Pectinesterase inhibitor from jelly fig (Ficus awkeotsang Makino) achene induces apoptosis of human leukemic U937 cells.

Abstract

The antitumor activity of pectinesterase inhibitor (PEI), a group of cationic polypeptides, from jelly fig (Ficus awkeotsang Makino) achene was first examined as a treatment for leukemia in this study. PEI displayed strong growth inhibition against human leukemic U937 cells via induction of apoptosis in a dose- and time-dependent manner. At a level of 50 microg/mL, PEI inhibited 90% of cell growth, and the concentration of PEI required to induce 50% of cell viability (LC50) was about 180 microg/mL. Meanwhile, cell cycle arrest at G2/M phase was observed when cells were incubated with 100 microg PEI/mL for 24 h. PEI displayed a dose-dependent influence on mitochondria transmembrane potential (MTP, delta psi m) of cells when detected by a flow cytometry. MTP of more than 50% cells was reduced when cells were incubated with PEI at levels higher than 50 microg PEI/mL for 24 h. In addition, PEI upregulated caspase-3 activity. Taken together, PEI potently inhibited the proliferation of human leukemic U937 cells via cell cycle arrest and apoptosis in association with MTP reduction and caspase-3 activation, respectively, and showed therapy potential for U937 cells.

• Authors: Jia-Huei Chang, Yuh-Tai Wang, Hung-Min Chang
• Journal: Annals of the New York Academy of Sciences (Ann N Y Acad Sci) Vol. 1042 Pg. 506-15 (May 2005) ISSN: 0077-8923 [Print] United States
• PMID: 15965097 (Publication Type: Journal Article)

Chemical References

• Annexin A5
• Enzyme Inhibitors
• Carboxylic Ester Hydrolases
• pectinesterase
• CASP3 protein, human
• Caspase 3
• Caspases

Topics

• Annexin A5 (metabolism)
• Apoptosis (drug effects)
• Carboxylic Ester Hydrolases (antagonists & inhibitors, metabolism)
• Caspase 3
• Caspases (metabolism)
• Enzyme Inhibitors (pharmacology)
• Ficus (chemistry)
• Fruit (chemistry)
• Humans
• Leukemia (metabolism, pathology)
• Mitochondria (drug effects, metabolism)
• U937 Cells