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Fraxinellone: From pesticidal control to cancer treatment
Pesticide Biochemistry and Physiology ( IF 4.2 ) Pub Date : 2020-09-01 , DOI: 10.1016/j.pestbp.2020.104624 Christian Bailly 1 , Gérard Vergoten 2
Pesticide Biochemistry and Physiology ( IF 4.2 ) Pub Date : 2020-09-01 , DOI: 10.1016/j.pestbp.2020.104624 Christian Bailly 1 , Gérard Vergoten 2
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Fraxinellone (FRA) is a degraded limonoid isolated from the root bark of Dictamnus plants. The potent insecticidal activity of FRA has led to the synthesis of numerous derivatives (presented here with the structure-activity relationships) active against the oriental armyworm Mythimna separata Walker. In addition to its pesticidal activity, the natural product displays potent anti-inflammatory and immuno-modulatory effects at the origin of hepatoprotective and anticancer properties. This mini-review provides an update of the mechanism of action of FRA to highlight the recently discovered capacity of the compound to deactivate cancer-associated fibroblasts and thus to limit the immunosuppressive tumor microenvironment. The anticancer mode of action of FRA raises new ideas to better understand its primary insecticidal activity. The relationship between drug-induced cancer cell death and insect cell death is discussed. A drug interaction with the insect cytokine growth-blocking peptide (GBP), a member of the large EGF family, is proposed, supported by preliminary molecular modeling data. Altogether, the review shed light on the pharmacological properties of fraxinellone as an antitumor agent and a natural insecticide.
中文翻译：
Fraxinellone：从杀虫剂控制到癌症治疗
Fraxinellone (FRA) 是一种从白茅属植物根皮中分离出来的降解柠檬苦素。FRA 的强效杀虫活性导致合成了许多对东方粘虫 Mythimna separata Walker 有活性的衍生物（此处以结构-活性关系呈现）。除了其杀虫活性之外，天然产物在保肝和抗癌特性的起源处显示出有效的抗炎和免疫调节作用。这篇小型综述提供了 FRA 作用机制的更新，以突出最近发现的化合物使癌症相关成纤维细胞失活的能力，从而限制免疫抑制性肿瘤微环境。FRA 的抗癌作用模式提出了新的思路，以更好地了解其主要杀虫活性。讨论了药物诱导的癌细胞死亡与昆虫细胞死亡之间的关系。在初步分子建模数据的支持下，提议与昆虫细胞因子生长阻断肽 (GBP)（大型 EGF 家族的成员）进行药物相互作用。总之，该综述阐明了弗拉辛酮作为抗肿瘤剂和天然杀虫剂的药理特性。
更新日期：2020-09-01
中文翻译：
Fraxinellone：从杀虫剂控制到癌症治疗
Fraxinellone (FRA) 是一种从白茅属植物根皮中分离出来的降解柠檬苦素。FRA 的强效杀虫活性导致合成了许多对东方粘虫 Mythimna separata Walker 有活性的衍生物（此处以结构-活性关系呈现）。除了其杀虫活性之外，天然产物在保肝和抗癌特性的起源处显示出有效的抗炎和免疫调节作用。这篇小型综述提供了 FRA 作用机制的更新，以突出最近发现的化合物使癌症相关成纤维细胞失活的能力，从而限制免疫抑制性肿瘤微环境。FRA 的抗癌作用模式提出了新的思路，以更好地了解其主要杀虫活性。讨论了药物诱导的癌细胞死亡与昆虫细胞死亡之间的关系。在初步分子建模数据的支持下，提议与昆虫细胞因子生长阻断肽 (GBP)（大型 EGF 家族的成员）进行药物相互作用。总之，该综述阐明了弗拉辛酮作为抗肿瘤剂和天然杀虫剂的药理特性。
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