Van Der Goot Research Articles

Semi-Preparation and X-ray Single-Crystal Structures of Sophocarpine-Based Isoxazoline Derivatives and Their Pesticidal Effects and Toxicology Study.

Recently, research and development of novel pesticides from natural plant products have received much attention. To accelerate the application of sophocarpine as the agrochemical candidate, a series of novel sophocarpine-based isoxazoline derivatives were prepared by the 1,3-dipolar [2 + 3] cycloaddition reaction of sophocarpine with different chloroximes. Their structures were well characterized by high-resolution mass spectra, infrared spectra, and proton/carbon-13 nuclear magnetic resonance spectra. Eight steric configurations of compounds 5a, 5e', 5f, 5g, 5h, 5i, 5r, and 5u' were further determined by X-ray single-crystallography. Against Aphis citricola Van der Goot, compounds 5n (LD50: 0.032 μg/nymph) and 5o (LD50: 0.024 μg/nymph) exhibited greater than 3.7- and 4.9-fold potent aphicidal activity compared to sophocarpine (LD50: 0.118 μg/nymph). Against Tetranychus cinnabarinus Boisduval, derivative 5g displayed the most promising acaricidal activity with the LC50 value of 0.247 mg/mL, which was 14.2-fold that of sophocarpine. Compounds 5d and 5g also exhibited good control efficacy against T. cinnabarinus. Scanning electron microscopy images indicated that compound 5g can destroy the mite cuticle layer. These results will provide the foundation for the structural modification and use of sophocarpine derivatives as agrochemicals in the future.

Synthesis and Pesticidal Activities of Ester Derivatives of the Labdane Diterpenoid Andrographolide at the C-3 Position Containing the Isoxazoline Fragment and Their Toxicology Study against Tetranychus cinnabarinus Boisduval.

Due to the long-term overuse of chemical pesticides, serious resistance and negative problems on human health and the ecological environment have appeared. To develop plant-product-based pesticide candidates, a series of novel andrographolide ester derivatives containing the isoxazoline skeleton were prepared at the C-3 position. Their pesticidal activities were evaluated against three typical pests such as Mythimna separata Walker, Aphis citricola Van der Goot, and Tetranychus cinnabarinus Boisduval. Against M. separata, compounds Ik, IIf, IIg, and IIk showed 1.6-1.8 times insecticidal activity compared to that of andrographolide; against A. citricola, compounds 6, Ih, and IIh possessed 3.7-3.9-fold aphicidal activity compared to that of andrographolide; against T. cinnabarinus, compounds Ib, Ig, and IIk exhibited 7.4-9.1-fold promising acaricidal activity compared to that of andrographolide. It is worth mentioning that effects of IIk on morphological changes of the treated mite cuticle layer structures were observed by the scanning electron microscope imaging method. Compound IIk can be studied as a pesticidal lead for further structural modification.

Construction and Single-Crystal Structures of N-Isoxazolin-5-ylcarbonylindole Derivatives, and Their Pesticidal Activities and Toxicology Study.

To explore natural product-based pesticide candidates, a series of indole derivatives containing the isoxazoline skeleton at the N-1 position were synthesized by 1,3-dipolar [2 + 3] cycloaddition reaction. Their structures were characterized by melting points (mp), infrared (IR) spectra, proton nuclear magnetic resonance spectra (1H NMR), carbon-13 nuclear magnetic resonance spectra (13C NMR), and high resolution mass spectrometry (HRMS). The single-crystal structures of five compounds were presented. Against Tetranychus cinnabarinus Boisduval, compound 3b showed greater than 3.8-fold acaricidal activity of indole and good control effects under glasshouse conditions. Against Aphis citricola Van der Goot, compounds 3b and 3q exhibited 48.3- and 36.8-fold aphicidal activity of indole and 6-methylindole, respectively. Particularly, compound 3b showed good bioactivities against T. cinnabarinus and A. citricola. Against Eriosoma lanigerum Hausmann, compound 3h and 3i showed 2.1 and 1.9 times higher aphicidal activity compared to indole. Furthermore, the construction of the epidermal cuticle layer of 3b-treated carmine spider mites was distinctly damaged, which ultimately led to their death.

Abstract 1572: POU5F1B is a human-restricted ROCK inhibitor-sensitive oncoprotein that restructures membrane nanodomains to increase cell adhesion

Abstract Evolution confers new species with distinctive biological features, which can translate in purely mechanistic speciation or in novel phenotypic traits. POU5F1B arose by retrotransposition of POU5F1 (OCT4) in the last common ancestor of modern Hominoidae. Its human product is endowed with oncogenic properties, notably promoting gastrointestinal cancer growth and metastasis. Here, we reveal that the oncogenic action of POU5F1B requires ubiquitination of lysine residues found only in the human protein. This post-translational modification is essential for POU5F1B to localize to the cytoplasm and become acylated by the DHHC17 palmitoyltransferase. This leads to POU5F1B association with detergent-resistant membrane subdomains, where it triggers the accumulation of integrins and signaling molecules, and to a stimulation of cell focal adhesion. Finally, we determined that POU5F1B stability is critically dependent on ROCK, a crucial regulator of cytoskeletal dynamics and cell motility. Citation Format: Laia Simó-Riudalbas, Sandra Offner, Laurence Abrami, Eduard M. Unterauer, Julien Duc, Evarist Planet, Ralf Jungmann, Gisou van der Goot, Didier Trono. POU5F1B is a human-restricted ROCK inhibitor-sensitive oncoprotein that restructures membrane nanodomains to increase cell adhesion [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2024; Part 1 (Regular Abstracts); 2024 Apr 5-10; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2024;84(6_Suppl):Abstract nr 1572.

Discovery of Pesticide Candidates from Natural Plant Products: Semisynthesis and Characterization of Andrographolide-Based Esters and Study of Their Pesticidal Properties and Toxicology.

To explore the use of nonfood plant-derived secondary metabolites for plant protection, a series of ester derivatives for controlling the major migratory agricultural pests were obtained by structural modification of andrographolide, a labdane diterpenoid isolated from Andrographis paniculata. Compound Id showed good insecticidal activity against the fall armyworm Spodoptera frugiperda Smith. Compounds IIa (LC50: 0.382 mg/mL) and IIIc (LC50: 0.563 mg/mL), the acaricidal activities of which were, respectively, 13.1 and 8.9 times that of andrographolide (LC50: 4.996 mg/mL), exhibited strong acaricidal and control effects against Tetranychus cinnabarinus Boisduval. Against Aphis citricola Van der Goot, compounds IIIc and IVb displayed 3.9- and 3.7-fold pronounced aphicidal activity of andrographolide. Effects of compound Id on three protective enzymes (superoxide dismutase, peroxidase, and catalase) of S. frugiperda were also observed. The obvious differences of epidermal cuticle structures of mites treated with compound IIa were determined by scanning electron microscopy. Structure-activity relationships indicated that 14-ester derivatives of andrographolide showed potential insecticidal/acaricidal activities and can be further utilized as lead compounds.

Taxonomy and Phylogeny of the Aphid Genus Nippolachnus Matsumura, 1917, with Synonymy of the Mysterious Neonippolachnus Shinji, 1924 (Hemiptera: Aphididae: Lachninae).

Nippolachnus Matsumura, 1917 is a small aphid genus from the tribe Tuberolachnini (Hemiptera: Lachninae) occurring in Southeast Asia. Species from this genus are quite characteristic and stand out among lachnids for their morphology and ecological associations. We have performed a revision and phylogenetic analyses to elucidate the relationships within Nippolachnus and other representatives of Tuberolachnini. Here, the taxonomy of the genus is revised based on morphological data to include seven species, three of them newly described: Nippolachnus chakrabartiisp. nov. from India, Nippolachnus sinensissp. nov. from China, and Nippolachnus malayaensissp. nov. from Indonesia. Nippolachnus appear to be non monophyletic genus and a new genus, Indolachnusgen. nov., is described to accommodate Nippolachnus himalayensis (van der Goot, 1917) as Indolachnus himalayensis (van der Goot, 1917) comb. nov. The new genus is a sister group to the remaining Nippolachnus species, which created a monophyletic clade. Neonippolachnus Shinji, 1924 syn. nov. is recognised as a synonym of Nippolachnus, and Neonippolachnus betulae Shinji, 1924 syn. nov. as a synonym of Nippolachnus micromeli Shinji, 1924. For the first time, a scanning electron microscopy study of the sexual generation of N. piri Matsumura, 1917 has been performed. Apterous and alate viviparous females of N. bengalensis Basu and Hille Ris Lambers, 1968, N. piri, and N. micromeli, and alate viviparous females of N. xitianmushanus Zhang and Zhong, 1982 are re-described and illustrated, as well as apterous and alate viviparous females of I. himalayensiscomb. nov. Hitherto unknown morphs of N. micromeli, N. piri, and N. xitianmushanus are described. A lectotype and paralectotypes of N. xitianmushanus are designated herein. Notes on distribution and host plants are given, and keys to apterous and alate viviparous females of the genera Nippolachnus and Indolachnus are also provided.

First person – Samuele Metti

ABSTRACT First Person is a series of interviews with the first authors of a selection of papers published in Journal of Cell Science, helping researchers promote themselves alongside their papers. Samuele Metti is co-first author on ‘ Native collagen VI delays early muscle stem cell differentiation’, published in JCS. Samuele conducted the research described in this article while a PhD student in Prof. Paolo Bonaldo's lab at University of Padova, Italy. He is now a postdoc in the lab of Prof. Gisou van der Goot at School of Life Science, École Polytechnique Fédérale de Lausanne, Switzerland, investigating how extracellular matrix proteins affect muscle stem cell behaviour.

Morpho-Molecular Characterization and Seasonality analysis of Greenidea psidii Van Der Goot on Guava in Terai Zone of West Bengal, India

Greenidea psidii, Guava aphid comes under the subfamily Greenideinae within the Aphididae and was first discovered in the World in 1916 on guava. In terai region of West Bengal these species are regarded as potential pest of guava (Psidium guajava). Therefore, quick and precise species identification is immediately needed for early detection and risk analysis followed by integrated management of the aphid pests. During morpho- taxonomy study we found that apterous aphids have long sized siphunculi, alongwith long setae present on the body. Moreover, the identity of the aphid species was confirmed through DNA barcoding of the mitochondrial cytochrome c oxidase sub unit I (COX-I) gene, another analytical tool for quick and precise identification. The COX-I sequence was successfully blasted for similarity search and uploaded in NCBI software (Accession No. OR085959). Maximum likelihood method for phylogenetic analysis reveals that all the G. psidii sequences were clustered in the same clade and confirmed the identity of the species of the present study. The seasonal fluctuation studies reveals that the maximum population of 21.85 aphids/ twigs and 17.45 aphids/ twigs were observed on 10th SW during 2021 and on 11th SW during 2022, respectively.

Are Appearances Deceiving? Morpho-Genetic Complexity of the Eumerus tricolor Group (Diptera: Syrphidae) in Europe, with a Focus on the Iberian Peninsula.

Eumerus Meigen, 1822 is one of the largest Syrphidae genera in the Palaearctic Region, with the highest levels of taxonomic diversity found in the Eumerus tricolor species group. Despite its high diversity, the interspecific levels of morphological variability can be low. Additionally, some species may show certain levels of intraspecific variability. Hence, species delimitation may become challenging. In this work, we assessed the diversity of the E. tricolor group in the Iberian Peninsula through an integrative analysis of nomenclature, morphology and the 5' (COI-5') and 3' (COI-3') end regions of the Cytochrome c oxidase subunit I gene. Two new species, Eumerus ancylostylus Aguado-Aranda & Ricarte sp. n. and Eumerus petrarum Aguado-Aranda, Nedeljković & Ricarte sp. n., were described, and their intra- and interspecific variations discussed. In addition, the first barcodes of Iberian members of the E. tricolor group were obtained, and the distribution ranges of all species were mapped within the study area. The systematic position of the new species is discussed based on the resulting COI-based trees. The male genitalia of Eumerus hispanicus van der Goot, 1966 and Eumerus bayardi Séguy, 1961 were studied and illustrated. A lectotype was designated for Eumerus lateralis (Zetterstedt, 1819). An updated dichotomous key for all known European species of the E. tricolor group is provided. The egg of E. petrarum sp. n. is also described.

Diversity of Aphid Fauna (Hemiptera: Aphididae) of Kerala

Extensive surveys were undertaken across Kerala during 2018-22, to explore the diversity of aphid fauna associated with different flora. The study recorded 25 species of aphids under 17 genera in four tribes belonging to four subfamilies of Aphididae. Aphidinae was the predominant subfamily, followed by Greenideinae, Hormaphidinae and Eriosomatinae. Aphidinae was represented by two tribes, Aphidini and Macrosiphini. The tribes Aphidini (Aphis (L.), Rhopalosiphum Koch, Hysteroneura Davis and Melanaphis van der Goot) and Macrosiphini (Pentalonia Coquerel, Brevicoryne van der Goot, Macrosiphoniella del Guercio, Macrosiphum Passerini, Metopolophium Mordvilko, Acyrthosiphon Mordvilko, Uroleucon Mordvilko and Aulacorthum Mordvilko) were represented by four and eight genera, respectively. The subfamily Greenideinae was represented by two genera in a single tribe (Greenideini); Hormaphidinae represented by two genera in a single tribe (Cerataphidini), while only one genus in a single tribe (Eriosomatini) was recorded in the subfamily Eriosomatinae. The genus Aphis was the most diverse with five species. Aphis gossypii Glover exhibited a wider host range with 20 host plants. The study records new distribution of three aphid species from south India and seven species from Kerala.

Synthesis of Piperine-Based Ester Derivatives with Diverse Aromatic Rings and Their Agricultural Bioactivities against Tetranychus cinnabarinus Boisduval, Aphis citricola Van der Goot, and Eriosoma lanigerum Hausmann.

Exploration of plant secondary metabolites or by using them as leads for development of new pesticides has become one of the focal research topics nowadays. Herein, a series of new ester derivatives of piperine were prepared via the Vilsmeier−Haack−Arnold (VHA) reaction, and their structures were characterized by infrared spectroscopy (IR), melting point (mp), proton nuclear magnetic resonance spectroscopy (1H NMR), and carbon nuclear magnetic resonance spectroscopy (13C NMR). Notably, the steric configurations of compounds 6 and 7 were confirmed by single-crystal analysis. Against T. cinnabarinus, compounds 9 and 11 exhibited 47.6- and 45.4-fold more pronounced acaricidal activity than piperine. In particular, compounds 9 and 11 also showed 2.6-fold control efficiency on the fifth day of piperine. In addition, compound 6 (>10−fold higher than piperine) displayed the most potent aphicidal activity against A. citricola. Furthermore, some derivatives showed good aphicidal activities against E. lanigerum. Moreover, the effects of compounds on the cuticles of T. cinnabarinus were investigated by the scanning electron microscope (SEM) imaging method. This study will pave the way for future high value added application of piperine and its derivatives as botanical pesticides.

Hitherto unknown sexual morphs of Brachysiphoniella montana (van der Goot, 1917) (Hemiptera: Aphididae).

Here, we describe the hitherto unknown sexual morphs (oviparous females and males) of Brachysiphoniella montana (van der Goot, 1917) (Aphididae: Aphidinae: Macrosiphini). Oviparous females and males from the Republic of Korea are described and illustrated in details. Descriptions of sexual morphs of this species confirm the holocyclic life cycle of Brachysiphoniella in areas with cooler months. Notes about distribution and host plants of the species are also given.

S-palmitoylation of PCSK9 induces sorafenib resistance in liver cancer by activating the PI3K/AKT pathway.

Sorafenib is currently the first-line treatment for advanced hepatocellular carcinoma (HCC). However, sorafenib resistance remains a significant challenge. Aberrant AKT signaling activation is a crucial mechanism driving sorafenib resistance in HCC. Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a vital role in antitumor immune responses. In this study, we demonstrate that aberrant PCSK9 upregulation promotes cell proliferation and sorafenib resistance in HCC by inducing AKT-S473 phosphorylation. After palmitoylation at cysteine 600, the binding affinity between PCSK9 and tensin homolog (PTEN) is dramatically increased, inducing lysosome-mediated PTEN degradation and subsequent AKT activation. We identify zinc finger DHHC-type palmitoyltransferase 16 (ZDHHC16) as a palmitoyltransferase that promotes PCSK9 palmitoylation at cysteine 600. We also develop a biologically active PCSK9-derived peptide that competitively inhibits PCSK9 palmitoylation, suppressing AKT phosphorylation and augmenting the antitumor effects of sorafenib in HCC.

Construction, Pesticidal Activities, Control Effects, and Detoxification Enzyme Activities of Osthole Ester/Amide Derivatives.

Pesticide research and development has entered an era of safety, efficiency, and environmental friendliness. Discovery of effective active products directly or indirectly from plant secondary metabolites as pesticide candidates has been one of the current research focuses. Herein, two series of new ester and amide derivatives were prepared by structural modifications of a natural coumarin-type product osthole at its C-4' position. Their structures were characterized by IR, mp, 1H NMR, and HRMS. Confirmation of steric configuration of seven compounds was based on single-crystal analysis. Against Tetranychus cinnabarinus Boisduval (Acari: Tetranychidae), (2'E)-3'-ethoxycarbonylosthole (4b) and (2'E)-3'-(n)hexyloxycarbonylosthole (4e) exhibited 3.2 and 3.1 times acaricidal activity of osthole, and particularly, they also showed 2.4 and 2.2 times control efficiency on the 5th day of osthole. Against Aphis citricola Van der Goot (Homoptera: Aphididae), (2'E)-3'-(p-CF3)benzyloxycarbonylosthole (4w), (2'E)-3'-benzylaminocarbonylosthole (5f), and (2'E)-3'-phenylethylaminocarbonylosthole (5g) showed 1.9-2.1-fold aphicidal activity of osthole. Furthermore, the changes in two detoxification enzyme [carboxylesterase (CarE) and glutathione S-transferase (GST)] activities over time in treated T. cinnabarinus were investigated. These results can pave the foundation for future design and preparation of osthole derivatives as botanical agrochemicals.

STING is an intrinsic checkpoint inhibitor that restrains the TH17 cell pathogenic program.

SUMMARYExternal and intrinsic factors regulate the transcriptional profile of T helper 17 (TH17) cells, thereby affecting their pathogenic potential and revealing their context-dependent plasticity. The stimulator of interferon genes (STING), a component of the intracellular DNA-sensing pathway, triggers immune responses but remains largely unexplored in T cells. Here, we describe an intrinsic role of STING in limiting the TH17 cell pathogenic program. We demonstrate that non-pathogenic TH17 cells express higher levels of STING than those activated under pathogenic conditions. Activation of STING induces interleukin-10 (IL-10) production in TH17 cells, decreasing IL-17A and IL-23R expression in a type I interferon (IFN)-independent manner. Mechanistically, STING-induced IL-10 production partially requires aryl hydrocarbon receptor (AhR) signaling, while the decrease of IL-17A expression occurs due to a reduction of Rorγt transcriptional activity. Our findings reveal a regulatory function of STING in the TH17 cell activation program, proposing it as a valuable target to limit TH17-cell-mediated inflammation.

High Value-Added Application of Natural Plant Products in Crop Protection: Honokiol Monoester/Diester Derivatives Containing the Novel Core Scaffold of Benzodihydrofuran and Their Agricultural Bioactivities and Control Effects.

To discover new potential botanical insecticides from plant secondary metabolites, a series of new honokiol-type monoester/diester derivatives containing the core scaffold of benzodihydrofuran were synthesized by structural modification of honokiol. Against Mythimna separata Walker, 2-hydroxymethy-5-(2'-(para-chlorobenzoyloxy)-5'-(1″,2″-epoxypropanyl))phenyl-2,3-dihydrobenzofuran (5) and 2-(2″-chloropyridin-5″-ylcarbonyloxy)methylene-5-(2'-(2″-chloropyridin-5″-ylcarbonyloxy)-5'-(1″,2″-epoxypropanyl))phenyl-2,3-dihydrobenzofuran (37) displayed >2.1-fold promising insecticidal activity of the precursor honokiol. Against Aphis citricola Van der Goot, 2-hydroxymethy-5-(2'-(tridecylcarbonyloxy)-5'-(1″,2″-epoxypropanyl))phenyl-2,3-dihydrobenzofuran (21) (LD50: 0.049 μg/nymph) and 2-(para-fluorobenzylcarbonyloxy)methylene-5-(2'-(para-fluorobenzylcarbonyloxy)-5'-(1″,2″-epoxypropanyl))phenyl-2,3-dihydrobenzofuran (31) (LD50: 0.040 μg/nymph) showed 3.5- and 4.3-folds potent aphicidal activity of honokiol (LD50: 0.171 μg/nymph), respectively. Interestingly, 2-(tridecylcarbonyloxy)methylene-5-(2'-(tridecylcarbonyloxy)-5'-(1″,2″-epoxypropanyl))phenyl-2,3-dihydrobenzofuran (46) (LC50: 0.186 mg/mL) and 2-(dodecylcarbonyloxy)methylene-5-(2'-(dodecylcarbonyloxy)-5'-(1″,2″-epoxypropanyl))phenyl-2,3-dihydrobenzofuran (53) (LC50: 0.159 mg/mL: >6.4-fold of honokiol (LC50: 1.024 mg/mL)) exhibited promising acaricidal activity and control efficiency against Tetranychus cinnabarinus Boisduval. Structure-activity relationships indicated that a specific length of the aliphatic chain is necessary for the agricultural activities of honokiol monoester/diester derivatives, especially for the acaricidal activity of diester derivatives.

Construction of new oxime esters of cholesterol containing piperic acid-like fragments as insecticidal agents against Aphis citricola Van der Goot (Homoptera: Aphididae) and Plutella xylostella Linnaeus (Lepidoptera: Plutellidae)

In order to application of cholesterol as pesticidal agents, a series of oxime esters of cholesterol containing piperic acid-like fragments were semi-synthesized by modification of cholesterol at the C-3 and C-6 positions. Their structures were characterized by 1H NMR, HRMS and mp, and their purity was determined by HPLC. Against Aphis citricola Van der Goot, derivatives Ib (R = 4-FPh) and In (R = 3,4-ethylenedioxystyryl) exhibited 5.0 and 4.8 folds more pronounced aphicidal activity of their precursor cholesterol. Against Plutella xylostella Linnaeus, compounds Ia (R = Ph) and If (R = 3,4-methylenedioxyphenyl) showed 2.2 and 2.0 folds more potent insecticidal activity of cholesterol. Their SARs were also observed.

Occurrence of Aphis odinae van der Goot and its natural enemies in cashew

Occurrence of Aphis odinae van der Goot and its natural enemies in cashew

Natural-product-based pesticides: Semisynthesis, structural elucidation, and evaluation of new cholesterol–matrine conjugates as pesticidal agents

To develop new potential pesticide candidates from low value-added natural bioactive products, a series of new cholesterol–matrine conjugates (I(a–e)–IV(a–e)) were prepared from two lead compounds cholesterol and matrine. Against Mythimna separata Walker, compound IVa exhibited 3.0 and 2.6 folds promising insecticidal activity of cholesterol and matrine, respectively; against Aphis citricola Van der Goot, compound IVd showed 4.3 and 2.2 folds potent aphicidal activity of their precursors; notably, it also showed good control effects in the greenhouse; against Plutella xylostella Linnaeus at a dose of 20 μg/nymph, compound IIIe exhibited 2.8 and 2.0 folds oral toxicity of cholesterol and matrine, respectively. Compounds IIIe, IVd and IVe can be used as the leads for further structural optimization as the insecticidal and aphicidal agents.

Construction of Cholesterol Oxime Ether Derivatives Containing Isoxazoline/Isoxazole Fragments and Their Agricultural Bioactive Properties/Control Efficiency.

To explore natural-product-based pesticidal candidates and high value-added application of cholesterol in agriculture, oximinoether derivatives of cholesterol-containing isoxazoline/isoxazole fragments (I-1∼I-16 and II-1∼II-18) were semiprepared by structural optimization of cholesterol. Their structures were characterized by optical rotation, high-resolution mass spectrometry (HRMS), IR, and 1H NMR spectroscopy. Particularly, the Z configurations of oxime fragments at the C-7 position of target compounds were undoubtedly determined by X-ray crystallography. Against Mythimna separata Walker, compounds 3e, I-8, I-14, and II-3 showed 2.4-2.7-fold growth inhibitory activity of the precursor cholesterol. Against Plutella xylostella Linnaeus, compounds I-6, I-7, and I-9 showed 2.4-2.7-fold oral toxicity of cholesterol. Against Aphis citricola Van der Goot, compounds 2e and II-15 exhibited 4.9 and 5.8-fold aphicidal activity of cholesterol, respectively. Notably, they showed good control effects (3.0-5.0-fold promising control efficiency of 1) against A. citricola in the greenhouse. Structure-activity relationships (SARs) suggested that the C-3 hydroxyl group and the C-7 position of cholesterol are two important modification sites. It will pave the way for future structural optimization and application of cholesterol derivatives as potential pesticidal agents in agriculture.