Title:
SELAGINELLA PULVINATA EXTRACTIVE AND PREPARATION METHOD AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2015/055116
Kind Code:
A1
Abstract:
An in-depth study is performed on selaginella pulvinata extractives in the present invention, and it is found that the selaginella pulvinata extractives have a significant anti-inflammatory activity. Multiple column chromatography separation technologies and a semi-preparation high-performance liquid chromatography separation method are used to extract and separate a class of compounds (DZJB1-6) with a 9,9-diphenyl-1-(phenylethynyl)-9H-fluorene new skeleton structure, named as selaginpulvilinsA-F (structural formula (I)). The six compounds extracted and separated from selaginella pulvinata are subjected to structural modification, and then a series of compounds are obtained. These compounds can significantly inhibit the activity of type-4 phosphodiesterase (PDE4), and can be used for preparing PDE4 inhibitors, and treating asthma, chronic obstructive pneumonia, inflammations, and the like. According to the present invention, a new structure is provided for the development of PDE4 inhibitors.
Inventors:
YIN SHENG (CN)
LUO HAIBIN (CN)
LIU XIN (CN)
HUANG YIYOU (CN)
LUO HAIBIN (CN)
LIU XIN (CN)
HUANG YIYOU (CN)
Application Number:
PCT/CN2014/088611
Publication Date:
April 23, 2015
Filing Date:
October 15, 2014
Export Citation:
Assignee:
SUN YATSEN UNIVERSITY (CN)
International Classes:
C07C39/23; A61K31/05; A61K31/09; A61K31/11; A61K31/192; A61K31/222; A61P29/00; C07C37/70; C07C41/34; C07C43/23; C07C45/78; C07C47/57; C07C47/575; C07C51/42; C07C65/19; C07C65/28; C07C67/48; C07C69/16; C07C69/21
Foreign References:
| CN103588616A | 2014-02-19 |
Other References:
LIU, X ET AL.: "Selaginpulvilins A-D, New Phosphodiesterase-4 Inhibitors with an Unprecedented Skeleton from Selaginella pulvinata", ORGANIC LETTERS., vol. 16, no. 1, 12 December 2013 (2013-12-12), pages 282
ZOU, HUI ET AL.: "Advances in Research on Chemical Constituents and Pharmacological Activities of Genus Selaginella", NATURAL PRODUCT RESEARCH AND DEVELOPMENT, vol. 24, no. 11, 30 November 2012 (2012-11-30), pages 1655 - 1670
ZOU, HUI ET AL.: "Advances in Research on Chemical Constituents and Pharmacological Activities of Genus Selaginella", NATURAL PRODUCT RESEARCH AND DEVELOPMENT, vol. 24, no. 11, 30 November 2012 (2012-11-30), pages 1655 - 1670
Attorney, Agent or Firm:
YOGO PATENT & TRADE MARK AGENCY LIMITED COMPANY (CN)
广州粤高专利商标代理有限公司 (CN)
广州粤高专利商标代理有限公司 (CN)
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