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  1. Article ; Online: Caracasine, An

    Martínez, Gricelis Patricia / Mijares, Michael Rodney / Chávez, Katiuska / Chirinos, Perla / Suárez, Alírica Isabel / Compagnone, Reinaldo Santi / De Sanctis, Juan Bautista

    Anti-cancer agents in medicinal chemistry

    2022  Volume 23, Issue 10, Page(s) 1145–1155

    Abstract: Background: Kaurane-type diterpenoids, obtained from various natural sources, have shown many biological activities, including anti-inflammatory and antitumor effects. Caracasine, an : Objective: The present study aimed to ascertain the compound's ... ...

    Abstract Background: Kaurane-type diterpenoids, obtained from various natural sources, have shown many biological activities, including anti-inflammatory and antitumor effects. Caracasine, an
    Objective: The present study aimed to ascertain the compound's mechanism of cell death induction using two leukaemia cell lines, Jurkat E6.1 (T cell) and HL-60 (promyeloblast cells).
    Methods: Cell death in Jurkat and HL60 cells were evaluated by flow cytometry for apoptosis with annexin-V/PI, mitochondrial membrane potential disturbance, changes in cell cycle, CD95 expression, caspase activation, Nuclear Factor kappa B inhibition, and differentiation into a neutrophil-like cell (dHL60).
    Results: Caracasine (10 μM) increased the G0/G1 phase in Jurkat and arrested the cell cycle in the S phase in HL60. Caracasine increased CD95 expression (
    Conclusion: Caracasine induced apoptosis through the intrinsic and extrinsic pathways in both cell lines were evaluated which could be the leading structure for new anti-leukemic and anti-inflammatory drugs.
    MeSH term(s) Humans ; Diterpenes, Kaurane/pharmacology ; Diterpenes, Kaurane/chemistry ; NF-kappa B/metabolism ; Diterpenes/pharmacology ; Apoptosis ; HL-60 Cells ; Leukemia/drug therapy ; Jurkat Cells
    Chemical Substances Diterpenes, Kaurane ; NF-kappa B ; Diterpenes
    Language English
    Publishing date 2022-04-11
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 2217610-X
    ISSN 1875-5992 ; 1871-5206
    ISSN (online) 1875-5992
    ISSN 1871-5206
    DOI 10.2174/1871520622666220415105615
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Antiviral activity of flavonoids present in aerial parts of

    Ortega, Joseph Thomas / Serrano, María Luisa / Suárez, Alírica Isabel / Baptista, Jani / Pujol, Flor Helene / Cavallaro, Lucía Vicenta / Campos, Héctor Rodolfo / Rangel, Héctor Rafael

    EXCLI journal

    2019  Volume 18, Page(s) 1037–1048

    Abstract: ... Marcetia ... ...

    Abstract Marcetia taxifolia
    Language English
    Publishing date 2019-11-05
    Publishing country Germany
    Document type Journal Article
    ISSN 1611-2156
    ISSN 1611-2156
    DOI 10.17179/excli2019-1837
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Caracasine acid, an ent-3,4-seco-kaurene, promotes apoptosis and cell differentiation through NFkB signal pathway inhibition in leukemia cells.

    Martinez, Gricelis Patricia / Mijares, Michael Rodney / Chávez, Katiuska / Suarez, Alirica Isabel / Compagnone, Reinaldo Santi / Chirinos, Perla / De Sanctis, Juan Bautista

    European journal of pharmacology

    2019  Volume 862, Page(s) 172624

    Abstract: Caracasine acid (CA) is an ent-3,4-seco-kaurene isolated from the plant Croton micans. Decreased cancer cell lines viability was reported upon CA treatment. The present study aimed to investigate the mechanism of CA induced cytotoxicity using two human ... ...

    Abstract Caracasine acid (CA) is an ent-3,4-seco-kaurene isolated from the plant Croton micans. Decreased cancer cell lines viability was reported upon CA treatment. The present study aimed to investigate the mechanism of CA induced cytotoxicity using two human cell lines, Jurkat E6.1 (human cell T lymphoma) and HL-60 (human acute promyelocytic leukemia). Significant increases of apoptotic cell death markers upon CA treatment were observed: annexin-V positiveness, potential mitochondrial disturbances, cell cycle changes, caspase activation, and CD95 expression. These effects were not detected in normal lymphocytes. CA induced the appearance of Bax, cleaved caspase 3, and cytochrome c release in Jurkat cells, and cleaved caspase 3 and phosphorylated p53 in HL60 cells. Likewise, downregulation of anti-apoptotic proteins such as Bcl-x (Jurkat), Bcl-2, and XIAP (HL60) was observed with CA treatment. Both pathways, intrinsic and extrinsic were activated when cell lines were treated with CA. NF-κB p65 inhibition was observed in Jurkat cells and cell differentiation in HL-60 cells. CA could be a potential leader compound for the development of new drugs for leukemia treatment in humans.
    MeSH term(s) Antineoplastic Agents, Phytogenic/pharmacology ; Antineoplastic Agents, Phytogenic/therapeutic use ; Apoptosis/drug effects ; Cell Differentiation/drug effects ; Cell Survival/drug effects ; Croton/chemistry ; Diterpenes, Kaurane/pharmacology ; Diterpenes, Kaurane/therapeutic use ; Drug Screening Assays, Antitumor ; HL-60 Cells ; Humans ; Jurkat Cells ; Leukemia/drug therapy ; Leukemia/pathology ; Signal Transduction/drug effects ; Transcription Factor RelA/antagonists & inhibitors ; Transcription Factor RelA/metabolism
    Chemical Substances Antineoplastic Agents, Phytogenic ; Diterpenes, Kaurane ; Rela protein, mouse ; Transcription Factor RelA ; caracasine acid
    Language English
    Publishing date 2019-08-23
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 80121-5
    ISSN 1879-0712 ; 0014-2999
    ISSN (online) 1879-0712
    ISSN 0014-2999
    DOI 10.1016/j.ejphar.2019.172624
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Inverse Molecular Docking Study of NS3-Helicase and NS5-RNA Polymerase of Zika Virus as Possible Therapeutic Targets of Ligands Derived from

    Buendia-Atencio, Cristian / Pieffet, Gilles Paul / Montoya-Vargas, Santiago / Martínez Bernal, Jessica A / Rangel, Héctor Rafael / Muñoz, Ana Luisa / Losada-Barragán, Monica / Segura, Nidya Alexandra / Torres, Orlando A / Bello, Felio / Suárez, Alírica Isabel / Rodríguez, Anny Karely

    ACS omega

    2021  Volume 6, Issue 9, Page(s) 6134–6143

    Abstract: Dengue and Zika are two mosquito-borne diseases of great impact on public health around the world in tropical and subtropical countries. DENV and ZIKV belong to the Flaviviridae family and ... ...

    Abstract Dengue and Zika are two mosquito-borne diseases of great impact on public health around the world in tropical and subtropical countries. DENV and ZIKV belong to the Flaviviridae family and the
    Language English
    Publishing date 2021-02-26
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.0c04719
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: Cytotoxic effects of Fisturalin-3 and 11-Deoxyfisturalin-3 on Jurkat and U937 cell lines.

    Mijares, Michael Rodney / Ochoa, Mariana / Barroeta, Amairelys / Martinez, Gricelis Patricia / Suarez, Alirica Isabel / Compagnone, Reinaldo Santi / Chirinos, Perla / Avila, Ramona / De Sanctis, Juan Bautista

    Biomedical papers of the Medical Faculty of the University Palacky, Olomouc, Czechoslovakia

    2013  Volume 157, Issue 3, Page(s) 222–226

    Abstract: Background: Fisturalines are bromotyrosine compounds isolated from marine sponges. Previous studies have shown antineoplasic, antiviral and antibacterial effects in Vitro; however, the possible effects of these compounds in hematologic malignancies have ...

    Abstract Background: Fisturalines are bromotyrosine compounds isolated from marine sponges. Previous studies have shown antineoplasic, antiviral and antibacterial effects in Vitro; however, the possible effects of these compounds in hematologic malignancies have not been assessed.
    Methods: In the present study, the antiproliferative and pro apoptotic effects of Fistularin-3 (F) and 11-Deoxyfistularin-3 (DF) were assessed using the MTT method and annexin V/propidium iodide by flow cytometry using the cell lines: Jurkat E6.1 and U937. In addition, the cell cycle was assessed by flow cytometry.
    Results: Inhibition of the proliferative response was concentration and time dependent. The IC50 of F was 7.39 and 8.10 µM for Jurkat E6.1 and U937 respectively. At 24 and 48 h, in the U937 cell line, but not in the Jurkat cell line, both compounds induced up to 35% annexin V increase. Necrosis was not observed in any case. Compound F induced, in both cell lines, a decrease in the number of cells in the S phase and increase in the G0/G1 phase. In the Jurkat cell line only, there was an increase in the number of cells in the G2/M phase. Compound DF was not as effective as F.
    Conclusions: F is more active than DF in repressing the cell cycle and inducing apoptosis. Both compounds are potentially useful in the development of new drugs to treat hematologic malignancies.
    MeSH term(s) Antibiotics, Antineoplastic/pharmacology ; Apoptosis/drug effects ; Biological Products/pharmacology ; Cell Cycle/drug effects ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Flow Cytometry ; Hematologic Neoplasms/drug therapy ; Humans ; Inhibitory Concentration 50 ; Jurkat Cells ; Tyrosine/analogs & derivatives ; Tyrosine/pharmacology ; U937 Cells
    Chemical Substances 11-Deoxyfistularin-3 ; Antibiotics, Antineoplastic ; Biological Products ; bromotyrosine ; fisturalin-3 ; Tyrosine (42HK56048U)
    Language English
    Publishing date 2013-09
    Publishing country Czech Republic
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 17196-7
    ISSN 1804-7521 ; 1213-8118 ; 0231-5599 ; 0862-481X
    ISSN (online) 1804-7521
    ISSN 1213-8118 ; 0231-5599 ; 0862-481X
    DOI 10.5507/bp.2012.089
    Database MEDical Literature Analysis and Retrieval System OnLINE

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