scholarly journals BIOPROSPECÇÃO DE ESPÉCIES VEGETAIS DA PRÉ-AMAZÔNIA BRASILEIRA COM EFEITO ANTINOCICEPTIVO

2021 ◽  
Author(s):  
Danielle Cristine Gomes Franco ◽  
Alex Brall Rodrigues Silva ◽  
Vitor Augusto Ferreira Dos Santos ◽  
Rosane Nassar Meireles Guerra
Keyword(s):  
Tail Flick ◽  
Vismia Guianensis

Introdução: No estado do Maranhão incluído na região da Pré-Amazônia, a diversidade da flora imprimiu a fitoterapia uma forte tradição popular de uso para tratamentos de enfermidades, porém, somente uma pequena parcela desses vegetais já foi avaliada cientificamente, destacando a importância da procura por novos agentes farmacologicamente ativos, encontrados nas plantas no intuito de obter drogas clinicamente ativas. Objetivo: Desta forma, o presente trabalho investigou o potencial analgésico de três extratos vegetais. Métodos: Utilizou-se dois extratos hidroalcoólicos preparados com folhas de Platonia insignis (EHPI) e Vismia guianensis (EHVG) e um extrato aquoso do mesocarpo de Attalea speciosa (EAB). A ação anti-nociceptiva foi avaliada por Tail flick em 25 camundongos Swiss fêmeas (n=5/grupo), distribuídos em 5 grupos, tratados como a seguir: grupo Controle recebeu solução salina tamponada com fosfato (PBS), por via oral e foi considerado como negativo; grupo Morfina: recebeu a droga (10mg/kg) via intraperitoneal, e foi utilizado como controle positivo; grupo EHPI (5mg/kg) via oral e grupo EHVG (5mg/kg) via oral e grupo EAB (5mg/kg) via oral. Resultados: Nos grupos EHPI, EHVG e EAB o tratamento com os extratos resultou em atividade anti-nociceptiva com magnitude semelhante à observada no grupo morfina, sobretudo nos intervalos de 60 e 120 minutos. Esses efeitos sugerem que os extratos podem ter efeito anti-nociceptivo central, uma vez que o modelo Tail-flick exibe uma resposta supra espinhal. Conclusão: Conclui-se que os extratos em estudo apresentaram atividade nociceptiva, sugerindo que a utilização desses compostos contidos nos extratos pode ser uma alternativa promissora no desenvolvimento de novas drogas com ação analgésica.

Anodyne activities of New Tetrazole derivatives from Triazine

2020 ◽  
Vol 11 (3) ◽  
pp. 3377-3383
Author(s):  
Arulmozhi R ◽  
Abirami N ◽  
Helen P Kavitha ◽  
Arulmurugan S ◽  
Vinoth Kumar J
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Pharmaceutical Chemistry ◽  
Tail Flick ◽  
Structural Fragment ◽  
Hot Plate ◽  
Standard Drug ◽  
New Class ◽  
Novel Drugs ◽  
Tetrazole Derivatives

The creation of novel drugs containing a tetrazole ring as a structural fragment has contributed considerably to the outstanding achievements of the pharmaceutical chemistry in the last decade. Tetrazoles are the heterocyclic compounds having diverse biological activities such as analgesic, antiinflammation, antimicrobial, anticancer, antidiabetic, etc., and an impending source in biosciences. In this paper, the authors describe the synthesis of novel tetrazoles from N, N-( 6-Phenyl-1,3,5-triazine-2,4-diyl) dibenzamide (PTDDB) and 2-phenyl-4, 6-di(2H-tetrazole-2-yl)-1,3,5-triazine(5a-i) were prepared per the proposed scheme. A new class of tetrazole heterocycles were synthesised and characterised. I n vivo analysis was carried out on the analgesic property of synthesised tetrazole derivatives (5a, 5b, 5c). Characterisation studies such as IR, 1H NMR, 13C NMR, Mass and elemental analysis were performed for the synthesised tetrazole derivatives. Some of the tetrazole derivatives 5a, 5b, and 5c were tested for anodyne activity using morphine as the standard drug. The data reveals that all the three compounds 5a, 5b and 5c taken for the study show analgesic activity by hot plate method and tail flick methods. Among tested compounds, compound 5c is found to have potent analgesic (anodyne) activity. The results of the study indicate that the sample taken for the study show fairly good business using morphine as the standard drug.

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 New ibuprofen derivatives with thiazolidine-4-one scaffold with improved pharmaco-toxicological profile

2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Ioana-Mirela Vasincu ◽  
Maria Apotrosoaei ◽  
Sandra Constantin ◽  
Maria Butnaru ◽  
Liliana Vereștiuc ◽  
...  
Keyword(s):  
Analgesic Effect ◽  
Visceral Pain ◽  
Biological Effects ◽  
Maximum Effect ◽  
Tail Flick ◽  
Paw Edema ◽  
Cell Viability Assay ◽  
Thermal Nociception ◽  
Analgesic Effects ◽  
Anti Inflammatory

Abstract Background Aryl-propionic acid derivatives with ibuprofen as representative drug are very important for therapy, being recommended especially for anti-inflammatory and analgesic effects. On other hand 1,3-thiazolidine-4-one scaffold is an important heterocycle, which is associated with different biological effects such as anti-inflammatory and analgesic, antioxidant, antiviral, antiproliferative, antimicrobial etc. The present study aimed to evaluated the toxicity degree and the anti-inflammatory and analgesic effects of new 1,3-thiazolidine-4-one derivatives of ibuprofen. Methods For evaluation the toxicity degree, cell viability assay using MTT method and acute toxicity assay on rats were applied. The carrageenan-induced paw-edema in rat was used for evaluation of the anti-inflammatory effect while for analgesic effect the tail-flick test, as thermal nociception in rats and the writhing assay, as visceral pain in mice, were used. Results The toxicological screening, in terms of cytotoxicity and toxicity degree on mice, revealed that the ibuprofen derivatives (4a-n) are non-cytotoxic at 2 μg/ml. In addition, ibuprofen derivatives reduced carrageenan-induced paw edema in rats, for most of them the maximum effect was recorded at 4 h after administration which means they have medium action latency, similar to that of ibuprofen. Moreover, for compound 4d the effect was higher than that of ibuprofen, even after 24 h of administration. The analgesic effect evaluation highlighted that 4 h showed increased pain inhibition in reference to ibuprofen in thermal (tail-flick assay) and visceral (writhing assay) nociception models. Conclusions The study revealed for ibuprofen derivatives, noted as 4 m, 4 k, 4e, 4d, a good anti-inflammatory and analgesic effect and also a safer profile compared with ibuprofen. These findings could suggest the promising potential use of them in the treatment of inflammatory pain conditions.

Anti-inflammatory and analgesic effects of methanol extract of red cultivar Allium cepa bulbs in rats and mice

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Adeoye Joshua Oyewusi ◽  
Olayinka Ayotunde Oridupa ◽  
Adebowale Bernard Saba ◽  
Ibironke Kofoworola Oyewusi ◽  
Jonny Olufemi Olukunle
Keyword(s):  
Allium Cepa ◽  
Methanol Extract ◽  
Biological Activities ◽  
Hot Water ◽  
Control Group ◽  
Tail Flick ◽  
Control Groups ◽  
Inflammatory Models ◽  
Paw Oedema ◽  
Anti Inflammatory

Abstract Objectives Several cultivars of Allium cepa L. have been studied for anti-inflammatory and analgesic activities but there is inadequate information on such biological activities of the concentrated extracts of the Nigerian grown red cultivar A. cepa bulb. Methods The anti-inflammatory models used in this study were Carrageenan-induced paw oedema and formalin-induced paw lick in rats, while acetic acid-induced abdominal writhing, hot plate reaction, hot water tail flick tests in mice were the analgesic models. Results At 30 min post-induction (pi), the inhibition of paw oedema (62.50%) by 200 mg/kg of methanol extract of red cultivar A. cepa bulb (MERCACB) was significantly (p<0.001) higher than that of indomethacin (15.63%) at 10 mg/kg. The paw oedema inhibition at 60 min pi by MERCACB (76.92%) was significantly higher than that of indomethacin (41.03%). At the early phase of formalin paw-lick test, the pain reaction time (PRT) of rat treated with MERCACB (400 mg/kg) was significantly lower than that of indomethacin and the control groups. The hotplate test revealed that PRT of mice treated with 800 mg/kg of MERCACB were significantly (p<0.01) longer in comparism to indomethacin and control groups. The PRT of mice subjected to thermal pain due to hot water and treated with 800 mg/kg of MERCACB was significantly (p<0.05) longer than that of the control group. Conclusions These findings indicate that MERCACB possesses potent anti-inflammatory and analgesic properties which confirm the traditional use of the plant for the treatment of inflammatory diseases and may be useful as a future therapeutic agent.

scholarly journals Evaluation of Bioactivities of Gouania tiliaefolia Lam., an Indigenous Traditional Medicinal Plant of Bangladesh

2019 ◽  
Vol 22 (2) ◽  
pp. 200-207
Author(s):  
Tufael Ahmed ◽  
Rifat Khan ◽  
Nafisa Tabassum ◽  
Fahima Aktar ◽  
Mohammad Kaisarul Islam
Keyword(s):  
Body Weight ◽  
Blood Glucose ◽  
Analgesic Activity ◽  
Methanol Extract ◽  
Phenolic Content ◽  
Total Phenolic ◽  
Oral Glucose ◽  
Tail Flick ◽  
Cytotoxic Activities ◽  
Crude Methanol Extract

The crude methanol extract of Gouania tiliaefolia Lam. was partitioned by the modified Kupchan method and the fractions were evaluated for total phenolic content, antioxidant, cytotoxic, thrombolytic, hypotonic and heat-induced membrane stabilizing activities. The petroleum ether soluble fraction (PESF) and methanol extract (ME) showed the highest phenolic content of 78.30 ±1.60 mg and 70.37 ± 0.84 mg, respectively, which were expressed in gallic acid equivalent (GAE). Similar trends were observed in case of anti-oxidant and cytotoxic activities, where the PESF possessed the highest free radical scavenging activity and brine shrimp lethality (IC50 = 2.88 ± 0.02 μg/ml, LC50 = 2.59 ± 0.14 μg/ml), followed by ME (IC50 = 4.79 ± 0.17 μg/ml, LC50 = 3.38 ± 0.08 μg/ml) and CSF (IC50 = 37.51 ± 0.96 μg/ml, LC50 = 73.55 ± 0.26 μg/ml). In case of assays for thrombolytic and membrane stabilizing activities, all extractives showed insignificant results compared to the respective standards. The crude methanol extract of G. tiliaefolia was used to examine the in-vivo analgesic (central and peripheral), antidiarrheal and antidiabetic activities in Swiss albino mice. In case of castor oil induced diarrhea, the ME gave better reduction of diarrhea by 71.43% (at 400 mg/kg-body weight) compared to loperamide (64.29%). Antidiabetic activity was evaluated by oral glucose tolerance test and the ME showed 71.42% and 75.39% reduction of blood glucose at doses 200 and 400 mg/kg-body weight, respectively when compared with the standard glibenclamide that reduced blood glucose by 66.17%. The central- and peripheral-analgesic activity was evaluated by the tail-flick test and acetic acid induced writhing test, respectively. In both the cases, ME demonstrated dose-dependent analgesic activity compared to the standards. Bangladesh Pharmaceutical Journal 22(2): 200-207, 2019

scholarly journals Effects of Electroacupuncture on Pain Threshold of Laboring Rats and the Expression of Norepinephrine Transporter andα2 Adrenergic Receptor in the Central Nervous System

2016 ◽  
Vol 2016 ◽  
pp. 1-8
Author(s):  
Qianli Tang ◽  
Qiuyan Jiang ◽  
Suren R. Sooranna ◽  
Shike Lin ◽  
Yuanyuan Feng ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Adrenergic Receptor ◽  
Pain Threshold ◽  
Norepinephrine Transporter ◽  
Control Group ◽  
Tail Flick ◽  
Pregnant Rats ◽  
Tail Flick Test ◽  
The Central Nervous System

To observe the effects of electroacupuncture on pain threshold of laboring rats and the expression of norepinephrine transporter andα2 adrenergic receptor in the central nervous system to determine the mechanism of the analgesic effect of labor. 120 pregnant rats were divided into 6 groups: a control group, 4 electroacupuncture groups, and a meperidine group. After interventions, the warm water tail-flick test was used to observe pain threshold. NE levels in serum, NET, andα2AR mRNA and protein expression levels in the central nervous system were measured. No difference in pain threshold was observed between the 6 groups before intervention. After intervention, increased pain thresholds were observed in all groups except the control group with a higher threshold seen in the electroacupuncture groups. Serum NE levels decreased in the electroacupuncture and MP groups. Increases in NET andα2AR expression in the cerebral cortex and decreases in enlarged segments of the spinal cord were seen. Acupuncture increases uptake of NE via cerebral NET and decreases its uptake by spinal NET. The levels ofα2AR are also increased and decreased, respectively, in both tissues. This results in a decrease in systemic NE levels and may be the mechanism for its analgesic effects.

Assessment of the Analgesic Effect of Centhaquin in Mouse Tail Flick and Hot-Plate Tests

Pharmacology ◽  
2011 ◽  
Vol 88 (5-6) ◽  
pp. 233-241 ◽  
Author(s):  
Shridhar V. Andurkar ◽  
Anil Gulati
Keyword(s):  
Analgesic Effect ◽  
Tail Flick ◽  
Hot Plate

Drastic Decrease in Isoflurane Minimum Alveolar Concentration and Limb Movement Forces after Thoracic Spinal Cooling and Chronic Spinal Transection in Rats

2005 ◽  
Vol 102 (3) ◽  
pp. 624-632 ◽  
Author(s):  
Steven L. Jinks ◽  
Carmen L. Dominguez ◽  
Joseph F. Antognini
Keyword(s):  
Spinal Cord ◽  
Spinal Cord Injury ◽  
Minimum Alveolar Concentration ◽  
Tail Flick ◽  
Noxious Stimulation ◽  
Partial Recovery ◽  
Spinal Transection ◽  
Thoracic Spinal ◽  
Cord Injury ◽  
Stimulation Of

Background Individuals with spinal cord injury may undergo multiple surgical procedures; however, it is not clear how spinal cord injury affects anesthetic requirements and movement force under anesthesia during both acute and chronic stages of the injury. Methods The authors determined the isoflurane minimum alveolar concentration (MAC) necessary to block movement in response to supramaximal noxious stimulation, as well as tail-flick and hind paw withdrawal latencies, before and up to 28 days after thoracic spinal transection. Tail-flick and hind paw withdrawal latencies were measured in the awake state to test for the presence of spinal shock or hyperreflexia. The authors measured limb forces elicited by noxious mechanical stimulation of a paw or the tail at 28 days after transection. Limb force experiments were also conducted in other animals that received a reversible spinal conduction block by cooling the spinal cord at the level of the eighth thoracic vertebra. Results A large decrease in MAC (to &lt;/= 40% of pretransection values) occurred after spinal transection, with partial recovery (to approximately 60% of control) at 14-28 days after transection. Awake tail-flick and hind paw withdrawal latencies were facilitated or unchanged, whereas reflex latencies under isoflurane were depressed or absent. However, at 80-90% of MAC, noxious stimulation of the hind paw elicited ipsilateral limb withdrawals in all animals. Hind limb forces were reduced (by &gt;/= 90%) in both chronic and acute cold-block spinal animals. Conclusions The immobilizing potency of isoflurane increases substantially after spinal transection, despite the absence of a baseline motor depression, or "spinal shock." Therefore, isoflurane MAC is determined by a spinal depressant action, possibly counteracted by a supraspinal facilitatory action. The partial recovery in MAC at later time points suggests that neuronal plasticity after spinal cord injury influences anesthetic requirements.

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