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1.
Materials (Basel) ; 16(19)2023 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-37834549

RESUMO

High-temperature forming behaviors of a 7046-aluminum alloy were investigated by hot compression experiments. The microstructural evolution features with the changes in deformation parameters were dissected. Results indicated the formation of massive dislocation clusters/cells and subgrains through the intense DRV mechanism at low compression temperature. With an increase in deformation temperature, the annihilation of dislocations and the coarsening of subgrains/DRX grains became prominent, due to the collaborative effects of the DRV and DRX mechanisms. However, the growth of subgrains and DRX grains displayed the weakening trend at high strain rates. Moreover, two constitutive models involving a physically based (PB) model and a gate recurrent unit (GRU) model were proposed for predicting the hot compression features. By validation analysis, the predicted values of true stress perfectly fit with the experimental data, indicating that both the proposed PB model and the GRU model can accurately predict the hot compression behaviors of 7046-aluminum alloys.

2.
J Environ Sci (China) ; 125: 662-677, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36375948

RESUMO

Smelting activities pose serious environmental problems due to the local and regional heavy metal pollution in soils they cause. It is therefore important to understand the pollution situation and its source in the contaminated soils. In this paper, data on heavy metal pollution in soils resulting from Pb/Zn smelting (published in the last 10 years) in China was summarized. The heavy metal pollution was analyzed from a macroscopic point of view. The results indicated that Pb, Zn, As and Cd were common contaminants that were present in soils with extremely high concentrations. Because of the extreme carcinogenicity, genotoxicity and neurotoxicity that heavy metals pose, remediation of the soils contaminated by smelting is urgently required. The primary anthropogenic activities contributing to soil pollution in smelting areas and the progressive development of accurate source identification were performed. Due to the advantages of biominerals, the potential of biomineralization for heavy metal contaminated soils was introduced. Furthermore, the prospects of geochemical fraction analysis, combined source identification methods as well as several optimization methods for biomineralization are presented, to provide a reference for pollution investigation and remediation in smelting contaminated soils in the future.


Assuntos
Metais Pesados , Poluentes do Solo , Poluentes do Solo/análise , Chumbo/análise , Biomineralização , Monitoramento Ambiental/métodos , Metais Pesados/análise , Poluição Ambiental/análise , Solo , China , Zinco/análise , Medição de Risco
3.
Materials (Basel) ; 15(1)2021 Dec 21.
Artigo em Inglês | MEDLINE | ID: mdl-35009153

RESUMO

The hot deformation characteristics of a GH4169 superalloy are investigated at the temperature and strain rate ranges of 1193-1313 K and 0.01-1 s-1, respectively, through Gleeble-3500 simulator. The hot deformed microstructures are analyzed by optical microscopy (OM), transmission electron microscopy (TEM), and electron backscattered diffraction (EBSD) technology. The effects of deformation parameters on the features of flow curves and annealing twins are discussed in detail. It is found that the shapes of flow curves are greatly affected by the deformation temperature. Broad peaks appear at low deformation temperatures or high strain rates. In addition, the evolution of annealing twins is significantly sensitive to the deformation degree, temperature, and strain rate. The fraction of annealing twins first decreases and then rises with the added deformation degree. This is because the initial annealing twin characters disappear at the relatively small strains, while the annealing twins rapidly generate with the growth of dynamic recrystallized grains during the subsequent hot deformation. The fraction of annealing twins is relatively high when the deformation temperature is high or the strain rate is low. In addition, the important role of annealing twins on dynamic recrystallization (DRX) behaviors are elucidated. The obvious bulging at initial twin boundaries, and the coherency of annealing twin boundaries with dynamic recrystallized grain boundaries, indicates that annealing twins can motivate the DRX nucleation during the hot deformation.

4.
Molecules ; 23(5)2018 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-29762539

RESUMO

The polar extract of the Dendrobium species or F. fimbriata (a substitute of Dendrobium), between the fat-soluble extract and polysaccharide has barely been researched. This report worked on the qualitative and quantitative studies of polar extracts from D. nobile, D. officinale, D. loddigesii, and F. fimbriata. Eight water-soluble metabolites containing a new diglucoside, flifimdioside A (1), and a rare imidazolium-type alkaloid, anosmine (4), were identified using chromatography as well as spectroscopic techniques. Their contents in the four herbs were high, approximately 0.9⁻3.7 mg/g based on the analysis of quantitative nuclear magnetic resonance (qNMR) spectroscopy. Biological activity evaluation showed that the polar extract of F. fimbriata or its pure component had good antioxidant and neuroprotective activity; compounds 1‒4 and shihunine (8) showed weak α-glucosidase inhibitory activity; 4 and 8 had weak anti-inflammatory activity. Under trial conditions, all samples had no cytotoxic activity.


Assuntos
Dendrobium/química , Dendrobium/metabolismo , Metaboloma , Metabolômica , Extratos Vegetais/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Metabolômica/métodos , Extratos Vegetais/farmacologia , Solubilidade , Água
5.
Nat Prod Res ; 32(24): 2887-2892, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29022767

RESUMO

One new depsidone, botryorhodine H (1), together with three known analogues, botryorhodines C, D and G (2-4), were obtained from the mangrove endophytic fungus Trichoderma sp. 307 by co-culturing with Acinetobacter johnsonii B2. Structures were determined by 1D and 2D NMR analyses and high-resolution mass spectrum. Compounds 1-3 showed α-glucosidase inhibitory activity with IC50 ranging from 8.1 to 11.2 µM, and compound 1 exhibited potent cytotoxicity against rat prolactinoma MMQ and rat pituitary adenoma GH3 cell lines (IC50 = 3.09 and 3.64 µM).


Assuntos
Inibidores de Glicosídeo Hidrolases/farmacologia , Trichoderma/química , Acinetobacter/citologia , Animais , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Linhagem Celular , Técnicas de Cocultura , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/uso terapêutico , Concentração Inibidora 50 , Estrutura Molecular , Neoplasias Hipofisárias/tratamento farmacológico , Extratos Vegetais/química , Policetídeos/química , Policetídeos/isolamento & purificação , Prolactinoma/tratamento farmacológico , Ratos
6.
Fitoterapia ; 124: 103-107, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29074224

RESUMO

Four new chromenopyridine derivatives, phochrodines A-D (1-4), were identified from mangrove entophytic fungus Phomopsis sp. 33# by means of various modern chromatographic, spectroscopic and single crystal X-ray diffraction techniques. Compounds 1-4 with an unusual 5H-chromeno[4,3-b]pyridine skeleton were the first naturally occurring chromenopyridines. Their anti-inflammatory, antioxidant and cytotoxic activities were evaluated. 3 and 4 showed moderate inhibition of nitric oxide production with IC50 values of 49.0 as well as 51.0µM, respectively. 4 had well ability to scavenge DPPH radical with IC50 value of 34.0µM. The four had no cytotoxic activity for MDA-MB-435 breast cancer cells.


Assuntos
Ascomicetos/química , Piridinas/isolamento & purificação , Rhizophoraceae/microbiologia , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular Tumoral , Sequestradores de Radicais Livres/isolamento & purificação , Humanos , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Células RAW 264.7
7.
Mar Drugs ; 14(11)2016 Nov 22.
Artigo em Inglês | MEDLINE | ID: mdl-27879655

RESUMO

Four new chromone derivatives, phomopsichins A-D (1-4), along with a known compound, phomoxanthone A (5), were isolated from the fermentation products of mangrove endophytic fungus Phomopsis sp. 33#. Their structures were elucidated based on comprehensive spectroscopic analysis coupled with single-crystal X-ray diffraction or theoretical calculations of electronic circular dichroism (ECD). They feature a tricyclic framework, in which a dihydropyran ring is fused with the chromone ring. Compounds 1-5 showed weak inhibitory activities on acetylcholinesterase as well as α-glucosidase, weak radical scavenging effects on 1,1-diphenyl-2-picrylhydrazyl (DPPH) as well as OH, and weak antimicrobial activities. Compounds 1-4 showed no cytotoxic activity against MDA-MB-435 breast cancer cells. Their other bioactivities are worthy of further study, considering their unique molecular structures.


Assuntos
Cromonas/química , Endófitos/química , Fungos/química , Acetilcolinesterase/metabolismo , Compostos de Bifenilo/metabolismo , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Cromonas/farmacologia , Cristalografia por Raios X/métodos , Fermentação/fisiologia , Humanos , Estrutura Molecular , Picratos/metabolismo , Difração de Raios X/métodos , Xantonas/química , Xantonas/farmacologia , alfa-Glucosidases/metabolismo
8.
Nat Prod Res ; 30(7): 755-60, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26222141

RESUMO

Four new lasiodiplodins (1-4), together with three known analogues, have been isolated from a mangrove endophytic fungus, Lasiodiplodia sp. 318#. Their structures were elucidated by spectroscopic techniques. Cytotoxic activities of compounds 1-7 were evaluated in vitro against human cancer lines THP1, MDA-MB-435, A549, HepG2 and HCT-116. Compound 4 exhibited moderate cytotoxic activities.


Assuntos
Antineoplásicos/química , Ascomicetos/química , Avicennia/microbiologia , Zearalenona/análogos & derivados , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Endófitos/química , Fermentação , Humanos , Fungos Mitospóricos , Estrutura Molecular , Zearalenona/química , Zearalenona/isolamento & purificação
9.
Nat Prod Commun ; 10(9): 1549-51, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26594756

RESUMO

A new benzodiazepine alkaloid containing terminal cyano group has been isolated from a mangrove endophytic fungus, Penicillium 299#. Structure elucidation was determined by 1D and 2D NMR spectroscopy and the absolute configuration was determined by electronic circular dichroism (ECD). The new compound showed no cytotoxic activities in vitro against human cancer lines MDA-MB-435, HepG2, HCT-116, and Calu-3.


Assuntos
Acanthaceae/microbiologia , Alcaloides/química , Benzodiazepinas/química , Penicillium/química
10.
Mar Drugs ; 13(4): 2306-26, 2015 Apr 14.
Artigo em Inglês | MEDLINE | ID: mdl-25874925

RESUMO

Our previous studies demonstrated that xyloketal B, a novel marine compound with a unique chemical structure, has strong antioxidant actions and can protect against endothelial injury in different cell types cultured in vitro and model organisms in vivo. The oxidative endothelial dysfunction and decrease in nitric oxide (NO) bioavailability are critical for the development of atherosclerotic lesion. We thus examined whether xyloketal B had an influence on the atherosclerotic plaque area in apolipoprotein E-deficient (apoE-/-) mice fed a high-fat diet and investigated the underlying mechanisms. We found in our present study that the administration of xyloketal B dose-dependently decreased the atherosclerotic plaque area both in the aortic sinus and throughout the aorta in apoE-/- mice fed a high-fat diet. In addition, xyloketal B markedly reduced the levels of vascular oxidative stress, as well as improving the impaired endothelium integrity and NO-dependent aortic vasorelaxation in atherosclerotic mice. Moreover, xyloketal B significantly changed the phosphorylation levels of endothelial nitric oxide synthase (eNOS) and Akt without altering the expression of total eNOS and Akt in cultured human umbilical vein endothelial cells (HUVECs). Here, it increased eNOS phosphorylation at the positive regulatory site of Ser-1177, while inhibiting phosphorylation at the negative regulatory site of Thr-495. Taken together, these findings indicate that xyloketal B has dramatic anti-atherosclerotic effects in vivo, which is partly due to its antioxidant features and/or improvement of endothelial function.


Assuntos
Antioxidantes/uso terapêutico , Aorta/efeitos dos fármacos , Apolipoproteínas E/deficiência , Fármacos Cardiovasculares/uso terapêutico , Endotélio Vascular/efeitos dos fármacos , Erros Inatos do Metabolismo Lipídico/tratamento farmacológico , Placa Aterosclerótica/prevenção & controle , Piranos/uso terapêutico , Animais , Antioxidantes/efeitos adversos , Antioxidantes/farmacologia , Aorta/metabolismo , Aorta/fisiopatologia , Aorta/ultraestrutura , Apolipoproteínas E/metabolismo , Fármacos Cardiovasculares/efeitos adversos , Fármacos Cardiovasculares/farmacologia , Células Cultivadas , Dieta Hiperlipídica/efeitos adversos , Endotélio Vascular/metabolismo , Endotélio Vascular/fisiopatologia , Endotélio Vascular/ultraestrutura , Células Endoteliais da Veia Umbilical Humana/citologia , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Células Endoteliais da Veia Umbilical Humana/metabolismo , Humanos , Erros Inatos do Metabolismo Lipídico/metabolismo , Erros Inatos do Metabolismo Lipídico/patologia , Erros Inatos do Metabolismo Lipídico/fisiopatologia , Masculino , Camundongos Knockout , Óxido Nítrico Sintase Tipo III/genética , Óxido Nítrico Sintase Tipo III/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Fosforilação/efeitos dos fármacos , Placa Aterosclerótica/etiologia , Processamento de Proteína Pós-Traducional/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/genética , Proteínas Proto-Oncogênicas c-akt/metabolismo , Piranos/efeitos adversos , Piranos/farmacologia , Organismos Livres de Patógenos Específicos , Vasodilatação/efeitos dos fármacos
11.
Anticancer Agents Med Chem ; 15(2): 258-66, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25641103

RESUMO

One known cyclic peptide, beauvericin, was isolated from the secondary metabolites of mangrove endophytic fungi Fusarium sp. (No. DZ27) in South China Sea. Its structure was determined by spectral analyses and comparisons with reference data from literatures. Beauvericin inhibited growth of KB and KBv200 cells potently with IC50 values of 5.76 ± 0.55 and 5.34 ± 0.09 µM, respectively. Furthermore, beauvericin induced apoptosis through mitochondrial pathway, including decrease of relative oxygen species generation, loss of mitochondrial membrane potential, release of cytochrome c, activation of Caspase-9 and -3, and cleavage of PARP. Additionally, regulation of Bcl-2 or Bax was not involved in the apoptosis induced by beauvericin in KB and KBv200 cells.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Depsipeptídeos/química , Depsipeptídeos/farmacologia , Fungos/química , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Caspase 9/metabolismo , Linhagem Celular Tumoral , Citocromos c/metabolismo , Fusarium/química , Humanos , Células KB , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Poli(ADP-Ribose) Polimerases/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Proteína X Associada a bcl-2/metabolismo
12.
Nat Prod Res ; 29(13): 1212-6, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25573432

RESUMO

Two new macrosporin dimers (1-2) along with four known compounds (3-6) were isolated from the extracts of the fungal strain Alternaria sp. XZSBG-1 from the sediment of the salt lake in the Bange, Tibetan, China. Their structures were determined by spectroscopic methods, mainly by 2D NMR spectra. Compounds 1 and 2 are new macrosporin dimers with symmetric chemical structures. In the cytotoxicity assay and inhibited alpha-glucosidase activity assay, all these compounds showed no notable inhibitory activity.


Assuntos
Alternaria/química , Antraquinonas/química , Linhagem Celular Tumoral , China , Fermentação , Sedimentos Geológicos/microbiologia , Humanos , Lactonas/química , Lagos/microbiologia , Estrutura Molecular , alfa-Glucosidases
13.
Molecules ; 19(10): 16529-42, 2014 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-25317580

RESUMO

Four new anthraquinone derivatives 1-4 were obtained along with seven known compounds 5-11 from the extracts of the fungal strain Alternaria sp. XZSBG-1 which was isolated from the sediments of the carbonate saline lake in Bange, Tibet, China. Their structures were determined by spectroscopic methods, mainly by 2D NMR spectra. Compound 1 is a novel tetrahydroanthraquinone with an epoxy ether bond between C-4a and C-9a. In the primary bioassays, compound 3 (alterporriol T) exhibited inhibition of a-glucosidase with a IC50 value 7.2 µM, and compound 9 showed good inhibitory activity against the HCT-116 and HeLa cell lines, with IC50 values of 3.03 and 8.09 µM, respectively.


Assuntos
Alternaria/isolamento & purificação , Antraquinonas/química , Antraquinonas/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Alternaria/química , Linhagem Celular Tumoral , Proliferação de Células , Células HCT116 , Células HeLa , Humanos , Células MCF-7 , Ressonância Magnética Nuclear Biomolecular , Tibet
14.
Fitoterapia ; 97: 241-6, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24972351

RESUMO

Three new metabolites (compounds 1-2 and 6), one azaphilone, and two meroterpenes, together with eleven known compounds have been isolated from a mangrove endophytic fungus, Penicillium 303#. Structure elucidation was achieved by 1D and 2D NMR spectroscopy. The absolute configurations of 1 and 2 were determined by electronic circular dichroism (ECD). Cytotoxic activities of new compounds 1-2 and 6 and compound 7were evaluated in vitro against human cancer lines MDA-MB-435, HepG2, HCT-116, and A549. Those compounds showed weak to moderate cytotoxic activities.


Assuntos
Endófitos/química , Penicillium/química , Terpenos/isolamento & purificação , Benzopiranos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Células HCT116 , Células Hep G2 , Humanos , Estrutura Molecular , Pigmentos Biológicos/isolamento & purificação , Terpenos/química , Áreas Alagadas
15.
Molecules ; 19(6): 8544-55, 2014 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-24959681

RESUMO

Four new polyphenols, loddigesiinols G-J (compounds 1-4) and a known compound, crepidatuol B (5), were isolated from the stems of Dendrobium loddigesii that have long been used in Traditional Chinese Medicine and have recently been used to treat type 2 diabetes. Compounds 1-5 structures were elucidated based on spectroscopic analysis. The absolute configurations of compounds 1-4 were determined using theoretical calculations of electronic circular dichroism (ECD), and the absolute configuration of compound 5 was determined by a comparison of the experimental ECD spectra and the literature data. Compounds 1-5 are strong inhibitors of α-glucosidase, with IC50 values of 16.7, 10.9, 2.7, 3.2, and 18.9 µM, respectively. Their activities were significantly stronger than trans-resveratrol as a positive control (IC50 values of 27.9 µM).


Assuntos
Dendrobium/metabolismo , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Fenantrenos/isolamento & purificação , Polifenóis/isolamento & purificação , Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/química , Medicina Tradicional Chinesa , Estrutura Molecular , Fenantrenos/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Caules de Planta/metabolismo , Polifenóis/química , alfa-Glucosidases/química
16.
Mar Drugs ; 12(5): 2840-50, 2014 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-24828291

RESUMO

Three new resveratrol derivatives, namely, resveratrodehydes A-C (1-3), were isolated from the mangrove endophytic fungus Alternaria sp. R6. The structures of these compounds were elucidated by analysis of their MS, 1D and 2D NMR spectroscopic data. All compounds showed broad-spectrum inhibitory activities against three human cancer cell lines including human breast MDA-MB-435, human liver HepG2, and human colon HCT-116 by MTT assay (IC50 < 50 µM). Among them, compounds 1 and 2 both exhibited marked cytotoxic activities against MDA-MB-435 and HCT-116 cell lines (IC50 < 10 µM). Additionally, compounds 1 and 3 showed moderate antioxidant activity by DPPH radical scavenging assay.


Assuntos
Alternaria/química , Antioxidantes/química , Estilbenos/química , Alternaria/metabolismo , Antibióticos Antineoplásicos/biossíntese , Antibióticos Antineoplásicos/química , Antibióticos Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Fermentação , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Humanos , Myoporum/microbiologia , Resveratrol
17.
Mar Drugs ; 11(7): 2616-24, 2013 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-23877026

RESUMO

The mangrove endophytic fungus Aspergillus terreus (No. GX7-3B) was cultivated in potato dextrose liquid medium, and one rare thiophene compound (1), together with anhydrojavanicin (2), 8-O-methylbostrycoidin (3), 8-O-methyljavanicin (4), botryosphaerone D (5), 6-ethyl-5-hydroxy-3,7-dimethoxynaphthoquinone (6), 3ß,5α-dihydroxy-(22E,24R)-ergosta-7,22-dien-6-one (7), 3ß,5α,14α-trihydroxy-(22E,24R)-ergosta-7, 22-dien-6-one (8), NGA0187 (9) and beauvericin (10), were isolated. Their structures were elucidated by analysis of spectroscopic data. This is the first report of a natural origin for compound 6. Moreover, compounds 3, 4, 5, 7, 8 and 10 were obtained from marine microorganism for the first time. In the bioactive assays in vitro, compounds 2, 3, 9 and 10 displayed remarkable inhibiting actions against α-acetylcholinesterase (AChE) with IC50 values 2.01, 6.71, 1.89, and 3.09 µM, respectively. Furthermore, in the cytotoxicity assays, compounds 7 and 10 exhibited strong or moderate cytotoxic activities against MCF-7, A549, Hela and KB cell lines with IC50 values 4.98 and 2.02 (MCF-7), 1.95 and 0.82 (A549), 0.68 and 1.14 (Hela), and 1.50 and 1.10 µM (KB), respectively; compound 8 had weak inhibitory activities against these tumor cell lines; compounds 1, 2, 3, 4, 5, 6 and 9 exhibited no inhibitory activities against them.


Assuntos
Organismos Aquáticos/química , Organismos Aquáticos/metabolismo , Aspergillus/química , Aspergillus/metabolismo , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Linhagem Celular Tumoral , China , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Humanos , Células KB , Células MCF-7 , Oceanos e Mares
18.
Nat Prod Res ; 27(20): 1882-7, 2013 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23521163

RESUMO

A new compound 1 (named botryosphaerin F), along with other three known compounds 2 (13,14,15,16-tetranorlabd-7-ene-19,6b:12,17-diolide), 3 (botryosphaerin B) and 4 (LL-Z1271ß), has been isolated from the mangrove fungus Aspergillus terreus (No. GX7-3B). The structure of the new compound was established by analysis of spectroscopic data. The hypothetical biogenic relationship of four sesquiterpene analogues was also described in this paper. Furthermore, in the cytotoxicity assays, compound 1 showed potent inhibiting activity towards MCF-7 and HL-60 cancer cell lines with 50% inhibition of cell growth (IC50) values of 4.49 and 3.43 µM, respectively, and compound 4 exhibited promising activity against HL-60 cell line with an IC50 value of 0.6 µM.


Assuntos
Aspergillus/química , Misturas Complexas/análise , Rhizophoraceae/microbiologia , Sesquiterpenos/isolamento & purificação , Fermentação , Humanos , Concentração Inibidora 50 , Células MCF-7 , Estrutura Molecular , Sesquiterpenos/química , Relação Estrutura-Atividade , Temperatura de Transição
19.
Mar Drugs ; 10(12): 2715-28, 2012 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-23201593

RESUMO

Deoxybostrycin (1) is an anthraquinone compound derived from the marine mangrove fungus Nigrospora sp. No. 1403 and has potential to be a lead for new drugs because of its various biological properties. A series of new derivatives (2-22) of deoxybostrycin were synthesized. The in vitro cytotoxicity of all the new compounds was tested against MDA-MB-435, HepG2 and HCT-116 cancer cell lines. Most of the compounds exhibit strong cytotoxicity with IC50 values ranging from 0.62 to 10 µM. Compounds 19, 21 display comparable cytotoxicity against MDA-MB-435 to epirubicin, the positive control. The primary screening results indicate that the deoxybostrycin derivatives might be a valuable source of new potent anticancer drug candidates.


Assuntos
Antraquinonas/farmacologia , Antineoplásicos/farmacologia , Ascomicetos/química , Antraquinonas/administração & dosagem , Antraquinonas/síntese química , Antineoplásicos/administração & dosagem , Antineoplásicos/síntese química , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Neoplasias do Colo/tratamento farmacológico , Neoplasias do Colo/patologia , Epirubicina/farmacologia , Feminino , Células HCT116 , Células Hep G2 , Humanos , Concentração Inibidora 50 , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia
20.
Mar Drugs ; 10(6): 1307-1320, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22822374

RESUMO

Cyclotripeptide X-13 is a core of novel marine compound xyloallenoide A isolated from mangrove fungus Xylaria sp. (no. 2508). We found that X-13 dose-dependently induced angiogenesis in zebrafish embryos and in human endothelial cells, which was accompanied by increased phosphorylation of eNOS and Akt and NO release. Inhibition of PI3K/Akt/eNOS by LY294002 or L-NAME suppressed X-13-induced angiogenesis. The present work demonstrates that X-13 promotes angiogenesis via PI3K/Akt/eNOS pathways.


Assuntos
Indutores da Angiogênese/farmacologia , Organismos Aquáticos/química , Neovascularização Fisiológica/efeitos dos fármacos , Óxido Nítrico Sintase Tipo III/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos , Indutores da Angiogênese/síntese química , Indutores da Angiogênese/química , Indutores da Angiogênese/isolamento & purificação , Animais , Produtos Biológicos/síntese química , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/farmacologia , Linhagem Celular , Cromonas/farmacologia , Células Endoteliais/efeitos dos fármacos , Células Endoteliais/metabolismo , Fungos/química , Células Endoteliais da Veia Umbilical Humana , Humanos , Morfolinas/farmacologia , NG-Nitroarginina Metil Éster/farmacologia , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo III/antagonistas & inibidores , Inibidores de Fosfoinositídeo-3 Quinase , Fosforilação/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/antagonistas & inibidores , Peixe-Zebra/metabolismo
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