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1.
Front Pharmacol ; 13: 883581, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35645805

RESUMO

Aberrant activation of platelet-derived growth factor receptor α (PDGFRA) has been implicated in tumorigenesis and radioiodine resistance of thyroid cancer, indicating its therapeutic potential. In the present study, we confirmed the association between PDGFRA and radioiodine resistance in thyroid cancer using bioinformatics analysis and constructed a prediction model of PDGFRA inhibitors using machine learning and molecular docking approaches. We then performed a virtual screening of a traditional Chinese medicine (TCM) derived compound library and successfully identified 4',5,7-trimethoxyflavone as a potential PDGFRA inhibitor. Further characterization revealed a significant inhibitory effect of 4',5,7-trimethoxyflavone on PDGFRA-MAPK pathway activation, and that it could upregulate expression of sodium iodide symporter (NIS) as well as improve radioiodine uptake capacity of radioiodine-refractory thyroid cancer (RAIR-TC), suggesting it a potential drug lead for the development of new RAIR-TC therapy.

2.
Chin Med ; 15: 90, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32863859

RESUMO

BACKGROUND: Due to the lack of enough interaction data among compositions, targets and diseases, it is difficult to construct a complete network of Traditional Chinese Medicine (TCM) that comprehensively reflects active compositions and their synergistic network in terms of specific diseases. Therefore, mapping of the full spectrum of interaction between compounds and their targets is of central importance when we use network pharmacology approach to explore the therapeutic potential of the TCM. METHODS: To address this challenge, we developed a large-scale simultaneous interaction prediction approach (SiPA) integrated one interaction network based simple inference model (SIM), focusing on 'logical relevance' between compounds, proteins or diseases, and another compound-target correlation space based interaction prediction model (CTCS-IPM) that was built on the basis of the canonical correlation analysis (CCA) to estimate the position of compounds (or targets) in compound-protein correlated space. Then SiPA was applied to discover reliable multiple interactions for interaction network expansion of a TCM, compound Salvia miltiorrhiza. By means of network analysis, potential active compounds and their related network synergy underlying cardiovascular diseases were evaluated between expanded and original interaction networks. Part of new interactions were validated with existing experimental evidence and molecular docking. RESULTS: As evaluated with known test dataset, the established combination approach was proved to make highly accurate prediction, showing a well prediction performance for the SIM and a high recall rate of 85.2% for the CTCS-IPM. Then 710 pairs of new compound-target interactions, 24 pairs of new compound-cardiovascular disease interactions and 294 pairs of new cardiovascular disease-protein interactions were predicted for compound Salvia miltiorrhiza. Results of network analysis suggested the network expansion could dramatically improve the completeness and effectiveness of the network. Validation results of literature and molecular docking manifested that inferred interactions had good reliability. CONCLUSIONS: We provided a practical and efficient way for large-scale inference of multiple interactions of TCM ingredients, which was not limited by the lack of negative samples, sample size and target 3D structures. SiPA could help researchers more accurately prioritize the effective compounds and more completely explore network synergy of TCM for treating specific diseases, indicating a potential way for effectively identifying candidate compound (or target) in drug discovery.

3.
Bioelectromagnetics ; 41(2): 148-155, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31912926

RESUMO

The dielectric properties of normal and tumor human tissues have been widely reported in recent years. However, the dielectric properties of intrathoracic lymph nodes (LNs) have not been reported. In this communication, we measured the dielectric properties (i.e., permittivity and conductivity) of ex vivo intrathoracic LNs obtained from lung cancer surgeries. Results show that the permittivity and conductivity of metastatic LNs are higher than those of normal LNs over the frequency range of 1 MHz-4 GHz. Statistically significant differences are observed at single specific frequencies (64, 128, 298, 433, and 915 MHz and 2.45 GHz). Our study provides the basic data to support future-related research and fills the research gap on the dielectric properties of LNs in the lungs. Bioelectromagnetics. 2020;41:148-155. © 2020 Bioelectromagnetics Society.


Assuntos
Neoplasias Pulmonares/patologia , Linfonodos/química , Linfonodos/patologia , Adulto , Idoso , Condutividade Elétrica , Humanos , Neoplasias Pulmonares/cirurgia , Metástase Linfática/patologia , Pessoa de Meia-Idade
4.
J Asian Nat Prod Res ; 19(10): 993-999, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28671852

RESUMO

In our research on novel secondary metabolites from micro-organisms, two new (1-2) and four known dihydroisocoumarins (3-6) were derived from soil fungus Hypoxylon sp. Their structures were determined with extensive NMR data analysis and ECD calculation comparing with those of experimental CD spectra. Interestingly, compounds 1 and 2 possessed the same planar structure and very similar NMR data, suggesting 1 and 2 were a pair of epimers at either C-3 or at C-4, confirmed by the totally opposite cotton effect around 250 nm in the CD spectra of 1 and 2. Moreover, for the first time, we revealed that the CD absorption peak at 250 nm was dominated by C-3 orientation, rather than the orientation of C-3 substituents, by intensive ECD investigations.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Isocumarinas/isolamento & purificação , Xylariales/química , Medicamentos de Ervas Chinesas/química , Isocumarinas/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Microbiologia do Solo , Estereoisomerismo
5.
Sheng Wu Yi Xue Gong Cheng Xue Za Zhi ; 27(6): 1233-6, 2010 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-21374970

RESUMO

This article is devoted to the design of a system for modulating intermediate frequency electrotherapy waveform output. Prescriptions with different output waveform combinations were produced using microcontroller unit (MCU). The rich output waveforms effectively improve tolerance of human adaptability and achieve a therapeutic effect.


Assuntos
Terapia por Estimulação Elétrica/instrumentação , Microcomputadores , Desenho Assistido por Computador , Desenho de Equipamento , Humanos , Design de Software
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