The protolytic properties of the sialorphin derivative Pal-Lys-Lys-Gln-His-Asn-Pro-Arg in an aqueous solution

IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Acta poloniae pharmaceutica Pub Date : 2023-10-11 DOI:10.32383/appdr/170103
Marek Pająk, Elżbieta Kamysz, Jakub Fichna, Magdalena Woźniczka
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Abstract

The present work describes the protolytic properties of the sialorphin derivative (Pal-Lys- Lys-Gln-His-Asn-Pro-Arg) in an aqueous solution, at constant temperature 25.0 ± 0.1 °C and ionic strength 0.1 M (NaClO4), over the entire pH range. The overall protonation constants of the studied ligand were calculated by the potentiometric method. The logarithm values of the stepwise dissociation constants of the sialorphin derivative were found to be: [LH] = 11.88 ± 0.09, [LH2]+ = 9.96 ± 0.03, [LH3]2+ = 8.71 ± 0.03, [LH4]3+ = 5.49 ± 0.03, [LH5]4+ = 2.82 ± 0.03. The percentage of each species formed in an aqueous solution was estimated from the species distribution curves as a function of pH (82% [LH] at pH 11.0, 68% [LH2]+ at pH 9.3, 95% [LH3]2+ at pH 7.1, 90% [LH4]3+ at pH 4.2, 85% [LH5]4+ at pH  2.0). The five protonation constants indicate that the studied ligand can be very active in forming complexes with different metal ions. In addition, the sialorphin derivative can also be tested as a bioactive material, which warrants its further in vitro and in vivo studies.
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唾液肽衍生物Pal-Lys-Lys-Gln-His-Asn-Pro-Arg在水溶液中的水解性质
本研究描述了唾液卟啉衍生物(Pal-Lys- Lys-Gln-His-Asn-Pro-Arg)在整个pH范围内恒温(25.0±0.1°C)和离子强度0.1 M (NaClO4)水溶液中的原解性质。用电位法计算了所研究配体的总质子化常数。结果表明:[LH] = 11.88±0.09,[LH2]+ = 9.96±0.03,[LH3]2+ = 8.71±0.03,[LH4]3+ = 5.49±0.03,[LH5]4+ = 2.82±0.03。根据pH值的分布曲线估算了水溶液中形成的每种物质的百分比(pH值为11.0时为82% [LH], pH值为9.3时为68% [LH2]+, pH值为7.1时为95% [LH3]2+, pH值为4.2时为90% [LH4]3+, pH值为2.0时为85% [LH5]4+)。五个质子化常数表明所研究的配体可以非常活跃地与不同的金属离子形成配合物。此外,唾液肽衍生物还可以作为生物活性物质进行测试,这为其进一步的体外和体内研究提供了依据。
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来源期刊
CiteScore
0.80
自引率
0.00%
发文量
74
审稿时长
6-12 weeks
期刊介绍: The international journal of the Polish Pharmaceutical Society is published in 6 issues a year. The journal offers Open Access publication of original research papers, short communications and reviews written in English, in all areas of pharmaceutical sciences. The following areas of pharmaceutical sciences are covered: Analysis, Biopharmacy, Drug Biochemistry, Drug Synthesis, Natural Drugs, Pharmaceutical Technology, Pharmacology and General. A bimonthly appearing in English since 1994, which continues “Acta Poloniae Pharmaceutica”, whose first issue appeared in December 1937. The war halted the activity of the journal’s creators. Issuance of “Acta Poloniae Pharmaceutica” was resumed in 1947. From 1947 the journal appeared irregularly, initially as a quarterly, then a bimonthly. In the years 1963 – 1973 alongside the Polish version appeared the English edition of the journal. Starting from 1974 only works in English are published in the journal. Since 1995 the journal has been appearing very regularly in two-month intervals (six books a year). The journal publishes original works from all fields of pharmacy, summaries of postdoctoral dissertations and laboratory notes.
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