scholarly journals In vivo and in silico evaluation of analgesic activity of Lippia alba

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Md. Abdullah Aziz ◽  
Manna Mehedi ◽  
Mst. Irin Akter ◽  
Sadiur Rahman Sajon ◽  
Kishor Mazumder ◽  
...  

Abstract Background This study was conducted to evaluate the analgesic activity of different extracts of Lippia alba (L. alba) along with in silico evaluation of analgesic activity of the isolated compounds from L. alba against cyclooxygenase-2 enzyme and ADME/T analysis of isolated compounds. Method In vivo analgesic activity of different extracts of L. alba was evaluated by acetic acid-induced writhing, tail immersion and hot plate on Swiss albino mice of either sex. In silico activity of the isolated compounds and ADME/T analysis were performed by Schrödinger-Maestro (Version 10.1) and OSIRIS Data warrior (version 4.6.1) softwares. Results Three different extracts (Methanolic extract: ME; Petroleum ether extract: PEE; Dichloromethane extract: DCME) of 250 mg/kg and 500 mg/kg doses were used in the experiments to evaluate analgesic activity. In acetic acid-induced writhing test, significant results were seen for PEE (500 mg/kg) and DCME (500 mg/kg), which were 53.09 ± 2.87 & 50.09 ± 4.24%, respectively. In tail immersion test, the best latency time was found at + 60 min for PEE (500 mg/kg) which is (5.65 ± 0.25) sec. For hot plate test, DCME at a dose 500 mg/kg showed the highest increase in latency time, which was 13.48 ± 0.33 s. In the case of in silico evaluation of analgesic activity, the compounds such as geranial, neral, (E)-caryophyllene, caryophyllene oxide, mussaenide, and 8-epi-loganin meet the condition of Lipinski’s rule of five. Among these safe compounds, 8-epi-loganin showed the best docking score of − 8.17 kcal/mol against cyclooxygenase-2 enzyme (PDB ID: 6COX), which was almost similar to that of the standard drug, Celecoxib (− 11.11 kcal/mol). Conclusion In conclusion, L. alba can be a potent source of analgesic medicine and further modification and simulation studies are required to establish the effectiveness of 8-epi-loganin.

Author(s):  
DHARMA RAJ MARASINI ◽  
JITENDRA PANDEY ◽  
LAXMAN PAUDEL SHARMA ◽  
LAXMI PAUDEL ◽  
ROSHNI GYAWALI ◽  
...  

Objective: Because of adverse side effects, caused by NSAIDs, tolerance, and dependence induced by opiates, the use of these analgesic agents has not been successful in all cases. Therefore, alternative analgesic drugs from plant sources are the new target now days. The objective of this study was to evaluate the analgesic activity of ethanolic extracts of stem barks and leaves of Ficus religiosa. Methods: The analgesic activity of ethanolic extract of stem barks and leaves was evaluated in the Swiss albino mice model using acetic acid-induced writing response and Eddy’s hot plate method. Analgesic activity was demonstrated with the percentage inhibition of acetic acid induced writings and the percentage increased in latency time of paw licking. The potency of test extracts was compared with standard drug, Diclofenac. Results: Ethanolic extract of leaves and bark of F. religiosa showed potential analgesic activity from both methods. From Eddy’s hot plate model, it was observed that the percentage of increased latency time at 90 min by ethanolic extract of leaves and stem bark was found to be 70.81 % (8.54 min) and 70.78 % (8.53 min) respectively at a dose of 400 mg/kg. Both of these results are statistically significant (p<0.05) as compared to the test group. Furthermore, both of these extracts showed the dose-dependent and time-dependent increased in latency time and these results are compared to that of standard drug Diclofenac. Similarly, ethanolic extract of leaves and stem at 400 mg/kg significantly inhibited the number of writhings induced by acetic acid. The percentage inhibition of writhings by ethanolic extract of leaves at a dose of 400 mg/kg was 68.47 % which was similar to that of standard drug Diclofenac (68.47 %). However, ethanolic extract of bark showed relatively lower percentage inhibition (60.79 %) as compared to leaf extract and standard, but the result was significant as compared to that of the test group (p<0.05). Conclusion: Ethanolic extracts of F. religiosa stem bark and leaf possess both central and peripheral analgesic properties and these effects may be beneficial for the management of pain.


Author(s):  
FREDDY TEILANG NONGKHLAW ◽  
MALSAWMTLUANGI C ◽  
PHAIBIANG LAPASAM ◽  
ANDREW LALTHASANGA

Objective: The present study was undertaken to screen the analgesic and the antidepressant activity of Gaultheria fragrantissima Wall. an ethnomedicinal plant of Meghalaya, India. Methods: In this study, the analgesic effect was induced by hot plate method and tail immersion test. The analgesic effect of two doses of the methanolic extract of Gaultheria fragrantissima Wall. was tested and diclofenac was used as a standard drug. The antidepressant activity was brought about by force swimming test and tail suspension test. The antidepressant effect of two doses of the methanolic extract of G. fragrantissima Linn. was tested and imipramine was used as a standard drug. The statistical analysis was carried out by one-way analysis of variance (ANOVA) followed by Tukey-Kramer multiple comparison tests using GraphPad InStat 3.0 software. Results: The analgesic study shows that the plant extract at two different doses (200 mg/kg and 400 mg/kg) possesses significant analgesic activity (p<0.01), whereby the two different doses of the plant extract showed a significant increase in the latency time were obtained at 120 min in hot plate method and increase in the latency time were obtained at 90 min in the tail immersion method, respectively. The antidepressant study shows us that the methanolic extract at 200 and 400 mg/kg produced significant reduction (p<0.001) in the immobility period when compared with that of control group animals in both the tests. Conclusion: The result of the study shows that the methanolic bark extract of G. fragrantissima Wall. possesses analgesic activity and antidepressant activity.


2013 ◽  
Vol 24 (1) ◽  
pp. 5-12
Author(s):  
Abhishek Tiwari ◽  
Anita Singh

AbstractIn the present synthesis a series of 1-(1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)-2-substituted phenylpyrazolidine-3,5-diones were prepared. By the reaction of N-methylbenzenamine with diethyl malonoate 4-hydroxy-1-methylquinolin-2(1H)-one were prepared, which on treatment with posphoryl chloride converted into 4-chloro-1-methylquinolin-2(1H)-one. Subsequently with substituted phenyl hydrazines 1-methyl-4-(2- substitutedphenylhydrazinyl)quinolin-2(1H)-one were obtained, which on reaction with diethyl malonate gave 1- (1-methyl-2-oxo-1,2-dihydroquinolin-4-yl)-2-substituted phenylpyrazolidine-3,5-diones. All structures were characterized by IR, 1HNMR & mass spectrometry. Further all the synthesized compounds were evaluated for their anti-nociceptive activity in mice by Eddy’s hot plate and acetic acid induced writhing response. All compounds have shown the activity. In hot plate model compounds QAA-04c and QAA-04d have given more activity than standard, whereas in case of acetic acid induced writhing model compounds QAA-04a and QAA- 04d have given significant analgesic activity which is comparable with the standard drug. Compound QAA-04b has shown least analgesic activity. Compound QAA-04a was almost equal in activity to the standard drug diclofenac sodium and was considered as the lead molecule.


2021 ◽  
Vol 50 (3) ◽  
pp. 577-583
Author(s):  
Rahma Hamayun ◽  
Muhammad Shahid Iqbal ◽  
Muhammad Imran Qadir

Analgesic, anti-inflammatory and anti-pyretic activities of n-hexane and aqueous ethanolic extracts of Malva neglecta in Swiss albino mice was evaluated. For each activity, the mice were divided into 4 groups: Group 1 served as control, Groups 2 and 3 were given n-hexane and aqueous ethanol extracts, respectively whereas Group 4 was treated with the standard drug. Analgesic activity was evaluated against acetic acid induced writhing, Eddy's hot plate method, and Formalin induced paw licking. Anti-inflammatory activity was evaluated by carrageenan-induced paw edema. The extracts were also examined for their anti-pyretic activities against yeast-induced pyrexia. Results showed that the n-hexane (p < 0.05) and aqueous ethanolic (p < 0.005) extracts of M. neglecta exhibited analgesic activity by reducing acetic acid-induced writhing, mean reaction time on hot plate model and formalin-induced paw licking in mice as compared to the control. The n-hexane extract (p < 0.05) as well as aqueous ethanolic (p < 0.005) extracts produced significant antiinflammatory activity as compared to the control. Both the n-hexane and aqueous ethanolic extracts revealed significant antipyretic activity (p < 0.005 and p < 0.05, respectively) in mice model. The results of the present study demonstrated that the n-hexane and aqueous ethanol extracts of M. neglecta possess analgesic, antiinflammatory and anti-pyretic activities. Bangladesh J. Bot. 50(3): 577-583, 2021 (September)


2016 ◽  
Vol 5 (4) ◽  
pp. 38-40 ◽  
Author(s):  
Rubab Tarannum Islam ◽  
Ahmed Tanjimul Islam ◽  
Mir Monir Hossain ◽  
Kishor Mazumder

The sunflower seed is the seed of the sunflower (Helianthus annuus). The methanol extract of seeds of Helianthus annuus were screened for analgesic activity in mice model to systematically explore the medicinal values of the plant. Acetic acid induced writhing and hot plate methods were used to confirm the central and peripheral analgesic action. In case of acetic acid-induced writhing test the extract showed significant (P <0.05) analgesic potential at doses 100 and 200 mg/kg body weight (50.35 and 57.85% inhibition, respectively). In the hot plate method, increase (p < 0.05) of latency period was also observed in comparison to standard aspirin. At 60 minutes, the latency period of two different doses (100 and 200 mg/kg body weight) was found at 13 ± 0.91 and 16.5 ± 1.55 second. The results obtained support the use of Helianthus annuus seeds in painful conditions acting both centrally and peripherally.Islam et al., International Current Pharmaceutical Journal, March 2016, 5(4): 38-40http://www.icpjonline.com/documents/Vol5Issue4/02.pdf


Author(s):  
SATHIYA VINOTHA AT ◽  
UMAMAGESWARI MS ◽  
UMAMAHESWARI A ◽  
VELARUL S

Objective: Plumeria alba (Apocynaceae), commonly known as “Frangipani” is an important medicinal plant, widely distributed throughout Southern India. In the traditional medicinal system, different parts of this plant have been mentioned to be useful in a wide variety of diseases. In this study, analgesic activity of aqueous and alcoholic extract of flowers of P. alba Linn was evaluated by hot-plate and acetic acid-induced writhing methods to substantiate and expand its clinical applications. Methods: The flowers of P. alba were collected from the local area in and around Coimbatore (India). The flowers were dried, powdered, and were extracted using soxhlet apparatus for 12 h using water and 95% of ethanol as a solvent. The test extracts were administered orally at a dose of 100 & 200 mg/kg while diclofenac sodium (10 mg/kg) served as standard. Results: The ethanolic flower extract of 200 mg/kg had significant analgesic activity in acetic acid-induced abdominal writhing response (***p<0.001) when compared to control and standard drug diclofenac. It also exhibited significant analgesic activity (***p<0.001) by increasing the pain reaction time of the rats in comparison to control and standard in hot plate method. Conclusion: The results suggest that ethanolic flower extracts of P. alba possess potent analgesic properties, which support its use in traditional medicine and suggesting that the plant should be further investigated for its pharmacological active natural products.


2018 ◽  
Vol 4 (1) ◽  
pp. 22-24
Author(s):  
Pankaj Jain ◽  
◽  
Sonika Jain ◽  
Surendra Kumar Swarnkar ◽  
Swapnil Sharma ◽  
...  

Aim: The present study evaluated the central and peripheral analgesic activity of methanolic leaf extract of Phoenix sylvestris (PSLME) in swiss albino mice. Method: Peripheral and central analgesic activity was evaluated by tail immersion and acetic acid writhing in swiss albino mice. Dextropropoxyphene was used as a standard drug in the dose of 65mg/kg body weight in both models. PSLME was tested at 100 and 500mg/kg dose level. Results: The result revealed that methanolic extract exhibit 48% and 40.5% writhing inhibition at 500 and 100 mg/kg doses whereas ~30% tail withdrawal reflexes inhibition at 500mg/kg which was analogous to the standard drug dextropropoxyphene. Conclusion: Methanolic extract of leaves of P. sylvestris possesses both peripheral and central analgesic activity in experimental animal.


Author(s):  
Bosco Lawarence ◽  
Murugan K

Objective: The objective of the present work is to isolate, purify, and fractionate anthocyanin from selected Osbeckia species and also to compare the analgesic and anti-inflammatory potentiality using animal models.Methods: Methodologies include extraction of anthocyanin from the in vitro callus culture of Osbeckia aspera and Osbeckia reticulata, purification using amberlite column chromatography, and fractionation by liquid chromatography-tandem mass spectrometry. The analgesic activity was determined by tail immersion method, analgesy meter, hot plate, and acetic acid-induced writhing test. Anti-inflammatory activity was evaluated by carrageenan-induced paw inflammation in mice.Results: Anthocyanin-producing callus cultures were established in MS medium fortified with various combinations of phytohormones and sucrose. Optimal callus formation in O. aspera was initiated on cultures containing 0.5 mg/L of 2, 4-D, and 0.5 mg/L 6-benzylaminopurine (BA). In O. reticulata callus was initiated in the presence of 1.2 mg/L BA and 1.4 mg/L naphthalene acetic acid. The same hormonal combination on extended treatments turned the white friable callus into red compact callus. Anthocyanins obtained from Osbeckia species were purified and fractionated containing malvidin-3-diglucoside, delphinidin, cyanidin aglycone, and peonidin. Purified anthocyanin of O. aspera at the concentrations 50, 100, 150, and 200 mg/kg after 120 min exhibited significant analgesic activity by tail immersion method, in comparison to O. reticulata. However, with hot plate method, anthocyanin of O. reticulata produced a significant analgesic activity even at lower doses (50 and 100 mg/kg) after 120 min. However, in writhing test, theepurified anthocyanin of O. aspera significantly stopped the number of writhes at a dose of 200 mg/kg and also by the anthocyanin of O. reticulata. In the evaluation of anti-inflammatory effect using plethysmometer, anthocyanin at doses of 100,150 and 200 mg/kg started producing anti-inflammatory effect after 30 min, which lasted until 120 min.Conclusion: It is concluded from the present study that the purified anthocyanin of Osbeckia possesses potent analgesic and anti-inflammatory activities.


2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Amjad Ali ◽  
Abdul Nasir ◽  
Syed Wadood Ali Shah ◽  
Atif Ali Khan Khalil ◽  
Mi-jeong Ahn ◽  
...  

Abstract Background In order to find a new natural resource for pain-relief, the analgesic effects of Ilex dipyrena crude extract, fractions, and subfractions were evaluated in in-vivo mouse models with possible mechanism of action. Methods Analgesic effects of crude extract (100 and 200 mg/kg body weight), fractions and subfractions (75 mg/kg body weight) were screened using heat-induced (tail-immersion and hot plate test) and chemical-induced (formalin and acetic acid) nociception models in mice. The samples were also tested for the elucidation of a possible mechanism through opioidergic and GABAergic systems. Results The administration of crude extract, fractions and subfractions produced analgesic responses in acetic acid, formalin, tail immersion, and hot plate model for pain similar to those obtained with the standard. Naloxone antagonized the antinociceptive effects of the tested samples, whereas bicuculline showed partial inhibition. Considering the analgesic response, crude extract, fractions, and subfractions demonstrated promising inhibitory activity against all test models for pain, which was further supported by the possible involvement of opioidergic and GABAergic systems. Conclusion The results suggest that this plant may be useful in the development of new analgesic drugs. Further research with regard to the isolation of bioactive compounds is required to verify these findings.


Author(s):  
Bosco Lawarence ◽  
Murugan K

Objective: The objective of the present work is to isolate, purify, and fractionate anthocyanin from selected Osbeckia species and also to compare the analgesic and anti-inflammatory potentiality using animal models.Methods: Methodologies include extraction of anthocyanin from the in vitro callus culture of Osbeckia aspera and Osbeckia reticulata, purification using amberlite column chromatography, and fractionation by liquid chromatography-tandem mass spectrometry. The analgesic activity was determined by tail immersion method, analgesy meter, hot plate, and acetic acid-induced writhing test. Anti-inflammatory activity was evaluated by carrageenan-induced paw inflammation in mice.Results: Anthocyanin-producing callus cultures were established in MS medium fortified with various combinations of phytohormones and sucrose. Optimal callus formation in O. aspera was initiated on cultures containing 0.5 mg/L of 2, 4-D, and 0.5 mg/L 6-benzylaminopurine (BA). In O. reticulata callus was initiated in the presence of 1.2 mg/L BA and 1.4 mg/L naphthalene acetic acid. The same hormonal combination on extended treatments turned the white friable callus into red compact callus. Anthocyanins obtained from Osbeckia species were purified and fractionated containing malvidin-3-diglucoside, delphinidin, cyanidin aglycone, and peonidin. Purified anthocyanin of O. aspera at the concentrations 50, 100, 150, and 200 mg/kg after 120 min exhibited significant analgesic activity by tail immersion method, in comparison to O. reticulata. However, with hot plate method, anthocyanin of O. reticulata produced a significant analgesic activity even at lower doses (50 and 100 mg/kg) after 120 min. However, in writhing test, theepurified anthocyanin of O. aspera significantly stopped the number of writhes at a dose of 200 mg/kg and also by the anthocyanin of O. reticulata. In the evaluation of anti-inflammatory effect using plethysmometer, anthocyanin at doses of 100,150 and 200 mg/kg started producing anti-inflammatory effect after 30 min, which lasted until 120 min.Conclusion: It is concluded from the present study that the purified anthocyanin of Osbeckia possesses potent analgesic and anti-inflammatory activities.


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