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Aim To investigate the antitumor effects of cimigenol ( KY17 ) , a novel cycloartane triterpenoid from Cimicifuga , in human colon cancer cells (HCT116).Methods MTT assay was used to deter-mine the effect of KY17 on the proliferation of mouse embryonic fibroblasts ( MEF) and human colon cancer HCT116 cell line.Flow cytometry was employed to de-tect the effect of KY17 on HCT116 cell cycle.Fluores-cence microscopy and flow cytometry were used to ana-lyze the apoptosis .Western blot was used to detect the expression of apoptotic protein (PARP).q-PCR ana-lyzed the expression of miRNA-34a.Results The IC50 of KY17 in MEF and HCT116 cells was 27.28 μmol· L-1 and 9.31μmol· L-1 , respectively.KY17 induced HCT116 cell cycle arrest in G2/M phase and the apoptotic protein PARP cleavage . In addition, KY17 up-regulated the expression of p 53 protein and miRNA-34a.Conclusions KY17 inhibits the prolifera-tion and the cell cycle is arrested in G 2/M, inducing the apoptosis of HCT116 cells. The mechanism is probably related to miRNA-34a up-regulation and p53 activation .
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OBJECTIVE To investigate the effect of root saponins of Panax notoginseng(RPNS) on different voltage-dependent calcium and potassium ion channels. METHODS By using the two-elec?trode voltage clamp (TEVC), the effect of RPNS 0.01, 0.06, 0.1, 0.6, 1 and 4 g · L- 1 was investigated on Cav1.2,and the effect of RPNS 1 g · L-1 was evaluated on Cav2.1,Cav2.2,Cav3.1, KCNH2,KCNQ1,KCNQ1/KCNE1 and BK channel. All the ion channels examined were expressed in Xenopus laevis oocytes. RESULTS TEVC suggested that the effect of RPNS on Cav1.2 exhibited the concentration-response relationship and its EC50 was 0.048 g · L-1. Compared with cell control,TEVC also showed that RPNS 1 g·L-1 had obviously inhibitory effect on Cav1.2,Cav2.2 and Cav3.1,and the inhibitory rate of RPNS 1 g · L-1 on the peak current of Cav1.2,Cav2.2 and Cav3.1 was(57.1 ± 8.6)%, (17.2 ± 0.7)% and(50.2 ± 7.7)%(P<0.01),respectively. RPNS 1 g · L-1 had obviously activated effect on BK channel,and the activated rate of RPNS 1 g·L-1 on the peak current of BK channel was(37.9± 2.7)%(P<0.01). RPNS 1 g·L-1 showed no significant effect on Cav2.1,KCNH2,KCNQ1 and KCNQ1/KCNE1. CONCLUSION RPNS may effectively inhibit Cav1.2 and Cav3.1,activate BK channel,but have little effect on Cav2.1,Cav2.2,KCNH2,KCNQ1 and KCNQ1/KCNE1.
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AIM@#To study the 9, 19-cycloartane triterpenes from the roots of Cimicifuga foetida.@*METHOD@#Chromatographic separations by silica gel, C18 reversed phase silica gel, and high-performance liquid chromatography (HPLC) were used. All of the structures were elucidated on the basis of spectroscopic analysis and chemical methods.@*RESULTS@#Five 9, 19-cycloartane triterpenes, (3β, 12β, 15α, 24R)-12, 2'-diacetoxy-24, 25-epoxy-15-hydroxy-16, 23-dione-3-O-α-L-arabinopyranoside (1), actein (2), 23-epi-26-deoxyactein (3), asiaticoside B (4), and 12β-hydroxycimigenol (5) were isolated from the roots of Cimicifuga foetida.@*CONCLUSION@#Compound 1 is a new triterpene with two acetoxy groups at C-2' and C-12.