One-pot cascade synthesis and in vitro evaluation of anti-inflammatory and antidiabetic activities of S-methylphenyl substituted acridine-1,8-diones

2017 ◽  
Vol 90 (4) ◽  
pp. 520-526 ◽  
Author(s):  
Lavanya Mallu ◽  
Dhakshanamurthy Thirumalai ◽  
Indira Viswambaran Asharani
Keyword(s):  
One Pot ◽  
In Vitro Evaluation ◽  
Anti Inflammatory

26043 In vitro evaluation of anti-inflammatory properties of a multifunctional sunscreen

2021 ◽  
Vol 85 (3) ◽  
pp. AB82
Author(s):  
Francine Papaiordanou ◽  
Gabriela Pacheco de Oliveira ◽  
Jéssica Parolina Salvador ◽  
Flavia Cardoso Males ◽  
Antonio Carlos Amedeo Vatimo ◽  
...  
Keyword(s):  
In Vitro Evaluation ◽  
Anti Inflammatory

In Vitro Evaluation of Actinobacterial Extracts for Anti-Inflammatory Properties

2022 ◽  
pp. 463-466
Author(s):  
Abirami Baskaran ◽  
Manigundan Kaari ◽  
Mary Shamya ◽  
Jerrine Joseph ◽  
Shanmugasundaram Thangavel ◽  
...  
Keyword(s):  
In Vitro Evaluation ◽  
Anti Inflammatory

scholarly journals Design, Synthesis and Comprehensive Investigations of Pyrrolo[3,4-d]pyridazinone-Based 1,3,4-Oxadiazole as New Class of Selective COX-2 Inhibitors

2020 ◽  
Vol 21 (24) ◽  
pp. 9623
Author(s):  
Łukasz Szczukowski ◽  
Edward Krzyżak ◽  
Adrianna Zborowska ◽  
Patrycja Zając ◽  
Katarzyna Potyrak ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Studies ◽  
One Pot ◽  
Design Synthesis ◽  
Biological Studies ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Dna Strand ◽  
Cox 2 Inhibitors

The long-term use of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) in treatment of different chronic inflammatory disorders is strongly restricted by their serious gastrointestinal adverse effects. Therefore, there is still an urgent need to search for new, safe, and efficient anti-inflammatory agents. Previously, we have reported the Mannich base-type derivatives of pyrrolo[3,4-d]pyridazinone which strongly inhibit cyclooxygenase, have better affinity to COX-2 isoenzyme and exert promising anti-oxidant activity. These findings encouraged us to perform further optimization of that structure. Herein, we present the design, synthesis, molecular docking, spectroscopic, and biological studies of novel pyrrolo[3,4-d]pyridazinone derivatives bearing 4-aryl-1-(1-oxoethyl)piperazine pharmacophore 5a,b–6a,b. The new compounds were obtained via convenient, efficient, one-pot synthesis. According to in vitro evaluations, novel molecules exert no cytotoxicity and act as selective COX-2 inhibitors. These findings stay in good correlation with molecular modeling results, which additionally showed that investigated compounds take a position in the active site of COX-2 very similar to Meloxicam. Moreover, all derivatives reduce the increased level of reactive oxygen and nitrogen species and prevent DNA strand breaks caused by oxidative stress. Finally, performed spectroscopic and molecular docking studies demonstrated that new compound interactions with bovine serum albumin (BSA) are moderate, formation of complexes is in one-to-one ratio, and binding site II (subdomain IIIA) is favorable.

New Di(heteroaryl)ethenes as Apoptotic Anti‐proliferative Agents Towards Breast Cancer: Design, One‐Pot Synthesis and In Vitro Evaluation

2020 ◽  
Vol 5 (8) ◽  
pp. 2581-2587
Author(s):  
Carmela Bonaccorso ◽  
Irina Naletova ◽  
Cristina Satriano ◽  
Giorgia Spampinato ◽  
Vincenza Barresi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
One Pot ◽  
In Vitro Evaluation ◽  
One Pot Synthesis

scholarly journals In vitro blood compatibility evaluation method: incubating while rotating hemodialyzers filled with fresh human blood

2020 ◽  
Author(s):  
Kinue Kamata ◽  
Yoshihiro Hatanaka ◽  
Hiromi Tanaka ◽  
Satoru Inoue ◽  
Yusuke Tokimizu ◽  
...  
Keyword(s):  
Vitamin E ◽  
Blood Cell ◽  
Experimental Method ◽  
Human Blood ◽  
Evaluation Method ◽  
Blood Compatibility ◽  
In Vitro Evaluation ◽  
Dialysis Membranes ◽  
Anti Inflammatory

AbstractOne of the often-used methods for in vitro evaluation of the blood compatibility of hemodialysis membranes is the circulation of human blood through a miniaturized hemodialyzer. The use of a rather small amount of human blood in its evaluation is one advantage of this method. However, because it is manufactured by a different process than actual ones, a miniaturized hemodialyzer membrane cannot always preserve the properties of actual hemodialyzers. To address this problem, we established a new experimental method that uses a relatively small amount of human blood and actual dialyzers. In this method, a test hemodialyzer and a control hemodialyzer filled with human blood obtained from the same donor is slowly rotated to prevent spontaneous blood cell sedimentation for 4 h at 37 °C. By use of this method, we were able to compare blood compatibility between a polysulfone (PS) membrane and a vitamin E (VE)-bonded PS membrane in terms of their relative antithrombotic, antioxidative, and anti-inflammatory properties. Consistent with many previous reports, the results clearly showed that compared with the PS membrane, VE-bonded PS membrane is more blood compatible. These findings suggest that our method is applicable, at least to in vitro blood compatibility evaluation of PS type dialysis membranes.

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