The inhibition of baicalein on pancreatic lipase investigated in vitro and in vivo

JSFA reports Pub Date : 2024-12-16 DOI:10.1002/jsf2.226

Rui-Yan Peng, Meng-Yao Hu, Hai-Xia Xu, Wen-Jun Wang, Zhong-Ping Yin, Ji-Guang Chen, Qing-Feng Zhang

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Abstract

Background

Obesity is increasing seriously worldwide. Inhibiting pancreatic lipase (PL) is an important way to prevent obesity. Baicalein, a dietary flavone, shows various physiological activities and has anti-obesity potential. Therefore, the inhibitory activity of baicalein on PL was investigated in present study.

Results

Baicalein exhibited a significant inhibitory effect on PL with IC₅₀ value of 68 μg/mL. Inhibition kinetics indicated that baicalein was a mixed-type inhibitor of PL. Fluorescence titration showed that baicalein could induce fluorescence quenching of PL. The binding constant (logK_a) and number of binding sites were calculated as 5.40 and 1.11, respectively. In addition, synchronous fluorescence analysis revealed that the quenching ratio of baicalein to tryptophan was greater than that of tyrosine. Circular dichroism (CD) spectrum showed that the binding of baicalein affected the secondary structure of the enzyme protein. Through molecular docking analysis, it confirmed that baicalein could interact with amino acid residues in lipase, thus reducing the enzyme catalytic activity. In vivo studies showed that oral administration of baicalein with a does of 50 mg/kg bwt significantly reduced fat absorption and increased its fecal excretion in rats.

Conclusion

Baicalein showed inhibitory activity on PL in both in vitro and in vivo studies. It may be a safe and effective dietary supplement for obesity prevention.

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体外和体内研究了黄芩素对胰脂肪酶的抑制作用

肥胖症在世界范围内日益严重。抑制胰脂肪酶（PL）是预防肥胖的重要途径。黄芩素是一种膳食黄酮，具有多种生理活性，具有抗肥胖潜力。因此，本研究对黄芩素对PL的抑制作用进行了研究。结果黄芩素对PL有明显的抑制作用，IC50值为68 μg/mL。抑制动力学表明黄芩素是一种混合型的PL抑制剂。荧光滴定显示黄芩素可以诱导PL的荧光猝灭，计算出结合常数logKa为5.40，结合位点数为1.11。此外，同步荧光分析显示黄芩苷对色氨酸的猝灭比大于酪氨酸。圆二色性（CD）光谱显示黄芩苷的结合影响了酶蛋白的二级结构。通过分子对接分析，证实黄芩素可以与脂肪酶中的氨基酸残基相互作用，从而降低酶的催化活性。体内研究表明，以50 mg/kg体重的剂量口服黄芩素可显著降低大鼠的脂肪吸收并增加其粪便排泄。结论黄芩素在体内和体外均对PL有抑制作用。它可能是一种安全有效的预防肥胖的膳食补充剂。

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JSFA reports

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