Abd-Alla Howaida I, Shalaby Nagwa M M, Hamed Manal A, El-Rigal Nagy Saba, Al-Ghamdi Samira N, Bouajila Jalloul
Department of Natural Compounds Chemistry, National Research Centre, Dokki, 12622, Giza, Egypt.
Department of Therapeutic Chemistry, National Research Centre, Dokki, 12622, Giza, Egypt.
Arch Pharm Res. 2016 Jan;39(1):10-20. doi: 10.1007/s12272-014-0544-9. Epub 2015 Jan 8.
Three sesquiterpene lactones [two germacranolides (micranthin and sintenin) and one guaianolide (4β,10α-dihydroxy-5β,7β,8βH-guaia-1,11(13)dien-12,8α-olide)] and four derivatives of 3-methoxy flavones (santin, quercetagetin-3,6,3'-trimethyl ether, quercetagetin-3,6-dimethyl ether, and 5,7 dihydroxy 3,3',4'-trimethoxy flavone) were isolated from the ethyl acetate extract (EAE) of the aerial parts of Achillea biebersteinii Afan. (Asteraceae). Evaluation of protective and therapeutic effects of EAE against ethanol-induced gastric ulcer in rats was carried. Antiulcer activity evaluation was done through measuring ulcer indices, stomach acidity, gastric volume and lesion counts. Oxidative stress markers; malondialdehyde, glutathione and superoxide dismutase were also estimated. The work was extended to determine the histopathological assessment of the stomach. Gastric ulcer exhibited a significant elevation of the ulcer index and oxidative stress markers. The extract attenuated these increments and recorded protective and therapeutic effects against gastric ulcer. Hyperglycaemia increases the mucosal susceptibility to ulcerogenic stimuli and predisposes gastric ulceration. In vitro α-amylase inhibitory assay was applied to evaluate the post prandial antihyperglycaemia activity. The result showing that the EAE has the ability to reduce starch-induced postprandial glycaemic excursions by virtue of potent intestinal α-amylase inhibitory activity. These findings demonstrated the remarkable potential of A. biebersteinii as valuable source of antiulcer agent with post prandial hyperglycaemia lowering effect.
从新疆蓍（菊科）地上部分的乙酸乙酯提取物（EAE）中分离出三种倍半萜内酯[两种吉马烷型内酯（微兰素和辛特宁）和一种愈创木烷型内酯（4β,10α-二羟基-5β,7β,8βH-愈创木-1,11(13)二烯-12,8α-内酯）]以及四种3-甲氧基黄酮衍生物（桑亭、槲皮万寿菊素-3,6,3'-三甲醚、槲皮万寿菊素-3,6-二甲醚和5,7-二羟基-3,3',4'-三甲氧基黄酮）。对EAE对大鼠乙醇诱导的胃溃疡的保护和治疗作用进行了评估。通过测量溃疡指数、胃酸度、胃容积和损伤计数进行抗溃疡活性评估。还评估了氧化应激标志物丙二醛、谷胱甘肽和超氧化物歧化酶。该研究进一步扩展至对胃进行组织病理学评估。胃溃疡表现出溃疡指数和氧化应激标志物显著升高。该提取物减轻了这些升高，并对胃溃疡具有保护和治疗作用。高血糖会增加黏膜对致溃疡刺激的易感性，并易引发胃溃疡。应用体外α-淀粉酶抑制试验评估餐后抗高血糖活性。结果表明，EAE凭借强大的肠道α-淀粉酶抑制活性，有能力降低淀粉诱导的餐后血糖波动。这些发现证明了新疆蓍作为具有餐后降血糖作用的抗溃疡剂宝贵来源的巨大潜力。
