scholarly journals Structural and Functional Characterization of Conotoxins from Conus achatinus Targeting NMDAR

Marine Drugs ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 135 ◽  
Author(s):  
Xiujie Liu ◽  
Ge Yao ◽  
Kang Wang ◽  
Yanli Liu ◽  
Xiukun Wan ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Functional Characterization ◽  
Tail Flick ◽  
Snail Species ◽  
Thermal Stimulus ◽  
Dependent Manner ◽  
Amino Acid Residues ◽  
Cone Snail ◽  
Hot Plate ◽  
Linear Peptide

Conotoxin-Ac1 and its variant conotoxin-Ac1-O6P, were isolated from the venom duct of Conus achatinus, a fish-hunting cone snail species collected in the Sea of Hainan, China. Conotoxin-Ac1 is linear peptide that contain 15 amino acids. In the present study, we synthesized and structurally and functionally characterized conotoxin-Ac1 as well as 19 variants. Electrophysiological results showed that conotoxin-Ac1 inhibited N-methyl-D-aspartate receptor subunit 2B (NR2B) with an IC50 of 8.22 ± 0.022 μM. Further structure-activity studies of conotoxin-Ac demonstrated that polar amino acid residues were important for modulating its active, and the replacement of N1, O9, E10, and S12 by Ala resulted in a significant decrease in potency to NR2B. °Furthermore, conotoxin-Ac1 and conotoxin-Ac1-O6P were tested in hot-plate and tail-flick assays to measure the potential analgesic activity to an acute thermal stimulus in a dose-dependent manner. Subsequently, the analgesic activity of conotoxin-Ac1 mutants was analyzed by the hot-plate method. The results show that N1, Y2, Y3, E10, N11, S12, and T15 play an important role in the analgesic activity of conotoxin-Ac1. N1 and S12 have significant effects on conotoxin-Ac1 in inhibiting NR2B and analgesic activity. In conclusion, we have discovered that conotoxin-Ac1 is an inhibitor of NMDAR and displays antinociceptive activity.

Assessment ofOpuntia ficus-indicain vivo Following Ethnobotanical Survey: Confirmation of its Analgesic Activity

2018 ◽  
Vol 16 (S1) ◽  
pp. S191-S196
Author(s):  
A. Mouhaddach ◽  
A. El-hadi ◽  
K. Taghzouti ◽  
M. Bendaou ◽  
R. Hassikou
Keyword(s):  
Body Weight ◽  
Analgesic Activity ◽  
Prickly Pear ◽  
Tail Flick ◽  
Ethnobotanical Study ◽  
Ethnobotanical Survey ◽  
Hot Plate ◽  
Traditional Use ◽  
Opuntia Ficus Indica ◽  
Plant Parts

Opuntia ficus-indica(the cactus or prickly pear) is a cactus belonging to the Opuntiae family. Several Opuntiae plant parts have been used in traditional Moroccan medicine. In this study, we investigated its most common use as an analgesic. An ethnobotanical study ofOpuntia ficus-indicawas first conducted in 10 areas in Morocco. Extracts fromOpuntia ficus-indicacladodes were obtained using a decoction method and its analgesic activity in mice was investigated by the hot plate and tail flick methods. Cladode extracts had significant (p<0.05) analgesic activity at intraperitoneal doses of 300, 500, and 1000 mg/kg body weight. Both methods revealed significantly increased latency at all three doses (p<0.05) compared to controls. These data suggest that the traditional use of this plant as an analgesic is valid; in fact, perhaps it may be a centrally-acting analgesic.

scholarly journals EVALUATION OF ANALGESIC ACTIVITY OF MURRAYA KOENIGII AND CORIANDRUM SATIVUM LEAVES EXTRACT IN ANIMAL MODEL.

2018 ◽  
Vol 11 (1) ◽  
pp. 328
Author(s):  
Kartik Salwe J ◽  
Mirunalini R ◽  
Jervin Mano ◽  
Manimekalai K
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Coriandrum Sativum ◽  
Control Group ◽  
Tail Flick ◽  
Murraya Koenigii ◽  
Hot Plate ◽  
Plate Method ◽  
Standard Drug ◽  
Soxhlet Apparatus

 Objective: The objective of the study was to investigate the analgesic activity of hydroalcoholic extract of Murraya koenigii and Coriandrum sativum leaves and compared it with standard drug in an animal model.Methods: Hydroalcoholic extracts of M. koenigii and C. sativum leaves were obtained using Soxhlet apparatus. The central analgesic property was screened by hot plate method in mice and tail flick method in rats. The pain reaction time (PRT) was measured at 30, 60, and 120 min. The peripheral analgesic activity was evaluated by acetic acid induced writhing in mice.Results: In hot plate method M. koenigii leaves extract at both doses and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. C. sativum leaves extract showed significant increase in PRT only at 60 and 120 min compared to control group. In tail flick method M. koenigii leaves extract at both doses, higher dose of C. sativum leaves extract and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. Higher dose of M. koenigii leaves extract (200 mg/kg) was comparable with standard drug tramadol in both the methods. M. koenigii leaves extract at both dose showed significant reduction in the number of writhing but C. sativum leaves extract failed to show any significant reduction in the number of writhing compared with control. Higher dose of M. koenigii leaves extract was comparable with standard drug tramadol.Conclusion: M. koenigii leaves extract showed both peripheral and central analgesic effect while C. sativum leaves extract showed only peripheral analgesic effect.

scholarly journals Dipeptide mimetic of the bdnf loop 4 possesses analgetic activity

2019 ◽  
Vol 485 (3) ◽  
pp. 366-369
Author(s):  
T. A. Gudasheva ◽  
M. A. Konstantinopolsky ◽  
A. V. Tarasiuk ◽  
L. G. Kolik ◽  
S. B. Seredenin
Keyword(s):  
Analgesic Activity ◽  
Neurotrophic Factor ◽  
Intraperitoneal Injection ◽  
Brain Derived Neurotrophic Factor ◽  
Tail Flick ◽  
Hot Plate ◽  
The Brain

Previously, we synthesized a dimeric dipeptide mimetic of the brain-derived neurotrophic factor (BDNF) loop 4, GSB-106, which, similarly to BDNF, activated TrkB, PI3K/AKT, and MAPK/ERK. When administered systemically, it exhibited neuroprotective, antidepressant, and antidiabetic activities and stimulated neurogenesis and synaptogenesis. In this study, we established that GSB-106 also exhibits the analgesic activity, typical for BDNF, which was revealed in rats in hot plate and tail flick tests 0.5–48 h after intraperitoneal injection at doses of 0.1 and 1 mg/kg.

scholarly journals Evaluation of analgesic activity of the methanol extract from the galls of Quercus infectoria alone and as an adjuvant in wistar rats

2020 ◽  
Vol 9 (5) ◽  
pp. 701
Author(s):  
Abishek P. Raichurkar ◽  
Shashikala Gowdara Hanumanth Reddy
Keyword(s):  
Analgesic Activity ◽  
Wistar Rats ◽  
Methanolic Extract ◽  
Inflammatory Diseases ◽  
Syringic Acid ◽  
Tail Flick ◽  
Hot Plate ◽  
Anti Inflammatory ◽  
Group 2 ◽  
Quercus Infectoria

Background: Non-steroidal anti-inflammatory drugs and opioids are the most preferred drugs for pain relief. Considering the gastrointestinal toxicity, dependence and other side effects, search for better analgesic drug continues. Quercus infectoria (QI) is from the family Fagaceae. The galls of QI are comprised of tannin (36 to 60%), gallic acid, ellagic acid, and syringic acid. They possess antioxidant, anti-inflammatory, antimicrobial, and anti-diabetic properties. In India, galls of QI have been used for the treatment of toothache, diarrhoea, sore throat and inflammatory diseases as a home remedy. This study was conducted to evaluate the analgesic activity of methanolic extract of galls of QI on wistar rats using tail-flick and Eddy’s hot-plate methods. The objective of the study was to evaluate the analgesic activity of methanolic extract of galls of QI alone and as an adjuvant with tramadol on Wistar rats.Methods: Total of 24 wistar rats were included in the study and divided into 4 groups. They received drugs intra-peritoneally as follows. In group 1, normal saline, in group 2, tramadol, in group 3, methanolic extract of galls of QI and in group 4, tramadol with methanolic extract of galls of QI was available.Results: Methanolic extract of galls of QI produced significant maximal possible analgesia (<0.001) at 30 and 60 minutes in tail-flick method whereas it failed to produce analgesia in hot-plate method during all time intervals.Conclusions: Methanolic extract of galls of QI showed analgesic activity in tail-flick method indicating that its possible mechanism of action is spinally mediated.

scholarly journals Evaluation of Analgesic Activity ofPapaver libanoticumExtract in Mice: Involvement of Opioids Receptors

2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Mohamad Ali Hijazi ◽  
Ahmed El-Mallah ◽  
Maha Aboul-Ela ◽  
Abdalla Ellakany
Keyword(s):  
Opioid Receptors ◽  
Analgesic Activity ◽  
Time Course ◽  
Ethanolic Extract ◽  
Maximum Activity ◽  
Tail Flick ◽  
Endemic Plant ◽  
Hot Plate ◽  
The Central Nervous System ◽  
Opioid Withdrawal Syndrome

Papaver libanoticumis an endemic plant to Lebanese region (family Papaveraceae) that has not been investigated before. The present study aimed to explore the analgesic activity of dried ethanolic extract ofPapaver libanoticum(PLE) using tail flick, hot plate, and acetic acid induced writhing models in mice. The involvement of opioid receptors in the analgesic mechanism was investigated using naloxone antagonism. Results demonstrated that PLE exhibited a potent dose dependent analgesic activity in all tested models for analgesia. The analgesic effect involved activation of opioid receptors in the central nervous system, where both spinal and supraspinal components might be involved. The time course for analgesia revealed maximum activity after three hours in both tail flick and hot plate methods, which was prolonged to 24 hours. Metabolites of PLE could be responsible for activation of opioid receptors. The EC50 of PLE was 79 and 50 mg/kg in tail flick and hot plate tests, respectively. The total coverage of analgesia by PLE was double that of morphine in both tests. In conclusion, PLE proved to have opioid agonistic activity with a novel feature of slow and prolonged effect. The present study could add a potential tool in the armaments of opioid drugs as a natural potent analgesic and for treatment of opioid withdrawal syndrome.

scholarly journals Phytochemical & Pharmacological Investigation of Stems of Passiflora foetida

2021 ◽  
pp. 408-414
Author(s):  
N. Michael Antony ◽  
Jennifer Fernandes ◽  
Jane Mathew
Keyword(s):  
Analgesic Activity ◽  
Ethanolic Extract ◽  
Tail Flick ◽  
Phytochemical Analysis ◽  
Significant Activity ◽  
Dependent Manner ◽  
Phytochemical Investigation ◽  
Soxhlet Apparatus ◽  
Passiflora Foetida

Aims: To carry out extraction, preliminary phytochemical analysis and invivo analgesic screening of extract of the stem of Passiflora foetida L. Methodology: Passiflora foetida L; Family: Passifloraceae, is an exotic fast-growing perennial and medicinal vine occurring in Germany, France and other European countries and USA and grown in different parts of India. Dried stems of Passiflora foetida L was coarsely powdered and maceration was done using Soxhlet apparatus. The ethanolic extract of stems of Passiflora foetida L was subjected to preliminary phytochemical tests. Then subjected to in vivo analgesic activity. Results: Phytochemical investigation of the stem of Passiflora foetida L preliminary test showed the presence of carbohydrates, glycosides, flavonoids and steroids. Acute toxicity study of ethanolic extract of stems of Passiflora foetida L was carried out and extracts were found to be safe up to 2000 mg/kg body weight. Pharmacological activities of stems of Passiflora foetida L was carried out from ethanolic extract. Conclusion: Phytochemical investigation of ethanolic extract of stems were carried out and Analgesic activity by tail flick method in rats and acetic acid induced writhing method in mice, showed statistically significant activity (P=.05) when compared to control. The ethanolic stem extract of Passiflora foetida L proved to have significant pain relieving action in a dose dependent manner.

Green synthesis of Zingiberis rhizoma-based carbon dots attenuates chemical and thermal stimulus pain in mice

Nanomedicine ◽  
2020 ◽  
Vol 15 (9) ◽  
pp. 851-869
Author(s):  
Meiling Zhang ◽  
Jinjun Cheng ◽  
Yue Zhang ◽  
Hui Kong ◽  
Suna Wang ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Carbon Dots ◽  
Functional Group ◽  
Biomedical Application ◽  
Chemical Stimulus ◽  
Thermal Stimulus ◽  
Hot Plate ◽  
Pyrolysis Method ◽  
Tail Immersion ◽  
Preliminary Study

Aim: To evaluate the analgesic activity of Zingiberis rhizoma-based carbon dots (ZR-CDs). Materials & methods: Novel ZR-CDs were prepared via a facile, green pyrolysis method. Microstructure, optical and functional group properties were characterized. Acetic acid writhing, hot-plate and tail-immersion tests were performed using mice to evaluate the analgesic activity of ZR-CDs, followed by a preliminary study on the analgesic mechanism. Results: ZR-CDs with a quantum yield of 5.2% had a diameter ranging from 2.23 to 3.77 nm. Remarkable analgesic effect of ZR-CDs was observed against both thermal and chemical stimulus tests, possibly mediated by an opioid-like mechanism and the regulation of 5-hydroxytryptamine levels. Conclusion: ZR-CDs have a promising potential for biomedical application in relieving pain-related diseases.

Involvement of opioidergic and serotonergic systems in the analgesic activity of Cissus quadrangularis L. stem extract in mice

2015 ◽  
Vol 26 (1) ◽  
Author(s):  
Tan Wee Nie ◽  
Mohamed Saleem Abdul Shukkoor ◽  
Rajesh Sreedharan Nair ◽  
Fatimah Khursiah Binti Amiruddin ◽  
Shamala Ramasamy
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Methanol Extract ◽  
Chloroform Extract ◽  
Tail Flick ◽  
Hot Plate ◽  
Cissus Quadrangularis ◽  
Stem Extract

AbstractDriedChloroform extract showed significant (p<0.05) analgesic effect at the doses of 75, 150 and 300 mg/kg in hot plate and tail flick tests. Methanol extract showed significant (p<0.05) analgesic effect at the dose of 300 mg/kg in hot plate and tail flick tests. Analgesic activity was not blocked (p<0.05) in the group pretreated with phentolamine but blocked in the groups pretreated with naloxone andThe chloroform extract was found to be more potent than methanol extract in inducing analgesic effect in mice, and the analgesic activity may be mediated through opioidergic and serotonergic pathways.

scholarly journals An experimental study to evaluate and compare the analgesic activity of calcitriol with morphine in albino mice at a tertiary care teaching hospital in Maharashtra, India

2016 ◽  
Vol 5 (1) ◽  
pp. 191 ◽  
Author(s):  
Abhinav David ◽  
Raj Kumar Goel ◽  
Prashant Patel ◽  
Rahul Kunkolol ◽  
Dattatray H. Nandal
Keyword(s):  
Experimental Study ◽  
Vitamin D ◽  
Analgesic Activity ◽  
Tertiary Care ◽  
Active Form ◽  
Analgesic Efficacy ◽  
Tail Flick ◽  
Hot Plate ◽  
Vitamin D Receptors ◽  
Albino Mice

Background: Vitamin D plays vital role in physiological functions in humans through its active form Calcitriol (Vitamin D3). Vitamin D receptors are found in most tissues, attributing to its classic and non-classic actions. Calcitriol exerts important regulatory effects on the molecular pathways involved in inflammation and pain. The present study is done for experimental evaluation of analgesic action of Calcitriol using pain models in albino mice.Methods: In this prospective, experimental study, healthy Swiss albino mice were taken after permission from IAEC. Mice were divided into five groups as Control- treated with normal saline, Standard- treated with morphine and Test groups- treated with Calcitriol in dose of 15 µg /kg/mice, 30 µg /kg/mice and 60 µg/kg/mice respectively. Evaluation of analgesic activity was done using Hot plate and Tail flick analgesiometer.Results: All the 3 test doses of Calcitriol although showed prolongation of reaction time in Hot plate method up to 60 mins but the analgesic activity was not significant in comparison with the standard Morphine. With Tail flick method Calcitriol failed to show any analgesic efficacy at 15-30 μg/Kg but showed some analgesia at 60 μg/Kg which was more than control but not at all comparable with the standard Morphine for thermal pain.Conclusions: The analgesic activity of Calcitriol was exhibited at higher doses. This property needs to be further evaluated by planning extensive animal experimentation using different animal models.

scholarly journals Does an Alteration in Nociceptive Response to Mineral Components of Dental Composites Involve Changes in Oxidative Status? a Brief Report

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Natalija Arsenijevic ◽  
Jovana Milenkovic ◽  
Pavle Milanovic ◽  
Aleksandra Arnaut ◽  
Milica Jovanovic ◽  
...  
Keyword(s):  
Calcium Phosphates ◽  
Dental Composites ◽  
Albino Rats ◽  
Tail Flick ◽  
Nociceptive Response ◽  
Thermal Stimulus ◽  
Hot Plate ◽  
Tail Flick Test ◽  
Simultaneous Application ◽  
Mineral Components

Abstract Since that use of bioactive mineral components of dental composites have been accompanied with various toxicities, including neurotoxicity, the aim of the study was to examine the effect of chronic application of hydroxyapatite, tricalcium phosphate and amorphous calcium phosphate in nanoparticles (nHA, nTCP, nACP) to parameters of sensitivity to thermal pain stimuli. Although the systemic toxicity of those compounds is frequently attributed to an oxidative damage, we also decided to examine the potential effects of Filipendula ulmaria extract on nociception alterations induced by the nano-sized mineral components of dental composites. Forty-two Wistar albino rats were divided into control and six experimental (equal) groups that orally received either nHA, nTCP, nACP alone, or simultaneously with FU extract for 30 days. Nociceptive alterations were quantified in the hot plate and tail flick test. The chronic administration of nHA and nACP resulted in significant increase in reactivity to thermal stimulus, with no significant change observed in nTCP group when compared to the control in the hot plate test, while simultaneous application of FU extract prevented any significant alteration of time to respond. The reaction time in the tail flick test for all three groups that received only nano calcium phosphates was reduced, with no changes in the groups treated with FU extract. The results of this study confirmed that calcium phosphates of mineral components of dental composites produced hyperalgesic effects, and this side effect were significantly attenuated by antioxidant supplementation.

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