title: Chemical constituents of the Annona glabra fruit and their cytotoxic activity.
abstract: BACKGROUND
  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.
  
  
  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-d-glucopyranoside (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.
  
  
  CONCLUSIONS
  The results suggested that the constituents from A. glabra may contain effective compounds which can be used as anticancer agents.
authors: Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST) , Caugiay, Hanoi , Vietnam .
authors: Nguyen Thi Thu
authors: NT
authors: Hien
authors: Nguyen Xuan
authors: NX
authors: Nhiem
authors: Duong Thi Hai
authors: DT
authors: Yen
authors: Dan Thi Thuy
authors: DT
authors: Hang
authors: Bui Huu
authors: BH
authors: Tai
authors: Tran Hong
authors: TH
authors: Quang
authors: Hoang Le
authors: HL
authors: Tuan Anh
authors: Phan Van
authors: PV
authors: Kiem
authors: Chau Van
authors: CV
authors: Minh
authors: Eun-Ji
authors: EJ
authors: Kim
authors: Seung Hyun
authors: SH
authors: Kim
authors: Hee Kyoung
authors: HK
authors: Kang
authors: Young Ho
authors: YH
authors: Kim
mesh_terms: D031041:Annona; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000302:isolation & purification* / Q000633:toxicity; D049109:Cell Proliferation / Q000187:drug effects; D003603:Cytotoxins / Q000737:chemistry* / Q000302:isolation & purification* / Q000633:toxicity; D005638:Fruit; D018922:HL-60 Cells; D006801:Humans; D010936:Plant Extracts / Q000737:chemistry* / Q000302:isolation & purification* / Q000633:toxicity
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003603:Cytotoxins; D010936:Plant Extracts
keywords: Annonaceae; HL-60; apoptosis