粗壮润楠化学成分及其活性研究  

Chemical constituents of Machilus robusta and their biological activities

作　　者：里艳茹[1,2] 黄胜男 寻园[2] 程林友 谢百波 LI Yan-ru;HUANG Sheng-nan;XUN Yuan;CHENG Lin-you;XIE Bai-bo(State Key Laboratory of Bioactive Substances and Function of Natural Medicine,Ministry of Education,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050;Beijing Hebabiz Biotechnology Co.,Ltd.,Beijing 102206;South Section of Guang'anmen Hospital,China Academy of Chinese Medical Sciences,Beijing 102618;Guangxi Hebabiz Pharmaceutical Co.,Ltd.,Qinzhou Guangxi 535008)

机构地区：[1]中国医学科学院北京协和医学院药物研究所,天然活性物质与功能国家重点实验,北京100050 [2]北京慧宝源生物技术股份有限公司,北京102206 [3]中国中医科学院广安门医院南区,北京102618 [4]广西慧宝源医药科技有限公司,广西钦州535008

出　　处：《中南药学》2022年第10期2279-2285,共7页Central South Pharmacy

基　　金：广西“创新驱动发展”科技重大专项-东盟药物创新中心建设及新药开发(No.桂科AA19254033)。

摘　　要：目的 研究粗壮润楠的化学成分,并对分离得到的化学成分进行生物活性筛选,为寻找新的生物活性成分、建立药材的质量标准奠定基础。方法 采用乙醇提取、乙酸乙酯萃取、硅胶柱色谱、Sephadex L^(-1)H-20柱色谱、反相中压柱色谱、闪式柱色谱以及反相HPL^(-1)C柱色谱分离等方法进行分离纯化;运用波谱数据分析鉴定化合物的结构。在细胞水平模型上,筛选化合物在神经保护、抗氧化、肿瘤细胞毒、肝保护和抗人类免疫缺陷病毒等方面的活性。结果 从粗壮润楠的乙酸乙酯部位共分离得到19个化合物,分别为α-芒柄花萜醇(1)、熊果酸(2)、白桦脂酸(3)、熊果醇(4)、8-(3,5-二羟基苯基)-1-丙基辛醇2,4-二羟基-6-十一烷基苯甲酸酯(5)、大黄素甲醚(6)、β-谷甾醇(7)、(+)-(7S,8R)-4-羟基-3,7-二甲氧基-1’,2’,3’,4’,5’,6’,7’-降七碳木脂烷-8’-酮(8)、(+)-去氢催吐萝芙木醇(9)、3-羟基-4-甲氧基苯丙烯酸乙酯(10)、4-羟基-3-甲氧基苯丙烯酸乙酯(11)、7-甲氧基香豆素(12)、5,7-二甲氧基-6-羟基香豆素(13)、4-羟基-3,5-二甲氧基苯甲酸(14)、苯甲酸(15)、对羟基苯甲醛(16)、对羟基苯乙醇(17)、3,4-二羟基苯甲酸(18)和3-羟基-4-甲氧基苯甲酸(19)。结论 化合物 1 和 5 为首次从樟科植物中分离得到,其余化合物均为首次从该植物中分离得到。化合物 9(10 μmol·L^(-1))对去血清诱导的PC12细胞损伤有保护作用,其相对保护率为(76.60±10.67)%。Objective To determine the chemical constituents of Machilus robusta and screen their bioactivities to find new bioactive components,establish the quality standard of medicinal materials.Methods The constituents were isolated with a combination of various chromatographic techniques including column chromatography over silica gel,Sephadex LH-20,C-18,and MCI gel (CHP20P) as well as reversed-phase HPLC.The bioactivities of the compounds on neuroprotection,antioxidation,tumor cytotoxicity,liver protection and anti-HIV were screened in vitro.Results The structures of 19 isolates were identifed by spectroscopic data analysis:α-onocerin (1),ursolic acid (2),betulinic acid (3),uvaol (4),8-(3,5-dihydroxyphenyl)-1-propyloctyl-2,4-dihydroxy-6-undecylbenzoate (5),3-methyl-6-methoxy-1,8-dihydroxy-9,10-anthraquinone (6),β-sitosterol (7),(+)-(7S,8R)-4-hydroxy-3,7-dimethoxy-1’,2’,3’,4’,5’,6’,7’-heptanorlignan-8’-one (8),(+)-dehydrovo-mifoliol (9),ethyl 3-hydroxy-4-methxoyphenylpropionate (10),ethyl ferulate (11),7-methxoycoumarin (12),5,7-dimethoxy-6-hydroxycoumarin (13),syringic acid (14),benzoic acid (15),p-hydroxybenzaldehyde (16),p-hydroxybenzoic ethanol (17),3,4-dihydroxybenzoic acid (18),and 3-hydroxy-4-methxoybenzoic acid (19).Conclusion Compounds 1 and 5 have been obtained from Lauraceae for the first time.Other compounds are obtained from Machilus robusta for the first time.Compound 9 shows neuroprotective activity against PC12 cell damage induced by the MPPwith relative protective rate of (76.60±10.67)% at 10 μmol·L^(-1).

关 键 词：润楠属 粗壮润楠 化学成分 活性筛选 

分 类 号：R285[医药卫生—中药学] R284.1[医药卫生—中医学]