RESUMEN
The methanolic extract [inhibition (%): 61.2±3.8 (p<0.01) at 100 µg/mL] and its EtOAc-soluble fraction [inhibition (%): 82.5±1.7 (p<0.01) at 100 µg/mL1 from the sclerotia of Inonotus obliquus collected in Japan significantly inhibited invasion of human fibrosarcoma HT1080 cells through matrigel-coated filters. In addition, the methanolic extract significantly inhibited lung tumor formation fifteen days after injection of BI6F10 melanoma cells in mice [inhibition (%) 66.1 ± 12:8 (p < 0.05) at 500 mg/kg/d, p.o.]. Lanostane-type triterpenes were isolated as the common principal constituents from Japanese and Russian . obliquus. Furtheremore, we examine the inhibitory effects of the constituents on the invasion of HT 1080 cells. Interestingly, 3ß-hydroxylanosta-8,24-dien- 21-al [inhibition (%) 37.9 ± 3.0 (p < 0.05) at 30 µM] significantly inhibited the invasion, and no cytotoxic effect at 30 µM was observed.
Asunto(s)
Antineoplásicos/farmacología , Basidiomycota/química , Triterpenos/farmacología , Animales , Línea Celular Tumoral , Femenino , Fibrosarcoma/tratamiento farmacológico , Fibrosarcoma/patología , Humanos , Ratones , Ratones Endogámicos C57BL , Invasividad NeoplásicaRESUMEN
The methanolic extract and its EtOAc-soluble fraction from the rhizomes of Zingiber cassumunar inhibited invasion of human fibrosarcoma HT 1080 cells. From the EtOAc-soluble fraction, eight new phenylbutanoids, cassumunols A-H, were isolated together with 30 known constituents. The structures of new phenylbutanoids were elucidated on the basis of chemical and physicochemical evidence. Principal constituents were examined the inhibitory effects on the invasion of HT 1080 cells. Among them, phlain I and III, (E)-1-(3,4-dimethoxyphenyl)buta-1,3-diene, (E)-1-(2,4,5-trimethoxyphenyl)buta-1,3-diene, and (-)-ß-sesquiphellandrene showed anti-invasion effects. Interestingly, (E)-1-(2,4,5-trimethoxyphenyl)buta-1,3-diene [inhibition (%) 46.8 ± 7.2 (p<0.05) at 30 µM] significantly inhibited the invasion, and only a weak cytotoxic effect was observed.
Asunto(s)
Butanoles/química , Extractos Vegetales/química , Zingiberaceae/química , Butanoles/aislamiento & purificación , Butanoles/toxicidad , Línea Celular Tumoral , Fibrosarcoma/tratamiento farmacológico , Humanos , Espectroscopía de Resonancia Magnética , Conformación Molecular , Invasividad Neoplásica/prevención & control , Neoplasias de Tejido Conjuntivo/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Extractos Vegetales/toxicidad , Rizoma/químicaRESUMEN
The methanolic (MeOH) extract from the rhizomes of Zingiber cassumunar showed nitric oxide (NO) production inhibitory effects induced by lipopolysaccharide (LPS) in mouse peritoneal macrophages. From the MeOH extract, six new phenylbutanoids, phlains I-VI, were isolated together with 16 known constituents. The structures of new phenylbutanoids were determined on the basis of physicochemical and chemical evidence. In addition, the inhibitory effects of the principal constituents on the NO production were examined. Among them, phlain III (IC50=24 microM), (E)-1-(3,4-dimethoxyphenyl)buta-1,3-diene (69 microM), (E)-1-(2,4,5-trimethoxyphenyl)buta-1,3-diene (83 microM), and cassumunaquinone 1 (47 microM) were found to show the inhibitory effects.