LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 8 of total 8

Search options

  1. Article ; Online: The Role of Chloroquine and Hydroxychloroquine in Immune Regulation and Diseases.

    Martinez, Gricelis P / Zabaleta, Mercedes E / Di Giulio, Camilo / Charris, Jaime E / Mijares, Michael R

    Current pharmaceutical design

    2020  Volume 26, Issue 35, Page(s) 4467–4485

    Abstract: Chloroquine (CQ) and hydroxychloroquine (HCQ) are derivatives of the heterocyclic aromatic compound quinoline. These economical compounds have been used as antimalarial agents for many years. Currently, they are used as monotherapy or in conjunction with ...

    Abstract Chloroquine (CQ) and hydroxychloroquine (HCQ) are derivatives of the heterocyclic aromatic compound quinoline. These economical compounds have been used as antimalarial agents for many years. Currently, they are used as monotherapy or in conjunction with other therapies for the treatment of autoimmune diseases such as systemic lupus erythematosus (SLE), rheumatoid arthritis (RA), Sjögren's syndrome (SS) and antiphospholipid antibody syndrome (APS). Based on its effects on the modulation of the autophagy process, various clinical studies suggest that CQ and HCQ could be used in combination with other chemotherapeutics for the treatment of various types of cancer. Furthermore, the antiviral effects showed against Zika, Chikungunya, and HIV are due to the annulation of endosomal/lysosomal acidification. Recently, CQ and HCQ were approved for the U.S. Food and Drug Administration (FDA) for the treatment of infected patients with the coronavirus SARSCoV- 2, causing the disease originated in December 2019, namely COVID-2019. Several mechanisms have been proposed to explain the pharmacological effects of these drugs: 1) disruption of lysosomal and endosomal pH, 2) inhibition of protein secretion/expression, 3) inhibition of antigen presentation, 4) decrease of proinflammatory cytokines, 5) inhibition of autophagy, 6) induction of apoptosis and 7) inhibition of ion channels activation. Thus, evidence has shown that these structures are leading molecules that can be modified or combined with other therapeutic agents. In this review, we will discuss the most recent findings in the mechanisms of action of CQ and HCQ in the immune system, and the use of these antimalarial drugs on diseases.
    MeSH term(s) Autoimmune Diseases/drug therapy ; Betacoronavirus ; COVID-19 ; Chloroquine/pharmacology ; Chloroquine/therapeutic use ; Coronavirus Infections ; Humans ; Hydroxychloroquine/pharmacology ; Hydroxychloroquine/therapeutic use ; Immune System/drug effects ; Pandemics ; Pneumonia, Viral ; SARS-CoV-2
    Chemical Substances Hydroxychloroquine (4QWG6N8QKH) ; Chloroquine (886U3H6UFF)
    Keywords covid19
    Language English
    Publishing date 2020-07-07
    Publishing country United Arab Emirates
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 1304236-1
    ISSN 1873-4286 ; 1381-6128
    ISSN (online) 1873-4286
    ISSN 1381-6128
    DOI 10.2174/1381612826666200707132920
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  2. Article: The Role of Chloroquine and Hydroxychloroquine in Immune Regulation and Diseases

    Martinez, Gricelis P / Zabaleta, Mercedes E / Di Giulio, Camilo / Charris, Jaime E / Mijares, Michael R

    Curr Pharm Des

    Abstract: Chloroquine (CQ) and hydroxychloroquine (HCQ) are derivatives of the heterocyclic aromatic compound quinoline. These economical compounds have been used as antimalarial agents for many years. Currently, they are used as monotherapy or in conjunction with ...

    Abstract Chloroquine (CQ) and hydroxychloroquine (HCQ) are derivatives of the heterocyclic aromatic compound quinoline. These economical compounds have been used as antimalarial agents for many years. Currently, they are used as monotherapy or in conjunction with other therapies for the treatment of autoimmune diseases such as systemic lupus erythematosus (SLE), rheumatoid arthritis (RA), Sjögren's syndrome (SS) and antiphospholipid antibody syndrome (APS). Based on its effects on the modulation of the autophagy process, various clinical studies suggest that CQ and HCQ could be used in combination with other chemotherapeutics for the treatment of various types of cancer. Furthermore, the antiviral effects showed against Zika, Chikungunya, and HIV are due to the annulation of endosomal/lysosomal acidification. Recently, CQ and HCQ were approved for the U.S. Food and Drug Administration (FDA) for the treatment of infected patients with the coronavirus SARSCoV- 2, causing the disease originated in December 2019, namely COVID-2019. Several mechanisms have been proposed to explain the pharmacological effects of these drugs: 1) disruption of lysosomal and endosomal pH, 2) inhibition of protein secretion/expression, 3) inhibition of antigen presentation, 4) decrease of proinflammatory cytokines, 5) inhibition of autophagy, 6) induction of apoptosis and 7) inhibition of ion channels activation. Thus, evidence has shown that these structures are leading molecules that can be modified or combined with other therapeutic agents. In this review, we will discuss the most recent findings in the mechanisms of action of CQ and HCQ in the immune system, and the use of these antimalarial drugs on diseases.
    Keywords covid19
    Publisher WHO
    Document type Article
    Note WHO #Covidence: #635689
    Database COVID19

    Kategorien

  3. Article ; Online: The role of Chloroquine and Hydroxychloroquine in Immune Regulation and Diseases

    Martinez, Gricelis P. / Zabaleta, Mercedes E. / Di Giulio, Camilo / Charris, Jaime E. / Mijares, Michael R.

    Current Pharmaceutical Design

    2020  Volume 26

    Abstract: Chloroquine (CQ) and hydroxychloroquine (HCQ) are derivatives of the heterocyclic aromatic compound quinoline. These economical compounds were used as antimalarial agents for many years. Currently, they are used as monotherapy or in conjunction with ... ...

    Abstract : Chloroquine (CQ) and hydroxychloroquine (HCQ) are derivatives of the heterocyclic aromatic compound quinoline. These economical compounds were used as antimalarial agents for many years. Currently, they are used as monotherapy or in conjunction with other therapies for the treatment of autoimmune diseases such as systemic lupus erythematosus (SLE), rheumatoid arthritis (RA), Sjögren's syndrome (SS) and antiphospholipid antibody syndrome (APS). Based on its effects on the modulation of the autophagy process, various clinical studies suggest that CQ and HCQ could be used in combination with other chemotherapeutics for the treatment of various types of cancer. Furthermore, the antiviral effects showed against Zika, Chikungunya, and HIV are due to the annulation of endosomal/lysosomal acidification. Recently, CQ and HCQ were approved for The U.S. Food and Drug Administration (FDA) for the treatment of infected patients with the coronavirus SARS-CoV-2, causing the disease originated in December 2019, namely COVID-2019. Several mechanisms have been proposed to explain the pharmacological effects of these drugs: 1) disruption of lysosomal and endosomal pH, 2) inhibition of protein secretion/expression, 3) inhibition of antigen presentation, 4) decrease of proinflammatory cytokines, 5) inhibition of autophagy, 6) induction of apoptosis and 7) inhibition of ion channels activation. Thus, evidence has shown that these structures are leader molecules that can be modified or combined with other therapeutic agents. In this review, we will discuss the most recent findings in the mechanisms of action of CQ and HCQ in the immune system, and the use of these antimalarial drugs on diseases.
    Keywords Pharmacology ; Drug Discovery ; covid19
    Language English
    Publisher Bentham Science Publishers Ltd.
    Publishing country nl
    Document type Article ; Online
    ZDB-ID 1304236-1
    ISSN 1873-4286 ; 1381-6128
    ISSN (online) 1873-4286
    ISSN 1381-6128
    DOI 10.2174/1381612826666200707132920
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    More links

    Kategorien

  4. 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

    More links

    Kategorien

  5. Article ; Online: Synthesis, Leishmanicidal, Trypanocidal, Antiproliferative Assay and Apoptotic Induction of (2-Phenoxypyridin-3-yl)naphthalene-1(2

    Blanco, Zuleima / Fernandez-Moreira, Esteban / Mijares, Michael R / Celis, Carmen / Martínez, Gricelis / De Sanctis, Juan B / Gurská, Soňa / Džubák, Petr / Hajdůch, Marián / Mijoba, Ali / García, Yael / Serrano, Xenón / Herrera, Nahum / Correa-Abril, Jhonny / Parra, Yonathan / Ángel, Jorge / Ramírez, Hegira / Charris, Jaime E

    Molecules (Basel, Switzerland)

    2022  Volume 27, Issue 17

    Abstract: The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of these pathologies invites us to search for new molecules with these characteristics. In this ... ...

    Abstract The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of these pathologies invites us to search for new molecules with these characteristics. In this research, we report 16 synthetic chalcone derivatives that were investigated for leishmanicidal and trypanocidal activities as well as for antiproliferative potential on eight human cancers and two nontumor cell lines. The final compounds 8−23 were obtained using the classical base-catalyzed Claisen−Schmidt condensation. The most potent compounds as parasiticidal were found to be 22 and 23, while compounds 18 and 22 showed the best antiproliferative activity and therapeutic index against CCRF-CEM, K562, A549, and U2OS cancer cell lines and non-toxic VERO, BMDM, MRC-5, and BJ cells. In the case of K562 and the corresponding drug-resistant K562-TAX cell lines, the antiproliferative activity has shown a more significant difference for compound 19 having 10.3 times higher activity against the K562-TAX than K562 cell line. Flow cytometry analysis using K562 and A549 cell lines cultured with compounds 18 and 22 confirmed the induction of apoptosis in treated cells after 24 h. Based on the structural analysis, these chalcones represent new compounds potentially useful for Leishmania, Trypanosoma cruzi, and some cancer treatments.
    MeSH term(s) Chagas Disease/drug therapy ; Chalcone/pharmacology ; Humans ; Leishmania ; Leishmaniasis/drug therapy ; Naphthalenes/therapeutic use ; Structure-Activity Relationship ; Trypanocidal Agents/chemistry ; Trypanosoma cruzi
    Chemical Substances Naphthalenes ; Trypanocidal Agents ; Chalcone (5S5A2Q39HX)
    Language English
    Publishing date 2022-08-31
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules27175626
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  6. 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

    More links

    Kategorien

  7. 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

    More links

    Kategorien

  8. Article ; Online: Synthesis, Leishmanicidal, Trypanocidal, Antiproliferative Assay and Apoptotic Induction of (2-Phenoxypyridin-3-yl)naphthalene-1(2 H )-one Derivatives

    Zuleima Blanco / Esteban Fernandez-Moreira / Michael R. Mijares / Carmen Celis / Gricelis Martínez / Juan B. De Sanctis / Soňa Gurská / Petr Džubák / Marián Hajdůch / Ali Mijoba / Yael García / Xenón Serrano / Nahum Herrera / Jhonny Correa-Abril / Yonathan Parra / Jorge Ángel / Hegira Ramírez / Jaime E. Charris

    Molecules, Vol 27, Iss 5626, p

    2022  Volume 5626

    Abstract: The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of these pathologies invites us to search for new molecules with these characteristics. In this ... ...

    Abstract The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of these pathologies invites us to search for new molecules with these characteristics. In this research, we report 16 synthetic chalcone derivatives that were investigated for leishmanicidal and trypanocidal activities as well as for antiproliferative potential on eight human cancers and two nontumor cell lines. The final compounds 8 – 23 were obtained using the classical base-catalyzed Claisen–Schmidt condensation. The most potent compounds as parasiticidal were found to be 22 and 23 , while compounds 18 and 22 showed the best antiproliferative activity and therapeutic index against CCRF-CEM, K562, A549, and U2OS cancer cell lines and non-toxic VERO, BMDM, MRC-5, and BJ cells. In the case of K562 and the corresponding drug-resistant K562-TAX cell lines, the antiproliferative activity has shown a more significant difference for compound 19 having 10.3 times higher activity against the K562-TAX than K562 cell line. Flow cytometry analysis using K562 and A549 cell lines cultured with compounds 18 and 22 confirmed the induction of apoptosis in treated cells after 24 h. Based on the structural analysis, these chalcones represent new compounds potentially useful for Leishmania , Trypanosoma cruzi , and some cancer treatments.
    Keywords Leishmaniasis ; Trypanosoma cruzi ; cancer ; apoptosis ; chalcone ; Organic chemistry ; QD241-441
    Subject code 500
    Language English
    Publishing date 2022-08-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    More links

    Kategorien

To top