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Gastric cancer (GC) has posed a great threat to the lives of people around the world. To date, safer and more cost-effective therapy for GC is lacking. Traditional Chinese medicine (TCM) may provide some new options for this. Guiqi Baizhu Formula (GQBZF), a classic TCM formula, has been extensively used to treat GC, while its bioactive components and therapeutic mechanisms remain unclear. In this study, we evaluated the underlying mechanisms of GQBZF in treating GC by integrative approach of chemical bioinformatics. GQBZF lyophilized powder (0.0625 mg/mL, 0.125 mg/mL) significantly attenuated the expression of p-IGF1R, PI3K, p-PDK1, p-VEGFR2 to inhibit the proliferation, migration and induce apoptosis of gastric cancer cells, which was consistent with the network pharmacology. Additionally, atractylenolide Ⅰ, quercetin, glycyrol, physcione and aloe-emodin, emodin, kaempferol, licoflavone A were found to be the key compounds of GQBZF regulating IGF1R and VEGFR2, respectively. And among which, glycyrol and emodin were determined as key active compounds against GC by farther vitro experiments and LC/MS. Meanwhile, we also found that glycyrol inhibited MKN-45 cells proliferation and enhanced apoptosis, which might be related to the inhibition of IGF1R/PI3K/PDK1, and emodin could significantly attenuate the MKN-45 cells migration, which might be related to the inhibition of VEGFR2-related signaling pathway. These results were verified again by molecular dynamics simulation and binding interaction pattern. In summary, this study suggested that GQBZF and its key active components (glycyrol and emodin) can suppress IGF1R/PI3K/PDK1 and VEGFR2-related signaling pathway, thereby inhibiting tumor cell proliferation and migration and inducing apoptosis. These findings provided an important strategy for developing new agents and facilitated clinical use of GQBZF against GC.

Titel:	Elucidation of the anti-gastric cancer mechanism of Guiqi Baizhu Formula by integrative approach of chemical bioinformatics.
Autor/in / Beteiligte Person:	Wang, Y ; Li, J ; Liu, X ; Zhang, Y ; Wang, C ; Guo, Q ; Jiang, B ; Jin, X ; Liu, Y
Link:	Zum Volltext
Zeitschrift:	International immunopharmacology, Jg. 134 (2024-06-15), S. 112245
Veröffentlichung:	Amsterdam ; New York : Elsevier Science, c2001-, 2024
Medientyp:	academicJournal
ISSN:	1878-1705 (electronic)
DOI:	10.1016/j.intimp.2024.112245
Schlagwort:	Humans Cell Line, Tumor Signal Transduction drug effects Pyruvate Dehydrogenase Acetyl-Transferring Kinase metabolism Phosphatidylinositol 3-Kinases metabolism Receptors, Somatomedin metabolism Network Pharmacology Antineoplastic Agents, Phytogenic pharmacology Stomach Neoplasms drug therapy Stomach Neoplasms metabolism Drugs, Chinese Herbal pharmacology Drugs, Chinese Herbal chemistry Cell Proliferation drug effects Apoptosis drug effects Cell Movement drug effects Receptor, IGF Type 1 metabolism Vascular Endothelial Growth Factor Receptor-2 metabolism Computational Biology methods
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article Language: English [Int Immunopharmacol] 2024 Jun 15; Vol. 134, pp. 112245. <i>Date of Electronic Publication: </i>2024 May 14. MeSH Terms: Stomach Neoplasms* / drug therapy ; Stomach Neoplasms* / metabolism ; Drugs, Chinese Herbal* / pharmacology ; Drugs, Chinese Herbal* / chemistry ; Cell Proliferation* / drug effects ; Apoptosis* / drug effects ; Cell Movement* / drug effects ; Receptor, IGF Type 1* / metabolism ; Vascular Endothelial Growth Factor Receptor-2* / metabolism ; Computational Biology* / methods ; Humans ; Cell Line, Tumor ; Signal Transduction / drug effects ; Pyruvate Dehydrogenase Acetyl-Transferring Kinase / metabolism ; Phosphatidylinositol 3-Kinases / metabolism ; Receptors, Somatomedin / metabolism ; Network Pharmacology ; Antineoplastic Agents, Phytogenic / pharmacology Contributed Indexing: Keywords: Emodin; Gastric cancer; Glycyrol; Guiqi Baizhu Formula; IGF1R/PI3K/PDK1; VEGFR2 Substance Nomenclature: 0 (Drugs, Chinese Herbal) ; EC 2.7.10.1 (Receptor, IGF Type 1) ; EC 2.7.10.1 (Vascular Endothelial Growth Factor Receptor-2) ; EC 2.7.10.1 (KDR protein, human) ; 0 (IGF1R protein, human) ; 0 (PDK1 protein, human) ; 0 (Pyruvate Dehydrogenase Acetyl-Transferring Kinase) ; EC 2.7.1.- (Phosphatidylinositol 3-Kinases) ; 0 (Receptors, Somatomedin) ; 0 (Antineoplastic Agents, Phytogenic) Entry Date(s): Date Created: 20240515 Date Completed: 20240602 Latest Revision: 20240602 Update Code: 20240602

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Elucidation of the anti-gastric cancer mechanism of Guiqi Baizhu Formula by integrative approach of chemical bioinformatics.