Garcia Francisca Adilfa de Oliveira, Tanae Mirtes Midori, Torres Luce Maria Brandão, Lapa Antônio José, de Lima-Landman Maria Teresa Riggio, Souccar Caden
Department of Pharmacology, School of Medicine of the Federal University of São Paulo (UNIFESP), Rua 3 de Maio, 100, CEP: 04044-020 São Paulo, SP, Brazil.
Department of Pharmacology, School of Medicine of the Federal University of São Paulo (UNIFESP), Rua 3 de Maio, 100, CEP: 04044-020 São Paulo, SP, Brazil.
Phytomedicine. 2014 Jul-Aug;21(8-9):1021-5. doi: 10.1016/j.phymed.2014.04.018. Epub 2014 May 15.
Baccharis trimera (Less.) D.C. (Asteraceae) is a medicinal species native to South America and used in Brazilian folk medicine to treat gastrointestinal and liver diseases, kidney disorders and diabetes. The aqueous extract (AE) of the aerial parts of this species presented two mainly constituents: the ent-clerodane diterpene (Fig. 1) and the neo-clerodane diterpene (Fig. 2). The objective of this work was to study their activities on the blockade of Ca(2+)-induced contractions in KCL-depolarized rat portal vein preparations, and on the influx and mobilization of cytosolic calcium in rat cardiomyocytes by fluorescence measurements. The results showed that both the neo- and the ent-clerodane diterpenes reduced the maximal contractions induced by CaCl2, in KCl depolarized rat portal vein preparations, without modifying the EC50. The data on the concentration of cytosolic calcium ([Ca(2+)]c) showed that, while the neo-clerodane diterpene stimulates the mobilization of [Ca(2+)]c in rat cardiomyocytes, this effect was not observed with the ent-clerodane diterpene. On the other hand, the influx of calcium was not altered by the neo-clerodane diterpene, but was reduced in the presence of the ent-clerodane diterpene, indicating that this compound induces a blockade of the voltage-dependent calcium channels.
三裂叶包果菊(Baccharis trimera (Less.) D.C.,菊科)是一种原产于南美洲的药用植物,在巴西民间医学中用于治疗胃肠道和肝脏疾病、肾脏疾病及糖尿病。该物种地上部分的水提取物(AE)有两种主要成分:对映-克罗烷二萜(图1)和新克罗烷二萜(图2)。本研究旨在通过荧光测量研究它们对氯化钾去极化的大鼠门静脉制剂中钙诱导收缩的阻断作用,以及对大鼠心肌细胞胞质钙内流和动员的影响。结果表明,新克罗烷二萜和对映-克罗烷二萜均可降低氯化钾去极化的大鼠门静脉制剂中氯化钙诱导的最大收缩,且不改变半数有效浓度(EC50)。胞质钙浓度([Ca(2+)]c)的数据显示,新克罗烷二萜可刺激大鼠心肌细胞中[Ca(2+)]c的动员,而对映-克罗烷二萜未观察到这种作用。另一方面,新克罗烷二萜不改变钙内流,但在对映-克罗烷二萜存在时钙内流减少,表明该化合物可诱导电压依赖性钙通道的阻断。