Base de dados : MEDLINE Pesquisa : B01.650.940.800.575.912.250.341.984.324 [Categoria DeCS] Referências encontradas : 107 [refinar] Mostrando: 1 .. 10   no formato [Detalhado]

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[PMID]: 27618025 [Au] Autor: Chang HS; Lin CH; Chen YS; Wang HC; Chan HY; Hsieh SY; Wu HC; Cheng MJ; Yuan GF; Lin SY; Lin YJ; Chen IS [Ad] Endereço: Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan. hschang@kmu.edu.tw. [Ti] Título: Secondary Metabolites of the Endophytic Fungus Lachnum abnorme from Ardisia cornudentata. [So] Source: Int J Mol Sci;17(9), 2016 Sep 08. [Is] ISSN: 1422-0067 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: Fractionation of an EtOAc-soluble fraction of the solid fermentate of an endophytic fungus, Lachnum abnorme Mont. BCRC 09F0006, derived from the endemic plant, Ardisia cornudentata Mez. (Myrsinaceae), resulted in the isolation of three new chromones, lachnochromonins D-F (1-3), one novel compound, lachabnormic acid (4), along with nine known compounds (5-13). Their structures were elucidated by spectroscopic analyses. Alternariol-3,9-dimethyl ether (6) was given the correct data as well as 2D spectral analyses for the first time. This is the first report of the isolation of one unprecedented compound 4 from Lachnum genus, while all known compounds were also found for the first time from Lachnum. The effects of some isolates (3, 4, 7-9, 10, and 13) on the inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-activated RAW 264.7 murine macrophages were also evaluated. Several compounds exhibited weak inhibitory activity on lipopolysaccharide (LPS)-stimulated NO production in RAW 264.7 macrophages. [Mh] Termos MeSH primário: Ascomicetos/química Cromonas/química Compostos Heterocíclicos com 1 Anel/farmacologia [Mh] Termos MeSH secundário: Animais Anti-Inflamatórios/química Anti-Inflamatórios/farmacologia Antioxidantes/química Antioxidantes/farmacologia Ardisia/microbiologia Ascomicetos/isolamento & purificação Extratos Celulares/química Extratos Celulares/farmacologia Linhagem Celular Cromonas/farmacologia Fibroblastos/efeitos dos fármacos Fibroblastos/metabolismo Compostos Heterocíclicos com 1 Anel/química Camundongos Óxido Nítrico/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Inflammatory Agents); 0 (Antioxidants); 0 (Cell Extracts); 0 (Chromones); 0 (Heterocyclic Compounds, 1-Ring); 0 (lachabnormic acid); 31C4KY9ESH (Nitric Oxide) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170328 [Lr] Data última revisão: 170328 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160913 [St] Status: MEDLINE

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[PMID]: 27319144 [Au] Autor: Nguekeu YM; Ndontsa BL; Mbouangouere R; Awouafack MD; Ito T; Tane P; Morita H [Ti] Título: A New Alkenylmethylresorcinol from the Fruits of Ardisia kivuensis. [So] Source: Nat Prod Commun;11(5):661-2, 2016 May. [Is] ISSN: 1934-578X [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: The phytochemical study of the MeOH extract from the fruits of Ardisia kivuensis was carried out using repeated silica gel column chromatography followed by Sephadex LH-20 to afford a new alkenylmethylresorcinol, ardisinol III (1) along with three known compounds, oleanolic acid, ß-sitosterol and pentacosanoic acid. The structure of 1 was elucidated using spectroscopic analysis (NMR and MS), and comparison with published data. Compound 1 had weak antioxidant activity (IC50 109.8 µg/mL) while other compounds were not active as compared to L-ascorbic acid (IC50 3.9 µg/mL). [Mh] Termos MeSH primário: Antioxidantes/análise Ardisia/química Resorcinóis/isolamento & purificação [Mh] Termos MeSH secundário: Frutas/química Estrutura Molecular Resorcinóis/química [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antioxidants); 0 (Resorcinols); 0 (ardisinol III) [Em] Mês de entrada: 1608 [Cu] Atualização por classe: 160620 [Lr] Data última revisão: 160620 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160621 [St] Status: MEDLINE

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[PMID]: 26992112 [Au] Autor: Guan YF; Song X; Qiu MH; Luo SH; Wang BJ; Van Hung N; Cuong NM; Soejarto DD; Fong HH; Franzblau SG; Li SH; He ZD; Zhang HJ [Ad] Endereço: School of Chinese Medicine, Hong Kong Baptist University, Hong Kong SAR, China. [Ti] Título: Bioassay-Guided Isolation and Structural Modification of the Anti-TB Resorcinols from Ardisia gigantifolia. [So] Source: Chem Biol Drug Des;88(2):293-301, 2016 08. [Is] ISSN: 1747-0285 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Tuberculosis (TB) is a highly contagious disease mainly caused by Mycobacterium tuberculosis H37 RV . Antitubercular (anti-TB) bioassay-guided isolation of the CHCl3 extract of the leaves and stems of the medicinal plant Ardisia gigantifolia led to the isolation of two anti-TB 5-alkylresorcinols, 5-(8Z-heptadecenyl) resorcinol (1) and 5-(8Z-pentadecenyl) resorcinol (2). We further synthesized 15 derivatives based on these two natural products. These compounds (natural and synthetic) were evaluated for their anti-TB activity against Mycobacterium tuberculosis H37 RV . Resorcinols 1 and 2 exhibited anti-TB activity with MIC values at 34.4 and 79.2 µm in MABA assay, respectively, and 91.7 and 168.3 µm in LORA assay, respectively. Among these derivatives, compound 8 was found to show improved anti-TB activity than its synthetic precursor (2) with MIC values at 42.0 µm in MABA assay and 100.2 µm in LORA assay. The active compounds should be regarded as new hits for further study as a novel class of anti-TB agents. The distinct structure-activity correlations of the parent compound were elucidated based on these derivatives. [Mh] Termos MeSH primário: Antituberculosos/química Antituberculosos/isolamento & purificação Ardisia/química Bioensaio Extratos Vegetais/farmacologia Resorcinóis/química Resorcinóis/isolamento & purificação [Mh] Termos MeSH secundário: Antituberculosos/farmacologia Espectroscopia de Ressonância Magnética Testes de Sensibilidade Microbiana Resorcinóis/farmacologia Espectrometria de Massas por Ionização por Electrospray [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antitubercular Agents); 0 (Plant Extracts); 0 (Resorcinols) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 170509 [Lr] Data última revisão: 170509 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160319 [St] Status: MEDLINE [do] DOI: 10.1111/cbdd.12756

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[PMID]: 26663534 [Au] Autor: Carlier A; Fehr L; Pinto-Carbó M; Schäberle T; Reher R; Dessein S; König G; Eberl L [Ad] Endereço: Department of Microbiology, University of Zurich, CH-8008, Zurich, Switzerland. [Ti] Título: The genome analysis of Candidatus Burkholderia crenata reveals that secondary metabolism may be a key function of the Ardisia crenata leaf nodule symbiosis. [So] Source: Environ Microbiol;18(8):2507-22, 2016 Sep. [Is] ISSN: 1462-2920 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A majority of Ardisia species harbour Burkholderia sp. bacteria within specialized leaf nodules. The bacteria are transmitted hereditarily and have not yet been cultured outside of their host. Because the plants cannot develop beyond the seedling stage without their symbionts, the symbiosis is considered obligatory. We sequenced for the first time the genome of Candidatus Burkholderia crenata (Ca. B. crenata), the leaf nodule symbiont of Ardisia crenata. The genome of Ca. B. crenata is the smallest Burkholderia genome to date. It contains a large amount of insertion sequences and pseudogenes and displays features consistent with reductive genome evolution. The genome does not encode functions commonly associated with plant symbioses such as nitrogen fixation and plant hormone metabolism. However, we identified unique genes with a predicted role in secondary metabolism in the genome of Ca. B. crenata. Specifically, we provide evidence that the bacterial symbionts are responsible for the synthesis of compound FR900359, a cyclic depsipeptide with biomedical properties previously isolated from leaves of A. crenata. [Mh] Termos MeSH primário: Ardisia/metabolismo Ardisia/microbiologia Burkholderia/genética Depsipeptídeos/biossíntese Folhas de Planta/microbiologia [Mh] Termos MeSH secundário: Sequência de Bases Evolução Biológica Transporte Biológico/genética Burkholderia/classificação Metabolismo dos Carboidratos/genética DNA Bacteriano/genética Genoma Bacteriano/genética Metabolismo Secundário/genética Plântulas Análise de Sequência de DNA Simbiose/genética Simbiose/fisiologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (DNA, Bacterial); 0 (Depsipeptides); 0 (FR900359) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170907 [Lr] Data última revisão: 170907 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 151215 [St] Status: MEDLINE [do] DOI: 10.1111/1462-2920.13184

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[PMID]: 27356376 [Au] Autor: Da GZ; Zhang XQ; Yao H; Wang ZP; Zhao B; Zhang C; Hu ZG [Ti] Título: [Identification of Ardisiae Japonicae Herba by ITS2 Sequence]. [So] Source: Zhong Yao Cai;38(11):2277-80, 2015 Nov. [Is] ISSN: 1001-4454 [Cp] País de publicação: China [La] Idioma: chi [Ab] Resumo: OBJECTIVE: The ITS2 sequence was used to identify Ardisiae Japonicae Herba collected from the market, in order to ensure the medicine quality of the market and to provide a reliable technical method. METHODS: The certified samples, including Ardisia japonica and its adulterants, were 56 samples of 17 species. All the sequences of the samples including six related sequences downloaded from NCBI were analyzed by computing the Kimura 2-parameter (K2P) genetic distance and the neighbor-joining (NJ) phylogenetic tree, then the method of DNA barcoding identification technology of Ardisiae Japonicae Herba based on ITS2 sequence was established. Combined with online comparison of sequences, the method was used to detect 15 samples of Ardisiae Japonicae Herba from the market to distinguish authenticity. RESULTS: The maximum and the average intra-specific K2P genetic distance of Ardisia japonica were all less than the minimum and the average inter-specific K2P genetic distance, and Ardisia japonica and its adulterants could be separated by computing the NJ phylogenetic tree. The identification results of online comparison and DNA barcoding identification were the same. In all of the 15 samples, 13 of them were genuine, and the other two samples were fake. CONCLUSION: The DNA barcoding identification technique method of Ardisiae Japonicae Herba is established based on ITS2 sequence, and it provides a reference method to distinguish the authenticity of Ardisiae Japonicae Herba quickly by gene recognition. [Mh] Termos MeSH primário: Ardisia/genética Código de Barras de DNA Taxonômico DNA Espaçador Ribossômico/genética Filogenia [Mh] Termos MeSH secundário: Ardisia/classificação DNA de Plantas/genética Plantas Medicinais/classificação Plantas Medicinais/genética [Pt] Tipo de publicação: ENGLISH ABSTRACT; JOURNAL ARTICLE [Nm] Nome de substância: 0 (DNA, Plant); 0 (DNA, Ribosomal Spacer) [Em] Mês de entrada: 1607 [Cu] Atualização por classe: 160630 [Lr] Data última revisão: 160630 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160701 [St] Status: MEDLINE

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[PMID]: 26658454 [Au] Autor: Schrage R; Schmitz AL; Gaffal E; Annala S; Kehraus S; Wenzel D; Büllesbach KM; Bald T; Inoue A; Shinjo Y; Galandrin S; Shridhar N; Hesse M; Grundmann M; Merten N; Charpentier TH; Martz M; Butcher AJ; Slodczyk T; Armando S; Effern M; Namkung Y; Jenkins L; Horn V; Stößel A; Dargatz H; Tietze D; Imhof D; Galés C; Drewke C; Müller CE; Hölzel M; Milligan G; Tobin AB; Gomeza J; Dohlman HG; Sondek J; Harden TK; Bouvier M; Laporte SA; Aoki J; Fleischmann BK; Mohr K; König GM; Tüting T; Kostenis E [Ad] Endereço: Molecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany. [Ti] Título: The experimental power of FR900359 to study Gq-regulated biological processes. [So] Source: Nat Commun;6:10156, 2015 Dec 14. [Is] ISSN: 2041-1723 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Despite the discovery of heterotrimeric αßγ G proteins ∼25 years ago, their selective perturbation by cell-permeable inhibitors remains a fundamental challenge. Here we report that the plant-derived depsipeptide FR900359 (FR) is ideally suited to this task. Using a multifaceted approach we systematically characterize FR as a selective inhibitor of Gq/11/14 over all other mammalian Gα isoforms and elaborate its molecular mechanism of action. We also use FR to investigate whether inhibition of Gq proteins is an effective post-receptor strategy to target oncogenic signalling, using melanoma as a model system. FR suppresses many of the hallmark features that are central to the malignancy of melanoma cells, thereby providing new opportunities for therapeutic intervention. Just as pertussis toxin is used extensively to probe and inhibit the signalling of Gi/o proteins, we anticipate that FR will at least be its equivalent for investigating the biological relevance of Gq. [Mh] Termos MeSH primário: Depsipeptídeos/farmacologia Subunidades alfa Gq-G11 de Proteínas de Ligação ao GTP/metabolismo Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos [Mh] Termos MeSH secundário: Animais Ardisia/química Linhagem Celular Tumoral Depsipeptídeos/química Subunidades alfa Gq-G11 de Proteínas de Ligação ao GTP/genética Seres Humanos Melanoma/metabolismo Camundongos Modelos Moleculares Estrutura Molecular Conformação Proteica Isoformas de Proteínas Transdução de Sinais Cauda/irrigação sanguínea Vasoconstrição/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Depsipeptides); 0 (FR900359); 0 (Protein Isoforms); EC 3.6.5.1 (GTP-Binding Protein alpha Subunits, Gq-G11) [Em] Mês de entrada: 1605 [Cu] Atualização por classe: 170922 [Lr] Data última revisão: 170922 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 151215 [St] Status: MEDLINE [do] DOI: 10.1038/ncomms10156

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[PMID]: 26638207 [Au] Autor: Yeong LT; Abdul Hamid R; Saiful Yazan L; Khaza'ai H; Mohtarrudin N [Ad] Endereço: Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400, Serdang, Selangor, Malaysia. joyce_ylt86@hotmail.com. [Ti] Título: Low dose triterpene-quinone fraction from Ardisia crispa root precludes chemical-induced mouse skin tumor promotion. [So] Source: BMC Complement Altern Med;15(1):431, 2015 Dec 05. [Is] ISSN: 1472-6882 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: Drastic increment of skin cancer incidence has driven natural product-based chemoprevention as a promising approach in anticancer drug development. Apart from its traditional usages against various ailments, Ardisia crispa (Family: Myrsinaceae) specifically its triterpene-quinone fraction (TQF) which was isolated from the root hexane extract (ACRH) was recently reported to exert antitumor promoting activity in vitro. This study aimed at determining chemopreventive effect of TQF against chemically-induced mouse skin tumorigenesis as well as elucidating its possible pathway(s). METHODS: Mice (n = 10) were initiated with single dose of 7,12-dimethylbenz[α]anthracene (DMBA) (390 nmol/100 µl) followed by, a week later, repeated promotion (twice weekly; 20 weeks) with 12-O-tetradecanoylphorbol-13-acetate (TPA) (1.7 nmol/100 µl). TQF (10, 30 and 100 mg/kg) and curcumin (10 mg/kg; reference) were, respectively, applied topically to DMBA/TPA-induced mice 30 min before each TPA application. Upon termination, histopathological and biochemical analysis, as well as Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) and transcription factor enzyme-linked immunosorbent assay (ELISA) assays were performed to elucidate the potential mechanism of TQF. RESULTS: With comparison to the carcinogen control, results revealed that lower dose of TQF (10 mg/kg) conferred antitumor promoting effect via significant (P < 0.05) suppression against lipid peroxidation (LPO), apoptotic index (cell death) and nuclear factor-kappa B (NF-κB), along with reduction of keratinocyte proliferation; whilst its higher dose (100 mg/kg) was found to promote tumorigenesis by significantly (P < 0.05) increasing LPO and apoptotic index, in addition to aggravating keratinocyte proliferation. CONCLUSIONS: This study evidenced that TQF, particularly at its lower dosage (10 mg/kg), ameliorated DMBA/TPA-induced mouse skin tumorigenesis. Though, future investigations are warranted to determine the lowest possible therapeutic dose of TQF in subsequent in vivo chemopreventive studies. [Mh] Termos MeSH primário: Anticarcinógenos/administração & dosagem Ardisia Quinonas/administração & dosagem Neoplasias Cutâneas/prevenção & controle Pele/efeitos dos fármacos Triterpenos/administração & dosagem [Mh] Termos MeSH secundário: 9,10-Dimetil-1,2-benzantraceno/efeitos adversos Administração Tópica Animais Transformação Celular Neoplásica/efeitos dos fármacos Fracionamento Químico Quimioprevenção Curcumina/administração & dosagem Modelos Animais de Doenças Ensaio de Imunoadsorção Enzimática Masculino Camundongos Camundongos Endogâmicos ICR Extratos Vegetais/administração & dosagem Raízes de Plantas Pele/patologia Neoplasias Cutâneas/induzido quimicamente Acetato de Tetradecanoilforbol/efeitos adversos [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Anticarcinogenic Agents); 0 (Plant Extracts); 0 (Quinones); 0 (Triterpenes); 57-97-6 (9,10-Dimethyl-1,2-benzanthracene); IT942ZTH98 (Curcumin); NI40JAQ945 (Tetradecanoylphorbol Acetate) [Em] Mês de entrada: 1604 [Cu] Atualização por classe: 151209 [Lr] Data última revisão: 151209 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 151207 [St] Status: MEDLINE [do] DOI: 10.1186/s12906-015-0954-3

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[PMID]: 25794927 [Au] Autor: Van NT; Vien TA; Van Kiem P; Van Minh C; Nhiem NX; Long PQ; Anh LT; Kim N; Park S; Kim SH [Ad] Endereço: Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi, Vietnam. [Ti] Título: Chemical components from the leaves of Ardisia insularis and their cytotoxic activity. [So] Source: Arch Pharm Res;38(11):1926-31, 2015 Nov. [Is] ISSN: 0253-6269 [Cp] País de publicação: Korea (South) [La] Idioma: eng [Ab] Resumo: One new oleanane triterpene glycoside, ardinsuloside (1), and twelve known compounds, demethoxybergenin (2), norbergenin (3), bergenin (4), 4-O-galloylbergenin (5), quercitrin (6), myricitrin (7), myricetin 3-O-(3''-O-galloyl)-α-L-rhamnopyranoside (8), desmanthine-2 (9), epicatechin 3-O-galloyl ester (10), 3'-methoxyepicatechin 3-O-galloyl ester (11), gallic acid (12), and methyl galloate (13) were isolated from the leaves of Ardisia insularis. Their structures were established on the basis of spectral and chemical evidence, which were in agreement with those reported in literature. The cytotoxic activities of these compounds were evaluated on three cancer cell lines namely A-549 (human lung cancer), HT-29 (Human colon adenocarcinoma), and OVCAR (human ovarian carcinoma). The results revealed that compound 1 inhibited A-549, HT-29, and OVCAR cell lines with IC50 values of 8.5 ± 1.2, 16.4 ± 3.1, and 13.6 ± 2.4 µM, respectively. The remaining compound showed weak cytotoxic activity. This result indicated that compound 1 could be useful in the treatment of cancer disease. [Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/farmacologia Ardisia/química Extratos Vegetais/farmacologia [Mh] Termos MeSH secundário: Adenocarcinoma/tratamento farmacológico Adenocarcinoma/patologia Antineoplásicos Fitogênicos/administração & dosagem Antineoplásicos Fitogênicos/isolamento & purificação Linhagem Celular Tumoral Feminino Células HT29 Seres Humanos Concentração Inibidora 50 Neoplasias Pulmonares/tratamento farmacológico Neoplasias Pulmonares/patologia Neoplasias Ovarianas/tratamento farmacológico Neoplasias Ovarianas/patologia Extratos Vegetais/administração & dosagem Extratos Vegetais/química Folhas de Planta [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antineoplastic Agents, Phytogenic); 0 (Plant Extracts) [Em] Mês de entrada: 1609 [Cu] Atualização por classe: 151111 [Lr] Data última revisão: 151111 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 150322 [St] Status: MEDLINE [do] DOI: 10.1007/s12272-015-0591-x

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[PMID]: 25521557 [Au] Autor: Dong XZ; Xie TT; Zhou XJ; Mu LH; Zheng XL; Guo DH; Liu P; Ge XY [Ad] Endereço: Departments of aClinical Pharmacology bPharmaceutical Care, Chinese PLA General Hospital, Beijing cCollege of Pharmacy, Tianjin University of Traditional Chinese Medicine, Tianjin dCollege of Pharmacy, Bengbu Medical College, Bengbu, China. [Ti] Título: AG4, a compound isolated from Radix Ardisiae Gigantifoliae, induces apoptosis in human nasopharyngeal cancer CNE cells through intrinsic and extrinsic apoptosis pathways. [So] Source: Anticancer Drugs;26(3):331-42, 2015 Mar. [Is] ISSN: 1473-5741 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: 3ß-O-{α-L-Pyran rhamnose-(1→3)-[ß-D-xylopyranose-(1→2)]-ß-D-glucopyranose-(1→4)-[ß-D-lucopyranose-(1→2)]-α-L-pyran arabinose}-cyclamiretin A (AG4) is a saponin component obtained from the Giantleaf Ardisia Rhizome (Rhizoma Ardisiae Gigantifoliae). The present study aimed to investigate the antitumor potential of AG4 and its possible mechanisms in human nasopharyngeal carcinoma cells (CNE). We exposed tumor cells to AG4 to investigate which cell line was the most sensitive to AG4. Cell viability was assessed using the MTT reduction assay, and the effects of AG4 on apoptosis, reactive oxygen species (ROS) content, mitochondrial membrane potential (MMP), and cell cycle were detected using a flow cytometer; the glutathione, superoxide dismutase and malondialdehyde activities were measured using colorimetric methods. The relative expressions of Bax, Bad, Bid, Bcl-2, and Fas mRNA were calculated using the (Equation is included in full-text article.)comparative method by real-time PCR studies and protein was detected by western blotting. AG4 markedly inhibited the growth of CNE cells by decreasing cell proliferation, inducing apoptosis, and blocking the cell cycle in the S phase. The release of caspase-3, caspase-8, and caspase-9 was stimulated by AG4 in CNE, and the decreased proliferation induced by AG4 was blocked by the inhibitor of pan caspase (Z-VAD-FMK). Moreover, the MMP was decreased in AG4-treated cells, and AG4-induced cell apoptosis was accompanied by a rapid and lasting increase in ROS, which was abolished by N-acetyl-L-cysteine (NAC); glutathione, superoxide dismutase, and malondialdehyde were regulated by AG4. AG4 inhibited Bcl-2 mRNA and protein expression and stimulated Bax, Bad, Bid, Fas mRNA, and protein expression in CNE cultures, suggesting an effect at the transcriptional and protein level. In addition, both the FasL inhibitor (AF-016) and the Bcl-2 family inhibitor (GX15-070) could prevent the cell apoptosis induced by AG4. The findings suggested that AG4-induced apoptosis in CNE cells involved a death receptor pathway and a Bcl-2 family-mediated mitochondrial signaling pathway by decreasing the MMPs in an ROS-dependent manner and regulating genes and proteins relative to apoptosis; also, regulation of cell cycles may also play a role in the antitumor mechanism of AG4. [Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/farmacologia Apoptose/efeitos dos fármacos Ardisia/química Neoplasias Nasofaríngeas/tratamento farmacológico Saponinas/farmacologia [Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/isolamento & purificação Carcinoma Caspase 3/metabolismo Caspase 8/metabolismo Caspase 9/metabolismo Ciclo Celular/efeitos dos fármacos Linhagem Celular Tumoral/efeitos dos fármacos Proliferação Celular/efeitos dos fármacos Ensaios de Seleção de Medicamentos Antitumorais Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos Seres Humanos Potencial da Membrana Mitocondrial/efeitos dos fármacos Neoplasias Nasofaríngeas/metabolismo Neoplasias Nasofaríngeas/patologia Espécies Reativas de Oxigênio/metabolismo Saponinas/isolamento & purificação [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (3-O-(pyran rhamnose-(1-3)-(xylopyranose-(1-2))-glucopyranose-(1-4)-(lucopyranose-(1-2))-pyran arabinose)cyclamiretin A); 0 (Antineoplastic Agents, Phytogenic); 0 (Reactive Oxygen Species); 0 (Saponins); EC 3.4.22.- (Caspase 3); EC 3.4.22.- (Caspase 8); EC 3.4.22.- (Caspase 9) [Em] Mês de entrada: 1511 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 141219 [St] Status: MEDLINE [do] DOI: 10.1097/CAD.0000000000000193

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[PMID]: 25494647 [Au] Autor: Mu LH; Gu YJ; Wang LH; Ma BP; Lu L; Liu P [Ad] Endereço: a Department of Clinical Pharmacology , General Hospital of PLA , Beijing 100853 , China. [Ti] Título: Biotransformation on the triterpenoid saponin of Ardisia gigantifolia by Aspergillus avenaceus AS 3.4454. [So] Source: J Asian Nat Prod Res;17(1):40-6, 2015. [Is] ISSN: 1477-2213 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Compound 1, a triterpenoid saponin from Ardisia gigantifolia Stapf. showing potential anti-tumor activity, was transformed into three derivatives (2-4) by Aspergillus avenaceus 3.4454. Among them, compounds 2 and 3 are new compounds. Their structures were elucidated on the basis of 1D NMR, 2D NMR, HR-ESI-MS, and optical rotation data. Compounds 1-3 were evaluated for their cytotoxicity against human hepatocellular carcinoma and normal liver cells by cell counting kit 8 colorimetric assay. Compound 3 displayed better cytotoxicity against Bel-7402 and HepG2 cell lines and much weaker cytotoxicity against normal liver L02 cell than that of positive control (epirubicin hydrochloride). [Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/isolamento & purificação Ardisia/química Ácido Oleanólico/análogos & derivados Saponinas/isolamento & purificação Triterpenos/isolamento & purificação [Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/química Antineoplásicos Fitogênicos/farmacologia Aspergillus/metabolismo Biotransformação Carcinoma Hepatocelular/tratamento farmacológico Células Hep G2 Seres Humanos Fígado/efeitos dos fármacos Estrutura Molecular Ressonância Magnética Nuclear Biomolecular Ácido Oleanólico/química Ácido Oleanólico/isolamento & purificação Ácido Oleanólico/farmacologia Saponinas/química Saponinas/farmacologia Triterpenos/química Triterpenos/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antineoplastic Agents, Phytogenic); 0 (Saponins); 0 (Triterpenes); 5172-34-9 (cyclamiretin A); 6SMK8R7TGJ (Oleanolic Acid) [Em] Mês de entrada: 1504 [Cu] Atualização por classe: 150121 [Lr] Data última revisão: 150121 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 141216 [St] Status: MEDLINE [do] DOI: 10.1080/10286020.2014.958997

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