Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition

Topic Information

Dear Colleagues,

At present, chemical pesticides remain an effective means to control pests. However, the consequent problems of pest resistance and resurgence, with serious repercussions such as chemical pesticide residues that impact food safety, human health, and the ecological environment, remain. Given that natural bioactive product-based pesticides originate from secondary metabolites of plants, fungi, bacteria, and other natural sources, which are produced under the selective forces driving co-evolution between organisms and the environment (life and non-life), they often experience less or slower resistance development and are more eco-friendly. Therefore, the application of natural bioactive products, which represent a priceless source of green pesticides, has received increasing attention. Conversely, when compared with chemical pesticides, to improve their agricultural properties, using them as lead compounds for structural optimization is highly desirable. Bioactive natural products, as an invaluable source for structural diversity and biological activity, can promote, either directly or indirectly, the discovery of green pesticide candidates. In particular, the study of their mechanisms of action against pests is also important for the development of pesticidal agents.

Therefore, as a part of this Topic, entitled “Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition”, we will present three recent achievements in this field, namely, the isolation and structural elucidation of natural bioactive products (NBPs), structural modification of NBPs, and discovery of the mechanisms of NBPs as pesticidal agents. Original research articles and review articles addressing major issues related to natural bioactive product-based pesticidal agents are welcome.

Prof. Dr. Min Lv
Prof. Dr. Hui Xu
Topic Editors

Keywords

Participating Journals

Journal Name	Impact Factor	CiteScore	Launched Year	First Decision (median)	APC
Agrochemicals agrochemicals	-	-	2022	16.7 Days	CHF 1000	Submit
Agronomy agronomy	3.3	6.2	2011	17.6 Days	CHF 2600	Submit
Insects insects	2.7	5.1	2010	16.7 Days	CHF 2600	Submit
International Journal of Molecular Sciences ijms	4.9	8.1	2000	16.8 Days	CHF 2900	Submit
Marine Drugs marinedrugs	4.9	9.6	2003	13.7 Days	CHF 2900	Submit
Toxins toxins	3.9	7.5	2009	20.3 Days	CHF 2700	Submit
Agriculture agriculture	3.3	4.9	2011	19.2 Days	CHF 2600	Submit
Biology biology	3.6	5.7	2012	16.4 Days	CHF 2700	Submit

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Published Papers (6 papers)

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All Agrochemicals Agronomy Insects IJMS Marine Drugs Toxins Agriculture Biology

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23 pages, 2295 KiB  

Open AccessArticle

Laboratory-Scale Evaluation of a Plant-Based Algaecide for Harmful and Non-Harmful Algae

by Raphael M. Kudela

Toxins 2025, 17(6), 270; https://doi.org/10.3390/toxins17060270 - 27 May 2025

Abstract

Harmful algal blooms can negatively impact freshwater, estuarine, and coastal marine systems globally and pose serious risks to water quality, human and ecosystem health, and food production. Algae can produce toxic compounds, directly interfere with aquaculture species through (e.g.,) the production of foam [...] Read more.

Harmful algal blooms can negatively impact freshwater, estuarine, and coastal marine systems globally and pose serious risks to water quality, human and ecosystem health, and food production. Algae can produce toxic compounds, directly interfere with aquaculture species through (e.g.,) the production of foam or mucilage, as well as causing diseases and disorders in fish, and can result in hypoxic conditions when the bloom senesces. Application of US Environmental Protection Agency (USEPA) registered algaecides can be effective, scalable, and inexpensive, but there is growing interest in plant- or bacterial-derived compounds that do not require the use of chemicals such as hydrogen peroxide or copper. The algaecide C7X1 is a plant-based organic algaecide that proves effective against a wide variety of algae, including harmful algal species such as Microcystis, Heterosigma, and Pseudo-nitzschia. Performance is comparable to other USEPA-registered algaecides, with low to moderate extracellular toxin release and a potential lifetime of weeks in treated waters. The mode of action is inhibition of photosynthesis, suggesting that direct off-target impacts on zooplankton and other organisms would be minimal. Full article

(This article belongs to the Topic Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition)

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29 pages, 9837 KiB  

Open AccessReview

Osthole: A Coumarin with Dual Roles in Biology and Chemistry

by Min Lv, Haixia Ding and Hui Xu

Biology 2025, 14(6), 588; https://doi.org/10.3390/biology14060588 - 22 May 2025

Viewed by 121

Abstract

Osthole is a natural coumarin-like compound isolated from the Fructus cnidii. In the last few years, this plant-derived product and its derivatives have aroused much attention for their interesting biological activities, including anticancer, anti-inflammatory, neuroprotective, and insecticidal effects. This review summarizes the [...] Read more.

Osthole is a natural coumarin-like compound isolated from the Fructus cnidii. In the last few years, this plant-derived product and its derivatives have aroused much attention for their interesting biological activities, including anticancer, anti-inflammatory, neuroprotective, and insecticidal effects. This review summarizes the recent progress on the biological activities of osthole and its derivatives from 2018 to early 2025, with a focus on their total synthesis, structural modifications, and mechanisms of action. Additionally, structure–activity relationships (SARs) of osthole derivatives are presented. This review aims to serve as a comprehensive reference for future research on osthole and its derivatives in both medicinal and agricultural applications. Full article

(This article belongs to the Topic Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition)

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15 pages, 8520 KiB  

Open AccessArticle

Natural Product-Based Fungicides: Design, Synthesis, and Antifungal Activity of Rhein Derivatives Against Phytopathogenic Fungi

by Xiang Zhu, Li Li, Jinchao Shi, Yao Tian, Guoqing Mao, Xiaojun Zhang, Linhua Yu and Junkai Li

Agronomy 2025, 15(5), 1148; https://doi.org/10.3390/agronomy15051148 - 8 May 2025

Viewed by 257

Abstract

With the long-term use of certain types of traditional chemical fungicides, phytopathogen resistance and environmental pollution have made the application of these fungicides face unprecedented challenges. Therefore, using the low toxicity and structural diversity of natural product analogs to develop alternatives has become [...] Read more.

With the long-term use of certain types of traditional chemical fungicides, phytopathogen resistance and environmental pollution have made the application of these fungicides face unprecedented challenges. Therefore, using the low toxicity and structural diversity of natural product analogs to develop alternatives has become an important tactic to improve control efficiency and reduce pathogen resistance, as well as environmental risks. In this study, thirty-eight rhein derivatives were synthesized after our continuous efforts aiming to discover new anthraquinone-based antifungal agents. Their structures were characterized by ¹H-NMR, ¹³C-NMR and high-resolution mass spectrometry. The antifungal activities of rhein derivatives were first evaluated against four phytopathogenic fungi. The bioassay results indicated that most derivatives exhibited good antifungal activity against Rhizoctonia solani at 0.5 mM in vitro. Compounds 3e, 3j, 4a, 9d and 10f showed potent activities against R. solani, with inhibition rates over 50% at a low concentration of 0.2 mM in vitro. In particular, compound 10a strongly inhibited the growth of Sclerotinia sclerotiorum, Fusarium graminearum and P. capsica, with EC₅₀ values of 0.079 mM, 0.082 mM and 0.134 mM, respectively, which are comparable to the commercial biofungicide phenazine-1-carboxylic acid (PCA). An in vivo study showed that 10a presented excellent curative and protective activities (92.1% and 91.1%, 0.2 mM) against wheat powdery mildew. The phytotoxicity results indicated that rhein amino acid derivatives could significantly eliminate phytotoxicity to rice and rape and could be safely used in these two crops. The resistance development assay indicated that these rhein derivatives could effectively avoid the risk of resistance development in these two strains of fungi, R. solani and S. sclerotiorum. In conclusion, rhein derivatives can be used for the development of potential agricultural fungicides. Full article

(This article belongs to the Topic Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition)

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18 pages, 5879 KiB  

Open AccessArticle

Design, Synthesis, and Herbicidal Activity of Novel 5-Acylbarbituric Acid Derivatives Containing a Pyrimidinedione Moiety

by Ke Chen, Shumin Wang, Shuyue Fu, Wei Gao, Junehyun Kim, Phumbum Park, Rui Liu and Kang Lei

Agronomy 2025, 15(4), 777; https://doi.org/10.3390/agronomy15040777 - 22 Mar 2025

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Abstract

In continuation of our efforts to identify novel herbicide lead compounds with enhanced activity, a series of eighteen 5-acylbarbituric acid derivatives containing a pyrimidinedione moiety were designed and synthesized. Their herbicidal activities were subsequently evaluated in the greenhouse. Bioassay results demonstrated that most [...] Read more.

In continuation of our efforts to identify novel herbicide lead compounds with enhanced activity, a series of eighteen 5-acylbarbituric acid derivatives containing a pyrimidinedione moiety were designed and synthesized. Their herbicidal activities were subsequently evaluated in the greenhouse. Bioassay results demonstrated that most of the newly synthesized compounds exhibited significant herbicidal efficacy at a dosage of 150 g ha⁻¹, with compounds BA-I-2, BA-II-2, BA-III-2, and BA-III-5 achieving complete inhibition of the tested weeds. Further investigation into the herbicidal spectrum revealed that compounds BA-II-2 and BA-III-2 displayed excellent herbicidal activity against 14 and 13 out of 16 tested weed species, respectively, with inhibition rates exceeding 80% at dosages as low as 18.8 g ha⁻¹. More promisingly, compound BA-III-2 was found to be safe for Triticum aestivum at a dosage of 37.5 g ha⁻¹. Molecular mode of action studies, including phenotypic observations, membrane permeability evaluations, and molecular docking, suggested that BA-III-2 may function as a protoporphyrinogen IX oxidase (PPO) inhibitor. The present work indicates that BA-III-2 holds potential as a PPO-inhibiting herbicide for effective weed control in wheat fields and is expected to provide important theoretical foundations for the development of novel and highly efficient herbicides. Full article

(This article belongs to the Topic Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition)

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28 pages, 4193 KiB  

Open AccessReview

4(3H)-Quinazolinone: A Natural Scaffold for Drug and Agrochemical Discovery

by Ke Chen, Shumin Wang, Shuyue Fu, Junehyun Kim, Phumbum Park, Rui Liu and Kang Lei

Int. J. Mol. Sci. 2025, 26(6), 2473; https://doi.org/10.3390/ijms26062473 - 10 Mar 2025

Viewed by 566

Abstract

4(3H)-quinazolinone is a functional scaffold that exists widely both in natural products and synthetic organic compounds. Its drug-like derivatives have been extensively synthesized with interesting biological features including anticancer, anti-inflammatory, antiviral, antimalarial, antibacterial, antifungal, and herbicidal, etc. In this review, we [...] Read more.

4(3H)-quinazolinone is a functional scaffold that exists widely both in natural products and synthetic organic compounds. Its drug-like derivatives have been extensively synthesized with interesting biological features including anticancer, anti-inflammatory, antiviral, antimalarial, antibacterial, antifungal, and herbicidal, etc. In this review, we highlight the medicinal and agrochemical versatility of the 4(3H)-quinazolinone scaffold according to the studies published in the past six years (2019–2024), and comprehensively give a summary of the target recognition, structure–activity relationship, and mechanism of its analogs. The present review is expected to provide valuable guidance for discovering novel lead compounds containing 4(3H)-quinazolinone moiety in both drug and agrochemical research. Full article

(This article belongs to the Topic Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition)

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10 pages, 2067 KiB  

Open AccessArticle

Euphraticanoids N–T: Aromadendrane-Type Diterpenes and Sesquiterpenes with Fungicidal Activities from Populus euphratica Resins

by Qinbin Jiang, Yun-Yun Liu, Danling Huang and Yong-Xian Cheng

Int. J. Mol. Sci. 2025, 26(5), 2187; https://doi.org/10.3390/ijms26052187 - 28 Feb 2025

Viewed by 405

Abstract

Seven previously undescribed terpenoids, including five prenylaromadendrane-type diterpenes euphraticanoids N–R (1–5) and two aromadendrane-type sesquiterpenes, euphraticanoids S and T (6 and 7), were isolated from Populus euphratica resins. Their structures, including their absolute configurations, were elucidated by [...] Read more.

Seven previously undescribed terpenoids, including five prenylaromadendrane-type diterpenes euphraticanoids N–R (1–5) and two aromadendrane-type sesquiterpenes, euphraticanoids S and T (6 and 7), were isolated from Populus euphratica resins. Their structures, including their absolute configurations, were elucidated by HRESIMS and spectroscopic analysis, ECD calculations, and crystallographic methods. In addition, an evaluation of the fungicidal activities of compound 1 was carried out, resulting in the discovery of 1 as a fungicidal candidate lead compound with an EC₅₀ of 15.7 and 68.6 mg/L against Curvularia mebaldsii and Fusarium graminearum, respectively. Full article

(This article belongs to the Topic Research on Natural Bioactive Product-Based Pesticidal Agents—2nd Edition)

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