4.7 Article

Phthalide Derivatives with Anticoagulation Activities from Angelica sinensis

Journal

JOURNAL OF NATURAL PRODUCTS
Volume 79, Issue 7, Pages 1857-1861

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.6b00080

Keywords

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Funding

  1. National Natural Science Foundation of China [81202916, 31400305]
  2. Project for Youth Backbone Teachers in the University of Henan Province [2013GGJS-129, 2015GGJS-130]
  3. Science and Technology Project of Henan Province [152102310113]
  4. Science and Technology Project of the Education Department of Henan Province [14A360012]

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Two new phthalide derivatives, angesinenolides A and B (1 and 2), were isolated from the roots of Angelica sinensis. Their structures were elucidated using HRMS, NMR, and X-ray crystallographic data. Compound 1 is the first example of a phthalide trimer presumably formed through two [2+2] cycloaddition reactions. Compound 2 is a unique dimeric phthalide with a peroxy bridge between C-3a and C-6. Both phthalides were evaluated for in vitro anticoagulation activities. Compound 1 reduced the level of fibrinogen (FIB). Compound 2 significantly extended thrombin time and activated partial thromboplastin time, as well as markedly reduced the content of FIB.

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