青荚叶的化学成分(英文)

Chemical Constituents from Helwingia japonica

目的:为阐明青荚叶(Helwingia japonica(Thunb.)Dietr.)地上部分95%乙醇提取物中具有蛋白酪氨酸磷酸酯酶1B(protein tyrosine phosphatase,PTP1B)抑制活性的化学成分。方法:分别从四川芦定县和平武县采得青荚叶样品A和B,运用多种层析手段进行分离纯化,通过波谱数据和理化性质进行化合物的鉴定。结果:样品A的95%乙醇提取物按极性分段后,HC、HE、HF、HG部分具有强的抑制PTP1B活性。从样品A的95%乙醇提取物中分离并鉴定了9个化合物(1-9)。样品B的95%乙醇提取物的乙酸乙酯部分显示PTP1B抑制活性(IC504.63g.mL-1),从中分离得到5个化合物(10-14)。鉴定它们为谷甾醇(1)、β-胡萝卜苷(2)、羽扇豆醇(3)、桦木醇(4)、桦木酸(5)、棕榈酸甘油酯(6)、桂皮酸(7)、6αH-4-烯-3-酮-豆甾醇(8)、6αH-4-烯-3-酮-豆甾醇(9)、p-menth-2-en-1β,4β,8-triol(10)、blumenol A(11)、2′,3′,4′,5′,6′-五羟基查尔酮(12)、洋芹素7-O-β-D-吡喃葡萄糖苷(13)和木犀草素7-O-β-D-吡喃葡萄糖苷(14)。结论:除了化合物13与14,其余均是在该植物中首次分离得到。据报道化合物5有PTP1B抑制活性,但考虑其在植物中的含量,青荚叶中的活性成分有待进一步研究。

AIM： To discover protein tyrosine phosphatase 1B （PTP1B） inhibitory compounds from the 95% ethanol extract of the aerial parts of Helwingia japonica （Thunb.） Dietr.. METHODS： Two plant samples （A and B） were collected respectively from Luding County and Pingwu County, Sichuan Province of China, and chromatography was used for separation, and spectroscopic methods were employed for the identification of isolated compounds. RESULTS： Fractions HC, HE, HF, HG of the 95% ethanol extract of sample A were active. From A nine compounds （1-9） were iso- lated. The AcOEt fraction of the 95% ethanol extract of the aerial parts of sample B showed PTP1B inhibitory activity with an IC50 of 4.63 ktg.mL-1, and five compounds （10-14） were isolated from this fraction. The isolated compounds were identified as fl-sitosterol （1）, β-daucosterol （2）, lupeol （3）, betulin （4）, betulinic acid （5）, hexadecanoic acid 2, 3-dihydroxypropyl ester （6）, cinnamic acid （7）, stignast-4-en-6β-3-one （8）, stignast-4-en-6a-3-one （9）, p-menth-2-en- 1β, 4β, 8-triol （10）, blumenol A （11）, 2＇, 3＇, 4＇, 5＇, 6＇-pentahydroxychalcone （12）, apigenin 7-O-β-D-glucopyranoside （13）, and luteolin 7-O-β-D-glucopyranoside （14）. CONCLUSION： Except compounds 13 and 14, all the other compounds are first isolated from Helwingia japonica （Thunb.） Dietr.. Compound 5 is a known PTP1B inhibitor. It is necessary to study the active compounds in this plant further when taking the yield of compound 5 into account.