Latest ArticlesThis study aimed to investigate the effect of the petroleum ether fraction of Xiaoyaosan (XY-A) in a rat depression model with consideration of an underlying mechanism based on gut microbiota and metabolomics. All procedures involving animal treatment were approved according to the Committee on the Ethics of Animal Experiments of Shanxi University. A rat model was established using the chronic unpredictable mild stress (CUMS) procedure and XY-A and venlafaxine (positive control) were used as intervention drugs. Sequencing of the 16S rRNA gene combined with LC-MS metabolomics was used to investigate the effects of XY-A on gut microbiota and metabolites in CUMS-induced depression, and Pearson correlation analysis was carried out on gut microbiota and metabolites. The results showed that XY-A significantly improved the depression-like behavior of CUMS rats and restored the level of brain-derived neurotrophic factor (BDNF) in the hippocampus. Gut microbiota analysis revealed that XY-A can increase the diversity of microbial species in CUMS rats and significantly restored the relative abundance of intestinal Rothia [Prevotella], with effects on intestinal inflammation and the production of short-chain fatty acids. Cecal content metabolomics identified twenty biomarkers that were altered by depression, whereas administration of XY-A ameliorated the changes in seventeen metabolites, with the most strongly affected metabolic pathways being linoleic acid metabolism, taurine and hypotaurine metabolism, primary bile acid biosynthesis, and arginine and proline metabolism. Correlation analysis further showed that there was a strong relationship between the gut microbiota and the cecal content metabolites. In summary, XY-A may exert antidepressant effects by regulating the composition of the gut microbiota and the metabolites and pathways of the cecum. The results provide a reference for the potential molecular mechanism of antidepressant action of XY-A.
To detect the inhibitory effect of Astragalus protein on the proliferation of hepatocellular carcinoma cell line HepG2, transcriptomics was used to explore the anti-tumor mechanism of Astragalus protein. The dried roots of Astragalus was precipitated by ammonium sulfate to obtain Huang Qi protein (HQP) with different molecular weights. The effect of HQP on HepG2 and its toxic effect were detected by hemocytometry. Cell necrosis was detected by flow cytometry and Hoechst/propidium iodide (PI) double staining. The necrotic marker protein receptor interacting serine/threonine kinase 1 (RIP1) was determined by Western blot. Transcriptome sequencing was performed on the control group and dosing group RNA, and differential expression genes were analyzed for RNA-seq results. qRT-PCR was used to verified the relative mRNA expression levels of candidate genes. The results showed that the inhibition of HepG2 proliferation was more obvious with the increase of HQP concentration. When the concentration of HQP was 100 μg·mL-1, the necrosis rate increased to 18.78%, and the number of red necrotic cells stained with PI was observed under the microscope. The Western blot results showed an increase in RIP1 protein levels. The results of RNA-seq analysis showed that 26 000 related genes were regulated by HQP, and 979 genes were more regulated. KEGG analysis found that some differentially expressed genes were associated with p53 signaling pathway, and qRT-PCR further verified that the sequencing results were reliable. HQP may cause programmed necrosis of HepG2 cells and may be involved in the p53 signaling pathway.
Recently, the hepatotoxicity issue regarding to Psoraleae Fructus (PF) has attracted remarkable concerns, which highlights the urgent need to explore the toxicity attenuation method for PF. In this study, we proposed an alcohol soaking and water rinsing method for pre-processing PF based on the record in the classics - "Lei Gong Pao Zhi Lun", aiming to attenuate the potential hepatotoxicity of PF. The optimal pre-processing methods and parameters were investigated by U*12(108) uniform design coupled with 3D-cultured human-derived liver organoids model and high-content imaging. The results showed that there were significant variations among the hepatotoxicity intensities of different pre-processed PF products. Four factors, including the concentration of alcohol, the ratio of material and alcohol in alcohol soaking, the time of alcohol soaking and the times of water rinsing, were found as independent significant factors (all P < 0.01). The optimal pre-process parameters were further predicted and verified as follows:the alcohol concentration is 80%, the times of alcohol soaking is 3, the ratio of alcohol and material of alcohol soaking is 3, the time for alcohol soaking is 30 h, the ratio of water and material of water rinsing is 2, the times of water rinsing is 3, the time water rinsing is 12 h and the time of steaming is 5 h. This research demonstrated that the alcohol soaking and water rinsing method can effectively reduce the potential hepatotoxicity of PF. This method provides a reference for reducing the risk of PF liver injury from the perspective of Chinese medicinal materials pre-processing.
The objective of this research was to clone 1-deoxy-D-xylulose 5-phosphate reductoisomerase gene (MoDXR) and its promoter sequence from Morinda officinalis and carry out bioinformatic analysis, cis-acting elements analysis, and prokaryotic expression. On the basis of the MoDXR gene sequence obtained from the M. officinalis transcriptome and with NCBI-ORFfinder analysis, a pair of specific primers were designed, and used for RT-PCR amplification. The promoter region sequence at the 5' end of MoDXR gene was isolated by the genome walking technique. Localization of MoDXR was carried out by subcellular analysis. The prokaryotic expression plasmid pET-28a-MoDXR was constructed and transfected into Escherichia coli BL21(DE3) chemically-competent cells; the recombiant plasmid expressed fusion protein after the induction by IPTG. The full-length cDNA of MoDXR was 2 015 bp, and open reading frame (ORF) size was 1 425 bp, and it encoded 474 amino acid residues and had a molecular mass of 51.27 kD. Sequence comparison with BlastP to the NCBI database revealed that MoDXR had high sequence similarity with many other DXRs, such as Coffea arabica DXR (CaDXR) and Rauvolfia verticillata DXR (RvDXR). A phylogenetic tree revealed that MoDXR had its closest relationship with DXR from Coffea arabica and Gardenia jasminoides. The subcellular localization revealed that MoDXR protein was located on the chloroplast. Plantcare analysis indicated that the promoter region sequence of MoDXR was 1 493 bp, covering multiple light, stress, and hormone-responsive cis-regulatory elements; protein electrophoresis showed that the expressed protein was the anticipated size. This research lays the foundation for further purification and structural and functional characterization of the MoDXR protein.
Four alkaloids were isolated from the total alkaloids of the twigs and leaves of Alstonia yunnanensis (Apocynaceae) by using silica gel, ODS, Sephadex LH-20, and HPLC chromatography. Structures were determined by physical, chemical and spectroscopic methods and identified as N4-methylpseudoakuammigine (1), pseudoakuammigine (2), vinorine (3), picraline (4). Among them, compound 1 is a new monoterpenoid indole alkaloid.
The chemical constituents of Rehmanniae Radix Preparata were prepared according to the traditional method of "jiu zheng jiu shai" and investigated using multiple chromatographic methods. Six alkaloids were isolated and their structures were elucidated from spectral data and physicochemical properties, as follows:rehmanniae alkaloid A (4-{[(5-O-á-D-galactopyranosyloxy)methyl]-1H-pyrrole-2-carbaldehyde-1-yl}butyric acidmethyl ester) (1), baimantuoluoamide B (2), capparisine C (3), harman-3-carboxylic acid (4), (2S)-1-[2-(furan-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carboxylate (5), and 1-[2-(furan-2-yl)-2-oxoethyl]pyrrolidin-2-one (6). Among them, compound 1 is a new alkaloid. Compounds 2-6 were newly isolated from Rehmannia glutinosa Libosch. The effect of compounds 1-6 on NRK-52e cell injury induced by LPS was investigated. The results show that compounds 1-3 exhibit protective effects against LPS-induced damage to NRK-52e cells.
Following small molecules and monoclonal antibodies, oligonucleotides are expected to overcome the rare and refractory human diseases. It has been attracted the attention of the pharmaceutical industry since the approval of six oligonucleotides in recent years because of their unique mechanism of regulating disease gene transcription at the RNA level. As a new class of drug molecules, oligonucleotides are highly polar, charged, and need to be improved by means of chemical modification and drug delivery systems. And therefore, they have different clinical pharmacology properties compared with chemical molecules and monoclonal antibodies, which pose new challenges for early clinical development. This paper reviews the characteristics of oligonucleotides from the perspective of technological development, mechanism of action, human pharmacokinetics, efficacy and safety.
Eight triterpenes were isolated from the methanol extract of Galbanum by various chromatographic methods including silica gel, ODS opening column, recrystallization and semi-preparative HPLC. Their structures were determined by spectroscopic methods and physicochemical properties as 3β, 19α, 21α-trihydroxyl-12-en-28-oic acid (1), sumaresinolic acid (2), 3β, 19α-dihydroxyl-12-en-28-oic acid (3), oleanolic acid (4), 3β, 6β, 19α-trihydroxyl-12-en-28-oic acid (5), 19α-hydroxy oleanonic acid (6), 6α-hydroxy oleanonic acid (7), and (11R, 12R)-3α, 6α-dihydroxy-epoxyolean-28α, 13α-olide (8). Among them, compound 1 is a new compound, while compounds 2-8 were newly isolated from the Apiaceae family. The ability of compounds 1-8 to inhibit cholinesterase was determined with an improved Ellman method. Compound 1 showed strong inhibitory activity against butyrylcholinesterase. The molecular docking results indicated that Trp82, His438, Phe329 and Ala328 played an important role in the binding of compound 1 to butyrylcholinesterase.
This work investigates the effects of Guilingji (GLJ) on D-galactose-induced aging and changes in serum metabolites by UHPLC-Q exactive orbitrap-MS in rats. The rat model of aging by subcutaneous injection of D-galactose (300 mg·kg-1) was used to analyze the effect of different concentrations of GLJ (37.5, 75, 150 mg·kg-1) on an open field test in aging rats. Rat serum was collected after 8 weeks and subjected to LC-MS to analyze the anti-aging effect of GLJ. Animal experimentation was approved according to the Committee on the Ethics of Animal Experiments of Shanxi University (SXULL2014032). GLJ significantly improved the autonomous activity of rats. Compared with the control group, 23 metabolites in the treated group changed significantly, involving three main pathways. The group that was given GLJ had altered regulation of 4 serum metabolites in two pathways. Our results indicate that GLJ can delay aging behavior in rats; the mechanism of this anti-ageing effect remains to be determined.
The resonance light scattering (RLS) spectral characteristics of the interaction between rose Bengal and mexiletine hydrochloride in the presence of cetylpyridinium bromide were investigated. A dual-wavelength resonance light scattering (DWO-RLS) method for the determination of mexiletine hydrochloride in drugs was established. In a weakly acidic solution, rose Bengal interacts with mexiletine hydrochloride and cetylpyridinium bromide to form a red ternary ion association complex, which led to a significantly enhanced resonance light scattering signal and produced two strong characteristic scattering peaks at 372 nm and 596 nm. In these two wavelengths the mass concentration of mexiletine hydrochloride was in the range of 0.004 to 0.65 mg·L-1 and had a good linear relationship with the resonance light scattering enhancement intensity (ΔIRLS), with detection limits of 0.003 2 mg·L-1 (372 nm) and 0.003 8 mg·L-1 (596 nm), respectively. When measured by the dual-wavelength resonance light scattering (DWO-RLS) technique, the detection limit was lower, only 0.001 8 mg·L-1. When the DWO-RLS method was applied to the determination of mexiletine hydrochloride in commercially available mexiletine hydrochloride tablets, and the recovery was 98.5%-103%, and the relative standard deviation was 2.0%-2.7%.
No. 86 Xueyuan South Road, Haidian District, Beijing
010-62662699(Operation and Technical Support)
qkjq@cast.org.cn
Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House
