scholarly journals Synthesis of fluoro-functionalized diaryl-λ3-iodonium salts and their cytotoxicity against human lymphoma U937 cells

2018 ◽  
Vol 14 ◽  
pp. 364-372 ◽  
Author(s):  
Prajwalita Das ◽  
Etsuko Tokunaga ◽  
Hidehiko Akiyama ◽  
Hiroki Doi ◽  
Norimichi Saito ◽  
...  
Keyword(s):  
Biological Properties ◽  
U937 Cells ◽  
Iodonium Salts ◽  
Diaryliodonium Salts ◽  
Sterically Demanding ◽  
Diaryliodonium Salt ◽  
Human Lymphoma ◽  
Normal Human ◽  
Human B Cell

Conscious of the potential bioactivity of fluorine, an investigation was conducted using various fluorine-containing diaryliodonium salts in order to study and compare their biological activity against human lymphoma U937 cells. Most of the compounds tested are well-known reagents for fluoro-functionalized arylation reactions in synthetic organic chemistry, but their biological properties are not fully understood. Herein, after initially investigating 18 fluoro-functionalized reagents, we discovered that the ortho-fluoro-functionalized diaryliodonium salt reagents showed remarkable cytotoxicity in vitro. These results led us to synthesize more compounds, previously unknown sterically demanding diaryliodonium salts having a pentafluorosulfanyl (SF5) functional group at the ortho-position, that is, unsymmetrical ortho-SF5 phenylaryl-λ3-iodonium salts. Newly synthesized mesityl(2-(pentafluoro-λ6-sulfanyl)phenyl)iodonium exhibited the greatest potency in vitro against U937 cells. Evaluation of the cytotoxicity of selected phenylaryl-λ3-iodonium salts against AGLCL (a normal human B cell line) was also examined.

scholarly journals Compliance and capacity of the normal human rectum: Physical considerations and measurement Pitfalls

2007 ◽  
Vol 54 (2) ◽  
pp. 49-57 ◽  
Author(s):  
A.P. Zbar
Keyword(s):  
Rectal Wall ◽  
Biological Properties ◽  
Impedance Planimetry ◽  
Organ Deformation ◽  
Wall Stiffness ◽  
Hollow Organ ◽  
Normal Human ◽  
Human Rectum ◽  
Volume Characteristics

The assessment of parameters which adequately represent rectal and neorectal compliance is complex. Biological properties of the rectum during distension and relaxation show significant departures from in vitro physical compliance measurements; as much dependent upon the viscoelastic characteristics of hollow organ deformation as upon the technique of compliance calculation. This review discusses the pressure/volume characteristics of importance in the rectum during distension from a bioengineering perspective and outlines the disparities of such measurements in living biological systems. Techniques and pitfalls of newer methods to assess rectal wall stiffness (impedance planimetry and barostat measurement) are discussed. .

Properties of Bifidobacteria and Their Use for Scientific and Practical Purposes

2021 ◽  
Vol 37 (3) ◽  
pp. 3-10
Author(s):  
L.I. Nikolaeva
Keyword(s):  
Bacterial Infections ◽  
Biological Properties ◽  
Biologically Active ◽  
Recombinant Vaccines ◽  
Scientific Publications ◽  
Wide Range ◽  
Normal Human ◽  
Made In

Bifidobacteria occupy a special place among various representatives of normal human microbiota. A wide range of probiotic preparations has been obtained based on cultivated strains of various bifidobacteria of the intestinal microbiota. A number of scientific publications noted the immunomodulatory, anticarcinogenic, and antiviral properties of bifidobacteria in vitro and in vivo. Recently, progress has been made in the research and application of this group of microorganisms in genetic engineering. It was established that vaccines against viral and bacterial infections and antitumor substances can be developed on the basis of various strains of bifidobacteria. Bifidobacteria can also be used as adjuvants for other vaccines, as well as delivery systems for biologically active substances to tumors. The prospects for the use of bifidobacteria for the development of recombinant vaccines are discussed. bifidobacteria, medical and biological properties, recombinant vaccines, drug delivery, adjuvants, plasmids This work was funded by the Epidemiology and Microbiology National Research Center. The authors are grateful to V. V. Kuprianov for valuable comments on the text of the review.

Effect of pure bovine brain-derived gangliosides on normal human B cell proliferation in vitro

1994 ◽  
Vol 49 (1-2) ◽  
pp. 189-195 ◽  
Author(s):  
Patrizia Frugoni ◽  
Ennio Filippo Secchi ◽  
Carlo Chizzolini
Keyword(s):  
Cell Proliferation ◽  
B Cell ◽  
Bovine Brain ◽  
Normal Human ◽  
Proliferation In Vitro ◽  
Human B Cell

The PKCβ Selective Inhibitor, Enzastaurin (LY317615), Inhibits Growth of Human Lymphoma Cells.

Blood ◽  
2005 ◽  
Vol 106 (11) ◽  
pp. 1483-1483 ◽  
Author(s):  
Randall M. Rossi ◽  
Alicia D. Henn ◽  
Rebecca Conkling ◽  
Monica L. Guzman ◽  
Timothy Bushnell ◽  
...  
Keyword(s):  
B Cell ◽  
Cell Lymphoma ◽  
Large Cell ◽  
Oral Gavage ◽  
Subcutaneous Transplantation ◽  
Human Lymphoma ◽  
Micromolar Range ◽  
Human B Cell

Abstract Activation of PKC contributes to tumor cell survival and proliferation and has been implicated in the pathogenesis of human B cell lymphomas. Specifically, PKCβ activation is increased in tumor cells from patients with poor prognosis diffuse large cell lymphoma (DLCL), suggesting that PKCβ may be a target for therapeutic intervention. In this study we tested the PKCβ inhibitor, Enzastaurin (LY317615), using both cell culture and xenograft assays, on a panel of eight DLCL lines (OCI-Ly3, OCI-Ly7, OCI-Ly10, OCI-Ly19, SUDHL-4, SUDHL-6, Farage, and Toledo). In suspension culture, Enzastaurin was cytotoxic to all lines tested, with an average IC50 at 48 hours of 2.0 micromolar (range 0.5–4.0 micromolar). Molecular analyses showed that Enzastaurin treatment inhibited phosphorylation of GSK3β, a potential pharmacodynamic marker of Enzastaurin activity. Subsequent studies were performed using two subclones of the DLCL lines OCI-Ly10 and OCI-ly19, which respectively represent the ABC (activated B cell) and GC (germinal center) molecular subclasses of DLCL. Each line was engineered to express luciferase, which permits real time in vivo imaging. Upon subcutaneous transplantation into immune deficient NOD/SCID mice, both lines formed reproducible tumors. Treatment with Enzastaurin (75mg/kg, b.i.d. oral gavage) was initiated during the first 1–2 weeks post-transplant, before palpable tumors were evident, and was continued for 14 consecutive days. The Enzastaurin treatment was well tolerated, with the only overt side effect being moderate weight loss. At the end of therapy, vehicle control treated tumors had become palpable and progressed to volumes of 40–60 cubic millimeters. In contrast, Enzastaurin treated tumors (both OCI-Ly10 and OCI-Ly19) showed no observable progression, remaining detectable by luciferase imaging, but non-palpable. Collectively, these data indicate the Enzastaurin can induce death of human DLCL lines in vitro and is at least cytostatic to human DLCL in vivo.

scholarly journals Interleukin 4 inhibits in vitro proliferation of leukemic and normal human B cell precursors.

1992 ◽  
Vol 90 (5) ◽  
pp. 1697-1706 ◽  
Author(s):  
D Pandrau ◽  
S Saeland ◽  
V Duvert ◽  
I Durand ◽  
A M Manel ◽  
...  
Keyword(s):  
B Cell ◽  
Interleukin 4 ◽  
In Vitro Proliferation ◽  
Normal Human ◽  
B Cell Precursors ◽  
Human B Cell

Presence and Possible Origin of ɛ(γ-Glutamyl)Lysine Isodipeptide in Human Plasma

1992 ◽  
Vol 67 (01) ◽  
pp. 060-062 ◽  
Author(s):  
J Harsfalvi ◽  
E Tarcsa ◽  
M Udvardy ◽  
G Zajka ◽  
T Szarvas ◽  
...  
Keyword(s):  
Human Plasma ◽  
Fibrinolytic Therapy ◽  
Normal Human Plasma ◽  
Normal Human ◽  
Hplc Technique ◽  
Significant Change

Summaryɛ(γ-glutamyl)lysine isodipeptide has been detected in normal human plasma by a sensitive HPLC technique in a concentration of 1.9-3.6 μmol/1. Incubation of in vitro clotted plasma at 37° C for 12 h resulted in an increased amount of isodipeptide, and there was no further significant change when streptokinase was also present. Increased in vivo isodipeptide concentrations were also observed in hypercoagulable states and during fibrinolytic therapy.

Inhibition of the Activities of α2-Plasmin inhibitor (PI) and CI inhibitor (CI-Inh) by the Synthetic Fibrinolytic Agent, 3-Hydroxypropyl Flufenamide (Flu-HPA)

1979 ◽  
Author(s):  
L Miles ◽  
J Burnier ◽  
M Verlander ◽  
M Goodman ◽  
A Kleiss ◽  
...  
Keyword(s):  
Plasminogen Activators ◽  
Inhibitory Effect ◽  
Mechanisms Of Action ◽  
Flufenamic Acid ◽  
Clot Lysis ◽  
Factor Xiia ◽  
Dependent Inhibition ◽  
Normal Human ◽  
Plasmin Inhibitor

Flu-HPA is one of a series of flufenamic acid derivations that enhances plasminogen-dependent clot lysis in vitro. Studies of possible mechanisms of action of Flu-HPA were undertaken. The influence of Flu-HPA on the inhibition of purified plasmin by purified PI was studied. PI activity was assessed by its inhibition of the clevage of the tripeptide S-2251 (H-D-Val-Leu-Lys-pNA) by plasmin. Flu-HPA was dissolved in DMF or in methonol and preincubated with PI before addition of plasmin. At Flu-HPA concentrations greater than 1mM and up to 60mM, the inhibitory activity of PI was totally lost. The inhibitory effect of normal human plasma on plasmin was also completely abolished at concentrations of Flu-HPA between 2.5 and 40mM. The effect of Flu-HPA on the inhibition of purified plasma kallikrein by purified CI-Inh was also studied. CI-Inh activity was measured by its inhibition of cleavage of the tripeptide Bz-Pro-Phe-Arg-pNA by kallikrein. When Flu-HPA, dissolved in DMF or in methonol, was preincubated with CI-Inh, a concentration dependent inhibition of CI-Inh activity was observed. CI-Inh activity was abolished by concentrations of Flu-HPA greater than 1mM. Flu-HPA also inhibited the activity of CI-Inh on purified Factor XIIa. These observations suggest that this flufenamic acid derivative may enhance fibrinolysis not only by inhibiting PI activity but also by decreasing the inactivation of plasminogen activators by CI-Inh.

One-Pot Synthesis and Conformational Analysis of 6-Membered Cyclic Iodonium Salts

2020 ◽  
Author(s):  
Lucien Caspers ◽  
Julian Spils ◽  
Mattis Damrath ◽  
Enno Lork ◽  
Boris Nachtsheim
Keyword(s):  
Conformational Analysis ◽  
Bronsted Acids ◽  
One Pot ◽  
Benzyl Alcohols ◽  
Iodonium Salts ◽  
Efficient Approach ◽  
One Pot Synthesis ◽  
Diaryliodonium Salts

In this article we describe an efficient approach for the synthesis of cyclic diaryliodonium salts. The method is based on benzyl alcohols as starting materials and consists of an Friedel-Crafts-arylation/oxidation sequence. Besides a deep optimization, particluar focusing on the choice and ratios of the utilized Bronsted-acids and oxidants, we explore the substrate scope of this transformation. We also discuss an interesting isomerism of cyclic iodonium salts substituted with aliphatic substituents at the bridge head carbon. <br>

In vitro Behaviour of Alumina-Hydroxiapatite Composites Coatings

2018 ◽  
Vol 69 (6) ◽  
pp. 1416-1418
Author(s):  
Alexandru Szabo ◽  
Ilare Bordeasu ◽  
Ion Dragos Utu ◽  
Ion Mitelea
Keyword(s):  
Pure Titanium ◽  
Titanium Substrate ◽  
High Strength ◽  
Biological Properties ◽  
Commercially Pure Titanium ◽  
Hvof Spraying ◽  
Before And After ◽  
Sbf Solution ◽  
Oxygen Fuel

Hydroxyapatite (HA) is a very common material used for biomedical applications. Usually, in order to improve its poor mechanical properties is combined or coated with other high-strength materials.The present paper reports the manufacturing and the biocompatibility behaviour of two different biocomposite coatings consisting of alumina (Al2O3) and hydroxyapatite (HA) using the high velocity oxygen fuel (HVOF) spraying method which were deposited onto the surface of a commercially pure titanium substrate. The biological properties of the Al2O3-HA materials were evaluated by in vitro studies. The morphology of the coatings before and after their immersing in the simulated body fluid (SBF) solution was characterized by scanning electron microscopy (SEM). The results showed an important germination of the biologic hydroxyapatite crystallite on the surface of both coatings.

Nanodrugs as a new approach in therapy of cardiovascular diseases and cancer with tumor-associated angiogenesis

2020 ◽  
Vol 28 ◽  
Author(s):  
Justyna Hajtuch ◽  
Karolina Niska ◽  
Iwona Inkielewicz-Stepniak
Keyword(s):  
Cardiovascular Disease ◽  
Cardiovascular Diseases ◽  
Controlled Drug Release ◽  
Biological Properties ◽  
Comprehensive Information ◽  
Conventional Drug ◽  
Key Factor ◽  
Functionalized Materials

Background: Cancer along with cardiovascular diseases are globally defined as leading causes of death. Importantly, some risk factors are common to these diseases. The process of angiogenesis and platelets aggregation are observed in cancer development and progression. In recent years, studies have been conducted on nanodrugs in these diseases that have provided important information on the biological and physicochemical properties of nanoparticles. Their attractive features are that they are made of biocompatible, well-characterized and easily functionalized materials. Unlike conventional drug delivery, sustained and controlled drug release can be obtained by using nanomaterials. Methods: In this article, we review the latest research to provide comprehensive information on nanoparticle-based drugs for the treatment of cancer, cardiovascular disease associated with abnormal haemostasis, and the inhibition of tumorassociated angiogenesis. Results: The results of the analysis of data based on nanoparticles with drugs confirm their improved pharmaceutical and biological properties, which gives promising antiplatelet, anticoagulant and antiangiogenic effects. Moreover, the review included in vitro, in vivo research and presented nanodrugs with chemotherapeutics approved by Food and Drug Administration. Conclusion: By the optimization of nanoparticles size and surface properties, nanotechnology are able to deliver drugs with enhanced bioavailability in treatment of cardiovascular disease, cancer and inhibition of cancer-related angiogenesis. Thus, nanotechnology can improve the therapeutic efficacy of the drug, but there is a need for a better understanding of the nanodrugs interaction in the human body, because this is a key factor in the success of potential nanotherapeutics.

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