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Cancer chemopreventive activity of compounds isolated from Waltheria indica.

Abstract：

ETHNOPHARMACOLOGICAL RELEVANCE:Waltheria indica L. is traditionally used in several countries against inflammatory related diseases and cancer, mainly as a decoction of the aerial parts. AIM OF THE STUDY:The transcription factor NF-κB is known to induce tumor promotion and progression and is considered a major player in inflammation-driven cancers. Therefore, inhibitors of this pathway possess cancer chemopreventive and chemotherapeutic activities. This study aimed first to confirm the use of Waltheria indica as a traditional anti-inflammatory remedy by assessing the NF-κB inhibitory activity and then to identify the major bioactive compounds. The isolated compounds were also tested for their QR inducing property, a complementary strategy in cancer chemoprevention able to target tumor initiation. Finally, the relevance of in vitro results was examined by investigating the occurrence of the active compounds in traditional preparations. MATERIALS AND METHODS:Compounds were isolated from the dichloromethane extract of the aerial parts using flash chromatography and semi-preparative HPLC. NF-κB inhibitory activity of pure compounds from Waltheria indica was assessed using a luciferase reporter assay in HEK293 cells. Their QR inducing activity was also assessed in Hepa1c1c7 cells. RESULTS:Twenty-nine compounds, of which 5 are new, were obtained from the dichloromethane extract and tested for their cancer chemoprevention activity. Eleven compounds inhibited NF-κB and/or induced QR in the low to mid µM range. Chrysosplenol E (20) was active in both tests. Two of the most potent NF-κB inhibitors, waltherione A (4) and waltherione C (5), as well as 20 were found in the traditional decoction, in which 4 and 5 were major compounds. CONCLUSION:The presence of potent NF-κB inhibitors and QR inducing compounds in the decoction of the aerial parts of Waltheria indica supports its traditional use in inflammatory-related diseases and cancer chemoprevention.

journal_name

J Ethnopharmacol

journal_title

Journal of ethnopharmacology

authors

Monteillier A,Cretton S,Ciclet O,Marcourt L,Ebrahimi SN,Christen P,Cuendet M

doi

10.1016/j.jep.2017.03.048

subject

Has Abstract

pub_date

2017-05-05 00:00:00

pages

214-225

eissn

0378-8741

issn

1872-7573

pii

S0378-8741(16)31399-X

journal_volume

203

pub_type

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Cancer chemopreventive activity of compounds isolated from Waltheria indica.