RESUMEN
Until now the genus Amana (Liliaceae), known as 'East Asian tulips', has contained just seven species. In this study, a phylogenomic and integrative taxonomic approach was used to reveal two new species, Amana nanyueensis from Central China and A. tianmuensis from East China. A. nanyueensis resembles Amana edulis in possessing a densely villous-woolly bulb tunic and two opposite bracts, but differs in its leaves and anthers. Amana tianmuensis resembles Amana erythronioides in possessing three verticillate bracts and yellow anthers, but differs in aspects of its leaves and bulbs. These four species are clearly separated from each other in principal components analysis based on morphology. Phylogenomic analyses based on plastid CDS further support the species delimitation of A. nanyueensis and A. tianmuensis and suggests they are closely related to A. edulis. Cytological analysis shows that A. nanyueensis and A. tianmuensis are both diploid (2n = 2x = 24), different from A. edulis, which is either diploid (northern populations) or tetraploid (southern populations, 2n = 4x = 48). The pollen morphology of A. nanyueensis is similar to other Amana species (single-groove germination aperture), but A. tianmuensis is quite different because of the presence of a sulcus membrane, which creates the illusion of double grooves. Ecological niche modelling also revealed a niche differentiation between A. edulis, A. nanyueensis and A. tianmuensis.
RESUMEN
Copper mediated C(sp2)-H amination and hydroxylation of arylphosphinic acid are accomplished by adopting phosphinamide as the directing group. This method is distinguished by its wide substrate scope and excellent functional group tolerance, thus allowing for the rapid preparation of organophosphorus compounds in organic synthesis.
RESUMEN
One long-standing issue in directed C-H functionalization is that either nitrogen or sulfur atoms present in heterocyclic substrates may bind preferentially to a transition-metal catalyst rather than to the desired directing group. This competitive binding has largely hindered the application of C-H functionalization in late-stage heterocycle drug discovery. Reported here is the use of an oxazoline-based directing group capable of overriding the poisoning effect of a wide range of heterocycle substrates. The potential use of this directing group in pharmaceutical drug discovery is illustrated by diversification of Telmisartan (an antagonist for the angiotensinâ II receptor) through copper-mediated C-H amination, hydroxylation, thiolation, arylation, and trifluoromethylation.
RESUMEN
Ten pyrazole derivatives were synthesized and evaluated for their ability to inhibit the replication of influenza virions. All the compounds were synthesized in good-to-excellent yield, and the structures were ascertained with the help of (1) H NMR, (13) C NMR, mass, and elemental analysis. Among the tested series, compound 4i was identified as the most potent analog against the H1N1 virus, with IC50 = 5.4 µM, while the rest of the compounds showed mild-to-moderate inhibition of infection. Moreover, these compounds showed excellent inhibitory activity against influenza A neuraminidase (NA), with IC50 values ranging from 2.15 to 7.54 µM, among which compound 4i showed the most prominent inhibition with IC50 = 1.32 µM. To further exemplify the molecular contacts with NA, a molecular docking study of 4i was conducted with the 3D crystal structure of enzyme H5N1-NA in complex. Results showed that target molecules interact in a similar fashion with oseltamivir and zanamivir by creating interatomic contacts with Trp178, Glu227, and Arg371. Moreover, in the toxicity assay with the porcine renal proximal cell line, LLC-PK1, the confocal images showed no appreciable change in morphological character at the highest tested dose.
Asunto(s)
Antivirales/química , Subtipo H1N1 del Virus de la Influenza A/efectos de los fármacos , Isoquinolinas/química , Neuraminidasa/antagonistas & inhibidores , Pirazoles/química , Animales , Antivirales/síntesis química , Antivirales/farmacología , Catálisis , Línea Celular , Supervivencia Celular/efectos de los fármacos , Cerio , Subtipo H1N1 del Virus de la Influenza A/enzimología , Isoquinolinas/síntesis química , Simulación del Acoplamiento Molecular , Neuraminidasa/química , Pirazoles/síntesis química , Pirazoles/farmacología , Relación Estructura-Actividad , Porcinos , Replicación Viral/efectos de los fármacosRESUMEN
OBJECTIVE: Construction of human full-length survivin gene-modified DCs vaccine and observe the biological characteristics and the role of laryngeal cancer treatment. METHODS: Construction of homologous recombination through the full-length survivin-human adenovirus (pAd-sur), and transfection of immature DCs, induced by access to sophisticated cultivate DCs, the proliferation of activated T lymphocytes; DCs vaccine different groups observed in vitro, in vivo biological activity. RESULTS: The success in bringing human to build a full-length survivin gene recombinant adenovirus vector pAd-sur; get with the typical characteristics of DCs, the expression level of the surface molecules of up to CD1a 46.2%, CD80 64.2%, CD83 80.5%, HLA-DR 84.3%, vaccine for in vitro cell killing rate 51.5%, compared with the control group, the difference was significant (t = 7.1358, P < 0.01). Gene-modified tumor cell vaccine group was 54.9% of apoptosis and necrosis rate of 21.9%, compared with the control group, the difference was significant (t value was 33.0209 and 17.5057, all P < 0.01). CONCLUSION: Human full-length survivin gene modified, DCs The expression of surface molecules than the rate of gene-modified DCs without a significant increase, with more to stimulate T lymphocyte proliferation, and promote secretion of gamma-IFN; in vivo, in vitro to promote the ability of anti-laryngeal cancer cells.
Asunto(s)
Vacunas contra el Cáncer/inmunología , Células Dendríticas/inmunología , Neoplasias Laríngeas/prevención & control , Proteínas Asociadas a Microtúbulos/genética , Proteínas Asociadas a Microtúbulos/inmunología , Animales , Línea Celular Tumoral , Femenino , Vectores Genéticos , Humanos , Proteínas Inhibidoras de la Apoptosis , Neoplasias Laríngeas/inmunología , Ratones , Ratones Desnudos , Organismos Modificados Genéticamente , SurvivinRESUMEN
OBJECTIVE: To learn about the complete genomic sequence of the Seoul virus strain ZT10 isolated from M. fartis. METHODS: The total RNA was extracted from the infected Vero E6 cells and amplified by RT-PCR. The purified PCR products were cloned into T-vector and sequenced. RESULTS: The results demonstrated that the complete genome of ZT10 was comprised of L(6530), M(3651) and S(1753) segments which encoded 2151-1133 and 429 amino acids respectively. CONCLUSION: Analysis of sequence revealed that the ZT10 belonged to Seoul virus. The nucleotide sequence identity of the M gene with Seoul virus was 84.0%-96.3%. The identity with Hantan vrisu (Prospect Hill virus, Tula virus) isolated from M. fartis was 57.5%-60.9%. The sequence identity of the S gene with Seoul virus was 87.9%-96.0% at nucleotide level and 96.9%-97.9% at amino acid level.
Asunto(s)
Orthohantavirus/genética , Orthohantavirus/aislamiento & purificación , Animales , Antígenos Virales/análisis , Línea Celular , Clonación Molecular , ADN Complementario/genética , ADN Viral/genética , Técnica del Anticuerpo Fluorescente Directa , Orthohantavirus/clasificación , Filogenia , Reacción en Cadena de la Polimerasa , Alineación de Secuencia , Análisis de Secuencia de ADNRESUMEN
OBJECTIVE: To study the risk factors of male infertility. METHOD: Case control study including 94 cases and control group with a ratio of 1 to 1. RESULTS: The risk factors of male infertility were long time heavy smoking habit (OR = 3.45, 95% CI: 1.95 - 6.10), illegal sexual intercourse (OR = 7.29, 95% CI: 2.54 - 20.89), growing vegetable under plastic in higher temperature (OR = 6.73, 95% CI: 1.91 - 23.69), contact with benzene chemicals (OR = 20.53, 95% CI: 4.67 - 90.25) and having Ureaplasma urealyticum (Uu) infection (OR = 5.55, 95% CI: 2.28 - 13.53). CONCLUSION: Male infertility was resulted from many factors repeatedly acting on men for long time. In order to prevent male infertility, issues as environmental pollution, occupational protection need to be improved while bad working condition and risky behavior should be changed.