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1.
Zhongguo Zhong Yao Za Zhi ; 46(1): 130-138, 2021 Jan.
Artigo em Zh | MEDLINE | ID: mdl-33645062

RESUMO

As a precious traditional Chinese medicine(TCM), snake bile has been widely used in numerous Chinese medicine prescriptions. Bile acid(BA) derivatives have been demonstrated as the primary chemical family in snake bile. In-depth chemical characterization of BAs is of great importance towards the establishment of quality standards and clarification of the effective material basis for snake bile. This study firstly employed ~1H-NMR to preliminarily analyze the chemical profiles of snake bile, an automated fraction collector was subsequently implemented to obtain the fractions-of-interest. The fraction was then concentrated and re-analyzed by LC-MS. Based on ~1H-NMR, BAs were found to be the main components of snake bile, and six BAs including CDCA, CA, TCDCA, TCA, TDCA and GCA were tentatively identified from the representative spectrum with the assistance of literature and reference compounds. Whereas the content of TCA in snake bile was too great, resulting in a great obstacle for the detection of trace components, the automated fraction collector was subsequently implemented to obtain the fractions-of-interest for LC-MS analysis. According to matching MS/MS information and retention time with reference compounds as well as database retrieval, a total of 57 BAs were detected and annotated. Because of the combination of ~1H-NMR and LC-MS platforms, the findings are beneficial for the in-depth characterization of BAs in snake bile, which provides references for the establishment of quality control and evaluation methods of snake bile.


Assuntos
Ácidos e Sais Biliares , Espectrometria de Massas em Tandem , Animais , Bile , Cromatografia Líquida , Serpentes
2.
Eur J Med Chem ; 201: 112510, 2020 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-32592915

RESUMO

ß-Lactam, commonly referred as azetidin-2-one, is a multifunctional building block for synthesizing ß-amino ketones, γ-amino alcohols, and other compounds. Besides its well known antibiotic activity, this ring system exhibits a wide range of activities, attracting the attention of researchers. However, the structurally diverse ß-lactam analogues as anticancer agents and their different molecular targets are poorly discussed. The purpose of this review is 3-fold: (1) to explore the molecular hybridization approach to design ß-lactams hybrids as anticancer agents; (2) the structure activity relationship of the most active anticancer ß-lactams and (3) to summarize their antitumor mechanisms.


Assuntos
Antineoplásicos/farmacologia , beta-Lactamas/farmacologia , Animais , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Desenho de Fármacos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , beta-Lactamas/química
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