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A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation.

Xu B, Chu F, Zhang Y, Wang X, Li Q, Liu W, Xu X, Xing Y, Chen J, Wang P, Lei H - Int J Mol Sci (2015)

Bottom Line: A combination of fluorescence staining observation and flow cytometric analysis indicated that 4a could induce HepG2 cell apoptosis.Further studies suggested that 4a-induced apoptosis is mediated through depolarization of the mitochondrial membrane potential and increase of intracellular free Ca2+ concentration.In addition, the structure-activity relationships of these derivatives were briefly discussed.

View Article: PubMed Central - PubMed

Affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. weichenxubing@126.com.

ABSTRACT
A series of novel ligustrazine-triterpenes derivatives was designed, synthesized and screened for their cytotoxicity against five cancer cell lines (Bel-7402, HepG2, HT-29, Hela, and MCF-7) and Madin-Darby canine kidney (MDCK). Current study suggested that most of the ligustrazine-triterpenes conjunctions showed better cytotoxicity than the starting materials. In particular, compound 4a exhibited better cytotoxic activity (IC50<5.23 μM) against Bel-7402, HT-29, MCF-7, Hela, and HepG2 than the standard anticancer drug cisplatin (DDP). The cytotoxicity selectivity detection revealed that 4a exhibited low cytotoxicity (IC50>20 μM) towards MDCK cells. A combination of fluorescence staining observation and flow cytometric analysis indicated that 4a could induce HepG2 cell apoptosis. Further studies suggested that 4a-induced apoptosis is mediated through depolarization of the mitochondrial membrane potential and increase of intracellular free Ca2+ concentration. In addition, the structure-activity relationships of these derivatives were briefly discussed.

No MeSH data available.


Related in: MedlinePlus

Cytotoxicity of 4a against HepG2 tumor cells and MDCK cells. The cytotoxicity of 4a was determined by MTT assay.
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ijms-16-21035-f001: Cytotoxicity of 4a against HepG2 tumor cells and MDCK cells. The cytotoxicity of 4a was determined by MTT assay.

Mentions: The treatment with increased doses of 4a (Figure 1) by MTT assay showed that the inhibition rate against MDCK was just about 26.50% at the concentration of 10 μM, while the inhibition rate against human hepatoma cell HepG2 was up to 99.87% at the same concentration. Therefore, at least in part, compound 4a had cytotoxicity selectively to human hepatocellular carcinoma cells in vitro.


A Series of New Ligustrazine-Triterpenes Derivatives as Anti-Tumor Agents: Design, Synthesis, and Biological Evaluation.

Xu B, Chu F, Zhang Y, Wang X, Li Q, Liu W, Xu X, Xing Y, Chen J, Wang P, Lei H - Int J Mol Sci (2015)

Cytotoxicity of 4a against HepG2 tumor cells and MDCK cells. The cytotoxicity of 4a was determined by MTT assay.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4613240&req=5

ijms-16-21035-f001: Cytotoxicity of 4a against HepG2 tumor cells and MDCK cells. The cytotoxicity of 4a was determined by MTT assay.
Mentions: The treatment with increased doses of 4a (Figure 1) by MTT assay showed that the inhibition rate against MDCK was just about 26.50% at the concentration of 10 μM, while the inhibition rate against human hepatoma cell HepG2 was up to 99.87% at the same concentration. Therefore, at least in part, compound 4a had cytotoxicity selectively to human hepatocellular carcinoma cells in vitro.

Bottom Line: A combination of fluorescence staining observation and flow cytometric analysis indicated that 4a could induce HepG2 cell apoptosis.Further studies suggested that 4a-induced apoptosis is mediated through depolarization of the mitochondrial membrane potential and increase of intracellular free Ca2+ concentration.In addition, the structure-activity relationships of these derivatives were briefly discussed.

View Article: PubMed Central - PubMed

Affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. weichenxubing@126.com.

ABSTRACT
A series of novel ligustrazine-triterpenes derivatives was designed, synthesized and screened for their cytotoxicity against five cancer cell lines (Bel-7402, HepG2, HT-29, Hela, and MCF-7) and Madin-Darby canine kidney (MDCK). Current study suggested that most of the ligustrazine-triterpenes conjunctions showed better cytotoxicity than the starting materials. In particular, compound 4a exhibited better cytotoxic activity (IC50<5.23 μM) against Bel-7402, HT-29, MCF-7, Hela, and HepG2 than the standard anticancer drug cisplatin (DDP). The cytotoxicity selectivity detection revealed that 4a exhibited low cytotoxicity (IC50>20 μM) towards MDCK cells. A combination of fluorescence staining observation and flow cytometric analysis indicated that 4a could induce HepG2 cell apoptosis. Further studies suggested that 4a-induced apoptosis is mediated through depolarization of the mitochondrial membrane potential and increase of intracellular free Ca2+ concentration. In addition, the structure-activity relationships of these derivatives were briefly discussed.

No MeSH data available.


Related in: MedlinePlus