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1.
Front Immunol ; 13: 913667, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35844610

RESUMO

Background: Antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis (AAV) is a multisystem autoimmune disease with small-vessel involvement. In AAV, microscopic polyangiitis (MPA) and granulomatosis with polyangiitis (GPA) are major clinicopathologic variants. In addition, myeloperoxidase (MPO) and proteinase 3 (PR3) are major target antigens. The objective of the study was to explore the predictive factors for long-term survival in AAV patients. Materials and Methods: A multicenter retrospective study was carried out on 407 patients between 2005 and 2020. Clinical parameters were obtained from laboratory tests including the ANCA types, antinuclear antibody (ANA), extractable nuclear antigen (ENA), anti-streptolysin O (ASO), glomerular filtration rate (GFR), and the laboratory examinations for the blood routine, liver function, renal function, and immunity, etc. The data for clinical parameters were collected from electronic medical records (EMRs), and the data for patient survival were acquired through regular follow-up. The association of clinical parameters with overall survival (OS) along with 3-year and 5-year survival rates was analyzed, and the nomogram as a predictive model was established according to the analysis results. Results: In the present study, 336 (82.6%) patients and 46 (11.3%) patients were diagnosed with MPA and GPA, respectively. The mean and median OS for all the patients were 2,285 and 2,290 days, respectively. The 1-year, 3-year, 5-year, and 10-year cumulative survival rates for all the patients were 84.2%, 76.3%, 57.2%, and 32.4%, respectively. Univariate and multivariate survival analyses indicated that the independent prognostic factors included age, pathological categories (MPA, GPA, and other types), serum ANCA types (negative or positive for MPO and/or PR3), ANA, ASO, GFR, lymphocyte, neutrophil-to-lymphocyte ratio (NLR), and C-reactive protein (CRP), and these clinical parameters except for ASO were used to construct a nomogram. The nomogram for 3-year and 5-year survival rates had a C-index of 0.721 (95% CI 0.676-0.766). The calibration curves showed that the predicted values of the nomogram for 3-year and 5-year survival rates were generally consistent with practical observed values, and decision curve analysis (DCA) further demonstrated the practicability and accuracy of the predictive model. Conclusion: Laboratory tests at diagnosis have great significance in the prediction of long-term survival in AAV patients.


Assuntos
Vasculite Associada a Anticorpo Anticitoplasma de Neutrófilos , Granulomatose com Poliangiite , Poliangiite Microscópica , Anticorpos Anticitoplasma de Neutrófilos , Humanos , Mieloblastina , Prognóstico , Estudos Retrospectivos
2.
Food Chem ; 374: 131716, 2022 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-34875434

RESUMO

Sanggenone C, oxyresveratrol, catechin and l-epicatechin exist in Morus and Hulless Barley as natural polyphenols with antityrosinase activity. Little research on their synergistic and structure-function relationships of them has been reported in recent years. In this paper, the inhibition mechanisms of these four plant polyphenols were investigated by enzyme kinetics, HPLC, fluorescence spectra, and molecular docking methods. The results showed that oxyresveratrol (IC50 = 1.096 ± 0.048 µg/mL), sanggenone C (IC50 = 13.360 ± 1.029 µg/mL), l-epicatechin (IC50 = 55.730 ± 1.762 µg/mL), and catechin (IC50 = 148.500 ± 3.355 µg/mL) exhibited tyrosinase inhibition activity. When sangenone C (14 µg/mL) was mixed with l-epicatechin (56 µg/mL) at 4:1 (40 µL + 10 µL), the highest tyrosinase inhibition was achieved. Molecular docking showed that the number and position of phenolic hydroxyls of polyphenols were the key for tyrosinase inhibition activity. This study provided new ideas for the application of these four plant polyphenols from Hulless Barley and Morus as tyrosinase inhibitors in food preservation.


Assuntos
Hordeum , Morus , Inibidores Enzimáticos , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase , Extratos Vegetais , Polifenóis
3.
J Innate Immun ; 12(4): 304-320, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31865314

RESUMO

Toll-like receptor 3 (TLR3) is a sensor of endogenous cell necrosis during the process of acute inflammation. Interleukin (IL)-1 receptor antagonist (IL-1Ra) is an anti-inflammatory cytokine and can negatively regulate the pathogenesis of inflammation. However, whether and how activation of TLR3 can regulate IL-1Ra expression has not been clarified. Here, we show that poly(I:C) induces IL-1Ra expression in primarily cultured human fibroblast-like synoviocytes and other types of cells. Induction of IL-1Ra by poly(I:C) was dependent on TLR3, but was independent of melanoma differentiation--associated protein 5 or retinoic acid-inducible gene I. Interferon regulatory factor 3 (IRF3) directly binds to the IL-1Ra promoter and promotes IL-1Ra expression in response to poly(I:C) stimulation. Induction of IL-1Ra by poly(I:C) was abolished by the inhibition of the NF-κB signaling, attenuated by the inhibition of the PI3K-Akt signaling, enhanced by inhibition of the ERK1/2 or MSK1/2 activation, but was independent of the p38 MAPK signaling. Treatment with poly(I:C) or Sendai virus elevated the levels of serum IL-1Ra in wild-type, but not in TLR3-/- or IRF3-/- mice. Our findings may provide new insights into the intrinsic anti-inflammatory function of TLR3 and double-stranded RNA-induced IL-Ra expression by TLR3 and its regulation.


Assuntos
Proteína Antagonista do Receptor de Interleucina 1/imunologia , Receptor 3 Toll-Like/imunologia , Animais , Linhagem Celular , Humanos , Inflamação/induzido quimicamente , Inflamação/genética , Inflamação/imunologia , Fator Regulador 3 de Interferon/genética , Proteína Antagonista do Receptor de Interleucina 1/genética , Camundongos , Camundongos Knockout , Poli I-C/farmacologia , Receptor 3 Toll-Like/genética
4.
J Cell Biochem ; 120(6): 9193-9202, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-30506723

RESUMO

Immunosuppressants have shown striking achievements in treating autoimmune diseases in recent years. It is urgent to develop more immunosuppressants to provide more options for patients. PO-296 [2-(6-chlorobenzo[d]oxazol-2-yl)-4,5,6,7-tetrahydro-2H-indazol-3-ol] was identified as a novel benzoxazole derivative. We observed that it exhibits an obvious immunosuppressive activity to T lymphocytes. PO-296 significantly inhibited the proliferation of activated human T lymphocyte without cytotoxicity. Moreover, PO-296 did not affect the expression of cluster of differentiation (CD)-25 or CD69 but induced T lymphocyte cycle arrest in the G0/G1 phase. Furthermore, PO-296 inhibited interleukin (IL)-6, IL-17, and interferon gamma expression but had no effect on IL-2, IL-4, or IL-10. Yet, importantly, PO-296 inhibited the phosphorylation of signal transducer and activator of transcription 5 (STAT5), increased the phosphorylation of p70S6K, but did not affect the phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt)/mitogen-activated protein kinase pathway. In conclusion, these findings indicate that PO-296 inhibits human activated T-lymphocyte proliferation by affecting the janus kinase 3 (JAK3)/STAT5 pathway. PO-296 possesses a potential lead compound for the design and development of new immunosuppressants for the treatment of autoimmune diseases.


Assuntos
Benzoxazóis/química , Benzoxazóis/farmacologia , Ativação Linfocitária/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Fator de Transcrição STAT5/metabolismo , Linfócitos T/efeitos dos fármacos , Linfócitos T/metabolismo , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Ensaio de Imunoadsorção Enzimática , Humanos , Interleucina-17/metabolismo , Interleucina-2/metabolismo , Interleucina-4/metabolismo , Interleucina-6/metabolismo , Linfócitos T/citologia
5.
Am J Cancer Res ; 8(3): 551-565, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29637008

RESUMO

Non-small-cell carcinoma (NSCLC) is one of the most lethal malignancies of lung cancers and its prognosis remains dismal due to the paucity of effective therapeutic targets. Recent reports show that Golgi membrane protein 1 (GOLM1) is highly expressed in a variety of tumor cells, functions as a negative regulator of T cells and then promotes tumor progression. However, its expression and role in NSCLC remain unclear. Herein, we showed that GOLM1 was markedly up-regulated in NSCLC cell lines and clinical tissues. Clinically, NSCLC patients with high expression of GOLM1 had shorter overall survival (OS) and high GOLM1 expression in tumor samples was significantly related to malignant phenotype, such as lymph node metastasis and high tumor stage. Ectopic expression of GOLM1 in NSCLC cells induced epithelial-to-mesenchymal transition (EMT) and promoted proliferation, migration, and invasion of NSCLC cells in vitro. Furthermore, GOLM1 overexpressing significantly promoted the tumorigenicity of NSCLC cells in vivo whereas silencing endogenous GOLM1 caused an opposite outcome. Moreover, we demonstrated that GOLM1 enhanced NSCLC aggressiveness by activating matrix metalloproteinase-13 (MMP13) signaling. Together, our results provided new evidence that GOLM1 overexpression promoted the progression of NSCLC and might represent a novel therapeutic target for its treatment.

6.
Plant Mol Biol ; 94(1-2): 61-78, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28247243

RESUMO

Hexokinase (HXK, EC 2.7.1.1) is a multifunctional protein that both is involved in catalyzing the first step of glycolysis and plays an important role in sugar signaling. However, the supporting genetic evidence on hexokinases (CsHXKs) from grape (Vitis vinifera L. cv. Cabernet Sauvignon) berries has been lacking. Here, to investigate the role of CsHXK isoforms as glucose (Glc) and abscisic acid (ABA) sensors, we cloned two hexokinase isozymes, CsHXK1 and CsHXK2 with highly conserved genomic structure of nine exons and eight introns. We also found adenosine phosphate binding, substrate recognition and connection sites in their putative proteins. During grape berry development, the expression profiles of two CsHXK isoforms, sucrose synthases (SuSys) and cell wall invertase (CWINV) genes increased concomitantly with high levels of endogenous Glc and ABA. Furthermore, we showed that in wild type grape berry calli (WT), glucose repressed the expression levels of sucrose synthase (SuSy) and cell wall invertase (CWINV) genes, while ABA increased their expression levels. ABA could not only effectively improve the expression levels of SuSy and CWINV, but also block the repression induced by glucose on the expression of both genes. However, after silencing CsHXK1 or CsHXK2 in grape calli, SuSy and CWINV expression were enhanced, and the expressions of the two genes are insensitive in response to Glc treatment. Interestingly, exogenous ABA alone could not or less increase SuSy and CWINV expression in silencing CsHXK1 or CsHXK2 grape calli compared to WT. Meantime, ABA could not block the repression induced by glucose on the expression of SuSy and CWINV in CsHXK1 or CsHXK2 mutants. Therefore, Glc signal transduction depends on the regulation of CsHXK1 or CsHXK2. ABA signal was also disturbed by CsHXK1 or CsHXK2 silencing. The present results provide new insights into the regulatory role of Glc and ABA on the enzymes related to sugar metabolism in grape berry.


Assuntos
Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Glucosiltransferases/metabolismo , Hexoquinase/metabolismo , Proteínas de Plantas/metabolismo , Vitis/enzimologia , beta-Frutofuranosidase/metabolismo , Ácido Abscísico/farmacologia , Sequência de Aminoácidos , Parede Celular/enzimologia , Frutas/enzimologia , Frutas/metabolismo , Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos , Glucose/farmacologia , Glucosiltransferases/genética , Hexoquinase/genética , Modelos Moleculares , Filogenia , Proteínas de Plantas/genética , Conformação Proteica , beta-Frutofuranosidase/genética
7.
Int J Oncol ; 49(5): 2127-2134, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27600372

RESUMO

Benzothiazole derivatives are known for various biological activities, and their potency in cancer therapy have received considerable attention in recent years. However, the poor water solubility of most benzothiazole derivatives has limited their clinical application. We developed BD926, a novel water-soluble benzothiazole derivative and showed here that it could inhibit the proliferation and induce apoptosis of human Ramos B-lymphoma cells. We further showed that BD926 triggered apoptosis through both mitochondria and endoplasmic reticulum pathways. Moreover, BD926 caused cell cycle arrest at G0/G1 stage. Furthermore, accumulation of reactive oxygen species (ROS) were observed after BD926 treatment and ROS inhibitor was able to attenuate BD926-induced apoptosis, which suggested that BD926-induced apoptosis may be due to over-producing ROS. These results demonstrate the anticancer effects of BD926 in cell models and raise the possibility for the application of BD926 in cancer therapy.


Assuntos
Apoptose/efeitos dos fármacos , Linfócitos B/patologia , Benzotiazóis/farmacologia , Retículo Endoplasmático/efeitos dos fármacos , Linfoma de Células B/patologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Linfócitos B/efeitos dos fármacos , Linfócitos B/metabolismo , Benzotiazóis/química , Western Blotting , Retículo Endoplasmático/metabolismo , Citometria de Fluxo , Humanos , Linfoma de Células B/tratamento farmacológico , Linfoma de Células B/metabolismo , Reação em Cadeia da Polimerase em Tempo Real , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Transdução de Sinais/efeitos dos fármacos , Células Tumorais Cultivadas
8.
Oncotarget ; 7(24): 37238-37249, 2016 Jun 14.
Artigo em Inglês | MEDLINE | ID: mdl-27191988

RESUMO

Zinc finger CCCH-type containing 15 (ZC3H15), also known as DRG family regulatory protein 1 (DFRP1), is a highly conserved eukaryotic protein that associates with active translation machinery. The aim of our study was to explore the clinical relevance and intrinsic functions of ZC3H15 in hepatocellular carcinoma (HCC). We constructed a cohort with 261 tumor and matched normal tissues from HCC patients. ZC3H15 protein and mRNA levels were determined using immunohistochemistry, western blot analysis, and quantitative polymerase chain reaction. ZC3H15 was highly expressed in the majority of HCC cases, and high ZC3H15 levels were significantly associated with high serum a-fetoprotein (AFP) levels (>20 ng/mL) and vascular invasion. Kaplan-Meier and Cox regression data indicated that elevated ZC3H15 was an independent predictor for HCC-specific disease-free survival (hazards ratio [HR], 1.789; 95% confidence interval [95% CI], 1.298-2.466 [P=0.0004]) and overall survival (HR, 1.613; 95% CI, 1.120-2.322 [P=0.0101]). Interaction of ZC3H15 with TRAF2 increased activation of NFκB signaling. These results suggest ZC3H15 is an independent prognostic marker in HCC patients that is clinicopathologically associated with tumor invasion and serum AFP levels.


Assuntos
Carcinoma Hepatocelular/mortalidade , Carcinoma Hepatocelular/patologia , Proteínas de Transporte/metabolismo , Neoplasias Hepáticas/mortalidade , Neoplasias Hepáticas/patologia , Adulto , Biomarcadores Tumorais/genética , Biomarcadores Tumorais/metabolismo , Western Blotting , Carcinoma Hepatocelular/sangue , Carcinoma Hepatocelular/cirurgia , Proteínas de Transporte/genética , Intervalo Livre de Doença , Feminino , Técnicas de Silenciamento de Genes , Humanos , Imuno-Histoquímica , Estimativa de Kaplan-Meier , Neoplasias Hepáticas/sangue , Neoplasias Hepáticas/cirurgia , Masculino , Pessoa de Meia-Idade , NF-kappa B/metabolismo , Invasividade Neoplásica , Prognóstico , RNA Mensageiro/metabolismo , RNA Interferente Pequeno/genética , Proteínas de Ligação a RNA , Reação em Cadeia da Polimerase em Tempo Real , Estudos Retrospectivos , Transdução de Sinais , Fator 2 Associado a Receptor de TNF/metabolismo , Análise Serial de Tecidos , alfa-Fetoproteínas/análise
9.
Zhongguo Zhong Yao Za Zhi ; 41(1): 92-95, 2016 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-28845647

RESUMO

A new isocoumarin, along with five known ones,were isolated from the fermentation products of an endophytic fungus Aspergillus versicolorby using various chromatographic techniques.Their structures were elucidated on the basis of extensivespectroscopic analysis, including 1D-and 2D-NMR techniques. Compound 1 was evaluated for cytotoxicity against five human tumor cell lines. The results showed that 1 exhibited weak cytotoxicityagainst NB4, SHSY5Y and MCF7 cells with IC50 values of 6.8, 4.3,8.8 µmol•L⁻¹, respectively.


Assuntos
Aspergillus/química , Endófitos/química , Isocumarinas/toxicidade , Melanthiaceae/microbiologia , Aspergillus/genética , Aspergillus/isolamento & purificação , Aspergillus/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Endófitos/genética , Endófitos/isolamento & purificação , Endófitos/metabolismo , Humanos , Isocumarinas/química , Isocumarinas/isolamento & purificação , Estrutura Molecular
10.
Zhongguo Zhong Yao Za Zhi ; 40(21): 4205-7, 2015 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-27071257

RESUMO

A phytochemical investigation on the stems of Garcinia bracteata collected from Xishuangbanna resulted in the isolation of a new flavone. By analysis of the HRESIMS, IR, UV, 1D and 2D NMR spectra, the structure of the new compound was determined as 7-methoxy-4',6-dihydroxy-8-isobutyryl-flavone(1). Compound 1 was also tested for its anti-tobacco mosaic virus(TMV) activity. Results suggested the 1 possessed remarkable anti-TMV activity, with an inhibition rate of 28.2%.


Assuntos
Antivirais/química , Antivirais/farmacologia , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Flavonas/química , Flavonas/farmacologia , Garcinia/química , Vírus do Mosaico do Tabaco/efeitos dos fármacos , Antivirais/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Flavonas/isolamento & purificação , Espectroscopia de Ressonância Magnética , Folhas de Planta/química , Vírus do Mosaico do Tabaco/crescimento & desenvolvimento
11.
J Asian Nat Prod Res ; 17(1): 27-32, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25355385

RESUMO

Two new 7,8-secolignans, neglectahenols E and F (1 and 2), together with four known 7,8-secolignans (3-6), were isolated from the fruits of Schisandra neglecta. The structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1-6 were tested for their anti-tobacco mosaic virus (anti-TMV) activities at the concentration of 20 µM. Compounds 1 and 6 showed high anti-TMV activities with inhibition rates of 38.2% and 32.7%, respectively. These rates are higher than that of a positive control. Compounds 2-5 also showed modest anti-TMV activities with inhibition rates in the range of 22.8-28.7%. These rates are close to that of a positive control.


Assuntos
Antivirais/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Lignina/isolamento & purificação , Schisandra/química , Vírus do Mosaico do Tabaco/efeitos dos fármacos , Antivirais/química , Antivirais/farmacologia , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Frutas/química , Lignanas , Lignina/química , Lignina/farmacologia , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular
12.
Case Rep Gastrointest Med ; 2014: 485714, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25371834

RESUMO

Cutaneous vasculitis, interstitial pneumonia with crazy-paving appearance on high-resolution computed tomography, and repeated positive perinuclear anti-neutrophil cytoplasmic antibodies (pANCA) are rarely found together in patients with inflammatory bowel disease in the existing literature. We report the case of a Chinese patient previously diagnosed with cutaneous vasculitis and interstitial pneumonia, who presented with acute pain and mass in his right lower quadrant a couple of years later. The terminal ileum biopsy and postoperative pathology confirmed Crohn's disease (CD).

13.
Molecules ; 19(11): 17173-86, 2014 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-25347460

RESUMO

In this study, a benzimidazole derivative named BMT-1 is revealed as a potential immunomodulatory agent. BMT-1 inhibits the activity of H+/K+-ATPases from anti-CD3/CD28 activated T cells. Furthermore, inhibition the H+/K+-ATPases by use of BMT-1 should lead to intracellular acidification, inhibiting T cell proliferation. To explore this possibility, the effect of BMT-1 on intracellular pH changes was examined by using BCECF as a pH-dependent fluorescent dye. Interestingly, increases in the pHi were observed in activated T cells, and T cells treated with BMT-1 showed a more acidic intracellular pH. Finally, BMT-1 targeted the H+/K+-ATPases and inhibited the proliferative response of anti-CD3/CD28-stimulated T cells. A cell cycle analysis indicated that BMT-1 arrested the cell cycle progression of activated T cells from the G1 to the S phase without affecting CD25 expression or interleukin-2 (IL-2) production; treating IL-2-dependent PBMCs with BMT-1 also led to the inhibition of cell proliferation. Taken together, these findings demonstrate that BMT-1 inhibits the proliferation of T cells by interfering with H+/K+-ATPases and down-regulating intracellular pHi. This molecule may be an interesting lead compound for the development of new immunomodulatory agents.


Assuntos
Benzimidazóis/farmacologia , Proliferação de Células/efeitos dos fármacos , ATPase Trocadora de Hidrogênio-Potássio/metabolismo , Inibidores da Bomba de Prótons/farmacologia , Linfócitos T/efeitos dos fármacos , Antígenos CD28/metabolismo , Complexo CD3/metabolismo , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Células Cultivadas , Regulação para Baixo/efeitos dos fármacos , Humanos , Concentração de Íons de Hidrogênio , Fatores Imunológicos/farmacologia , Interleucina-2/metabolismo , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/metabolismo , Ativação Linfocitária/efeitos dos fármacos , Linfócitos T/metabolismo
14.
Org Lett ; 15(17): 4446-9, 2013 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-23944990

RESUMO

Scopariusic acid (1), a new ent-clerodane-based meroditerpenoid with a unique cyclobutane ring and an unusual 1-octen-3-ol substituent, together with its biosynthetic related compound 2, were isolated from the aerial parts of Isodon scoparius. The structures of 1 and 2, including their absolute configurations, were determined by spectroscopic methods, single-crystal X-ray diffraction analysis, and chemical methods. Compound 1 showed weak cytotoxicity and moderate immunosuppressive activity.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/isolamento & purificação , Imunossupressores/química , Imunossupressores/isolamento & purificação , Isodon/química , Antineoplásicos Fitogênicos/farmacologia , Cristalografia por Raios X , Diterpenos do Tipo Caurano/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Células HL-60 , Humanos , Imunossupressores/farmacologia , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular
15.
Org Lett ; 14(23): 6052-5, 2012 Dec 07.
Artigo em Inglês | MEDLINE | ID: mdl-23181909

RESUMO

Chaetoconvosins A and B (1 and 2), two novel cytochalasan alkaloids with a new 6/6/5/5/7 pentacyclic ring system, were isolated from the solid-state fermented medium of the wheat rhizospheric fungus Chaetomium convolutum cib-100. Their structures were elucidated on the basis of spectroscopic data. The structure of chaetoconvosin A (1) was confirmed by X-ray crystallographic analysis. Chaetoconvosin B (2), the major metabolite, showed remarkable inhibitory ability on root elongation and moderate cytotoxicity against several cancer cell lines.


Assuntos
Alcaloides/isolamento & purificação , Antineoplásicos/isolamento & purificação , Chaetomium/química , Alcaloides/química , Alcaloides/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Conformação Molecular , Estrutura Molecular
16.
Org Lett ; 14(13): 3450-3, 2012 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-22679912

RESUMO

Calophyline A (1), a novel unprecedented rearranged monoterpenoid indole alkaloid, along with a new natural product N-methyl aspidodasycarpine (2) and six known analogues, was isolated from the trunk barks of Winchia calophylla. The structure of compound 1 was elucidated on the basis of spectroscopic data and then confirmed by a single-crystal X-ray crystallographic analysis. A hypothetical biogenetic pathway for compound 1 was proposed. All isolated compounds were evaluated for their in vitro cytotoxicity against a small panel of human cancer cell lines.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apocynaceae/química , Alcaloides de Triptamina e Secologanina/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Modelos Moleculares , Conformação Molecular , Casca de Planta/química , Extratos Vegetais/química , Alcaloides de Triptamina e Secologanina/química , Alcaloides de Triptamina e Secologanina/isolamento & purificação , Estereoisomerismo , Relação Estrutura-Atividade
17.
Planta Med ; 78(1): 52-8, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-21964815

RESUMO

Eight new 19-oxygenated ENT-kaurane diterpenoids were isolated from the aerial parts of Isodon pharicus. Their structures were determined by means of extensive spectroscopic techniques including interpretation of 1D and 2D NMR spectra. Selected compounds were evaluated for their cytotoxicity against NB4, A549, PC-3, MCF-7, and SH-SY5Y cell lines.


Assuntos
Diterpenos/química , Isodon/química , Extratos Vegetais/química , Linhagem Celular Tumoral , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Humanos , Estrutura Molecular , Componentes Aéreos da Planta , Extratos Vegetais/farmacologia
18.
Arch Pharm Res ; 34(6): 875-9, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21725806

RESUMO

Three new ent-abietanoids, named xerophilusins XIV-XVI, and four known analogues, as well as four known chemical constituents were isolated from the leaves of Isodon xerophilus. Their structures were elucidated by extensive spectroscopic studies, and comparison with literature data. In addition, the cytotoxic activity of the ent-abietanoids against chronic myelogenous leukemia (K562), stomach adenocarcinoma (MKN45), and hepatocellular carcinoma (HepG2) human cell lines was investigated and no activities were observed.


Assuntos
Abietanos/farmacologia , Isodon/química , Extratos Vegetais/farmacologia , Abietanos/química , Abietanos/isolamento & purificação , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Análise Espectral
19.
J Nat Prod ; 73(11): 1803-9, 2010 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-20949916

RESUMO

A new ent-atisanoid, eriocatisin A (1), six new ent-abietanoids, eriocasins B-E (2-4, 7), 3-acetyleriocasin C (5), and 3ß-acetoxyeriocasin D (6), and seven new ent-kauranoids, maoesins A-F (8, 10-14) and 3α-acetoxy-maoesin A (9), together with 21 known compounds, were isolated from the aerial parts of Isodon eriocalyx. The structures of 1-14 were determined by spectroscopic data interpretation. All compounds isolated were evaluated for their in vitro growth inhibitory activity against the HT-29, BEL-7402, and SK-OV-3 human cancer cell lines. Compounds 17, 18, and 20 showed inhibitory effects for all three tumor cell lines used, with IC(50) values in the range 2.1-7.3 µM.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Isodon/química , Antineoplásicos Fitogênicos/química , Diterpenos/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular
20.
Org Lett ; 12(6): 1208-11, 2010 Mar 19.
Artigo em Inglês | MEDLINE | ID: mdl-20180522

RESUMO

A new cytotoxic triterpenoid, schinalactone A (1), together with two new biogenetically related compounds, schinalactones B (2) and C (3), has been isolated from the roots and stems of Schisandra sphenanthera.Their structures were elucidated on the basis of extensive spectroscopic analysis. Compounds 1 and 2 showed significant cytotoxicity against PANC-1 cell lines with IC(50) values of 5.9 and 4.1 microM, respectively. A plausible biosynthetic pathway of 1 was also postulated.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Schisandra/química , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Humanos , Conformação Molecular , Raízes de Plantas/química , Caules de Planta/química , Estereoisomerismo , Relação Estrutura-Atividade , Triterpenos/química , Triterpenos/isolamento & purificação
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