RESUMO
To develop novel 2-cyanoacrylate derivatives with potential bioactivity, a number of 2-cyanoacrylate compounds, including substituted pyrazole or 1,2,3-triazole ring, were designed, prepared, and structurally detected by 1H NMR, 13C NMR, and elemental analysis. The biological assessment displayed that some designed compounds had significant herbicidal activities against Brassica juncea, Chenopodium serotinum, Rumex acetosa, Alopecurus aequalis, Polypogon fugax, and Poa annua at a dosage of 1500 g/ha. Furthermore, some derivatives still expressed satisfactory herbicidal activities against Brassica juncea, Chenopodium serotinum, and Rumex acetosa when the dosage was lowered to 150 g/ha, especially the inhibitory effects of compounds 9a, 9d, 9f, 9i, 10a, 10b, 10e, and 10n against Brassica juncea were all over 80%, compounds 9d, 9f, 9g, 9h, 9i, 10h, 10i, 10m, 10n, and 10o possessed more than 70% inhibition rates against Chenopodium serotinum, and compound 9d indicated 70% herbicidal activity against Rumex acetosa. These results provided an important basis for further design and discovery of biologically active 2-cyanoacrylate compounds.
Assuntos
Cianoacrilatos , Herbicidas , Herbicidas/química , Espectroscopia de Ressonância Magnética , Poaceae , Triazóis/química , Relação Estrutura-AtividadeRESUMO
The oxidosqualene cyclase family of Rosa rugosa (RrOSC) provides a starting point for the triterpenoid pathway, which contributes to the medicinal value of the extraction of tissues of Rosa rugosa. However, the structure and function of key RrOSCs of active triterpenoids remain ambiguous. In this study, a total of 18 RrOSC members with conservative gene structures and motifs were identified based on the genome of Rosa rugosa. The RrOSCs were located on three chromosomes including two gene clusters that derived from gene replication. The phylogenetic relationship divided RrOSCs into six groups, and the RrOSCs of GI and GIV that were represented by lupeol or α-amyrin were identified as likely to include candidate genes for producing active triterpenoids. Considering the high expression or specific-tissue expression of the candidates, RrOSC1, RrOSC10, RrOSC12, and RrOSC18 were considered the key genes. RrOSC12 was identified in vitro as lupeol synthase. The results provided fundamental information and candidate genes for further illustration of the triterpenoid pathway involved in the pharmacological activities of Rosa rugosa.
Assuntos
Ácido Oleanólico , Rosa , Triterpenos , Rosa/metabolismo , Filogenia , Triterpenos/química , Extratos Vegetais/farmacologiaRESUMO
Rosa rugosa, a renowned ornamental plant, is cultivated for its essential oil containing valuable monoterpenes, sesquiterpenes, and other compounds widely used in the floriculture industry. Farnesyl diphosphate synthase (FPPS) is a key enzyme involved in the biosynthesis of sesquiterpenes and triterpenes for abiotic or biotic stress. In this study, we successfully cloned and characterized a full-length FPPS- encoding cDNA identified as RrFPPS1 using RT-PCR from R. rugosa. Phylogenetic analysis showed that RrFPPS1 belonged to the angiosperm-FPPS clade. Transcriptomic and RT-qPCR analyses revealed that the RrFPPS1 gene had tissue-specific expression patterns. Subcellular localization analysis using Nicotiana benthamiana leaves showed that RrFPPS1 was a cytoplasmic protein. In vitro enzymatic assays combined with GC-MS analysis showed that RrFPPS1 produced farnesyl diphosphate (FPP) using isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP) as substrates to provide a precursor for sesquiterpene and triterpene biosynthesis in the plant. Additionally, our research found that RrFPPS1 was upregulated under salt treatment. These substantial findings contribute to an improved understanding of terpene biosynthesis in R. rugosa and open new opportunities for advancements in horticultural practices and fragrance industries by overexpression of the RrFPPS1 gene in vivo increased FPP production and subsequently led to elevated sesquiterpene yields in the future. The knowledge gained from this study can potentially lead to the development of enhanced varieties of R. rugosa with improved aroma, medicinal properties, and resilience to environmental stressors.
Assuntos
Hemiterpenos , Compostos Organofosforados , Rosa , Sesquiterpenos , Geraniltranstransferase/genética , Rosa/genética , Filogenia , Estresse Salino , Clonagem MolecularRESUMO
Rosa rugosa is highly regarded for its aesthetic and therapeutic qualities. In particular, R. rugosa's flowers are known to produce essential oils containing a mixture of volatile terpenes, phenylpropanoids, and other compounds. Despite this, extensive research exists on volatile terpenes in flowers, while the knowledge of non-volatile terpenes in distinct tissues is still limited. Using UPLC-ESI-MS/MS, a comprehensive analysis of the terpene metabolites in five different tissues of R. rugosa was conducted. These metabolites accumulated in distinct tissues, and the majority of them were triterpenoids. Transcriptome data were collected from five tissues using RNA-seq. Transcriptomics and metabolomics were utilized to evaluate the triterpene biosynthesis pathway, resulting in new insights into its regulation and biosynthesis. The RrOSC10 was identified as a key enzyme in converting 2,3-oxidosqualene into α-amyrin, potentially contributing to the triterpene biosynthesis pathway. Furthermore, the expression of the RrOSC10 gene was upregulated by salinity for 0.5 h and 1 h, with subsequent downregulation at 2 h. This study lays a foundation for future research on the biosynthesis and accumulation of triterpenes in R. rugosa.
RESUMO
Background: Rotator cuff tear has become one of the diseases affecting people's living quality. Conventional anchor materials such as titanium alloy and poly-lactic acid can lead to postoperative complications like bone defects and aseptic inflammation. Magnesium (Mg)-based implants are biodegradable and biocompatible, with strong potential to be applied in orthopaedics. Methods: In this study, we developed a high-purity (HP) Mg suture anchor and studied its mechanical properties and degradation behavior in vitro. Furthermore, we described the use of high-purity Mg to prepare suture anchor for the rotator cuff repair in sheep. Results: The in vitro tests showed that HP Mg suture anchor possess proper degradation behavior and appropriate mechanical property. Animal experiment indicated that HP Mg suture anchor provided reliable anchoring function in 12 weeks and showed no toxic effect on animal organs. Conclusion: In summary, the HP Mg anchor presented in this study had favorable mechanical property and biosecurity.The translational potential of this article: The translational potential of this article is to use high-purity Mg to develop a degradable suture anchor and verify the feasibility of the application in animal model. This study provides a basis for further research on the clinical application of biodegradable high-purity Mg suture anchor.