A gum Arabic assisted sustainable drug delivery system for adult Drosophila
A gum Arabic assisted sustainable drug delivery system for adult Drosophila
复制标题
阿拉伯胶辅助成年果蝇可持续给药系统
DOI：
10.1242/bio.052241
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发表时间：
2020-06
期刊：
影响因子：
2.4
通讯作者：
Deng Hansong
中科院分区：
文献类型：
--
作者：
Liang Qiying;Ma Peng;Zhang Qi;Yin Youjie;Wang Ping;Wang Saifei;Zhang Yao;Han Ruolei;Deng Hansong
摘要 由于缺乏连续给药系统和众多化合物的溶解度差，阻碍了对成年果蝇的大规模化合物筛选。在这里，我们发现阿拉伯胶（金合欢树胶/塞内加尔树胶）是一种广泛使用的稳定剂，也可以乳化亲脂性化合物，并极大地增加其对果蝇和小鼠靶组织的可及性。我们进一步开发了一种基于阿拉伯胶的药物输送系统，其中药物被研磨成阿拉伯胶，并通过 U 形玻璃毛细管虹吸而乳化在喂给苍蝇的液体食物中。该系统不影响食物摄入或细胞活力。由于药物是通过虹吸作用连续输送的，因此化合物浪费最少，食物更换频率较低，使该系统成为大规模长期筛查的理想选择。在我们对 NCI DTP 库中的抗肿瘤药物进行初步筛选时，我们使用了结直肠癌的果蝇模型，并鉴定了两种特别疏水且在之前的筛选中未鉴定出的药物。我们的数据表明，阿拉伯胶有利于动物模型中的药物输送，该系统适用于果蝇的长期高通量药物筛选。该系统将加速慢性和认知疾病的药物发现。摘要：药物不溶性和缺乏连续递送系统是果蝇大规模化合物筛选的巨大挑战。作者开发了U-GLAD系统，可以成功解决这些问题。
ABSTRACT Large-scale compound screening in adult flies is hampered by the lack of continuous drug delivery systems and poor solubility of numerous compounds. Here we found that gum Arabic (Acacia/Senegal gum), a widely used stabilizer, can also emulsify lipophilic compounds and profoundly increase their accessibility to target tissues in Drosophila and mice. We further developed a gum Arabic-based drug delivery system, wherein the drug was ground into gum Arabic and emulsified in liquid food fed to flies by siphoning through a U-shape glass capillary. This system did not affect food intake nor cell viability. Since drugs were continuously delivered by siphoning, minimal compound waste and less frequent food changes make this system ideal for large-scale long-term screenings. In our pilot screening for antitumor drugs in the NCI DTP library, we used a Drosophila model of colorectal cancer and identified two drugs that are especially hydrophobic and were not identified in previous screenings. Our data demonstrated that gum Arabic facilitates drug delivery in animal models and the system is suitable for long-term high-throughput drug screening in Drosophila. This system would accelerate drug discovery for chronic and cognitive conditions. Summary: Drug insolubility and a lack of a continuous delivery system are big challenges for large-scale compound screenings in flies. The authors developed a U-GLAD system that can successfully solve these issues.
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DOI：
10.1073/pnas.0702726104
发表时间：
2007-05-15
影响因子：
11.1
作者：
Ja, William W.;Carvalho, Gil B.;Benzer, Seymour
通讯作者：
Benzer, Seymour
影响因子：
4.3
作者：
Willoughby LF;Schlosser T;Manning SA;Parisot JP;Street IP;Richardson HE;Humbert PO;Brumby AM
通讯作者：
Brumby AM
影响因子：
12.4
作者：
Fan, Y.;Bergmann, A.
通讯作者：
Bergmann, A.
DOI：
10.3390/molecules22111789
发表时间：
2017-11-10
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
de Abreu Costa L;Henrique Fernandes Ottoni M;Dos Santos MG;Meireles AB;Gomes de Almeida V;de Fátima Pereira W;Alves de Avelar-Freitas B;Eustáquio Alvim Brito-Melo G
通讯作者：
Eustáquio Alvim Brito-Melo G
影响因子：
9.2
作者：
McClung, C;Hirsh, J
通讯作者：
Hirsh, J