Synthesis and Biological Evaluation of Andrographolide Derivatives as Anti-inflammatory Agent

2018 ◽  
Vol 24 (30) ◽  
pp. 3529-3533 ◽  
Author(s):  
Zeyu Zhu ◽  
Haibing Duan ◽  
Mei Jing ◽  
Lipeng Xu ◽  
Pei Yu
Keyword(s):  
Bacterial Infections ◽  
Inflammatory Diseases ◽  
Cell Activity ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Special Effects ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

Background: Andrographolide (Andro) is a main active ingredient of the natural plant Andrographis paniculata, which has special effects on bacterial infections and inflammatory diseases. Objective: We previously synthesized Andrographolide derivatives AL-1 and investigated its anti-inflammatory activity. For further research, we decided to modify the structure of AL-1 and expected to have better antiinflammatory activity. Methods: By conjugating with anti-inflammatory and anti-bacterial group, we designed and synthesized the andrographolide derivative AL-2, AL-3 and AL-4. The anti-inflammatory activity of AL-2, AL-3 and AL-4 was also evaluated by detecting cell activity and Nitric Oxide (NO) release. <p> Results: The new compounds AL-2, AL-3 and AL-4 increased cell viability in lipopolysaccharide (LPS)-induced RAW 264.7 cell, which could have a certain anti-inflammatory activity, and inhibited the release of NO in cells to reduce the inflammatory response of cells. Conclusion: The new compounds AL-2, AL-3 and AL-4 may be candidates of anti-inflammatory drugs in the future.

Docking Studies, Synthesis and Biological Evaluation of β-aryl-β-hydroxy Propanoic Acids for Anti-inflammatory Activity

2017 ◽  
Vol 13 (2) ◽  
pp. 186-195 ◽  
Author(s):  
Jelena Savic ◽  
Sanda Dilber ◽  
Marina Milenkovic ◽  
Jelena Kotur-Stevuljevic ◽  
Bojan Markovic ◽  
...  
Keyword(s):  
Docking Studies ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

scholarly journals Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

2021 ◽  
Vol 14 (7) ◽  
pp. 692
Author(s):  
Ryldene Marques Duarte da Cruz ◽  
Francisco Jaime Bezerra Mendonça-Junior ◽  
Natália Barbosa de Mélo ◽  
Luciana Scotti ◽  
Rodrigo Santos Aquino de Araújo ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Structural Characteristics ◽  
Tiaprofenic Acid ◽  
Inflammatory Activity ◽  
Drug Candidates ◽  
Biological Target ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Privileged Structures

Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, despite their severe side effects and their exclusive action in improving symptoms, without effectively promoting the cure. However, recent advances in the fields of pharmacology, medicinal chemistry, and chemoinformatics have provided valuable information and opportunities for development of new anti-inflammatory drug candidates. For drug design and discovery, thiophene derivatives are privileged structures. Thiophene-based compounds, like the commercial drugs Tinoridine and Tiaprofenic acid, are known for their anti-inflammatory properties. The present review provides an update on the role of thiophene-based derivatives in inflammation. Studies on mechanisms of action, interactions with receptors (especially against cyclooxygenase (COX) and lipoxygenase (LOX)), and structure-activity relationships are also presented and discussed. The results demonstrate the importance of thiophene-based compounds as privileged structures for the design and discovery of novel anti-inflammatory agents. The studies reveal important structural characteristics. The presence of carboxylic acids, esters, amines, and amides, as well as methyl and methoxy groups, has been frequently described, and highlights the importance of these groups for anti-inflammatory activity and biological target recognition, especially for inhibition of COX and LOX enzymes.

Synthesis and Biological Evaluation of the Anti-Inflammatory Activity for some Novel Oxpholipin-11D Analogues

2015 ◽  
Vol 11 (7) ◽  
pp. 705-711
Author(s):  
El-Sayed M. Lashine ◽  
Abdel Fattah Haikal ◽  
Mansour E. Abou Kul ◽  
Lina A. Nasrallah ◽  
Ahmed M. Naglah
Keyword(s):  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

scholarly journals Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs

2018 ◽  
Vol 147 ◽  
pp. 34-47 ◽  
Author(s):  
Komba Thomas ◽  
Terry W. Moody ◽  
Robert T. Jensen ◽  
Jason Tong ◽  
Cassie L. Rayner ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity

2019 ◽  
Vol 352 (3) ◽  
pp. 1800298 ◽  
Author(s):  
Marcela Vettorazzi ◽  
Laura Vila ◽  
Santiago Lima ◽  
Lina Acosta ◽  
Felipe Yépes ◽  
...  
Keyword(s):  
Sphingosine Kinase ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Sphingosine Kinase 2 ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

scholarly journals New Eunicellin-Type Diterpenes from the Panamanian Octocoral Briareum asbestinum

Marine Drugs ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 84 ◽  
Author(s):  
Marcelino Gutiérrez ◽  
Ricardo Santamaría ◽  
José Félix Gómez-Reyes ◽  
Héctor M. Guzmán ◽  
Javier Ávila-Román ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Biological Activities ◽  
Chemical Study ◽  
Inflammatory Activity ◽  
Bocas Del Toro ◽  
Chemical Structures ◽  
Wide Range ◽  
Marine Compounds ◽  
Anti Inflammatory ◽  
New Compounds

Gorgonian octocorals are considered a prolific source of secondary metabolites with a wide range of biological activities, including anti-inflammatory activity. In particular, the genus Briareum is known for producing a wealth of diterpenes with complex chemical structures. The chemical study of the methanolic extract of Briareum asbestinum collected in Bocas del Toro, on the Caribbean side of Panama, led to the isolation of three new eunicellin-type diterpenes: briarellin T (1), asbestinin 27 (2), asbestinin 28 (3) and the previously described asbestinin 17 (4). The structures of the new compounds were determined by extensive NMR analyses and HRMS. Anti-inflammatory activity assays showed a significant reduction of the pro-inflammatory cytokines TNF-α, IL-6, IL-1β and IL-8 as well as a downregulation of COX-2 expression in LPS-stimulated THP-1 macrophages. These findings support the potential use of these marine compounds as therapeutic agents in the treatment of inflammatory diseases.

scholarly journals Synthesis and Biological Evaluation of Nonaprenylsulfates

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801
Author(s):  
Suryachandra R. Ravada ◽  
Lakshmareddy Emani ◽  
Ganeswara R. Mallula ◽  
Trimurtulu Golakoti
Keyword(s):  
Brine Shrimp ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Synthetic Analogue ◽  
Paw Edema ◽  
Naturally Occurring ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

A naturally occurring nonaprenylsulfate (1) and its synthetic analogue (2) were synthesized from substituted phenolic precursors in three steps with an overall yield of 40–45%. Both compounds exhibited potent anti-inflammatory activity against 5-lipoxygenase, and potent brine shrimp lethality. They also showed moderate anti-oxidant activity in the super oxide radical scavenging model. Nonaprenylsulfate (1) showed moderate inhibition of paw edema in Freund's Complete Adjuvant (FCA) induced model of arthritis, thus confirming its anti-inflammatory activity.

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