scholarly journals EVALUATION OF ANTIHYPERLIPIDEMIC, ANTI-INFLAMMATORY, AND ANALGESIC ACTIVITIES OF EURYCOMA LONGIFOLIA IN ANIMAL MODELS

Author(s):  
Phebe Hendra ◽  
Fenty . ◽  
Putu Ririn Andreani ◽  
Bernadetha Maria Estika Pangestuti ◽  
Jeffry Julianus

Objective: To investigate the antihyperlipidemic, anti-inflammatory and analgesic properties of of E. longifolia root extract in animal models.Methods: In this study, glucose-fructose enriched diet-induced hyperlipidemia, carrageenan-induced paw edema and acetic acid-induced writhing were used to evaluate the anti-hypertriglyceridemia, anti-inflammatory and analgesic activities, respectively. At the end of the experiment of glucose-fructose enriched diet-induced hyperlipidemia, blood samples were collected and estimation of blood lipids were carried out. Edema thickness was measured using digital caliper at 0, 15, 30, 45, 60, 90, 120, 150, 180, 210, 240, 270, 300, 330, and 360 min after carrageenan injection. The number of abdominal writhing for each mouse was observed and counted during a period of 1 h post injection of acetic acid.Results: E. longifolia root extract demonstrated a significant reduction of triglyceride levels (p<0.05) compared with the control group in glucose-fructose enrich diet in rats. In anti-inflammatory test, the extract significantly inhibited the carrageenan induced paw edema formation (p<0.05). The extract also significantly decreased the number of writhing in acetic acid-induced mice (p<0.05).Conclusion: E. longifolia root extract shown a significant anti-hypertriglyceridemia, anti-inflammatory and analgesic activities. Further studies are needed to determine mechanisms for its acitivities of E. longifolia root extract.

Biomedicines ◽  
2021 ◽  
Vol 9 (7) ◽  
pp. 716
Author(s):  
Oksana Sintsova ◽  
Irina Gladkikh ◽  
Anna Klimovich ◽  
Yulia Palikova ◽  
Viktor Palikov ◽  
...  

Currently the TRPV1 (transient receptor potential vanilloid type 1) channel is considered to be one of the main targets for pro-inflammatory mediators including TNF-α. Similarly, the inhibition of TRPV1 activity in the peripheral nervous system affects pro-inflammatory mediator production and enhances analgesia in total. In this study, the analgesic and anti-inflammatory effects of HCRG21, the first peptide blocker of TRPV1, were demonstrated in a mice model of carrageenan-induced paw edema. HCRG21 in doses of 0.1 and 1 mg/kg inhibited edema formation compared to the control, demonstrated complete edema disappearance in 24 h in a dose of 1 mg/kg, and effectively reduced the productionof TNF-α in both doses examined. ELISA analysis of blood taken 24 h after carrageenan administration showed a dramatic cytokine value decrease to 25 pg/mL by HCRG21 versus 100 pg/mL in the negative control group, which was less than the TNF-α level in the intact group (40 pg/mL). The HCRG21 demonstrated potent analgesic effects on the models of mechanical and thermal hyperalgesia in carrageenan-induced paw edema. The HCRG21 relief effect was comparable to that of indomethacin taken orally in a dose of 5 mg/kg, but was superior to this nonsteroidal anti-inflammatory drug (NSAID) in duration (which lasted 24 h) in the mechanical sensitivity experiment. The results confirm the existence of a close relationship between TRPV1 activity and TNF-α production once again, and prove the superior pharmacological potential of TRPV1 blockers and the HCRG21 peptide in particular.


2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Brian Muyukani Wangusi ◽  
Laetitia Wakonyu Kanja ◽  
Isaac Mpapuluu Ole-Mapenay ◽  
Jared Misonge Onyancha

Maerua triphylla root extracts are used by Maasai and Kikuyu communities in Kenya to manage headaches, stomachaches, migraines, and rheumatism. However, scientific data on their safety and efficacy are limited. The current study aims to investigate the safety, phytochemical constituents, analgesic, and anti-inflammatory activities of M. triphylla root extracts. Aqueous and methanol M. triphylla root extracts were prepared by cold maceration, and the extracts’ safety was evaluated using Wistar rats according to the Organization for Economic Cooperation and Development (2008) guidelines. Standard qualitative phytochemical screening methods were used for the detection of various phytochemical groups in the extracts. Analgesic activity assay in Swiss albino mice was done using the acetic acid-induced writhing test, while anti-inflammatory activity was determined in Wistar rats using the acetic acid-induced paw edema method. The methanol and aqueous extracts revealed LD50 > 2000 mg/kg bw, classifying them as nontoxic. The presence of cardiac glycosides, flavonoids, alkaloids, and phenols was observed in both extracts. However, saponins were only present in the methanol extract. In the analgesic study, mice that received 100 mg/kg bw and 500 mg/kg bw of aqueous root extract of M. triphylla had significantly lower acetic acid-induced writhing than mice that received acetylsalicylic acid 75 mg (reference drug) ( p < 0.05 ). Additionally, mice that received 500 mg/kg bw of methanol root extract of M. triphylla had significantly lower acetic acid-induced writhing than mice that received the acetylsalicylic acid 75 mg ( p < 0.05 ). In the anti-inflammatory study, there was no significant difference ( p < 0.05 ) between the inhibitory activity of different doses of the aqueous root extract of M. triphylla and a 50 mg/kg dose of diclofenac sodium (reference drug) on acetic acid-induced paw edema in rats. Moreover, there was no significant difference in the inhibitory activity of 100 mg/kg bw and 500 mg/kg bw doses of the methanol root extract of M. triphylla and a 50 mg/kg dose of diclofenac sodium on acetic acid-induced paw edema ( p > 0.05 ). These findings suggest that the roots of M. triphylla may be useful in the safe mitigation of pain and inflammation and therefore support their ethnomedicinal use in the management of pain and inflammation.


Author(s):  
Mavuto Gondwe ◽  
Anda Mpalala ◽  
Lusanda Zongo ◽  
David Kamadyaapa ◽  
Eugene Ndebia ◽  
...  

Objective: The objective of the study was to evaluate the anti-inflammatory and antinociceptive effects of Artemisia afra.Methods: Animals were randomly divided into five groups of six animals each and administered with normal saline (2 ml/kg), indomethacin (10 mg/ kg), and A. afra at doses of 100, 200, and 400 mg/kg, respectively. For the anti-inflammatory activity, carrageenan-induced paw edema was used while the hot plate and acetic acid induced-writhing tests were used to assess the antinociceptive activity.Results: Pretreatment with A. afra at a dose of 100 mg/kg did not show any significant biological effects (p>0.05) for any of the three tests, when compared against saline-treated control group. At a dose of 200 mg/kg, A. afra demonstrated significant effects (p<0.01), during the 5th h reducing carrageenan-induced paw edema by 12%. The highest dose (400 mg/kg) of A. afra demonstrated more potent effects by decreasing the carrageenan-induced paw swelling (p<0.001–0.05) during the 3rd, 4th, and 5th h, by up to 38% when compared against saline-treated control group. Both the 200 and 400 mg/kg, A. afra doses achieved a significant increase (p<0.05) in reaction time in the hot plate test. In the acetic acid-induced writhing test, pretreatment with A. afra (400 mg/kg) significantly reduced pain by 39% (p<0.01) by comparison with the saline control.Conclusion: Experimental data demonstrated that aqueous extract of A. afra possesses anti-inflammatory and antinociceptive properties in experimental acute inflammation and pain. These findings support the usage of A. afra in managing inflammation and pain in traditional practice.


The synthesis of new NSAIDs with improved efficacy and selectivity towards COX2, which encouraged by the various biological activities of 1,2,4-triazoles and 1,3,4-thiadiazoles. In this experiment, the production of 1,2,4-triazolothiadiazoles derivatives from Ibuprofen, Naproxen and Indomethacin. We have enhanced anti-inflammatory and analgesic activities by conventional method and microwave-assisted technique, and then compare the time consuming by reaction and yield percent of the product in both way, besides evaluation of anti-inflammatory action of the target compounds by pharmacological test with predictable selectivity towards COX-2 enzyme. Synthesis of the target compounds (P1a-3b, N1a-3b and I1a-3b) has been successfully accomplished by checking purity, characterization, also identification of the synthetic compounds which detected by estimation of physical properties, FT-IR and ¹H-NMR spectroscopy. In vivo potent anti-inflammatory activity of the ending compounds is evaluating in rats utilizing egg-white prompted edema model of inflammation. The experienced compounds (P1a-3b, N1a-3b and I1a-3b) and the reference drugs (Ibuprofen, Naproxen and Indomethacin) produced significant reduction in paw edema in compare to the effect of control group. Wholly tested compounds produced considerable decrease of paw edema in contrast to control group. However, compounds (P3b, N3b and I1b) have considerable more paw edema declining than Ibuprofen, Naproxen and Indomethacin. Intermediate and target compounds are synthesis by microwave method have better result by time and yield in compare with conventional way. The synthesized compounds (Pa1-3b and N1a-3b) may exhibit expected selectivity towards COX-2 enzyme properly due to their large size than its parent Ibuprofen, Naproxen.


2019 ◽  
Vol 3 (2) ◽  
pp. 112-116
Author(s):  
Samuel O. Onoja ◽  
Glory C. Onyebuchi ◽  
Ifeoma I. Ijeh ◽  
Maxwell I. Ezeja

AbstractThis study evaluate the anti-inflammatory and analgesic properties ofHelianthus annuusLinn. in rats. Methanol extract ofHelianthus annuus(HAE) leaf was used in this study. Formalin- and egg-albumin induced-paw edema were used to investigate the anti-inflammatory activities while acetic acid-induced writhing reflex and tail flick models were used to evaluate the analgesic properties. The doses of HAE used were 150, 300 and 600 mg/kg. Acetylsalicylic acid (ASA) was used as reference drug in the anti-inflammatory and writhing reflex models while pentazocine (reference drug) was used in tail flick model. The negative control was dosed 5% tween-20 (10 ml/kg). The HAE exhibited significant (P < 0.05) dose-dependent anti-inflammatory and analgesic activities. At 3 hour (h) post treatment, the HAE (300 mg/kg) produced 33.33% and 32.94% while ASA produced 36.36% and 35.29% reduction in paw volume in the formalin and egg-albumin induced paw edema models respectively when compared with negative control. In the acetic acid-induced writhing reflex, ASA and HAE (600 mg/kg) produced 67.89% and 35.78% reduction in the number of writhing, respectively when compared with the negative control. Pentazocine and HAE (300 mg/kg) caused 67.62% and 35.24% increase in pain reaction time when compared with the negative control. The study affirms the folkloric uses ofHelianthus annuusin the management of pain and inflammation.


2021 ◽  
Author(s):  
H. Shafaroodi ◽  
J. Asgarpanah ◽  
J. Asgarpanah

Ferula stenocarpa is an aromatic herb whose fruits are widely used in Persian traditional medicine as a painkiller and to relive inflammation-based disorders. Considering the higher content of essential oil in the fruits, the oil’s anti-inflammatory and analgesic activities were investigated in an animal model in vivo. The analgesic effect of Ferula stenocarpa fruits essential oil was evaluated via testing the writhing triggered by acetic acid examination and hot plate technique. Moreover, the acute anti-inflammatory effects were studied through the paw edema triggered in mice. Using 20 and 40 mg/kg of the oil revealed an analgesic impact considering the increment in the reaction time needed for the hot plate approach. Furthermore, all examined doses of the oil caused a reduction in the frequency of writhes in the mice. It was observed that the oil (40 mg/kg) followed by 10 and 20 mg/kg caused inflammatory reduction. The findings indicated that the oil may possess significant activities against acute inflammation. It had both peripheral and central pain-killing impacts. α-Pinene (43.1%) and β-pinene (22.9%) as the main constituents of the oil, can be considered as the responsible compounds to manage inflammation and pain.


Author(s):  
KOUAME DJÈ KOUAMÉ WENCESLAS ◽  
N’DIA KOUADIO FRÉDÉRIC ◽  
KOUAKOU KOUAKOU LÉANDRE ◽  
YAPO ANGOUÉ PAUL

Objective: Justicia flava is a plant commonly used in traditional medicine for the treatment of frictions, convulsions, body aches, pains, and fever. The aim of this study was to determine the anti-inflammatory properties of an aqueous extract of J. flava (AEJf) in rats. Methods: Thus, 36 rats were divided into six groups of six rats each for each test. Acute anti-inflammatory activity was evaluated by induction of plantar edema following injections of egg albumin, carrageenan, or histamine. AEJf and aspirin (100 mg/kg bw) were orally administered to rats with doses ranged from 62.5 to 500 mg/kg bw before (preventive study) and after (curative study) the induction of edema. The rat’s paw edema was measured using a digital caliper thereafter. For a sub-chronic anti-inflammatory activity, sterilized cotton pellets (20±0.5 mg) were implanted in the anterior dorsal region for granuloma formation. Animals received the different doses of AEJf (62.5–500 mg/kg bw) for 7 days and on the 8th day, cotton pellets were removed and weighed, dried, and weighed again. Results: The results of the oral administration of AEJf at doses of 62.5, 125, 250, and 500 mg/kg bw to rats showed similar acute anti-inflammatory properties such as aspirin (100 mg/kg bw) on carrageenan (1%), fresh egg albumin, and histamine injection-induced rats’ paw edema. AEJf caused 77.63% (preventive study) and 28.1% (curative study) inhibitions of carrageenan (1%) solution-induced paw edema and 61% (preventive study) and 29.62% (curative study) inhibitions of fresh egg albumin-induced paw edema. AEJf also inhibited histamine-induced edema (1 mg/mL) by 83.67% compared to the control group. AEJf significantly reduced the weight of granuloma tissue elicited by the insertion of sterile cotton pellets from 34.53 to 46.98% for wet cottons and from 45.73 to 59.45% for dry cottons. Conclusion: AEJf possessed anti-inflammatory activity on acute and sub-chronic inflammations in rats.


Author(s):  
Samira Salem ◽  
Essaid Leghouchi ◽  
Rachid Soulimani ◽  
Jaouad Bouayed

Abstract. Paw edema volume reduction is a useful marker in determining the anti-inflammatory effect of drugs and plant extracts in carrageenan-induced acute inflammation. In this study, the anti-inflammatory effect of Lobaria pulmonaria (LP) and Parmelia caperata (PC), two lichen species, was examined in carrageenan-induced mouse paw edema test. Compared to the controls in carrageenan-induced inflammation (n = 5/group), our results showed that pretreatment by single oral doses with PC extract (50–500 mg/kg) gives better results than LP extract (50–500 mg/kg) in terms of anti-edematous activity, as after 4 h of carrageenan subplantar injection, paw edema formation was inhibited at 82–99% by PC while at 35–49% by LP. The higher anti-inflammatory effect of PC, at all doses, was also observed on the time-course of carrageenan-induced paw edema, displaying profile closely similar to that obtained with diclofenac (25 mg/kg), an anti-inflammatory drug reference (all p < 0.001). Both LP and PC, at all doses, significantly ameliorated liver catalase (CAT) activity (all p < 0.05). However, superoxide dismutase (SOD) activity, glutathione peroxidase (GPx) activity and glutathione (GSH) levels were found increased in liver of PC- compared to LP-carrageenan-injected mice. Our findings demonstrated on one hand higher preventive effects of PC compared to LP in a mouse carrageenan-induced inflammatory model and suggested, on the other hand, that anti-inflammatory effects elicited by the two lichens were closely associated with the amelioration in the endogenous antioxidant status of liver.


2019 ◽  
Author(s):  
A. EL Moussaoui ◽  
F. Jawhari ◽  
K. EL Ouahdani ◽  
I. Es-Safi ◽  
D. Bousta ◽  
...  

Our present study focuses on the evaluation of the analgesic, anti-inflammatory and healing activity of Withania frutescens L. The anti-inflammatory result has an inhibition percentage of 78.87% ± 7.08 at 450 mg/kg and 75.14% ± 6.39 at 400 mg/kg and 89.75% ± 3.44 for diclofenac (1%). When applied locally, the 10% cream has an inflammation inhibition of 96.87% ± 5.85 and 76.14% ± 7.88 for the 5% cream with 89.87 ± 6.20 of reference (Indomethacin). The abdominal contractions of rats treated with the root extract are significantly lower than those of the control group that received only physiological NaCl solution, with 41.20 ± 2.30 for the extract and 82.20 ± 5.04 for NaCl and 53.40 ± 4.94 for the reference. The healing activity of the studied extract records a percentage of contraction of about 93.20% ± 3.36 (Extract 10%), 84.50% ± 3.84 (Extract 5%), 48.47% ± 2.15 (control) and 81.88 ± 2.24 for the reference.


2019 ◽  
Vol 16 (10) ◽  
pp. 1157-1166
Author(s):  
Rodrigo César da Silva ◽  
Fabiano Veiga ◽  
Fabiana Cardoso Vilela ◽  
André Victor Pereira ◽  
Thayssa Tavares da Silva Cunha ◽  
...  

Background: : A new series of O-benzyloximes derived from eugenol was synthesized and was evaluated for its antinociceptive and anti-inflammatory properties. Methods: : The target compounds were obtained in good global 25-28% yields over 6 steps, which led us to identify compounds (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-(4- (methylthio)benzyloxime (8b), (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- bromobenzyloxime (8d) and (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- (methylsulfonyl)benzyloxime (8f) as promising bioactive prototypes. Results:: These compounds have significant analgesic and anti-inflammatory effects, as evidenced by formalin-induced mice paw edema and carrageenan-induced mice paw edema tests. In the formalin test, compounds 8b and 8f evidenced both anti-inflammatory and direct analgesic activities and in the carrageenan-induced paw edema, with compounds 8c, 8d, and 8f showing the best inhibitory effects, exceeding the standard drugs indomethacin and celecoxib. Conclusion: : Molecular docking studies have provided additional evidence that the pharmacological profile of these compounds may be related to inhibition of COX enzymes, with slight preference for COX-1. These results led us to identify the new O-benzyloxime ethers 8b, 8d and 8f as orally bioactive prototypes, with a novel structural pattern capable of being explored in further studies aiming at their optimization and development as drug candidates.


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