RESUMO
Cynanchum viminale subsp. australe, more commonly known as caustic vine, is a leafless succulent that grows in the northern arid zone of Australia. Toxicity toward livestock has been reported for this species, along with use in traditional medicine and its potential anticancer activity. Disclosed herein are novel seco-pregnane aglycones cynavimigenin A (5) and cynaviminoside A (6), together with new pregnane glycosides cynaviminoside B (7) and cynavimigenin B (8). Cynavimigenin B (8) contains an unprecedented 7-oxobicyclo[2.2.1]heptane moiety in the seco-pregnane series, likely arising from a pinacol-type rearrangement. Interestingly, these isolates displayed only limited cytotoxicity in cancer and normal human cell lines, in addition to low activity against acetylcholinesterase and Sarcoptes scabiei bioassays, suggesting that 5-8 are not associated with the reported toxicity of this plant species.
Assuntos
Cáusticos , Cynanchum , Humanos , Acetilcolinesterase , Austrália , Glicosídeos/farmacologia , Pregnanos/farmacologia , Raízes de PlantasRESUMO
BACKGROUND: Special diet with restricted branched-chain-amino-acids used for treating maple syrup urine disease can lead to specific amino acid deficiencies. CASE CHARACTERISTICS: We report a neonate who developed skin lesions due to isoleucine deficiency while using specialised formula. INTERVENTION/OUTCOME: Feeds were supplemented with expressed breast milk. This caused biochemical and clinical improvement with resolution of skin lesions. MESSAGE: Breast milk is a valuable and necessary adjunct to specialized formula in maple syrup urine disease to prevent specific amino acid deficiency in the neonatal period.
Assuntos
Isoleucina , Doença da Urina de Xarope de Bordo , Acrodermatite , Aleitamento Materno , Diagnóstico Diferencial , Humanos , Fórmulas Infantis , Recém-Nascido , Isoleucina/administração & dosagem , Isoleucina/deficiência , Doença da Urina de Xarope de Bordo/dietoterapia , Doença da Urina de Xarope de Bordo/genética , Doença da Urina de Xarope de Bordo/fisiopatologia , Zinco/deficiênciaRESUMO
Structure-based virtual screening of two libraries containing 567â¯981 molecules was used to discover novel, selective BuChE inhibitors, which are potentially superior symptomatic treatments in late-stage Alzheimer's disease. Compound 16 was identified as a highly selective submicromolar inhibitor of BuChE (huBuChE IC50 = 0.443 µM) with high permeability in the PAMPA-BBB model. The X-ray crystal structure of huBuChE in complex with 16 revealed the atomic-level interactions and offers opportunities for further development of the series.