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1.
| Hit, Lead & Candidate Discovery | Inflammation is a complex biological process that is generally occurs in response to pathological triggers. Both neurodegenerative diseases and cancer have been linked to inflammation. The analgesic and anti‐inflammatory effects of cupressuflavone (CUF) isolated from Cupressus macrocarpa were examined. The analgesic effects of CUF (40, 80 and 160 mg/kg po) were assessed in the acetic acid‐induced writhing and hot plate models in mice with diclofenac sodium as the reference standard (100 mg/kg). CUF dose‐dependently inhibited the writhing response in mice by 25, 48, and 62%, at the three CUF doses with 160 mg/kg being equivalent to the diclofenac control. CUF dose‐dependently increased the hot plate model reaction time with a maximal effect after 120 min. In the carrageenan‐induced paw edema model of inflammation, CUF demonstrated anti‐inflammatory activity by inhibiting paw edema by 55, 60, and 64% at doses of 40, 80, and 160 mg/kg po, respectively. CUF also reduced the plasma pro‐inflammatory mediators PGE 2 (44, 54, and 58%), TNF‐α (26, 37, and 53%), IL‐1β (19, 33, and 41%), and IL‐6 (32, 44, and 55%) at the three doses tested with the highest dose having similar effects to diclofenac sodium (100 mg/kg). This finding from this study indicates that CUF has both analgesic and anti‐inflammatory effects. 相似文献
2.
Metformin‐dependent mechanisms have been implicated in the antinociceptive effect of some non‐steroidal anti‐inflammatory drugs (NSAIDs). In this study, the effect of local peripheral or systemic administration of metformin on the local peripheral or systemic antinociception induced by indomethacin, ketorolac and metamizole was assessed in the rat carrageenan‐induced thermal hyperalgesia model. Rats were injected with carrageenan (1%, 50 µl) into the right hindpaw which reduced paw withdrawal latency, a measure of thermal hyperalgesia. Local peripheral or systemic administration of indomethacin, ketorolac or metamizole dose‐dependently reduced carrageenan‐induced thermal hyperalgesia. Local peripheral pre‐treatment with metformin (800 µg/paw) partially inhibited the anti‐hyperalgesic effect of indomethacin (200 µg/paw) and metamizole (200 µg/paw), but not that of ketorolac (200 µg/paw). In contrast, systemic pre‐treatment with metformin (200 mg/kg) attenuated the antihyperalgesic effect of metamizole (10 mg/kg), but not that observed with either indomethacin (10 mg/kg) or ketorolac (10 mg/kg). These findings suggest that some but not all NSAIDs have effects mediated by metformin‐dependent mechanisms. Drug Dev Res 78 : 98–104, 2017. ©2017 Wiley Periodicals, Inc. 相似文献
3.
The anti‐inflammatory and analgesic activities of a polyphenol‐rich fraction (TMEF) obtained from Terminalia muelleri Benth. were measured. The analgesic activity of TMEF was tested using acetic acid‐induced writhing and hot plate models in mice. The anti‐inflammatory activity was assessed using carrageenan‐induced paw edema model by measuring PGE 2, TNF‐α, IL‐1β, and IL‐6 plasma levels as well as the paw thickness. TMEF was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard (100 mg/kg) in all experiments. The group treated with 400 mg/kg of TMEF showed a greater inhibition in the number of writhes (by 63%) than the standard‐treated group (61%). Pretreatment with TMEF increased the analgesic effect in hot plate test in a dose‐dependent manner with a maximum effect after 120 min. TMEF pretreatment alos reduced the edema thickness by 48, 53, and 62% at the tested doses, respectively. TMEF administration inhibited the carrageenan‐induced elevations in PGE 2 (by 34, 43, and 47%), TNF‐α (18, 28, and 41%), IL‐1β (14, 22, and 29%), and IL‐6 (26, 31, and 46%). Four phenolic compounds were isolated from Terminalia muelleri for the first time. Drug Dev Res 78 : 146‐154, 2017. © 2017 Wiley Periodicals, Inc. 相似文献
4.
The present study was designed to evaluate the possible antinociceptive interaction between diacerhein and some antiepileptic drugs (carbamazepine, topiramate and gabapentin) on formalin‐induced nociception. Diacerhein, each of the antiepileptics or a fixed dose‐ratio combination of these drugs was assessed after local peripheral and oral administration in rats. lsobolographic analyses were used to define the interaction between drugs. Diacerhein, antiepileptic drugs (carbamazepine, topiramate and gabapentin) or their combinations yielded a dose‐dependent antinociceptive effect when administered by both routes. Theoretical ED 30 values for the combination estimated from the isobolograms were obtained as follows: diacerhein‐carbamazepine (85.99 ± 7.07 μg/paw; 56.53 ± 4.56 mg/kg po), diacerhein‐topiramate (197.97 ± 22.90 μg/paw; 13.06 ± 2.44 mg/kg po) and diacerhein‐gabapentin (96.87 ± 17.73 μg/paw; 17.90 ± 4.70 mg/kg p.o.) for the local peripheral and oral administration routes, respectively. These values were significantly higher than the experimentally obtained ED 30 values: diacerhein‐carbamazepine (49.33 ± 3.37 μg/paw; 35.49 ± 7.91 mg/kg po), diacerhein‐topiramate (133.00 ± 39.10 μg/paw; 8.87 ± 1.46 mg/kg po) and diacerhein‐gabapentin (70.98 ± 14.73 μg/paw; 10.95 ± 3.23 mg/kg po). The combinations produced their antinociceptive effects without motor impairment in the rotarod test indicating synergistic interactions with a good side effect profile. 相似文献
5.
| Hit, Lead & Candidate Discovery | The acetic acid‐induced writhing and hot plate models in mice were utilized to determine the analgesic effect of epicatechin gallate (ECG) isolated from Bauhinia hookeri. The anti‐inflammatory activity of ECG was determined using carrageenan‐induced paw edema model. The pro‐inflammatory mediators (PGE 2, TNF‐α, IL‐1β, and IL‐6) were estimated in the plasma of different treatment groups. ECG was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard drug (100 mg/kg) in all experiments. ECG significantly ( p < .001) suppressed the writhing response in mice. The inhibition percentages were 32, 52, and 62%, at the tested doses of ECG, respectively as compared to the positive control group receiving acetic acid only. Furthermore, ECG significantly ( p < .001) increased the reaction time in hot plate model. The maximum analgesic effect was evident after 120 min. ECG demonstrated a significant anti‐inflammatory activity as evidenced by the inhibition of carrageenan‐induced paw edema (46, 50, and 58%, at the tested doses, respectively). This effect was persistent all over the experimental period. ECG produced a significant ( p < .001) reduction in plasma PGE 2 (by 27, 38, and 50%), TNF‐α (15, 33, and 41%), IL‐1β (17, 25, and 33%), and IL‐6 (22, 32, and 43%), at the tested doses, respectively. This study supports the use of ECG as both analgesic and anti‐inflammatory agent. 相似文献
6.
Objectives Friedelin was isolated from Azima tetracantha Lam. leaves collected from Kallakurichi, Villuppuram district, Tamil Nadu, India. The anti‐inflammatory, analgesic and antipyretic activities of friedelin have been investigated in Wistar rats and mice. Methods Friedelin was isolated from the hexane extract of leaves of A. tetracantha using column chromatography. The effects of friedelin on inflammation were studied by using carrageenan‐induced hind paw oedema, croton oil‐induced ear oedema, acetic acid‐induced vascular permeability, cotton pellet‐induced granuloma and adjuvant‐induced arthritis. The analgesic effect of friedelin was evaluated using the acetic acid‐induced abdominal constriction response, formalin‐induced paw licking response and the hot‐plate test. The antipyretic effect of friedelin was evaluated using the yeast‐induced hyperthermia test in rats. Key findings In the acute phase of inflammation, maximum inhibitions of 52.5 and 68.7% ( P < 0.05) were noted with 40 mg/kg friedelin in carrageenan‐induced paw oedema and croton oil‐induced ear oedema, respectively. Administration of friedelin (40 mg/kg) significantly ( P < 0.05) decreased the formation of granuloma tissue induced by cotton pellet at a rate of 36.3%. In the adjuvant‐induced arthritis test friedelin inhibited 54.5% of paw thickness. Friedelin inhibited acetic acid‐induced vascular permeability in mice. Friedelin also produced significant ( P < 0.05) analgesic activity in the acetic acid‐induced abdominal constriction response and formalin‐induced paw licking response. In the hot‐plate test, friedelin did not show any significant results when compared with control. Treatment with friedelin showed a significant ( P < 0.05) dose‐dependent reduction in pyrexia in rats. Conclusions The results suggested that friedelin possessed potent anti‐inflammatory, analgesic and antipyretic activities. 相似文献
7.
目的：研究中华眼镜蛇毒灌服给药对小鼠的镇痛作用。方法：将ICR和昆明种小鼠,采用3种致疼痛模型,即冰醋酸所致扭体反应、小鼠热板法致痛实验和甲醛致炎性疼痛反应;中华眼镜蛇毒经热变性复性处理,将其灌胃给药30-270μg／kg。结果：中华眼镜蛇毒粗毒灌服给药能减少腹腔注射醋酸引起的扭体次数,延长热引起的疼痛反应潜伏期和减少甲醛引起的舔足反应。结论：中华眼镜蛇毒灌服给药具有良好的镇痛作用,且给药途径方便、安全范围大,具有进一步开发成新型镇痛药的潜力。 相似文献
8.
| Preclinical Research & Development | The combination of nonsteroidal anti‐inflammatory drugs (NSAIDs) with herbal products having analgesic and anti‐inflammatory effects may increase their beneficial effects and limit their side effects. In this study, the effects of an interaction between α‐bisabolol and the NSAID, diclofenac on nociception (formalin test), inflammation (paw inflammation produced by carrageenan) and gastric injury in rat was assessed. Diclofenac, α‐bisabolol, or diclofenac–α‐bisabolol combinations produced antinociceptive and anti‐inflammatory effects in rat ( p < .05). The systemic administration of diclofenac, but not α‐bisabolol, produced gastric damage while the diclofenac–α‐bisabolol combinations produced limited gastric damage. Effective dose (ED 40) values were determined for each individual drug and analyzed isobolographically. The theoretical ED 40 values for the antinociceptive (98.89 mg/kg) and the anti‐inflammatory (41.2 mg/kg) effects differed from the experimental ED 40 values (antinociception: 38.7 mg/kg and anti‐inflammation: 13.4 mg/kg). We concluded that the interactions between diclofenac and α‐bisabolol are synergistic. These data suggest that the diclofenac–α‐bisabolol combinations can interact to produce minor gastric damage, thereby offering a safer therapeutic alternative for the clinical management of inflammation and/or inflammatory pain. 相似文献
9.
The coadministration of non‐steroidal anti‐inflammatory drugs (NSAIDs) with medicinal plant extracts may increase anti‐inflammatory activity, thus permitting the use of lower NSAID doses and limiting the side effects. The aim of this study was to explore the interactions between an ethanolic extract of M. chamomilla extract (MCE) with two NSAIDs, diclofenac and indomethacin on carrageenan‐induced paw inflammation and gastric injury in rats. Diclofenac, indomethacin and MCE, or combinations with MCE produced an anti‐inflammatory effect. Effective dose (ED) values were estimated for the individual drugs, and isobolograms were constructed. The final experimental ED values were 483.7 mg/kg for diclofenac + MCE combination, and 212.6 mg/kg for indomethacin + MCE. These values were lower (p < 0.05) than the theoretical ED values (1186.9 mg/kg for diclofenac + MCE combination, and 1183.8 mg/kg for indomethacin + MCE). These data suggest that the interactions between NSAIDs and MCE that mediate the anti‐inflammatory effects at the systemic level are synergistic and may have therapeutic advantages for the clinical treatment of inflammatory processes. Drug Dev Res 78 : 360‐367, 2017. © 2017 Wiley Periodicals, Inc. 相似文献
10.
Salvia tiliifolia Vahl (Lamiaceae) is used for the empirical treatment of pain and inflammation. The diterpenoid tilifodiolide (TFD) was isolated from Salvia tiliifolia. The in vitro anti‐inflammatory effects of TFD (0.1–200 µM) were assessed using murine macrophages stimulated with LPS and estimating the levels of pro‐inflammatory mediators for 48 h. The in vivo anti‐inflammatory activity of TFD was assessed using the carrageenan‐induced paw edema test for 6 h. The antinociceptive effects of TFD were evaluated using the formalin test and the acetic acid induced‐writhing test. The effects of TFD on locomotor activity were assessed using the open field test and the rotarod test. TFD inhibited the production of TNF‐α (IC 50 = 5.66 µM) and IL‐6 (IC 50 = 1.21 µM) in macrophages. TFD (200 mg/kg) showed anti‐inflammatory effects with similar activity compared to 10 mg/kg indomethacin. The administration of TFD induced antinociception in the phase 1 (ED 50 = 48.2 mg/kg) and the phase 2 (ED 50 = 28.9 mg/kg) of the formalin test. In the acetic acid assay, TFD showed antinociceptive effects (ED 50 = 32.3 mg/kg) with similar potency compared to naproxen (ED 50 = 36.2 mg/kg). In the presence of different inhibitors in the acetic acid assay, only the co‐administration of TFD and naloxone reverted the antinociceptive activity shown by TFD alone. TFD did not affect locomotor activity in mice. TFD exerts in vitro and in vivo anti‐inflammatory activity and in vivo antinociceptive effects. 相似文献
11.
Objectives In the present study we investigated the antinociceptive, anti‐inflammatory and antipyretic effects of 7‐hydroxycoumarin (7‐HC) in animal models. Methods The effects of oral 7‐HC were tested against acetic acid‐induced writhing, formalin test, tail flick test, complete Freund's adjuvant (CFA)‐induced hypernociception, carrageenan‐induced paw oedema, lipopolysaccharide‐induced fever and the rota rod test. Key findings 7‐HC (3–60 mg/kg) produced a dose‐related antinociception against acetic acid‐induced writhing in mice and in the formalin test. In contrast, treatment with 7‐HC did not prevent thermal nociception in the tail flick test. A single treatment with 7‐HC, 60 mg/kg, produced a long‐lasting antinociceptive effect against CFA‐induced hypernociception, a chronic inflammatory pain stimulus. Notably, at 60 mg/kg per day over 4 days the administration of 7‐HC produced a continuous antinociceptive effect against CFA‐induced hypernociception. 7‐HC (30–120 mg/kg) produced anti‐inflammatory and antipyretic effects against carrageenan‐induced inflammation and lipopolysaccharide‐induced fever, respectively. Moreover, 7‐HC was found to be safe with respect to ulcer induction. In the rota rod test, 7‐HC‐treated mice did not show any motor performance alterations. Conclusions The prolonged antinociceptive and anti‐inflammatory effects of 7‐HC, in association with its low ulcerogenic activity, indicate that this molecule might be a good candidate for development of new drugs for the control of chronic inflammatory pain and fever. 相似文献
12.
The aim of this study was to evaluate the efficacy of multiple applications of S(+)‐flurbiprofen plaster (SFPP), a novel Nonsteroidal anti‐inflammatory drug (NSAID) patch, for the alleviation of inflammatory pain and edema in rat adjuvant‐induced arthritis (AIA) model as compared to other NSAID patches. The AIA model was induced by the injection of Mycobacterium butyricum and rats were treated with a patch (1.0 cm × 0.88 cm) containing each NSAID (SFP, ketoprofen, loxoprofen, diclofenac, felbinac, flurbiprofen, or indomethacin) applied to the paw for 6 h per day for 5 days. The pain threshold was evaluated using a flexion test of the ankle joint, and the inflamed paw edema was evaluated using a plethysmometer. cyclooxygenase (COX)?1 and COX‐2 inhibition was evaluated using human recombinant proteins. Multiple applications of SFPP exerted a significant analgesic effect from the first day of application as compared to the other NSAID patches. In terms of paw edema, SFPP decreased edema from the second day after application, Multiple applications of SFPP were superior to those of other NSAID patches, in terms of the analgesic effect with multiple applications. These results suggest that SFPP may be a beneficial patch for providing analgesic and anti‐inflammatory effects clinically. Drug Dev Res 77 : 206–211, 2016. © 2016 The Authors Drug Development Research Published by Wiley Periodicals, Inc. 相似文献
13.
Gabapentin is an anticonvulsant used to treat neuropathic pain. Mangiferin is an antioxidant that has antinociceptive and antiallodynic effects in inflammatory and neuropathic pain models. The purpose of this study was to determine the interaction between mangiferin and gabapentin in the development and maintenance of formalin‐induced secondary allodynia and hyperalgesia in rats. Gabapentin, mangiferin, or their fixed‐dose ratio combination were administrated peripherally. Isobolographic analyses was used to define the nature of the interaction of antiallodynic and/or antihyperalgesic effects of the two compounds. Theoretical ED 50 values for the combination were 74.31 µg/paw and 95.20 µg/paw for pre‐ and post‐treatment, respectively. These values were higher than the experimental ED 50 values, 29.45 µg/paw and 37.73 µg/paw respectively, indicating a synergistic interaction in formalin‐induced secondary allodynia and hyperalgesia. The antiallodynic and antihyperalgesic effect induced by the gabapentin/mangiferin combination was blocked by administration of L‐NAME, the soluble guanylyl cyclase inhibitor, ODQ and glibenclamide. These data suggest that the gabapentin‐ mangiferin combination produces a synergistic interaction at the peripheral level. Moreover, the antiallodynic and hyperalgesic effect induced by the combination is mediated via the activation of an NO‐cyclic GMP‐ATP‐sensitive K + channel pathway. Drug Dev Res 78 : 390‐402, 2017. © 2017 Wiley Periodicals, Inc. 相似文献
14.
The present study aimed to investigate the antinociceptive and anti‐inflammatory effects of the cyclic dipeptide cyclo‐Gly‐Pro (CGP) in mice. Antinociceptive activity was assessed by employing different pain models, such as formalin test, acetic acid‐induced writhing, hot plate test, and carrageenan‐induced hyperalgesia, in mice. The number of c‐Fos‐immunoreactive cells in the periaqueductal gray (PAG) was evaluated in CGP‐treated mice. Anti‐inflammatory activity was evaluated using paw oedema induced by carrageenan, compound 48/80, serotonin, and prostaglandin E 2 (PGE 2) and analyzed by plethysmometry. Quantitation of myeloperoxidase (MPO) in the paw was carried out to analyze the presence of neutrophils in the tissue. Intraperitoneal injection of CGP produced a significant inhibition in both neurogenic and inflammatory phases of formalin‐induced pain. The antinociceptive effect of CGP, evaluated in the acetic acid‐induced writhing test, was detected for up to 6 h after treatment. Further, in the hot plate test, antinociceptive behaviour was evoked by CGP, and this response was inhibited by naloxone. Animals treated with CGP did not present changes in motor performance. In CGP‐treated mice there was an increase in the number of c‐Fos‐positive neurons in the periaqueductal gray. In another set of experiments, CGP attenuated the hyperalgesic response induced by carrageenan. Furthermore, CGP also reduced the carrageenan‐increased MPO activity in paws. In addition, CGP also reduced the paw oedema evoked by compound 48/80, serotonin, and PGE 2. Taken together, these results may support a possible therapeutic application of the cyclic dipeptide cyclo‐Gly‐Pro toward alleviating nociception and damage caused by inflammation conditions. 相似文献
15.
| Strategy, Management and Health Policy | | Preclinical Research | Flufenamic acid (FFA) is a nonsteroidal anti‐inflammatory drug, used in the treatment of rheumatoid arthritis, osteoarthritis, spondylitis, and other disorders. The objective of this study was to enhance the dissolution rate of the drug by the solid dispersion in the matrices of Pluronic F‐127 (PL) and Gelucire 50/13 (GL). Different drug : polymer ratios were selected for the preparation of FFA solid dispersions using solvent evaporation technique. The prepared FFA solid dispersions were characterized by differential scanning calorimetry and Fourier transform infrared spectroscopy. The dissolution study depicted that the presence of drug in solid dispersion enhances its dissolution as compared with the drug itself and the drug : polymer ratio 1:1 was superior in enhancing FFA dissolution rate from solid dispersions. The in vitro skin permeation from Carbopol 940 gel base through abdominal rat skin membranes was investigated. The data showed that FFA‐PL followed by FFA‐GL solid dispersion enhanced drug permeation through rat skin, while untreated drug showed slower permeation. Furthermore, FFA in its PL and GL solid dispersions exhibited a potent local anti‐inflammatory activity against formalin‐induced paw edema from Carbopol gel base compared with the untreated drug, and this activity reached its peak (96% and 84%, respectively) after 4 h. 相似文献
16.
The objective of this study was to evaluate the pharmacological antihyperalgesic interaction between N‐palmitoylethanolamide (PEA) and acetaminophen in diabetic rats using the formalin paw test. Streptozotocin (STZ)‐induced diabetic rats received subcutaneous injections in the paw of PEA alone (1–100 μg/paw) or acetaminophen alone (3–300 μg/paw) 15 min before formalin (0.5%) injection. The results revealed concentration‐dependent responses produced by PEA (EC 50 = 7.19 ± 0.7 μg/paw) and acetaminophen (EC 50 = 57.9 ± 1.9 μg/paw). Isobolographic analysis was used to evaluate the pharmacological interaction between the PEA + acetaminophen using the EC 50 value and a fixed 1:1 ratio combination. The isobologram demonstrated that the combination investigated in this study produced a synergistic interaction; the experimental value (EC 50= 23.64 ± 1.9 μg/paw) was significantly smaller than those that resulted from theoretical calculations (EC 50 = 32.56 μg/paw). These results provide evidence that PEA in combination with acetaminophen could be useful for pain therapy in neuropathic diabetic patients. Drug Dev Res 76 : 228–234, 2015. © 2015 Wiley Periodicals, Inc. 相似文献
17.
Morin, a flavonoid isolated from Morus alba L. (Moraceae), possesses anti‐inflammatory, antiangiogenic among other biological activities. This study investigated its effect on type II collagen‐induced arthritis (CIA) in rats and explored the underlying mechanisms in view of synovial angiogenesis. Morin administered po attenuated arthritic progression as indicated by reduction of arthritis scores and paw swelling. It also markedly reduced serum levels of the proinflammatory cytokines, tumor necrosis factor alpha (TNF‐α) and interleukin‐6 (IL‐6), but increased the level of anti‐inflammatory cytokine interleukin‐10, and ameliorated histopathological changes of joints. Morin markedly inhibited expression of CD31, vascular endothelial growth factor (VEGF), and basic fibroblast growth factor in synovial membrane tissues, and decreased serum levels of VEGF in CIA rats. In vitro, morin markedly inhibited VEGF‐induced migration and tube formation in human umbilical vein endothelial cells. These results indicate that morin had antirheumatoid potential, and its mechanism might be associated with inhibition of synovial angiogenesis. Drug Dev Res 76 : 463–473, 2015. © 2015 Wiley Periodicals, Inc. 相似文献
18.
Naproxen is an anti‐inflammatory drug used in a variety of anti‐inflammatory syndromes. There is evidence showing that tizanidine enhances the anti‐inflammatory effect in rats. This study examines the pharmacokinetics of naproxen when it is combined with tizanidine. Combining these two drugs is an attractive modality for inflammation complaints. Oral coadministration of naproxen/tizanidine produced a synergistic anti‐inflammatory effect in rats. The swelling of the rat paw was measured by a plethysmometer using carrageenan as an inflammatory agent. In this study, rats received oral doses of naproxen (1, 3, and 4.2 mg/kg), and these doses were combined with a fixed dose of tizanidine (0.01 mg/kg). To evaluate the pharmacokinetic interaction between naproxen/tizanidine, blood samples were obtained at selected times in the 24 h after oral administration and were analyzed using a validated high‐performance liquid chromatography method. Systemic administration of naproxen alone or in combination with tizanidine produced a dose‐dependent anti‐inflammatory effect. In the pharmacokinetic interaction study, no statistically significant difference was observed for the naproxen concentration‐time profiles in the presence of tizanidine. The experimental findings suggest that systemic tizanidine is able to increase the naproxen‐induced anti‐inflammatory effect in rats. This effect was not due to a modification of the bioavailability of naproxen. 相似文献
19.
Ocimum gratissimum L. leaves have attracted considerable attention from researchers because of their medicinal value that include anti‐inflammatory, analgesic, antimicrobial, and antioxidant activities. In the present study, the toxicity and the protective effect of phenolic extract of O. gratissimum leaf (EAFO g ) against acute inflammation and oxidative stress in rats was assessed. EAFOg, enriched in phenols had no cytotoxic effect against CHO‐k1 cells, and no lethality against brine shrimp eggs or mice at a dose of 2000 mg/kg. EAFOg (50 and 100 mg/kg) reduced paw edema by 47% and 61%, compared to 29% with the COX‐2 inhibitor, SC58125 (1 mg/kg) and 81% with indomethacin (5 mg/kg), respectively. In the rat carrageenan‐induced air pouch model, EAFO g reduced exudate volume, leucocyte count, nitrite, TNF‐α, and myeloperoxidase activity. EAFO g also protected against carrageenan‐induced lipid peroxidation and glutathione depletion. These results provide evidence of the protective effects of EAFO g against acute inflammation and oxidative stress in rats. Drug Dev Res 78 : 135‐145, 2017. © 2017 Wiley Periodicals, Inc. 相似文献
20.
Rhodiola rosea L. (Crassulaceae) is used for enhancing physical and mental performance. Recent studies demonstrated that R. rosea had anti‐inflammatory activity in animal models, for example, carrageenan‐ and nystatin‐induced edema in rats, possibly by inhibiting phospholipase A 2 and cyclooxygenases‐1 and ‐2. In addition, R. rosea had antinociceptive activity in thermal and chemical pain tests as well as mechanical hyperalgesia. The purpose of the present study was to assess the antihyperalgesic effect of an ethanol extract of Rhodiola rosea ( R. rosea) in a diabetic rat model. Rats were administered a single dose of s treptozotocin (STZ; 50 mg/kg, i.p.) and hyperalgesia was evaluated four weeks later. Formalin‐evoked (0.5%) flinching was increased in diabetic rats compared with nondiabetic controls Systemic (1–100 mg/kg, i.p.) and local (0.1–10 mg/paw into the dorsal surface of the right hind paw) administration of R. rosea ethanol extract dose‐dependently reduced formalin‐induced hyperalgesia in diabetic rats. The antihyperalgesic effect of R. rosea was compared with gabapentin. These results suggest that R. rosea ethanol extract may have potential as a treatment for diabetic hyperalgesia. Drug Dev Res 77 : 29–36, 2016. © 2016 Wiley Periodicals, Inc. 相似文献
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