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Flavonoids from Cirsium japonicum var. maackii pappus as inhibitors of aldose reductase and their simultaneous determination

机译:来自柳叶柳的黄酮类化合物。 Maackii pappus作为醛糖还原酶的抑制剂及其同时测定

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摘要

Aldose reductase is an enzyme in the polyol pathway which is associated in the progression of diabetic complications. In this study, we evaluated the inhibitory activity of Cirsium japonicum var. maackii pappus (CJP) against rat lens aldose reductase (RLAR). The ethanolic extract, fractions and isolated flavonoids were subjected to an RLAR assay. Isolation of chloroform (CHCl3) and ethyl acetate (EtOAc) fractions led to the identification of four flavonoids: hispidulin (1), cirsimaritin (2), apigenin (3), and cirsimarin (4). The RLAR assay results suggested that the EtOAc fraction and flavonoids 1 and 3 promoted better AR inhibition than did TMG (control). The half-maximal inhibitory concentration (IC50) of compounds 1 and 3 was 0.77 and 3.19 mu M, respectively. A simultaneous determination of flavonoid content using HPLC-UV indicated that CJP contained large amounts of compounds 2 and 3 (1.65 and 1.84 mg/g, respectively). Flavonoids from Cirsium species have been widely reported to show various pharmacological activities. This study indicated that CJP has the potential to prevent diabetic complications and was a potential source of flavonoids.
机译:醛糖还原酶是多元醇途径中的酶,其在糖尿病并发症的进展中有关。在这项研究中,我们评估了杂志的抑制活性。对对大鼠镜片醛糖还原酶(RLAR)的Maackii pappus(cjp)。对乙醇提取物,级分和分离的黄酮进行RLAR测定。将氯仿(CHCl3)和乙酸乙酯(EtOAc)级分的分离导致鉴定四种类黄酮:Hispidulin(1),肝素(3),Apigenin(3)和Cirsimarin(4)。 RLAR测定结果表明EtOAc级分和黄酮类化合物1和3促进了比TMG(对照)更好的AR抑制。化合物1和3的半最大抑制浓度(IC 50)分别为0.77和3.19μm。使用HPLC-UV同时测定类黄酮含量,表明CJP含有大量的化合物2和3(分别为1.65和1.84mg / g)。循环物种中的黄酮类药物已被广泛据报道显示各种药理活动。本研究表明,CJP有可能预防糖尿病并发症,并且是黄酮类化合物的潜在来源。

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