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BioAssay: AID 399546

Spasmolytic activity in guinea pig ileum assessed as inhibition of spontaneous contraction relative to papaverine

A CH(2)Cl(2)-MeOH (1:1) extract prepared from the whole plant of Nidema boothii inhibited spontaneous contractions (IC(50) = 6.26 +/- 2.5 microg/mL) of the guinea-pig ileum. Bioassay-guided fractionation of the active extract led to the isolation of the novel spiro compound 1, which was given the trivial name nidemone, and the new dihydrophenanthrene 3, characterized as more ..
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 Tested Compounds
 Tested Compounds
All(17)
 
 
Unspecified(17)
 
 
 Tested Substances
 Tested Substances
All(17)
 
 
Unspecified(17)
 
 
 Related BioAssays
 Related BioAssays
AID: 399546
Data Source: ChEMBL (547575)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-05-14

Data Table ( Complete ):           View All Data
Tested Compounds:
Description:
Title: Spasmolytic effects, mode of action, and structure-activity relationships of stilbenoids from Nidema boothii.

Abstract: A CH(2)Cl(2)-MeOH (1:1) extract prepared from the whole plant of Nidema boothii inhibited spontaneous contractions (IC(50) = 6.26 +/- 2.5 microg/mL) of the guinea-pig ileum. Bioassay-guided fractionation of the active extract led to the isolation of the novel spiro compound 1, which was given the trivial name nidemone, and the new dihydrophenanthrene 3, characterized as 1,5,7-trimethoxy-9,10-dihydrophenanthrene-2,6-diol. In addition, the known stilbenoids aloifol II (2), 1,5,7-trimethoxyphenanthrene-2,6-diol (4), ephemeranthoquinone (5), gigantol (6), ephemeranthol B (7), 2,4-dimethoxyphenanthrene-3,7-diol (8), lusianthridin (9), and batatasin III (10) were obtained. The isolates were characterized structurally by spectroscopic data interpretation. Compounds 2-6, 9, and 10 induced notable concentration-dependent inhibition of the spontaneous contractions of the guinea-pig ileum with IC(50) values that ranged between 0.14 and 2.36 microM. Bibenzyl analogues 23-35 were synthesized and tested pharmacologically. The results indicated that for maximum spasmolytic activity the bibenzyls should have oxygenated substituents on both aromatic rings; on the other hand, methylation of free hydroxyl groups as well as the increment of oxygenated groups in relation to compounds 6 and 10 decreased the smooth muscle relaxant activity. It was also demonstrated that bibenzyls 6 and 10 might exert their spasmolytic action not only by a nitrergic mechanism but also by inhibiting CaM-mediated processes.
(PMID: 14987052)
Comment
Putative Target:
ChEMBL Target ID: 102380
Target Type: TISSUE
Pref Name: Ileum
Organism: Cavia porcellus
Tax ID: 10141
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
BAO: Assay Format: tissue-based format
Assay Tissue: Ileum
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ratio IC50 activity commentRatio IC50 activity commentString
2Ratio IC50 standard flagRatio IC50 standard flagInteger
3Ratio IC50 qualifierRatio IC50 qualifierString
4Ratio IC50 published valueRatio IC50 published valueFloat
5Ratio IC50 standard valueRatio IC50 standard valueFloat

Data Table (Concise)
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