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作 者:张勇[1,2,3] 阿吉艾克拜尔·艾萨[1,3] 朱维良 ZHANG Yong;HAJI Akber Aisa;ZHU Wei-liang(State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization,CAS Laboratory of Chemistry of Plant Resources in Arid Regions,Xinjiang Technical Institute of Physics and Chemistry,Chinese Academy of Sciences,Urumqi 830011,China;CAS Key Laboratory of Receptor Research,Stake Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China;University of Chinese Academy of Sciences,Beijing 100049,China)
机构地区:[1]中国科学院新疆理化技术研究所,省部共建新疆特有药用资源利用国家重点实验室培育基地,中国科学院干旱区植物资源化学重点实验室,新疆乌鲁木齐830011 [2]中国科学院上海药物研究所,新药研究国家重点实验室,中国科学院受体结构与功能重点实验室,上海201203 [3]中国科学院大学,北京100049
出 处:《药学学报》2022年第7期2139-2145,共7页Acta Pharmaceutica Sinica
基 金:国家自然科学基金资助项目(81603270)。
摘 要:采用大孔吸附树脂、反相硅胶、葡聚糖凝胶及微孔树脂等多种色谱技术,从谷精草水提取中分离得到10个化合物。通过NMR、ESI-MS、HR-ESI-MS、UV、IR等波谱技术并结合化学方法对其进行了结构鉴定,分别为6-methoxyquercetin-3-O-(2′′′-vanilloyl)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside(1)、丁香脂素-4′-O-β-D-葡萄糖苷(2)、芦丁(3)、1-O-feruloylglycerol(4)、邻苯二酚(5)、吐叶醇(6)、β-D-(6-O-trans-feruloyl)fructofuranosyl-α-D-O-glucopyranosied(7)、二氢阿魏酸(8)、鸟嘌呤核苷(9)和槲皮素-3-O-β-D-龙胆二糖苷(10),化合物1为新化合物,化合物2、4~10为首次从谷精草属植物中分离得到,化合物3为首次从该植物中分离得到。分子对接结果显示化合物1具有潜在的肿瘤坏死因子-α(TNF-α)转换酶抑制活性。体外抗炎活性实验证实,化合物1在1、10和100μmol·L能显著抑制脂多糖(LPS)诱导的RAW264.7细胞中TNF-α的升高,具有较好的体外抗炎活性。Ten compounds were isolated from the water extract of Eriocaulon buergerianum by HP20,ODS,Sephadex LH-20 and MCI Gel CHP-20 column chromatographic methods.Their structures were identified by spectroscopic and chemical approaches as 6-methoxyquercetin-3-O-(2′′′-vanilloyl)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside(1),syringaresinol-4′-O-β-D-glucopyranoside(2),rutin(3),1-O-feruloylglycerol(4),1,2-benzenediol(5),vomifoliol(6),β-D-(6-O-trans-feruloyl)fructofuranosyl-α-D-O-glucopyranosied(7),dihydroferulic acid(8),guanosine(9)and quercetin-3-O-β-gentiobioside(10).The compound 1 is a new compound,the compounds 2 and 4-10 were obtained from Eriocaulon genus for the first time,and the compound 3 was isolated from this plant for the first time.Molecular docking study showed that 1 is a potential inhibitor of TNF-α.The compound 1 was evaluated for their anti-inflammatory activities in vitro,and 1 showed significant inhibitory activity against TNF-αproduction in lipopolysaccharide(LPS)-induced RAW264.7 macrophage cells at the concentrations of 1,10 and 100μmol·L.
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