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- Volume 21, Issue 1, 2022
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Inflammatory and Anti-Allergy Agents) - Volume 21, Issue 1, 2022
Volume 21, Issue 1, 2022
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Diosgenin: Mechanistic Insights on its Anti-inflammatory Effects
Diosgenin (DG), a well-known steroid saponin, has shown anti-inflammatory effects. This review was aimed to discuss all published literature concerning the anti-inflammatory effects of diosgenin. Based on the modulatory impact of DG on the NF-ΚB pathway, its supplementation is associated with downregulation of the NF-ΚB pathway and TGF-β, resulting in inhibition of inflammation. It appears that upstream modulators of NF-ΚB signaling pathways such as Tlrs and downstream mediators include iNOS and COX-2, leading to the inhibition of the inflammatory response and development of pathological conditions. Due to the low toxicity of the herbal compounds, the risk of the side effects of DG use for the management of inflammatory disorders such as asthma, rheumatism, rhinitis, and arthritis is lower than that of synthetic glucocorticoids. It has been shown that regulation of NF-ΚB and oxidative stress signaling pathways by DG is beneficial against cardiotoxicity induced by chemotherapeutic agents such as doxorubicin.
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Evaluation of Pleotropic Protective Activity of Capparis spinose Extract on Arthritis Rat Model
Authors: Mohammed Yosri, Mahmoud M. Elaasser, Marwa M. Abdel-Aziz, Hanna Y. Ahmed and Basma H. AminBackground: Capparis spinosa grows in Asian and Mediterranean desert areas. Different parts of Capparis spinosa, including flowers, have been used in various folk medicine applications. Objective: This study aims to evaluate the anti-arthritic potential of ethanolic extract of Egyptian Capparis spinosa flowers in a rat model of rheumatoid arthritis. Moreover, analysis of Capparis spinosa extract was performed using LC-qTOF-MS/MS. Methods: Animals were split into six groups: negative control group, induced arthritic animals, arthritic rats receiving 7, 14 and 28 mg/kg of Capparis spinosa extract, respectively, in three groups to detect the optimum dose, and the induced group receiving a standard drug. The arthritic score was checked daily for 15 days after induction. After animals were sacrificed, their joints and muscles were subjected to microscopic and ultra-structure examinations. Ex vivo culturing of osteoclasts was performed. Cytokine levels were measured in all examined groups. Results: The results revealed 7 mg/kg of Capparis spinosa extract as the optimal dose, which decreased inflammation signs through controlling chondrocytes, osteoclasts, and levels of inflammatory mediators. Conclusion: LC-Mass analysis revealed Capparis spinosa extract to contain a mixture of flavonol glycosides, flavan-3-ols and hydroxycinnamic acid derivatives, which may provide beneficial multifunction in regulating arthritic symptoms.
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In vitro Anti-hemolytic Effect, in vivo Anti-inflammatory and in vitro Anti-oxidant Activity of Anchusa azurea Mill
Background: Anchusa azurea Mill. (AA) is a medicinal plant largely used traditionally in folk medicine in Algeria; it is locally named hamham. It is effective in the treatment of various diseases. Objectives: The aim of the present study is to determine the antioxidant, anti-inflammatory, and anti- hemolytic effects of phenolic fractions from Anchusa azurea Mill. Methods: In this study, various extracts from Anchusa azurea Mill. (AA) using solvents with increasing polarity were prepared. The quantification of polyphenols and flavonoids was determined. The anti-radical activity of the different extracts was evaluated using DPPH and by measuring the inhibition of the oxidative degradation of β-carotene. The In-vitro antihemolytic effect of the plant extracts is determined (CrE, ChE, AcE, and AqE). For each extract, four concentrations were tested: 10.59, 21.18, 42.37, 84.74 μg/ml. Vitamin C is used as a standard. The free-radical attack was measured by measuring the HT50 (Half-Hemolysis Time). The anti-inflammatory effect using PMA on mice of the methanolic extract (CrE) was evaluated. Results: The quantification of polyphenols and flavonoids showed that ethyl acetate extract (AcE) contains a higher amount of polyphenols. However, chloroform extract (ChE) presents a higher amount of flavonoids. AcE showed an important scavenging activity using the DPPH radical (IC50= 68.35 μg/ml). The results showed that AcE also exhibited a significant inhibition effect on the oxidation of β-carotene/linoleic acid (84.33 %). All extracts increased the HT50 values (Half-Hemolysis Time) in a dose-dependent manner. The three highest concentrations (21.18, 42.37, and 84.74 μg / ml) of ChE caused a very significant delay (p ≤ 0.001) of hemolysis compared to the negative control and the positive control “VIT C”. The anti-inflammatory effect of using PMA on mice showed that the methanolic extract (CrE) of AA reduced the weight of the ear edema. Conclusion: This plant has a strong pharmacological power, which supports its traditional medicinal use.
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Synthesis and Biological Activity of the Pyridine-hexacyclic-steroid Derivative on a Heart Failure Model
Background: Several drugs with inotropic activity have been synthesized; however, there is very little information on biological activity exerted by steroid derivatives in the cardiovascular system. Objective: The aim of this research was to prepare a steroid-pyridine derivative to evaluate the effect it exerts on left ventricular pressure and characterize its molecular interaction. Methods: The first stage was carried out through the synthesis of a steroid-pyridine derivative using some chemical strategies. The second stage involved the evaluation of the biological activity of the steroid-pyridine derivative on left ventricular pressure using a model of heart failure in the absence or presence of the drugs, such as flutamide, tamoxifen, prazosin, metoprolol, indomethacin, and nifedipine. Results: The results showed that steroid-pyridine derivative increased left ventricular pressure in a dose-dependent manner (0.001-100 nM); however, this phenomenon was significantly inhibited only by nifedipine at a dose of 1 nM. These results indicate that positive inotropic activity produced by the steroid-pyridine derivative was via calcium channel activation. Furthermore, the biological activity exerted by the steroid-pyridine derivative on the left ventricle produces changes in cAMP concentration. Conclusion: It is noteworthy that positive inotropic activity produced by this steroid-pyridine derivative involves a different molecular mechanism compared to other positive inotropic drugs. Therefore, this steroid could be a good candidate for the treatment of heart failure.
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Xylopic Acid Suppresses Adjuvant-induced Arthritis in Sprague Dawley Rats via Reduction in Serum Levels of IL-6 and TNF-alpha
Authors: Newman Osafo, Aaron O. Antwi and Sarah Otu-BoakyeBackground: Xylopic acid (XA) is the principal constituent obtained from the biofractionation of the dried fruits of Xylopia aethiopica. Our initial reports have established the acute anti-inflammatory activity of this kaurene diterpene. Objective: Currently, we investigate the chronic anti-inflammatory activity of xylopic acid. Methods: The adjuvant-induced arthritis model in rats was employed in carrying out the study. Results: It was observed from the study that XA significantly (P < 0.05) suppressed the oedema associated with adjuvant arthritis while preventing associated joint deformation as identified from the radiographs. Histopathological analysis of joints of treated animals revealed signs of bone reformation and re-calcification following XA administration. From the haematological analysis, xylopic acid significantly decreased eosinophil sedimentation rate (ESR) while also decreasing white blood cells (WBC), which were increased after arthritis induction. Serum analysis showed the inhibitory effect of XA on serum expression of IL-6 and TNF-alpha in arthritic rats. Conclusion: Our study demonstrates the anti-arthritic activity of orally administered XA while pointing to a possible mechanism of its anti-inflammatory action.
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Evaluation Of Anti-inflammatory Mediated Anti-hemorrhoidal Activity of Lawsonia inermis on Croton Oil Induced Hemorrhoidal Rats
Authors: Sai K. Nallajerla and Suhasin GantaBackground: Hemorrhoids are a common recto-anal disorder commonly known as piles or tissue clumps in the rectum. In normal individuals, they were known as anal cushions. In the anus, they are composed of rectal blood vessels, muscles, and elastic fibres. When bulged, it can cause bleeding, constipation, itching, severe pain, and bleeding in the anus. Inflammation of the anal cushion remains major pathogenesis for the development of hemorrhoids. Inflammatory mediators like neutrophils, TNF-α, and IL-6 seem to play a major role in the development of disease. Objective: This study aims to carry out the ethanolic leaf extract of Lawsonia inermis (L. inermis) and evaluate its anti-hemorrhoidal activity both in vitro and in vivo. Furthermore, Molecular Docking was performed on the crystal structure of COX-2 with the selective compound 23d-(R) (PDB ID: 3NTG) protein. Methods: The current study is to estimate an anti-inflammatory mediated anti-hemorrhoidal activity of ethanolic leaf extract of L. inermis at different doses of 200 mg/kg/ir and 400 mg/kg/ir in croton oil-induced hemorrhoidal rats. Pilex ointment is taken as a reference standard in the present study. Evan's blue extravasation technique were applied in the study to quantify the proinflammatory protein. Results: From the study results, a dose-dependent effect was found for ethanolic leaf extract of Lawsonia inermis at 200 mg/kg and 400 mg/kg causing a significant reduction of serum Proinflammatory mediators TNF-α, IL-6, and plasma neutrophils in croton oil-induced hemorrhoidal rats. Conclusion: Studies represented that the plant extract can significantly inhibit protein denaturation of egg albumin in in vitro and found to reduce croton oil induced inflammatory mediators in hemorhhoidal rats.
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Volumes & issues
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Volume 23 (2024)
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Volume 22 (2023)
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Volume 21 (2022)
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Volume 20 (2021)
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Volume 19 (2020)
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Volume 18 (2019)
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Volume 17 (2018)
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Volume 16 (2017)
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Volume 15 (2016)
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Volume 14 (2015)
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Volume 13 (2014)
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Volume 12 (2013)
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Volume 11 (2012)
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Volume 10 (2011)
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Volume 9 (2010)
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Volume 8 (2009)
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Volume 7 (2008)
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Volume 6 (2007)
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Volume 5 (2006)
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