Latest ArticlesThe objective of this study was to examine the antimetastatic effects of cordycepin and elucidate its molecular mechanism using MHCC97H cells in vitro and in vivo. Cellular proliferation was detected with MTT assay. The migration and metastatic potential were measured with scratch wound healing as well as transwell migration assays in vitro. Protein expression was detected by Western blotting. Antitumor and antimetastatic effects of cordycepin were evaluated by subcutaneous xenograft and lung metastatic model in vivo. The results demonstrated that cordycepin significantly inhibited MHCC97H cells proliferation and metastasis which was due to the down-regulation of AKT, p-AKT, p-GSK-3β, β-catenin, N-cadherin, MMP-7, MMP-9 and up-regulation the expression of E-cadherin. Furthermore, cordycepin inhibited tumor growth and metastasis in a dose-dependent manner in vivo. Cordycepin(40 and 20 mg·kg-1)and 5-fluorouracil group significantly inhibited the tumor weights to 0.38 ± 0.04, 0.61 ± 0.08 and 0.65 ± 0.07 g, respectively, comparing with the control group(1.52 ± 0.46 g)(P < 0.01), but not 10 mg·kg-1 cordycepin group(1.13 ± 0.36 g)(P > 0.05); the lung metastasis nodus numbers showed the same results, which in all group above(48.9 ± 7.2, 67.2 ± 9.4, 73.6 ± 8.6, respectively)were fewer than the control group(123.5 ± 14.5)(P < 0.01), except 10 mg·kg-1 cordycepin(106.4 ± 11.3)(P > 0.05). Collectively, cordycepin inhibited MHCC97H cell proliferation and metastasis in vivo and in vitro.
This study was designed to investigate the effect of 2, 3, 5, 4'-tetrahydroxystilbene-2-O-β-D-glycoside(TSG)on hypoxia/reoxygenation(H/R)-induced oxidative stress injury and its potential mechanism in human bronchial epithelial cell(BEAS-2B)cells. BEAS-2B cells were exposed to H/R treatment. Level of intracellular ROS was detected using DCFH-DA probe and fluorescence microplate reader. Production of MDA and activity of SOD were evaluated with MDA and SOD kits. Nucleus was shaped by DAPI staining. Translocation of Bax to mitochondria was observed in MCF-7/GFP-Bax cells. Change in mitochondrial membrane potential was detected by JC-1 staining. Release of cytochrome C from mitochondria was detected by immunofluorescence. Expressions of mitochondrial/cytoplasmic Bax and cytochrome C, caspase-9, caspase-3, phosphorylated MAPK, HIF-1α and phosphorylated p53(p-p53) were determined by Western blotting. TSG significantly improved cell viability and reduced H/R-induced ROS production in BEAS-2B cells, while significantly decreased MDA production. It inhibited Bax translocation and nucleus fracture, reversed the decrease in mitochondrial membrane potential and inhibited the release of cytochrome C and following activation of caspase-9/caspase-3. Simultaneously, TSG down-regulated the signals of SAPK JNK1/2 and p38 MAPK without an impact in ERK1/2. It attenuated expression of HIF-1α and phosphorylation of p53. This study suggests that TSG could protect BEAS-2B against H/R-induced apoptosis, perhaps through the MAPK, HIF-1α and p53 pathways.
A series of novel xanthones with terminal amine substituents at xanthone's C3 and C6 positions were designed and synthesized as potential ligands for telomeric G-quadruplex DNA. All the compounds in this series were bound to telomeric G-quadruplex in a "thread intercalation" manner that illustrated both in molecular docking and spectrometric studies. Among them, 10c and 10d showed better binding abilities and specific affinity toward G-quadruplex DNA HTG21 over ctDNA in the fluorescence assay. The antiproliferative activities of four screened compounds were examined in three cancer cells by MTT in vitro, and their inhibitory effects were observed at low micromolar ranges. In addition, the PCR stop assay demonstrated that 10c and 10d effectively inhibited the amplification ability of telomerase.
In this study, eleven containing gallic acid moiety derivatives of Matijin-Su(MTS)were synthesized and evaluated for their anti-HBV activities in HepG2 2.2.15 cells in an effort to find novel effective anti-hepatitis B virus(HBV)agents. Compounds 5c, 6c and 6d exhibited significant anti-HBV activity with IC50 values of 6.12, 8.44 and 9.86 μmol·L-1, respectively. Incorporation of gallic acid moiety into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.
To study the chemical constituents of the fruits of Fructus carotae, silica gel column chromatography and preparative HPLC were used to isolate and purify the extract of Fructus carotae. The structures of obtained compounds were elucidated on the basis of physicochemical property and spectral data. Nine guaiane-type sesquiterpenes were isolated and identified as 8β-angeloyloxy-11-hydroxy-4-guaien-3-one(1), 11-acetoxy-4-guaien-3-one(2), 11-acetoxy-8β-isobutyryl-4-guaien-3-one(3), 11-acetoxy-8β-propionyl-4-guaien-3-one(4), 11-hydroxy-4-guaien-3-one(5), 11-acetoxy-8β-angeloyloxy-1β-hydroxy-4-guaien-3-one(6), 11-acetoxy-8β-angeloyloxy-4-guaien-3-one(7), 11-acetoxy-8β-hydroxy-4-guaien-3-one(8)and 8β, 11-dihydroxy-4-guaien-3-one(9). Compound 1 is a new compound, compound 5 is a new natural product, and compounds 2-4 were isolated from this genus for the first time.
Panax quinquefolium and Panax ginseng were investigated using non-linear chemical fingerprint technology, and a novel method to identify two ginsengs and different producing areas of P. quinquefolium was put forward. The non-linear chemical fingerprints of P. quinquefolium(collected from Canada, Jilin and Shaanxi)and P. ginseng (collected from Jilin)were obtained by reactions took place in the system of "H2SO4-MnSO4-CH3COCH3-NaBrO3" and their system similarities were evaluated. In the meantime, the quality difference in P. quinquefolium from different producing areas was evaluated using HPLC to determine the contents of main 7 ginsenosides. As a result, the non-linear chemical fingerprints exhibited a good reproducibility and characteristic when dosage of detection was 0.4 g and the reaction temperature was 37 ℃. The fingerprint characteristics of P. quinquefolium were obviously different from P. ginseng. The two species of ginsengs could be distinguished by the visual fingerprint characteristics, and P. quinquefolium from different producing areas were identified by the system similarities. Furthermore, HPLC analysis showed that the quality P. quinquefolium from different producing areas was varied, which indicated that rapid identification and quality evaluation of P. quinquefolium become very important and necessary. Compared with HPLC technology, non-linear chemical fingerprint is a more convenient, rapid and economic technology. This study provides a novel strategy to distinguish and evaluate P. quinquefolium and P. ginseng, which will provide a reference for the quality evaluation and control of Chinese medicine.
An ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UHPLC-Q-TOF/MS)method has been established to analyze the bioactive components of the aqueous extract of Euodiae Fructusand detect the metabolites in rats after oral administration of the aqueous extract. Compounds were detected by analyzing their retention times, high resolution mass data, mass spectra and comparing with the reference substances. As a result, 27 compounds were characterized from the aqueous extract of Euodiae Fructus, and 25 compounds were identified on the basis of the reference substances. 16 parent compounds and 35 metabolites were detected in rats' plasma, urine and feces samples, and all of the parent compounds were determined unambiguously through comparison with the reference substances. Four classes of compounds were identified from the aqueous extract of Euodiae Fructus, including phenolic acids, limonins, flavonoid glycosides and alkaloids. Phenolic acids, flavonoid glycosides and alkaloids were detected in rats' plasma, urine and feces, while limonins were detected in the urine and feces. The main metabolism pathways of these compounds in rats might include hydroxyl, hydrogenation, methylation, sulfating, glucuronidation, and so on. The results of this study provide references in the material basis of Euodiae Fructus in vivo.
A new type of L. Bulgaricus microcapsule was prepared to improve stability and resistance of L.Bulgaricus probiotics in harsh environments. An optimal method of preparation of L. Bulgaricus microcapsule is as follow. L. Bulgaricus was mixed with 3% alginate solution. The concentration of bacterial suspension was 1×109 cfu·mL-1. The mixture was microencapsulated by extrusion into 2% CaCl2 solution with a dispensing equipment. After 30 min solidification, the gel beads were lyophilized to obtain L.Bulgaricus microcapsules. The microencapsulation technology was aimed to improve the stability and survival rate of L. Bulgaricus. The microcapsule was spherical with uniform particle size and intact structure. The tolerance of acid, high temperature, high humidity and the long-term stability of freeze-dried powder and microcapsule were evaluated. The results indicated that microencapsulation technic could greatly improve stability and resistance of L. Bulgaricus probiotics in harsh environments.
This study was designed to establish the method of characterization of surface free energy(SFE)and evaluate the compaction properties of pharmaceutical materials based on SFE. We investigated the contact angles of materials with water and diiodomethane under different compression pressures. The contact angles of materials at 353 MPa compression pressure were utilized to calculate the related parameters of SFE ultimately. The area under tensile strength-compression pressure curve(AUTSC)and pressure yield(Py)were employed to evaluate the compactibility of material. Additionally, Pearson correlation analysis was utilized to analyze the relationship between the SFE and the compaction properties of pharmaceutical materials. The results exhibited that SFE had a significant correlation with the compaction properties of materials(P < 0.05). Moreover, the related parameters of SFE, i.e., cohesive work(Wco)and polarity index(PI)of SFE, were positively correlated with Py of Heckel equation and negatively related with AUTSC. The higher values of Wco and PI, the stronger repulsive force among the particles, led to a worse compaction behavior. In this study, we established the method for characterization of the compaction behavior of materials based on SFE initially. This study also demonstrated that SFE could evaluate the compaction behavior effectively, which provides a better understanding of compaction behavior for pharmaceutical researchers.
This study aims to synthesize new phospholipids, 1, 3-dipalmaminophospholipid(Pad-PC-Pad), and prepare shear-stress sensitive liposomes(SSSL). 1H NMR and MS indicated that Pad-PC-Pad were fully synthesized successfully. SSSL were prepared by filming-rehydration method with Pad-PC-Pad, which loaded calcein with aggregation-caused quenching(ACQ)characteristics to evaluate shear-stress sensitivity of liposomes and release behavior of liposomes in vitro. The results showed that the particle size of liposomes was 106.91 ± 1.24 nm and liposomes had lenticular morphology under transmission electron microscope. The release of calcein was increased with ultrasonic power, which suggests that the liposomes is shear-stress sensitive. Moreover, the liposomes exhibited a releasing effect for obstructed region under high shear-stress in a model system. Therefore, we synthesized quick functional phospholipid Pad-PC-Pad and the liposomes made from Pad-PC-Pad was shear-stress sensitive, which may be used for treatment of thrombosis.
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