Batista Leônia Maria, de Almeida Ana Beatriz Albino, de Pietro Magri Luciana, Toma Walber, Calvo Tamara Regina, Vilegas Wagner, Souza Brito Alba Regina Monteiro
Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal da Paraíba (UFPB), João Pessoa, PB, Brazil.
Biol Pharm Bull. 2004 Mar;27(3):328-32. doi: 10.1248/bpb.27.328.
Syngonanthus arthrotrichus SILVEIRA, popularly known as "sempre-vivas mini-saia," is found in mountains of the Espinhaço range in the Brazilian states of Bahia and Minas Gerais. Extracts of this species contain several constituents, including flavonoids which may have antiulcerogenic activity. An ethanolic extract (EEOH), and flavonoid-rich (FRF) and flavonoid-deficient (FDF) fractions obtained from the scapes of S. arthrotrichus were investigated for their ability to prevent ulceration of the gastric mucosa in mice and rats. In the ethanol/HCl-induced ulcer model, lansoprazole (30 mg/kg), EEOH (50, 100, 250 mg/kg) given orally protected the gastric mucosal against injury in mice by 79%, 78%, 73%, and 64% respectively. In the ethanol-induced gastric ulcer model in rats, the lansoprazole (30 mg/kg), FRF and FDF (100 mg/kg) significantly protected the gastric mucosal of rats by 65%, 38% and 25% respectively when compared with the negative control group. In indomethacin/bethanechol-induced gastric ulcers, cimetidine (100 mg/kg) and the EEOH (100, 250 mg/kg) inhibited gastric ulcer formation by 73%, 55% and 32% respectively. In this exactly model other treatments as cimetidine, FRF and FDF (100 mg/kg) each caused 54%, 36% and 45% inhibition, respectively. In the stress-induced gastric ulcer model, cimetidine (100 mg/kg) and the EEOH (50, 100, 250 mg/kg), inhibited gastric ulcer formation by 63%, 73%, 68% and 69% respectively. In the same model, cimetidine, FRF and FDF (100 mg/kg) significantly protected the gastric mucosal of the mice by 60%, 51% and 47% when compared to the control group. In pylorus-ligated mice, cimetidine (positive control) and FRF significantly decreased gastric acid secretion, increased gastric pH and reduced the acid output when compared to the negative control. FDF had no significant effect on these parameters. The protection provided by FRF probably involved an antisecretory mechanism mediated by flavonoids which were absent in FDF. The amount of adherent mucous in the stomach contents was also evaluated with the treatments carbenoxolone (200 mg/kg), FRF and FDF (100 mg/kg) treatment. Each treatments significantly increased the amount of adherent mucous in the gastric juice (8.67+/-1.73, 3.35+/-1.59, 2.1+/-0.41 mg/g of wet tissue, respectively) compared to the control group, indicating a cytoprotective action on the gastric mucosa. Treatment with FRF plus indomethacin and FDF plus indomethacin reduced the prostaglandin biosyntesis (13.6+/-6.5, 27+/-5.5 pg/well) by the mucosa, indicating that the cytoprotective action on the gastric mucosa was not related to the level of prostaglandins. Only FDF (38+/-17 pg/well) maintained the level of prostaglandins and guaranteed the integrity of the mucosa. The results indicate that the EEOH, FRF and FDF have antisecretory and cytoprotective actions, that may be related to the presence of luteoline in the extract and active fractions.
节毛合柱花(Syngonanthus arthrotrichus SILVEIRA),俗称“迷你裙永生花”,生长在巴西巴伊亚州和米纳斯吉拉斯州的埃斯皮尼亚ço山脉。该物种的提取物含有多种成分,包括可能具有抗溃疡活性的黄酮类化合物。研究了节毛合柱花茎的乙醇提取物(EEOH)、富含黄酮类化合物的部分(FRF)和缺乏黄酮类化合物的部分(FDF)预防小鼠和大鼠胃黏膜溃疡的能力。在乙醇/盐酸诱导的溃疡模型中,口服兰索拉唑(30 mg/kg)、EEOH(50、100、250 mg/kg)分别使小鼠胃黏膜免受损伤的比例为79%、78%、73%和64%。在大鼠乙醇诱导的胃溃疡模型中,与阴性对照组相比,兰索拉唑(30 mg/kg)、FRF和FDF(100 mg/kg)分别使大鼠胃黏膜得到显著保护,保护比例分别为65%、38%和25%。在吲哚美辛/氨甲酰甲胆碱诱导的胃溃疡中,西咪替丁(100 mg/kg)和EEOH(100、250 mg/kg)分别抑制胃溃疡形成的比例为73%、55%和32%。在该模型中,其他治疗方法如西咪替丁、FRF和FDF(100 mg/kg)分别导致54%、36%和45%的抑制率。在应激诱导的胃溃疡模型中,西咪替丁(100 mg/kg)和EEOH(50、100、250 mg/kg)分别抑制胃溃疡形成的比例为63%、73%、68%和69%。在同一模型中,与对照组相比,西咪替丁、FRF和FDF(100 mg/kg)分别使小鼠胃黏膜得到显著保护,保护比例为60%、51%和47%。在幽门结扎的小鼠中,与阴性对照组相比,西咪替丁(阳性对照)和FRF显著降低胃酸分泌,提高胃pH值并减少酸输出。FDF对这些参数没有显著影响。FRF提供的保护可能涉及黄酮类化合物介导的抗分泌机制,而FDF中不存在这种机制。还使用甘珀酸(200 mg/kg)、FRF和FDF(100 mg/kg)处理评估了胃内容物中黏附黏液的量。与对照组相比,每种处理均显著增加了胃液中黏附黏液的量(分别为8.67±1.73、3.35±1.59、2.1±0.41 mg/g湿组织),表明对胃黏膜有细胞保护作用。FRF加吲哚美辛和FDF加吲哚美辛处理降低了黏膜中前列腺素的生物合成(13.6±6.5、27±5.5 pg/孔),表明对胃黏膜的细胞保护作用与前列腺素水平无关。只有FDF(38±17 pg/孔)维持了前列腺素水平并保证了黏膜的完整性。结果表明,EEOH、FRF和FDF具有抗分泌和细胞保护作用,这可能与提取物和活性部分中木犀草素的存在有关。