Evaluation of antipyretic, antinocieptive and sedative effects of Tribulus terrestris, Mimosa pigra and Alkanna tinctoria methanolic extracts

Pain is one of the most common cause for hospital visits. It plays an important role in inflammation and serves as a warning sign to avoid further injury. Analgesics are used to manage pain and provide comfort to patients. However, prolonged usage of pain treatments like opioids and NSAIDs are accompanied with undesirable side effects. Therefore, research to identify novel compounds that produce analgesia with lesser side effects are necessary. The present study investigated the antinociceptive potentials of a natural compound, cardamonin, isolated from Boesenbergia rotunda (L) Mansf. using chemical and thermal models of nociception. Our findings showed that intraperitoneal and oral administration of cardamonin (0.3, 1, 3, and 10 mg/kg) produced significant and dose-dependent inhibition of pain in abdominal writhing responses induced by acetic acid. The present study also demonstrated that cardamonin produced significant analgesia in formalin-, capsaicin-, and glutamate-induced paw licking tests. In the thermal-induced nociception model, cardamonin exhibited significant increase in response latency time of animals subjected to hot-plate thermal stimuli. The rota-rod assessment confirmed that the antinociceptive activities elicited by cardamonin was not related to muscle relaxant or sedative effects of the compound. In conclusion, the present findings showed that cardamonin exerted significant peripheral and central antinociception through chemical- and thermal-induced nociception in mice through the involvement of TRPV1, glutamate, and opioid receptors.

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Investigating the analgesic properties of Kurkinorin, a novel mu-opioid receptor analogue of Salvinorin A

10.26686/wgtn.17060342 ◽

2021 ◽

Author(s):

◽

Nirajmohan Shivaperumal

Keyword(s):

Body Temperature ◽

Inflammatory Pain ◽

Core Body Temperature ◽

Salvinorin A ◽

Mu Opioid ◽

Analgesic Effects ◽

Paw Oedema ◽

Antinociceptive Effects ◽

Core Body ◽

Significant Motor

<p>Background: The mu-opioid receptor (MOPr) activating drugs such as morphine, fentanyl, etorphine and methadone are used to treat moderate to severe pain. However, their long-term use produces serious adverse effects such as respiratory depression, sedation, tolerance, nausea, dependence, and constipation and this signifies the search for an alternate pain therapeutic agent. Here we report the investigation of antinociceptive and side effect profiles of a structurally unique MOPr-activating drug, kurkinorin from Salvinorin A (Sal A) that was compared with morphine and herkinorin. Methods: Adult male B6-SJL mice (22-29 g) were used to investigate the antinociceptive effects of kurkinorin, herkinorin and morphine utilising the 50° C warm-water tail-withdrawal assay. The 2% intra-dermal formalin assay was used to evaluate acute nociceptive and inflammatory pain and paw oedema. The side effect profiles were evaluated by measuring core-body temperature and utilising behavioural tests of motor co-ordination (accelerating rotarod test). Kurkinorin’s rewarding properties were assessed using the conditioned place preference (CPP) assay in male Sprague-Dawley rats (240-350 g). Results: Kurkinorin produced significant antinociceptive effects in the tail-withdrawal assay at both 5 (p<0.01, 10 min, p<0.001, 15-60 min) and 10 mg/kg (p<0.001, 5-90 min, p<0.01, 120 min) and attenuated both nociceptive and inflammatory pain in the 2% intra-dermal formalin model in mice. The analgesic effects of kurkinorin at 10 mg/kg were similar to the analgesic effects of morphine at the same dose. The decrease in pain score in the intra-dermal formalin assay with kurkinorin and morphine produced a corresponding reduction of paw oedema. In comparison, herkinorin had reduced analgesic effects in the tail-withdrawal assay (10 mg/kg, p<0.05, 30 min) and attenuated inflammatory pain in the intra-dermal formalin assay (10 mg/kg, p<0.001) with reduced paw oedema (10 mg/kg, p<0.05). Morphine produced significant motor incoordination effects from 15-60 min post injection whereas kurkinorin produced no significant motor impairment. Kurkinorin and herkinorin (5 mg/kg, i.p) did not produce rewarding effects, whereas morphine produced a significant, rewarding effect in the CPP assay. Kurkinorin produced no change in the core body temperature while morphine significantly reduced the body temperature. Conclusions: Kurkinorin is central acting and is as potent as morphine in attenuating acute nociceptive and inflammatory pain. It produced no significant sedative and rewarding effects. Therefore, kurkinorin has been identified as a structurally new class of mu-opioid analgesic, displaying improvements compared to morphine.</p>

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Investigating the analgesic properties of Kurkinorin, a novel mu-opioid receptor analogue of Salvinorin A

10.26686/wgtn.17060342.v1 ◽

2021 ◽

Author(s):

◽

Nirajmohan Shivaperumal

Keyword(s):

Body Temperature ◽

Inflammatory Pain ◽

Core Body Temperature ◽

Salvinorin A ◽

Mu Opioid ◽

Analgesic Effects ◽

Paw Oedema ◽

Antinociceptive Effects ◽

Core Body ◽

Significant Motor

<p>Background: The mu-opioid receptor (MOPr) activating drugs such as morphine, fentanyl, etorphine and methadone are used to treat moderate to severe pain. However, their long-term use produces serious adverse effects such as respiratory depression, sedation, tolerance, nausea, dependence, and constipation and this signifies the search for an alternate pain therapeutic agent. Here we report the investigation of antinociceptive and side effect profiles of a structurally unique MOPr-activating drug, kurkinorin from Salvinorin A (Sal A) that was compared with morphine and herkinorin. Methods: Adult male B6-SJL mice (22-29 g) were used to investigate the antinociceptive effects of kurkinorin, herkinorin and morphine utilising the 50° C warm-water tail-withdrawal assay. The 2% intra-dermal formalin assay was used to evaluate acute nociceptive and inflammatory pain and paw oedema. The side effect profiles were evaluated by measuring core-body temperature and utilising behavioural tests of motor co-ordination (accelerating rotarod test). Kurkinorin’s rewarding properties were assessed using the conditioned place preference (CPP) assay in male Sprague-Dawley rats (240-350 g). Results: Kurkinorin produced significant antinociceptive effects in the tail-withdrawal assay at both 5 (p<0.01, 10 min, p<0.001, 15-60 min) and 10 mg/kg (p<0.001, 5-90 min, p<0.01, 120 min) and attenuated both nociceptive and inflammatory pain in the 2% intra-dermal formalin model in mice. The analgesic effects of kurkinorin at 10 mg/kg were similar to the analgesic effects of morphine at the same dose. The decrease in pain score in the intra-dermal formalin assay with kurkinorin and morphine produced a corresponding reduction of paw oedema. In comparison, herkinorin had reduced analgesic effects in the tail-withdrawal assay (10 mg/kg, p<0.05, 30 min) and attenuated inflammatory pain in the intra-dermal formalin assay (10 mg/kg, p<0.001) with reduced paw oedema (10 mg/kg, p<0.05). Morphine produced significant motor incoordination effects from 15-60 min post injection whereas kurkinorin produced no significant motor impairment. Kurkinorin and herkinorin (5 mg/kg, i.p) did not produce rewarding effects, whereas morphine produced a significant, rewarding effect in the CPP assay. Kurkinorin produced no change in the core body temperature while morphine significantly reduced the body temperature. Conclusions: Kurkinorin is central acting and is as potent as morphine in attenuating acute nociceptive and inflammatory pain. It produced no significant sedative and rewarding effects. Therefore, kurkinorin has been identified as a structurally new class of mu-opioid analgesic, displaying improvements compared to morphine.</p>

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Chloroformic and Methanolic Extracts of Olea europaea L. Leaves Present Anti-Inflammatory and Analgesic Activities

ISRN Pharmacology ◽

10.5402/2011/564972 ◽

2011 ◽

Vol 2011 ◽

pp. 1-5 ◽

Cited By ~ 5

Author(s):

R Chebbi Mahjoub ◽

M. Khemiss ◽

M. Dhidah ◽

A. Dellaï ◽

A. Bouraoui ◽

...

Keyword(s):

Olea Europaea ◽

Intraperitoneal Administration ◽

Methanolic Extracts ◽

Antinociceptive Effects ◽

Anti Inflammatory ◽

Analgesic Activities ◽

Rats And Mice ◽

Dose Dependent ◽

Inflammatory Effect ◽

Olea Europaéa

Olea europaea L. is used in traditional medicine in the Mediterranean areas. Its natural products are used in the treatment of different disorders, like fighting fever and some infectious diseases such as malaria, the treatment of arrhythmia, and relief of intestinal spasms. The aim of the current study is to investigate the possible anti-inflammatory and anatinociceptive effects of methanol and chloroformic extracts prepared from leaves of Olea europaea L. The anti-inflammatory and antinociceptive effects of the different extracts of Olea europaea leaves were assessed after intraperitoneal administration into rats and mice, using the carrageenan-induced paw edema model in rats to test the anti-inflammatory effect and the acetic acid-induced writhing in mice to test the analgesic effect. The chloroformic and methanolic leaves extracts, studied at the doses of 50, 100, and 200 mg/kg (Body Weight: BW), exhibited significant dose-dependent anti-inflammatory and analgesic activities. Based on the results obtained, it can be concluded that Olea europaea leaves extracts have anti-inflammatory and antinociceptive effects.

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Antinociceptive effects of methanolic extracts of Pistacia aethiopica and Warbugia ugandensis in mice

The Journal of Phytopharmacology ◽

10.31254/phyto.2020.9502 ◽

2020 ◽

Vol 9 (5) ◽

pp. 300-307

Author(s):

Ireri Moses Munene ◽

◽

Njagi Eliud Nyaga Mwaniki ◽

Ngugi Mathew Piero ◽

◽

...

Keyword(s):

Early Phase ◽

Diclofenac Sodium ◽

Late Phase ◽

Folk Medicine ◽

Stem Bark ◽

Phytochemical Screening ◽

Leaf Extracts ◽

Pain Model ◽

Methanolic Extracts ◽

Antinociceptive Effects

Pistacia aethiopica and Warbugia ugandensis are medicinal plants used in folk medicine among the Embu, Kenya. Despite being in use since antiquity, no empirical data is available to validate their claimed use in pain management. This study evaluated the antinociceptive effects of methanolic extracts of these plants in mice. Qualitative phytochemical profile of the methanolic extracts was also established. The antinociceptive studies used formalin pain model. Harbone and Kotaki protocols for qualitative phytochemical screening were used. Stem bark extracts of P. aethiopica inhibited paw licking in mice by between 47.24% 55.13% in the early phase and by between 30.69%-52.12% in the late phase. W. ugandensis leaf extracts inhibited paw licking by between 38.45%- 51.85% in the early phase and by between 43.48%-65.61% in the late phase. Diclofenac sodium inhibited paw licking by between 30.33%- 30.36% in the early phase and by between 62.93% and 77.08% in the late phase. Phytochemical screening revealed presence of saponins, alkaloids, flavonoids, phenols and terpenoids. This study established existence of antinociceptive effects in the methanolic extracts of P. aethiopica and W. ugandensis in mice. The observed effects were ascribed to the presence of phytochemicals working individually or synergistically.

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Sedative and antinociceptive effects of romifidine and xylazine in Thoroughbred mares

Arquivo Brasileiro de Medicina Veterinária e Zootecnia ◽

10.1590/s0102-09352006000600009 ◽

2006 ◽

Vol 58 (6) ◽

pp. 1030-1036 ◽

Cited By ~ 5

Author(s):

F.G. Christovão ◽

G. Zamur ◽

M.I. Mataqueiro ◽

A. Queiroz-Neto

Keyword(s):

Locomotor Activity ◽

Block Design ◽

Antinociceptive Effect ◽

Sedative Effect ◽

Latency Time ◽

Individual Behaviour ◽

Withdrawal Reflex ◽

Antinociceptive Effects ◽

Sedative Effects ◽

Head Height

The sedative and antinociceptive effects of romifidine (0.1mg/kg) and of xylazine (1.0mg/kg) on Thoroughbred mares were studied. Sedation was evaluated by quantifying spontaneous locomotor activity (SLA) and head height (HH) in animals placed in automated individual behaviour stalls. Antinociception was determined utilizing a heat irradiation lamp recording the latency time for the hoof withdrawal reflex (HWRL) and the latency time for the skin twitch reflex (STRL) in a randomised block design with 10 replicates. Comparison of the sedative effects of romifidine and of xylazine on SLA showed a faster effect for xylazine. Regarding the sedative effect of the substances based on HH, romifidine caused a longer-lasting effect. Romifidine caused an increase in HWRL and STRL, and xylazine, an agent known for its analgesic effect, did not have an antinociceptive effect based on STRL result. The antinociceptive effect of romifidine was more pronounced than the xylazine effect.

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Scanning Electron Microscopy and X-Ray Analyses of Dental Tissues from a Hibernator

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100090877 ◽

1976 ◽

Vol 34 ◽

pp. 178-179

Author(s):

M. L. Zimny ◽

A. C. Haller

Keyword(s):

Electron Microscopy ◽

Scanning Electron Microscopy ◽

Body Temperature ◽

Ground Squirrel ◽

Alveolar Bone ◽

X Ray ◽

Dental Tissues ◽

Bone Minerals ◽

Apical Tooth ◽

Scanning Electron

During hibernation the ground squirrel is immobile, body temperature reduced and metabolism depressed. Hibernation has been shown to affect dental tissues varying degrees, although not much work has been done in this area. In limited studies, it has been shown that hibernation results in (1) mobilization of bone minerals; (2) deficient dentinogenesis and degeneration of alveolar bone; (3) presence of calculus and tears in the cementum; and (4) aggrevation of caries and pulpal and apical tooth abscesses. The purpose of this investigation was to study the effects of hibernation on dental tissues employing scanning electron microscopy (SEM) and related x-ray analyses.

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