| Description | Paromomycin binds specifically to the RNA oligonucleotide at the A site of bacterial 30S ribosomes, thereby causing misreading and premature termination of translation of mRNA and inhibition of protein synthesis followed by cell death. Paromomycin Sulfate (Aminosidine sulfate) is the sulfate salt form of paromomycin, a structural derivative of neomycin, an aminoglycoside antibiotic with amebicidal and bactericidal effects against predominantly aerobic gram-negative bacteria. |
| In vitro | 在CL临床病例和实验模型中,用paromomycin药膏涂抹L. major造成的损伤比L. panamensis和L. amazonensis造成的恢复的更快、更彻底. |
| In vivo | 作为一种氨基糖苷类抗生素,Paromomycin对许多革兰氏阳性菌、革兰氏阴性菌、一些原生动物和绦虫均显示出较强的抗菌活性。小鼠巨噬细胞模型中无鞭毛体敏感度的体外分析表明,L. tropica和菌系L. major(ED50s：1~5 μM) 比L. mexicana (ED50：39 μM) 和L. braziliensis (ED50：150 μM。 |
| Synonyms | Aminosidine sulfate, Paromomycin sulfate salt, 硫酸巴龙霉素, 巴龙霉素硫酸盐 |
| molecular weight | 713.71 |
| Molecular formula | C23H47N5O18S |
| CAS | 1263-89-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 10 mM DMSO: Insoluble |
| References | 1. Davidson RN, et al. ParomomycinTrans R Soc Trop Med Hyg, 2009, 103(7), 653-660. 2. Simon L. Croft, et al. Clin Microbiol Rev, 2006, 19(1), 111-126 3. Li Zhu, Ruonan Liu, Tangrong Liu, Xuan Zou, Zhe Xu, Huashi Guan. A novel strategy to screen inhibitors of multiple aminoglycoside-modifying enzymes with ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry[J]. Journal of Pharmaceutical and Biomedical Analysis. 2019 Feb 5;164:520-527. |
| Kinase | Concentration–response and kinetic studies: The microsomal protein (30 μg), [1β-3H]androstenedione (6.6 × 105 dpm) and NADPH (270 μM) are used for the concentration–response experiment with an incubation time of 20 minutes. The Aminoglutethimide is initially tested at 10 μM and 100 μM concentrations, followed by a full concentration–response study with at least 8 concentrations ranging from 0.01 μM to 160 μM. For the initial velocity study the concentration of [1β-3H]androstenedione is varied from 7.5 to 100 nM and the incubation time is set to 5 minutes. The tritiated water formed during the conversion of the tritiated substrate, [1β-3H]androstenedione, to estrone is quantified by liquid scintillation counting. Each assay is performed three times in duplicate and the results are treated by nonlinear regression analysis allowing the determination of the half-maximal inhibitory concentration (IC50). |