番荔枝中类黄酮的含量及其抗增殖、降血糖、抗炎和自由基清除活性。
The flavonoid content and antiproliferative, hypoglycaemic, anti-inflammatory and free radical scavenging activities of Annona dioica St. Hill.
机构信息
Faculdade de Ciências Agrárias, Universidade Federal da Grande Dourados, Dourados, MS, Brazil.
出版信息
BMC Complement Altern Med. 2013 Jan 11;13:14. doi: 10.1186/1472-6882-13-14.
BACKGROUND
Annona dioica St. Hill (Annonacaeae) is a Brazilian plant used in folk medicine for the treatment of several types of rheumatisms and diarrhoea. The focus of this work was to evaluate the in vitro antiproliferative and antioxidant activity and the in vivo hypoglycaemic and anti-inflammatory activity of A. dioica and identify the principal constituents of this plant.
METHODS
The crude methanol extract (EAD) and hexane (HF), chloroform (CF), ethyl acetate (EAF) and hydromethanol fractions (HMF) were evaluated for free radical scavenging activity using the DPPH assay. The EAD and EAF were assayed for hypoglycaemic activity in rats. The EAD was tested in an antiproliferation assay and for anti-inflammatory effects in paw oedema, in addition to myeloperoxidase activity induced by carrageenan (Cg) in mice. The EAF was assayed using chromatographic methods.
RESULTS
The fractionation of the EAF through chromatographic methods identified derivatives of the flavonoids quercetin and kaempferol. Among all the tested fractions, the ethyl acetate and hydromethanol fractions were the most potent, exhibiting an IC50 of 8.53 and 10.57 μg/mL, respectively, which is comparable to that of the commercial antioxidant butylated hydroxytoluene (BHT). The oral administration of the EAD (100 mg/kg) and EAF (15 mg/kg) inhibited the increase of glucose levels, resulting in a hypoglycaemic effect. The EAD (30 to 300 mg/kg) exhibited an anti-oedematogenic effect in Cg-induced paw oedema in a time- and dose-dependent manner. The results showed a reduction of MPO activity by A. dioica 6 h after the induction of paw oedema at all doses tested with maximal inhibition at 300 mg/kg.
CONCLUSIONS
Our results reveal for the first time that compounds contained in the A. dioica leaves exert anti-inflammatory, hypoglycaemic, antiproliferative, and antioxidant effects. The antioxidant activity may be associated with the presence of flavonoids.
背景
番荔枝（番荔枝科）是一种巴西植物，在民间医学中用于治疗多种类型的风湿病和腹泻。这项工作的重点是评估番荔枝的体外增殖抑制和抗氧化活性以及体内降血糖和抗炎活性，并鉴定该植物的主要成分。
方法
用 DPPH 法评估粗甲醇提取物（EAD）和正己烷（HF）、氯仿（CF）、乙酸乙酯（EAF）和水-甲醇馏分（HMF）的自由基清除活性。在大鼠中评估 EAD 和 EAF 的降血糖活性。在爪水肿、角叉菜胶（Cg）诱导的小鼠髓过氧化物酶活性的抗炎作用以及增殖抑制试验中测试 EAD。用色谱法测试 EAF。
结果
通过色谱法对 EAF 的分离鉴定出黄酮类化合物槲皮素和山奈酚的衍生物。在所有测试的馏分中，乙酸乙酯和水-甲醇馏分的活性最强，IC50 分别为 8.53 和 10.57μg/mL，与商业抗氧化剂丁基羟基甲苯（BHT）相当。EAD（100mg/kg）和 EAF（15mg/kg）的口服给药抑制了葡萄糖水平的升高，导致降血糖作用。EAD（30 至 300mg/kg）在 Cg 诱导的爪水肿中表现出时间和剂量依赖性的抗水肿作用。结果显示，在所有测试剂量下，EAD 可降低诱导爪水肿后 6 小时的 MPO 活性，最大抑制作用发生在 300mg/kg 时。
结论
我们的研究结果首次表明，番荔枝叶中的化合物具有抗炎、降血糖、增殖抑制和抗氧化作用。抗氧化活性可能与类黄酮的存在有关。
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