Posted by naturalproductman on November 25, 2015
Gunda Georg and co-workers at the University of Minnesota reported in the Journal of Medicinal Chemistry on the addition of a phosphonooxymethyl group onto triptolide to increase its water solubility by greater than 3,580 times. (slight mistake: Scheme 2 in the paper has the use of benzoyl peroxide shown as “Bn2O2” when it should be “Bz2O2” – Bn2O2 would be benzyl peroxide). Another interesting point from this paper is that this natural product has multiple modes of action where it can covalently attach to proteins (XPB, xeroderma pigmentosum B) or non-covalently (DCTPP1, dCTP pyrophosphatase). Other modified attempts to form soluble prodrugs of this natural product (e.g. carboxylic acid, amino acid esters) resulted in difficult removal of the prodrug group.
J. Med. Chem. paper
Posted in Alzheimer's, Cancer, Diterpene, Epoxides, Medicinal Chemistry, Prodrug | 1 Comment »
Posted by naturalproductman on January 25, 2012
Rodney Fernandes and co-workers from IIT Bombay have reported in European JOC on the synthesis of arundic acid.
European JOC paper
Posted in Alzheimer's, Asymmetric, Carboxylic acids, Cascade Reactions, Diseases, Methodology, Neurodegenerative, Total Synthesis | Leave a Comment »
Posted by naturalproductman on January 17, 2012
Miwa Kubo and co-workers at Tokushima Bunri University have reported in Tetrahedron Letters on some norsesquiterpenoids from Illicium jiadifengpi possessing neurotrophic activity. This Illicium species is the same name that merrilactone came from (Illicium merrillianum)
Posted in Alzheimer's, Diseases, Neurodegenerative, Norsesquiterpenes | Leave a Comment »
Posted by naturalproductman on November 19, 2011
Jan Bieschke and co-workers at Washington University in St. Louis have reported in Biochemistry on the inhibition of theaflavins as inhibitors of amyloid-beta and alpha-synuclein fibrillogenesis.
Posted in Alzheimer's, Aromatic, Diseases, Flavins, Parkinson's, Polyphenolic | Leave a Comment »
Posted by naturalproductman on October 30, 2011
Theo Luider and colleagues at Erasmus Medical Center in the Netherlands have reported in the Journal of Proteome Research on the higher concentration of PZP (Pregnancy Zone Protein) in presymptomatic Alzheimer’s disease group of women.
Journal of Proteome Research paper
Posted in Alzheimer's, Diseases, Peptides, Proteomics | Leave a Comment »
Posted by naturalproductman on May 16, 2011
Philip Williams and co-workers at the University of Hawaii have reported in Phytochemistry on the isolation of sebestenoids. Sebestenoid D had an IC50 value of 65 micromolar against BACE1 aspartic protease in the presence of detergent.
Posted in Alzheimer's, Aromatic, Diseases | Leave a Comment »
Posted by naturalproductman on March 5, 2011
Yadin Dudai and colleagues at the Weizmann Institute have reported in Science on a protein that is responsible for improving long term memory (PKMzeta).
Posted in Alzheimer's, Diseases, Proteins | Leave a Comment »
Posted by naturalproductman on January 24, 2011
Toshiyuki Kan and co-workers at the University of Shizuoka and Global COE program have reported in Chem Comm on a total synthesis of nobiletin where they incorporated a 11C isotope to visualize the compound through PET (positron emission tomography) in order to see where it goes in the rat brain. Nobiletin was found to enhance PKA/ERK/CREB signalling in rat hippocampal neurons.
Chem Comm paper
Posted in Alzheimer's, Aromatic, Diseases, Methodology, Total Synthesis | Leave a Comment »
Posted by naturalproductman on December 13, 2010
When I saw the term “galubulimima” I knew that the corresponding author was related to Lewis Mander – he and co-workers have recently isolated a new set of galubulimima alkaloids.
Posted in Alkaloids, Alzheimer's, Diseases | Leave a Comment »