Zhongguo Zhongyao Zazhi最新文献

The chemical constituents from the fruits of Morus nigra distributed in Xinjiang were investigated by various chromatographic separation methods, including silica gel column chromatography, reversed-phase silica gel column chromatography, Sephadex LH-20 gel column chromatography, and preparative high-performance liquid chromatography. Based on the physicochemical properties and spectroscopic data of the isolated compounds, as well as literature data, 15 compounds were identified as morusnigrane A(1), 4-hydroxylonchocarpin(2), isobavachalcone(3), euchrenone a7(4), apigenin(5), medicarpin(6),(3R)-vestitol(7), pinnatifidanin CⅡ(8), pinnatifidanin CⅠ(9),(+)-lyoniresinol(10), artotonkin(11), resveratrol(12), 4-hydroxycinnamic acid(13), myrrhain A(14), and 2,5-di-tert-butylphenol(15). Compound 1 was a new 2-arylbenzofuran, and compounds 7-9, 14, and 15 were isolated from the genus Morus for the first time. 2-Arylbenzofurans 1 and 11, flavonoids 2-4, lignans 8 and 9, and phenolic acid 14 showed inhibitory effects on the proliferation of MH7A synovial fibroblasts with the IC_(50) values ranging from(5.17±0.05) to(152.97±0.20) μmol·L~(-1), displaying the potential of anti-rheumatoid arthritis.

This study aims to systematically compare the volatile components of raw Coptidis Rhizoma, Euodia rutaecarpa-processed Coptidis Rhizoma, and E. rutaecarpa juice, identify characteristic volatile markers of E. rutaecarpa-processed Coptidis Rhizoma, and elucidate the chemical basis of its "pungent" odor. The volatile components were analyzed by using headspace-gas chromatography-ion mobility spectrometry(HS-GC-IMS) and identified via the National Institute of Standards and Technology(NIST) 2020 and IMS databases. Chemical fingerprints of the three samples were compared by using VOCal 04.07 software and the Gallery Plot plugin. Chemometric analysis of the three samples was performed by SIMCA 14.1 software, with variables of variable importance in projection(VIP)>1.0, P<0.05, and fold change(FC)>1.2 or <0.83 as characteristic volatile markers of E. rutaecarpa-processed Coptidis Rhizoma. Relative odor activity values(ROAV) were calculated to evaluate odor contributions of the three samples. A total of 161 volatile components were detected by HS-GC-IMS, with 124 identified, including esters, ketones, aldehydes, and 12 other chemical categories. Common major volatile classes in raw Coptidis Rhizoma, E. rutaecarpa-processed Coptidis Rhizoma, and E. rutaecarpa juice were esters, ketones, aldehydes, terpenes, and alcohols. After processing, E. rutaecarpa-processed Coptidis Rhizoma exhibited reduced relative peak intensities in eight categories(esters, ketones, aldehydes, terpenes, alcohols, organic acids, ethers, and phenols) and increased intensities in four categories(heterocyclic compounds, sulfur-containing compounds, alkenes, and aromatic hydrocarbons), likely due to the addition of E. rutaecarpa juice. Chemometric analysis and fingerprinting showed distinct differences among the three samples, with the clustering of each sample differentiated clearly. ROAV analysis revealed significant increases in pungent-related components, such as 1-penten-3-one, n-pentanal dimer, 2-butylfuran, and methyl thiocyanate in E. rutaecarpa-processed Coptidis Rhizoma, which correlated with the introduction of E. rutaecarpa juice. The processing of E. rutaecarpa-processed Coptidis Rhizoma significantly altered the composition of volatile components by introducing chemical constituents from E. rutaecarpa juice and promoting chemical reactions, thereby enhancing the characteristic "pungent" odor profile. The study provides a reference for the scientific processing of E. rutaecarpa-processed Coptidis Rhizoma decoction pieces.

This study aimed to investigate the effect of corilagin(Cor) on the formation of foam cells derived from J774A.1 macrophages and to explore its underlying mechanism based on the endoplasmic reticulum stress(ERS)-endoplasmic reticulum autophagy(ER-phagy) pathway. J774A.1 macrophages were used as the research model and divided into the control group, oxidized low-density lipoprotein(ox-LDL) group, tunicamycin(TM) group, and Cor treatment groups with different concentrations. Cell proliferation activity was assessed using the MTT assay. Intracellular lipid droplet accumulation was observed by oil red O staining. The levels of total cholesterol(TC) and free cholesterol(FC) in cells, as well as interleukin-6(IL-6) and monocyte chemoattractant protein-1(MCP-1) in the cell supernatants, were measured using enzyme-linked immunosorbent assay(ELISA). Intracellular reactive oxygen species(ROS) levels and apoptosis were analyzed by flow cytometry. The interaction between Cor and the eukaryotic translation initiation factor 2α(eIF2α) target protein was predicted by molecular docking. The expression levels of ERS-and autophagy-related proteins were detected by Western blot. The results showed that, compared with the model group, Cor dose-dependently reduced intracellular lipid droplets. The cholesterol ester(CE)/TC ratio was significantly decreased in the low-, medium-, and high-dose Cor groups, indicating reduced lipid deposition. In the high-dose Cor group, the levels of inflammatory cytokines IL-6 and MCP-1 in the supernatant were significantly reduced. In addition, intracellular ROS levels and apoptosis rates were markedly decreased. The optimal binding affinity between Cor and eIF2α was-8.4 kcal·mol~(-1). Furthermore, the high-dose Cor significantly downregulated the expression levels of phosphorylated(p)-eIF2α/eIF2α, activating transcription factor 4(ATF4), glucose-regulated protein 78(GRP78), C/EBP homologous protein(CHOP), nuclear factor-κB(NF-κB), Bcl-2-associated X protein(Bax), and testis expressed gene 264(Tex264), while upregulating the expression level of B-cell lymphoma-2(Bcl-2). In conclusion, Cor inhibits the formation of macrophage-derived foam cells by regulating the expression of proteins in the eIF2α-ATF4-Tex264 signaling pathway, thereby suppressing ERS-induced excessive ER-phagy and apoptosis in macrophages.

Chronic obstructive pulmonary disease(COPD) is one of the top three leading causes of death worldwide and can be divided into acute exacerbation and stable phases. Acute exacerbation of COPD(AECOPD) is the main trigger of disease progression and mortality in COPD patients, while the stable phase is a chronic and continuous stage of the disease. With continuous updates to relevant guidelines, modern medicine has achieved certain therapeutic effects in the treatment of COPD. However, long-term use of antibiotics and glucocorticoid drugs tends to drug resistance and may cause adverse reactions. Traditional Chinese medicine(TCM) attaches great importance to syndrome differentiation and has unique advantages in the treatment of lung diseases, following the principle of "treating the symptoms in acute conditions and the root in chronic ones". According to TCM theory, the pathological location of COPD is the lungs and is related to the spleen and kidneys. The disease is characterized by deficiency in origin and excess in manifestations, with phlegm and deficiency as the main pathogenesis factors. During the acute exacerbation phase, phlegm is the predominant factor, running through the disease course, and often mixed with heat, dampness(turbidity), cold, or blood stasis. These may appear in various combinations, leading to syndromes such as phlegm-heat obstructing the lungs, phlegm-turbidity blocking the lungs, external cold with internal fluid retention, and phlegm-blood stasis blocking the lungs. In the stable phase, deficiency is predominant, commonly involving deficiencies of the lungs, spleen, and kidneys. This article explored the clinical strategies of classical formulae in the treatment of COPD in recent years based on COPD staging and pathogenic factors and presented two medical cases for peer reference and discussion.

As a powerful α-glucosidase inhibitor, 1-deoxynojirimycin(DNJ) polyhydroxy alkaloid is one of the main active ingredients of TCM Mori Folium in the prevention and treatment of diabetes. DNJ has four hydroxylation positions(C-3, C-4, C-5, and C-7). Our research group has previously elucidated the biosynthetic pathway of DNJ from lysine to 2-methylpiperidine and characterized two CYP450 hydroxylases involved in the C-4 position(MaCYP71BG22) and C-7 position(MaCYP82C169) hydroxylation. To further explore the key hydroxylase genes of other hydroxylation positions, this study employed molecular docking technology to screen one candidate hydroxylase gene, MaCYP71BE347, from the transcriptome data of mulberry leaves and conducted bioinformatics analysis and functional study on it. The coding sequence length of MaCYP71BE347 is 1 419 bp, encoding 472 amino acids. It is an alkaline, unstable and hydrophilic protein that is closely related to Morus notabilis and has conserved CYP450 hydroxylase motifs such as helix K, Meander, and heme binding sites. The yeast whole cell catalysis results showed that MaCYP71BE347 protein can catalyze selective hydroxylation at the C-5 position of 2-methylpiperidine to 2-methylpiperidine-5-ol and had no hydroxylation function for piperidine, 1-methylpiperidine, 2-hydroxymethylpiperidine, and 4-hydroxypiperidine. The Agrobacterium mediated mulberry genetic transformation system and virus-induced gene silencing(VIGS) transformation system confirmed the participation of MaCYP71BE347 in the biosynthesis of DNJ in mulberry leaves. This study discovered the CYP450 enzyme MaCYP71BE347, which catalyzes the C-5 hydroxylation of the piperidine ring in the biosynthesis pathway of DNJ and is a key enzyme gene element in the biosynthesis pathway of DNJ, laying the foundation for the subsequent complete analysis of the hydroxylation process of DNJ biosynthesis in mulberry leaves.

Gastrointestinal malignant tumors are a group of severely life-threatening tumors. Their incidence and mortality rates consistently rank among the top 10 cancers worldwide and are increasing year by year. Based on his long-term clinical practice, Professor Zhou Zhongying proposes the theory of "cancer toxin". The research team led by Professor CHENG Hai-bo further establishes the pathogenesis theory of cancer toxin, holding that cancer toxin is the key factor in the occurrence and development of tumors, and thus taking "anti-cancer and detoxification" as the basic therapeutic principle. With the vigorous promotion of TCM, various active ingredients of TCM are extracted and make a difference in tumor therapy. These active ingredients can inhibit tumor cells in a multi-target and multi-pathway manner. Cinobufotalin is an active ingredient extracted from the skin of Bufo gargarizans with detoxifying, anti-swelling, and pain-relieving effects and is widely used in the treatment of intermediate and advanced tumors. Clinical studies have revealed that cinobufotalin enhances tumor control rates, prolongs survival time, improves quality of life, and reduces the incidence of adverse reactions when combined with chemotherapy, radiotherapy, or targeted therapies. The mechanism studies have demonstrated that cinobufotalin plays a therapeutic role by inhibiting cell proliferation and invasion, inducing tumor cell apoptosis, modulating immune response, reversing drug resistance, etc. This paper reviews the research progress on cinobufotalin from the perspective of pathogenesis theory of cancer toxin through summarizing domestic and international reported research on clinical application and mechanism of cinobufotalin against gastrointestinal malignant tumors in recent years. The findings aim to provide a theoretical basis for research on the anti-tumor effect of cinobufotalin and a reference for standardized use and in-depth research of drugs.

Rhododendri Mollis Flos is a Chinese herbal medicine derived from Rhododendron molle(Ericaceae), with diterpenoids being its primary bioactive constituents. Diterpene synthases are key enzymes in the biosynthetic pathway of diterpenoids. Transcriptome analysis of R. molle identified two ent-copalyl diphosphate synthase(CPS) genes(RmTPS33 and RmTPS64) and one ent-kaurene synthase(KS) gene(RmTPS65). Full-length cloning, bioinformatics analysis, and functional characterization of these three genes yielded the following results.(1) The open reading frames of RmTPS33, RmTPS64, and RmTPS65 were 2 280, 2 476, and 2 370 bp, encoding 759, 819, and 789 amino acid residues, respectively.(2)Multiple sequence alignment and phylogenetic analysis demonstrated that both RmTPS33 and RmTPS64 contained conserved CPS family motifs(LHS, PNV, and DxDD) and belonged to the TPS-c subfamily. RmTPS65 possessed conserved α-domain motifs(DDxxD and NSE/DTE) of class Ⅰ diterpene synthases and was classified into the TPS-e/f subfamily.(3) Functional assays confirmed that both RmTPS33 and RmTPS64 catalyzed the protonation-induced cyclization of GGPP to form ent-CPP, with RmTPS33 exhibiting higher catalytic activity than RmTPS64. RmTPS65 catalyzed the diphosphate elimination of ent-CPP to produce a single product, 16α-hydroxy-ent-kaurane. Furthermore, protein engineering of RmTPS33 and RmTPS64 suggested that their activity divergence stemmed from variant amino acids within functional domains. This study successfully cloned three diterpene synthases gene(RmTPS33, RmTPS64, and RmTPS65), expanding the current diterpene synthase gene repository and establishing a foundation for investigating biosynthetic pathway genes of active compounds in R. molle.

This study aimed to investigate the mechanism by which the Bushen Culuan Formula(BSCL) promotes angiogenesis induction in KGN via the CXCR4/HIF-1α signaling pathway. A cell model was established by treating KGN with triptolide, and based on this model, the optimal concentration of the CXCR4 inhibitor(AMD3100) was determined. CCK-8 assay was used to detect the effects of different concentrations of BSCL-medicated serum on the viability of KGN. After the optimal concentrations of each reagent were determined, KGN were divided into five groups: control group, triptolide group, AMD3100 group, BSCL group, and inhibitor group to corresponding interventions under different conditions. The migration ability, invasion ability, apoptosis rate, expression levels of intracellular related proteins, and secretion levels of pro-angiogenic factors were evaluated in each group. These results suggest that although the 10% BSCL-medicated serum could not regulate KGN through the Ang1/Tie2 pathway, it target and regulate the CXCR4/HIF-1α signaling pathway, enhance migration and invasion, significantly reduce early and total apoptosis rates, enhance the viability of granulosa cells within the follicle and promoting the high-level secretion of angiogenesis-inducing signaling factors such as CD34, VEGFA, EPO, and Ang2, to achieve the purpose of improving early-onset ovarian insufficiency caused by impaired ovarian angiogenesis.

This study aims to establish a model for rapid non-destructive quantitation of main phenolic acids in Salviae Miltiorrhizae Radix et Rhizoma by hyperspectral imaging combined with chemometric methods. Hyperspectral imaging was performed for 420 Salviae Miltiorrhizae Radix et Rhizoma samples collected from Shandong, Hebei, Shanxi, Sichuan, and Anhui. Original spectral data(ORI) were preprocessed by first derivative(D1), second derivative(D2), savitzky-golay(SG) smoothing, multiplicative scattering correction(MSC), and standard normal variate(SNV) algorithms. Models for predicting the content of salvianolic acid B, lithospermic acid, danshensu, salvianolic acid Y, and rosmarinic acid were constructed via partial least squares regression(PLSR), backpropagation neural network(BPNN), and random forest regression(RFR). Additionally, iterative retained information variable(IRIV), successive projections algorithm(SPA), uninformative variables elimination(UVE), and variable iterative space shrinkage approach(VISSA) were employed for feature extraction to refine model efficiency. The results demonstrated that the PLSR model exhibited the best predictive performance. Significant differences in the number of wavelengths selected by different feature extraction methods directly impacted model performance. Therefore, preprocessing methods should be combined adaptively with appropriate feature extraction techniques to enhance model robustness. The optimal models for each component were as follows. VISSA-D1-PLSR models were selected for predicting salvianolic acid B, lithospermic acid, and salvianolic acid Y, with prediction set coefficient of determination(R_p~2) values of 0.942, 0.818, and 0.797 and residual predictive deviation(RPD) values of 4.158, 2.308, and 2.186, respectively. For danshensu and rosmarinic acid, the full-spectrum SG-PLSR models demonstrated the best performance, with R_p~2 values of 0.803 and 0.702 and RPD values of 2.162 and 1.782, respectively. This study demonstrates that HSI technology combined with chemometric methods can provide reliable technical support for predicting multiple phenolic acids in Salviae Miltiorrhizae Radix et Rhizoma and the real-time rapid evaluation of this medicinal material.

This study explored the changes in color and odor of Raphani Semen at different processing stages using intelligent sensory technologies, such as colorimeters and electronic noses, to establish a model for discriminating "processing degree". The total chromaticity value(E~*ab)、 lightness(L~*)、 redness-greenness value(a~*)、 yellowness-blueness value(b~*) and odor profiles of both raw Raphani Semen and its processed products were collected and objectively characterized using colorimeters and electronic noses. Discriminant models were constructed using methods like partial least squares discriminant analysis(PLS-DA), rank correlation analysis, and linear discriminant analysis(LDA) to rapidly differentiate raw Raphani Semen and products processed at varying degrees. The results showed that as the degree of processing increased, the overall color of Raphani Semen darkened, with an increase in redness and a decrease in yellowness, while the E~*ab, L~*, and b~* values decreased. Among the different processing degrees, Raphani Semen showed the strongest response to nitrogen oxides, followed by sulfides, aromatic compounds, and organic sulfides. Nitrogen oxides were identified as the primary differential volatile component distinguishing Raphani Semen processed at different levels. The "processing degree" discriminant model, based on color parameters(L~*, a~*, b~*), and odor parameters, achieved a correct classification rate of 97.5% and 80.0%, respectively. This study provides a reference for the standardization of the frying process for Raphani Semen and offers a new approach for discriminating the "degree of processing" in other medicinal herb slices.