Aphids are agricultural pest insects that transmit viruses and cause feeding damage on a global scale. Current pest control practices involving the excessive use of synthetic insecticides over many years have resulted in aphid resistance to a number of pesticides. In nature, plants produce secondary metabolites during their interaction with insects and these metabolites can act as toxicants, antifeedants, anti-oviposition agents and deterrents towards the insects. In a previous study, we demonstrated that the butanol fraction from a crude methanolic extract of an important plant species,
Isodon rugosus
showed strong insecticidal activity against the pea aphid,
Acyrthosiphon pisum
. To further explore this finding, the current study aimed to exploit a bioactivity-guided strategy to isolate and identify the active compound in the butanol fraction of
I
.
rugosus
. As such, reversed-phase flash chromatography, acidic extraction and different spectroscopic techniques were used to isolate and identify the new compound, rosmarinic acid, as the bioactive compound in
I
.
rugosus
. Insecticidal potential of rosmarinic acid against
A
.
pisum
was evaluated using standard protocols and the data obtained was analyzed using qualitative and quantitative statistical approaches. Considering that a very low concentration of this compound (LC
90
= 5.4 ppm) causes significant mortality in
A
.
pisum
within 24 h, rosmarinic acid could be exploited as a potent insecticide against this important pest insect. Furthermore,
I
.
rugosus
is already used for medicinal purposes and rosmarinic acid is known to reduce genotoxic effects induced by chemicals, hence it is expected to be safer compared to the current conventional pesticides. While this study highlights the potential of
I
.
rugosus
as a possible biopesticide source against
A
.
pisum
, it also provides the basis for further exploration and development of formulations for effective field application.