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1.
Bioorg Med Chem Lett ; 25(16): 3168-71, 2015 Aug 15.
Article in English | MEDLINE | ID: mdl-26112446

ABSTRACT

Betulinic acid (1) has been modified to ionic derivatives (2-5) to improve its water solubility and biological activities. The binding properties of these derivatives with respect to human serum albumin (HSA) was examined and found to be similar to current anti-HIV drugs. These compounds did not inhibit HIV reverse transcriptase, however, 1, 2 and 5 inhibited herpes simplex type 2 (HSV-2) replication at concentrations similar to those reported for acyclovir (IC50 ∼ 0.1-10 µM) and with minimal cellular cytotoxicity. IC50 values for antiviral activity against HSV-2 186 were 1.6, 0.6, 0.9, 7.2, and 0.9 µM for compounds 1-5, respectively.


Subject(s)
Herpesvirus 2, Human/physiology , Triterpenes/chemistry , Acyclovir/pharmacology , Animals , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Chlorocebus aethiops , HIV Reverse Transcriptase/antagonists & inhibitors , HIV Reverse Transcriptase/metabolism , HIV-1/enzymology , Humans , Pentacyclic Triterpenes , Triterpenes/pharmacology , Vero Cells , Virus Replication/drug effects , Betulinic Acid
2.
Curr Opin Chem Biol ; 20: 69-77, 2014 Jun.
Article in English | MEDLINE | ID: mdl-24875635

ABSTRACT

Nitrogen-Vacancy (NV) color center in diamond is a flourishing research area that, in recent years, has displayed remarkable progress. The system offers great potential for realizing futuristic applications in nanoscience, benefiting a range of fields from bioimaging to quantum-sensing. The ability to image single NV color centers in a nanodiamond and manipulate NV electron spin optically under ambient condition is the main driving force behind developments in nanoscale sensing and novel imaging techniques. In this article we discuss current status on the applications of fluorescent nanodiamonds (FND) for optical super resolution nanoscopy, magneto-optical (spin-assisted) sub-wavelength localization and imaging. We present emerging applications such as single molecule spin imaging, nanoscale imaging of biomagnetic fields, sensing molecular fluctuations and temperatures in live cellular environments. We summarize other current advances and future prospects of NV diamond for imaging and sensing pertaining to bio-medical applications.


Subject(s)
Nanoparticles/chemistry , Nitrogen/chemistry , Animals , Biosensing Techniques , Color , Humans , Molecular Imaging
3.
Acta Crystallogr Sect E Struct Rep Online ; 67(Pt 10): m1409-10, 2011 Oct 01.
Article in English | MEDLINE | ID: mdl-22065366

ABSTRACT

The title compound, [Sn(C(6)H(5))(2)(C(12)H(11)N(4)S(2))Cl]·CH(4)O, is formed during the reaction between 2-acetyl-thia-zole 4-phenyl-thio-semicarbazone (Hacthptsc) and diphenyl-tin(IV) dichloride in methanol. In the crystal structure, the Sn atom exhibits an octa-hedral geometry with the [N(2)S] anionic tridentate thio-semicarbazone ligand having chloride trans to the central N and the two phenyl groups trans to each other. The Sn-Cl distance is 2.5929 (6), Sn-S is 2.4896 (6) and Sn-N to the central N is 2.3220 (16) Å. The MeOH mol-ecules link the Sn complexes into one-dimensional chains via N-H⋯O and O-H⋯Cl hydrogen bonds.

4.
Acta Crystallogr Sect E Struct Rep Online ; 67(Pt 6): m816-7, 2011 Jun 01.
Article in English | MEDLINE | ID: mdl-21754688

ABSTRACT

In the title compound, [Hg(C(12)H(11)N(4)S(2))I(C(12)H(12)N(4)S(2))], the Hg atom is in a distorted square-pyramidal coordination, defined by the iodide ligand, by the S atom of the neutral ligand in the apical position, and by the N atom of the thia-zole ring, the thio-ureido N and the S atom of the deprotonated ligand. The deprotonated ligand intra-molecularly hydrogen bonds to the thia-zole ring N atom, while the deprotonated ligand forms an inter-molecular hydrogen bond to the thiol-ate S atom. The deprotonation of the tridentate ligand and its coordination to Hg via the S atom strikingly affects the C-S bond lengths. In the free ligand, the C-S bond distance is 1.685 (7) Å, whereas it is 1.749 (7) Šin the deprotonated ligand. Similarly, the Hg-S bond distance is slightly longer to the neutral ligand [2.6682 (18) Å] than to the deprotonated ligand [2.5202 (19) Å]. The Hg-I distance is 2.7505 (8) Å.

5.
ACS Appl Mater Interfaces ; 3(3): 668-73, 2011 Mar.
Article in English | MEDLINE | ID: mdl-21306127

ABSTRACT

Pb (II) is a common water pollutant with high toxicity. According to the CDC, about 310,000 U.S. children of ages 1-5 have high levels of lead in their blood that it is due to the exposure to lead from plastic toys and other products. As a result, the development of ultrasensitive assays for the real-time detection of Pb(II) from plastic toys and paints is very important for water controlling, clinical toxicology and industrial processes. Driven by the need to detect trace amounts of Pb(II) from water samples, we report a label-free, highly selective and ultra sensitive glutathione modified gold nanoparticle based dynamic light scattering (DLS) probe for Pb(II) recognition in 100 ppt level from aqueous solution with excellent discrimination against other heavy metals. The sensitivity of our assay to detect Pb(II) level in water is almost 2 orders of magnitude higher than the EPA standard limit. We have also demonstrated that our DLS assay is capable of measuring the amount of Pb(II) in paint, plastic toys, and water from MS river. A possible mechanism and operating principles of our DLS assay have been discussed. Ultimately, this nanotechnology driven assay could have enormous potential applications in rapid, on-site monitoring of Pb(II) from day-to-day sample.


Subject(s)
Colorimetry/instrumentation , Gold/chemistry , Lead/analysis , Nanoparticles/chemistry , Paint/analysis , Plastics/chemistry , Water Pollutants, Chemical/chemistry , Equipment Design , Equipment Failure Analysis , Light , Nanoparticles/ultrastructure , Refractometry/instrumentation , Scattering, Radiation
6.
ACS Nano ; 4(3): 1739-49, 2010 Mar 23.
Article in English | MEDLINE | ID: mdl-20155973

ABSTRACT

Breast cancer is the most common cancer among women, and it is the second leading cause of cancer deaths in women today. The key to the effective and ultimately successful treatment of diseases such as cancer is early and accurate diagnosis. Driven by the need, in this article, we report for the first time a simple colorimetric and highly sensitive two-photon scattering assay for highly selective and sensitive detection of breast cancer SK-BR-3 cell lines at a 100 cells/mL level using a multifunctional (monoclonal anti-HER2/c-erb-2 antibody and S6 RNA aptamer-conjugated) oval-shaped gold-nanoparticle-based nanoconjugate. When multifunctional oval-shaped gold nanoparticles are mixed with the breast cancer SK-BR-3 cell line, a distinct color change occurs and two-photon scattering intensity increases by about 13 times. Experimental data with the HaCaT noncancerous cell line, as well as with MDA-MB-231 breast cancer cell line, clearly demonstrated that our assay was highly sensitive to SK-BR-3 and it was able to distinguish from other breast cancer cell lines that express low levels of HER2. The mechanism of selectivity and the assay's response change have been discussed. Our experimental results reported here open up a new possibility of rapid, easy, and reliable diagnosis of cancer cell lines by monitoring the colorimetric change and measuring TPS intensity from multifunctional gold nanosystems.


Subject(s)
Breast Neoplasms/pathology , Colorimetry/methods , Gold/chemistry , Metal Nanoparticles/chemistry , Photons , Scattering, Radiation , Absorption , Antibodies, Monoclonal/chemistry , Antibodies, Monoclonal/immunology , Antibodies, Monoclonal/metabolism , Aptamers, Nucleotide/metabolism , Cell Line, Tumor , Humans , Molecular Probes/chemistry , Molecular Probes/metabolism , Receptor, ErbB-2/immunology , Spectrum Analysis, Raman
7.
J Biol Chem ; 284(43): 29283-9, 2009 Oct 23.
Article in English | MEDLINE | ID: mdl-19700405

ABSTRACT

The T4 bacteriophage helicase loader (gp59) is one of the main eight proteins that play an active role in the replisome. gp59 is a small protein (26 kDa) that exists as a monomer in solution and in the crystal. It binds preferentially to forked DNA and interacts directly with the T4 helicase (gp41), single-stranded DNA-binding protein (gp32), and polymerase (gp43). However, the stoichiometry and structure of the functional form are not very well understood. There is experimental evidence for a hexameric structure for the helicase (gp41) and the primase (gp61), inferring that the gp59 structure might also be hexameric. Various experimental approaches, including gel shift, fluorescence anisotropy, light scattering, and fluorescence correlation spectroscopy, have not provided a clearer understanding of the stoichiometry. In this study, we employed single-molecule photobleaching (smPB) experiments to elucidate the stoichiometry of gp59 on a forked DNA and to investigate its interaction with other proteins forming the primosome complex. smPB studies were performed with Alexa 555-labeled gp59 proteins and a forked DNA substrate. Co-localization experiments were performed using Cy5-labeled forked DNA and Alexa 555-labeled gp59 in the presence and absence of gp32 and gp41 proteins. A systematic study of smPB experiments and subsequent data analysis using a simple model indicated that gp59 on the forked DNA forms a hexamer. In addition, the presence of gp32 and gp41 proteins increases the stability of the gp59 complex, emphasizing their functional role in T4 DNA replication machinery.


Subject(s)
Bacteriophage T4/metabolism , DNA Replication/physiology , DNA, Viral/metabolism , DNA-Binding Proteins/metabolism , Multiprotein Complexes/metabolism , Viral Proteins/metabolism , Bacteriophage T4/chemistry , DNA Helicases/chemistry , DNA Helicases/metabolism , DNA Primase/chemistry , DNA Primase/metabolism , DNA, Viral/chemistry , DNA-Binding Proteins/chemistry , DNA-Directed DNA Polymerase/chemistry , DNA-Directed DNA Polymerase/metabolism , Multiprotein Complexes/chemistry , Photobleaching , Protein Binding/physiology , Viral Proteins/chemistry
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