scholarly journals Anticancer and Anti-Inflammatory Activities of a Standardized Dichloromethane Extract fromPiper umbellatumL. Leaves

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Leilane Hespporte Iwamoto ◽  
Débora Barbosa Vendramini-Costa ◽  
Paula Araújo Monteiro ◽  
Ana Lúcia Tasca Gois Ruiz ◽  
Ilza Maria de Oliveira Sousa ◽  
...  
Keyword(s):  
Solid Tumor ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Tumor Model ◽  
Oral Route ◽  
Paw Edema ◽  
Anti Inflammatory ◽  
Cancer And Inflammation

Despite the advances in anticancer drug discovery field, the worldwide cancer incidence is remarkable, highlighting the need for new therapies focusing on both cancer cell and its microenvironment. The tumor microenvironment offers multiple targets for cancer therapy, including inflammation. Nowadays, almost 75% of the anticancer agents used in chemotherapy are derived from natural products, and plants are an important source of new promising therapies. Continuing our research onPiper umbellatumspecies, here we describe the anticancer (in vitroantiproliferative activity andin vivoEhrlich solid tumor model) and anti-inflammatory (carrageenan-induced paw edema and peritonitis models) activities of a standardized dichloromethane extract (SDE) fromP. umbellatumleaves, containing 23.9% of 4-nerolidylcatechol. SDE showedin vitroandin vivoantiproliferative activity, reducing Ehrlich solid tumor growth by 38.7 and 52.2% when doses of 200 and 400 mg/kg, respectively, were administered daily by oral route. Daily treatments did not produce signals of toxicity. SDE also reduced paw edema and leukocyte migration on carrageenan-induced inflammation models, suggesting that the anticancer activity of SDE fromPiper umbellatumleaves could involve antiproliferative and anti-inflammatory effects. These findings highlightP. umbellatumas a source of compounds against cancer and inflammation.

scholarly journals (E)-2-Cyano-3-(1H-Indol-3-yl)-N-Phenylacrylamide, a Hybrid Compound Derived from Indomethacin and Paracetamol: Design, Synthesis and Evaluation of the Anti-Inflammatory Potential

2020 ◽  
Vol 21 (7) ◽  
pp. 2591
Author(s):  
Pablo Silva ◽  
Maria de Almeida ◽  
Jamire Silva ◽  
Sonaly Albino ◽  
Renan Espírito-Santo ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Significant Inhibition ◽  
In Vitro Assays ◽  
Paw Edema ◽  
Substituted Anilines ◽  
Hybrid Compound ◽  
Design Synthesis ◽  
Anti Inflammatory

The compound (E)-2-cyano-3-(1H-indol-3-yl)-N-phenylacrylamide (ICMD-01) was designed and developed based on the structures of clinically relevant drugs indomethacin and paracetamol through the molecular hybridization strategy. This derivative was obtained by an amidation reaction between substituted anilines and ethyl 2-cyanoacetate followed by a Knoevenagel-type condensation reaction with indole aldehyde that resulted in both a viable synthesis and satisfactory yield. In order to assess the immunomodulatory and anti-inflammatory activity, in vitro assays were performed in J774 macrophages, and significant inhibitions (p < 0.05) of the production of nitrite and the production of cytokines (IL-1β and TNFα) in noncytotoxic concentrations were observed. The anti-inflammatory effect was also studied via CFA-induced paw edema in vivo tests and zymosan-induced peritonitis. In the paw edema assay, ICMD01 (50 mg kg−1) showed satisfactory activity, as did the group treated with dexamethasone, reducing edema in 2–6 h. In addition, there was no significant inhibition of PGE2, IL-1β or TNFα in vivo. Moreover, in the peritonitis assay that assesses leukocyte migration, ICMD-01 exhibited promising results. Therefore, these preliminary studies demonstrate this compound to be a strong candidate for an anti-inflammatory drug together with an improved gastrointestinal safety profile when compared to the conventional anti-inflammatory drugs.

scholarly journals Molecular Insight into the Anti-Inflammatory Effects of the Curcumin Ester Prodrug Curcumin Diglutaric Acid In Vitro and In Vivo

2020 ◽  
Vol 21 (16) ◽  
pp. 5700 ◽  
Author(s):  
Rianthong Phumsuay ◽  
Chawanphat Muangnoi ◽  
Peththa Wadu Dasuni Wasana ◽  
Hasriadi Hasriadi ◽  
Opa Vajragupta ◽  
...  
Keyword(s):  
Time Course ◽  
Area Under The Curve ◽  
Dependent Manner ◽  
Paw Edema ◽  
Inflammatory Agent ◽  
Potent Inhibition ◽  
Anti Inflammatory ◽  
Ester Prodrug

Curcumin diglutaric acid (CurDG), an ester prodrug of curcumin, has the potential to be developed as an anti-inflammatory agent due to its improved solubility and stability. In this study, the anti-inflammatory effects of CurDG were evaluated. The effects of CurDG on inflammatory mediators were evaluated in LPS-stimulated RAW 264.7 macrophage cells. CurDG reduced the increased levels of NO, IL-6, and TNF- α, as well as iNOS and COX-2 expression in cells to a greater extent than those of curcumin, along with the potent inhibition of MAPK (ERK1/2, JNK, and p38) activity. The anti-inflammatory effects were assessed in vivo by employing a carrageenan-induced mouse paw edema model. Oral administration of CurDG demonstrated significant anti-inflammatory effects in a dose-dependent manner in mice. The effects were significantly higher compared to those of curcumin at the corresponding doses (p < 0.05). Moreover, 25 mg/kg curcumin did not exert a significant anti-inflammatory effect for the overall time course as indicated by the area under the curve data, while the equimolar dose of CurDG produced significant anti-inflammatory effects comparable with 50, 100, and 200 mg/kg curcumin (p < 0.05). Similarly, CurDG significantly reduced the proinflammatory cytokine expression in paw edema tissues compared to curcumin (p < 0.05). These results provide the first experimental evidence for CurDG as a promising anti-inflammatory agent.

scholarly journals Inhibitory Effects of Traditional Herbal Formula Pyungwi-San on Inflammatory ResponseIn VitroandIn Vivo

2013 ◽  
Vol 2013 ◽  
pp. 1-19 ◽  
Author(s):  
Ji Young Cha ◽  
Ji Yun Jung ◽  
Jae Yup Jung ◽  
Jong Rok Lee ◽  
Il Je Cho ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inflammatory Mediators ◽  
Raw 264.7 Cells ◽  
Prostaglandin E ◽  
Herbal Formula ◽  
Paw Edema ◽  
Cox 2 ◽  
Anti Inflammatory

Pyungwi-san (PWS) is a traditional basic herbal formula. We investigated the effects of PWS on induction of cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), pro-inflammatory cytokines (interleukin-6 (IL-6) and tumor necrosis factor-α(TNF-α)) and nuclear factor-kappa B (NF-κB) as well as mitogen-activated protein kinases (MAPKs) in lipopolysaccharide-(LPS-) induced Raw 264.7 cells and on paw edema in rats. Treatment with PWS (0.5, 0.75, and 1 mg/mL) resulted in inhibited levels of expression of LPS-induced COX-2, iNOS, NF-κB, and MAPKs as well as production of prostaglandin E2(PGE2), nitric oxide (NO), IL-6, and TNF-αinduced by LPS. Our results demonstrate that PWS possesses anti-inflammatory activities via decreasing production of pro-inflammatory mediators through suppression of the signaling pathways of NF-κB and MAPKs in LPS-induced macrophage cells. More importantly, results of the carrageenan-(CA-) induced paw edema demonstrate an anti-edema effect of PWS. In addition, it is considered that PWS also inhibits the acute edematous inflammations through suppression of mast cell degranulations and inflammatory mediators, including COX-2, iNOS and TNF-α. Thus, our findings may provide scientific evidence to explain the anti-inflammatory properties of PWSin vitroandin vivo.

In vitro and in vivo delivery of atorvastatin: A comparative study of anti-inflammatory activity of atorvastatin loaded copolymeric micelles

2017 ◽  
Vol 32 (8) ◽  
pp. 1127-1138 ◽  
Author(s):  
Sina Andalib ◽  
Pezhman Molhemazar ◽  
Hossein Danafar
Keyword(s):  
Inflammatory Responses ◽  
Inflammatory Activity ◽  
Lipid Lowering ◽  
Precipitation Method ◽  
Paw Edema ◽  
Scanning Calorimetry ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Statins have been shown to exert ‘pleiotropic effects’ independent of their cholesterol lowering actions that include anti-inflammatory properties. In this study we synthesized mono methoxy poly (ethylene glycol)–poly (ε-caprolactone) (mPEG-PCL) di block copolymers. The structure of the copolymers was characterized by H nuclear magnetic resonance, Fourier-transform infrared spectroscopy, differential scanning calorimetry and gel permeation chromatography techniques. In this method, atorvastatin was encapsulated within micelles through a single-step nano-precipitation method, leading to the formation of atorvastatin-loaded mPEG-PCL (atorvastatin/mPEG-PCL) micelles. The resulting micelles were characterized further by various techniques such as dynamic light scattering and atomic force microscopy. In this study the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles on acute models of inflammation are analyzed, to compare the effect of indometacin in rats. Carrageenan induces rat paw edema; six animals of each group (10 groups) received indometacin, atorvastatin, and atorvastatin/mPEG-PCL micelles orally 1, 6, 12 and 24 h before carrageenan injection in paw. The paw edema thickness measured at 1, 2, 3 and 4 h after injection and percentage inhibition of edema in various groups were calculated. The results showed that the zeta potential of micelles was about −16.6 mV and the average size was 81.7 nm. Atorvastatin was encapsulated into mPEG-PCL micelles with loading capacity of 14.60 ± 0.96% and encapsulation efficiency of 62.50 ± 0.84%. Atorvastatin and atorvastatin/mPEG-PCL micelles showed significant anti-inflammatory activity in the present study. The anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles was significant in comparison with indometacin. Atorvastatin/mPEG-PCL micelles showed more anti-inflammatory activity than atorvastatin. This study revealed the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles and suggested the statins have a potential inflammatory activity along with its lipid lowering properties. Contrary to anti-inflammatory effects, the pro-inflammatory responses are independent of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition and can be mediated directly by atorvastatin.

scholarly journals EFFECT OF TERPENES AS PENETRATION ENHANCERS ON THE RELEASE AND PERMEATION KINETICS OF MELOXICAM GELS FORMULATIONS

2020 ◽  
pp. 1-5
Author(s):  
Raj Kumari ◽  
Pallavi Matta ◽  
Meenakshi Sharma ◽  
Madhu Verma
Keyword(s):  
Penetration Enhancers ◽  
Peppermint Oil ◽  
Clove Oil ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Lemongrass Oil ◽  
Anti Inflammatory ◽  
Rat Paw

Introduction: The transdermal route of administration has been extensively accepted as one of the potential route for the local and systemic delivery of drugs. The greatest obstacle in drug absorption is the highly organized stratum corneum (SC), which hinder drug transport. The probable solution leads to inclusion of penetration enhancers for reversibly disorganizing the barrier characteristic of stratum corneum. Objective: The main objective of the research work was to study the influence of peppermint oil, lemongrass oil, clove oil and turpentine oil as penetration enhancers on the percutaneous absorption of Meloxicam (ME) from a Carbopol 934 based gel formulation. Materials and Methods: ME gel sample was divided into 5 batches i.e., F1, F2, F3, F4, F5. Except F1, all other batches were incorporated with penetration enhancers (5% w/w) namely peppermint oil, clove oil, lemongrass oil and turpentine oil. The formulations were further evaluated for in-vitro drug release studies using a standard cellophane membrane at 37± 0.5˚ C in phosphate buffer pH 7.4 and a comparative anti-inflammatory activity was conducted using rat paw edema method. Result and Discussion: In-vitro permeation studies using a standard cellophane membrane showed that the rank order of enhancement ratio (ERflux) for Meloxicam as peppermint oil (1.414) > clove oil (1.353) > lemongrass oil (1.326) > turpentine oil (1.272) proving peppermint oil as the most competent penetration enhancer for Meloxicam. Further In- vivo anti-inflammatory activity were carried out using the standard rat paw edema method. The in vivo studies revealed that gel containing peppermint, clove, lemongrass and turpentine exhibited 2.53, 2.0, 1.9 and 1.38 times higher anti-inflammatory effect as compared to meloxicam (standard). Conclusion: It can be concluded from the study that all the 4 terpenes significantly increases the permeation of meloxicam gels and can be used as effective penetration enhancers.

scholarly journals IN VITRO ANTIOXIDANT AND IN VIVO ANTI-INFLAMMATORY ACTIVITY OF THE AERIAL PART OF BLUMEA ERIANTHA DC

2018 ◽  
Vol 10 (7) ◽  
pp. 75 ◽  
Author(s):  
Urmila U. Tambewagh ◽  
Supada Rambhau Rojatkar
Keyword(s):  
Antioxidant Activity ◽  
Aerial Part ◽  
Methanol Extract ◽  
Reducing Power ◽  
Dependent Manner ◽  
Paw Edema ◽  
Anti Inflammatory ◽  
In Vitro Antioxidant Activity

Objective: Objective of the present study was to carry out in vivo anti-inflammatory and in vitro antioxidant activity of methanol extract of aerial part of the Blumea eriantha DC belonging to family Asteraceae.Methods: The shade dried aerial part of B. eriantha (0.5 kg) was powdered and extracted with methanol (1.5 x 3L) at room temperature (24h x 3). After filtration combined all the three extracts and were concentrated on rotary evaporator under reduced pressure at 40 °C, thereby providing crude methanol extract which was subsequently employed for further studies. Anti-inflammatory effect was studied by carrageenan-induced paw edema model in rats at dose level 100, 200, and 400 mg/kg. Acute oral toxicity study and in vitro antioxidant potential of the extract was also studied. The in vitro antioxidant activity of methanol extract of aerial part of Blumea eriantha DC was evaluated against 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydrogen peroxide (H2O2) and hydroxyl (OH) radicalscavenging and reducing power assays.Results: The results indicate that methanol extract of Blumea eriantha (BEME, 400 mg/kg) exhibited significant inhibition (p<0.001) of increase in paw edema at 5th h. IC50 value of BEME showed significant antioxidant activity. The extract exhibits promising free radical scavenging effect of DPPH, H2O2, OH and reducing power in a dose-dependent manner up to 100µg/ml concentration while the reference standard Ascorbic acid demonstrated more scavenging potential than the methanol extract of Blumea eriantha The methanol extract was found to be safe at the dose of 2000 mg/kg.Conclusion: The results of the experimental study confirmed that methanol extract of Blumea eriantha DC possesses significant anti-inflammatory and antioxidant activity.

scholarly journals In- vitro antioxidant and In vivo Anti-inflammatory Potentials of Marantochloa Leucantha (Marantaceae) Extracts and Fractions

2019 ◽  
Vol 18 (2) ◽  
pp. 233-240
Author(s):  
Wilfred O Obonga ◽  
Charles O Nnadi ◽  
Chinonye C Chima ◽  
Sunday N Okafor ◽  
Edwin O Omeje
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging ◽  
Paw Edema ◽  
Frap Assay ◽  
Rat Paw Edema ◽  
Etoac Fraction ◽  
High Antioxidant Activity ◽  
Anti Inflammatory

This study evaluated the antioxidant and anti-inflammatory properties of Marantochloa leucantha (Marantaceae). The in vitro antioxidant activity of the extracts and solvent fractions was evaluated by 1,1-diphenyl- 2-picrylhydrazyl (DPPH) radical scavenging and ferric reducing antioxidant potential (FRAP) assay models and in vivo anti-inflammatory activity by the rat paw edema model. The phytochemical screening indicated the presence of tannins, terpenoids, steroids, flavonoids, reducing sugar and phenolics. The antioxidant assay showed that all the extracts exhibited high antioxidant activity comparable with ascorbic and gallic acid controls. In DPPH model, a 250 μg/ml EtOAc fraction of the leaves showed antioxidant activity of 93.9 ± 1.7 % (EC50 0.82 μg/ml) and a 1000 μg/ml of same stem fraction produced 91.9 ± 0.3 % activity (EC50 1.38 μg/ml). In the FRAP model, EtOAc fraction exhibited 31.1±0.7 and 92.0 ± 2.2 μM Fe2+/g of dried leaves and stem, respectively at 1000 μg/ml FeSO4 equivalent. The anti-inflammatory potential of the plant showed that the crude stem extract and fractions at 200 - 600 mg/kg exhibited significant (p < 0.01) dose-related inhibition of paw edema in rats. A 200 mg/kg EtOAc fraction showed 18.8 % inhibition compared to 31 % observed in diclofenac-treated rats in 2 h post albumin challenge. These findings validated the folkloric use of this plant in the treatment of diseases associated to the oxidative stress and could further provide promising lead compounds with potent antioxidant and anti-inflammatory activities Dhaka Univ. J. Pharm. Sci. 18(2): 233-240, 2019 (December)

Evaluation of Biological Activity of Derivatives of 1,3,4 Thiadiazole, 1,3,4-Oxadiazole and 1,2,4-Triazole

2020 ◽  
Vol 20 ◽  
Author(s):  
Gaurav M. Doshi ◽  
Mayuresh U. Bansode ◽  
Rakesh R. Somani
Keyword(s):  
Erythrocyte Membrane ◽  
Paw Edema ◽  
Toxic Dose ◽  
Rat Paw Edema ◽  
Maximum Decrease ◽  
Inhibitory Activities ◽  
Anti Inflammatory ◽  
Rat Paw

Objectives: 1,3,4-thiadiazole (A), 1,3,4-oxadiazole (B) and 1,2,4-triazole (C) derivatives have been known for their immense pharmacotherpaeutic potential. The current research article attempts to further explore and understand the probable biochemical mechanism related to anti-inflammatory activity of derivatives. Methods: The screened A, B and C derivatives were investigated for both in-vitro (Erythrocyte Membrane stabilization activity, Proteinase enzyme inhibitory activities) and in-vivo correlation using acute and chronic anti-inflammatory potential by carrageenan induced rats paw edema and cotton pellet granuloma methods respectively. The activity was studied after interpreting acute toxicity studies results. Results: In vitro studiesin the case of Erythrocyte Membrane stability and Proteinase enzyme inhibitory activities exhibited by A, B, and C at 100 ppm were found to be 48.89%, 51.08% and 50.08% and 66.78%, 76.91% and 57.41% respectively. The maximum toxic dose was found to be 2000 mg/kg. The derivatives were studied for two-dose levels viz; Lower (100 mg/kg) and higher dose (200 mg/kg). In rat paw edema maximum decrease was obtained for A (50.05%), B (50.05%) and C (51.06%) at lower and higher dose at 68.76%, 55.61%, and 65.26% respectively for effect up to 24 h. In the chronic model of cotton pelletgranuloma viz; higher and lower doses of A, B and C exhibited 38.15%, 33.19% and 30.25 % and 19.45%, 18.55% and 17.55 % respectively. Conclusion: The studied models depicted that derivatives A, B and C have the probable potential as anti-inflammatory agents. Further studies need to undertaken to explore their potential in the different therapeutic areas.

Inhibition of iNOS by Benzimidazole Derivatives: Synthesis, Docking, and Biological Evaluations

2021 ◽  
Vol 17 ◽  
Author(s):  
Richa Minhas ◽  
Yogita Bansal
Keyword(s):  
Inflammatory Activity ◽  
Benzimidazole Derivatives ◽  
Critical Study ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Inos Inhibitors ◽  
Rat Paw

Background: Inducible nitric Oxide Synthase (iNOS) plays a key role in the progression of inflammatory diseases by accelerating the production of NO, which makes it an intriguing target to treat inflammation in complex diseases. Therefore, the search is on to develop molecules as selective iNOS inhibitors. Objective: The present work was aimed to design, synthesize and evaluate benzimidazole-coumarin coupled molecules as anti-iNOS agents through in silico and pharmacological studies. Methods: A critical study of literature reports on iNOS inhibitors led to the selection of a (un)substituted coumarin nucleus, 2-aminobenzimidazole, and a 4-atom linker as important structural components for iNOS inhibition. Two series of compounds (7-16 and 17-26) were designed and synthesized by coupling these components. The compounds were subjected to docking using iNOS (1QW4) and nNOS (1QW6) as targets. All compounds were evaluated for NO and iNOS inhibitory activities in vitro. The selected compound was finally evaluated for anti-inflammatory activity in vivo using the carrageenan-induced rat paw edema model. Results : All compounds showed moderate to good inhibition of NO and iNOS in vitro. Compound 12 was the most potent inhibitor of NO and iNOS. Hence, it was evaluated in vivo for toxicity and anti-inflammatory activity. It was found to be safe in acute toxicity studies, and effective in reducing the rat paw edema significantly. Its anti-inflammatory behaviour was similar to that of aminoguanidine, which is a selective iNOS inhibitor. Conclusion: The newly synthesized benzimidazole-coumarin hybrids may serve as potential leads for the development of novel anti-iNOS agents.

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