UMR 1270 QUALITROP, Université des Antilles, Campus de Fouillole, BP 250, 97157, Pointe à Pitre Cedex, Guadeloupe; EA 7525 Vulnérabilité Cardiovasculaire, Pathologie Métabolique et Endocrinienne, Université des Antilles, Campus de Fouillole, BP 250, 97157, Pointe à Pitre Cedex, Guadeloupe.
UMR 1270 QUALITROP, Université des Antilles, Campus de Fouillole, BP 250, 97157, Pointe à Pitre Cedex, Guadeloupe; Department of Biology, Université des Antilles, Campus de Fouillole, BP 250, 97157, Pointe à Pitre Cedex, Guadeloupe.
J Ethnopharmacol. 2023 Oct 28;315:116619. doi: 10.1016/j.jep.2023.116619. Epub 2023 May 16.
Extracts of the aerial part of Phyllanthus amarus have been extensively used in several countries to cure diabetes. No data is available on the impact of gastrointestinal digestion of such crude extracts on their antidiabetic activity.
The aim of this study was to identify active fractions and compounds of fresh aerial parts of P. amarus extracted by an infusion method that are responsible for antidiabetic effects occurring at the level of glucose homeostasis.
An aqueous extract was obtained by an infusion method and its polyphenolic composition was analysed by reverse phase UPLC-DAD-MS. The influence of in vitro gastrointestinal digestion was evaluated both on the chemical composition and on the antidiabetic effect of P. amarus infusion extract using glucose-6-phosphatase enzyme inhibition and stimulation of glucose uptake.
Analysis of the chemical composition of the crude extract revealed the presence of polysaccharides and various families of polyphenols such as phenolic acids, tannins, flavonoids and lignans. After simulated digestion, the total content of polyphenols decreased by about 95%. Caffeoylglucaric acid derivates and lignans exhibited strong stimulation of glucose uptake similar to metformin with an increase of 35.62 ± 6.14% and 34.74 ± 5.33% respectively. Moreover, corilagin, geraniin, the enriched polysaccharides fraction and the bioaccessible fraction showed strong anti-hyperglycemic activity with about 39-62% of glucose-6-phosphatase inhibition.
Caffeoylglucaric acid isomers, tannin acalyphidin M1 and lignan demethyleneniranthin were reported for the first time in the species. After in vitro gastroinstestinal digestion, the composition of the extract changed. The dialyzed fraction showed strong glucose-6-phosphatase inhibition.
叶下珠的地上部分提取物已在多个国家广泛用于治疗糖尿病。目前尚无数据表明此类粗提取物的胃肠道消化对其抗糖尿病活性的影响。
本研究的目的是鉴定叶下珠新鲜地上部分经浸提法提取的具有抗糖尿病作用的活性部位和化合物，这些活性部位和化合物作用于葡萄糖稳态水平。
采用浸提法获得水提物，并通过反相 UPLC-DAD-MS 分析其多酚组成。采用葡萄糖-6-磷酸酶抑制和刺激葡萄糖摄取的方法，评估体外胃肠消化对叶下珠浸提物的化学成分和抗糖尿病作用的影响。
对粗提取物的化学成分分析表明，存在多糖和各种多酚类物质，如酚酸、单宁、类黄酮和木脂素。模拟消化后，多酚总含量下降约 95%。咖啡酰葡萄糖酸衍生物和木脂素表现出与二甲双胍相似的强烈刺激葡萄糖摄取作用，分别增加 35.62±6.14%和 34.74±5.33%。此外，柯里拉京、鹤氏鞣花酸、富多糖部分和生物可利用部分对葡萄糖-6-磷酸酶表现出较强的抑制活性，抑制率约为 39-62%。
首次在该物种中报道了咖啡酰葡萄糖酸异构体、单宁阿卡里平 M1 和木脂素去甲尼兰汀。体外胃肠消化后，提取物的组成发生了变化。可透析部分对葡萄糖-6-磷酸酶有很强的抑制作用。
