RESUMO
Two new phthalide derivatives, (-)-3-carboxypropyl-7-hydroxyphthalide (1) and (-)-3-carboxypropyl-7-hydroxyphthalide methyl ester (2), were isolated from the endophytic fungus Penicillium vulpinum isolated from the Chinese medicinal plant Sophora tonkinensis. Their structures were elucidated using spectroscopic methods, mainly on 1D and 2D NMR. Compound 1 exhibited medium antibacterial activities against Bacillus subtilis, Shigella dysenteriae and Enterobacter areogenes with MIC values of 12.5-25 µg/mL, and 2 showed a medium inhibition to E. areogenes with MIC value of 12.5 µg/mL.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Benzofuranos/química , Penicillium/química , Sophora/microbiologia , Bacillus subtilis/efeitos dos fármacos , Benzofuranos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Endófitos/química , Enterobacter/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Penicillium/isolamento & purificação , Plantas Medicinais/microbiologia , Shigella dysenteriae/efeitos dos fármacosRESUMO
Pancreatic cancer is a lethal disease, and new treatments need to be explored. Huaier extract is a traditional Chinese medicine that has been found to exert antitumor properties in some cancers. However, the role of Huaier extract in pancreatic cancer has not been examined. In this study, we found that the proliferation, migration, invasion and EMT (epithelial-mesenchymal transition) of pancreatic cancer cells were suppressed by treatment with Huaier extract and that apoptosis increased. We also observed that expression of ß-catenin was inhibited by Huaier extract. Furthermore, an animal study showed that Huaier extract slowed tumor growth in pancreatic cancer. Our results reveal that Huaier extract suppresses pancreatic cancer by inhibiting Wnt/ß-catenin pathway both in vitro and in vivo.
Assuntos
Misturas Complexas , Medicina Tradicional Chinesa , Neoplasias Pancreáticas/tratamento farmacológico , Trametes , Via de Sinalização Wnt/efeitos dos fármacos , beta Catenina/antagonistas & inibidores , Animais , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Transição Epitelial-Mesenquimal/efeitos dos fármacos , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Neoplasias Pancreáticas/patologia , Sophora/microbiologia , Trametes/química , Via de Sinalização Wnt/fisiologiaRESUMO
A new eremophilane sesquiterpene, xylareremophil (1), together with five known eremophilanes, 1α,10α-epoxy-3α-hydroxyeremophil-7(11)-en-12,8ß-olide (2), 1,10α,13-trihydroxyeremophil-7(11)-en-12,8-olide (3), 1α,10α-epoxy-13-hydroxyeremophil-7(11)-en-12,8ß-olide (4), mairetolides B (5) and G (6) were isolated from the endophytic fungus Xylaria sp. GDG-102 cultured from Sophora tonkinensis. Their structures were elucidated on the basis of spectroscopic data analysis. The absolute configurations of 1 was determined by comparing computed electronic circular dichroism (ECD) and optical rotation (OR) with experimental results. Compounds 1, 5 and 6 showed antibacterial activities against Proteus vulgaris, Micrococcus luteus, Micrococcus lysodeikticus and Bacillus subtilis with MIC values of 25-100 µg/mL.
Assuntos
Antibacterianos/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Xylariales/química , Antibacterianos/química , Bacillus subtilis/efeitos dos fármacos , Dicroísmo Circular , Avaliação Pré-Clínica de Medicamentos , Endófitos/química , Testes de Sensibilidade Microbiana , Micrococcus luteus/efeitos dos fármacos , Estrutura Molecular , Sesquiterpenos/isolamento & purificação , Sophora/microbiologiaRESUMO
A new phthalide derivative, xylarphthalide A (1), along with two known compounds (-)-5-carboxylmellein (2) and (-)-5-methylmellein (3), were isolated from the endophytic fungus Xylaria sp. GDG-102 cultured from the Chinese medicinal plant Sophora tonkinensis. Their structures were identified by MS and NMR experiments, and the absolute configuration of 1 was further confirmed by single-crystal X-ray diffraction analysis. Compound 1-3 showed antibacterial activities against Bacillus megaterium, Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Shigella dysenteriae with MIC values of 12.5-25 µg/mL.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Benzofuranos/química , Benzofuranos/farmacologia , Xylariales/química , Bacillus subtilis/efeitos dos fármacos , Cristalografia por Raios X , Endófitos/química , Escherichia coli/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Plantas Medicinais/microbiologia , Sophora/microbiologia , Staphylococcus aureus/efeitos dos fármacosRESUMO
Two new cyclopentapeptides, xylapeptide A (1) with an uncommon L-pipecolinic acid moiety, and xylapeptide B (2) having a common L-proline residue were identified from an associated fungus Xylaria sp. isolated from the Chinese medicinal plant Sophora tonkinensis. Their planar structures were elucidated by a comprehensive analysis of NMR and MS spectroscopic spectra. The absolute configurations were determined by Marfey's method and single-crystal X-ray diffraction (Cu Kα) analysis. Xylapeptide A (1) is the first example of cyclopentapeptide with L-Pip of terrestrial origin and showed strong antibacterial activity against Bacillus subtilis and B. cereus with MIC value of 12.5 µg/mL.
Assuntos
Antibacterianos/química , Bacillus/efeitos dos fármacos , Peptídeos Cíclicos/química , Xylariales/química , Antibacterianos/farmacologia , Bacillus cereus/efeitos dos fármacos , Bacillus subtilis/efeitos dos fármacos , Cristalografia por Raios X , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Peptídeos Cíclicos/farmacologia , Sophora/microbiologia , Xylariales/isolamento & purificaçãoRESUMO
Understanding the influence of arbuscular mycorrhizal (AM) fungi on the expressions of the dominant plant-related genes under heavy metal (HM) stress is important for developing strategies to reclaim polluted sites. In this study, we cloned full-length cDNAs of phytochelatin synthase gene (PCS1) and Actin of Sophora viciifolia Hance., a predominant plant in Qiandongshan lead and zinc mine, by rapid amplification of cDNA ends. Consequently, we studied the response of SvPCS1 to Funneliformis mosseae inoculation under lead stress (0, 50, and 200 µM Pb(NO3)2) at different durations (1, 3, and 7 days) using quantitative reverse-transcription polymerase chain-reaction (qRT-PCR) technique. The Pb concentrations and chlorophyll fluorescence parameters were also measured to assay Pb toxicity to Sophora viciifolia. We found that Pb concentrations in roots increased with increasing Pb application and the durations; the F v /F m , F v /F o , qP, and Y(II) decreased; NPQ rose with increasing Pb concentrations; mycorrhizal symbiosis alleviated the Pb toxicity to plants; and SvPCS1 was constitutively expressed in the roots. It was also found that F. mosseae inoculation could promote the expression of SvPCS1 with the concentration ≤ 200 µM at the exposure time shorter than 7 days.
Assuntos
Aminoaciltransferases/genética , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Glomeromycota/fisiologia , Chumbo/toxicidade , Micorrizas/fisiologia , Raízes de Plantas/efeitos dos fármacos , Poluentes do Solo/toxicidade , Sophora/efeitos dos fármacos , Clorofila/metabolismo , DNA Complementar/genética , Proteínas de Plantas/genética , Raízes de Plantas/microbiologia , Raízes de Plantas/fisiologia , Sophora/microbiologia , Sophora/fisiologiaRESUMO
The endophytic strain Zong1 isolated from root nodules of the legume Sophora alopecuroides was characterized by conducting physiological and biochemical tests employing gfp-marking, observing their plant growth promoting characteristics (PGPC) and detecting plant growth parameters of inoculation assays under greenhouse conditions. Results showed that strain Zong1 had an effective growth at 28 ºC after placed at 4-60 ºC for 15 min, had a wide range pH tolerance of 6.0-11.0 and salt tolerance up to 5% of NaCl. Zong1 was resistant to the following antibiotics (µg/mL): Phosphonomycin (100), Penicillin (100) and Ampicillin (100). It could grow in the medium supplemented with 1.2 mmol/L Cu, 0.1% (w/v) methylene blue and 0.1-0.2% (w/v) methyl red, respectively. Zong1 is closely related to Pseudomonas chlororaphis based on analysis the sequence of 16S rRNA gene. Its expression of the gfp gene indicated that strain Zong1 may colonize in root or root nodules and verified by microscopic observation. Furthermore, co-inoculation with Zong1 and SQ1 (Mesorhizobium sp.) showed significant effects compared to single inoculation for the following PGPC parameters: siderophore production, phosphate solubilization, organic acid production, IAA production and antifungal activity in vitro. These results suggest strains P. chlororaphi Zong1 and Mesorhizobium sp. SQ1 have better synergistic or addictive effect. It was noteworthy that each growth index of co-inoculated Zong1+SQ1 in growth assays under greenhouse conditions is higher than those of single inoculation, and showed a significant difference (p < 0.05) when compared to a negative control. Therefore, as an endophyte P. chlororaphis Zong1 may play important roles as a potential plant-growth promoting agent.
Assuntos
Endófitos/isolamento & purificação , Endófitos/metabolismo , Pseudomonas/isolamento & purificação , Pseudomonas/metabolismo , Sophora/microbiologia , Antibacterianos/farmacologia , Antibiose , Ácidos Carboxílicos/metabolismo , Análise por Conglomerados , DNA Bacteriano/química , DNA Bacteriano/genética , DNA Ribossômico/química , DNA Ribossômico/genética , Endófitos/classificação , Endófitos/genética , Fungos/crescimento & desenvolvimento , Concentração de Íons de Hidrogênio , Ácidos Indolacéticos/metabolismo , Dados de Sequência Molecular , Fosfatos/metabolismo , Filogenia , Desenvolvimento Vegetal , Raízes de Plantas/microbiologia , Pseudomonas/classificação , Pseudomonas/genética , RNA Ribossômico 16S/genética , Análise de Sequência de DNA , Sideróforos/metabolismo , Cloreto de Sódio/metabolismo , Sophora/crescimento & desenvolvimento , TemperaturaRESUMO
The endophytic strain Zong1 isolated from root nodules of the legume Sophora alopecuroides was characterized by conducting physiological and biochemical tests employing gfp-marking, observing their plant growth promoting characteristics (PGPC) and detecting plant growth parameters of inoculation assays under greenhouse conditions. Results showed that strain Zong1 had an effective growth at 28 ºC after placed at 4-60 ºC for 15 min, had a wide range pH tolerance of 6.0-11.0 and salt tolerance up to 5% of NaCl. Zong1 was resistant to the following antibiotics (µg/mL): Phosphonomycin (100), Penicillin (100) and Ampicillin (100). It could grow in the medium supplemented with 1.2 mmol/L Cu, 0.1% (w/v) methylene blue and 0.1-0.2% (w/v) methyl red, respectively. Zong1 is closely related to Pseudomonas chlororaphis based on analysis the sequence of 16S rRNA gene. Its expression of the gfp gene indicated that strain Zong1 may colonize in root or root nodules and verified by microscopic observation. Furthermore, co-inoculation with Zong1 and SQ1 (Mesorhizobium sp.) showed significant effects compared to single inoculation for the following PGPC parameters: siderophore production, phosphate solubilization, organic acid production, IAA production and antifungal activity in vitro. These results suggest strains P. chlororaphi Zong1 and Mesorhizobium sp. SQ1 have better synergistic or addictive effect. It was noteworthy that each growth index of co-inoculated Zong1+SQ1 in growth assays under greenhouse conditions is higher than those of single inoculation, and showed a significant difference (p < 0.05) when compared to a negative control. Therefore, as an endophyte P. chlororaphis Zong1 may play important roles as a potential plantgrowth promoting agent.
Assuntos
Endófitos/isolamento & purificação , Endófitos/metabolismo , Pseudomonas/isolamento & purificação , Pseudomonas/metabolismo , Sophora/microbiologia , Antibiose , Antibacterianos/farmacologia , Análise por Conglomerados , Ácidos Carboxílicos/metabolismo , DNA Bacteriano/química , DNA Bacteriano/genética , DNA Ribossômico/química , DNA Ribossômico/genética , Endófitos/classificação , Endófitos/genética , Fungos/crescimento & desenvolvimento , Concentração de Íons de Hidrogênio , Ácidos Indolacéticos/metabolismo , Dados de Sequência Molecular , Filogenia , Desenvolvimento Vegetal , Fosfatos/metabolismo , Raízes de Plantas/microbiologia , Pseudomonas/classificação , Pseudomonas/genética , /genética , Análise de Sequência de DNA , Sideróforos/metabolismo , Cloreto de Sódio/metabolismo , Sophora/crescimento & desenvolvimento , TemperaturaRESUMO
BACKGROUND: The roots of Sophora flavescens (Leguminosae) have been used in East Asian countries as an herbal medicine and a food ingredient for thousands of years. The aim of the present study was to investigate the effects of S. flavescens fermentation on endotoxin-induced uveitis (EIU) in rats. METHODS: EIU was induced in rats via a footpad injection of lipopolysaccharide (LPS). Immediately after the LPS inoculation, fermented and non-fermented extracts of S. flavescens (FSE and NFSE, respectively) were administered orally, and the aqueous humor was collected from both eyes 24 hours later. The anti-inflammatory effects of FSE and NFSE were examined in terms of regulation of nuclear factor kappa B (NF-κB) activation and the expression of interleukin-1ß (IL-1ß), tumor necrosis factor-α (TNF-α), inducible nitric oxide synthase (iNOS), intercellular cell adhesion molecule (ICAM)-1, and cyclooxygenase-2 (COX-2). The regulation of maleic dialdehyde (MDA) levels and polymorphonuclear cell (PMN) infiltration by FSE and NFSE were also examined. RESULTS: Treatment with FSE significantly inhibited LPS-induced increases in IL-1ß and TNF-α production and the expression of iNOS, ICAM-1 and COX-2. Moreover, FSE suppressed LPS-induced NF-κB activation, and reduced both MDA levels and infiltration by PMN. CONCLUSION: These results indicate that solid state fermentation may enhance the anti-inflammatory effects of S. flavescens.