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1.
Chem Biodivers ; 11(7): 1078-87, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-25044593

RESUMO

Three chromone analogs, 1-3, a chlorinated alkaloid sclerotioramine (4), together with two 11-noreremophilane-type sesquiterpenes with a conjugated enolic OH group and a brominated one, 5 and 6, respectively, were isolated from Penicillium citreonigrum (HQ738282). Compounds 1, 5, and 6 were new. Biological tests revealed that 4 exhibited a significant activity (IC50 7.32 µg/ml), and 6 showed a moderate activity (IC50 16.31 µg/ml) in vitro against HepG2 cell line, and 4 also displayed an activity comparable to that of acarbose against α-glucosidase.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Penicillium/química , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Alcaloides/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Cristalografia por Raios X , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Halogenação , Células Hep G2 , Humanos , Modelos Moleculares , Neoplasias/tratamento farmacológico , Sesquiterpenos/isolamento & purificação
2.
Chem Pharm Bull (Tokyo) ; 61(3): 363-5, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23449205

RESUMO

A new 12-membered ring lactone, (3S),(6R)-6-hydroxylasiodiplodin (1), with two known analogues, (3R)-lasiodiplodin (2), and (3R),(5S)-5-hydroxylasiodiplodin (3) were isolated from the EtOH extracts of normal Apriona germari (Hope)-associated fungus Sarocladium kiliense grown in rice medium. The structures of compounds 1-3 were elucidated by a combination of spectroscopic data interpretation, single-crystal X-ray diffraction analysis, and modified Mosher's method.


Assuntos
Hypocreales/química , Lactonas/química , Zearalenona/análogos & derivados , Cristalografia por Raios X/métodos , Difração de Raios X/métodos , Zearalenona/química
3.
Bioorg Med Chem Lett ; 22(1): 743-6, 2012 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-22137847

RESUMO

This study has achieved the design and diversity-oriented synthesis of novel 1,4-thiazepine derivatives embedded with carbazole, pyrazole or isoxazole motif via microwave-assisted multicomponent reactions under solvent-free condition, thus providing a green and facile access to 1,4-thiazepine derivatives with prominent features of high structural diversity, short reaction time, high yields and environmental friendliness. More importantly, these novel compounds have been subjected to the test of in vitro antioxidant and cytotoxic activities, resulting in the finding that these 1,4-thiazepine derivatives not only have significant antioxidant activity, but also exhibit remarkably selective cytotoxicity to carcinoma cell line HCT 116.


Assuntos
Antioxidantes/farmacologia , Química Farmacêutica/métodos , Tiazepinas/síntese química , Antineoplásicos/farmacologia , Carbazóis/química , Linhagem Celular Tumoral , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Células HCT116 , Humanos , Micro-Ondas , Modelos Químicos , Pirazóis/química , Solventes , Temperatura , Tiazepinas/farmacologia
4.
Yao Xue Xue Bao ; 42(7): 750-6, 2007 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-17882960

RESUMO

Sterols are one of the active classes of compounds in Inonotus obliquus for their effective therapy of many diseases. In field environment, this fungus accumulates large amount of sterols. In cultured mycelia, however, this class of compounds is less accumulated. For analyzing the factors responsible for differing sterol composition, the field-grown and cultured mycelia were extracted with 80% ethanol at room temperature and total sterols were prepared using silicon gel column chromatography followed by identification using either GC-MS or spectroscopic methods. For culturing Inonotus obliquus, the seed culture was grown either in basic medium consisting of glucose (2%), yeast extract (0.5%), KH2PO4 (0.01%), MgSO4.7H20 (0.05%) and distilled water at pH 6.5, or the basic medium supplemented with serial concentrations of AgNO3. The results indicated that field-grown mycelia contained lanosterol and inotodiol (comprised 45. 47% and 25. 36% of the total sterols, respectively) and other 10 sterols (comprising the remaining 30.17%) including ergosterol biosynthetic intermediates such as 24-methylene dihydrolanosterol, 4,4-dimethylfecosterol, 4-methyl fecosterol, fecosterol and episterol. Column chromatography also led to the isolation of lanosterol, Inotodiol, trametenolic acid, foscoparianol B and a new triterpenoid foscoparianol D in field-grown mycelia. In comparison, the cultured mycelia only contained three sterols with ergosterol as the predominant one (82.20%). Lanosterol only accounted for 3.68%. Supplementing Ag+ into the culture at 0.28 micromol x L(-1) greatly enhanced content of lanosterol (accounting for 56.81%) and decreased the content of ergosterol (18.5%) together with the presence of intermediates for ergosterol biosynthesis. These results suggested that the sterol composition in mycelia of the fungus can be diversified by supplementing substances inhibiting enzymatic process towards the synthesis of ergosterol. Harsh growth conditions in field environment (i.e. temperature variation, UV irradiation etc.) can delay the synthesis of ergosterol and hereby diversify the sterol composition in the mycelia of Inonotus obliquus.


Assuntos
Basidiomycota/química , Ergosterol/biossíntese , Lanosterol/biossíntese , Nitrato de Prata/farmacologia , Basidiomycota/crescimento & desenvolvimento , Meios de Cultura/farmacologia , Técnicas de Cultura , Cromatografia Gasosa-Espectrometria de Massas , Lanosterol/análogos & derivados , Micélio/química
5.
Yao Xue Xue Bao ; 40(5): 438-42, 2005 May.
Artigo em Inglês | MEDLINE | ID: mdl-16220789

RESUMO

AIM: To investigate the chemical constituents of the secondary metabolites of the roots of Daphne genkwa. METHODS: The roots of D. genkwa were extracted with 95% ethanol at 60-70 degrees C for 7 days to obtain the crude extract. The crude extract was purified by silica gel and Sephadex LH-20 column chromatography as well as the HPLC techniques. The structures of the isolates were elucidated by combined spectroscopic methods including 1D and 2D NMR, MS, UV, IR and CD. RESULTS: Three new biflavonoids were isolated from the ethanol extract of the roots of D. genkwa and their structures were identified as daphnodorin H-3-methyl ether (1), daphnodorin H-3"-methyl ether (2) and daphnodorin G-3"-methyl ether (3). CONCLUSION: Compounds 1, 2 and 3 are three new biflavonoids.


Assuntos
Biflavonoides/isolamento & purificação , Daphne/química , Plantas Medicinais/química , Biflavonoides/química , Etanol , Conformação Molecular , Estrutura Molecular , Raízes de Plantas/química
6.
Pharmacol Biochem Behav ; 79(4): 651-9, 2004 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-15582673

RESUMO

There is evidence that the excessive generation of reactive oxygen free radicals contributes to the brain injury associated with cerebral ischemia. In the present study, the protective effect of chronic administration of ethyl docosahexaenoate (E-DHA) against oxidative brain injury was evaluated in the gerbil model of transient cerebral ischemia. Weanling male gerbils were orally pretreated with either E-DHA (200 mg/kg) or vehicle, once a day, for 10 weeks and subjected to bilateral occlusion of common carotid arteries for 10 min. At the different reperfusion times, E-DHA pretreatment significantly inhibited the increases in the production of brain salicylate-derived 2,5-dihydroxybenzoic acid (2,5-DHBA) and content of brain malonildialdehyde (MDA). The superoxide dismutase (SOD) activity was not modified; however, pretreatment with E-DHA significantly prevented the level of brain-reduced glutathione (GSH) and activities of brain glutathione peroxidase (GSH-P(X)) and catalase (CAT) from declines caused by cerebral ischemia. Moreover, ischemia and reperfusion-induced delayed neuronal loss in the hippocampus CA1 sector and locomotor hyperactivity were also significantly attenuated by pretreatment with E-DHA. These results suggested that the neuroprotective effect of E-DHA might be due to its antioxidant property.


Assuntos
Isquemia Encefálica/tratamento farmacológico , Ácidos Docosa-Hexaenoicos/administração & dosagem , Fármacos Neuroprotetores/administração & dosagem , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Isquemia Encefálica/metabolismo , Radicais Livres/metabolismo , Gerbillinae , Masculino , Atividade Motora/efeitos dos fármacos , Atividade Motora/fisiologia
7.
Yao Xue Xue Bao ; 39(12): 990-2, 2004 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-15813027

RESUMO

AIM: To investigate the chemical constituents of the roots of Daphne genkwa. METHODS: Silica gel and Sephadex LH-20 column chromatographic techniques were employed for the isolation and purification. The structure was elucidated by a combination of spectroscopic analyses. RESULTS: A new dicoumarin named isodaphnoretin was isolated and the structure was established as 7-hydroxy-6-methoxy-4-[(2-oxo-2H-1-benzopyran-7-yl)-oxyl]-2H-1-benzopyran-2-one. CONCLUSION: Isodaphnoretin is a new compound.


Assuntos
Cumarínicos/isolamento & purificação , Daphne/química , Plantas Medicinais/química , Cumarínicos/química , Conformação Molecular , Estrutura Molecular , Raízes de Plantas/química
8.
Guang Pu Xue Yu Guang Pu Fen Xi ; 24(1): 111-3, 2004 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-15768991

RESUMO

The interaction of berberine and Human Serum Albumin (HSA) has been studied by fluorescence and UV-Vis absorption spectroscopy. With fluorescence quenching method, the binding constant K was found to be 1.168 x 10(5) L x mol(-1) and the number of binding site n was 5.26. The binding distance (R = 3.44 nm) and energy transfer efficiency (E = 0.303) were also obtained according to Förster's non-radiation energy transfer theory. The energy transfer path between tyrosine residual and tryptophan residual was cut by berberine in the site of HSA and weak fluorescence berberine-HSA complex was also observed.


Assuntos
Berberina/farmacocinética , Sítios de Ligação/efeitos dos fármacos , Transferência de Energia/efeitos dos fármacos , Fluorescência , Albumina Sérica/metabolismo , Berberina/farmacologia , Interações Medicamentosas , Humanos , Modelos Químicos , Albumina Sérica/química , Triptofano/metabolismo , Tirosina/metabolismo
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