4 research outputs found
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<sup>− 1</sup>. 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<sup>− 1</sup>) 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 <sup>111</sup>In-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 <sup>111</sup>In-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 <sup>111</sup>In 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 polyÂ(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 IC<sub>50</sub> compared
to the nontargeted formulations. Also, the enhanced LHRHr-mediated
uptake of the targeted MNCs resulted in enhancement in the T<sub>2</sub>-weighted negative contrast in cellular phantom gels. Taken together,
the LHRH-conjugated MNCs show good potential as ovarian cancer theranostics