Cassaine Diterpenoid Amide from Stem Bark of <i>Erythrophleum fordii</i> Suppresses Cytotoxic and Induces Apoptosis of Human Leukemia Cells
Tu Thanh Thi Nguyen,
Dao Cuong To,
Phuong Hien Thi Vo,
Thanh Hoa Tran,
Phi Hung Nguyen,
Hien Minh Nguyen,
Manh Hung Tran
Affiliations
Tu Thanh Thi Nguyen
Traditional Medicine Faculty, Hanoi Medical University, 1 Ton That Tung street, Dong Da District, Hanoi 116001, Vietnam
Dao Cuong To
Faculty of Pharmacy, Phenikaa University, Yen Nghia, Ha Dong district, Hanoi 12116, Vietnam
Phuong Hien Thi Vo
Faculty of Biology and Biotechnology, University of Science, Vietnam National University Hochiminh City, 227 Nguyen Van Cu street, District 5, Ho Chi Minh City 748000, Vietnam
Thanh Hoa Tran
Biomedical Science Department, VNUK Institute for Research & Executive Education, The University of Danang, 158A Le Loi street, Hai Chau District, Danang City 551000, Vietnam
Phi Hung Nguyen
Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet street, Cau Giay District, Hanoi 122100, Vietnam
Hien Minh Nguyen
Faculty of Pharmacy, Ton Duc Thang University, 19 Nguyen Huu Tho street, District 7, Ho Chi Minh City 758307, Vietnam
Manh Hung Tran
Faculty of Chemistry, University of Science, Vietnam National University Ho Chi Minh city, 227 Nguyen Van Cu Street, District 5, Ho Chi Minh City 748000, Vietnam
Cassaine diterpenoids amides from the stem bark of Vietnamese Erythrophleum fordii Oliver were screened for their cytotoxic activity against human cancer cells. The cell proliferation assay results showed that, among the active compounds, 3β-acetyl-nor-erythrophlamide (3AEP) exhibited the most potential cytotoxicity against human leukemia HL-60 and KG cells with IC50 values of 12.0 ± 1.2 and 18.1 ± 2.7 µM, respectively. Treatment of 3AEP resulted in the apoptosis of HL-60 cells via the activation of caspase 3, and poly (ADP-ribose) polymerase (PARP). Molecular docking in silico results showed that the 3AEP can bind to both the procaspase-3 allosteric site and the PARP-1 active site, with binding energies of −7.51 and −9.63 kcal/mol respectively. These results indicated that the stem bark of Vietnamese E. fordii and its cassaine diterpenoid amides may be useful in the apoptosis induction of human leukemia cancer cells.