Medicinal Chemistry

Mian Zhang

Publications

• Research Article
  Anti-inflammatory Properties of an Active Sesquiterpene Lactone and its Structure-Activity Relationship
  Author(s): Yang Hu, Fei Zhang, Chaofeng Zhang and Mian ZhangYang Hu, Fei Zhang, Chaofeng Zhang and Mian Zhang
  
  A sesequiterpenoid, 2α-hydroxyl-3β-angeloylcinnamolide (HAC) was isolated from the Chinese medicinal herb Polygonum jucundum Lindex. (Polygonaceae) with anti-inflammatory activities in vivo. In the present study, we investigated the anti-inflammation effects of HAC on lipopolysaacharide (LPS)-induced murine RAW264.7 cells. As the results, we found that HAC dose-dependently decreased NO over-production with IC50 value of 17.68 μM but showed very weak inhibition on TNF-α release with IC50 value of 98.66 μM. Meanwhile, eight novel derivatives modified at C-2 position of HAC were synthesized to further explore the structure-activity relationships (SARs) of HAC on antiinflammation effects. Compound PJH-1, an acetyl easer of HAC, showed better inhibition on over-production of NO and TNF-α (IC50, 7.31 and 3.38 μM, respectively.. Read More»
  DOI: 10.4172/2161-0444.1000286

  Abstract PDF