scholarly journals STUDY OF ANTI-INFLAMMATORY POTENTIAL OF WHOLE CELL EXRACTS OF CYANOBACTERIA BY MEMBRANE STABILIZATION & TRYPSIN INHIBITION ASSAY

2021 ◽  
Vol 23 (1) ◽  
Author(s):  
Shraddha Ratnaparkhe ◽  
Devyani Mali
Keyword(s):  
Tissue Damage ◽  
Inflammatory Activity ◽  
Inhibition Assay ◽  
Loss Of Function ◽  
Membrane Stabilization ◽  
Whole Cell ◽  
Cell Extracts ◽  
Trypsin Inhibition ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Inflammation is a complex mechanism in response to any infection, injury, or irritation. The prolonged inflammation leads to tissue damage and loss of function result in various disease conditions like osteoarthritis, and autoimmune diseases like lupus, rheumatoid arthritis, asthma and Crohn’s disease. Anti-inflammatory drugs are used to control inflammatory response and prevent tissue damage .Cyanobacteria are rich sources of phytochemicals like phenolics, flavonoids are known to have anti-inflammatory activity. Because of ease of cultivation and faster growth rate than plants, they are preferred candidates over plants. This study focuses on screening of cyanobacterial isolates for their anti-inflammatory activity. The human erythrocytes (HRBC) membrane stabilization assay indicated the potential of whole cell extracts of cyanobacteria to stabilize lysosomal membrane and thereby prevent tissue damage by lysosomal chemokines and enzymes. The trypsin inhibition assay is an indicator for potential to inhibit proteinases and decelerate tissue damage. The whole cell extracts of 10 cyanobacterial isolates of different genus namely Weistellopsis, Pseudophormidium, Oscillatoria, Nostoc, Phormidium, Chlorella, Hapalosiphon under study showed 85%-94% membrane stabilization in hypotonicity induced hemolysis and 92% to 97% membrane stabilization in heat induced hemolysis. The test extracts also showed 48% to 52% inhibition of trypsin. Thus, the isolates under study have application as anti-inflammatory agent.

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.

scholarly journals Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues

2021 ◽  
Vol 89 (2) ◽  
pp. 22
Author(s):  
Mariia Mishchenko ◽  
Sergiy Shtrygol’ ◽  
Andrii Lozynskyi ◽  
Semen Khomyak ◽  
Volodymyr Novikov ◽  
...  
Keyword(s):  
Drug Design ◽  
Anticonvulsant Activity ◽  
Inflammatory Activity ◽  
Significant Protection ◽  
Protection Level ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Target Agent

Neuroinflammation is an integral part of epilepsy pathogenesis and other convulsive conditions, and non-steroidal anti-inflammatory drugs (NSAIDs) present a potent tool for the contemporary search and design of novel anticonvulsants. In the present paper, evaluation of the anticonvulsant activity of the potential NSAID dual COX-2/5-LOX inhibitor darbufelone methanesulfonate using an scPTZ model in mice in dose 100 mg/kg is reported. Darbufelone possesses anticonvulsant properties in the scPTZ model and presents interest for in-depth studies as a possible anticonvulsant multi-target agent with anti-inflammatory activity. The series of 4-thiazolidinone derivatives have been synthesized following the analogue-based drug design and hybrid-pharmacophore approach using a darbufelone matrix. The synthesized derivatives showed a significant protection level for animals in the scPTZ model and are promising compounds for the design of potential anticonvulsants with satisfactory drug-like parameters.

Identification of phytoconstituents of Tragia involucrata leaf extracts and evaluate their correlation with anti-inflammatory & antioxidant properties

2021 ◽  
Vol 20 ◽  
Author(s):  
Vinodhini Velu ◽  
Swagata Banerjee ◽  
Vidya Rajendran ◽  
Gaurav Gupta ◽  
Dinesh Kumar Chellappan ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Petroleum Ether ◽  
Ethyl Acetate Extract ◽  
Petroleum Ether Extract ◽  
Inflammatory Activity ◽  
Ether Extract ◽  
Membrane Stabilization ◽  
Leaf Extracts ◽  
Anti Inflammatory

Aims: The present investigation was aimed at exploring the phytoconstituents using Gas Chromatography Mass Spectroscopy and to evaluate antioxidant and anti-inflammatory properties of the leaf extracts. Materials and Methods: The extracts were obtained sequentially with petroleum ether, ethyl acetate and water using soxhlet apparatus. The anti-inflammatory property of the identified compounds using GC- MS spectroscopy was evaluated in silico. The antioxidant activity was performed by DPPH and H2O2 method whereas anti-inflammatory study was carried out by HRBC membrane stabilization method. Terpenoids were found to be major constituents in petroleum ether extract while, phenols and flavonoids were predominantly found in ethyl acetate extract. Results and Discussion: The GC-MS analysis of the extract revealed six major molecules including Squalene, 19β, 28- epoxyleanan-3-ol and 2-tu-Butyl-5-chloromethyl-3-methyl-4-oxoimidazolidine-1-carboxylic acid. The ethyl acetate extract showed a significant antioxidant activity (P<0.01) in both DPPH method (70.87 %) and H2O2 method (73.58%) at 200 µg mL-1 . Increased membrane stabilization of petroleum ether extract was observed in the in vitro anti-inflammatory activity study. A strong relationship between the terpenoid content and anti-inflammatory activity was obtained from the correlation (0.971) and docking study. Conclusion: These results justify T. involucrata to be a rich source of terpenoids with potent antiinflammatory property.

scholarly journals ANTI-INFLAMMATORY STUDY OF ANREDERA CORDIFOLIA LEAVES AND CENTELLA ASIATICA HERBS AND ITS COMBINATIONS USING HUMAN RED BLOOD CELL-MEMBRANE STABILIZATION METHOD

2016 ◽  
Vol 9 (5) ◽  
pp. 78 ◽  
Author(s):  
Entris Sutrisno ◽  
Ketut Adnyana I ◽  
Elin Yulinah Sukandar ◽  
Irda Fidrianny ◽  
Widhya Aligita
Keyword(s):  
Cell Membrane ◽  
Blood Cell ◽  
Ethyl Alcohol ◽  
Red Blood Cell ◽  
Centella Asiatica ◽  
Inflammatory Activity ◽  
Membrane Stabilization ◽  
Alcohol Extract ◽  
Red Blood Cell Membrane ◽  
Anti Inflammatory

ABSTRACTObjective: Inflammation is body reactions in response to tissue injury and infection. In 2011, non-steroidal anti-inflammatory drug (NSAID) was thehighest demand drug in Indonesia. However, long-term treatment using NSAID can cause several side effects to cardiovascular and digestive system.This research aimed to investigate anti-inflammatory properties of binahong leaves (Anredera cordifolia) and pegagan herbs (Centella asiatica).Methods: Ethyl alcohol extract of A. cordifolia leaves and C. asiatica herbs was evaluated for its anti-inflammatory properties using human redblood cell (RBC) – membrane stabilization assay. The extract concentrations used in this study was 100, 200, 400, and 800-ppm, and apigenin andasiaticoside concentration were 1, 2, 3, 4, 5, 6, 10, and 100 ppm. Diclofenac natrium (DN) was used as a standard drug.Results: The results showed that A. cordifolia extract (ACE) alone, C. asiatica extract (CAE) alone, and the combination of ACE and CAE could inhibit thehemolysis of RBC in hypotonic solution. The optimum concentration for ACE alone was 100 ppm; for CAE alone was 400 ppm; and for the combinationof ACE and CAE was 50 ppm and 50 ppm, respectively. Apigenin and asiaticoside in concentration of 1-10 ppm showed more than 97% inhibition ofhemolysis. DN as a standard drug showed optimum inhibition at concentration of 400 ppm.Conclusion: The ethyl alcohol extract of A. cordifolia leaves and C. asiatica herbs showed anti-inflammatory activity, both as a single treatment or ascombinations, and apigenin and asiaticoside were responsible for anti-inflammatory activity in C. asiatica.Keywords: Anti-inflammation, Human red blood cell – membrane stabilization, Anredera cordifolia, Centella asiatica.

scholarly journals UJI AKTIVITAS ANTIINFLAMASI INFUSA BUNGA PUKUL EMPAT SECARA IN VITRO

2021 ◽  
Vol 9 (1) ◽  
pp. 21
Author(s):  
Hidayatul Ihsan ◽  
Iman Surya Pratama ◽  
Nisa Isnaeni Hanifa
Keyword(s):  
Cell Membrane ◽  
Blood Cell ◽  
Red Blood Cell ◽  
Test Group ◽  
Inflammatory Activity ◽  
Test Results ◽  
Membrane Stabilization ◽  
Red Blood Cell Membrane ◽  
Mirabilis Jalapa ◽  
Anti Inflammatory

The stew of Mirabilis jalapa L. flower has been used traditionally as an anti-inflammatory. Phytochemical screening of Mirabilis jalapa L. flower showed flavonoid content which is known to have anti-inflammatory activity. This study aims to determine the anti-inflammatory activity of Mirabilis jalapa L. flower infusion using the red blood cell membrane stabilization method by inducing hypotonicity and heat. The test group consisted of Mirabilis jalapa L. flower infusion with a concentration of 2.5%; 5%; and 10% w / v, positive control (diclofenac sodium 0.01% w / v and aspirin 0.01% w / v), and negative control (distilled water). The anti-inflammatory activity of Mirabilis jalapa L. flower infusion was determined by the percentage of membrane stabilization and inhibition of red blood cell hemolysis. Data from the test results were statistically analyzed both parametric and nonparametric with SPSS. Mirabilis jalapa L. flower infusion contains flavonoids, tannins and terpenoids. The test results showed that the 10% concentration of Mirabilis jalapa L. flower infusion had the largest percentage of red blood cell hemolysis protection on hypotonicity induction, that is 99.50% (p>0.05) and the largest percentage of hemolysis inhibition on heat induction, that is 50.27% ( p≤0.05). From these results, it can be concluded that the Mirabilis jalapa L. flower infusion has potential as an anti-inflammatory by stabilizing the red blood cell membrane.

scholarly journals SYNTHESIS NEW POTENTIAL ANTI-INFLAMMATORY AGENT SODIUM SALT OF PENTAGAMAVUNON-0

2010 ◽  
Vol 4 (3) ◽  
pp. 180-185
Author(s):  
Enade Perdana Istyastono ◽  
Rr. Sri Untari Siwi S.M.P ◽  
Andreas Asdi Utama ◽  
Supardjan A.M
Keyword(s):  
Inflammatory Activity ◽  
Physiological Changes ◽  
Solubility In Water ◽  
Curcumin Analogues ◽  
Inflammatory Agent ◽  
Curcumin Derivatives ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Living Tissues ◽  
Anti Inflammation

Inflammation is the response of living tissues to injury. The process affects physiological changes such as erythema, edema, asthma and fever. Non-steroid Anti-inflammatory Drugs (NSAIDs) have been developed since they could inhibit inflammation process because of its ability to inhibit biosynthesis of prostaglandin, one of inflammation mediators, through inhibition of cyclooxigenase (COX) enzymes. Molecules, which have been reported having anti-inflammatory activity, for example, are curcumin, some curcumin derivatives and curcumin analogues. One of curcumin analogues that has been  developed is pentagamavunon-0 (PGV-0) whose IUPAC name is 2,5-bis(4'-hidroxy-3'-methoxy-benzylidene)cyclo-pentanone. But PGV-0, which is like curcumin, practically insoluble in water, so it causes problems in the development. The aim of this research is to synthesize a derivative of PGV-0, a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0), which is hoped to have a better anti-inflammatory activity and solubility in water than PGV-0. PGV-0 was synthesized by reacting vanillin and cyclopentanone catalized by acid. Na-pentagamavunonate-0 was synthesized with PGV-0 as a starting material using an appropriate method. This research was able to synthesize new compound that was estimated as a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0).   Keywords: Curcumin, PGV-0, Na-pentagamavunonate-0, anti-inflammation

Phytochemical, In vitro Anti-inflammatory and Antimicrobial Potential of Hugonia mystax L.

2021 ◽  
pp. 169-173
Author(s):  
K.P. Jaiganesh ◽  
T.J. Jasna ◽  
A.C. Tangavelou
Keyword(s):  
Tamil Nadu ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Phytochemical Analysis ◽  
Membrane Stabilization ◽  
Traditional System ◽  
Antimicrobial Potential ◽  
Biochemical Compounds ◽  
Anti Inflammatory

Hugonia mystax L., (Linaceae), is commonly distributed in the thorny scrubs and tropical dry evergreen forests of Tamil Nadu, which has been valued for centuries in traditional system of medicine for the treatment of various ailments. In the present study was an attempt to investigate the phytochemical nature and anti-inflammatory, antimicrobial potential by adopting suitable methods. Phytochemical analysis of Hugonia mystax L., plant extracts revealed the presence of various biochemical compounds such as alkaloids, flavonoids, glycosides, triterpenoids and saponins etc. Since triterpenoids and flavonoids have remarkable anti-inflammatory activity, so our present work aims at evaluating in vitro anti inflammatory activity of Hugonia mystax L., by HRBC membrane stabilization method. The inhibition of hypotonicity induced HRBC membrane lysis was taken as a measure of the anti-inflammatory activity. The percentage of membrane stabilization for ethanolic extracts and Diclofenac sodium were done at different concentrations. The maximum membrane stabilization of Hugonia mystax L., extracts was found to be 94.97 % at a dose of 2000 μg/ml. Therefore, our studies support the isolation and the use of active constituents from Hugonia mystax L., in treating inflammations.

Anti-nociceptive and anti-inflammatory activity of synthesized novel benzoxazole derivatives

2021 ◽  
Vol 20 ◽  
Author(s):  
Mansi L. Patil ◽  
Swati S. Gaikwad ◽  
Naresh J. Gaikwad
Keyword(s):  
Cytotoxic Activity ◽  
Research Study ◽  
Ex Vivo ◽  
Immunological Response ◽  
Inflammatory Activity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Introduction: Pain is an immunological response to any infection or inflammation and long term use of pain management therapy includes use of Nonsteroidal anti-inflammatory drugs which is associated with occurrence of toxicity as well as gastrointestinal bleeding. Therefore, the investigation of new analgesic and anti-inflammatory agents remains a major challenge. Aims: The objective of this research study is to undergo the pharmacological evaluation of newly synthesized benzoxazole derivatives. These novel derivatives were evaluated for anti-nociceptive, anti-inflammatory and cytotoxic activity using various in-vivo and ex-vivo methods. Methods: The study was carried out using swiss mice (adult male) weighing between 20gm to 30gm and were divided into groups containing (n=6) six animals in each group for treatment. The anti-nociceptive activity was performed by using 0.1ml of 0.6% v/v acetic acid as nociception inducer and evaluated by the diminished number of abdominal writhes. The anti-inflammatory activity was done using 0.1 ml of 2% w/v Carrageenan induced paw edema method was observed which was evaluated by calculating the percent maximum possible effect. Histopathological evaluation and cytotoxic activity of the compounds was carried out. Results: The results of this research study revealed that synthesized derivatives (a, b, c, d and e) showed promising anti-nociceptive and anti-inflammatory effect along significantly higher cytotoxic activity in MCF-7 cell lines. Conclusion: It can be concluded that synthesized derivatives (a, b, c, d and e) have potential anti-nociceptive and anti-inflammatory effect along with cytotoxic activity and certain modification in structure may result in potent activity.

scholarly journals A REVIEW ON IN VIVO AND IN VITRO EXPERIMENTAL MODELS TO INVESTIGATE THE ANTI-INFLAMMATORY ACTIVITY OF HERBAL EXTRACTS

2018 ◽  
Vol 11 (11) ◽  
pp. 29
Author(s):  
Inayat Kabir ◽  
Imtiyaz Ansari
Keyword(s):  
Reference Model ◽  
Experimental Models ◽  
Inflammatory Activity ◽  
Herbal Extracts ◽  
Double Positive ◽  
Arthritis Models ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

The article emphasizes the anti-inflammatory effects of herbal extracts on different experimental models that are repeatedly used to test the in vivo anti-inflammatory activity of herbal components. Edema, granuloma and arthritis models are used to test the anti-inflammatory activity of plant extracts whereas formalin or acetic acid-induced writhing test and hot plate methods are the most repeatedly used to evaluate anti-nociceptive potentials of the herbal extracts. Although adjuvant-induced and collagen-induced arthritis models are also quite efficient, they have been used seldom to evaluate anti-inflammatory tendencies of the herbs. Here, we suggest a double positive reference model using both steroid and nonsteroidal anti-inflammatory drugs at the same time, instead of using only one of them either.

Sign in / Sign up

Export Citation Format

Share Document