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1.
Polymers (Basel) ; 16(15)2024 Jul 24.
Artigo em Inglês | MEDLINE | ID: mdl-39125132

RESUMO

The present study aimed to fabricate innovative fibrous materials with various biological activities from poly(3-hydroxybutyrate), sodium hyaluronate (HA), chitosan (Ch), Melissa officinalis (MO), Hypericum perforatum (HP) extract, or a combination of both extracts. Electrospinning or electrospinning followed by dip coating and the subsequent formation of a polyelectrolyte complex were the methods used to prepare these materials. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), thermogravimetric analysis (TGA), and attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) were applied for investigating the morphology of materials, their thermal characteristics, and their surface chemical composition. The composition and design of the mats had an influence on the in vitro release behavior of the main bioactive compounds present in the MO and HP extracts incorporated in the materials. It was found that as-created materials comprising a combination of both extracts and a Ch/HA complex exerted higher antioxidant activity than that of (non-)coated MO-containing mats and Ch/HA-coated mats containing HP. The novel materials manifested antibacterial efficacy towards the pathogenic bacteria S. aureus and E. coli, as evidenced by the performed microbiological screening. Furthermore, the mats possessed a great growth inhibitory effect on HeLa cancer cells but had a less pronounced effect on the growth of normal mouse BALB/3T3 fibroblasts. The loading of both extracts in the mats and the formation of coating led to the enhancement of the in vitro anticancer and antibacterial activities of the materials. Thus, the novel materials have potential for use in local cancer therapy as well as for use as wound dressings.

2.
Polymers (Basel) ; 15(14)2023 Jul 24.
Artigo em Inglês | MEDLINE | ID: mdl-37514529

RESUMO

Novel fibrous materials with diverse biological properties containing a model drug of the 8-hydroxyquinoline group-5-amino-8-hydroxyquinoline (5A8Q)-were fabricated using a one-pot method by electrospinning poly(vinyl alcohol) (PVA)/carboxymethyl cellulose (CMC)/5A8Q solutions. Experiments were performed to prepare Cu2+ (Fe3+) complexes of the crosslinked PVA/CMC/5A8Q materials. The formation of complexes was proven by using scanning electron microscopy (SEM), attenuated total reflection Fourier-transform infrared (ATR-FTIR) spectroscopy, energy-dispersive X-ray spectroscopy (EDX) and X-ray photoelectron spectroscopy (XPS). The release of 5A8Q and 5A8Q.Cu2+ (Fe3+) was studied and their in vitro release profiles were mostly impacted by the hydrophilic/hydrophobic properties of the materials. The performed microbiological assays revealed that fibrous materials containing 5A8Q and their complexes exhibited good antibacterial and antifungal efficacy. Their activity was stronger against bacteria S. aureus than against bacteria E. coli and fungi C. albicans. Cell viability tests using MTT showed that the presence of 5A8Q and its complexes in the fibrous materials resulted in a significant decrease in the HeLa and MCF-7 cancer cell viability for the various times of cell incubation. Moreover, the observed cytotoxicity of the mats against cancer cells was greater than that against non-cancer HaCaT keratinocytes. All these properties make the novel materials potential candidates for the design of wound healing materials and as drug delivery systems for local therapy of cervical and breast cancer.

3.
Biomedicines ; 11(6)2023 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-37371641

RESUMO

Hemocyanins are oxygen-transporting glycoproteins in the hemolymph of some invertebrate species that attracted scientific interest as potential anticancer agents. The present study aims to assess the in vitro and in vivo anticancer activity of hemocyanins isolated from Helix aspersa, Helix lucorum, and Rapana venosa in the Graffi myeloid tumor model. The in vitro antitumor activity of the hemocyanins was determined by a MTT test and cytomorphological analysis by fluorescent and transmission electron microscopy. The in vivo effects of the hemocyanins were examined in hamsters transplanted with Graffi tumor. The serum antibody titers against the tested hemocyanins and tumor antigen were determined by ELISA. Histopathological assessment of the morphological features related to antitumor effect, immune system response, and toxicity in some internal organs was performed. The results of in vitro studies indicated that the tested hemocyanins induced significant antiproliferative and apoptogenic effects. The in vivo investigations demonstrated a protective antitumor effect, expressed in reduced transplantability, suppression of tumor growth and metastasis, reduced mortality, prolonged survival time, and absence of toxic side effects. The present study indicated that the antitumor activity of the studied hemocyanins was due to both immune stimulation and direct effects on the tumor cells, and they displayed their potential as therapeutic agents against hematological malignances.

4.
Antioxidants (Basel) ; 12(6)2023 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-37371973

RESUMO

A new type of fibrous mat based on a cellulose derivative-cellulose acetate (CA) or CA and water-soluble polymers (polyvinylpyrrolidone, PVP or poly(vinyl alcohol), PVA)-loaded with the model drug 5-nitro-8-hydroxyquinoline (5N) was fabricated via electrospinning or electrospinning in conjunction with electrospraying. Scanning electron microscopy (SEM), X-ray diffraction analysis (XRD), Fourier-transform infrared spectroscopy (FTIR), water contact angle measurements and ultraviolet-visible spectroscopy (UV-Vis) were used for the complex characterization of the obtained novel material. The decoration of CA fibers with a water-soluble polymer containing the drug resulted in the facilitation of wetting and fast drug release. The 5N-containing fibrous material showed antioxidant activity. Moreover, the proposed materials' antibacterial and antifungal properties were tested against S. aureus, E. coli, P. aeruginosa and C. albicans. Well-distinguished, sterile zones with diameters above 3.5 cm were observed around all 5N-containing mats. The mats' cytotoxicity toward HeLa carcinoma cells and normal mouse BALB/c 3T3 fibroblasts was assessed. The 5N-in-CA, PVP,5N-on-(5N-in-CA) and PVA,5N-on-(5N-in-CA) fibrous mats possessed anticancer efficacies and much lower levels of toxicity against normal cells. Therefore, the as-created novel electrospun materials, which are based on polymers loaded with the drug 5N via electrospinning/electrospraying, can potentially be applied for topical wound healing and for local cancer therapy.

5.
Polymers (Basel) ; 14(24)2022 Dec 08.
Artigo em Inglês | MEDLINE | ID: mdl-36559747

RESUMO

Innovative fibrous materials from cellulose derivative, cellulose acetate (CA) and water-soluble polyether, polyethylene glycol (PEG) loaded with natural biologically active compounds (BAC), quercetin (QUE) and rutin (RUT), have been successfully fabricated by blend electrospinning and dual electrospinning. Scanning electron microscopy revealed that the mean fiber diameters of all the obtained fibers were in the nanometer range. QUE and RUT incorporated in the fibrous mats were in the amorphous state, as evidenced by the performed differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. The presence of the polyether in the developed fibrous material assisted the in vitro release of the biologically active compounds by improving the hydrophilicity and wettability of the mats. Rutin-containing fibrous materials manifest the highest antioxidative activity, as determined by the 2,2-diphenyl-1-picryl-hydrazyl-hydrate free radical method. The cytotoxicity of the fabricated novel materials was evaluated using a tumor cell line and normal mouse fibroblast cells. The mats containing QUE and QUE/RUT independent of the applied spinning method show a higher cytotoxic effect against cancer cells and 3 to 4.5 times lower cytotoxicity to a noncancer cell line. These features make the quercetin- and rutin-containing fibrous materials promising candidates for pharmaceutical, cosmetic, and biomedical use.

6.
Polymers (Basel) ; 14(22)2022 Nov 18.
Artigo em Inglês | MEDLINE | ID: mdl-36433129

RESUMO

The Schiff base derivative (Ch-8Q) of chitosan (Ch) and 8-hydroxyquinoline-2-carboxaldehyde (8QCHO) was prepared and fibrous mats were obtained by the electrospinning of Ch-8Q/polylactide (PLA) blend solutions in trifluoroacetic acid (TFA). Complexes of the mats were prepared by immersing them in a solution of CuCl2 or FeCl3. Electron paramagnetic resonance (EPR) analysis was performed to examine the complexation of Cu2+(Fe3+) in the Ch-8Q/PLA mats complexes. The morphology of the novel materials and their surface chemical composition were studied by scanning electron microscopy (SEM), attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR) and X-ray photoelectron spectroscopy (XPS). The performed microbiological screening demonstrated that in contrast to the neat PLA mats, the Ch-8Q-containing mats and their complexes were able to kill all S. aureus bacteria within 3 h of contact. These fibrous materials had efficiency in suppressing the adhesion of pathogenic bacteria S. aureus. In addition, Ch-8Q/PLA mats and their complexes exerted good anticancer efficacy in vitro against human cervical HeLa cells and human breast MCF-7 cells. The Ch-8Q-containing fibrous materials had no cytotoxicity against non-cancer BALB/c 3T3 mouse fibroblast cells. These properties render the prepared materials promising as wound dressings as well as for application in local cancer treatment.

7.
ACS Omega ; 7(41): 36403-36414, 2022 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-36278048

RESUMO

During the past years, the synthesis of polymer prodrug structures, based on natural phytochemical compounds with a great range of valuable biological properties, has become a promising solution in cancer prevention, imaging, and detection. Curcumin (Curc) remains one of the most studied natural products, due to the impressive palette of biological properties and the possibility to be easily loaded in various micro- and nanostructures and chemically modified. In this study, pegylated curcumin derivatives were prepared by a direct esterification reaction between poly(ethylene glycol)diacid (PEG of 600 g/mol molar mass, PEG600) and Curc in the presence of N,N'-dicyclohexylcarbodiimide (PEG600-Curc). The successful reaction resulted in a water-soluble stable product that was characterized by infrared spectroscopy (Fourier transform infrared (FT-IR)) and proton (1H) and carbon (13C) NMR. The effect of the pH values of buffer solutions on PEG600-Curc spectral properties (absorption and photoluminescence) was investigated by UV-vis and fluorescence spectrophotometry. Based on the biological tests, it was confirmed that PEG600-Curc exhibits cytotoxic activity against Graffi cell lines, as a function of the Curc concentration in the conjugate and the incubation time. PEG600-Curc antibacterial activity was validated in microbiological tests against pathogenic microorganisms such as Staphylococcus aureus. Most importantly, despite the covalent attachment of Curc to PEG and the slight reduction in the therapeutic index of the conjugate, both the anticancer and antimicrobial activities remain the highest reported, thus opening the gate for further, more clinically oriented studies.

8.
Macromol Biosci ; 22(6): e2200015, 2022 06.
Artigo em Inglês | MEDLINE | ID: mdl-35451564

RESUMO

Composite fibrous materials are prepared from poly(ethylene oxide) (PEO) and beeswax (BW) by single-spinneret electrospinning using chloroform as a common solvent. The obtained fibers have core-sheath-like structure, as evidenced by the water contact angle values and corroborated by the results on the elemental composition of the fiber's surface determined by X-ray photoelectron spectroscopy (XPS) and by analyses with scanning electron microscopy of fibers before and after selective extraction of PEO or BW. Furthermore, the core-sheath-like structure is proven by transmission electron microscopy. This is attributed to self-assembly of BW molecules on the surface of the formed fibers driven by the incompatibility between PEO and BW. 5-Nitro-8-hydroxyquinoline (NQ) is embedded as a model drug with antibacterial, antifungal, and anticancer properties in the PEO/BW fibrous materials. XPS analyses reveal that NQ is present on the surface of the PEO/BW/NQ materials. Using a purposely designed cell for fixation of the fibrous materials the NQ release in phosphate buffer solution with рН 7.4 is followed. The new PEO/BW/NQ fibrous materials exhibit antibacterial activity against S. aureus and E. coli, antifungal effect against C. albicans, and selective anticancer activity against HeLa (human cervical adenocarcinoma cells) and SH-4 (human melanoma cells) cell lines.


Assuntos
Polietilenoglicóis , Staphylococcus aureus , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Escherichia coli , Óxido de Etileno/farmacologia , Humanos , Polietilenoglicóis/química , Ceras
9.
Polymers (Basel) ; 13(16)2021 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-34451230

RESUMO

Novel poly(vinyl alcohol) (PVA)/chitosan (Ch)-based fibrous materials containing an ionizable model drug, 8-hydroxyquinoline-5-sulfonic acid (SQ), were successfully fabricated by electrospinning. Complexes between the components of the crosslinked PVA/Ch/SQ mats and Cu2+ and Fe3+ ions were formed. The coordination of these ions in the mats was examined by electron paramagnetic resonance spectroscopy (EPR). The microbiological screening against S. aureus and C. albicans revealed that both the incorporation of SQ in the mats and the complexation with Cu2+ and Fe3+ imparted to these materials antibacterial and antifungal activities. Moreover, the SQ-containing mats and their complexes displayed good cytotoxicity against human cervical HeLa tumor cells. The most prominent was the cytotoxicity of the Cu2+ complex of the mats. The combined antibacterial, antifungal and in vitro antitumor activities render these novel materials promising candidates for wound dressing applications and for application in the local treatment of cervical tumors.

10.
Polymers (Basel) ; 13(10)2021 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-34069809

RESUMO

Novel eco-friendly fibrous materials with complex activities from cellulose acetate and cellulose acetate/polyethylene glycol (CA,PEG) containing 5-chloro-8-hydroxyquinoline as a model drug were obtained by electrospinning. Several methods, including scanning electron microscopy, X-ray diffraction analysis, ultraviolet-visible spectroscopy, water contact angle measurements, and mechanical tests, were utilized to characterize the obtained materials. The incorporation of PEG into the fibers facilitated the drug release. The amounts of the released drug from CA/5-Cl8Q and CA,PEG/5-Cl8Q were 78 ± 3.38% and 86 ± 3.02%, respectively (for 175 min). The antibacterial and antifungal activities of the obtained materials were studied. The measured zones of inhibition of CA/5-Cl8Q and CA,PEG/5-Cl8Q mats were 4.0 ± 0.18 and 4.5 ± 0.2 cm against S. aureus and around 4.0 ± 0.15 and 4.1 ± 0.22 cm against E. coli, respectively. The complete inhibition of the C. albicans growth was detected. The cytotoxicity of the obtained mats was tested toward HeLa cancer cells, SH-4 melanoma skin cells, and mouse BALB/c 3T3 fibroblasts as well. The CA/5-Cl8Q and CA,PEG/5-Cl8Q materials exhibited anticancer activity and low normal cell toxicity. Thus, the obtained fibrous materials can be suitable candidates for wound dressing applications and for application in local cancer treatment.

11.
J Ethnopharmacol ; 267: 113519, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33137432

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Astragalus glycyphyllos L. has been extensively used in Bulgarian folk medicine as an antihypertensive, diuretic, anti-inflammatory, anti-tumour, in cases of cardiac insufficiency, renal inflammation, calculosis, etc. AIM OF THE STUDY: To evaluate the possible in vitro/in vivo anti-proliferative/anti-tumour activity of a purified saponins' mixture (PSM) obtained from the plant. MATERIALS AND METHODS: Viability and proliferative activity of the Graffi myeloid tumour cells was assessed by MTT test. The morphological alterations were visualized and analysed by fluorescent microscopy after intravital double staining. An in vivo model of Graffi tumour bearing hamsters was used to examine the influence of PSM on transplantability, tumour growth, survival and mortality as well as to observe pathomorphological changes. RESULTS: Graffi tumour cells were sensitive to purified saponins' mixture after 24 and 48 h treatment. The treatment induced a statistically significant decrease of the viability/proliferation of the Graffi tumour cells. These effects were concentration- and time-dependent. Fluorescent microscopy studies showed that these antiproliferative effects were connected to the induction of apoptosis. The in vivo study showed the presence of a stromal component, single mononuclear cells in the stroma. Multiple incorrect mitotic figures were observed in the tumour tissue from the control group. Well-formed stroma with accumulation of mononuclear cells and mitotic cells were found in the group, treated with PSM. The tumour weight was decreased in the group, treated with PMS. CONCLUSION: The results indicate that PSM exhibited in vitro/in vivo antiproliferative/anti-tumour effects.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Astrágalo , Proliferação de Células/efeitos dos fármacos , Leucemia Experimental/tratamento farmacológico , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Astrágalo/química , Cricetinae , Feminino , Vírus da Leucemia Murina/patogenicidade , Leucemia Experimental/patologia , Leucemia Experimental/virologia , Masculino , Mesocricetus , Extratos Vegetais/isolamento & purificação , Cultura Primária de Células , Infecções por Retroviridae/virologia , Saponinas/isolamento & purificação , Carga Tumoral/efeitos dos fármacos , Células Tumorais Cultivadas , Infecções Tumorais por Vírus/virologia
12.
Mater Sci Eng C Mater Biol Appl ; 116: 111185, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32806241

RESUMO

Novel fibrous materials from polylactide (PLA) and Schiff base from Jeffamine ED® and 8-hydroxyquinoline-2-carboxaldehyde (Jeff-8Q) or its complex with Cu2+ (Jeff-8Q.Cu2+) were successfully prepared by using one-pot electrospinning or electrospinning combined with dip-coating. These approaches enabled the fabrication of materials of diverse design: non-woven textile in which Jeff-8Q or Jeff-8Q.Cu2+ was predominantly in the fibers' bulk (type "in") or was deposited as a thin film on the surface of the fibers (type "on"). The morphology of the mats and chemical composition of their surface were analyzed by means of scanning electron microscopy (SEM) and X-ray photoelectron spectroscopy (XPS). The coordination of Cu2+ ions in Jeff-8Q.Cu2+/inPLA and Jeff-8Q.Cu2+/onPLA mats was examined by electron paramagnetic resonance (EPR) spectroscopy. It was found that the in vitro release of Jeff-8Q (Jeff-8Q.Cu2+) from the type "on" mats was more rapid than that of the type "in" mats. Enhancement of the antioxidant activity of the Jeff-8Q.Cu2+-containing fibrous mats as compared to mats containing Jeff-8Q was observed. In contrast to the neat PLA mat, the Jeff-8Q- and Jeff-8Q.Cu2+-containing mats (both type "in" and "on") displayed high in vitro antitumor activity against human cervical HeLa cells. The obtained materials are promising for use in local tumor treatment.


Assuntos
Antioxidantes , Bases de Schiff , Antioxidantes/farmacologia , Células HeLa , Humanos , Oxiquinolina , Poliésteres
13.
Biomedicines ; 8(7)2020 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-32635655

RESUMO

Hemocyanins are oxygen-transporting glycoproteins in the hemolymph of arthropods and mollusks that attract scientific interest with their diverse biological activities and potential applications in pharmacy and medicine. The aim of the present study was to assess the in vitro antitumor activity of hemocyanins isolated from marine snail Rapana venosa (RvH) and garden snails Helix lucorum (HlH) and Helix aspersa (HaH), as well the mucus of H. aspersa snails, in the HT-29 human colorectal carcinoma cell line. The effects of the hemocyanins on the cell viability and proliferation were analyzed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and the alterations in the tumor cell morphology were examined by fluorescent and transmission electron microscopy. The results of the MTT assay showed that the mucus and α-subunit of hemocyanin from the snail H. aspersa had the most significant antiproliferative activity of the tested samples. Cytomorphological analysis revealed that the observed antitumor effects were associated with induction of apoptosis in the tumor cells. The presented data indicate that hemocyanins and mucus from H. aspersa have an antineoplastic activity and potential for development of novel therapeutics for treatment of colorectal carcinoma.

14.
Int J Pharm ; 584: 119426, 2020 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-32445907

RESUMO

Berberine chloride (Brb) is a natural isoquinoline quaternary alkaloid that displayed a set of beneficial biological properties such as antioxidant, antimicrobial, antitumor, anti-inflammatory, and antiviral. Brb is poorly soluble in water and body fluids and its intestinal absorption is very low, which predetermine its low bioavailability. Polymeric nanoparticles seem to be a good platform to overcome these drawbacks. In this study, for the first time, stable aqueous dispersions of nanoparticles (NPs) based on complexes of Brb and poly(methacrylic acid) (PMA) or poly(acrylic acid) (PAA), were successfully prepared by mixing their dilute aqueous solutions as evidenced by the performed dynamic light scattering (DLS) and transmission electron microscopy (TEM) analyses. It was found that the mean diameter and zeta potential of NPs depended on the Brb molar fraction. In the case of Brb/PMA and Brb/PAA NPs the encapsulation efficiency was observed to approach a maximum value of 58.9 ± 0.5% and of 78.4 ± 0.9%, respectively, at values of Brb molar fraction at which maximum amount of complexes was obtained. The performed differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analyses revealed that Brb incorporated in the NPs was in the amorphous state. The Brb release profile was pH-dependent. The Brb-containing NPs displayed good antioxidant capacity close to that of free Brb. In vitro cell viability studies demonstrated that the Brb/PMA (PAA) NPs exerted a higher cytotoxicity against HeLa tumor cell than non-tumor BALB/c 3T3 mouse fibroblast cells. Thus, the obtained NPs are promising candidates in the drug delivery systems in the treatment of cervical tumors.


Assuntos
Resinas Acrílicas/química , Antineoplásicos/farmacocinética , Antioxidantes/farmacologia , Berberina/farmacologia , Nanopartículas/química , Ácidos Polimetacrílicos/química , Animais , Antineoplásicos/administração & dosagem , Antioxidantes/administração & dosagem , Células 3T3 BALB , Proteínas da Membrana Bacteriana Externa , Berberina/administração & dosagem , Química Farmacêutica/métodos , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/farmacologia , Liberação Controlada de Fármacos , Difusão Dinâmica da Luz , Células HeLa , Humanos , Concentração de Íons de Hidrogênio , Camundongos , Camundongos Endogâmicos BALB C , Microscopia Eletrônica de Transmissão , Tamanho da Partícula
15.
Antioxidants (Basel) ; 9(3)2020 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-32168830

RESUMO

The aim of present study was to obtain novel fibrous materials based on cellulose derivative and polyethylene glycol loaded with natural biologically active compound quercetin by electrospinning. Several methods including scanning electron microscopy (SEM), IR spectroscopy, X-ray diffraction analysis (XRD), water contact angle measurements, differential scanning calorimetry (DSC), and UV-VIS spectroscopy were utilized to characterize the obtained materials. The incorporation of polyethylene glycol in the fibrous material resulted in increased hydrophilicity and burst release of quercetin from the fibers. Quercetin-containing fibrous mats exhibited high antioxidant activity as estimated by DPPH free radical scavenging method. In vitro tests with HeLa tumor cells and SH-4 melanoma skin cells were performed in order to determine the cytotoxicity of the novel materials. It was found that the fibrous CA/PEG/QUE materials exhibited high cytotoxic effect against both cell lines. Therefore, the novel polymeric materials containing quercetin are promising candidates for biomedical and pharmaceutical applications.

16.
Int J Biol Macromol ; 107(Pt A): 689-702, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28919524

RESUMO

Novel fibrous materials from poly(ε-caprolactone) (PCL), chitosan (Ch) and natural phenolic acid ferulic acid (FA) of diverse design were successfully prepared by electrospinning or electrospinning combined with dip-coating. FA incorporated in the PCL fibrous mats or in the Ch coating was in the amorphous state as evidenced by the performed differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. The release of FA was affected by the composition and design of the polymer matrix. The incorporation of a combination of FA and Ch in the fibrous mats imparted to these materials higher killing rates against pathogenic bacteria S. aureus than that of FA-containing mats or Ch-coated mats alone. The FA-containing fibrous materials as well as those coated with Ch or Ch-FA inhibited the adhesion of S. aureus bacteria. Moreover, FA preserved its antioxidant activity when incorporated in the fibers or in the Ch coating. It was found that the cytotoxicity of all types of FA-containing mats against HeLa tumor cells was higher than that of the free FA. Thus, the obtained fibrous materials can be suitable candidates for wound dressing applications and for application in local treatment of cervical tumors.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Quitosana/farmacologia , Materiais Revestidos Biocompatíveis/farmacologia , Ácidos Cumáricos/farmacologia , Antibacterianos/química , Antineoplásicos/química , Antioxidantes/química , Sobrevivência Celular/efeitos dos fármacos , Quitosana/química , Materiais Revestidos Biocompatíveis/química , Ácidos Cumáricos/química , Técnicas Eletroquímicas , Células HeLa , Humanos , Viabilidade Microbiana/efeitos dos fármacos , Nanofibras/química , Nanofibras/ultraestrutura , Poliésteres/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento , Propriedades de Superfície
17.
J Mater Sci Mater Med ; 29(1): 9, 2017 Dec 23.
Artigo em Inglês | MEDLINE | ID: mdl-29275497

RESUMO

Curcumin (Curc) exhibits anti-inflammatory, antibacterial and antitumor activity. However, its clinical application is limited by its poor bioavailability related to its extremely low water solubility. Novel materials allowing enhanced release of Curc in aqueous medium were obtained. The new materials consisted of electrospun fibers from cellulose acetate (CA) (mean fiber diameter ca. 780 nm ± 110 nm) with electrosprayed Curc/polyvinylpyrrolidone (Curc/PVP) particles. Scanning electron microscopy (SEM) showed that separated and evenly distributed particles of Curc/PVP were deposited on the surface of the mats and on the inner layers of the mat. X-ray diffraction studies showed that Curc was in amorphous state. In vitro studies demonstrated that Curc release was facilitated from Curc/PVP-on-CA mats (ca. 78% for 24 h) compared with the materials in which Curc was incorporated in CA fibers (17% for 24 h). Moreover, the curcumin-containing materials exhibited antibacterial activity against Gram-positive bacteria Staphylococcus aureus (S. aureus) and Gram-negative bacteria Escherichia coli (E. coli). Curc/PVP-on-CA fibrous mats exhibited high in vitro cytotoxicity towards HeLa tumor cells. Therefore, the obtained materials are promising for antibacterial wound dressing applications as well as for application in local treatment of cervical tumors.


Assuntos
Antineoplásicos/administração & dosagem , Materiais Biocompatíveis/química , Celulose/análogos & derivados , Curcumina/administração & dosagem , Pirróis/química , Antibacterianos/administração & dosagem , Bandagens , Celulose/química , Escherichia coli/efeitos dos fármacos , Células HeLa , Humanos , Teste de Materiais , Microscopia Eletrônica de Varredura , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureus/efeitos dos fármacos , Difração de Raios X
18.
Anticancer Agents Med Chem ; 16(12): 1512-1522, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27349447

RESUMO

The partial efficacy and high toxicity of the current anticancer chemotherapeutics as well as the development of multiple drug resistance are the major problems in cancer therapy. Therefore, there is an emergency need for the development of novel well-tolerated anticancer agents with different mode of action that could be successfully used in combination with other drugs as an adjuvant therapy. The inhibition of intracellular signaling pathways associated with cancer growth and invasiveness is a main therapeutic approach in cancer treatment. It is well known that lipid metabolism is involved in the regulation of key cellular processes such as proliferation, differentiation and apoptosis. Statins and alkylphospholipids are both relatively new synthetic agents with considerable anticancer properties that disturb lipid metabolism and subsequently modulate proliferation and cell survival signaling pathways, leading to apoptosis. Numerous in vitro and in vivo studies have shown promising results for the use of statins and alkylphospholipids as potential therapeutic agents in the treatment of various human malignancies. However, more investigations and clinical trials are needed to assess their optimal safe dose and maximal efficacy and better understand the molecular mechanisms underlying the antitumor effects of these drugs.


Assuntos
Antineoplásicos/farmacologia , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia , Metabolismo dos Lipídeos/efeitos dos fármacos , Neoplasias/tratamento farmacológico , Fosfolipídeos/farmacologia , Animais , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases/química , Estrutura Molecular , Neoplasias/patologia , Fosfolipídeos/química
20.
Braz. arch. biol. technol ; 57(5): 675-684, Sep-Oct/2014. graf
Artigo em Inglês | LILACS | ID: lil-723055

RESUMO

Pure C-phycocyanin (C-PC) was isolated from Arthronema africanum to evaluate its potential antitumor effects in vivo and in vitro. Experimental myeloid Graffi tumor in hamsters was used as a model. The cell proliferation assay showed that C-PC treatment, at concentration of 100 µg mL-1 for 24 h, significantly inhibited the growth of Graffi tumor cells (51.4% viability). Agarose gel electrophoresis of the genomic DNA of treated cells displayed time-and concentration-dependent fragmentation pattern, typical for apoptosis. Apoptotic process was related to the increase in cellular manganese and copper/zinc superoxide dismutases and glutathione reductase activities, coupled with a low catalase activity. In vivo C-PC administration (5.0 mg kg-1 body weight) suppressed the tumor transplantability and growth, while the mean survival time of the tumor-bearing hamsters was increased. The results revealed promising antitumor activities of A. africanum C-PC and suggested the potential of this natural biliprotein pigment for future pharmacological and medical applications. The study provided new data on the mechanism of the C-PC induced apoptosis in which the imbalance of antioxidant enzymes that favoured hydrogen peroxide accumulation might play a leading role.

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