Carlina Oxide类似物的合成及其杀虫功效和细胞毒性评价,Journal of Natural Products

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Carlina Oxide类似物的合成及其杀虫功效和细胞毒性评价
Journal of Natural Products ( IF 3.3 ) Pub Date : 2023-05-12 , DOI: 10.1021/acs.jnatprod.3c00137
Eleonora Spinozzi ₁ , Marta Ferrati ₁ , Cecilia Baldassarri ₁ , Filippo Maggi ₁ , Roman Pavela _{2,

3} , Giovanni Benelli ₄ , Cristina Aguzzi ₅ , Laura Zeppa ₅ , Loredana Cappellacci ₁ , Alessandro Palmieri ₆ , Riccardo Petrelli ₁

Affiliation

从植物来源中分离出的化合物代表了传统杀虫剂的创新且有前途的替代品。Carlina Oxide 是从Carlina acaulis L.（菊科）精油 (EO) 中分离出来的化合物，具有作为生物杀虫剂的巨大潜力，对各种节肢动物媒介和农业害虫有效，对非目标物种具有中等毒性。由于野生来源的产量有限，因此需要探索新的合成路线来获得具有改善的生物活性和更低的毒性的该化合物和类似物。在此，开发了卡琳娜氧化物类似物的化学合成。在媒介家蝇和致倦库蚊上评估了它们的杀虫活性说，并在人角质形成细胞系 (HaCaT) 上评估了它们的细胞毒性。将这些化合物的活性与天然对应物 EO 和 Carlina Oxide 的活性进行了比较。在家蝇测试中，类似物与纯化的氧化卡琳娜相当有效。在CX。在 quinquefasciatus检测中，间氯类似物的功效（LC ₅₀为 0.71 μg mL ^–1 ）明显高于EO 和 carlina 氧化物（LC ₅₀分别为 1.21 和 1.31 μg mL ^–1），并且比 carlina 氧化物具有更好的安全性在角质形成细胞上。总体而言，这项研究可以为可用作天然杀虫剂的卡琳娜氧化物类似物的农用化学生产开辟道路。

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Synthesis of Carlina Oxide Analogues and Evaluation of Their Insecticidal Efficacy and Cytotoxicity

Compounds isolated from botanical sources represent innovative and promising alternatives to conventional insecticides. Carlina oxide is a compound isolated from Carlina acaulis L. (Asteraceae) essential oil (EO) with great potential as bioinsecticide, being effective on various arthropod vectors and agricultural pests, with moderate toxicity on non-target species. Since the production from the wild source is limited, there is the need of exploring new synthetic routes for obtaining this compound and analogues with improved bioactivity and lower toxicity. Herein, the chemical synthesis of carlina oxide analogues was developed. Their insecticidal activity was assessed on the vectors Musca domestica L. and Culex quinquefasciatus Say, and their cytotoxicity was evaluated on a human keratinocyte cell line (HaCaT). The compounds’ activity was compared with that of the natural counterparts EO and carlina oxide. In housefly tests, the analogues were comparably effective to purified carlina oxide. In Cx. quinquefasciatus assays, the meta-chloro analogue provided a significantly higher efficacy (LC₅₀ of 0.71 μg mL^–1) than the EO and carlina oxide (LC₅₀ 1.21 and 1.31 μg mL^–1, respectively) and a better safety profile than carlina oxide on keratinocytes. Overall, this study can open the way to an agrochemical production of carlina oxide analogues employable as nature-inspired insecticides.

更新日期：2023-05-12

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