J Ethnopharmacol. 2017 Mar 27. pii: S0378-8741(16)31399-X. doi: 10.1016/j.jep.2017.03.048. [Epub ahead of print]
- 1
- School
of Pharmaceutical Sciences, University of Geneva, University of
Lausanne, CMU - Rue Michel-Servet 1, 1211 Geneva 4, Switzerland.
Electronic address: Aymeric.Monteillier@unige.ch.
- 2
- School
of Pharmaceutical Sciences, University of Geneva, University of
Lausanne, CMU - Rue Michel-Servet 1, 1211 Geneva 4, Switzerland.
Electronic address: Sylvian.Cretton@unige.ch.
- 3
- School
of Pharmaceutical Sciences, University of Geneva, University of
Lausanne, CMU - Rue Michel-Servet 1, 1211 Geneva 4, Switzerland.
Electronic address: Olivier.Ciclet@unige.ch.
- 4
- School of
Pharmaceutical Sciences, University of Geneva, University of Lausanne,
CMU - Rue Michel-Servet 1, 1211 Geneva 4, Switzerland. Electronic
address: Laurence.Marcourt@unige.ch.
- 5
- Department of
Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid
Beheshti University, G. C., Evin, Tehran, Iran. Electronic address:
s_ebrahimi@sbu.ac.ir.
- 6
- School of Pharmaceutical
Sciences, University of Geneva, University of Lausanne, CMU - Rue
Michel-Servet 1, 1211 Geneva 4, Switzerland. Electronic address:
philippe.christen@unige.ch.
- 7
- School of Pharmaceutical
Sciences, University of Geneva, University of Lausanne, CMU - Rue
Michel-Servet 1, 1211 Geneva 4, Switzerland. Electronic address:
muriel.cuendet@unige.ch.
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.
Copyright © 2017 Elsevier Ireland Ltd. All rights reserved.
KEYWORDS:
Adouetin
X (PubChem CID: 5281577); Adouetin Y (PubChem CID: 5281578); Adouetin
Y’ (PubChem CID: 101731531); Chrysosplenol E (PubChem CID: 5315857);
NF-κB; Oxyanin A (PubChem CID: 5281676); Vitexicarpin (PubChem CID:
5315263); Waltheria indica;
Waltherione A (PubChem CID: 11474862); Waltherione C (PubChem CID:
102362412); inflammation; quinone reductase; traditional medicine
