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16

Plant Bioprospecting for Biopesticides and Bioinsecticides

Aradhana Lucky Hans and Sangeeta Saxena
Department of Biotechnology, Babasaheb Bhimrao Ambedkar University, Lucknow, India

16.1 ­Introduction

Agriculture holds an exceptional position in the growth of a country, especially developing

ones. The major setback it faces is from the attack of various pests causing harm to crops.
Loss due to harmful pest causes severe economic losses of agricultural crops and commodi-
ties. This threat to economic loss in the quality of agricultural crops has paved a way to
major insights in the field of research and new discoveries of pest-controlling agents.
Therefore, one of the crucial components of agricultural management is efficient manage-
ment of these pests. They can be managed and controlled by the application of various
pesticides in the different ways and at the different time points.
Over the years, chemical pesticides have made a great contribution to the fight against
several pests and diseases. However, the repetitive and indiscriminate use of these pesti-
cides has developed insecticide resistance in many major pests causing resurgence of minor
pests, which in turn resulted in irreparable damage to crops. A new range of pests had even
more and wider range of pesticide application, making the situation even more worse.
Harmful effects, such as soil and water contamination and dramatic increase of the harm-
ful residues, cause harm to both environment and human health. The use of chemical
insecticides in crop pest control programs around the world had caused tremendous dam-
age to the environment, pest resurgence, pest resistance to insecticides, and lethal effects
on nontarget organisms [1].
It is evident that population rise has been a continuous process and to meet the needs,
agriculture also has been pacing up at faster rate. The improvement in the yield and pro-
duction of agriculture can be easily credited to the application of pesticides, therefore
improving production in agriculture is most certain. The indiscriminate use of pesticides
over the years, particularly in developing countries, has caused enough damage in various
spheres. Overlooking the safety measures and recommended usage has led to many health-
related problems. The risk is not only on humans but on the surrounding environment and
the nontarget flora and fauna that are exposed to these harmful chemicals. The residues

Bioprospecting of Plant Biodiversity for Industrial Molecules, First Edition.

Edited by Santosh Kumar Upadhyay and Sudhir P. Singh.
© 2021 John Wiley & Sons Ltd. Published 2021 by John Wiley & Sons Ltd.
336 16  Plant Bioprospecting for Biopesticides and Bioinsecticides

linger in the air, water, and soil and persist for a long duration causing more damage to the
environment. According to World Heath Organizations (WHO), about 25 million cases of
acute occupational pesticide poisoning and 20 000 deaths occurred globally per year. This
adverse effect of these pesticides is a matter of great concern, leading to awareness about
safety of food and environment. A search for alternatives to these nonjudiciously used
chemicals is catching up pace toward a more greener and cleaner alternative. In recent
decades, there has been a heap change in the viewpoint, causing some changes in the use
of conventional chemical pesticides [2]. Pertaining to the high risk with the use of chemi-
cal pesticides, integrated pest management (IPM) programs have brought out application
of pesticides with more efficient and judicious manner. Eventually these changes have sig-
nificantly reduced pesticide use and improved pest management practices. As a result,
there is an increasing demand for less toxic or environmentally safe pesticides that would
pose less risk to application as well as consumption. The need of the hour is to look for
alternatives that are less adverse and possess lesser health risk and be more environment-
friendly. Moving back from chemical toward natural resource would be more apt owing to
immeasurable diversity of molecules present in the nature. To look for an alternative that
would be ecologically better and environmentally safe, biopesticides seem to be the choic-
est option. Also, chemical pesticides are more expensive in comparison to biopesticides.
Plants are regarded as one of the most diverse and richest resources of various important
bioactive natural products. Since ancient times, the use of plants by the natives of various
parts of the world as pesticidal has been well utilized. Innumerable active compounds have
been identified from plants and still the source has not exhausted its prospective. Hence,
this interminable reservoir of bioactive compounds should be screened, searched, and
secured for more applications. Biopesticides conceptualized natural enemy or predatory
organism or their products that would include plants, microbial products, or by-products as
they were capable of managing or reducing pests. There is an obvious urge for the impetus
in developing biopesticides as they have the potential to protect plants from pest infesta-
tion. In search for novel bioactive substances from botanicals, screening of diverse plants
can be of much utility. This process of discovering and further commercialization of new
products based on biological resource is known as bioprospecting. Nature has been an
unending reservoir wherein one can unleash plant compounds that can be helpful in con-
trolling various pests. Biological resource comparatively has higher diversity than the
chemical compounds, holding more potential for novel compounds for agricultural appli-
cation [3]. In this chapter, the present scenario of plant-based biopesticides, advantages,
and future prospects will be discussed.

16.2 ­Current Scenario in India

Due to its rich biodiversity, India offers plenty of scope in terms of sources for natural biologi-
cal control organisms as well as natural plant-based pesticides. Traditional knowledge avail-
able with the highly diverse indigenous communities in India may provide valuable clues for
developing newer and effective biopesticides. Owing to its biological background biopesti-
cides are eco-friendly, easily biodegradable, and safer alternative to chemical pesticides.
Although the production is not as par chemical pesticide, yet the demand is pacing up the
production every passing year. Presently, biopesticides may represent approximately 4.2% of
 16.3 ­Plants-Based Active Compound 337

Table 16.1  List of biopesticides from their resource plants and target pests.

Plant product used

as biopesticide Target pests Plants

Limonene and Fleas, aphids, and mites also kill fire ants, several Citrus fruits
Linalool types of flies, paper wasps, and house crickets
Neem/ A variety of sucking and chewing insect Azadirachta indica
Azadirachtin
Pyrethrum/ Ants, aphids, roaches, fleas, flies, and ticks Chrysanthemum cineraria
Pyrethrins folium
Rotenone Leaf-feeding insects, such as aphids, certain Genus Lonchocarpus
beetles (asparagus beetle, bean leaf beetle, majorly from Lonchocarpus
Colorado potato beetle, cucumber beetle, flea utilis and Lonchocarpus
beetle, strawberry leaf beetle, and others) and urucu
caterpillars, as well as fleas and lice on animals
Ryania Caterpillars (European corn borer, corn earworm, Ryana speciosa
and others) and thrips
Sabadilla Squash bugs, harlequin bugs, thrips, caterpillars, South American lily
leaf hoppers, and stink bugs Schoenocaulon officinale
Nicotine Caterpillars chewing pests Nicotiana tabacum
Acetogenins Lepidopterans and Colorado potato beetle Annona spp., including A.
(Leptinotarsa decemlineata) squamosa and A. muricate
Capsaicinoids Lepidopterans and Hemiptera insects Capsicum spp.

the total pesticides market in India. There are more than 6000 species that are screened of
which 2500 plant species were found to possess biologically active compounds against vari-
ous kinds of pests. The important plant families containing the biopesticide plants are
Apocynaceae, Asteraceae, Euphorbiaceae, Fabaceae, Meliaceae (maximum), Myrtaceae,
Ranunculaceae, and Rosaceae  [4]. The higher demand for organic, chemical-free food has
augmented the demand of eco-friendly chemicals isolated from different parts of plants
(Table. 16.1). They can be from leaves, barks, roots, fruits, flowers, seeds, or seed kernels. In
nature, the higher plants have the ability to synthesize and produce various kinds of second-
ary metabolites that are naturally avoided by insects. Some are able to interfere in the insect
life cycle, which are known as semiochemicals. Majorly four types of botanical products are
used for insect control (neem, pyrethrum, rotenone, and essential oils); few others such as
ryania, sabadilla, acetogenins, capsaicinoids, and nicotine have limited use. Additionally,
plant oils and extracts also seem to have effect on insects that have even lesser use.

16.3 ­Plants-Based Active Compounds

16.3.1 Azadirachtin
The plant Neem or Azadirachta indica is the most extensively used plant for insect pest
management. Several farmers in Indian villages collect the neem seeds to prepare crude
seed kernel extract for pest control. Various reports highlight that neem-related products
338 16  Plant Bioprospecting for Biopesticides and Bioinsecticides

do not leave any toxic residues on application on plants. Neem oil is said to be effective
against mites, soft-bodied insects, and phytopathogens. The compound Azadirachtin is
said to have low toxicity toward mammals and pollinators [5] according to Environmental
Protection Agency. This compound is isolated from the kernels and used in various biofor-
mulations of biopesticides. Effect of azadirachtin on insects can be in two major ways. It
blocks the synthesis and release of ecdysteroids (molting hormones), leading to incom-
plete ecdysis in young insects and sterility in adult female insects. The other effect seems
to be its antifeedant property inhibiting pest attack. These excellent effects of neem on
pest definitely make neem to the millennium paradigm toward the development of biope-
sticides. The reason is there is a plethora of neem-based commercial products Neemmark,
Wellgrow, Azatin, Bio-neem, Nimbin, Neemark, to name a few, used effectively through-
out the world.

16.3.2 Pyrethrins
Pyrethrum is obtained from dries flowers of Chrysanthemum cineraria folium and has
been and is globally used as a biopesticide  [6]. Pyrethrins are insecticidal chemicals
extracted from the dried pyrethrum flower. The flower heads are processed into a powder
to make dust. This dust can be used directly or infused into water to make a spray.
Technical-grade pyrethrum, the resin used in formulating commercial insecticides, typi-
cally contains pyrethrin from a range of 20–25%  [7]. Effect of pyrethrins on insects is
characterized by rapid knockdown particularly in flying insects and hyperactivity and
convulsions in other insects. The mode of action is quite similar to commercial chemical
pesticides such as DDT (Dichloro-diphenyl-trichloroethane) and other organochloride-
based insecticides, effecting mostly the neurotoxic action potential blocking voltage-gated
sodium channels in nerve axons. Pyrethrins are less toxic and easily break down in sun-
light as they are liable to the UV rays, making them safer alternatives to chemical
pesticides.

16.3.3 Rotenone
Rotenone is prepared from the plant species belonging to the genus Lonchocarpus majorly
from Lonchocarpus utilis and Lonchocarpus urucu. A cube resin, root extract is the major
component consisting of active ingredients rotenone, deguelin, and tephrosin. Rotenone is
also used as blends along with pyrethrins and approved as organic insecticides. Rotenone
is an important insecticide extracted from various other leguminous plants. It is an effec-
tive insecticide, it blocks the electron transport chain and prevents energy production act-
ing as mitochondrial toxin. To be effective it must be ingested. It is considered similar to
DDT but is much lesser toxic in its formulated products. In insects, rotenone exerts its toxic
effects primarily on nerve and muscle cells, causing rapid cessation of feeding. Death
occurs several hours to a few days after exposure. The disruption energy metabolism and
the subsequent loss of ATP result in a slowly developing toxicity, and the effects of all these
compounds include inactivity, paralysis, and death.
 16.3 ­Plants-Based Active Compound 339

16.3.4 Sabadilla
Sabadilla is derived from the seeds of South American lily Schoenocaulon officinale. They
have active ingredients as celandine-type alkaloids and toxic to mammals, but in commer-
cial preparations, the active ingredients is at very low concentration, diluting its toxic effect.
These alkaloids are similar to pyrethrins and are used on citrus crops and avocado in
organic farming.
The mode of action of these alkaloids affects nerve cell membrane action, causing loss of
nerve action potential, causing paralysis and death [6].

16.3.5 Ryania
These botanical insecticides are derived from stem of Ryana speciosa. It contains an alka-
loid ryanodine that interferes with calcium release in muscle tissue. It is a slow-acting
abdominal toxin. The effect exerted by it is not rapid, rather delayed as insects do not imme-
diately stop feeding after ingesting it. Although not much has been studied about its mode
of action yet, it is said to be effective in hot weather. It is found to be toxic against citrus
thrips and fruit moths [8].

16.3.6 Nicotine
Another alkaloid is nicotine, which is obtained from the leaves of tobacco plant or Nicotiana
tabacum and few related species. Nicotine, along with nornicotine and anabasine, is a syn-
aptic toxin that mimics the neurotransmitter acetylcholine. They cause similar effects as
that of organophosphate and carbamate insecticides. It can be absorbed dermally and is
toxic to humans; therefore, the use has seen a decline. It is a fast-acting killer for soft-­
bodied insects but not to all chewing pests. It mimics acetylcholine, neurotransmitter
­causing uncontrolled nerve firing. It is said that nicotine is fairly selective and affects only
certain types of insects [9].

16.3.7 Acetogenins
Acetogenins have been traditionally prepared from Annona spp., including A. squamosa
and A. muricate, which are used as botanical pesticides. These are source of fruit juice in
some parts of Asia. The major acetogenins are obtained from the seeds of A. squamosa [8].
These compounds show toxicity as slow-acting gut poison, mostly effective against chew-
ing pest, especially Lepidopteran pest and Colorado potato beetle (Leptinotarsa decemline-
ata). The mode of action of acetogenins is similar to rotenone. They work in blocking
energy production in mitochondria.

16.3.8 Capsaicinoids
Peppers are very abundant in nature and found around easily. They are extremely pungent
and hot in nature. The burning sensation in chilli owes to the presence of capsaicinoids
340 16  Plant Bioprospecting for Biopesticides and Bioinsecticides

found only in Capsicum spp. The main components of capsaicinoids are capsacin,
­dihydrocapsaicin, nordihydrocapsaicin, etc. Various reports have been indicating the
broad-­spectrum activity of capsaicin against insects such as Myzus persicae, Bemicia tabaci,
Sitophilus zeamais, Alfalfa weevil, to name a few [10–11]. The mode of action is majorly by
impairing the nervous system of insects or dysfunction of Na or K-gated channels.

16.3.9  Essential Oils

In addition to these, there are many plants that contain essential oil, which is a complex
mixture of volatile compounds accumulated in seeds, flowers, and leaves. These are vola-
tile in nature, complex secondary metabolites having a strong odor, and lipophilic in
nature [12]. These compounds interfere with physiological, biochemical, metabolic func-
tions of insects. Therefore, plant essential oil compounds are considered to be alternative
insect-controlling compounds and act as biopesticides. They have a wide range of quality
that is sufficient to manage insects and pests well. They have the ability to delay develop-
ment activities such as adult emergence and fertility, deterrent effect on oviposition [13],
arrestant and repellent action [14]. They have antifeedant and larvicidal activity [15].
The volatile components of essential oils are classified into four main groups: terpenes,
benzene derivatives, hydrocarbons, and other miscellaneous compounds. Monoterpenoids
are the most representative molecules consisting 90% of essential oils having diverse func-
tion. They have acyclic alcohols (linalool, citronellol, geraniol), cyclic alcohols (menthol,
terpineol, isopulegol), bicyclic alcohols (borneol, verbenol), phenol (thymol, carvacrol),
ketones (carvone, menthone, thujone), aldehydes (citronellal, citral), acids (chrysanthemic
acid), and oxides (cineole) [16]. Linalool has been studied and found to have effect on the
nervous system, affecting ion transport and release of acetylcholine esterase in insects [16].
The mode of action of most monoterpenes is by causing a drastic reduction in the number
of intact mitochondria and Golgi bodies, impairing respiration and photosynthesis, and
decreasing cell membrane permeability [17].
The essential oils of Ocimum basilicum contain active compounds juvocimenes, which
are an analogue of juvenile hormones of insects. Matricaria recutita contains precocenes,
which stimulate the production of juvenile hormone that suppresses the growth of insects
during molting. Additionally, some aromatic plants such as coriander, marigold have
strong odor, which act act insect repellents and act in managing the harmful pests.
Therefore, an analytical approach in selecting right biomolecules for the production of
biopesticides having broader range of activity would be a preferable alternative for eco-
friendly pest management. From unravelling new and better molecules to utilizing them
into useful application in the field is the actual need of the hour. Mere pilling up of numer-
ous novel compounds would not be ideal, rather disseminating into biochemicals will be
highly appreciated.

16.4 ­Advantages and Future Prospects of Bioinsecticides

Advantages attributed to biopesticide usage over chemically synthesized products are

many (Figure 16.1). They are supposedly less toxic, more selective in combating unwanted
biological targets, possess higher efficiency at lower concentrations, decompose more
 16.4  ­Advantages and Future Prospects of Bioinsecticide 341

Botanical pesticides Chemical pesticides

Weekly to monthly
Hourly application at
Application application at pre
preharvest interval
harvest interval

Repellent, growth,
morphological and Toxic, repellent, non-
Mode of physiological selective harms non-
action interference, selectively target organisms too
toxic target pests

Attaining Efficacy on repeated Efficacy on fewer

efficacy application application

Degradation Takes few days to Takes almost years to

degrade degrade

Environmentally safe, Accumulation in

Outcome safe on heat environment, health
sustainable agriculture risks, loss of
biodiversity

Figure 16.1  Advantages of botanical pesticides over chemical pesticides. Source: Adapted from
Lengai et al. [18] Licence no. 4870610831544.

quickly, reducing adverse environmental effects. They can be used as an active component
of IPM and reduce the use of conventional chemical pesticides while crop yields remain
high. To use biopesticides effectively, however, one needs to know a great deal about man-
aging pests.
In IPM-related programs, biopesticides are needed to be the preferred component in
implementation of resistance management programs. The agrochemical industry is shift-
ing from chemical to botanicals owing to its great implications. The demand for chemical-
free food is increasing, and so is the awareness. The consumers are now more willing to pay
beyond the regular prices for foods produced organically without the use of chemicals.
Adaptation toward botanical pesticides from the more prominent chemical pesticides is
gradual.
Although the scenario is fast changing, yet a lot has to be changed in the coming years to
get a higher impact in modern agriculture. Resistance risk analysis is a key requirement, as
efficacy demonstration of pesticide active substances and their formulations is mandatory.
This kind of resistance risk assessment requires examination of the inherent risk (associ-
ated with the government authorities of the product and the pest) and the agronomic risk
(influenced by the crop, the geographic area, and the use pattern). Therefore, resistance
342 16  Plant Bioprospecting for Biopesticides and Bioinsecticides

risk analysis is a complex issue, and the basis for risk assessment requires a clear willing-
ness on the stakeholders to cooperate in order to maintain a sustainable, viable, and safe
agricultural environment.
The actual benefits of biopesticides can be best realized in developing countries such as
India, where farmers are not always able to afford chemical insecticides. The ancient and
traditional use of plants and plant derivatives for protection of stored products is estab-
lished well in our country. Although synthetic insecticides might be affordable to growers
(e.g. through government subsidies), yet limited literacy and a lack of protective equipment
result in thousands of accidental poisonings annually. The lack of judicious use of pesti-
cides and the health and environmental risk it possesses can be overcome by the use of
biopesticides. No security measure is taken care of while applying chemical pesticides; this
kind of risk will be curbed by botanicals.
The area under organic cultivation (crops) in India is estimated to be around 100 000
hectare. Besides, there are lakhs of hectare of forest area being certified as organic.
Furthermore, some states such as Uttaranchal and Sikkim have taken botanicals on a larger
scale and declared their states as organic. The future is in need of making a shift from syn-
thetic to natural source to minimize the adversity of chemicals. The nature has immense
treasure instead of damaging approach; care should be taken to utilize and coexist benefit-
ting the crop and its growers.

16.5 ­Conclusions

To acquire knowledge is good, but to apply the same is even better. The same stands true for
biopesticides. Bioprospecting for novel molecules having varied properties should be car-
ried out. But, perhaps it is time to converge the attention of the research community toward
the development and application of known botanicals rather than screen more plants and
isolate further novel bioactive substances that satisfy our curiosity but are unlikely to be of
much utility [19].
The development of the biopesticide industries has to adopt a strategic, comprehensive
and more forward, and applicable approach. With the growing population and the growing
need of population, there will be greater need of crops and other products. The biopesticide
industry has to pace up to stand par with the chemical industry. For this, the policymakers,
government authorities, and the consumers demand has to work in sync. These together
will boost up the importance and ease of trade will make it more available in the market for
easy application. The increasing concern of consumers and government on food safety has
led growers to explore new environmentally friendly methods to replace, or at least supple-
ment, the current chemical-based practices. The use of biopesticides has emerged as prom-
ising alternative to chemical pesticides. Biopesticides have a precious role to play in the
future of the IPM strategies. It is evident that the path would not be as easy although we
have a wealth of knowledge and resource, but application still remains at a nascent stage.
The efficacy of biopesticides in managing insect pests is sure very effective, but the mat-
ter that needs to be pondered upon is their limited source. Though nature has immense
treasure of these important botanicals, yet, the supply is limited, since a large number of
source plants are needed for extraction of desired active compounds. And the supply in
   ­Reference 343

nature or natural habitat is marginal and would exhaust if used extensively. Therefore,
commercial agriculture of such plants would raise income and keep the supply of required
raw material at pace. To scale up the produce, landscapes that are not under direct cultiva-
tion can be utilized.
The process of extraction and processing of the biopesticides using appropriate methods
should be worked upon also considering cost cutting during production. An efficient pro-
duction with fluent distribution up to the smallhold farmers will see the real success of
biopesticides. A better marketing strategy for biopesticides will also help in better circula-
tion in the much upscale pesticide market. Also, a regular education or awareness program
to farmers and supplier would boost up the botanicals immensely. All of such measures
will surely help biopesticide to amplify its application in the market.
Apart from all these things, there are some areas that to my concern seem to be impor-
tant to be pondered upon. Generally, discovering something hidden in nature and report-
ing seems to be satisfying, yet, how much is it valued or accepted is a critical point of
discussion. A far more acceptable approach that also is rewarding is proving one’s hypoth-
esis; publication-wise too this seems better. Reporting a potent botanical compound and
moving onto its application in the fields is a long process. Yet, there are many compounds
successfully being applied in fields, such as Pyrethrin and Azadirachtin, etc. Therefore, the
dawn of biopesticides is decent, but to see it a daylight, more effort with applicable focus
is needed.

A
­ cknowledgment

ALH and SS would like to acknowledge the funding from DST NPDF-SERB.

R
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