Comparison of cytotoxicity and DNA damage potential induced by ent-kaurene diterpenoids from Isodon plant.

Abstract:

:The cytotoxicity of six ent-kaurene diterpenoids isolated from the leaves of Isodon japonica (Burm.f.) Hara var. galaucocalyx (maxin) Hara was evaluated against three human tumour HepG2, GLC-82 and HL-60 cell lines through SRB assay, and their DNA damage potential (against HepG2 cell line) was assessed by comet assay. Among the six ent-kaurene diterpenoids, Rabdosin B was most cytotoxic, followed by Oridonin, Epinodosin, Rabdosinate, Lasiokaurin and Epinodosinol. All of the six ent-kaurene diterpenoids induced significant DNA damage (p < 0.05) to HepG2 cells in a time- and dose-dependent manner except Lasiokaurin and Eponodosinol at 6 µmol L⁻¹ for 24 h. The structure-activity relationships (SARs) were discussed and it was found that exo-methylene cyclopentanone in the molecular structure was important for maintaining the cytotoxicity and DNA damage potential of the compounds.-OAc group at site C-1 in Lasiokaurin had a higher stereospecific blockade, which made the compound have less cytotoxicity and DNA damage potential than Oridonin (-OH at C-1).

journal_name

Nat Prod Res

journal_title

Natural product research

authors

Ding L,Zhou Q,Wang L,Wang W,Zhang S,Liu B

doi

10.1080/14786410802267734

subject

Has Abstract

pub_date

2011-09-01 00:00:00

pages

1402-11

issue

15

eissn

1478-6419

issn

1478-6427

pii

913191477

journal_volume

25

pub_type

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