Synthesis of Hippospongic Acid A Analogues Designed for Investigating the Structure-Activity Relationship of its Biological Activity

2000 ◽  
Vol 53 (12) ◽  
pp. 909 ◽  
Author(s):  
Yoshikazu Hiraga ◽  
Mariko Ago ◽  
Munetaka Tokumasu ◽  
Ken Kaku ◽  
Katsuo Ohkata

Analogues of hippospongic acid A, which inhibit the gastrulation of sea urchin embryos, were synthesized. From a study on structure—activity relationships, the conjugated carboxylic acid moiety was found to be an essential feature for biological activity.

2017 ◽  
Vol 6 (6) ◽  
pp. 343-348
Author(s):  
Lokadi Pierre Luhata ◽  
◽  
Wembi Gaston Luhata ◽  
◽  

Tilirosides (TLD) are glycosidic flavonoids (GFD) from originating in plants that exhibit a range of bioactivities of great interest for healthcare: antioxidant, anti-microbial, antifungal, anti-diabetic and antihyperlipedemic, antiviral and cytotoxic, anti–inflammatory, anti-rheumatism, inhibition of neuroinflammation and acute inflammation and hepatoprotective activities. TLD are biosynthesized in plants in three main steps. First, the synthesis of the aglycone (a flavonoid) occurs, which follows the shikimate pathway with cinnamoylCoA as a starter unit. Second, there is the glucosylation of the aglycone using Uridine diphosphosugar (UDPglucose) as the agent for glycosylation. Finally, the coumaroyl part is added. The Structure Activity Relationship of TLD reveals that the addition of the para coumaric acid moiety considerably modifies their bioactivity.


2014 ◽  
Vol 71 (7) ◽  
pp. 928-936 ◽  
Author(s):  
Benjamin M Nugent ◽  
Ann M Buysse ◽  
Michael R Loso ◽  
Jon M Babcock ◽  
Timothy C Johnson ◽  
...  

2010 ◽  
Vol 20 (15) ◽  
pp. 4620-4623 ◽  
Author(s):  
Jae-Hwan Kwak ◽  
Yoseob Kim ◽  
Hyunjeong Park ◽  
Jae-Yong Jang ◽  
Keun Kuk Lee ◽  
...  

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