Bioactive metabolites of Brazilian Red Propolis: Cytotoxic, antimalarial, and antimicrobial properties.

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL Fitoterapia Pub Date : 2024-12-18 DOI:10.1016/j.fitote.2024.106351

Jennyfer Andrea Aldana-Mejía, Victor Pena Ribeiro, Kumudini M Meepagala, Jairo Kenupp Bastos, Samir A Ross

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Abstract

Brazilian Red Propolis (BRP) is a natural product known for its rich chemical composition and therapeutic potential. This study investigates the phytochemical profile and evaluates the cytotoxic, antiplasmodial, and antimicrobial properties of red propolis extract and its isolated compounds vestitol (1), neovestitol (2), medicarpin (3), 7-O-methylvestitol (4), and oblongifolin B (5). The extract showed selective cytotoxicity against cancer cell lines (IC₅₀: 16-39 μg/mL). Compound 3 exhibited a promising cytotoxicity against SK-OV-3 with and IC₅₀ of 6.65 μM. BRP had moderate antimicrobial effects; however, 3 was effective against Cryptococcus neoformans (IC₅₀: 19.29 μM), while 5 was active against Pseudomonas aeruginosa (IC₅₀: 15.77 μM). BRP exhibited antiplasmodial activity against Plasmodium falciparum strains D6 and W2 (IC₅₀: 13.8 μg/mL and 5.7 μg/mL); also, 4 and 5 had IC₅₀ concentrations ranging from: 2.99-6.96 μM). Molecular docking for P. falciparum lactate dehydrogenase (PfLDH), suggest that compound 4 has significant interactions with critical residues in the PfLDH active site, such as TYR85, THR97, and ASP53, and falls within optimal ranges for oral bioavailability. These findings highlight the significant bioactive potential of BRP and its compounds, suggesting their potential as therapeutic agents in vitro and in-silico. Further studies are recommended to explore their mechanisms of action and therapeutic applications.

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巴西红蜂胶的生物活性代谢物：细胞毒性、抗疟疾和抗菌特性。

巴西红蜂胶（BRP）是一种天然产品，以其丰富的化学成分和治疗潜力而闻名。本研究研究了红蜂胶提取物及其分离化合物vestitol(1)、neovestitol(2)、medicarpin(3)、7-O-methylvestitol(4)和oblongifolin B(5)的植物化学性质，并对其细胞毒、抗疟原虫和抗菌性能进行了评价。该提取物对癌细胞具有选择性细胞毒性（IC50: 16-39 μg/mL）。化合物3对SK-OV-3具有良好的细胞毒性，IC50为6.65 μM。BRP抗菌效果中等；其中，3株对新型隐球菌（IC50: 19.29 μM）有效，5株对铜绿假单胞菌（IC50: 15.77 μM）有效。BRP对恶性疟原虫D6和W2株具有抗疟原虫活性（IC50分别为13.8 和5.7 μg/mL）；4和5的IC50浓度范围为：2.99 ~ 6.96 μM)。对恶性疟原虫乳酸脱氢酶（PfLDH）的分子对接表明，化合物4与PfLDH活性位点的关键残基如TYR85、THR97和ASP53有显著的相互作用，处于口服生物利用度的最佳范围内。这些发现突出了BRP及其化合物的显著生物活性潜力，表明它们在体外和计算机上作为治疗药物的潜力。建议进一步研究其作用机制和治疗应用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Fitoterapia 医学-药学

CiteScore

5.80

自引率

2.90%

发文量

198

审稿时长

1.5 months

期刊介绍： Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.