scholarly journals Synthesis of some New Azo Compounds of Salicylic Acid Derivatives and Determination of their In vitro Anti-inflammatory Activity

2019 ◽  
Vol 35 (2) ◽  
pp. 870-876
Author(s):  
Husam Hamza Salman ◽  
Huda Salih Abood ◽  
Usama Hamid Ramadhan

This study included the preparation of a series of some new azo compounds by diazo coupling aromatic amines with salicylic acid derivatives. The prepared compounds identified using precise elemental analysis (C.H.N.), the results supported the structure of concerned compounds. The synthesized azo compounds also identified by using infrared spectroscopy and 1H-NMR spectroscopy. Anti-inflammatory activity of the compounds were determined in-vitro by human red blood cell (HRBC) membrane stability method, the compounds showed a significant activity to protection of the cell membrane. Other compounds show moderate to low activity, sodium diclofenac was used as positive control.

Author(s):  
Adek Zamrud Adnan ◽  
Muhammad Taher ◽  
Tika Afriani ◽  
Annisa Fauzana ◽  
Dewi Imelda Roesma ◽  
...  

 Objective: The aim of this study was to investigate in vitro anti-inflammatory activity of tinocrisposide using lipopolysaccharides (LPS)-stimulated RAW 264.7 macrophage cells. Tinocrisposide is a furano diterpene glycoside that was isolated in our previous study from Tinospora crispa.Methods: Anti-inflammatory effect was quantified spectrometrically using Griess method by measuring nitric oxide (NO) production after the addition of Griess reagent.Results: The sample concentrations of 1, 5, 25, 50, and 100 μM and 100 μM of dexamethasone (positive control) have been tested against the LPS-stimulated RAW 264.7 cells, and the results showed NO level production of 39.23, 34.00, 28.9, 20.25, 16.3, and 13.68 μM, respectively, and the inhibition level of 22.67, 33.00, 43.03, 60.10, 68.00, and 73%, respectively.Conclusions: From the study, it could be concluded that tinocrisposide was able to inhibit the formation of NO in the LPS-stimulated RAW 264.7 cells in concentration activity-dependent manner, with half-maximal inhibition concentration 46.92 μM. It can be developed as anti-inflammatory candidate drug because NO is a reactive nitrogen species which is produced by NO synthase. The production of NO has been established as a mediator in inflammatory diseases.


Bionatura ◽  
2020 ◽  
Vol 5 (4) ◽  
pp. 1387-1393
Author(s):  
Irina Francesca González Mera ◽  
Orestes Darío López Hernández ◽  
Vivian Morera Córdova

Epidendrum coryophorum belongs to the Orchidaceae family. Traditional uses of some species for this genus include infusions of the leaves used for kidney problems, treat influenza, conjunctivitis, liver pain, relieve kidney symptoms, and hypoglycemic effect. This work's objective was to determine the phytochemical profile of the ethanolic extract of Epidendrum coryophorum leaves and to evaluate the potential anti-inflammatory activity in vitro of the extract employing the erythrocyte membrane stabilization method. The phytochemical screening carried out in this work suggested phenols, coumarins, flavonoids, tannins, steroids, and sterols in the ethanolic extract of Epidendrum coryophorum leaves. Cardiotonic glycosides and carbohydrates were also found. The ethanolic extract's UV-Vis spectrum showed absorption maxima at 268 nm and 332 nm, which could correspond to flavonoids of the flavonoid classes, 3-OH substituted flavonols, or isoflavones. The quantitative determination of total phenols of the ethanolic extract was carried out using the Folin-Ciocalteu method. The total phenolic content expressed as mg Gallic acid equivalent (G.A.E.) per gram of extract was found to be 19,96 mgGAE/g of Epidendrum coryophorum. The ethanolic extract of Epidendrum coryophorum leaves showed hemolysis inhibition values ​​of 18,19% at 1,0 mg/mL, 38,98% at 1,5 mg/mL and 40,94% at 2,5 mg/mL compared with aspirin (positive control) giving values ​​of 65,33% at 1,0 mg/mL, 72,26% at 1,5 mg/mL and 73,75% at 2,5 mg/mL. The values ​​obtained for inhibition of hemolysis with ethanolic extract, compared with the values ​​obtained with a pure anti-inflammatory, are significant and demonstrate anti-inflammatory activity in Epidendrum coryophorum. Keywords: Epidendrum coryophorum, total phenolic content, microencapsulation, anti-inflammatory activity


Author(s):  
Jayashree V ◽  
Bagyalakshmi S ◽  
Manjula Devi K ◽  
Richard Daniel D

<p>ABSTRACT<br />Objective: To study the in vitro anti-inflammatory activity of 4-benzylpiperidine.<br />Methods: This study was conducted to evaluate the in vitro anti-inflammatory activity of 4-benzylpiperidine using in vitro models such as inhibition<br />of albumin denaturation and proteinase inhibitory activity.<br />Results: This study revealed the dose-dependent inhibition of protein denaturation and proteinase inhibitory activity by 4-benzylpiperidine.<br />Conclusion: In the present study, results indicate that the 4-benzylpiperidine possess anti-inflammatory properties. The drug inhibited the heat<br />induced albumin denaturation and proteinase inhibitory activity. It shows dose-dependent significant activity when compared with a standard drug.<br />Hence, this study gives an idea that the 4-benzylpiperidine can be used as a lead compound for designing a potent anti-inflammatory drug which can<br />be used to cure inflammation.<br />Keywords: Anti-inflammatory activity, 4-Benzylpiperidine, Protein denaturation, Proteinase inhibitory activity.</p>


2018 ◽  
Vol 8 (6-s) ◽  
pp. 174-181
Author(s):  
Valdi Steve Djova ◽  
Ascension Maximilienne Nyegue ◽  
François-Xavier Etoa

  Aqueous extract bark of Anthocleista schweinfurthii (ASE) was investigated for anti-arthritic, anti-inflammatory activities and phytochemicals screening. Phytochemical screening was carried out according, to LC-MS procedures, the anti-inflammatory effect of ASE was evaluated in vitro inhibition of 15-lipoxygenase (15-LOX) enzyme and  proteinase inhibiting action assays. The anti-arthritic activity was performed according to the Bovine Serum Albumin (BSA) test. The chemical composition of ASE showed that it was mainly composed of isocyanate, biphenyltriol, methoxyflavanone, soscoparin and glucopyroside. In the anti-inflammatory assays, ASE showed selective inhibition of 15-lipooxygenase with IC50 value of and moderate activity against the inhibition of proteinase action with IC50 value of L. Both the methods  showed that the ASE posses good anti-inflammatory activity. ASE had strong in vitro anti-arthritic activity with IC50 of , the positive control Diclofenac had IC50 value of  The result of this study justified the use of this plant in traditional Cameroonian medicine in the treatment of inflammation. ASE may offer a new source of potential therapeutic agents for the effective treatment of arthritis and inflammation.    Keywords: Anthocleista schweinfurthii, phytochemical screening, anti-arthritic activity, anti-inflammatory activity,     


2020 ◽  
Vol 11 (4) ◽  
pp. 7317-7322
Author(s):  
Sebastin V ◽  
Gopalakrishnan G ◽  
Sreejith M ◽  
Anoob Kumar K I

Plants of the genus Argyreia have ethnomedicinal importance, and several pharmacological activities are also reported. In this study, the anti-inflammatory activity of different extracts of Argyreia imbricata was evaluated by in vitro and in vivo methods. In both evaluations, standard, Diclofenac sodium was used for comparative evaluation. In this study, extraction of powdered whole plant material was done with different solvents viz., petroleum ether, chloroform, ethyl acetate and methanol by soxhelation. In vitro anti-inflammatory activity of all the prepared extracts was evaluated by stabilization of human red blood cell (HRBC) membrane in different temperature and tonicity conditions. Among the six different concentrations of four tested extracts, the ethyl acetate and methanol extracts (1000μg/ml) showed significant activity in the in vitro evaluation. They were selected for the in vivo evaluation on the paw oedema induced by carrageenan on Wistar albino rats. Two doses, 200mg.kg-1 and 400mg.kg-1 of the test extracts were subjected to evaluation. Both the tested extracts showed the activity, particularly, the methanol extract in the dose of 400mg.kg-1 showed significant activity. Results of this study strongly supported the anti-inflammatory activity of the tested extracts. Further, studies on toxicity, identification, isolation of the active constituents may give useful results.


2011 ◽  
Vol 6 (10) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Shivraj H. Nile ◽  
Chandrahasy N. Khobragade

The methanolic extract of Tephrosia purpurea (Leguminosae) shoots was evaluated in-vitro for its anti-inflammatory and xanthine oxidase inhibitory activity. Anti-inflammatory activity was measured by the Diene-conjugate, HET-CAM and β-glucuronidase methods. The enzyme inhibitory activity was tested against isolated cow milk xanthine oxidase. The average anti-inflammatory activity of T. purpurea shoot extract in the concentration range of 1-2 μg/mL in the reacting system revealed significant anti-inflammatory activities, which, as recorded by the Diene-conjugate, HET-CAM and β-glucuronidase assay methods, were 45.4, 10.5, and 70.5%, respectively. Screening of the xanthine oxidase inhibitory activity of the extract in terms of kinetic parameters revealed a mixed type of inhibition, wherein the Km and Vmax values in the presence of 25 to 100 μg/mL shoot extract was 0.20 mM/mL and 0.035, 0.026, 0.023 and 0.020 μg/min, while, for the positive control, the Km and Vmax values were 0.21 mM/mL and 0.043 μg/min, respectively. These findings suggest that T. purpurea shoot extract may possess constituents with good medicinal properties that could be exploited to treat the diseases associated with oxidative stress, xanthine oxidase enzyme activity and inflammation.


2011 ◽  
Vol 138-139 ◽  
pp. 1174-1178
Author(s):  
Li Ming Bai ◽  
Fan Xu Meng ◽  
Li Jie Zhao ◽  
Ming Zhao

The Anti-inflammatory activity of pentacyclic triterpenes, oleananes (1,2), urasanes (3-11), lupanes (12,13), taraxasteranes (14,15), which isolated from Nerium oleander L, were examined. Ursolic acid (5) showed significant activity and compounds (1, 12) and (14) showed weak to modelate activity toward inhibitory activity on ICAM-1 expression.


2020 ◽  
Vol 21 (2) ◽  
pp. 149-157
Author(s):  
Zahra Iqbal ◽  
Ausaf Ahmad ◽  
Ziyaul Haque ◽  
Mohammed S. Khan ◽  
Mohd S. Khan ◽  
...  

Background: Flavonol derivative and phenolic acids derived from the plants function as free radical scavengers, reducing agents, and quenchers for the formation of singlet oxygen. Flavonoids and phenolic constituents also play an important role in various human diseases and disorders primarily through modulation of inflammatory responses. Objective: To estimate the Flavonol Derivatives (FD) and phenolic acids (PA) in Capsicum annuum (CA) and other important phytochemicals having an anti-inflammatory effect. Method: In the present study, FD and PA were estimated in CA and in vitro anti-inflammatory activity (pilot study) was determined and correlation was established. Results: The results were found to be significant using RP-HPLC. FD and PA were found to be 0.0659±0.0058 and 0.0862±0.0.0134 mg/gram dry weight, respectively. For in vitro anti-inflammatory activity, the inhibition of albumin denaturation and antiproteinase activity was found to be maximum in Quercetin (QE) with 98.230±1.589% and 59.906±1.529%, respectively. Heat-induced hemolysis of erythrocytes was found to be maximum in salicylic acid (SA) (71.830±2.838%). Hypotonicity-induced hemolysis showed significant activity with QE (76.770±3.475%). Lipoxygenase and cyclooxygenase inhibition was found to be maximum in QE with 56.930±4.069% and 61.660±3.135%, respectively. Conclusion: A strong positive correlation of 0.9 was observed between the extract of CA and standard QE and SA against the anti-inflammatory activity. Therefore, the role of FD and PA has been postulated to be an active phytochemical of CA accountable for its anti-inflammatory activity. However further work is desirable to fully elucidate the phytochemicals responsible for their anti-inflammatory activity and to develop better herbal drug formulations.


Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1323 ◽  
Author(s):  
Maria Stefania Lepanto ◽  
Luigi Rosa ◽  
Rosalba Paesano ◽  
Piera Valenti ◽  
Antimo Cutone

Lactoferrin (Lf), a cationic glycoprotein able to chelate two ferric irons per molecule, is synthesized by exocrine glands and neutrophils. Since the first anti-microbial function attributed to Lf, several activities have been discovered, including the relevant anti-inflammatory one, especially associated to the down-regulation of pro-inflammatory cytokines, as IL-6. As high levels of IL-6 are involved in iron homeostasis disorders, Lf is emerging as a potent regulator of iron and inflammatory homeostasis. Here, the role of Lf against aseptic and septic inflammation has been reviewed. In particular, in the context of aseptic inflammation, as anemia of inflammation, preterm delivery, Alzheimer’s disease and type 2 diabetes, Lf administration reduces local and/or systemic inflammation. Moreover, Lf oral administration, by decreasing serum IL-6, reverts iron homeostasis disorders. Regarding septic inflammation occurring in Chlamydia trachomatis infection, cystic fibrosis and inflammatory bowel disease, Lf, besides the anti-inflammatory activity, exerts a significant activity against bacterial adhesion, invasion and colonization. Lastly, a critical analysis of literature in vitro data reporting contradictory results on the Lf role in inflammatory processes, ranging from pro- to anti-inflammatory activity, highlighted that they depend on cell models, cell metabolic status, stimulatory or infecting agents as well as on Lf iron saturation degree, integrity and purity.


2008 ◽  
Vol 3 (10) ◽  
pp. 1934578X0800301 ◽  
Author(s):  
Emrizal ◽  
Farediah Ahmad ◽  
Hasnah M. Sirat ◽  
Fadzureena Jamaludin ◽  
Nik Musa'adah Mustapha ◽  
...  

Anti-inflammatory activity of a crude extract of Piper magnibaccum (Piperaceae) and of compounds isolated from it was established using the TPA-induced mouse ear edema model and an in vitro quantitative lipoxygenase inhibition assay. Five compounds were isolated from P. magnibaccum [β-sitosterol, N-isobutyl-(2 E,4 E)-tetradecadienamide, linoleic acid, 13-(4′, 5′-dimethoxytridecanoyl)piperidine, and piperine]. The light petroleum extract of the plant exhibited significant anti-inflammatory activity in both models. N-isobutyl-(2 E,4 E)-tetradecadienamide showed significant activity, with an IE % value of 70.2 + 5.4 in the TPA-induced mouse ear edema model and 87.2 + 0.11 in the in vitro quantitative lipoxygenase inhibition assay.


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