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1.
Pharmaceuticals (Basel) ; 14(7)2021 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-34358079

RESUMO

Euphorbia usambarica is a traditional medicine used for gynecologic, endocrine, and urogenital illnesses in East Africa; however, its constituents and bioactivities have not been investigated. A variety of compounds isolated from Euphorbia species have been shown to have activity against latent HIV-1, the major source of HIV-1 persistence despite antiretroviral therapy. We performed bioactivity-guided isolation to identify 15 new diterpenoids (1-9, 14-17, 19, and 20) along with 16 known compounds from E. usambarica with HIV-1 latency reversal activity. Euphordraculoate C (1) exhibits a rare 6/6/3-fused ring system with a 2-methyl-2-cyclopentenone moiety. Usambariphanes A (2) and B (3) display an unusual lactone ring constructed between C-17 and C-2 in the jatrophane structure. 4ß-Crotignoid K (14) revealed a 250-fold improvement in latency reversal activity compared to crotignoid K (13), identifying that configuration at the C-4 of tigliane diterpenoids is critical to HIV-1 latency reversal activity. The primary mechanism of the active diterpenoids 12-14 and 21 for the HIV-1 latency reversal activity was activation of PKC, while lignans 26 and 27 that did not increase CD69 expression, suggesting a non-PKC mechanism. Accordingly, natural constituents from E. usambarica have the potential to contribute to the development of HIV-1 eradication strategies.

2.
Int J Mol Sci ; 22(14)2021 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-34298911

RESUMO

Osteoarthritis (OA) is the most common articular degenerative disease characterized by chronic pain, joint inflammation, and movement limitations, which are significantly influenced by aberrant epigenetic modifications of numerous OA-susceptible genes. Recent studies revealed that both the abnormal activation and differential expression of histone deacetylases (HDACs) might contribute to OA pathogenesis. In this study, we investigated the chondroprotective effects of a marine-derived HDAC inhibitor, panobinostat, on anterior cruciate ligament transection (ACLT)-induced experimental OA rats. The intra-articular administration of 2 or 10 µg of panobinostat (each group, n = 7) per week from the 6th to 17th week attenuates ACLT-induced nociceptive behaviors, including secondary mechanical allodynia and weight-bearing distribution. Histopathological and microcomputed tomography analysis showed that panobinostat significantly prevents cartilage degeneration after ACLT. Moreover, intra-articular panobinostat exerts hypertrophic effects in the chondrocytes of articular cartilage by regulating the protein expressions of HDAC4, HDAC6, HDAC7, runt-domain transcription factor-2, and matrix metalloproteinase-13. The study indicated that HDACs might have different modulations on the chondrocyte phenotype in the early stages of OA development. These results provide new evidence that panobinostat may be a potential therapeutic drug for OA.


Assuntos
Ligamento Cruzado Anterior/efeitos dos fármacos , Cartilagem Articular/efeitos dos fármacos , Condrócitos/efeitos dos fármacos , Inibidores de Histona Desacetilases/farmacologia , Osteoartrite do Joelho/tratamento farmacológico , Dor/tratamento farmacológico , Panobinostat/farmacologia , Animais , Ligamento Cruzado Anterior/metabolismo , Lesões do Ligamento Cruzado Anterior/tratamento farmacológico , Lesões do Ligamento Cruzado Anterior/metabolismo , Doenças das Cartilagens/tratamento farmacológico , Doenças das Cartilagens/metabolismo , Cartilagem Articular/metabolismo , Condrócitos/metabolismo , Modelos Animais de Doenças , Masculino , Osteoartrite do Joelho/metabolismo , Dor/metabolismo , Ratos , Ratos Wistar , Suporte de Carga
3.
Z Naturforsch C J Biosci ; 76(1-2): 43-47, 2021 Jan 27.
Artigo em Inglês | MEDLINE | ID: mdl-32681789

RESUMO

Eremurus persicus (Jaub. & Spach) Boiss. belonging to Xanthorrhoeaceae family is an endemic medicinal plant widely distributed in Iran. Its leaves have been traditionally used as a food and also as medicinal plant. Regarding the widespread application of E. persicus in Iranian folk medicine, and the insignificant investigation of its components, this study aimed at the isolation and identification of major secondary metabolites of this plant. By applying various chromatographic techniques, corchoionoside A (1), 4-amino-4-carboxychroman-2-one (2), isoorientin (3), ziganein 5-methyl ether (4), auraptene (5), and imperatorin (6) were isolated from the EtOAc and CHCl3 fractions of the crude extract. Except isoorientin (3), all the identified phytoconstituents were reported for the first time from Eremurus genus.

4.
Biomolecules ; 10(3)2020 02 27.
Artigo em Inglês | MEDLINE | ID: mdl-32120929

RESUMO

Strobilanthes cusia (Nees) Kuntze is a Chinese herbal medicine used in the treatment of respiratory virus infections. The methanol extract of S. cusia leaf contains chemical components such as ß-sitosterol, indirubin, tryptanthrin, betulin, indigodole A, and indigodole B that have diverse biological activities. However, the antiviral action of S. cusia leaf and its components against human coronavirus remains to be elucidated. Human coronavirus NL63 infection is frequent among immunocompromised individuals, young children, and in the elderly. This study investigated the anti-Human coronavirus NL63 (HCoV-NL63) activity of the methanol extract of S. cusia leaf and its major components. The methanol extract of S. cusia leaf effectively inhibited the cytopathic effect (CPE) and virus yield (IC50 = 0.64 µg/mL) in HCoV-NL63-infected cells. Moreover, this extract potently inhibited the HCoV-NL63 infection in a concentration-dependent manner. Among the six components identified in the methanol extract of S. cusia leaf, tryptanthrin and indigodole B (5aR-ethyltryptanthrin) exhibited potent antiviral activity in reducing the CPE and progeny virus production. The IC50 values against virus yield were 1.52 µM and 2.60 µM for tryptanthrin and indigodole B, respectively. Different modes of time-of-addition/removal assay indicated that tryptanthrin prevented the early and late stages of HCoV-NL63 replication, particularly by blocking viral RNA genome synthesis and papain-like protease 2 activity. Notably, tryptanthrin (IC50 = 0.06 µM) and indigodole B (IC50 = 2.09 µM) exhibited strong virucidal activity as well. This study identified tryptanthrin as the key active component of S. cusia leaf methanol extract that acted against HCoV-NL63 in a cell-type independent manner. The results specify that tryptanthrin possesses antiviral potential against HCoV-NL63 infection.


Assuntos
Acanthaceae/química , Antivirais/farmacologia , Coronavirus Humano NL63/fisiologia , Quinazolinas/farmacologia , Internalização do Vírus/efeitos dos fármacos , Acanthaceae/metabolismo , Animais , Antivirais/química , Antivirais/isolamento & purificação , Antivirais/uso terapêutico , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Infecções por Coronavirus/tratamento farmacológico , Infecções por Coronavirus/virologia , Coronavirus Humano NL63/isolamento & purificação , Humanos , Macaca mulatta , Medicina Tradicional Chinesa , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Folhas de Planta/metabolismo , Quinazolinas/química , Quinazolinas/isolamento & purificação , Quinazolinas/uso terapêutico
5.
J Ethnopharmacol ; 250: 112493, 2020 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-31863859

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Lindernia crustacea (L.) F.Muell. (Scrophulariaceae) was selected for phytochemical investigation owing to its traditional use against human herpes virus infection and its anti-Epstein-Barr virus (EBV) effect. AIMS OF THE STUDY: The present study focused on the phytochemical investigation of L. crustacea including the isolation and structure determination of its biologically active compounds. Compounds with anti-EBV effects were also investigated. MATERIALS AND METHODS: The EtOH extract of L. crustacea was subsequently partitioned using different solvents. The EtOAc fraction was subjected to several chromatographic methods to obtain pure compounds. The structures of all isolates were established by spectroscopic analysis and compared with previously reported physical data. The anti-EBV effect was evaluated in an EBV-containing Burkitt's lymphoma cell line (P3HR1) to study the expression of EBV lytic proteins. RESULTS: Thirty-three compounds, including one diterpene (1), four anthraquinones (2-5), two ionones (6 and 7), fourteen phenylpropanoid glycosides (8-21), five flavonoids (22-26), one lignan glycoside (27), one phenethyl alcohol glycoside (28), one phenylpropene glycoside (29), one glucosyl glycerol derivative (30), one furanone (31), and two cinnamic acid derivatives (32 and 33), were isolated from the ethanolic extract of the plant. All isolated compounds were obtained for the first time from Lindernia sp. The evaluation of the anti-EBV activity of L. crustacea crude extract, partitioned fractions, and constituents was performed for the first time. Phytol (1), aloe-emodin (2), byzantionoside B (7), a mixture of trans-martynoside (8) and cis-martynoside (9), a mixture of trans-isomartynoside (10) and cis-isomartynoside (11), luteolin-7-O-ß-D-glucopyranoside (24), and apigenin-7-O-[ß-D-apiofuranosyl (1→6)-ß-D-glucopyranoside] (25) exhibited significant inhibitory effects on the EBV lytic cycle at 20 µg/mL in the immunoblot analysis. On the other hand, (6R,7E,9R)-3-oxo-α-ionol-ß-D-glucopyranoside (6) and a mixture of trans-dolichandroside A (12) and cis-dolichandroside A (13) showed moderate anti-EBV activity at 20 µg/mL. CONCLUSIONS: L. crustacea and its active isolates could be developed as potential candidates against EBV. Our findings provide scientific evidence for the traditional use of L. crustacea for its antiviral effects.


Assuntos
Antivirais/farmacologia , Herpesvirus Humano 4/efeitos dos fármacos , Extratos Vegetais/farmacologia , Scrophulariaceae/química , Antivirais/isolamento & purificação , Linfoma de Burkitt/virologia , Linhagem Celular , Humanos , Proteínas Imediatamente Precoces/genética , Transativadores/genética
6.
Bioorg Med Chem Lett ; 29(23): 126742, 2019 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-31648857

RESUMO

Japanese encephalitis virus (JEV), a mosquito-borne flavivirus, occasionally causes severe central nervous system disorders in the risk zone where more than 3 billion people reside. Our prior studies demonstrated antiviral potential of 4,5-dihydrofuran-3-carboxylate compound CW-33 (ethyl 2-(3',5'-dimethylanilino)-4-oxo-4,5-dihydrofuran-3-carboxylate) and its derivative CW-33A ((ethyl 2-(2-fluoroanilino)-4-oxo-4,5-dihydrofuran-3-carboxylate) against JEV infection ((Int. J. Mol. Sci. 2016, 17: E1386; Sci. Rep. 2018, 8: 16595). This study synthesized six new CW-33 derivatives containing chloro, or bromo groups at the C-2, C-3, or C-4 of anilino ring of CW-33, and assessed the antiviral activity and mechanisms of these chloro- and bromo-anilino substitutedderivatives. CW-33K, CW-33L and CW-33M had the bromo-substituents at the C-2, C-3, or C-4 of anilino ring of CW-33, respectively, showing the higher anti-JEV activity than CW-33 and other derivatives. CW-33K (ethyl 2-(2-bromoanilino)-4-oxo-4,5-dihydrofuran-3-carboxylate) exhibited the highest antiviral efficacy and therapeutic index. The IC50 value of CW-33K was less than 5 µM for reducing JEV-induced cytopathic effect, virus infectivity and virus yield. CW-33K significantly inhibited the JEV replication at the early and late stages, suppressing viral RNA synthesis and intracellular JEV particle production. The study demonstrated that the CW-33 derivative with a bromosubstitutionat the C-2 anilino ring improved the antiviral activity JEV, providing the structure-antiviral activity relationship for the development of anti-JEV agents.


Assuntos
Antivirais/uso terapêutico , Efeito Citopatogênico Viral/efeitos dos fármacos , Vírus da Encefalite Japonesa (Espécie)/efeitos dos fármacos , Antivirais/farmacologia , Humanos
7.
Virus Res ; 273: 197767, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31560964

RESUMO

Human coronavirus NL63 (HCoV-NL63), one of the main circulating HCoVs worldwide, causes respiratory tract illnesses like runny nose, cough, bronchiolitis and pneumonia. Recently, a severe respiratory illness outbreak of HCoV-NL63 has been reported in a long-term care facility. Sambucus FormosanaNakai, a species of elderberry, is a traditional medicinal herb with anti-inflammatory and antiviral potential. The study investigated the antiviral activity of Sambucus FormosanaNakai stem ethanol extract and some phenolic acid constituents against HCoV-NL63. The extract was less cytotoxic and concentration-dependently increased anti-HCoV-NL63 activities, including cytopathicity, sub-G1 fraction, virus yield (IC50 = 1.17 µg/ml), plaque formation (IC50 = 4.67 µg/ml) and virus attachment (IC50 = 15.75 µg/ml). Among the phenolic acid constituents in Sambucus FormosanaNakai extract, caffeic acid, chlorogenic acid and gallic acid sustained the anti-HCoV-NL63 activity that was ranked in the following order of virus yield reduction: caffeic acid (IC50 = 3.54 µM) > chlorogenic acid (IC50 = 43.45 µM) > coumaric acid (IC50 = 71.48 µM). Caffeic acid significantly inhibited the replication of HCoV-NL63 in a cell-type independent manner, and specifically blocked virus attachment (IC50 = 8.1 µM). Therefore, the results revealed that Sambucus Formosana Nakai stem ethanol extract displayed the strong anti-HCoV-NL63 potential; caffeic acid could be the vital component with anti-HCoV-NL63 activity. The finding could be helpful for developing antivirals against HCoV-NL63.


Assuntos
Antivirais/farmacologia , Coronavirus Humano NL63/efeitos dos fármacos , Células Epiteliais/efeitos dos fármacos , Hidroxibenzoatos/farmacologia , Extratos Vegetais/farmacologia , Sambucus/química , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Infecções por Coronavirus , Células Epiteliais/virologia , Humanos , Hidroxibenzoatos/química , Concentração Inibidora 50 , Rim/citologia , Rim/virologia , Macaca mulatta , Extratos Vegetais/química , Caules de Planta/química , Sistema Respiratório/citologia , Sistema Respiratório/virologia , Ligação Viral/efeitos dos fármacos
8.
Artigo em Inglês | MEDLINE | ID: mdl-28419924

RESUMO

Phytoecdysteroids are known for their various beneficial bioactivities in mammals including a non-hormonal anabolic and adaptogenic effect. Cyanotis arachnoidea extracts are extensively utilized worldwide as ecdysteroid-rich materials for various purposes, e.g. food supplementation, use in agriculture and aquaculture, etc. Preparative chromatography of ecdysteroids requires extensive use of methods of different selectivity, and only a very limited number of papers are available on related application of modern liquid-liquid chromatographic techniques. In this work, a centrifugal partition chromatography (CPC) method was developed for the isolation of two minor ecdysteroids, dacryhainansterone and calonysterone, from a pre-purified commercial extract of Cyanotis arachnoidea. The biphasic solvent system was optimized by HPLC, and was composed of n-hexane - ethyl acetate - methanol - water (1:5:1:5, v/v/v/v). The isolated dacryhainansterone and calonysterone represented 99.1% and 99.7% purity, respectively. Calonysterone exerts a stronger effect on the protein kinase B (Akt) phosphorylation in mammalian skeletal muscle cells than the abundant 20-hydroxyecdysone, while no related data are available on dacryhainansterone. Despite their presence in food supplements, neither compound has appropriately been assessed for safety and efficacy. The reported method allows the gram scale isolation of these compounds, opening ways to their in-depth pharmacological investigation.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Commelinaceae/química , Ecdisteroides/isolamento & purificação , Extratos Vegetais/química , Acetatos/química , Centrifugação/métodos , Cromatografia de Fase Reversa/métodos , Ecdisteroides/análise , Hexanos/química , Metanol/química , Solventes/química
9.
Nat Prod Commun ; 11(8): 1099-1102, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30725567

RESUMO

Utilizing the pER8:GUS transgenic plant bioassay system to monitor estrogenic activity-guided fractionation, one new constituent, erycaffrain A, together with I known compounds were isolated from the ethanolic extract of Erythrina caffra. The structures of the isolated compounds were identified in combination with spectroscopic analyses. This is the first study reporting the estrogenic activity of E. caffra. The new compound exhibited as a SREM, but.also showed both estrogenic and anti-estrogenic activities in the MCF-7 cancer cell model. Several known phytoestrogens in this plant also revealed possible new functions for E. caffra stem.


Assuntos
Erythrina/química , Antagonistas de Estrogênios/química , Estrogênios/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Antagonistas de Estrogênios/farmacologia , Estrogênios/farmacologia , Genes Reporter , Humanos , Células MCF-7 , Estrutura Molecular , Plantas Geneticamente Modificadas
10.
J Nat Prod ; 78(10): 2346-54, 2015 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-26461164

RESUMO

Pandanus amaryllifolius Roxb. (Pandanaceae) is used as a flavor and in folk medicine in Southeast Asia. The ethanolic crude extract of the aerial parts of P. amaryllifolius exhibited antioxidant, antibiofilm, and anti-inflammatory activities in previous studies. In the current investigation, the purification of the ethanolic extract yielded nine new compounds, including N-acetylnorpandamarilactonines A (1) and B (2); pandalizines A (3) and B (4); pandanmenyamine (5); pandamarilactones 2 (6) and 3 (7), and 5(E)-pandamarilactonine-32 (8); and pandalactonine (9). The isolated alkaloids, with either a γ-alkylidene-α,ß-unsaturated-γ-lactone or γ-alkylidene-α,ß-unsaturated-γ-lactam system, can be classified into five skeletons including norpandamarilactonine, indolizinone, pandanamine, pandamarilactone, and pandamarilactonine. A plausible biosynthetic route toward 1-5, 7, and 9 is proposed.


Assuntos
Alcaloides/isolamento & purificação , Alcaloides/metabolismo , Pandanaceae/química , Alcaloides/química , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/metabolismo , Furanos/química , Furanos/isolamento & purificação , Furanos/metabolismo , Lactonas/química , Lactonas/isolamento & purificação , Lactonas/metabolismo , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Componentes Aéreos da Planta/química , Folhas de Planta/química , Pirrolidinas/química , Pirrolidinas/isolamento & purificação , Pirrolidinas/metabolismo , Estereoisomerismo , Taiwan
11.
Bioorg Med Chem Lett ; 25(19): 4333-6, 2015 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-26277406

RESUMO

Two novel alkaloids named pandalisines A (1) and B (2), constituting a new class of C8-substituted indolizidine moiety, were isolated from the leaves of Pandanus utilis. The structures of these new compounds were established by their mass and spectroscopic data. The absolute configuration was determined by the comparison of experimental CD and calculated ECD spectra. A plausible biosynthetic pathway for compounds 1 and 2 is advanced. The cytotoxic activities of the isolated alkaloids against A-549, Hep-G2, and MDA-MB-231 cancer cell lines were evaluated. The result showed that 1 and 2 are the first non-cytotoxic indolizidine alkaloids.


Assuntos
Indolizidinas/química , Pandanaceae/química , Folhas de Planta/química , Linhagem Celular Tumoral , Células Hep G2 , Humanos , Indolizidinas/isolamento & purificação , Estrutura Molecular
12.
Molecules ; 20(4): 6844-55, 2015 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-25913925

RESUMO

One new benzofuran, (2R)-(2',4'-dihydroxybenzyl)-6,7-methylenedioxy-2,3-dihydrobenzofuran (1), one new phenylisocoumarin, 3-(2'-hydroxyphenyl)-6,8-dihydroxy-7-methoxy-isocoumarin (2), and one new benzofuroisocoumarin, platyphyllarin C (3), were isolated from the ethanolic extract of Liriope platyphylla aerial parts, along with seventeen known compounds. The structures of the isolates were established by spectroscopic analysis and comparison with the literature data. The results indicated that structures 1-3 are uncommon in Nature. Benzofuroisocoumarin 4, flavonoids 9, 10, and 13-15, and homoisoflavonoids 19 and 20 exhibited significant binding activity to estrogen-receptor α and/or ß as demonstrated by the SEAP reporter assay system in an MCF-7 cell-line.


Assuntos
Estrogênios/farmacologia , Liriope (Planta)/química , Compostos Fitoquímicos/química , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Cromanos/química , Cromanos/isolamento & purificação , Cromanos/farmacologia , Receptor alfa de Estrogênio/metabolismo , Receptor beta de Estrogênio/metabolismo , Estrogênios/química , Estrogênios/isolamento & purificação , Humanos , Isocumarinas/química , Isocumarinas/isolamento & purificação , Isocumarinas/farmacologia , Células MCF-7 , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia
13.
Chem Res Toxicol ; 28(5): 897-906, 2015 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-25856345

RESUMO

Numerous breast cancer patients who achieve an initial response to HER-targeted therapy rapidly develop resistance within one year, leading to treatment failure. Observations from clinical samples indicate that such resistance correlates with an increase in Src, EGFR, and PI3K/Akt activities and a decrease in PTEN activity. Furthermore, Akt survival signaling activation is also found in tumors treated by toxic chemotherapeutic agents. Because cotreatment with a PI3K inhibitor is a promising strategy to delay acquired resistance by preventing secondary gene activation, we therefore investigated the effects of a newly identified compound, (-)-Liriopein B (LB), on PI3K/Akt signaling activity in breast cancer cells. Our results showed that nontoxic doses of LB are able to inhibit AKT activation in both luminal-like MCF-7 and basal-like MDA-MB-231 breast cancer cells. Low doses of LB also inhibited cell migration, invasion, and cancer-stem cell sphere formation. Suppression of EGF-induced EGFR and ERK1/2 activation by LB might contribute in part to retardation of cancer progression. Furthermore, LB increases sensitivity of MDA-MB-231 cells to gefitinib in vitro, suggesting that EGFR may not be the only target of LB. Finally, a small scale in vitro kinase assay screen demonstrated that LB has a potent inhibitory effect on multiple kinases, including PI3K, Src, EGFR, Tie2, lck, lyn, RTK5, FGFR1, Abl, and Flt. In conclusion, this study demonstrates for the first time that the compound LB improves tumor therapeutic efficacy and suggests LB as a promising candidate for studying new leads in the development of kinase inhibitors.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Mama/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas de Plantas/farmacologia , Inibidores de Proteínas Quinases/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Mama/metabolismo , Mama/patologia , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Receptores ErbB/metabolismo , Feminino , Humanos , Liriope (Planta)/química , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Proteínas de Plantas/química , Proteínas de Plantas/isolamento & purificação , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/isolamento & purificação
14.
Virus Res ; 192: 16-24, 2014 Nov 04.
Artigo em Inglês | MEDLINE | ID: mdl-25150190

RESUMO

The compound LPRP-Et-97543 was isolated from Liriope platyphylla roots and was observed to have potential anti-viral effects in HepG2.2.15 cells against hepatitis B virus (HBV). The antiviral mode was further clarified, and the HBV-transfected Huh7 cells were used as the platform. During viral gene expression, LPRP-Et-97543 treatment had apparent effects on the viral precore/pregenomic and S/preS RNA. Promoter activity analysis demonstrated that LPRP-Et-97543 significantly reduced Core, S, and preS but not X promoter activities. Further examination showed that putative signaling pathways were involved in this inhibitory effect, indicating that NF-κB may serve a putative mediator of HBV gene regulation with LPRP-Et-97543. In addition, the nuclear expression of p65/p50 NF-κB member proteins was attenuated with LPRP-Et-97543 and augmented cytoplasmic IκBα protein levels but without affecting the expression of these proteins in HBV non-transfected cells during treatment. Moreover, LPRP-Et-97543 reduced the binding activity of NF-κB protein to CS1 element of HBV surface gene in a gel retardation analysis and inhibited CS1 containing promoter activity in HBV expressed cells. However, HBV transfection significantly enhances CS1 containing promoter activity without compound treatment in cells. Finally, transfection of the p65 expression plasmid significantly reversed the inhibitory effect of LPRP-Et-97543 on the replicated HBV DNA level in HBV positive cells. In conclusion, this study suggests that the mechanism of HBV inhibition by LPRP-Et-97543 may involve the feedback regulation of viral gene expression and viral DNA replication by HBV viral proteins, which interferes with the NF-κB signaling pathway.


Assuntos
Antivirais/farmacologia , Regulação Viral da Expressão Gênica/efeitos dos fármacos , Vírus da Hepatite B/efeitos dos fármacos , Vírus da Hepatite B/fisiologia , Liliaceae/química , Extratos Vegetais/farmacologia , Replicação Viral/efeitos dos fármacos , Antivirais/isolamento & purificação , Linhagem Celular , Humanos , Extratos Vegetais/isolamento & purificação
15.
J Nat Prod ; 77(7): 1624-31, 2014 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-25025240

RESUMO

Cirsium japonicum var. australe, used as a folk medicine in Taiwan, has been employed traditionally in the treatment of diabetes and inflammatory symptoms. Bioactivity-guided fractionation of its ethanolic extract, utilizing centrifugal partition chromatography monitored by DPPH-TLC analysis, led to the isolation of three new acetylenic phenylacrylic acid esters (1-3) and two new polyacetylenes (4 and 5), together with seven known compounds (6-12). The structures of 1-5 were elucidated by spectroscopic methods including 1D and 2D NMR techniques. The absolute configurations of 4 and 7 were determined utilizing Mosher's method and ECD/CD experiments. The DPPH scavenging activity of the constituents isolated from the C. japonicum var. australe ethanolic extract was evaluated. The potential antidiabetic activity of some of the isolates was evaluated using in vitro cellular glucose uptake and oil red staining assays.


Assuntos
Cirsium/química , Poli-Inos/isolamento & purificação , Poli-Inos/farmacologia , Anti-Inflamatórios/uso terapêutico , Compostos Azo , Compostos de Bifenilo/farmacologia , Diabetes Mellitus/tratamento farmacológico , Glucose/metabolismo , Medicina Tradicional , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Picratos/farmacologia , Poli-Inos/química , Taiwan
16.
Res Dev Disabil ; 34(11): 3654-9, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24012594

RESUMO

This study assessed the possibility of rehabilitating two adolescents with cerebral palsy (CP) using a Kinect-based system in a public school setting. The system provided 3 degrees of freedom for prescribing a rehabilitation program to achieve customized treatment. This study was carried out according to an ABAB reversal replication design in which A represented the baseline and B represented intervention phases. Data showed that the two participants significantly increased their motivation for upper limb rehabilitation, thus improving exercise performance during the intervention phases. Practical and developmental implications of the findings are discussed.


Assuntos
Braço/fisiologia , Paralisia Cerebral/reabilitação , Modalidades de Fisioterapia , Amplitude de Movimento Articular/fisiologia , Terapia Assistida por Computador/métodos , Jogos de Vídeo , Adolescente , Paralisia Cerebral/fisiopatologia , Paralisia Cerebral/psicologia , Feminino , Humanos , Motivação , Modalidades de Fisioterapia/psicologia , Resultado do Tratamento , Jogos de Vídeo/psicologia
17.
Artigo em Inglês | MEDLINE | ID: mdl-23762164

RESUMO

Liriope spicata is a well-known herb in traditional Chinese medicine, and its root has been clinically demonstrated to be effective in the treatment of metabolic and neural disorders. The constituents isolated from Liriope have also recently been shown to possess anticancer activity, although the mechanism of which remains largely unknown. Here, we illustrate the anticancer activity of LPRP-9, one of the active fractions we fractionated from the Liriope platyphylla root part (LPRP) extract. Treatment with LPRP-9 significantly inhibited proliferation of cancer cell lines MCF-7 and Huh-7 and down-regulated the phosphorylation of AKT. LPRP-9 also activates the stress-activated MPAK, JNK, p38 pathways, the p53 cell-cycle checkpoint pathway, and a series of caspase cascades while downregulating expression of antiapoptotic factors Bcl-2, Bcl-XL, and survivin. Such activities strongly suggest a role for LPRP-9 in apoptosis and autophagy. We further purified and identified the compound (-)-Liriopein B from LPRP-9, which is capable of inhibiting AKT phosphorylation at low concentration. The overall result highlights the anticancer property of LPRP-9, suggests its mechanism for inhibition of proliferation and promotion of cell death for cancer cells via regulation of multitarget pathways, and denotes the importance of purifying components of fraction LPRP-9 to aid cancer therapy.

18.
Org Biomol Chem ; 11(22): 3742-55, 2013 Jun 14.
Artigo em Inglês | MEDLINE | ID: mdl-23629449

RESUMO

Our previous studies identified an Fmoc-(S,R)-tryptophan-containing dipeptide derivative, 1, which selectively inhibited neutrophil elastase release induced by formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP) in human neutrophils. In an attempt to improve pharmacological activity, a series of tryptophan-containing dipeptides were synthesized and their pharmacological activities were investigated in human neutrophils. Of these, five compounds 3, 6, 19a, 24a, and 24b exhibited potent and dual inhibitory effects on FMLP-induced superoxide anion (O2˙(-)) generation and neutrophil elastase release in neutrophils with IC50 values of 0.23/0.60, 1.88/2.47, 1.87/3.60, 0.12/0.37, and 1.32/1.03 µM, respectively. Further studies indicated that inhibition of superoxide production in human neutrophils by these dipeptides was associated with the selective inhibition of formyl peptide receptor 1 (FPR1). Furthermore, the results of structure-activity relationship studies concluded that the fragment N-benzoyl-Trp-Phe-OMe (3) was most suitable as a core structure for interaction with FPR1, and may be approved as a lead for the development of new drugs in the treatment of neutrophilic inflammatory diseases. As some of the synthesized compounds exhibited separable conformational isomers, and showed diverse bioactivities, the conformation analysis of these compounds is also discussed herein.


Assuntos
Dipeptídeos/química , Dipeptídeos/farmacologia , Receptores de Formil Peptídeo/antagonistas & inibidores , Triptofano/análogos & derivados , Triptofano/farmacologia , Adulto , Dipeptídeos/síntese química , Desenho de Fármacos , Humanos , N-Formilmetionina Leucil-Fenilalanina/metabolismo , Neutrófilos/efeitos dos fármacos , Neutrófilos/metabolismo , Elastase Pancreática/metabolismo , Receptores de Formil Peptídeo/metabolismo , Superóxidos/metabolismo , Triptofano/síntese química , Adulto Jovem
19.
Food Chem ; 140(1-2): 305-14, 2013 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-23578647

RESUMO

The ethanolic extract of Liriope platyphylla (Liliaceae) roots showed potential oestrogenic and anti-platelet activities. Twenty-six compounds were isolated and classified as 10 skeletons, including two unusual new dihydrobenzofuroisocoumarins, (+)-platyphyllarin A (1) and B (2), one new butanoate, ethyltributanoate (3), and two new homoisoflavanones, (-)-liriopein A (4) and B (5), along with 21 known compounds, including six homoisoflavonoids, one chalcone, six amides, one lignan, one fatty acid derivative, one alkaloid, three benzenoids, and two steroids. The biosynthetic pathway of compounds 1 and 2 was proposed in the current investigation. The oestrogenic activity of the isolates was evaluated utilising the pER8:GUS reporter assay system in transgenic Arabidopsis plant as well as the SEAP reporter assay system in MCF-7 breast cancer cell-line; the anti-platelet activity was evaluated using the anti-platelet aggregation assay. Several components exhibited significant oestrogenic and anti-platelet activities; demonstrating for the first time the potential use of L. platyphylla as a nutritional supplement for cardiovascular and endocrine diseases.


Assuntos
Plaquetas/efeitos dos fármacos , Isoflavonas/farmacologia , Liliaceae/química , Liriope (Planta)/química , Extratos Vegetais/farmacologia , Plaquetas/fisiologia , Linhagem Celular Tumoral , Estrogênios/química , Humanos , Isoflavonas/química , Extratos Vegetais/química , Raízes de Plantas/química , Ativação Plaquetária/efeitos dos fármacos
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