Reckoning apigenin and kaempferol as a potential multi-targeted inhibitor of EGFR/HER2-MEK pathway of metastatic colorectal cancer identified using rigorous computational workflow

Sharma, Abhilasha; Sinha, Sonam; Rathaur, Pooja; Vora, Jaykant; Jha, Prakash C.; Johar, Kaid; Rawal, Rakesh; Shrivastava, Neeta

doi:10.1007/s11030-022-10396-7

Cited by 6 publications

(1 citation statement)

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“…More and more evidence shows that M11 (chrysin) has strong antitumor activity and inhibits drug resistance through Notch 1, microRNAs, signal transducer and activator of transcription 3 (STAT 3), nuclear factor kappa B (NF-κB), PI 3 K/Akt, MAPK, and other molecular pathways [27]. M1 (apigenin) and M3 (kaempferol) are potential inhibitors of EGFR, HER 2, and MEK 1 [28]. M1 (apigenin) significantly inhibited the activation of MAPK pathways in downstream inflammation by reducing the expression of TNF-α, IL-6, and NF-κB, as well as the expression of apoptotic proteins Bax and caspase-3 [29].…”

Section: Biological Activity Of Galangin and Its Metabolitesmentioning

confidence: 99%

Analysis of Galangin and Its In Vitro/In Vivo Metabolites via Ultra-High-Performance Liquid Chromatography/Quadrupole Time-of-Flight Mass Spectrometry

Feng

Ma²,

Yin

et al. 2022

Metabolites

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Galangin, a naturally available flavonoid, induces a variety of pharmacological activities and biological effects via several mechanisms. However, in vivo metabolism of galangin has not been fully explored, which means knowledge of its pharmacodynamics and application potential is limited. The objective of this study was to establish an ultra-high-performance liquid chromatography–quadrupole time-of-flight mass spectrometry method for the rapid profiling and identification of galangin metabolites in vitro and in vivo using unique online information-dependent acquisition with multiple mass defect filtering combined with dynamic background subtraction in positive ion mode. A total of 27 metabolites were detected and characterized, among which eight metabolites in liver microsomes and four metabolites in intestinal microflora were characterized, and 27 metabolites from rat plasma, bile, urine, feces, and a number of different tissue samples were characterized. Thirteen major metabolic pathways including hydrogenation, hydroxylation, glycosylation, methylation, acetylation, glucuronidation, and sulfation were observed to be attributable to the biotransformation of the metabolites. This study provides evidence for the presence of in vitro and in vivo metabolites and the pharmacokinetic mechanism of galangin. Moreover, the study promotes the further development and utilization of galangin and the plant from which it is derived, Alpinia officinarum Hance.

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Section: Biological Activity Of Galangin and Its Metabolitesmentioning

confidence: 99%