scholarly journals Antinociceptive Effect of Single Components Isolated from Agrimonia pilosa Ledeb. Extract

2019 ◽  
Vol 87 (3) ◽  
pp. 18
Author(s):  
Jing Hui Feng ◽  
Hee Jung Lee ◽  
Set Byeol Kim ◽  
Jeon Sub Jung ◽  
Soon Sung Lim ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Formalin Injection ◽  
Second Phase ◽  
Dependent Manner ◽  
Thermal Pain ◽  
Icr Mice ◽  
Chemically Induced ◽  
Pain Models ◽  
Antinociceptive Effects ◽  
Dose Dependent

Agrimonia pilosa Ledeb. produces an antinociceptive effect in ICR mice in both chemically induced and thermal pain models. In the present study, we examined the antinociceptive effects of single components isolated from Agrimonia pilosa Ledeb. (AP) extract in ICR mice. Three active compounds isolated from AP, including rutin, luteolin-7-O-glucuronide, and apigenin-7-O-glucuronide, were isolated and identified by comparing EI-MS, 1H-, 13C-NMR, and UV. We studied the antinociceptive effects of three single components administered orally at doses of 10 and 20 mg/kg in monosodium urate (MSU)-treated pain model as measured by von Frey test. Among these compounds, apigenin-7-O-glucuronide was more effective in the production of antinociceptive effects. We further characterized the antinociceptive effects and possible mechanisms of apigenin-7-O-glucuronide in writhing and formalin tests. Oral administration of Apigenin-7-O-glucuronide caused a reduction in the number of writhing and effectively reduced the pain behavior observed during the second phase of the formalin test in a dose-dependent manner. In addition, the pretreatment of yohimbine instead of naloxone or methysergide attenuated apigenin-7-O-glucuronide-induced antinociception in the writhing test. Moreover, apigenin-7-O-glucuronide caused reduction in the expression of p-P38, p-CREB, and p-mTOR induced by formalin injection. Our results indicate that apigenin-7-O-glucuronide shows an antinociceptive effect in various pain models. In addition, spinal α2-adrenergic receptors appear to be involved in the production of antinociception induced by apigenin-7-O-glucuronide. Furthermore, the antinociceptive effect of apigenin-7-O-glucuronide appears to be mediated by reduction in the expression of p-P38, p-CREB and p-mTOR levels in the spinal cord.

Antinociceptive Profiles of Platycodin D in the Mouse

2004 ◽  
Vol 32 (02) ◽  
pp. 257-268 ◽  
Author(s):  
Seong-Soo Choi ◽  
Eun-Jung Han ◽  
Tae-Hee Lee ◽  
Ki-Jung Han ◽  
Han-Kyu Lee ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Control Level ◽  
Tail Flick ◽  
Triterpene Saponins ◽  
Tail Flick Test ◽  
Platycodin D ◽  
Pain Models ◽  
Antinociceptive Effects ◽  
Dose Dependent ◽  
Higher Doses

Platycodin D (PD), one of several triterpene saponins, was isolated from roots of Platycodon grandiflorum. We previously reported that intracerebroventricular (i.c.v.) administration of PD showed an antinociceptive effect as measured by the tail-flick assay. However, its exact role in the regulation of antinociception in the various types of pain models has not yet been characterized. Thus, we attempted to find antinociceptive profiles of PD in various pain models. PD administered intraperitoneally (i.p.), i.c.v. or intrathecally (i.t.) showed antinociceptive effects in dose-dependent manners as measured by the tail-flick, writhing and formalin tests. In the tail-flick test, PD at the low doses reached the peak after 15 minutes and returned to the control level after 60 minutes. However, higher doses of PD showed a strong antinociception at least for 1 hour. PD administered i.t. showed stronger antinociception than that induced by i.c.v. administration PD in both tail-flick and writhing tests. In the formalin test, PD administered i.p., i.c.v. or i.t. showed antinociceptive effects during both the first (direct nociceptive stimulation) and second (late inflammatory) phases. Pretreatment with naltrexone i.p., i.c.v. or i.t. did not affect PD-induced inhibition of the tail-flick response. Our results suggest that PD shows a strong antinociceptive effect on the tail-flick, writhing and formalin tests, acting on central nervous system. However, PD-induced antinociception may not be mediated by the opioid receptors.

Evaluation of the Analgesic Effect of Aqueous Extract of Brugmansia suaveolens Flower in Mice: Possible Mechanism Involved

2010 ◽  
Vol 11 (4) ◽  
pp. 345-350 ◽  
Author(s):  
Ana Luiza Muccillo-Baisch ◽  
Alexander Garcia Parker ◽  
Gianni Peraza Cardoso ◽  
Marta Regina Cezar-Vaz ◽  
Maria Cristina Flores Soares
Keyword(s):  
Aqueous Extract ◽  
Benzodiazepine Receptors ◽  
Antinociceptive Effect ◽  
Dependent Manner ◽  
Hot Plate Test ◽  
Antinociceptive Effects ◽  
Brugmansia Suaveolens ◽  
The Central Nervous System ◽  
Dose Dependent ◽  
Abdominal Constriction

The study was conducted to test the aqueous extract of Brugmansia suaveolens (AEBs) flowers for their antinociceptive effects in mice. In the hot plate test, a significant increase in reaction time for two doses of AEBs at 60, 90, 120, and 150 min after treatment was noted. Pretreatment of animals with naloxone (5 mg/kg, intraperitoneally [IP]) left the antinociceptive effect of AEBs at a dose of 100 mg/kg unaffected at 60, 90, 120, and 150 min after treatment and at a dose of 300 mg/kg at 30 min but not at 90, 120, and 150 min. In the writhing test, the AEBs significantly inhibited acetic acid—induced abdominal constriction and was equally potent at both doses. Pretreatment with naloxone (5 mg/kg, IP) left the antinociceptive effect of both doses of AEBs unaffected. Pretreatment with NG-nitro-L-arginine methyl ester (L-NAME; 20 mg/kg, IP) caused a significant change in the number of abdominal constrictions but did not change the antinociceptive effect of AEBs. Pretreatment of animals with methylene blue also did not change the effect of AEBs on the number of writhing movements in mice. Flumazenil (5 mg/kg, IP) antagonized the antinociceptive effects of diazepam and also reversed the antinociceptive effect of AEBs. AEBs showed a depressant effect on the central nervous system, and the treatment of mice with pentobarbital combined with AEBs increased the animals’ sleeping time in a dose-dependent manner. These results suggest that the antinociceptive activity of AEBs may be related in part to benzodiazepine receptors, although peripheral mechanisms cannot be excluded.

scholarly journals Comparison of antinociceptive effect of the antiepileptic drug gabapentin to that of various dosage combinations of gabapentin with lamotrigine and topiramate in mice and rats

2011 ◽  
Vol 02 (02) ◽  
pp. 130-136 ◽  
Author(s):  
Keshab Raj Paudel ◽  
SK Bhattacharya ◽  
GP Rauniar ◽  
BP Das
Keyword(s):  
Pain Perception ◽  
Late Phase ◽  
Antinociceptive Effect ◽  
Experimental Pain ◽  
Mechanical Hyperalgesia ◽  
Tail Flick ◽  
Hot Plate ◽  
Analgesic Effects ◽  
Pain Models ◽  
Antinociceptive Effects

ABSTRACT Introduction: Newer anticonvulsants have a neuromodulatory effect on pain perception mechanisms in a hyperexcitable and damaged nervous system. Aim: This study was designed to study the analgesic effects of gabapentin alone and in combination with lamotrigine and topiramate in experimental pain models. Materials and Methods: Adult albino mice (n = 490) weighing 20–30 g and rats (n = 130) weighing 100–200 g were injected intraperitoneally with gabapentin, lamotrigine, and topiramate alone and in different dose combinations. The hot-plate method, tail-flick method, capsaicin-induced mechanical hyperalgesia, and formalin assay were used to assess the antinociceptive effects. Results: Of the three antiepileptic drugs, when given separately, gabapentin was more efficacious than either topiramate or lamotrigine in all the pain models. Combination of 25 mg/kg gabapentin with 25 mg/kg topiramate was more efficacious (P <.05) than 50 mg/kg gabapentin alone in the capsaicin-induced mechanical hyperalgesia test. Similarly, 50 mg/kg gabapentin with 50 mg/kg topiramate or 5 mg/kg lamotrigine was more efficacious (P <.05) than 50 or 100 mg/kg gabapentin alone in late-phase formalin-induced behaviors. Conclusions: Combination of gabapentin with either lamotrigine or topiramate produced better results than gabapentin alone in capsaicin-induced mechanical hyperalgesia test and in late-phase formalin-induced behaviors.

Effect of galanin on glucose-, arginine-, or potassium-stimulated insulin release

1989 ◽  
Vol 256 (5) ◽  
pp. E619-E623
Author(s):  
T. Yoshimura ◽  
J. Ishizuka ◽  
G. H. Greeley ◽  
J. C. Thompson
Keyword(s):  
Insulin Release ◽  
High Glucose ◽  
Second Phase ◽  
Dependent Manner ◽  
Perfused Pancreas ◽  
Isolated Perfused Pancreas ◽  
Second Phases ◽  
High Concentrations ◽  
Dose Dependent ◽  
Stimulation Of

We have examined the effect of galanin infusion on glucose-stimulated release of insulin from the isolated perfused pancreas of the rat to better characterize the effect of galanin on the first and second phases of insulin release. The effects of galanin on insulin release stimulated by L-arginine or high concentrations of potassium were also examined. When perfusion of galanin was started 4 min before the start of perfusion of high glucose (16.7 mM), galanin (10(-8)-10(-11) M) inhibited both the first and second phases of insulin release in a dose-dependent manner. When perfusion of galanin (10(-8) or 10(-9) M) was started simultaneously with high glucose (16.7 mM), only the second phase of insulin release was suppressed (P less than 0.05). Galanin (10(-9) M) failed to inhibit insulin release stimulated by L-arginine (10 and 5 mM) or potassium (25 and 20 mM). These findings suggest that the inhibitory action of galanin on glucose-stimulated insulin release is exerted on early intracellular events that occur during the stimulation of insulin release and that are common to both phases. Because galanin does not inhibit insulin release stimulated by L-arginine or potassium, galanin may inhibit glucose-stimulated closure of potassium channels.

Oxytocin affects apical sodium conductance in rabbit cortical collecting duct

1993 ◽  
Vol 265 (4) ◽  
pp. F487-F503 ◽  
Author(s):  
T. Inoue ◽  
M. Naruse ◽  
M. Nakayama ◽  
K. Kurokawa ◽  
T. Sato
Keyword(s):  
Receptor Antagonist ◽  
Collecting Duct ◽  
Rat Kidney ◽  
Physiological Role ◽  
Free Calcium ◽  
Second Phase ◽  
Dependent Manner ◽  
Cortical Collecting Duct ◽  
Acetoxymethyl Ester ◽  
Dose Dependent

The physiological role of oxytocin (OT) in the kidney is still unclear, although autoradiographic data have shown the existence of OT receptors in the rat kidney. We examined the effect of OT in the microperfused rabbit cortical collecting duct (CCD) by using conventional cable analysis and microscope photometry. On addition of 10(-9) M OT to the bath, the lumen-negative transepithelial voltage (VT) transiently increased and the transepithelial resistance (RT) and the fractional resistance of the apical membrane (FRA) (1st phase) both decreased. After this initial change, the lumen-negative VT gradually decreased below its baseline level and RT and FRA (second phase) both increased. These electrical changes were dose dependent and were prevented by the addition of 10(-5) M amiloride to the lumen. Although responses to OT were not prevented by 10(-9) M arginine vasopressin (AVP) or 10(-6) M of a V1-receptor antagonist (OPC-21268) or V2-receptor antagonist (OPC-31260), they were inhibited by the addition of the specific OT antagonist des-Gly-NH2-[d(CH2)3,Tyr(Me),Thr]OVT. Additional studies of intracellular free calcium ([Ca2+]i) revealed that 10(-8)-10(-6) M OT caused an increase in [Ca2+]i in CCD in a dose-dependent manner. Also, pretreatment with 2 x 10(-8) M bis-(aminophenoxy)ethane-tetraacetic acid-acetoxymethyl ester, an intracellular Ca2+ chelator, abolished the electrical and [Ca2+]i responses to OT. Pretreatment with 5 x 10(-4) M 8-(4-chlorophenylthio)-adenosine 3',5'-cyclic monophosphate (CPT-cAMP) partially prevented the electrical responses to OT, thus reducing the decrease in lumen-negative VT below its basal level and the increase in RT after the 1st phase. These data show that OT affects the apical Na+ conductance of collecting duct cells through OT receptors distinct from the AVP receptors and that the effect of OT may, at least in part, be brought about by a mechanism(s) dependent on the increase in [Ca2+]i and cAMP production.

Nitrous Oxide Revisited

2005 ◽  
Vol 103 (4) ◽  
pp. 845-854 ◽  
Author(s):  
Philippe Richebé ◽  
Cyril Rivat ◽  
Cyril Creton ◽  
Jean-Paul Laulin ◽  
Pierre Maurette ◽  
...  
Keyword(s):  
Nitrous Oxide ◽  
Morphine Tolerance ◽  
Acute Tolerance ◽  
Dependent Manner ◽  
Analgesic Effects ◽  
Pain Models ◽  
Opioid Induced Hyperalgesia ◽  
Incisional Pain ◽  
Fentanyl Administration ◽  
Dose Dependent

Background Although opioids are unsurpassed analgesics for surgery, they also induce an N-methyl-D-aspartate-dependent enhancement of postoperative hyperalgesia. Because nitrous oxide (N2O) has anti-N-methyl-D-aspartate properties, the purpose of this study was to evaluate nitrous oxide ability to prevent such an opioid-induced hyperalgesia in rats. Methods First, preventive effects of 50/50% N2O-O2 on the development of delayed hyperalgesia observed after inflammatory pain (hind paw carrageenan injection on D0) were examined for several days. Second, the ability of nitrous oxide (10-40%) to limit opioid-induced hyperalgesia induced by fentanyl was evaluated in nonsuffering rats. Third, antihyperalgesic effects of various nitrous oxide concentrations (20-50%) were assessed in both inflammatory and incisional pain models in fentanyl-treated rats (4 x 100 microg/kg subcutaneously). Finally, the analgesic effect of a single dose of morphine was evaluated 24 h after fentanyl administration and nitrous oxide (D0) to assess its preventive effect on acute morphine tolerance in both nonsuffering and hind paw-incised rats. Results When applied on D0, nitrous oxide reduced delayed hyperalgesia induced by inflammation. Exposure to nitrous oxide on D0 also reduced opioid-induced hyperalgesia in nonsuffering rats in a dose-dependent manner. In fentanyl-treated rats with inflammatory or incisional pain, nitrous oxide strongly limited both magnitude and duration of hyperalgesia. Moreover, nitrous oxide exposure on D0 opposed development of acute tolerance to analgesic effects of morphine administered on D1 in both nonsuffering and incised fentanyl-treated rats. Conclusions Nitrous oxide, an N-methyl-D-aspartate receptor antagonist, prevented the enhancement of pain sensitivity induced by both nociceptive inputs and fentanyl and opposed acute morphine tolerance. Results suggest that perioperative nitrous oxide use reduces exaggerated postoperative pain and morphine consumption.

scholarly journals Antinociceptive and Anti-edematous Activities of the Essential Oils of Two Balkan EndemicLaserpitium Species

2014 ◽  
Vol 9 (1) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Višnja Popović ◽  
Silvana Petrović ◽  
Maja Tomić ◽  
Radica Stepanović-Petrović ◽  
Ana Micov ◽  
...  
Keyword(s):  
Essential Oil ◽  
Essential Oils ◽  
Antinociceptive Effect ◽  
Dependent Manner ◽  
Paw Edema ◽  
Oral Gavage ◽  
Inflammatory Conditions ◽  
Pressure Test ◽  
Male Wistar Rats ◽  
Dose Dependent

In this paper antinociceptive and anti-edematous effects are examined of the essential oils of the underground parts of two Balkan endemic Laserpitium species (Apiaceae), L. zernyi and L. ochridanum. Furthermore, the essential oil of the underground parts of L. ochridanum is chemically characterised by GC and GC-MS. Antinociceptive and anti-edematous effects were measured in a rat model of localized inflammation, induced by carrageenan, using apparatus for the modified paw-pressure test, and plethysmometer, respectively. The effects of both Laserpitium essential oils were measured after oral gavage administration to male Wistar rats in doses of 25, 50 and 100 mg/kg. The main constituents of L. ochridanum essential oil were: α-pinene (33.2%), α-bisabolol (10.3%) and chamazulene (14.9%). The essential oil of L. zernyi was previously shown to be rich in α-pinene (31.6%) and α-bisabolol (30.9%). Both examined essential oils produced a significant dose-dependent antinociceptive effect. The corresponding ED50±SEM in producing antinociception were 45.9±4.9 mg/kg and 42.4±2.1 mg/kg for L. zernyi and L. ochridanum oil, respectively. Both essential oils also significantly reduced paw edema in a dose-dependent manner. The estimated ED50±SEM values for the anti-edematous effect were 36.3±4.5 mg/kg for L. zernyi oil and 45.1±11.3 mg/kg for L. ochridanum oil. These results suggest that the essential oils of both investigated Laserpitium species may be effective against pain and edema present in various inflammatory conditions.

scholarly journals Anti-arthralgic activity of the n-hexane extract (HTp) of yellow oleander seeds; Thevetia peruviana (Pers.) K. Schum

2021 ◽  
Author(s):  
Joy Ifunanya Odimegwu ◽  
Fatiha Oyebola Olabisi
Keyword(s):  
Scientific Evidence ◽  
Positive Control ◽  
Test Subject ◽  
Dependent Manner ◽  
Thevetia Peruviana ◽  
Relieve Pain ◽  
Pain Models ◽  
Hexane Extracts ◽  
Cardioactive Glycosides ◽  
Dose Dependent

Thevetia peruviana (Pers.) K.Schum. (Apocynaceae) seeds are known to possess cardioactive glycosides such as thevetin A, thevetin B, nerifolin etc. They are also used locally for general pain relief for which there is no scientific evidence to our knowledge. Arthralgia is regarded generally as pain without inflammation. It is endemic in the society and sufferers continue to imbibe pain relieving drugs in their tons all over the world. Analgesic activity test was carried out using the formalin-induced pain models, at 0.1g, 0.2g and 0.3g/kg doses of n-hexane extracts of Thevetia peruviana seeds (HTp) in Wistar mice. Diclofenac was used as positive control. Acute toxicity test was carried out at doses of 1000, 2500 and 5000 mg/kg weight of test subject. It was observed that HTp at concentrations of 0.1g, 0.2g and 0.3g/kg showed significant analgesic effect at compared to the control. The percentage inhibition observed was 29.60%, 44.80% and 50.72% for the early pain phase and 100% for the late pain phase respectively, indicating HTps NSAID-like property. HTp showed the highest percentage inhibition at 300 mg/kg (50.72 %) and significant; P < 0.005 pain reduction. HTp did not produce any toxicity up to a dose of 5000 mg/kg weight which is very interesting as the seeds are known for their toxicity due to the cardiac glycoside presence. The results of the study suggest that HTp does indeed relieve pain significantly in a dose dependent manner, thus justifying its use in management of arthralgia. Keywords: Arthralgia, Herbal medicine, Pain,Thevetia peruviana, yellow oleander

Attenuating Effect of Portulaca oleracea Extract on Chronic Constriction Injury Induced Neuropathic Pain in Rats: An Evidence of Anti-oxidative and Anti-inflammatory Effects

2019 ◽  
Vol 18 (4) ◽  
pp. 342-349 ◽  
Author(s):  
Fatemeh Forouzanfar ◽  
Hossein Hosseinzadeh ◽  
Mohammad B. Khorrami ◽  
Samira Asgharzade ◽  
Hassan Rakhshandeh
Keyword(s):  
Neuropathic Pain ◽  
Chronic Constriction Injury ◽  
Portulaca Oleracea ◽  
Dependent Manner ◽  
Tnf Α ◽  
Antinociceptive Effects ◽  
Drug Treatments ◽  
Thiol Content ◽  
Anti Inflammatory ◽  
Dose Dependent

Background: Neuropathic pain responds poorly to drug treatments. The present study investigated the therapeutic effect of Portulaca oleracea, in chronic constriction injury (CCI)-induced neuropathic pain in rats. Objective & Methods: Neuropathic pain was performed by putting four loose ligatures around the sciatic nerve. CCI resulted in the development of heat hyperalgesia, mechanical allodynia and cold allodynia accompanied by an increase in the contents of TNF-α, IL1β, malondialdehyde, with a reduction in total thiol content. Results: Administration of Portulaca oleracea (100 and 200 mg/kg intraperitoneal) for 14 days in CCI rats significantly alleviated pain-related behaviors, oxidative damage and inflammatory cytokines in a dose-dependent manner. Conclusion: In conclusion, it is suggested that the antinociceptive effects of Portulaca oleracea might be due to antioxidant and anti-inflammatory properties.

Comparison of ramp and square-wave exposure to thyrotrophin-releasing hormone or depolarizing K+ on cytosolic Ca2+ concentration and prolactin secretion in GH4C1 cells

1994 ◽  
Vol 142 (1) ◽  
pp. 145-152
Author(s):  
N Sato ◽  
X Wang ◽  
M A Greer
Keyword(s):  
Hormone Secretion ◽  
Wave Exposure ◽  
Rate Of Change ◽  
Second Phase ◽  
Tissue Fluid ◽  
Dependent Manner ◽  
Thyrotrophin Releasing Hormone ◽  
Releasing Hormone ◽  
Square Wave ◽  
Dose Dependent

Abstract The standard method of studying hormone secretion in vitro is to make instantaneous changes in the concentration of stimulators in the medium. However, in vivo the extracellular concentration of such substances changes more gradually; secretion does not occur in square-wave bursts and agonists or antagonists transmitted through the bloodstream are diluted and diffused by plasma or tissue fluid to further decelerate the rate of change in concentration at the cell surface. We have therefore compared in GH4C1 cells the dynamics of changes in cytosolic Ca2+ concentration ([Ca2+]i) and prolactin (PRL) secretion in response to two very different secretagogues, thyrotrophin-releasing hormone (TRH) and depolarizing K+, using a square-wave or ramp exposure for 5 min. The dynamics of hormone secretion were analysed by column perifusion (2 × 106 cells/column). Ca2+ dynamics were monitored by dual excitation microfluorimetry from 20–30 optically isolated cells using the Ca2+ indicator, fura-2. With square-wave exposure, both TRH (0·1–100 nm) and K+ (10–50 mm) induced dose-dependent increases in [Ca2+]i and PRL secretion. Concentrations of TRH >1 nm caused a two-phase increase in [Ca2+]i with an initial high-amplitude first phase and a low-amplitude second phase. Depolarizing K+ induced a sharp increase in [Ca2+]i which peaked within 15 seconds, then declined gradually on a sloping plateau. Both TRH and K+ induced an acute dose-dependent PRL secretory burst peaking within 2·5 min with a subsequent rapid decline. With ramp exposure, high doses of TRH (final concentration 10–100 nm) triggered an acute rise in [Ca2+]i; however, the peaks were clearly lower than those induced by the maximum concentration reached given as a square-wave. TRH (0·1–100 nm) induced PRL secretion in a dose-dependent manner. Ramp depolarizing K+ induced dose-dependent parallel 'ramp' increases in [Ca2+]i concentration and PRL secretion without a 'burst' rise in either. These data suggest that a rise in [Ca2+]i plays a more critical role in K+-induced than in TRH-induced PRL secretion; intracellular transduction systems which do not involve [Ca2+]i appear more important for the latter. Journal of Endocrinology (1994) 142, 145–152

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