天然产物研究与开发 ›› 2022, Vol. 34 ›› Issue (11): 1892-1899.doi: 10.16333/j.1001-6880.2022.11.010

• 研究简报 • 上一篇    下一篇

密花樫木根化学成分及其蛋白酪氨酸磷酸酶1B抑制活性研究

杨   帆,张亚梅*   

  1. 江西中医药大学 江西民族传统药现代科技与产业发展协同创新中心,南昌 330004
  • 出版日期:2022-11-25 发布日期:2022-11-25
  • 基金资助:
    国家自然科学基金(31760092);江西中医药大学校级科技创新团队发展计划(CXTD22002)

Study on chemical constituents from the roots of Dysoxylum densiflorum and their protein tyrosine phosphatase 1B inhibitory activity

YANG Fan,ZHANG Ya-mei*   

  1. Jiangxi Collaborative Innovation Center of Modern Technology and Industrial Development of Ethnic Traditional Medicine,Jiangxi University of Chinese Medicine,Nanchang 330004,China
  • Online:2022-11-25 Published:2022-11-25

摘要:

为研究密花樫木(Dysoxylum densiflorum)根的化学成分及其蛋白酪氨酸磷酸酶1B(PTP-1B)抑制活性。利用多种色谱方法从密花樫木根乙酸乙酯萃取物中分离得到23个化合物,并运用现代波谱技术鉴定其结构,分别为5(10),13E-halimadiene-3α,15-diol(1)、(-)-agbanindiol A(2)、polylauioid H(3)、2-oxopopulifolic acid(4)、dysoxydenone C(5)、2-oxo-ent-cleroda-3,13Z-dien-15-oic acid(6)、nakamurol B(7)、methyl (13E)-2-oxoneocleroda-3,13-dien-15-oate(8)、15-acetoxy-ent-3,13E-clerodadien-2-one(9)、(3α,4β,13E)-neoclerod-13-ene-3,4,15-triol(10)、5(10),14-halimadiene-3α,13ξ-diol(11)、dysokusone A(12)、14,15-dinorclerod-3-ene-2,13-dione(13)、3,4-epoxyclerodan-13E-en-15-oic acid(14)、dysokusone G(15)、15-acetyloxyl-3α,4β-dihydroxy-neoclerod-13Z-ene(16)、[1α(E),2β,4aβ,8aα]-5-(decahydro-4a-hydroy-1,2,5,5-tetra-methyl-1-naphthalenyl)-3-methl-2-penten-1-ol(17)、kolavenol(18)、(13E)-2-oxoneocleroda-3,13-dien-15-ol(19)、2β-hydroxykolavenol(20)、ent-3β,4β-epoxyclerod-13E-en-15-ol(21)、2-oxodihydrokolavenol acetate(22)和(3α,4β,13E)-4-ethoxyneoclerod-13-ene-3,15-diol(23)。化合物246~911131417~2022~23为首次从樫木属植物中分离得到。采用体外PTP-1B抑制活性评价所得化合物的生物活性,发现化合物3121621具有抑制PTP-1B作用,其IC50值分别为31.25±0.64、0.30±0.56、0.64±0.51和78.50±0.59 μmol/L。

关键词: 密花樫木, 化学成分, PTP-1B抑制活性

Abstract:

In order to study the chemical constituents from the roots of Dysoxylum densiflorum and their protein tyrosine phosphatase 1B(PTP-1B) inhibitory activity.Twenty-three compounds were isolated from the D. densiflorum applying various chromatographic techniques.Their structures were elucidated and identified as 5(10),13E-halimadiene-3α,15-diol(1),(-)-agbanindiol A(2),polylauioid H(3),2-oxopopulifolic acid(4),dysoxydenone C(5),2-oxo-ent-cleroda-3,13Z-dien-15-oic acid(6),nakamurol B(7),methyl (13E)-2-oxoneocleroda-3,13-dien-15-oate(8),15-acetoxy-ent-3,13E-clerodadien-2-one(9),(3α,4β,13E)-neoclerod-13-ene-3,4,15-triol(10),5(10),14-halimadiene-3α,13ξ-diol(11),dysokusone A(12),14,15-dinorclerod-3-ene-2,13-dione(13),3,4-epoxyclerodan-13E-en-15-oic acid(14),dysokusone G(15),15-acetyloxyl-3α,4β-dihydroxy-neoclerod-13Z-ene(16),[1α(E),2β,4aβ,8aα]-5-(decahydro-4a-hydroy-1,2,5,5-tetra-methyl-1-naphthalenyl)-3-methl-2-penten-1-ol(17),kolavenol(18),(13E)-2-oxoneocleroda-3,13-dien-15-ol(19),2β-hydroxykolavenol(20),ent-3β,4β-epoxyclerod-13E-en-15-ol(21),2-oxodihydrokolavenol acetate(22),(3α,4β,13E)-4-ethoxyneoclerod-13-ene-3,15-diol(23).Compounds 2,4,6-9,11,13,14,17-20,22-23 are obtained from Dysoxylum for the first time.Compounds 3,12,16 and 21 had PTP-1B inhibitory activity with the IC50 values were 31.25±0.64,0.30±0.56,0.64±0.51 and 78.50±0.59 μmol/L,respectively.

Key words: Dysoxylum densiflorum, chemical composition, PTP-1B inhibitory activity

中图分类号:  R284