一些黄酮及其衍生物的氧钒配合物之合成及生物活性
Synthesis of vanadyl complexes with flavonoids and derivatives and their biological activities
钒化合物具有抗糖尿病和癌症预防等多种药理活性,具有很高的应用前景。为克服钒化合物潜在的金属毒性,途径之一是提高配体和配合物的抗氧化活性。本文合成了一些氧钒-黄酮及其衍生物配合物,比较了他们的抗氧化能力和在糖尿病大鼠模型上的降糖作用效果。结果发现,槲皮素、槲皮素5'-磺酸、杨梅素和山奈酚以羰基和3-羟基与氧钒离子形成配合物,而柚皮素和橙皮素则难形成明确配合物。氧钒-黄酮配合物的抗氧化活性优于传统曲酸配体化合物。其中,槲皮素、杨梅素和山奈酚氧钒配合物具有良好的降糖效果,而槲皮素5'-磺酸配合物虽然其水溶性较好,但其降糖作用却不明显。本文结果为抗糖尿病氧钒配合物构效关系研究提供了新的依据。
Vanadium compounds have a wide spectrum of biological activities, e.g. antidiabetic, anticancer, spermicidal, and anti-inflammatory; amongst, the anti-diabetic activity is the most attractive, making vanadium complexes good candidates for developing therapeutic agents for diabetes. To overcome the potential metal toxicity, researchers put great efforts in improve the antioxidant activities of ligands as well as complexes. Considering flavonoids are excellent natural antioxidants and ligands, we synthesized a series of vanadyl-flavonoid compounexes and evaluated their antioxidant capacity and hypoglycemic effects. The result showed that quercetin and the derivative quercetin 5'-sulfonate, myricetin, kaempferol formed coordination compounds by the carbonyl and 3-hydroxyl groups while naringenin and hesperetin did not. The vanadyl-flavonoid complexes exhibit much better antioxidant capacity than vanadyl maltolato and derivatives. Vanayl complexes with quercetin, myricetin, kaempferol showed good hypoglycemic effects while bis(quercetin 5'-sulfonate)oxovanadium did not although it exhibited much better solubility than the parental compouns. The present work provide new insights to the structure-activity relationship of antidiabetic vanadium compounds.
杨晓达、魏涌标
药学生物化学
氧钒配合物黄酮抗氧化剂糖尿病
vanadiumFlavonoidsAntioxidantDiabetes
杨晓达,魏涌标.一些黄酮及其衍生物的氧钒配合物之合成及生物活性[EB/OL].(2012-09-24)[2025-08-16].http://www.paper.edu.cn/releasepaper/content/201209-269.点此复制
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