Synthesis and Cytotoxicity Evaluation of Panaxadiol Derivatives

Hong PU; Chengmei Dong; Cheng Zou; Qing Zhao; Wenyue Duan; Yanmei Chen; Lianqing Zhang; Jianlin HU

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Synthesis and Cytotoxicity Evaluation of Panaxadiol Derivatives

VernacularTitle:人参二醇衍生物的合成及其细胞毒活性研究
Author: Hong PU ¹ ; Chengmei DONG ² ; Cheng ZOU ³ ; Qing ZHAO ⁴ ; Wenyue DUAN ³ ; Yanmei CHEN ³ ; Lianqing ZHANG ³ ; Jianlin HU ³
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1. School of Pharmaceutical Sciences, Hunan University of Medicine, Hunan Provincial Key Laboratory for Synthetic Biology of Traditional Chinese Medicine, Huaihua 418000, China；School of Pharmaceutical Sciences, Kunming Medical University, Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming 650500, China
2. School of Pharmaceutical Sciences, Kunming Medical University, Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming 650500, China；School of Pharmaceutical Sciences, Kunming Health Vocational College, Kunming 650600, China
3. School of Pharmaceutical Sciences, Kunming Medical University, Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming 650500, China
4. School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China
Publication Type:Journal Article
Keywords: panaxadiol； bioisosterism； NO donor ； cinnamic acid derivatives；cytotoxicity
From: Chinese Journal of Modern Applied Pharmacy 2024;41(13):1765-1774
CountryChina
Language:Chinese
Abstract: 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.