Discovery and bioassay of disubstituted β-elemene-NO donor conjugates: synergistic enhancement in the treatment of leukemia.
10.1016/S1875-5364(23)60404-2
- Author:
Junlong ZHU
1
;
Xiaoying JIANG
1
;
Xinyu LUO
1
;
Yuan GAO
1
;
Rui ZHAO
1
;
Junjie LI
1
;
Hong CAI
1
;
Xiawen DANG
1
;
Xiangyang YE
2
;
Renren BAI
3
,
4
;
Tian XIE
5
Author Information
1. School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China; Key Laboratory of Elemene Class Anti-cancer Chinese Medicines; Engineering Laboratory of Development and Application of Traditional Chinese Medicines; Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China.
2. School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China; Key Laboratory of Elemene Class Anti-cancer Chinese Medicines; Engineering Laboratory of Development and Application of Traditional Chinese Medicines; Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China. Electronic address: xyye@hznu.edu.cn.
3. School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China; Key Laboratory of Elemene Class Anti-cancer Chinese Medicines; Engineering Laboratory of Development and Application of Traditional Chinese Medicines; Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China. Electronic address: renrenbai@
4. com.
5. School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China; Key Laboratory of Elemene Class Anti-cancer Chinese Medicines; Engineering Laboratory of Development and Application of Traditional Chinese Medicines; Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China. Electronic address: xbs@hznu.edu.cn.
- Publication Type:Journal Article
- Keywords:
Antitumor activity;
Chronic myeloid leukemia;
Nitric oxide donor;
Structural modification;
β-elemene
- MeSH:
Humans;
Mice;
Animals;
Cell Line, Tumor;
Nitric Oxide Donors/pharmacology*;
Sesquiterpenes/pharmacology*;
Leukemia/drug therapy*;
Biological Assay;
Cell Proliferation
- From:
Chinese Journal of Natural Medicines (English Ed.)
2023;21(12):916-926
- CountryChina
- Language:English
-
Abstract:
Natural products are essential sources of antitumor drugs. One such molecule, β-elemene, is a potent antitumor compound extracted from Curcuma wenyujin. In the present investigation, a series of novel 13,14-disubstituted nitric oxide (NO)-donor β-elemene derivatives were designed, with β-elemene as the foundational compound, and subsequently synthesized to evaluate their therapeutic potential against leukemia. Notably, the derivative labeled as compound 13d demonstrated a potent anti-proliferative activity against the K562 cell line, with a high NO release. In vivo studies indicated that compound 13d could effectively inhibit tumor growth, exhibiting no discernible toxic manifestations. Specifically, a significant tumor growth inhibition rate of 62.9% was observed in the K562 xenograft tumor mouse model. The accumulated data propound the potential therapeutic application of compound 13d in the management of leukemia.
