Publisher(s): China Academic Journals (CD Edition) Electronic Publishing House Co., Ltd.
ISBN: ISBN 978-7-499-00978-3 pdf
First Published: 2020.11.23
Discipline(s): Medicine & Public Health
Price: $109 (for individuals) (中国大陆地区个人用户点此直接购买)
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Inflammation, as part of China’s Medicine Progress Series, has 76 excellent articles on inflammation research. These articles included were recommended by the editorial boards of the journals in which they were originally published, covering theoretical, drug, mechanism, clinical, and nursing research and fully demonstrating the cutting-edge advances in inflammation treatment in China, with methodological support and objective conclusions. The original articles are published in Chinese, and this book is a compilation of English versions of selected articles.
LIU Changxiao is the honorary president, tenured principal scientist and academic committee director of Tianjin Institute of Pharmaceutical Research, and the director of the State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, the Center
Chinese Journal of Medicinal Chemistry,Part 2: Drug Research,Vol 26,No. 01
A series of flavonols were designed, synthesized and the target compounds were obtained from phloroglucinol via Friedel-Crafts acylation, condensation, Algar-Flynn-Oyamada and the Claisen rearrangement reactions. Their structures were confirmed by MS and 1H-NMR. The non-cytotoxicity of synthesized compounds on cultured BV2 microglial cells was measured by using CCK-8 assay, and none showed any cytotoxicity in BV2 cells at the dose of 1–100 μmol·L -1. The cellular model of neuroinflmmation was established by incubation of BV2 cells with lipopolysaccharide (LPS) and interferon γ (IFN-γ) for 24 h, and the release of nitric oxide (NO) from BV2 cells were detected by using Griess assay. Preincubation of BV2 cells with compounds 6a and 10a (10 μmol·L -1) for 24 h obviously inhibited the over-production and release of inflammatory mediator NO induced by LPS/IFN-γ.
2. Synthesis of dehydroepiandrosterone derivatives and their inhibitory activities on neuroinflammation
Chinese Journal of Medicinal Chemistry,Part 2: Drug Research,Vol 26,No. 02
Glial activation-mediated neuroinflammation plays a pivotal role in the process of several neuroinflammatory diseases including stroke, Alzheimer's diseases, Parkinson's diseases, multiple sclerosis and ischemia. Inhibition of microglial activation may ameliorate neuronal degeneration under the inflammatory conditions. In the present study, a series of dehydroepiandrosterone derivatives were designed and synthesized. The anti-inflammatory effects of these compounds were evaluated using LPS-stimulated BV-2 microglia cells. Those derivatives were prepared from readily available dehydroepiandrosterone and its downstream product 15 β,16 β-cyclopropane-dehydroepiandrosterone by incorporating amino acid methyl esters at C-3 hydroxyl group, and oxidation at C-4 or C-7 position. Among all the 16 compounds, several analogs exhibited potent inhibitory activities on nitric oxide production (inhibition rate > 75%) with no or weak cell toxicity at 20 μmol·L ?1. The related SARs and function mechanism is worth further research and discussion.
3. Synthesis and anti-inflammatory activity evaluation of (2-chloroquinolin-3-yl) methyleneaminoguanidine derivatives
Chinese Journal of Medicinal Chemistry,Part 2: Drug Research,Vol 27,No. 03
A series of (2-chloroquinolin-3-yl) methyleneaminoguanidine derivatives ( 5a– 5m) were synthesized and evaluated for their anti-inflammatory activity by xylene-induced ear-edema test in mice. 6-Hydroxy-3,4-dihydro-2-quinolinone was used to react with a variety of substituted chloromethylbenzene compounds to afford corresponding 6-(substituted benzyloxy)-3,4-dihydroquinolin-2(1 H)-ones, followed by Vilsmeier-Haack reaction to give 6-(substituted benzyloxy)-2-chloroquinolin-3-carbaldehydes, which reacted with aminoguanidine bicarbonate to afford the target compounds. The structures of the target compounds were characterized by 1H-NMR, 13C-NMR, IR, and MS. Pharmacological tests showed that most compounds exhibited moderate to good anti-inflammatory activity, among which compound 5a (R = H) showed the most potent activity, superior to that of positive control ibuprofen.
Acta Pharmaceutica Sinica,Part 2: Drug Research,Vol 53,No. 04
Twenty new target compounds were synthesized by the Huang-minlon reduction reaction and Friedel-Crafts acylation reaction in this study. Their inhibitory effects of the new compounds were tested on NO production in LPS-induced mouse macrophage RAW264.7 cells, a cellular inflammation model. The structure-activity relationships were discussed. The structures of target compounds were confirmed by ESI-MS, 1H NMR and 13C NMR. In vitro activity experiments showed that 18 compounds had definite anti-inflammatory effects at the concentration of 40 μmol·L -1, among which 9a, 8b, 7c and 9c showed strong anti-inflammatory activities, and IC 50 of 7c and 9c were comparable to the positive control drug ibuprofen.
Chinese Journal of Medicinal Chemistry,Part 2: Drug Research,Vol 28,No. 05
A series of novel 2-arylmethylene-1-indones were synthesized and their inhibitory activities against LPS-induced TNF-α and IL-6 release were evaluated, and the preliminary structure–activity relationship was discussed. The target compounds were synthesized via step method. The anti-inflammtory activities of 10 new compounds were evaluated by an enzyme-linked immunosorbent assay (ELISA). Preliminary result showed that most of compounds effectively inhibited the LPS-induced expression of TNF-αand IL-6. In particular, compound 3h showed the strongest inhibitory potency amongst the tested compounds, and had the highest inhibition 64.5% (TNF-α) and 73.9% (IL-6), respectively.