Núcleo de Investigações Químico-Farmacêuticas (NIQFAR) and Programa de Mestrado em Ciências Farmacêuticas, Universidade do Vale do Itajaí (UNIVALI), Itajaí, SC, Brazil.
Planta Med. 2011 Jul;77(10):1035-43. doi: 10.1055/s-0030-1250745. Epub 2011 Jan 31.
Cipura paludosa (Iridaceae) is a plant that is distributed in the north region of Brazil. Its bulbs are used in folk medicine to treat inflammation and pain. Four naphthalene derivatives have been isolated from the bulbs of this plant. Three of them have been identified as the known naphthalene derivatives, eleutherine, iso-eleutherine, and hongkonin. The structure of the fourth and new component was determined as 11-hydroxyeleutherine by extensive NMR study. In addition, the IN VIVO effect of the two major compounds, eleutherine and iso-eleutherine, was evaluated in carrageenan-induced hypernociception and inflammation in mice. Eleutherine and iso-eleutherine (1.04-34.92 µmol/kg), dosed intraperitoneally (i.p.) or orally (p.o.), decreased the carrageenan-induced paw oedema (i.p. - inhibitions of 36 ± 7 % and 58 ± 14 %, respectively; p.o. - inhibitions of 36 ± 7 % and 58 ± 14 %, respectively). Iso-eleutherine, but not eleutherine, significantly reduced (inhibitions of 39 ± 4 %) the plasma extravasation induced by intradermal (i.d.) injection of carrageenan. Likewise, eleutherine and iso-eleutherine (1.04-34.92 µmol/kg, i.p. or p.o.) were also effective in preventing the carrageenan-induced hypernociceptive response (i.p. - inhibition of 59 ± 4 % and 63 ± 1 %, respectively; p.o. - inhibitions of 36 ± 7 % and 58 ± 14 %, respectively). It was also suggested that the anti-inflammatory and anti-hypernociceptive effects of eleutherine or iso-eleutherine partly depend on the interference with the synthesis or activity of mast cell products, kinins, cytokine, chemokines, prostanoids, or sympathetic amines. Our findings show that two major compounds of C. paludosa contain pharmacologically active constituents that possess antinociceptive and anti-inflammatory activity, justifying, at least in part, its popular therapeutic use for treating conditions associated with pain.
沼泽泽兰（鸢尾科）是一种分布于巴西北部地区的植物。其鳞茎在民间医学中用于治疗炎症和疼痛。从该植物的鳞茎中分离出了四种萘衍生物。其中三种已被鉴定为已知的萘衍生物，即非洲防己碱、异非洲防己碱和红古豆碱。第四种和新的成分的结构通过广泛的 NMR 研究确定为 11-羟基非洲防己碱。此外，还评估了两种主要化合物，即非洲防己碱和异非洲防己碱，在角叉菜胶诱导的小鼠痛觉过敏和炎症中的体内作用。非洲防己碱和异非洲防己碱（1.04-34.92 µmol/kg），腹腔内（i.p.）或口服（p.o.）给药，可减少角叉菜胶诱导的足肿胀（i.p. - 分别抑制 36±7%和 58±14%；p.o. - 分别抑制 36±7%和 58±14%）。异非洲防己碱而非非洲防己碱显著减少（抑制 39±4%）由皮内（i.d.）注射角叉菜胶引起的血浆渗出。同样，非洲防己碱和异非洲防己碱（1.04-34.92 µmol/kg，i.p. 或 p.o.）也能有效预防角叉菜胶诱导的痛觉过敏反应（i.p. - 抑制 59±4%和 63±1%，分别；p.o. - 分别抑制 36±7%和 58±14%）。研究还表明，非洲防己碱或异非洲防己碱的抗炎和抗痛觉过敏作用部分依赖于干扰肥大细胞产物、激肽、细胞因子、趋化因子、前列腺素或交感胺的合成或活性。我们的研究结果表明，沼泽泽兰的两种主要化合物含有具有镇痛和抗炎活性的药理活性成分，这至少部分解释了其在民间医学中用于治疗与疼痛相关疾病的广泛应用。
