In the present study, the chemical composition, antinociceptive effect and acute toxicity of essential oils（EOs） of Asarum heterotropoides Fr. Schmidt var. mandshuricum（Maxim.） Kitag.（AHM）, A. sieboldii Miq. var...In the present study, the chemical composition, antinociceptive effect and acute toxicity of essential oils（EOs） of Asarum heterotropoides Fr. Schmidt var. mandshuricum（Maxim.） Kitag.（AHM）, A. sieboldii Miq. var. seoulense Nakai（ASS） and A. himalaicum Hook. f. et Thoms. ex Klotzsch.（AH） were comparatively evaluated. A total of 55 compounds were identified in EOs of AHM, ASS and AH by GC-MS. Methyleugenol（20.16%–62.89%）, safrole（2.67%–32.42%）, 3,5-dimethoxytoluene（2.00%–18.59%） and eucarvone（1.52%–19.16%） were the major constituents of EO of AHM, and methyleugenol（48.35%–61.06%）, eucarvone（11.13%–13.93%） and elemicin（4.79%–11.14%） were the major constituents of EO of ASS. The EO of AH was different from that of AHM and ASS, in which patchouli alcohol（27.42%–51.95%） and elemicin（13.11%–42.23%） were found in a greater amount. Moreover, the antinociceptive effect of EOs of AHM（5.5, 11.0, 16.5 μL/kg） and AH（2.0, 4.0, 6.0 μL/kg） was comparatively assayed in acetic acid-induced writhing, hot plate and formalin tests. The results indicated a weak central, but potent peripheral antinociceptive effect of EO of AHM, and more potent central and peripheral antinociceptive effect of EO of AH. The LD50 of the EOs of AHM and AH were 1.7 and 7.7 mL/kg, respectively. These findings suggest that EOs of AHM and AH possess evident antinociceptive activity and are probably safe within the range of its clinical doses. However, their chemical compositions are quite different. Therefore, AH can be clinically used as an herbal medicinal product with broad analgesic effects, but should not be confused with AHM and ASS used in traditional Chinese medicine.展开更多
Background: Codiaeum variegatum, sometimes called garden croton, is a tropical plant in the Euphorbiaceae family. Historically used to cure various conditions, including intestinal infections, fever, ulcers, wounds, a...Background: Codiaeum variegatum, sometimes called garden croton, is a tropical plant in the Euphorbiaceae family. Historically used to cure various conditions, including intestinal infections, fever, ulcers, wounds, and gonorrhea. This work aimed to investigate the antinociceptive effects of ethanolic extract of Codiaeum variegatum leaves (EECV) in animal models. Methods: Five different pain models—the hot plate, tail immersion, acetic acid-induced writhing, formalin, and glutamate-induced nociception tests—were utilized to assess the antinociceptive activity in mice. The traditional drugs such as diclofenac sodium (10 mg/kg, i.p.) and morphine sulphate (5 mg/kg). EECV was administered orally at varying doses of 100, 200, and 300 mg/kg (0.1 mL/mouse), while the control group was given deionized water. Results: The current study found that all mouse models of heat- and chemical-induced pain had robust EECV reflections of their antinociceptive properties (*p Conclusions: The current finding offers a fresh perspective on the ethanolic extract of Codiaeum variegatum leaves’ antinociceptive properties in mice. This plant’s phytochemical analysis revealed the presence of triterpenoids, sterols, alkaloids, flavonoids, and general glycosides, all of which may have antinociceptive properties. More research on the mechanism of action and associated pharmacological studies, such as in vivo analysis, medication formulation, and clinical trials, is strongly advised.展开更多
Twelve new grayanoids(1-12)along with five known compounds were isolated from flowers of Rhododendron molle.Their structures were fully characterized using a combination of spectroscopic analyses,computational calcula...Twelve new grayanoids(1-12)along with five known compounds were isolated from flowers of Rhododendron molle.Their structures were fully characterized using a combination of spectroscopic analyses,computational calculations,and single crystal X-ray diffraction.Rhomollone A(1)possesses an unprecedented 5/6/6/5 tetra-cyclic ring system(B-nor grayanane)incorporating a cyclopentene-1,3-dione scaffold.Rhodomollein XLIII(2)is a dimeric grayanoid,containing a novel 14-membered heterocyclic ring with a C2 symmetry axis.The antinociceptive activities of compounds 3,4,6,7,and 12-17 were evaluated by an acetic acid-induced writhing test.Among them,compounds 3,7,12,15 and 16 displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from41.9%to 91.6%.Compounds 6 and 13 inhibited 46.0%and 39.4%of the acetic acid-induced writhes at a dose of 2 mg/kg,while compound 17 inhibited 34.3%of the writhes at a dose of 0.4 mg/kg.展开更多
Background: Diospyros malabarica (Desr.) Kostel, a small to medium-sized tree in the Ebenaceae family, is known as “Deshi Gab” in Bangladesh. Fever, diabetes, snake bite, diarrhea, biliousness, and ulcer ailments ar...Background: Diospyros malabarica (Desr.) Kostel, a small to medium-sized tree in the Ebenaceae family, is known as “Deshi Gab” in Bangladesh. Fever, diabetes, snake bite, diarrhea, biliousness, and ulcer ailments are all treated with the herb. This study’s goal was to examine in mouse models the antinociceptive properties of methanol extract of Diospyros malabarica leaves (MEDM). Methods: For the purpose of determining the antinociceptive activity in mice, five distinct pain models including hot plate, tail immersion, acetic acid-induced writhing, formalin and glutamate-induced nociception tests were used. The conventional medications were morphine sulphate (5 mg/kg, intraperitoneally) and diclofenac sodium (10 mg/kg, intraperitoneally). While the control group was expecting deionized water, MEDM was given orally at dosages of 200, 400, and 600 mg/kg (0.1 mL/mouse, orally). Results: According to the current research, MEDM strongly reflected the antinociceptive activity of all mouse models of chemical and heat-induced pain (*p < 0.05). 400 and 600 mg/kg demonstrated a considerable (*p < 0.05) ability to prolong the reaction of latency to pain in opposition to thermally produced nociception in hot plate and tail immersion tests. Inhibition levels in the acetic acid-induced writhing test were 11.57%, 37.77%, and 51.83%, respectively. The extract suppressed 20.78%, 45.48%, and 56.93% of licking during the initial stages of formalin-induced nociception. In the late phase, the extract showed higher rates of licking than the control group (13.14%, 50.28%, and 66.85%). The glutamate-induced nociception test was significantly (*p < 0.05) prevented by the plant extract. Compared to the control, it demonstrated an inhibition of licking of 22.85%, 47.32%, and 63.42%, respectively. Conclusions: It is evident that the plant extract has exceptional analgesic properties. To determine the precise processes behind antinociceptive effect and to identify the substances that produce this activity, more research is required. The展开更多
Objective:To evaluate the antinociceptive activity of the methanol extract of Ricinus communis leaves(MRCL).Methods:Antinociceptive activity was evaluated using acetic acid induced writhing test,formalin induced paw l...Objective:To evaluate the antinociceptive activity of the methanol extract of Ricinus communis leaves(MRCL).Methods:Antinociceptive activity was evaluated using acetic acid induced writhing test,formalin induced paw licking and tail immersion method in mice at doses of 100,125 and 130 mg/kg bw.Results:The results indicated that MRCL exhibited considerable antinociceptive activity against three classical models of pain in mice.Preliminary phytochemical analysis suggested the presence of saponin,steroids and alkaloids.Conclusions:It can be concluded that MRCL possesses antinociceptive potential that may be due to saponin,steroids and alkaloids in it.展开更多
Objective:To study the screening of essential oils of Skimmia laureola leaves(SLO)for acute toxicity,antinociceptive,antipyretic and anticonvulsant activities in various animal models.Methods:SLO were extracted using ...Objective:To study the screening of essential oils of Skimmia laureola leaves(SLO)for acute toxicity,antinociceptive,antipyretic and anticonvulsant activities in various animal models.Methods:SLO were extracted using modified Clevenger type apparatus.Acute toxicity test was used in mice to observe its safety level.Antinociceptive activity of SLO was evaluated in acetic acid induced writhing and hot plate tests.Yeast induced hyperthermic mice and pentylenetetrazole induced convulsive mice were used for the assessment of its antipyretic and anticonvulsant profile respectively.Results:Substantial safety was observed for SLO in acute toxicity test.SLO showed a high significant activity in acetic acid induced writhing test in a dose dependent manner with maximum pain attenuation of 68.48%at 200 mg/kg i.p.However,it did not produce any relief in thermal induced pain at test doses.When challenged against pyrexia evoked by yeast,SLO manifested marked amelioration in hyperthermic mice,dose dependently.Maximum anti-hyperthermic activity(75%)was observed at 200 mg/kg i.p.after 4 h of drug administration.Nevertheless,SLO had no effect on seizures control and mortality caused by pentylenetetrazole.Conclusions:In vivo studies of SLO showed prominent antinociceptive and antipyretic activities with ample safety profile and thus provided pharmacological base for the traditional uses of the plant in various painful conditions and pyrexia.Additional detail studies are required to ascertain its clinical application.展开更多
Two new sesquiterpenes, trivially named ricinusoids A(1) and ricinusoids B(2), were isolated from ethyl acetate fraction of Ricinus communis. The structures of new compounds were elucidated by detailed spectroscopic t...Two new sesquiterpenes, trivially named ricinusoids A(1) and ricinusoids B(2), were isolated from ethyl acetate fraction of Ricinus communis. The structures of new compounds were elucidated by detailed spectroscopic techniques, including 1 D-and 2 D-NMR, UV, IR spectroscopy, and mass spectrometry. The compounds(1-2) were also assessed for in-vivo sedative and analgesic like effects in open field and acetic acid induced writhing tests respectively at 5, 10, and 20 mg·kg^(–1) i.p. Pretreatment of both test compounds caused significant(P ≤ 0.05) reduction in locomotive activity like sedative agents and abdominal constrictions like analgesics. Both compounds(1-2) possessed marked sedative and antinociceptive effects in animal models.展开更多
Objective Qing Fu Juan Bi Tang(QFJBT)is an anti-arthritic Chinese medicine formula consisting of five herbs:Aconiti Lateralis Radix Praeparata(Fu Zi,附子),Sinomenii Caulis(Qing Feng Teng,青风藤),Astragali Radix(Huang ...Objective Qing Fu Juan Bi Tang(QFJBT)is an anti-arthritic Chinese medicine formula consisting of five herbs:Aconiti Lateralis Radix Praeparata(Fu Zi,附子),Sinomenii Caulis(Qing Feng Teng,青风藤),Astragali Radix(Huang Qi,黄芪),Paeoniae Radix Alba(Bai Shao,白芍)and Moutan Cortex(Mu Dan Pi,牡丹皮),which have well-established histories of use for treatment of rheumatic and arthritic diseases.We intended to establish the optimized and standardized pharmaceutical procedures and manufacturing processes for the pilot production of QFJBT to develop it as a novel botanical drug product for treatment of rheumatoid arthritis(RA).Methods The combinative approaches of chemical assessment,toxicological and pharmacological evaluation were explored to define the pharmaceutical preparation of QFJBT.Results The optimized and standardized pharmaceutical procedures and manufacturing processes for the pilot production of QFJBT were established in terms of greatest chemical contents of bioactive constituents,potent anti-inflammatory and antinociceptive activities,and favorable safety profile.Quality analysis of the pilot product of QFJBT by high-performance liquid chromatography(HPLC)demonstrated that the chromatographic fingerprint profiles of three batches of QFJBT were basically identical and the contents of four characteristic and bioactive markers were relatively consistent.General toxicological studies showed a favorable safety profile of QFJBT.The maximum tolerated single dose of QFJBT was determined in both sexes of rats to be 33.63 g/kg body weight which is equivalent to 346 times of clinical dose.In the chronic oral toxicity study,the results of laboratory investigation showed that QFJBT at doses of 3.89,6.80 and 9.72 g/kg body weight(equivalent to 40,70 and 100-fold clinical doses,respectively)caused no changes in all hematological parameters and blood biochemical parameters of rats.No mortality or specific toxic responses were observed in animals after three months of repeated dosing with QFJBT.Conclusion The op展开更多
BACKGROUND Inflammatory bowel diseases(IBD)are a worldwide health problem and mainly affect young people,consequently affecting the workforce.Available treatments are often associated with side effects,and new therape...BACKGROUND Inflammatory bowel diseases(IBD)are a worldwide health problem and mainly affect young people,consequently affecting the workforce.Available treatments are often associated with side effects,and new therapeutic options are needed.For centuries,plants have represented important substrates in the field of drug development.Lafoensia pacari(L.pacari)is a plant whose pharmaceutical potential has been described,and may have biological activity relevant to the treatment of IBD symptoms.AIM To investigate the activity of keto-alcoholic extracts of L.pacari with respect to ameliorating the inflammatory and nociceptive symptoms of acute experimental colitis in mice.METHODS Keto-alcoholic extracts of L.pacari leaves and bark were administered to male andfemale Swiss mice weighing 25 g to 30 g(n=8 male mice and n=8 female mice).The effect of these extracts was observed in an acetic acid-induced acute experimental model of colitis with regard to antinociception/analgesia and inflammatory tissue damage.Recorded macroscopic indices included the Wallace score and the colon weight obtained using a precision scale.Mechanical hyperalgesia was determined using an electronic analgesimeter.Behavior related to overt pain was determined by quantifying the number of writhing instances within 20 min of administration of acetic acid.Molecular docking was performed using human and murine cyclooxygenase-2(COX-2)with 3 flavonoids(ellagic acid,kaempferol,and quercetin)on the AutoDock Vina software.Analysis of variance followed by Tukey’s posttest was used with P<0.05 indicating significance.RESULTS In this murine model of colitis,administration of extracts from L.pacari ameliorated acetic acidinduced writhing and colitis-associated inflammatory pain.These improvements may be attributable to the reduction in edema,inflammation(e.g.,ulcers,hyperemia,and bowel wall damage),and the intensity of abdominal hyperalgesia.The keto-alcoholic extracts of L.pacari leaves and bark administered at a dose of either 100 mg/kg or 300 mg/kg signifi展开更多
Background:Ceiba pentandra is a medicinal plant used as alternative therapy to control parasitic nematodes in livestock.Objective:This study aims to investigate anti-parasitic effect of aqueous stem back extract of Ce...Background:Ceiba pentandra is a medicinal plant used as alternative therapy to control parasitic nematodes in livestock.Objective:This study aims to investigate anti-parasitic effect of aqueous stem back extract of Ceiba pentandra(L.)Gaertn through the evaluation of its anthelmintic,anti-inflammatory and analgesic activities.Methods:In vitro,the efficacy of aqueous extract(75 to 2400μg·mL−1)diluted in phosphate buffered saline(PBS)was tested against three stages of the life cycle of Haemonchus contortus through larval migration inhibition assay(LMIA),egg hatch assay(EHA),and adult worms motility inhibition assay(AMIA).In vivo,anti-inflammatory and antinociceptive properties of the aqueous extract(150 and 300 mg·kg−1)was evaluated on rodent using phlogistic and algic chemicals.Results:Significant inhibition activity(P<0.05)was obtained on EHA with the greatest inhibition of 46.63%obtained at 2400μg·mL−1.The plant treatment dramatically(P<0.05)inhibited L3 larval migration as compared to PBS.The highest inhibition rate was 53.33%at 1200μg·mL−1.Adding of polyvinylpolyrrolidone(PVPP)to the extract significantly(P<0.01)reduced at 38.6%the activity of the plant extract on larval migration compared to extract without PVPP.The Ceiba pentandra extract reduced(P<0.05)worm motility after 24 h post exposure as compared to control.In vitro,aqueous extract significantly(P<0.05)inhibited the paw inflammation induced by carragenine,with a significant(P<0.05)reduction of the number of abdominal contortions induced by acetic acid to 41.11%at 300 mg·kg−1 and the paw licking time induced by formaline in both phases to 57.22%and 63.59%at 300 mg·kg−1 likened to control.Conclusions:In vitro results suggest that,this plant possess anti-parasitic properties.Antinociceptive and anti-inflammatory effects of C.pentandra can contribute to its anti-parasitic property.展开更多
BACKGROUND： It has been previously shown that intrathecal administration of either ouabain or neosdgmine can produce antinociceptive effects. Moreover, ouabain and neostigmine are differently associated with acetylch...BACKGROUND： It has been previously shown that intrathecal administration of either ouabain or neosdgmine can produce antinociceptive effects. Moreover, ouabain and neostigmine are differently associated with acetylcholine. OBJECTIVE： It has been hypothesized that intrathecal administration of ouabain, in combination with neostigmine, can produce antinociceptive synergistic effects. Atropine, as a competitive antagonist, was pre-injected to verify the mechanisms of action. DESIGN, TIME AND SETTING： This study was a randomized, controlled, animal experiment, performed at the State Key Laboratory of Oncology in Southern China between May 2006 and February 2007. MATERIALS： A total of 102 healthy, adult, Sprague Dawley rats were included. Ouabain and neostigmine （Sigma, USA）, as well as atropine （Tanabe Seiyaku, Japan）, were also used. METHODS： Varied doses of ouabain, neostigmine, and a combination of the two were intrathecally injected into rats. Six rats were allotted for each dose group. Intrathecal pretreatment with atropine was tested 10 minutes prior to intrathecal administration of neostigmine or the combination of ouabain and neostigmine. MAIN OUTCOME MEASURES： Tail-flick tests were performed to measure tail-flick latency （seconds） prior to and after administration. The response in the tail-flick test was expressed as the percentage of maximum possible effect （% MPE）, where % MPE = [tail-flick latency after administration （seconds） -mean baseline value for tail-flick latency]/[ 10 seconds - the mean baseline value for tail-flick latency （seconds）] x 100%. RESULTS： Rat spinal intrathecal administration of either ouabain or neostigmine alone produced antinociceptive effects in a dose-dependent manner. Intrathecally administration of neostigmine （0.05, 0.1, 0.3 μg ） in combination with ouabain （1 μ g ） produced enhanced antinociceptive effects, with a % MPE of 29%, 78%, and 95%, respectively （P 〈 0.05）. Intrathecally administration of 0.3μg neostigmine （% 展开更多
基金the National Science and Technology Support Program during the Twelfth Five-Year Plan of China(Grant No.2011BAI03B05)the Distinguished Professor Foundation of Liaoning Province of China of 2011,Innovative Drug Incubation Base Plan Project from Liaoning Province of China of 2013(Grant No.2013226027) National College Students Innovative and Entrepreneurial Training Program of China(Grant No.201310163019)
文摘In the present study, the chemical composition, antinociceptive effect and acute toxicity of essential oils（EOs） of Asarum heterotropoides Fr. Schmidt var. mandshuricum（Maxim.） Kitag.（AHM）, A. sieboldii Miq. var. seoulense Nakai（ASS） and A. himalaicum Hook. f. et Thoms. ex Klotzsch.（AH） were comparatively evaluated. A total of 55 compounds were identified in EOs of AHM, ASS and AH by GC-MS. Methyleugenol（20.16%–62.89%）, safrole（2.67%–32.42%）, 3,5-dimethoxytoluene（2.00%–18.59%） and eucarvone（1.52%–19.16%） were the major constituents of EO of AHM, and methyleugenol（48.35%–61.06%）, eucarvone（11.13%–13.93%） and elemicin（4.79%–11.14%） were the major constituents of EO of ASS. The EO of AH was different from that of AHM and ASS, in which patchouli alcohol（27.42%–51.95%） and elemicin（13.11%–42.23%） were found in a greater amount. Moreover, the antinociceptive effect of EOs of AHM（5.5, 11.0, 16.5 μL/kg） and AH（2.0, 4.0, 6.0 μL/kg） was comparatively assayed in acetic acid-induced writhing, hot plate and formalin tests. The results indicated a weak central, but potent peripheral antinociceptive effect of EO of AHM, and more potent central and peripheral antinociceptive effect of EO of AH. The LD50 of the EOs of AHM and AH were 1.7 and 7.7 mL/kg, respectively. These findings suggest that EOs of AHM and AH possess evident antinociceptive activity and are probably safe within the range of its clinical doses. However, their chemical compositions are quite different. Therefore, AH can be clinically used as an herbal medicinal product with broad analgesic effects, but should not be confused with AHM and ASS used in traditional Chinese medicine.
文摘Background: Codiaeum variegatum, sometimes called garden croton, is a tropical plant in the Euphorbiaceae family. Historically used to cure various conditions, including intestinal infections, fever, ulcers, wounds, and gonorrhea. This work aimed to investigate the antinociceptive effects of ethanolic extract of Codiaeum variegatum leaves (EECV) in animal models. Methods: Five different pain models—the hot plate, tail immersion, acetic acid-induced writhing, formalin, and glutamate-induced nociception tests—were utilized to assess the antinociceptive activity in mice. The traditional drugs such as diclofenac sodium (10 mg/kg, i.p.) and morphine sulphate (5 mg/kg). EECV was administered orally at varying doses of 100, 200, and 300 mg/kg (0.1 mL/mouse), while the control group was given deionized water. Results: The current study found that all mouse models of heat- and chemical-induced pain had robust EECV reflections of their antinociceptive properties (*p Conclusions: The current finding offers a fresh perspective on the ethanolic extract of Codiaeum variegatum leaves’ antinociceptive properties in mice. This plant’s phytochemical analysis revealed the presence of triterpenoids, sterols, alkaloids, flavonoids, and general glycosides, all of which may have antinociceptive properties. More research on the mechanism of action and associated pharmacological studies, such as in vivo analysis, medication formulation, and clinical trials, is strongly advised.
基金supported by grants from the National Natural Science Foundation of China(Nos.21572274 and 21732008)the CAMS Innovation Fund for Medical Sciences(No.2016-I2M1-010,China)
文摘Twelve new grayanoids(1-12)along with five known compounds were isolated from flowers of Rhododendron molle.Their structures were fully characterized using a combination of spectroscopic analyses,computational calculations,and single crystal X-ray diffraction.Rhomollone A(1)possesses an unprecedented 5/6/6/5 tetra-cyclic ring system(B-nor grayanane)incorporating a cyclopentene-1,3-dione scaffold.Rhodomollein XLIII(2)is a dimeric grayanoid,containing a novel 14-membered heterocyclic ring with a C2 symmetry axis.The antinociceptive activities of compounds 3,4,6,7,and 12-17 were evaluated by an acetic acid-induced writhing test.Among them,compounds 3,7,12,15 and 16 displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from41.9%to 91.6%.Compounds 6 and 13 inhibited 46.0%and 39.4%of the acetic acid-induced writhes at a dose of 2 mg/kg,while compound 17 inhibited 34.3%of the writhes at a dose of 0.4 mg/kg.
文摘Background: Diospyros malabarica (Desr.) Kostel, a small to medium-sized tree in the Ebenaceae family, is known as “Deshi Gab” in Bangladesh. Fever, diabetes, snake bite, diarrhea, biliousness, and ulcer ailments are all treated with the herb. This study’s goal was to examine in mouse models the antinociceptive properties of methanol extract of Diospyros malabarica leaves (MEDM). Methods: For the purpose of determining the antinociceptive activity in mice, five distinct pain models including hot plate, tail immersion, acetic acid-induced writhing, formalin and glutamate-induced nociception tests were used. The conventional medications were morphine sulphate (5 mg/kg, intraperitoneally) and diclofenac sodium (10 mg/kg, intraperitoneally). While the control group was expecting deionized water, MEDM was given orally at dosages of 200, 400, and 600 mg/kg (0.1 mL/mouse, orally). Results: According to the current research, MEDM strongly reflected the antinociceptive activity of all mouse models of chemical and heat-induced pain (*p < 0.05). 400 and 600 mg/kg demonstrated a considerable (*p < 0.05) ability to prolong the reaction of latency to pain in opposition to thermally produced nociception in hot plate and tail immersion tests. Inhibition levels in the acetic acid-induced writhing test were 11.57%, 37.77%, and 51.83%, respectively. The extract suppressed 20.78%, 45.48%, and 56.93% of licking during the initial stages of formalin-induced nociception. In the late phase, the extract showed higher rates of licking than the control group (13.14%, 50.28%, and 66.85%). The glutamate-induced nociception test was significantly (*p < 0.05) prevented by the plant extract. Compared to the control, it demonstrated an inhibition of licking of 22.85%, 47.32%, and 63.42%, respectively. Conclusions: It is evident that the plant extract has exceptional analgesic properties. To determine the precise processes behind antinociceptive effect and to identify the substances that produce this activity, more research is required. The
文摘Objective:To evaluate the antinociceptive activity of the methanol extract of Ricinus communis leaves(MRCL).Methods:Antinociceptive activity was evaluated using acetic acid induced writhing test,formalin induced paw licking and tail immersion method in mice at doses of 100,125 and 130 mg/kg bw.Results:The results indicated that MRCL exhibited considerable antinociceptive activity against three classical models of pain in mice.Preliminary phytochemical analysis suggested the presence of saponin,steroids and alkaloids.Conclusions:It can be concluded that MRCL possesses antinociceptive potential that may be due to saponin,steroids and alkaloids in it.
基金Supported by Higier Education of Pakistan (HEC) with Grant No.bm6-071/HEC/Pak
文摘Objective:To study the screening of essential oils of Skimmia laureola leaves(SLO)for acute toxicity,antinociceptive,antipyretic and anticonvulsant activities in various animal models.Methods:SLO were extracted using modified Clevenger type apparatus.Acute toxicity test was used in mice to observe its safety level.Antinociceptive activity of SLO was evaluated in acetic acid induced writhing and hot plate tests.Yeast induced hyperthermic mice and pentylenetetrazole induced convulsive mice were used for the assessment of its antipyretic and anticonvulsant profile respectively.Results:Substantial safety was observed for SLO in acute toxicity test.SLO showed a high significant activity in acetic acid induced writhing test in a dose dependent manner with maximum pain attenuation of 68.48%at 200 mg/kg i.p.However,it did not produce any relief in thermal induced pain at test doses.When challenged against pyrexia evoked by yeast,SLO manifested marked amelioration in hyperthermic mice,dose dependently.Maximum anti-hyperthermic activity(75%)was observed at 200 mg/kg i.p.after 4 h of drug administration.Nevertheless,SLO had no effect on seizures control and mortality caused by pentylenetetrazole.Conclusions:In vivo studies of SLO showed prominent antinociceptive and antipyretic activities with ample safety profile and thus provided pharmacological base for the traditional uses of the plant in various painful conditions and pyrexia.Additional detail studies are required to ascertain its clinical application.
基金financially supported by the Higher Education Commission of Pakistan(No.2003)
文摘Two new sesquiterpenes, trivially named ricinusoids A(1) and ricinusoids B(2), were isolated from ethyl acetate fraction of Ricinus communis. The structures of new compounds were elucidated by detailed spectroscopic techniques, including 1 D-and 2 D-NMR, UV, IR spectroscopy, and mass spectrometry. The compounds(1-2) were also assessed for in-vivo sedative and analgesic like effects in open field and acetic acid induced writhing tests respectively at 5, 10, and 20 mg·kg^(–1) i.p. Pretreatment of both test compounds caused significant(P ≤ 0.05) reduction in locomotive activity like sedative agents and abdominal constrictions like analgesics. Both compounds(1-2) possessed marked sedative and antinociceptive effects in animal models.
基金support from the National Natural Science Foundation of China(No.81704065)China Postdoctoral Science Foundation(No.2016M600632 and No.2017T100604)+3 种基金Hunan Provincial Natural Science Foundation(No.2017JJ3239 and No.2018JJ2293)Hunan Education Department’s Science&Research Project(No.17K069)Hunan Provincial Science&Research Project of Chinese Medicine(No.201790)National First-class Disciple Construction Project of Chinese Medicine of Hunan University of Chinese Medicine
文摘Objective Qing Fu Juan Bi Tang(QFJBT)is an anti-arthritic Chinese medicine formula consisting of five herbs:Aconiti Lateralis Radix Praeparata(Fu Zi,附子),Sinomenii Caulis(Qing Feng Teng,青风藤),Astragali Radix(Huang Qi,黄芪),Paeoniae Radix Alba(Bai Shao,白芍)and Moutan Cortex(Mu Dan Pi,牡丹皮),which have well-established histories of use for treatment of rheumatic and arthritic diseases.We intended to establish the optimized and standardized pharmaceutical procedures and manufacturing processes for the pilot production of QFJBT to develop it as a novel botanical drug product for treatment of rheumatoid arthritis(RA).Methods The combinative approaches of chemical assessment,toxicological and pharmacological evaluation were explored to define the pharmaceutical preparation of QFJBT.Results The optimized and standardized pharmaceutical procedures and manufacturing processes for the pilot production of QFJBT were established in terms of greatest chemical contents of bioactive constituents,potent anti-inflammatory and antinociceptive activities,and favorable safety profile.Quality analysis of the pilot product of QFJBT by high-performance liquid chromatography(HPLC)demonstrated that the chromatographic fingerprint profiles of three batches of QFJBT were basically identical and the contents of four characteristic and bioactive markers were relatively consistent.General toxicological studies showed a favorable safety profile of QFJBT.The maximum tolerated single dose of QFJBT was determined in both sexes of rats to be 33.63 g/kg body weight which is equivalent to 346 times of clinical dose.In the chronic oral toxicity study,the results of laboratory investigation showed that QFJBT at doses of 3.89,6.80 and 9.72 g/kg body weight(equivalent to 40,70 and 100-fold clinical doses,respectively)caused no changes in all hematological parameters and blood biochemical parameters of rats.No mortality or specific toxic responses were observed in animals after three months of repeated dosing with QFJBT.Conclusion The op
文摘BACKGROUND Inflammatory bowel diseases(IBD)are a worldwide health problem and mainly affect young people,consequently affecting the workforce.Available treatments are often associated with side effects,and new therapeutic options are needed.For centuries,plants have represented important substrates in the field of drug development.Lafoensia pacari(L.pacari)is a plant whose pharmaceutical potential has been described,and may have biological activity relevant to the treatment of IBD symptoms.AIM To investigate the activity of keto-alcoholic extracts of L.pacari with respect to ameliorating the inflammatory and nociceptive symptoms of acute experimental colitis in mice.METHODS Keto-alcoholic extracts of L.pacari leaves and bark were administered to male andfemale Swiss mice weighing 25 g to 30 g(n=8 male mice and n=8 female mice).The effect of these extracts was observed in an acetic acid-induced acute experimental model of colitis with regard to antinociception/analgesia and inflammatory tissue damage.Recorded macroscopic indices included the Wallace score and the colon weight obtained using a precision scale.Mechanical hyperalgesia was determined using an electronic analgesimeter.Behavior related to overt pain was determined by quantifying the number of writhing instances within 20 min of administration of acetic acid.Molecular docking was performed using human and murine cyclooxygenase-2(COX-2)with 3 flavonoids(ellagic acid,kaempferol,and quercetin)on the AutoDock Vina software.Analysis of variance followed by Tukey’s posttest was used with P<0.05 indicating significance.RESULTS In this murine model of colitis,administration of extracts from L.pacari ameliorated acetic acidinduced writhing and colitis-associated inflammatory pain.These improvements may be attributable to the reduction in edema,inflammation(e.g.,ulcers,hyperemia,and bowel wall damage),and the intensity of abdominal hyperalgesia.The keto-alcoholic extracts of L.pacari leaves and bark administered at a dose of either 100 mg/kg or 300 mg/kg signifi
文摘Background:Ceiba pentandra is a medicinal plant used as alternative therapy to control parasitic nematodes in livestock.Objective:This study aims to investigate anti-parasitic effect of aqueous stem back extract of Ceiba pentandra(L.)Gaertn through the evaluation of its anthelmintic,anti-inflammatory and analgesic activities.Methods:In vitro,the efficacy of aqueous extract(75 to 2400μg·mL−1)diluted in phosphate buffered saline(PBS)was tested against three stages of the life cycle of Haemonchus contortus through larval migration inhibition assay(LMIA),egg hatch assay(EHA),and adult worms motility inhibition assay(AMIA).In vivo,anti-inflammatory and antinociceptive properties of the aqueous extract(150 and 300 mg·kg−1)was evaluated on rodent using phlogistic and algic chemicals.Results:Significant inhibition activity(P<0.05)was obtained on EHA with the greatest inhibition of 46.63%obtained at 2400μg·mL−1.The plant treatment dramatically(P<0.05)inhibited L3 larval migration as compared to PBS.The highest inhibition rate was 53.33%at 1200μg·mL−1.Adding of polyvinylpolyrrolidone(PVPP)to the extract significantly(P<0.01)reduced at 38.6%the activity of the plant extract on larval migration compared to extract without PVPP.The Ceiba pentandra extract reduced(P<0.05)worm motility after 24 h post exposure as compared to control.In vitro,aqueous extract significantly(P<0.05)inhibited the paw inflammation induced by carragenine,with a significant(P<0.05)reduction of the number of abdominal contortions induced by acetic acid to 41.11%at 300 mg·kg−1 and the paw licking time induced by formaline in both phases to 57.22%and 63.59%at 300 mg·kg−1 likened to control.Conclusions:In vitro results suggest that,this plant possess anti-parasitic properties.Antinociceptive and anti-inflammatory effects of C.pentandra can contribute to its anti-parasitic property.
基金the National Natural Science Foundation of China, No. 30571794,C03030301Sci-tech Development Program,No.303040077001
文摘BACKGROUND： It has been previously shown that intrathecal administration of either ouabain or neosdgmine can produce antinociceptive effects. Moreover, ouabain and neostigmine are differently associated with acetylcholine. OBJECTIVE： It has been hypothesized that intrathecal administration of ouabain, in combination with neostigmine, can produce antinociceptive synergistic effects. Atropine, as a competitive antagonist, was pre-injected to verify the mechanisms of action. DESIGN, TIME AND SETTING： This study was a randomized, controlled, animal experiment, performed at the State Key Laboratory of Oncology in Southern China between May 2006 and February 2007. MATERIALS： A total of 102 healthy, adult, Sprague Dawley rats were included. Ouabain and neostigmine （Sigma, USA）, as well as atropine （Tanabe Seiyaku, Japan）, were also used. METHODS： Varied doses of ouabain, neostigmine, and a combination of the two were intrathecally injected into rats. Six rats were allotted for each dose group. Intrathecal pretreatment with atropine was tested 10 minutes prior to intrathecal administration of neostigmine or the combination of ouabain and neostigmine. MAIN OUTCOME MEASURES： Tail-flick tests were performed to measure tail-flick latency （seconds） prior to and after administration. The response in the tail-flick test was expressed as the percentage of maximum possible effect （% MPE）, where % MPE = [tail-flick latency after administration （seconds） -mean baseline value for tail-flick latency]/[ 10 seconds - the mean baseline value for tail-flick latency （seconds）] x 100%. RESULTS： Rat spinal intrathecal administration of either ouabain or neostigmine alone produced antinociceptive effects in a dose-dependent manner. Intrathecally administration of neostigmine （0.05, 0.1, 0.3 μg ） in combination with ouabain （1 μ g ） produced enhanced antinociceptive effects, with a % MPE of 29%, 78%, and 95%, respectively （P 〈 0.05）. Intrathecally administration of 0.3μg neostigmine （%
