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[PMID]: 28946127 [Au] Autor: Wang Z; Zhu W; Gao M; Wu C; Yang C; Yang J; Wu G; Yang B; Kuang H [Ad] Endereço: Key Laboratory of Chinese Materia Medica (Ministry of Education), Heilongjiang University of Chinese Medicine, 24 Heping Road, Xiangfang District, Harbin 150040, China. [Ti] Título: Simultaneous determination of cucurbitacin B and cucurbitacin E in rat plasma by UHPLC-MS/MS: A pharmacokinetics study after oral administration of cucurbitacin tablets. [So] Source: J Chromatogr B Analyt Technol Biomed Life Sci;1065-1066:63-69, 2017 Oct 15. [Is] ISSN: 1873-376X [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Cucurbitacin B (CuB) and cucurbitacin E (CuE) are tetracyclic triterpene compounds from Cucurbitaceae, and the main bioactive compounds of cucurbitacins tablets that used to treatment of chronic hepatitis. Pharmacological research has been very comprehensive, and there are few studies on pharmacokinetics, especially about CuE. An Ultra High Performance Liquid Chromatography-tandem Mass Spectrometry (UHPLC-MS/MS) method with high selectivity, simplicity and sensitivity has been used for quantitative analysis of Cucurbitacin B (CuB) and cucurbitacin E (CuE). Plasma samples were pretreatment by Liquid-liquid extraction (LLE) method with dichloromethane. The chromatographic separation was achieved on a C column (Agilent Eclipse Plus, 1.8µm, 50×2.1mm) using gradient elution with water - methanol at a flow rate of 0.3mL/min and the column temperature was set at 30°C. The method was validated according to FDA guidelines. Lower limit of quantification (LLOQ) was 1.60ng/mL for CuB and 1.58ng/mL for CuE. Correlation coefficients of CuB and CuE were more than 0.99 in rat plasma. All values of intra-day and inter-day precision (RSD%) were not exceeded 15%, the accuracy (RE%) were within -5.57 to 5.20% for CuB and -3.33 to 7.37% for CuE. The mean extraction recoveries were more than 80%. Pharmacokinetic parameters were also evaluated by UHPLC-MS/MS method. The results suggestion that this method was successfully applied to pharmacokinetic study of CuB and CuE in rat plasma after oral administration cucurbitacin tablets. [Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos Espectrometria de Massas em Tandem/métodos Triterpenos/sangue Triterpenos/farmacocinética [Mh] Termos MeSH secundário: Administração Oral Animais Cucurbitacinas/administração & dosagem Cucurbitacinas/farmacocinética Modelos Lineares Masculino Extratos Vegetais Ratos Ratos Sprague-Dawley Reprodutibilidade dos Testes Sensibilidade e Especificidade Comprimidos Triterpenos/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Plant Extracts); 0 (Tablets); 0 (Triterpenes); 0115W5MABF (cucurbitacin B); 60137-06-6 (Cucurbitacins); V8A45XYI21 (cucurbitacin E) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170926 [St] Status: MEDLINE

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[PMID]: 28573224 [Au] Autor: Wang WD; Liu Y; Su Y; Xiong XZ; Shang D; Xu JJ; Liu HJ [Ad] Endereço: Department of Thoracic surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China. [Ti] Título: ANTITUMOR AND APOPTOTIC EFFECTS OF CUCURBITACIN A IN A-549 LUNG CARCINOMA CELLS IS MEDIATED VIA G2/M CELL CYCLE ARREST AND M-TOR/PI3K/AKT SIGNALLING PATHWAY. [So] Source: Afr J Tradit Complement Altern Med;14(2):75-82, 2017. [Is] ISSN: 2505-0044 [Cp] País de publicação: Nigeria [La] Idioma: eng [Ab] Resumo: BACKGROUND: The main aim of this study was to demonstrate the antitumor potential of cucurbitacin A on A-549 NSCLC (non-small cell lung cancer cells). The effects of Cucurbitacin A on apoptotic induction, cell physic, cell cycle failure and m-TOR/PI3K/Akt signalling pathway were also investigated in the present study. MATERIALS AND METHODS: MTT assay and clonogenic assay were carried out to study effects of this compound on cell cytotoxicity and colony forming tendency in A-549 cells. Moreover, phase and fluorescence microscopic techniques were used to examine the effects on cell morphology and induction of apoptosis. The effects on cell cycle phase distribution were investigated by flow cytometry and effects on m-TOR/PI3K/Akt signalling proteins were assessed by western blot analysis. RESULTS: Results showed that cucurbitacin A induced dose-dependent cytotoxic effects along with suppressing the colony forming tendency in these cells. Cucurbitacin A also induced morphological changes in these cells featuring chromatin condensation, cell shrinkage and apoptotic body formation. G2/M phase cell cycle collapse was also induced by Cucurbitacin A along with inhibition of expression levels of m-TOR/PI3K/Akt proteins. CONCLUSIONS: In conclusion, cucurbitacin A inhibits cancer growth in A-549 NSCLC cells by inducing apoptosis, targeting m-TOR/PI3K/Akt signalling pathway and G2/M cell cycle. [Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/uso terapêutico Pontos de Checagem do Ciclo Celular/efeitos dos fármacos Cucurbitacinas/uso terapêutico Neoplasias Pulmonares/tratamento farmacológico Pulmão/efeitos dos fármacos Fosfotransferases/metabolismo Fitoterapia [Mh] Termos MeSH secundário: Células A549 Antineoplásicos Fitogênicos/farmacologia Apoptose Carcinoma/tratamento farmacológico Carcinoma/metabolismo Cucurbitaceae/química Cucurbitacinas/farmacologia Seres Humanos Neoplasias Pulmonares/metabolismo Neoplasias Pulmonares/patologia Fosfatidilinositol 3-Quinases/metabolismo Extratos Vegetais/farmacologia Extratos Vegetais/uso terapêutico Proteínas Proto-Oncogênicas c-akt/metabolismo Transdução de Sinais Serina-Treonina Quinases TOR/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antineoplastic Agents, Phytogenic); 0 (Plant Extracts); 60137-06-6 (Cucurbitacins); EC 2.7.- (Phosphotransferases); EC 2.7.1.- (Phosphatidylinositol 3-Kinases); EC 2.7.1.1 (MTOR protein, human); EC 2.7.1.1 (TOR Serine-Threonine Kinases); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170816 [Lr] Data última revisão: 170816 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170603 [St] Status: MEDLINE [do] DOI: 10.21010/ajtcam.v14i2.9

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[PMID]: 28171685 [Au] Autor: Ahmed MS; El-Senduny F; Taylor J; Halaweish FT [Ad] Endereço: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt, El-Sherouk, Cairo, Egypt. [Ti] Título: Biological screening of cucurbitacin inspired estrone analogs targeting mitogen-activated protein kinase (MAPK) pathway. [So] Source: Chem Biol Drug Des;90(3):478-484, 2017 Sep. [Is] ISSN: 1747-0285 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Assembly of cucurbitacin inspired estrone analogs has been previously synthesized and screened against melanoma cell lines. Further synthetic optimization was executed via installation of Azide polar functional moiety across 23, 24 α, ß-unsaturated ketone side chain using Michael addition reaction. This was followed by biological screening against melanoma cell lines employing MTT assay, in-cell-based ELISA assay, and Western blot analysis to monitor the potential of the synthesized analogs to inhibit the phosphorylated ERK levels. This resulted in evolution of MH-4 possessing IC of 3.59 µm with significant decrease in the p-ERK and targeting MAPK pathway. [Mh] Termos MeSH primário: Cucurbitacinas/toxicidade Estrona/toxicidade Sistema de Sinalização das MAP Quinases/efeitos dos fármacos [Mh] Termos MeSH secundário: Sítios de Ligação Linhagem Celular Tumoral Sobrevivência Celular/efeitos dos fármacos Cucurbitacinas/química Cucurbitacinas/metabolismo Ensaio de Imunoadsorção Enzimática Estrona/análogos & derivados Estrona/metabolismo Seres Humanos Proteína Quinase 1 Ativada por Mitógeno/análise Proteína Quinase 1 Ativada por Mitógeno/metabolismo Proteína Quinase 3 Ativada por Mitógeno/análise Proteína Quinase 3 Ativada por Mitógeno/metabolismo Simulação de Acoplamento Molecular Fosforilação Estrutura Terciária de Proteína Proteínas Proto-Oncogênicas B-raf/química Proteínas Proto-Oncogênicas B-raf/metabolismo [Pt] Tipo de publicação: LETTER [Nm] Nome de substância: 2DI9HA706A (Estrone); 60137-06-6 (Cucurbitacins); EC 2.7.11.1 (BRAF protein, human); EC 2.7.11.1 (Proto-Oncogene Proteins B-raf); EC 2.7.11.24 (Mitogen-Activated Protein Kinase 1); EC 2.7.11.24 (Mitogen-Activated Protein Kinase 3) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171009 [Lr] Data última revisão: 171009 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170208 [St] Status: MEDLINE [do] DOI: 10.1111/cbdd.12963

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[PMID]: 28167007 [Au] Autor: Varricchio A; De Lucia A; Varricchio AM; Della Volpe A; Mansi N; Pastore V; Ciprandi G [Ad] Endereço: UOSD Videondoscopia delle vas ASL-Napoli1-Centro, P.O. S.Gennaro, Naples, Italy. [Ti] Título: Sinuclean Nebules treatment in children suffering from otitis media with effusion. [So] Source: Int J Pediatr Otorhinolaryngol;94:30-35, 2017 Mar. [Is] ISSN: 1872-8464 [Cp] País de publicação: Ireland [La] Idioma: eng [Ab] Resumo: OBJECTIVE: Otitis media with effusion (OME) is an ear disorder defined by the presence of fluid in the middle ear without signs or symptoms of acute infection. The current randomized, double-blind, controlled study aimed to evaluate whether Sinuclean Nebules treatment, administered by nasal douche (Rinowash), could induce ear healing better than isotonic saline in children with OME. METHODS: The study was randomized, double-blind, and controlled. Group A (30 children) was treated with Sinuclean Nebules 45 and Group B (31 children) was treated with isotonic saline; both compounds were administered by nasal nebulization with Rinowash nasal douche twice/day in the morning and in the evening for 10 days, followed by a one-week suspension, and after by a second course as the first. Tympanogram and audiometry were performed at baseline and after treatment. RESULTS: Considering the global evaluation of the treatment: in Group A, 28 (93.3%) patients had complete resolution and 2 (6.7%) had partial resolution; in Group B, all patients had failure of treatment. There was a significant difference between groups (p < 0.0001). CONCLUSION: The current randomized-controlled study demonstrated that Sinuclean Nebules was effective and in the treatment of children with OME. [Mh] Termos MeSH primário: Cucurbitaceae Cucurbitacinas/uso terapêutico Otite Média com Derrame/tratamento farmacológico Extratos Vegetais/uso terapêutico [Mh] Termos MeSH secundário: Administração Intranasal Audiometria Criança Pré-Escolar Cucurbitacinas/administração & dosagem Método Duplo-Cego Feminino Testes Auditivos Seres Humanos Masculino Nebulizadores e Vaporizadores Otite Média com Derrame/terapia Extratos Vegetais/administração & dosagem Irrigação Terapêutica [Pt] Tipo de publicação: JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL [Nm] Nome de substância: 0 (Plant Extracts); 60137-06-6 (Cucurbitacins) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170817 [Lr] Data última revisão: 170817 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170208 [St] Status: MEDLINE

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[PMID]: 27061415 [Au] Autor: Wang S; Guan X; Zhong X; Yang Z; Huang W; Jia B; Cui T [Ad] Endereço: Affiliated Hospital of Beihua University, Jilin, 132011, China. [Ti] Título: Simultaneous determination of cucurbitacin IIa and cucurbitacin IIb of Hemsleya amabilis by HPLC-MS/MS and their pharmacokinetic study in normal and indomethacin-induced rats. [So] Source: Biomed Chromatogr;30(10):1632-40, 2016 Oct. [Is] ISSN: 1099-0801 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: A selective and sensitive HPLC-MS/MS method was developed for the simultaneous determination of cucurbitacin IIa (cuIIa) and cucurbitacin IIb (cuIIb), the major bioactive cucurbitacins of Hemsleya amabilis, in rat plasma using euphadienol as internal standard (IS). After liquid-liquid extraction with dichloromethane, separation was achieved on a Syncronis HPLC C18 column (150 mm × 4.6 mm, 5 µm) using an isocratic mobile phase system consisting of acetonitrile-water (85:15, v/v) at a flow rate of 0.6 mL/min with a split ratio of 1:2. Detection was performed on a TSQ Quantum Ultra mass spectrometer equipped with an positive-ion electrospray ionization source. The lower limits of quantification (LLOQs) were 0.25 and 0.15 ng/mL for cuIIa and cuIIb, respectively. The intra- and inter-day precision was <11.5% for the LLOQs and each quality control level of the analytes, and accuracy was between -9.1 and 7.6%. The extraction recoveries of the analytes and IS from rat plasma were all >87.1%. The method was fully validated and applied to compare the pharmacokinetic profiles of the two cucurbitacins in rat plasma after oral administration of H. amabilis extract between normal and indomethacin-induced rats. Copyright © 2016 John Wiley & Sons, Ltd. [Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos Cucurbitacinas/farmacocinética Indometacina/administração & dosagem Espectrometria de Massas em Tandem/métodos [Mh] Termos MeSH secundário: Animais Limite de Detecção Ratos Padrões de Referência Reprodutibilidade dos Testes [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (cucurbitacin IIa); 0 (cucurbitacin IIb); 60137-06-6 (Cucurbitacins); XXE1CET956 (Indomethacin) [Em] Mês de entrada: 1701 [Cu] Atualização por classe: 170130 [Lr] Data última revisão: 170130 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160411 [St] Status: MEDLINE [do] DOI: 10.1002/bmc.3733

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[PMID]: 26856457 [Au] Autor: Fabini E; Fiori GM; Tedesco D; Lopes NP; Bertucci C [Ad] Endereço: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy. [Ti] Título: Surface plasmon resonance and circular dichroism characterization of cucurbitacins binding to serum albumins for early pharmacokinetic profiling. [So] Source: J Pharm Biomed Anal;122:166-72, 2016 Apr 15. [Is] ISSN: 1873-264X [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Cucurbitacins are a group of tetracyclic triterpenoids, known for centuries for their anti-cancer and anti-inflammatory properties, which are being actively investigated over the past decades in order to elucidate their mechanism of action. In perspective of being used as therapeutic molecules, a pharmacokinetic characterization is crucial to assess the affinity toward blood carrier proteins and extrapolate distribution volumes. Usually, pharmacokinetic data are first collected on animal models and later translated to humans; therefore, an early characterization of the interaction with carrier proteins from different species is highly desirable. In the present study, the interactions of cucurbitacins E and I with human and rat serum albumins (HSA and RSA) were investigated by means of surface plasmon resonance (SPR)-based optical biosensing and circular dichroism (CD) spectroscopy. Active HSA and RSA sensor chip surfaces were prepared through an amine coupling reaction protocol, and the equilibrium dissociation constants (Kd) for the different cucurbitacins-serum albumins complexes were then determined by SPR analysis. Further information on the binding of cucurbitacins to serum albumins was obtained by CD competition experiments with biliverdin, a specific marker binding to subdomain IB of HSA. SPR data unveiled a previously unreported binding event between CucI and HSA; the determined binding affinities of both compounds were slightly higher for RSA with respect to HSA, even though all the compounds can be ranked as high-affinity binders for both carriers. CD analysis showed that the two cucurbitacins modify the binding of biliverdin to serum albumins through opposite allosteric modulation (positive for HSA, negative for RSA), confirming the need for caution in the translation of pharmacokinetic data across species. [Mh] Termos MeSH primário: Dicroísmo Circular/métodos Cucurbitacinas/química Cucurbitacinas/metabolismo Albumina Sérica/química Albumina Sérica/metabolismo Ressonância de Plasmônio de Superfície/métodos [Mh] Termos MeSH secundário: Animais Sítios de Ligação Seres Humanos Ligação Proteica Ratos [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Serum Albumin); 60137-06-6 (Cucurbitacins) [Em] Mês de entrada: 1612 [Cu] Atualização por classe: 161230 [Lr] Data última revisão: 161230 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160210 [St] Status: MEDLINE

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[PMID]: 26780083 [Au] Autor: Silva IT; Geller FC; Persich L; Dudek SE; Lang KL; Caro MS; Durán FJ; Schenkel EP; Ludwig S; Simões CM [Ad] Endereço: Departamento de Ciências Farmacêuticas, CIF, CCS, Universidade Federal de Santa Catarina (UFSC), Campus Universitário Trindade, Florianópolis, 88040-900, SC, Brazil. [Ti] Título: Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549. [So] Source: Invest New Drugs;34(2):139-48, 2016 Apr. [Is] ISSN: 1573-0646 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Cucurbitacins and their derivatives are triterpenoids that are found in various plant families, and are known for their pharmacological and biological activities, including anti-cancer effects. Lung cancer represents a major public health problem, with non-small-cell lung cancer (NSCLC) being the most frequent and aggressive type of lung cancer. The objective of this work was to evaluate four cucurbitacins (CUCs) for their cytotoxic activity, effects on apoptosis induction, cell cycle progression, anti-migratory, and anti-invasive effects on the human NSCLC cell line (A549 cells). Our findings showed that these CUCs could suppress human NSCLC cell growth in vitro through their effects on the PI3Kinase and MAPK pathways, which lead to programmed cell death induction, as well as inhibition of cell migration and cell invasion. Additionally, these effects culminate in apoptosis induction and G2/M cell cycle arrest by modulating cyclin B1 expression, and in the mitigation of strategic steps of lung cancer metastasis, including migration and invasion of A549 cells. These results suggest that two natural (DDCB and CB) and two novel semisynthetic derivatives of cucurbitacin B (ACB and DBCB) could be considered as promising compounds with antitumor potential. [Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos Cucurbitacinas/farmacologia Cucurbitacinas/uso terapêutico Neoplasias Pulmonares/tratamento farmacológico Neoplasias Pulmonares/patologia [Mh] Termos MeSH secundário: Células A549 Carcinoma Pulmonar de Células não Pequenas/enzimologia Carcinoma Pulmonar de Células não Pequenas/patologia Caspases/metabolismo Pontos de Checagem do Ciclo Celular/efeitos dos fármacos Movimento Celular/efeitos dos fármacos Proliferação Celular/efeitos dos fármacos Cucurbitacinas/química Ciclina B1/metabolismo Regulação para Baixo/efeitos dos fármacos Proteína-Tirosina Quinases de Adesão Focal/metabolismo Seres Humanos Neoplasias Pulmonares/enzimologia Metaloproteinase 2 da Matriz/metabolismo Metaloproteinase 9 da Matriz/metabolismo Invasividade Neoplásica Fosforilação/efeitos dos fármacos Transdução de Sinais/efeitos dos fármacos Fator de Necrose Tumoral alfa/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Cyclin B1); 0 (Tumor Necrosis Factor-alpha); 60137-06-6 (Cucurbitacins); EC 2.7.10.2 (Focal Adhesion Protein-Tyrosine Kinases); EC 3.4.22.- (Caspases); EC 3.4.24.24 (Matrix Metalloproteinase 2); EC 3.4.24.35 (Matrix Metalloproteinase 9) [Em] Mês de entrada: 1612 [Cu] Atualização por classe: 171019 [Lr] Data última revisão: 171019 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160119 [St] Status: MEDLINE [do] DOI: 10.1007/s10637-015-0317-4

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[PMID]: 26566075 [Au] Autor: Wang JW; Xu JH; Li J; Zhao MH; Zhang HF; Liu DC; Zhou X; Xu H [Ti] Título: Improvement of the Antitumor Efficacy of Intratumoral Administration of Cucurbitacin Poly(Lactic-co-Glycolic Acid) Microspheres Incorporated in In Situ-Forming Sucrose Acetate Isobutyrate Depots. [So] Source: J Pharm Sci;105(1):205-11, 2016 Jan. [Is] ISSN: 1520-6017 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Localized drug delivery strategies for cancer therapy have been introduced for decades as a means of increasing drug concentration at tumor target site and minimizing systemic toxicities. In this paper, a combination of microspheres (MSs) and sucrose acetate isobutyrate (SAIB) in situ-forming implants (ISFIs) was evaluated for improving antitumor efficacy via intratumoral injection. Monodispersed cucurbitacin (Cuc)-loaded Poly (lactic-co-glycolic acid) (PLGA) MSs with mean diameter of about 5 µm were fabricated by Shirasu porous Glass (SPG) membrane emulsification technique, and their properties were investigated. The in vitro drug release pattern, antimelanoma efficiency, and drug distribution in tumor of three different intratumoral injection systems, that is, MSs, SAIB ISFIs, and combination of MSs and SAIB ISFIs (SAIB-MSs), was investigated. The Cuc-loaded MSs prepared by PLGA (LA/GA = 50:50, inherent viscosity = 0.87 dL/g), has an appropriate release pattern with lower initial burst and delayed drug release. SAIB-MSs have a much slower drug release rate than that of MSs or SAIB ISFIs. SAIB-MSs showed the best antitumor efficacy in melanoma-bearing mice model, and the results of drug distribution in tumor revealed that the incorporation MSs in SAIB solution obviously extended the residence of drug in tumor. The low Cuc concentration in tumor periphery region after intratumoral administration of SAIB-MSs demonstrated poor drug penetration of this system. For further improving the antitumor efficacy of intratumoral chemotherapy, elegant designing to carriers with both extended residency and wide drug distribution in tumor is needed. [Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/administração & dosagem Antineoplásicos Fitogênicos/farmacologia Cucurbitacinas/administração & dosagem Cucurbitacinas/farmacologia Sacarose/análogos & derivados [Mh] Termos MeSH secundário: Animais Antineoplásicos Fitogênicos/química Cucurbitacinas/química Preparações de Ação Retardada Implantes de Medicamento Emulsões Excipientes Injeções Intralesionais Ácido Láctico Masculino Melanoma/tratamento farmacológico Melanoma/metabolismo Camundongos Camundongos Endogâmicos C57BL Microesferas Tamanho da Partícula Ácido Poliglicólico Sacarose/química Distribuição Tecidual [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antineoplastic Agents, Phytogenic); 0 (Delayed-Action Preparations); 0 (Drug Implants); 0 (Emulsions); 0 (Excipients); 0 (polylactic acid-polyglycolic acid copolymer); 26009-03-0 (Polyglycolic Acid); 33X04XA5AT (Lactic Acid); 57-50-1 (Sucrose); 60137-06-6 (Cucurbitacins); H5KI1C3YTV (sucrose acetate isobutyrate) [Em] Mês de entrada: 1610 [Cu] Atualização por classe: 161230 [Lr] Data última revisão: 161230 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 151114 [St] Status: MEDLINE

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[PMID]: 26503558 [Au] Autor: Cai Y; Fang X; He C; Li P; Xiao F; Wang Y; Chen M [Ad] Endereço: * State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, P.R. China. [Ti] Título: Cucurbitacins: A Systematic Review of the Phytochemistry and Anticancer Activity. [So] Source: Am J Chin Med;43(7):1331-50, 2015. [Is] ISSN: 0192-415X [Cp] País de publicação: Singapore [La] Idioma: eng [Ab] Resumo: Cucurbitacins are highly oxidized tetracyclic triterpenoids that are widely present in traditional Chinese medicines (Cucurbitaceae family), possess strong anticancer activity, and are divided into 12 classes from A to T with over 200 derivatives. The eight most active cucurbitacin components against cancer are cucurbitacin B, D, E, I, IIa, L glucoside, Q, and R. Their mechanisms of action include antiproliferation, inhibition of migration and invasion, proapoptosis, and cell cycle arrest promotion. Cucurbitacins are also found to be the inhibitors of JAK-STAT3, Wnt, PI3K/Akt, and MAPK signaling pathways, which play important roles in the apoptosis and survival of cancer cells. Recently, new studies have discovered synergistic anticancer effects by using cucurbitacins together with clinically approved chemotherapeutic drugs, such as docetaxel and methotrexate. This paper provides a summary of recent research progress on the anticancer property of cucurbitacins and the various intracellular signaling pathways involved in the regulation of cancer cell proliferation, death, invasion, and migration. Therefore, cucurbitacins are a class of promising anticancer drugs to be used alone or be intergraded in current chemotherapies and radiotherapies to treat many types of cancers. [Mh] Termos MeSH primário: Antineoplásicos Fitogênicos Cucurbitacinas/farmacologia Cucurbitacinas/uso terapêutico Neoplasias/tratamento farmacológico Neoplasias/patologia Fitoterapia [Mh] Termos MeSH secundário: Animais Apoptose/efeitos dos fármacos Pontos de Checagem do Ciclo Celular/efeitos dos fármacos Linhagem Celular Tumoral Movimento Celular/efeitos dos fármacos Proliferação Celular/efeitos dos fármacos Transformação Celular Neoplásica/efeitos dos fármacos Cucurbitacinas/química Cucurbitacinas/classificação Quimioterapia Combinada Seres Humanos Metotrexato/uso terapêutico Conformação Molecular Invasividade Neoplásica Transdução de Sinais/efeitos dos fármacos Relação Estrutura-Atividade Taxoides/uso terapêutico [Pt] Tipo de publicação: JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antineoplastic Agents, Phytogenic); 0 (Taxoids); 15H5577CQD (docetaxel); 60137-06-6 (Cucurbitacins); YL5FZ2Y5U1 (Methotrexate) [Em] Mês de entrada: 1609 [Cu] Atualização por classe: 151207 [Lr] Data última revisão: 151207 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 151028 [St] Status: MEDLINE [do] DOI: 10.1142/S0192415X15500755

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[PMID]: 26437392 [Au] Autor: Chawech R; Jarraya R; Girardi C; Vansteelandt M; Marti G; Nasri I; Racaud-Sultan C; Fabre N [Ad] Endereço: Université de Toulouse, UPS, Pharma-DEV, UMR 152, Université Toulouse 3, Faculté des Sciences Pharmaceutiques, F-31062 Toulouse cedex 09, France. chawech.rachid@gmail.com. [Ti] Título: Cucurbitacins from the Leaves of Citrullus colocynthis (L.) Schrad. [So] Source: Molecules;20(10):18001-15, 2015 Sep 30. [Is] ISSN: 1420-3049 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: Two new tetracyclic cucurbitane-type triterpene glycosides were isolated from an ethyl acetate extract of Citrullus colocynthis leaves together with four known cucurbitacins. Their structures were established on the basis of their spectroscopic data (mainly NMR and mass spectrometry). Evaluation of the in vitro cytotoxic activity of the isolated compounds against two human colon cancer cell lines (HT29 and Caco-2) and one normal rat intestine epithelial cell line (IEC6), revealed that one of the isolated compounds presented interesting specific cytotoxic activity towards colorectal cell lines. [Mh] Termos MeSH primário: Citrullus colocynthis/química Cucurbitacinas/química Extratos Vegetais/química Folhas de Planta/química [Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/química Antineoplásicos Fitogênicos/farmacologia Linhagem Celular Tumoral Cucurbitacinas/farmacologia Relação Dose-Resposta a Droga Seres Humanos Concentração Inibidora 50 Estrutura Molecular Ressonância Magnética Nuclear Biomolecular Extratos Vegetais/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antineoplastic Agents, Phytogenic); 0 (Plant Extracts); 60137-06-6 (Cucurbitacins) [Em] Mês de entrada: 1606 [Cu] Atualização por classe: 151006 [Lr] Data última revisão: 151006 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 151006 [St] Status: MEDLINE [do] DOI: 10.3390/molecules201018001

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