Hydro-alcoholic extract of Otostegia integrifolia Benth (Lamiacae) produces peripheral antinociception and central analgesia in mice models

2019 ◽  
Author(s):  
Abel Degu Woldesenbete ◽  
Rediet Tesfaye

Abstract Objective Pain and inflammatory conditions are the commonest health problems reported to this date. The advent of numerous pharmacologic agents cannot still abated the demand due to the associated side effects, the search for satisfactory new molecule particularly from herbal sources is the main endeavor as experience shows. Thus, this study evaluated the analgesic activity of the 80% methanol leaf extract of Otostegia integrifolia in mice models of pain.Results Analgesic effect of various oral doses of the hydro-alcoholic extract (100, 200 and 400 mg/kg) was determined in hot plate and acetic acid induced writhing methods. In all models, the higher doses of the extract (400mg/kg) exhibited significant central and peripheral analgesic activities without significant difference compared to the standard drugs morphine and aspirin respectively. However, the lowest dose of the extract lacks central analgesic activity. The experimental finding from this study corroborates perhaps the presence of similar constituents within the genus Otostegia that might be responsible for the analgesic effects observed on other species. Thus, Otostegia integrifolia could be potential source for development of new analgesics.

Author(s):  
Aravind Patil ◽  
Vijaya Chandra Reddy Konda

Background: Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage. In spite of many advances in pain research, we are unable to deal in an effective way. The cost for new drug development is increasing day by day. Drug repurposing is an approach to look for new use in drugs that are already approved for other indications. Mexiletine is a sodium channel blockers that is being approved for treatment of arrhythmias. It is being tried in treatment of various painful conditions. The present study is to evaluate the dose-dependent analgesic activity of mexiletine with ibuprofen.Methods: The analgesic activity of mexiletine was compared at doses of 15mg/kg, 30mg/kg and 45mg/kg with the standard dose of ibuprofen at 10mg/kg in male Wistar rats in thermal model of tail flick analgesiometer.Results: At lower doses (15mg/kg) of mexiletine, analgesic activity of ibuprofen was significantly higher. At higher doses (30 mg/kg and 45 mg/kg) of mexiletine, it was observed that there is no significant difference between the analgesic activities of both drugs.Conclusions: Mexiletine demonstrated a dose-dependent analgesic activity. There was no statistically significant difference between the analgesic activities of higher doses of mexiletine when compared to ibuprofen.


2021 ◽  
Vol 11 (3) ◽  
pp. 3626-3633

This study aimed to investigate hepatoprotective and anti-inflammatory activities of the hydro-alcoholic extract of Oxalis debilis (ODHE) leaves. Acute oral toxicity evaluated ODHE in graded oral doses (100, 500, 1000, 3000, and 5000 mg/kg body weight) in rats. The hepatoprotective activity was evaluated in CCl4 intoxicated rats at 200 and 400 mg/kg body weight doses of ODHE, while anti-inflammatory activity was determined by carrageenan-induced paw edema in rats at 200, 400, 800 mg/kg body weight doses of ODHE. The ODHE was safe at the highest dose of 5000 mg/kg in experimental rats. In hepatoprotective activity, ODHE significantly reduced the serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and total bilirubin (TB) levels as compared to the CCl4control group. On the other hand, ODHE showed an anti-inflammatory effect similar to that of the control group in the carrageenan-induced paw edema model. The histopathological findings showed a significant difference between the ODHE (400 mg/kg) and CCl4 groups. The present experiment showed that ODHE has significant hepatoprotective and anti-inflammatory activities. Results confirm the use of O. debilis in folk medicine in the treatment of hepatotoxicity and inflammation.


2021 ◽  
Vol 12 (3) ◽  
pp. 669-673
Author(s):  
Mahesh S ◽  
Swapnil Y Chaudhari ◽  
Mukesh Nariya ◽  
Patgiri B J

Background: Inflammation is a complex process mainly comprises of three phases namely acute, sub-acute and chronic. In acute inflammatory conditions fluid and granulocytic cells accumulate at the site of injury because of the changes in small blood vessels. This response often activates systemic response such as leucocytosis, protein catabolism, fever and synthesis of C-reactive protein, an acute-phase protein In Ayurvedic texts, several herbo-mineral preparations to fight against inflammation have been found; among them, Vatavidhvamsana Rasa (VVR) is one, which is said to be remarkable in inflammation condition. Aim and Objectives: To assess the anti-inflammatory and analgesic effects of VVR in pharmacologically validated models. Materials and methods: Wistar strain albino rats weighing 200 ± 20 of either sex were used in the study. VVR was administered at a dose of 22.5 mg/kg for the rat. Results: Vatavidhvamsana Rasa (VVR) showed a significant decrease in the carrageenan-induced paw oedema after 1-hour interval in comparison to the control group (P<0.05) and at 3 hours and 5 hours intervals it showed a non-significant decrease in carrageenan-induced paw oedema in albino rats.  In the analgesic activity, VVR treated group showed a significant increase in radiant heat response at 30 min. interval (P<0.05) and non-significant increase at 60 mins in comparison to initial and control group. Conclusion: The results concluded that Vatavidhvamsana Rasa has anti-inflammatory and analgesic activity. Accordingly, it can be used in the management of pain and inflammatory conditions. 


2021 ◽  
Vol 21 (No 1) ◽  
Author(s):  
Anjoo Kamboj ◽  
Sanjana Piplani

Synthetic analgesic drugs have prominent side effects like gastritis, gastric ulcer, kidney disorder and cardiac arrhythmias. The genus Solanum has been primarily used for various therapeutic effects, mainly analgesics, in the indigenous system of medicine. The current research aimed to investigate and compare the analgesic activities of methanolic extracts of leaves of Solanum indicum, Solanum surattense and Solanum torvum. Using acetic acid induced writhing method and hot plate method, the analgesic activity was evaluated. Significant anti-nociceptive effects were observed on both animal models after the application of different doses of the extracts of Solanum species. The results exhibited that MESI, MESS and MEST at a dose of 200 and 400 mg/kg produced analgesic effects equivalent to diclofenac (10 mg/kg). However the extracts at 400 mg/ kg exhibited more pronounced analgesic activity. The results of this study demonstrated that the analgesic effects of all the three species were significant to each other and validate the traditional use of the plants of this Genus for the treatment of pain.


2002 ◽  
Vol 80 (3) ◽  
pp. 297-304 ◽  
Author(s):  
Mohammed Bajji ◽  
Jean-Marie Kinet ◽  
Stanley Lutts

The effects of salt and osmotic stresses on the germination processes in seeds of the perennial halophyte species Atriplex halimus L. were compared using iso-osmotic concentrations of NaCl and mannitol. The lowest stress intensity delayed germination, while higher doses of NaCl and mannitol reduced final germination percentages. No significant difference occurred between the effects of these solutes on germination percentages or seedling dry weights. At an external osmotic potential of –0.7 MPa, however, the water content of mannitol-treated seedlings was reduced compared to that of seedlings that developed from NaCl-exposed seeds. The K, Mg, and Pi content decreased in seedlings that developed from mannitol-treated seeds while calcium concentration was strongly reduced in those arising from NaCl-treated seeds. Inhibited seeds were able to germinate at levels similar to those of the control after rinsing in deionized water and imbibition in control conditions. Seedlings produced from NaCl pre-treated seeds had a lower Ca and a higher Na content than control seedlings. The effect of salinity on the germination phase of development is mainly due to its osmotic component, and inhibition of germination is reversible. Both salt and osmotic stresses may have an impact on the mobilization of minerals from the seeds to the young seedling, but this effect does not have any consequence on growth processes analysed on a short-term basis.Key words: Atriplex halimus, halophyte, osmotic stress, recovery of seed germination, salinity.


1997 ◽  
Vol 87 (6) ◽  
pp. 1348-1358 ◽  
Author(s):  
Jorn Lotsch ◽  
Gerd Kobal ◽  
Anne Stockmann ◽  
Kay Brune ◽  
Gerd Geisslinger ◽  
...  

Background The analgesic activity of morphine-6-glucuronide (M-6-G) is well recognized for its contribution to the effects of morphine and its possible use as an opioid analgesic with a wider therapeutic range than morphine. The present study attempted to quantify the relative contribution of M-6-G to analgesia observed after systemic administration of morphine. Methods In a placebo-controlled, sixfold crossover study in 20 healthy men, the effects of M-6-G were assessed at steady-state plasma concentrations of M-6-G identical to and two and three times higher than those measured after administration of morphine. Morphine and M-6-G were administered as an intravenous bolus followed by infusion over 4 h. Dosage A was M-6-G-bolus of 0.015 mg/kg plus infusion of 0.0072 mg x kg(-1) x h(-1). Dosage B was M-6-G-bolus of 0.029 mg/kg plus infusion of 0.014 mg x kg(-1) x h(-1). Dosage C was M-6-G-bolus of 0.044 mg/kg plus infusion of 0.022 mg x kg(-1) x h(-1). Dosage D was a morphine bolus of 0.14 mg/kg plus infusion of 0.05 mg x kg(-1) x h(-1) for 4 h. Dosage E was M-6-G combined with morphine (doses A + D). Dosage F was a placebo. The analgesic effects of M-6-G and morphine were measured before administration of the bolus and after 3.5 h using an experimental pain model based on pain-related cortical potentials and pain ratings after specific stimulation of the nasal nociceptor with short pulses of gaseous carbon dioxide. Results Morphine significantly reduced subjective and objective pain correlates compared with placebo. In contrast, M-6-G produced no statistically significant effects. The addition of M-6-G to morphine did not increase the effects of morphine. Morphine produced significantly more side effects than M-6-G. Conclusion After short-term intravenous administration at doses that produce plasma concentrations of M-6-G similar to those seen after administration of morphine, M-6-G had no analgesic effects in the present placebo-controlled study in healthy volunteers.


2017 ◽  
Vol 2 (2) ◽  
pp. 147
Author(s):  
Triswanto Sentat ◽  
Susiyanto Pangestu

Kersen leaf (Muntingia calabura L.) contains tannins, flavonoids and polyphenol compounds allegedly have analgesic effect. The objective was to determine the analgesic effect of ethanol extract of kersen leaves and to determine the most effective analgesic dose. This study was an experimental research. Leaves were extracted with ethanol 70% and the analgesic effect test was divided into 5 groups: negative control treatment (distilled water), positive control (mefenamic acid 2.6mg/kg), kersen leaf ethanol extract first dose (100mg/kg), second dose (200mg/kg) and tthird dose (400mg/kg). Giving treatments by oral, after 30 minutes, the mices were given a pain inductor with 0.5% acetic acid by intra peritonial administration. Analgesic power was calculated by counting the number of writhing in mice for 1 hour. The results showed that the ethanol extract of cherry leaf has analgesic effect. From the calculation of the first dose analgesic power (42.9%), second dose (59.4%) and the third dose 69.9%. Statistical test results kruskal wallis value of p=0.011 (p<0.05) showed a significant difference between all analgesic treatment groups. The conclusion of this study is all of the ethanol extract had analgesic effects on male white mice, whereas a dose of 400mg/kg is the most effective analgesic dose.


1995 ◽  
Vol 83 (4) ◽  
pp. 844-849. ◽  
Author(s):  
Stephen E. Abram ◽  
Therese C. O'Connor

Background Intrathecal carbachol produces consistent analgesia in animals without appreciable adverse effects. Little is known about the ability of this drug to provide analgesia as stimulus intensity is increased. Likewise, there are few data regarding interactions between carbachol and other intrathecal analgesics. Methods Using two different noxious radiant heat intensities, one applied to each hind limb, analgesic effects of 1, 3, 10, and 30 micrograms intrathecal carbachol on paw withdrawal latencies were measured. Similar testing was done for intrathecal morphine and clonidine. ED50 fractions (1/2, 1/4, 1/8, 1/16) of drug combinations of carbachol-morphine and carbachol-clonidine were administered, responses to the low intensity stimulus were recorded, and the ED50 of each combination was established and isobolographic analysis of the drug interactions was carried out. Results The 30-micrograms dose of carbachol was associated with transient agitation, salivation, and hind limb weakness. No other adverse effects were noted. The ED50 (95% confidence interval) of intrathecal carbachol was 2.34 micrograms (1.34-4.04) for low intensity stimulation and 12.64 micrograms (4.18-38.25) for high intensity. There was no significant difference between high- and low-intensity ED50 values for intrathecal morphine and clonidine. The analgesic effect of the carbachol-morphine and carbachol-clonidine combinations were significantly greater than the calculated additive effects. The ED50 for the carbachol-morphine combination was 12% of the expected additive value and the ED50 for the carbachol-clonidine combination was 30% of the expected additive value. Conclusions Intrathecal carbachol provides analgesia to noxious thermal stimulation of the hind paw in rats. It is relatively less effective at providing analgesia than intrathecal morphine or clonidine when stimulus intensity is raised. Intrathecal carbachol is synergistic when combined with intrathecal morphine or clonidine.


2007 ◽  
Vol 64 (8) ◽  
pp. 538-542
Author(s):  
Svetlana Pavlovic ◽  
Sladjana Zivkovic ◽  
Goran Koracevic

Background/Aim. The inhibition of factor Xa (FX) by the use of low-molecular heparin (LMH) is important clinical procedure in patients with moderate and high risk for the developament of venous thromboembolism (VTE) and pulmonary embolism (PE). The aim of this study was to determine the level of inhibition of FXa by the use of prophylactic doses of LMH nadroparin-calcium and reviparine-sodium which were applied in urological patients with moderate risk for VTE and PE. Methods. The examination included 80 urological patients divided into 4 groups after urological, uroradiological and anesthesiological preoperative preparation and categorization of anesthesiological risk according to the ASA III classification. The first two groups, of 20 patients each, received the recommended doses of LMH in accordance with the preoperative risk, and an inhibition of FXa 48 hours after the surgical operation and four hours after the administration of LMH was determined. Heptest and homogenous anti-Xa test were used for monitoring of FXa inhibition. Since the obtained anti-Xa values were not satisfactory, two more groups were formed and given double the recommended doses. In these new groups, inhibition of FXa was in recommended range. Standard descriptive statistical parameters were used for describing the charateristics of the people from the formed groups. Results. All the patients examined were clinically estimated as patients of moderate risk, for VTE and PE. There were no statistically singificant difference in body weight of the patients who received nadroparin-calcium 0.3 ml and reviparine-sodium 0.25 ml and those who received their double doses, respectively. The level of FXa inhibition in the group in which the dose of nadroparin-calcium of 0.6 ml was applied was statistically significantly higher than in the group which received the dose of 0.3 ml (Mann-Whitney U test: Z = 5.416; p < 0.0001). The level of FXa in the group given reviparine-sodium 0.5 ml was significantly higher than in the group which received the half of this dose (Mann-Whitney U test: Z = 5.416; p < 0.0001). This research did not confirm a statistically significant difference in the levels of FXa inhibition in patients who received nadroparincalcium as VTE and PE prophilaxis in the dose of 0.6 ml and those who received reviparin-sodium 0.5 ml (in two doses of 0.25 ml) (Mann-Whitney U test: Z = 0.163; p > 0.05). Conclusion. According to biochemical monitoring, the recommended doses of LMH are insufficient for the prophylactic inhibition of FXa in urological pateints with moderate risk for VTE and PE, so the higher doses which inhibit FXa are recommended. .


2020 ◽  
pp. 43-45
Author(s):  
Nadia Akram ◽  
Seeba Hussain ◽  
Debarshi Jana

Background : Vitiligo is the most prevalent pigmentary disorder which occurs worldwide, with an incidence rate between 0.1-4 percent. It is anticipated that the discovery of biological pathways of vitiligo pathogenesis with provide novel therapeutic and prophylactic targets for future approaches to the treatment and prevention of vitiligo. The purposes of this study were evaluating the efficacy of supplemental zinc on the treatment of vitiligo. Methods : This randomized clinical trial was conducted for a period of one year. Thiry five patients among 86 participatnts were eligible to entrance to the study. The patients in two equal randomized groups took topical corticosteroid and comination of oral zinc sulfate-topical corticosteroid. Results : The of responses in the corticosteroid group and the zinc sulfat-corticosteroid combination group were 21.43% and 24.7% respectively. Conclusion : Although, the response to corticosteroid plus zinc sulfate was more than corticosteroid, there was no statistically significant difference between them. It appeared that more robust long-term randomized controlled trials on more patients, may be with higher doses of zinc sulfate, are needed to fully establish the efficacy of oral zinc in management of vitiligo.


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