Plukenetia volubilis叶片是抗幽门螺旋杆菌药物的来源。

IF 4.4 2区 医学 Q1 PHARMACOLOGY & PHARMACY Frontiers in Pharmacology Pub Date : 2024-10-23 eCollection Date: 2024-01-01 DOI:10.3389/fphar.2024.1461447
Aditya Tan, Katia Castanho Scortecci, Nathalia Maira Cabral De Medeiros, Wirginia Kukula-Koch, Thomas J Butler, Sinéad Marian Smith, Fabio Boylan
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引用次数: 0

摘要

导言:幽门螺杆菌感染是全球范围内的一个重大问题,它广泛流行,并与胃炎、消化性溃疡、胃癌和粘膜相关淋巴组织(MALT)淋巴瘤有关。与此同时,由于抗生素耐药性不断增加,以及疗程长和副作用大导致的患者依从性问题,目前治疗方案的有效性受到了限制。Plukenetia volubilis(又称沙棘)是生物活性分子的重要来源。然而,有关其抗菌活性,尤其是对幽门螺杆菌的抗菌活性的研究还很缺乏:本研究采用体外和硅学方法探讨了伏牛花叶水提取物的抗幽门螺杆菌活性。采用高效液相色谱-电喷雾离子化和四极杆飞行时间质谱法(HPLC-ESI-QTOF-MS-MS)分析了叶片水提取物的化学成分特征,并鉴定了一些黄酮类化合物(如黄芪苷)和一些酚类化合物。然后,使用高速逆流色谱法(HSCCC)对从叶片水提取物中提取的乙酸乙酯进行分馏:结果:证实了从山奈酚中提取的黄酮类化合物的存在,并首次在伏牛花中分离出了黄芪苷。伏牛花水浸液、乙酸乙酯提取物和分离出的黄芪苷对幽门螺杆菌 J99 和两种临床分离株具有抗菌活性(例如,对克拉霉素耐药的临床分离株 SSR366 的最小抑菌浓度分别为 0.53、0.51 和 0.49 μg/mL)。然后,利用分子对接幽门螺杆菌的潜在蛋白靶标,通过硅学分析验证了黄芪甲素可与这些蛋白相互作用:这些研究结果表明,伏牛花粉和黄芪苷对幽门螺杆菌具有抑菌活性,经过进一步研究,有望用于治疗幽门螺杆菌。
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Plukenetia volubilis leaves as source of anti-Helicobacter pylori agents.

Introduction: Helicobacter pylori infection is a major issue worldwide, with widespread prevalence, combined with its link to gastritis, peptic ulcers, gastric cancer, and mucosa-associated lymphoid tissue (MALT) lymphoma. Meanwhile, effectiveness of current treatment protocols is limited by increasing antibiotic resistance and patient compliance issues due to long regimens and side effects. Plukenetia volubilis, or sacha inchi, is a valuable source of bioactive molecules. However, studies on its antimicrobial activity, especially against H. pylori, are lacking.

Methods: In this study, the anti-H. pylori activity of P. volubilis leaves water extract was explored using in vitro and in silico approaches. High-Performance Liquid Chromatography coupled to Electrospray Ionisation and Quadrupole Time-of-Flight Mass Spectrometry (HPLC-ESI- QTOF-MS-MS) analysis of the water extract from the leaves was used to characterise the chemical composition of the plant and allowed identification of some flavonoids, such as astragalin, and some phenolic compounds. Then, high-speed counter current chromatography (HSCCC) was used to fractionate the ethyl acetate partition obtained from the water extract from the leaves.

Results and discussion: The presence of flavonoids derived from kaempferol was confirmed and astragalin was isolated for the first time in P. volubilis. The P. volubilis water infusion, ethyl acetate extract and the isolated astragalin exhibited anti-bacterial activity against H. pylori J99 and two clinical isolates (e.g., minimum inhibitory concentrations of 0.53, 0.51 and 0.49 μg/mL, respectively, for clarithromycin-resistant clinical isolate SSR366). Then, using molecular docking for potential protein targets for H. pylori, it was verified that astragalin could interact with these proteins by in silico analysis.

Conclusion: These findings highlight that P. volubilis and astragalin produce a bacteriostatic activity against H. pylori and may have potential to be used in treatment against H. pylori, after further research.

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来源期刊
Frontiers in Pharmacology
Frontiers in Pharmacology PHARMACOLOGY & PHARMACY-
CiteScore
7.80
自引率
8.90%
发文量
5163
审稿时长
14 weeks
期刊介绍: Frontiers in Pharmacology is a leading journal in its field, publishing rigorously peer-reviewed research across disciplines, including basic and clinical pharmacology, medicinal chemistry, pharmacy and toxicology. Field Chief Editor Heike Wulff at UC Davis is supported by an outstanding Editorial Board of international researchers. This multidisciplinary open-access journal is at the forefront of disseminating and communicating scientific knowledge and impactful discoveries to researchers, academics, clinicians and the public worldwide.
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