scholarly journals Enzymes associated with anti-inflammatory potentialities of purified terpenoid extracts from the selected sea weeds

2020 ◽  
Vol 11 (3) ◽  
pp. 497-505
Author(s):  
Sumayya S S ◽  
Lubaina A S ◽  
Murugan K

Introduction: Macrophages are phagocytic WBCs involved in the immune defense and will be activated during inflammatory disorders. The synthesis of cytokines and mediators, particularly nitric oxide (NO) is triggered by the macrophage activator. NO induces many biological events. Therefore, NO regulation is proven to be potential for exploring anti-inflammatory drugs. Aim: The anti-inflammatory action of the purified terpenoid extracts from red algae such as Hypnea musciformis, Gracilaria dura and Kappaphycus alvarezii on LPS induced RAW 264.7 macrophages on lipoxygenase, cyclooxygenase, hyaluronidase, xanthine oxidase and myeloperoxidase inhibitory effects were evaluated. Methods: The methanolic extract of the sea weeds were subjected to silica gel column chromatography and the fraction was further subjected to GC-MS analysis. Then, the potentiality of the purified terpenoid extracts to inhibit various inflammation causing enzymes such as COX, LOX, hyaluronidase, xanthineoxidase and myeloperoxidase were carried out. Findings: The terpenoid extracts reduced the enzyme activities in a dose dependent manner as compared to control group. The extracts inhibited xanthine oxidase activity effectively at 250 µg/ml i.e., a maximum inhibitory activity of 62.1% as compared to the standard drug, allopurinol. The extract significantly inhibited lipoxygenase activity, with highest inhibitory activity at 100 µg/ml. The nitric acid synthesis was reduced to 8.5 µM by Hypnea musciformis. Conclusion: The present study revealed that the purified terpenoid extracts from H. musciformis exhibited potent anti-inflammatory activities followed by G. dura and K. alvarezii via regulating the anti-inflammatory enzymes. These findings provide justification for the traditional use of the red algae in inflammatory conditions.

Author(s):  
Murugan K ◽  
Sumayya S s ◽  
Lubaina A S

Marine natural products from seaweeds have been the focus of research for novel products of pharmacological interest. Bioactivities of the phytochemicals derived from marine algae are important ingredients in many products, such as cosmetics and drugs for treating cancer and other lifestyle disorders. In this context, the aim of the present study is to compare the anti-inflammatory, analgesic, antipyretic properties of the purified terpenoids from the selected red algae Hypnea musciformis, Gracilaria dura and Kappaphycus alvarezii. Initially, the acute toxicity of the purified terpenoid extract was analyzed and was greater than 4000 mg/kg bw. In vitro BSA denaturation assay revealed significant % inhibition as compared to control. In the carrageenan induced paw edema, the purified terpenoids extract of H. musciformis exhibited remarkable soothing activity with 68.8% percentage of inhibition, which was comparable with that of indomethacin. Meanwhile G. dura and K. alvarezii showed 53 and 50% of inhibition respectively. Analgesic activity was determined by hot plate and acetic acid induced writhing test. In the hot plate test, terpenoids extract of H. musciformis and G. dura significantly increased the hot-plate latency as compared to normal saline, which reflects their analgesic efficacy. In the writhing test, terpenoid extracts from H. musciformis, G. dura and K. alvarezii inhibited the writhing response induced by acetic acid in a concentration dependent manner that suggests its varied mode of inhibition of stretching episodes. Lastly, the antipyretic activity was analyzed. Terpenoid extracts from H. musciformis, G. dura and K. alvarezii revealed a significant (P < 0.01) antipyretic activity up to 180 min.  In summary, the study demonstrates the anti-inflammatory, analgesic and antipyretic effects of terpenoids extracts from H. musciformis, G. dura and K. alvarezii on experimental models, suggesting its therapeutic potential in the treatment of peripheral painful and inflammatory pathologies.


2021 ◽  
Vol 20 (2) ◽  
pp. 426-430
Author(s):  
Nurhasan Agung Prabowo ◽  
Zainal Arifin Adnan ◽  
Arief Nurudhin ◽  
Yulyani Werdiningsih ◽  
Kukuh Prasetyo

Background: Systemic lupus erythematosus is a chronic autoimmune disease that affects target organs. mesenchymal stem cell conditioned medium has immunosuppressive, anti-inflammatory, and immunoregulatory properties in lupus. Methyl prednisolone is a standard drug for lupus with immunosuppressive and anti-inflammatory properties. This study aims to compare the therapeutic effect of mesenchymal stem cell conditioned medium administration compared to methyl prednisolone on interleukin 10 levels and the degree of pulmonary vasculitis of lupus mice. Methods: The subjects were 24 female mice of Mus musculus Balb/C strain, which were categorized into 4 groups of 8 mice, i.e. the control group receiving 0.5 cc of 0.9% NaCl injection and placebo, the lupus group receiving 0.5 cc of pristane injection and placebo, and the treatment mesenchymal stem cell conditioned medium group receiving 0.5 cc pristane injection and mesenchymal stem cell conditioned medium 0,5 cc, and methylprednisolone group receiving 0,5 cc pristiane injection and methylprednisolone p.o 1,5 mg/kgbodyweight. After 24 days the mice were terminated and kidney and blood samples were taken. Statistical analysis was performed using ANOVA test followed by independent T-test. The p value was considered significant when the p < 0.05. Results: The study showed that there was no difference on the levels of interleukin level10 among mesenchymal stem cell conditioned medium goup and methyl prednisolone group (CM = 5,94 ± 2,49 pg/mL, mp = 5,86+1,73 pg/mL; p = 1) and the degree of pulmonary vasculitis (CM= 1,94 ± 0,25, MP=1,89+ 0,11 pg/ml; p = 0.667). Mesenchymal stem cell conditioned medium as good as methyl prednisolone in decreasing levels of interleukin 10 and the degree of pulmonary vasculitis in lupus mice. Conclusion: Mesenchymal stem cell conditioned medium as good as methyl prednisolone in decreasing levels of interleukin 10 and the degree of pulmonary vasculitis in lupus mice Bangladesh Journal of Medical Science Vol.20(2) 2021 p.426-430


2016 ◽  
Vol 19 (1) ◽  
pp. 15-24
Author(s):  
Muhammad Shoaib Akhtar ◽  
Zulfiqar Khan ◽  
Muhammad Naveed Mushtaq ◽  
Muhammad Salman Akhtar

The current study was planned to evaluate comparative anti-inflammatory, analgesic and anti-pyretic activities of two newly synthesized organo-antimony (v) ferrocenyl benzoate derivatives with piroxicam. Anti-microbial activity of these compounds was also screened against two microorganisms. Analgesic effect of test compounds was evaluated by formalin-induced paw licking test in mice. The test compounds at 50 and 100 mg/kg b.w. doses exhibited significant (p<0.001) reduction of paw licking in treated mice comparable with standard drug piroxicam. Anti-inflammatory activity was assessed against carrageenan-induced paw oedema. The compound A produced anti-inflammatory effects comparable with standard piroxicam in dose dependent manner whereas compound B showed better effects than piroxicam at dose of 100 mg/kg body weight. To investigate anti-pyretic activity, fever was induced by administration of Brewer’s yeast in mice. Compound A showed highly significant inhibition of pyrexia (p<0.001) comparable to piroxicam after 3 hours while compound B (50 and 100 mg/kg) produced relatively lower anti-pyretic effect than standard drug. Antibacterial activity determined by disc diffusion method showed that compound B was relatively more effective than compound A against Staphylococcus aureus and Klebsiella pneumoniae. It is conceivable that both the tested compounds possessed anti-inflammatory, analgesic, anti-pyretic and anti-microbial effects even after the structural modification of parent compound.Bangladesh Pharmaceutical Journal 19(1): 15-24, 2016


2019 ◽  
Vol 97 (7) ◽  
pp. 611-622 ◽  
Author(s):  
Mohammed M. Heikal ◽  
Ahmed A. Shaaban ◽  
Wagdi F. Elkashef ◽  
Tarek M. Ibrahim

Febuxostat, a highly potent xanthine oxidase inhibitor with an antioxidant effect, inhibits elevated xanthine oxidase, leading to reduction of reactive oxygen species and oxidative stress, the main causes of vascular inflammation in hyperlipidemia. The aim of this study was to test the potential antioxidant and anti-inflammatory effects of febuxostat and (or) stopping a high-fat diet on the biochemical parameters in rabbits with hyperlipidemia induced by a high-fat diet. Male New Zealand rabbits were distributed into 3 groups: a normal control group fed standard chow for 12 weeks and 2 other groups fed a high-fat diet with 1% cholesterol for 8 weeks, and then shifted to standard chow for 4 weeks. During the last 4 weeks, one high-fat diet group received 0.5% carboxymethyl cellulose, whereas the other group was treated with febuxostat (2 mg/kg per day p.o.). Febuxostat significantly lowered low-density lipoprotein cholesterol (“bad” cholesterol) compared to the untreated group (high-fat diet group). Febuxostat also displayed a potent anti-inflammatory and antioxidant activity by decreasing serum levels of lipid peroxidation index, proinflammatory cytokines, and enhancing antioxidant enzyme activity. Stopping the hyperlipidemic diet in the high-fat diet group did not show improvement. These findings indicate the antioxidant and anti-inflammatory effects of febuxostat that may be common mechanisms of the anti-hyperlipidemic effect of this drug. Stopping a hyperlipidemic diet without treatment is not sufficient once injury has occurred.


Author(s):  
Jun Yin ◽  
In Hyoek Hwang ◽  
Min Won Lee

Abstract Background Carpinus tschonoskii (CT) has been previously studied for various activities in the improvement of skin diseases. In the present study, we examined the in vitro anti-acne vulgaris (AV) effect of CT leaves (CTL) and tellimagrandin I (TI), one of the main ellagitannins from CT, including skin barrier improvement and 5α-reductase inhibitory activity. Methods To test the anti-AV activities of CTL and TI, firstly, anti-oxidative and anti-inflammatory activities including DPPH radical scavenging activity, nitric oxide (NO) inhibitory activity, and cytokines [interleukin (IL)-6 and IL-8] were tested. Skin barrier improvement experiments were tested using developing cornified envelope (CE) formation, and filaggrin mRNA expression level was determined by RT-PCR. The 5α-reductase inhibitory activity was determined by measuring the testosterone levels in rat liver microsomes. Results CTL and TI showed potent anti-oxidative activity and anti-inflammatory activities. Especially, the cytokine production inhibitory activities of TI were found to be similar to the positive control, epigallocatechin gallate (EGCG). CTL and TI enhanced the CE formation and filaggrin mRNA expression levels and showed potent activities compared to that in the positive control, 1.5 mM Ca2+. In additionally, CTL and TI showed 5α-reductase inhibitory activities in a dose-dependent manner. Conclusion The results showed that CTL and TI inhibit AV endogenous factors such as 5α-reductase and inflammatory cytokines and affect exogenous factors such as developing skin barrier function (CE and filaggrin levels). Therefore, CTL and TI may be plant-derived agent, promising in the treatment of acne vulgaris.


Author(s):  
Jolanta Dzik

The bacteria Legionella, being able to infect both macrophages and protozoans, reduce oxidative phosphorylation and induce glycolysis, which allows pathogens to grow and replicate in these cells. In amoeba-like inflammatory macrophages (M1), the phagocytizing cells of the primary immune defense, an increase in the rate of glycolysis is followed by a decrease of oxidative phosphorylation. The opposite takes place in anti-inflammatory macrophages (M2). They change from glycolysis to oxidative metabolism when AMP-dependent kinase (AMPK) is activated by a high ratio of AMP/ATP. Stimulation of macrophages with anti-inflammatory cytokines causes activation of AMPK. Infection of macrophages with the parasitic flagellate Leishmania infantum induces a switch from an initial glycolytic phase to oxidative phase with the essential role of AMPK in this change. Activated AMPK induces catabolic pathways effectively producing ATP as well as processes requiring the energy supply. AMPK regulates the migration of cells and enhances the phagocytic activity of macrophages. In macrophages, bacterial products activate TLRs and NF-κB signaling, causing an increase of transcription of hypoxia-induced factor HIF-1α (a subunit of HIF-1). This brings about induction of the enzyme and transporter expression essential for glycolysis and the pentose phosphate pathway to proceed and makes biosynthetic processes and ROS production in macrophages possible. Hypoxia augments macrophage phagocytosis in a HIF‐1α‐dependent manner. Multicellular parasites experience changes in the availability of oxygen in their life cycle. In the nematode Ascaris suum, HIF participates in the pre-adaptation to hypoxic conditions after infection of their hosts. Also, the freshwater and marine invertebrates meet changes of oxygen concentrations. In the anaerobic branch of the respiratory chain of these invertebrates, fumarate serves as the terminal electron acceptor that is reduced to succinate in complex II of the ETC. In mammalian cells, accumulation of succinate under hypoxic conditions suggests that the mammalian complex II may reduce fumarate to succinate, too. The data reviewed here show that the ability to shift the cell metabolism towards glycolysis observed in activated macrophages can be traced back in evolution to metabolic changes characterizing protozoans infected with bacteria. Anabolic needs of multiplying bacteria direct host metabolism to glycolysis that produces, aside from ATP, precursors of the amino acids used by the pathogen for its protein synthesis. M1-activated mammalian macrophages behave in the same way. Regulation of metabolism in M1 and M2 macrophages is further enhanced by HIF-1 and AMPK, respectively. These archaic functions of AMPK and HIF, important also to control phagocytosis and cell migration were extended to embryonic development in multicellular organisms.


Author(s):  
PANKAJ SHARMA ◽  
RAJU L

Objective: The objective of the study was to investigate the pharmacognosy as well as the antioxidant, anti-inflammatory potential of the Katha powder. Methods: The Coarsely dried chips of Acacia catechu heartwood were treated with 10 % hydro-alcoholic solution to obtain Katha as the final product. The powdered Katha was standardized through pharmacognostic parameters. This Katha power is showing the good solubility in the hot water having astringent in the taste. The powder microscopy of the Katha powder is to be demonstrated fragments of acicular crystals, fibers, and bordered pitted vessels. Katha powder antioxidant potential is to be accessed by using the 2, 2-diphenyl-1-picryl hydrazyl assay and NO Scavenging assay using ascorbic acid as a standard drug. Further, the Katha powder is to be subjected for the assessment of its anti-inflammatory potential by the use of heat-induced hemolysis as well as hypotonicity-induced hemolysis approach by the use of the aspirin or diclofenac sodium as a standard drug. Results: Microscopical investigations were showed that Katha showing the presence of fragments of acicular crystals, fibers, and bordered pitted vessels. In vitro study shows that the Katha powder has excellent antioxidant as well as anti-inflammatory potential in a dose-dependent manner in comparison of the result of heartwood of A. catechu. Conclusion: So from this investigation, it is to be suggested that the Katha powder is rich in the phenolic compound and the experimentation study shows that the drug is to possess a good antioxidant as well as anti-inflammatory property.


Author(s):  
sherine ibrahim ◽  
ahmed fayez ◽  
ahmed maher

IntroductionLiver fibrosis is currently the 11th most common cause of death worldwide. Because of self-renewal, available sources for isolation, and high differentiation properties, multipotent mesenchymal stromal stem cells are suggested to be potential tool for treatment of liver fibrosis. In this study, we examined the anti-fibrotic and anti-inflammatory activity of bone marrow-derived multipotent mesenchymal stromal stem cells (MSCs) on liver fibrosis induced by carbon tetrachloride on rats relative to silymarin as a standard drug.Material and methodsThis study was performed on 40 male Sprague Dawley rats divided into 4 groups of ten rats each: Group 1 served as controls, Group 2 served as CCl4 (diseased) group, Group 3 served as silymarin treated group and Group 4 served as MSCs treated group. Liver fibrosis was assessed by determination of liver markers and fibrogenesis related genes together with the anti-inflammatory markers in the liver tissue. DNA fragmentation was assessed by Comet assay.ResultsMSCs treatment reduced all liver fibrosis markers as well as the oxidative stress and inflammatory markers. Additionally, MSCs reduced the expression of integrins and fibronectin compared with the control group as well as decreasing DNA fragmentation.ConclusionsTreatment by MSCs significantly ameliorates liver fibrosis in rats. This amelioration was a result of acting on both the anti-inflammatory and anti-fibrotic activity of hepatocytes.


2023 ◽  
Vol 83 ◽  
Author(s):  
Romina Chitsaz ◽  
Atefeh Zarezadeh ◽  
Jinous Asgarpanah ◽  
Parvaneh Najafizadeh ◽  
Zahra Mousavi

Abstract: Rubiadin is identified as a bioactive anthraquinone that exists in some quinone rich plants. The current research was carried out to evaluate the potential anti-inflammatory impact of Rubiadin in acute and chronic inflammation test models in rodents. The anti-inflammatory activity of Rubiadin was examined in cotton pellet-induced granuloma and carrageenan-induced edema as chronic and acute inflammation models in rats. TNF-α level and histopathological changes were assessed using sampled foot tissue of rat in the acute model. Also, the IL-1β level was assessed in the chronic model. One-way ANOVA (post hoc Tukey’s) analysis was used for comparing the groups. Rubiadin (0.5 mg/kg, i.p.) induced a significant reduction in TNF α level and the paw edema compared to the control group in carrageenan test. Also, it was observed that the anti-inflammatory activity of Rubiadin (0.5 mg/kg, i.p.) is comparable to mefenamic acid (30 mg/kg, i.p.) as the standard drug. Rubiadin was effective in granuloma induced by cotton pellet concerning the granuloma and transudate formation amount. Rubiadin’s anti-inflammatory effects were associated with a significant IL-1β decrease in this model. The results suggest that Rubiadin as a natural compound can possess significant peripheral anti-inflammatory impacts.


2015 ◽  
Vol 10 (11) ◽  
pp. 1934578X1501001
Author(s):  
Shivraj Hariram Nile ◽  
Doo Hwan Kim

Cudrania tricuspidata is a plant used in folk medicine in Korea for treatment of diseases related to oxidative stress and inflammation. In this study the leaf and shoot extract was studied for its antioxidant, anti-inflammatory, and xanthine oxidase (XO) inhibitory activities. The extract with predominant phenolics was quantified using HPLC-DAD. Antioxidant activity was measured using ABTS [2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) and FRAP (ferric ion reducing antioxidant power), and anti-inflammatory activity by diene-conjugate and β-glucuronidase assays. The average antioxidant effects of C. tricuspidata extracts (1–2 mg/mL) revealed significant activity of 32.5% to 50.2% (ABTS) and 24.2 to 40.5% (FRAP) compared with Trolox, having 55.1% (ABTS) and 42.6% (FRAP) activity, respectively. The anti-inflammatory activities showed as 26.5% to 40.5% (DC) and 40.2% to 70.2% (βG) inhibition compared with the control {phenylbutazone; 42.1% (DC) and 80.2% (βG) inhibition, respectively}. The XO inhibitory activity of the plant extract revealed 90.5% inhibition of that of the control (allopurinol) (97% inhibition at 100 μg/mL concentration). The kinetic parameters of XO inhibition revealed a noncompetitive type of inhibition, where, K m and V max of C. tricuspidata extracts (25 to 100 μg/mL) were 0.25 mM/mL and 0.040, 0.036, 0.032, and 0.030 (μg/min), while for the positive control K m and V max the values were 0.30 mM/mL and 0.045 (μg/min), respectively. Results suggest that C. tricuspidata can be exploited against diseases associated with free radical formation and xanthine oxidase activity.


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