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2.
PLoS One ; 18(8): e0289370, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37552704

RESUMEN

The male genitalia of Surazomus algodoal Ruiz & Valente, 2017 are described. Since this is the first attempt to describe male genitalia in the schizomids, we propose new terminology to describe the sclerites of the male genital chamber in the order. We believe that the male genitalia may provide a large set of characters for taxonomic research in schizomids, as the female genitalia have proven to do. The setae and other cuticular structures were investigated using light and scanning electron microscopy (SEM). The female of S. algodoal is described for the first time, including the genitalia, and we highlight the sexual dimorphism present in the species. We also present descriptions of: 1) microtrichia, with respect to their presence/length/distribution, 2) cuticular sensilla, glandular openings and other cuticular structures, proposing new terminology, 3) setae of the pedipalpal trochanter and tarsus. Some changes on the terminology of setae of pedipalpal tibia are also given. These advances may be useful for description in other schizomids. The pygidial glands, mostly ignored in modern papers, were assessed and commented upon.


Asunto(s)
Arácnidos , Animales , Femenino , Masculino , Genitales Masculinos , Genitales , Sensilos/ultraestructura , Microscopía Electrónica de Rastreo
3.
Nanoscale ; 15(17): 7854-7869, 2023 May 04.
Artículo en Inglés | MEDLINE | ID: mdl-37060148

RESUMEN

Several vaccines against COVID-19 use a recombinant SARS-CoV-2 receptor-binding domain (RBD) as antigen, making the purification of this protein a key step in their production. In this work, citrate-coated magnetic iron oxide nanoparticles were evaluated as nano adsorbents in the first step (capture) of the purification of recombinant RBD. The nanoparticles were isolated through coprecipitation and subsequently coated with sodium citrate. The citrate-coated nanoparticles exhibited a diameter of 10 ± 2 nm, a hydrodynamic diameter of 160 ± 3 nm, and contained 1.9 wt% of citrate. The presence of citrate on the nanoparticles' surface was confirmed through FT-IR spectra and thermogravimetric analysis. The crystallite size (10.1 nm) and the lattice parameter (8.3646 Å) were determined by X-ray diffraction. In parallel, RBD-containing supernatant extracted from cell culture was exchanged through ultrafiltration and diafiltration into the adsorption buffer. The magnetic capture was then optimized using different concentrations of nanoparticles in the purified supernatant, and we found 40 mg mL-1 to be optimal. The ideal amount of nanoparticles was assessed by varying the RBD concentration in the supernatant (between 0.113 mg mL-1 and 0.98 mg mL-1), which resulted in good capture yields (between 83 ± 5% and 94 ± 4%). The improvement of RBD purity after desorption was demonstrated by SDS-PAGE and RP-HPLC. Furthermore, the magnetic capture was scaled up 100 times, and the desorption was subjected to chromatographic purifications. The obtained products recognized anti-RBD antibodies and bound the ACE2 receptor, proving their functionality after the developed procedure.


Asunto(s)
COVID-19 , SARS-CoV-2 , Humanos , Vacunas contra la COVID-19 , Ácido Cítrico , Espectroscopía Infrarroja por Transformada de Fourier , Citratos
4.
Microorganisms ; 10(8)2022 Aug 22.
Artículo en Inglés | MEDLINE | ID: mdl-36014102

RESUMEN

Infections remain a major cause of morbidity and mortality among hematopoietic stem cell transplant (HSCT) recipients. Unlike Epstein-Barr Virus (EBV) and Human Cytomegalovirus (HCMV), Human Herpesvirus (HHV) 6, HHV7 and HHV8 are not routinely monitored in many centers, especially in the pediatric population of low-medium income countries. We screened EBV, HCMV, HHV6, HHV7 and HHV8 in 412 leukocytes-plasma paired samples from 40 pediatric patients assisted in a tertiary hospital in Mexico. Thirty-two underwent allo-HSCT, whereas eight received auto-HSCT. Overall viral detection frequencies in allo- and auto-HSCT were: EBV = 43.7% and 30.0%, HCMV = 5.0% and 6.7%, HHV6 = 7.9% and 20.0% and HHV7 = 9.7% and 23.3%. HHV8 was not detected in any sample. Interestingly, HHV6 and HHV7 were more frequent in auto-HSCT, and HHV6 was observed in all episodes of multiple detection in auto-HSCT patients. We found EBV DNA in plasma samples, whereas HCMV, HHV6 and HHV7 DNA were predominantly observed in leukocytes, indicative of their expansion in cellular compartments. We also found that IL-1ß, IL-2, IL-6 and IL-8 were significantly increased in episodes in which multiple viruses were simultaneously detected, and samples positive for EBV DNA and graft-versus-host disease had a further increase of IL-1ß and IL-8. In conclusion, the EBV, HCMV, HHV6 and HHV7 burdens were frequently detected in allo- and auto-HSCT, and their presence associated with systemic inflammation.

5.
Curr Zool ; 68(1): 81-92, 2022 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-35169631

RESUMEN

Males can control female reproduction using genital plugs to impede access by rivals. In social bees, ants, and wasps, plugging may involve traumatic mating, with females being harmed. In stingless bees, chances are that plugs may promote ovarian activan, and are thought to ensure single mating-a general tendency among the social Hymenoptera. However, understanding on relationships between mating plugs, traumatic mating, and mating systems in stingless bees remains limited. To address this, we (1) compared mated queens of 7 Neotropical species to understand the patterns of copulatory marks in females and (2) compared pre- and post-mating genitalia of males and females in Melipona fasciculata to depict plug functional morphology. Data revealed an unprecedented consequence of mating in stingless bees: the characteristic marks left by mating plugs on female abdomens and the inferences that can be made from them. To our surprise, in 1 species M. fasciculata we found that queens retain the plug long after mating, and may carry it for the rest of their lives. All the other 6 species retained the plug for only a short period. Remated queens were only found in M. seminigra, whose multiple copulatory marks match previous findings of polyandry in this species. Our study shows that queens can remate, and suggests that male genital morphology may determine in part the time persistence of plugs. We conclude that traumatic mating plugs do not fully prevent remating in stingless bees and that mating systems are not uniform in this group. Nonetheless, exceptional cases of facultative polyandry in social insects-for example, when mating plugs fail-may confirm a general tendency for single mating in close link with efficient mating plugs.

6.
Int J Mol Sci ; 23(3)2022 Feb 02.
Artículo en Inglés | MEDLINE | ID: mdl-35163649

RESUMEN

Yin-Yang transcription factor 1 (YY1) is involved in tumor progression, metastasis and has been shown to be elevated in different cancers, including leukemia. The regulatory mechanism underlying YY1 expression in leukemia is still not understood. Bioinformatics analysis reveal three Hypoxia-inducible factor 1-alpha (HIF-1α) putative binding sites in the YY1 promoter region. The regulation of YY1 by HIF-1α in leukemia was analyzed. Mutation of the putative YY1 binding sites in a reporter system containing the HIF-1α promoter region and CHIP analysis confirmed that these sites are important for YY1 regulation. Leukemia cell lines showed that both proteins HIF-1α and YY1 are co-expressed under hypoxia. In addition, the expression of mRNA of YY1 was increased after 3 h of hypoxia conditions and affect several target genes expression. In contrast, chemical inhibition of HIF-1α induces downregulation of YY1 and sensitizes cells to chemotherapeutic drugs. The clinical implications of HIF-1α in the regulation of YY1 were investigated by evaluation of expression of HIF-1α and YY1 in 108 peripheral blood samples and by RT-PCR in 46 bone marrow samples of patients with pediatric acute lymphoblastic leukemia (ALL). We found that the expression of HIF-1α positively correlates with YY1 expression in those patients. This is consistent with bioinformatic analyses of several databases. Our findings demonstrate for the first time that YY1 can be transcriptionally regulated by HIF-1α, and a correlation between HIF-1α expression and YY1 was found in ALL clinical samples. Hence, HIF-1α and YY1 may be possible therapeutic target and/or biomarkers of ALL.


Asunto(s)
Subunidad alfa del Factor 1 Inducible por Hipoxia/metabolismo , Leucemia-Linfoma Linfoblástico de Células Precursoras/metabolismo , Factor de Transcripción YY1/metabolismo , Adolescente , Línea Celular Tumoral , Niño , Preescolar , Regulación Neoplásica de la Expresión Génica , Humanos , Lactante , Recién Nacido
7.
Zootaxa, v. 5124, n. 4, p. 431–457, abr. 2022
Artículo en Inglés | Sec. Est. Saúde SP, SESSP-IBPROD, Sec. Est. Saúde SP | ID: bud-4299

RESUMEN

Huriini Simon, 1901 currently consists of six genera and 17 species, distributed exclusively in South America. In this work, the huriine genus Guriurius Marta, Bustamante, Ruiz & Rodrigues, gen. nov. is proposed with two new species herein described: Guriurius minuano Marta, Bustamante, Ruiz & Rodrigues, sp. nov. (type species) and Guriurius nancyae Marta, Bustamante, Ruiz & Rodrigues, sp. nov. The female of Atelurius segmentatus Simon, 1901 is described and illustrated for the first time. Scoturius dipterioides Perger & Rubio, 2018 is transferred to Atelurius Simon, 1901 due to the morphological similarity of copulatory ducts of epigyne, and Hurius pisac Galiano, 1985 is transferred to Simonurius Galiano, 1988 due to the similarities in body shape and female genitalia. Simonurius campestratus (Simon, 1901) is synonymized with Simonurius quadratarius (Simon, 1901). The interpretation of genitalic characters in Huriini is discussed. In addition, we provide new distributional records for Admesturius bitaeniatus (Simon, 1901), Ad. mariaeugeniae Bustamante & Scioscia, 2014, Ad. schajovskoyi Galiano, 1988, At. segmentatus Simon, 1901, Scoturius tigris Simon, 1901, Hurius aeneus (Mello-Leitão, 1941), and Simonurius gladifer (Simon, 1901). Except for Urupuyu Ruiz & Maddison, 2015, all huriine genera are rediagnosed in the new context of tribe and genus composition.

9.
Zootaxa ; 5057(2): 241-259, 2021 Oct 21.
Artículo en Inglés | MEDLINE | ID: mdl-34811211

RESUMEN

Gypogyna Simon, 1900 is revised. Three species are recognized and diagnosed. The type species, Gypogyna forceps Simon, 1900, is redescribed and recorded from several localities in South America. Gypogyna amazonica Ruiz sp. nov. is described based on a male from Manaus, Brazil. Gypogyna mexicana Ruiz Bustamante sp. nov. is described based on specimens of both sexes from the state of Jalisco, Mexico. In addition, some comments on cheliceral dentiton and genital morphology are discussed.


Asunto(s)
Arañas , Distribución Animal , Animales , Femenino , Masculino , Tamaño de los Órganos
11.
Medicina (B Aires) ; 81(3): 474-477, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34137713

RESUMEN

Borrelia burgdorferi infection (Lyme disease) is one of the few identifiable causes of neuralgic amyotrophy. Bilateral diaphragmatic paralysis is considered rare in borreliosis, and the pattern of long-term recovery of diaphragm function is also uncertain. Transdiaphragmatic pressure is the gold standard for diagnosis of bilateral diaphragmatic paralysis, a study that has been reported on few occasions. We present a case of neuralgic amyotrophy associated with Borrelia infection and bilateral diaphragmatic paralysis that provides a detailed follow-up of the spirometric evolution, of the maximum static pressures in the mouth and of transdiaphragmatic pressure from the onset of symptoms and the long term. This case allows us to know one of the possible evolutionary profiles of diaphragmatic dysfunction in neuralgic amyotrophy due to borreliosis.


La infección por Borrelia burgdorferi (enfermedad de Lyme) es una de las pocas causas identificables de amiotrofia neurálgica. La parálisis diafragmática bilateral es considerada rara en la borreliosis y el patrón de recuperación a largo plazo de la función del diafragma también es incierto. La presión transdiafragmática es el patrón de oro para el diagnóstico de parálisis diafragmática bilateral, un estudio que ha sido informado en pocas ocasiones. Se presenta un caso de amiotrofia neurálgica asociado a infección por Borrelia y parálisis diafragmática bilateral, que aporta un seguimiento detallado de la evolución espirométrica, de las presiones estáticas máximas en la boca y de la presión transdiafragmática desde el inicio de los síntomas y a largo plazo. Este caso permite conocer uno de los posibles perfiles evolutivos de la disfunción diafragmática en la amiotrofia neurálgica por borreliosis.


Asunto(s)
Neuritis del Plexo Braquial , Neuroborreliosis de Lyme , Parálisis Respiratoria , Diafragma/diagnóstico por imagen , Estudios de Seguimiento , Humanos , Neuroborreliosis de Lyme/complicaciones , Neuroborreliosis de Lyme/diagnóstico , Parálisis Respiratoria/diagnóstico , Parálisis Respiratoria/etiología
12.
Medicina (B.Aires) ; Medicina (B.Aires);81(3): 474-477, jun. 2021. graf
Artículo en Inglés | LILACS | ID: biblio-1346489

RESUMEN

Abstract Borrelia burgdorferi infection (Lyme disease) is one of the few identifiable causes of neuralgic amyotrophy (AN). Bilateral diaphragmatic paralysis is considered rare in borreliosis, and the pattern of long-term recovery of diaphragm function is also uncertain. Transdiaphragmatic pressure is the gold standard for diagnosing bilateral diaphragmatic paralysis, a study that has been reported on a few occasions. We pres ent a case of AN associated with borrelia infection and bilateral diaphragmatic paralysis that provides a detailed follow-up of the spirometric evolution, the maximum static pressures in the mouth, and the transdiaphragmatic pressure from the onset of symptoms and in the long term. This case allows us to know one of the possible evolutionary profiles of diaphragmatic dysfunction in AN due to borreliosis.


Resumen La infección por Borrelia burgdorferi (enfermedad de Lyme) es una de las pocas causas identificables de amiotrofia neurálgica. La parálisis diafragmática bilateral es considerada rara en la borreliosis y el patrón de recuperación a largo plazo de la función del diafragma también es incierto. La presión transdiafragmática es el patrón de oro para el diagnóstico de parálisis diafragmática bilateral, un estudio que ha sido informado en pocas ocasiones. Se presenta un caso de amiotrofia neurálgica asociado a infección por Borrelia y parálisis diafrag mática bilateral, que aporta un seguimiento detallado de la evolución espirométrica, de las presiones estáticas máximas en la boca y de la presión transdiafragmática desde el inicio de los síntomas y a largo plazo. Este caso permite conocer uno de los posibles perfiles evolutivos de la disfunción diafragmática en la amiotrofia neurálgica por borreliosis.


Asunto(s)
Humanos , Parálisis Respiratoria/diagnóstico , Parálisis Respiratoria/etiología , Neuritis del Plexo Braquial , Neuroborreliosis de Lyme/complicaciones , Neuroborreliosis de Lyme/diagnóstico , Diafragma/diagnóstico por imagen , Estudios de Seguimiento
13.
Stem Cell Rev Rep ; 17(5): 1590-1606, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-33728560

RESUMEN

Accumulating evidence strongly indicates that the presence of cancer stem cells (CSCs) leads to the emergence of worse clinical scenarios, such as chemo- and radiotherapy resistance, metastasis, and cancer recurrence. CSCs are a highly tumorigenic population characterized by self-renewal capacity and differentiation potential. Thus, CSCs establish a hierarchical intratumor organization that enables tumor adaptation to evade the immune response and resist anticancer therapy. YY1 functions as a transcription factor, RNA-binding protein, and 3D chromatin regulator. Thus, YY1 has multiple effects and regulates several molecular processes. Emerging evidence indicates that the development of lethal YY1-mediated cancer phenotypes is associated with the presence of or enrichment in cancer stem-like cells. Therefore, it is necessary to investigate whether and to what extent YY1 regulates the CSC phenotype. Since CSCs mirror the phenotypic behavior of stem cells, we initially describe the roles played by YY1 in embryonic and adult stem cells. Next, we scrutinize evidence supporting the contributions of YY1 in CSCs from a number of various cancer types. Finally, we identify new areas for further investigation into the YY1-CSCs axis, including the participation of YY1 in the CSC niche.


Asunto(s)
Células Madre Neoplásicas , Carcinogénesis/patología , Humanos , Recurrencia Local de Neoplasia/patología , Células Madre Neoplásicas/metabolismo , Factores de Transcripción/metabolismo , Factor de Transcripción YY1/genética , Factor de Transcripción YY1/metabolismo
14.
Zootaxa ; 4899(1): zootaxa.4899.1.6, 2020 Dec 30.
Artículo en Inglés | MEDLINE | ID: mdl-33756828

RESUMEN

Five new species of thiodinines are described: Atomosphyrus wandae sp. nov. (♂, from state of Piauí, Brazil); Cyllodania marietae sp. nov. (♂♀, from Ecuador); Tartamura turbo sp. nov. (♂♀, from state of Pará, Brazil); Thiodina camilae sp. nov. (♂♀, from the Dominican Republic); and Thiodina tyrioni sp. nov. (♂♀, from Arizona, U.S.A.). New records of Thiodina firme Bustamante Ruiz, 2017, Tartamura adfectuosa (Galiano, 1977), T. agatelin Bustamante Ruiz, 2017 and T. huao Bustamante Ruiz, 2017 are provided.


Asunto(s)
Arañas , Animales
15.
Zootaxa ; 4899(1): zootaxa.4899.1.16, 2020 Dec 30.
Artículo en Inglés | MEDLINE | ID: mdl-33756838

RESUMEN

The Neotropical genus Marma Simon, 1902 is revised. With exception of the holotype of M. femella (Caporiacco, 1955), which was redescribed in previous work, all the other species of the genus were revised based on their types. The type species, M. baeri Simon, 1902, and M. nigritarsis (Simon, 1900) are redescribed based on newly collected specimens. The third and last species presently listed in the World Spider Catalog, M. femella, is confirmed as valid. Two species presently considered synonyms of M. nigritarsis are revalidated: M. rosea (Mello-Leitão, 1941) and M. argentina (Mello-Leitão, 1941). Two species are synonymized: Thysema dorae Mello-Leitão, 1944, syn. nov. with Ocnotelus argentinus Mello-Leitão, 1941 and Paralophostica centralis Soares Camargo, 1948, syn. nov. with Agelista rosea Mello-Leitão, 1941. Pseudoamphidraus variegatus Caporiacco, 1947 and M. trifidocarinata Caporiacco, 1947 are confirmed as synonyms of M. nigritarsis. Six new species from northern/northeastern Brazil are described: M. abaira sp. nov. (♀), M. linae sp. nov. (♂♀), M. pipa sp. nov. (♂♀), M. sinuosa sp. nov. (♂♀), M. spelunca sp. nov. (♂♀) and M. wesolowskae sp. nov. (♂♀). Also, the male of M. argentina is described for the first time. We give new diagnostic illustrations and updated distribution records for all the species of the genus.


Asunto(s)
Arañas , Distribución Animal , Animales , Masculino
16.
Zootaxa ; 4563(3): zootaxa.4563.3.3, 2019 Mar 04.
Artículo en Inglés | MEDLINE | ID: mdl-31716529

RESUMEN

Seven new species of Amphidraus Simon, 1900 are described from Brazil: A. araripe sp. nov. (♂♀), A. boomerang sp. nov. (♂), A. cornipalpis sp. nov. (♂♀), A. draconitupan sp. nov. (♂♀), A. manauara sp. nov. (♂♀), A. sacrificatus sp. nov. (♂) and A. shenlong sp. nov. (♂). Morphological variation in the male palp of A. draconicaudatus Salgado Ruiz, 2017 and A. caxiuanan Salgado Ruiz, 2017 is discovered and evaluated.


Asunto(s)
Arañas , Animales , Brasil , Masculino
17.
Zootaxa ; 4658(1): zootaxa.4658.1.5, 2019 Aug 21.
Artículo en Inglés | MEDLINE | ID: mdl-31716759

RESUMEN

In this paper we redescribe the type species of Mago O. Pickard-Cambridge, M. intentus O. Pickard-Cambridge, and describe Mago brimodes Ruiz Maddison sp. nov. from Ecuador. Based on both morphological features and the 16SND1 gene region, we concluded that the larger spiders traditionally identified as Mago, such as Mago acutidens Simon and related species, are not closely related to the small dark M. intentus (type species) and M. brimodes. Matinta Ruiz Maddison gen. nov. is therefore proposed to hold most species previously included in Mago. The following species are transferred from Mago to the new genus: Matinta acutidens (Simon, 1900) comb. nov. (type species), Matinta apophysis (Costa Ruiz, 2017) comb. nov., Matinta balbina (Patello Ruiz, 2014) comb. nov., Matinta chickeringi (Caporiacco, 1954) comb. nov., Matinta delicata (Patello Ruiz, 2014) comb. nov., Matinta fasciata (Mello-Leitão, 1940) comb. nov., Matinta fonsecai (Soares Camargo, 1948) comb. nov., Matinta furcata (Costa Ruiz, 2017) comb. nov., Matinta jurutiensis (Patello Ruiz, 2014) comb. nov., Matinta longidens (Simon, 1900) comb. nov., Matinta mimica (Costa Ruiz, 2017) comb. nov., Matinta opiparis (Simon, 1900) comb. nov., Matinta pardo (Costa Ruiz, 2017) comb. nov., Matinta procax (Simon, 1900) comb. nov., Matinta saperda (Simon, 1900) comb. nov., Matinta silvae (Crane, 1943) comb. nov., Matinta similis (Patello Ruiz, 2014) comb. nov., Matinta steindachneri (Taczanowski, 1878) comb. nov. and Matinta vicana (Simon, 1900) comb. nov. Mago dentichelis Crane, 1949 is transferred to Noegus Simon.


Asunto(s)
Arañas , Distribución Animal , Estructuras Animales , Animales , Tamaño Corporal , Ecuador , Tamaño de los Órganos
18.
PLoS One ; 14(3): e0213268, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30893324

RESUMEN

Surazomus saturninoae sp. nov. is described from eastern Amazon. The male has a pentagonal flagellum, similar to those of three other species in the genus. These four species are herein gathered as the arboreus-group of Surazomus. We present a brief synopsis of chaetotaxy description in hubbardiines and several homology proposals for the flagellum of the species in the arboreus-group: the posterior lobes may be homologous to the lateral lobes of hubbardiine species with trilobed flagella; the setal brush with 4-5 setae on the posterior lobe may be composed of one Dl2 seta and enlarged lobular microsetae; the single, median posterior coupling pocket may be homologous to the pair of posterior pockets seen in other hubbardiines; the single, median anterior coupling pocket may be homologous to the pair of pockets on the anterior border of the flagellum seen in other hubbardiines. Based on the morphology of these pockets and the chelicerae within Surazomus, we discuss the anchoring mechanism during the mating march.


Asunto(s)
Arácnidos/clasificación , Arácnidos/fisiología , Flagelos/fisiología , Reproducción , Sensilos/fisiología , Distribución Animal , Estructuras Animales/anatomía & histología , Estructuras Animales/crecimiento & desarrollo , Animales , Arácnidos/anatomía & histología , Femenino , Masculino , Sensilos/anatomía & histología
19.
Anticancer Agents Med Chem ; 19(6): 760-771, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30451119

RESUMEN

BACKGROUND: Some reports have demonstrated the role of the G Protein-coupled Estrogen Receptor (GPER) in growth and proliferation of breast cancer cells. OBJECTIVE: In an effort to develop new therapeutic strategies against breast cancer, we employed an in silico study to explore the binding modes of tetrahydroquinoline 2 and 4 to be compared with the reported ligands G1 and G1PABA. METHODS: This study aimed to design and filter ligands by in silico studies determining their Lipinski's rule, toxicity and binding properties with GPER to achieve experimental assays as anti-proliferative compounds of breast cancer cell lines. RESULTS: In silico studies suggest as promissory two tetrahydroquinoline 2 and 4 which contain a carboxyl group instead of the acetyl group (as is needed for G1 synthesis), which add low (2) and high hindrance (4) chemical moieties to explore the polar, hydrophobic and hindrance effects. Docking and molecular dynamics simulations of the target compounds were performed with GPER to explore their binding mode and free energy values. In addition, the target small molecules were synthesized and assayed in vitro using breast cancer cells (MCF-7 and MDA-MB-231). Experimental assays showed that compound 2 decreased cell proliferation, showing IC50 values of 50µM and 25µM after 72h of treatment of MCF-7 and MDA-MB-231 cell lines, respectively. Importantly, compound 2 showed a similar inhibitory effect on proliferation as G1 compound in MDA-MB-231 cells, suggesting that both ligands reach the GPER-binding site in a similar way, as was demonstrated through in silico studies. CONCLUSION: A concentration-dependent inhibition of cell proliferation occurred with compound 2 in the two cell lines regardless of GPER.


Asunto(s)
Antineoplásicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Quinolinas/farmacología , Receptores de Estrógenos/antagonistas & inhibidores , Receptores Acoplados a Proteínas G/antagonistas & inhibidores , Antineoplásicos/síntesis química , Antineoplásicos/química , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/patología , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Humanos , Modelos Moleculares , Estructura Molecular , Quinolinas/síntesis química , Quinolinas/química , Receptores de Estrógenos/metabolismo , Receptores Acoplados a Proteínas G/metabolismo , Relación Estructura-Actividad , Termodinámica , Células Tumorales Cultivadas
20.
Artículo en Inglés | MEDLINE | ID: mdl-29861776

RESUMEN

Plants are a significant reservoir of cytotoxic agents, including compounds with the ability to interfere with multidrug-resistant (MDR) cells. With the aim of finding promising candidates for chemotherapy, 91 native and naturalized plants collected from the central region of Argentina were screened for their cytotoxic effect toward sensitive and MDR P-glycoprotein (P-gp) overexpressing human leukemia cells by means of MTT assays. The ethanol extracts obtained from Aldama tucumanensis, Ambrosia elatior, Baccharis artemisioides, Baccharis coridifolia, Dimerostemma aspilioides, Gaillardia megapotamica, and Vernonanthura nudiflora presented outstanding antiproliferative activity at 50 µg/mL, with inhibitory values from 93 to 100%, when tested on the acute lymphoblastic leukemia (ALL) cell line CCRF-CEM and the resistant derivative CEM-ADR5000, while 70-90% inhibition was observed against the chronic myelogenous leukemia (CML) cell K562 and its corresponding resistant subline, Lucena 1. Subsequent investigation showed these extracts to possess marked cytotoxicity with IC50 values ranging from 0.37 to 29.44 µg/mL, with most of them being below 7 µg/mL and with ALL cells, including the drug-resistant phenotype, being the most affected. G. megapotamica extract found to be one of the most effective and bioguided fractionation yielded helenalin (1). The sesquiterpene lactone displayed IC50 values of 0.63, 0.19, 0.74, and 0.16 µg/mL against K562, CCRF-CEM, Lucena 1, and CEM/ADR5000, respectively. These results support the potential of these extracts as a source of compounds for treating sensitive and multidrug-resistant leukemia cells and support compound 1 as a lead for developing effective anticancer agents.

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