scholarly journals Optimization of the Purifying Process for Columbianetin-β-D-Glucopyranoside from Angelicae Pubescentis Radix and Evaluation of Its Analgesic Activity Using Hot Plate Test

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Yaqian Zhang ◽  
Yuqiao Yang ◽  
Ye Shang ◽  
Chunxiao Liang ◽  
Jun He ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Adsorption Process ◽  
Kinetic Curve ◽  
Isotherm Models ◽  
Elution Volume ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Desorption Process ◽  
Adsorption And Desorption ◽  
Plate Test

The objective of this work was to provide an economic and practical method for the purification of columbianetin-β-D-glucopyranoside from Angelicae Pubescentis Radix extract. In the static adsorption and desorption, the effects of resin type (D101, HP-20, AB-8, GDX-201, and DA201), contact time (10–360 min), and temperature (298–318 K) were assessed on columbianetin-β-D-glucopyranoside adsorption efficiency in laboratory. GDX-201 resin showed the best adsorption and desorption properties for columbianetin-β-D-glucopyranoside. The kinetic data revealed that the equilibrium time for columbianetin-β-D-glucopyranoside adsorption was achieved within 150 min. Moreover, the adsorption kinetic curve was well in accordance with the pseudo-second-order equation (R2 > 0.99). The rate controlling step of the adsorption process was the intraparticle diffusion. The Langmuir isotherm models (R2 > 0.99) could describe the whole adsorption process, which was exothermic and spontaneous according to the result of thermodynamics tests. In the dynamic adsorption and desorption process, the optimum loading flow (4, 5, and 6 BV/h), ethanol concentration (0–60%), and elution volume (10–230 mL) were optimized. Under optimal conditions of 4 BV/h loading flow, 6.7 BV loading volume, 25% ethanol, and 14 BV elution volume, the content of columbianetin-β-D-glucopyranoside in the product was increased 29.61-fold from 0.45% to 13.32 ± 0.64% with yield of 88.03 ± 2.76% by an experiment of lab-scale enlargement. Then, columbianetin-β-D-glucopyranoside was further purified by PHPLC and its purity was more than 98%. Additionally, the analgesic activity of the columbianetin-β-D-glucopyranoside was assessed by hot plate test. The experimental results showed that columbianetin-β-D-glucopyranoside significantly increased the latency of pain response in mice. This study demonstrated columbianetin-β-D-glucopyranoside could be as a potentially natural analgesic component. It could be summed up that the established method was successfully applied to purifying columbianetin-β-D-glucopyranoside from Angelicae Pubescentis Radix extract.

scholarly journals Analgesic Activity of the Kappa Opioid Receptor Agonist RU-1205 in Rats

2018 ◽  
Vol 3 (2) ◽  
pp. 13 ◽  
Author(s):  
AA Spasov ◽  
OY Grechko ◽  
DM Shtareva ◽  
AI Raschenko ◽  
Natalia Eliseeva ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Analgesic Activity ◽  
Analgesic Effect ◽  
Physical Dependence ◽  
Receptor Activation ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test

Introduction: Opioid analgesics are the most efficient and widely used drugs for the management of moderate to severe pain. However, side effects associated with mu receptor activation, such as respiratory depression, tolerance and physical dependence severely limit their clinical application. Currently, the kappa-opioid system is the most attractive in terms of the clinical problem of pain, because kappa-agonists do not cause euphoria and physical dependence. The purpose of this study was to evaluate the antinociceptive effect of the novel compound - RU-1205. Methods: The analgesic activity of RU-1205 was studied on nociceptive models that characterize the central and peripheral pathways of pain sensitivity (hot plate test, electrically induced vocalisation, formalin test, writhing test). Results: RU-1205 exhibited highly potent antinociceptive effects in rodent models of acute pain with ED50 values of 0.002 - 0.49 mg /kg. Pretreatment with the κ-opioid receptor antagonist norBinaltorphimine significantly attenuated the analgesic activity of investigated substance in a hot plate test. Conclusions: It was established that the compound shows a significant dose-dependent central and peripheral analgesic effect. It was assumed kappa-opioidergic mechanism of analgesic effect of RU-1205.

scholarly journals Comparison the analgesic activity of watery suspension of Nigella sativa Linn. seeds with Naproxen in mice

2010 ◽  
Vol 9 (3) ◽  
pp. 56
Author(s):  
W. H. Al-Shebani, And F. J. Al-Tahan
Keyword(s):  
Reaction Time ◽  
Analgesic Activity ◽  
Nigella Sativa ◽  
Antinociceptive Effect ◽  
Analgesic Action ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
The Third ◽  
Significant Increment

The present study was designed to investigated the antinociceptive effect of the waterysuspension of Nigella sativa seeds compared with that of Naproxen by using hot plate test, whichmainly measures the threshold of stimulus required to elicit a response , in mice at 30, 60, 90, 120minutes after administration of the test agents. Twenty four albino Swiss mice of either sex weredivided in four groups with (6) animals each, the first group was treated orally with 1000 mg/kgBW of watery suspension of Nigella seeds, the second group was treated orally with naproxen atdose of 500 mg/kg BW ,the third group drenched with 500mg/kg BW of watery suspension ofNigella seeds and 250 mg/kg BW of naproxen ,whereas the last group serve as control. Nigellasativa seeds suspension significantly (p<0.05) prolonged the latency of response at all posttreatmentobservation times (30, 60, 90 and 120 minutes) , the analgesic action of naproxen wasdiminished with time compared with Nigella seeds.Combination of equal amounts of Nigellaseeds and Naproxen (half the originally used doses) caused significant increment (p<0.05) ofanalgesic reaction time longer than shown by each agent when given alone indicating an obvioussynergistic effect between watery suspension of Nigella seeds and Naproxen.

scholarly journals The analgesic activity of new sulfur-containing di- and tetrahydropyridine derivatives in the hot plate test

2021 ◽  
pp. 45-55
Author(s):  
E.Yu. Bibik ◽  
◽  
L.I. Kurbanov ◽  
S.A. Grygoryan ◽  
D.S. Krivokolysko ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
High Efficiency ◽  
Pain Syndrome ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Reference Drug ◽  
Plate Test ◽  
Metamizole Sodium ◽  
Sulfur Containing

Nowadays the search of new high-efficiency and safe drugs for the pharmacotherapy of diseases accompanied by pain syndrome is an active area of modern pharmacological research. 170 new derivatives of di- and tetrahydropyridines synthesized on the basis of the Chemex Research Laboratory, Vladimir Dahl Lugansk State University were exposed to the virtual bioscreening using the Swiss Target Prediction software. The paper describes screening studies in vivo of 5 samples of sulfur-containing di- and tetrahydropyridines (laboratory codes d02-138, as-262, f02-079, cv-074, cv-143) in the standard hot plate test in comparison with the reference drug — metamizole sodium. The compounds in the dose of 5 mg/kg were given intragastrically 1 hour and a half before placing the rats on the hot plate, the reference drug in the dose of 7 mg/kg also was given intragastrically 1 hour and a half before placing the rats on the hot plate. The compounds with laboratory codes as-262 (allyl 6-({2-[(4-acetylphenyl)amino]-2-oxoethyl}thio)-5-cyano-4-(2-furyl)-2-methyl-1,4-dihydropyridine-3-carboxylate) and d02-138 (ethyl 4-[({[3-cyano-5-{[(2,4-dichlorophenyl)amino]carbonyl}-4-(2-furyl)-6-methyl-1,4-dihydropyridinе-2-yl]thio}acetyl)amino]benzoate) possess the most pronounced analgesic activity in the dose of 5 mg/kg, they demonstrated 2.03 and 1.9-fold efficiency in comparison to metamizole sodium respectively. The rest three specimens demonstrated metamizole sodium-like analgesic activity.

scholarly journals Synthesis, characterization and pharmacological activity of new 2- imino –thiazolidine-4-one derivatives

2019 ◽  
Vol 10 (3) ◽  
pp. 1763-1769 ◽  
Author(s):  
Raghdah M. Alwiswasy ◽  
Raheem Jameel M ◽  
Basim Jasim Hameed
Keyword(s):  
Acetic Acid ◽  
Pharmacological Activity ◽  
Analgesic Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Edema Model ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Analgesic Activities

A new 2-iminothiazolidin-4-ones compound and its derivatives were synthesized and characterized by FT-IR, CHN, and 1HNMR techniques. The target compounds were assessed for their anti-inflammatory and analgesic activities, and the study was performed using Swiss albino mice (25-30 g) for investigation. A hind edema model caused by , while the analgesic activity was assessed using an acetic acid-induced writhing and a hot plate test evaluated the anti-inflammatory activity.

scholarly journals Anti-inflammatory and Analgesic Effects in Rodent Models of Ethanol Extract of Clausena anisata Roots and their Chemical Constituents

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Emmanuel Kofi Kumatia ◽  
Kofi Annan ◽  
Rita Akosua Dickson ◽  
Abraham Yeboah Mensah ◽  
Isaac Kingsley Amponsah ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Crude Extract ◽  
Analgesic Effect ◽  
Chemical Constituents ◽  
Ethanol Extract ◽  
Phytochemical Analysis ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Anti Inflammatory

The in vivo anti-inflammatory and analgesic activities of the crude ethanol extract and chemical constituents of Clausena anisata roots were investigated. The crude extract, which was devoid of any visible acute toxicity, displayed significant anti-inflammatory effect at the dose of 1000 mg/kg (p.o.) when assessed using the carrageenan-induced oedema model. In the acetic acid-induced writhing and hot plate tests, it produced a very significant ( p < 0.001), dose-dependent analgesic effect, with maximum analgesic activity of 72.1% at 1000 mg/kg (p.o.). Phytochemical analysis of the crude extract resulted in the isolation of four coumarins (anisocoumarin B, osthol, imperatorin and xanthotoxol) and a carbazole alkaloid, heptaphylline. Among the isolated compounds, osthol and anisocoumarin B produced the highest anti-inflammatory activity at 9 mg/kg (p.o.): slightly better than the positive control, indomethacin. Except for xanthotoxol, all the isolated compounds administered at 6 mg/kg (p.o.) produced significant analgesic activity and higher than diclofenac; with heptaphylline being the most potent (48.7%). The analgesic activity of anisocoumarin B (50.4%) was the highest among the isolates tested and the standard, tramadol, in the hot plate test. The nonselective opioid receptor antagonist, naloxone, abolished the analgesic effect of the crude extract and the tested isolates (anisocoumarin B and xanthotoxol) in the hot plate test suggesting an effect via the central opioidergic system. These findings provide the scientific basis for the use of C. anisata roots in traditional medicine as anti-inflammatory and analgesic agents.

Prenatal Pregabalin Exposure Alters Postnatal Pain Sensitivity and Some Behavioral Responses in Adult Offspring Rats

2020 ◽  
Vol 15 (3) ◽  
pp. 205-214
Author(s):  
Manzumeh-Shamsi Meymandi ◽  
Gholamreza Sepehri ◽  
Amirhossein Moslemizadeh ◽  
Seyyed Sajjad Vakili Shahrbabaki
Keyword(s):  
Locomotor Activity ◽  
Open Field ◽  
Prenatal Exposure ◽  
Pain Sensitivity ◽  
Sucrose Preference ◽  
Pain Response ◽  
Adult Offspring ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test

Background: Prenatal antiepileptic drug exposure could demonstrate both congenital malformations and behavioral impairments in offspring. Objective: This study was performed to assess the effects of prenatal exposure to pregabalin (PGB) on pain response, anxiety, motor activity and some behavior of adult offspring rats. Methods: Pregnant Wistar rats received PGB (7.5, 15 and 30 mg/kg/ip) during embryonic days 9.5- 15.5. The pain response, anxiety-like behaviors, locomotor activity, motor balance and coordination and anhedonia of adult offspring were examined by tail-flick and hot plate test, open field test, elevated plus maze (EPM), beam balance test and sucrose preference test in their 60th day of life, respectively. Results: Prenatal exposure to PGB revealed significant dose-dependent reduction in pain sensitivity (increase in pain latency response) in the hot plate test, especially in females, while anxiety-like behavior assessed in EPM and open field significantly reduced in males. In the open field, locomotor activity reduced significantly after exposure to PGB 30 mg/kg and motor coordination decreased dose-dependently, especially in males. Anhedonia, as an indication of sucrose preference or pleasure response, was not changed. Conclusion: These findings suggest that prenatal PGB exposure could be associated with significant changes in pain response, anxiety, locomotor activity and coordination in adult offspring rats.

scholarly journals Anti-nociceptive and anti-inflammatory effects of an aqueous extract of blended leaves of Ocimum gratissimum and Psidium guajava

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Akinyinka O. Alabi ◽  
Abayomi M. Ajayi ◽  
Osarume Omorogbe ◽  
Solomon Umukoro
Keyword(s):  
Acetic Acid ◽  
Aqueous Extract ◽  
Psidium Guajava ◽  
Antinociceptive Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Promising Alternative ◽  
Plate Test ◽  
Ocimum Gratissimum ◽  
Anti Inflammatory

Abstract Background To investigate the antinociceptive and anti-inflammatory activities of aqueous extract of a blended mixture of dried leaves of Ocimum gratissimum and Psidium guajava, a traditional analgesic drug polyherbal (TADP) used as a remedy for pain-related conditions. Methods Antinociceptive activity of TADP (100, 200 and 400 mg/kg) was evaluated in the hot plate test and acetic acid-induced nociception in mice while the anti-inflammatory was evaluated in carrageenan-induced paw oedema in rats. Levels of nitrite, myeloperoxidase, glutathione and malondialdehyde were assayed in carrageenan-induced paw tissue. Results TADP (200 and 400 mg/kg) significantly prolong the latency time in the hot-plate test. TADP (100–400 mg/kg) produced a dose-dependent significant inhibition of the acetic-acid induced abdominal constriction. The antinociceptive activity of TADP in the presence of naloxone and atropine was not reversed whereas yohimbine and glibenclamide significantly reversed it. TADP (100, 200 and 400 mg/kg) significantly reduced the swelling in the carrageenan-induced oedema model and also produced a reduction in the nitrite and myeloperoxidase level. TADP (400 mg/kg) significantly reduced malondialdehyde concentration and increase glutathione level in the carrageenan-induced rat paw. TADP significantly decrease the number of cellular infiltrates in the histopathological assessment. Conclusion These results indicate that polyherbal product containing blended leaves of Ocimum gratissimum and Psidium guajava possess antinociceptive and anti-inflammatory properties, hence represents a promising alternative remedy in inflammation-induced pain.

scholarly journals Enhancement of morphine-induced antinociception after electroconvulsive shock in mice

2021 ◽  
Vol 17 ◽  
pp. 174480692199262
Author(s):  
Ken Iwata ◽  
Yukio Takamatsu ◽  
Nagafumi Doi ◽  
Kazutaka Ikeda
Keyword(s):  
Dose Response ◽  
Response Curve ◽  
Antinociceptive Effect ◽  
Dose Response Curve ◽  
Expression Level ◽  
Morphine Injection ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Pain Patients

Electroconvulsive therapy (ECT) has been applied for chronic pain for decades. The amounts of opioids to treat pain are sometimes reduced after a series of ECT. The effect of ECT on morphine-induced analgesia and its mechanism underlying the reduction of morphine requirement has yet to be clarified. Therefore, we administered electroconvulsive shocks (ECS) to mice and investigated the antinociceptive effect of morphine in a hot plate test. We examined the expression level of µ-opioid receptor in the thalami of mice 25 h after administration of ECS compared to the thalami of mice without ECS administration using western blotting. ECS disturbed the development of a decrease in the percentage of maximal possible effect (%MPE), which was observed 24 h after a morphine injection, when ECS was applied 25, 23, 21, and 12 h before the second administration of morphine. We also examined the effect of ECS on the dose-response curve of %MPE to morphine-antinociception. Twenty-five hours after ECS, the dose-response curve was shifted to the left, and the EC50 of morphine given to ECS-pretreated mice decreased by 30.1% compared to the mice that were not pretreated with ECS. We also found that the expression level of µ-opioid receptors was significantly increased after ECS administration. These results confirm previous clinical reports showing that ECT decreased the required dose of opioids in neuropathic pain patients and suggest the hypothesis that this effect of ECT works through the thalamus.

Synthesis of 8-alkoxy-1,3-dimethyl-2, 6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides as analgesic and anti-inflammatory agents

2015 ◽  
Vol 21 (5) ◽  
pp. 273-278 ◽  
Author(s):  
Grażyna Chłoń-Rzepa ◽  
Agnieszka W. Jankowska ◽  
Małgorzata Zygmunt ◽  
Krzysztof Pociecha ◽  
Elżbieta Wyska
Keyword(s):  
Analgesic Activity ◽  
Structural Element ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Peripheral Mechanism ◽  
Anti Inflammatory ◽  
Factor Α ◽  
Necrosis Factor ◽  
Inhibit Tumor Necrosis Factor

AbstractA series of new 8-alkoxy-1,3-dimethyl-2,6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides 6–12 was synthesized and evaluated for the analgesic activity in two in vivo models: the writhing syndrome and the hot-plate tests. Among the investigated derivatives, compounds with N′-arylidenehydrazide moiety 9–12 show analgesic activity significantly higher than that of acetylsalicylic acid, which may indicate the importance of this structural element for analgesic properties. The lack of the activity in the hot-plate test may suggest that the analgesic activity of the newly synthesized compounds is mediated by a peripheral mechanism. The selected compounds 7 and 12 inhibit tumor necrosis factor α production in a rat model of lipopolysaccharide-induced endotoxemia, similarly to theophylline, which may confirm their anti-inflammatory properties.

scholarly journals Investigation of competitive adsorption and desorption of heavy metals from aqueous solution using raw rock: Characterization kinetic, isotherm, and thermodynamic

2021 ◽  
Vol 348 ◽  
pp. 01016
Author(s):  
Rajaa Bassam ◽  
Marouane El Alouani ◽  
Nabila Jarmouni ◽  
Jabrane Maissara ◽  
Mohammed El Mahi Chbihi ◽  
...  
Keyword(s):  
Heavy Metals ◽  
Adsorption Process ◽  
Freundlich Isotherm ◽  
Langmuir Model ◽  
Second Order ◽  
Isotherm Models ◽  
Desorption Process ◽  
Pseudo Second Order ◽  
Rock Characterization ◽  
Metals Adsorption

Heavy metals are the most dangerous inorganic pollutants Due to their bioaccumulation and their nonbiodegradability, for this, several studies have focused on the recovery of these metals from water using different techniques. In this context, our study consists of evaluating an efficient and eco-friendly pathway of competitive recovery of heavy metals (Cd, Cr and As) from aqueous solutions by adsorption using raw rock. This adsorbent was characterized before and after the adsorption process by several techniques. The multi-metals adsorption process in the batch mode was undertaken to evaluate the effect of adsorbent mass, contact time, pH, Temperature, and initial heavy metals concentration. The kinetic data were analyzed using the pseudo-first-order, pseudo-second-order and intra-particle diffusion kinetic models. According to the modeling of the experimental results, the adsorption kinetics of heavy metals were adapted to the pseudo-second-order model. The adsorption isotherms were evaluated by the Langmuir and Freundlich isotherm models. The experimental isotherm data of heavy metals were better fitted with the Langmuir model rather than Freundlich isotherm models. The maximum experimental adsorption capacities (Qmax) predicted by the Langmuir model are 15.23 mg/g for Cd (II), 17.54 mg/g for Cr (VI) and 16.36 mg/g for As (III). The values of thermodynamic parameters revealed that the heavy metals adsorption was exothermic, favorable, and spontaneous in nature. The desorption process of heavy metals showed that this raw rock had excellent recycling capacity. Based on the results, these untreated clays can be used as inexpensive and environmentally friendly adsorbents to treat water contaminated by heavy metals.

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