[A new phloroglucinol compound from Dryopteris fragrans].

Two phloroglucinol compounds(1-2) were isolated and purified from 95% ethanol extract of Dryopteris fragrans through various column chromatographies on silica gel, Sephadex LH-20, medium pressure column chromatography, and preparative HPLC. Their structures were elucidated as 2',4',6'-trihydroxy-5'-methyl acetate-3'-methyl-1'-butyrophenone(1) and aspidinol B(2) based on their chemical and physicochemical methods and spectroscopic data. Compound 1 is a new phloroglucinol compound named "dryofraginol".

Integrative analysis of epigenomics, transcriptomics, and proteomics to identify key targets and pathways of Weining granule for gastric cancer.

ETHNOPHARMACOLOGICAL RELEVANCE: Weining granule (WNG) is a "Qi-Enriching and Kidney-Tonifying, Spleen-Reinforcing and Stasis-Removing" formula for gastric cancer (GC). Past research we noted WNG inhibited cell growth and raised apoptosis in GC. However, the underlying mechanism of WNG for GC have yet to be systematically clarified. AIM OF THE STUDY: We sought to characterize the molecular landscape of GC cells in vitro after WNG treated, to identify the molecular targets and pathways that were associated with WNG for inducing the apoptosis of GC cells, and further to clarify underlying molecular mechanism of WNG for GC. MATERIALS AND METHODS: We performed the techniques of RNA sequencing, tandem mass tags (TMT) based quantitative proteomics, and reduced representation bisulfite sequencing (RRBS) in WNG-treated/or untreated SGC-7901 GC cells to gain a comprehensive molecular portrait of WNG treatment. Then we integrated methylomics, transcriptomics, and proteomics data to carry out the bioinformatics analysis, and constructed the protein-protein interaction (PPI) network to identify molecular targets, and to discover the underlying signaling pathways associated with WNG for GC by network analysis. Besides, we verified the candidate target genes by Kaplan-Meier plotter database. RESULTS: We identified 1249 significant differentially expressed genes (DEGs) from RNA expression datasets, 191 significant differentially abunabundant proteins (DAPs) from proteomics datasets, and 8293 significant differentially methylated regions (DMRs) from DNA methylation datasets. GO and KEGG analysis showed DEGs, DAPs, and DMRs enriched in the cancer-related biological processes of calcium signaling pathway, pathways in cancer, metabolic pathways, MAPK signaling pathway, PI3K-Akt signaling pathway, and transcriptional misregulation in cancer. We integrated three profile datasets and performed network analysis to distinguish the hub genes, and finally the genes of SOD2, HMOX1, MMP1, SRXN1, NOTCH1, MAPK14, TXNIP, VEGFA, POLR2F, and HSPA9 were identified. The Kaplan-Meier plotter confirmed that SOD2, MMP1, SRXN1, NOTCH1, MAPK14, TXNIP, VEGFA, and HSPA9 were significantly correlated with OS in GC patients (P < 0.01), while HMOX1 and POLR2F expression were not significantly relevant to survival of GC patients (P > 0.01). CONCLUSIONS: SOD2, MMP1, SRXN1, NOTCH1, MAPK14, TXNIP, VEGFA, and HSPA9 were the predictive pharmaceutical targets of WNG for GC. The anticancer function of WNG was significantly associated with the pathways of focal adhesion pathway, PI3K-Akt signaling pathway, MAPK signaling pathway, and Wnt signaling pathway.

A new phloroglucinol compound from Dryopteris fragrans / 中国中药杂志

Two phloroglucinol compounds(1-2) were isolated and purified from 95% ethanol extract of Dryopteris fragrans through various column chromatographies on silica gel, Sephadex LH-20, medium pressure column chromatography, and preparative HPLC. Their structures were elucidated as 2',4',6'-trihydroxy-5'-methyl acetate-3'-methyl-1'-butyrophenone(1) and aspidinol B(2) based on their chemical and physicochemical methods and spectroscopic data. Compound 1 is a new phloroglucinol compound named "dryofraginol".

Phenolic constituents from Rheum nobile and their antioxidant activity.

Although the rhizomes of Rheum nobile Hook. f. et Thoms (Polygonaceae) are widely used in Tibetan medicine, no previous investigations regarding the biological activities and rarely chemical constituents of this plant have been reported. As part of an ongoing search for novel bioactive agents, a phytochemical investigation of R. nobile led to the isolation of two new compounds Rheumone B (1) and piceatannol-4'-O-ß-D-(6″-O-acetyl)-glucoside (2), together with 15 known compounds by gel filtration over Sephadex LH-20 and preparative HPLC. Their structures were determined by combined spectroscopic methods. Compounds 1-10 were evaluated for their ability to scavenge 2,2-diphenyl-1-picrylhydzyl (DPPH) radical and compounds 7-10 showed relatively strong scavenging abilities with IC50 values from 2.76 µM to 11.80 µM. In conclusion, naphthalene glycosides, stilbene glycosides, flavanols, especially anthraquinones are main chemical constituents of this plant. The ability to scavenge DPPH radical of compound 8 was the highest among compounds 1-10.

Preparation and physicochemical characterization of T-OA PLGA microspheres.

As the carrier of water-insoluble drugs, microspheres can play a role in increasing solubility and delaying releasing essence. The objective of this study was to improve the solubility and to delay the release of a newly discovered antitumor compound 3ß-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester (T-OA). Early-stage preparation discovery concept (EPDC) was employed in the present study. The preparation, physicochemical characterization, and drug release properties of PLGA microspheres were evaluated. T-OA-loaded PLGA microspheres were prepared by an oil-in-water (O/W) emulsification solvent evaporation method. Characterization and release behaviors of the T-OA PLGA microspheres were evaluated by X-ray diffract (XRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and high performance liquid chromatography (HPLC). The results demonstrated that T-OA-loaded PLGA microspheres could be successfully obtained through solvent evaporation method with appropriate morphologic characteristics and high encapsulation efficiency. The XRD analysis showed that T-OA would be either molecularly dispersed in the polymer or distributed in an amorphous form. The DSC and FTIR analysis proved that there were interactions between T-OA and PLGA polymer. SEM observations displayed the morphology of the microspheres was homogeneous and the majority of the spheres ranged between 50 and 150 µm. The drug release behavior of the microspheres in the phosphate buffered saline medium exhibited a sustained release and the duration of the release lasted for more than 23 days, which was fit with zero-order release pattern with r2 = 0.9947. In conclusion, TOA-loaded PLGA microspheres might hold great promise for using as a drug-delivery system in biomedical applications.

Two new glycosides from Dryopteris fragrans with anti-inflammatory activities.

Phytochemical investigation on the aqueous extract from Dryopteris fragrans led to the isolation of one new chromone glycoside, frachromone C (1), and one new coumarin glycoside, dryofracoulin A (2), together with one known undulatoside A (3). Their structures were elucidated by a combination of 1D and 2D NMR, HRMS, and chemical analysis. Compounds 1-3 exhibited inhibition on nitric oxide production in lipopolysaccharide induced RAW 264.7 macrophages with their IC50 values of 45.8, 65.8, and 49.8 µM, respectively.

[UPLC/Q-TOF MS and NMR plant metabolomics approach in studying the effect of growth year on the quality of Polygala tenuifolia].

Growth year is one of the important factors for the quality of Polygala tenufolia. In this study, primary metabolites and secondary metabolites were compared in 1, 2 and 3 years old P. tenufolia cultivated in Shaanxi Heyang. The samples were subjected to ultra-high performance liquid chromatography (UPLC)-quadrupole time-of-flight mass spectrometry (Q-TOF MS) and nuclear magnetic resonance (NMR) analysis, and the obtained data were analyzed using principal component analysis (PCA) and other statistical analysis methods. In addition, content and correlation of different metabolites were also calculated. The results showed no significance between main component contents in 2 year-old and 3 year-old P. Tenufolia, but 1 year-old was statistically different. The contents of primary metabolites, such as fructose, sucrose, and choline increased as time goes on, while glycine and raffinose decreased. The contents of secondary metabolites, such as onjisaponin Fg, polygalasaponin XXVIII, polygalasaponin XXXII increased, while polygalaxanthone III and parts of oligosaccharide multi-ester including tenuifoliose A, tenuifoliose C, tenuifoliose C2 and tenuifoliose H decreased with the extension of the growth years. Growth years has important impact on the quality of P. tenuifolia and the existing growing years of commodity P. tenuifolia have its scientific evidence. This study supplied a new method for the quality evaluation of Chinese medicinal materials.

[UPLC/Q-TOF MS-Based Metabolomics Analysis of Chemical uiterences in Different Polygala tenuifolia Varieties].

OBJECTIVE: The chemical differences of Polygala tenuifolia varieties-JinYuan 1 (JY1), FenYuan 2 (FY2) and traditional FenYang (FY) were studied, in order to provide reference for the breeding of Polygala tenuifolia. METHODS: The samples of JY1, FY2 and FY were subjected to ultra-high performance liquid chromatography (UPLC) quadrupole time-of-flight mass spectrometry (Q-TOF MS) analysis. The obtained data were analyzed using Principal Component Analysis (PCA) and other statistical analysis methods, and differential metabolites were further figured out. RESULTS: Compared with FY,sucrose esters (such as sibiricoses A5 and tenuifoliside B) and oligosaccharides (such as tenuifoliose K) in JY1 and FY2 contributed more to the separation of Polygala tenuifolia varieties in the PCA score plot. Compared with JYl, The sugar esters (such as tenuifoliside B and tenuifoliside A) and oligosaccharides( such as tenuifoliose A) in the FY2 also contributed more to the separation of Polygala tenuifolia varieties in the PCA score plot. In addition, the relative contents of sibiricaxanthone A,3,6'-disinapoly sucrose and senegin III showed significant differences among FY, JY1 and FY2. CONCLUSION: As new Polygala tenuifolia varieties, JY1 and FY2 had certain differences and respective advantages on the chemical composition compared with FY,which could provide data support for the directional breeding of Polygala tenuifolia based on the contents of some active compounds.

UPLC/Q-TOF MS and NMR plant metabolomics approach in studying the effect of growth year on the quality of Polygala tenuifolia / 药学学报

Growth year is one of the important factors for the quality of Polygala tenufolia. In this study, primary metabolites and secondary metabolites were compared in 1, 2 and 3 years old P. tenufolia cultivated in Shaanxi Heyang. The samples were subjected to ultra-high performance liquid chromatography (UPLC)-quadrupole time-of-flight mass spectrometry (Q-TOF MS) and nuclear magnetic resonance (NMR) analysis, and the obtained data were analyzed using principal component analysis (PCA) and other statistical analysis methods. In addition, content and correlation of different metabolites were also calculated. The results showed no significance between main component contents in 2 year-old and 3 year-old P. Tenufolia, but 1 year-old was statistically different. The contents of primary metabolites, such as fructose, sucrose, and choline increased as time goes on, while glycine and raffinose decreased. The contents of secondary metabolites, such as onjisaponin Fg, polygalasaponin XXVIII, polygalasaponin XXXII increased, while polygalaxanthone III and parts of oligosaccharide multi-ester including tenuifoliose A, tenuifoliose C, tenuifoliose C2 and tenuifoliose H decreased with the extension of the growth years. Growth years has important impact on the quality of P. tenuifolia and the existing growing years of commodity P. tenuifolia have its scientific evidence. This study supplied a new method for the quality evaluation of Chinese medicinal materials.

[New processing procedure for Croton tiglium with study on comparison of Croton tiglium and processed product].

OBJECTIVE: To build a new processing procedure for Croton tiglium, providing a more simple, efficient and safe way of processing. METHODS: Used the contents of isoguanosine and toxic protein in Croton tiglium as the indexes to investigate the effect of different temperature, thickness and baked time on processing for Croton tiglium. After established all factors and levels, processed a batch of Croton tiglium under optimum processing conditions and compared it with raw Croton tiglium in the test of acute toxicity and gastrointestinal propulsive motility. RESULTS: The parameters of optimum processing were as follows:the temperature was set at 180 degrees C, the thickness of placement was 3 cm and baked time was 90 min. The LD50 value of raw Croton tiglium and the processed Croton tiglium was 888 mg/kg and 2139 mg/kg respectively. CONCLUSION: The processing procedure is simple, affordable, safe and efficient, deserved to promote for application.

Protective effect of Acanthopanax gracilistylus-extracted Acankoreanogenin A on mice with fulminant hepatitis.

The release of pro-inflammatory cytokines in both acute (IL-1ß and TNF-α) and chronic [high mobility group box 1 protein (HMGB1)] phases, is thought to play important roles in the development of fulminant hepatitis (FH). Triterpenoid Acankoreanogenin A (AA) which is extracted from the leaves of the Acanthopanax gracilistylus W.W. Smith (AGS) has shown its inhibiting effect on TNF-α, IL-1ß and HMGB1 release in vitro in our preliminary experiments. In present study, we investigated the effect of AA on mice with fulminant hepatitis in vivo. Fulminant hepatitis mice model was established by intraperitoneally injecting galactosamine (GalN) and lipopolysaccharide (LPS). The levels of serum of TNF-α, IL-1ß, ALT, AST and HMGB1 from AA-treated mice were measured at different time points. Our results demonstrated that pre-treatment of mice with AA markedly reduced the serum levels of TNF-α, IL-1ß, HMGB1, ALT and AST with the improvement in histological features. And the survival rate from AA-treated fulminant hepatitis mice was increased. Furthermore, delayed administration of AA after peak occurrence of the early pro-inflammatory cytokines still endowed significant protection against GalN/LPS-induced lethality. The post-treatment of AA could significantly attenuate the release of HMGB1, but not the TNF-α and IL-1ß. These results indicate that AA inhibits the systemic release of pro-inflammatory cytokine HMGB1, and dose-dependently rescue the mice from lethal GalN/LPS-induced fulminant hepatitis, which suggests this component as a candidate therapy for fulminant hepatitis.

[A technique for investigating the component of cantharidin blisters by flow cytometry].

OBJECTIVE: Cantharidimide cause blister. The effect of blister on immunoregulation was investigated. METHODS: Cantharidimide was placed on the skin, 48h later, the blister was analyzed by flow cytometry. RESULTS: The blister contained 1 x 10(6) - 1 x 10(7) cells per ml, most of which were neutrophils, macrophages, dendritic cells (DC), and IL-12 secreted by Thl cells. CONCLUSION: There are high concent of DC in the blister, which is differential and induce the secretion of Th1, the activation of T cell. The blister modulate the biological response of patients and is helpful for treatment with infective disease.