从 Fibraurea tinctoria Lour 中分离和定量棕榈碱：体外抗氧化活性和体内抗糖尿病活性评估

IF 4.7 2区医学 Q1 CHEMISTRY, MEDICINAL

Drug Design, Development and Therapy Pub Date : 2024-08-02 DOI:10.2147/dddt.s454091

Indah Purwaningsih, Iman Permana Maksum, Dadan Sumiarsa, Sriwidodo Sriwidodo

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引用次数: 0

摘要

目的：本研究旨在从 Fibraurea tinctoria Lour 茎中分离出棕榈碱并确定其特征，定量测定其含量，并确定其抗氧化和抗糖尿病活性：采用硅胶柱色谱法从 Fibraurea tinctoria Lour 茎的甲醇提取物中分离出巴马汀。通过光谱数据分析以及与文献的比较，对分离出的化合物进行了结构阐释。高效液相色谱法（HPLC）用于定量测定粗甲醇提取物和馏分中的巴马汀。采用 DPPH 和非酶 SOD 模拟法评估甲醇提取物、馏分和分离化合物的抗氧化活性。通过分子对接法对α-葡萄糖苷酶和 DPP-IV 酶的抗糖尿病活性进行了硅学评估。巴马汀被用作测试配体，并与小檗碱及其原配体或标准化合物进行了比较：结果：分离出的化合物被鉴定为巴马汀。通过高效液相色谱法对巴马汀化合物进行定量，结果表明在提取物和所有馏分中都发现了巴马汀。在使用 DPPH 法进行的体外抗氧化活性测试中，馏分 4 的活性最高，IC50 值为 91 ppm。相反，采用非酶切 SOD 模拟法，甲醇提取物、馏分 5 和分离化合物（巴马汀）表现出极强的抗氧化活性，IC50 值分别为 18、20 和 28 ppm。巴马汀的抗糖尿病活性被认为具有抑制这两种酶的潜力：这些结果表明，Fibraurea tinctoria Lour 茎具有作为抗氧化剂和抗糖尿病剂的潜力。需要进一步开展植物化学和药理学研究，以验证该植物物种在治疗各种疾病，尤其是糖尿病方面的应用：小檗碱巴马汀抗氧化剂抗糖尿病

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

Purpose: This study aimed to isolate and characterize palmatine from Fibraurea tinctoria Lour stems, quantify its content, and determine its antioxidant and antidiabetic activities.
Patients and Methods: Palmatine was isolated from the methanol extract of Fibraurea tinctoria 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 IC₅₀ 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 IC₅₀ 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 Fibraurea tinctoria 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.

Keywords: Fibraurea tinctoria Lour, berberine, palmatine, antioxidant, antidiabetic

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来源期刊

Drug Design, Development and Therapy CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY

CiteScore

9.00

自引率

0.00%

发文量

382

审稿时长

>12 weeks

期刊介绍： Drug Design, Development and Therapy is an international, peer-reviewed, open access journal that spans the spectrum of drug design, discovery and development through to clinical applications. The journal is characterized by the rapid reporting of high-quality original research, reviews, expert opinions, commentary and clinical studies in all therapeutic areas. Specific topics covered by the journal include: Drug target identification and validation Phenotypic screening and target deconvolution Biochemical analyses of drug targets and their pathways New methods or relevant applications in molecular/drug design and computer-aided drug discovery* Design, synthesis, and biological evaluation of novel biologically active compounds (including diagnostics or chemical probes) Structural or molecular biological studies elucidating molecular recognition processes Fragment-based drug discovery Pharmaceutical/red biotechnology Isolation, structural characterization, (bio)synthesis, bioengineering and pharmacological evaluation of natural products** Distribution, pharmacokinetics and metabolic transformations of drugs or biologically active compounds in drug development Drug delivery and formulation (design and characterization of dosage forms, release mechanisms and in vivo testing) Preclinical development studies Translational animal models Mechanisms of action and signalling pathways Toxicology Gene therapy, cell therapy and immunotherapy Personalized medicine and pharmacogenomics Clinical drug evaluation Patient safety and sustained use of medicines.