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Ultra High-Performance Liquid Chromatography-Mass Spectrometry and Self-established Database Analysis of Chinese Herbal Medicine Components

Chinese herbal medicine is complex and has numerous unknown compounds, making qualitative research crucial. Ultra-high-performance liquid chromatography ...

high-resolution-tandem-mass-spectrometry-for-studying-chemical

High-resolution Tandem Mass Spectrometry for Studying Chemical Constituents of <em>Gynura bicolor DC</em>

The separation and analysis of the desired chemical components are important subjects for the fundamental research of traditional Chinese medicine (TCM). ...

Chongqing Traditional Chinese Medicine Hospital

Chongqing Hospital of Traditional Chinese Medicine

Aloe-emodin (AE) is among the primary bioactive anthraquinones present in traditional Chinese medicinal plants such as Rheum palmatum L. Multidrug resistance protein 2 (ABCC2/ MRP2) is an important efflux transporter of substances associated with cellular oxidative stress. However, the effects of traditional Chinese medicine on this protein remain unclear.

Aloe-emodin induces hepatotoxicity by the inhibition of multidrug resistance protein 2.

The glyoxalase system is a ubiquitous enzymatic network which plays important roles in biological life. It consists of glyoxalase 1 (GLO1), glyoxalase 2 (GLO2), and reduced glutathione (GSH), which perform an essential metabolic function in cells by detoxifying methylglyoxal (MG) and other endogenous harmful metabolites into non-toxic d-lactate. MG and MG-derived advanced glycation endproducts (AGEs) are associated with various diseases, such as diabetes, cardiovascular disease, neurodegenerative disorders and cancer, and GLO1 is a key rate-limiting enzyme in the anti-glycation defense. The abnormal activity and expression of GLO1 in various diseases make this enzyme a promising target for drug design and development. This review focuses on the regulatory mechanism of GLO1 in diverse pathogenic conditions with a thorough discussion of GLO1 regulators since their discovery, including GLO1 activators and inhibitors. The different classes, chemical structure and structure-activity relationship are embraced. Moreover, assays for the discovery of small molecule regulators of the glyoxalase system are also introduced in this article. Compared with spectrophotometer-based assay, microplate-based assay is a more simple, rapid and quantitative high-throughput method. This review will be useful to design novel and potent GLO1 regulators and hopefully provide a convenient reference for researchers.

Glyoxalase system: A systematic review of its biological activity, related-diseases, screening methods and small molecule regulators.

The Src-homology 2 domain-containing phosphatase 2 (SHP2), which is encoded by PTPN11, participates in many cellular signaling pathways and is closely related to various tumorigenesis. Inhibition of the abnormal activity of SHP2 by small molecules is an important part of cancer treatment. Here, three abietane diterpenoids, named compounds -, were isolated from  var. . Spectroscopic analysis was used to identify the exact structure of the compounds. The enzymatic kinetic experiment and the cellular thermal shift assay showed compound  selectively inhibited SHP2 activity in vitro. Molecular docking indicated compound  targeted the SHP2 catalytic domain. The predicted pharmacokinetic properties by SwissADME revealed that compound  passed the majority of the parameters of common drug discovery rules. Compound  restrained A549 proliferation (IC = 8.68 ± 0.96 μM), invasion and caused A549 cell apoptosis by inhibiting the SHP2-ERK/AKT signaling pathway. Finally, compound  (Ajuforrestin A) is a potent and efficacious SHP2 inhibitor and may be a promising compound for human lung epithelial cancer treatment.

Chunyan Zhou

General Surgery

Chongqing Traditional Chinese Medicine Hospital

Ultra High-Performance Liquid Chromatography-Mass Spectrometry and Self-established Database Analysis of Chinese Herbal Medicine Components

High-resolution Tandem Mass Spectrometry for Studying Chemical Constituents of Gynura bicolor DC

Chunyan Zhou

.css-o250i3{font-size:18px;font-family:Open Sans,sans-serif;line-height:21.6px;}General Surgery

Chongqing Traditional Chinese Medicine Hospital

Ultra High-Performance Liquid Chromatography-Mass Spectrometry and Self-established Database Analysis of Chinese Herbal Medicine Components

High-resolution Tandem Mass Spectrometry for Studying Chemical Constituents of Gynura bicolor DC

General Surgery