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New Silver(I) Coordination Compound Loaded into Polymeric Nanoparticles as a Strategy to Improve In Vitro Anti-Helicobacter pylori Activity.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-06-09 , DOI: 10.1021/acs.molpharmaceut.9b01264 Bruna Almeida Furquim de Camargo 1 , Débora Eduarda Soares Silva 2 , Anderson Noronha da Silva 1 , Débora Leite Campos 1 , Tamara Renata Machado Ribeiro 1 , Maria Júlia Mieli 3 , Melina Borges Teixeira Zanatta 4 , Patrícia Bento da Silva 1 , Fernando Rogerio Pavan 1 , Cristiano Gallina Moreira 1 , Flávia Aparecida Resende 3 , Amauri Antônio Menegário 4 , Marlus Chorilli 1 , Adelino Vieira de Godoy Netto 2 , Taís Maria Bauab 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-06-09 , DOI: 10.1021/acs.molpharmaceut.9b01264 Bruna Almeida Furquim de Camargo 1 , Débora Eduarda Soares Silva 2 , Anderson Noronha da Silva 1 , Débora Leite Campos 1 , Tamara Renata Machado Ribeiro 1 , Maria Júlia Mieli 3 , Melina Borges Teixeira Zanatta 4 , Patrícia Bento da Silva 1 , Fernando Rogerio Pavan 1 , Cristiano Gallina Moreira 1 , Flávia Aparecida Resende 3 , Amauri Antônio Menegário 4 , Marlus Chorilli 1 , Adelino Vieira de Godoy Netto 2 , Taís Maria Bauab 1
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Helicobacter pylori inhabits the gastric epithelium and can promote the development of gastric disorders, such as peptic ulcers, acute and chronic gastritis, mucosal lymphoid tissue (MALT), and gastric adenocarcinomas. To use nanotechnology as a tool to increase the antibacterial activity of silver I [Ag(I)] compounds, this study suggests a new strategy for H. pylori infections, which have hitherto been difficult to control. [Ag (PhTSC·HCl)2] (NO3)·H2O (compound 1) was synthesized, characterized, and loaded into polymeric nanoparticles (PN1). PN1 had been developed by nanoprecipitation with poly(ε-caprolactone) polymer and poloxamer 407 surfactant. System characterization assays showed that the PNs had adequate particle sizes and ζ-potentials. Transmission electron microscopy confirmed the formation of polymeric nanoparticles (PNs). Compound 1 had a minimum inhibitory concentration for H. pylori of 3.90 μg/mL, which was potentiated to 0.781 μg/mL after loading. The minimum bactericidal concentration of 7.81 μg/mL was potentiated 5-fold to 1.56 μg/mL in PN. Compound 1 loaded in PN1 displayed better activity for H. pylori biofilm formation and mature biofilm. PN1 reduced the toxicity of compound 1 to MRC-5 cells. Loading compound 1 into PN1 inhibited the mutagenicity of the free compound. In vivo, the system allowed survival of Galleria mellonella larvae at a concentration of 200 μg/mL. This is the first demonstration of the antibacterial activity of a silver complex enclosed in polymeric nanoparticles against H. pylori.
中文翻译：
新的银（I）配位化合物加载到聚合物纳米粒子，以提高体外抗幽门螺杆菌活性的策略。
幽门螺杆菌栖息在胃上皮中，可促进胃部疾病的发展，例如消化性溃疡，急慢性胃炎，粘膜淋巴组织（MALT）和胃腺癌。为了将纳米技术用作提高银I [Ag（I）]化合物抗菌活性的工具，这项研究提出了一种迄今为止难以控制的幽门螺杆菌感染的新策略。[Ag（PhTSC·HCl）2 ]（NO 3）·H 2合成，表征O（化合物1）并将其装载到聚合物纳米颗粒（PN1）中。PN1是通过聚（ε-己内酯）聚合物和泊洛沙姆407表面活性剂的纳米沉淀而开发的。系统表征分析表明，PNs具有足够的粒径和ζ电位。透射电子显微镜证实了聚合物纳米颗粒（PNs）的形成。化合物1对幽门螺杆菌的最小抑菌浓度为3.90μg/ mL，在加载后增强至0.781μg/ mL。PN中的最低杀菌浓度为7.81μg/ mL，可增强5倍至1.56μg/ mL。PN1中的化合物1对幽门螺杆菌显示出更好的活性生物膜形成和成熟的生物膜。PN1降低了化合物1对MRC-5细胞的毒性。将化合物1装入PN1会抑制游离化合物的诱变性。在体内，该系统可以使浓度为200μg/ mL的马齿Gall幼虫存活。这是封闭在聚合物纳米颗粒中的银配合物对幽门螺杆菌的抗菌活性的首次证明。
更新日期：2020-07-06
中文翻译：
新的银（I）配位化合物加载到聚合物纳米粒子，以提高体外抗幽门螺杆菌活性的策略。
幽门螺杆菌栖息在胃上皮中，可促进胃部疾病的发展，例如消化性溃疡，急慢性胃炎，粘膜淋巴组织（MALT）和胃腺癌。为了将纳米技术用作提高银I [Ag（I）]化合物抗菌活性的工具，这项研究提出了一种迄今为止难以控制的幽门螺杆菌感染的新策略。[Ag（PhTSC·HCl）2 ]（NO 3）·H 2合成，表征O（化合物1）并将其装载到聚合物纳米颗粒（PN1）中。PN1是通过聚（ε-己内酯）聚合物和泊洛沙姆407表面活性剂的纳米沉淀而开发的。系统表征分析表明，PNs具有足够的粒径和ζ电位。透射电子显微镜证实了聚合物纳米颗粒（PNs）的形成。化合物1对幽门螺杆菌的最小抑菌浓度为3.90μg/ mL，在加载后增强至0.781μg/ mL。PN中的最低杀菌浓度为7.81μg/ mL，可增强5倍至1.56μg/ mL。PN1中的化合物1对幽门螺杆菌显示出更好的活性生物膜形成和成熟的生物膜。PN1降低了化合物1对MRC-5细胞的毒性。将化合物1装入PN1会抑制游离化合物的诱变性。在体内，该系统可以使浓度为200μg/ mL的马齿Gall幼虫存活。这是封闭在聚合物纳米颗粒中的银配合物对幽门螺杆菌的抗菌活性的首次证明。
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