ABSTRACT
Objective: To investigate the chemical compositions and anticancer activity of Mollugo pentaphylla. Methods: These compounds were isolated by various technologies, such as silica gel, Sephadex LH-20 and high performance liquid chromatography. Their structures were elucidated on the basis of physicochemical properties and spectroscopic data. The cytotoxic activities of compounds 1-5 against five cancer cell lines were tested by MTT. Results: Six compounds were isolated from this plant and identified as mollugoside E (1), 3-O-[α-L-rhamnopyranosy1 (1→2)-α-L-arabinopyranosyl]-28-O-[β-D-glucopyranosyl (1→6)-β-D- glucopyranosyl]oleanolic acid (2), raddeanoside R8 (3), raddeanin A (4), mollugogenol A (5), and oleanolic acid (6). The cytotoxic activities results showed that compounds 1-5 had certain inhibitory effects on human prostate cancer DU145 cell lines, cervical cancer Hela cell lines and early-juvenile leukemia HL 60 cell lines, especially on HL 60 cells with IC50 value of 10.21, 38.43, 40.28, 20.59, and 83.16 μmol/L, respectively. Conclusion: Compound 1 is a new triterpenoid saponin and compounds 2-4 are isolated first time from M. pentaphylla. The cytotoxic activities results showed that compounds 1-5 had certain inhibitory effects on DU145, Hela and HL 60 cell lines.
ABSTRACT
Objective To explore raddeanin A(RA) inhibiting the proliferation of HCT116 cells and its related mechanism.Methods The MTT method was used to observe the RA inhibition on the proliferation of gastric cancer cells HCT116.Flow cytometry was used to detect the RA effects on cell apoptosis.Transmission electron microscope(TEM) was used to observe RA induced autophagy.Western blot was used to test expression of apoptosis and autophagy related proteins.Results RA could significantly inhibit the proliferation of HCT16 cells with concentration and time dependence;double layer membrane of autophagosome was detected by TEM;FCM showed that RA induced apoptosis in HCT116 cells,moreover the apoptosis rate was increased with the concentration increase;Western blot showed that the expression of autophagy related proteins(Beclin1 and LC3) was increased,the expression of apoptosis inhibition protein Bcl-2 was decreased.On the contrary,the expression of apoptosis promotion proteins(Bax,Cleaved-caspase-3,Cleaved-PARP) was increased,the expression of mTOR protein in the mTOR signal pathway was increased,while the p-mTOR protein expression was decreased.When the mTOR pathway inhibitor rapamycin(RAPA) was added to cells,Beclin-1,LC3,Cleaved-caspase-3,Cleaved-PARP proteins were increased,and apoptosis rate was also increased.Conclusion RA can inhibit the proliferation of HCT116 cells and can induce cellular autophagy and apoptosis,its mechanism may be realized by regulating the mTOR signal pathway.
ABSTRACT
[Objective]To review the antitumor progress of Raddeanin A in nearly 10 years. [Method] Col ecting the antitumor research literature about Raddeanin A for nearly 10 years, describing its antitumor research mechanism, such as inducting of cellapoptosis blocking the cellcycle, blocking STATs signaling pathways and inhibiting the tumor angiogenesis. [Result] Raddeanin A could induce the H460 cellapoptosis, block LoVo cellcycle and STATs signaling pathways of LoVo cells, and inhibit HepG-2 cellangiogenesis. [Conclusion] The antitumor mechanism of Raddeanin A could be inducting of cellapoptosis, blocking the cellcycle, blocking STATs signaling pathways and inhibiting the tumor angiogenesis.