UPCOMING THEMATIC ISSUE – DEVELOPMENT OF NANO-FORMULATIONS USING QUALITY BY DESIGN (QbD) APPROACH – NANOSCIENCE & NANOTECHNOLOGY – ASIA

NNA-THEMATIC FLYER -Gautam Singhvi

https://benthamscience.com/journals/nanoscience-and-nanotechnology-asia/special-issues/

 

OPEN ACCESS ARTICLE – Sulfonamides as Inhibitors of Leishmania – Anti-Infective Agents

Journal: Anti-Infective Agents

Author(s): Jade Katinas*, Rachel Epplin, Christopher Hamaker, Marjorie A. Jones

Graphical Abstract:

 

Abstract:

Introduction: Leishmaniasis is an endemic disease caused by the protozoan parasite Leishmania. Current treatments for the parasite are limited by cost, availability and drug resistance as the occurrence of leishmaniasis continues to be more prevalent. Sulfonamides are a class of compounds with medicinal properties which have been used to treat bacterial and parasitic disease via various pathways especially as antimetabolites for folic acid.

Methods: New derivatives of sulfonamide compounds were assessed for their impact on Leishmania cell viability and potential pathways for inhibition were evaluated. Leishmania tarentolae (ATCC Strain 30143) axenic promastigote cells were grown in brain heart infusion (BHI) medium and treated with varying concentrations of the new sulfonamide compounds. Light microscopy and viability tests were used to assess the cells with and without treatment.

Discussion: A non-water soluble sulfonamide was determined to have 90-96% viability inhibition 24 hours after treatment with 100 μM final concentration. Because Leishmania are also autotrophs for folate precursors, the folic acid pathway was identified as a target for sulfonamide inhibition. When folic acid was added to untreated Leishmania, cell proliferation increased. A water soluble derivative of the inhibitory sulfonamide was synthesized and evaluated, resulting in less viability inhibition with a single dose (approximately 70% viability inhibition after 24 hours with 100 μM final concentration), but additive inhibition with multiple doses of the compound.
Results: However, the potential mechanism of inhibition was different between the water-soluble and non-water soluble sulfonamides. The inhibitory effects and potential pathways of inhibition indicate that these compounds may be new treatments for this disease.

 

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EDITOR’S CHOICE – Differential Regulation of CYP3A4 and CYP3A5 and its Implication in Drug Discovery – INFECTIOUS DISORDERS – Current Drug Metabolism

Journal: Current Drug Metabolism

Author(s): Ogheneochukome Lolodi, Yue-Ming Wang, William C. Wright, Taosheng Chen*

Graphical Abstract:

 

Abstract:

Background: Cancer cells use several mechanisms to resist the cytotoxic effects of drugs, resulting in tumor progression and invasion. One such mechanism capitalizes on the body’s natural defense against xenobiotics by increasing the rate of xenobiotic efflux and metabolic inactivation. Xenobiotic metabolism typically involves conversion of parent molecules to more soluble and easily excreted derivatives in reactions catalyzed by Phase I and Phase II drug metabolizing enzymes.

Methods: We performed a structured search of peer-reviewed literature on P450 (CYP) 3A, with a focus on CYP3A4 and CYP3A5.

Results: Recent reports indicate that components of the xenobiotic response system are upregulated in some diseases, including many cancers. Such components include the pregnane X receptor (PXR), CYP3A4 and CYP3A5 enzymes. The CYP3A enzymes are a subset of the numerous enzymes that are transcriptionally activated following the interaction of PXR and many ligands.

Conclusion: Intense research is ongoing to understand the functional ramifications of aberrant expression of these components in diseased states with the goal of designing novel drugs that can selectively target them.

Read more here: http://www.eurekaselect.com/152811

 

WISHING A VERY HAPPY BIRTHDAY TO DR. RUEY-SHIN JUANG!

Dr. Ruey-Shin Juang

DR. RUEY-SHIN JUANG

EDITOR-IN-CHIEF: Current Biochemical Engineering

Department of Chemical and Materials Engineering
Chang Gung University
Kwei-Shan, Taoyuan
Taiwan

 

UPCOMING THEMATIC ISSUE – INFECTIOUS CAUSES OF CHILDHOOD DISABILITY – Infectious Disorders – Drug Targets

IDDT-THEMATIC FLYER-Gulam Khandaker

https://benthamscience.com/journals/infectious-disorders-drug-targets/

Thought of the Day!

nikoskazantzakis1-2x

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Medicinal Chemistry Volume 14, Issue 2
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Anti-Cancer Agents in Medicinal Chemistry Volume 17, Issue 14
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WISHING A VERY HAPPY BIRTHDAY TO DR. BIN WU!

Confetti Golden Birthday Card

DR. BIN WU

EDITOR-IN-CHIEF: The Natural Products Journal
Zhejiang University
Hangzhou
China

WISHING A VERY HAPPY BIRTHDAY TO DR. SEAN L. KITSON!

Dark Blue with Neon Birthday Elements Birthday Poster

DR. SEAN L. KITSON

EDITOR-IN-CHIEF: Current Radiopharmaceuticals

Department of Biocatalysis and Isotope Chemistry Almac Sciences
Almac House
Craigavon
Northern Ireland