摘要
研究小驳骨(Justicia gendarussa Burm.f.)中乙酸乙酯部位的化学成分。综合运用反复硅胶柱色谱、ODS开放柱、凝胶柱色谱、反相半制备型HPLC,对小驳骨的95%乙醇提取物中乙酸乙酯部位的化学成分进行分离纯化,并通过HR-ESI-MS、NMR等光谱数据及X射线单晶衍射共鉴定了21个化合物的结构,分别为2,3,3a,5-四氢-1H-苯并[d]吡咯并[2,1-b][1,3]恶嗪-1-酮(1)、4′-羟基苯乙酮(2)、apocynin(3)、白首乌二苯酮(4)、对羟基苯甲醛(5)、水杨酸(6)、2,4-二羟基苯乙酮(7)、2,5-二羟基苯乙酮(8)、1,3,5-三甲氧基苯(9)、丁香酮(10)、壬二酸(11)、(+)-松脂素-O-β-D-吡喃葡萄糖苷(12)、corchoionoside C(13)、patuletin-3-O-glucoside(14)、commicarpiflavonol glucoside A(15)、1,2,3-三甲氧基-5-硝基苯(16)、4-硝基苯酚(17)、单油酸甘油酯(18)、tetradecanoate(19)、硬脂酸(20)、棕榈酸(21)。化合物1、16为新天然产物,所有化合物均首次从该植物中分离得到。对从中分离得到的单体化合物进行抗炎活性的筛选,其中,槲皮素作为阳性药,其IC50值为16.94±0.40μM。化合物4、6、8具有显著的抗炎活性,其值均小于16.94±0.40μM。
To investigate the chemical constituents of the ethyl acetate fractions in Justicia gendarussa Burm.f..The chemical constituents in ethyl acetate fractions of 95% ethanol extract from J.gendarussa were isolated and purified by repeated silica gel column chromatography,ODS open column,Sephadex LH-20 chromatography and semi-preparative HPLC.Based on HR-ESI-MS,NMR,X-ray single crystal diffraction and other spectral data,21 compounds were identified as 2,3,3 a,5-tetrahydro-1H-benzo[d]pyrrolo[2,1-b][1,3]oxazin-1-one(1),4′-hydroxyacetophenone(2),apocynin(3),baishouwu benzophenone(4),p-hydroxybenzaldehyde(5),salicylic acid(6),2,4-dihydroxyacetophenone(7),2,5-dihydroxyacetophenone(8),1,3,5-trimethoxybenzene(9),syringylethanone(10),nonanedioic acid(11),(+)-pinoresinol-O-β-D-glucopyranoside(12),corchoionoside C(13),patuletin-3-O-glucoside(14),commicarpiflavonol glucoside A(15),1,2,3-trimethoxy-5-nitrobenzene(16),4-nitrophenol(17),glyceryl monooleate(18),tetradecanoate(19),steraric acid(20),palmitatic acid(21).Compounds 1 and 16 were discovered from natural resources for the first time.All compounds were isolated from this plant for the first time and were screened for anti-inflammatory activities.The IC50 values of compounds 4,6 and 8 were lower than that of positive drug(quercetin as positive control,IC50=16.94±0.40 μM),which indicated compounds 4,6 and 8 had significant anti-inflammatory activities.
作者
张海新
夏召
许天启
陈宜敏
周光雄
ZHANG Hai-xin;XIA Zhao;XU Tian-qi;CHEN Yi-min;ZHOU Guang-xiong(Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research,Institute of Traditional Chinese Medicine and Natural Product,College of Pharmacy,Jinan University,Guangzhou 510632,China)
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2020年第7期1148-1155,共8页
Natural Product Research and Development
基金
国家重点研究计划(2017YFC1703800)
自然科学基金面上项目(81573578)
广州市科技计划(201704030120)。
关键词
小驳骨
乙酸乙酯部位
X射线衍射
抗炎活性
Justicia gendarussa Burm.f.
ethyl acetate fraction
X-ray diffraction
anti-inflammatory
