doi:10.3850/978-981-08-7615-9_BS09


Identification and Evaluation of Apoptotic Compounds from Garcinia Oligantha with Caspase-3 Fret Biosensor


Ting Yu1, Xue Mei Gao2, Hong Xi Xu2,a and Kathy Qian Luo1,b

1Division of Bioengineering, School of Chemical and Biomedical Engineering, Nanyang Technological University, 70 Nanyang Drive, Singapore 637459.

bkluo@ntu.edu.sg

2Chinese Medicine Laboratory, Hong Kong Jockey Club Institute of Chinese Medicine, Shatin, N.T., Hong Kong, People’s Republic of China

axuhongxi88@gmail.com

ABSTRACT

Ten compounds were isolated from the stems and leaves of Garcinia oligantha. These compounds were evaluated for their apoptosis-inducing effects using HeLa-C3 cells which were genetically engineered to produce a fluorescent biosensor capable of detecting caspase-3 activation. Among ten tested compounds, six of them were found to be strong apoptotic inducers, which induced cell apoptosis at 10 μM or lower concentrations. Especially, compound 1 and 2 could induce HeLa-C3 cell apoptosis at 2.5 μM and compound 3 at 5 μM. Moreover, MTT assay showed that compound 1, 2 and 3 were effective in inhibiting cell proliferation and their 72 h IC50 values in cervical cancer HeLa cells were determined to be 0.9 μM, 1.58 μM and 1.52 μM, respectively. The apoptotic activity of compound 1, 2 and 3 was further confirmed by Western blot analysis in detecting the cleavage of PARP, which is the endogenous substrate of caspase-3, in HeLa cells treated with these compounds. All these findings show that compound 1, 2 and 3 are potent apoptosis inducers and should be further studied for discovering their anticancer effects as well as the molecular mechanism of anticancer action.



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