who had suffered a severe stroke and promoted gastrointestinal motility. The combination of acupuncture and early enteral nutrition could reduce damage to the gastrointestinal mucosal barrier caused by stress, changes in metabolism, and improved gastrointestinal function.


Assuntos
Terapia por Acupuntura , Acidente Vascular Cerebral , Humanos , Nutrição Enteral/efeitos adversos , Glicemia , Acidente Vascular Cerebral/complicações , Acidente Vascular Cerebral/terapia , Albuminas
2.
Molecules ; 27(5)2022 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-35268807

RESUMO

Oxytropis falcata Bunge is a plant used in traditional Tibetan medicine, with reported anti-inflammatory and antioxidants effects and alleviation of myocardial ischemia reperfusion injury (MIRI). However, the underlying mechanism against MIRI and the phytochemical composition of O. falcata are vague. One fraction named OFF1 with anti-MIRI activity was obtained from O. falcata, and the chemical constituents were identified by ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS). The potential targets and signaling pathways involved in the action of O. falcata against MIRI were predicted by network pharmacology analysis, and its molecular mechanism on MIRI was determined by in vitro assays. The results revealed that flavonoids are the dominant constituents of OFF1. A total of 92 flavonoids reported in O. falcata targeted 213 potential MIRI-associated factors, including tumor necrosis factor (TNF), prostaglandin-endoperoxide synthase 2 (PTGS2), and the NF-κB signaling pathway. The in vitro assay on H9c2 cardiomyocytes subjected to hypoxia/reoxygenation injury confirmed that the flavonoids in OFF1 reduced myocardial marker levels, apoptotic rate, and the inflammatory response triggered by oxidative stress. Moreover, OFF1 attenuated MIRI by downregulating the ROS-mediated JNK/p38MAPK/NF-κB pathway. Collectively, these findings provide novel insights into the molecular mechanism of O. falcata in alleviating MIRI, being a potential therapeutic candidate.


Assuntos
Traumatismo por Reperfusão Miocárdica , Oxytropis , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Traumatismo por Reperfusão Miocárdica/metabolismo , NF-kappa B/metabolismo , Oxytropis/química , Transdução de Sinais
3.
Bioorg Chem ; 111: 104886, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33836342

RESUMO

Our present and previous phytochemical investigations on Leptopus lolonum have resulted in the isolation of almost 30 phenylpropanoid-conjugated pentacyclic triterpenoids (PCPTs). During the continuous study on PCPTs, this kind of triterpenoid ester is considered as a natural product with low toxicity because of it's widely distribution in natural plants and edible fruits including kiwi fruit, durian, jujube, pawpaw, apple and pear. In the present work, we report the isolation, structural elucidation and cytotoxic evaluation of four new PCPTs (1-4) which obtained from L. lolonum. In addition, the possible biosynthesis pathway for 28-norlupane triterpenoid and potent effect of phenylpropanoid moiety for increasing the cytotxic effect of triterpenoids were also discussed. Among these compounds, compound 1 exhibited the highest cytotoxic effect on HepG2 cells with IC50 value of 11.87 µM. Further flow cytometry and western blot analysis demonstrated that 1 caused G1 cell cycle arrest by up-regulated the expression of phosphorylated p53 protein in HepG2 cells and induced cell apoptosis via MAPK and Akt pathways. These results emphasized the potential of PCPTs as lead compounds for developing anti-cancer drugs.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Malpighiales/química , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais/química , Propanóis/química , Propanóis/isolamento & purificação , Propanóis/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Relação Estrutura-Atividade , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
4.
Pharmazie ; 76(2): 55-60, 2021 02 25.
Artigo em Inglês | MEDLINE | ID: mdl-33714280

RESUMO

Ferulic acid, a hydroxyl derivative extracted from plants, is abundant in free state in seeds and leaves, or covalently linked with cell wall polysaccharides, lignin and different polymers. It has various pharmacological activities, including antioxidant and anti-inflammatory effects, regulates immunity, protects the cardiovascular system, and contributes to the prevention of tumors and diabetes. The protective effect on cardiovascular system is the most valuable one in view of clinical application. Here, we are reviewing the research progress concerning the pharmacological effects of ferulic acid and its derivatives on cardiovascular diseases in the past five years, mainly focusing on mechanisms of action and clinical application. This should provide guidance for clinical applications of ferulic acid and its derivatives in the treatment of cardiovascular diseases.


Assuntos
Doenças Cardiovasculares/tratamento farmacológico , Ácidos Cumáricos/farmacologia , Animais , Humanos , Extratos Vegetais , Plantas/química
5.
Bioorg Chem ; 107: 104628, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33461038

RESUMO

Most of Euphorbiaceae plants are considered as folk medicinal plants because of their various pharmacological effects. However, there are eight Leptopus genus plants which belong to Euphorbiaceae have never be investigated. Thus, four Leptopus genus plants were collected to study their chemical constituents and pharmacological activities. In the present work, the cytotoxicities of the extracts of four Leptopus genus plants were evaluated before phytochemical experiments. And nine new phenylpropanoid-conjugated pentacyclic triterpenoids, along with twenty-two known compounds were isolated from the whole plants of Leptopus lolonum. The structures of these new compounds were unequivocally elucidated by HRESIMS and 1D/2D NMR data. All triterpenoids were screened for their cytotoxicities against four cancer cell lines including HepG2, MCF-7, A549 and HeLa. Among these isolates, the triterpenoid with a phenylpropanoid unit showed increasing cytotoxicity on cancer cells, which suggested the importance of the phenylpropanoid moiety.


Assuntos
Antineoplásicos Fitogênicos/química , Malpighiales/química , Propanóis/química , Triterpenos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Malpighiales/metabolismo , Conformação Molecular , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Plantas Medicinais/química , Plantas Medicinais/metabolismo , Relação Estrutura-Atividade , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
6.
Chem Biodivers ; 16(7): e1900170, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31134745

RESUMO

The tumor-suppressor function of p53 makes it an attractive drug target. Efforts were mostly put on stabilization of the functional p53 or reactivation of mutated p53. Previous studies have shown that small molecules targeting Loop1/Sheet3 (L1/S3) can reactivate the R175H-p53 and stabilize p53 in vitro. Since the L1/S3 pocket is shared by the mutate and the wild type (WT) p53, virtual screening is introduced to identify natural products targeting the L1/S3 of WT p53. Considering the high flexibility of Loop1, ensemble docking method is utilized for different clusters of the L1/S3. Seven conformations were chosen for docking. As one of the 181 selected candidates, torilin not only improved p53 activity, but also increased p21 protein expression level, which lies downstream of p53, therefore suppressing HCT116 cancer cell growth. Torilin may covalently bind to Cys124 of p53 by 2-methyl-2-butenal (2M2B) group, as torilin derivatives, which do not contain the 2M2B group, were not able to increase the p53 transcription activity. In conclusion, this study demonstrated that L1/S3 of WT-p53 is a druggable pocket, and torilin has a potential cytotoxicity through activating the p53 pathway.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Descoberta de Drogas , Simulação de Acoplamento Molecular , Proteína Supressora de Tumor p53/antagonistas & inibidores , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Células HCT116 , Células HT29 , Humanos , Conformação Molecular , Simulação de Dinâmica Molecular , Relação Estrutura-Atividade , Células Tumorais Cultivadas , Proteína Supressora de Tumor p53/metabolismo
7.
Zhongguo Zhong Yao Za Zhi ; 44(24): 5358-5362, 2019 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-32237380

RESUMO

The ginseng endophytic bacteria F1 is a potential biocontrol agent for ginseng bacterial soft rot. In this paper,the chemotactic response of ginseng endophytic bacteria F1 on 8 kinds of sugar and amino acids was detected by capillary method to explore its biocontrol mechanism. The chemotactic response of F1 strain to 4 kinds of better chemotaxis substances such as glucose,glycine,L-rhamnoseand L-glutamic acid under parameters( concentration,time,temperature and pH) was studied. The results showed that under the same experimental conditions( incubation temperature 25 ℃,incubation time 60 min,chemotaxis concentration 1 mg·L~(-1)),ginseng endophytic bacteria F1 showed different degrees of response to the eight substances tested. The phenomenon of positive chemotaxis of the measured sugars and amino acids was obvious,and the chemotactic response to total ginsenosides was low. The degree of chemotaxis response is positively correlated with the chemotaxis index within a certain range of parameters,but as the temperature,p H,time,concentration and other factors continue to increase,the chemotaxis effect decreases,and F1 optimizes the chemotaxis of the four substances. The parameters are as follows: glucose: 25 ℃,10 mg·L~(-1),45 min,pH 7; glycine: 30 ℃,10 mg·L~(-1),75 min,pH7; L-rhamnose: 30 ℃,1 mg·L~(-1),30 min,pH 6; L-glutamic acid: 25 ℃,0. 1 mg·L~(-1),45 min,pH 8. The chemotactic response is more sensitive to low concentrations of chemotactic substances.


Assuntos
Bactérias/efeitos dos fármacos , Quimiotaxia , Endófitos/fisiologia , Panax/química , Exsudatos de Plantas/farmacologia , Aminoácidos/farmacologia , Endófitos/efeitos dos fármacos , Ginsenosídeos/farmacologia , Açúcares/farmacologia
8.
Acta Pharmacol Sin ; 40(5): 608-619, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30315252

RESUMO

Tamoxifen (TMX) is an antiestrogen drug that is used in the treatment and prevention of all stages of estrogen-dependent breast cancer. Adverse effects of TMX include hepatotoxicity. In this study, we investigated the therapeutic effects of osthole, isolated from medicinal plants especially Fructus Cnidii, on TMX-induced acute liver injury in mice. Mice were injected with osthole (100 mg/kg, ip) or vehicle, followed by TMX (90 mg/kg, ip) 24 h later. We showed that a single injection of TMX-induced liver injury and oxidative stress. Pretreatment with osthole attenuated TMX-induced liver injury evidenced by dose-dependent reduction of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities. Pretreatment with osthole also blunted TMX-induced oxidative stress, evidenced by significant increase of reduced glutathione (GSH) as well as reduction of malondialdehyde (MDA) and hydrogen peroxide (H2O2). Consistently, osthole significantly enhanced the expressions of antioxidant genes (GPX1, SOD2, GCL-c, and G6pdh), but suppressed those of pro-oxidant genes (NOX2 and ACOX). Furthermore, osthole inhibited the production of inflammatory cytokines, reduced the metabolic activation of TMX, and promoted its clearance. We further revealed that osthole elevated hepatic cAMP and cGMP levels, but inhibition of PKA or PKG failed to abolish the hepatoprotective effect of osthole. Meanwhile, prominent phosphorylation of p38 was observed in liver in response to TMX, which was significantly inhibited by osthole. Pretreatment with SB203580, a p38 inhibitor, significantly attenuated TMX-induced increase of ALT and AST activities, reduced oxidative stress, and reversed the alterations of gene expression caused by TMX. Moreover, pretreatment with L-buthionine sulfoximine (BSO), an inhibitor of GSH synthesis, partly reversed the effect of osthole on TMX-induced liver injury. Consistently, pretreatment with N-acetyl-L-cysteine (NAC) significantly attenuated TMX-induced increase in ALT and AST activities. Notably, both BSO and NAC had no detectable effect on the phosphorylation levels of p38. Collectively, our results suggest that osthole prevents TMX hepatotoxicity by suppressing p38 activation and subsequently reducing TMX-induced oxidative damage.


Assuntos
Antioxidantes/uso terapêutico , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Cumarínicos/uso terapêutico , Moduladores de Receptor Estrogênico/toxicidade , Tamoxifeno/toxicidade , Alanina Transaminase/sangue , Alanina Transaminase/metabolismo , Animais , Antioxidantes/administração & dosagem , Aspartato Aminotransferases/sangue , Aspartato Aminotransferases/metabolismo , Cumarínicos/administração & dosagem , Citocinas/metabolismo , Relação Dose-Resposta a Droga , Moduladores de Receptor Estrogênico/administração & dosagem , Peróxido de Hidrogênio/metabolismo , Inflamação/prevenção & controle , Fígado/patologia , Masculino , Malondialdeído/metabolismo , Camundongos Endogâmicos BALB C , Estresse Oxidativo/efeitos dos fármacos , Tamoxifeno/administração & dosagem
9.
Pharmazie ; 73(9): 526-532, 2018 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-30223936

RESUMO

Artesunate is a semi-synthetic derivative of a Chinese herb named Artemisia annua L. that is commonly used as an antimalarial agent in the history of traditional Chinese medicine. Many studies have reported artesunate possesses anti-inflammatory and immunoregulation properties. The present study was conducted to explore whether artesunate was effective in experimental autoimmune myasthenia gravis (EAMG) in Lewis rats. Our data showed that artesunate could improve the clinical symptoms and suppress the development of EAMG. Artesunate exerted its immunomodulatory effects by inhibiting lymphocyte proliferation and the expression of costimulatory molecules CD86, modulating Th1/Th2 cytokine expression levels, and enhancing the level of Treg cells. The final result of administration of artesunate was the decreased synthesis of anti-R97-116 IgG, IgG2a, and IgG2b antibodies. The treatment effect of artesunate was more obvious at dose of 10 mg/kg. These date suggest that artesunate might be a potential drug for the treatment of human myasthenia gravis (MG).


Assuntos
Artesunato/farmacologia , Fatores Imunológicos/farmacologia , Miastenia Gravis Autoimune Experimental/tratamento farmacológico , Linfócitos T Reguladores/imunologia , Animais , Antimaláricos/administração & dosagem , Antimaláricos/farmacologia , Artesunato/administração & dosagem , Proliferação de Células/efeitos dos fármacos , Citocinas/imunologia , Relação Dose-Resposta a Droga , Feminino , Fatores Imunológicos/administração & dosagem , Miastenia Gravis Autoimune Experimental/imunologia , Miastenia Gravis Autoimune Experimental/fisiopatologia , Ratos , Ratos Endogâmicos Lew , Células Th1/imunologia , Células Th2/imunologia , Regulação para Cima
10.
Acta Pharmacol Sin ; 39(1): 74-84, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29022574

RESUMO

Acetaminophen (APAP) overdose leads to severe hepatotoxicity. Osthole, a natural coumarin found in traditional Chinese medicinal herbs, has therapeutic potential in the treatment of various diseases. In this study, we investigated the effects of osthole against APAP-induced hepatotoxicity in mice. Mice were administered osthole (100 mg·kg-1·d-1, ip) for 3 d, then on the fourth day APAP (300 mg/kg, ip) was co-administered with osthole. The mice were euthanized post-APAP, their serum and livers were collected for analysis. Pretreatment with osthole significantly attenuated APAP-induced hepatocyte necrosis and the increases in ALT and AST activities. Compared with the mice treated with APAP alone, osthole pretreatment significantly reduced serum MDA levels and hepatic H2O2 levels, and improved liver GSH levels and the GSSG-to-GSH ratio. Meanwhile, osthole pretreatment markedly alleviated the APAP-induced up-regulation of inflammatory cytokines in the livers, and inhibited the expression of hepatic cytochrome P450 enzymes, but it increased the expression of hepatic UDP-glucuronosyltransferases (UGTs) and sulfotransferases (SULTs). Furthermore, osthole pretreatment reversed APAP-induced reduction of hepatic cAMP levels, but pretreatment with H89, a potent selective PKA inhibitor, failed to abolish the beneficial effect of osthole, whereas pretreatment with L-buthionine sulfoximine, a GSH synthesis inhibitor, abrogated the protective effects of osthole on APAP-induced liver injury, and abolished osthole-caused alterations in APAP-metabolizing enzymes. In cultured murine primary hepatocytes and Raw264.7 cells, however, osthole (40 µmol/L) did not alleviate APAP-induced cell death, but it significantly suppressed APAP-caused elevation of inflammatory cytokines. Collectively, we have demonstrated that osthole exerts a preventive effect against APAP-induced hepatotoxicity by inhibiting the metabolic activation of APAP and enhancing its clearance through an antioxidation mechanism.


Assuntos
Acetaminofen/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Cumarínicos/uso terapêutico , Substâncias Protetoras/uso terapêutico , Acetaminofen/administração & dosagem , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/uso terapêutico , Antioxidantes/administração & dosagem , Antioxidantes/uso terapêutico , Cumarínicos/administração & dosagem , Sistema Enzimático do Citocromo P-450/metabolismo , Glucuronosiltransferase/metabolismo , Glutationa/metabolismo , Hemorragia/prevenção & controle , Peróxido de Hidrogênio/metabolismo , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Necrose/prevenção & controle , Estresse Oxidativo/efeitos dos fármacos , Células RAW 264.7 , Sulfotransferases/metabolismo
11.
Bol. latinoam. Caribe plantas med. aromát ; 16(6): 520-528, nov. 2017. tab, graf
Artigo em Inglês | LILACS | ID: biblio-914913

RESUMO

Artemisia genus (family Asteraceae) has been widely used as medicines and cosmetic. The chemical compositions of essential oils extracted from five Artemisia species (A. anethoides, A. giraldii, A. roxburghiana, A. rubripes and A. sacrorum) were analyzed and the repellent activities of five essential oils were investigated by testing percent repellency (PR) in petri dish against Tribolium castaneum. By GC-MS analysis, the common components of the five essential oils were eucalyptol (11.09%-50.05%), camphor (6.28%-33.10%), terpinen- 4-ol (2.46%-12.41%), ß-caryophyllene (0.63%-10.68%) and germacrene D (2.28%-10.01%). 3,3,6-trimethyl-1,4-heptadien-6-ol (11.72%), 2-isopropyl-5-methyl-3-cyclohexen-1-one (24.80%) and ß-farnesene (12.23%) were the characteristic compounds in essential oils of A. sacrorum, A. anethoides and A. rubripes respectively. The essential oils of five plants showed repellent activity against T. castaneum. The PR of others four essential oils were comparable with DEET expect for A. sacrorum. The results indicated that the essential oils of A. anethoides, A. giraldii, A. roxburghiana and A. rubripes had the potential to be developed as repellent for control of T. castaneum.


El género Artemisia (familia Asteraceae) ha sido ampliamente utilizado como medicamentos y cosméticos. Se analizaron las composiciones químicas de los aceites esenciales extraídos de cinco especies de Artemisia (A. anethoides, A. giraldii, A. roxburghiana, A. rubripes y A. sacrorum) y se investigaron las actividades repelentes de cinco aceites esenciales mediante la prueba de repelencia porcentual (PR) en placa de petri contra Tribolium castaneum. Por análisis GC-MS, los componentes comunes de los cinco aceites esenciales fueron eucaliptol (11,09% -50,05%), alcanfor (6,28% -33,10%), terpinen-4-ol (2,46% -12,41%), ß-cariofileno 0,63% -10,68%) y germacrén D (2,28% -10,01%). 3,3,6-trimetil-1,4-heptadien-6-ol (11,72%), 2-isopropil-5-metil-3-ciclohexen-1-ona (24,80%) y ß-farneseno (12,23%). Los compuestos característicos en los aceites esenciales de A. sacrorum, A. anethoides y A. rubripes respectivamente. Los aceites esenciales de cinco plantas mostraron actividad repelente contra T. castaneum. El PR de otros cuatro aceites esenciales eran comparables con DEET esperado para A. sacrorum. Los resultados indicaron que los aceites esenciales de A. anethoides, A. giraldii, A. roxburghiana y A. rubripes tienen el potencial de ser desarrollados como repelentes para el control de T. castaneum.


Assuntos
Animais , Tribolium/efeitos dos fármacos , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Artemisia/química , Repelentes de Insetos/farmacologia , Terpenos/análise , Besouros/efeitos dos fármacos , Óleos Voláteis/química , Extratos Vegetais/química , Asteraceae/química , Cromatografia Gasosa-Espectrometria de Massas
12.
Zhongguo Zhong Yao Za Zhi ; 42(11): 2052-2057, 2017 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-28822147

RESUMO

Plate assay and spore germination method were used to study the chemotaxis response of Alternaria panax to arginine, glutamic acid, aspartic acid and threonine. The result showed that the optimum temperature of A. panax chemotaxis response to four amino acids were all 25 ℃. And chemotaxis responses of A. panax were different under conditions of different concentration and pH value. The chemotaxin reached to the highest under the condition of 2 mg•L⁻¹ and pH value was 7 for arginine, glutamic acid and threonine while 20 mg•L⁻¹ and pH value was 6 for aspartic acid . The data of chemotactic migration index (CMI) were 1.24, 1.38, 1.27, 1.31 and chemotactic growth rates(CGR) were 0.451 0, 0.353 0, 0.381 3, 0.228 8 and spores germination rates(SGR) were 57.33%,63%,56.67%,58% and the dry weight of mycelial (DWM) were 372.9, 348.5, 314.4, 390.2 mg•L⁻¹ respectively. It indicated that the low and middle concentration of amino acid had significant promoting effect on chemotaxis response of A. panax. As important substances generated in ginseng root, amino acids exhibited an efficient chemotactic effect on A. panax, and some even show inhibition effect under high concentration.


Assuntos
Alternaria/efeitos dos fármacos , Aminoácidos/farmacologia , Quimiotaxia , Panax/química , Raízes de Plantas/química , Alternaria/citologia
13.
Acta Pharmacol Sin ; 38(8): 1120-1128, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28603288

RESUMO

Osthole, a natural coumarin found in traditional Chinese medicinal plants, has shown multiple biological activities. In the present study, we investigated the preventive effects of osthole on inflammatory bowel disease (IBD). Colitis was induced in mice by infusing TNBS into the colonic lumen. Before TNBS treatment, the mice received osthole (100 mg·kg-1·d-1, ip) for 3 d. Pretreatment with osthole significantly ameliorated the clinical scores, colon length shortening, colonic histopathological changes and the expression of inflammatory mediators in TNBS-induced colitis. Pretreatment with osthole elevated serum cAMP levels; but treatment with the PKA inhibitor H89 (10 mg·kg-1·d-1, ip) did not abolish the beneficial effects of osthole on TNBS-induced colitis. In mouse peritoneal macrophages, pretreatment with osthole (50 µmol/L) significantly attenuated the LPS-induced elevation of cytokines at the mRNA level; inhibition of PKA completely reversed the inhibitory effects of osthole on IL-1ß, IL-6, COX2, and MCP-1 but not on TNFα. In Raw264.7 cells, the p38 inhibitor SB203580 markedly suppressed LPS-induced upregulation of the cytokines, whereas the PKA inhibitors H89 or KT5720 did not abolish the inhibitory effects of SB203580. Moreover, in LPS-stimulated mouse peritoneal macrophages, SB203580 strongly inhibited the restored expression of IL-1ß, IL-6, COX2, and MCP-1, which was achieved by abolishing the suppressive effects of osthole with the PKA inhibitors. Western blot analysis showed that osthole significantly suppressed the phosphorylation of p38, which was induced by TNBS in mice or by LPS in Raw264.7 cells. Inhibition of PKA partially reversed the suppressive effects of osthole on p38 phosphorylation in LPS-stimulated cells. Collectively, our results suggest that osthole is effective in the prevention of TNBS-induced colitis by reducing the expression of inflammatory mediators and attenuating p38 phosphorylation via both cAMP/PKA-dependent and independent pathways, among which the cAMP/PKA-independent pathway plays a major role.


Assuntos
Colite/prevenção & controle , Cumarínicos/uso terapêutico , Proteínas Quinases Dependentes de AMP Cíclico/metabolismo , AMP Cíclico/metabolismo , Transdução de Sinais/efeitos dos fármacos , Animais , Western Blotting , Colite/induzido quimicamente , Citocinas/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Reação em Cadeia da Polimerase em Tempo Real , Ácido Trinitrobenzenossulfônico/farmacologia
14.
Microb Drug Resist ; 23(4): 516-522, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27792585

RESUMO

The study aimed to investigate the association of prevalent genotypes in China (HBV/C and HBV/B) with HBV drug-resistant mutations. A total of 13,847 nucleos(t)ide analogue (NA)-treated patients with chronic HBV infection from North China were enrolled. HBV genotypes and resistant mutations were determined by direct sequencing and confirmed by clonal sequencing if necessary. HBV/B, HBV/C, and HBV/D occupied 14.3%, 84.9%, and 0.8% across the study population, respectively. NA usage had no significant difference between HBV/B- and HBV/C-infected patients. Lamivudine-resistant mutations were more frequently detected in HBV/C-infected patients, compared with HBV/B-infected patients (31.67% vs. 25.26%, p < 0.01). Adefovir- and entecavir-resistant mutation detection rates were similar, but the mutational pattern was different between the two genotypes. For adefovir-resistant mutations, HBV/C-infected patients had a higher detection rate of rtA181 V (HBV/C 5.29% vs. HBV/B 1.36%, p < 0.01) and a lower detection rate of rtN236T (2.70% vs. 6.54%, p < 0.01). For entecavir-resistant mutations, HBV/C-infected patients had a higher detection rate of rtM204 V/I+T184 substitution or S202G/C (3.66% vs. 2.16%, p < 0.01) and a lower detection rate of rtM204 V/I+M250 V/I/L substitution (0.67% vs. 1.46%, p < 0.01). Multidrug-resistant mutations (defined as coexistence of mutation to nucleoside and nucleotide analogues) were detected in 104 patients. HBV/C-infected patients had a higher detection rate of multidrug-resistant mutation than HBV/B-infected patients (0.83% vs. 0.35%, p < 0.05). The study for the first time clarified that HBV/C-infected patients had a higher risk to develop multidrug-resistant mutations, compared with HBV/B-infected patients; and HBV/C- and HBV/B-infected patients had different inclinations in the ETV-resistant mutational pattern.


Assuntos
Antivirais/uso terapêutico , Farmacorresistência Viral Múltipla/genética , Vírus da Hepatite B/genética , Hepatite B Crônica/tratamento farmacológico , Taxa de Mutação , Proteínas Virais/genética , Adenina/análogos & derivados , Adenina/uso terapêutico , Adulto , China , Estudos de Coortes , Feminino , Expressão Gênica , Genótipo , Guanina/análogos & derivados , Guanina/uso terapêutico , Vírus da Hepatite B/classificação , Vírus da Hepatite B/efeitos dos fármacos , Vírus da Hepatite B/isolamento & purificação , Hepatite B Crônica/virologia , Humanos , Lamivudina/uso terapêutico , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Organofosfonatos/uso terapêutico , Filogenia
15.
Antivir Ther ; 20(2): 141-7, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-24992206

RESUMO

BACKGROUND: This study aimed to clarify the clinical significance of drug-resistant HBV in nucleoside/nucleotide analogue (NA)-naive Chinese patients with chronic HBV infection in real clinical practice. METHODS: A total of 845 NA-naive patients who were admitted to Beijing 302 Hospital between July 2007 and March 2012 were included in the study. HBV drug-resistant mutations were examined by direct sequencing of the viral reverse transcriptase gene and verified by clonal sequencing. Phenotypic analysis of viral replication capacity and drug susceptibility were performed by measuring viral replicative intermediate level in 1.1-mer mutant or wild-type HBV amplicon-transfected HepG2 cells in absence or presence of serially diluted drugs. RESULTS: Drug-resistant mutations were detected in 2.01% (17/845) of the patients by direct sequencing, including 15 with lamivudine-resistant mutations (rtM204V, rtM204I), one with adefovir-resistant mutation (rtA181V), and one with both lamivudine- and adefovir-resistant mutations (rtA181V, rtM204I). Clonal sequencing identified 13 drug-resistant HBV strains: rtL80I+M204I, rtL80I+M204V, rtL180M+M204I, rtL180M+M204V, rtM204I, rtM204V, rtL80I+L180M+M204I, rtL80I+L180M+M204V, rtA181V, rtA181V+M204I, rtA181T+N236T, rtA181V+N236T and rtN236T. Phenotypic analysis showed that two pre-existing lamivudine-resistant strains (rtL80I+M204I, rtL180M+M204V) had >1,000-fold resistance to lamivudine, and one pre-existing adefovir-resistant strain (rtA181V+N236T) had 15.4-fold resistance to adefovir compared with the wild-type strain. A follow-up study showed that the presence of pre-existing rtM204I strain in one patient increased from 20% at baseline to 85% after 13 months of entecavir treatment with corresponding recession of wild-type strain in the viral pool. CONCLUSIONS: The incidence of drug-resistant HBV mutations was low in NA-naive Chinese HBV-infected patients. Pre-existing mutants had similar resistance characteristics to those from NA refractory patients.


Assuntos
Antivirais/uso terapêutico , Farmacorresistência Viral/genética , Vírus da Hepatite B/genética , Hepatite B Crônica/tratamento farmacológico , Mutação , DNA Polimerase Dirigida por RNA/genética , Proteínas Virais/genética , Adenina/análogos & derivados , Adenina/uso terapêutico , Adulto , China , Células Clonais , Feminino , Expressão Gênica , Genótipo , Guanina/análogos & derivados , Guanina/uso terapêutico , Células Hep G2 , Vírus da Hepatite B/efeitos dos fármacos , Vírus da Hepatite B/enzimologia , Hepatite B Crônica/patologia , Hepatite B Crônica/virologia , Humanos , Lamivudina/uso terapêutico , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Organofosfonatos/uso terapêutico , Fenótipo , DNA Polimerase Dirigida por RNA/metabolismo , Análise de Sequência de DNA , Proteínas Virais/antagonistas & inibidores , Proteínas Virais/metabolismo
16.
Planta Med ; 80(17): 1597-604, 2014 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-25340467

RESUMO

Total steroid saponins isolated from Dioscorea zingiberensis have shown a variety of beneficial bioactivities. However, there are no reports about their neuroprotective effects, until now. Therefore, in the present study, we explored the neuroprotective effects of the total steroid saponins from D. zingiberensis on rats against transient focal cerebral ischemia-reperfusion and their underlying mechanisms. Healthy adult Sprague-Dawley rats were randomly assigned to six groups. After pretreatment with D. zingiberensis total steroid saponins intragastrically for six days, the rats were subjected to an ischemia injury by surgery on the middle cerebral artery occlusion for 90 min. Compared to the ischemia-reperfusion group, the D. zingiberensis total steroid saponin group of rats, especially those given a 30-mg/kg dose, showed not only a marked reduction in neurological deficit scores, cerebral infarct volume, and brain edema, but also an increase in neuron survival (Nissl bodies) in the hippocampal cornuammons 1 and cortex hemisphere of the ipsilateral ischemia. At the same time, the inflammatory cytokines in serum induced by the middle cerebral artery occlusion were significantly decreased by the preadministration of D. zingiberensis total steroid saponins. Furthermore, the increase of caspase-3 was evidently reduced in the hippocampal cornuammons 1 and cortex of the hemisphere injured brain. Finally, the downregulating antiapoptotic Bcl-2 and upregulating proapoptotic Bax proteins were obviously suppressed. Taken together, the current findings suggest that D. zingiberensis total steroid saponins played a potential neuroprotective role against a severe injury induced by transient focal cerebral ischemic reperfusion in a rat experimental model, and this role may be mediated by its anti-inflammatory and antiapoptotic actions.


Assuntos
Anti-Inflamatórios/farmacologia , Apoptose/efeitos dos fármacos , Dioscorea/química , Fármacos Neuroprotetores/farmacologia , Traumatismo por Reperfusão/prevenção & controle , Saponinas/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Masculino , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Ratos Sprague-Dawley , Saponinas/química , Saponinas/isolamento & purificação
17.
Int Immunopharmacol ; 23(2): 407-16, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25066758

RESUMO

The aim of our present study is to explore the anti-arthritic potential effect of total steroid saponins (TSSNs) extracted from the rhizome of Dioscorea zingiberensis C.H.Wright (DZW) and to investigate the underlying mechanisms. This work was performed using adjuvant-induced arthritis (AIA) rats in vivo and lipopolysaccharide (LPS) simulated 264.7 macrophage cells in vitro. In AIA-induced arthritic rats, TSSN significantly alleviated the arthritic progression through evaluating arthritic score, immune organ indexes, paw swelling, and body weight. This phenomenon was well correlated with significant suppression of the overproduction of inflammation cytokines (IL-1, IL-1ß, IL-6, and TNF-α), oxidant stress makers (MDA and NO), eicosanoids (LTB4 and PGE2), and inflammatory enzymes (5-LOX and COX-2) versus the AIA rats without treatment. On the contrary, the release of SOD and IL-10 was profoundly increased. What's more, TSSN could obviously ameliorate the translocation of NF-κB to the nucleus through phosphorylation of the p65 and IκBα in vivo and in vitro. The current findings demonstrated that TSSN could protect the injured ankle joint from further deterioration and exert its satisfactory anti-arthritis properties through anti-inflammatory and anti-oxidant effects via inactivating the NF-κB signal pathway. This research implies that DZW may be a useful therapeutic agent for the treatment of human arthritis.


Assuntos
Artrite/induzido quimicamente , Dioscorea/química , Extratos Vegetais/farmacologia , Rizoma/química , Saponinas/farmacologia , Esteroides/farmacologia , Animais , Antirreumáticos/administração & dosagem , Antirreumáticos/farmacologia , Artrite/tratamento farmacológico , Relação Dose-Resposta a Droga , Adjuvante de Freund/toxicidade , Metotrexato/farmacologia , Estrutura Molecular , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Saponinas/administração & dosagem , Saponinas/química , Esteroides/administração & dosagem , Esteroides/química
18.
Pharm Biol ; 52(5): 539-43, 2014 May.
Artigo em Inglês | MEDLINE | ID: mdl-24236532

RESUMO

CONTEXT: To this day, there are no reports that marine compounds isolated from microorganisms of the Lianyungang area of China have been used for the treatment of Alzheimer's disease. OBJECTIVE: The present study was to isolate fungi from the sea sediment of the Lianyungang area and screen for acetylcholineseterase inhibition activities of ethyl acetate extracts. MATERIALS AND METHODS: Fungi were isolated from the sea sediment and fermented. After centrifugation, the supernate was extracted with ethyl acetate. The ethyl acetate extract was then fractionated into five fractions. Acetylcholinesterase inhibition activities of the ethyl acetate extracts and five sub-fractions were tested at a concentration of 500 µg/mL with the Ellman's method. RESULTS: Forty-three marine fungi were isolated; 15 extracts inhibited acetylcholinestrease >50% and 3 extracts inhibited the acetylcholinesterase >80% at the concentration of 500 µg/mL. The 3 extracts (L1705, S1101, SH0701) inhibited AChE dose-dependently with IC50 values of 11.3 ± 1.2, 72.1 ± 2.3, and 7.8 ± 2.8 µg/mL, respectively. After the extract of SH0701 was fractionated into five fractions, the ethyl acetate fraction possessed the highest acetylcholinesterase inhibitory activity with an inhibition rate of 71.55% at the concentration of 10 µg/mL. The fungus SH0701 was identified as Aspergillus ochraceus SH0701 according to morphology and molecular identification. DISCUSSION AND CONCLUSION: The present results indicates that some ethyl acetate extracts of marine fungi isolated from Lianyungang area of China could inhibit AChE potently. Therefore, some novel AChE inhibitors might exist in those extracts.


Assuntos
Acetilcolinesterase/metabolismo , Organismos Aquáticos , Inibidores da Colinesterase/farmacologia , Fungos , Sedimentos Geológicos/microbiologia , Animais , Organismos Aquáticos/química , Organismos Aquáticos/isolamento & purificação , Encéfalo/enzimologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Relação Dose-Resposta a Droga , Fungos/química , Fungos/isolamento & purificação , Concentração Inibidora 50 , Medicina Tradicional Chinesa , Coelhos
19.
Zhongguo Zhong Yao Za Zhi ; 38(19): 3313-8, 2013 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-24422399

RESUMO

To establish a HPLC-ELSD fingerprint for total steroid saponins in herbs of Dioscorea zingiberensis. Welchrom C,8 (4. 6 mm x 250 mm,5 microm) chromatographic column was adopted and eluted with the mobile phase of acetonitrile (A)-water (B) at the flow rate of 1.0 mL min-1. The column temperature was room temperature. The ELSD conditions were as follows: the temperature of drift tube was 90.0 degreeC, the flow rate of carrier gas (N2) was 2. 8 L min-1, and the injection volume was 10 microL. After the detection of 10 batches of samples,the common mode of HPLC-ELSD fingerprint for total steroid saponins in herbs of D. zingiberensis was established for the first time,and 25 common peaks were determined. Among them, 10 peaks were identified by comparing with reference substances. The similarities of 10 batches of herbs were evaluated in the common mode. All of them were higher than 0. 80. This method is so accurate, reliable and highly repeatable that it can provide scientific basis for evaluating and controlling the quality of total steroid saponins in herbs of D. zingiberensis.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Dioscorea/química , Dioscorea/classificação , Dioscorea/citologia , Saponinas/análise
20.
Am J Chin Med ; 40(6): 1157-66, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23227788

RESUMO

This study was designed to compare the weight reduction effects of acupuncture for obese women with or without perimenopausal syndrome. We observed 60 women with either simple obesity or perimenopausal obesity (obesity complicated with perimenopausal syndrome) treated by five acupuncture treatments given in the first week of three successive four-week treatment courses, and obesity indexes including body weight, body mass index, obesity degree and waist/hip ratio were evaluated. Versus baseline, the obesity indexes decreased at the end of each treatment course in women with simple obesity (p < 0.05 or p < 0.01), while women with perimenopausal obesity showed no decrease at the end of the first course of treatment, and these indexes decreased at the end of the second and the third courses of treatment (p < 0.05). There was no difference when comparing obesity indexes recorded at the end of three courses of treatment and at the end of three-month follow-up between women with simple obesity and those with perimenopausal obesity. The results suggest that acupuncture reduced body weight in the obese women, and the weight loss occurred earlier in the treatment process for simple obesity than perimenopausal obesity.


Assuntos
Acupuntura , Obesidade/terapia , Perimenopausa , Redução de Peso , Feminino , Humanos , Pessoa de Meia-Idade , Projetos Piloto
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