1.Dendrocalamus latiflorus and its component rutin exhibit glucose-lowering activities by inhibiting hepatic glucose production via AKT activation.
Kun LUO ; Wenting HUANG ; Liansheng QIAO ; Xiaoling ZHANG ; Di YAN ; Zhiyu NING ; Chengmei MA ; Honglei DANG ; Dong WANG ; Hongyan GUO ; Lan XIE ; Jing CHENG
Acta Pharmaceutica Sinica B 2022;12(5):2239-2251
The potential medicinal value of Ma bamboo (Dendrocalamus latiflorus), one of the most popular and economically important bamboo species in China, has been underestimated. In the present study, we found that D. latiflorus leaf extract (DLE) reduced fasting blood glucose levels, body weight, and low-density lipoprotein cholesterol with low liver toxicity in db/db mice. In addition, gene expression profiling was performed and pathway enrichment analysis showed that DLE affected metabolic pathways. Importantly, DLE activated the AKT signaling pathway and reduced glucose production by downregulating glucose-6-phosphatase (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1) expression. Moreover, network pharmacology analysis identified rutin as an active component in DLE through targeting insulin growth factor 1 receptor (IGF1R), an upstream signaling transducer of AKT. Due to its hypoglycemic effects and low toxicity, DLE may be considered an adjuvant treatment option for type 2 diabetes patients.
2.Synthesis and Cytotoxicity Evaluation of Panaxadiol Derivatives
Hong PU ; Chengmei DONG ; Cheng ZOU ; Qing ZHAO ; Wenyue DUAN ; Yanmei CHEN ; Lianqing ZHANG ; Jianlin HU
Chinese Journal of Modern Applied Pharmacy 2024;41(13):1765-1774
OBJECTIVE
To obtain stronger cytotoxic activity of panaxadiol derivatives.
METHODS
The 3-amino panaxadiol was prepared by the bioelectronic isosteric principle, and then 18 derivatives of cinnamic acid, NO donor and other types of panaxadiol derivatives were synthesized, among them, 12 compounds had not been reported in the literature, and their structures had been confirmed by 1H-NMR, 13C-NMR and mass spectrometry. These compounds were evaluated for their cytotoxic activity by MTS assay against human leukemia cell line HL-60, liver cancer cell line SMMC-7721, lung cancer cell line A-549, breast cancer cell line MCF-7, and colon cancer cell line SW480.
RESULTS
These results showed that compounds 6c, 7 as well as 7j exhibited potent inhibitory activities against all five tumor cells, especially the IC50 values of compound 7 against HL-60 and SMMC-7721cells were 3.41 and 4.51 μmol·L−1, respectively. It was significantly superior to panaxadiol in cytotoxicity.
CONCLUSION
These results show that 7 and 7j can be used as promising lead compounds for further research.