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@#Firstly, three 3-arylcoumarins 4a- 4c were synthesized from p-aminophenylacetic acid and salicylaldehyde by Perkin condensation reaction and hydrochloric acid acidification; subsequent-amidation reaction of 4a- 4c with substituted benzoyl chlorides 6a- 6h furnished; ten 3-(4′-benzoyl amino-phenyl)coumarins 7a- 7j. The structures of all target compounds were fully characterised by NMR and ESI-MS. Those target compounds were screened for-glucosidase inhibitory and advanced glycation end products(AGEs)formation inhibitory activity. The results showed that compound 7f had good inhibitory activity against α-glucosidase(IC50=10. 84±0. 36 μmol/L); compound 7g possessed much more potent inhibitory activity against AGEs formation(IC50=5. 01±0. 55 μmol/L)than the positive control aminoguanidine hydrochloride(IC50=290. 31±7. 32 μmol/L). These results provided a theoretical basis for further research on antidiabetic drugs.
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Objective· To prepare nanobowls,establish the method for characterizing nanoparticles,and test drug loading efficiency and release efficiency of nanobowls.Methods · The polystyrene nanoparticles (PSNPs) were prepared by the means of the normal emulsion polymerization.The peanuts nanoparticles (PNPs) were synthesized by the swelling process of PSNPs and the selective crosslinking between 3-(trimethoxysilyl) propyl methacrylate and tetraethylorthosilicate.Finally,the polystyrene was dissolved to obtain nanobowls.Dynamic light scattering (DLS) was used to analyze the size of each kind of nanoparticles.Transmission electron microscope (TEM) was used to observe the morphology of nanoparticles.Nanobowls loaded doxorubicin hydrochloride as a model drug though continuous shaking were used to measure drug loading capacity and release efficiency.Results· PSNPs,coated polystyrene nanoparticles (CPSNPs),PNPs,silica peanuts nanoparticles (Si-PNPs) and nanobowls were synthesized successfully.The size of nanobowls was (126.7±4.9) nm and the Zeta potential was (-30.2±1.1) mV.The final nanoparitcles could be used to load drug easily.The drug loading efficiency and loading capacity reached 51.1％ and 9.3％,respectively.Moreover,the nanobowls had the expected sustained release effect.Conclusion · The prepared nanobowls are loaded with drugs successfully,which can release drug slowly and almost completely.The nanobowls can be used for drug release delivery.
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Objective To prepare the puerarin-loaded PEGylated mesoporous silica nanoparticles (PUE@PEG-MSNs) and evaluate its protection on the acute myocardial ischemic rats. Methods PEG-MSNs functionalized mesoporous silica nanoparticles were achieved by the condensation method, and then they were loaded by PUE. The morphology of PUE@PEG-MSNs was examined by detection methods of particle diameter, Zeta potential, transmission electron microscope (TEM), and Fourier transform infrared spectra (FTIR). Moreover, the drug loading and encapsulation rate were measured by HPLC. Sixty acute ischemic myocardial model rats were prepared by coronary artery ligation, and then they were randomly divided into six groups: Sham, MIRI model, puerarin injection, low-, mid-, and high-dose PUE@PEG-MSNs groups. Different doses of PUE@PEG-MSNs and puerarin injection were given 5 min after the ligation. Monitoring the changes of ST, the blood was collected at the end of reperfusion for detecting the changes of serum creatine kinase (CK), lactic dehydrogenase (LDH), aspartate aminotransferase (AST), and malondialdehyde (MDA). The myocardial infarct size was also determined. Results PUE@PEG-MSNs presented uniform spherical morphology and particle size distribution. The particle size and Zeta potential was 300 nm and -30 mV respectively. The drug loading and entrapment efficiency was 14.7% and 67.8% respectively. Both puerarin injection and PUE@PEG-MSNs could reduce the ST-elevation of electrocardiogram, decrease the contents of CK, LDH, AST, and MDA, and reduce the myocardial infarct size. The efficacy of mid- and high-dose PUE@PEG- MSNs groups was better than that of puerarin injection group. Conclusion PUE@PEG-MSNs were successfully prepared and exerted the protective effects on the acute myocardial ischemic rats.
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Objective: To prepare nanobowls, establish the method for characterizing nanoparticles, and test drug loading efficiency and release efficiency of nanobowls. Methods: The polystyrene nanoparticles (PSNPs) were prepared by the means of the normal emulsion polymerization. The peanuts nanoparticles (PNPs) were synthesized by the swelling process of PSNPs and the selective crosslinking between 3-(trimethoxysilyl) propyl methacrylate and tetraethylorthosilicate. Finally, the polystyrene was dissolved to obtain nanobowls. Dynamic light scattering (DLS) was used to analyze the size of each kind of nanoparticles. Transmission electron microscope (TEM) was used to observe the morphology of nanoparticles. Nanobowls loaded doxorubicin hydrochloride as a model drug though continuous shaking were used to measure drug loading capacity and release efficiency. Results: PSNPs, coated polystyrene nanoparticles (CPSNPs), PNPs, silica peanuts nanoparticles (Si-PNPs) and nanobowls were synthesized successfully. The size of nanobowls was (126.7±4.9) nm and the Zeta potential was (-30.2±1.1) mV. The final nanoparitcles could be used to load drug easily. The drug loading efficiency and loading capacity reached 51.1% and 9.3%, respectively. Moreover, the nanobowls had the expected sustained release effect. Conclusion: The prepared nanobowls are loaded with drugs successfully, which can release drug slowly and almost completely. The nanobowls can be used for drug release delivery.
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Abstract Compound usnic acid (1), isolated from lichen Evernia prunastri (Cajamarca-Peru) and the synthesis and characterization of its acyl-hydrazone (2), from the condensation reaction between usnic acid and isoniazid in an ethanol solution under reflux, giving an overall yield of 95%, were evaluated. Both compounds were evaluated and compared with isoniazid according to its anti-Mycobacterium tuberculosis activity based on the tetrazolium microplate assay (TEMA). Compound 1 had MIC (minimal inhibitory concentration) value of 16.0 μg/mL in each test of H37Rv (susceptible type), TB DM 97 (resistant wild type) and MDR DM 1098 (multi drug resistances type) strains. In similar tests, compound 2 MIC values were 2.0, 64.0 and 64.0 μg/mL respectively.
Resumen Se evaluó el ácido úsnico (1), aislado del liquen Evernia prunastri (Cajamarca-Perú), producto natural conocido por sus actividades biológicas, y, del mismo modo, se evaluó la síntesis de su derivado acil-hidrazona (2), obtenido a partir de una reacción de condensación entre el ácido úsnico y la isoniazida en solución etanólica a reflujo, con un rendimiento global de 95%. Ambos compuestos fueron evaluados y comparados con la isoniazida según su actividad anti-Mycobacterium tuberculosis basada en el ensayo de susceptibilidad mediante el método TEMA. Los resultados mostraron que el compuesto 1 presenta valores de MIC de 16,0 μg/mL frente a las cepas H37Rv, TB DM 97 y MDR DM 1098, mientras que el compuesto 2 presenta valores de MIC de 2,0; 64,0 y 64,0 μg/mL respectivamente.
Resumo Foi avaliado o ácido úsnico (1), um produto natural conhecido pelas suas atividades biológicas, isolado a partir do líquen Evernia prunastri (Cajamarca-Peru), assim mesmo foi avaliada a síntese do seu derivado, a acil-hidrazona (2), obtido a partir de uma reação de condensação com refluxo entre o ácido úsnico e a isoniazida em solução etanólica, com um rendimento global de 95%. A atividade anti-Mycobacterium tuberculosis de ambos compostos foi avaliada e comparada com a isoniazida mediante testes de sensibilidade obtidos pelo método TEMA. Os resultados mostraram que o composto 1 apresenta o valor de MIC de 16,0 μg/mL contra variedades H37Rv, TB DM 97 e MDR DM 1098; enquanto que para o composto 2 os valores de MIC são de 2,0; 64,0 e 64,0 μg/mL, respectivamente.
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OBJECTIVE: To synthesize a kind of novel cytotoxin with multi-drug-resistance reverting properties and study their cytotoxicity. METHODS: The target compounds were obtained from N-benzyl-4-piperidones and benzaldehyde derivatives on the condition of 20°C, 7-8 h, taking dry hydrogen chloride as catalyst, using aldol condensation reaction, inspected by TLC and purified through recrystallization. RESULTS: Five N-benzyl-3, 5-bis(arylmethylene)-4-piperidone derivatives were synthesized. The yield was over 49%. Their structures were characterized by 1H-NMR, ESI-MS with melting points. The data of cytotoxicity was obtained. CONCLUSION: The synthetic route is convenient and efficient; The compounds had good inhibiting activity for a few kinds of tumor cells. Copyright 2012 by the Chinese Pharmaceutical Association.