Ferreira J, Floriani A E, Filho V C, Delle Monache F, Yunes R A, Calixto J B, Santos A R
Núcleo de Investigações Químico-Farmacêuticas (NIQFAR)/CCS, Universidade do Vale do Itajaí, SC, Brazil.
Life Sci. 2000 Jan 21;66(9):791-802. doi: 10.1016/s0024-3205(99)00652-9.
The antinociceptive effect of the methanolic extract (ME) and two triterpenes isolated from E. mosenii (Orchidaceae) has been investigated in chemical and thermal models of nociception in mice. The ME of E. mosenii (0.3-30 mg kg(-1), i.p. or 50-400 mg kg(-1), p.o.) produced dose-related, significant and long-lasting (4 to 6 h) inhibition of acetic acid-induced abdominal constriction, with ID50 values of 3.9 and 137.0 mg kg(-1), respectively. Pholidotin and 24-methylenecycloartenol isolated from E. mosenii (0.1-3.0 mg kg(-1), i.p.) also produced marked and dose-related inhibition of acetic acid-induced pain, with ID50 values of 0.9 and 1.1 mg kg(-1). However, these compounds and the ME were about 3- to 13-fold more potent at the level of ID50 than diclofenac when assessed in acetic acid-induced abdominal constriction. The ME of E. mosenii in the same range of doses produced dose-related inhibition of both phases of formalin-induced licking, with mean ID50 values for the first and the second phases of 0.9, 122.0 mg kg(-1) and 0.7, 258.0 mg kg(-1), respectively by i.p. or p.o. routes. In addition, the ME (0.3-30 mg kg(-1), i.p., or 50-400 mg kg(-1), p.o.) also caused dose-related inhibition of capsaicin-induced neurogenic pain with mean ID50 values of 5.2 and 130.0 mg kg(-1), respectively. Treatment of animals with naloxone (5 mg kg(-1), i.p.) completely reversed the antinociceptive effect caused by morphine (5 mg kg(-1), s.c.) and that caused by ME of E. mosenii (1 mg kg(-1), i.p.) when assessed against either phase of the formalin-induced pain. Furthermore, when assessed in the hot-plate test, ME (100 mg kg(-1), i.p.) and morphine (10 mg kg(-1), s.c.) caused significant increase in response latency. However, ME given daily for to 7 consecutive days did not develop tolerance to itself nor did it induce cross-tolerance to morphine. Taken together these data demonstrate that the ME of E. mosenii elicited pronounced antinociception, when assessed by i.p. or p.o. routes, against several models of pain. Its actions involve, at least in part, an interaction with opioid system, seeming no to be related with a non-specific peripheral or central depressant actions. Finally, the active principle(s) responsible for the antinociceptive action of E. mosenii is likely related to the presence of the triterpenes.
已在小鼠伤害感受的化学和热模型中研究了从莫氏火烧兰（兰科）分离得到的甲醇提取物（ME）和两种三萜类化合物的抗伤害感受作用。莫氏火烧兰的ME（0.3 - 30 mg kg⁻¹，腹腔注射或50 - 400 mg kg⁻¹，口服）对醋酸诱导的腹部收缩产生剂量相关、显著且持久（4至6小时）的抑制作用，腹腔注射和口服的半数抑制剂量（ID50）值分别为3.9和137.0 mg kg⁻¹。从莫氏火烧兰中分离得到的蛇菰醇和24 - 亚甲基环阿尔廷醇（0.1 - 3.0 mg kg⁻¹，腹腔注射）也对醋酸诱导的疼痛产生显著且剂量相关的抑制作用，ID50值分别为0.9和1.1 mg kg⁻¹。然而，在醋酸诱导的腹部收缩实验中评估时，这些化合物和ME在ID50水平下的效力比双氯芬酸强约3至13倍。相同剂量范围内的莫氏火烧兰ME对福尔马林诱导舔舐的两个阶段均产生剂量相关的抑制作用，腹腔注射或口服途径给药时，第一阶段和第二阶段的平均ID50值分别为0.9、122.0 mg kg⁻¹和0.7、258.0 mg kg⁻¹。此外，ME（0.3 - 30 mg kg⁻¹，腹腔注射，或50 - 400 mg kg⁻¹，口服）也对辣椒素诱导的神经源性疼痛产生剂量相关的抑制作用，平均ID50值分别为5.2和130.0 mg kg⁻¹。当针对福尔马林诱导疼痛的任一阶段进行评估时，用纳洛酮（5 mg kg⁻¹，腹腔注射）处理动物可完全逆转吗啡（5 mg kg⁻¹，皮下注射）和莫氏火烧兰ME（1 mg kg⁻¹，腹腔注射）引起的抗伤害感受作用。此外，在热板试验中评估时，ME（100 mg kg⁻¹，腹腔注射）和吗啡（10 mg kg⁻¹，皮下注射）可使反应潜伏期显著延长。然而，连续7天每日给予ME并未产生自身耐受性，也未诱导对吗啡的交叉耐受性。综上所述，这些数据表明，通过腹腔注射或口服途径评估时，莫氏火烧兰的ME对多种疼痛模型均有明显的抗伤害感受作用。其作用至少部分涉及与阿片系统的相互作用，似乎与非特异性外周或中枢抑制作用无关。最后，负责莫氏火烧兰抗伤害感受作用的活性成分可能与三萜类化合物的存在有关。
Zotero 插件