Centro de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, 1749-016, Lisbon, Portugal.
UR11ES33'Integrated Physiology', Faculty of Sciences of Bizerte, Carthage University, Tunis, Tunisia.
Arch Pharm Res. 2017 Nov;40(11):1278-1286. doi: 10.1007/s12272-017-0959-1. Epub 2017 Sep 21.
Bioactive compounds, such as isorhamnetin and piscidic acid, were obtained from decoctions of cladodes (stem pads from Opuntia ficus-indica). The effect of these phenolic compounds, in a fiber-free extract, were evaluated as inhibitors of cholesterol permeation through a Caco-2 cell monolayer and as 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. A reduction of 38% in cholesterol permeation through the Caco-2 cell monolayer was obtained, and the phenolic compounds all permeated between 6 and 9%. A mixture of these compounds showed an IC of 20.3 μg/mL as an enzyme inhibitor, whereas piscidic acid alone showed an IC of 149.6 μg/mL; this was slightly outperformed by the isorhamnetin derivatives. Docking studies confirmed that both piscidic acid and isorhamnetin derivatives, present in the decoction, could adequately bind to the enzyme active site. These results reveal that O. ficus-indica, and cladodes derived there from, is a promising plant for use in the development of new functional foods and pharmaceutical products.
从龙舌兰（Opuntia ficus-indica）的茎髓（茎垫）提取到生物活性化合物，如山奈酚和粘果酸。评估这些酚类化合物在无纤维提取物中的作用，作为胆固醇渗透通过 Caco-2 细胞单层的抑制剂和 3-羟基-3-甲基戊二酰辅酶 A 还原酶抑制剂。通过 Caco-2 细胞单层的胆固醇渗透降低了 38%，酚类化合物的渗透都在 6%到 9%之间。这些化合物的混合物表现出 20.3μg/mL 的 IC 作为酶抑制剂，而单独的粘果酸的 IC 为 149.6μg/mL；这略优于山奈酚衍生物。对接研究证实，提取液中存在的粘果酸和山奈酚衍生物都可以与酶的活性位点充分结合。这些结果表明，龙舌兰和由此衍生的茎髓是开发新型功能性食品和药物产品的有前途的植物。
