Abstract：
BACKGROUND: 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.
OBJECTIVE: 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.
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 +ATP channels, α2-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+ATP channels and α2-adrenoreceptors. 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).
CONCLUSIONS: 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.
OBJECTIVE: 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.
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 +ATP channels, α2-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+ATP channels and α2-adrenoreceptors. 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).
CONCLUSIONS: 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.
摘要：
背景：Fridericiachica（Bonpl。)L.G.Lohmann(Bignoniaceae)，是巴西本地人的登山者，在所有巴西生物群落中发现。它在巴西主要被称为“carajiru”，从叶子制成的家用药物已被用于治疗包括胃溃疡和其他胃肠道疾病在内的疾病。
目的：本研究的目的是使用体内啮齿动物模型研究胡志明市叶乙醇提取物（HEFc）预防和治疗性抗溃疡的胃肠道功效以及作用机制。
方法：F.chica被收集在Juna市，马托格罗索,并将其叶子用于通过浸渍技术（70％的乙醇以1：10的比例，w/v)得到HEFc。HEFc的色谱分析通过高效液相色谱-光电二极管阵列-电喷雾电离-质谱(HPLC-PDA-ESI-MS)-LCQFleet™系统进行。为了确定HEFc（1、5和20mg/kg，p.o.),在各种由酸化乙醇引起的胃溃疡动物模型中评估胃保护活性，水约束应力，吲哚美辛,（急性），和酸性乙酸（慢性）。此外,在小鼠中评估HEFC的促动力特性。通过组织病理学分析和胃分泌物的测定（体积，自由和总酸度)，胃屏障粘液，激活PG，NO,K+ATP通道,α2-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，IL1-β,和IL-10）水平。
结果：分析了HEFc的化学成分，并分析了芹菜素，scutellarin,并确认了carajurone的身份.HEFc（1、5和20mg/kg）显示出对HCl/EtOH诱导的急性溃疡的作用，溃疡面积减少64.41％（p<0.001），54.23%(p<0.01)，38.71%(p<0.01)，分别。在吲哚美辛实验中,测试的剂量没有变化，而在水浸束缚应激性溃疡中，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在1和20mg/kg的剂量下增加了粘液产生，分别为28.14％（p<0.05）和38.36％（p<0.01），分别。在幽门结扎诱导的胃溃疡模型中，HEFc使所有剂量的总酸度降低了54.23%，65.08%,在1mg/kg（p<0.05）的剂量下，胃分泌量为38.47％（p<0.05），在5mg/kg的剂量下，游离酸度增加了11.86％（p<0.05）。EHFc（1mg/kg）的给药可能通过刺激前列腺素的释放并激活KATP通道和α2-肾上腺素受体而显示出胃保护作用。此外，HEFc的胃保护作用涉及CAT和GSH活性的增加，MPO活性和MDA水平降低。在慢性胃溃疡模型中,在所有剂量下，HEFc（1、5和20mg/kg）显着降低溃疡面积（p<0.001）71.37％，91.00%,和93.46%，分别。在组织学分析中，HEFc通过刺激肉芽组织的形成并因此促进上皮化促进胃部病变的愈合。另一方面,关于HEFc对胃排空和肠转运的影响，据观察，提取物没有改变胃排空，但在剂量为1mg/kg时肠道转运增加（p<0.01）。
结论：这些结果证实了Fridericiachica叶治疗胃溃疡的优势，这是众所周知的。发现HEFc通过多靶点途径具有抗溃疡特性，这可能与胃防御机制的增加和防御因子的减少有关。HEFc可以被视为一种潜在的新的抗溃疡草药，因为它的抗溃疡特性，这可能归因于类黄酮的混合物，芹菜素,Scutellarin和carajurone.
目的：本研究的目的是使用体内啮齿动物模型研究胡志明市叶乙醇提取物（HEFc）预防和治疗性抗溃疡的胃肠道功效以及作用机制。
方法：F.chica被收集在Juna市，马托格罗索,并将其叶子用于通过浸渍技术（70％的乙醇以1：10的比例，w/v)得到HEFc。HEFc的色谱分析通过高效液相色谱-光电二极管阵列-电喷雾电离-质谱(HPLC-PDA-ESI-MS)-LCQFleet™系统进行。为了确定HEFc（1、5和20mg/kg，p.o.),在各种由酸化乙醇引起的胃溃疡动物模型中评估胃保护活性，水约束应力，吲哚美辛,（急性），和酸性乙酸（慢性）。此外,在小鼠中评估HEFC的促动力特性。通过组织病理学分析和胃分泌物的测定（体积，自由和总酸度)，胃屏障粘液，激活PG，NO,K+ATP通道,α2-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，IL1-β,和IL-10）水平。
结果：分析了HEFc的化学成分，并分析了芹菜素，scutellarin,并确认了carajurone的身份.HEFc（1、5和20mg/kg）显示出对HCl/EtOH诱导的急性溃疡的作用，溃疡面积减少64.41％（p<0.001），54.23%(p<0.01)，38.71%(p<0.01)，分别。在吲哚美辛实验中,测试的剂量没有变化，而在水浸束缚应激性溃疡中，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在1和20mg/kg的剂量下增加了粘液产生，分别为28.14％（p<0.05）和38.36％（p<0.01），分别。在幽门结扎诱导的胃溃疡模型中，HEFc使所有剂量的总酸度降低了54.23%，65.08%,在1mg/kg（p<0.05）的剂量下，胃分泌量为38.47％（p<0.05），在5mg/kg的剂量下，游离酸度增加了11.86％（p<0.05）。EHFc（1mg/kg）的给药可能通过刺激前列腺素的释放并激活KATP通道和α2-肾上腺素受体而显示出胃保护作用。此外，HEFc的胃保护作用涉及CAT和GSH活性的增加，MPO活性和MDA水平降低。在慢性胃溃疡模型中,在所有剂量下，HEFc（1、5和20mg/kg）显着降低溃疡面积（p<0.001）71.37％，91.00%,和93.46%，分别。在组织学分析中，HEFc通过刺激肉芽组织的形成并因此促进上皮化促进胃部病变的愈合。另一方面,关于HEFc对胃排空和肠转运的影响，据观察，提取物没有改变胃排空，但在剂量为1mg/kg时肠道转运增加（p<0.01）。
结论：这些结果证实了Fridericiachica叶治疗胃溃疡的优势，这是众所周知的。发现HEFc通过多靶点途径具有抗溃疡特性，这可能与胃防御机制的增加和防御因子的减少有关。HEFc可以被视为一种潜在的新的抗溃疡草药，因为它的抗溃疡特性，这可能归因于类黄酮的混合物，芹菜素,Scutellarin和carajurone.
