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    Plant-Derived Pesticides

    Subjects: Plant Sciences
    View times: 28
    Submitted by: Augusto Souto
    (This entry belongs to Entry Collection "Environmental Sciences ")


    Pests and diseases are responsible for most of the losses related to agricultural crops, either in the field or in storage. Moreover, due to indiscriminate use of synthetic pesticides over the years, several issues have come along, such as pest resistance and contamination of important planet sources, such as water, air and soil. Therefore, in order to improve efficiency of crop production and reduce food crisis in a sustainable manner, while preserving consumer’s health, plant-derived pesticides may be a green alternative to synthetic ones.

    1. Introduction

    Pesticides may be defined as any compound or mixture of components intended for preventing, destroying, repelling or mitigating any pest [1]. Additionally, herbicides or weed-killers may also be considered as pesticides, and are used to kill unwanted plants in order to leave the desired crop relatively unharmed and well provided with nutrients, leading to a more profitable harvest [2].
    Nevertheless, the world food production is constantly affected by insects and pests during crop growth, harvest and storage. As a matter of fact, there is an estimated loss of 18–20% regarding the annual crop production worldwide, reaching a value of more than USD 470 billion [3]. Furthermore, insects and pests not only represent a menace to our homes, gardens and reservoirs of water, but also, they transmit a number of diseases by acting as hosts to some disease-causing parasites. Therefore, the mitigation or control of pests’ activities may lead to a substantial reduction of the world food crisis as well as the improvement of human and animal health [2].

    2. Plant Derived Insecticides That Affect Respiratory or Energy System

    Cellular respiration is a process that converts nutrient compounds into energy or adenosine triphosphate (ATP) at a molecular level. More specifically, this process is performed by the electron transport chain of the mitochondria, which comprises several important enzymes that are potential targets for insecticides. Rotenone is the most common natural product among rotenoids, a type of isoflavonoid and is usually found in species from Derris and Lonchocarpus (in Fabaceae) and Rhododendron (in Ericaceae), spread throughout East Indies, Malaya and South America [4].

    Rotenone is defined as a complex I inhibitor of the mitochondrial respiratory chain, which works both as contact and stomach poison. It blocks the nicotinamide adenine dinucleotide (NADH) dehydrogenase, stopping the flow of electrons from NADH to coenzyme Q, therefore, preventing ATP formation from NADH, but maintaining ATP formation through flavine adenine dinucleotide (FADH 2); therefore, it is one of the slowest acting botanical insecticide, and yet readily degradable by air and sunlight, taking several days to kill insects, affecting primarily nerve and muscle cells, leading to cessation of feeding, followed by death, from several hours to a few days after exposure. Moreover, this bio-based pesticide is constantly applied to protect lettuce and tomato crops as it has a broad spectrum of activity against mite pests, including leaf-feeding beetles, lice, caterpillars, mosquitoes, ticks, fire ants and fleas. Furthermore, its effects are substantially synergized by PBO or pyrodone (MGK 264).

    Rotenone is highly toxic to mammals and fish [5][6]. Its activity and persistence are comparable to dichlorodiphenyltrichloroethane (DDT) [2] ; moreover, previous studies have correlated a possible link between its exposure and Parkinson’s Disease (PD) [7]. However, in spite of its high toxicity, rotenoids may be a potential source of novel complex I inhibitors, acting as a prototype for the development of safer and more efficient pesticide derivatives [8].

    Acetogenins (annonins, asimicin, squamocin, annonacins) obtained from Annona squamosa L. (Annonaceae) are well known for their pest control properties. A botanical formulation based on annonins wherein asimicin is the major pesticidal compound has been patented [9].

    3. Plant Derived Insecticides That Affect the Endocrine System

    Chemical constituents that interfere with the endocrine system of insects are classified as insect growth regulators (IGR). They may act either as juvenile insect hormone mimics or inhibitors, as well as chitin synthesis inhibitors (CSI). Normally, the juvenile hormones are produced by insects in order to keep its immature state. When a sufficient growth has been reached, the production of the hormone stops, triggering the molt to the adult stage [10]. Triterpenes from Catharanthus roseus (L.) G. Don (Apocynaceae), such as α-amyrin acetate and oleanolic acid, have demonstrated interesting growth regulator activity [11]. Acyclic sesquiterpenes such as davanone, ipomearone and the juvenile hormone from silkworm are perfect examples of natural products with IGR activity as well. Therefore, the constant application of IGR towards the crops will maintain the insects in its larvae state, preventing a successful molting and resulting in an efficient pest control [12]. On the other hand, it has been reported the antijuvenile hormone activity of two chromenes found in Ageratum conyzoides L. (Asteraceae), precocene I and II promotes a precocious metarmophosis of the larvae and production of sterile, moribund and dwarfish adults after exposure [13]. Although, resistance to azadirachtin has been demonstrated [14], indicating that insects can develop resistance to natural hormones or hormone-related compounds; however, this class of compounds remains a natural potential for commercial bio-based pesticides [12]. Additionally, complex polyphenolic fractions also present a wide range of insecticidal activities, interfering with the fecundity and inducing the disruption of the oogenesis [15][16] (WO 94/13141).

    Moreover, previous researches have reported a natural insecticide of broad-spectrum activity, which has low mammalian toxicity and is the least toxic among botanical insecticides. It is called azadirachtin, a complex tetranortriterpenoid limonoid, majorly found in the seeds of Azadirachta indica A. Juss. (Meliaceae), a plant species commonly known as the Neem tree which originated from Burma, but is currently grown in more arid, tropical and subtropical zones of Southeast Asia, Africa, Americas and Australia [5][17][18]. Azadirachtin is considered a contact poison of systemic activity, which may be categorized in two ways: direct effects towards cells and tissues, or indirect effects, represented by endocrine system interference. It is a powerful compound that acts mainly as a feeding deterrent and insect growth regulator, comprising a wide variety of insect taxa including Lepidoptera, Diptera, Hemiptera, Orthoptera, Hymenoptera [18]. As for its growth regulatory effects, azadirachtin affects the neurosecretory system of the brain insect, blocking the release of morphogenetic peptide hormones (e.g., prothoracicotropic hormone (PTTH) and allatostatins). These hormones control the function of the prothoracic glands and the corpora allata, respectively. Therefore, as the moulting hormone (which controls new cuticle formation and ecdyses) and the juvenile hormone (JH) (which controls the juvenile stage at each moult) are regulated by prothoracic glands and the corpora allata, any disruption on this biochemical cascade may lead to moult disruption, moulting defects or sterility. The effects on feeding, developmental and reproductive disruption are caused by effects of the molecule directly on somatic and reproductive tissues and indirectly through the disruption of endocrine processes [18].

    Neem-based non-commercial products are normally found as neem oil, obtained from the cold pressing of its seeds, in order to control phytopathogens (including insects). The other product is a medium-polarity extract containing azadirachtin (0.2–0.6% of seed/weight) [2], whereas the actual commercial product is a 1 to 4.5% azadirachtin solution [19]. Despite its 20 h half-life, it ensures a reasonable persistence in field applications due to its systemic action [2].

    In relation to CSIs, they inhibit the production of chitin, a β-(1,4)-linked homopolymer of N-acetyl-D-glucosamine, one of the most important structural components of nearly all fungi cell walls, and also a major component of the insect exoskeleton, which provides physical protection and osmoregulation. As chitin is absent on plant and mammalian species, while it is abundant in arthropods and most fungi, chitin biosynthesis has become an important target for developing more specific insecticides and antifungal agents. Previous research has reported chitin synthase inhibition activity of 2-benzoyloxycinnamaldehyde (2-BCA), a natural product isolated from the roots of Pleuropterus ciliinervis Nakai (Polygonaceae), which is a plant species traditionally used in Chinese folk medicine to treat inflammation and several types of infection [20].

    4. Plant Derived Insecticides That Affect the Water Balance

    Insects have a thin layer of wax covering their body, which provides the ecological function of preventing water loss from the cuticular surface. For instance, vegetable crude oils of rice bran, cotton seed and palm kernel, as well as saponins (natural soaps) may act by disrupting this protective waxy covering, affecting the water balance of insects through a rapid water loss from the cuticle, therefore leading to death by desiccation. Interestingly, the action of soaps affects the wax covering of insects [21]. The action of soaps on the wax covering of insects is influenced by the temperature [22]. Additionally, the crude oils may also act by interfering with insect respiration by plugging the orifices called spiracles, resulting in death by asphyxiation, controlling several types of insects such as whiteflies, mites, caterpillars, leafhoppers and beetles [1].

    This entry is adapted from 10.3390/molecules26164835


    1. Walia, S.; Saha, S.; Rana, V. Phytochemical Pesticides. In Advances in Plant Biopesticides; Singh, D., Ed.; Springer: New Delhi, India, 2014; pp. 295–322.
    2. Okwute, S.K. Plants as Potential Sources of Pesticidal Agents: A Review. In Pesticides—Advances in Chemical and Botanical Pesticides, 1st ed.; eBook; Soundararajan, R.P., Ed.; IntechOpen: London, UK, 2012; pp. 207–232.
    3. Sharma, S.; Kooner, R.; Arora, R. Insect Pests and Crop Losses. In Breeding Insect Resistant Crops for Sustainable Agriculture; Arora, R., Sandhu, S., Eds.; Springer: Singapore, 2017; pp. 45–66.
    4. Isman, M. Botanical Insecticides, Deterrents, and Repellents in Modern Agriculture and an Increasingly Regulated World. Annu. Rev. Entomol. 2006, 51, 45–66.
    5. Rattan, R.S. Mechanism of action of insecticidal secondary metabolites of plant origin. Crop. Prot. 2010, 29, 913–920.
    6. Casida, J.; Durkin, K. Neuroactive Insecticides: Targets, Selectivity, Resistance, and Secondary Effects. Annu. Rev. Entomol. 2013, 58, 99–117.
    7. Sherer, T.; Richardson, J.; Testa, C.; Seo, B.; Panov, A.; Yagi, T.; Matsuno-Yagi, A.; Miller, G.; Greenamyre, J. Mechanism of toxicity of pesticides acting at complex I: Relevance to environmental etiologies of Parkinson’s disease. J. Neurochem. 2007, 100, 1469–1479.
    8. Hollingworth, R.; Ahammadsahib, K.; Gadelhak, G.; McLaughlin, J.L. New inhibitors of Complex I of the mitochondrial electron transport chain with activity as pesticides. Biochem. Soc. Trans. 1994, 22, 230–233.
    9. Walia, S.; Saha, S.; Tripathy, V.; Sharma, K. Phytochemical biopesticides: Some recent developments. Phytochem. Rev. 2017, 16, 989–1007.
    10. Birnbaum, L. When environmental chemicals act like uncontrolled medicine. Trends Endocrinol. Metab. 2013, 24, 321–323.
    11. Singh, D.; Mehta, S.S.; Neoliya, N.K.; Shukla, Y.N.; Mishra, M. New possible insect growth regulators from Catharanthus roseus. Curr. Sci. 2003, 84, 1184–1186.
    12. Abreu, P.M.; Heggie, W. Terpenoides e Esteroides. In Biossíntese de Produtos Naturais, 1st ed.; Lobo, A.M., Lourenço, A.M., Eds.; IST Press: Lisboa, Portugal, 2008; pp. 119–149.
    13. Kamboj, A.; Saluja, A. Ageratum conyzoides L.: A review on its phytochemical and pharmacological profile. Int. J. Green Pharm. 2008, 2, 59–68.
    14. Feng, R.; Isman, M.B. Selection for resistance to azadirachtin in the green peach aphid, Myzuspersicae. Experientia 1995, 51, 831–833.
    15. Di Ilio, V.; Cristofaro, M. Polyphenolic extracts from the olive mill wastewater as a source of biopesticides and their effects on the life cycle of the Mediterranean fruit fly Ceratitiscapitata (Diptera, Tephriditae). Int. J. Trop. Insect Sci. 2021, 41, 359–366.
    16. Larif, M.; Zarrouk, A.; Soulaymani, A.; Elmidaoui, A. New innovation in order to recover the polyphenols of olive mill wastewater extracts for use as a biopesticide against the Euphylluraolivina and Aphis citricola. Res. Chem. Intermed. 2013, 39, 4303–4313.
    17. Copping, L.G.; Duke, S.O. Natural products that have been used commercially as crop protection agents. Pest Manag. Sci. 2007, 63, 524–554.
    18. Mordue, A.J.; Nisbet, A.J. Azadirachtin from the neem tree Azadirachtaindica: Its action against insects. An. Soc. Do Bras. 2000, 29, 615–632.
    19. Bernardi, D.; Botton, M.; Cunha, U.; Bernardi, O.; Malausa, T.; Garcia, M.; Nava, D. Effects of azadirachtin on Tetranych usurticae (Acari: Tetranychidae) and its compatibility with predatory mites (Acari: Phytoseiidae) on strawberry. Pest Manag. Sci. 2013, 69, 75–80.
    20. Kang, T.H.; Hwang, E.I.; Yun, B.S.; Park, K.D.; Kwon, B.; Shin, C.; Kim, S. Inhibition of chitin synthases and antifungal activities by 2’-benzoyloxycinnamaldehyde from Pleuropterusciliinervis and its derivatives. Biol. Pharm. Bull. 2007, 30, 598–602.
    21. Cui, C.; Yang, Y.; Zhao, T.; Zou, K.; Peng, C.; Cai, H.; Wan, X.; Hou, R. Insecticidal Activity and Insecticidal Mechanism of Total Saponins from Camellia oleifera. Molecules 2019, 24, 4518.
    22. Wigglesworth, V.B. Transpiration Through the Cuticle of Insects. J. Exp. Biol. 1945, 21, 97–114.