Centro de Investigaciones Farmacognósticas de la Flora Panameña (CIFLORPAN), Facultad de Farmacia, Universidad de Panamá, Estafeta de Correos, 0824-00172, Panamá, Panamá.
Departamento de Farmacología, Facultad de Medicina, Universidad de Panamá, Panama.
Comb Chem High Throughput Screen. 2024 Feb 21;27(4):545-554. doi: 10.2174/1386207326666230703095928.
The microplate benchtop brine shrimp test (BST) has been widely used for screening and bio-guided isolation of many active compounds, including natural products. Although the interpretation given to the results appears dissimilar, our findings suggest a correlation between positive results with a specific mechanism of action.
This study aimed to evaluate drugs belonging to fifteen pharmacological categories having diverse mechanisms of action and carry out a bibliometric analysis of over 700 citations related to microwell BST.
Test compounds were evaluated in a serial dilution on the microwell BST using healthy nauplii of and after 24 hrs of exposition, the number of alive and dead nauplii was determined, and the LC was estimated. A metric study regarding the citations of the BST miniaturized method, sorted by type of documents cited, contributing country, and interpretation of results was conducted on 706 selected citations found in Google Scholar.
Out of 206 drugs tested belonging to fifteen pharmacological categories, twenty-six showed LC values <100 μM, most of them belonging to the category of antineoplastic drugs; compounds with different therapeutical uses were found to be cytotoxic as well. A bibliometric analysis showed 706 documents citing the miniaturized BST; 78% of them belonged to academic laboratories from developing countries located on all continents, 63% interpreted their results as cytotoxic activity and 35% indicated general toxicity assessment.
BST is a simple, affordable, benchtop assay, capable of detecting cytotoxic drugs with specific mechanisms of action, such as protein synthesis inhibition, antimitotic, DNA binding, topoisomerase I inhibitors, and caspases cascade interfering drugs. The microwell BST is a technique that is used worldwide for the bio-guided isolation of cytotoxic compounds from different sources.
微孔板盐水虾试验（BST）已广泛用于筛选和生物导向分离许多活性化合物，包括天然产物。尽管给出的结果解释似乎不同，但我们的发现表明阳性结果与特定作用机制之间存在相关性。
本研究旨在评估属于十五种药理学类别的药物，这些药物具有不同的作用机制，并对与微孔 BST 相关的 700 多个引文进行文献计量分析。
使用 和健康无节幼体在微孔 BST 上进行连续稀释测试化合物，暴露 24 小时后，确定存活和死亡无节幼体的数量，并估计 LC 值。对从 Google Scholar 中选择的 706 个引文进行分类，按引用文献类型、贡献国家和结果解释进行微型 BST 引用的度量研究。
在属于十五种药理学类别的 206 种测试药物中，有 26 种药物的 LC 值<100 μM，其中大多数属于抗肿瘤药物类别；还发现具有不同治疗用途的化合物具有细胞毒性。文献计量分析显示，有 706 篇文献引用了微型 BST；其中 78%属于来自各大洲发展中国家的学术实验室，63%将其结果解释为细胞毒性活性，35%表示一般毒性评估。
BST 是一种简单、经济实惠的台式测定法，能够检测具有特定作用机制的细胞毒性药物，如蛋白质合成抑制、抗有丝分裂、DNA 结合、拓扑异构酶 I 抑制剂和 Caspases 级联干扰药物。微孔 BST 是一种在全球范围内用于从不同来源生物导向分离细胞毒性化合物的技术。
