Silva Sandra Regina, Souza-Silva Gabriel, Moreira Carolina Paula de Souza, Vasconcelos Olívia Maria de Sousa Ribeiro, Silveira Micheline Rosa, Barbosa Francisco Antonio Rodrigues, Magalhães Sergia Maria Starling, Mol Marcos Paulo Gomes
Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 30510010, Brazil.
Fundação Ezequiel Dias, Departamento de Pesquisa e Desenvolvimento, Belo Horizonte 30510010, Brazil.
Toxics. 2024 Oct 10;12(10):729. doi: 10.3390/toxics12100729.
Tenofovir disoproxil fumarate (TDF) is an antiretroviral drug extensively used by people living with HIV. The TDF molecule is hydrolysed in vivo and liberates tenofovir, the active part of the molecule. Tenofovir is a very stable drug and the discharge of its residues into the environment can potentially lead to risk for aquatic species. This study evaluated the TDF biodegradation and removal by cultures of with the bacteria . Concentrations of TDF of 12.5, 25.0, and 50.0 mg/L were used in this study. The process occurred in two stages. In the first 72 h, TDF was de-esterified, forming the tenofovir monoester intermediate by abiotic and enzymatic processes associated in an extracellular medium. In a second step, the monoester was removed from the culture medium by intracellular processes. The tenofovir or other by-products of TDF were not observed in the test conditions. At the end of the experiment, 88.7 to 94.1% of TDF and its monoester derivative were removed from the culture medium over 16 days. This process showed higher efficiency of TDF removal at the concentration of 25 mg/L. Tenofovir isoproxil monoester has partial antiviral activity and has shown to be persistent, maintaining a residual concentration after 16 days in the culture medium, therefore indicating the need to continue research on methods for total removal of this product from the aquatic environment.
富马酸替诺福韦二吡呋酯(TDF)是一种被HIV感染者广泛使用的抗逆转录病毒药物。TDF分子在体内水解并释放出替诺福韦,即该分子的活性部分。替诺福韦是一种非常稳定的药物,其残留物排放到环境中可能会对水生物种造成潜在风险。本研究评估了用 细菌培养物对TDF的生物降解和去除情况。本研究使用了浓度为12.5、25.0和50.0 mg/L的TDF。该过程分两个阶段进行。在最初的72小时内,TDF发生去酯化反应,通过细胞外介质中相关的非生物和酶促过程形成替诺福韦单酯中间体。第二步,单酯通过细胞内过程从培养基中去除。在测试条件下未观察到替诺福韦或TDF的其他副产物。实验结束时,在16天内从培养基中去除了88.7%至94.1%的TDF及其单酯衍生物。该过程在25 mg/L浓度下显示出更高的TDF去除效率。替诺福韦异丙酯单酯具有部分抗病毒活性,并且已显示具有持久性,在培养基中16天后仍保持残留浓度,因此表明需要继续研究从水生环境中完全去除该产品的方法。