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1.
J Ethnopharmacol ; 334: 118542, 2024 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-38992404

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Dried roots of Peucedanum decursivum, a traditional Chinese medicine (TCM), has historically respiratory diseases such as cough, thick phlegm, headache, fever, and gynecological diseases, rheumatoid arthritis, and nasopharyngeal carcinoma. AIM OF THE STUDY: Made an endeavor to evaluate the research trajectory of P. decursivum, comprehensively discern its developmental status, and offer a guideline for future investigations. MATERIALS AND METHODS: A meticulous search of literatures and books from 1955 to 2024 via databases like PubMed, Web of Science and CNKI was conducted, including topics and keywords of " P. decursivum" "Angelica decursivum" and "Zihua Qianhu". RESULTS: P. decursivum and its prescriptions have traditionally been used for treating phlegm-heat cough, wind-heat cough, gastrointestinal diseases, pain relief and so on. It contains 234 identified compounds, encompassing coumarins, terpenes, volatile oils, phenolic acids, fatty acids and derivatives. It exhibits diverse pharmacological activities, including anti-asthmatic, anti-inflammatory, antioxidant effects, anti-hypertensive, anti-diabetic, anti-Alzheimer, and anti-cancer properties, primarily attributed to coumarins. Microscopic identification, HPLC fingerprinting, and bioinformatics identification are the primary methods currently used for the quality control. CONCLUSION: P. decursivum demonstrates anti-asthmatic, anti-inflammatory, and antioxidant effects, aligning with its traditional use. However, experimental validation of its efficacy against phlegm and viruses is needed. Additionally, analgesic effects mentioned in historical texts lack modern pharmacological studies. Numerous isolated compounds exhibit highly valuable medicinal properties. Future research can delve into exploring these substances further. Rigorous of heavy metal contamination, particularly Cd and Pb, is necessary. Simultaneously, investigating its pharmacokinetics and toxicity in humans is crucial for the safety.


Assuntos
Apiaceae , Etnobotânica , Etnofarmacologia , Compostos Fitoquímicos , Controle de Qualidade , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/uso terapêutico , Apiaceae/química , Animais , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/uso terapêutico , Medicina Tradicional Chinesa/métodos
2.
Materials (Basel) ; 17(7)2024 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-38612084

RESUMO

With the fast development of the cold chain transportation industry, the traditional refrigeration method results in significant energy consumption. To address the national call for energy saving and emission reduction, the search for a new type of energy storage material has already become a future development trend. According to the national standard GB/T28577 for the classification and basic requirements of cold chain logistics, the temperature in frozen logistics is typically below -18 °C. In this study, n-undecane with a phase change temperature of -26 °C is chosen as the core material of microcapsules. Poly(methyl methacrylate) is applied as the shell material, with n-undecane microcapsules being prepared through suspension polymerization for phase change cold storage materials (MEPCM). Using characterization techniques including SEM, DSC, FTIR, and laser particle size analysis, the effects of three types of emulsifiers (SMA, Tween-80, Tween-80/span-80 (70/30)), SMA emulsifier dosage, core-shell ratio, and emulsification rate on the thermal performance and micro-surface morphology of n-undecane/PMMA microcapsules were studied. The results indicate that when comparing SMA, Tween-80, and Tween-80/span-80 (70/30) as emulsifiers, the dodecane/PMMA microcapsules prepared with SMA emulsifier exhibit superior thermal performance and micro-surface morphology, possessing a complete core-shell structure. The optimal microstructure and the highest enthalpy of phase change, measuring 120.3 kJ/kg, are achieved when SMA is used as the emulsifier with a quantity of 7%, a core-to-wall ratio of 2.5:1, and an emulsification speed of 2000 rpm. After 200 hot and cold cycles, the enthalpy of phase change decreased by only 18.6 kJ/kg, indicating the MEPCM thermal performance and cycle life. In addition, these optimized microcapsules exhibit favorable microstructure, uniform particle size, and efficient energy storage, making them an excellent choice for the refrigeration and freezing sectors.

3.
Food Chem X ; 20: 101026, 2023 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-38144751

RESUMO

The drying characteristics, rehydration capacity, color, infrared spectra and volatile components of iron stick yam slices were investigated under different alternating current (AC) voltages (13, 17, 21 kV), hot air drying (HAD) (60 °C) and natural drying (AD) by electrohydrodynamic (EHD) drying and HAD experimental devices. The results showed that slices of iron stick yam dried the quickest with HAD, which also had the fastest drying rate; while drying the slices of iron stick yam with EHD led to a better rehydration capacity, higher brightness L* and whiteness, a more stable protein secondary structure, and a greater variety and content of volatile components compared with AD and HAD. These finding indicated that EHD is a more promising method for drying iron stick yam.

4.
Polymers (Basel) ; 15(3)2023 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-36771937

RESUMO

Double network (DN) hydrogels composed of self-assembling low-molecular-weight gelators and a hybrid polymer network are of particular interest for many emerging biomedical applications, such as tissue regeneration and drug delivery. The major benefits of these structures are their distinct mechanical properties as well as their ability to mimic the hierarchical features of the extracellular matrix. Herein, we describe a hybrid synthetic/natural polymer gel that acts as the initial network based on sodium alginate and a copolymer, namely poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro (5,5) undecane). The addition of amino acids and peptide-derived hydrogelators, such as Fmoc-Lys-Fmoc-OH and Fmoc-Gly-Gly-Gly-OH, to the already-made network gives rise to DNs crosslinked via non-covalent interactions. Fourier transform infrared spectroscopy (FTIR) and thermal analysis confirmed the formation of the DN and highlighted the interactions between the two component networks. Swelling studies revealed that the materials have an excellent water absorption capacity and can be classified as superabsorbent gels. The rheological properties were systematically investigated in response to different variables and showed that the prepared materials present injectability and a self-healing ability. SEM analysis revealed a morphology consisting of a highly porous and interconnected fibrous network. Finally, the biocompatibility was evaluated using the MTT assay on dermal fibroblasts, and the results indicated that the new structures are non-toxic and potentially useful for biomedical applications.

5.
Food Chem ; 402: 134015, 2023 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-36137382

RESUMO

Cooking improves food aroma, but few studies have explored how cooking affects food aromas. Here, aroma changes in mildly salted large yellow croaker (Larimichthys crocea, MSLYC) after steaming, baking, frying, and deep frying was investigated. The raw fish was dominated by fishy notes but after cooking, the aroma became dominated by fatty notes. Nine volatiles, including hexanal, nonanal, (E, Z)-2, 6-nonadienal, (E, E)-2, 4-decadienal, 1-octen-3-ol, linalool, ethyl hexanoate, acetic acid and anethole, were identified as key odor-active compounds using GC-MS, OAV, and omission tests analyses. Changes in the concentrations of key odor-active compounds were mainly due to evaporation, oxidation of linolenic acids, and thermal catalyzed reactions. Interestingly, anethole was the key odor-active compound, providing new insight into the underlying reactions of cooked fish aroma.


Assuntos
Perciformes , Compostos Orgânicos Voláteis , Animais , Odorantes/análise , Compostos Orgânicos Voláteis/análise , Culinária/métodos , Ácidos Linolênicos
6.
Mar Drugs ; 20(11)2022 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-36354986

RESUMO

Marine natural products (MNPs) continue to be in the spotlight in the global drug discovery endeavor. Currently, more than 32,000 structurally diverse secondary metabolites from marine sources have been isolated, making MNPs a vital source for researchers to look for novel drug candidates. The marine-derived psammaplysins possess the rare and unique 1,6-dioxa-2-azaspiro [4.6] undecane backbone and are represented by 44 compounds in the literature, mostly from sponges of the order Verongiida. Compounds with 1,6-dioxa-2-azaspiro [4.6] undecane moiety exist in the literature under five names, including psammaplysins, ceratinamides, frondoplysins, ceratinadins, and psammaceratins. These compounds displayed significant biological properties including growth inhibitory, antimalarial, antifouling, protein tyrosine phosphatase inhibition, antiviral, immunosuppressive, and antioxidant effects. In this review, a comprehensive literature survey covering natural occurrence of the psammaplysins and related compounds, methods of isolation, structural differences, the biogenesis, and biological/pharmacological properties, will be presented.


Assuntos
Antimaláricos , Produtos Biológicos , Produtos Biológicos/química , Descoberta de Drogas , Alcanos , Antimaláricos/farmacologia
7.
Acta Crystallogr E Crystallogr Commun ; 78(Pt 2): 149-153, 2022 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-35145741

RESUMO

The racemic title compound, [Fe(C5H5)(C16H27O2)], comprises an α,ω-diol-substituted undecyl chain with a ferrocenyl substituent at at one terminus. The alkane chain is inclined to the substituted ring of the ferrocene grouping by 84.22 (13)°. The ferrocene rings are almost eclipsed and parallel. The crystal structure features O-H⋯O and C-H⋯O hydrogen bonds and C-H⋯π contacts that stack the mol-ecules along the c-axis direction. A Hirshfeld surface analysis reveals that H⋯H inter-actions (83.2%) dominate the surface contacts.

8.
J Hazard Mater ; 424(Pt D): 127700, 2022 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-34799160

RESUMO

n-Undecane (C11) is the main component of volatile organic compounds (VOCs) emitted from the printing industry, and its emission to the atmosphere should be controlled. In this study, a dielectric barrier discharge reactor coupled with CeO2/γ-Al2O3 catalysts was used to degrade C11. The effect of the chemical state of CeO2 on C11 degradation was evaluated by varying the CeO2 loading on γ-Al2O3. The C11 conversion and COx selectivity were as high as 92% and 80%, respectively, under mild reaction conditions of energy density 34 J/L and 423 K to degrade 134 mg/m3 C11 in a simulated air using 10 wt%CeO2 impregnated on γ-Al2O3. After analyses using in-situ plasma diffuse reflectance Fourier transform infrared spectroscopy and gas chromatography-mass spectrometry, it was found that most of C11 were degraded to CO2, and the main by-products on catalyst surfaces were alcohols and ketones. It was concluded from X-ray photoemission spectroscopy that the good performance of the 10 wt%CeO2/γ-Al2O3 catalyst was due to its high Ce3+/(Ce3++Ce4+) ratio as well as the oxygen vacancies. The Ce3+/(Ce3++Ce4+) ratio of CeO2 on γ-Al2O3 is crucial for the degradation of C11, providing a further roadmap for the plasma catalytic oxidation of alkanes.

9.
Insects ; 12(12)2021 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-34940173

RESUMO

The main aim of this work was to identify semiochemicals from the jewel beetle Coraebus undatus (F.) (Coleoptera: Buprestidae) that may aid in the improvement of current monitoring tools. First, HS-SPME collections revealed that individually sampled adults (>7 days old) of both sexes release the spiroacetal 1,7-dioxaspiro[5.5]undecane (olean). Electroantennographic recordings from both sexes exposed to increasing amounts of olean followed a dose-dependent pattern, with females being more responsive than males to the highest amount of the compound (100 µg). In double-choice assays, adults older than seven days were significantly attracted to olean, whereas this attraction was not detected in insects aged less than seven days. Indeed, a repellent effect was observed in young females. Subsequent field trials employing sticky purple prism traps revealed that there were no differences among the number of insects caught in control and olean-baited traps at two different release rates (0.75 and 3.75 mg/day). Interestingly, all the trapped specimens were determined as mated females, regardless of the presence of olean. Overall, these findings provide a basis for unraveling the chemical ecology of the species, although further research is still needed to determine the specific role of this compound within the chemical communication of the species.

10.
Gels ; 7(4)2021 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-34940301

RESUMO

This study reports a strategy for developing a biohybrid complex based on a natural/synthetic polymer conjugate as a gel-type structure. Coupling synthetic polymers with natural compounds represents an important approach to generating gels with superior properties and with potential for biomedical applications. The study presents the preparation of hybrid gels with tunable characteristics by using a spiroacetal polymer and alginate as co-partners in different ratios. The new network formation was tested, and the structure was confirmed by FTIR and SEM techniques. The physical properties of the new gels, namely their thermal stability and swelling behavior, were investigated. The study showed that the increase in alginate content caused a smooth increase in thermal stability due to the additional crosslinking bridges that appeared. Moreover, increasing the content of the synthetic polymer in the structure of the gel network ensures a slower release of carvacrol, the encapsulated bioactive compound.

11.
Extremophiles ; 24(6): 863-873, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32944821

RESUMO

In the last decades, efforts to reduce the use of fossil fuels have increased the search for alternative sustainable sources of renewable energy. In this scenario, hydrocarbons derived from fatty acids are among the compounds that have been drawing attention. The intracellular production of hydrocarbons by bacteria derived from cold environments such as the Antarctic continent is currently poorly investigated, as extremophilic microorganisms provide a great range of metabolic capabilities and may represent a key tool in the production of biofuels. The aim of this study was to explore the ability of bacterial cells derived from extreme environments to produce hydrocarbons with potential for further use as biofuels. Seven bacteria isolated from Antarctic samples were evaluated for hydrocarbon production using GC-MS approaches. Two isolates, identified as Arthrobacter livingstonensis 593 and Pseudoalteromonas arctica 628, were able to produce the hydrocarbon undecane (CH3-(CH2)9-CH3) in concentrations of 1.39 mg L-1 and 1.81 mg L-1, respectively. Results from the present work encourage further research focusing on the optimization of hydrocarbon production by the isolates identified as producers, which may be used in further aircraft biofuel production. This is the first report on the production of the undecane compound by bacteria isolated from waterlogged soil and sponge from Antarctica.


Assuntos
Alcanos/metabolismo , Arthrobacter/metabolismo , Biocombustíveis , Pseudoalteromonas/metabolismo , Regiões Antárticas , Microbiologia do Solo
12.
Bioorg Med Chem ; 28(14): 115560, 2020 07 15.
Artigo em Inglês | MEDLINE | ID: mdl-32616183

RESUMO

We report the design, synthesis, and evaluation of a series of 1-oxa-8-azaspiro[4.5]decane and 1,5-dioxa-9-azaspiro[5.5]undecane derivatives as selective σ1 receptor ligands. All seven ligands exhibited nanomolar affinity for σ1 receptors (Ki(σ1) = 0.47 - 12.1 nM) and moderate selectivity over σ2 receptors (Ki(σ2)/ Ki(σ1) = 2 - 44). Compound 8, with the best selectivity among these ligands, was selected for radiolabeling and further evaluation. Radioligand [18F]8 was prepared via nucleophilic 18F-substitution of the corresponding tosylate precursor, with an overall isolated radiochemical yield of 12-35%, a radiochemical purity of greater than 99%, and molar activity of 94 - 121 GBq/µmol. Biodistribution studies of [18F]8 in mice demonstrated high initial brain uptake at 2 min. Pretreatment with SA4503 resulted in significantly reduced brain-to-blood ratio (70% - 75% at 30 min). Ex vivo autoradiography in ICR mice demonstrated high accumulation of the radiotracer in σ1 receptor-rich brain areas. These findings suggest that [18F]8 could be a lead compound for further structural modifications to develop potential brain imaging agents for σ1 receptors.


Assuntos
Compostos Aza/farmacocinética , Receptores sigma/análise , Compostos de Espiro/farmacocinética , Animais , Compostos Aza/síntese química , Compostos Aza/química , Encéfalo/diagnóstico por imagem , Relação Dose-Resposta a Droga , Radioisótopos de Flúor/química , Ligantes , Masculino , Camundongos , Camundongos Endogâmicos ICR , Estrutura Molecular , Ensaio Radioligante , Compostos de Espiro/síntese química , Compostos de Espiro/química , Relação Estrutura-Atividade , Distribuição Tecidual , Receptor Sigma-1
13.
Molecules ; 25(7)2020 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-32231089

RESUMO

The critical roles of keratinocytes and resident mast cells in skin allergy and inflammation have been highlighted in many studies. Cyclic adenosine monophosphate (cAMP), the intracellular second messenger, has also recently emerged as a target molecule in the immune reaction underlying inflammatory skin conditions. Here, we investigated whether undecane, a naturally occurring plant compound, has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes and we further explored the potential involvement of the cAMP as a molecular target for undecane. We confirmed that undecane increased intracellular cAMP levels in mast cells and keratinocytes. In sensitized mast cells, undecane inhibited degranulation and the secretion of histamine and tumor necrosis factor α (TNF-α). In addition, in sensitized keratinocytes, undecane reversed the increased levels of p38 phosphorylation, nuclear factor kappaB (NF-κB) transcriptional activity and target cytokine/chemokine genes, including thymus and activation-regulated chemokine (TARC), macrophage-derived chemokine (MDC) and interleukin-8 (IL-8). These results suggest that undecane may be useful for the prevention or treatment of skin inflammatory disorders, such as atopic dermatitis, and other allergic diseases.


Assuntos
Alcanos/farmacologia , Antialérgicos/farmacologia , Anti-Inflamatórios/farmacologia , Queratinócitos/efeitos dos fármacos , Mastócitos/efeitos dos fármacos , Degranulação Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , AMP Cíclico/metabolismo , Citocinas/genética , Citocinas/metabolismo , Humanos , Mediadores da Inflamação/metabolismo , RNA Mensageiro/genética , Transdução de Sinais
14.
Molecules ; 25(4)2020 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-32075135

RESUMO

Dodonea viscosa (L.) Jacq from Reunion Island (Indian Ocean) was investigated for its leaf essential oil composition. The plant was extracted by hydrodistillation and its essential oil analysed by gas chromatography coupled to mass spectrometry. This study revealed that oxygenated nor-diterpenes and diterpenes were one of the major chemical classes (> 50%) mainly consisting of three modified cyclopropylclerodanes containing a bicyclo[5.4.0]undecane ring system: one new furanoid norditerpene, dodovisate C, and two furanoid diterpenes, the known methyl dodovisate A and the new methyl iso-dodovisate A. These three compounds were isolated by liquid chromatography and their structures established on the basis of spectroscopic studies. The absolute configuration of dodovisate C was elucidated through a joint experimental and theoretical (B3LYP/6-311+G(d,p)) electronic circular dichroism study. The relative configurations of methyl dodovisate A and methyl iso-dodovisate A were determined using linear regressions of theoretical chemical shifts versus experimental values with the (B3LYP/6-311+G(d,p)) method.


Assuntos
Diterpenos Clerodânicos/química , Óleos Voláteis/química , Sapindaceae/química , Cromatografia Líquida de Alta Pressão , Dicroísmo Circular , Diterpenos Clerodânicos/classificação , Diterpenos Clerodânicos/isolamento & purificação , Cromatografia Gasosa-Espectrometria de Massas , Folhas de Planta/química
15.
IUCrdata ; 5(Pt 10): x201380, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36339030

RESUMO

The structure of 7-meth-oxy-penta-cyclo-[5.4.0.02,6.03,10.05,9]undecane-8,11-dione, C12H12O3, at 150 K has monoclinic (P21/c) symmetry. The penta-cyclo-undecane cage compound is composed of four five-membered rings, a planar four-membered ring and a six-membered ring in a boat conformation fused into a closed strained-cage framework. All of the five-membered rings adopt an envelope conformation.

16.
Mar Drugs ; 16(12)2018 11 23.
Artigo em Inglês | MEDLINE | ID: mdl-30477099

RESUMO

Two new bromotyrosine alkaloids, ceratinadins E (1) and F (2), were isolated from an Okinawan marine sponge Pseudoceratina sp. as well as a known bromotyrosine alkaloid, psammaplysin F (3). The gross structures of 1 and 2 were elucidated on the basis of spectroscopic data. The absolute configurations of 1 and 2 were assigned by comparison of the NMR and ECD data with those of a known related bromotyrosine alkaloid, psammaplysin A (4). Ceratinadins E (1) and F (2) are new bromotyrosine alkaloids possessing an 8,10-dibromo-9-methoxy-1,6-dioxa-2-azaspiro[4.6]undeca-2,7,9-trien-4-ol unit with two or three 11-N-methylmoloka'iamine units connected by carbonyl groups, respectively. Ceratinadin E (1) exhibited antimalarial activities against a drug-resistant and a drug-sensitive strains of Plasmodium falciparum (K1 and FCR3 strains, respectively).


Assuntos
Alcaloides/farmacologia , Antimaláricos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Poríferos , Tirosina/análogos & derivados , Alcaloides/química , Alcaloides/isolamento & purificação , Animais , Antimaláricos/química , Antimaláricos/isolamento & purificação , Dicroísmo Circular , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Compostos de Espiro/química , Compostos de Espiro/isolamento & purificação , Compostos de Espiro/farmacologia , Tirosina/química , Tirosina/isolamento & purificação , Tirosina/farmacologia
17.
J Phys Chem Ref Data ; 46(3)2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29230074

RESUMO

This paper presents new wide-ranging correlations for the viscosity and thermal conductivity of n-undecane based on critically evaluated experimental data. The correlations are designed to be used with a recently published equation of state that is valid from the triple point to 700 K, at pressures up to 500 MPa, with densities below 776.86 kg m-3. The estimated uncertainty for the dilute-gas viscosity is 2.4%, and the estimated uncertainty for viscosity in the liquid phase for pressures up to 60 MPa over the temperature range 260 K to 520 K is 5%. The estimated uncertainty is 3% for the thermal conductivity of the low-density gas, and 3% for the liquid over the temperature range from 284 K to 677 K at pressures up to 400 MPa. Both correlations behave in a physically reasonable manner when extrapolated to the full range of the equation of state, however care should be taken when using the correlations outside of the validated range. The uncertainties will be larger outside of the validated range, and also in the critical region.

18.
Int J Biol Macromol ; 98: 407-418, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28153463

RESUMO

The approach of covalent conjugation for coupling synthetic polymers with biomolecules represents an appealing strategy to produce new compounds with distinctive properties for biomedical applications. In the present study we generated hybrid gels with tunable characteristics by using hyaluronic acid (HA) and four variants of poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro[5.5] undecane) (PITAU) copolymers, differing through the molar ratios between comonomers. The new bioconjugate compounds were realized by using a ″grafting to″ strategy, for further ensuring new ways for coupling of various bioactive compounds, taking into account that the grafted copolymers are dual sensitive to pH and temperature. The procedure of chemical crosslinking, by opening the anhydride cycle of the copolymer with the hydroxyl groups of hyaluronic acid, was used to prepare the bioconjugates. The chemical conjugation between HA and PITAU copolymers, as well as the structure of the new compounds, was confirmed by FTIR and NMR techniques. The physical properties of the new gels as thermal stability, swelling capacity, and rheological properties were investigated. The bioconjugate networks were also investigated as drug delivery carriers by using indomethacin as a model drug. In vitro and in vivo tests attested the homogeneity of the bioactive compounds as well as a good biochemical response, showing good biocompatibility for the new structures.


Assuntos
Portadores de Fármacos/química , Ácido Hialurônico/química , Polímeros/química , Piridinas/química , Animais , Géis , Indometacina/química , Indometacina/uso terapêutico , Masculino , Camundongos , Dor Nociceptiva/tratamento farmacológico
19.
Chem Heterocycl Compd (N Y) ; 53(8): 827-845, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-32214420

RESUMO

This review discusses the biological activity and synthesis of 1,9-diazaspiro[5.5]undecanes, including those ring-fused with arenes and heteroarenes and/or containing a carbonyl group at position 2. These compounds could be used for the treatment of obesity, pain, as well as various immune system, cell signaling, cardiovascular, and psychotic disorders.

20.
Int J Pharm ; 515(1-2): 165-175, 2016 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-27725270

RESUMO

Over the last 10 years, the development of intelligent biomaterials for medical and pharmaceutical applications has attracted growing interest by combining interdisciplinary efforts. Between them nanogels represent one of the most attractive carriers for innovative drug delivery systems. In the present investigation new variants of multi-responsive nanogels have been synthesized by crosslinking poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro [5.5] undecane) copolymer (having different molar ratios between comonomers) with 1,12-dodecandiol. The new structures were obtained by using modification of itaconic anhydride moieties in the copolymer. This is a convenient method for the preparation of a network with increased functionality, which further may ensure new strategies for coupling various bioactive compounds, especially owing to the behavior of the used copolymers, which present dual pH and temperature sensitive characteristics. The chemical structure of the new compounds was confirmed by FTIR and 1H RMN spectra. Also, the evaluation of thermal stability by thermogravimetric analysis sustains the covalent bonds occurring between the copolymer and diol. The dual responsiveness of the nanogel structures to temperature and pH was put into evidence by DLS studies. This feature can be used for the development of drug delivery systems, which can mimic biological response behavior to a certain extent. The new synthesized nanogels were tested as drug delivery systems by using diclofenac as a model drug. The results obtained from in vitro and in vivo investigation confirm the bioactivity of the nanogel networks.


Assuntos
Polietilenoglicóis/química , Polietilenoimina/química , Alcanos/química , Materiais Biocompatíveis/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Concentração de Íons de Hidrogênio , Nanogéis , Polímeros/química , Temperatura
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