RESUMEN
Objective: To investigate the occupational damage to workers exposed to chromate in a steel plant. Methods: In January 2021, a retrospective analysis was used to select 850 workers exposed to chromate (observation group) and 598 workers not exposed to chromate (control group) in a steel plant in Shandong Province from 2016 to 2017 as the investigation. We collected their occupational-related information, blood routine, fasting blood sugar, nasal lesions, skin lesions, chest X-rays and other inspection results, compared the differences in the abnormal detection rate of the two groups of respondents, and analyzed the occupational hazards of chromium workers. Results: Incidence of nasal damage, skin lesion, up-regulation of ALT (Alanine aminotransferase), abnormal chest radiograph, abnormal serum biochemical index, and abnormal serum glucose level were observed higher in the exposed group than those in the control group (χ(2)=125.69, 12.25, 5.82, 10.37, 10.46, 20.66, P=0.000, 0.000, 0.016, 0.001, 0.001, 0.000). Among the symptoms, the incidence of erythra, nasal septum deviation, nasal mucosal congestion, nasal mucosal erosion and rhinitis were more frequent than those in the control group (χ(2)=101.54, 4.07, 13.20, 32.05, P=0.000, 0.044, 0.000, 0.000). There was no significant increase in the incidence of work type, age, length of work and the area of nasal mucosa erosion in the observation group compared with the control table, and the difference was not statistically significant (χ(2)=5.31ã0.42ã0.28, P=0.505, 0.662, 0.871) . Conclusion: Occupational hazards of long-term exposure to chromate cannot be ignored. Attention should be paid to strengthening occupational protection and health education of workers exposed to chromium, and increasing their attention.
Asunto(s)
Enfermedades Nasales , Exposición Profesional , Cromatos/análisis , Cromatos/toxicidad , Cromo , Humanos , Exposición Profesional/efectos adversos , Exposición Profesional/análisis , Estudios Retrospectivos , AceroRESUMEN
Occupational chromium rhinopathy is chronic nasal damage caused by chromic anhydride, chromate and dichromate 6-valent chromium compounds. In 2016, 700 people who were exposed to chromium slag in steel plant were checked out. 24 people were found to have nasal injuries. The expert group confirmed 1 case of occupational severe chromium rhinosis and 23 cases of occupational mild chromium rhinosis.There was no significant difference in the incidence, type of work and duration of injury among 24 patients (P>0.05) . Active measures should be taken to prevent chromium rhinopathy and the technological process should be reformed. Occupational health education and occupational health monitoring should be strengthened to avoid exposure of chromium and its compounds through nose and respiratory tract, and to reduce or eliminate the occurrence of chromium rhinosis.
Asunto(s)
Cromo , Enfermedades Nasales , Exposición Profesional , Cromatos , Cromo/envenenamiento , Humanos , Enfermedades Nasales/inducido químicamente , Sistema RespiratorioRESUMEN
AIMS: This work was performed to characterize new secondary metabolites with neuraminidase (NA) inhibitory activity from marine actinomycete strains. METHODS AND RESULTS: An actinomycete strain IFB-A01, capable of producing new NA inhibitors, was isolated from the gut of shrimp Penasus orientalis and identified as Streptomyces seoulensis according to its 16S rRNA sequence (over 99% homology with that of the standard strain). Repeated chromatography of the methanol extract of the solid-substrate culture of S. seoulensis IFB-A01 led to the isolation of streptoseolactone (1), and limazepines G (2) and H (3). The structures of 1-3 were determined by a combination of IR, ESI-MS, 1D ((1) H and (13) C NMR, and DEPT) and 2D NMR experiments (HMQC, HMBC, (1) H-(1) H COSY and NOESY). Compounds 1-3 showed significant inhibition on NA in a dose-dependent manner with IC50 values of 3.92, 7.50 and 7.37 µmol l(-1), respectively. CONCLUSIONS: This is the first report of two new (1 and 2) and known (3, recovered as a natural product for the first time in the work) NA inhibitors from the marine-derived actinomycete S. seoulensis IFB-A01. SIGNIFICANCE AND IMPACT OF THE STUDY: The three natural NA inhibitors maybe of value for the development of drug(s) necessitated for the treatment of viral infections.
Asunto(s)
Benzodiazepinas/aislamiento & purificación , Lactonas/aislamiento & purificación , Neuraminidasa/antagonistas & inhibidores , Streptomyces/química , Animales , Benzodiazepinas/química , Clostridium perfringens/enzimología , Lactonas/química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Penaeidae/microbiología , ARN Ribosómico 16S/genética , Streptomyces/genéticaRESUMEN
Two new benzo[j]fluoranthene-based secondary metabolites named daldinone C (1) and daldinone D (2), along with two known metabolites, altechromone A and (4S)-5,8-dihydroxy-4-methoxy-alpha-tetralone, were isolated from the CHCl3/MeOH (1:1) extract of a solid culture of the endophyte Hypoxylon truncatum IFB-18 harbored inside the symptomless stem tissue of Artemisia annua. The structures of the new compounds were elucidated by MS and 1D and 2D NMR spectra and by X-ray diffraction analysis. Their absolute configurations were determined unambiguously by a combination of their CD data and the established exciton chirality rule. Compounds 1 and 2 were substantially cytotoxic against SW1116 cells, with IC50 values of 49.5 and 41.0 microM, respectively, comparable to that (37.0 microM) of 5-fluorouracil. The biosynthetic pathway for 1 and 2 was postulated with the natural occurrence of benzo[j]fluoranthene analogues discussed in brief.
Asunto(s)
Antineoplásicos , Ascomicetos/química , Fluorenos , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Artemisia annua , China , Cristalografía por Rayos X , Ensayos de Selección de Medicamentos Antitumorales , Fluorenos/química , Fluorenos/aislamiento & purificación , Fluorenos/farmacología , Humanos , Concentración 50 Inhibidora , Conformación Molecular , Estructura Molecular , Plantas MedicinalesRESUMEN
AIMS: Fungal infection is still a life-threatening risk for the immunocompromised population such as AIDS patients and those who receive treatments with immunosuppressors and/or frequent administrations of wide-spectrum antibiotics, which inevitably lead to the drug resistance and unbalanced microflora populations. The present work was accordingly performed to characterize more potent antifungal metabolites from various cultures of marine fungi residing in white croaker Argyrosomus argentatus. METHODS AND RESULTS: The three most common opportunistic human pathogens Candida albicans (CCCCM ID 00148), Aspergillus niger (CCCCM ACCC 30005) and Trichophyton rubrum (CCCCM ID 00001) were selected as test fungi. A total of 16 cultivable fungal strains were isolated from the variant tissues of Ar. argentatus collected from the Yellow Sea, followed by preliminary antifungal screenings of the EtOAc extracts of the corresponding cultures. As a result, the inhibition of the three target fungi, plus being allergic to isolators' skin, were discerned with the EtOAc extract of the fungus under the isolation number Z16 that was identified subsequently as Myrothecium sp. by a combination of morphological and 18S rDNA finger-typing characteristics. A follow-up bioassay fractionation of the EtOAc extract, in conjunction with spectral analyses [MS, (1)H-NMR, (13)C-NMR, distortionless enhancement by polarization transfer (DEPT), heteronuclear multiple quantum coherence (HMQC) and heteronuclear multiple bond resonance (HMBC)] wherever required, afforded eventually the characterization of a new acid (compound 1: 4,5-ditridecyl-octanedioic acid), three macrocyclic trichothecenes including roridin A (compound 2), verrucarin A (compound 3) and 8beta-acetoxy-roridin H (compound 4), (22E,24R)-cerevisterol (compound 5) and N-phenyl-beta-amino-naphthalene (compound 6). In vitro antifungal tests showed that the three trichothecenes were active against A. niger, T. rubrum and C. albicans with MICs of 31.25, 62.5 and 125 microg ml(-1) for compound 2, 250, 125 and 31.25 microg ml(-1) for compound 3 as well as 125, 62.5 and 125 microg ml(-1) for compound 4 respectively. The MICs of ketoconazole (co-assayed herewith as a positive reference) against A. niger, T. rubrum and C. albicans were 31.25, 250, 31.25 microg ml(-1) respectively. A preliminary structure-activity relationship of the antifungal trichothecenes was highlighted in brief. CONCLUSIONS: The present investigation demonstrated that marine fungus Myrothecium sp. Z16 associated with white croaker (Ar. argentatus), was an efficient producer of a new acid and antifungal trichothecenes, the latter presumably being also the allergic substances in the culture. SIGNIFICANCE AND IMPACT OF THE STUDY: The title marine fungus was investigated to be a resource of new aliphatic acid, and trichothecenes with potent antifungal and dermal toxic actions.
Asunto(s)
Antifúngicos/aislamiento & purificación , Ascomicetos/metabolismo , Perciformes/microbiología , Animales , Antifúngicos/farmacología , Ascomicetos/crecimiento & desarrollo , Aspergillus niger/efectos de los fármacos , Candida albicans/efectos de los fármacos , Medios de Cultivo , ADN Ribosómico , Ácidos Dicarboxílicos/farmacología , Micotoxinas/farmacología , Naftalenos/farmacología , Resonancia Magnética Nuclear Biomolecular/métodos , Fitosteroles/farmacología , Relación Estructura-Actividad , Trichophyton/efectos de los fármacos , Tricotecenos/farmacologíaRESUMEN
The effects of the carbon and nitrogen sources, initial pH and incubation temperature on laccase production by the endophytic fungus Monotospora sp. were evaluated. The optimal temperature and initial pH for laccase production by Monotospora sp. in submerged culture were found to be 30 degrees C and 8.5, respectively. Maltose (2 g l(-1)) and ammonium tartrate (10 g l(-1)) were the most suitable carbon and nitrogen source for laccase production. Under optimal culture medium, the maximum laccase activity was determined to be 13.55 U ml(-1), which was approximately four times higher than that in basal medium. This is the first report on laccase production by an endophytic fungus.
Asunto(s)
Ascomicetos/enzimología , Reactores Biológicos , Cynodon/microbiología , Lacasa/biosíntesis , Carbono/análisis , Concentración de Iones de Hidrógeno , Maltosa , Nitrógeno/análisis , Tartratos , TemperaturaRESUMEN
Differential functionalization of the phenolic groups in genistein was carried out in excellent yields under ultrasonic irradiation. The isoflavone ring had proved to be unstable under stirring at 60 degrees C and phenyl benzyl ketone was unexpectedly isolated instead of the genistein derivative.
Asunto(s)
Genisteína/análogos & derivados , Genisteína/síntesis química , Sonicación , Genisteína/aislamiento & purificación , Genisteína/efectos de la radiación , IsomerismoRESUMEN
Repellent and insecticidal activities of essential oils extracted from leaves of Artemisia princeps Pamp and seeds of Cinnamomum camphora (L.) Presl. against storage pests Sitophillus oryzae L. and Bruchus rugimanus Bohem were investigated. Results showed that the two individual oils displayed good, but their mixture (1:1) exhibited much better repellent activities at concentrations from 250 to 1000 microg g(-1) and insecticidal actions at concentrations 1000 microg g(-1) against the test beetles S. oryzae and B. rugimanus. Oils from A. princeps and C. camphora applied individually were significantly toxic to seed germination of wheat at 500 microg ml(-1). However, no toxic effects were found when the two oils were mixed (1:1 w/w) at the same concentration. These observations indicated that the mixture of the two plant-derived oils had a synergic effect and could be used in the control of storage pests.
Asunto(s)
Artemisia/química , Cinnamomum camphora/química , Repelentes de Insectos/farmacología , Insecticidas/farmacología , Aceites Volátiles/farmacología , Semillas/efectos de los fármacos , Animales , Escarabajos/efectos de los fármacos , Germinación , Pruebas de Toxicidad/métodos , Triticum/efectos de los fármacos , Vicia faba/efectos de los fármacos , Gorgojos/efectos de los fármacosRESUMEN
In addition to 7-methoxy-2-methyl-3,4,5-trihydroxyanthraquinone (1), physcion (2), macrosporin (3), deoxybostrycin (4), altersolanol B (5) and dactylariol (6), a new hexahydroanthraquinone named pleospdione (7) was isolated from the culture of Pleospora sp . IFB-E006, an endophytic fungus residing in the normal stem of Imperata cylindrical (Gramineae). Structure determination of pleospdione was accomplished using IR, HR-ESI-MS, 1D and 2D NMR spectral analysis. Compounds 4 - 6 exhibited significant cytotoxic activity against human colon cancer (SW1116) and leukemia (K562) cell lines while compounds 1, 2 and 7 were only weakly or moderately active.
Asunto(s)
Antraquinonas/química , Antraquinonas/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Ascomicetos/química , Poaceae/microbiología , Antraquinonas/aislamiento & purificación , Antineoplásicos/aislamiento & purificación , Humanos , Células K562 , Estructura Molecular , Resonancia Magnética Nuclear BiomolecularRESUMEN
Free radicals and other reactive oxygen species (ROS) are generated by all aerobic cells and are widely believed to play a significant role in aging as well as a number of degenerative or pathological diseases. This study compared the free radical-scavenging properties and antioxidant activity of YCP, a polysaccharide from the mycelium of a marine filamentous fungus Phoma herbarum YS 4108 and its two chemically sulfated derivatives YCP-S1 and YCP-S2. Sulfation, which masks hydroxyl groups of YCP polysaccharide molecule, could introduce new antioxidant activity, such as superoxide and hydroxyl radicals scavenging activity, metal chelating action, lipid peroxidation and linoleic acid oxidation inhibition capability. Furthermore, sulfated YCP was more potent than YCP at protecting erythrocytes against oxidative damage hemolysis. The current data suggest for the first time that sulfation of polysaccharide significantly increases its antioxidant activity and the chemical modification of polysaccharides may allow the preparation of derivatives with new properties and a variety of applications.
Asunto(s)
Antioxidantes/química , Antioxidantes/farmacología , Hongos/metabolismo , Polisacáridos/biosíntesis , Polisacáridos/química , Sulfatos/química , Animales , Quelantes/química , Quelantes/farmacología , Eritrocitos/citología , Eritrocitos/efectos de los fármacos , Hemólisis/efectos de los fármacos , Radical Hidroxilo/química , Ácido Linoleico/química , Peroxidación de Lípido/efectos de los fármacos , Ratas , Espectroscopía Infrarroja por Transformada de Fourier , Superóxidos/químicaRESUMEN
YCP, a mitogenic polysaccharide with its molecular weight (MW) of 2.4 x 10(3) kDa, was isolated from the mycelium of the marine filamentous fungus Phoma herbarum YS4108 by a combination of ion-exchange chromatography on DEAE-32 and gel permeation over Sephacryl S-400. The detailed compositional, spectroscopic and methylation analyses of the polysaccharide demonstrated that its backbone possessed most likely a linear alpha-(1 --> 4) bonded glucopyranoside main chain co-bearing through side alpha-(1 --> 6)-linkage. The alpha-(1 --> 4) bondage of the glucopyranoside building blocks in YCP was confirmed by the observation that it could be hydrolyzed by the alpha-amylase produced by Bacillus licheniformis. A reliable concentration monitoring experimentation highlighted that the reducing sugars released continuously from YCP during its incubation with the enzyme, and the MW of the main resulting fragment weighed 0.8 x 10(4) Da with approximately 10% of YCP converted to maltose, maltotriose and glucose after a 120-min enzymatic degradation. Finally, YCP was found to be able to increase phagocytic activity of mice in vitro and in vivo, indicating that it may be looked up as a potent immunomodulator that could activate macrophages.
Asunto(s)
Hongos/química , Polisacáridos/aislamiento & purificación , Animales , Cromatografía por Intercambio Iónico , Relación Dosis-Respuesta a Droga , Estabilidad de Enzimas , Femenino , Hongos/metabolismo , Hidrólisis , Macrófagos Peritoneales/citología , Macrófagos Peritoneales/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Masculino , Metilación , Ratones , Mitógenos/farmacología , Monosacáridos/metabolismo , Fagocitosis , Polisacáridos/química , Polisacáridos/metabolismo , Polisacáridos/farmacología , Bazo/citología , Bazo/efectos de los fármacos , Factores de Tiempo , alfa-Amilasas/metabolismoRESUMEN
A number of studies indicate that free radicals are involved in the neurodegeneration in Parkinson's and Alzheimer's diseases. EPS2, an exopolysaccharide with a mean molecular weight of 1.3 x 10(5) Da, was isolated by ion-exchange and sizing chromatography from the culture of Keissleriella sp. YS4108, a marine filamentous fungus. Compositionally, it is composed of galactose, glucose, rhamnose, mannose and glucuronic acid in an approximate proportion of 50:8:1:1:0.4. The protective effects of EPS2 on peroxide hydrogen (H2O2)-induced cell lesion, level of lipid peroxidation, antioxidant enzyme activities were investigated in the rat pheochromocytoma line PC12 cells. Following a 1-h exposure of the cells to H2O2, a significant reduction in cell survival and activities of glutathione peroxidase (GSH-Px) and catalase (CAT), as well as increased levels in malondialdehyde (MDA) production and lactate dehydrogenase (LDH) release were observed. However, preincubation of the cells with EPS2 prior to H2O2 exposure elevated the cell survival and GSH-Px and CAT activities, and decreased the level of MDA and LDH activity in a dose-dependent manner. In conclusion, EPS2 possesses pronounced protective effects against H2O2-induced cell toxicity. The finding is of a higher value in searching for new therapeutic agent for treating oxidative damage-derived neurodegenerative disorders.
Asunto(s)
Ascomicetos/metabolismo , Supervivencia Celular/efectos de los fármacos , Citoprotección/efectos de los fármacos , Peróxido de Hidrógeno/farmacología , Estrés Oxidativo/efectos de los fármacos , Polisacáridos Bacterianos/farmacología , Animales , Supervivencia Celular/fisiología , Citoprotección/fisiología , Relación Dosis-Respuesta a Droga , Interacciones Farmacológicas , Estrés Oxidativo/fisiología , Células PC12 , RatasRESUMEN
Two antibacterial and xanthine oxidase inhibitory cerebrosides, one of which is chemically new, were characterized from the chloroform-methanol (1:1) extract of Fusarium sp. IFB-121, an endophytic fungus in Quercus variabilis. By means of chemical and spectral methods [IR, electrospray ionization MS (ESI-MS), tandem ESI-MS, 1H and 13C NMR, distortionless enhancement by polarization transfer, COSY, heteronuclear multiple-quantum coherence, heteronuclear multiple-bond correlation, and 2-D nuclear Overhauser effect correlation spectroscopy], the structure of the new metabolite named fusaruside was established as (2S,2'R,3R,3'E,4E,8E,10E)-1-O-beta-D-glucopyranosyl-2-N-(2'-hydroxy-3'-octadecenoyl)-3-hydroxy-9-methyl-4,8,10-sphingatrienine, and the structure of the other was identified as (2S,2'R,3R,3'E,4E,8E)-1-O-beta-D-glucopyranosyl-2-N-(2'-hydroxy-3'-octadecenoyl)-3-hydroxy-9-methyl-4,8-sphingadienine. Both new and known cerebrosides, although inactive to Trichophyton rubrum and Candida albicans, showed strong antibacterial activities against Bacillus subtilis, Escherichia coli, and Pseudomonas fluorescens, with their minimum inhibitory concentrations being 3.9, 3.9, and 1.9 microg/mL, and 7.8, 3.9, and 7.8 microg/mL, respectively. Furthermore, both metabolites were inhibitory to xanthine oxidase, with the IC50 value of fusaruside being 43.8 +/- 3.6 microM and the known cerebroside being 55.5 +/- 1.8 microM.
Asunto(s)
Antibacterianos/metabolismo , Cerebrósidos/metabolismo , Inhibidores Enzimáticos/metabolismo , Fusarium/química , Quercus/microbiología , Xantina Oxidasa/antagonistas & inhibidores , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Cerebrósidos/química , Cerebrósidos/aislamiento & purificación , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Xantina Oxidasa/metabolismoRESUMEN
Aspergillus fumigatus CY018 was recognized as an endophytic fungus for the first time in the leaf of Cynodon dactylon. By bioassay-guided fractionation, the EtOAc extract of a solid-matrix steady culture of this fungus afforded two new metabolites, named asperfumoid (1) and asperfumin (2), together with six known bioactive compounds including monomethylsulochrin, fumigaclavine C, fumitremorgin C, physcion, helvolic acid and 5alpha,8alpha-epidioxy-ergosta-6,22-diene-3beta-ol as well as other four known compounds ergosta-4,22-diene-3beta-ol, ergosterol, cyclo(Ala-Leu) and cyclo(Ala-Ile). Through detailed spectroscopic analyses including HRESI-MS, homo- and hetero-nuclear correlation NMR experiments (HMQC, COSY, NOESY and HMBC), the structures of asperfumoid and asperfumin were established to be spiro-(3-hydroxyl-2,6-dimethoxyl-2,5-diene-4-cyclohexone-(1,3')-5'-methoxyl-7'-methyl-(1'H, 2'H, 4'H)-quinoline-2',4'-dione) and 5-hydroxyl-2-(6-hydroxyl-2-methoxyl-4-methylbenzoyl)-3,6-dimethoxyl-benzoic methyl ester, respectively. All of the 12 isolates were subjected to in vitro bioactive assays against three human pathogenic fungi Candida albicans, Tricophyton rubrum and Aspergillus niger. As a result, asperfumoid, fumigaclavine C, fumitremorgin C, physcion and helvolic acid were shown to inhibit C. albicans with MICs of 75.0, 31.5, 62.5, 125.0 and 31.5 microg/mL, respectively.
Asunto(s)
Antifúngicos/metabolismo , Aspergillus fumigatus/metabolismo , Cynodon/microbiología , Emodina/análogos & derivados , Ergosterol/análogos & derivados , Ácido Fusídico/análogos & derivados , Microbiología Industrial/métodos , Antifúngicos/farmacología , Aspergillus fumigatus/aislamiento & purificación , Benzoatos/metabolismo , Benzofenonas/química , Candida albicans/efectos de los fármacos , Emodina/metabolismo , Emodina/farmacología , Ergosterol/metabolismo , Alcaloides de Claviceps , Ácido Fusídico/metabolismo , Ácido Fusídico/farmacología , Éteres de Hidroxibenzoatos , Hidroxibenzoatos/química , Alcaloides Indólicos/metabolismo , Alcaloides Indólicos/farmacología , Indoles/metabolismo , Indoles/farmacología , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Péptidos Cíclicos/metabolismo , Hojas de la Planta/microbiología , Pironas/química , Pironas/metabolismo , Quinolonas/química , Quinolonas/metabolismoRESUMEN
Fractionation of the extract of Aspergillus niger. IFB-E003, an endophyte in Cyndon dactylon, gave four known compounds naphtho-gamma-pyrones rubrofusarin B, fonsecinone A, asperpyrone B and aurasperone A, which were further investigated biologically. Rubrofusarin B was shown to be cytotoxic to the colon cancer cell line SW1116 (IC50: 4.5 microgml-1), and aurasperone A inhibitory on XO (xanthine oxidase) (IC50: 10.9 micromoll-1). Moreover, the four naphtho-gamma-pyrones exhibited growth inhibitions against the five test microbes with MICs ranging in between 1.9 and 31.2 microgml(-1). The present recognition of rubrofusarin B and aurasperone A as strong co-inhibitors on XO, colon cancer cell and some microbial pathogens is of significance for the imperative discovery of new relevant therapeutic agents.
Asunto(s)
Antiinfecciosos/farmacología , Aspergillus niger/metabolismo , Inhibidores Enzimáticos/farmacología , Pironas/farmacología , Xantina Oxidasa/antagonistas & inhibidoresRESUMEN
The inhibitory effects of six flavonoids from Hypericum perforatum were assessed spectrophotometrically using nitric oxide synthase (NOS) in blood and cerebral homogenate of rats. Of the assayed compounds, quercetin and hyperoside showed concentration-dependent enzyme inhibitory actions. The IC50 values of quercetin for inhibiting NOS in rat cerebral homogenate and blood were 63.06 and 57.54 microM, and those of hyperoside 56.23 and 158.49 microM, respectively. The competitive patterns were discerned with the inhibition of the two flavonoids on NOS in serum and cerebral homogenate (except a mixed type inhibition was observed with quercetin in inhibiting cerebral NOS). Furthermore, similar inhibitions were found for quercetin upon NOS in cerebral homogenate and blood. However, a stronger inhibitory effect of hyperoside on the enzyme was discerned in cerebrum than in blood. These results suggested that the galactose moiety in hyperoside may be associated with the selectivity of the NOS inhibition.
Asunto(s)
Inhibidores Enzimáticos/farmacología , Hypericum , Óxido Nítrico Sintasa/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Animales , Corteza Cerebral/enzimología , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/administración & dosificación , Inhibidores Enzimáticos/uso terapéutico , Flavonoides/administración & dosificación , Flavonoides/farmacología , Flavonoides/uso terapéutico , Óxido Nítrico Sintasa/antagonistas & inhibidores , Óxido Nítrico Sintasa/sangre , Óxido Nítrico Sintasa/metabolismo , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico , Tallos de la Planta , Ratas , Ratas Sprague-DawleyRESUMEN
A new benzophenone, named rhizoctonic acid (1), together with three known compounds monomethylsulochrin (2), ergosterol (3) and 3beta,5alpha,6beta-trihydroxyergosta-7,22-diene (4) were isolated through bioassay-guided fractionations from the culture of Rhizoctonia sp. (Cy064), an endophytic fungus in the leaf of Cynodon dactylon. The structure of the new acid 1 was elucidated to be 5-hydroxy-2-(2-hydroxy-6-methoxy-4-methylbenzoyl)-3-methoxybenzoic acid by a combination of spectral analyses. Furthermore, the structure of monomethylsulochrin 2 was confirmed by 13C-NMR analysis. All four metabolites were subjected to a more detailed in vitro assessment of their antibacterial action against five clinically isolated and one reference (ATCC 43504) Helicobacter pylori strains.
Asunto(s)
Antiinfecciosos/farmacología , Cynodon/microbiología , Helicobacter pylori/efectos de los fármacos , Fitoterapia , Rhizoctonia , Antiinfecciosos/administración & dosificación , Antiinfecciosos/uso terapéutico , Helicobacter pylori/clasificación , Humanos , Pruebas de Sensibilidad Microbiana , Hojas de la Planta/microbiologíaRESUMEN
A total of seventeen phytochemicals including seven alkaloids (piperine, strychnine, brucine, stachydrine, tetrandrine, frangchinoline and sinomenine), four phenols (paeonol, honokiol, magnolol and eugenol) and six anthraquinones (emodin, rhein, chrysorphanol, aloe-emodin, physcion and 1,8-dihydroxyanthraquinone) was examined for inhibitory activity of monoamine oxidase (MAO) A and B from rat brain mitochondrial. Among these compounds, piperine and paeonol were found to be inhibitory against MAO A in a dose-dependent manner with IC(50) values of 49.3 and 54.6 microM, respectively. Piperine, paeonol and emodin were shown to inhibit MAO B in a dose-dependent manner with the IC(50) data of 91.3, 42.5 and 35.4 microM, respectively. Lineweaver-Burk transformation of the inhibition data indicated that the inhibitory action of piperine on MAO A was of mixed type, and that of paeonol on the same type of the enzyme was of non-competitive type. For piperine, the K(i) and K(I) were determined to be 35.8 and 25.7microM, respectively. For paeonol, the K(i) was estimated to be 51.1 microM. The inhibition of piperine and paeonol on MAO B was of competitive type with K(i) values of 79.9 and 38.2 microM, respectively. The inhibition of emodin on MAO B was of mixed type with the K(i) and K(I) data of 15.1 and 22.9 microM, respectively. The present investigation showed that the phytochemicals piperine, paeonol and emodin are potent MAO inhibitors whereas other compounds were inactive against any type of MAO at 100 microM in the present assay.
Asunto(s)
Inhibidores de la Monoaminooxidasa/farmacología , Monoaminooxidasa/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Plantas Medicinales , Alcaloides/administración & dosificación , Alcaloides/farmacología , Alcaloides/uso terapéutico , Animales , Antraquinonas/administración & dosificación , Antraquinonas/farmacología , Antraquinonas/uso terapéutico , Encéfalo/efectos de los fármacos , Encéfalo/enzimología , Mitocondrias/efectos de los fármacos , Mitocondrias/enzimología , Inhibidores de la Monoaminooxidasa/administración & dosificación , Inhibidores de la Monoaminooxidasa/uso terapéutico , Fenoles/administración & dosificación , Fenoles/farmacología , Fenoles/uso terapéutico , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico , RatasRESUMEN
A new oxoaporphine alkaloid, sinofranine, was isolated from the stem of Sinofranchetia chinensis. The structure of the new alkaloid was elucidated by a combination of spectral methods (IR, MS, 1H and 13C-NMR, NOED and COSY).