关键词: Analgesic Cholinergic Agents Cynara scolymus GABA Mice Opioid Pain Measurient

来  源:   DOI:10.3344/kjp.23355   PDF(Pubmed)

Abstract:
UNASSIGNED: Cynara scolymus has bioactive constituents and has been used for therapeutic actions. The present study was undertaken to investigate the mechanisms underlying pain-relieving effects of the hydroethanolic extract of C. scolymus (HECS).
UNASSIGNED: The antinociceptive activity of HECS was assessed through formalin and acetic acid-induced writhing tests at doses of 50, 100 and 200 mg/kg intraperitoneally. Additionally, naloxone (non-selective opioid receptors antagonist, 2 mg/kg), atropine (non-selective muscarinic receptors antagonist, 1 mg/kg), chlorpheniramine (histamine HH1-receptor antagonist, 20 mg/kg), cimetidine (histamine H2-receptor antagonist, 12.5 mg/kg), flumazenil (GABAA/BDZ receptor antagonist, 5 mg/kg) and cyproheptadine (serotonin receptor antagonist, 4 mg/kg) were used to determine the systis implicated in HECS-induced analgesia. Impact of HECS on locomotor activity was executed by open-field test. Determination of total phenolic content (TPC) and total flavonoid content (TFC) was done. Evaluation of antioxidant activity was conducted iploying 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay.
UNASSIGNED: HECS (50, 100 and 200 mg/kg) significantly indicated dose dependent antinociceptive activity against pain-related behavior induced by formalin and acetic acid (P < 0.001). Pretreatment with naloxone, atropine and flumazenil significantly reversed HECS-induced analgesia. Antinociceptive effect of HECS riained unaffected by chlorpheniramine, cimetidine and cyproheptadine. Locomotor activity was not affected by HECS. TPC and TFC of HECS were 59.49 ± 5.57 mgGAE/g dry extract and 93.39 ± 17.16 mgRE/g dry extract, respectively. DPPH free radical scavenging activity (IC50) of HECS was 161.32 ± 0.03 μg/mL.
UNASSIGNED: HECS possesses antinociceptive activity which is mediated via opioidergic, cholinergic and GABAergic pathways.
摘要:
Cynarascolymus具有生物活性成分,已用于治疗作用。本研究旨在研究C.scolymus(HECS)的乙醇提取物的镇痛作用的潜在机制。
通过50、100和200mg/kg剂量的福尔马林和乙酸诱导的扭体试验,腹膜内评估了HECS的抗伤害感受活性。此外,纳洛酮(非选择性阿片受体拮抗剂,2mg/kg),阿托品(非选择性毒蕈碱受体拮抗剂,1mg/kg),扑尔敏(组胺HH1受体拮抗剂,20mg/kg),西咪替丁(组胺H2受体拮抗剂,12.5mg/kg),氟马西尼(GABAA/BDZ受体拮抗剂,5mg/kg)和赛庚啶(5-羟色胺受体拮抗剂,4mg/kg)用于确定与HECS诱导的镇痛有关的系统。HECS对运动活动的影响通过旷场试验进行。测定总酚含量(TPC)和总黄酮含量(TFC)。采用2,2-二苯基-1-吡啶酰肼(DPPH)自由基清除试验进行抗氧化活性评价。
HECS(50、100和200mg/kg)显着表明对福尔马林和乙酸引起的疼痛相关行为的剂量依赖性抗伤害感受活性(P<0.001)。用纳洛酮预处理,阿托品和氟马西尼可显著逆转HECS诱导的镇痛作用。不受扑尔敏影响的HECS的伤害感受作用,西咪替丁和赛庚啶。运动活动不受HECS影响。HECS的TPC和TFC为59.49±5.57mgGAE/g干提取物和93.39±17.16mgRE/g干提取物,分别。HECS的DPPH自由基清除活性(IC50)为161.32±0.03μg/mL。
HECS具有抗伤害感受活性,该活性是通过opiopideric介导的,胆碱能和GABA能途径。
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