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植物体递送增强了酚类提取物的生物活性。

Phytosomal delivery enhances bioactivity of phenolic extract.

作者信息

Direito Rosa, Sousa Inês, Antunes Filipa, Barbalho Sandra Maria, Simões Sandra, Bronze Maria Rosário, Reis Catarina, Gaspar Maria Manuela, Figueira Maria Eduardo

机构信息

Laboratory of Systems Integration Pharmacology, Clinical and Regulatory Science, Research Institute for Medicines (iMed.ULisboa), Universidade de Lisboa, Lisbon, Portugal.

Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal.

出版信息

Front Nutr. 2025 Aug 14;12:1659572. doi: 10.3389/fnut.2025.1659572. eCollection 2025.

Abstract

INTRODUCTION

Consuming foods rich in bioactive compounds can delay chronic non-communicable diseases. Dragon fruit, known for its bioactive compounds with typically low bioavailability-attributed to high polarity, poor permeability, and rapid firstpass metabolism-benefits from strategies like encapsulation to enhance efficacy.

METHODS

This study developed and assessed phytosomes loaded with dragon fruit extract (Hylocereus costaricensis) and compared their biological activity and against the raw extract. Spectrophotometric analysis of the extract revealed 410.4 mg GAE/L of total phenolic compounds and 139.3 mg CE/L of flavonoids. HPLC-DAD-MS/MS identified key components such as citric acid, succinic acid, cyanidin-3-O-rutinoside, ferulic acid, betanin, and rutin. Phytosomes encapsulated 46 ± 2% of phenolics, with a mean diameter of 1,329 ± 121.0 nm, PDI 0.633 ± 0.039, and -potential -16 ± 1 mV.

RESULTS

Antioxidant capacities, assessed by the DPPH method, showed that the phytosomal formulation with 46% phenolic content was as effective as the raw extract. antihyperglycemic studies showed no significant effect from the raw extract (5 mg GAE/kg), but phytosomes (2.3 mg GAE/kg) matched the efficacy of metformin (300 mg/kg). An acute inflammation model using carrageenan-induced paw edema indicated that phytosomes (2.3 mg GAE/kg) had superior anti-inflammatory effects compared to the raw extract (5 mg GAE/kg).

DISCUSSION

In summary, dragon fruit extract has antioxidant, antihyperglycemic, and anti-inflammatory properties. These findings support that phytosomal encapsulation significantly improves the bioavailability and efficacy of phenolic-rich crude extract, highlighting their potential in functional food development, nutraceutical applications, and as helpers to conventional therapeutic strategies.

摘要

引言

食用富含生物活性化合物的食物可延缓慢性非传染性疾病。火龙果以其生物活性化合物而闻名,这些化合物通常具有低生物利用度,这归因于其高极性、低渗透性和快速的首过代谢,通过包封等策略可提高其功效。

方法

本研究开发并评估了负载火龙果提取物(红肉火龙果)的植物脂质体,并将其生物活性与未加工提取物进行了比较。提取物的分光光度分析显示,总酚类化合物含量为410.4mg GAE/L,黄酮类化合物含量为139.3mg CE/L。HPLC-DAD-MS/MS鉴定出关键成分,如柠檬酸、琥珀酸、矢车菊素-3-O-芸香糖苷、阿魏酸、甜菜红素和芦丁。植物脂质体包封了46±2%的酚类物质,平均直径为1329±121.0nm,多分散指数为0.633±0.039,ζ电位为-16±1mV。

结果

通过DPPH法评估的抗氧化能力表明,酚类含量为46%的植物脂质体制剂与未加工提取物的效果相当。抗高血糖研究表明,未加工提取物(5mg GAE/kg)没有显著效果,但植物脂质体(2.3mg GAE/kg)与二甲双胍(300mg/kg)的功效相当。使用角叉菜胶诱导的爪肿胀的急性炎症模型表明,与未加工提取物(5mg GAE/kg)相比,植物脂质体(2.3mg GAE/kg)具有更强的抗炎作用。

讨论

总之火龙果提取物具有抗氧化、抗高血糖和抗炎特性。这些发现支持植物脂质体包封显著提高了富含酚类的粗提物的生物利用度和功效,突出了它们在功能性食品开发、营养保健应用以及作为传统治疗策略辅助手段方面的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7a86/12391043/c3fc591cf3cc/fnut-12-1659572-g001.jpg

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