The 5α-reductase converts testosterone to dihydrotestosterone (DHT), and excess DHT could cause androgen-related diseases such as androgenetic alopecia and benign prostatic hyperplasia (BPH). To discover new 5α-reductase inhibitors, effective drug screening method with high throughput is thus essential. In this study, fully automated chip-based nanoelectrospray ionization-mass spectrometry (nano-ESI-MS) was innovatively utilized as a screening tool for 5α-reductase inhibitory assay in direct infusion mode, which simplified sample pretreatment and greatly improved experimental efficiency. The preliminary data indicated that curcumin, a natural anti-inflammatory compound, exhibited notably 5α-reductase inhibition activity. Moreover, the obtained results of the chip-based nano-ESI-MS were well consistent with those of HPLC-MS, which suggested that the chip-based nano-ESI-MS could be treated as a rapid and high-throughput drugs screening strategy in pharmaceutical development.
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The authors would like to thank ASPEC Technologies Limited (Beijing, China) and Mr. Xiaokun Duan for their kind support of TriVersa NanoMate ion source.
The work was financially supported by the Natural Science Foundation of China (Nos. 81530096, 81573581), the Shanghai Sailing Program (No. 19YF1448800), and the China Postdoctoral Science Foundation Funded Project (No. 2019 M661597).
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Zheng, R., Li, L., Deng, X. et al. Fully automated chip-based nanoelectrospray ionization-mass spectrometry as an effective tool for rapid and high-throughput screening of 5α-reductase inhibitors. Anal Bioanal Chem 412, 1685–1692 (2020). https://doi.org/10.1007/s00216-020-02408-y
- 5α-Reductase inhibitor
- Benign prostatic hyperplasia
- Nanoelectrospray ionization
- Mass spectrometry
- Steroid hormones