评价 Fridericia chica(Bonpl.)L.G. Lohmann 叶的水醇提取物的胃保护和溃疡愈合特性。
Evaluation of the gastroprotective and ulcer healing properties by Fridericia chica (Bonpl.) L.G. Lohmann hydroethanolic extract of leaves.
机构信息
Programa de Pós-graduação em Ciências da Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.
Programa de Pós-graduação em Ciências da Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil; Área de Histologia e Biologia Celular, Departamento de Ciências Básicas em Saúde, Faculdade de Medicina, Universidade Federal de Mato Grosso (UFMT), Cuiabá, Brazil.
出版信息
J Ethnopharmacol. 2023 Jun 12;309:116338. doi: 10.1016/j.jep.2023.116338. Epub 2023 Mar 2.
ETHNOPHARMACOLOGICAL RELEVANCE
Fridericia chica (Bonpl.) L.G. Lohmann (Bignoniaceae), is a climber native to Brazil, found in all Brazilian biomes. It is mostly known in Brazil as "carajiru," and home medicines made from the leaves have been used to cure disorders including stomach ulcers and other gastrointestinal disorders.
AIM OF THE STUDY
The objective of the study was to investigate the F. chica hydroethanolic extract of leaves (HEFc) preventative and curative antiulcer gastrointestinal efficacy as well as the mechanisms of action using in vivo rodent models.
MATERIALS AND METHODS
F. chica was collected in the municipality of Juína, Mato Grosso, and its leaves were used to prepare the extract by maceration technique (70% hydroethanol in the 1:10 ratio, w/v) to obtain the HEFc. The chromatographic analysis of HEFc was carried out by High Performance Liquid Chromatography-Photo Diode Array-Electrospray Ionization-Mass Spectrometry (HPLC-PDA-ESI-MS)- LCQ Fleet™ system. To determine the potential antiulcer potential of HEFc (1, 5 and 20 mg/kg, p.o.), the gastroprotective activity was assessed in various animal models of stomach ulcers caused by acidified ethanol, water constraint stress, indomethacin, (acute), and acid acetic (chronic). Additionally, the prokinetic properties of the HEFC were assessed in mice. The gastroprotective underlying mechanisms were evaluated by the histopathological analysis and determination of gastric secretion (volume, free and total acidity), gastric barrier mucus, activation of PGs, NO, K channels, α-adrenoceptor, antioxidant activity (GSH, MPO and MDA), NO and mucosal cytokines (TNF-α, IL-1β, and IL-10) levels.
RESULTS
The chemical composition of HEFc was analyzed and apigenin, scutellarin, and carajurone were identified. HEFc (1, 5 and 20 mg/kg) showed effect against acute ulcers induced by HCl/EtOH with a reduction in the ulcerated area of 64.41% (p < 0.001), 54.23% (p < 0.01), 38.71% (p < 0.01), respectively. In the indomethacin experiment, there was no change in the doses tested, whereas in the water immersion restraint stress ulcer there was a reduction of lesions at doses of 1, 5, and 20 mg/kg by 80.34% (p < 0.001), 68.46% (p < 0.01) and 52.04% (p < 0.01). HEFc increased the mucus production at doses of 1 and 20 mg/kg in 28.14% (p < 0.05) and 38.36% (p < 0.01), respectively. In the pyloric ligation-induced model of gastric ulceration, the HEFc decreased the total acidity in all doses by 54.23%, 65.08%, and 44.40% (p < 0.05) and gastric secretory volume in 38.47% at dose of 1 mg/kg (p < 0,05) and increased the free acidity at the dose of 5 mg/kg by 11.86% (p < 0.05). The administration of EHFc (1 mg/kg) showed a gastroprotective effect possibly by stimulating the release of prostaglandins and activating K channels and αadrenoreceptors. Also, the gastroprotective effect of HEFc involved an increase in CAT and GSH activities, and a reduction in MPO activity and MDA levels. In the chronic gastric ulcer model, the HEFc (1, 5 and 20 mg/kg) decreased the ulcerated area significantly (p < 0.001) at all doses by 71.37%, 91.00%, and 93.46%, respectively. In the histological analysis, HEFc promoted the healing of gastric lesions by stimulating the formation of granulation tissue and consequently epithelialization. On the other hand, regarding the effect of HEFc on gastric emptying and intestinal transit, it was observed that the extract did not alter gastric emptying, but there was an increase in intestinal transit at the dose of 1 mg/kg (p < 0.01).
CONCLUSION
These outcomes confirmed the advantages of Fridericia chica leaves for the treatment of stomach ulcers, which are well-known. HEFc was discovered to have antiulcer characteristics through multitarget pathways, which might be related to an increase in stomach defense mechanisms and a decrease in defensive factor. HEFc can be regarded as a potential new antiulcer herbal remedy because of its antiulcer properties, which may be attributed to the mixture of flavonoids, apigenin, scutellarin and carajurone.
民族药理学相关性
Fridericia chica(Bonpl.)L.G. Lohmann(紫葳科),是一种原产于巴西的攀援植物,分布于巴西所有生物群落。在巴西,它主要被称为“carajiru”,而由其叶子制成的家庭药物被用于治疗包括胃溃疡和其他胃肠道疾病在内的多种疾病。
研究目的
本研究的目的是调查 Fridericia chica 水醇提取物(HEFc)对预防和治疗胃溃疡的胃肠道疗效以及使用体内啮齿动物模型的作用机制。
材料和方法
Fridericia chica 在马托格罗索州的 Juína 市采集,使用浸渍技术(1:10 的 70%水乙醇,w/v)从其叶子中制备提取物,以获得 HEFc。通过高效液相色谱-光电二极管阵列-电喷雾电离-质谱联用(HPLC-PDA-ESI-MS)-LCQ Fleet™系统进行 HEFc 的色谱分析。为了确定 HEFc(1、5 和 20mg/kg,po)的潜在抗溃疡潜力,在酸化乙醇、水约束应激、吲哚美辛(急性)和乙酸酸化(慢性)引起的各种动物胃溃疡模型中评估了 HEFc 的胃保护活性。此外,还评估了 HEFc 的促动力特性在小鼠中。通过组织病理学分析和胃分泌(体积、游离和总酸度)、胃屏障粘液、PGs、NO、K 通道、α-肾上腺素受体、抗氧化活性(GSH、MPO 和 MDA)、NO 和粘膜细胞因子(TNF-α、IL-1β 和 IL-10)水平评估了 HEFc 的潜在抗溃疡作用机制。
结果
分析了 HEFc 的化学成分,鉴定出了芹菜素、野黄芩苷和 carajurone。HEFc(1、5 和 20mg/kg)对盐酸/乙醇引起的急性溃疡具有作用,溃疡面积分别减少了 64.41%(p<0.001)、54.23%(p<0.01)和 38.71%(p<0.01)。在吲哚美辛实验中,未改变测试剂量,而在水浸应激溃疡中,1、5 和 20mg/kg 剂量的病变减少了 80.34%(p<0.001)、68.46%(p<0.01)和 52.04%(p<0.01)。HEFc 增加了 1 和 20mg/kg 剂量下的粘液产生,分别增加了 28.14%(p<0.05)和 38.36%(p<0.01)。在幽门结扎诱导的胃溃疡模型中,HEFc 在所有剂量下均降低了总酸度 54.23%、65.08%和 44.40%(p<0.05)和胃分泌体积 38.47%(p<0.05)在 1mg/kg 剂量下,并且在 5mg/kg 剂量下增加了游离酸度 11.86%(p<0.05)。EHFc(1mg/kg)的给药表现出胃保护作用,可能是通过刺激前列腺素的释放和激活 K 通道和α肾上腺素受体来实现的。此外,HEFc 的胃保护作用涉及 CAT 和 GSH 活性的增加,以及 MPO 活性和 MDA 水平的降低。在慢性胃溃疡模型中,HEFc(1、5 和 20mg/kg)在所有剂量下均显著降低溃疡面积(p<0.001),分别为 71.37%、91.00%和 93.46%。在组织病理学分析中,HEFc 通过刺激肉芽组织形成和随后的上皮化来促进胃损伤的愈合。另一方面,关于 HEFc 对胃排空和肠转运的影响,观察到提取物不改变胃排空,但在 1mg/kg 剂量下增加了肠转运(p<0.01)。
结论
这些结果证实了 Fridericia chica 叶子在治疗胃溃疡方面的优势,这是众所周知的。通过多靶点途径发现 HEFc 具有抗溃疡特性,这可能与增加胃防御机制和降低防御因子有关。由于其抗溃疡特性,HEFc 可被视为一种潜在的新型抗溃疡草药,这可能归因于类黄酮、芹菜素、野黄芩苷和 carajurone 的混合物。