[关键词]
[摘要]
目的 研究乌饭树Vaccinium bracteatum叶化学成分及其抗补体活性。方法 通过溶血实验,以抗补体活性作为导向分离手段,对乌饭树叶各部位进行抗补体活性测试,运用多种色谱方法进行分离纯化,采用现代谱学技术鉴定化合物结构,确定抗补体活性成分。结果 从乌饭树叶70%乙醇提取物中分离得到28个化合物,分别鉴定为三十五烷(1)、三十一烷(2)、赤杨酮(3)、木栓酮(4)、表木栓醇(5)、羽扇豆醇(6)、齐墩果酸(7)、熊果酸(8)、东莨菪素(9)、反式对羟基桂皮酸(10)、柯伊利素(11)、芹菜素(12)、山柰酚(13)、山楂酸(14)、科罗索酸(15)、蔷薇酸(16)、2α, 3α-二羟基熊果酸(17)、19α-羟基熊果酸(18)、咖啡酸(19)、异荭草苷(20)、荭草苷(21)、牡荆苷(22)、异牡荆苷(23)、槲皮素-3-O-α-L-鼠李糖苷(24)、异槲皮苷(25)、柯伊利素-7-O-β-D-葡萄糖苷(26)、槲皮素(27)、木犀草素(28)。对其中的25个化合物进行抗补体活性实验,化合物5、7、8、11~13、15、18~20、23~25、27、28对经典途径的补体激活具有不同程度的抑制作用。结论 化合物1、3、6、14~18、23、25为首次从该植物中分离得到,熊果酸的抗补体活性最强,50%抑制溶血浓度(CH50)为0.014 mg/mL。
[Key word]
[Abstract]
Objective To study the chemical constituents in the leaves of Vaccinium bracteatum and their anti-complementary activity. Methods The isolation was guided by anti-complementary activity test, compounds were isolated and purified by silica gel and Sephadex LH-20 column chromatographies as well as preparative HPLC. The structures were identified by the various spectroscopic data. The compounds were evaluated for the anti-complementary activity in vitro. Results Twenty-eight compounds were isolated and identified as pentatriacontane (1), hentriantane (2), glutinone (3), friedelin (4), epifriedelanol (5), lupeol (6), oleanolic acid (7), ursolic acid (8), scopoletin (9), trans-p-hydroxycinnamic acid (10), chrysoeriol (11), apigenin (12), kaempferol (13), maslinic acid (14), corosolic acid (15), euscaphic acid (16), 2α, 3α-dihydroxyurs-12-en-oic acid (17), 19α-hydroxyoleanolic acid (18), caffeic acid (19), isoorientin (20), orientin (21), vitexin (22), isovitexin (23), quercetin-3-O-α-L-rhamnoside (24), isoquerecitrin (25), chrysoeriol- 7-O-β-D-glucopyranoside (26), quceritin (27), and luteolin (28). Among them 25 compounds were tested for their anti-complementary activity and 5, 7, 8, 11—13, 15, 18—20, 23—25, 27, and 28 show the various inhibitions on the complement system towards the classical pathway. Conclusion Compounds 1, 3, 6, 14—18, 23, 25 are obtained from this plant for the first time. Ursolic acid shows the strongest activity in vitro with the CH50 of 0.014 mg/mL.
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[基金项目]
江苏省优势学科项目资助(PAPD)