Project's information

Project's title Research on isolation process of acetogenin and other bioactive compounds and their cancer activities from Annona glabra
Research hosting institution Institute of Marine Biochemistry (IMBC)
Project leader’s name Nguyen Xuan Nhiem
Project duration 01/01/2013 - 01/01/2014
Project’s budget 500.000.000 Vnd
Classify Excellent
Goal and objectives of the project

- Isolation process of acetogenin from Annona glabra.
- Isolation other bioactive compounds from Annona glabra
- Evaluation acetogenin and isolated compounds on cancer cell lines in vitro

Main results

Theoretical results:
- Collected fresh fruits (10 kg) of and leaves (25 kg).
- Isolation process of acetogenin (MeOH extract (20 g)/time).
- Identified the physical characters and structure of acetogenin (squamocin M).
- Isolated squamocin M for in vitro assay (10,93 g).
- Isolated 22 compounds (5 new and 17 known) from the fruits of Annonaglabra.
- Semisynthesis of six squamocin M derivatives.
- Evaluated inhibitory growth of the methanol extracts of fruit and leaves A. glabra on LU-1 and KB cancer cell lines activities.
- Evaluated cytotoxic activity of 22 isolated compounds and six squamocin M derivatives on LU-1, MCF-7, SK-Mel2, and KB cancer cell lines. Compounds 3, 4, and 6 showed significant cytotoxic activities with the IC50 ranging from 0.65 to 7.34 µM. The results of cytotoxic activity of six squamocin M derivatives indicated that tetrahydrofuran with α-hydroxyl group played important on cytotoxic activity.
- Compounds 15 and 22 exhibited inhibitory cytotoxic activity on HL-60 cancer cell line with IC50 of 9.02 and 8.72 µM, respectively. They are did not inhibit the growth of HEL-299 normal cell line. Further studies showed that these compounds killed HL-60 cell line as apoptosis mechanism.
- Compounds 1-22 were also evaluated inflammatory activity. The results indicated compounds 3 and 12 showed the inhibitory NO production, with IC50 values of 0.01 and 0.10, respectively.

34.2015nguyenxuannhiem

34.2015nguyenxuannhiem1

Novelty and actuality and scientific meaningfulness of the results

- Isolated 22 compounds including 5 new and 17 known compounds from the fruits of Annonaglabra.
- Isolation process of acetogenin (20 g of MeOH extract/time).
- Compounds 3, 4, and 6 showed significant cytotoxic activities with the IC50 ranging from 0.65 to 7.34 µM.
- Compounds 15 and 22 exhibited inhibitory cytotoxic activity on HL-60 cancer cell line with IC50 of 9.02 and 8.72 µM, respectively. They are did not inhibit the growth of HEL-299 normal cell line.
- Compounds 1-22 were also evaluated inflammatory activity. The results indicated compounds 3 and 12 showed the inhibitory NO production, with IC50 values of 0.01 and 0.10, respectively.

Products of the project

With the presence results, the project have published 01 SCI, 02 SCI-E papers and 2 Vietnam national papers. In addition, the project will contribute to train one PhD student.

Research region

The members of project would like to thank Vietnam Academy of Science and Technology and Institute of Marine Biochemisry have supported the finance. The authors respectfully request VAST and IMBC help us to continue to research and develop pharmaceutical products to serve public health.