The antibacterial activity of phytochemically characterised fractions from Folium Syringae

<div><p>To identify the most active antimicrobial fraction of Folium Syringae, four common pathogens were used in an <i>in vitro</i> screening. The results indicated that the combination of the 30% and 60% ethanol fraction (FSC) obtained from the water extraction was the most active fraction with a minimal inhibitory concentration of 0.65 mg mL^− 1. FSC was also found to be able to protect mice from a lethal infection of <i>Staphylococcus aureus</i> at clinical dosage (0.2 g kg^− 1) with a survival rate of 83.3%. The antibacterial activity of FSC was then tested using the serum pharmacology method which revealed that FSC exhibits a more long-lasting activity than the positive control (levofloxacin hydrochloride). The main components were confirmed to be iridoid glycosides and flavones by HPLC–MS analysis.</p></div

Development of Hypoxia Enhanced ¹¹¹In-Labeled Bombesin Conjugates: Design, Synthesis, and In Vitro Evaluation in PC-3 Human Prostate Cancer

The gastrin-releasing peptide receptor (BB2r) has shown great promise for tumor targeting due to the increase of the receptor expression in a variety of human cancers including prostate, breast, small-cell lung, and pancreatic cancer. From clinical investigations, prostate cancer has been shown to be among the most hypoxic of the cancers investigated. Many solid tumors contain regions of hypoxia due to poor organization and efficiency of the vasculature. However, hypoxia is typically not present in normal tissue. Nitroimidazoles, a thoroughly investigated class of hypoxia selective drugs, have been shown to be highly retained in hypoxic tissues. The purpose of this study is to determine if the incorporation of hypoxia trapping moieties into the structural paradigm of BB2r-targeted peptides will increase the retention time of the agents in prostate cancer tumors. The present work involves the design, syntheses, purification, and in vitro investigation of hypoxia enhanced ¹¹¹In-BB2r-targeted radioconjugates. A total of four BB2r-targeted conjugates (<b>1</b>–<b>4</b>) were synthesized and coupled with increasing numbers of 2-nitroimidazoles, a hypoxia trapping moiety. Conjugates were radiolabeled with ¹¹¹In and purified by HPLC prior to in vitro studies. Receptor saturation assays under both normoxic and hypoxic conditions showed that the BB2r receptor expression on the PC-3 human prostate cancer cell line was not significantly affected by oxygen levels. Competitive binding assays revealed that incorporation of 2-nitroimidazoles had a detrimental effect to BB2r binding when adequate spacer groups, between the hypoxia trapping agent and the pharmacophore, were not employed. All of the 2-nitroimidazole containing BB2r-targeted agents exhibited significantly higher longitudinal retention in PC-3 cells under hypoxic conditions compared to the analogous normoxic studies. Protein association analysis revealed a 3-fold increase in binding of a 2-nitroimidazole containing BB2r-targeted agent under hypoxic relative to normoxic conditions. The positive nature of these results indicate that further exploration into the potential of hypoxia selective trapping agents for BB2r-targeted agents, as well as other targeted compounds, is warranted

Additional file 1 of Green tea consumption and incidence of cardiovascular disease in type 2 diabetic patients with overweight/obesity: a community-based cohort study

Supplementary Material

Luteinizing Hormone Releasing Hormone-Targeted Cisplatin-Loaded Magnetite Nanoclusters for Simultaneous MR Imaging and Chemotherapy of Ovarian Cancer

Given the superior soft tissue contrasts obtained by MRI and the long residence times of magnetic nanoparticles (MNPs) in soft tissues, MNP-based theranostic systems are being developed for simultaneous imaging and treatment. However, development of such theranostic nanoformulations presents significant challenges of balancing the therapeutic and diagnostic functionalities in order to achieve optimum effect from both. Here we developed a simple theranostic nanoformulation based on magnetic nanoclusters (MNCs) stabilized by a bisphosphonate-modified poly­(glutamic acid)-<i>b</i>-(ethylene glycol) block copolymer and complexed with cisplatin. The MNCs were decorated with luteinizing hormone releasing hormone (LHRH) to target LHRH receptors (LHRHr) overexpressed in ovarian cancer cells. The targeted MNCs significantly improved the uptake of the drug in cancer cells and decreased its IC₅₀ compared to the nontargeted formulations. Also, the enhanced LHRHr-mediated uptake of the targeted MNCs resulted in enhancement in the T₂-weighted negative contrast in cellular phantom gels. Taken together, the LHRH-conjugated MNCs show good potential as ovarian cancer theranostics