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1.
Article in Chinese | WPRIM | ID: wpr-928138

ABSTRACT

Quality evaluation of Chinese medicinal decoction pieces is vital for the development of the downstream industries, and is an important channel for implementing the strategy of "higher quality, higher price, and priority for the high quality" for traditional Chinese medicine. At the moment, the quality of Chinese medicinal decoction pieces is mainly evaluated based on chemical component examination. Considering the weak preliminary research foundation and poor research conditions, traditional experience-based evaluation is undervalued in the quality rating of Chinese medicinal decoction pieces. However, traditional experience is a summary of the quality of Chinese medicinal materials based on clinical experience, which thus can be a potential basis for the quality evaluation of the decoction pieces. It is a challenge in the evaluation of Chinese medicinal decoction pieces to objectify the traditional experience-based evaluation from multiple aspects such as chemistry, effect, and characterization via modern techniques. Therefore, this study developed the "experience-ingredients-activity-electronic sensing" evaluation system for Chinese medicinal decoction pieces on the basis of experience-based assessment, chemical ingredients that can truly reflect the traditional experience, biological effect assessment, and electronic sensory evaluation, which is expected to quantify the traditional experience of quality evaluation of Chinese medicinal decoction pieces via chemistry, biology, and sensory simulation. The evaluation system can serve as a reference for clinical experience-based quality evaluation of Chinese medicinal decoction pieces.


Subject(s)
China , Drugs, Chinese Herbal , Electronics , Medicine, Chinese Traditional , Restraint, Physical
2.
Article in Chinese | WPRIM | ID: wpr-905868

ABSTRACT

Objective:To explore effects of different extracts and monomers of <italic>Lepidium meyenii </italic>(Maca) on the proliferation of mouse splenic lymphocytes and induction of interleukin-2 (IL-2) and tumor necrosis factor-<italic>α</italic> (TNF-<italic>α</italic>) by observing their immunomodulatory effects. Method:An octadecylsilyl (ODS) column was used to enrich the methanol extract of <italic>L. meyenii</italic> in stages to obtain six fractions and three monomers. Different groups of extracts and monomers of <italic>L. meyenii </italic>at different doses were set up. Cell counting Kit-8 (CCK-8) was used to detect the effect on the proliferation of mitogen-free, concanavalin A (Con A)-induced, and lipopolysaccharides (LPS)-induced mouse splenic lymphocytes. Enzyme-linked immunosorbent assay (ELISA) was used to determine the levels of IL-2 and TNF-<italic>α</italic>. Result:<italic>L. meyenii </italic>extracts Fr<sub>3</sub> and Fr<sub>6</sub>, and monomers <italic>N</italic>-benzyl hexadecanamide and 1,2-dihydro-4-carboxaldehyde-3-benzyl-<italic>N</italic>-hydroxypyridine slightly promoted the proliferation of Con A-induced T lymphocytes and LPS-induced B lymphocytes (<italic>P</italic><0.01) as compared with the conditions in the model group. <italic>L. meyenii</italic> extracts and monomers significantly induced the secretion of IL-2 and TNF-<italic>α</italic> by splenic lymphocytes (<italic>P</italic><0.01). Conclusion:<italic>L. meyenii</italic> extracts and monomers can achieve immunological enhancement by promoting the secretion of IL-2 and TNF-<italic>α</italic>, and facilitate the proliferation of splenic lymphocytes. The active components are presumedly macamides and pyridine alkaloids, and the specific mechanism still needs to be further explored.

3.
Article in Chinese | WPRIM | ID: wpr-888184

ABSTRACT

Indolealkylamines(IAAs) are the main hydrophilic substances in toad skin, mainly including free N-methyl-5-hydroxytryptamine, bufotenine, bufotenidine, dehydrobufotenine, and binding bufothionine. In this study, the LPS-activated neutrophils were used to investigate the structure-activity relationship and anti-inflammatory mechanism of the above-mentioned five monomers from the toad skin in vitro. The neutrophils were divided into the control group, model group(1 μg·mL~(-1) LPS), positive drug group(100 μg·mL~(-1) indometacin), as well as the low-(50 μg·mL~(-1)), medium-(100 μg·mL~(-1)) and high-dose(200 μg·mL~(-1)) free N-methyl-5-hydroxytryptamine, bufotenine, bufotenidine, dehydrobufotenine, and binding bufothionine groups. The levels of IL-6, TNF-α and IL-1β in the neutrophil supernatant of each group was measured by enzyme-linked immunosorbent assay(ELISA) after LPS stimulation, followed by the detection of apoptosis in each group after Annexin V/PI staining. The protein expression levels of caspase-3, Bax, Bcl-2, beclin1, LC3-I, and LC3-Ⅱ were assayed by Western blot. The results showed that IAAs reduced the excessive secretion of inflammatory cytokines caused by LPS compared with the model group. Besides, the activity of each free IAAs(N-methyl-5-hydroxytryptamine, bufotenine, bufotenidine and dehydrobufotenine), especially bufotenine, was stronger than that of the binding bufothionine. As revealed by Annexin V/PI staining, LPS delayed the early apoptosis of neutrophils compared with the control group, while bufotenine promoted the apoptosis of neutrophils in a dose-dependent manner, which might be related to the elevated expression of apoptosis-related protein Bax/Bcl-2. In addition, LPS activated the autophagy pathways in neutrophils. This study confirmed the efficacy of IAAs in reducing the secretion of inflammatory cytokines in neutrophils induced by LPS for the first time. For instance, bufotenine exerts the anti-inflammatory effect possibly by inducing the apoptosis of neutrophils.


Subject(s)
Animals , Anti-Inflammatory Agents/pharmacology , Apoptosis , Bufonidae , Lipopolysaccharides/toxicity , Neutrophils , Skin
4.
Article in Chinese | WPRIM | ID: wpr-771503

ABSTRACT

In order to find the endogenous potential biomarkers of in vitro hepatic injury caused by NCTD-Na and elucidate the mechanism of hepatic injury of NCTD-Na,ultra-high performance liquid chromatography coupled quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS/MS) was used for lipidomics detection.Multivariate statistical analysis was used to study the endogenous lipid metabolic changes of human normal liver cells LO2 injury after the treatment with sodium norcantharidate(NCTD-Na).The results showed that the half maximal inhibitory concentration(IC50) of NCTD-Na was 0.034 mmol·L-1.A total of 280 differential metabolites were found between the control group and the low-dose group,with VIP > 2.0 and P 2.0 and P 2.0,P<0.05,RSD<30% and in a dose-dependent manner.It was found that most of the above differential metabolites were lipid metabolites after the analysis of simple preparnation methods and database search.A total of 32 potential biomarkers were identified,including 3 phosphatidylcholine(PC),5 lysophosphatidylcholine(Lyso PC),3 ceramide(Cer),1 sphingomyelin(SM),1 phosphatidylethanolamine(PE),10 lysophosphatidylethanolamine(LysoPE),4 diacylglycerol(DG),1 Phosphatidic acid(PA),1 lysophosphatidic acid(Lyso PA),1 phosphatidyl glycerol(PG),1 fatty acid hydroxy fatty acid(FAHFA) and 1 phosphatidylserine(PS).The changes of PCs,Cers,SM,PE and DGs were closely related liver protection,DNA methylation and self-repair in hepatocytes,apoptosis,methylation and detoxification of carcinogens,as well as lipid peroxides production process.Also,they had impact on the proliferation of hepatocytes,differentiation and gene transcription disorders.Cells stimulated by NCTD-Na could promote the production of PA as well as the synthesis and catabolism of FAHFA in a variety of ways.The levels of Lyso PCs,LysoPEs and Lyso PA were correlated with PCs,PE and PA;PE and PS might have valgus during apoptosis,triggering phagocytosis.


Subject(s)
Bridged Bicyclo Compounds, Heterocyclic , Pharmacology , Cells, Cultured , Hepatocytes , Metabolism , Humans , Lipid Metabolism , Lipids , Tandem Mass Spectrometry
5.
Article in Chinese | WPRIM | ID: wpr-307088

ABSTRACT

Fifteen compounds were isolated from the toad skin by a combination of various chromatographic methods including macroporous resin, silica gel, ODS and semi-preparative HPLC. Their structures were identified as 4,5-dimethyl-1,3,4,5-tetrahydropyrrolo[4,3,2-de]quinolin-6-ol(1), serotonin(2), N-methyl serotonin(3), O-methyl bufotenine(4), 1,2,3,4-tetrahydro-6-hydroxy-β-carboline(5), O-methylserotonin(6), glycinebetaine(7), caffeine(8), bufotenine(9), shepherdine(10), tryptophan(11), (5-hydroxy-1H-indol-3-yl)acetic acid(12), 5-hydroxy tryptophol(13), 2-methyl-6-hydroxy-1,2,3,4-tetrahydro-β-carboline(14), bufothionine(15). Among them, compound 1 was a new compound,compound 5 was a new natural product. Compounds 4-8 and 10-14 were separated from toad skin for the first time.

6.
Acta Pharmaceutica Sinica ; (12): 1159-1163, 2012.
Article in Chinese | WPRIM | ID: wpr-274683

ABSTRACT

Influenza virus RNA-dependent RNA polymerase (RdRP) is essential for replication and expression of influenza virus genome. Viral genomic sequences encoding RdRP are highly conservative, thus making it a potential anti-influenza drug target. A cell-based influenza RdRP inhibitor screening assay was established by a luciferase reporter system to analyze the activity of RdRP. Specificity study and statistic analysis showed that the screening assay is sensitive and reproducible.


Subject(s)
Amantadine , Pharmacology , Antiviral Agents , Pharmacology , Drug Evaluation, Preclinical , Methods , Genes, Reporter , HEK293 Cells , Humans , Influenzavirus A , Luciferases , Genetics , Metabolism , Oseltamivir , Pharmacology , Plasmids , RNA-Dependent RNA Polymerase , Metabolism , Reproducibility of Results , Ribavirin , Pharmacology , Sensitivity and Specificity , Transfection , Zanamivir , Pharmacology
7.
Article in English | WPRIM | ID: wpr-341429

ABSTRACT

<p><b>OBJECTIVE</b>To explore the feasibility and efficiency of extracting protein from bone tissue using trichloroacetic acid (TCA)-acetone precipitation method.</p><p><b>METHODS</b>Hydrochloric acid (HCL) decalcification method and TCA-acetone precipitation method were separately used for bone protein extraction. The efficiencies of these two methods were compared.</p><p><b>RESULTS</b>TCA-acetone precipitation method had significantly higher extraction efficiency. Compared with HCL decalcification method, it had less pollution from bone marrow hematopoietic tissue. Protein band distribution was similar between these two methods.</p><p><b>CONCLUSION</b>TCA-acetone precipitation method is useful for bone proteomics research.</p>


Subject(s)
Acetone , Animals , Bone and Bones , Chemistry , Chemical Precipitation , Male , Proteins , Proteomics , Methods , Rats , Rats, Wistar , Trichloroacetic Acid
8.
Acta Pharmaceutica Sinica ; (12): 247-252, 2010.
Article in Chinese | WPRIM | ID: wpr-250635

ABSTRACT

Strict regulation of HIV-1 PR function is critical for efficient production of mature viral particles. During viral protein expression and viral assembly, HIV-1 PR located within Gag-Pol precursor must be inactive to prevent premature cytoplasmic processing of the viral Gag and Gag-Pol precursors. Premature activation of HIV-1 precursors leads to major defects in viral assembly and production of viral particles. A cell-level premature activation of HIV-1 precursors assay using bioluminescence resonance energy transfer (BRET) was established. Three thousand compounds were screened to evaluate this assay. The results showed that the assay is sensitive, specific and stable (Z' factor is 0.905).


Subject(s)
Anti-HIV Agents , Pharmacology , Benzoxazines , Pharmacology , Bioluminescence Resonance Energy Transfer Techniques , Methods , Fusion Proteins, gag-pol , Genetics , Metabolism , HEK293 Cells , HIV Protease , Metabolism , Physiology , HIV-1 , High-Throughput Screening Assays , Methods , Humans , Plasmids , Genetics , Protein Precursors , Metabolism , Physiology , Pyridazines , Pharmacology , Transfection , Virion , Virus Assembly , gag Gene Products, Human Immunodeficiency Virus , Genetics , Metabolism
9.
Acta Pharmaceutica Sinica ; (12): 257-262, 2010.
Article in Chinese | WPRIM | ID: wpr-250633

ABSTRACT

The HIV-1 Rev protein facilitates nuclear export of unspliced and singly spliced viral transcripts containing RRE RNA through the CRM1 export pathway. Inhibition of Rev-mediated RNA nuclear export can arrest HIV-1 transcriptional process, which clearly, reveals a target for anti-HIV drug development. In this work, a cell-based assay has been established for screening anti-HIV compounds targeting the Rev-mediated RNA nuclear export. This assay utilized a codon-optimized green fluorescent protein (GFP) as reporter gene, which expression is in a Rev-dependent manner. Any compound that inhibits the Rev-mediated RNA nuclear export is identified by reducing emission of GFP. The Z' score of this model is 0.8220. Three thousands compounds were screened and the positive rate was 9.3% with a cutoff at 50% inhibition. IMB7C7, one of the positive compounds, efficiently inhibits viral production from HIV-1 infected cells.


Subject(s)
Active Transport, Cell Nucleus , Anti-HIV Agents , Pharmacology , Cell Nucleus , Metabolism , Codon , Fatty Acids, Unsaturated , Pharmacology , Genes, Reporter , Green Fluorescent Proteins , Genetics , Metabolism , HEK293 Cells , HIV-1 , Genetics , High-Throughput Screening Assays , Humans , Karyopherins , Genetics , Metabolism , RNA, Viral , Receptors, Cytoplasmic and Nuclear , Genetics , Metabolism , Transfection , Virus Replication , rev Gene Products, Human Immunodeficiency Virus , Genetics , Metabolism
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