Target Identification of Bioactive Natural Products

Zhou, Yiqing; Xiao, Youli

doi:10.6023/a17110484

Cited by 8 publications

(2 citation statements)

References 49 publications

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“…The interaction of active natural products with intracellular targets is the foundation for producing pharmacological effects. Proteins are major executors of cellular functions, while the targets are proteins that interact with natural products in most cases ( Zhou and Xiao, 2017 ). The quantitative proteomics research strategy of TMT labeling, which is a common high-throughput screening method ( Ross et al, 2004 ; Kalesh et al, 2016 ), is used to identify the probable intracellular targets of licoricidin against MGC-803 cells.…”

Section: Discussionmentioning

confidence: 99%

Licoricidin combats gastric cancer by targeting the ICMT/Ras pathway in vitro and in vivo

Bai

et al. 2022

Front. Pharmacol.

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Licoricidin, a type of isoflavonoid, is extracted from the root of Glycyrrhiza glabra. It has been widely proven that licoricidin possesses multiple biological activities, including anti-cancer effects and a powerful antimicrobial effect against Helicobacter pylori (H. pylori). However, the exact mechanism of licoricidin against gastric cancer remains unclear. In this study, we comprehensively explored the effects of licoricidin on MGC-803 gastric cancer cells in vitro and in vivo and further elucidated its mechanism of action. Our results revealed that licoricidin exhibited multiple anti-gastric cancer activities, including suppressing proliferation, inducing apoptosis, arresting the cell cycle in G0/G1 phase, and inhibiting the migration and invasion abilities of MGC-803 gastric cancer cells. In addition to this, a total of 5861 proteins were identified by quantitative proteomics research strategy of TMT labeling, of which 19 differential proteins (two upregulated and 17 downregulated) were screened out. Combining bioinformatics analyses and the reported roles in cancer progression of the 19 proteins, we speculated that isoprenyl carboxyl methyltransferase (ICMT) was the most likely target of licoricidin. Western blot assays and IHC assays subsequently proved that licoricidin significantly downregulated the expression of ICMT, both in MGC-803 cells and in xenograft tumors. Moreover, licoricidin effectively reduced the level of active Ras-GTP and blocked the phosphorylation of Raf and Erk, which may be involved in its anti-gastric cancer effects. In summary, we first demonstrated that licoricidin exerted favorable anti-gastric cancer activities via the ICMT/Ras pathway, which suggests that licoricidin, as a natural product, could be a novel candidate for the management of gastric cancer.

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Section: Discussionmentioning

confidence: 99%

Licoricidin combats gastric cancer by targeting the ICMT/Ras pathway in vitro and in vivo

Bai

et al. 2022

Front. Pharmacol.

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“…Many publications have systematically introduced the techniques for active targets of natural products ( Zeng and Peng, 2018;Zhou and Xiao, 2018) as quantitative mass spectrometry. We briefly introduce the frontier techniques in CCMF research below, such as CETSA, DARTS and MST.…”

Section: Research Methods Of Molecular Targetsmentioning

confidence: 99%

Compound-based Chinese medicine formula: From discovery to compatibility mechanism

Luan

Zhang

et al. 2020

Journal of Ethnopharmacology

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Ethnopharmacological relevance: Chinese medicine formula (CMF) has a long history of clinical use in the treatment of various diseases under the guidance of traditional Chinese medicine (TCM) theory. The application of CMF can be divided into three levels, crude extracts, homologous compounds mixture, and specific compounds. However, the modern scientific connotation of the CMF theory has not been clarified. Aim of the review: To critically evaluate the research strategy for the investigation of compound-based CMF (CCMF). Materials and methods: The related information was collected from the scientific databases, including CNKI, Elsevier, ScienceDirect, PubMed, SpringerLink, Web of Science, and Wiley Online. Results: The research design including discovery, screening, optimization, pharmacodynamics models, and target research techniques including the targets for compatibility compounds were evaluated. Essentially it has been evaluated that the in vitro multicellular three-dimensional culture or organoid model has been proposed for the optimization model for compatibility research of CCMF. Based on these, the traditional compatibility theory of CMF, such as Monarch-Minister-Assistant-Guide (Jun-Chen-Zuo-Shi in Chinese), can probably be elucidated by the CCMF research. Conclusions: CCMF has the clear advantage of providing the exact composition and controllable quality of modern medicines, in addition to having the characteristics of multi-ingredients and multi-targets synergistic effects of TCM. However, CCMF is still associated with challenges which need to be addressed for its future use.

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Native-compound-Coupled Affinity Matrix (NCAM) in target identification and validation of bioactive compounds: Application, mechanism and outlooks

Ma,

Li,

Gou

et al. 2023

Bioorganic Chemistry

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Target Identification of Bioactive Natural Products

Cited by 8 publications

References 49 publications

Licoricidin combats gastric cancer by targeting the ICMT/Ras pathway in vitro and in vivo

Licoricidin combats gastric cancer by targeting the ICMT/Ras pathway in vitro and in vivo

Compound-based Chinese medicine formula: From discovery to compatibility mechanism

Native-compound-Coupled Affinity Matrix (NCAM) in target identification and validation of bioactive compounds: Application, mechanism and outlooks

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