Discovery of novel limonin derivatives as potent anti-inflammatory and analgesic agents.
10.1016/S1875-5364(18)30052-9
- Author:
Shao-Chi WANG
1
,
2
;
Yun YANG
3
;
Jing LIU
1
,
2
;
Ai-Dou JIANG
4
;
Zhao-Xing CHU
5
;
Si-Ying CHEN
4
;
Guo-Qing GONG
6
;
Guang-Wei HE
5
;
Yun-Gen XU
1
,
7
;
Qi-Hua ZHU
1
,
8
Author Information
1. State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China
2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
3. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
4. Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China.
5. Hefei YiGong Pharmaceutical Co., Ltd., Hefei 230088, China.
6. Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China. Electronic address: gonggq@hotmail.com.
7. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China. Electronic address: xu_yungen@hotmail.com.
8. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China. Electronic address: zhuqihua@vip.126.com.
- Publication Type:Journal Article
- Keywords:
Analgesic;
Anti-inflammatory;
Limonin derivatives
- MeSH:
Analgesics;
administration & dosage;
chemical synthesis;
chemistry;
Animals;
Anti-Inflammatory Agents;
administration & dosage;
chemical synthesis;
chemistry;
Drug Discovery;
Edema;
drug therapy;
Humans;
Limonins;
administration & dosage;
chemical synthesis;
chemistry;
Mice;
Molecular Structure;
Pain;
drug therapy
- From:
Chinese Journal of Natural Medicines (English Ed.)
2018;16(3):231-240
- CountryChina
- Language:English
-
Abstract:
Novel series of limonin derivatives (V-A-1-V-A-8, V-B-1-V-B-8) were synthesized by adding various tertiary amines onto the C (7)-position of limonin. The synthesized compounds possessed favorable physicochemical property, and the intrinsic solubility of the novel compounds were significantly improved, compared with limonin. Different pharmacological models were used to evaluate the analgesic and anti-inflammatory activities of the target compounds. Compound V-A-8 exhibited the strongest in vivo activity among the novel limonin analogs; its analgesic activity was more potent than aspirin and its anti-inflammatory activity was stronger than naproxen under our testing conditions.
