17912-85-5Relevant academic research and scientific papers
COMPOUNDS AND USES THEREOF IN THE TREATMENT/PREVENTION OF GRAM-NEGATIVE BACTERIAL INFECTIONS
-
Page/Page column 30; 31, (2014/09/29)
The present disclosure relates to compounds of formula I in the treatment and/or prevention of a Gram-negative bacterial infection in a multicellular organism. The disclosure also relates to a pharmaceutical composition comprising said compound, a method of treatment and/or prevention of said infection comprising the administration of said compound, and the use of said compound for the manufacture of a medicament for treating and/or preventing said infection. The disclosure also relates to the modulation of the activity of a type three secretion system in a Gram-negative bacterium.
Solving the supply of resveratrol tetramers from Papua New Guinean rainforest anisoptera species that inhibit bacterial type III secretion systems
Davis, Rohan A.,Beattie, Karren D.,Xu, Min,Yang, Xinzhou,Yin, Sheng,Holla, Harish,Healy, Peter C.,Sykes, Melissa,Shelper, Todd,Avery, Vicky M.,Elofsson, Mikael,Sundin, Charlotta,Quinn, Ronald J.
, p. 2633 - 2640 (2015/02/19)
The supply of (-)-hopeaphenol (1) was achieved via enzymatic biotransformation in order to provide material for preclinical investigation. High-throughput screening of a prefractionated natural product library aimed to identify compounds that inhibit the bacterial virulence type III secretion system (T3SS) identified several fractions derived from two Papua New Guinean Anisoptera species, showing activity against Yersinia pseudotuberculosis outer proteins E and H (YopE and YopH). Bioassay-directed isolation from the leaves of A. thurifera, and similarly A. polyandra, resulted in three known resveratrol tetramers, (-)-hopeaphenol (1), vatalbinoside A (2), and vaticanol B (3). Compounds 1-3 displayed IC50 values of 8.8, 12.5, and 9.9 μM in a luminescent reporter-gene assay (YopE) and IC50 values of 2.9, 4.5, and 3.3 μM in an enzyme-based YopH assay, respectively, which suggested that they could potentially act against the T3SS in Yersinia. The structures of 1-3 were confirmed through a combination of spectrometric, chemical methods, and single-crystal X-ray structure determinations of the natural product 1 and the permethyl ether analogue of 3. The enzymatic hydrolysis of the β-glycoside 2 to the aglycone 1 was achieved through biotransformation using the endogenous leaf enzymes. This significantly enhanced the yield of the target bioactive natural product from 0.08% to 1.3% and facilitates ADMET studies of (-)-hopeaphenol (1).
Resveratrol oligomers from Vatica albiramis
Abe, Naohito,Ito, Tetsuro,Ohguchi, Kenji,Nasu, Minori,Masuda, Yuichi,Oyama, Masayoshi,Nozawa, Yoshinori,Ito, Masafumi,Iinuma, Munekazu
experimental part, p. 1499 - 1506 (2010/12/24)
Five new stilbenoids, vatalbinosides A-E (1-5), and 13 known compounds (6-18) were isolated from the stem of Vatica albiramis. The effects of these new compounds on interleukin-1β-induced production of matrix metalloproteinase-1 (MMP-1) in human dermal fibroblasts were examined. Three resveratrol tetramers, (-)-hopeaphenol (6), vaticanol C (13), and stenophyllol C (14), were identified as strong inhibitors of MMP-1 production.
