RESUMEN
Hybrid biocomposite scaffolds (HBS) that serve as a carrier for cell proliferation and differentiation are increasingly used for tissue regeneration. 3D hybrid scaffold based on collagen-grafted-chitosan-glucan fiber (CO-g-CGF-HBS) was prepared by freeze-drying technique. The swelling percentage, hydrolytic stability, and modulus of elasticity of HBS were enhanced after the chemical modification of CO with CGF. Pore size and porosity of HBS were decreased with an increased CGF ratio. HBS exhibits a higher reduction rate against different types of bacteria compared with a control sample. Thus, chemical modification of CO with different ratios of CGF significantly improved the physicochemical, antibacterial properties of HBS.
Asunto(s)
Quitosano , Materiales Biocompatibles/química , Proliferación Celular , Quitosano/química , Colágeno/química , Glucanos , Porosidad , Ingeniería de Tejidos/métodos , Andamios del Tejido/químicaRESUMEN
Collagen (CO)/chitosan-glucan complex (CSGC) hollow fibers encapsulated aloe vera (AV) dressing scaffold (CO/CSGC@AV) were fabricated for the first time by the freeze-dried process. Extraction process, morphology, mechanical properties, pore size, porosity, swelling ability, and degradation behavior of composites scaffold were investigated. CSGC hollow fibers were extracted from mycelium of Schizophyllum commune CSGC hollow fiber exhibited inner diameter of (600⯱â¯250â¯nm) and outer fiber diameter of (2.5⯱â¯0.5⯵m). The results of swelling and hydrolytic degradation studies demonstrated that the physicochemical of CO/CSGC@AV was significantly enhanced by CSGC in a concentration-dependent manner. The mechanical property of the CO/CSGC@AV was improved after encapsulated AV into CSGC hollow fibers compared with native CO. The pore size and porosity of the CO/CSGC@AV were slightly decreased in the presence of AV. All these results suggested that the new dressing scaffold has a potential for clinical skin regeneration, particularly for infected chronic wounds and ulcers.
Asunto(s)
Aloe/metabolismo , Vendajes , Quitosano , Colágeno , Glucanos , Schizophyllum/metabolismo , Quitosano/química , Quitosano/aislamiento & purificación , Colágeno/química , Colágeno/aislamiento & purificación , Liofilización , Glucanos/química , Glucanos/aislamiento & purificación , Extractos Vegetales/química , Porosidad , Resistencia a la TracciónRESUMEN
Novel nanofibers mats were fabricated by electrospinning of polyvinyl alcohol/hyaluronan (PVA/HA) solutions in the presence of silver nanoparticles (AgNPs). The AgNPs were synthesized by in-situ chemical reduction of silver ions (Ag+) using HA as a reducing and stabilizing agent. Narrow size distribution and spherical shape of AgNPs were achieved by optimizing the initial silver nitrate concentration (0.01 to 1â¯M) and reaction time (10-60â¯min). HA-AgNPs nanocomposite and PVA/HA-AgNPs nanofibrous mats were fabricated by electrospinning technique from aqueous solution containing a different mass ratio of PVA and HA-AgNPs and characterized by UV/Vis spectroscopy, SEM, TEM, DLS, XRD, TGA, and ATR-FTIR. Mechanical and rheological properties were also investigated and discussed. The novel nanofibrous mats show great potential in skin regeneration and drug carrier applications.
Asunto(s)
Tecnología Química Verde , Ácido Hialurónico/química , Nanopartículas del Metal/química , Nanocompuestos/química , Alcohol Polivinílico/química , Plata/química , Vendajes , Portadores de Fármacos , Electroquímica , Iones , Nanofibras , Tamaño de la Partícula , Reología , Nitrato de Plata/química , Solventes , Espectroscopía Infrarroja por Transformada de Fourier , Propiedades de SuperficieRESUMEN
In-situ formed hyaluronan/silver (HA/Ag) nanoparticles (NPs) were used to prepare composite fibers/fabrics for the first time. Different concentrations of silver nitrate (1, 2mg/100ml) were added at ambient temperature to sodium hyaluronate solution (40mg/ml), then the pH was increased to 8 by adding sodium hydroxide. The in-situ formed HA/Ag-NPs were used to prepare fibers/nonwoven fabrics by wet-dry-spinning technique (WDST). UV/vis spectroscopy, SEM, TEM, DLS, XPS, XRD and TGA were employed to characterize the structure and composition of the nanocomposite, surface morphology of fiber/fabrics, particle size of Ag-NPs, chemical interactions of Ag0 and HA functional groups, crystallinity and thermal stability of the wound dressing, respectively. The resultant HA/Ag-NPs1 and HA/Ag-NPs2 composite showed uniformly dispersed throughout HA fiber/fabrics (SEM), an excellent distribution of Ag-NPs with 25±2, nm size (TEM, DLS) and acceptable mechanical properties. The XRD analysis showed that the in-situ preparation of Ag-NPs increased the crystallinity of the resultant fabrics as well as the thermal stability. The antibacterial performance of medical HA/Ag-NPs fabrics was evaluated against gram negative bacteria E. coli K12, exhibiting significant bactericidal activity. The fibers did not show any cytotoxicity against human keratinocyte cell line (HaCaT). In-vivo animal tests indicated that the prepared wound dressing has strong healing efficacy (non-diabetics/diabetics rat model) compared to the plain HA fabrics and greatly accelerated the healing process. Based on our results, the new HA/Ag-NPs-2mg nonwoven wound dressing fabrics can be used in treating wounds and chronic ulcers as well as cell carrier in different biological research and tissue engineering.
Asunto(s)
Vendajes , Ácido Hialurónico/uso terapéutico , Nanofibras/química , Nanofibras/uso terapéutico , Plata/química , Úlcera/tratamiento farmacológico , Cicatrización de Heridas/efectos de los fármacos , Animales , Células Cultivadas , Cristalización , Estabilidad de Medicamentos , Humanos , Ácido Hialurónico/química , Masculino , Pruebas de Sensibilidad Microbiana , Nanofibras/ultraestructura , Tamaño de la Partícula , RatasRESUMEN
Some new fluorine containing substituted 3-thioxo-1,2,4-triazin-5-ones (2-17) have been synthesized and evaluated for in vitro anti human immune virus (HIV) activity. Most of the new compounds displayed a lethal activity, while compounds 2, 6, 7, 10, 11 and 14 displayed a significant antiviral activity. The structures are supported by elemental analysis, IR, UV and 1H-NMR spectral data.
Asunto(s)
Antivirales/síntesis química , Flúor , VIH/efectos de los fármacos , Triazinas/síntesis química , Línea Celular , Flúor/farmacología , Formazáns/metabolismo , Humanos , Linfocitos/microbiología , Compuestos de Sulfhidrilo/síntesis química , Compuestos de Sulfhidrilo/farmacología , Triazinas/farmacologíaRESUMEN
In a search for new anticancer agents fluorine bearing trisubstituted 3-thioxo-1,2,4-triazin-5-ones (2-12) have been prepared and characterized by their elemental analysis, UV, IR and 1H-NMR spectral data. The in vitro anticancer activity of all the compounds has been determined. Compounds 3 and 7 showed a moderate activity against Leukemia/Lymphoma, Small/Non small Cell Lung, Colon carcinoma and Melanoma Cells.
Asunto(s)
Antineoplásicos/síntesis química , Tiazinas/síntesis química , Animales , Antineoplásicos/farmacología , Humanos , Espectroscopía de Resonancia Magnética , Neoplasias Experimentales/tratamiento farmacológico , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , Tiazinas/farmacología , Células Tumorales Cultivadas/efectos de los fármacosRESUMEN
A number of various thioethers derived from 3-hydrazone-5,6-diphenyl-1,2,4-triazines have been synthesized and evaluated for anticancer and anti HIV activities. The structures are supported by elemental analysis, IR, UV and 1H-NMR spectral data. Most of the tested compounds displayed a significant activity against Leukemia/Lymphoma, CNS, Ovarian and Small cell lung cancer.
Asunto(s)
Antineoplásicos/síntesis química , Antivirales/síntesis química , VIH/efectos de los fármacos , Hidrazonas/síntesis química , Triazinas/síntesis química , Antineoplásicos/farmacología , Antivirales/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Hidrazonas/farmacología , Triazinas/farmacología , Células Tumorales CultivadasRESUMEN
The synthesis of 4-substituted amino-6-styryl/alkyl/aryl-1,2,4-triazin- 3,5(2H)diones (4a-d and 15) involving the cyclocondensation of N4-arylaminosemicarbazides(3a-d and 13) with some alpha-ketoacids is described. The behaviour of these triazinones towards amine, hydrazine, isothiocyanate, aromatic aldehyde and gl. acetic acid have been investigated. Structure elucidation of the new compounds has been carried out with the help of elemental analysis, IR, UV and 1H-NMR spectra. The antifungal activity of the prepared compounds has been assayed both in vitro and in vivo against some phytopathogenic fungi associated with wheat grains, were the compound 3b showed a high protection of the grains of wheat against the fungal infection.
Asunto(s)
Hongos/efectos de los fármacos , Fungicidas Industriales/síntesis química , Triazinas/síntesis química , Fungicidas Industriales/farmacología , Pruebas de Sensibilidad Microbiana , Triazinas/farmacología , Triticum/microbiologíaRESUMEN
Studies on the chemical reactivity of fluorine containing bioactive 1,2,4-triazines are reviewed. The synthesis, unique features and biological significance of these constituents are discussed.
Asunto(s)
Antiinfecciosos/síntesis química , Antineoplásicos/síntesis química , Triazinas/síntesis química , Antiinfecciosos/farmacología , Antineoplásicos/farmacología , Triazinas/farmacologíaRESUMEN
The role of uncondensed 1,2,4-triazine derivatives and the related compounds as biocidal plant protection agents such as herbicides, bactericidal, fungicidal, antimicrobial, protozacides, anticoccidal, parasiticides, insecticides, acaricdes and pesticides, is reviewed.
Asunto(s)
Plaguicidas/toxicidad , Plantas/efectos de los fármacos , Triazinas/toxicidad , Herbicidas/química , Herbicidas/toxicidad , Plaguicidas/química , Triazinas/químicaRESUMEN
Studies on the chemical reactivity of bioactive 3-amino-1,2,4-triazines are reviewed. The synthesis, unique features and pharmacological significance of these constituents are discussed.
Asunto(s)
Triazinas/química , Animales , Fármacos Anti-VIH/síntesis química , Fármacos Anti-VIH/química , Fármacos Anti-VIH/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacología , Humanos , Espectrofotometría Ultravioleta , Triazinas/síntesis química , Triazinas/farmacologíaRESUMEN
The role of uncondensed 1,2,4-triazine compounds and related heterobicyclic systems in AIDS and Cancer is reviewed. Their medicinal applications are also reported.
Asunto(s)
Fármacos Anti-VIH/farmacología , Antineoplásicos/farmacología , Compuestos Bicíclicos Heterocíclicos con Puentes/farmacología , Triazinas/farmacología , Fármacos Anti-VIH/química , Antineoplásicos/química , Compuestos Bicíclicos Heterocíclicos con Puentes/química , Humanos , Triazinas/químicaRESUMEN
1,6-Dihydro-3(2H)-thioxo-6-spiro-(9'-fluorene)-1,2,4-triazin -5(4H)-one (1) has been used to synthesize several analogous compounds via nucleophilic substitution reactions. Spectroscopic data are given in support of the proposed structures. Some of the new products possessed good anti HIV and anticancer activities.
Asunto(s)
Antineoplásicos/síntesis química , Antivirales/síntesis química , VIH/efectos de los fármacos , Compuestos de Espiro/síntesis química , Triazinas/síntesis química , Antineoplásicos/farmacología , Antivirales/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Compuestos de Espiro/farmacología , Triazinas/farmacología , Células Tumorales Cultivadas , Zidovudina/farmacologíaRESUMEN
A number of heterobicyclic compounds such as 1,3,5-thiazine, thiazolidinone, pyrimidine, pyrimidinedione, imidazole, quinazolinone and 1,2,4-triazinone derivatives have been sythesized by reaction of 1,6-dihydro-3(2H)-thioxo-6-spiro-(9'- fluorene)-1,2,4-triazin-5(4H)-one (1) with sulphur/nitrogen compounds in neutral or alkaline media. Structure elucidation of the new compounds have been carried out with the help of elemental analysis and spectral data. Some of these compounds were tested for in vitro anti HIV and anticancer activities.
Asunto(s)
Antineoplásicos/síntesis química , Antivirales/síntesis química , VIH/efectos de los fármacos , Triazinas/síntesis química , Antineoplásicos/farmacología , Antivirales/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , Triazinas/farmacología , Células Tumorales Cultivadas , Zidovudina/farmacologíaRESUMEN
The synthesis of 1,2,4-triazines bearing a 1,2,4-triazinone moiety and of 1,2,4-triazolo[4,3-b]-1,2,4-triazonones have been achieved by reaction of 1,6-dihydro-3-hydrazino-6-spiro- (9-fluorenyl)-1,2,4-triazin-5(4H)-one with various oxo- and halo-compounds. Structures of the products have been deduced by elemental analysis and spectral data. Significant anti-HIV and anticancer activities were observed in vitro for some members of the series.
Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Antivirales/síntesis química , Antivirales/farmacología , VIH/efectos de los fármacos , Triazinas/síntesis química , Triazinas/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Pruebas de Sensibilidad Microbiana , Células Tumorales CultivadasRESUMEN
Some new heterobicyclic nitrogen systems 5-18 and/or thioethers 20, 22 bearing the 1,2,4-triazine moiety have been synthesized via condensation of 3-formylamino-1,2,4-triazine 3 with nitrogen compounds followed by heterocyclization with oxygen reagents. Thioether analogs 20, 22 have been obtained from fusion of compound 19 with 4-chlorothiophenol. The structure of the products have been established by elemental analysis and spectral data. The anti-HIV and anticancer activities of some products have also been investigated where compounds 20a, c and 22b exhibited a moderate activity. The biocidal-structures activity correlation was also studied.
Asunto(s)
Fármacos Anti-VIH/síntesis química , Antineoplásicos/síntesis química , Triazinas/síntesis química , Fármacos Anti-VIH/farmacología , Antineoplásicos/farmacología , Fenómenos Químicos , Química Física , Ensayos de Selección de Medicamentos Antitumorales , VIH/efectos de los fármacos , Humanos , Indicadores y Reactivos , Triazinas/farmacología , Células Tumorales CultivadasRESUMEN
Some new heterobicyclic nitrogen systems bearing the 1,2,4-triazine moiety (3-22) have been achieved by treatment of 3-amino-5,6-disubstituted-1,2,4-triazines 2a-h with some cyclic and acyclic oxygen compounds followed by heterocyclization. Structures of the products have been deduced by elemental analysis and spectral data. Significant anti-HIV and anticancer activities were observed in vitro for some members of the series, where compounds 5 and 18 showed a moderate activity.
Asunto(s)
Fármacos Anti-VIH/síntesis química , Antineoplásicos/síntesis química , Triazinas/síntesis química , Fármacos Anti-VIH/farmacología , Antineoplásicos/farmacología , Fenómenos Químicos , Química Física , Ensayos de Selección de Medicamentos Antitumorales , VIH-1/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Relación Estructura-Actividad , Triazinas/farmacologíaRESUMEN
Some new fused heterobicyclic nitrogen systems such as 1,2,4-triazino[3,4-b] [1,3,4] thiadiazolones/thiadiazinones 4-15 and the related compounds 16-21 have been synthesized from treatment of 4-amino-3-mercapto-6-substituted-1,2,4-triazin-5-ones 1 with bifunctional oxygen and halogen compounds via heterocyclization reactions. Structures of the products have been deduced from their elemental analysis and spectral data. Significant anti-HIV and anticancer activities were observed in vitro for some members of the series, compounds 1e, 4e, 4f, 5, 6 and 16 showing a significant activity in Leukemia, Lung, Breast and CNS anticancer evaluation.
Asunto(s)
Fármacos Anti-VIH/síntesis química , Fármacos Anti-VIH/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Compuestos Heterocíclicos/síntesis química , Compuestos Heterocíclicos/farmacología , Triazinas/síntesis química , Triazinas/farmacología , Fenómenos Químicos , Química Física , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Relación Estructura-Actividad Cuantitativa , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , Células Tumorales CultivadasRESUMEN
In the search for new antimicrobial compounds, several new sulfur bearing heterobicyclic moieties (4-11) have been synthesized by acylation and alkylation of acetamide, thioacetamide and semicarbazide derivatives. The structure of the products was deduced from elemental analyses as well as spectral data (IR, 1H NMR and MS). Significant antimicrobial activities were obtained for all new compounds especially against Fusarium oxysporum.
Asunto(s)
Antiinfecciosos/síntesis química , Benzoxazoles/síntesis química , Tiazoles/síntesis química , Antibacterianos , Antiinfecciosos/farmacología , Aspergillus fumigatus/efectos de los fármacos , Bacterias/efectos de los fármacos , Benzoxazoles/farmacología , Fenómenos Químicos , Química Física , Fusarium/efectos de los fármacos , Helminthosporium/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Espectrofotometría Infrarroja , Tiazoles/farmacologíaRESUMEN
4-Thiazolidinones have been reported to possess biological activity especially fungicidal activity. With an intention to prepare some more 4-thiazolidinones as drugs for anti HIV and anticancer activity, we have synthesized some more 4-thiazolidinones by the action of mercaptoacetic acid on Schiff's base and/or heterocyclization of N-substituted thioureas with monochloracetic acid. Characterization of 4-thiazolidinone was deduced upon elemental and spectral analysis.