Discovery of novel limonin derivatives as potent anti-inflammatory and analgesic agents
| Autor: | Qihua Zhu, Ai-Dou Jiang, Jing Liu, Zhao-Xing Chu, Yang Yun, Guoqing Gong, Yun-Gen Xu, Si-Ying Chen, Guang-Wei He, Shaochi Wang |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Limonins Naproxen Limonin medicine.drug_class Analgesic Anti-Inflammatory Agents Pain Pharmacology Analgesic agents Anti-inflammatory 03 medical and health sciences chemistry.chemical_compound Mice In vivo Drug Discovery medicine Animals Edema Humans Solubility Aspirin Analgesics Molecular Structure General Medicine 030104 developmental biology Complementary and alternative medicine chemistry medicine.drug |
| Zdroj: | Chinese journal of natural medicines. 16(3) |
| ISSN: | 1875-5364 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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