Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm, characterized by the occurrence of the t(9;22)(q34;q11) translocation. First-line therapy for CML consists of treatment with imatinib mesylate, which selectively inhibits the BCR-ABL protein by competing for its ATP-binding site. Adenine nucleotide signaling is modulated by the ectonucleotidases and this pathway is related to tumorigenic processes.
View Article and Find Full Text PDFThe genus (Hypericaceae) is a recognized source of therapeutic agents, being some species widely used due to their wound healing properties. In a previous study, south Brazilian species and demonstrated potential to induce proliferation of keratinocytes. In the present study, the effect of phloroglucinol derivatives isolated from on cell proliferation of human keratinocytes, fibroblasts and stem cells was investigated.
View Article and Find Full Text PDFMethotrexate is a folic acid antagonist and its incorporation into nanoformulations is a promising strategy to increase the drug antiproliferative effect on human breast cancer cells by overexpressing folate receptors. To evaluate the efficiency and selectivity of nanoformulations containing methotrexate and its diethyl ester derivative, using two mechanisms of drug incorporation (encapsulation and surface functionalization) in the in vitro cellular uptake and antiproliferative activity in non-tumoral immortalized human keratinocytes (HaCaT) and in human breast carcinoma cells (MCF-7). Methotrexate and its diethyl ester derivative were incorporated into multiwall lipid-core nanocapsules with hydrodynamic diameters lower than 160 nm and higher drug incorporation efficiency.
View Article and Find Full Text PDFDoxorubicin (Dox) clinical use is limited by dose-related cardiomyopathy, becoming more prevalent with increasing cumulative doses. Previously, we developed Dox-loaded lipid-core nanocapsules (Dox-LNC) and, in this study, we hypothesized that self-assembling and interfacial reactions could be used to obtain arginylglycylaspartic acid (RGD)-surface-functionalized-Dox-LNC, which could target tumoral cells overexpressing αvβ3 integrin. Human breast adenocarcinoma cell line (MCF-7) and human glioblastoma astrocytoma (U87MG) expressing different levels of αvβ3 integrin were studied.
View Article and Find Full Text PDFThe data presented here are related to the research paper entitled "PCL--P(MMA--DMAEMA) new triblock copolymer for novel pH-sensitive nanocapsules intended for drug delivery to tumors" by Franco et al. [1]. Characterization data of PCL-diol, macroinitiator Br-PCL-Br, homopolymers (PMMA and PDMAEMA) and copolymers (batch 1 and batch 2) analyzed by FTIR, SEC and NMR, as well as, characterization of PCL-NS formulation by laser diffraction and DLS analysis, initial nanocapsule formulations and 1-NC and 2-NC formulations, including hydrodynamic diameter at different pH media, and DMSO cytotoxicity.
View Article and Find Full Text PDFCancer is a major public health problem in the world, being breast cancer the most frequent cancer affecting women. Despite advances in detection and treatment, mortality rates remain high. Therefore, new approaches for breast cancer treatments are necessary.
View Article and Find Full Text PDFPurpose: This study was conducted a promising approach to surface functionalization developed for lipid-core nanocapsules and the merit to pursue new strategies to treat solid tumors.
Methods: Bromelain-functionalized multiple-wall lipid-core nanocapsules (Bro-MLNC-Zn) were produced by self-assembling following three steps of interfacial reactions. Physicochemical and structural characteristics, in vitro proteolytic activity (casein substrate) and antiproliferative activity (breast cancer cells, MCF-7) were determined.
In this study, a phytochemical and biological investigation on five South Brazilian Hypericum species (Hypericum caprifoliatum, Hypericum carinatum, Hypericum connatum, Hypericum myrianthum, and Hypericum polyanthemum) was carried out. The phloroglucinol-enriched fractions (PEF) of the flowering aerial parts were analyzed by high-performance liquid chromatography for the content of uliginosin A (1), japonicin A (2), uliginosin B (3), hyperbrasilol B (4), and the three benzopyrans, that is, 6-isobutyryl-5,7-dimethoxy-2,2-dimethyl-benzopyran (HP1) (5), 7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethyl-benzopyran (HP2) (6), and 5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethyl-benzopyran (HP3) (7). After chemical characterization, the PEF were assayed for cell proliferation on human keratinocyte cell line by MTT.
View Article and Find Full Text PDFDipeptidyl peptidase IV (DPPIV/CD26) is a multifunctional protein with intrinsic peptidase activity that inactivates or degrades some bioactive peptides. It is the main cellular binding protein for ecto-adenosine deaminase and interacts with extracellular matrix proteins, besides participating in different signaling pathways. Due to these multiple functions, DPPIV/CD26 has been shown to be closely related to the tumor process.
View Article and Find Full Text PDFEthnopharmacological Relevance: Wounds are normally resolved in a few days, but chronic wounds represent a major burden because of economic and social factors. Thereby, the search for new agents is ongoing and natural products become a great target. Also, Brazil as a consumer of herbal medicines with rich social diversity is promising for ethnopharmacological studies.
View Article and Find Full Text PDFDipeptidyl peptidase IV (DPPIV/CD26) is a transmembrane glycoprotein that inactivates or degrades some bioactive peptides and chemokines. For this reason, it regulates cell proliferation, migration and adhesion, showing its role in cancer processes. This enzyme is found mainly anchored onto the cell membrane, although it also has a soluble form, an enzymatically active isoform.
View Article and Find Full Text PDFCancer stem cells (CSCs) comprise a tumor subpopulation responsible for tumor maintenance, resistance to chemotherapy, recurrence and metastasis. The identification of this cell group is very important, but there is still no consensus on its characterization. Several CSC markers have been described, like CD133, CD24, CD44 and ALDH1, but more research to identify new markers to facilitate the identification of CSC in a heterogeneous tumoral mass is required.
View Article and Find Full Text PDFIn cervical cancer, HPV infection and disruption of mechanisms involving cell growth, differentiation, and apoptosis are strictly linked with tumor progression and invasion. Tumor microenvironment is ATP and adenosine rich, suggesting a role for purinergic signaling in cancer cell growth and death. Here we investigate the effect of extracellular ATP on human cervical cancer cells.
View Article and Find Full Text PDFRaloxifene hydrochloride (RH) is considered to be an antiproliferative agent of mammary tissue. The aim of this study was to investigate the effect of the encapsulation of RH in polymeric nanocapsules with anionic or cationic surface on its release profile and antiproliferative activity. They were prepared by interfacial deposition of preformed polymer, followed by wide physicochemical characterization.
View Article and Find Full Text PDFCervical cancer is the third most frequent cancer in women worldwide. Adenine nucleotide signaling is modulated by the ectonucleotidases that act in sequence, forming an enzymatic cascade. Considering the relationship between the purinergic signaling and cancer, we studied the E-NTPDases, ecto-5'-nucleotidase, and E-NPPs in human cervical cancer cell lines and keratinocytes.
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