scholarly journals Resonance Transfer of Excitation Energy between Non-steroidal Anti-inflammatory Drugs and Aromatic Amino Acids

1970 ◽  
Vol 18 (1) ◽  
pp. 186-190 ◽  
Author(s):  
KOJI MIZUNO ◽  
SHUNICHI HATA ◽  
SUIICHI TOMIOKA
Keyword(s):  
Amino Acids ◽  
Excitation Energy ◽  
Aromatic Amino Acids ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Resonance Transfer

scholarly journals The conjugation of nonsteroidal anti-inflammatory drugs (NSAID) to small peptides for generating multifunctional supramolecular nanofibers/hydrogels

2013 ◽  
Vol 9 ◽  
pp. 908-917 ◽  
Author(s):  
Jiayang Li ◽  
Yi Kuang ◽  
Junfeng Shi ◽  
Yuan Gao ◽  
Jie Zhou ◽  
...  
Keyword(s):  
Amino Acids ◽  
Critical Concentration ◽  
Therapeutic Agents ◽  
Multiple Roles ◽  
Small Peptides ◽  
Covalent Linkage ◽  
Physiological Conditions ◽  
Racemic Ibuprofen ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Here we report supramolecular hydrogelators made of nonsteroidal anti-inflammatory drugs (NSAID) and small peptides. The covalent linkage of Phe–Phe and NSAIDs results in conjugates that self-assemble in water to form molecular nanofibers as the matrices of hydrogels. When the NSAID is naproxen (1), the resultant hydrogelator 1a forms a hydrogel at a critical concentration (cgc) of 0.2 wt % at pH 7.0. Hydrogelator 1a, also acting as a general motif, enables enzymatic hydrogelation in which the precursor turns into a hydrogelator upon hydrolysis catalyzed by a phosphatase at physiological conditions. The conjugates of Phe–Phe with other NSAIDs, such as (R)-flurbiprofen (2), racemic flurbiprofen (3), and racemic ibuprofen (4), are able to form molecular hydrogels, except in the case of aspirin (5). After the conjugation with the small peptides, NSAIDs exhibit improved selectivity to their targets. In addition, the peptides made of D-amino acids help preserve the activities of NSAIDs. Besides demonstrating that common NSAIDs are excellent candidates to promote aromatic–aromatic interaction in water to form hydrogels, this work contributes to the development of functional molecules that have dual or multiple roles and ultimately may lead to new molecular hydrogels of therapeutic agents for topical use.

scholarly journals Phytochemical research and anti-inflammatory activity of the dry extracts from northern highbush blueberry leaves

2021 ◽  
pp. 40-48
Author(s):  
Oleksandr Stremoukhov ◽  
Oleh Koshovyi ◽  
Mykola Komisarenko ◽  
Igor Kireyev ◽  
Andriy Gudzenko ◽  
...  
Keyword(s):  
Amino Acids ◽  
Phenolic Compounds ◽  
Side Effects ◽  
New Drugs ◽  
Inflammatory Activity ◽  
Highbush Blueberry ◽  
Northern Highbush Blueberry ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Blueberry Leaves

All over the world, non-steroidal anti-inflammatory drugs (NSAIDs) are taken annually by about three hundred million people and this figure is constantly increasing. At the same time, NSAIDs are also one of the most common causes of side effects of drug therapy. The development and implementation of new anti-inflammatory drugs, including those of plant origin, with minimal side effects is an urgent task of modern pharmaceutical science. Vaccinium corymbosum L. (family Ericaceae), which is gaining more and more popularity among berry crops and is successfully cultivated in Ukraine, is promising in this direction for research. The aim: phytochemical analysis of dry extracts from blueberry leaves to establish the possibility of creating new drugs with anti-inflammatory activity. Materials and methods. The objects of the study were dry extracts of northern highbush blueberry leaves. The content of amino acids and phenolic compounds was determined by HPLC and spectrophotometry. The prototypal activity was studied in vivo and in vitro. Research results. 4 dry extracts were obtained from northern highbush blueberry leaves. In the extracts obtained by HPLC, 7 amino acids were identified, including 3 essential ones: arginine, histidine, and phenylalanine. As a result of the HPLC study, 7 phenolic compounds were identified in extracts from the leaves of northern highbush blueberry: 5 flavonoids - rutin, quercetin-3-O-glucoside, kaempferol-3-O-glucoside, quercetin and kaempferol and 2 hydroxycinnamic acids, chlorogenic and caffeic acid. For the first time, the anti-inflammatory effect of extracts from blueberry leaves was investigated. It was revealed that extract 1 at a dose of 50 mg/kg and extract 4 modified with arginine at a dose of 25 mg/kg have the highest anti-inflammatory activity. Conclusions. The results of the conducted studies indicate that extracts from the leaves of northern highbush blueberry in terms of the content of biologically active substances are promising sources for the creation of new drugs and dietary supplements with anti-inflammatory activity

Synthesis of Acetaminophen Analogues Containing α-Amino Acids and Fatty Acids for Inhibiting Hepatotoxicity

Synthesis ◽  
2019 ◽  
Vol 51 (19) ◽  
pp. 3683-3696
Author(s):  
Seunghee Jung ◽  
Yuya Kawashima ◽  
Takuya Noguchi ◽  
Nobuyuki Imai
Keyword(s):  
Amino Acids ◽  
Fatty Acids ◽  
Side Effects ◽  
Lower Incidence ◽  
Reactive Metabolite ◽  
Benzoquinone Imine ◽  
Aniline Derivatives ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Acetaminophen is a popular antipyretic analgesic medicine that has weaker anti-inflammatory properties and lower incidence of side effects than nonsteroidal anti-inflammatory drugs (NSAIDs). However, acetaminophen causes hepatotoxicity due to the reactive metabolite N-acetyl-p-benzoquinone imine (NAPQI). We have obtained acetaminophen analogues in 57–99% yields by using aniline derivatives with protected α-amino acids and fatty acids via the corresponding mixed carbonic carboxylic anhydrides in aqueous MeCN. We have also succeeded in synthesizing AM404 analogues in 76–97% yields, which are expected to be promising candidates for reducing hepatotoxicity.

scholarly journals The Hypolipidemic and Anti-Inflammatory Activity of Boronated Aromatic Amino Acids in CF1 Male Mice

1999 ◽  
Vol 6 (6) ◽  
pp. 337-344
Author(s):  
Merrill C. Miller ◽  
A. Sood ◽  
Bernard F. Spielvogel ◽  
Iris H. Hall
Keyword(s):  
Amino Acids ◽  
Serum Cholesterol ◽  
Mechanism Of Action ◽  
Proteolytic Enzymes ◽  
Endotoxic Shock ◽  
Aromatic Amino Acids ◽  
Central Pain ◽  
Male Mice ◽  
Hypolipidemic Agents ◽  
Anti Inflammatory

The boronated aromatic amino acids were shown to be potent hypolipidemic agents in mice lowering both serum cholesterol and triglycerides after 16 days. Selective compounds were as effective as the clinical standards. Furthermore, the compounds were effective anti-inflammatory agents reducing local and central pain as well as suppressing LPS induced endotoxic shock in mice. These agents inhibited lysosomal and proteolytic enzymes of the liver and macrophages as a part of their mechanism of action.

Polyphenols from Cymbopogon citratus inhibit iNOS expression and NO production – a promising source of new anti-inflammatory drugs

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
V Francisco ◽  
A Figueirinha ◽  
B Neves ◽  
C Garcia-Rodriguez ◽  
M Lopes ◽  
...  
Keyword(s):  
Inos Expression ◽  
No Production ◽  
Cymbopogon Citratus ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Promising Source

Heparin and proteoglycans as anti-inflammatory drugs

1996 ◽  
Vol 16 (01) ◽  
pp. 56-59
Author(s):  
D. J. Tyrrell ◽  
C. P. Page
Keyword(s):  
Inflammatory Diseases ◽  
Therapeutic Applications ◽  
Wide Range ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

SummaryEvidence continues to accumulate that the pleiotropic nature of heparin (beyond its anticoagulant potency) includes anti-inflammatory activities at a number of levels. It is clear that drugs exploiting these anti-inflammatory activities of heparin may offer exciting new therapeutic applications to the treatment of a wide range of inflammatory diseases.

The Efficient Preparation of Radiolabeled Aromatic Amino Acids via Cu-Mediated Radiofluorination using Ni-complexes

2019 ◽  
Author(s):  
A Craig ◽  
N Kolks ◽  
E Urusova ◽  
BD Zlatopolskiy ◽  
B Neumaier
Keyword(s):  
Amino Acids ◽  
Aromatic Amino Acids
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