Design and synthesis of carbamate and thiocarbamate derivatives and their inhibitory activities of NO production in LPS activated macrophages

2012 ◽  
Vol 22 (9) ◽  
pp. 3301-3304 ◽  
Author(s):  
Guo Hua Jin ◽  
Hwa Jin Lee ◽  
Hyo Jin Gim ◽  
Jae-Ha Ryu ◽  
Raok Jeon
Keyword(s):  
No Production ◽  
Activated Macrophages ◽  
Design And Synthesis ◽  
Inhibitory Activities

ChemInform Abstract: Synthesis of Heterocycle-Linked Thiourea and Their Inhibitory Activities of NO Production in LPS Activated Macrophages.

ChemInform ◽  
2010 ◽  
Vol 41 (20) ◽  
Author(s):  
Ye-Jin Cheon ◽  
Hyo Jin Gim ◽  
Hee Ryun Jang ◽  
Jae-Ha Ryu ◽  
Raok Jeon
Keyword(s):  
No Production ◽  
Activated Macrophages ◽  
Inhibitory Activities

scholarly journals Synthesis of Heterocycle-linked Thioureas and Their Inhibitory Activities of NO Production in LPS Activated Macrophages

2010 ◽  
Vol 31 (1) ◽  
pp. 27-30 ◽  
Author(s):  
Ye-Jin Cheon ◽  
Hyo-Jin Gim ◽  
Hee-Ryun Jang ◽  
Jae-Ha Ryu ◽  
Raok Jeon
Keyword(s):  
No Production ◽  
Activated Macrophages ◽  
Inhibitory Activities

scholarly journals Structural Characterization and Assessment of Anti-Inflammatory and Anti-Tyrosinase Activities of Polyphenols from Melastoma normale

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3913
Author(s):  
Rui-Jie He ◽  
Jun Li ◽  
Yong-Lin Huang ◽  
Ya-Feng Wang ◽  
Bing-Yuan Yang ◽  
...  
Keyword(s):  
Enzyme Inhibitors ◽  
Enzyme Inhibitor ◽  
Structure Identification ◽  
No Production ◽  
Protective Effects ◽  
Successful Isolation ◽  
Ic50 Values ◽  
Development And Utilization ◽  
Inhibitory Activities ◽  
Anti Inflammatory

Polyphenols, widely distributed in the genus Melastoma plants, possess extensive cellular protective effects such as anti-inflammatory, anti-tyrosinase, and anti-obesity, which makes it a potential anti-inflammatory drug or enzyme inhibitor. Therefore, the aim of this study is to screen for the anti-inflammatory and enzyme inhibitory activities of compounds from title plant. Using silica gel, MCI, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, the extract of Melastoma normale roots was separated. Four new ellagitannins, Whiskey tannin C (1), 1-O-(4-methoxygalloyl)-6-O-galloyl-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (2), 1-O-galloyl-6-O-(3-methoxygalloyl)-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (3), and 1-O-galloyl-6-O-vanilloyl-2,3-O-(S)-hexahydroxydiphenoyl-β-d-glucose (4), along with eight known polyphenols were firstly obtained from this plant. The structures of all isolates were elucidated by HRMS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW2 64.7 cells, we investigated the anti-inflammatory activities of compounds 1–4, unfortunately, none of them exhibit inhibit nitric oxide (NO) production, their IC50 values are all > 50 μM. Anti-tyrosinase activity assays was done by tyrosinase inhibition activity screening model. Compound 1 showed weak tyrosinase inhibitory activity with IC50 values of 426.02 ± 11.31 μM. Compounds 2–4 displayed moderate tyrosinase inhibitory activities with IC50 values in the range of 124.74 ± 3.12–241.41 ± 6.23 μM. The structure–activity relationships indicate that hydroxylation at C-3′, C-4′, and C-3 in the flavones were key to their anti-tyrosinase activities. The successful isolation and structure identification of ellagitannin provide materials for the screening of anti-inflammatory drugs and enzyme inhibitors, and also contribute to the development and utilization of M. normale.

neo-Clerodane diterpenes from Ajuga ciliata and their inhibitory activities on LPS-induced NO production

2012 ◽  
Vol 5 (3) ◽  
pp. 563-566 ◽  
Author(s):  
Ping Guo ◽  
Yushan Li ◽  
Da-qing Jin ◽  
Jing Xu ◽  
Yisha He ◽  
...  
Keyword(s):  
No Production ◽  
Clerodane Diterpenes ◽  
Inhibitory Activities

ChemInform Abstract: New Myrsinol Diterpenes from Euphorbia prolifera and Their Inhibitory Activities on LPS-Induced NO Production.

ChemInform ◽  
2012 ◽  
Vol 43 (41) ◽  
pp. no-no
Author(s):  
Jing Xu ◽  
Da-qin Jin ◽  
Yuanqiang Guo ◽  
Chunfeng Xie ◽  
Yonggang Ma ◽  
...  
Keyword(s):  
No Production ◽  
Inhibitory Activities

scholarly journals Biological and Inflammatory Effects of Antigen 5 from Polybia paulista (Hymenoptera, Vespidae) Venom in Mouse Intraperitoneal Macrophages

Toxins ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 850
Author(s):  
Murilo Luiz Bazon ◽  
Luis Gustavo Romani Fernandes ◽  
Isabela Oliveira Sandrini Assugeni ◽  
Lucas Machado Pinto ◽  
Patrícia Ucelli Simioni ◽  
...  
Keyword(s):  
Peritoneal Macrophages ◽  
In Vivo Studies ◽  
M2 Macrophage ◽  
No Production ◽  
Activated Macrophages ◽  
In Vitro Production ◽  
Polybia Paulista ◽  
Antigen 5

The social wasp Polybia paulista (Hymenoptera, Vespidae) is highly aggressive, being responsible for many medical occurrences. One of the most allergenic components of this venom is Antigen 5 (Poly p 5). The possible modulation of the in vitro immune response induced by antigen 5 from P. paulista venom, expressed recombinantly (rPoly p 5), on BALB/c mice peritoneal macrophages, activated or not with LPS, was assessed. Here, we analyzed cell viability changes, expression of the phosphorylated form of p65 NF-κB subunit, nitric oxide (NO), proinflammatory cytokines production, and co-stimulatory molecules (CD80, CD86). The results suggest that rPoly p 5 does not affect NO production nor the expression of co-stimulatory molecules in mouse peritoneal macrophages. On the other hand, rPoly p 5 induced an increase in IL-1β production in non-activated macrophages and a reduction in the production of TNF-α and MCP-1 cytokines in activated macrophages. rPoly p 5 decreased the in vitro production of the phosphorylated p65 NF-κB subunit in non-activated macrophages. These findings suggest an essential role of this allergen in the polarization of functional M2 macrophage phenotypes, when analyzed in previously activated macrophages. Further investigations, mainly in in vivo studies, should be conducted to elucidate Polybia paulista Ag5 biological role in the macrophage functional profile modulation.

scholarly journals Design and Synthesis of Benzimidazole-Iminosugars and Their Inhibitory Activities against Glycosidases

2021 ◽  
Vol 41 (7) ◽  
pp. 2861
Author(s):  
Xu Liu ◽  
Lulu Su ◽  
Zhaoxi Zhou ◽  
Liping Niu ◽  
Ligang Gao ◽  
...  
Keyword(s):  
Design And Synthesis ◽  
Inhibitory Activities

Design and Synthesis of 2-Substitutedphenyl Benzo[D]Thiazole Derivatives and Their β-Amyloid Aggregation and Cholinesterase Inhibitory Activities

2019 ◽  
Vol 53 (4) ◽  
pp. 322-328 ◽  
Author(s):  
Merve Zengin ◽  
Oya Unsal-Tan ◽  
Tuba Tüylü Küçükkılınç ◽  
Beyza Ayazgok ◽  
Ayla Balkan
Keyword(s):  
Amyloid Aggregation ◽  
Thiazole Derivatives ◽  
Design And Synthesis ◽  
Β Amyloid ◽  
Inhibitory Activities

Structure-guided design and synthesis of isoflavone analogs of GW4064 with potent lipid accumulation inhibitory activities

2018 ◽  
Vol 28 (23-24) ◽  
pp. 3726-3730 ◽  
Author(s):  
Rongmao Qiu ◽  
Guoshun Luo ◽  
Xuerong Cai ◽  
Linyi Liu ◽  
Mingqi Chen ◽  
...  
Keyword(s):  
Lipid Accumulation ◽  
Design And Synthesis ◽  
Inhibitory Activities
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