Potent Anti-inflammatory Compound Research Articles

Evolution of selective COX-2 inhibitor from Alangium salvifolium: an in silico approach

Pain and inflammation are linked with a number of pathological conditions. Several studies are in progress worldwide to find natural healing agents with better safety profile. Our current study is aimed to evaluate Alangium salvifolium (family: Alangeaceae) derived analgesic compounds for therapeutic drug discovery by computational approach. Literature based studies are used to explore the compounds of A. salvifolium. Ligands are prepared by following the appropriate procedures and finally in silico molecular docking analysis performed by GOLD 4.2. After post docking analysis salviifosides A of Alangium salvifolium is found to have interaction on COX-2 protein by obtaining highest fitness score 50.64 and molecular interaction suggests that it could be a potent anti-inflammatory compound and it may be worth for further clinical trials.

Anti-inflammatory properties of the medicinal mushroom Cordyceps militaris might be related to its linear (1→3)-β-D-glucan.

The Ascomycete Cordyceps militaris, an entomopathogenic fungus, is one of the most important traditional Chinese medicines. Studies related to its pharmacological properties suggest that this mushroom can exert interesting biological activities. Aqueous (CW and HW) and alkaline (K5) extracts containing polysaccharides were prepared from this mushroom, and a β-D-glucan was purified. This polymer was analysed by GC-MS and NMR spectrometry, showing a linear chain composed of β-D-Glcp (1→3)-linked. The six main signals in the 13C-NMR spectrum were assigned by comparison to reported data. The aqueous (CW, HW) extracts stimulated the expression of IL-1β, TNF-α, and COX-2 by THP-1 macrophages, while the alkaline (K5) extract did not show any effect. However, when the extracts were added to the cells in the presence of LPS, K5 showed the highest inhibition of the pro-inflammatory genes expression. This inhibitory effect was also observed for the purified β-(1→3)-D-glucan, that seems to be the most potent anti-inflammatory compound present in the polysaccharide extracts of C. militaris. In vivo, β-(1→3)-D-glucan also inhibited significantly the inflammatory phase of formalin-induced nociceptive response, and, in addition, it reduced the migration of total leukocytes but not the neutrophils induced by LPS. In conclusion, this study clearly demonstrates the anti-inflammatory effect of β-(1→3)-D-glucan.

Gold(I) complexes of 9-deazahypoxanthine as selective antitumor and anti-inflammatory agents.

The gold(I) mixed-ligand complexes involving O-substituted derivatives of 9-deazahypoxanthine (HLn) and triphenylphosphine (PPh3) with the general formula [Au(Ln)(PPh3)] (1–5) were prepared and thoroughly characterized by elemental analysis, FT-IR and multinuclear NMR spectroscopy, ESI+ mass spectrometry, single crystal X-ray (HL5 and complex 2) and TG/DTA analyses. Complexes 1–5 were evaluated for their in vitro antitumor activity against nine human cancer lines, i.e. MCF7 (breast carcinoma), HOS (osteosarcoma), A549 (adenocarcinoma), G361 (melanoma), HeLa (cervical cancer), A2780 (ovarian carcinoma), A2780R (ovarian carcinoma resistant to cisplatin), 22Rv1 (prostate cancer) and THP-1 (monocytic leukaemia), for their in vitro anti-inflammatory activity using a model of LPS-activated macrophages, and for their in vivo antiedematous activity by λ-carrageenan-induced hind paw edema model on rats. The results showed that the complexes 1–5 exhibit selective in vitro cytotoxicity against MCF7, HOS, 22Rv1, A2780 and A2780R, with submicromolar IC50 values for 2 against the MCF7 (0.6 µM) and HOS (0.9 µM). The results of in vitro cytotoxicity screening on primary culture of human hepatocytes (HEP220) revealed up to 30-times lower toxicity of compounds against healthy cells as compared with cancer cells. Additionally, the complexes 1–5 significantly influence the secretion and expression of pro-inflammatory cytokines TNF-α and IL-1β by a similar manner as a commercially used anti-arthritic drug Auranofin. The tested complexes also significantly influence the rate and overall volume of the edema, caused by the intraplantar application of λ-carrageenan polysaccharide to rats. Based on these promising results, the presented compounds could qualify to become feasible candidates for advanced testing as potential antitumor and anti-inflammatory drug-like compounds.

Anti-inflammatory activity of methyl ferulate isolated from Stemona tuberosa Lour

ObjectiveTo evaluate the anti-inflammatory activity of methyl ferulate (MF) isolated from the roots of Stemona tuberosa (S. tuberosa) Lour (Stemonaceae) in lipopolysaccharide activated macrophage cells. MethodsMethanol extracts of a root powder of S. tuberosa were prepared for isolation of a potential anti-inflammatory agent using ultrasound extraction combined with repeated chromatography on silica gel. After the quantitative analyses, anti-inflammatory activity of the isolated compound was evaluated by measurement of cytokine release, NO generation, expression of cyclooxygenase-2 and phosphorylation of mitogen activated protein kinases including p38 and c-Jun NH2-terminal kinase using quantitative kits and Western blotting with specific antibodies. ResultsThe isolation process yielded a potential anti-inflammatory compound with a purity level of 99% determined by high performance liquid chromatography. The compound was identified as MF by using nuclear magnetic resonance. MF strongly inhibited the release of pro-inflammatory cytokines from macrophages, including IL-6, TNFα, IFNγ, yet it did not affect the anti-inflammatory cytokine IL-10. Phosphorylation of p38 and c-Jun NH2-terminal kinase were clearly reduced in MF-treated macrophages stimulated with lipopolysaccharide. cyclooxygenase-2 expression and NO generation by macrophages were also suppressed when the cells were treated with MF. ConclusionsThe data suggested that MF is a possible inhibitor of the mitogen activated phosphor kinase pathway and could be a potential anti-inflammatory agent isolated for the first time in medicinal plant S. tuberosa.

1,8-Naphthyridines IX. Potent anti-inflammatory and/or analgesic activity of a new group of substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides, of some their Mannich base derivatives and of one novel substituted 5-amino-10-oxo-10H-pyrimido[1,2-a][1,8]naphthyridine-6-carboxamide derivative

A new group of 5-(alkylamino)-9-isopropyl[1,2,4]triazolo[4,3-a][1,8]naphthyridine derivatives bearing a CONHR group at the 6-position (1c–g), designed to obtain new effective analgesic and/or anti-inflammatory agents, were synthesized and tested along with three new 9-alkyl-5-(4-alkyl-1-piperazinyl)-N,N-diethyl [1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides (2b–d). Besides, a new class of analogues of compounds 1 and 2, bearing a Mannich base moiety at the 9-position (12a–d), as well as the novel N,N-diethyl-5-(isobutylamino)-8-methyl-10-oxo-10H-pyrimido[1,2-a][1,8]naphthyridine-6-carboxamide (15) were prepared and tested. Compounds 1c–g exhibited very interesting anti-inflammatory properties in rats, whereas compounds 2b–d and 15 proved to be endowed with prevalent analgesic activity frequently associated with sedative effects in mice. On the contrary, the Mannich bases 12a–d resulted inactive. The most effective (80% inhibition of oedema) and potent (threshold dose 1.6 mg kg−1 with 31% inhibition of oedema) anti-inflammatory compound 1d did not show gastrolesive effects following 100 mg kg−1 oral administration in rats.

Indole-3-ethylsulfamoylphenylacrylamides: Potent histone deacetylase inhibitors with anti-inflammatory activity

A series of 2-methyl-1H-indol-3-ethylsulfamoylphenylacrylamides based on LBH589–PXD101 core have been synthesized and evaluated for their histone deacetylase (HDAC) inhibitory and anti-inflammatory activity. In vitro, compounds 9–12 show 2.6-fold better HDAC inhibition and 3-fold better IL-6 suppression compared to LBH589·HCl (1·HCl). Furthermore, these compounds did not show apparent cell viability suppression on macrophages while in contrast, treatment with 1·HCl resulted in significant reduction in cell viability as demonstrated by an MTT assay. Repressed expression of iNOS, COX-2 and reduced phosphorylation of p65 revealed the inhibitory effect of these analogues on inflammatory mediator release which is related to inhibited NF-ĸB signals. (N-Hydroxy-3-{3-[2-(2-methyl-1H-indol-3-yl)-ethylsulfamoyl]-phenyl}-acrylamide) (9), exhibited ability superior to that of 1·HCl, was able to reduce carrageenan-induced acute inflammation in an animal model. Compounds 9–12 have potential anti-inflammatory activity and compound 9 can serve as lead compound for further development.

Synthesis and evaluation of a series of novel asymmetrical curcumin analogs for the treatment of inflammation.

Curcumin has been reported to possess multiple bioactivities, such as antioxidant, anticancer, and anti-inflammatory properties, however the clinical application of curcumin has been significantly limited by its instability and poor metabolism. Modification of curcumin has led to discovery and development of lots of novel therapeutic candidates. In recent years acute and chronic inflammation has been the focus of numerous studies in various diseases. Here, we synthesized a series of asymmetrical curcumin analogs with high in vitro chemical stability, and their anti-inflammatory activity was evaluated in LPS-stimulated macrophages. According to the bio-screening results and QSAR analysis, these analogs exhibited potent activities against LPS-induced TNF-α and IL-6 release. Among the analogs of the potent anti-inflammatory activity, compounds 3b8 and 3b9 exhibited significant protection and possess enhanced anti-inflammatory activity thereby attenuated the LPS-induced septic death in mice.

Chrysin, an anti-inflammatory molecule, abrogates renal dysfunction in type 2 diabetic rats

Diabetic nepropathy (DN) is considered as the leading cause of end-stage renal disease (ESRD) worldwide, but the current available treatments are limited. Recent experimental evidences support the role of chronic microinflammation in the development of DN. Therefore, the tumor necrosis factor-alpha (TNF-α) pathway has emerged as a new therapeutic target for the treatment of DN. We investigated the nephroprotective effects of chrysin (5, 7-dihydroxyflavone) in a high fat diet/streptozotocin (HFD/STZ)-induced type 2 diabetic Wistar albino rat model. Chrysin is a potent anti-inflammatory compound that is abundantly found in plant extracts, honey and bee propolis. The treatment with chrysin for 16weeks post induction of diabetes significantly abrogated renal dysfunction and oxidative stress. Chrysin treatment considerably reduced renal TNF-α expression and inhibited the nuclear transcription factor-kappa B (NF-кB) activation. Furthermore, chrysin treatment improved renal pathology and suppressed transforming growth factor-beta (TGF-β), fibronectin and collagen-IV protein expressions in renal tissues. Chrysin also significantly reduced the serum levels of pro-inflammatory cytokines, interleukin-1beta (IL-1β) and IL-6. Moreover, there were no appreciable differences in fasting blood glucose and serum insulin levels between the chrysin treated groups compared to the HFD/STZ-treated group. Hence, our results suggest that chrysin prevents the development of DN in HFD/STZ-induced type 2 diabetic rats through anti-inflammatory effects in the kidney by specifically targeting the TNF-α pathway.

Polymorphic Signature of the Anti-inflammatory Activity of 2,2′-{[1,2-Phenylenebis(methylene)]bis(sulfanediyl)}bis(4,6-dimethylnicotinonitrile)

Weak noncovalent interactions are the basic forces in crystal engineering. Polymorphism in flexible molecules is very common, leading to the development of the crystals of same organic compounds with different medicinal and material properties. Crystallization of 2,2′-{[1,2-phenylenebis(methylene)]bis(sulfanediyl)}bis(4,6-dimethylnicotinonitrile) by evaporation at room temperature from ethyl acetate and hexane and from methanol and ethyl acetate gave stable polymorphs 4a and 4b, respectively, while in acetic acid, it gave metastable polymorph 4c. The polymorphic behavior of the compound has been visualized through single-crystal X-ray and Hirshfeld analysis. These polymorphs are tested for anti-inflammatory activity via the complete Freund’s adjuvant-induced rat paw model, and compounds have exhibited moderate activities. Studies of docking in the catalytic site of cyclooxygenase-2 were used to identify potential anti-inflammatory lead compounds. These results suggest that the supramolecular aggregate str...

A randomized double blind, placebo controlled phase 2 trial of BIIL 284 BS (an LTB4 receptor antagonist) for the treatment of lung disease in children and adults with cystic fibrosis

Airway inflammation, mediated in part by LTB4, contributes to lung destruction in patients with cystic fibrosis (CF). LTB(4)-receptor inhibition may reduce airway inflammation. We report the results of a randomized, double-blind, placebo-controlled study of the efficacy and safety of the leukotriene B(4) (LTB(4))-receptor antagonist BIIL 284 BS in CF patients. CF patients aged ≥6 years with mild to moderate lung disease were randomized to oral BIIL 284 BS or placebo once daily for 24 weeks. Co-primary endpoints were change in FEV(1) and incidence of pulmonary exacerbation. After 420 (155 children, 265 adults) of the planned 600 patients were randomized, the trial was terminated after a planned interim analysis revealed a significant increase in pulmonary related serious adverse events (SAEs) in adults receiving BIIL 284 BS. Final analysis revealed SAEs in 36.1% of adults receiving BIIL 284 BS vs. 21.2% receiving placebo (p = 0.007), and in 29.6% of children receiving BIIL 284 BS vs. 22.9% receiving placebo (p = 0.348). In adults, the incidence of protocol-defined pulmonary exacerbation was greater in those receiving BIIL 284 BS than in those receiving placebo (33.1% vs. 18.2% respectively; p = 0.005). In children, the incidence of protocol-defined pulmonary exacerbation was 19.8% in the BIIL 284 BS arm, and 25.7% in the placebo arm (p = 0.38). While the cause of increased SAEs and exacerbations due to BIIL 284 BS is unknown, the outcome of this trial provides a cautionary tale for the administration of potent anti-inflammatory compounds to individuals with chronic infections, as the potential to significantly suppress the inflammatory response may increase the risk of infection-related adverse events.

Amburanins A and B fromAmburana cearensis: Daphnodorin-Type Biflavonoids that Modulate Human Neutrophil Degranulation

). At concentration higher than 25 µg mL -1 , both compounds suppressed nearly 92% of the neutrophil degranulation and 53% of myeloperoxidase activity, thus indicating that they are potential anti-inflammatory lead compounds.

Facile Synthesis, Characterization and Anti-Inflammatory Effect of 3-Aminoindolizine Derivatives

Four 3-aminoindolizines were synthesized from the substituted 2-bromopyridines and propargyl amines with the aim of obtaining potential anti-inflammatory compounds, which were characterized by NMR, IR, ESI-MS and elemental analysis. Their biological activities were evaluated by the bacterial lipopolysaccharide (LPS) stimulation of mouse cells in the RAW264.7 inflammation model. The target compounds4a-4drevealed moderate anti-inflammatory effects with the inhibitions of 45%~61% at 50 μM. The bioactive 3-aminoindolizines might be used for further optimization as potential anti-inflammatory drugs.

Penicillinolide A: A New Anti-Inflammatory Metabolite from the Marine Fungus Penicillium sp. SF-5292

In the course of studies on bioactive metabolites from marine fungi, a new 10-membered lactone, named penicillinolide A (1) was isolated from the organic extract of Penicillium sp. SF-5292 as a potential anti-inflammatory compound. The structure of penicillinolide A (1) was mainly determined by analysis of NMR and MS data and Mosher’s method. Penicillinolide A (1) inhibited the production of NO and PGE2 due to inhibition of the expression of iNOS and COX-2. Penicillinolide A (1) also reduced TNF-α, IL-1β and IL-6 production, and these anti-inflammatory effects were shown to be correlated with the suppression of the phosphorylation and degradation of IκB-α, NF-κB nuclear translocation, and NF-κB DNA binding activity. In addition, using inhibitor tin protoporphyrin (SnPP), a competitive inhibitor of HO activity, it was verified that the inhibitory effects of compound 1 on the production of pro-inflammatory mediators and NF-κB DNA binding activity were partially associated with HO-1 expression through Nrf2 nuclear translocation.

English

The aim of the present study is to investigate the effect of rutin, a potent antioxidant and anti-inflammatory compound on experimentally-induced diabetic neuropathy (DN) in male Wistar rats. In diabetic and normal rats, the pain-related behavior tests were performed before and after rutin (50 and 100 mg/kg/day for 6 weeks) treatments. In serum, fasting glucose, insulin, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and interleukin-1β (IL-1β) levels were estimated and in sciatic nerve, thiobarbituric acid reactive substances (TBARS), reduced glutathione (GSH) levels, and superoxide dismutase (SOD), catalase (CAT), glutathione-S-transferase (GST), glutathione-reductase (GR) and glutathione peroxidase (GSH-Px) activities were measured. Diabetic rats developed neuropathy which was apparent from decreased tail-flick and paw-withdrawal latencies and by following decrease in performance on Rota-Rod treadmill. Rutin treatments ameliorated the hyperalgesia, analgesia and improved motor coordination. Streptozotocin (STZ) significantly increased TBARS and decreased GSH levels in sciatic nerve where rutin treatment significantly protected those changes. In diabetic rats, SOD, CAT, GST, GSH-Px and GR activities were significantly inhibited. Rutin treatment significantly ameliorated decrease in antioxidant defense. Present results demonstrate protective effect of rutin in diabetic neuropathy through attenuation of oxidative stress and they suggest that rutin is a potential drug for the prevention of early diabetic-induced neuropathy. Key words: Streptozotocin, rutin, oxidative stress, neuropathy, diabetes.

The Effects of Intestinal LPS Exposure on Inflammatory Responses in a Porcine Enterohepatic Co-culture System

A porcine enterohepatic co-culture system, with primary hepatocytes as bottom layer and IPEC-J2 epithelial cells as upper layer, was developed to study the effects of lipopolysaccharides (LPS) on the gene expression profile of pro-inflammatory cytokines (interleukin-8 (IL-8) and tumor necrosis factor-α) and CYP enzymes (CYP1A1, CYP1A2, CYP3A29). The barrier integrity of IPEC-J2 cells was investigated by transepithelial electrical resistance measurements and by fluorescein isothiocyanate-dextran-based test. Basolateral IL-8 production was significantly elevated in LPS-treated IPEC-J2 and primary hepatocyte mono-cultures as well as in the co-culture system, in a dose-independent manner. The LPS-induced changes in the expression of the CYP1A2 and CYP3A29 genes in hepatocyte mono-cultures differed from those in co-culture after LPS treatment on the apical side of the IPEC-J2 cell layer. CYP1A2 was downregulated by the LPS treatment in mono-cultures but upregulated at 10 μg/ml LPS in co-culture; gene expression of CYP3A29 showed no significant LPS-induced change in the hepatocyte mono-culture but was significantly downregulated in co-culture. The newly established co-culture system capable of mimicking enterohepatic interplay in LPS-induced inflammatory responses in vitro can be used in the future for reliable screening of potential anti-inflammatory compounds.

Neuroprotective Effect of Silymarin by Modulation of Endogenous Biomarkers in Streptozotocin Induced Painful Diabetic Neuropathy

Aim of the present study is to investigate the effect of silymarin (SM), a potent antioxidant and anti-inflammatory compound on experimentally-induced Diabetic Neuropathy (DN) in male Wistar rats. Diabetes was induced by single streptozotocin (STZ) injection in rats. Pain-related behavior tests were performed including tail flick, paw-pressure analgesia and Rota-rod performance. Silymarin treatment was started after 21st day of diabetes induction and continued for 6 consecutive weeks. In serum fasting glucose, insulin, tumor necrosis factor-&alpha (TNF-α), interleukin-6 (IL-6) and interleukin-1&beta (IL-1&beta) levels were estimated and in sciatic nerve, thiobarbituric acid reactive substances (TBARS), reduced glutathione (GSH), Superoxide Dismutase (SOD), catalase (CAT), glutathione-s-transferase (GST), glutathione-reductase (GR) and glutathione peroxidase (GSH-Px) activities were measured. Diabetic rats developed neuropathy which was apparent from decreased tail-flick latency and paw-withdrawal latency.This was escorted by decreased motor coordination as assessed by performance on Rota-rod treadmill. Treatment with SM ameliorated the hyperalgesia, analgesia and improved motor coordination. STZ significantly increased TBARS and decreased GSH levels in sciatic nerve where silymarin treatment significantly protected those changes. Enzymatic activities such as SOD, CAT, GST, GSH-Px and GR were significantly inhibited in sciatic nerve of diabetic rats. The SM treatment significantly ameliorated decrease in antioxidant defense. Our results clearly demonstrate protective effect of SM is mediated through attenuation of oxidative stress and suggest therapeutic potential of SM in attenuation of diabetic neuropathy.

Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile

Glucocorticoids are highly effective therapies for a range of inflammatory diseases. Advances in the understanding of the diverse molecular mechanisms underpinning glucocorticoid action suggest that anti-inflammatory molecules with reduced side effect liabilities can be discovered. Here we set out to explore whether modification of the 17α position of the steroid nucleus could generate molecules with a unique pharmacological profile and to determine whether such molecules would retain anti-inflammatory activity. The pharmacological properties of GW870086 were compared with fluticasone propionate (FP) using a range of cellular and in vivo model systems, including extensive gene expression profiling. GW870086 repressed inflammatory cytokine release from lung epithelial cells in a similar manner to FP but antagonized the effect of dexamethasone on MMTV-driven reporter gene transactivation. GW870086 had a strong effect on the expression of some glucocorticoid-regulated genes (such as PTGS2), while having minimal impact on the expression of other known target genes (such as SGK). GW870086 retained the ability to strengthen tight junctions in epithelial cell culture but, unlike FP, was unable to protect the culture from elastase-mediated damage. In murine models of irritant-induced contact dermatitis and ovalbumin-induced allergic inflammation, GW870086 showed comparable anti-inflammatory efficacy to FP. GW870086 is a potent anti-inflammatory compound with a unique ability to regulate only a subset of those genes that are normally affected by classical glucocorticoids. It has the potential to become a new topical steroid with a different safety profile to existing therapies.

The Antiinflammatory Action and Pharmacokinetics of a Novel Glucosamine-based Di-Peptide Aminosugar

We have previously shown favorable in vitro gut permeability for three novel di-peptide esters of glucosamine (GlcN) likely facilitated by the peptide transporter 1 (PepT1). Herein, we report the development of a novel assay for the determination of bioavailability of the peptide ester of interest, the anti-inflammatory properties of a glycine-valine ester derivative of GlcN (GVG) as well as its pharmacokinetics under healthy and inflammatory conditions. A pre-column derivatization (with 9-fluorenylmethoxycarbonyl) HPLC assay was developed to study bioavailability of GVG, GlcN or cleaved GlcN in the rats that were cannulated in their right jugular vein for blood collection. The compounds of interest were orally administered to both healthy and arthritic rats. Serial blood samples and urine were collected and assayed for the compounds. The stability of the GVG was also tested after incubation with the rat feces. Efficacy of GVG was tested in inflamed rats (injection of 0.2 mL of Mycobacterium butyricum in squalene) following GVG (20 and 30 mg/kg/day GlcN equivalent) or GlcN (20 and 90 mg/kg/day) administration. Arthritis index was calculated at the end of the experiment. The assay was linear (ranged between 0.05-20 μg/mL) and reproducible (intra- and inter-day<10%). Among the tested compounds, only GVG showed a significantly higher plasma concentrations and urinary excretion than GlcN (≈3-fold increase). GVG showed a favorable stability in the rat feces. Adjuvant arthritis was completely prevented with doses greater than 20 mg/kg/day with GVG being 3-fold more potent than GlcN. The examined glycine-valine-GlcN di-peptide aminosugar is a potent anti-inflammatory compound due to its favorable properties to deliver GlcN into the systemic circulation.

In-vitro antioxidant and in-vivo anti-inflammatory activities of aerial parts of Cassia species

Cassia species are native to Southeast Asia and sub-Saharan Africa and are commonly used as food and in a broad variety of medicinal applications. Cassia species are widely used in India, but there are few reports in the literature of studies on its chemical compositions and biological properties. In this study, the antioxidant and anti-inflammatory activities of two plants of Cassia species namely Cassia siamea (Lam.) and Cassia javanica (Linn.) were evaluated and the total phenolic compounds and flavonoid contents were determined.The antioxidant activity of the extracts was measured using scavenging of 2,2′-Diphenyl-1-picrylhydrazyl hydrate (DPPH), bleaching of β-carotene and % inhibition of H2O2. The anti-inflammatory activity was evaluated using carrageenan induced paw edema method on Wistar albino rats. The etahnolic extracts of aerial parts of C. siamea and C. javanica were evaluated for in vivo anti-inflammatory activity against the animal model of female Wistar albino rats. Ethanol extracts showed significant and dose-dependent anti-inflammatory effects. The contents of flavonoids and total phenolic compounds could be correlated with the antioxidant and anti-inflammatory activities observed for C. siamea and C. javanica. Our findings suggest that aerial parts of C. siamea and C. javanica contain potential antioxidant and anti-inflammatory compounds, which could be tested as drug candidates against oxidative and inflammation-related pathological processes in medicinal chemistry studies.

Inhibitor Effect of Antioxidant Flavonoids Quercitin, and Capsaicin in Mast Cell Inflammation

Mast cells are essential not only for allergies but also for innate and acquired immunity, autoimmunity and inflammation, and they are recognized as a new type of immunoregulatory cells capable of producing different cytokines. Natural compounds have long been recognized to possess anti-inflammatory, antioxidant and anticancergenic activity. Quercitin is an inhibitor for mast cells and is a potent antioxidant, cytoprotective and anti-inflammatory compound and has a negative effect on intracellular regulator signal events initiated by FceRI receptor cross-linking and other activating receptors on mast cells. These observations candidate quercitin as a therapeutic compound in association with other therapeutic molecules. Capsaicin is a compound derived from peppers, especially capsicum, and is involved in stimulating circulation aiding digestion and relieving pain. Capsaicin receptor sub type I (VRI) is expressing in neurons and is present in a number of brain nuclei and in non-neuronal tissues, mediating inflammatory response. Capsaicin is involved in migraine, allergic symptoms, arthritis pain and gastric secretion. In this paper we review the biological effects of quercitin and capsaicin.