General Toxicity screening of Royleanone derivatives using an Artemia salina model

E. Ntungwe, Vera M. S. Isca, A. Díaz-Lanza, Carlos A. M. Afonso, P. Rijo
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Abstract

Cancer is the second leading cause of death globally. World Health Organization recorded an estimated 9.6 million deaths attributed to cancer in 2018. There is an urgent need for new anticancer drugs with novel modes of action. Natural products remain a valuable source for the identification and development of novel treatment options for cancer. Plectranthus species are well-known medicinal species used extensively for the treatment of different illnesses. These species are rich in diterpenoids which are reported to be responsible for various pharmacological activities including cytotoxic activities. Brine shrimp (Artemia salina) is broadly used in lethality studies and this model is a convenient starting point for cytotoxicity study when screening for general toxicity of natural products. This assay is based on their ability to kill a laboratory cultured nauplii. In this work, we report the general toxicity of some derivatives from 6,7-dehydroroyleanone (1) and 7α-acetoxy-6β-hydroxyroyleanone (2) compounds. The A. salina bioassay is a simple, rapid, and low-cost test, and is very useful for preliminary assessment of general toxicity in natural products thereby guiding the determination of possible biological activities.
利用盐蒿模型筛选Royleanone衍生物的一般毒性
癌症是全球第二大死因。据世界卫生组织记录,2018年约有960万人死于癌症。迫切需要具有新型作用方式的新型抗癌药物。天然产物仍然是鉴别和开发癌症新治疗方案的宝贵来源。石竹属植物是众所周知的药用植物,广泛用于治疗各种疾病。这些物种富含二萜,据报道,二萜具有多种药理活性,包括细胞毒性活性。卤虾(Artemia salina)在致死性研究中被广泛使用,在筛选天然产物的一般毒性时,该模型是细胞毒性研究的一个方便的起点。这项试验是基于它们杀死实验室培养的nauplii的能力。在这项工作中,我们报道了6,7-脱氢royleone(1)和7α-乙酰氧基-6 - β-羟基royleone(2)化合物衍生物的一般毒性。盐藻生物测定是一种简单、快速、低成本的试验方法,可用于初步评价天然产物的一般毒性,从而指导确定其可能的生物活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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