Click chemistry and drug delivery: A bird's-eye view

Click chemistry has been proven to be very useful in drug delivery. Due to the availability of a large number of click reactions with a various characteristics, selection of appropriate chemistry for a given application is often not a trivial task. This review is written for pharmaceutical researchers who are interested in click chemistry applications and yet may not be click chemistry experts. For this, the review gives an overview of available click reactions organized by application types. Further, the general understanding of click reactions being fast and high yielding sometimes overshadows the need to analyze reaction kinetics in assessing suitability of a given reaction for certain applications. For this, we highlight the need to analyze the relationship among reaction kinetics, concentration effects, and reaction time scales, knowing that lack of such analysis could easily lead to failures. Further, possible issues such as chemical stability with various click reagents are also discussed to aid experimental designs. Recent examples and extensive references are also provided to aid in-depth understanding of technical details. We hope this review will help those interested in using click chemistry in drug delivery to select the appropriate reactions/reagents and minimize the number of pitfalls.

Organic carbon monoxide prodrug, BW-CO-111, in protection against chemically-induced gastric mucosal damage

Metal-based carbon monoxide (CO)-releasing molecules have been shown to exert anti-inflammatory and anti-oxidative properties maintaining gastric mucosal integrity. We are interested in further development of metal-free CO-based therapeutics for oral administration. Thus, we examine the protective effect of representative CO prodrug, BW-CO-111, in rat models of gastric damage induced by necrotic ethanol or aspirin, a representative non-steroidal anti-inflammatory drug. Treatment effectiveness was assessed by measuring the microscopic/macroscopic gastric damage area and gastric blood flow by laser flowmetry. Gastric mucosal mRNA and/or protein expressions of HMOX1, HMOX2, nuclear factor erythroid 2-related factor 2, COX1, COX2,

Nature's marvels endowed in gaseous molecules I: Carbon monoxide and its physiological and therapeutic roles

Nature has endowed gaseous molecules such as O

Hydrogen sulfide prodrugs-a review

Hydrogen sulfide (H2S) is recognized as one of three gasotransmitters together with nitric oxide (NO) and carbon monoxide (CO). As a signaling molecule, H2S plays an important role in physiology and shows great potential in pharmaceutical applications. Along this line, there is a need for the development of H2S prodrugs for various reasons. In this review, we summarize different H2S prodrugs, their chemical properties, and some of their potential therapeutic applications.

The progress in research for human pulse system modeling and pulse condition information analysis / 生物医学工程学杂志

This article introduces the significance, methods and applications in human pulse study, with an emphasis on the history, current situation and progress of pulse system modeling and pulse signal analysis. The problems in present study and the methods for the future investigations were analyzed.

CD45 MOLECULE AND GENERATION OF EPIDERMAL γδ T CELLS FROM MICE / 免疫学杂志

To investigate the role of CD45 protein tyrosine phosphatase in γδ T cell development,we exa-mined whether Vγ3 dendritic epidermal T cells (DETC),a subset of γδ T cells uniquely reside in the murine epidermis were altered in the CD45-gene -deficient mice.In situ immunolabelling on epidermal sheets demonstrsted that the CD45-deficient mice had a normal density and immunophenotype of Vγ3 DETC in comparison to the wild-type control mice.RT-PCR revealed that similar levels of Vγ3 TCR mRNA were present in the epidermis of both CD45-deficient mice and wild-type controls.FCM showed no significant difference in the proportion of Vγ3 T cells in the epidermal cells between the two genotypes.In addition, the frequency of Vγ2 T cells, another subset of γδT cells in lymph nodes was normal in CD45-deficient mice.These results indicate that althouh CD45 is crucial for the development of αβΤ cells,it might be not necessary for the thymic maturation of γδ T cells including Vγ3 DETC and Vγ2 T cells.