合欢皮中抑制脂肪酸合酶活性成分的提取分离
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摘要
目的提取并分析合欢皮中抑制脂肪酸合酶(FAS)的活性成分。方法以抑制FAS活性为导向,对合欢皮75%乙醇提取物的正丁醇相(AJ-B)进行大孔树脂和硅胶柱层析分离,得到主要成分较为集中的组分Fr4,并且通过半制备高效液相色谱法(HPLC)分离Fr4中的活性成分。结果分离到有活性成分的化合物H2,并鉴定出该化合物为无梗五加苷B,油红O染色实验证实其对肿瘤细胞(HepG2)脂滴生成有影响。结论合欢皮中无梗五加苷B对FAS活性具有抑制作用,且在HepG2细胞中初步证实其有抑制脂滴生成的作用。
Objective In this paper, compound accounting for inhibitory activity of fatty acid synthase(FAS) in Albiziae cortex was studied. Methods Guided by inhibition of FAS activity,the n-butanol phase of the 75% ethanol extract of Albiziae cortex was separated by macroporous adsorbent resin and silica gel column chromatography.Fraction 4 with relatively enriched active compound were further purified using semi-preparative HPLC. Results The active compound H2 was isolated,and was identified to be acanthoside B. Oil red staining experiment confirmed the effect of H2 on lipid droplet formation in tumor cells(HepG2). Conclusion Acanthoside B has an inhibitory effect on fatty acid synthase,and the inhibition of lipid droplet formation in HepG2 cells was preliminarily confirmed.
Objective In this paper, compound accounting for inhibitory activity of fatty acid synthase(FAS) in Albiziae cortex was studied. Methods Guided by inhibition of FAS activity,the n-butanol phase of the 75% ethanol extract of Albiziae cortex was separated by macroporous adsorbent resin and silica gel column chromatography.Fraction 4 with relatively enriched active compound were further purified using semi-preparative HPLC. Results The active compound H2 was isolated,and was identified to be acanthoside B. Oil red staining experiment confirmed the effect of H2 on lipid droplet formation in tumor cells(HepG2). Conclusion Acanthoside B has an inhibitory effect on fatty acid synthase,and the inhibition of lipid droplet formation in HepG2 cells was preliminarily confirmed.
引文
[1]李夏冰.47种植物提取物对脂肪酸合酶及乳腺癌细胞抑制作用[D].北京:中国林业科学研究院,2017.
[2]VANCE D,GOLDBERG I,MITSUHASHI O,et al.Inhibition of fatty acid synthetases by the antibiotic cerulenin[J].Biochemical and Biophysical Research Communications,1972,48(3):649-656.
[3]KUHAJDA F P,PIZER E S,LI J N,et al.Synthesis and antitumor activity of an inhibitor of fatty acid synthase[J].Proceedings of the National Academy of Sciences of the United States of America,2000,97(7):3450-3454.
[4]WANG X,TIAN W.Green tea epigallocatechin gallate:A natural inhibitor of fatty-acid synthase[J].Biochemical and Biophysical Research Communications,2001,288(5):1200-1206.
[5]WANG X,SONG K S,GUO Q X,et al.The galloyl moiety of green tea catechins is the critical structural feature to inhibit fattyacid synthase[J].Biochemical Pharmacology,2003,66(10):2039-2047.
[6]国家药典委员会.中华人民共和国药典[M].北京:中国医药科技出版社,2010:97.
[7]崔树德.中药大全[M].哈尔滨:黑龙江科学技术出版社,1998:677.
[8]韩莉,崔景荣,李敏,等.合欢皮皂苷对S180实体瘤小鼠抑瘤作用的研究[J].中华现代医学杂志,1999,12(13):23.
[9]田维毅,马春玲,白惠卿,等.合欢皮醇提物的红细胞免疫效应及体内抗瘤机制研究[J].四川中医,2002,20(4):10.
[10]李曰.合欢皮总皂苷抗血管治疗对小鼠肿瘤血供模式及脂合成代谢的影响[D].无锡:江南大学,2015.
[11]WU D,MA X F,TIAN W X.Pomegranate husk extract,punicalagin and ellagic acid inhibit fatty acid synthase and adipogenesis of 3T3-L1 adipocyte[J].Journal of Functional Foods,2013,5(2):633-641.
[12]SHAHAT A A,ABDEL-AZIM N S,PIETERS L,et al.Isolation and NMR spectra of syringaresinol-beta-D-glucoside from Cressa cretica[J].Fitoterapia,2004,75(7):771-773.
[2]VANCE D,GOLDBERG I,MITSUHASHI O,et al.Inhibition of fatty acid synthetases by the antibiotic cerulenin[J].Biochemical and Biophysical Research Communications,1972,48(3):649-656.
[3]KUHAJDA F P,PIZER E S,LI J N,et al.Synthesis and antitumor activity of an inhibitor of fatty acid synthase[J].Proceedings of the National Academy of Sciences of the United States of America,2000,97(7):3450-3454.
[4]WANG X,TIAN W.Green tea epigallocatechin gallate:A natural inhibitor of fatty-acid synthase[J].Biochemical and Biophysical Research Communications,2001,288(5):1200-1206.
[5]WANG X,SONG K S,GUO Q X,et al.The galloyl moiety of green tea catechins is the critical structural feature to inhibit fattyacid synthase[J].Biochemical Pharmacology,2003,66(10):2039-2047.
[6]国家药典委员会.中华人民共和国药典[M].北京:中国医药科技出版社,2010:97.
[7]崔树德.中药大全[M].哈尔滨:黑龙江科学技术出版社,1998:677.
[8]韩莉,崔景荣,李敏,等.合欢皮皂苷对S180实体瘤小鼠抑瘤作用的研究[J].中华现代医学杂志,1999,12(13):23.
[9]田维毅,马春玲,白惠卿,等.合欢皮醇提物的红细胞免疫效应及体内抗瘤机制研究[J].四川中医,2002,20(4):10.
[10]李曰.合欢皮总皂苷抗血管治疗对小鼠肿瘤血供模式及脂合成代谢的影响[D].无锡:江南大学,2015.
[11]WU D,MA X F,TIAN W X.Pomegranate husk extract,punicalagin and ellagic acid inhibit fatty acid synthase and adipogenesis of 3T3-L1 adipocyte[J].Journal of Functional Foods,2013,5(2):633-641.
[12]SHAHAT A A,ABDEL-AZIM N S,PIETERS L,et al.Isolation and NMR spectra of syringaresinol-beta-D-glucoside from Cressa cretica[J].Fitoterapia,2004,75(7):771-773.