Chemical constituents of the Annona glabra fruit and their cytotoxic activity

Nguyen Thi Thu Hien, Nguyen Xuan Nhiem, Duong Thi Hai Yen, Dan Thi Thuy Hang, Bui Huu Tai, Tran Hong Quang, Hoang Le Tuan Anh, Phan Van Kiem, Chau Van Minh, Eun Ji Kim, Seung Hyun Kim, Hee Kyoung Kang, Young Ho Kim

Research output: Contribution to journalArticlepeer-review

20 Citations (Scopus)


Context: Traditional Chinese medicines have attracted increasing interest as potential sources of novel drugs with a wide range of biological and pharmacological activities. Annona glabra Linn (Annonaceae) is used in traditional medicine as an anticancer drug. Phytochemical investigation of this plant led to the isolation of acetogenins, ent-kauranes, peptides, and alkaloids. In addition, compounds exhibited anticancer, anti-HIV-reserve, and antimalaria. Objective: Isolation, structure determination, and cytotoxic activity evaluation of compounds from the methanol extract from A. glabra fruits. Materials and methods: Using chromatographic methods to isolate compounds from the A. glabra methanol extract. The cytotoxic activity of compounds was evaluated by a 3-[4,5- dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. In addition, compounds which showed significant cytotoxic activity were chosen for further study apoptosis characteristics. Results: One new, (2E,4E,1'R,3'S,5'R,6'S)-dihydrophaseic acid 1,3'-di-O-β-D-glucopyranoside, and eight known compounds, (2E,4E,1'R,3'S,5'R,6'S)-dihydrophaseic acid 3'-O-β-D-glucopyranoside (2), icariside D2 (3), icariside D2 6'-O-β-D-xylopyranoside (4), 3,4-dimethoxyphenyl O-β-Dglucopyranoside (5), 3,4-dihydroxybenzoic acid (6), blumenol A (7), cucumegastigmane I (8), and icariside B1 (9), were isolated from the fruits of A. glabra. Icariside D2 (3) was found to show significant cytotoxic activity on the HL-60 cell line with the IC50 value of 9.0 ± 1.0 μM and did not show cytotoxic activity on the Hel-299 normal cell line. The further test indicated that compound 3 induced apoptosis via alteration of expression of apoptosis-related proteins and decreased phosphorylation of AKT in HL-60 cells. Discussion and conclusion: The results suggested that the constituents from A. glabra may contain effective compounds which can be used as anticancer agents.

Original languageEnglish
Pages (from-to)1602-1607
Number of pages6
JournalPharmaceutical Biology
Issue number11
Publication statusPublished - 2015

Bibliographical note

Funding Information:
The authors report that they have no conflicts of interest. This research was supported by Vietnam Academy of Science and Technology (VAST 04.04/13-14) and by a grant from the Priority Research Center Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (2009-0093815), Republic of Korea.

Publisher Copyright:
© 2015 Informa Healthcare USA, Inc.

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine


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