Study on the taste-masking effect and mechanism of Acesulfame K on berberine hydrochloride

Abstract

Objective

In our previous taste-masking study, we found that Acesulfame K (AK) had a better taste-masking effect than other high-efficiency sweeteners for several representative bitter natural drugs in aqueous decoction. Furthermore, we performed a preliminary taste-masking study of AK for representative bitter API Berberine Hydrochloride (BH) and found that it had a good taste-masking effect. We also found that flocculent precipitation was generated in the BH solution, but it was not clear whether it was related to the good taste-masking effect. This study was conducted to explore the taste-masking effect and mechanism of AK on BH.

Methods

The taste-masking effect of AK on BH was evaluated based on the Traditional Human Taste Panel Method and the electronic tongue evaluation method. DSC, XRD, and molecular simulation techniques were used to explore the mechanism of AK on BH, from the macro level and molecular level, respectively.

Results

When evaluating the taste-masking effect, we found that 0.1% AK had the best taste-masking effect on BH, while higher concentrations had a worse taste-masking effect. DSC and XRD revealed that the flocculent precipitation was a complex AK-BH. Finally, by simulating the binding of AK, BH, and TAS2R46 receptors, we found the unique taste-masking mechanism of AK.

Conclusion

The sweet taste stimulus of AK can mask the bitter taste stimulus of BH, and AK can generate AK-BH with BH to reduce the contact between BH and bitter taste receptors. Additionally, it could block the expression of the TAS2R46 receptors.

Graphical Abstract

Keywords:

• Acesulfame K
• berberine hydrochloride
• taste-masking
• traditional human taste panel method
• E-tongue
• TAS2R

Acknowledgments

Thanks to Professor Zhongyi Zhang of the Zhengzhou University of Light Industry for assisting in the DSC analysis. And thank Associate Professor Bing Xu of Beijing University of Chinese Medicine, Associate Researcher Zhaozhou Lin of Beijing Institution of Tongrentang, and Dr. Xinguang Liu of Henan University of Chinese Medicine for their linguistic assistance during the preparation of this manuscript.

Author contributions

Ruixin Liu conceptualized and designed the research and drafted the initial manuscript. Junhan Shi, Yousong Yue, and Chenxu Li made contributions to the study of THTPM. Xiangxiang Wu, Haiyang Li, and Xinjing Gui contributed to the E-tongue evaluation and DSC analysis. Jing Yao, Lu Zhang, and Junming Wang contributed to the X-ray diffraction analysis. Haiyang Li, Xuehua Fan, and Yanli Wang contributed to the study of taste-masking mechanisms at the molecular level. Xuelin Li provided some assistance in the drafting and revision of the article. Haiyang Li, Xuehua Fan, and Xiangxiang Wu also contributed to the data analysis, drafting, and revising of the paper, so Haiyang Li, Xuehua Fan, and Xiangxiang Wu contributed equally to this work. Ruixin Liu and Junhan Shi reviewed and critically revised the manuscript, and agreed to be accountable for all aspects of the work.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

We sincerely thank the National Natural Science Foundation of China Youth Fund Project (81001646), National Natural Science Foundation of China General Project (81774452 and 81773892), Henan Province Health Young and Middle-Aged Subject Leader Project (HNSWJW-2020014), Henan Province High-Level Talents Special Support ‘Central Plains Thousand Talents Plan’—‘Central Plains Youth Top-Notch Talents’ Project (ZYQR201912158), and Henan TCM Top-Notch Talents Training Project (Key Project) (2019ZYBJ07).