基于抗氧化和α-葡萄糖苷酶抑制活性导向下三叶五加根的化学成分研究OA
Chemical constituents of Acanthopanax trifoliatus roots guided by antioxidant and α-glucosidase inhibitory activities
研究三叶五加(Acanthopanax trifoliatus(Linn.)Merr)根中的化学成分.采用甲醇提取三叶五加根,经石油醚、乙酸乙酯分步萃取得到甲醇提取物及石油醚、乙酸乙酯萃取部位,通过MTT法检测各部位细胞毒性后,再进行α-葡萄糖苷酶抑制活性及抗氧化活性筛选,明确乙酸乙酯部位为活性最佳组分.针对该部位,综合运用大孔吸附树脂、正反相硅胶柱层析、Sephadex LH-20、半制备高效液相等色谱技术进行成分分离纯化,结合波谱解析与理化性质鉴定化合物结构,并通过分子对接、α-葡萄糖苷酶抑制实验及DPPH与ABTS自由基清除实验对部分单体化合物进行活性评价.从乙酸乙酯部位分离得到14个化合物,分别鉴定为绿原酸(1)、咖啡酸(2)、槲皮素(3)、柚皮苷(4)、icariside E4(5)、原儿茶酸(6)、开环异落叶松脂醇(7)、原儿茶酸甲酯(8)、(±)-松脂素(9)、piperitol(10)、β-谷甾醇(11)、(+)-芝麻素(12)、15α-hydroxy-ent-kaur-16-en-19-oic acid(13)、苄基-O-β-D-吡喃葡萄糖苷(14).其中化合物5、13、14为首次从五加科植物中分离得到,化合物2、4~10、12~14为首次从三叶五加植物中分离得到,且具α-葡萄糖苷酶抑制作用的化合物1~3、7同时具备抗氧化活性.
Investigation on the Chemical Constituents in the Roots of Acanthopanax trifoliatus(Linn.)Merr.,with methanol used for extraction,followed by sequential partitioning with petroleum ether and ethyl acetate to obtain the methanol extract,petroleum ether fraction,and ethyl acetate fraction.After evaluating the cytotoxicity of these fractions via the MTT assay,α-glucosidase inhibitory and antioxidant activities were screened,identifying the ethyl acetate fraction as the most bioactive com-ponent.Targeting this fraction,a combination of chromatographic techniques including macroporous resin chromatography,nor-mal-phase and reversed-phase silica gel column chromatography,Sephadex LH-20 gel filtration,and semi-preparative high-performance liquid chromatography(HPLC)was employed for the isolation and purification of chemical constituents.The structures of the isolated compounds were elucidated by spectroscopic analysis combined with physicochemical properties.Ad-ditionally,molecular docking,α-glucosidase inhibitory assay,and DPPH/ABTS free radical scavenging assays were performed to evaluate the bioactivities of selected monomeric compounds.Fourteen compounds were isolated from the ethyl acetate frac-tion and identified as chlorogenic acid(1),caffeic acid(2),quercetin(3),naringin(4),icariside E4(5),protocatechuic acid(6),(-)(2R,3R)-secoisolariciresinol(7),protocatechuic acid methyl ester(8),(±)-pinoresinol(9),piperitol(10),β-sitosterol(11),(+)-sesamin(12),15α-hydroxy-ent-kaur-16-en-19-oic acid(13),and benzyl-O-β-D-glucopyr-anoside(14).Among these,compounds 5,13,and 14 were isolated from the family Araliaceae for the first time,while com-pounds 2,4-10,and 12-14 were isolated from A.trifoliatus for the first time.Notably,compounds 1-3 and 7,which exhibi-ted α-glucosidase inhibitory activity,also possessed antioxidant activity.
姜美泠;蒋诗琴;陈杨;戴玲;谭浩;刘向前
湖南中医药大学药学院,长沙 410208湖南中医药大学药学院,长沙 410208||永州市中医医院,永州 425799湖南中医药大学药学院,长沙 410208湖南科技职业学院药学院,长沙 410200湖南省人民医院(湖南师范大学附属第一医院),长沙 410016湖南中医药大学药学院,长沙 410208
医药卫生
三叶五加化学成分分子对接α-葡萄糖苷酶抗氧化
Acanthopanax trifoliatuschemical constituentsmolecular dockingα-glucosidaseantioxidant
《天然产物研究与开发》 2026 (8)
1687-1697,1789,12
湖南省自然科学基金(2024JJ7357)湖南中医药大学"十四五"重点学科-生物工程学科(校行发规字[2023]2号)湖南省自然科学基金科教联合项目(2023JJ60213)
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