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Antifungal activity of farnesol incorporated in liposomes and associated with fluconazole
Chemistry and Physics of Lipids ( IF 3.4 ) Pub Date : 2020-10-12 , DOI: 10.1016/j.chemphyslip.2020.104987
Camila Fonseca Bezerra 1 , José Geraldo de Alencar Júnior 2 , Rosilaine de Lima Honorato 3 , Antonia Thassya Lucas Dos Santos 3 , Josefa Carolaine Pereira da Silva 3 , Taís Gusmão da Silva 3 , Antonio Linkoln Alves Borges Leal 4 , Janaína Esmeraldo Rocha 4 , Thiago Sampaio de Freitas 4 , Thiago Adler Tavares Vieira 5 , Maria Clara Fonseca Bezerra 6 , Débora Lima Sales 4 , Marta Regina Kerntopf 4 , Gyllyandeson de Araujo Delmondes 4 , José Maria Barbosa Filho 7 , Laisla Rangel Peixoto 7 , Allyson Pontes Pinheiro 3 , Jaime Ribeiro-Filho 8 , Henrique Douglas Melo Coutinho 4 , Maria Flaviana Bezerra Morais-Braga 3 , Teresinha Gonçalves da Silva 9
Affiliation  

Candida infections represent a threat to human health. Candida albicans is the main causative agent of invasive candidiasis, especially in immunosuppressed patients. The emergence of resistant strains has required the development of new therapeutic strategies. In this context, the use of liposomes as drug carrier systems is a promising alternative in drug development. Thus, considering the evidence demonstrating that sesquiterpene farnesol is a bioactive compound with antifungal properties, this study evaluated the activity farnesol-containing liposomes against different Candida strains. The IC50 of farnesol and its liposomal formulation was assessed in vitro using cultures of Candida albicans, Candida tropicalis, and Candida krusei. The Minimum Fungicidal Concentration (MFC) was established by subculture in solid medium. The occurrence of fungal dimorphism was analyzed using optical microscopy. The effects on antifungal resistance to fluconazole were assessed by evaluating the impact of combined therapy on the growth of Candida strains. The characterization of liposomes was carried out considering their vesicular size, polydispersion index, and zeta medium potential, in addition to electron microscopy analysis. Farnesol exerted an antifungal activity that might be associated with the inhibition of fungal dimorphism, especially in Candida albicans. The incorporation of farnesol into liposomes significantly increased its antifungal activity against C. albicans, C. tropicalis, and C. krusei. In addition, liposomal farnesol potentiated the action of fluconazole against C. albicans and C. tropicalis. On the other hand, the association of unconjugated farnesol with fluconazole resulted in antagonistic effects. In conclusion, farnesol-containing liposomes have the potential to be used in antifungal drug development. However, further research is required to investigate how the antifungal properties of farnesol are affected by the interaction with liposomes, contributing to the modulation of antifungal resistance to conventional drugs.



中文翻译:

掺入脂质体并与氟康唑相关的法尼醇的抗真菌活性

念珠菌感染对人类健康构成威胁。白色念珠菌是侵袭性念珠菌病的主要病原体,尤其是在免疫抑制患者中。耐药菌株的出现需要开发新的治疗策略。在这种情况下,使用脂质体作为药物载体系统是药物开发中一个有前途的替代方案。因此,考虑到证据表明倍半萜烯法尼醇是一种具有抗真菌特性的生物活性化合物,本研究评估了含法尼醇脂质体对不同念珠菌菌株的活性。法呢醇及其脂质体制剂的 IC 50在体外使用培养物进行评估白色念珠菌、热带念珠菌克柔念珠菌。最低杀真菌浓度 (MFC) 是通过在固体培养基中继代培养确定的。使用光学显微镜分析真菌二态性的发生。通过评估联合治疗对念珠菌菌株生长的影响来评估对氟康唑的抗真菌耐药性的影响。除了电子显微镜分析外,脂质体的表征还考虑了它们的囊泡大小、多分散指数和 zeta 介质电位。Farnesol 发挥抗真菌活性,这可能与抑制真菌二态性有关,尤其是在白色念珠菌中. 法尼醇掺入脂质体显着增加了其对白色念珠菌、热带念珠菌克柔念珠菌的抗真菌活性。此外,脂质体法尼醇增强了氟康唑对白色念珠菌热带念珠菌的作用。另一方面,未结合的法呢醇与氟康唑的结合导致拮抗作用。总之,含法尼醇的脂质体具有用于抗真菌药物开发的潜力。然而,需要进一步研究来研究法尼醇的抗真菌特性如何受到与脂质体相互作用的影响,从而有助于调节对常规药物的抗真菌耐药性。

更新日期:2020-10-30
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