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1.
Fitoterapia ; 153: 104950, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34089787

RESUMO

The root of Isatis indigotica is used as a traditional Chinese medicine (termed Isatidis Radix) due to its antiviral effects. We examined compounds isolated from Isatidis Radix and elucidated the structures of three new natural alkaloids, and we examined the possible mechanisms or active targets of indole alkaloids occurring in blood of rats treated by gavage. Three new natural products were isolated from Radix Isatidis for the first time, including 1-methoxy-2-indoleacetonitrile, 1-hydroxy-3-indoleacetonitrile, 8-Methoxy-1, 2-dihydroquinoline, and 4 compounds isolated from this medicinal material for the first time. Their structures were elucidated using nuclear magnetic resonance. The components of Isatidis Radix were analysed using liquid chromatography tandem mass spectrometry, and 33 compounds were detected in plasma of treated rats; 24 of these compounds were indole alkaloids, and they included the newly identified compounds. Molecular docking and in vitro antithrombin activity tests showed HA inhibition activity of indoleacetonitriles.


Assuntos
Antivirais/farmacologia , Alcaloides Indólicos/farmacologia , Isatis/química , Animais , Antivirais/isolamento & purificação , China , Medicamentos de Ervas Chinesas , Alcaloides Indólicos/isolamento & purificação , Masculino , Simulação de Acoplamento Molecular , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Raízes de Plantas/química , Ratos , Ratos Sprague-Dawley
2.
Transl Pediatr ; 9(5): 713-719, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33209736

RESUMO

The widespread use of carbapenems has caused a notable spread of carbapenem-resistant Klebsiella pneumoniae (CRKP). The incidence of CRKP-associated infections is rising significantly in neonatal intensive care units (NICUs), which poses a grave challenge to clinical treatment. This paper is to highlight the drug treatment of CRKP with purulent meningitis in children and explore the safety of levofloxacin in children. We retrospectively analyzed the clinical data of combination therapy with levofloxacin and aztreonam in a newborn with purulent meningitis caused by CRKP. As clinical pharmacists, we evaluated the risks and benefits of quinolones for anti-infective treatment in newborns, helped clinicians adjust the anti-infective protocol of levofloxacin combined with aztreonam and provided pharmaceutical care throughout the course of treatment. In the end, the child had no fever, no dyspnea, and no obvious abnormalities in brain color Doppler ultrasound. The intracranial infection was finally controlled, and the child improved and was discharged, with no apparent neurological, skeletal, joint, tendon, or cardiac adverse events. For newborns with CRKP-associated purulent meningitis, fluoroquinolones combined with other drugs such as polymyxin, tigecycline, aminoglycosides, minocycline, that Klebsiella pneumoniae is susceptible to (when no safe and effective anti-infective alternatives are available) can reduce the mortality rate of newborns with purulent meningitis caused by carbapenem-resistant gram-negative bacteria. We analyzed the drug resistance mechanisms of CRKP, the selection of antibiotic agents, the safety of quinolones in children, the permeability of the blood-brain barrier to quinolones, and the selection of the quinolone dose. Personalized combination therapy improves treatment outcomes and reduces adverse reactions, especially in patients with resistant bacteria infection.

3.
Zhongguo Zhong Yao Za Zhi ; 39(15): 2814-8, 2014 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-25423814

RESUMO

The contents of adenosine, gastrodin, 4-hydroxybenzyl alcohol, 4-hydroxybenzaldehyde, parishin and sulfur dioxide residue were compared in differently-processed Gastrodiae Rhizoma to provide the basis for a reasonable processing method of Gastrodiae Rhizoma. The analysis was performed on a Merck Purospher STAR column (4.6 mm x 250 mm, 5 µm) with a mobile phase consisting of methanol and water (containing 0.1% formic acid) under gradient elution at a flow rate of 1.0 mL x min(-1). The eluates were detected at 270 nm, and the column temperature was 35°C. The content of adenosin, gastrodin, 4-hydroxybenzyl alcohol, 4-hydroxy-benzaldehyde and parishin in processing of boiling or sulfur-fumigated were lower than that of in processing of steaming. Furthermore, the sulfur dioxide residue of sulphur-fumigated groups exceed 400 mg x kg(-1). This stable and reliable method will contribute to the quality control of different processed Gastrodiae Rhizoma.


Assuntos
Contaminação de Medicamentos , Medicamentos de Ervas Chinesas/química , Gastrodia/química , Dióxido de Enxofre/análise , Tecnologia Farmacêutica/métodos
4.
Pharm Dev Technol ; 16(3): 228-36, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-20136349

RESUMO

Novel magnetic alginate-chitosan beads were prepared for the controlled delivery of albendazole. The magnetic beads were characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM), and vibrating sample magnetometry (VSM). The swelling behavior and in vitro release of albendazole from the beads has been investigated. The magnetic hydrogel beads had showed unique pH-dependent swelling behaviors and a continuous release of the entrapped albendazole occurred. From the magnetometer measurements data, the magnetic alginate-chitosan beads also had superparamagnetic property as well as fast magnetic response. The magnetic beads may be used as a magnetic drug targeting system for albendazole in the gastrointestinal tract.


Assuntos
Albendazol/administração & dosagem , Alginatos/química , Antiprotozoários/administração & dosagem , Quitosana/química , Nanopartículas de Magnetita/química , Albendazol/farmacocinética , Antiprotozoários/farmacocinética , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Hidrogel de Polietilenoglicol-Dimetacrilato/química , Concentração de Íons de Hidrogênio , Magnetismo , Microscopia Eletrônica de Varredura , Microesferas , Espectroscopia de Infravermelho com Transformada de Fourier , Tecnologia Farmacêutica/métodos
5.
Drug Dev Ind Pharm ; 36(7): 867-77, 2010 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-20345282

RESUMO

BACKGROUND: Drug delivery system using polymer-coated magnetic carriers is considered as an effective strategy for passive targeting, which can not only increase drug utilization but also reduce the adverse reaction. With the carriers, sensitivity to physical stimuli (e.g., magnetic field, pH) has been developed and drugs were conjugated to form incorporating magnetic particles, so that drugs could be located to desire position. METHOD: Novel magnetic alginate (Alg)-chitosan (CS) beads loaded with albendazole (ABZ) were prepared and evaluated for pH sensitivity and drug release characteristics. The effects of six different factors (Alg concentration, the weight ratio of drug to polymer, the weight ratio of magnetite nanoparticles to polymer, CaCl2 concentration, CS concentration, the volume ratio of Alg to CS) were studied on the swelling ability of the magnetic beads. The magnetic beads were characterized by Fourier transform infrared spectroscopy, scanning electron microscope, and vibrating sample magnetometry. In addition, the delivery behavior of ABZ from the magnetic beads was studied. RESULT: The magnetic Alg-CS beads had showed unique pH-dependent swelling behaviors and a continuous release of ABZ. From the magnetometer measurements data, the beads also had superparamagnetic property as well as fast magnetic response. CONCLUSION: The pH-sensitive magnetic beads may be used as a magnetic drug targeting system for ABZ in the gastrointestinal tract.


Assuntos
Albendazol/administração & dosagem , Alginatos/química , Anti-Helmínticos/administração & dosagem , Quitosana/química , Portadores de Fármacos , Albendazol/farmacocinética , Anti-Helmínticos/farmacocinética , Materiais Biocompatíveis , Interpretação Estatística de Dados , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Concentração de Íons de Hidrogênio , Magnetismo , Microesferas , Nanopartículas , Polietilenoglicóis/química , Espectroscopia de Infravermelho com Transformada de Fourier , Tecnologia Farmacêutica
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