Presentation at PacifiChem,
in Honolulu, Hawaii, USA

Health promoting use and composition analysis of medicinal citrus products

Substances like polymethoxyflavones (PMFs) found in citrus peels possess biological properties such as anti-tumor, anti-inflammation, anti-hyperglycemia and anti-hyperlipidemia, etc. There are a few citrus derived products whose major sources are from citrus peel extracts. The potential health application of a citrus peel product from a Citrus Research Center of Japan has prompted us to investigate the contents of PMFs and other nutraceuticals to establish a correlation between the chemical composition and efficacy. We have identified and quantified PMFs as well as some other flavonoids that have been reported previously to have biological activity as single compounds. The biological activity, analytical methodology, data analysis and composition-activity relationship will be described in this presentation.

Michiko Suzawa1 & Shiming Li2,3
Yutaka Miyauchi1, Terry Nash1, Nancy E. Rawson3, Chi-Tang Ho2

1) Miyauchi Citrus Research Center, Ltd., Japan
2) Department of Food Science, Rutgers University, New Brunswick, NJ
3) WellGen, Inc., North Brunswick, NJ, USA

▧ Biological activities Gold Lotion (GL)
 ▻ Anti-inflammation: iNOS, TNF-α
 ▻ Anti-microbial: Streptococcus, S. aurenus, S. griseus, P. digitatum, F. oxysporus, T. aentagrophytes,
   M. gypseum, P. aeruginosa, V. parahacmolyticus, etc.
 ▻ Hair growth stimulating agent
 ▻ Skin whitening

▧ Anti-inflammation protocol
 ▻ Inhibition of LPS-induced nitric oxide and TNF-α production
  by GL in RAW264.7 murine macrophages (introduction of graphs and pictures omitted) list below:
    Effect of GL on LPS-induced TNF-α production in RAW264.7 cells,
    Effect of GL on cell viability in RAW264.7 cells,
    Effects of GL on LPS-induced NO production and iNOS protein induction in RAW264.7 cells,
    Effect of GL on LPS- induced nuclear translocation of NF-κB(p65) in RAW 264.7 cells,
    Effect of GL on LPS-induced degradation of 1κB-α in RAW 264.7 cells

 ▻ Mechanism of inhibitory action of GL on NO and TNF-α production
    By Dr. Komiyama of Kitasato University, Japan

 ▻ TPA-induced skin inflammation model
    By Dr. Min-Hsiung Pan of Taiwan University, Taiwan
    (pictures omitted)
 ▻ Radical scavenging activity of GL
   The inhibitory activity of GL on hydroxyl radical generated in a
   cell-free chemical system (FeSO/HO) was investigated by the RE2X, JEOL(ESR).
   Scavenging of hydroxyl radical was determined using DMPO.

▧ GL analysis (graphs and quantification omitted)
  The results from in vivo were omitted this time for applying the patent.

▧ Summary
 ▻ GL significantly inhibited LPS-induced TNF-α and NO production without any cytotoxic activity.
 ▻ GL also clearly inhibited translocation of NK-κB subunit p65 from cytoplasm into the nucleus
   in RAW  264.7 cells.
 ▻ GL did not show the degradation of IκBα induced by LPS stimulation.
 ▻ GL possessed radical scavenging activity in vitro.