Determination of Schaftoside and Isoschaftoside in Rat Plasma Utilizing UPLC‐MS/MS DOI
Jianbo Li,

Runrun Wang,

Mengmeng Shao

et al.

Biomedical Chromatography, Journal Year: 2025, Volume and Issue: 39(6)

Published: May 12, 2025

ABSTRACT To evaluate the pharmacokinetics, absolute bioavailability, and plasma concentrations of schaftoside isoschaftoside in rats, an UPLC‐MS/MS method was employed. For sample preparation, proteins were precipitated using chilled methanol. The separation achieved on a UPLC HSS T3 column with mobile phase consisting methanol water (with 0.1% formic acid water), at flow rate 0.4 mL/min. Detection performed electrospray ionization (ESI) positive ion mode, coupled multiple reaction monitoring (MRM) for quantitative analysis. Rats received oral doses (1 mg/kg) (5 mg/kg), pharmacokinetic profiles both compounds compared. calibration curve demonstrated excellent linearity within concentration range 1–2000 ng/mL, correlation coefficients ( r values) exceeding 0.99. Following intravenous administration, significant differences observed AUC (0–t) between isoschaftoside, whereas their half‐lives (t 1/2 ) remained comparable. bioavailability rat determined to be 0.95% 0.22%, respectively.

Language: Английский

Total Synthesis of Auriculatin and Millexatin F and Discovery of Their Antibacterial Mechanism DOI Creative Commons

Yufei Che,

Qiying Wang, Zhanjun Hou

et al.

ACS Omega, Journal Year: 2025, Volume and Issue: 10(16), P. 16265 - 16276

Published: April 15, 2025

The emergence of multidrug-resistant (MDR) bacteria necessitates the urgent development novel antibacterial agents. This study reported first total synthesis two isoflavones, auriculatin (1) and millexatin F (2), derived from tropical medicinal plant Millettia extensa. Through in vitro evaluations, both compounds 1 2 possessed significant activities (MICs = 0.5-4 μg/mL) rapid bactericidal properties against Gram-positive bacteria, along with high safety for mammalian cells. Mechanistic studies revealed that (2) interact bacterial cell membranes, inducing alterations morphology membrane permeability a rise leakage intracellular DNA proteins, thereby leading to death. In addition, our indicated could phosphatidylethanolamine (PE) cardiolipin (CL) cytoplasmic membranes Gram-negative bacteria. Furthermore, showed increased efficacy when combined permeabilizer (polymyxin B nonapeptide), indicating potential broader application. These findings underscore therapeutic promise as lead candidates fight infections.

Language: Английский

Citations

0
Determination of Schaftoside and Isoschaftoside in Rat Plasma Utilizing UPLC‐MS/MS DOI
Jianbo Li,

Runrun Wang,

Mengmeng Shao

et al.

Biomedical Chromatography, Journal Year: 2025, Volume and Issue: 39(6)

Published: May 12, 2025

ABSTRACT To evaluate the pharmacokinetics, absolute bioavailability, and plasma concentrations of schaftoside isoschaftoside in rats, an UPLC‐MS/MS method was employed. For sample preparation, proteins were precipitated using chilled methanol. The separation achieved on a UPLC HSS T3 column with mobile phase consisting methanol water (with 0.1% formic acid water), at flow rate 0.4 mL/min. Detection performed electrospray ionization (ESI) positive ion mode, coupled multiple reaction monitoring (MRM) for quantitative analysis. Rats received oral doses (1 mg/kg) (5 mg/kg), pharmacokinetic profiles both compounds compared. calibration curve demonstrated excellent linearity within concentration range 1–2000 ng/mL, correlation coefficients ( r values) exceeding 0.99. Following intravenous administration, significant differences observed AUC (0–t) between isoschaftoside, whereas their half‐lives (t 1/2 ) remained comparable. bioavailability rat determined to be 0.95% 0.22%, respectively.

Language: Английский

Citations

0