Vela S M, Souccar C, Lima-Landman M T, Lapa A J
Department of Pharmacology, Escola Paulista de Medicina, Universidade Federal de São Paulo, Brazil.
Planta Med. 1997 Feb;63(1):36-9. doi: 10.1055/s-2006-957599.
Stachytarpheta cayennensis Schauer (Verbenaceae) is used in folk medicine to treat gastric and intestinal disturbances. The freeze-dried aqueous extract of the whole plant tested to rodents up to the dose of 2 g kg-1, p.o., did not produce signs of toxicity. The extract (0.5-2 g kg-1, p.o.) increased the intestinal motility and protected mice against ulcers induced by restraintin-cold, ethanol or indomethacin. Injected into the duodenal lumen the extract inhibited the basal acid secretion as well as that induced by histamine and bethanecol in pylorus-ligated mice. Partition of the aqueous extract in organic solvents yielded semipurified fractions whose antiacid activity guided further chemical purification. All the fractions were chromatographically characterized, the main substances in the active extract being flavonoids and amines; some substances were revealed only under UV light. The most purified active fraction obtained presented a specific activity 5-10 times higher than that detected in the original extract. Data from pharmacological studies indicate that the antiulcer activity of S. cayennensis is related to a specific inhibition of gastric acid secretion. Cholinergic and histaminergic stimulation of acid secretion were similarly reduced by the extracts suggesting inhibition of common steps in both pathways, possibly at the level of histamine release/H2 receptor interaction, or at the proton pump. Whatever the mechanisms involved, the present data confirm the plant effectiveness as antiacid/antiulcer and laxative.
卡宴假马鞭（Stachytarpheta cayennensis Schauer，马鞭草科）在民间医学中用于治疗胃肠道紊乱。对啮齿动物口服高达2 g kg-1剂量的全株冻干水提取物，未产生毒性迹象。该提取物（0.5 - 2 g kg-1，口服）可增强肠道蠕动，并保护小鼠免受冷束缚、乙醇或吲哚美辛诱导的溃疡。将提取物注入十二指肠腔可抑制幽门结扎小鼠的基础胃酸分泌以及组胺和氨甲酰甲胆碱诱导的胃酸分泌。水提取物在有机溶剂中的分配得到了半纯化级分，其抗酸活性指导了进一步的化学纯化。所有级分均通过色谱法进行了表征，活性提取物中的主要物质为黄酮类化合物和胺类；一些物质仅在紫外光下可见。获得的最纯活性级分的比活性比原始提取物中检测到的高5 - 10倍。药理学研究数据表明，卡宴假马鞭的抗溃疡活性与胃酸分泌的特异性抑制有关。提取物同样降低了胆碱能和组胺能对胃酸分泌的刺激，表明抑制了两条途径中的共同步骤，可能是在组胺释放/H2受体相互作用水平或质子泵水平。无论涉及何种机制，目前的数据证实了该植物作为抗酸/抗溃疡和泻药的有效性。
