RESUMEN
ABSTRACT: Male infertility is a global issue caused by poor sperm quality, particularly motility. Enhancement of the sperm quality may improve the fertilization rate in assisted reproductive technology (ART) treatment. Scriptaid, with a novel human sperm motility-stimulating activity, has been investigated as a prospective agent for improving sperm quality and fertilization rate in ART. We evaluated the effects of Scriptaid on asthenozoospermic (AZS) semen, including its impact on motility stimulation and protective effects on cryopreservation and duration of motility, by computer-aided sperm analysis (CASA). Sperm quality improvement by Scriptaid was characterized by increased hyaluronan-binding activity, tyrosine phosphorylation, adenosine triphosphate (ATP) concentration, mitochondrial membrane potential, and an ameliorated AZS fertilization rate in clinical intracytoplasmic sperm injection (ICSI) experiments. Furthermore, our identification of active Scriptaid analogs and different metabolites induced by Scriptaid in spermatozoa lays a solid foundation for the future biomechanical exploration of sperm function. In summary, Scriptaid is a potential candidate for the treatment of male infertility in vitro as it improves sperm quality, prolongs sperm viability, and increases the fertilization rate.
RESUMEN
An efficient and practical Cu(I)-catalyzed oxidative cyclization cascade reaction of diverse amines, alkyne esters and maleimides has been developed. The reactions can afford 4,6-dioxopyrrolo[3,4-b]pyrrole-2,3-dicarboxylates and related derivatives with satisfactory yields by altering the reaction conditions slightly. The substrate scope highlights the flexibility of the catalyst, and a reaction mechanism is also proposed.
RESUMEN
Three new xanthones, 22,23-dihydroxydihydrogambogenic acid (1), 12-hydroxygambogefic acid A (2), and hanburixanthone (3), along with thirteen known compounds were isolated from the resin of Garcinia hanburyi. The structures of the new compounds were determined by detailed analysis of 1D and 2D NMR spectra and by comparison with related model compounds. All compounds were tested for their cytotoxicities against A549, HCT116, and MDA-MB-231, and most of them showed significant effects on the cell lines.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Garcinia/química , Resinas de Plantas/química , Xantonas/química , Xantonas/farmacología , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Células HCT116/efectos de los fármacos , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Xantonas/análisis , Xantonas/aislamiento & purificaciónRESUMEN
In the title compound, C(11)H(11)NO(3), the dihedral angle between the benzene ring and the cyclo-propane ring is 63.2â (1)°. In the crystal, mol-ecules are linked through classical cyclic carb-oxy-lic acid O-Hâ¯O hydrogen-bond inter-actions [graph set R(2) (2)(8)] giving centrosymmetric dimers which are extended along the b-axis direction through amide N-Hâ¯O hydrogen-bond inter-actions, giving one-dimensional ribbon structures. Weak C-Hâ¯O inter-actions are also present in the structure.
RESUMEN
Three new xanthones, garcinolic acid (1), 10α-ethoxy-9,10-dihydromorellic acid (2), and 10α-ethoxy-9,10-dihydrogambogenic acid (3), along with six known compounds were isolated from the resin of Garcinia hanburyi. These compounds were tested for their cytotoxicities against A549, HCT116, SK-BR-3 and HepG2, and showed high inhibitory effects on the cell lines.
Asunto(s)
Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Garcinia/química , Resinas de Plantas/química , Xantonas/química , Línea Celular Tumoral , Humanos , Estructura MolecularRESUMEN
A novel furansesquiterpenoid, tetraenol, was isolated from a relict shrub plant, Tetraena mongolica, collected from the northern desert of the Ningxia Hui Autonomous Region. The structure of the new compound was elucidated on the basis of spectroscopic analysis.
Asunto(s)
Componentes Aéreos de las Plantas/química , Rosaceae/química , Sesquiterpenos/química , China , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Conformación Molecular , Sesquiterpenos/aislamiento & purificaciónRESUMEN
Three new polyoxygenated steroids, nanjiol A (1), B (2), and C (3), were isolated from an East China Sea soft coral Nephthea bayeri, and their structures were characterized by spectroscopic methods and comparison with known compounds. The new molecules were structurally related to (20S)-cholesta-1,4-diene-18,20-diol-3-one (4), a typical metabolite from the black coral Antipathes subpinnata.
Asunto(s)
Antozoos/química , Antineoplásicos/aislamiento & purificación , Esteroides/aislamiento & purificación , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Carcinoma Hepatocelular , China , Ensayos de Selección de Medicamentos Antitumorales , Espectroscopía de Resonancia por Spin del Electrón , Células HL-60/efectos de los fármacos , Humanos , Concentración 50 Inhibidora , Leucemia Mieloide , Conformación Molecular , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Espectroscopía Infrarroja por Transformada de Fourier , Estereoisomerismo , Esteroides/química , Esteroides/farmacología , Células Tumorales Cultivadas/efectos de los fármacosRESUMEN
A new sulphonoglycolipid, crassicaulisine, has been isolated from the red alga Chondria crassicaulis Harv.. Four known compounds were also found from the title plant. The structure of the new compound was elucidated on the basis of chemical reactions and spectroscopic analysis.
