PTP1B Inhibitory and Anti-inflammatory Properties of Constituents from Eclipta prostrata L.

The white-flowered leaves of Eclipta prostrata L. together with leaves of Scoparia dulcis and Cynodon dactylon are mixedly boiled in water and given to diabetic patients resulting in the significant improvement in the management of diabetes. However, the active constituents from this plant for antidiabetic and anti-obesity properties are remaining unclear. Thus, this study was to discover anti-diabetes and anti-obesity activities through protein tyrosine phosphatases (PTP)1B inhibitory effects. We found that the fatty acids (23, 24) showed potent PTP1B inhibition with IC50 values of 2.14 and 3.21 µM, respectively. Triterpenoid-glycosides (12-15) also exhibited strong to moderate PTP1B inhibitory effects, with IC50 values ranging from 10.88 to 53.35 µM. Additionally, active compounds were investigated for their PTP1B inhibitory mechanism and docking analysis. On the other hand, the anti-inflammatory activity from our study revealed that compounds (1-4, 7, 8, 10) displayed the significant inhibition nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Especially, compound 9 showed the potent inhibitory effects in LPS-induced NO production on RAW264.7 cell. Therefore, further Western blot analysis was performed to identify the inhibitory expression including heme oxygenase-1 (HO-1) and inhibitor of kappaB (IκB) phosphorylation.

Sappanone A Prevents Left Ventricular Dysfunction in a Rat Myocardial Ischemia Reperfusion Injury Model.

The incidence of myocardial infarction, among the causes of cardiovascular morbidity and mortality, is increasing globally. In this study, left ventricular (LV) dysfunction, including LV systolic and diastolic function, was investigated in a rat myocardial ischemia/reperfusion injury model with echocardiography. The homoisoflavanone sappanone A is known for its anti-inflammatory effects. Using echocardiography, we found that sappanone A administration significantly improved LV systolic and diastolic function in a rat myocardial ischemia/reperfusion injury model, especially in the early phase development of myocardial infarction. Based on myocardial infarct size, serum cardiac marker assay, and histopathological evaluation, sappanone A showed higher efficacy at the doses used in our experiments than curcumin and was evaluated for its potential to improve LV function.

Quantitative analysis of betaine in Lycii Fructus by HILIC-ELSD.

A rapid and simple high-performance liquid chromatography (HPLC) method with evaporative light scattering detection (ELSD) was developed for the determination of betaine from Lycii Fructus. Betaine was separated with an Atlantis hydrophilic interaction liquid chromatography silica column (4.6 × 150 mm, 5 µm, 100 Å) by isocratic elution using 30 mM ammonium acetate buffer and acetonitrile (20:80, v/v %) as the mobile phase. The flow rate was 1.0 mL/min, and the temperature for the spray chamber and drift tube was set at 30 and 50 °C, respectively. The method was fully validated with respect to linearity, precision, accuracy, stability and robustness. The HPLC/ELSD method was applied successfully to the quantification of betaine in the extract of Lycii Fructus. The HPLC analytical method for pattern recognition analysis was validated by repeated analysis of twenty-six L. barbarum L. from China (BC01-BC26), 3 L. barbarum L. (BJ27-BJ29) from Japan, 12 L. chinense Miller from China (CC30-CC41) and 51 L. chinense Miller samples (CK42-CK92) from Korea. The results indicate that the established HPLC/ELSD method is suitable for quality evaluation of Lycii Fructus.

Pharmacokinetics and tissue distribution of psammaplin A, a novel anticancer agent, in mice.

This study reports the pharmacokinetics and tissue distribution of a novel histone deacetylase and DNA methyltransferase inhibitor, psammaplin A (PsA), in mice. PsA concentrations were determined by a validated LC-MS/MS assay method (LLOQ 2 ng/mL). Following intravenous injection at a dose of 10 mg/kg in mice, PsA was rapidly eliminated, with the average half-life (t(1/2, λn)) of 9.9 ± 1.4 min and the systemic clearance (CL(s)) of 925.1 ± 570.1 mL/min. The in vitro stability of PsA was determined in different tissue homogenates. The average degradation t(1/2) of PsA in blood, liver, kidney and lung was found relatively short (≤ 12.8 min). Concerning the in vivo tissue distribution characteristics, PsA was found to be highly distributed to lung tissues, with the lung-to-serum partition coefficients (K(p)) ranging from 49.9 to 60.2. In contrast, PsA concentrations in other tissues were either comparable with or less than serum concentrations. The high and specific lung targeting characteristics indicates that PsA has the potential to be developed as a lung cancer treatment agent.

A new cytotoxic coumarin, 7-[(E)-3',7'-dimethyl-6'-oxo-2',7'-octadienyl] oxy coumarin, from the leaves of Zanthoxylum schinifolium.

A new coumarin, 7-[(E)-3',7'-dimethyl-6'-oxo-2',7'-octadienyl]oxy coumarin (1), together with three known compounds, schinilenol (2), schinindiol (3) and 7-[(E)-7'-hydroxy-3',7'-dimethylocta-2',5'-dienyloxy]-coumarin (4) were isolated from the methylene chloride fraction of Z. schinifolium by normal and reverse phase column chromatographies. Their structures were determined on the basis of physical and spectroscopic evidences. Compound 1 (IC(50) 8.10 µM) showed potent cytotoxicity compared to auraptene (IC(50) 55.36 µM) against Jurkat T cells. The other isolated compounds 2 and 4 exhibited weak cytotoxicities.