RESUMEN
ETHANOPHARMACOLOGICAL RELEVANCE: Potentilla kleiniana Wight et Arn is a wide-spread wild plant in the mountainous areas in southern China. The whole herb has been used as a traditional herbal medicine to treat fever, arthritis, malaria, insect and snake bites, hepatitis, and traumatic injury. In vitro studies have reported the antibacterial activity use of the plant in traditional medicinal systems. AIM OF THE STUDY: The aim of this study was to investigate the inhibitory activity of total flavonoid from Potentilla kleiniana Wight et Arn (TFP) on methicillin-resistant Staphylococcus aureus (MRSA) in planktonic state and biofilm state. MATERIALS AND METHODS: Antibacterial activities of TFP on planktonic MRSA were determined by agar diffusion method, microtiter plate assay and time-kill curve assay. Electrical conductivity, membrane permeability, membrane potential and autoaggregation were analyzed to study TFP effects on planktonic MRSA growth. Crystal violet (CV) staining and confocal laser scanning microscopy (CLSM) were analyzed to study TFP effects on aggregation and maturation of MRSA biofilm. After TFP treatment, extracellular polymeric substances (EPS) production were examined. Morphological changes in planktonic and MRSA biofilm following TFP treatment were determined with scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Moreover, α-Toxin protein expression and adhesion-related gene expression were also determined. RESULTS: The minimum inhibitory concentration (MIC) of TFP against MRSA was 20 µg/mL. The agar diffusion method and time-kill curve assay results indicated that TFP inhibited planktonic MRSA growth. TFP treatment significantly inhibited planktonic MRSA growth by inhibiting autoaggregation, α-hemolysin activity, α-Toxin protein expression, but increasing electrolyte leakage, membrane permeability and membrane potential and impacting cell structure. Moreover, TFP treatment significantly inhibited aggregation and maturation on MRSA biofilm by decreasing surface hydrophobicity, EPS production and adhesion-related gene expression. CONCLUSION: The results of this trial provide scientific experimental data on the traditional use of Potentilla Kleiniana Wight et Arn for traumatic injury treatment and further demonstrate the potential of TFP to be developed as a novel anti-biofilm drug.
Asunto(s)
Biopelículas/efectos de los fármacos , Biopelículas/crecimiento & desarrollo , Flavonoides/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Potentilla/química , Factores de Virulencia/metabolismo , Antibacterianos/química , Antibacterianos/farmacología , Flavonoides/química , Regulación Bacteriana de la Expresión Génica/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Microscopía Confocal , Microscopía Electrónica de Rastreo , Microscopía Electrónica de Transmisión , Factores de Virulencia/genéticaRESUMEN
Tripolinolate A (TLA) is recently identified as a new compound from a halophyte plant Tripolium vulgare and has been shown to have significant in vitro activity against the proliferation of colorectal cancer and glioma cells. This study was designed to further investigate the effects of TLA on the proliferation of human normal cells, and the apoptosis and cell cycle in colorectal cancer cells, and the growth of tumors in the colorectal cancer-bearing animals. The data obtained from this study demonstrated that: 1) TLA had much less cytotoxicity in the human normal cells than the colorectal cancer cells; 2) TLA remarkably induced apoptosis in the human colorectal cancer cells and blocked cell cycle at G2/M phase, and 3) TLA had significant anti-colorectal cancer activity in the tumor-bearing animals.
Asunto(s)
Antineoplásicos Fitogénicos/administración & dosificación , Asteraceae/química , Neoplasias Colorrectales/tratamiento farmacológico , Medicamentos Herbarios Chinos/administración & dosificación , Fenoles/administración & dosificación , Animales , Antineoplásicos Fitogénicos/química , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Neoplasias Colorrectales/fisiopatología , Medicamentos Herbarios Chinos/química , Ésteres/administración & dosificación , Ésteres/química , Fase G2/efectos de los fármacos , Humanos , Masculino , Ratones , Ratones Endogámicos BALB C , Fenoles/químicaRESUMEN
Chemical investigation of the cultures of marine Streptomyces sp. 182SMLY led to the discovery of two new polycyclic anthraquinones, which were elucidated as N-acetyl-N-demethylmayamycin (1) and streptoanthraquinone A (2) based on the extensive spectroscopic analysis including 2D NMR, HRESIMS, and an electronic circular dichroism (ECD) calculation. Both anthraquinones remarkably suppressed the proliferation of four different glioma cell lines with IC50 values in a range from 0.5 to 7.3 µM and induced apoptosis in the glioma cells. The ratios of IC50 for normal human astrocytes to IC50 for glioma cells were 6.4-53 for 1 and >14-31 for 2. N-acetyl-N-demethylmayamycin (1) also inhibited the growth of methicillin-resistant Staphylococcus aureus with MIC 20.0 µM.
Asunto(s)
Antibacterianos/farmacología , Antineoplásicos/farmacología , Quinonas/farmacología , Staphylococcus aureus/efectos de los fármacos , Streptomyces/metabolismo , Animales , Línea Celular Tumoral/efectos de los fármacos , China , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Concentración 50 Inhibidora , Ratas , Agua de Mar , Relación Estructura-ActividadRESUMEN
Four new stilbene derivatives, polygonumosides A-D (1-4), were isolated from the processed roots of Polygonum multiflorum. Their structures were elucidated by spectroscopic analysis, including 1D and 2D NMR and ECD. Polygonumosides A (1) and B (2), possessing an unprecedented tetracyclic skeleton, were assigned as 2S- and 2R-2-(4-hydroxyphenyl)-9,10,11-trihydroxy-2H-benzo[c]furo[2,3-f]chromen-7(3H)-one-4-O-ß-d-glucopyranosides, respectively, while polygonumosides C (3) and D (4) were assigned as a pair of diastereomeric stilbene glucoside dimers.
Asunto(s)
Medicamentos Herbarios Chinos/aislamiento & purificación , Glucósidos/aislamiento & purificación , Polygonum/química , Estilbenos/aislamiento & purificación , Medicamentos Herbarios Chinos/química , Glucósidos/química , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Raíces de Plantas/química , Estilbenos/químicaRESUMEN
Two new phenylpropanoid glycosides, 1,3,4-tri-O-(E)-caffeoyl-ß-d-glucopyranoside (1) and 1,4-di-O-(E)-caffeoyl-ß-d-glucopyranoside (2), along with four known phenylpropanoid glycosides (3-6), were isolated from the roots of Aruncus sylvester. The structures of 1 and 2 were elucidated using various spectroscopic methods. Compounds 1 and 2 displayed significant scavenging activity of 2,2-diphenyl-1-picrylhydrazyl free radicals with IC50 values of 110 and 258 µM (ascorbic acid: IC50 = 574 µM).
Asunto(s)
Ácidos Cafeicos/aislamiento & purificación , Medicamentos Herbarios Chinos/aislamiento & purificación , Depuradores de Radicales Libres/aislamiento & purificación , Glucósidos/aislamiento & purificación , Fenilpropionatos/aislamiento & purificación , Rosaceae/química , Antioxidantes/química , Compuestos de Bifenilo/farmacología , Ácidos Cafeicos/química , Medicamentos Herbarios Chinos/química , Depuradores de Radicales Libres/química , Radicales Libres/química , Glucósidos/química , Estructura Molecular , Fenilpropionatos/química , Picratos/farmacologíaRESUMEN
Two flavonoids with an unusual 2',4',5'-trisubstituted B-ring (1 and 2), four myricetin derivatives (3-methylmyricetin-3'-O-beta-D-xylopyranoside (3), myricetin-3-O-alpha-L-rhamnopyranoside, myricetin-3-O-beta-D-galactopyranoside, and 3-methylmyricetin), and myricetin were isolated from the roots of Pteroxygonum giraldii Damm. & Diels. Their structures were elucidated using various spectroscopic methods and acid hydrolysis. Compound 1 was a new flavonoid and the NMR spectroscopic data of compounds 2 and 3 are reported for the first time.