Research progress on T cell glycolytic metabolism in oral lichen planus / 口腔疾病防治

@#Oral lichen planus (OLP) is a chronic inflammatory disease of the oral mucosa. The pathogenesis of OLP is still unclear. Immune abnormalities mediated by T cells and related cytokines play a crucial role in the pathogenesis of OLP. In recent years, glycolytic metabolism-related transporters, enzymes and regulators, such as glucose transporter-1 (Glut1), glyceraldehyde 3-phosphate dehydrogenase (GAPDH), lactate dehydrogenase A (LDHA), mammalian target of rapamycin (mTOR) and hypoxia inducible factor-1α (HIF-1a), have attracted an increasing amount of attention in OLP by regulating the proliferation and differentiation of T cells and the secretion of inflammatory factors. It has been shown that 2-deoxy-D-glucose (2-DG) or rapamycin (RAPA) inhibits the glycolytic metabolism of T cells and then inhibits OLP. This article reviews the research progress of glycolytic metabolism-related transporters, enzymes and regulatory factors in OLP in recent years.

Synthesis and antitumor activity evaluation of glycoconjugates derived from natural product harmine / 中国药科大学学报

@#Based on our previous work, the study herein designed and synthesized eight glycoconjugates of natural product harmine (14a-14h)by introducing a cyclohexylmethyloxyl group at its C7 position and coupling a methyl-2-amino-β-D-glucopyranoside to the N9 position through different lengths of alkyl chains.In vitro anti-tumor activity screening and structure-activity relationship studies showed that the antitumor activity of the conjugates increased with the lengthening of the alkyl chain in the linker.Compound 14h exhibited significantly better proliferative inhibitory activity against MDA-MB-231 breast cancer cells than harmine.As compared to harmine, the introduction of the carbohydrate moiety improved the water solubility of compound 14h and enhanced its tumor cell selectivity through the Warburg effect.Mechanism of action studies revealed that compound 14h induced apoptosis and G0/G1 cell cycle arrest in MDA-MB-231 cells, and inhibited tumor cell migration by interfering with epithelial-mesenchymal transition process.This study provides a new approach for the development of antitumor drugs based on harmine.

Evaluation of 10-minute post-injection 11C-PiB PET and its correlation with 18F-FDG PET in older adults who are cognitively healthy, mildly impaired, or with probable Alzheimer's disease

Objective: Positron emission tomography (PET) allows in vivo evaluation of molecular targets in neurodegenerative diseases, such as Alzheimer's disease. Mild cognitive impairment is an intermediate stage between normal cognition and Alzheimer-type dementia. In vivo fibrillar amyloid-beta can be detected in PET using [11C]-labeled Pittsburgh compound B (11C-PiB). In contrast, [18F]fluoro-2-deoxy-d-glucose (18F-FDG) is a neurodegeneration biomarker used to evaluate cerebral glucose metabolism, indicating neuronal injury and synaptic dysfunction. In addition, early cerebral uptake of amyloid-PET tracers can determine regional cerebral blood flow. The present study compared early-phase 11C-PiB and 18F-FDG in older adults without cognitive impairment, amnestic mild cognitive impairment, and clinical diagnosis of probable Alzheimer's disease. Methods: We selected 90 older adults, clinically classified as healthy controls, with amnestic mild cognitive impairment, or with probable Alzheimer's disease, who underwent an 18F-FDG PET, early-phase 11C-PiB PET and magnetic resonance imaging. All participants were also classified as amyloid-positive or -negative in late-phase 11C-PiB. The data were analyzed using statistical parametric mapping. Results: We found that the probable Alzheimer's disease and amnestic mild cognitive impairment group had lower early-phase 11C-PiB uptake in limbic structures than 18F-FDG uptake. The images showed significant interactions between amyloid-beta status (negative or positive). However, early-phase 11C-PiB appears to provide different information from 18F-FDG about neurodegeneration. Conclusions: Our study suggests that early-phase 11C-PiB uptake correlates with 18F-FDG, irrespective of the particular amyloid-beta status. In addition, we observed distinct regional distribution patterns between both biomarkers, reinforcing the need for more robust studies to investigate the real clinical value of early-phase amyloid-PET imaging.

Radiation protection effect of furosemide intervention on 18F-FDG PET/CT imaging / 中华放射医学与防护杂志

Objective:To investigate the radiation protection effect of furosemide intervention on 18F-2-deoxy-D-glucose ( 18F-FDG) positron emission tomography/computed tomography (PET/CT) imaging. Methods:A total of 146 patients were randomly divided into two groups, with test group of 74 patients and control group of 72. The test group was administrated orally with furosemide of 40 mg for each one before injection, while the normal control group did not undergo special treatment. 60 and 120 min after 18F-FDG injection, the horizontal measurement of ambient dose equivalent rates was carried out at 0.5 m from the front of both chest and abdomen respectively. Results:For the test group, the ambient dose equivalent rates were measured to be (30.80±8.61) and (41.38±11.06) μSv/h 60 min after injection of 18F-FDG whereas (18.26±4.85) and (24.66±6.50) μSv/h 120 min after injection, respectively, both lower than in the control group and with statistically significant difference between the both ( t =15.36, 13.13, 18.73, 17.29, P<0.05) . No significant difference was found between mediastinal SUV max and liver SUV max in the experimental group and control group ( P>0.05) . Multivariate ANOVA showed that body surface area was a major factor influencing ambient dose equivalent rate regardless of furosemide injection ( t=-13.52, 2.96, P<0.05) , and no obvious effects of age and sex on ambient dose equivalence rate were found. Conclusions:Furosemide intervention can promote urination, effectively reduce the internal radiation exposure of the examinated patietns in the premise of not affecting the image quality, and therefore provide a better radiation protection effect.

Metabolic dysregulation and emerging therapeutical targets for hepatocellular carcinoma

Hepatocellular carcinoma (HCC) is an aggressive human cancer with increasing incidence worldwide. Multiple efforts have been made to explore pharmaceutical therapies to treat HCC, such as targeted tyrosine kinase inhibitors, immune based therapies and combination of chemotherapy. However, limitations exist in current strategies including chemoresistance for instance. Tumor initiation and progression is driven by reprogramming of metabolism, in particular during HCC development. Recently, metabolic associated fatty liver disease (MAFLD), a reappraisal of new nomenclature for non-alcoholic fatty liver disease (NAFLD), indicates growing appreciation of metabolism in the pathogenesis of liver disease, including HCC, thereby suggesting new strategies by targeting abnormal metabolism for HCC treatment. In this review, we introduce directions by highlighting the metabolic targets in glucose, fatty acid, amino acid and glutamine metabolism, which are suitable for HCC pharmaceutical intervention. We also summarize and discuss current pharmaceutical agents and studies targeting deregulated metabolism during HCC treatment. Furthermore, opportunities and challenges in the discovery and development of HCC therapy targeting metabolism are discussed.

2-Deoxy-D-Glucose: A Ray of Hope in COVID Pandemic

Coronavirus disease-19 (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus 2 is a respiratory tract infection that has already made a huge negative impact in global health situation. Transmission mainly occurs through droplets, and the virus is highly contagious. Mainly symptomatic treatments are given at present with some drugs for serious patients with unproven efficacy and safety. In this context, Institute of Nuclear Medicine and Allied Sciences, a research laboratory of Defence Research and Development Organization in collaboration with Dr. Reddy’s Laboratories, Hyderabad, has introduced a new medicine named 2-Deoxy-d-glucose (2-DG) (which has been previously tried in cancer) for the treatment of seriously ill COVID patients with a target to reduce the oxygen demand. Clinical trials showed evidence that 2-DG effectively reduces oxygen requirement in seriously ill patients, and real-time polymerase chain reaction conversion is also faster. Recently, 2-DG is approved for the use in critically ill patients by the Drug Controller General of India in May 2021. The introduction of 2-DG brings a new hope in reducing the mortality in COVID patients.

Tomografía por emisión de positrones asociada con tomografía computarizada en la estadificación de los linfomas / Positron emission tomography combined with computed tomography for the staging of lymphomas

Introducción: Los estudios de imágenes son esenciales para la estadificación de los linfomas. La utilización de la imagen funcional que proporciona la tomografía por emisión de positrones con 18F-2-deoxi-2-fluoro-D-glucosa asociada a la tomografía computarizada ha cambiado fundamentalmente el concepto de estadificación y reestadificación de los linfomas. Constituye una prueba diagnóstica que ha ganado aceptación universal, sobre todo después de la publicación y adopción de las guías de Lugano. Objetivo: Analizar la importancia que tienen las imágenes que proporciona la tomografía por emisión de positrones con 18F-2-deoxi-2-fluoro-D-glucosa asociada a la tomografía computarizada en la estadificación actual de los linfomas. Métodos: Se realizó una revisión bibliográfica, en español y en inglés, de la última década. Se utilizaron los motores de búsqueda de Pubmed, Google y SciELO. Se recolectó y organizó la información siguiendo cronológicamente la aparición de las innovaciones para facilitar la estadificación de los linfomas. Análisis y síntesis de la información: Se hace un recorrido desde la introducción de la tomografía computarizada, la tomografía por emisión de positrones y la asociación de estas, hasta su aplicación en el estudio de los linfomas. Se describe la evolución de los sistemas de clasificación para los linfomas y la utilidad del empleo de la tomografía por emisión de positrones con 18F-2-deoxi-2-fluoro-D-glucosa asociada a la tomografía computarizada en la estadificación de los linfomas. Conclusiones: Es de gran importancia que, en el momento actual, el manejo óptimo de un paciente con linfoma ávido de 18F-2-deoxi-2-fluoro-D-glucosa incluya la estadificación inicial con tomografía por emisión de positrones asociada con tomografía computarizada. Esto permitirá hacer más precisa la etapificación inicial del paciente, optimizar su tratamiento y evaluación de la terapia implementada; así como un mejor pronóstico y evitar estudios invasivos(AU)

Introduction: Imaging studies are essential for staging of lymphomas. The usage of functional imaging provided by positron emission tomography with 18F-2-deoxy-2-fluoro-D-glucose combined with computed tomography has fundamentally changed the concept of staging and re-staging of lymphomas. It constitutes a diagnostic test that has gained universal acceptance, especially after the publication and adoption of the Lugano guidelines. Objective: To analyze the importance of the images provided by positron emission tomography with 18F-2-deoxy-2-fluoro-D-glucose combined with computed tomography in current staging of lymphomas. Methods: A bibliographic review was carried out, in Spanish and in English, within the last decade. We used the search engines of Pubmed, Google, and SciELO. The information was collected and organized by chronologically following the origin of the innovations that facilitate the staging of lymphomas. Information analysis and synthesis: An analysis is carried out from the introduction of computed tomography, positron emission tomography, and the combination of both, to their application in the study of lymphomas. We described the evolution of lymphoma classification systems and the usefulness of positron emission tomography with 18F-2-deoxy-2-fluoro-D-glucose combined with computed tomography for the staging of lymphomas. Conclusions: At the present time, it is of great importance for a patient with lymphoma needing 18F-2-deoxy-2-fluoro-D-glucose to receive optimal management of his or her condition, including initial staging with positron emission tomography combined with computed tomography. This will allow to make the initial staging of the patient more precise, to optimize his or her treatment and evaluation of the implemented therapy, as well as to obtain a better prognosis, avoiding invasive studies(AU)

Establishment of quality evaluation methods for pieces and standard decoction of honey-fried Descurainiae Semen / 中国中药杂志

To establish a content determination method for quality control of the pieces and standard decoction of honey-fried Descurainiae Semen. Standard decoction of honey-fried Descurainiae Semen was prepared with standardized process, and high performance liquid chromatography coupled with diode-array detector(HPLC-DAD) was used to detect its characteristic fingerprint and determine the content of quercetin-3-O-β-D-glucose-7-O-β-D-gentiobioside. In addition, the transfer rate, dry extract rate and pH value were calculated. The results showed that the established method had a high accuracy. The content of quercetin-3-O-β-D-glucose-7-O-β-D-gentiobioside in 13 batches of standard decoction was 0.03-0.12 mg·mL~(-1); the transfer rate was 13.4%-23.1%; the rate of extracts was 1.9%-5.5%, and the pH was between 5.4-5.9. The similarity coefficients were all greater than 0.85, indicating good homogeneity for the different batches of decoction. There were 7 common peaks in the characteristic chromatogram, one of which was quercetin-3-O-β-D-glucose-7-O-β-D-gentiobioside. In this paper, the established content determination and quality evaluation method for Descurainiae Semen pieces and decoction was simple, rapid and reproducible, providing reference for the quality control of honey-fried Descurainiae Semen pieces, standard decoction and its preparations.

Effect of protease inhibitor from Agaricus bisporus on glucose uptake and oxidative stress in 3T3-L1 adipocytes

Objective: To explore the effect of the protease inhibitor from Agaricus bisporus (J.E. Lange) Imbach (AbPI) on glucose uptake and oxidative stress in 3T3-L1 adipocytes. Methods: Adipocytes were differentiated and stained with Oil-Red-O staining to confirm adipogenesis. The toxic/protective effect of AbPI on the adipocytes was determined by MTT assay, intracellular reactive oxygen species generation through flow cytometry, and morphologically through confocal microscopy using propidium iodide, 4,6-diamino-2-phenylindol dihydrochloride, and 2',7'-dichlorofluorescein diacetate dyes. The uptake of fluorescent glucose analog, 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-d-glucose by adipocytes was also studied through confocal microscopy. Results: MTT assay showed that the cell survival rate was (28.00±3.00)%, (92.33±2.60)%, and (71.34±2.10)% in the presence of 2 mM H

The application of fluorine-18-fluorodeoxyglucose positron emission tomography/computed tomography in inflammation and infectious disease / 生物医学工程学杂志

2-［ F］-fluoro-2-deoxy-D-glucose positron emission tomography/computed tomography ( F-FDG PET/CT) combining positron emission tomography with computed tomography is used to evaluate the body's glucose metabolic changes under different conditions. In addition to its established role in oncological imaging, F-FDG PET/CT has clinical utility in suspected inflammation and infection. The technique can identify the source of infection in a timely fashion ahead of morphological changes, map the extent and severity of inflammation, guide the site for tissue biopsy and assess therapy response. This article reviewed the use of F-FDG PET/CT in infection and inflammation, such as fever of unknown origin, sarcoidosis, vessel vasculitis, osteomyelitis, joint prosthesis or implant-related complications, human immunodeficiency virus-related infections, and other indications, such as inflammatory bowel disease, so as to provide reference for clinicians to select F-FDG PET/CT to help them in the diagnosis and treatment of inflammatory diseases.

Effect of protease inhibitor from Agaricus bisporus on glucose uptake and oxidative stress in 3T3-L1 adipocytes

Objective: To explore the effect of the protease inhibitor from Agaricus bisporus (J.E. Lange) Imbach (AbPI) on glucose uptake and oxidative stress in 3T3-L1 adipocytes. Methods: Adipocytes were differentiated and stained with Oil-Red-O staining to confirm adipogenesis. The toxic/protective effect of AbPI on the adipocytes was determined by MTT assay, intracellular reactive oxygen species generation through flow cytometry, and morphologically through confocal microscopy using propidium iodide, 4,6-diamino-2-phenylindol dihydrochloride, and 2',7'-dichlorofluorescein diacetate dyes. The uptake of fluorescent glucose analog, 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-d-glucose by adipocytes was also studied through confocal microscopy. Results: MTT assay showed that the cell survival rate was (28.00±3.00)％, (92.33±2.60)％, and (71.34±2.10)％ in the presence of 2 mM H2O2, AbPI alone, and AbPI and H2O2 both, respectively, in comparison to the control. Oil-Red-O staining indicated that AbPI enhanced adipogenesis. AbPI stimulated the glucose uptake by adipocytes similar to the drug rosiglitazone, and showed insulin-sensitizing effect in the presence of insulin, but failed to stimulate the uptake in the absence of insulin. Intracellular reactive oxygen species generation was reduced in differentiating adipocytes upon AbPI treatment. Confocal microscopy showed that the damaged cell population rose to 3.50％, 117.84％, and 261.50％ in the presence of AbPI alone, AbPI with H2O2, and H2O2 alone, respectively. Conclusions: The protease inhibitor enhances glucose uptake by adipocytes and exhibits a cytoprotective effect on them.

Correlation between bone protection of 1,2,3,4,6-pentyl-O-galloyl-beta-D-glucose and Nrf2/HO-1 signaling pathway / 药学学报

To study the osteoprotective effect of 1,2,3,4,6-pentyl-O-galloyl-beta-D-glucose (PGG) its anti-osteoblast apoptosis related mechanism was investigated. A model of zebrafish osteoporosis induced by prednisolone (Pred, 25 μmol·L-1) was established in vivo, and calcein staining was used to detect the effect of PGG on the bone area of ​​zebrafish. Bone marrow mesenchymal stem cells were cultured in vitro, and the number of calcified nodules was observed by alizarin red staining, and the relevant indexes of osteoblast differentiation runt-related transcription factor 2 (Runx 2), osteocalcin (OCN) mRNA level were detected by qRT-PCR. The osteoblast cell line MC3T3-E1 cells was cultured in vitro, and 400 μmol·L-1 hydrogen peroxide (H2O2) was used to intervene the injury to detect the effect of PGG on osteoblasts under oxidative stress. The effect of PGG on osteoblast activity was detected by MTT assay. The effect of PGG on apoptosis was observed by Hoechst 33342 staining. Western blot was used to detect the expression of Bcl-2, Bax, nuclear factor erythroid-2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1). DCFH-DA fluorescence staining for detection of reactive oxygen species (ROS) levels. JC-1 staining was used to detect mitochondrial membrane potential levels. The results showed that PGG could significantly increase the vertebral area of ​​the zebrafish model when compared with the model group. On the 14 th day of osteoblast differentiation, the number of calcified nodules in the PGG group was significantly increased when compared with the control group and the mRNA levels of Runx 2 and OCN were also significantly increased. In addition, under oxidative stress, PGG could increase osteoblast viability, significantly reduce the number of apoptotic cells, and increase the ratio of Bcl-2/Bax. Fluorescence staining results show that PGG decreased intracellular ROS fluorescence density and increased mitochondrial membrane potential. Western blot data showed that PGG could promote the expression of Nrf2 in the nuclear and enhance the expression of downstream protein HO-1. In conclusion, PGG could improve osteoporosis in zebrafish, and this effect may be related to the regulation of Nrf2/HO-1 signaling pathway to improve mitochondrial dysfunction, anti-oxidative stress in osteoblast apoptosis and promote bone formation. This study provides new ideas and clues for the discovery of anti-osteoporosis drugs.

Presence of carbohydrate binding modules in extracellular region of class C G-protein coupled receptors (C GPCR): An in silico investigation on sweet taste receptor

Sweet taste receptor (STR) is a C GPCR family member and a suggested drug target for metabolic disorders such asdiabetes. Detailed characteristics of the molecule as well as its ligand interactions mode are yet considerably unclear due toexperimental study limitations of transmembrane proteins. An in silico study was designed to find the putative carbohydratebinding sites on STR. To this end, a-D-glucose and its a-1,4-oligomers (degree of polymerization up to 14) were chosen asprobes and docked into an ensemble of different conformations of the extracellular region of STR monomers (T1R2 andT1R3), using AutoDock Vina. Ensembles had been sampled from an MD simulation experiment. Best poses were furtherenergy-minimized in the presence of water molecules with Amber14 forcefield. For each monomer, four distinct bindingregions consisting of one or two binding pockets could be distinguished. These regions were further investigated withregard to hydrophobicity and hydrophilicity of the residues, as well as residue compositions and non-covalent interactionswith ligands. Popular binding regions showed similar characteristics to carbohydrate binding modules (CBM). Observationof several conserved or semi-conserved residues in these binding regions suggests a possibility to extrapolate the results toother C GPCR family members. In conclusion, presence of CBM in STR and, by extrapolation, in other C GPCR familymembers is suggested, similar to previously proposed sites in gut fungal C GPCRs, through transcriptome analyses. STRmodes of interaction with carbohydrates are also discussed and characteristics of non-covalent interactions in C GPCRfamily are highlighted.

Content Comparison of Mannose,Glucose and Narinhenin in Dendrobium officinale and Dendrobium huoshanense / 中国实验方剂学杂志

Objective: To optimize the pre-column derivation high performance liquid chromatography (HPLC) content determination method of D-mannose and D-glucose as well as the content determination method of narinhenin in Dendrobium officinale and D. huoshanense, and compare the contents of D-mannose,D-glucose and narinhenin between D. officinale and D. huoshanense. Method: A pre-column derivation HPLC method modified by Chinese Pharmacopoeia(Ch.P) 2015 was used to simultaneously determine the contents of D-mannose and D-glucose,with acetonitrile-0.02 mol·L-1 ammonium acetate solution as mobile phase for gradient elution. Kromasil 100-5 C18 was performed with the wavelength set at 250 nm,and the flow rate was 1 mL·min-1;column temperature was 30℃. HPLC content determination of narinhenin was performed on Kromasil 100-5 C18 with the acetonitrile-methanol-0.4% phosphoric acid solution as mobile phase for gradient elution,and the wavelength was set at 290 nm; the flow rate was 0.8 mL·min-1,and column temperature was 40℃. Result: D-mannose and D-glucose showed a good linear relationship within the range of 0.15-3.0 μg and 0.075-2.25 μg (r=0.999 9); and their average recoveries were 99.01% (RSD 2.1%) and 101.69% (RSD 2.0%) respectively. In addition, the other methodological researches such as repeatability and durability all met the requirements. The contents of D-mannose(Cm),D-glucose(Cg) and sum of them (Cm+Cg) were 12.75%-36.40%,2.93%-18.39% and 19.23%-54.58% in 43 batch of D. officinale. Almost all of the results except very few samples reached the D-mannose standard in Ch.P 2015, and the total content of D-mannose and D-glucose was also up to the total polysccharide standard in Ch.P. The correlation between content and origin was not significant. The contents of D-mannose(Cm),D-glucose(Cg) and sum of them (Cm+Cg) were 14.33%-29.47%,6.64%-15.20%,and 25.73%-44.37% in 12 batch of D. huoshanense. These contents and ratio of peak areas of D-mannose to D-glucose (Am/Ag) were within the scope of D. officinale's; in addition, their average contents were basically the same with those in D. officinale (about 33%).Next,naringenin showed a good linear relationship within the range of 0.020 8-0.832 0 μg (r=0.999 9),and its average recovery was 101.96% (RSD 1.8%). The content of naringenin was 0.053 2-0.122 4 mg·g-1 (average value of 0.081 0 mg·g-1) in 11 batch of D. officinale, slightly higher than 0.040 3-0.090 0 mg ·g-1 (average value of 0.068 3 mg ·g-1) in 7 batch of D. huoshanense. All of these results of narinfenin did not reach the content lower limit in Ch.P. Conclusion: The method used to determinate the content of D-mannose and D-glucose is reproducible, and their sum content is possible to substitute the total polysccaride determination (with higher errors) in D. officinale; monosaccharide content determination can be used for quantitative quality control of D. huoshanense. However, it could not distinguish D. officinale and D. huoshanense by determining the contents of polysccharide,D-glucose,D-mannose and narinhenin, and shall be combined with other specificity methods for further identification.

Effects of processing on pharmacokinetics of Descurainiae Semen's constituents in rats / 中国中药杂志

An UPLC-MS/MS method simultaneously determining contents of quercetin-3-O-β-D-glucose-7-O-β-D-gentiobioside and sinapic acid in rats' plasma was firstly established and applied to study the effects of processing on pharmacokinetics of Descurainiae Semen's active constituents. Complantatoside A as internal standard,methanol used for protein precipitation,the method was validated according to the instructions of CFDA. Rats' plasma was collected after being oral administrated equal dosage of 60% ethanal extract of raw or processed Descurainiae Semen at different point of time,then the concentrations were determined to calculate pharmacokinetic parameters using DAS 3. 2. 6. And the parameters were analyzed using SPSS 23. 0,meantime the concentration-time curve was drawn.The results showed that processing had no effects on the pharmacokinetics of QGG,but could improve the absorption of sinapic acid and slow down the excretion.

Intestinal absorption of phenolic acids in Rhus chinensis extracts by in situ single-pass perfusion model in rats / 中国中药杂志

The intestinal absorption properties of four main effective components(gallic acid, ocinolglucoside, ethyl gallate and penta-O-galloyl-β-D-glucose) in Rhus chinensis extracts were investigated by in situ single-pass intestinal perfusion model in rats. The liquid accumulation of perfusion was corrected by gravimetry. The HPLC method was established to determine the concentration of the four effective components in the intestinal perfusion. It showed significant differences(Pethyl gallate>gallic acid>ocinolglucoside, with significant differences between them(P<0.05). In conclusion, gallic acid, orpheolglucoside, ethyl gallate and pentacyl-glucose could be absorbed in the whole intestine. Their absorption rate and permeation ability were related to the intestinal section and the perfusate concentration. These results indicated potential active transport or facilitated diffusion in the intestinal transport process of the four effective components.

Simultaneous determination of thirteen components of Mortan Cortex in different regions by HPLC / 中草药

Objective: To establish an HPLC method for the analysis of thirteen main chemical constituents (gallicacid, 5-hydroxymethylfurfural, methylgallate, oxypaeoniflora, catechins, paeoniflorin, 1,2,3,6-tetra- O-galloyl-D-glucose, 1,2,4,6-tetra-O- galloyl-D-glucose, benzoicacid, 1,2,3,4,6-penta-O-galloyl-D-glucose, mudanpioside C, benzoyloxypaeoniflorin, and paeonal) in Moutan Cortex from different origins. Methods: The methanol (50%) reflux extraction was adopted to Moutan Cortex. Separation was carried out on C18 (250 mm × 4.6 mm, 5 μm), the mobile phase was eluted with acetonitrile-0.5% phosphoric acid. The flow rate was 1.0 mL/min, the detection wavelength was 254 nm, and the column temperature was 30 ℃. Results :The linear relation of thirteen main active components measured in the range of mass concentration was good with perfect precision, repeatability, and stability, the value of which was all more than 0.999 5. Conclusion: The HPLC method established for simultaneous determination of thirteen main chemical compositions in Mortan Cortex is effective, accurate, and reproducible, which can be used for the quality control of Mortan Cortex.

Quality evaluation and discrimination of Polygonati Rhizoma from three origins based on polysaccharide composition and content / 中草药

Objective: To compare the composition and content of polysaccharides in Polygonati Rhizoma by qualitative and quantitative analysis combined with chemometrics, and provide the reference for the quality evaluation of Polygonati Rhizoma. Methods Fourier transform infrared spectroscopy (FTIR) and pre-column derivatization-HPLC (PMP-HPLC) were employed to reveal the differences of polysaccharide among the three species, and the content of total polysaccharide was determined by ultraviolet spectroscopy (UV). Results:The result indicated that the average spectra and the second derivative atlas in FTIR fingerprint of Polygonati Rhizoma was significantly different. The PCA, PLS-DA and HCA analysis provided a further refinement of the method to distinguish three species. Furthermore, the PMP-HPLC showed that the components of monosaccharide and polysaccharides of three species were different. The main common components of the 10 common peaks were identified, which were as follows: D-mannose, D-ribose, L-rhamnose, D-galacturonic acid, D-glucuronic acid, D-galactose, D-glucose, D-xylose, D-arabinose and L-fucose. The content of the total polysaccharide meeted the requirements of Chinese pharmacopoeia 2015 edition Conclusion:The study provided a new reference for quality evaluation of P. Rhizoma.

Virtual screening of Chinese herbal monomer against EV71 3C protease / 中草药

Objective: To search for Chinese herbal monomer with the antiviral activity of enterovirus 71 (EV71) 3C protease by virtual screening. Methods: A total of 1998 monomers from antiviral Chinese herbs downloaded from TCM Database@Taiwan database were chosen as screening ligands, and EV71 3C protease was selected as a target. The binding mode of Chinese herbal monomer and EV71 3C protease was simulated through the molecular docking tools of AutoDock Vina. The monomers were sorted according to the binding free energy. The binding poses of the monomers with docking scores less than -37.673 kJ/mol were visualized by Discovery Studio 2018 Visualizer program. Results: Two monomers, namely, procyanidin B5 and 1,2,3,6-tetra-O-galloyl- β-D-glucose, were obtained with the lowest binding energies. Conclusion: The promising candidate monomers with anti-EV71 3C protease activity were screened out from traditional Chinese medicine, providing an alternative method for further development of therapeutically useful anti-EV71 agents.

Simultaneous determination of nine components in Paeoniae Radix Rubra by HPLC / 中草药

Objective A high performance liquid chromatographic method (HPLC) was established to simultaneously quantify the paeoniflorin, oxypaeoniflora, albiflorin, benzoyl paeoniflorin, benzoic acid, catechin, paeonol, gallic acid, and 1,2,3,4,6-penta-O- galloy-D-glucose of Paeoniae Radix Rubra. Methods The mobile phase comprised of acetonitrile and water containing 0.1% phosphoric acid. Column temperature was 30 oC, flow rate was 1.0 mL/min, and chromatography was monitored at 230 nm. Results The correlation coefficients between concentration and chromatographic peak area of gallic acid, oxypaeoniflora, catechin, albiflorin, paeoniflorin, 1,2,3,4,6-penta-O-galloy-D-glucose, benzoic acid, benzoyl paeoniflorin, and paeonol were respectively over 0.999 in the ranges of 0.004-1.200, 0.010-1.500, 0.044-0.660, 0.038-1.140, 0.042-2.100, 0.050-1.250, 0.040-0.600, 0.042-1.260, and 0.004-1.080 mg/mL, with good precision, stability, repeatability, and recovery. Conclusion The method is effective, accurate and reproducible, and can be used for the quality control of Paeoniae Radix Rubra.