The acute anti-inflammatory action of xylopic acid isolated from Xylopia aethiopica

2018 ◽  
Vol 29 (6) ◽  
pp. 659-669 ◽  
Author(s):  
Newman Osafo ◽  
David D. Obiri ◽  
Aaron O. Antwi ◽  
Oduro K. Yeboah
Keyword(s):  
Acute Inflammation ◽  
Protein Denaturation ◽  
Prostaglandin E ◽  
Paw Oedema ◽  
Dependent Inhibition ◽  
Dried Fruit ◽  
Anti Inflammatory ◽  
Xylopia Aethiopica ◽  
Inflammatory Action

AbstractBackgroundOur earlier studies had given evidence of the traditional application ofXylopia aethiopicain the management of inflammation. The principal constituent obtained from its bio-fractionation is xylopic acid. It is a crystalline diterpene that belongs to the class of kauranes. This work sets out to investigate the anti-inflammatory potential of the xylopic acid isolated from the dried fruit ofX. aethiopica.MethodsA preliminary anti-inflammatory study, using the protein denaturation model, andin vivoanti-inflammatory assay were employed in the investigation of acute inflammation. The modulation of the effect of the pro-inflammatory markers histamine, serotonin, bradykinin, and prostaglandin E2by xylopic acid was investigated byin vivomice paw oedema models.ResultsXylopic acid showed a concentration-dependent inhibition of albumen denaturation with an IC50of 15.55 μg mL−1. Xylopic acid (10, 30, 100 mg kg−1) inhibited the maximal oedema and the average paw thickness (oedema) over the period of each study considerably for all phlogistic agents employed (i.e. carrageenan, histamine, serotonin, bradykinin, and prostaglandin E2) in the inflammation induction for both prophylactic and therapeutic protocols.ConclusionThis study establishes that xylopic acid has anti-inflammatory action in acute inflammation.

Fibrinolytic, Anti-Inflammatory and Cytotoxic Potentialities of Extracts and Chemical Constituents of Manglicolous Lichen, Graphis ajarekarii Patw. & C. R. Kulk

2020 ◽  
Vol 10 (1) ◽  
pp. 87-93 ◽  
Author(s):  
Vinay Bharadwaj Tatipamula ◽  
Girija Sastry Vedula
Keyword(s):  
Protein Denaturation ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Fibrin Clot ◽  
Hydroalcoholic Extract ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Background: Lichens which are betide to mangroves are termed as Manglicolous Lichens (ML). As these ML are habituated under stress conditions, they are screened for unique metabolites and biological activities. Objective: The study aimed to establish the chemical and biological profile of ML, Graphis ajarekarii. Methods: The Ethyl Acetate Extract of G. ajarekarii (EAE) was subjected to chromatographic techniques and the obtained isolates were characterized by spectroscopic analysis. The hydroalcoholic extract of G. ajarekarii (AE), EAE, isolates and Hydroalcoholic Extract of host (HE) were evaluated for fibrinolytic (fibrin clot method), in vitro (protein denaturation method) and in vivo (formalin-induced rat paw oedema assay), anti-inflammatory and cytotoxicity (MTT assay) activities. Results: Chemical investigation of the EAE led to the isolation of two known compounds namely atranorin (1) and ribenone (2), which were confirmed by spectral data. The AE and EAE gradually lysed the fibrin clot with 94.54 and 65.07%, respectively, at 24 h. The AE inhibited protein denaturation of about 88.06%, while the standard (Indomethacin) with 93.62%. Similarly, the in vivo antiinflammatory analysis of AE (200 mg/mL) showed potent reduction of rat paw oedema than the standard, whereas EAE and 1 depicted moderate depletion. In addition, the AE revealed prominence inhibition on MCF-7, DU145 and K-562 with IC50 values of 69.5, 42.5 and 38 µg/mL, respectively, whereas the HE exhibited mild inhibitory profile against fibrin clot, inflammation and cancer. Conclusion: From the results, it can be concluded that the G. ajarekarii has an aptitude to act against coagulation, inflammation and cancer cells.

scholarly journals Anti-Inflammatory Effects of 3-Formyl, 7-Flavonols Derivatives by Microwave Enhanced Chemistry Assisted - Vilsmeier Haack Synthesis

2019 ◽  
Vol 12 (04) ◽  
pp. 1779-1791
Author(s):  
M. Karpakavalli ◽  
A.Y. Sangilimuthu ◽  
A.Usha Raja Nanthini ◽  
G.Nagaraja Perumal ◽  
S. Mohan ◽  
...  
Keyword(s):  
Protein Denaturation ◽  
Population Increase ◽  
Spectral Studies ◽  
Dimethyl Formamide ◽  
Mass Spectral ◽  
Paw Oedema ◽  
Rf Values ◽  
Anti Inflammatory

In the modern medicines the novel and active molecules are essential to act against various diseases and increase the needs day by day due to population increase. In view of that, we attempt to make a variety of synthetic molecules against inflammation by a new and popular greener microwave assisted and faster method such as Microwave Enhanced Chemistry assisted Vilsmeier Haack Synthesis (MEC-VHS). In this paper, we report the synthesis of nitro- dinitro- and acetyl- derivatives of 3- formyl, 7-flavonols using MEC-VHS techniques against inflammation as anti-inflammatory agent. These derivatives were synthesized via pinkish formylation complex of dimethyl formamide and phosphorous oxychloride by microwave irradiation resulted as suspension by base. The re-crystallized products were characterized through Co-TLC, λmax, IR, HPTLC, 1HNMR, CHN analysis and mass spectral studies. The HPTLC finger print profiles obtained were of with a prominent single peak and with a matching Rf values compared to that obtained by an ordinary Co-TLC technique. All the synthesized compounds were screened for their anti-inflammatory activity by in vitro protein denaturation method and in vivo carrageenan induced paw oedema method and it was found that all the compounds excepting the un-substituted 3-formyl, 7-flavonols gave an equi- or more potent activity as compared to that of the standard.

scholarly journals EVALUATION OF EFFECT OF AQUEOUS EXTRACT OF PORTULACA OLERACEA LINN. LEAVES IN ACUTE INFLAMMATION

2020 ◽  
pp. 1-2
Author(s):  
M. Medhabati ◽  
L. Babycha ◽  
L. Tarinita ◽  
Bikram Tewari ◽  
Saumya Kanti Sinha
Keyword(s):  
Aqueous Extract ◽  
Acute Inflammation ◽  
Portulaca Oleracea ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Standard Drug ◽  
Paw Oedema ◽  
The Mean ◽  
Anti Inflammatory ◽  
Inflammatory Action

In the present study, the anti-inflammatory activity of aqueous extract of Portulaca oleracea (POE 200, 400 and 600mg/kg) was studied using carrageenan induced paw oedema in albino rats. The mean increase in paw volume was recorded. POE produced significant (p<,0.01) anti-inflammatory activity when compared to the control. The anti-inflammatory action of POEcan be attributed to its flavonoid contents which are known to act through inhibition of prostaglandin biosynthesis. However, the test drug at maximum dose (600mg/kg) was found to be less effective than the standard drug, aspirin (100mg/Kg).

scholarly journals Annexin I and dexamethasone effects on phospholipase and cyclooxygenase activity in human synoviocytes

2000 ◽  
Vol 9 (3-4) ◽  
pp. 125-132 ◽  
Author(s):  
Annaleise V. Sampey ◽  
Paul Hutchinson ◽  
Eric F. Morand
Keyword(s):  
Flow Cytometry ◽  
Arachidonic Acid ◽  
Binding Sites ◽  
Prostaglandin E ◽  
Annexin I ◽  
Dependent Inhibition ◽  
Anti Inflammatory ◽  
Rate Limiting ◽  
Cox2 Expression

Annexin I is a glucocorticoid-induced mediator with anti-inflammatory activity in animal models of arthritis. We studied the effects of a bioactive annexin I peptide, ac 2–26, dexamethasone (DEX), and interleukin-1β (IL-1β) on phospholipase A2(PLA2) and cyclooxygenase (COX) activities and prostaglandin E2(PGE2) release in cultured human fibroblast-like synoviocytes (FLS). Annexin I binding sites on human osteoarthritic (OA) FLS were detected by ligand binding flow cytometry. PLA2activity was measured using3H-arachidonic acid release, PGE2release and COX activity by ELISA, and COX2 content by flow cytometry. Annexin I binding sites were present on human OA FLS. Annexin I peptide ac 2–26 exerted a significant concentration-dependent inhibition of FLS constitutive PLA2activity, which was reversed by IL-1β. In contrast, DEX inhibited IL-1β-induced PLA2activity but not constitutive activity. DEX but not annexin I peptide inhibited IL-1β-induced PGE2release. COX activity and COX2 expression were significantly increased by IL-1β. Annexin I peptide demonstrated no inhibition of constitutive or IL-1β-induced COX activity. DEX exerted a concentration-dependent inhibition of IL-1β-induced but not constitutive COX activity. Uncoupling of inhibition of PLA2and COX by annexin I and DEX support the hypothesis that COX is rate-limiting for PGE2synthesis in FLS. The effect of annexin I but not DEX on constitutive PLA2activity suggests a glucocorticoid-independent role for annexin I in autoregulation of arachidonic acid production. The lack of effect of annexin I on cytokine-induced PGE2production suggests PGE2-independent mechanisms for the anti-inflammatory effects of annexin Iin vivo.

scholarly journals Kinetic Study of the Hydrolysis of synthesized Ibuprofen Ester and its Biological Activity

2013 ◽  
Vol 10 (3) ◽  
pp. 1062-1070
Author(s):  
Baghdad Science Journal
Keyword(s):  
Side Effect ◽  
Effect Study ◽  
Reference Drug ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
The Stability ◽  
Kinetic Hydrolysis ◽  
Hydrolysis Of ◽  
Inflammatory Action

It is known that the oral administration of ibuprofen caused an irritation of stomach as a side effect due to its carboxylic moiety. Ibuprofen ester was synthesized by linking the carboxylic moiety of ibuprofen and the hydroxylic group of paracetamol to reduce its side effect. Study the kinetic hydrolysis of prepared ester was examined at different values of physiological pH (1.0, 5.8, 6.4 and 7.4) at 37 ± 0.1 of 1 hour period. Measurements of absorbance were carried out by UV-Visible spectrophotometer to follow the stability of ester, it showed Pseudo first order hydrolysis. The pH- apparent rate profiles of ester was exhibited a good stability at pH 1.0 and pH 5.8. Pharmacological activity in vivo of prepared ester was evaluated in relation to analgesic and anti-inflammatory activity using the acetic acid method and the hind paw oedema inhibition, respectively. Acetyl salicylic acid (aspirin) was used as a reference drug for the above tests. The synthesized ester showed higher analgesic and anti-inflammatory action than aspirin.

scholarly journals Anti-inflammatory properties of Dirinaria consimilis extracts in albino rats

2018 ◽  
Vol 4 (1) ◽  
pp. 3-8 ◽  
Author(s):  
Vinay Bharadwaj Tatipamula ◽  
Girija Sastry Vedula
Keyword(s):  
Protein Denaturation ◽  
Chloroform Extract ◽  
Acetone Extract ◽  
Albino Rats ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

BackgroundEarlier, the lichens are used in traditional medicines by different cultures across the world. As the Dirinaria genus has been shown to be biologically active against inflammation in folklore, we assessed the in vitro and in vivo anti-inflammatory profile of Dirinaria consimilis.Material and methodsInitially, the hydroalcoholic extract of lichen, D. consimilis (Dc-HE) was prepared and re-extracted with n-hexane, chloroform, ethyl acetate, acetone and methanol. The resultant extracts were evaluated for their in vitro (protein denaturation method), acute toxicity and in vivo (formalin-induced rat paw oedema assay) anti-inflammatory studies.ResultsAmong all the tested extracts, the acetone and chloroform extract of D. consimilis depicted prominent anti-inflammatory activity in both the bioassays. The acetone extract inhibited protein denaturation with IC50 value of about 468 µg/mL while the standard (Indomethacin) with 120 µg/mL. Moreover, the Dc-HE was screened for acute toxicity studies in male albino rats up to 2000 mg/Kg b.w dosage. The in vivo anti-inflammatory analysis of acetone extract (200 mg/mL) showed potent reduction of rat paw oedema nearer to that of the standard, whereas chloroform extract depicted moderate depletion and the other extracts revealed mild inhibitory profile against inflammation.ConclusionThis study reveals that the lichen, D. consimilis might be a good source of anti-inflammatory agents.

scholarly journals ANTI-INFLAMMATORY EFFECTS OF PROPOXAZEPAM ON DIFFERENT MODELS OF INFLAMMATION

2020 ◽  
Vol 5 (2) ◽  
pp. 105-112 ◽  
Author(s):  
N. Ya. Golovenko ◽  
T. A. Kabanova ◽  
S. A. Andronati ◽  
O. I. Halimova ◽  
V. B. Larionov ◽  
...  
Keyword(s):  
Acute Inflammation ◽  
Experimental Models ◽  
Paw Edema ◽  
Preclinical Trial ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
First Time ◽  
Inflammatory Action

Background. Propoxazepam, 7-bromo-5-(2-chlorophenyl)-3-propoxy-1H-benzo[e][1,4]diazepin-2(3H)-one, is a promising analgesic and anticonvulsant and is on preclinical trial. Objective. The aim of the research was to study the anti-inflammatory and analgesic action of Propoxazepam. Methods. The anti-inflammatory action was evaluated by carrageenan induced rat paw edema, formalin-induced paw licking response in mice and bradykinin-induced pain response in rat models. Results. It was established for the first time that the administration of Propoxazepam caused a significant anti-inflammatory activity when tested in different in vivo chemical experimental models of induced inflammation, i.e. carrageenan-, bradykinin- and formalin-induced inflammation tests. Conclusions. Propoxazepam significantly reduced acute and sub-acute inflammation and proved its efficacy and similar to anti-inflammatory action.

scholarly journals Unravelling the Biological Activities of the Byttneria pilosa Leaves Using Experimental and Computational Approaches

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4737
Author(s):  
Mifta Ahmed Jyoti ◽  
Niloy Barua ◽  
Mohammad Shafaet Hossain ◽  
Muminul Hoque ◽  
Tahmina Akter Bristy ◽  
...  
Keyword(s):  
Protein Denaturation ◽  
Biological Activities ◽  
Significant Inhibition ◽  
Biologically Active ◽  
Dependent Inhibition ◽  
Anti Inflammatory ◽  
Isolated Compound ◽  
Dose Dependent

Byttneria pilosa is locally known as Harijora, and used by the native hill-tract people of Bangladesh for the treatment of rheumatalgia, snake bite, syphilis, fractured bones, elephantiasis and an antidote for poisoning. The present study was carried out to determine the possible anti-inflammatory, analgesic, neuropharmacological and anti-diarrhoeal activity of the methanol extract of B. pilosa leaves (MEBPL) through in vitro, in vivo and in silico approaches. In the anti-inflammatory study, evaluated by membrane stabilizing and protein denaturation methods, MEBPL showed a significant and dose dependent inhibition. The analgesic effect of MEBPL tested by inducing acetic acid and formalin revealed significant inhibition of pain in both tests. During the anxiolytic evaluation, the extract exhibited a significant and dose-dependent reduction of anxiety-like behaviour in mice. Similarly, mice treated with MEBPL demonstrated dose-dependent reduction in locomotion effect in the open field test and increased sedative effect in the thiopental sodium induced sleeping test. MEBPL also showed good anti-diarrheal activity in both castor oil induced diarrheal and intestinal motility tests. Besides, a previously isolated compound (beta-sitosterol) exhibited good binding affinity in docking and drug-likeliness properties in ADME/T studies. Overall, B. pilosa is a biologically active plant and could be a potential source of drug leads, which warrants further advanced study.

scholarly journals Dangguijakyak-San Protects against 1-Methyl-4-phenyl-1,2,3,6,-tetrahydropyridine-Induced Neuronal Damage via Anti-Inflammatory Action

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Deok-Sang Hwang ◽  
Hyo Geun Kim ◽  
Jun-Bock Jang ◽  
Myung Sook Oh
Keyword(s):  
Neuronal Damage ◽  
Cell Damage ◽  
Substantia Nigra Pars Compacta ◽  
Inflammatory Factors ◽  
Dopaminergic Cell ◽  
Therapeutic Implications ◽  
Anti Inflammatory ◽  
Inflammatory Action

Dangguijakyak-san (DJS), a famous traditional Korean multiherbal medicine, has been used to treat gynecological and neuro-associated disease. Recent studies demonstrated that DJS has multiple bioactivities including neuroprotection. In the present study, we were to investigate the effect of DJS and its mechanism in anin vitroandin vivomodel of Parkinson’s disease (PD). In primary mesencephalic culture system, DJS attenuated the dopaminergic cell damage induced by 1-methyl-4-phenylpyridine toxicity, and it inhibited production of inflammatory factors such as tumor necrosis factorα(TNF-α), nitric oxide (NO), and activation of microglial cells. Then, we confirmed the effect of DJS in a mouse PD model induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). In the pole test, DJS at 50 mg/kg/day for 5 days showed increase of motor activity showing shortened time to turn and locomotor activity compared with the MPTP only treated mice. In addition, DJS significantly protected nigrostriatal dopaminergic neuron from MPTP stress. Moreover, DJS showed inhibition of gliosis in the substantia nigra pars compacta. These results have therapeutic implications for DJS in the treatment of PD via anti-inflammatory effects.

scholarly journals Hydro ethanol extract of Holarrhena floribunda stem bark exhibits anti-anaphylactic and anti-oedematogenic effects in murine models of acute inflammation

2020 ◽  
Author(s):  
Stephen Antwi ◽  
Daniel Oduro-Mensah ◽  
David Darko Obiri ◽  
Newman Osafo ◽  
Aaron Opoku Antwi ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Serotonin Receptor ◽  
Acute Inflammation ◽  
Late Phase ◽  
Ethanol Extract ◽  
Stem Bark ◽  
Bark Extract ◽  
Prostaglandin E ◽  
Sprague Dawley ◽  
Anti Inflammatory

Abstract Background: Holarrhena floribunda stem bark has anecdotal use in Ghanaian folk medicine for management of inflammatory conditions. This study was conducted to investigate the in vivo anti-inflammatory activity of the bark extract using models of acute inflammation in male Sprague Dawley rats, C57BL/6 mice and 36 ICR mice. Methods: A 70 % hydro-ethanol extract of the stem bark (HFE) was evaluated at doses of 5–500 mg/kg bw. Local anaphylaxis was modelled by the pinnal cutaneous anaphylactic test. Systemic anaphylaxis or sepsis were modeled by compound 48/80 or lipopolysaccharide, respectively. Clonidine-induced catalepsy was used to investigate effect on histamine signaling. Anti-oedematogenic effect was assessed by induction with carrageenan. Effects on mediators of biphasic acute inflammation were studied using histamine and serotonin (early phase) or prostaglandin E2 (late phase).Results: HFE demonstrated anti-inflammatory and/or anti-oedematogenic activity comparable to standard doses of aspirin and diclofenac (inhibitors of cyclooxygenases-1 and -2), chlorpheniramine (histamine H1-receptor antagonist), dexamethasone (glucocorticoid receptor agonist), granisetron (serotonin receptor antagonist) and sodium cromoglycate (inhibitor of mast cell degranulation). All observed HFE bioactivities increased with dose.Conclusions: The data provide evidence that the extract of H. floribunda stem bark has anti-anaphylactic and anti-oedematogenic effects; by interfering with signalling or metabolism of histamine, serotonin and prostaglandin E2 which mediate progression of inflammation. The anti-inflammatory and antihistaminic activities of HFE may be relevant in the context of management of COVID-19.

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