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从黄连中分离和定量小檗碱:体外抗氧化活性和计算机辅助抗糖尿病活性评价。

Isolation and Quantification of Palmatine from Lour: In Vitro Antioxidant Activity and In Silico Antidiabetic Activity Evaluation.

机构信息

Department of Chemistry, Faculty of Mathematics and Natural Science, Universitas Padjadjaran, Sumedang, 45363, Indonesia.

Department of Medical Laboratory Technology, Poltekkes Kemenkes Pontianak, Pontianak, 78124, Indonesia.

出版信息

Drug Des Devel Ther. 2024 Aug 2;18:3443-3459. doi: 10.2147/DDDT.S454091. eCollection 2024.

Abstract

PURPOSE

This study aimed to isolate and characterize palmatine from Lour stems, quantify its content, and determine its antioxidant and antidiabetic activities.

PATIENTS AND METHODS

Palmatine was isolated from the methanol extract of Lour stems by silica gel column chromatography. Structural elucidation of the isolated compounds was performed using spectral data analysis and comparison with the literature. High-Performance Liquid Chromatography (HPLC) was used to quantitatively determine palmatine in the crude methanol extract and fractions. The DPPH and non-enzymatic SOD mimic methods were used to assess the antioxidant activity of the methanol extract, fractions, and isolated compounds. The antidiabetic activity was evaluated in silico by the molecular docking method of alpha-glucosidase and DPP-IV enzymes. Palmatine was used as a test ligand and was compared with berberine and its native ligand or standard compounds.

RESULTS

The isolated compound was identified as palmatine. Quantification of palmatine compound by HPLC showed that palmatine was found in the extract and all fractions. In the in vitro antioxidant activity test using the DPPH method, fraction 4 showed the highest activity, with an IC value of 91 ppm. In contrast, using the non-enzymatic SOD mimic method, the methanol extract, fraction 5, and isolated compound (palmatine) exhibited very strong antioxidant activity, with IC values of 18, 20, and 28 ppm, respectively. The in silico antidiabetic activity of palmatine is thought to have the potential to inhibit these two enzymes.

CONCLUSION

These results showed that Lour stems have potential as an antioxidant and antidiabetic agent. Further research on phytochemical and pharmacological is required to validate the use of this plant species for the treatment of various diseases, especially diabetes mellitus.

摘要

目的

本研究旨在从莲叶茎中分离并鉴定小檗碱,定量其含量,并测定其抗氧化和抗糖尿病活性。

方法

通过硅胶柱层析从莲叶茎甲醇提取物中分离小檗碱。通过光谱数据分析和与文献比较对分离化合物的结构进行了鉴定。高效液相色谱(HPLC)用于定量测定粗甲醇提取物和馏分中的小檗碱。DPPH 和非酶 SOD 模拟方法用于评估甲醇提取物、馏分和分离化合物的抗氧化活性。采用分子对接法对α-葡萄糖苷酶和 DPP-IV 酶进行了抗糖尿病活性评价。以小檗碱为测试配体,与黄连素及其天然配体或标准化合物进行了比较。

结果

分离得到的化合物被鉴定为小檗碱。通过 HPLC 对小檗碱化合物进行定量,结果表明小檗碱存在于提取物和所有馏分中。在 DPPH 法体外抗氧化活性试验中,第 4 馏分显示出最高的活性,IC 值为 91 ppm。相比之下,在非酶 SOD 模拟法中,甲醇提取物、第 5 馏分和分离化合物(小檗碱)表现出非常强的抗氧化活性,IC 值分别为 18、20 和 28 ppm。小檗碱的计算机模拟抗糖尿病活性被认为有可能抑制这两种酶。

结论

这些结果表明,莲叶茎具有作为抗氧化剂和抗糖尿病剂的潜力。需要进一步进行植物化学和药理学研究,以验证该植物物种用于治疗各种疾病(特别是糖尿病)的用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b08d/11302523/934986f40d26/DDDT-18-3443-g0001.jpg

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