著者:別形式 | Suzuki, Ryuichiro / Tanaka, Tomohiro / Yamamoto, Miki / Sakagami, Hiroshi / Tomomura, Mineko / Tomomura, Akito / Satoh, Kazue / Shirataki, Yoshiaki |
著者:所属(別形式) | Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences / Josai University, Faculty of Pharmaceutical Sciences / Meikai University School of Dentistry / Meikai University School of Dentistry / Meikai University School of Dentistry / Showa University, School of Medicine / Josai University, Faculty of Pharmaceutical Sciences |
抄録 | Background: In the current study, we isolated four known compounds, two phenanthrenes, 2,5-dihydroxy-4,9-dimethoxy phenanthrene [1] and 4-methoxyphenanthrene-2,7-diol (flavanthrinin) [2], one phenanthrenequinone, 5-hydroxy-2,3-dimethoxy-1,4-phenanthrenequinone [3], and one flavone, 3,5,7-trihydroxyflavone (galangin) [4], from the ethyl acetate (EtOAc) extract of Odontoglossum Harvengtense 'Tutu' through bioassay-guided fractionation, and investigated their biological activities. Materials and Methods: The isolated compounds were identified with spectroscopic analysis and through comparison to literature values. Cytotoxic activity towards human tumor and normal cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Nitric oxide (NO) was determined by the Griess method. Radical scavenging activity was determined by electron spin resonance (ESR) spectroscopy. Osteoclastogenesis was monitored by tartrate-resistant acid phosphatase (TRAP) activity. Results: The compounds had slightly higher cytotoxicity towards human oral squamous cell carcinoma and leukemia cell lines as compared with human normal oral cells, yielding a tumor specificity value of 1.1-2.7. Among these four compounds, 1 most potently inhibited the lipopolysaccharide (LPS)-stimulated NO production and the receptor activator of nuclear factor-κB ligand (RANKL)-stimulated osteoclastogenesis by mouse macrophage-like RAW264.7 cells. Micromolar concentrations of 1 scavenged the NO radical produced from 1-hydroxy-2-oxo-3-(N-3-methyl-3-aminopropyl)-3-methyl-1- triazene. Conclusion: The present study demonstrated, for the first time, that 1 inhibited both macrophage activation and osteoclast differentiation, suggesting its possible anti-inflammatory action. |