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

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)

Author(s):  
Madhavi K ◽  
Sree Ramya G

Objective: Objective of the study was to synthesize and evaluate a series of novel compounds, ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)- 4,5-dimethylthiophene-3-carboxylates, for in vitro antioxidant and in vivo anti-inflammatory activities.Methods: Ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylates were synthesized by knoevenagel condensation of active methylene group of ethyl 2-(2-cyanoacetamido)-4,5-dimethylthiophene-3-carboxylate with substituted benzaldehydes. The synthesized compounds were evaluated for their in vitro antioxidant properties in three different models, viz., reduction of 1,1-diphenyl-2-pycrylhydrazyl free radical, scavenging of nitric oxide free radical, and ferric ion-induced lipid peroxidation using rat brain homogenate. Few selected compounds with good antioxidant properties were pharmacologically evaluated for anti-inflammatory activity by carrageenan-induced rat paw edema model.Results: Clean and efficient synthetic procedure was used for the preparation of series of compounds. The structures of synthesized compounds were confirmed by infrared, 1H nuclear magnetic resonance and mass spectra. The antioxidant activity data revealed that the compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5-dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant activity. Hence, the active compounds were evaluated for anti-inflammatory activity and found to possess good activity. The percentage inhibition of rat paw edema obtained for the evaluated compounds was in the range of 70.2-83.1, comparable to the standard drug diclofenac (85.0%).Conclusion: The use of inexpensive, eco-friendly and readily available reagents, easy work-up and high purity of products makes the procedure a convenient and robust method for the synthesis of title compounds. The compounds of ethyl 2-(2-cyano-3-(substituted phenyl)acrylamido)-4,5- dimethylthiophene-3-carboxylate containing phenolic substitution showed greater antioxidant and anti-inflammatory activities.


2017 ◽  
Vol 32 (8) ◽  
pp. 1127-1138 ◽  
Author(s):  
Sina Andalib ◽  
Pezhman Molhemazar ◽  
Hossein Danafar

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.


Author(s):  
Raj Kumari ◽  
Pallavi Matta ◽  
Meenakshi Sharma ◽  
Madhu Verma

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.


Author(s):  
Urmila U. Tambewagh ◽  
Supada Rambhau Rojatkar

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.


2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Sumit Bahadur Baruwal Chhetri ◽  
Deepa Khatri ◽  
Kalpana Parajuli

Diploknema butyracea (Roxb.) H.J. Lam is a multipurpose tree used by the Nepalese indigenous people for medicinal purposes such as rheumatism, asthma, and ulcer and other purposes such as cooking and lighting. However, there is no scientific evidence for the medicinal uses of this plant. The present study aimed to explore the phytochemical constituents, estimate the total phenolic content, evaluate antioxidant activity, and investigate the in vivo anti-inflammatory and analgesic activities of aqueous extract of Diploknema butyracea (Roxb.) H.J. Lam bark (ADBB). Phytochemical screening was performed using standard methods. The total phenolic content was determined using the Folin–Ciocalteu method. The in vitro antioxidant activity was determined using 2, 2-diphenyl-1-picrylhydrazyl radical scavenging assay and nitric oxide radical scavenging assay. For the in vivo studies, the plant extract was given in three different doses (50, 100, and 200 mg/kg body weight) to male albino Wistar rats. Anti-inflammatory and analgesic studies were carried out using the carrageenan-induced rat paw edema and the hot plate method, respectively. Results revealed the presence of different phytoconstituents such as flavonoids, tannins, glycosides, terpenoids, and carbohydrates together with a considerable amount of phenolic compounds. Antioxidant assays indicated the potent antioxidant activity of the plant extracts. The higher dose of D. butyracea (200 mg/kg) exhibited a maximum and significant inhibition (53.20%) of rat hind paw edema volume at 4 h and showed a greater increment in latency time (12.15 ± 1.81 sec) in the hot plate test at 120 min. The present study demonstrated the antioxidant, anti-inflammatory, and analgesic potential of ADBB, which supports its traditional medicinal use.


Author(s):  
Gaurav M. Doshi ◽  
Mayuresh U. Bansode ◽  
Rakesh R. Somani

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.


2021 ◽  
Vol 17 ◽  
Author(s):  
Richa Minhas ◽  
Yogita Bansal

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.


Author(s):  
Soumia Bouzidi ◽  
Benkiki Naima ◽  
Allaoua Zina

ABSTRACTObjective: The aim of this study is to evaluate the in vitro antioxidant activity of Paronychia capitata various extracts, acute toxicity, the in vivoantipyretic and anti-inflammatory activities of the n-butanol extract.Methods: The antioxidant properties were tested using 2,2-diphenyl 1-picrylhydrazyl radical scavenging and β-carotene linoleic acid system, thetotal phenolic and flavonoid contents were determined. Furthermore, anti-inflammatory activity and antipyretic activity of the n-butanol extractwere assessed on male Wistar rats at the dose levels 250, 500 mg/kg body weight, using the egg albumin-induced edema, and brewer’s yeast-inducedpyrexia method, respectively.Results: The n-butanol extract of P. capitata had considerably the highest antiradical activity with inhibitory concentration 50 value of 8.667 μg/ml.Conclusion: The experimental data demonstrated that n-butanol extract of P. capitata possess significantly remarkable anti-inflammatory andantipyretic activities compared to the standard drugs.Keywords: Caryophyllaceae, Flavonoid, Inflammation, Fever, Paronychia capitata.


2012 ◽  
Vol 81 (2) ◽  
pp. 346-350 ◽  
Author(s):  
Martina C. Meinke ◽  
Sabine Schanzer ◽  
Stefan F. Haag ◽  
Federica Casetti ◽  
Marcel L. Müller ◽  
...  

2016 ◽  
Vol 6 (11) ◽  
pp. 735
Author(s):  
Nazma Shaheen ◽  
Avonti Basak Tukun ◽  
Saiful Islam ◽  
Nafis Md. Irfan ◽  
Ishrat Nourin Khan ◽  
...  

Background: Rising tide of chronic nutrition related non-communicable diseases yoked with extant under nutrition problems makes it imperative to carry out scientific research for finding functional foods. Although the emergence of these diseases are believed to be related to a constellation of dietary, socio-economic and lifestyle related risk factors, central to the pathogenesis of these diseases (or disease states) are free radicals, oxidative stress, and inflammatory processes typically accompanied by pain. Therefore, functional whole foods with physiologically active antioxidants, anti-inflammatory, and analgesic compounds seem to be the most promising option to deal with the pathogenesis of existing and emerging chronic diseases burden of Bangladesh.Methods: Edible portions of 70 commonly consumed Bangladeshi foods – including one cereal, five legumes, fourteen vegetables, four tea varieties, five oil seeds, twenty spices, and twenty one fruits – were evaluated for total phenol content (TPC) by Folin-Ciocalteau assay. To evaluate functional potentiality, in vitro antioxidant capacity (AC) of selected food items were evaluated by DPPH radical scavenging assays, in vitro anti-inflammatory potential by observing the production of pro-inflammatory cytokine TNF-α using J774A.1 cells stimulated with lipopolysaccharide (LPS), in vivo anti-inflammatory potential by measuring carrageenan induced rat paw edema reduction and in vivo analgesic potential by acetic acid induced writhing test in mice. Results: Spices, oilseeds, and teas showed high concentration of TPC among the analysed foods while spices and teas exhibited notable AC. Green tea showed highest concentrations of TPC (2349 mg Gallic Acid Equivalent / g) and AC (2432 µmole Trolox Equivalent/g).  Fourteen food items showed potential in vitro anti-inflammatory activity with confirmatory dose response effect shown by 8 items. In vivo, black sesame and yellow mustard expressed anti-inflammatory and analgesic effects in a dose dependent manner.Conclusion: This study found commonly consumed food items representing different food groups of Bangladesh to contain diverse range of polyphenols and antioxidant capacities. Of these, black sesame and yellow mustard demonstrated anti-inflammatory and analgesic potential in animal model. The findings of this study can be used to promote polyphenols rich foods through dietary guidelines and facilitate epidemiological research investigating diet-disease relationships. 


Sign in / Sign up

Export Citation Format

Share Document