scholarly journals In vivo and in vitro pharmacological activities of Tacca integrifolia rhizome and investigation of possible lead compounds against breast cancer through in silico approaches

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Shahriar Ahmed ◽  
Ahmed Rakib ◽  
Md. Ashiqul Islam ◽  
Bibi Humayra Khanam ◽  
Farhana Binta Faiz ◽  
...  

Abstract Background The study was conducted to evaluate the analgesic, anti-inflammatory, antipyretic properties of ethanolic extract of Tacca integrifolia rhizome (EETI) in mice and cytotoxic effects in brine shrimp nauplii followed by a PASS prediction study for some isolated compounds of T. integrifolia. Additionally, this experiment included the in silico molecular docking and ADME/T property analyses of some phytochemicals. Methods Formalin- induced paw licking test and acetic acid-induced writhing test for analgesic activity, carrageenan-induced paw edema test for anti-inflammatory potential and Brewer’s yeast-induced pyrexia test for antipyretic activity were applied. Antinociceptive and antineoplastic activity for breast cancer were revealed with PASS program. Schrodinger suite 2015 was used to evaluate the binding interaction and ADME/T properties of selected phytoconstituents with estrogen receptor alpha. Results In formalin-induced paw licking test, EETI at the doses of 200 and 400 mg/kg BW showed highly significant inhibition of writhing in both neurogenic and inflammatory phases. While EETI also exhibited highly significant, compared to control, writhing inhibition for both the doses in acetic acid-induced writhing test. Moderate anti-inflammatory effect at a dose of 400 mg/kg BW was noticed in paw-edema test. It also showed 77.51% of maximum antipyretic effect which was significantly effective compared to standard drug paracetamol (150 mg/kg) in Brewer’s yeast-induced pyrexia test. The EETI showed potential cytotoxic activity with LC50 value of 114.46 μg/mL. The PASS prediction revealed the potential antinociceptive and antineoplastic activity of target compounds. The compounds betulinic acid, quercetin-3-α-arabinoside, catsanogenin were found to be effective in molecular docking study. Conclusion It is evident that the EETI possesses highly significant analgesic activity with remarkable anti-inflammatory and antipyretic activity. The phytoconstituents have potential antinociceptive and antineoplastic (breast cancer) activity. Graphical abstract

Author(s):  
Sarath Sasi Kumar ◽  
Anjali T

Objective: In silico design and molecular docking of 1,2-benzisoxazole derivatives for their analgesic and anti-inflammatory activity using computational methods.Methods: In silico molecular properties of 1,2-benzisoxazole derivatives were predicted using various software’s such as Chemsketch, Molinspiration, PASS and Schrodinger to select compounds having optimum drug-likeness, molecular descriptors resembling those of standard drugs and not violating the ‘Lipinski rule of 5’. Molecular docking was performed on active site of nicotinic acetylcholine receptor (PDB: 2KSR) for analgesic activity and COX-2 (PDB: 6COX) for anti-inflammatory activity using Schrodinger under maestro molecular modelling environment.Results: From the results of molecular docking studies of 1,2-benzisoxazole derivatives, all the compounds showed good binding interactions with Nicotinic acetylcholine receptor and COX-2. Compounds 4a and 4c showed highest binding scores (-7.46 and-7.21 respectively) with nicotinic acetylcholine receptor and exhibited maximum analgesic activity. Compound 4a showed highest binding score (-7.8) with COX-2 and exhibited maximum anti-inflammatory activity.Conclusion: All the derivatives of 1,2-benzisoxazole showed good analgesic and anti-inflammatory activity as predicted using molecular docking on respective receptors.


2019 ◽  
Vol 5 (1) ◽  
pp. 18-23
Author(s):  
Selina Kabir ◽  
Ronok Zahan ◽  
Abdullah Mohammad Sarwaruddin Chowdhury ◽  
Choudhury Mahmood Hasan ◽  
Mohammad Abdur Rashid

Background: Polyalthia simiarum (Hook. F. &Thomson) exhibits different effects in human body. Objective: As a part of ongoing research on medicinal plants of Bangladesh, the present study is focused to investigate the analgesic and anti-inflammatory activities of stem bark of Polyalthia simiarum (Annonaceae). Methodology: The ethyl acetate (EA) and petroleum ether (PE) extracts were subjected to qualitative chemical investigation for the identification of different phytoconstituents. The analgesic activity was determined for its central and peripheral pharmacological actions using tail immersion method and acetic acid-induced writhing test. The anti-inflammatory activity was evaluated by carrageenan induced paw edema in rats. Analgesic and anti-inflammatory data were evaluated statistically analysed by Dunnett’s-T test. Result: Both extracts at the dose of 50- and 100 mg/kg b.w., produced significant increase in pain threshold in tail immersion method whereas significantly reduced the writhing caused by acetic acid in a dose dependent manner. The EA and PE extracts showed anti-inflammatory activities at 50- and 100 mg/kg body weight. Among all the extracts, the EA extract showed a dose dependent and comparable analgesic activity in all the tested methods and also reduced the paw edema considerably (27.5% and 39.1% inhibition after 4h), in dose dependent manner when compared to carrageenan induced control rat. Conclusion: Therefore, the EA and PE extracts of Polyalthia simiarum were capable to exhibit moderate analgesic and anti-inflammatory activities. This is the first report of analgesic and anti-inflammatory potential of Polyalthia simiarum and can be further investigated to isolate the active compounds responsible for the biological activities. Journal of National Institute of Neurosciences Bangladesh, 2019;5(1): 18-23


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)


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.


Author(s):  
N. M. Mahmudul Alam Bhuiya ◽  
Mahmud Hasan ◽  
Zobaer Al Mahmud ◽  
Nazmul Qais ◽  
Mohammad Shah Hafez Kabir ◽  
...  

AbstractBackgroundThe objective of the study was to evaluate the antinociceptive, antipyretic and anti-inflammatory activities of ethanolic extract, methanolic extract andMethodsThe anti-nociceptive potentials of the extracts were studied using the acetic acid-induced writhing test in mice and the antipyretic activity was investigated using yeast-induced pyrexia in rats. Anti-inflammatory activity test was done on rats at a dose by using carrageenan-induced paw edema test.ResultsIn acetic acid-induced writhing inhibition study in Swiss albino mice, the crude methanolic extract at 200 mg/kg and 400 mg/kg doses and theConclusionsThis study thereby indicates that leaves of


2021 ◽  
Author(s):  
Nazma Shaheen ◽  
Afiatul Azam ◽  
Amlan Ganguly ◽  
Saeed Anwar ◽  
Md Sorwer Alam Parvez ◽  
...  

Black cumin (Nigella sativa) is a widely used ingredient of traditional medicine for its broad-spectrum pharmacological actions, including anti-allergic, bronchial asthma, and anti-inflammatory properties. We sought to evaluate BC extracts' efficacy for their anti-allergic and anti-inflammatory properties using a comprehensive in vitro, in vivo, and silico experimental setup. To investigate whether BC extract has anti-inflammatory, anti-allergic, and analgesic therapeutic potentials in vitro and in vivo. The activity of BC was assessed through anti-allergic activity on rat basophilic leukemia-2H3 cell line, anti-inflammatory activity on J774.1A cell line, anti-inflammatory activity by carrageenan-induced rat paw edema, analgesic activity by acetic acid-induced writhing test, and ingenuity analysis of the BC extracts in inflammation control. BC exerted potent anti-allergic activity by inhibiting antigen-induced degranulation. An anti-inflammatory effect is shown by inhibiting TNF-α pro-duction. The acetic acid-induced writhing test shown a dose-dependent reduction of writhing number following BC administration. Rat paw edema test shown the dose-dependent reduction of paw edema volume following BC administration. Ingenuity Pathway Analysis (IPA) suggested BC extracts containing ferulic acid, p-coumaric acid, kaempferol, and quercetin can inhibit inflammation. This study suggests that bioactive compounds in BC extract act as an anti-allergic and anti-inflammatory agent by regulating several downstream and upstream inflammation pathways.


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.


Author(s):  
Murugan K ◽  
Sumayya S s ◽  
Lubaina A S

Marine natural products from seaweeds have been the focus of research for novel products of pharmacological interest. Bioactivities of the phytochemicals derived from marine algae are important ingredients in many products, such as cosmetics and drugs for treating cancer and other lifestyle disorders. In this context, the aim of the present study is to compare the anti-inflammatory, analgesic, antipyretic properties of the purified terpenoids from the selected red algae Hypnea musciformis, Gracilaria dura and Kappaphycus alvarezii. Initially, the acute toxicity of the purified terpenoid extract was analyzed and was greater than 4000 mg/kg bw. In vitro BSA denaturation assay revealed significant % inhibition as compared to control. In the carrageenan induced paw edema, the purified terpenoids extract of H. musciformis exhibited remarkable soothing activity with 68.8% percentage of inhibition, which was comparable with that of indomethacin. Meanwhile G. dura and K. alvarezii showed 53 and 50% of inhibition respectively. Analgesic activity was determined by hot plate and acetic acid induced writhing test. In the hot plate test, terpenoids extract of H. musciformis and G. dura significantly increased the hot-plate latency as compared to normal saline, which reflects their analgesic efficacy. In the writhing test, terpenoid extracts from H. musciformis, G. dura and K. alvarezii inhibited the writhing response induced by acetic acid in a concentration dependent manner that suggests its varied mode of inhibition of stretching episodes. Lastly, the antipyretic activity was analyzed. Terpenoid extracts from H. musciformis, G. dura and K. alvarezii revealed a significant (P < 0.01) antipyretic activity up to 180 min.  In summary, the study demonstrates the anti-inflammatory, analgesic and antipyretic effects of terpenoids extracts from H. musciformis, G. dura and K. alvarezii on experimental models, suggesting its therapeutic potential in the treatment of peripheral painful and inflammatory pathologies.


2015 ◽  
Vol 17 (2) ◽  
pp. 224-229 ◽  
Author(s):  
T.S.C. SILVA ◽  
I.B. SUFFREDINI ◽  
E.L. RICCI ◽  
S.R.C. FERNANDES ◽  
V.JR GONÇALVES ◽  
...  

ABSTRACT:he Lantana camara L. belongs to the family Verbenaceae, which contains several active compounds in leaves and roots and which are reported to have medicinal and insecticidal properties. Studies of plants within the same family show the existence of anti-inflammatory activity in paw edema induced by carrageenan, serotonin and histamine and analgesic activity in the acetic acid writhing and tail-flick tests. The present study investigated whether the L. camara extract (ACE) also exerts these effects. The ACE toxicity was studied in male mice, and the percentage of mortality recorded 7 days after treatment was assessed. The ACE was evaluated as an antinociceptive agent in the hot plate, tail-flick and acetic acid writhing tests at a nontoxic dose of 1.0 g/Kg. The results showed that 1.5 g/Kg of ACE was not able to cause death, and doses of 3.0 and 4.0 g/Kg caused 50% and 60% death, respectively, in male mice. In all of the antinociceptive tests, 1 g/Kg of ACE markedly reduced responses to pain. Our findings suggest that ACE may have active anti-inflammatory and antinociceptive properties in much smaller doses than toxic.


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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