Exploiting the Evolutionary Relationship between Malarial Parasites and Plants To Develop New Herbicides

Maxime G. Corral, Julie Leroux, Stefan Tresch, Trevor Newton, Keith A. Stubbs, Joshua S. Mylne

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Herbicide resistance is driving a need to develop new herbicides. The evolutionary relationship between apicomplexan parasites, such as those causing malaria, and plants is close enough that many antimalarial drugs are herbicidal and so represent novel scaffolds for herbicide development. Using a compound library from the Medicines for Malaria Venture, the model plant Arabidopsis thaliana, and a physicochemical database of known herbicides, a compound was discovered that showed post-emergence herbicidal activity equal to commercial herbicides. Using structure–activity analysis, important points for its potency were found. The compound was also tested and found to be active against common crop weeds. Physiological profiling suggested the compound was a photosystem II inhibitor, representing a new scaffold for herbicide development. Overall this approach demonstrates the viability of using antimalarial compounds as lead compounds for the development of much needed new herbicides.

Original languageEnglish
Pages (from-to)9881-9885
Number of pages5
JournalAngewandte Chemie - International Edition
Volume56
Issue number33
DOIs
Publication statusPublished - 7 Aug 2017

Fingerprint

Herbicides
Parasites
Antimalarials
Malaria
Scaffolds
Herbicide Resistance
Photosystem II Protein Complex
Lead compounds
Arabidopsis
Libraries
Medicine
Crops
Databases

Cite this

@article{469a3b79e8294861a3559e5365fc3a54,
title = "Exploiting the Evolutionary Relationship between Malarial Parasites and Plants To Develop New Herbicides",
abstract = "Herbicide resistance is driving a need to develop new herbicides. The evolutionary relationship between apicomplexan parasites, such as those causing malaria, and plants is close enough that many antimalarial drugs are herbicidal and so represent novel scaffolds for herbicide development. Using a compound library from the Medicines for Malaria Venture, the model plant Arabidopsis thaliana, and a physicochemical database of known herbicides, a compound was discovered that showed post-emergence herbicidal activity equal to commercial herbicides. Using structure–activity analysis, important points for its potency were found. The compound was also tested and found to be active against common crop weeds. Physiological profiling suggested the compound was a photosystem II inhibitor, representing a new scaffold for herbicide development. Overall this approach demonstrates the viability of using antimalarial compounds as lead compounds for the development of much needed new herbicides.",
keywords = "Arabidopsis, drug discovery, herbicides, malaria",
author = "Corral, {Maxime G.} and Julie Leroux and Stefan Tresch and Trevor Newton and Stubbs, {Keith A.} and Mylne, {Joshua S.}",
year = "2017",
month = "8",
day = "7",
doi = "10.1002/anie.201705400",
language = "English",
volume = "56",
pages = "9881--9885",
journal = "Angewandte Chemie - International Edition",
issn = "1433-7851",
publisher = "Wiley-VCH Verlag GmbH & Co. KGaA",
number = "33",

}

Exploiting the Evolutionary Relationship between Malarial Parasites and Plants To Develop New Herbicides. / Corral, Maxime G.; Leroux, Julie; Tresch, Stefan; Newton, Trevor; Stubbs, Keith A.; Mylne, Joshua S.

In: Angewandte Chemie - International Edition, Vol. 56, No. 33, 07.08.2017, p. 9881-9885.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Exploiting the Evolutionary Relationship between Malarial Parasites and Plants To Develop New Herbicides

AU - Corral, Maxime G.

AU - Leroux, Julie

AU - Tresch, Stefan

AU - Newton, Trevor

AU - Stubbs, Keith A.

AU - Mylne, Joshua S.

PY - 2017/8/7

Y1 - 2017/8/7

N2 - Herbicide resistance is driving a need to develop new herbicides. The evolutionary relationship between apicomplexan parasites, such as those causing malaria, and plants is close enough that many antimalarial drugs are herbicidal and so represent novel scaffolds for herbicide development. Using a compound library from the Medicines for Malaria Venture, the model plant Arabidopsis thaliana, and a physicochemical database of known herbicides, a compound was discovered that showed post-emergence herbicidal activity equal to commercial herbicides. Using structure–activity analysis, important points for its potency were found. The compound was also tested and found to be active against common crop weeds. Physiological profiling suggested the compound was a photosystem II inhibitor, representing a new scaffold for herbicide development. Overall this approach demonstrates the viability of using antimalarial compounds as lead compounds for the development of much needed new herbicides.

AB - Herbicide resistance is driving a need to develop new herbicides. The evolutionary relationship between apicomplexan parasites, such as those causing malaria, and plants is close enough that many antimalarial drugs are herbicidal and so represent novel scaffolds for herbicide development. Using a compound library from the Medicines for Malaria Venture, the model plant Arabidopsis thaliana, and a physicochemical database of known herbicides, a compound was discovered that showed post-emergence herbicidal activity equal to commercial herbicides. Using structure–activity analysis, important points for its potency were found. The compound was also tested and found to be active against common crop weeds. Physiological profiling suggested the compound was a photosystem II inhibitor, representing a new scaffold for herbicide development. Overall this approach demonstrates the viability of using antimalarial compounds as lead compounds for the development of much needed new herbicides.

KW - Arabidopsis

KW - drug discovery

KW - herbicides

KW - malaria

UR - http://www.scopus.com/inward/record.url?scp=85023201764&partnerID=8YFLogxK

U2 - 10.1002/anie.201705400

DO - 10.1002/anie.201705400

M3 - Article

VL - 56

SP - 9881

EP - 9885

JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

SN - 1433-7851

IS - 33

ER -