Quality evaluation of phytomedicines is limited to small molecules as quality markers, even for herbs with high sugar contents. We established a high-resolution method for distinguishing similar medicinal materials using sugar as quality marker, taking Schisandrae Chinensis Fructus (SCF) and Schisandrae Sphenantherae Fructus (SSF) as an example. High performance liquid chromatography with an evaporative light-scattering detector (HPLC-ELSD), high performance size exclusion chromatography coupled with multi-angle laser light scattering detector and refractive index detector (HPSEC-MALLS-RID) and high performance liquid chromatography with photo-diode array (HPLC-PDA) after 1-phenyl-3-methyl-5-pyrazolone (PMP) pre-column derivatization were used respectively to determine monosaccharide contents, molecular weights and monosaccharide compositions of polysaccharides in this study. The differences of SCF and SSF from ten producing areas were compared by principal component analysis (PCA) and hierarchical cluster analysis (HCA). Results showed that contents of fructose and glucose were similar between SCF and SSF. Molecular weight (Mw) of SCF polysaccharides was ranging from 1.561 × 102 to 6.599 × 102 kDa, and that of SSF polysaccharides was ranging from 8.524 × 102 to 1.7416 × 103 kDa. Schisandra polysaccharides were mainly composed of mannose, galacturonic acid, glucose, galactose and arabinose. Based on PCA and HCA, SCF and SSF from ten different areas were classified into three categories. With great accuracy, sensitivity and stability, the methods established in this study had important reference value for quality evaluation, development and utilization of saccharide components in medicinal materials.
The pericarps of Zanthoxylum bungeanum (ZBP) and leaves of Zanthoxylum bungeanum (ZBL) are popular spices in China, and they have pharmacological activities as well. In this experiment, the volatile organic compounds (VOCs) of the pericarps of Zanthoxylum bungeanum in Sichuan (SJ) and its leaves (SJY) and the pericarps of Zanthoxylum bungeanum in Shaanxi (SHJ) and its leaves (SHJY) were analyzed by headspace-gas chromatography-ion mobility spectrometry (HS-GC-IMS) and headspace solid phase microextraction-gas chromatography-mass spectrometry (HS-SPME-GC-MS). The fingerprint of HS-GC-IMS and the heat maps of HS-SPME-GC-MS were established. Principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA) were performed. The results showed that a total of 95 components were identified, 62 components identified by HS-SPME-GC-MS and 40 components identified by HS-GC-IMS, of which 7 were the same. The analysis found that SJ and SHJ were obviously distinguished, while SJY and SHJY were not. There were considerably fewer VOCs in the leaves than in the pericarps. In the characterization of the VOCs of ZBL and ZBP, the flavor of ZBP was more acrid and stronger, while the flavor of ZBL was lighter and slightly acrid. Thirteen and eleven differential markers were identified by HS-GC-IMS and HS-SPME-GC-MS, respectively. This is helpful in distinguishing between SHJ and SJ, which contributes to their quality evaluation.
Although utilization of fluorine compounds has a long history, synthesis of chiral fluorinated amino acid derivatives with structural diversity and high stereoselectivity is still very appealing and challenging. Here, we report a biomimetic study of enantioselective [1,3]-proton shift of β,β-difluoro-α-imine amides catalyzed by chiral quinine derivatives. A wide range of corresponding β,β-difluoro-α-amino amides were achieved in good yields with high enantioselectivities. The optically pure β,β-difluoro-α-amino acid derivatives were further obtained, which have high application values in the synthesis of fluoro peptides, fluoro amino alcohols and other valuable fluorine-containing molecules.
Background/Objectives: Breast cancer remains the leading malignancy affecting women worldwide, with significant mortality rates. This study aimed to evaluate the prognostic significance of FOXM1 expression specifically in hormone receptor-positive, HER2-negative (HR+HER2-) breast cancer patients with high KPNA2 expression, and to identify potential FOXM1-targeted therapeutic strategies for this patient subgroup. Methods: We analyzed RNA sequencing and microarray data from three independent cohorts: Mackay Memorial Hospital patient samples, The Cancer Genome Atlas, and Gene Expression Omnibus databases. The expression levels of KPNA2, FOXM1, CCNB1, and CCNB2 were evaluated, with particular emphasis on stratifying patients based on KPNA2 expression levels. Their associations with clinical outcomes were assessed using Gene Set Enrichment Analysis and survival analyses. Results: While KPNA2 expression showed strong positive correlations with FOXM1, CCNB1, and CCNB2 across all datasets, our analysis revealed a distinct prognostic pattern in HR+HER2- breast cancer patients with high KPNA2 expressions. In this specific subgroup, low FOXM1 expression emerged as a favorable prognostic indicator, despite the generally poor prognosis associated with high KPNA2 levels. Gene Set Enrichment Analysis demonstrated significant enrichment of the G2/M checkpoint pathway in high KPNA2-expressing patients, suggesting potential therapeutic vulnerability to FOXM1 inhibition in this subgroup. Conclusions: This study establishes FOXM1 expression as a critical prognostic marker, specifically in KPNA2-high HR+HER2- breast cancer patients, where low FOXM1 levels correlate with improved survival outcomes. These findings suggest that FOXM1 inhibition could be particularly effective in patients with high KPNA2 expression, offering a novel therapeutic strategy for this specific molecular subtype. Several FOXM1 inhibitors, including thiostrepton and FDI-6, warrant investigation as potential targeted treatments for KPNA2-high HR+HER2- breast cancer patients.
In the presence of CBr4 and a suitable base, the cyclization reaction of N-aryl enamines proceeds with high efficiency leading to a series of 1H-indoles and 3H-indoles with moderate to good yields.
The study was conducted to investigate the effects of four dietary amino acid levels on the productive performance,blood indices and amino acid concentrations in milk of lactating sows based on ideal dietary amino acid pattern.Two hundred Large White×Landrace sows,with similar body conditions and parturition dates,were allocated to four groups with fifty replicates per group and one sow per replicate.The sows were fed with four diets with total lysine levels of 0.9%(trial group 1),1.0%(trial group 2),1.1%(trial group 3)and 1.2%(trial group 4)and the same digestible amino acid pattern(digestible lysine∶digestible valine∶digestible threonine∶digestible sulphur amino acids∶digestible tryptophane=100∶85∶66∶60∶19)by adding synthetic amino acids.The results showed that weaning litter weight gain in trial group 2 was higher than that in trial groups 1 and 4 by 4.48% and 4.34%(P0.01);average daily weight gain in trial group 2 was higher than that in trial groups 1 and 4 by 5.46% and 4.74%(P0.01).Backfat thickness loss in trial group 2 was higher than that in trial group 4 by 0.57 mm(P0.05).The concentration of plasma urea nitrogen in trial group 2 was significantly lower than that in the other groups(P0.05).The concentrations of plasma lysine,threonine,valine,methionine,isoleucine,citrullinde,glutamate,glycine(P0.01)and leucine(P0.05)in trial group 2 were significantly lower than those in trial group 4,and there was no significant difference with those in trial groups 1 and 3(P0.05)expect that the concentrations of plasma lysine and threonine in trial group 2 were significantly lower than those in trial group 1(P0.05).Plasma total amino acids in trial group 2 were the lowest(P0.05 or P0.01).The concentration of lysine in milk was significantly lower than that in trial group 4(P0.01),but there was no significant difference with trial groups 1 and 3(P0.05);the concentrations of valine(P0.05),isoleucine(P0.05),leucine(P0.05),alanine(P0.05),tyrosine(P0.05)and glutamate(P0.05)in milk in trial group 2 were higher than those in the other groups.In conclusion,based on ideal dietary amino acid pattern,when the daily total lysine intake was 59 g/d(1.0% lysine in a diet),the lactating sows could have the highest amino acid utilization and the best productive performance.
Front Cover. Sinomenium acutum is widely distributed in Korea, Japan and China, and its rattan stem as a kind of traditional Chinese Medicine (Sinomenii Caulis) has a broad range of physiological activities such as anti-inflammation, anticancer and anti-arrhythmia. Furthermore, it has been used to treat rheumatoid arthritis and its symptoms in recorded history in China. Three new alkaloids (1 – 3), one new diphenyl ether (4), along with fifteen known alkaloids (5 – 19), were isolated from the rattan stems of S. acutum. The isolated compounds were tested for the anti-inflammatory potential by measuring the amount of NO production, compounds 4 and 5 had strong NO inhibitory activity as reported by C. Wang et al. in their research article at 10.1002/cbdv.202200334.
We have developed a unified approach to 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles with ethyl acetate decoration by treating hydrazides, thiohydrazides and imidohydrazide with ethyl 3,3,3-trifluoropropanoate in the presence of a suitable base.
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