Moshi Mainen J, Nondo Ramadhani S O, Haule Emmanuel E, Mahunnah Rogasian L A, Kidukuli Abdul W
Department of Biological and Preclinical Studies, Muhimbili University of Health and Allied Sciences, P,O, Box 65001, Dar es Salaam, Tanzania.
BMC Res Notes. 2014 Feb 19;7:91. doi: 10.1186/1756-0500-7-91.
A decoction of Crassocephallum vitellinum (Benth.) S. Moore (Asteraceae) is used in Kagera Region to treat peptic ulcers. This study seeks to evaluate an aqueous ethanol extract of aerial parts of the plant for safety and efficacy.
An 80% ethanolic extract of C. vitellinum at doses of 100, 200, 400 and 800 mg/kg body wt was evaluated for ability to protect Sprague Dawley rats from acidified ethanol gastric ulceration in comparison with 40 mg/kg body wt pantoprazole. The extract and its dichloromethane, ethyl acetate, and aqueous fractions were also evaluated for acute toxicity in mice, brine shrimp toxicity, and antibacterial activity against four Gram negative bacteria; Escherichia coli (ATCC 25922), Salmonella typhi (NCTC 8385), Vibrio cholera (clinical isolate), and Streptococcus faecalis (clinical isolate). The groups of phytochemicals present in the extract were also determined.
The ethanolic extract of C. vitellinum dose-dependently protected rat gastric mucosa against ethanol/HCl insult to a maximum of 88.3% at 800 mg/kg body wt, affording the same level of protection as by 40 mg/kg body wt pantoprazole. The extract also exhibited weak antibacterial activity against S. typhi and E. coli, while its ethyl acetate, dichloromethane and aqueous fractions showed weak activity against K. pneumonia, S.typhi, E. coli and V. cholera. The extract was non-toxic to mice up to 5000 mg/kg body wt, and the total extract (LC50 = 37.49 μg/ml) and the aqueous (LC50 = 87.92 μg/ml), ethyl acetate (LC50 = 119.45 μg/ml) and dichloromethane fractions (88.79 μg/ml) showed low toxicity against brine shrimps. Phytochemical screening showed that the extract contains tannins, saponins, flavonoids, and terpenoids.
The results support the claims by traditional healers that a decoction of C.vitellinum has antiulcer activity. The mechanism of cytoprotection is yet to be determined but the phenolic compounds present in the extract may contribute to its protective actions. However, the dose conferring gastro-protection in the rat is too big to be translated to clinical application; thus bioassay guided fractionation to identify active compound/s or fractions is needed, and use of more peptic ulcer models to determine the mechanism for the protective action.
在卡盖拉地区，人们使用粘冠草（菊科）煎剂治疗消化性溃疡。本研究旨在评估该植物地上部分的水乙醇提取物的安全性和有效性。
将粘冠草80%乙醇提取物以100、200、400和800mg/kg体重的剂量给药，与40mg/kg体重的泮托拉唑相比，评估其保护斯普拉格-道利大鼠免受酸化乙醇引起的胃溃疡的能力。还对该提取物及其二氯甲烷、乙酸乙酯和水相部分进行了小鼠急性毒性、卤虫毒性以及对四种革兰氏阴性菌的抗菌活性评估；这四种菌分别为大肠杆菌（ATCC 25922）、伤寒沙门氏菌（NCTC 8385）、霍乱弧菌（临床分离株）和粪肠球菌（临床分离株）。同时还测定了提取物中存在的植物化学成分组。
粘冠草乙醇提取物对大鼠胃黏膜具有剂量依赖性的保护作用，可抵御乙醇/盐酸损伤，在800mg/kg体重时保护率最高可达88.3%，与40mg/kg体重的泮托拉唑提供的保护水平相同。该提取物对伤寒沙门氏菌和大肠杆菌也表现出较弱的抗菌活性，而其乙酸乙酯、二氯甲烷和水相部分对肺炎克雷伯菌、伤寒沙门氏菌、大肠杆菌和霍乱弧菌表现出较弱活性。该提取物在高达5000mg/kg体重时对小鼠无毒，总提取物（LC50 = 37.49μg/ml）及其水相（LC50 = 87.92μg/ml）、乙酸乙酯相（LC50 = 119.45μg/ml）和二氯甲烷相（88.79μg/ml）对卤虫表现出低毒性。植物化学筛选表明，该提取物含有单宁、皂苷、黄酮类化合物和萜类化合物。
结果支持传统治疗师关于粘冠草煎剂具有抗溃疡活性的说法。细胞保护机制尚待确定，但提取物中存在的酚类化合物可能有助于其保护作用。然而，在大鼠中赋予胃保护作用的剂量过大，无法转化为临床应用；因此，需要进行生物测定指导的分级分离以鉴定活性化合物或组分，并使用更多消化性溃疡模型来确定保护作用的机制。
