title: Anti-inflammatory potential of a lipid-based formulation of a rotenoid-rich fraction prepared from Boerhavia diffusa.
abstract: BACKGROUND
  Boerhavia diffusa L. (Nyctaginaceae) roots are used in Ayurveda for treating inflammatory diseases. Generally poor oral bioavailability is a major problem associated with herbal drugs.
  
  
  OBJECTIVE
  To develop a phospholipid complex of rotenoid-rich fraction (RRF) and evaluate its in vivo anti-inflammatory activity and pharmacokinetic study.
  
  
  METHODS
  RRF was prepared from a 70% ethanol extract of B. diffusa roots. This RRF was complexed with phosphatidylcholine by refluxing in 70% ethanol. In vivo anti-inflammatory activity of RRF-PC and RRF was determined using the carrageenan-induced rat paw edema method, at a dose equivalent to 100 mg/kg p.o. of RRF. Edema volume was calculated at 3 and 5 h. The plasma concentration of boeravinone B was estimated in rats at a same dose level. Blood samples were collected at 1, 2, 4, 6, 8, 10, 12, 24, and 36 h.
  
  
  RESULTS
  (1)H and (31)P NMR spectra of RRF-PC showed up-field shift of protons of the (+)N(CH3)3 group (3.37 → 3.23) and the phosphorus atom (-1.26 → -1.57 ppm), respectively, which confirmed phospholipid complex formation between phosphatidylcholine [PO4 and (+)N(CH3)3 groups] and phytoconstituents by hydrogen bonding. The RRF-PC showed significantly enhanced in vivo anti-inflammatory activity (64%) as compared with RRF (48%) and ibuprofen (50%) at 5 h (p < 0.001). Furthermore, detected plasma concentration of boeravinone B was two times higher in RRF-PC (75 ng/mL) as compared with RRF (40 ng/mL).
  
  
  CONCLUSIONS
  The present study demonstrated an increased anti-inflammatory potential and higher plasma level of boeravinone B in lipid-based formulation (RRF-PC) as compared with RRF.
authors: Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER) , Mohali, Punjab , India.
authors: Khemraj
authors: K
authors: Bairwa
authors: Sanjay Madhukar
authors: SM
authors: Jachak
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000627:therapeutic use*; D002626:Chemistry, Pharmaceutical; D004487:Edema / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D008055:Lipids; D039281:Nyctaginaceae; D010936:Plant Extracts / Q000302:isolation & purification / Q000627:therapeutic use*; D018517:Plant Roots; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000893:Anti-Inflammatory Agents; D005419:Flavonoids; D008055:Lipids; D010936:Plant Extracts; C560379:boeravinone B
keywords: Boeravinone B; oral bioavailability; phosphatidylcholine; phospholipid complex