ABSTRACT
@#This study investigated the anti-angiogenic activities of two diarylheptanoids, together with a structure analogue, curcumin. The activity and toxicity of these three compounds were compared using transgenic zebrafish as in vivo model and human umbilical vein endothelial cell(HUVEC)as in vitro model. Anti-angiogenic index(AI)was used as the ratio between LC50 and EC50. The results suggested that in both in vitro and in vivo assay, curcumin exerted the most potent anti-angiogenic effect but with lowest toxicity among these compounds; Yakuchinone A was the second potent; Yakuchinone B has the lowest activity but with the highest toxicity in all three compounds. Taken together, curcumin was the best angiogenic inhibitor in these three diarylheptanoids.
ABSTRACT
AIM@#To study the chemical constituents of the rhizomes of Alpinia officinarum Hance.@*METHOD@#Compounds were isolated by repeated column chromatography, and their structures were elucidated on the basis of spectral analysis. The cytotoxic activities of these compounds were evaluated with the T98G and B16F10 cell lines by the MTT assay.@*RESULTS@#A dimeric diarylheptanoid, named alpinin B (1), along with three known diarylheptanoids were obtained, and their structures were identified as alpinin B (1), 1, 7-diphenyl-3,5-heptanedione (2), (4E)-1, 7-diphenylhept-4-en-3-one (3) and (4E)-7- (4-hydroxyphenyl)-1-phenylhept-4-en-3-one (4).@*CONCLUSION@#Compound 1 is a new dimeric diarylheptanoid. The biosynthetic pathway of 1 was speculated to originate from a Michael reaction between compounds 2 and 3. Compound 3 showed cytotoxicity against the human glioblastoma T98G cell line with IC50 of 27 μmol·L(-1).