Antinociceptive Activity of the Essential Oil Formulation from the Roots of Saussaura lappa Clarks

2020 ◽  
Vol 19 (2) ◽  
pp. 127-132
Author(s):  
Siddig Ibrahim Abdelwahab ◽  
Shyam Sunder Pancholi ◽  
Syam Mohan ◽  
Muhammad Hadi Sultan ◽  
Pankaj Tripathi ◽  
...  

Saussurea lappa Clarke (Compositae) is well known as a medicinal plant. Its roots are traditionally used in alleviating pain and swelling. In the current research, we have evaluated the antinociceptive activity of essential oil obtained from the roots of S. lappa. In addition, the development and evaluation of a pharmaceutical-grade cream was also conducted in this study. Extraction of essential oil from the roots of the plant was performed by a steam distillation method using the Clevenger apparatus. The antinociceptive activity was assessed in Sprague Dawley rats using tail flick, hot plate, and analgesic-meter, where diclofenac was used as a standard reference analgesic agent. S. lappa showed analgesic activity in all test systems in a dose- and time-dependent manner. In addition, the formulated cream obtained from the essential oil showed very promising pharmaceutical and pharmacological properties. The analgesic activity of S. lappa may be due to its interaction with opioid receptors and involvement of peripheral analgesia. The ability of S. lappa to show both slow- and fast-onset analgesic effects suggests it could be used as a drug candidate for pain management. The current findings thus warrant further research in the development of this novel analgesic agent.

Author(s):  
Yajnesh P. Sahu ◽  
Sachchidanand Pandey ◽  
Sabita Mohapatra

Background: Currently, two classes of analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics are used to manage pain in different clinical situations. Chronic uses of these drugs have various adverse effects like gastric ulceration/bleeding, analgesic nephropathy and respiratory depression, physical dependence, addiction, respectively. Xanthine oxidase inhibitors, used for chronic gout, might have a role in alleviation of pain, as per literature survey. Hence, the present study was carried out to evaluate the potential analgesic activity of allopurinol and febuxostat in different experimental models.Methods: The analgesic activity of allopurinol and febuxostat was assessed by employing two different experimental pain models-tail flick latency model in rats for central analgesia and acetic acid induced writhing model in mice for peripheral analgesia and was compared with tramadol and aspirin.Results: Allopurinol and febuxostat produced significant central and peripheral analgesic effects as is evident from increase in reaction time in tail flick test and inhibition in number of writhes in acetic acid induced writhing test.Conclusions: The results of the present study demonstrate marked analgesic effect of allopurinol and febuxostat.


Author(s):  
Mimouna Yakoubi ◽  
Nasser Belboukhari ◽  
Khaled Sekkoum ◽  
Mohammed Bouchekara ◽  
Hassan Y. Aboul-Enein

Warionia saharae Benth & Coss (W.s) (Asteraceae) is a monospecific genus endemic to Algeria and Morocco. Its leaves are used in their traditional medicine, such as gastrointestinal and inflammatory diseases; for instance, rheumatoid arthritis treatment. In this work, our team investigated the anti-inflammatory and analgesic effects of essential oil extracted from the dried upper parts of Warionia saharae based on different standard experimental test models. The analgesic activity was assessed by central and peripheral models, such as “hot plate” and “writhing” tests on Swiss albino mice. The hot plate test used latency measurements to assess acute cutaneous pain sensitivity, as a result; the latency of the hind-paw pain response was by licking and either shaking or jumping, those occurrences were recorded. Writhing test as a chemical method used to induce pain of peripheral origin in mice by injecting acetic acid intraperitoneally (IP). This results in characteristic stretching behavior of the animals (cramps and contortions). The evaluation of the analgesic activity, shows that the essential oil of this plant induces a decrease in the number of abdominal cramps in the contortion test and a maximum inhibition of pain. As for the anti-inflammatory effect, it was studied by the “paw edema” test, a phlogogenic agent (formaldehyde) was used to stimulate inflammation in the paws of mice. Anti-inflammatory properties can be observed by inhibiting this edema compared to the standard drug Diclofenac. In conclusion, Warionia saharae essential oil (75 mg/kg) showed a strong anti-inflammatory and analgesic activities which supports the conventional use of this plant in traditional medicine.


Author(s):  
Tayfun Baser ◽  
Ercan Ozdemir ◽  
Ahmet Kemal Filiz ◽  
Ahmet Sevki Taskiran ◽  
Sinan Gursoy

Ghrelin is a peptide hormone released from the gastric endocrine glands and shows analgesic activity apart from its various physiological effects. Nevertheless, the effects of ghrelin receptor (GHS-R) agonists on morphine analgesia and tolerance have not been elucidated yet. The purpose of the study was to evaluate the effects of the ghrelin receptor agonist hexarelin and antagonist [D-Lys3]-GHRP-6 on morphine antinociception and tolerance in rats. A total of 104 Wistar albino male adults rats (weighing approximately 220-240 g) were used in the experiments. To induce morphine tolerance a 3-day cumulative dose regimen was used in rats. Then, randomly selected rats were evaluated for morphine tolerance on day 4. The analgesic effects of hexarelin (0.2 mg/kg), [D-Lys3]-GHRP-6 (10 mg/kg), and morphine (5 mg/kg) were measured at 30-min intervals (0, 30, 60, 90, and 120 min) by tail-flick and hot-plate analgesia tests. The findings suggest that hexarelin in combination with morphine attenuates analgesic tolerance to morphine. On the other hand, ghrelin receptor antagonist [D-Lys3]-GHRP-6 has no significant analgesic activity on the morphine tolerance in analgesia tests. Besides, co-administration of hexarelin and morphine increases the analgesic effect. In conclusion, these data indicate that administration of GHS-R agonist hexarelin with morphine enhances the antinociception and attenuates morphine tolerance.


Author(s):  
N. Michael Antony ◽  
Jennifer Fernandes ◽  
Jane Mathew

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.


Marine Drugs ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 135 ◽  
Author(s):  
Xiujie Liu ◽  
Ge Yao ◽  
Kang Wang ◽  
Yanli Liu ◽  
Xiukun Wan ◽  
...  

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.


Author(s):  
Yasmeen A. Maniyar ◽  
Dasari Sriraj

Background: Vitex negundo Linn (Family: Verbenaceae), locally known as ‘Nirgundi’ an important medicinal plant is a woody, aromatic shrub growing to a small tree. It commonly bears tri- or penta-foliate leaves on quadrangular branches, which give rise to bluish-purple coloured flowers in branched tomentose cymes. It has been claimed to possess analgesic activity apart from many medicinal properties. The aim of the present study was to evaluate both the peripheral and central analgesic activity of ethanolic extract of Vitex negundo flowers (EEVNF) in experimental animals.Methods: Acute toxicity test was done following the Organization of Economic Cooperation and Development guidelines. EEVNF (100mg/kg, 200mg/kg, and 400 mg/kg body weight [b.w.] p.o) was evaluated for peripheral analgesic activity by the acetic acid (0.7%) induced writhing test and central analgesic activity by the tail flick method respectively using aspirin (100mg/kg b.w. and 300mg/kg b.w.) as the standard drug.Results: EEVNF significantly decreased the number of writhing in writhing test at all the doses (p<0.001) and increased the reaction time in tail-flick method (p<0.001) at all the doses when compared to control. EEVNF in the dosage of 400mg/kg b.w. produced analgesic effects which was comparable with that of the standard drug aspirin at dose 100mg/kg b.w in writhing test and produced greater analgesic activity than that of standard drug aspirin at dose 300mg/kg b.w in tail flick method.Conclusions: EEVNF has significant peripheral and central analgesic activity.


2000 ◽  
Vol 93 (2) ◽  
pp. 520-528 ◽  
Author(s):  
Tomoyuki Kawamata ◽  
Keiichi Omote ◽  
Hajime Sonoda ◽  
Mikito Kawamata ◽  
Akiyoshi Namiki

Background The studies on the mechanisms of ketamine antinociception have led to conflicting results. In this study, the authors investigated the contribution of supraspinal monoaminergic descending inhibitory system to ketamine analgesia for acute nociception and inflammation-induced hyperalgesia. Methods Male Sprague-Dawley rats were used. The paw withdrawal latencies to radiant heat stimuli were measured to assess the thermal nociceptive threshold. The analgesic effects of intrathecal or intraperitoneal ketamine were examined in the rats that received unilateral intraplantar carrageenan and in those that were untreated. In addition, it was examined whether pretreatment with intrathecal yohimbine or methysergide inhibited the analgesic effects of ketamine. Using an intrathecal microdialysis method, noradrenaline and 5-hydroxytryptamine concentrations in lumbar cerebrospinal fluid were measured after intraperitoneal ketamine in both saline- and carrageenan-treated rats. Results In the untreated rats, intraperitoneal but not intrathecal ketamine produced antinociceptive effects in a dose-dependent manner. Pretreatment with intrathecal yohimbine or methysergide inhibited these antinociceptive effects. Intraplantar carrageenan significantly reduced paw withdrawal latencies on the injected paw but not on the contralateral paw. Both intraperitoneal and intrathecal ketamine reversed the shortened paw withdrawal latencies on the injected side in a dose-dependent manner without any effects on the contralateral side. Neither yohimbine nor methysergide inhibited these antihyperalgesic effects. In analyses of monoamines, the magnitude of increase in monoamines after intraperitoneal ketamine was significantly smaller in the carrageenan-treated rats than in the saline-treated rats. Conclusion These results demonstrated that ketamine produced antinociceptive effects through an activation of the monoaminergic descending inhibitory system, whereas, in a unilateral peripheral inflammation-induced hyperalgesic state, the monoaminergic system did not contribute to the antihyperalgesic effects of ketamine. The mechanisms of the antinociceptive and antihyperalgesic properties of ketamine are different.


2007 ◽  
Vol 2 (12) ◽  
pp. 1934578X0700201 ◽  
Author(s):  
Vietla S. Rao ◽  
Juliana L. Maia ◽  
Francisco A. Oliveira ◽  
Thelma L.G. Lemos ◽  
Mariana H. Chaves ◽  
...  

The chemical composition of the essential oil from Protium heptaphyllum resin was analyzed by GC/MS and the oil examined for antinociceptive activity in chemical and thermal tests. Fourteen compounds were characterized, representing 95.8% of the total essential oil, with the monoterpenes α-phellandrene (10.4%), α-terpinene (13.7%) and 1,8-cineole (58.7%) as major components. Oral administration of the essential oil (50 and 100 mg/kg) significantly inhibited chemical nociception induced by capsaicin and formalin in mice. In rats, the oil also effectively enhanced the radiant heat-induced tail-flick latency response at a dose of 100 mg/kg. However, the essential oil, at either dose, was ineffective against thermal pain in the hot-plate test.


Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4355
Author(s):  
Alok K. Paul ◽  
Nuri Gueven ◽  
Nikolas Dietis

Efficient repetitive clinical use of morphine is limited by its numerous side effects, whereas analgesic tolerance necessitates subsequent increases in morphine dose to achieve adequate levels of analgesia. While many studies focused on analgesic tolerance, the effect of morphine dosing on non-analgesic effects has been overlooked. This study aimed to characterize morphine-induced behavior and the development and progression of morphine-induced behavioral tolerance. Adult male Sprague–Dawley rats were repetitively treated with subcutaneous morphine for 14 days in two dose groups (A: 5 mg/kg/day (b.i.d.) → 10 mg/kg/day; B: 10 mg/kg/day (b.i.d.) → 20 mg/kg/day). Motor behavior was assessed daily (distance traveled, speed, moving time, rearing, rotation) in an open-field arena, before and 30 min post-injections. Antinociception was measured using tail-flick and hot-plate assays. All measured parameters were highly suppressed in both dosing groups on the first treatment day, followed by a gradual manifestation of behavioral tolerance as the treatment progressed. Animals in the high-dose group showed increased locomotor activity after 10 days of morphine treatment. This excitatory phase converted to an inhibition of behavior when a higher morphine dose was introduced. We suggest that the excitatory locomotor effects of repetitive high-dose morphine exposure represent a signature of its behavioral and antinociceptive tolerance.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Gao Wu ◽  
Hanbin Wu

Objective. To evaluate the synergistic analgesic effect of essential oil ofZanthoxylum schinifoliumSieb. et Zucc. (EOZ) and verapamil (Ver).Method. The qualitative and quantitative composition of EOZ were determined with gas chromatography/Mass spectrometer. The interaction between EOZ and Ver in antinociceptive activity was evaluated by using acetic acid-induced writhing, hot plate, and tail flick tests in mice and in isolated toad sciatic nerve test.Results. Linalool, limonene, and sabinene are the major components of EOZ. EOZ (middle-dose: 40 mg·kg−1, high-dose: 80 mg·kg−1) and EOZ + Ver (Each dose group) have remarkable analgesic effects on pain in mice induced by acetic acid-induced writhing, hot plate, and tail flick tests. Low-dose EOZ (20 mg·kg−1) had no analgesic action, but when it is combined with Ver it has shown significant antinociception. Verapamil has a faint analgesic effect but was not able to inhibit action potential transmission in toad sciatic nerve. EOZ (0.2%) and EOZ + Ver (0.2% + 0.05%) also inhibited action potential transmission in toad sciatic nerve. Combination of EOZ with Ver had a greater analgesic effect and inhibition of nerve action potential transmission compared to its components EOZ and Ver.Conclusion. The combination of EOZ with Ver produces a synergistic analgesic effect.


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