Structure–activity relationships of eight ent-kaurene diterpenoids from three Isodon plants

Structure–activity relationships of eight ent-kaurene diterpenoids from three Isodon plants Eight ent-kaurene diterpenoids were isolated from three Isodon plants, Isodon excisoides (Sun ex C. H. Hu) C. Y. Wu et H. W. Li, Isodon weisiensis C. Y. Wu, and Isodon racemosa (Hemsl.) Hara. Their cytotoxicities were tested by SRB assay against four human tumor cell lines, HepG2, Tb, HO-8910 and SGC-7901. The DNA damage degrees on their Hep G2 cells were evaluated by Comet assay. The results showed that ent-kaurene diterpenoids were selectively toxic against these four tumor cell lines. Weisiensic C had the lowest cytotoxicity against four cell lines and degree of DNA damage on the Hep G2 cell line. Leukamenin E and Glaucocalyxin A had similar IC50 values and also induced a similar degree of DNA damage. The cytotoxicity and degree of DNA damage of eight ent-kaurene diterpenoids on Hep G2 was in the order Leukamenin E > Glaucocalyxin A > Wangzaozin A > Kamebanin > Macrocalyxin D > Weisiensin B > Excisanin K > Weisiensic C. The structure–activity relationships indicated that there was some correlation between the substituents and their structures of ent-kaurene diterpenoids and their activities on Hep G2 cells. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Structure–activity relationships of eight ent-kaurene diterpenoids from three Isodon plants

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Publisher
Springer Netherlands
Copyright
Copyright © 2010 by Springer Science+Business Media B.V.
Subject
Chemistry; Inorganic Chemistry ; Physical Chemistry ; Catalysis
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-010-0144-3
Publisher site
See Article on Publisher Site

Abstract

Eight ent-kaurene diterpenoids were isolated from three Isodon plants, Isodon excisoides (Sun ex C. H. Hu) C. Y. Wu et H. W. Li, Isodon weisiensis C. Y. Wu, and Isodon racemosa (Hemsl.) Hara. Their cytotoxicities were tested by SRB assay against four human tumor cell lines, HepG2, Tb, HO-8910 and SGC-7901. The DNA damage degrees on their Hep G2 cells were evaluated by Comet assay. The results showed that ent-kaurene diterpenoids were selectively toxic against these four tumor cell lines. Weisiensic C had the lowest cytotoxicity against four cell lines and degree of DNA damage on the Hep G2 cell line. Leukamenin E and Glaucocalyxin A had similar IC50 values and also induced a similar degree of DNA damage. The cytotoxicity and degree of DNA damage of eight ent-kaurene diterpenoids on Hep G2 was in the order Leukamenin E > Glaucocalyxin A > Wangzaozin A > Kamebanin > Macrocalyxin D > Weisiensin B > Excisanin K > Weisiensic C. The structure–activity relationships indicated that there was some correlation between the substituents and their structures of ent-kaurene diterpenoids and their activities on Hep G2 cells.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Jun 12, 2010

References

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