scholarly journals Oral and Topical Anti-Inflammatory Activity of Jatropha integerrima Leaves Extract in Relation to Its Metabolite Profile

Plants ◽  
2022 ◽  
Vol 11 (2) ◽  
pp. 218
Author(s):  
Engy A. Mahrous ◽  
Ahmed H. Elosaily ◽  
Abeer A. A. Salama ◽  
Ahmed M. Salama ◽  
Soheir M. El-zalabani

Jatropha integerrima Jacq., family: Euphorbiaceae, is used in India and subtropical Africa to treat different skin conditions. In this study we evaluated the anti-inflammatory activity of J. integerrima leaves extract (JILE) using rat paw edema model. The extract was administered orally (200 and 400 mg/kg) or applied topically as creams at 2.5, 5, and 10% strength. Four hours post-treatment, maximum reduction of edema volume by 63.09% was observed after oral administration of JILE (400 mg/kg) as compared to indomethacin with 60.43%. The extract anti-inflammatory effect was accompanied by a decrease in NO, prostaglandin PGE2, TNF-a and PKC levels by 19, 29.35, 16.9, and 47.83%, respectively. Additionally, topical applications of JILE showed dose dependent reduction in paw edema and resulted in normalized levels of PGE2, TNF-a, and PKC when used as 10% cream. Signs of inflammations were reduced or absent from paw tissue of animals receiving JILE either orally or topically. Finally, liquid chromatography/mass spectrometry analysis of JILE resulted in the annotation of 133 metabolites including 24 diterpenoids, 19 flavonoids, 10 phenolic acid conjugates, 8 cyclic peptides, 6 phytosterols, 4 sesquiterpenes, and 4 coumarins. Several of the annotated metabolites have known anti-inflammatory activity including vitexin, isovitexin, fraxitin, scopeltin, stigmasterol, and many diterpenoidal derivatives.

Author(s):  
Mallikarjuna Rao Talluri ◽  
Battu Ganga Rao ◽  
Y. Venkateswaea Rao

The present study was intended to evaluate Anti-inflammatory activity ofC. rottleriextracts (Hydroalcoholic, Methanol, Ethyl acetate and Hexane). The Anti-inflammatory activity ofC.rottleriextracts at doses of 125mg/kg, 250mg/kg and 500mg/kg using carrageenan induced rat paw edema model compared with standard drug (Indomethacin). The selected plant extracts significantly inhibited paw edema along with the standard drug Indomethacin. Of all extracts, methanol extract produced significant effect on reduction of increased paw thickness, hydro alcoholic and ethyl acetate extracts produced moderate percentage inhibition and hexane extract produced low level of percentage inhibition in reducing paw edema on carrageenan induced rats. In all extracts, methanol extract at a dose of 500mg/kg showed more percentage inhibition i.e . 53.47±2.19. From the results obtained during the study it is concluded thatC. rottlerihaving the bioactive molecule responsible for Anti-inflammatory activity by individually or by combination of different bio-active compounds present in it. Further is necessary for isolation and characterization of bioactive molecules which are responsible for the selected plant biological activities.


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.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Rajkamal Mittal ◽  
Arvind Sharma ◽  
Sandeep Arora

The purpose of study is to formulate and evaluate ufasomal gel of dexamethasone. Ufasomal suspension was made by sonication method using different concentrations of Span 80, Span 20 and cholesterol along with 25 mg of drug. Ufasomal gel was formulated by hydration method using carbopol 940. Ufasomal vesicles appeared as spherical and multilamellar under Transmission Electron Microscope. Ufasomal formulation prepared with drug to oleic acid molar ratio 8:2 (UF-2) produced greater number of vesicles and greater entrapment efficiency. UF-2 was optimized for further evaluation. The transdermal permeation and skin partitioning of from optimized formulation was significantly higher () as compared to plain drug and plain gel formulation which is due to presence of surfactant acting as permeation enhancer. Permeation of optimized formulation was found to be about 4.7 times higher than plain drug gel. Anti-inflammatory activity evaluated by inhibition Carrageenan induced rat paw edema model. Significant reduction of edema () was observed in comparison to the commercial product. Hence oleic acid based vesicles can be used as alternate carrier for topical delivery.


Author(s):  
D B Joshi

Series of novel Schiff bases of Isatin the  equimolar amines and 5-Dicrboxymethyl (R=COO2Me) substituted isatins (1 mmol of each) were added to 96% w/w ethanol (20 mL) containing 8 drops of glacial acetic acid. The mixture was heated under reflux for 5 h and then cooled to room temperature. The resulting solid was collected by filtration, washed with cold ethanol and dried in open air. The derivatives thus prepared had sufficient analytical purity. anticonvulsant activity performed by method as Animals were weighed and numbered. Mice were divided into 7 groups of six animals each. Group 1 served as control which was treated with vehicle (2% v/v Tween 80), group 2 was treated with standard drug phenytoin (25 mg/kg, i.p.) and groups 3– 7 were treated with newly synthesized oxadiazole derivatives (25 mg/kg, i. p.). One hour after injection, the animals were subjected to electro shock through ear electrodes of 80 mA for 0.2 sec by electroconvulsiometer AND ANTI-inflammatory activity measured by Weigh the animals and number them. Mark the animals with picric acid for individual animal identification. Divide rats into 5 groups of 6 rats each. Note the initial paw volume of each rat by dipping just beyond tibio-tarsal junction by mercury displacement method. The pharmacological screening of the synthesized compounds showed anti convulsant activity ranging from 56.2 % to 76.3 % inhibition of epileptic seizures in mice, where as the standard drug Phenytoin showed 83.95 % inhibition of epileptic seizures in mice. The compound iiih4 from each group was found to be nearly potent to Phenytoin which is used as standard drug. Anti-inflammatory activity ranging from 31.09 to 63.11 % inhibition of rat paw edema volume after 3 hours, whereas the standard drug Indomethacin showed 62.06 % inhibition of rat paw edema volume after 4 hours.  The compound iiih3 was found to be nearly more potent then indomethacin which is used as standard drug Keywords: Isatin; Schiff bases; Anti convulsant activity; Anti-inflammatory activity; Isatin.


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.


1996 ◽  
Vol 24 (01) ◽  
pp. 31-36 ◽  
Author(s):  
Chun-Ching Lin ◽  
Den-En Shieh

Five extracts (n-hexane, chloroform, ethyl acetate, n-butanol and water) of Scutellaria rivularis Benth. were evaluated for their anti-inflammatory activity against carrageenan-induced paw edema in rats and compared with indomethacin. The result indicated that chloroform extract proved to be the most effective in all of the extracts. Consequently, three major components (baicalin, baicalein and wogonin) of the chloroform extract were further tested for their anti-inflammatory activity using the same model. It was found that baicalin exhibits the greatest inhibition activity against carrageenan-induced rat paw edema.


2011 ◽  
Vol 76 (8) ◽  
pp. 1057-1067 ◽  
Author(s):  
Sadaf Gilani ◽  
Suroor Khan ◽  
Ozair Alam ◽  
Vijender Singh ◽  
Alka Arora

A series of thiazolidin-4-one (2a-h, 3a-h), azetidin-2-one (4a- h) and 1,3,4-oxadiazole (5a-h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. The structures of the new compounds were supported by their IR, 1H-NMR and mass spectral data. All compounds were evaluated for their anti-inflammatory activity by the carrageenan-induced rat paw edema test method. Eleven of the new compounds, out of 32, showed very good anti-inflammatory activity in the carrageenan-induced rat paw edema test, with significant analgesic activity in the tail immersion method together with negligible ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde content (MDA), which is one of the by-products of lipid peroxidation. The study showed that the compounds inhibited the induction of gastric mucosal lesions and it can be suggested from the results that their protective effects may be related to inhibition of lipid peroxidation in the gastric mucosa.


2011 ◽  
Vol 6 (10) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Andrea Maxia ◽  
Cinzia Sanna ◽  
Maria Assunta Frau ◽  
Alessandra Piras ◽  
Manvendra Singh Karchuli ◽  
...  

The topical anti-inflammatory activity of essential oil of Pistacia lentiscus L. was studied using carrageenan induced rat paw edema and cotton pellet induced granuloma. The effect on serum tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in rats inserted with cotton pellet was also investigated. On topical application, the oil exhibited a significant decrease in paw edema. The oil also inhibited cotton pellet-induced granuloma, and reduced serum TNF-α and IL-6. It can be concluded that the essential oil of Pistacia lentiscus reduces leukocyte migration to the damaged tissue and exhibits anti-inflammatory activity.


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