Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0220723 (PCA)
 4,687 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The synthesis and structure-activity relationships of a number of 1,3-bis(aryloxy)propanes, which are in vivo antagonists of LTD4 in the guinea pig, are described. One of these compounds, 4 (Wy-44,329), was not only approximately equipotent with the standard 1 (FPL 55712) in the LTC4 (ID50 = 0.17 and 0.23 mg/kg iv, respectively) and LTD4 (ID50 = 0.11 and 0.15 mg/kg iv, respectively) challenge models but also possessed greater potency in the ovalbumin challenge model (ID50 = 0.47 mg/kg and 4.1 mg/kg iv, respectively) and a longer duration of action. This compound was a competitive LTD4 antagonist on guinea pig ileum (pA2 = 9.4) and possessed mediator release (rat PCA, ID50 = 0.26 mg/kg iv) and 5-lipoxygenase (IC50 = 32 microM vs. 5-HETE) inhibitory activities.
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PMID:Novel 1,3-bis(aryloxy)propanes as leukotriene D4 antagonists. 380 66

Some natural compounds isolated from Chinese plants were found to have strong inhibitory activity for 5-lipoxygenase and were thus able to inhibit leucotriene synthesis. Among these compounds, caffeic acid was selected for study; more than 100 of its derivatives were synthesized and tested for 5-lipoxygenase inhibitory activity. Two derivatives, TMK-919 and TMK-920, proved to be 100 times more potent than the parent compound and were able to inhibit the homologous PCA reaction significantly in rats at a dose of 10 mg/kg, i.v.
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PMID:New lipoxygenase inhibitors isolated from Chinese plants. Development of new anti-allergic drugs. 388 51

The methanolic extract of the roots of Asiasarum sieboldi has been evaluated for anti-allergic effects on various experimental models in vitro and in vivo. Bioassay-guided fractionation of the methanolic extract resulted in isolation of suppressive compounds in the PCA test: methyleugenol (1), elemicin (2), gamma-asarone (3), (-)-asarinin (4), and (-)-sesamin (5). Furthermore, elemicin (2) and (2E,4E,8Z,10E)-N-isobutyl-2,4,8,10-dodecatetraenami de (6) were found to exhibit an inhibitory action on 5-lipoxygenase (5-LOX) from RBL-1 cells. 3',4'-Dimethoxycinnamaldehyde (7) and xanthoxylol (8) potently reduced the contractile response of guinea pig ileal strips to LTD4.
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PMID:Studies on anti-allergic components in the roots of Asiasarum sieboldi. 820 62

The application of metabolomics in phytochemical analysis is an innovative strategy for targeting active compounds from a complex plant extract. Species of the Asteraceae family are well-known to exhibit potent anti-inflammatory (AI) activity. Dual inhibition of the enzymes COX-1 and 5-LOX is essential for the treatment of several inflammatory diseases, but there is not much investigation reported in the literature for natural products. In this study, 57 leaf extracts (EtOH-H2O 7:3, v/v) from different genera and species of the Asteraceae family were tested against COX-1 and 5-LOX while HPLC-ESI-HRMS analysis of the extracts indicated high diversity in their chemical compositions. Using O2PLS-DA (R2 > 0.92; VIP > 1 and positive Y-correlation values), dual inhibition potential of low-abundance metabolites was determined. The O2PLS-DA results exhibited good validation values (cross-validation = Q2 > 0.7 and external validation = P2 > 0.6) with 0% of false positive predictions. The metabolomic approach determined biomarkers for the required biological activity and detected active compounds in the extracts displaying unique mechanisms of action. In addition, the PCA data also gave insights on the chemotaxonomy of the family Asteraceae across its diverse range of genera and tribes.
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PMID:A Metabolomic Approach to Target Compounds from the Asteraceae Family for Dual COX and LOX Inhibition. 2618 33