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1.
Bioorg Chem ; 132: 106342, 2023 03.
Artigo em Inglês | MEDLINE | ID: mdl-36621157

RESUMO

The privileged structure binds to multiple receptors with high affinity, which is helpful to the development of new bioactive compounds. Indole is classified as a privileged structure, which may be one of the most important structural categories in drug discovery. As a special subset of indole compounds, 2-phenylindole seems to be one of most promising forerunners of drug development. In this paper, 106 articles were referenced to review the structural changes, biological activities and structure-activity relationship of compounds in recent 20 years, and classified them according to their pharmacological activities, from several aspects, including anticancer, antibacterial, anti-inflammatory, analgesic, antiviral, anti-parasite, the biological activities target to central nervous system, et al. It also points out the importance of artificial intelligence (AI) technology in discovery of new 2-phenylindole compounds in a broader prospect. This review will provide some ideas for researchers to develop new indole drugs.


Assuntos
Antibacterianos , Inteligência Artificial , Relação Estrutura-Atividade , Antibacterianos/farmacologia , Indóis/farmacologia , Indóis/química , Anti-Inflamatórios não Esteroides/farmacologia
2.
Int J Biol Macromol ; 263(Pt 2): 130452, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38417755

RESUMO

As a traditional Chinese medicinal and edible homologous plant, Onosma glomeratum Y. L. Liu has been used for treating lung diseases in Tibet. In this study, a pectin polysaccharide, OGY-LLPA, with a molecular weight of 62,184 Da, was isolated and characterized by GC-MS and NMR analysis. It mainly consists of galacturonic acid (GalA), galactose (Gal), rhamnose (Rha), and arabinose (Ara), with a linear main chain of galacturonic acid (homogalacturonan, HG) inserted by part of rhamnose galacturonic acid (rhamnogalacturonan, RG), attaching with arabinogalactan (AG) branches at RG-I. Both in the LPS-induced A549 cell model and LPS-induced pneumonia mouse model, OGY-LLPA demonstrated strong anti-inflammatory effects, even comparable to DEX, indicating its potential as an anti-pneumonia candidate agent. Moreover, low-dose OGY-LLPA alleviated LPS-induced pulmonary inflammation by inhibiting the NF-κB signaling pathway. Overall, these findings could not only contribute to the utilization of Onosma glomeratum Y. L. Liu., but also provides a theoretical basis for the treatment of inflammation-related diseases.


Assuntos
Ácidos Hexurônicos , NF-kappa B , Pneumonia , Camundongos , Animais , Lipopolissacarídeos , Ramnose , Polissacarídeos/farmacologia , Polissacarídeos/uso terapêutico , Polissacarídeos/análise , Transdução de Sinais , Pneumonia/induzido quimicamente , Pneumonia/tratamento farmacológico
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