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
,
2
,
3
,
4
;
Xiaoying JIANG
1
,
2
,
3
,
4
;
Xinyu LUO
1
,
2
,
3
,
4
;
Yuan GAO
1
,
2
,
3
,
4
;
Rui ZHAO
1
,
2
,
3
,
4
;
Junjie LI
1
,
2
,
3
,
4
;
Hong CAI
1
,
2
,
3
,
4
;
Xiawen DANG
1
,
2
,
3
,
4
;
Xiangyang YE
1
,
2
,
3
,
5
;
Renren BAI
1
,
2
,
3
,
6
;
Tian XIE
1
,
2
,
3
,
7
Author Information
1. School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China
2. Key Laboratory of Elemene Class Anti-cancer Chinese Medicines
3. Engineering Laboratory of Development and Application of Traditional Chinese Medicines
4. Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China.
5. Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China. Electronic address: xyye@hznu.edu.cn.
6. Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China. Electronic address: renrenbai@126.com.
7. 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.
