Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí, Rua Uruguai, 458, 88302-202, Itajaí, SC, Brazil.
Arch Pharm Res. 2012 Mar;35(4):623-31. doi: 10.1007/s12272-012-0405-3. Epub 2012 May 3.
In a search for new and effective analgesic substances from the Brazilian biodiversity, the present study evaluates the chemical composition and antinociceptive potential of the methanol extract and a pure compound obtained from the seeds of Garcinia achachairu Rusby (Clusiaceae). The methanolic seed extract was directly subjected to purification by column chromatography and the purification was monitored by thin-layer chromatography. The main isolated compound was identified as Guttiferone A by comparison of conventional spectroscopic data (IR, NMR-(1)H and (13)C) to the literature data which was isolated for the first time from this plant. When evaluated in the acetic acid-induced nociception model in mice, the methanolic seed extract had an ID(50) (Inhibitory dose) of 13.1 (11.23-14.91) mg/kg and a maximal inhibition of 72 ± 4%. In the same model, Guttiferone A had an ID(50) of 4.54 (3.29-6.24) mg/kg and a maximal inhibition of 73 ± 5%. The methanolic seed extract and Guttiferone A were also active in pain models induced by formalin, capsaicin, glutamate and carrageenan. These data suggest that the antinociceptive effect of Guttiferone A partly depends on its interference with the synthesis or activity of the cytokine TNF-α, the keratinocyte-derived chemokine KC, and/or PGE(2). These data support, at least in part, the use of G. achachairu in folk medicine and suggest that this plant is an important source of compounds with a suitable profile for development as new and effective medicinal agents to treat pain processes.
在从巴西生物多样性中寻找新的有效的镇痛物质的过程中，本研究评估了 Garcinia achachairu Rusby（藤黄科）种子的甲醇提取物和一种纯化合物的化学组成和镇痛潜力。甲醇种子提取物直接通过柱色谱法进行纯化，并通过薄层色谱法监测纯化过程。通过比较常规光谱数据（IR、NMR-（1）H 和（13）C）与文献数据，将主要分离出的化合物鉴定为 Guttiferone A，这是首次从该植物中分离出来的。当在醋酸诱导的小鼠疼痛模型中进行评估时，甲醇种子提取物的 ID（50）（抑制剂量）为 13.1（11.23-14.91）mg/kg，最大抑制率为 72±4%。在相同的模型中，Guttiferone A 的 ID（50）为 4.54（3.29-6.24）mg/kg，最大抑制率为 73±5%。甲醇种子提取物和 Guttiferone A 也对福尔马林、辣椒素、谷氨酸和角叉菜胶诱导的疼痛模型有效。这些数据表明，Guttiferone A 的镇痛作用部分取决于其对细胞因子 TNF-α、角质形成细胞衍生趋化因子 KC 和/或 PGE（2）的合成或活性的干扰。这些数据至少部分支持了 G. achachairu 在民间医学中的应用，并表明该植物是具有适合开发为新的有效的治疗疼痛过程的药物的化合物的重要来源。
