Dienediamine: A safe surrogate for the herbicide paraquat

Paraquat (PQ) has been used as an herbicide worldwide because of its potent activity against weeds. However, it is highly toxic to humans. The very high fatality of PQ poisoning is due to its inherent toxicity and the lack of any effective treatment. Consequently, developing a non-toxic herbicide with comparable efficacy to PQ will contribute to global food security and help prevent PQ-related fatalities. Herein, we report a new herbicide called dienediamine, which was discovered from how to intervene the redox cycle of PQ, an inherent toxicity nature. Dienediamine, the “reduced” form of PQ with no function as an electron transfer agent, was shown to be non-toxic through comprehensive in vivo and in vitro experiments at molar concentrations equivalent to PQ’s absolute lethal dose. Remarkably, dienediamine can undergo conversion to PQ under natural sunlight and ambient air conditions, exhibiting herbicidal activities that are comparable to those of PQ. The conversion of dienediamine to PQ, which is toxic to chloroplasts, is the key mechanism underlying its potent herbicidal activity. Our study discovers that dienediamine is a safe and superior alternative to PQ, possessing significant potential for application in sustainable agriculture globally.