In vitro studies of a bradykinin B1/B2 antagonist linked to a human neutrophil elastase inhibitor: a heterodimer for the treatment of inflammatory disorders

1997 ◽  
Vol 75 (6) ◽  
pp. 633-638
Author(s):  
A H Leimer ◽  
H B Kroona ◽  
J K Blodgett ◽  
E T Whalley ◽  
S E Ross ◽  
...  
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
In Vitro Studies ◽  
Human Neutrophil Elastase ◽  
Neutrophil Elastase Inhibitor ◽  
Elastase Inhibitor ◽  
Inflammatory Disorders

scholarly journals Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 358 ◽  
Author(s):  
Andreia Nunes ◽  
Joana Marto ◽  
Lídia Maria Gonçalves ◽  
Sandra Simões ◽  
Rita Félix ◽  
...  
Keyword(s):  
Serine Protease ◽  
Neutrophil Elastase ◽  
In Vitro Cytotoxicity ◽  
Human Neutrophil Elastase ◽  
Therapeutic Effects ◽  
Neutrophil Elastase Inhibitor ◽  
Analytical Methodology ◽  
Elastase Inhibitor

Human neutrophil elastase (HNE) is a serine protease that degrades matrix proteins. An excess of HNE may trigger several pathological conditions, such as psoriasis. In this work, we aimed to synthesize, characterize and formulate new HNE inhibitors with a 4-oxo-β-lactam scaffold with less toxicity, as well as therapeutic index in a psoriasis context. HNE inhibitors with 4-oxo-β-lactam scaffolds were synthesized and characterized by NMR, FTIR, melting point, mass spectrometry and elemental analysis. In vitro cytotoxicity and serine protease assays were performed. The compound with the highest cell viability (AAN-16) was selected to be incorporated in an emulsion (AAN-16 E) and in a microemulsion (AAN-16 ME). Formulations were characterized in terms of organoleptic properties, pH, rheology, droplet size distribution, in vitro drug release and in vivo psoriatic activity. All compounds were successfully synthesized according to analytical methodology, with good yields. Both formulations presented suitable physicochemical properties. AAN-16 E presented the most promising therapeutic effects in a murine model of psoriasis. Overall, new HNE inhibitors were synthesized with high and selective activity and incorporated into topical emulsions with potential to treat psoriasis.

SC-39026, a specific human neutrophil elastase inhibitor

1987 ◽  
Vol 147 (2) ◽  
pp. 666-674 ◽  
Author(s):  
Akira Nakao ◽  
Richard A. Partis ◽  
Geralyn P. Jung ◽  
Richard A. Mueller
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Human Neutrophil Elastase ◽  
Neutrophil Elastase Inhibitor ◽  
Elastase Inhibitor

A Novel Oral Neutrophil Elastase Inhibitor (ONO-6818) Inhibits Human Neutrophil Elastase-induced Emphysema in Rats

2002 ◽  
Vol 166 (4) ◽  
pp. 496-500 ◽  
Author(s):  
Takashige Kuraki ◽  
Masayoshi Ishibashi ◽  
Masanori Takayama ◽  
Motokimi Shiraishi ◽  
Minoru Yoshida
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Human Neutrophil Elastase ◽  
Neutrophil Elastase Inhibitor ◽  
Elastase Inhibitor

scholarly journals Isodeoxyhelicobasidin, a novel human neutrophil elastase inhibitor from the culture broth of Volvariella bombycina

2009 ◽  
Vol 62 (6) ◽  
pp. 333-334 ◽  
Author(s):  
Guang-Hua Xu ◽  
Young-Hee Kim ◽  
Soo-Jin Choo ◽  
In-Ja Ryoo ◽  
Chang-Ji Zheng ◽  
...  
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Culture Broth ◽  
Human Neutrophil Elastase ◽  
Neutrophil Elastase Inhibitor ◽  
Elastase Inhibitor
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