Journal
ONCOTARGETS AND THERAPY
Volume 11, Issue -, Pages 361-373Publisher
DOVE MEDICAL PRESS LTD
DOI: 10.2147/OTT.S154412
Keywords
lupane triterpenoid; nitric oxide; anticancer; apoptosis; NONOate; Bcl-2 family
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Funding
- Outstanding Leaders Training Program of Pudong Health Bureau of Shanghai [PWR12015-06, PWRd2017-11]
- program of Shanghai Pudong Hospital [201602]
- Fudan University
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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.
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