scholarly journals Biological Evaluation and Docking Analysis of Daturaolone as Potential Cyclooxygenase Inhibitor

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Abdur Rauf ◽  
Francesco Maione ◽  
Ghias Uddin ◽  
Muslim Raza ◽  
Bina S. Siddiqui ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Active Constituent ◽  
Ligand Complex ◽  
Reference Drug ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Dose Dependent

This study deals with the isolation of the active constituent(s) from a methanolic extract ofPistacia integerrimaJ. L. Stewart barks and it was also oriented to evaluate thein vivoandin silicoanti-inflammatory activity. By NMR and crystallography techniques, we have isolated a triterpenoid identified as daturaolone (compound1). This compound showedin vivoa significant and dose dependent (1–30 mg/kg) anti-inflammatory activity on carrageenan-induced mouse paw oedema (ED50= 10.1 mg/kg) and on acetic acid-induced writhing responses in mice (ED50= 13.8 mg/kg). In thein vivoexperiments, the effect of tested compound was also evaluated in presence of the reference drug diclofenac (1–30 mg/kg). Moreover,in silicoanalysis of receptor ligand complex shows that compound1interacts with cyclooxygenases (COXs) binding sites displaying an interesting interaction with COX-1. These findings suggest that compound1isolated fromP.integerrimapossessesin vivoanti-inflammatory and antinociceptive potentials, which are supportedin silicoby an interaction with COXs receptors.

scholarly journals Anti-Inflammatory Activity of the Stem Bark Methanol Extract of Picralima nitida

2021 ◽  
pp. 22-28
Author(s):  
O. V. Ikpeazu ◽  
M. I. Ezeja ◽  
K. K. Igwe
Keyword(s):  
Blood Cell ◽  
Red Blood Cell ◽  
Stem Bark ◽  
Inflammatory Activity ◽  
Reference Drug ◽  
Egg Albumin ◽  
Paw Oedema ◽  
Anti Inflammatory

Aims: To investigate the anti-inflammatory activity of Picralima nitida stem bark methanol extract (PNSBE). Study Design: The study was carried out using in vivo (carrageenan-induced paw oedema and egg albumin-induced paw oedema) and in vitro (Human red blood cell (HRBC) membrane stabilization assay) models in rat. Place and Duration of Study: Department of Veterinary Physiology and Pharmacology, Michael Okpara University of Agriculture, Umudike, Abia State, Nigeria from March to July, 2020. Methodology: The extract was used at the doses of 100, 200 and 400 mg/kg while diclofenac (20 mg/kg) was used as the standard reference drug for the in vivo study (carrageenan-induced paw oedema and egg albumin). For the in vitro study (red blood cell haemolysis), the extract was used at the concentrations of 25, 50, 100, 200 and 400 µg/ml while diclofenac 250 µg/ml was used. Results: In the carrageenan-induced paw oedema model, the extract at the doses used and the reference drug significantly (p < 0.05) reduced the paw edema in the rats at 1 hour in a dose dependent manner. Also, in the egg albumin model, the paw oedema of treated rats was significantly (P < 0.05) reduced by PNSBE dose dependently reducing the mean rat paw oedema from 0.99 ± 0.12 to 0.61 ± 0.06 at the first hour. There was also a concentration dependent inhibition of red blood cell haemolysis by the extract in the HRBC membrane stabilization assay. Conclusion: Picralma nitida demonstrated a significant anti-inflammatory activity in this study.

scholarly journals Anti-Inflammatory Activity of Oxycarotenoid Extracts Isolated from Coriander Leaves (Coriandrum Sativum) and Curry Leaves (Murraya koenigii) on Carrageenan Induced Acute Inflammation in Rats

2021 ◽  
Author(s):  
AM ANUSHA ◽  
PA SHERENA ◽  
PT ANNAMALA ◽  
JK Mukkadan
Keyword(s):  
Body Weight ◽  
Coriandrum Sativum ◽  
Leafy Vegetables ◽  
Inflammatory Activity ◽  
Murraya Koenigii ◽  
Curry Leaves ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Coriander Leaves

Introduction: Green leafy vegetables are important sources of polyphenols and carotenoids which possess both antioxidant and anti-inflammatory activities. Aim: To study the anti-inflammatory activity of oxycarotenoid extracts isolated from coriander leaves (Coriandrumsativum) and curry leaves (Murraya koenigii) in carrageenan induced acute paw oedema in rats. Materials and Methods: Oxycarotenoid extracts were isolated from the coriander leaves (Coriandrum sativum) and curry leaves (Murraya koenigii) and they were assessed for anti-inflammatory activities by in-vivo methods. The in-vivo anti-inflammatory activity was evaluated in carrageenan induced acute paw oedema model. Indomethacin at a dose of 20 mg/Kg body weight was used as standard anti-inflammatory drug. Results: The results revealed that oxycarotenoids extracted from coriander leaves administered at a dose of 40 mg/kg body weight showed an inhibition of 53.33% whereas the oxycarotenoids extracted from curry leaves showed an inhibition of 60% at the sixth hour after carrageenan injection. The results are comparable with those of indomethacin (20 mg/Kg body weight) administered group which showed an inhibition of 55.53% Conclusion: These findings suggest that oxycarotenoid extracts isolated from leafy vegetables (coriander leaves and curry leaves) have significant anti-inflammatory activities.

scholarly journals Synthesis, Molecular Modelling and Biological Evaluation of Novel Pyrimidine Derivatives as Anti-inflammatory Agents

2020 ◽  
pp. 49-67
Author(s):  
Naglaa Mohamed Ahmed ◽  
Shahira Nofal ◽  
Samir Mohamed Awad
Keyword(s):  
Docking Studies ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Pyrimidine Derivatives ◽  
Reference Drug ◽  
Rat Paw Edema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1 ◽  
Good Agreement

Aim: As part of ongoing studies in developing new anti-inflammatory agents, 2-thioxo-1,2,3,4-tetrahydropyrimidine derivative 1 was synthesized by direct Biginelli condensation and used for the synthesis of novel series of  pyrimidin-2-thione derivatives  (2a-d to 7a-b). Materials and Methods: All compounds were examined for their anti-inflammatory activity using the carrageenan-induced rat paw edema assay in comparison to ibuprofen, as a reference drug. Molecular docking studies were carried out using SYBLYL-X v.2.1 software. Study Design: A series of pyrimidine derivatives were synthesized by a simple and available method leads to a molecule of promising anti-inflammatory activity, the docking studies show good agreement with anti-inflammatory results. Future researches are recommended to assure the importance of these new derivatives for various applications. Place and Duration of Study: Pharmaceutical Organic Chemistry Department and Pharmacology and Toxicology Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt, between February 2018 and March 2019. Results: Compounds showed 61 to 86% anti-inflammatory activity where-as ibuprofen showed 69% activity. Compounds 2a, 2b, 2c, 2d, 3a, 3b, 3c, 3d, 7a, 7b induced strong anti-inflammatory activity, comparable with that of ibuprofen, they showed significantly difference at 4h post-carrageenan. Compound 3c (86%) showed the best result of edema inhibition in rats. Moreover, compounds 1, 2c and 3c were subjected to in vitro enzyme assay investigations against COX-1 and COX-2. All tested compounds showed higher potency towards COX-2 over COX-1. Compound 3c realized higher potency towards COX-2 (IC50= 0.046 μM) than compounds 1(IC50= 0.21 μM) and 2c (IC50=0.11 μM) as well as ibuprofen (IC50= 43.628 μM). Structure-activity relationship (SAR) has been discussed. Conclusion: A series of pyrimidine derivatives were synthesized by a simple and available method gave a molecule of promising anti-inflammatory activity, the docking studies showed good agreement with anti-inflammatory results.

scholarly journals Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs

Biomolecules ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 1568
Author(s):  
Alaa S. Abd-El-Aziz ◽  
Maysun R. Benaaisha ◽  
Amani A. Abdelghani ◽  
Rabin Bissessur ◽  
Laila H. Abdel-Rahman ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inflammatory Activity ◽  
Breast Cancer Cell Lines ◽  
Cell Viability Assay ◽  
Reference Drug ◽  
Anti Inflammatory

Designing nanocarriers with actions directed at a specific organ or tissue is a very promising strategy since it can significantly reduce the toxicity of a bioactive drug. In this study, an organometallic dendrimer was used to synthesize a biocompatible drug delivery system by attaching aspirin to the periphery of the dendrimer. Our goal is to enhance the bioavailability and anticancer activity of aspirin and reduce its toxicity through successive generations of organoiron dendrimers. The biological activity of aspirin-based dendrimer complexes was evaluated. The result of antimicrobial activity of the synthesized dendrimers also demonstrated an increase in their antimicrobial activity with increased generation of the dendrimers for most types of microorganisms. This study reveals for the first time that organoiron dendrimers linked with aspirin exhibit an excellent Gram-negative activity comparable to the reference drug Gentamicin. All synthesized dendrimers were tested for their anticancer activity against breast cancer cell lines (MCF-7), hepatocellular cell lines (Hep-G2), and a non-cancer cell line, Human Embryonic Kidney (HEK293), using the MTT cell viability assay and compared against a standard anticancer drug, Doxorubicin. Compounds G3-D9-Asp and G4-D12-Asp exhibited noticeable activity against both cell lines, both of which were more effective than aspirin itself. In addition, the in vivo anti-inflammatory activity and histopathology of swollen paws showed that the designed aspirin-based dendrimers displayed significant anti-inflammatory activity; however, G2-D6-Asp showed the best anti-inflammatory activity, which was more potent than the reference drug aspirin during the same period. Moreover, the coupling of aspirin to the periphery of organoiron dendrimers showed a significant reduction in the toxicity of aspirin on the stomach.

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents

2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng
Keyword(s):  
Antiinflammatory Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pyrazole Derivatives ◽  
Reference Drug ◽  
Tnf Α ◽  
Anti Inflammatory

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

scholarly journals Anti-inflammatory activity of Syzygium cumini leaf against experimentally induced acute and chronic inflammations in rodents

2011 ◽  
Vol 1 (1) ◽  
pp. 6 ◽  
Author(s):  
Anirban Roy ◽  
Sanjib Bhattacharya ◽  
Jitendra N. Pandey ◽  
Moulisha Biswas
Keyword(s):  
Inflammatory Activity ◽  
Dependent Manner ◽  
Syzygium Cumini ◽  
Large Size ◽  
Paw Oedema ◽  
Chronic Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Dose Dependent ◽  
Rat Paw Oedema

<p><em>Syzygium cumini<strong> </strong></em>(L.) Skeels (Myrtaceae), commonly known as <em>Jam </em>in Bengali, <em>Jamun</em> in Hindi and <em>Black Plum</em> or <em>Black Berry</em> in English, is a large size evergreen tree indigenous to India and is cultivated for its fruits. In the present study, the methanol extract of leaves from <em>S. cumini </em>(MESC) was evaluated for anti-inflammatory activity in experimental acute (carrageenan, histamine and serotonin induced rat paw oedema) and chronic models (cotton pellet induced rat granuloma). In all models, the MESC (100 and 200 mg/kg body wt. p.o.) exhibited significant anti-inflammatory activity (<em>p &lt; 0.001</em>) in a dose dependent manner. These findings revealed that the <em>S. cumini </em>leaf had remarkable acute and chronic anti-inflammatory actions in the tested rodent models.</p>

scholarly journals Cascade Transformations of 1-R-Ethynyl-9,10-anthraquinones with Amidines: Expanding Access to Isoaporphinoid Alkaloids

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6883
Author(s):  
Sergey Francevich Vasilevsky ◽  
Ol’ga Leonidovna Krivenko ◽  
Irina Vasilievna Sorokina ◽  
Dmitry Sergeevich Baev ◽  
Tatyana Genrikhovna Tolstikova ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Concanavalin A ◽  
In Silico ◽  
Intraperitoneal Injection ◽  
Antitumor Drug ◽  
Inflammatory Activity ◽  
Antitumor Properties ◽  
Anti Inflammatory

The interaction of acetamidine and phenylamidine with peri-R-ethynyl-9,10-anthraquinones in refluxing n-butanol leads to the formation of cascade transformations products: addition/elimination/cyclization―2-R-7H-dibenzo[de,h]quinolin-7-ones and(or) 2-R-3-aroyl-7H-dibenzo[de,h]quinolin-7-ones. The anti-inflammatory and antitumor properties of the new 2-R-7H-dibenzo[de,h]quinolin-7-ones were investigated in vivo, in vitro, and in silico. The synthesized compounds exhibit high anti-inflammatory activity at dose 20 mg/kg (intraperitoneal injection) in the models of exudative (histamine-induced) and immunogenic (concanavalin A-induced) inflammation. Molecular docking data demonstrate that quinolinones can potentially intercalate into DNA similarly to the antitumor drug doxorubicin.

scholarly journals Kinetic Study of the Hydrolysis of synthesized Ibuprofen Ester and its Biological Activity

2013 ◽  
Vol 10 (3) ◽  
pp. 1062-1070
Author(s):  
Baghdad Science Journal
Keyword(s):  
Side Effect ◽  
Effect Study ◽  
Reference Drug ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
The Stability ◽  
Kinetic Hydrolysis ◽  
Hydrolysis Of ◽  
Inflammatory Action

It is known that the oral administration of ibuprofen caused an irritation of stomach as a side effect due to its carboxylic moiety. Ibuprofen ester was synthesized by linking the carboxylic moiety of ibuprofen and the hydroxylic group of paracetamol to reduce its side effect. Study the kinetic hydrolysis of prepared ester was examined at different values of physiological pH (1.0, 5.8, 6.4 and 7.4) at 37 ± 0.1 of 1 hour period. Measurements of absorbance were carried out by UV-Visible spectrophotometer to follow the stability of ester, it showed Pseudo first order hydrolysis. The pH- apparent rate profiles of ester was exhibited a good stability at pH 1.0 and pH 5.8. Pharmacological activity in vivo of prepared ester was evaluated in relation to analgesic and anti-inflammatory activity using the acetic acid method and the hind paw oedema inhibition, respectively. Acetyl salicylic acid (aspirin) was used as a reference drug for the above tests. The synthesized ester showed higher analgesic and anti-inflammatory action than aspirin.

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