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Authors Zhang L, Hou S, Li B, Pan J, Jiang L, Zhou G, Gu H, Zhao C, Lu H, Ma F
Received 18 October 2017
Accepted for publication 6 December 2017
Published 15 January 2018 Volume 2018:11 Pages 361—373
DOI https://doi.org/10.2147/OTT.S154412
Checked for plagiarism Yes
Review by Single-blind
Peer reviewer comments 2
Editor who approved publication: Dr Ingrid Espinoza
Background: Betulinic acid (BA) is a complex lupane triterpenoid with unique
antineoplastic activity. However, its antiproliferative activity is far from
satisfaction. In order to improve its anticancer efficacy, betulinic acid was
conjugated with a nitric oxide (NO)-releasing moiety to get a novel hybrid,
BA-78.
Methods: The antiproliferative activity of BA-78 against
6 cell lines and the ability of releasing nitric oxide were determined. The
pro-apoptosis mechanism of BA-78 was investigated as well.
Results: BA-78 exhibited time-dependent release of NO, and it
displayed higher antiproliferative potential than BA through increasing
apoptosis and inducing cell cycle arrest at G1 phase. Western blotting results
showed that BA-78 increased the expression of Bax, Bid, Bad and cytochrome C
and reduced the level of anti-apoptosis proteins including Bcl-2 and Bcl-xl.
Conclusion: Our study revealed that novel compound BA-78,
possessing betulinic acid and nitric oxide (NO)-releasing moiety, could be
developed as an antitumor agent.
Keywords: lupane
triterpenoid, nitric oxide, anticancer, apoptosis, NONOate, Bcl-2 family