New labdane diterpenoids from Alpinia galanga: A new type of GLP-1 secretagogues targeting the PKA-CREB and PI3K-Akt signaling axes

doi:10.1002/ardp.202400383

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	New labdane diterpenoids from Alpinia galanga: A new type of GLP-1 secretagogues targeting the PKA-CREB and PI3K-Akt signaling axes
	Liu, Pei; Gongpan, Pianchou; Wu, Sheng-Li; Li, Xin-Yu; Huang, Xiao-Yan; Ma, Yun-Bao; Geng, Chang-An
	2024
发表期刊	ARCHIV DER PHARMAZIE
ISSN	0365-6233
卷号	357 期号:10 页码:-
摘要	Glucagon-like peptide-1 (GLP-1) secretagogues are fascinating pharmacotherapies to overcome the defects of GLP-1 analogs and dipeptidyl peptidase-4 (DPP-4) inhibitors in treating diabetes and obesity. To discover new GLP-1 secretagogues from natural sources, alpigalangols A-Q (1-17), 17 new labdane diterpenoids including four unusual nor-labdane and N-containing ones, were isolated from the fruits of Alpinia galanga. Most of the isolates showed GLP-1 promotive effects in NCl-H716 cells, of which compounds 3, 4, 12, and 14-17 were revealed with high promoting rates of 246.0%-413.8% at 50 mu M. A mechanistic study manifested that the most effective compound 12 upregulated the mRNA expression of Gcg and Pcsk1, and the protein phosphorylation of PKA, CREB, and GSK3 beta, but was inactive on GPBAR and GPR119 receptors. Network pharmacology analysis indicated that the PI3K-Akt pathway was involved in the GLP-1 stimulation of 12, which was highly associated with AKT1, CASP3, PPARG, and ICAM1 proteins. This study suggests that A. galanga is rich in diverse labdane diterpenoids with GLP-1 promoting effects, representing a new type of antidiabetic candidates from natural sources.
DOI	10.1002/ardp.202400383
WOS记录号	WOS:001272848800001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/76174
专题	中国科学院昆明植物研究所
推荐引用方式 GB/T 7714	Liu, Pei,Gongpan, Pianchou,Wu, Sheng-Li,et al. New labdane diterpenoids from Alpinia galanga: A new type of GLP-1 secretagogues targeting the PKA-CREB and PI3K-Akt signaling axes[J]. ARCHIV DER PHARMAZIE,2024,357(10):-.
APA	Liu, Pei.,Gongpan, Pianchou.,Wu, Sheng-Li.,Li, Xin-Yu.,Huang, Xiao-Yan.,...&Geng, Chang-An.(2024).New labdane diterpenoids from Alpinia galanga: A new type of GLP-1 secretagogues targeting the PKA-CREB and PI3K-Akt signaling axes.ARCHIV DER PHARMAZIE,357(10),-.
MLA	Liu, Pei,et al."New labdane diterpenoids from Alpinia galanga: A new type of GLP-1 secretagogues targeting the PKA-CREB and PI3K-Akt signaling axes".ARCHIV DER PHARMAZIE 357.10(2024):-.

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