title: Berberine as a chemical and pharmacokinetic marker of the butanol-extracted Food Allergy Herbal Formula-2.
abstract: BACKGROUND
  Food Allergy Herbal Formula-2 (FAHF-2) provided protection against peanut anaphylaxis in a murine model and induced beneficial immune-modulation in humans. Butanol-refined FAHF-2, B-FAHF-2, retained safety and efficacy in the peanut allergic murine model at only 1/5 of FAHF-2 dosage. One compound, berberine, was isolated and identified in vitro as a bioactive component present in FAHF-2 and B-FAHF-2. The aim of this study was to investigate berberine as a chemical and pharmacokinetic marker of B-FAHF-2.
  
  
  METHODS
  The consistency of constituents between B-FAHF-2 and FAHF-2 was tested. Peanut allergic C3H/HeJ mice were orally administered with 1mg of berberine or B-FAHF-2 containing an equivalent amount of berberine, and the ability to protect against peanut anaphylaxis and pharmacokinetic parameters were determined. Human intestinal epithelial cells (Caco-2) were cultured with berberine with or without the nine individual herbal constituents in B-FAHF-2, and the absorbed berberine levels were determined.
  
  
  RESULTS
  Berberine is one of the major components in B-FAHF-2 and FAHF-2 formula. In a peanut allergic mouse model, B-FAHF-2, but not berberine, protected mice from anaphylaxis reactions. Pharmacokinetic profiles showed that the Cmaxof B-FAHF-2 fed mice was 289.30±185.40ng/mL; whereas berberine alone showed very low bioavailability with Cmaxvalue of 35.13±47.90ng/mL. Caco-2 cells influx assay showed that 7 of 9 herbal constituents in B-FAHF-2 increased berberine absorption at rates ranging from 18 to 205%.
  
  
  CONCLUSIONS
  B-FAHF-2 remarkably increased the bioavailability of berberine. Berberine can be used as chemical and pharmacokinetic marker of B-FAHF-2. Other herbal components in B-FAHF-2 may facilitate the absorption of berberine.
authors.affiliation: Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
authors.forename: Nan
authors.initials: N
authors.lastname: Yang
authors.affiliation: Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
authors.forename: Kamal
authors.initials: K
authors.lastname: Srivastava
authors.affiliation: Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
authors.forename: Ying
authors.initials: Y
authors.lastname: Song
authors.affiliation: Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
authors.forename: Changda
authors.initials: C
authors.lastname: Liu
authors.affiliation: Hematology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
authors.forename: Sool
authors.initials: S
authors.lastname: Cho
authors.affiliation: Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States; Life Science and Technology, Changchun University of Science and Technology, Changchun 130022, China.
authors.forename: Yujuan
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States. Electronic address: xiu-min.li@mssm.edu.
authors.forename: Xiu-Min
authors.initials: XM
authors.lastname: Li
mesh_terms: D000485:Allergens / Q000737:chemistry / Q000276:immunology*; D000707:Anaphylaxis / Q000209:etiology / Q000517:prevention & control*; D000818:Animals; D001599:Berberine / Q000737:chemistry / Q000276:immunology*; D000440:Butanols / Q000737:chemistry; D018938:Caco-2 Cells; D005260:Female; D006801:Humans; D007073:Immunoglobulin E / Q000097:blood; D007371:Interferon-gamma / Q000378:metabolism; D015848:Interleukin-5 / Q000378:metabolism; D051379:Mice; D008809:Mice, Inbred C3H; D021183:Peanut Hypersensitivity / Q000150:complications / Q000188:drug therapy*; D010936:Plant Extracts / Q000737:chemistry / Q000276:immunology*
chemical_list: D000485:Allergens; D000440:Butanols; C497376:Food Allergy Herbal Formula-2; D015848:Interleukin-5; D010936:Plant Extracts; D001599:Berberine; D007073:Immunoglobulin E; D007371:Interferon-gamma
keywords: Berberine; Butanol-extracted Food Allergy Herbal Formula-2; Caco-2 cells; Food allergy; Pharmacokinetics