Lafourcade Prada Ariadna, Rodríguez Amado Jesus Rafael, Trentin Perdomo Renata, Gomes Giovanna Bicudo, Tavares de Almeida Danielle Ayr, Cavalheiro Leandro Fontoura, Gasparotto Junior Arquimedes, Florentino Neto Serafim, Utrera Martines Marco Antonio
Postgraduate Program in Biotechnology, Faculty of Pharmacy, Food and Nutrition, Universidade Federal do Mato Grosso do Sul, Campo Grande CEP 79070-900, Mato Grosso do Sul, Brazil.
Postgraduate Program in Health Sciences, Faculty of Health Sciences, Federal University of Grande Dourados, Dourados CEP 79825-070, Mato Grosso do Sul, Brazil.
Pharmaceuticals (Basel). 2025 Jul 24;18(8):1094. doi: 10.3390/ph18081094.
Diabetes and cancer are two of the most life-threatening disorders affecting individuals of all ages worldwide. This study aimed to develop a novel (bocaiuva) fruit pulp oil-loaded nanoemulsion and evaluate its inhibitory effects on α-glucosidase and pancreatic lipase, as well as its antiglycant activity and cytotoxicity against cancer cells. Additionally, this study assessed the impact of both the oil and the nanoemulsion on blood cells. The pulp oil was extracted by cold pressing. The oil's physicochemical properties were determined according to the AOAC and the Brazilian Pharmacopeia. The lipid profile was performed by GC-MS. The nanoemulsion was prepared by the phase inversion method using ultrasonic stirring for particle size reduction and for homogenization. Response Surface Methodology was used for optimizing nanoemulsion preparation. Enzyme inhibition tests were conducted using assay kits. Cytotoxicity in cancer cells was evaluated using the Sulforhodamine B assay. Comprehensive physicochemical and chemical characterization of bocaiuva oil was performed, identifying oleic acid (71.25%) as the main component. The oil contains 23.04% saturated fatty acids, 73.79% monounsaturated acids, and 3.0% polyunsaturated fatty acids. The nanoemulsion (particle size 173.6 nm; zeta potential -14.10 mV) inhibited α-glucosidase (IC: 43.21 µg/mL) and pancreatic lipase (IC: 41.99 µg/mL), and revealed a potent antiglycation effect (oxidative IC0: 18.36 µg/mL; non-oxidative pathway IC: 16.33 µg/mL). The nanoemulsion demonstrated good cytotoxicity and selectivity against prostate cancer cells (IC: 19.13 µg/mL) and breast cancer cells (IC: 27.22 µg/mL), without inducing hemolysis, platelet aggregation, or anticoagulant effects. In this study, a comprehensive physical and chemical characterization of bocaiuva fruit pulp oil was conducted for the first time as a preliminary step toward its future standardization as an active ingredient in cosmetic and pharmaceutical formulations. The resulting nanoemulsion represents a novel alternative for managing diabetes and cancer. Although the nanoemulsion exhibited lower cytotoxicity compared to doxorubicin, it remains promising due to its composition of essential fatty acids, phenols, and carotenoids, which offer multiple health benefits. Further studies are needed to validate its efficacy and safety in clinical applications.
糖尿病和癌症是全球影响各年龄段人群的两种最具生命威胁的疾病。本研究旨在开发一种新型的(博卡尤瓦)果浆油负载纳米乳液,并评估其对α-葡萄糖苷酶和胰脂肪酶的抑制作用、抗糖化活性以及对癌细胞的细胞毒性。此外,本研究还评估了该油和纳米乳液对血细胞的影响。果浆油通过冷榨提取。根据美国官方分析化学家协会(AOAC)和巴西药典测定该油的理化性质。通过气相色谱 - 质谱联用(GC - MS)分析脂质谱。采用相转变法并通过超声搅拌来减小粒径和进行均质化制备纳米乳液。使用响应面法优化纳米乳液的制备。使用试剂盒进行酶抑制试验。使用磺酰罗丹明B测定法评估癌细胞的细胞毒性。对博卡尤瓦油进行了全面的理化和化学表征,确定油酸(71.25%)为主要成分。该油含有23.04%的饱和脂肪酸、73.79%的单不饱和脂肪酸和3.0%的多不饱和脂肪酸。纳米乳液(粒径173.6 nm;ζ电位 - 14.10 mV)抑制α-葡萄糖苷酶(IC₅₀:43.21 μg/mL)和胰脂肪酶(IC₅₀:41.99 μg/mL),并显示出强大的抗糖化作用(氧化途径IC₅₀:18.36 μg/mL;非氧化途径IC₅₀:16.33 μg/mL)。纳米乳液对前列腺癌细胞(IC₅₀:19.13 μg/mL)和乳腺癌细胞(IC₅₀:27.22 μg/mL)表现出良好的细胞毒性和选择性,且不诱导溶血、血小板聚集或抗凝作用。在本研究中,首次对博卡尤瓦果浆油进行了全面的理化表征,这是其未来作为化妆品和药物制剂中的活性成分实现标准化的初步步骤。所得纳米乳液是管理糖尿病和癌症的一种新型替代物。尽管与阿霉素相比,纳米乳液表现出较低的细胞毒性,但由于其富含必需脂肪酸、酚类和类胡萝卜素的成分具有多种健康益处,它仍然具有前景。需要进一步研究以验证其在临床应用中的有效性和安全性。