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1.
Zhongguo Zhong Yao Za Zhi ; 42(16): 3152-3158, 2017 Aug.
Artículo en Zh | MEDLINE | ID: mdl-29171235

RESUMEN

Isocorydine and its analogs were extracted from Dicranostigma leptopodum and Stephania yunnanensis through the method of natural products chemistry. Its derivatives were prepared by chemical structure modifications from isocorydine. MTT method was used to study the inhibitory effect of those compounds on the growth of HepG2, HeLa and MGC-803 cancer cell lines in vitro. The results showed that isocorydine and its analogs all have the growth inhibition for those cancer cell lines. This paper investigated the structure-activity relationship of isocorydine and its derivatives with anticancer activity in the aspect of stereochemical structure, functional groups positions of the compounds and the electron density of aromatic rings based on the single crystal diffraction structure and the molecular docking of EGFR and isocorydine.


Asunto(s)
Antineoplásicos/farmacología , Aporfinas/farmacología , Línea Celular Tumoral , Receptores ErbB , Humanos , Simulación del Acoplamiento Molecular , Estructura Molecular , Relación Estructura-Actividad
2.
Huan Jing Ke Xue ; 44(8): 4479-4488, 2023 Aug 08.
Artículo en Zh | MEDLINE | ID: mdl-37694642

RESUMEN

Cadmium (Cd) heavy metal pollution has posed serious threats to soil health and the safe production utilization of agricultural products. A pot experiment was conducted to study the effects of biochar (BC) and nitrogen fertilizer with three levels, namely 2.6 g·pot-1 (N1), 3.5 g·pot-1 (N2), 4.4 g·pot-1 (N3) biochar combined with nitrogen fertilizer (BCN1, BCN2, and BCN3), on soil Cd fractions, Cd enrichment, the transport of rice, and soil enzyme activity, as well as the changes in microbial community composition and complex interactions between microorganisms through high-throughput sequencing. The results showed that biochar combined with nitrogen fertilizer led to the transformation of Cd from the exchangeable state to the residue state, and the proportion of the exchangeable state was significantly reduced by 6.2%-14.7%; by contrast, the proportion of the residue state increased by 18.6%-26.4% relative to that in CK. In addition, singular treatments of nitrogen fertilizer enhanced the accumulation capacities of Cd in roots, which increased by 22%-33.5% compared with that in CK. By contrast, the BC and BCN treatments reduced Cd accumulation in roots and the transfer capacity from stems to rice husks and husk to rice. Furthermore, the BCN treatments promoted soil enzyme activities (urease, acid phosphatase, invertase, and catalase). MiSeq sequencing showed that BCN treatments increased the abundance of the main species of soil bacterial microbes (such as Acidobacteriales, Solibacterales, Pedosphaerales, and Nitrospirales). Moreover, co-occurrence network analysis showed that the complexity of the soil bacterial network was enhanced under the N, BC, and BCN treatments. Overall, biochar combined with nitrogen fertilizer reduced soil Cd availability, inhibited the capacity of Cd accumulation and the transport of rice, and improved the soil eco-environmental quality. Thus, using BCN could be a feasible practice for the remediation of Cd-polluted agricultural soil.


Asunto(s)
Cadmio , Oryza , Fertilizantes , Suelo , Acidobacteria , Nitrógeno
3.
Curr Pharm Biotechnol ; 22(1): 159-167, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-32216736

RESUMEN

BACKGROUND: Tripterine (TRI), an active monomer in Tripterygium wilfordii, has significant pharmacological activities, such as anti-inflammatory, immunosuppressive and anti-tumor activities. TRI may be used to treat allergic diseases because of its characteristics of immunosuppression. OBJECTIVE: This study aims to explore the anti-allergic effect of TRI. METHODS: It was tested in vivo and in vitro in this study. RESULTS: The results showed that TRI could significantly inhibit histamine release from rat peritoneal mast cells; the inhibitory effect of TRI on histamine release was stronger than that of other known histamine inhibitors such as disodium cromoglyceride. TRI also significantly inhibited systemic anaphylactic shock induced by compound 48/80 and skin allergy induced by IgE, and inhibited the expression of inflammatory factors secreted by Human Mast Cells (HMC-1) induced by Phorbol 12-Myristate 13- Acetate (PMA) and calcium carrier A23187. In the animal model of allergic rhinitis induced by Ovalbumin (OA), the scores of friction, histamine, IgE, inflammatory factors and inflammatory cells decreased after TRI was administered orally or nasally. CONCLUSION: TRI, as an active immunoregulatory factor, has great potential in the treatment of mast cell-mediated allergic diseases.


Asunto(s)
Anafilaxia/tratamiento farmacológico , Antialérgicos/farmacología , Liberación de Histamina/efectos de los fármacos , Mastocitos/efectos de los fármacos , Rinitis Alérgica/tratamiento farmacológico , Triterpenos/farmacología , Animales , Antialérgicos/uso terapéutico , Calcimicina/farmacología , Citocinas/metabolismo , Modelos Animales de Enfermedad , Medicamentos Herbarios Chinos/uso terapéutico , Humanos , Masculino , Mastocitos/metabolismo , Ratones Endogámicos BALB C , FN-kappa B/metabolismo , Triterpenos Pentacíclicos , Ratas , Rinitis Alérgica/inmunología , Acetato de Tetradecanoilforbol/farmacología , Triterpenos/uso terapéutico , p-Metoxi-N-metilfenetilamina/farmacología
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