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姜辣素纳米脂质体包封:体外抗炎和抗癌活性评价。

Encapsulation of gingerol into nanoliposomes: Evaluation of in vitro anti-inflammatory and anti-cancer activity.

机构信息

Pharmacological and Diagnostic Research Centre, Faculty of Pharmacy, Al-Ahliyya Amman University, Amman, Jordan.

Cell Therapy Center, The University of Jordan, Amman, Jordan.

出版信息

Biomed Chromatogr. 2024 Aug;38(8):e5899. doi: 10.1002/bmc.5899. Epub 2024 May 26.

DOI:10.1002/bmc.5899
PMID:38797863
Abstract

Nanoliposomes (NLs) are ideal carriers for delivering complex molecules and phytochemical products, but ginger by-products, despite their therapeutic benefits, have poor bioavailability due to their low water solubility and stability. Crude ginger extracts (CGEs) and 6-gingerol were individually encapsulated within NLs for in vitro activity assessment. In vitro evaluation of anti-proliferative and anti-inflammatory properties of encapsulated 6-gingerol and CGE was performed on healthy human periodontal ligament (PDL) fibroblasts and MDA-MB-231 breast cancer cells. Encapsulation efficiency and loading capacity of 6-gingerol reached 25.23% and 2.5%, respectively. NLs were found stable for up to 30 days at 4°C with a gradual load loss of up to 20%. In vitro cytotoxic effect of encapsulated 6-gingerol exceeded 70% in the MDA-MB-231 cell line, in a comparable manner with non-encapsulated 6-gingerol and CGE. The effect of CGE with an IC of 3.11 ± 0.39, 7.14 ± 0.80, and 0.82 ± 0.55 μM and encapsulated 6-gingerol on inhibiting IL-8 was evident, indicating its potential anti-inflammatory activity. Encapsulating 6-gingerol within NLs enhanced its stability and facilitated its biological activity. All compounds, including vitamin C, were equivalent at concentrations below 2 mg/mL, with a slight difference in antioxidant activity. The concentrations capable of inhibiting 50% of 2,2-diphenyl-1-picrylhydrazyl (DPPH) substrate were comparable.

摘要

纳米脂质体 (NLs) 是输送复杂分子和植物化学产品的理想载体,但生姜副产物尽管具有治疗功效,但由于其低水溶性和稳定性,生物利用度较差。将姜提取物 (CGE) 和 6-姜酚分别包封在 NLs 中,用于体外活性评估。在健康人牙周韧带 (PDL) 成纤维细胞和 MDA-MB-231 乳腺癌细胞上,对包封的 6-姜酚和 CGE 的抗增殖和抗炎特性进行了体外评价。6-姜酚的包封效率和载药量分别达到 25.23%和 2.5%。NLs 在 4°C 下稳定长达 30 天,负载损失逐渐达到 20%。包封的 6-姜酚在 MDA-MB-231 细胞系中的体外细胞毒性作用超过 70%,与未包封的 6-姜酚和 CGE 相当。CGE 的 IC 为 3.11±0.39、7.14±0.80 和 0.82±0.55μM,对抑制 IL-8 的作用明显,表明其具有潜在的抗炎活性。将 6-姜酚包封在 NLs 内可提高其稳定性并增强其生物学活性。所有化合物,包括维生素 C,在低于 2mg/mL 的浓度下效果相当,抗氧化活性略有差异。抑制 2,2-二苯基-1-苦基肼基 (DPPH) 底物 50%的浓度相当。

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