关键词: %MPE, % maximum possible effect Antinociceptive CNS safety pharmacology CNS, central nervous system CP extract, Clerodendrum petasites S. Moore ethanolic extract Clerodendrum petasites IACUC, Institutional Animal Care and Use Committee NSAIDs, nonsteroidal anti-inflammatory drugs Thai herb

来  源:   DOI:10.1016/j.jtcme.2022.11.001   PDF(Pubmed)

Abstract:
UNASSIGNED: Clerodendrum petasites, an herbal plant in Thailand, has been used for many years in folk medicine. However, scientific evidence regarding CNS safety pharmacology and antinociceptive activity of C. petasites (CP) has not yet been well characterized.
UNASSIGNED: The present study aimed to assess the CNS safety pharmacology and antinociceptive and antiinflammatory effects of CP extract.
UNASSIGNED: The effect of CP extract on CNS safety pharmacology was assessed using LABORAS automated home cage monitoring and rotarod test. Its pharmacological activity was evaluated both in-vitro, and in-vivo using hot-plate, acetic acid-induced writhing, formalin, and carrageenan-induced paw edema models.
UNASSIGNED: CP extract significantly improved thermal and chemical nociceptive behaviors and acute inflammatory pain at all doses: 300, 600, and 1200 mg/kg, p.o. The antiinflammatory effect of CP extract in inflammatory pain models was comparable to the effect of positive control: indomethacin 10 mg/kg at all dose levels tested. Further, the CP extract at 600 mg/kg dose significantly inhibited 82.3% of carrageenan-induced total edema. In-vitro, CP extract at 12.5, 25, and 50 μg/mL concentrations significantly reduced the expression of LPS-induced nitric oxide, IL-6, and TNF-α expression in both RAW 264.7 macrophage and BV-2 microglial cell lines. In addition, CP extract did not show any potential effects on the CNS, indicated by no significant effects on motor coordination, spontaneous locomotor activity, general behaviors, and well-being compared to vehicle-treated mice (p > 0.05). Overall, the present study evidences the potential antinociceptive, antiinflammatory efficacies of CP extract with a favorable CNS safety profile.
摘要:
未经批准:克罗登鼓花瓣,泰国的草药植物,已经在民间医学中使用了很多年。然而,关于C.petasites(CP)的CNS安全性药理学和抗伤害感受活性的科学证据尚未得到很好的表征。
未经批准:本研究旨在评估CP提取物的CNS安全药理学和镇痛和抗炎作用。
UNASSIGNED:使用LABORAS自动家笼监测和旋转杆测试评估了CP提取物对CNS安全性药理学的影响。其药理活性在体外进行了评估,在体内使用热板,乙酸引起的扭动,福尔马林,和角叉菜胶诱导的爪水肿模型。
UNASSIGNED:CP提取物在所有剂量(300、600和1200mg/kg)下均能显著改善热和化学伤害性行为和急性炎性疼痛,CP提取物在炎性疼痛模型中的抗炎作用与阳性对照的作用相当:在所有测试的剂量水平下,吲哚美辛10mg/kg。Further,600mg/kg剂量的CP提取物显着抑制角叉菜胶诱导的总水肿的82.3%。体外,12.5、25和50μg/mL浓度的CP提取物显着降低了LPS诱导的一氧化氮的表达,RAW264.7巨噬细胞和BV-2小胶质细胞系中IL-6和TNF-α的表达。此外,CP提取物对中枢神经系统没有任何潜在的影响,对运动协调没有显著影响,自发的运动活动,一般行为,和与媒介物处理的小鼠相比的幸福感(p>0.05)。总的来说,本研究证明了潜在的抗伤害感受,具有良好CNS安全性的CP提取物的抗炎功效。
公众号