RESUMEN
Nowadays, cultivated variants and adulterants of Astragali Radix (AR) have flooded the market, causing the quality assurance of AR to be challenging. To address this issue, we combined network pharmacology with chromatographic fingerprinting and multicomponent quantitative analysis for the quality evaluation of AR. Specifically, through network pharmacology, a complete understanding of the active components and pharmacological activities of AR was established. In addition, establishing fingerprint profiles and multicomponent quantitation by high-performance liquid chromatography (HPLC) is convenient and comprehensive, and can more fully reflect the overall situation of the distribution of various chemical components. To evaluate and differentiate AR from different origins, hierarchical cluster analysis and principal component analysis were performed. The result showed that AR acts synergistically through multiple targets and pathways. The content of chemical components in AR from different origins varied significantly. Combining network pharmacology and multicomponent quantification results, astragaloside II and IV and formononetin can be used as quality markers for the quality control of AR. This study provides a comprehensive and reliable strategy for the quality evaluation of AR and identifies its quality markers to ensure the quality of the herb.
Asunto(s)
Planta del Astrágalo , Medicamentos Herbarios Chinos , Planta del Astrágalo/química , Astragalus propinquus , Cromatografía Líquida de Alta Presión/métodos , Medicamentos Herbarios Chinos/química , Farmacología en RedRESUMEN
Three new aconitine-type C19-diterpenoid alkaloid namely novolunines A (1), B (2), and C (3), along with fifteen known diterpenoid alkaloids were isolated from the roots of Aconitum novoluridum, whose phytochemical investigations have never been reported before. The structures of three new alkaloids were established on the basis of spectra data (high-resolution electrospray ionization (HR-ESI)-MS, IR, one dimensional (1D)- and 2D-NMR). Noteworthily, novolunines A (1) and B (2) are two diterpenoid alkaloids bearing conformational isomerism. In addition, the diterpenoid alkaloids 1-3 did not show any anti-acetylcholinesterase (AChE) or anti-inflammatory activities.
Asunto(s)
Acetilcolinesterasa/metabolismo , Aconitum/química , Antiinflamatorios/farmacología , Inhibidores de la Colinesterasa/farmacología , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/aislamiento & purificación , Electrophorus , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Ratones , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Células RAW 264.7RESUMEN
Three types of new Euphorbia diterpene pseudo-alkaloids possessing 5/6/7/3 (1), 5/6/6/4 (2-5), and 5/7/7/4 (6-7) fused ring skeletons were obtained through an unexpected BF3·Et2O/CH3CN-mediated structural conversion and amination of lathyrane diterpene (Euphorbia factor L1), in which the solution acetonitrile had been introduced into the Euphorbia diterpene as a nitrogen source and tandem amination/oxirane-opening (cyclopropane-opening)/oxa-Michael addition reaction was involved in the conversion. The structures of new Euphorbia diterpene pseudo-alkaloids were elucidated by a combination of spectroscopic data and single crystal X-ray diffraction analysis. The basic skeletons of Euphorbia diterpene pseudo-alkaloids 1 and 2-5 could fall into the structural types of euphoractine B and euphoractine A diterpenes, respectively, suggesting the possible biogenetic pathway relationship between lathyrane diterpene with euphoractines A and B types diterpenes. Pseudo-alkaloids 1-7 did not show any potential cytotoxicity against several tumor cell lines.
Asunto(s)
Alcaloides Diterpénicos/química , Diterpenos/química , Euphorbia/química , Ácidos de Lewis/química , Vías Biosintéticas , Línea Celular Tumoral , China , Humanos , Estructura Molecular , Fitoquímicos/química , Semillas/químicaRESUMEN
The animate-inanimate distinction is fundamental to understand our physical world and language processing. Previous studies have shown that animate nouns are more prone to be assigned the actor role and are easier to integrate with a verb than inanimate nouns. On the basis of these characteristics of animate nouns, this study aimed to investigate whether animate nouns could facilitate the noun-noun integration. Animate-inanimate noun pairs and inanimate-inanimate noun pairs were used in an imagery task. With electroencephalogram recording, participants were instructed to integrate the two unrelated nouns in each pair to form an interactive mental imagery. These results showed a larger P600 for the animate-inanimate pairs than the inanimate-inanimate pairs. As the P600 component reflects the integration process, specifically, the more elaborate the encoding, the larger the P600 amplitude. Thus, this larger P600 amplitude indicated that a more vivid mental imagery was formed when integrating an animate noun and an inanimate noun than integrating two inanimate nouns. Thus, these results suggest that animate nouns could facilitate the integration of two unrelated nouns during the imagery task.
Asunto(s)
Comprensión/fisiología , Potenciales Evocados/fisiología , Lenguaje , Análisis y Desempeño de Tareas , Adulto , Electroencefalografía/métodos , Femenino , Humanos , Masculino , Semántica , Adulto JovenRESUMEN
Acetylcholinesterase (AChE) is the target of organophosphate (OP) and carbamate insecticides. Mutations in the AChE gene (ace) leading to decreased insecticide susceptibility is the main resistance mechanism in insects. In this study, two Chilo auricilius acetylcholinesterase genes, designated as Caace1 and Caace2, were cloned using RT-PCR and RACE. Caace1 cDNA is 2534 bp, with ORF of 2082 bp, and it encodes an acetylcholinesterase 1 (CaAChE1) protein comprising a calculated 693 amino acid (aa) residues. Caace2 cDNA contains 2280 bp, with a full-length ORF of 1917 bp, encoding acetylcholinesterase 2 (CaAChE2) comprising a calculated 638 aa residues. At the aa level, CaAChE1 displays the highest similarity (97%) with the Chilo suppressalis AChE1, and CaAChE2 shows the highest similarity with the C. suppressalis AChE2 (99%). From the restriction fragment length polymorphism (RFLP) PCR (RFLP-PCR) analysis, one mutation in Caace1, similar to the ace1 mutation associated with triazophos resistance in C. suppressalis, was detected. Detailed examination of field populations of C. auricilius indicated this resistance mutation in C. auricilius is still quite infrequent. Based on the assay of AChE activity and RFLP-PCR testing, an individual that contains resistance mutation has lower AChE activities, while the individual that does not contain the resistance mutation has higher AChE activities. This study provides a basis for future investigations into the mechanism of OP resistance in C. auricilius, as well as a guidance for C. auricilius control with reasonable choice of pesticides.