Impact of natural products on discovery of, and innovation in, crop protection compounds

Abstract

Natural products (NPs) have long been an important source of, and inspiration for, developing novel compounds to control weeds, pathogens and insect pests. In this review, we use a dataset of 800 historic, current and emerging crop protection compounds to explore the influence of NPs on the introduction of new crop protection compounds (fungicides, herbicides, insecticides) as a function of time. NPs, their semisynthetic derivatives (NPDs) and compounds inspired by NPs (NP mimics, NPMs) account for 17% of all crop protection compounds. NPs, NPDs, and NPMs have been a fairly constant source of new agrochemicals over the past 70 years. NP synthetic equivalents (NPSEs) is a fourth group of NP-related crop protection compounds composed of synthetic compounds which by chance also happen to have an NP model (but are not involved in the discovery). If NPSE compounds are also included, then 50% of all crop protection compounds hypothetically could have had a NP origin. Similar trends also hold true for the impact of NPs on the discovery of new modes of action (MoA) or innovation in crop protection compounds as measured by the number of first-in-class compounds. NPs have had the largest impact on the numbers and global sales (2018 USD) of insecticides compared to fungicides and herbicides. The present analysis highlights NPs as a longstanding and continuing source of new chemistry, new MoAs and innovation in crop protection compound discovery.

The search for new herbicide mechanisms of action: Is there a ‘holy grail’?

“…49 2.2 Natural products with new modes of action as lead compounds and target site identification Natural products have been a source of new chemistries and new MOAs for pesticides, including herbicides. 50,51 Of commercial herbicides, natural products, modified natural products (e.g. semisynthesis), and natural product mimics (purely synthetic) account for about 15% of the MOAs of commercial herbicides, but another 35% of these MOAs could have been derived from research with natural phytotoxins.…”

“…semisynthesis), and natural product mimics (purely synthetic) account for about 15% of the MOAs of commercial herbicides, but another 35% of these MOAs could have been derived from research with natural phytotoxins. 51 There are many natural phytotoxins with MOAs that are different than those of commercial herbicides. Many of these are mentioned and/or discussed in the review of Dayan and Duke.…”

“…Natural products have been a source of new chemistries and new MOAs for pesticides, including herbicides 50,51 . Of commercial herbicides, natural products, modified natural products (e.g.…”

“…Of commercial herbicides, natural products, modified natural products (e.g. semi‐synthesis), and natural product mimics (purely synthetic) account for about 15% of the MOAs of commercial herbicides, but another 35% of these MOAs could have been derived from research with natural phytotoxins 51 . There are many natural phytotoxins with MOAs that are different than those of commercial herbicides.…”

ПЕРСПЕКТИВНЫЕ НАПРАВЛЕНИЯ ИСПОЛЬЗОВАНИЯ БИОЛОГИЧЕСКИХ И БИОРАЦИОНАЛЬНЫХ ГЕРБИЦИДОВ В РАСТЕНИЕВОДСТВЕ РОССИИ (Обзор)

“…Существующие биорациональные средства защиты растений, включая БХГ, можно условно разделить на четыре группы: микробные препараты токсинного действия; грубые экстракты растительного или микробного происхождения; индивидуальные природные соединения (или их смеси) различной степени очистки; синтетические аналоги природных соединений (10). Последние, строго говоря, не относятся к природным, поэтому в настоящей статье химические гербициды на их основе мы рассматривать не будем.…”