New ursolic acid derivatives bearing 1,2,3-triazole moieties: design, synthesis and anti-inflammatory activity in vitro and in vivo

2021 ◽

Vol 21 ◽

Author(s):

Mingzhu Luan ◽

Huiyun Wang ◽

Jiazhen Wang ◽

Xiaofan Zhang ◽

Fenglan Zhao ◽

...

Keyword(s):

Ursolic Acid ◽

Inflammatory Diseases ◽

Kidney Diseases ◽

Inflammatory Activity ◽

Inflammatory Factors ◽

Inflammatory Stimuli ◽

Bowel Diseases ◽

Anti Inflammatory

: In vivo and in vitro studies reveal that ursolic acid (UA) is able to counteract endogenous and exogenous inflammatory stimuli, and has favorable anti-inflammatory effects. The anti-inflammatory mechanisms mainly include decreasing the release of histamine in mast cells, suppressing the activities of lipoxygenase, cyclooxygenase and phospholipase, and reducing the production of nitric oxide and reactive oxygen species, blocking the activation of signal pathway, down-regulating the expression of inflammatory factors, and inhibiting the activities of elastase and complement. These mechanisms can open up new avenues for the scientific community to develop or improve novel therapeutic approaches to tackle inflammatory diseases such as arthritis, atherosclerosis, neuroinflammation, liver diseases, kidney diseases, diabetes, dermatitis, bowel diseases, cancer. The anti-inflammatory activity, the anti-inflammatory mechanism of ursolic acid and its therapeutic applications are reviewed in this paper.

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Design and Synthesis of 2-Mercapto Benzoxazole coupled Benzyl Triazoles as Anti-inflammatory Agents Targeting COX-2 Enzyme

Asian Journal of Chemistry ◽

10.14233/ajchem.2020.22956 ◽

2020 ◽

Vol 32 (12) ◽

pp. 3209-3218

Author(s):

K. Praveen Kumar ◽

Y. Prashanthi ◽

G. Rambabu ◽

Md. Ataur Rahman ◽

J.S. Yadav

Keyword(s):

Chemical Space ◽

Biological Evaluation ◽

Inflammatory Activity ◽

Design Synthesis ◽

Standard Drug ◽

Design And Synthesis ◽

Cox 2 ◽

Anti Inflammatory

In this study, we report the design, synthesis and the biological evaluation of 19 analogues of 2-mercapto benzoxazole coupled benzyl triazoles (BOTs) based on analysis of the binding site and literature of chemical space. These BOTs were evaluated both in vitro and in vivo for their anti-inflammatory activity. Eleven compounds showed less than 10 μM in vitro COX-2 enzyme activities. The most potent analogue among the BOT analogues were BOT15, BOT3 and BOT19 with IC50 3.40 μM, 4.50 μM and 4.57 μM respectively against COX-2. The in vivo anti-inflammatory activity of two BOTs has significantly higher than that of standard drug, ibuprofen. 2-Mercapto benzoxazole coupled benzyl triazoles (BOTs) were also tested for their antioxidant capacity and proved to be an as active scavenger, better than ascorbic acid.

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Novel paeonol derivatives: Design, synthesis and anti-inflammatory activity in vitro and in vivo

Bioorganic Chemistry ◽

10.1016/j.bioorg.2020.103735 ◽

2020 ◽

Vol 98 ◽

pp. 103735 ◽

Cited By ~ 1

Author(s):

Yang Sheng Hu ◽

Xu Han ◽

Pei Jing Yu ◽

Ming Ming Jiao ◽

Xin Hua Liu ◽

...

Keyword(s):

Inflammatory Activity ◽

Design Synthesis ◽

Anti Inflammatory

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Design, Synthesis, Antioxidant, Anti-inflammatory Activity and Molecular Docking Studies of Novel 3,4,5-Trisubstituted-1,2,4-Triazole Derivatives Bearing Benzimidazole Moiety

Letters in Organic Chemistry ◽

10.2174/1570178617999201014164403 ◽

2020 ◽

Vol 17 ◽

Author(s):

Ramamurthy Katikireddy ◽

Ramu Kakkerla ◽

M.P.S. Murali Krishna ◽

Gandamalla Durgaiah ◽

Narasimha Reddy Yellu

Keyword(s):

Molecular Docking ◽

Docking Studies ◽

Biological Data ◽

Inflammatory Activity ◽

Design Synthesis ◽

Molecular Docking Studies ◽

Cox 2 ◽

Anti Inflammatory

: 5-(7-Methyl-2-propyl-1H-benzo[d]imidazol-5-yl)-4-phenyl-4H-1,2,4-triazole-3-thiols(6a-i) have been synthesized from key intermediate 7-methyl-2-propyl-1H-benzo[d]imidazole-5-carbohydrazide(3). The hydrazide was treated with different aryl isothiocyanatesto give corresponding thiosemicarbazone derivatives, which underwent cyclization in 4N sodium hydroxide to affordcorresponding title compound. All the compounds evaluated for their in vitro antioxidant and in vivo anti-inflammatory activity. From the results, compounds 6b and 6e have shown potential antioxidant and anti-inflammatory activity. The biological data was further supported by molecular docking studies, which revealed the binding pattern and the affinity of the molecules in the active site of COX-2.

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Design, synthesis, and anti-inflammatory activity both in vitro and in vivo of new betulinic acid analogues having an enone functionality in ring A

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2006.09.012 ◽

2006 ◽

Vol 16 (24) ◽

pp. 6306-6309 ◽

Cited By ~ 38

Author(s):

Tadashi Honda ◽

Karen T. Liby ◽

Xiaobo Su ◽

Chitra Sundararajan ◽

Yukiko Honda ◽

...

Keyword(s):

Betulinic Acid ◽

Inflammatory Activity ◽

Design Synthesis ◽

Anti Inflammatory

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ANTI-INFLAMMATORY ACTIVITY OF CURCUMIN AND CAPSAICIN AUGMENTED IN COMBINATION

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i6.18635 ◽

2017 ◽

Vol 9 (6) ◽

pp. 145

Author(s):

Thriveni Vasanth Kumar ◽

Manjunatha H. ◽

Rajesh Kp

Keyword(s):

Acetic Acid ◽

Protective Effect ◽

Vascular Permeability ◽

Diclofenac Sodium ◽

Significant Inhibition ◽

Inflammatory Activity ◽

Anti Inflammatory ◽

The Individual

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.

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