scholarly journals Design, Synthesis and Study of Nitrogen Monoxide Donors as Potent Hypolipidaemic and Anti-Inflammatory Agents

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 19
Author(s):  
Panagiotis Theodosis-Nobelos ◽  
Georgios Papagiouvanis ◽  
Maria Pantelidou ◽  
Panos N. Kourounakis ◽  
Chrysoula Athanasekou ◽  
...  
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Nitrogen Monoxide ◽  
Membrane Lipid ◽  
Minor Effect ◽  
Design Synthesis ◽  
Multifactorial Diseases ◽  
Anti Inflammatory ◽  
A Minor

Inflammation and oxidative stress are involved in cardiovascular diseases. Nitrogen monoxide participates in the regulation of endothelial processes. Thus, derivatives of classic nonsteroidal anti-inflammatory drugs (NSAIDs), trolox or cinnamic acids esterified with 2-(nitrooxy)ethanol were designed and studied. It was found that the nitrogen monoxide (NO) releasing activity was comparable to that of S-nitroso-N-acetylpenicillamine. The nitrooxy derivatives decreased potently lipid indices in the plasma of hyperlipidaemic rats (30–85%). All compounds presented increased anti-inflammatory activity in vivo, inhibiting carrageenan-induced rat paw oedema as high as 76%, up to six times higher than that of the parent acids. Lipoxygenase inhibitory activity was significant for most of them, although the parent molecules exerted a minor effect (IC50 > 0.2 mM). Those compounds incorporating an antioxidant structure inhibited rat microsomal membrane lipid peroxidation strongly and possessed radical scavenging activity. These results indicated that the described compounds could act at different targets in multifactorial diseases, further limiting the possible adverse effects of drug combinations.

scholarly journals Evaluation of Anti-Inflammatory and Analgesic Activities of Methanolic Extract of Aitchisonia Rosea in Albino Mice

2020 ◽  
Vol 8 (1) ◽  
pp. 31-36
Author(s):  
Shahid Rasool ◽  
Ambreen Malik Uttra ◽  
Mehreen Malik Uttra ◽  
Faheem Ahmed ◽  
Khizar Abbas
Keyword(s):  
Acetic Acid ◽  
Methanolic Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Paw Edema ◽  
Egg Albumin ◽  
Inflammatory Conditions ◽  
Albino Mice ◽  
Anti Inflammatory

Objective:  Current analysis aims at in-vivo investigation of analgesic and anti-inflammatory activities of Aitchisonia rosea methanolic extract. Methods: Albino mice (20-30 g) were used in the study. Extract at 200, 400 and 800 mg/kg doses was tested against egg albumin and carrageenan induced mice paw edema along with formalin persuaded paw licking and acetic acid prompted writhing for analgesic activity. Results: Results depicted dose reliant and significant (p<0.001) inhibition of carrageenan as well as egg albumin brought paw edema, abdominal constrictions/ hind limb stretching tempted by acetic acid and formalin instigated paw licking. Capability of crude extract to halt inflammatory and analgesic response was akin to that of ibuprofen in all models. Conclusion: The current findings support the use of Aitchisonia rosea for inflammatory conditions, which might be attributed to its previously proven high alkaloid, flavonoids, phenol, tannins content and free radical scavenging activity.

scholarly journals CHEMICAL ANALYSIS, ANTIOXIDANT, ANTI-INFLAMMATORY AND ANTINOCICEPTIVE EFFECTS OF ACETONE EXTRACT OF ALGERIAN SOLENOSTEMMA ARGEL (DELILE) HAYNE LEAVES

2020 ◽  
pp. 72-81
Author(s):  
DAOUIA KELTOUM BENMAAROUF ◽  
DIANA C. G. A. PINTO ◽  
BERNARD CHINA ◽  
SAFIA ZENIA ◽  
KHEIRA BOUZID BENDESARI ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Granuloma Formation ◽  
Paw Edema ◽  
Oral Toxicity ◽  
Traditional Use ◽  
Anti Inflammatory ◽  
Dose Dependent

Objective: To investigate the qualitative composition of the acetonic extract from leaves of S. argel (AESA) and their anti-inflammatory and analgesic properties in vivo. Methods: AESA profile was established by UHPLC/DAD/ESI-MS2. AESA was subjected to the acute oral toxicity study according to the OECD-420 method. Antioxydant activity of AESA was performed by DPPH radical scavenging assay. Anti-inflammatory effects of AESA were determined in two animal models: carrageenan-induced paw edema in rats and cotton pellet-induced granuloma formation in rats. Further, anti-nociceptives activities of AESA were assessed by hot plate test, acetic acid-induced abdominal writhing test and formalin test. Results: The in vivo AESA toxicity was low. AESA expresses a maximum radical scavenging activity with a IC50 value of 36,05 μg/ml. The AESA at 250 and 400 mg/kg significantly reduced carrageen an induced paw edema by 70.09% and 85.53% 6h after carrageenan injection, respectively. AESA produced significant dose-dependent anti-inflammatory effect against cotton pellets-induced granuloma formation in rats. In addition, AESA at 250 and 400 mg/kg significantly reduced acetic acid-induced writhing by 56.83 and 80.41%, respectively. Oral administration of 250 and 400 mg/kg of AESA caused a significant dose dependent anti-nociceptive effect in both neurogenic and inflammatory phases of formalin-induced licking. AESA also impacted the pain latency in the hot plat test. Conclusion: These data suggest that AESA possesses antioxidant, anti-inflammatory and anti-nociceptive effects. These results support the traditional use of S. argel to cure pain and inflammatory diseases in the Algerian Sahara.

scholarly journals Antioxidant, anti-inflammatory, analgesic and anti-proliferating activities of Grewia heterotricha Mast.

Biomedicine ◽  
2020 ◽  
Vol 40 (3) ◽  
pp. 272-277
Author(s):  
B. Usha ◽  
Karanth Jyothsna ◽  
Joshi Chandrashekhar G.
Keyword(s):  
Aqueous Extract ◽  
Methanolic Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Dpph Radical Scavenging Activity ◽  
Leaf Extracts ◽  
Anti Inflammatory ◽  
Dpph Radical Scavenging

Introduction and Aim: Plants are considered to be novel source of active compounds having pharmacological properties and help in the development of therapeutic agents. Hence, this study was undertaken to evaluate the antioxidant, anti-inflammatory, analgesic and anti-proliferating activity of aqueous and methanolic leaf extracts of Grewia heterotricha Mast. Materials and Methods: The aqueous and methanolic leaf extracts of the plant were assessed for their in-vitro antioxidant activity by DPPH radical scavenging activity, in-vivo anti-inflammatory activity by carrageenan induced rat paw edema method, in-vivo analgesic activity by acetic acid-induced writhing test and in-vitro anti- proliferating activity by MTT assay. Results: The methanolic extract had shown very significant DPPH radical scavenging activity with IC50 value 98.95?g/ml than aqueous extract and showed a significant reduction in the paw volume of rats at the concentration of 100 mg/kg body weight indicating potent anti-inflammatory activity compared with the reference standard Diclofenac sodium. Both the extracts showed significant analgesic effect (p<0.001) in acetic acid-induced pain models in a dose dependent manner. The methanolic extract showed higher analgesic activity compared to aqueous extract by inhibiting the pain indicated by a decrease in the number of writhes. In addition, both the extracts showed a decrease in MCF-7 cell viability at the concentration of 550µg/ml. Compared to the aqueous extract, MEGH has shown more cytotoxic effect on the cancer cell lines. Conclusion: The results suggest that both aqueous and methanolic extracts of Grewia heterotricha Mast. leaves possess potent antioxidant, analgesic, anti-inflammatory and anti-proliferating properties, which supports the use of the plant in traditional medicine. Further investigation is required to illuminate on its active compounds.   Keywords: Analgesic; anti-inflammatory; DPPH; cytotoxic.

scholarly journals In Vivo and In Vitro Evaluation of Preventive Activity of Inflammation and Free Radical Scavenging Potential of Plant Extracts from Oldenlandia corymbosa L.

2021 ◽  
Vol 11 (19) ◽  
pp. 9073
Author(s):  
Mahci Al Bashera ◽  
Ashik Mosaddik ◽  
Gaber El-Saber Batiha ◽  
Mohammed Alqarni ◽  
Md. Ashraful Islam ◽  
...  
Keyword(s):  
Free Radical ◽  
Protein Denaturation ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Scavenging Activity ◽  
Total Antioxidant ◽  
Anti Inflammatory

Aims: The present study evaluates the anti-inflammatory and antioxidant activity of the crude dichloromethane (CDCME), ethyl acetate (CEAE), and methanol (CMeE) extracts from the plant Oldenlandia corymbosa L. Background:Oldenlandia species have been popular among the people of the Indian subcontinent to treat several types of internal and external inflammation for a long time. Plant decoctions have been used to battle inflammation in cases of tonsilitis, pneumonia and cholecystitis, among others. Objective: The present work designed to demonstrate the properties of the previously mentioned plant extracts to prevent inflammation both in vivo and in vitro. This work is the first investigation of such extracts from this species and their relationship with anti-inflammatory activity. Method: The anti-inflammatory properties of the Oldenlandia corymbosa L. extracts were evaluated in vitro with the Red Blood Cell (RBC) membrane stabilization method and the protein denaturation method and in vivo with the carrageenan-induced paw oedema method. Furthermore, the free radical scavenging activity of the extracts was carried out with the 1,1-diphenyl-2- picrylhydrazyl (DPPH) radical oxidation, total antioxidant capacity and iron reduction assay. Result: Both in vivo and in vitro studies showed that CDCME had the most predominant effects with the value of 80.5% for RBC membrane stabilization, 60% for inhibition of protein denaturation at the concentration of 1000 µg/mL and 63.28% (after 3 h, * p < 0.05) for inhibition of paw oedema (300 mg/kg bwt) compared to carrageenan-induced mice. The free radical scavenging activity was studied by DPPH, total antioxidant and reducing activity assay. CDCME showed scavenging activity in all the methods and an IC50 value of 473.86 µg/mL for DPPH method. Conclusions: The findings of the study remarked that CDCME of the plant has strong anti-inflammatory and antioxidant effects that validate the traditional use of the plant to get remedy from pain. Other: The plants Oldenlandiacorymbosa Linn were provided by the Bangladesh Council of Scientific and Industrial Research Laboratory campus, Rajshahi, Bangladesh. Experiments on animals were conducted by ethical permission of Institute of Biological Sciences, University of Rajshahi, Bangladesh (license no: 225/320-IAMEBBC/IBSc).

Gabapentin Antioxidant Derivatives with Anti-Inflammatory and Neuroprotective Potency

2021 ◽  
Vol 18 ◽  
Author(s):  
Georgios Papagiouvannis ◽  
Panagiotis Theodosis-Nobelos ◽  
Paraskevi Tziona ◽  
Antonios Gavalas ◽  
Panos N. Kourounakis ◽  
...  
Keyword(s):  
Structural Characteristics ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Protein Glycation ◽  
Inflammatory Activity ◽  
Biochemical Pathways ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Effective Drugs

Aims: The aim of this work is to investigate the antioxidant and anti-inflammatory potency of novel gabapentin derivatives, which could be proven useful as neuroprotective agents. Background: Alzheimer’s Disease (AD) is one of the most common neurodegenerative disorders worldwide. Due to its multi-factorial character, no effective treatment has been obtained yet. In this direction, the multi-targeting compounds approach could be useful for the development of novel, more effective drugs against AD. Oxidative stress and inflammation are highly involved in the progression of neurodegeneration, while gabapentin has been investigated for the treatment of behavioral symptoms in AD. Objective: In this work, derivatives of cinnamic acid, trolox and 3,5-di-tertbutyl-4-hydroxybenzoic acid amidated with gabapentin methyl ester, were designed and studied. Compounds with these structural characteristics are expected to act in various biochemical pathways, affecting neurodegenerative processes. Methods: The designed compounds were synthesized with classical amidation methods, purified by flash column chromatography, and identified spectrometrically (1H-NMR and 13C-NMR). Their purity was determined by CHN elemental analysis. They were tested in vitro for their antioxidant and anti-inflammatory properties, and for their inhibitory effect on acetylcholinesterase. Their in vivo anti-inflammatory activity was also tested. Results: Those molecules incorporating an antioxidant moiety possessed inhibitory activity against rat microsomal membrane lipid peroxidation and oxidative protein glycation, as well as radical scavenging activity. Moreover, most of them presented moderate inhibition towards lipoxygenase (up to 51% at 100μΜ) and acetylcholinesterase (AchE) (IC50 up to 274μΜ) activities. Finally, all synthesized compounds presented in vivo anti-inflammatory activity, decreasing carrageenan-induced rat paw edema up to 53% and some of them could inhibit cyclooxygenase significantly. Conclusion: These results indicate that the designed compounds could be proven useful as multi-targeting molecules against AD, since they affect various biochemical pathways associated with neurodegeneration. Thus, more effective drugs can be obtained, and possible adverse effects of drug combination can be limited.

scholarly journals Anti-Inflammatory Potential Evaluation (In-Vitro and In-Vivo) of Arthrophytum scoparium Aerial Part

2020 ◽  
Vol 10 (5) ◽  
pp. 213-218
Author(s):  
Sabrina Manel Kaddour ◽  
Lekhmici Arrar ◽  
Abderrahmane Baghiani
Keyword(s):  
Protein Denaturation ◽  
Radical Scavenging Activity ◽  
Folk Medicine ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Traditional Use ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Arthrophytum scoparium is plant commonly used in folk medicine in Algeria to treat numerous human diseases especially infectious, Rheumatism, diabetes and cancer. However, its anti-inflammatory activity and the underlying mechanisms have not been studied systematically. The present study aims to assess both the in vitro and in vivo anti-inflammatory potential and antioxidant activity of the plant. Results showed that A. scoparium chloroform extract (ChE) contains the largest amount of phenolic and flavonoid compounds. In-vitro bioassay consisted of investigating the effect of the plant extracts against protein denaturation (BSA and egg albumin). In-vivo anti-inflammatory activity was evaluated by measuring the percentage inhibition of carrageenan-induced rat paw edema after oral administration of the extracts. Results showed that inhibition of protein denaturation was maximum in case of A. scoparium crude extract (CrE) with dose dependant manner. Similarly in the in-vivo study, carrageenan induced inflammation was significantly antagonized by CrE with inhibition of 87.02% at 400 mg/kg. CrE extracts showed the highest scavenger effect against hydroxyl and hydrogen peroxide. The CrE showed potent anti-inflammatory activity in both the conditions in vivo and in vitro. In conclusion different A. scoparium extracts scavenged reactive oxygen species efficiently; it may be due to the presence of its flavonoids and polyphenols. These results support the traditional use of this plant. Keywords: Arthrophytum scoparium, polyphenols, anti-inflammatory activity, radical scavenging activity.

Jobelyn® exhibited anti-inflammatory, antioxidant, and membrane-stabilizing activities in experimental models

2015 ◽  
Vol 26 (5) ◽  
Author(s):  
Solomon Umukoro ◽  
Oluwafemi Gabriel Oluwole ◽  
Anthony T. Eduviere ◽  
Omogbiya Itievere Adrian ◽  
Abayomi M. Ajayi
Keyword(s):  
Chronic Inflammation ◽  
Acute Inflammation ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Experimental Models ◽  
Hypotonic Medium ◽  
Air Pouch ◽  
Anti Inflammatory ◽  
Air Pouch Model

AbstractJobelynAcute inflammation was induced with intraplanter injection of carrageenan and increase in rat paw volume was measured using plethysmometer. The volume of fluid exudates, number of leukocytes, concentrations of malondialdehyde (MDA), and glutathione (GSH) in the fluid were measured on day 5 after induction of chronic inflammation with carrageenan in the granuloma air pouch model. RBC lysis induced by hypotonic medium as determined by release of hemoglobin was measured spectrophotometerically.JB (50–200 mg/kg) given orally produced a significant inhibition of acute inflammation induced by carrageenan in rats. It reduced the volume and number of leukocytes in inflammatory fluid in the granuloma air pouch model of chronic inflammation. It further decreased the levels of MDA in the fluid suggesting antioxidant property. JB elevated the concentrations of GSH in inflammatory exudates indicating free radical scavenging activity. It also significantly inhibited RBC lysis caused by hypotonic medium, suggesting membrane-stabilizing property.JB has in vivo anti-inflammatory activity, which may be related to its antioxidant and membrane-stabilizing properties, supporting its use for the treatment of arthritic disorder.

scholarly journals IL-6 Is Not Absolutely Essential for the Development of a TH17 Immune Response after an Aerosol Infection with Mycobacterium tuberculosis H37rv

Cells ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 9
Author(s):  
Kristina Ritter ◽  
Jan Christian Sodenkamp ◽  
Alexandra Hölscher ◽  
Jochen Behrends ◽  
Christoph Hölscher
Keyword(s):  
Immune Response ◽  
Inflammatory Diseases ◽  
Mycobacterial Infection ◽  
Minor Effect ◽  
Mycobacterium Tuberculosis H37rv ◽  
Th 17 ◽  
Anti Inflammatory ◽  
A Minor ◽  
Aerosol Infection ◽  
Deficient Mice

Anti-inflammatory treatment of chronic inflammatory diseases often increases susceptibility to infectious diseases such as tuberculosis (TB). Since numerous chronic inflammatory and autoimmune diseases are mediated by interleukin (IL)-6-induced T helper (TH) 17 cells, a TH17-directed anti-inflammatory therapy may be preferable to an IL-12-dependent TH1 inhibition in order to avoid reactivation of latent infections. To assess, however, the risk of inhibition of IL-6-dependent TH17-mediated inflammation, we examined the TH17 immune response and the course of experimental TB in IL-6- and T-cell-specific gp130-deficient mice. Our study revealed that the absence of IL-6 or gp130 on T cells has only a minor effect on the development of antigen-specific TH1 and TH17 cells. Importantly, these gene-deficient mice were as capable as wild type mice to control mycobacterial infection. Together, in contrast to its key function for TH17 development in other inflammatory diseases, IL-6 plays an inferior role for the generation of TH17 immune responses during experimental TB.

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