碳硅烷树枝状聚合物与马拉维若联合抗 HIV 的体外协同活性。
Synergistic activity of carbosilane dendrimers in combination with maraviroc against HIV in vitro.
机构信息
aLaboratorio InmunoBiología Molecular, Hospital General Universitario Gregorio Marañón bInstituto de Investigación Sanitaria del Gregorio Marañón cInorganic Chemistry Department, University of Alcalá, Alcalá de Henares dCentro Investigación Biomédica en Red, Bioingeniería, Biomateriales y Nanomedicina; CIBER-BNN, Madrid eLaboratory of Immunovirology, Clinic Unit of Infectious Diseases, Microbiology and Preventive Medicine, Institute of Biomedicine of Seville, IBiS, Virgen del Rocío University Hospital/CSIC/University of Seville, Spain.
出版信息
AIDS. 2013 Aug 24;27(13):2053-8. doi: 10.1097/QAD.0b013e328361fa4a.
OBJECTIVE
Dendrimers have been shown as effective and safe anti-HIV compounds with great potential as topical microbicides. Currently, the most advanced microbicides are based on antiretrovirals. However, nowadays none of them has shown any success in clinical trials.
DESIGN
Antiviral activity and combinatorial profile of different combinations between CCR5 co-receptor antagonist, maraviroc (MRV), and polyanionic carbosilane dendrimers against HIV-1 strains were evaluated.
METHODS
Cellular in-vitro models were used to evaluate the antiviral action of combinations of carbosilane dendrimers/MRV against CCR5 and dual tropic viral strains in TZM.bl cells and peripheral blood mononuclear cells. Combinatorial analysis was performed using Calcusyn software.
RESULTS
In the majority of combinations tested, dendrimers showed synergistic profile with MRV against CCR5 and dual tropic HIV-1.
CONCLUSION
The evaluated two-drug combinations increase their antiviral potency supporting further clinical investigations to develop combinatorial formulated topical microbicides to fight against the worldwide HIV spread.
目的
树状大分子已被证明是有效的和安全的抗 HIV 化合物，具有作为局部杀微生物剂的巨大潜力。目前，最先进的杀微生物剂基于抗逆转录病毒药物。然而，目前没有一种在临床试验中取得成功。
设计
评估 CCR5 共受体拮抗剂马拉维若（MRV）和聚阴离子碳硅烷树状大分子与 HIV-1 株之间不同组合的抗病毒活性和组合特征。
方法
使用细胞体外模型评估 TZM.bl 细胞和外周血单核细胞中碳硅烷树状大分子/MRV 组合对 CCR5 和双嗜性病毒株的抗病毒作用。使用 Calcusyn 软件进行组合分析。
结果
在所测试的大多数组合中，树状大分子与 MRV 对 CCR5 和双嗜性 HIV-1 表现出协同作用。
结论
评估的两种药物组合增加了它们的抗病毒效力，支持进一步的临床研究，以开发组合配方的局部杀微生物剂来对抗全球 HIV 的传播。
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