Design and synthesis of urea and thiourea derivatives and their inhibitory activities on lipopolysaccharide-induced NO production

2007 ◽  
Vol 17 (12) ◽  
pp. 3317-3321 ◽  
Author(s):  
Yoon Jung Kim ◽  
Jae-Ha Ryu ◽  
Ye Jin Cheon ◽  
Hyo Jin Lim ◽  
Raok Jeon
Keyword(s):  
No Production ◽  
Thiourea Derivatives ◽  
Design And Synthesis ◽  
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 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

scholarly journals New Alkaloids and Anti-inflammatory Constituents from the Leaves of Antidesma ghaesembilla

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200
Author(s):  
Phan Van Kiem ◽  
Le Canh Viet Cuong ◽  
Do Thi Trang ◽  
Nguyen Xuan Nhiem ◽  
Hoang Le Tuan Anh ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Activity ◽  
No Production ◽  
Raw 264.7 ◽  
Chemical Methods ◽  
Raw 264.7 Macrophages ◽  
Chemical Structures ◽  
Bv2 Cells ◽  
Inhibitory Activities ◽  
Physical And Chemical

Using various chromatographic methods, two new alkaloids, antidesoic acids A (1) and B (2) along with fourteen known compounds (3-16) were isolated from the leaves of Antidesma ghaesembilla Gaertn. Their chemical structures were elucidated by physical and chemical methods. All the isolated compounds were evaluated for their inhibitory activity on LPS-stimulated nitric oxide (NO) production in BV2 cells and RAW 264.7 macrophages. Bisflavone 8 significantly inhibited LPS-stimulated NO production in BV2 cells and RAW 264.7 macrophages with IC50 values of 5.4 and 8.0 μM, respectively. Compounds 1–3, 7, 10, 12, 14, and 16 showed moderate inhibitory activities with IC50 values ranging from 11.7 to 77.4 μM.

scholarly journals A New Pentacyclic Triterpene fromHumata tyermanniMoore with the Inhibitory Activities against LPS-Induced NO Production in RAW264.7 Macrophages

2013 ◽  
Vol 2013 ◽  
pp. 1-4
Author(s):  
Lei Zhang ◽  
Feng Wang ◽  
Zhen-You Jiang ◽  
Yao-Kui Zhu ◽  
Ying-Zhou Cen
Keyword(s):  
Nitric Oxide ◽  
Spectral Analysis ◽  
2D Nmr ◽  
No Production ◽  
Pentacyclic Triterpene ◽  
Raw264.7 Macrophages ◽  
Inhibitory Activities

One new pentacyclic triterpene, hopane-22 (29)-en-24ol(2), with five known hopane-type pentacyclic triterpene compounds: hop-22(29)-ene(1), adiantone(3), 22-hydroxyhopane(4), 6α, 22-dihydroxyhopane(5), and 17(21)-hopene(6)were isolated fromHumata tyermanniMoore. The structure of compound2was elucidated on the basis of its 1D and 2D NMR spectral analysis. All these compounds were evaluated for their inhibitory activities of LPS-induced nitric oxide (NO) production in RAW264.7 macrophages.

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