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1.
Bioorg Chem ; 148: 107482, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38795582

RESUMEN

Toad venom, a traditional Chinese medicine, exhibits remarkable medicinal properties of significant therapeutic value. The peptides present within toad venom possess a wide range of biological functions, yet the neuropeptide B (NPB) and it modification requires further exploration to comprehensively understand its mechanisms of action and potential applications. In this study, a fusion peptide, ANTP-BgNPB, was designed to possess better analgesic properties through the transdermal modification of BgNPB. After optimizing the conditions, the expression of ANTP-BgNPB was successfully induced. The molecular dynamics simulations suggested that the modified protein exhibited improved stability and receptor binding affinity compared to its unmodified form. The analysis of the active site of ANTP-BgNPB and the verification of mutants revealed that GLN3, SER38, and ARG42 were crucial for the protein's recognition and binding with G protein-coupled receptor 7 (GPR7). Moreover, experiments conducted on mice using the hot plate and acetic acid twist body models demonstrated that ANTP-BgNPB was effective in transdermal analgesia. These findings represent significant progress in the development of transdermal delivery medications and could have a significant impact on pain management.


Asunto(s)
Analgésicos , Diseño de Fármacos , Animales , Analgésicos/química , Analgésicos/farmacología , Ratones , Péptidos/química , Péptidos/farmacología , Administración Cutánea , Masculino , Relación Estructura-Actividad , Simulación de Dinámica Molecular , Estructura Molecular , Relación Dosis-Respuesta a Droga , Dolor/tratamiento farmacológico , Humanos
2.
Molecules ; 28(8)2023 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-37110862

RESUMEN

Toad venom is a traditional Chinese medicine with high medicinal value. The existing quality evaluation standards of toad venom have obvious limitations because of the lack of research on proteins. Thus, it is necessary to screen suitable quality markers and establish appropriate quality evaluation methods for toad venom proteins to guarantee their safety and efficacy in clinical applications. SDS-PAGE, HPLC, and cytotoxicity assays were used to analyze differences in protein components of toad venom from different areas. Functional proteins were screened as potential quality markers by proteomic and bioinformatic analyses. The protein components and small molecular components of toad venom were not correlated in content. Additionally, the protein component had strong cytotoxicity. Proteomics analysis showed that 13 antimicrobial proteins, four anti-inflammatory and analgesic proteins, and 20 antitumor proteins were differentially expressed extracellular proteins. A candidate list of functional proteins was coded as potential quality markers. Moreover, Lysozyme C-1, which has antimicrobial activity, and Neuropeptide B (NPB), which has anti-inflammatory and analgesic activity, were identified as potential quality markers for toad venom proteins. Quality markers can be used as the basis of quality studies of toad venom proteins and help to construct and improve safe, scientific, and comprehensive quality evaluation methods.


Asunto(s)
Venenos de Anfibios , Bufanólidos , Animales , Venenos de Anfibios/química , Proteómica , Bufonidae , Medicina Tradicional China , Antiinflamatorios , Bufanólidos/farmacología
3.
Int J Med Mushrooms ; 23(8): 25-37, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34587423

RESUMEN

Continuous monoculture can increase plant morbidity and reduce crop yields. However, the Ganoderma lucidum mushroom possesses unique nutrient acquisition methods and displays an altered response to the generation of reactive oxygen species (ROS). The effects of continuous cropping on G. lucidum remain unclear. Here, we investigated the effects of consecutive monoculture soil on the yield, bioactive components, antioxidant properties, nutrient metabolism, and enzyme activity of G. lucidum. The results showed no significant differences in terms of yield between the control check and treatment groups after 2 years. However, the content of polysaccharides and triterpenoids after 2 years of treatment and the content of total phenols and flavonoids after 3 years of treatment significantly increased. Moreover, the antioxidant activity (AOA) of the polysaccharides under consecutive monoculture soil treatments also significantly increased. These differences were caused by changes in nutrient metabolism and the activities of antioxidant and ligninolytic enzymes. Under continuous monoculture soil treatment, the content of reducing sugars, water-soluble sugars, free amino acids, and water-soluble proteins significantly increased. The activities of superoxide dismutase, manganese peroxidase, and lignin peroxidase increased with the time of continuous monoculture, while the activities of peroxidase, catalase, and laccase decreased. The increase in ligninolytic enzymes was postulated to mediate the ROS scavenging ability of G. lucidum. In conclusion, continuous cropping soil could increase the levels of bioactive components and AOAs of G. lucidum.


Asunto(s)
Agaricales , Reishi , Antioxidantes/análisis , Flavonoides , Suelo
4.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 27(5): 444-8, 2007 May.
Artículo en Chino | MEDLINE | ID: mdl-17650801

RESUMEN

OBJECTIVE: To observe the changes of behavior and amino acids in brain tissue of rats with adjuvant arthritis, and effects of Xinfeng Capsule (XFC) on them. METHODS: AA model was induced by complete Freund's adjuvant in rats. Five groups including the normal control group, the model group, the XFC group, the methotrexate (MTX) group and the Tripterygium wilfordii polysaccharide (TPT) group were set up. The changes of behavior, amino acids in brain tissue, swelling degree of joints, and arthritis index (AI) were observed and the correlation analysis on these indexes was performed. RESULTS: Compared with those in the normal control, the frequency of independent activity obviously decreased in the model rats, accompanied with increased number of step-down errors, shortened step down latency (SDL) and prolonged escape latency (EL), also the level of gamma-aminobutyric acid (GABA) in brain tissue elevated and glutamic acid (GLU)/GABA reduced (P <0.05). Compared with those in the model group, all the above indexes were improved significantly in the XFC group after treatment (P <0.05), while they changed insignificantly in the MTX and TPT groups (P> 0.05), the degree of joint swelling and AI were obviously lower in the 3 treated groups (P< 0.05). Correlation analysis showed the frequency of independent activity and SDL were negatively correlated to the swelling degree of joint, and levels of AI, glycine (GLY) and GABA respectively, but positively correlated with GLU/GABA (P<0.05); while EL and number of step-down errors were positively correlated to AI, GLY and GABA respectively, but negatively correlated to GLU/GABA (P < 0.05). CONCLUSION: Immune stress could lead to the changes of rat behavior and amino acids in brain tissue. XFC treatment could improve the behavior of AA rats through regulating the levels of amino acids in brain tissue.


Asunto(s)
Aminoácidos/metabolismo , Artritis Experimental/fisiopatología , Conducta Animal/efectos de los fármacos , Encéfalo/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Animales , Conducta Animal/fisiología , Encéfalo/metabolismo , Cápsulas , Masculino , Distribución Aleatoria , Ratas , Ratas Wistar , Resultado del Tratamiento
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