RESUMO
Penctrimertone (1), a novel citrinin dimer bearing a 6/6/6/6 tetracyclic ring scaffold, along with two known compounds xerucitrinic acid A (2) and citrinin (3) were isolated from the endophytic fungus Penicillium sp. T2-11. Their structures were unequivocally established by a comprehensive interpretation of the spectroscopic data, with the stereochemistry for 1 was defined by a combination of TDDFT-ECD calculations and the DP4+ probability analysis based on NMR chemical shift calculations. Bioassays revealed that compound 1 exhibited noticeable antimicrobial activities and moderate cytotoxicity. A plausible biosynthetic pathway of 1 was also proposed.
Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Citrinina/farmacologia , Gastrodia/microbiologia , Penicillium/química , Antibacterianos/isolamento & purificação , Antineoplásicos/isolamento & purificação , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/farmacologia , Linhagem Celular Tumoral , Queixo , Citrinina/isolamento & purificação , Endófitos/química , Humanos , Estrutura Molecular , Rizoma/microbiologiaRESUMO
The 21th century is the century of exploring and utilizing the underground space. In the future, more and more people will spend more and more time living or/and working in the underground space. However,we know little about the effect on the health of human caused by the underground environment. Herein,we systematically put forward the strategic conception of the deep-underground medicine,in order to reveal relative effects and mechanism of the potential factors in the deep underground space on human's physiological and psychological healthy,and to work out the corresponding countermeasures. The original deep-underground medicine includes the following items. â To model different depth of underground environment according to various parameters (such as temperature,radiation,air pressure, rock,microorganism), and to explore their quantitative character and effects on human health and mechanism. â¡ To study the psychological change, maintenance of homeostasis and biothythm of organism in the deep underground space. ⢠To learn the association between psychological healthy of human and the depth, structure, physical environment and working time of underground space. ⣠To investigate the effect of different terrane and lithology on healthy of human and to deliberate their contribution on organism growth. ⤠To research the character and their mechanism of growth,metabolism,exchange of energy,response of growth, aging and adaptation of cells living in deep underground space. ⥠To explore the physiological feature,growth of microbiome and it's interaction with host in the deep underground space. ⦠To develop deep-underground simulation space, the biologically medical technology and equipments. As a research basis,a deep-underground medical lab under a rock thickness of about 1 470 m has been built,which aims to operate the research of the effect on living organism caused by different depth of underground environment.
Assuntos
Pesquisa Biomédica/tendências , Espaços Confinados , HumanosRESUMO
Four new neoclerodane diterpenoids, leucansalvialins FI (1-4), and one rare 18(4â¯ââ¯3)-abeo-abietane diterpenoid, leucansalvialin J (5), were isolated from the aerial part of Salvia leucantha Cav., along with 14 known analogues. Leucansalvialin F (1) represents the first rearranged salvigenane type clerodane-17,12:18,6-diolide. Their structures were elucidated by 1D and 2D NMR spectroscopic data analysis, and the absolute configurations of 1, 2, 3, and 5 were determinded by X-ray diffraction crystal analysis and the ECD technique. All of the isolated components were evaluated for their neurotrophic activities on PC12 cells and all new compounds were evaluated for their cytotoxicity against five human cancer cell lines (HL-60, A-549, SMMC-7721, MCF-7, and SW480). Compounds 2 and 5 showed moderate neuroprotective effects in an in vitro assay.
Assuntos
Abietanos/isolamento & purificação , Diterpenos/isolamento & purificação , Fármacos Neuroprotetores/isolamento & purificação , Salvia/química , Abietanos/farmacologia , Animais , Linhagem Celular Tumoral , Diterpenos/farmacologia , Diterpenos Clerodânicos , Humanos , Estrutura Molecular , Fármacos Neuroprotetores/farmacologia , Células PC12 , Componentes Aéreos da Planta/química , RatosRESUMO
A new coumarin, anisucoumaramide (1), and a new δ-truxinate derivative, anisumic acid (2), were isolated from Clausena anisum-olens. Their structures were elucidated from extensive NMR and MS data. The absolute configurations of the coumarins were assigned using the experimental and calculated electronic circular dichroism data. Anisucoumaramide (1) represents the first example of a naturally occurring coumarin of which the terpenoidal side chain does not comply with the biosynthesis isoprene rule due to the presence of an unprecedented acetamido motif directly connected with the terpenoidal side chain. The δ-truxinate derivative was isolated from Clausena species for the first time. Compound 1 showed high selectivity for the MAO-B isoenzyme and inhibitory activity in the nanomolar range. Putative biosynthesis pathways toward 1 and 2 are proposed.