Inhibitory Effect of Hederasaponin B on Gastric Cancer HGC-27 Cells and Its Mechanism Based on Bioinformatics / 中国实验方剂学杂志

ObjectiveTo investigate the inhibitory effect of hederasaponin B on gastric cancer HGC-27 cell and the mechanism. MethodMethyl thiazolyl tetrazolium （MTT） assay， hematoxylin-eosin （HE） staining， 4'，6-diamidino-2-phenylindote （DAPI） staining， colony formation assay， scratch assay， and flow cytometry were employed for the analysis of apoptosis and cell cycle. Thereby， the inhibitory effect of hederasaponin B on gastric cancer HGC-27 cell was investigated. Then the Pharm Mapper， UniProt， Swissdock， STRING， and Metascape were used for target screening， gene annotation， molecular docking， protein-protein interaction （PPI） network construction， Gene Ontology （GO） term and Kyoto Encyclopedia of Genes and Genomes （KEGG） pathway analysis to explore the mechanism. ResultHederasaponin B （15， 30， 60， 120 μmol·L-1） can significantly reduce the survival rate of HGC-27 cell （P<0.01） in a time-dependent and dose-dependent manner compared with the blank group. It had no significant toxicity to normal GES-1 cell at concentration below 120 μmol·L-1. Compared with the blank group， hederasaponin B （30， 60， 120 μmol·L-1） induced cytoplasmic vacuolization， and nuclear deformation and karyopyknosis， inhibited the migration of HGC-27 cell （P<0.01）， and brought about the apoptosis （P<0.05， P<0.01） and cell cycle arrest of HGC-27 cell （P<0.05， P<0.01）. Hederasaponin B （10， 20， 30 μmol·L-1） also suppressed the independent survival ability and proliferation ability of HGC-27 cell （P<0.01）. The possible action targets were kinesin-like protein KIF11， cGMP-specific 3，5 cyclic phosphodiesterase， caspase-3， serine/threonine protein kinase Chk1， proto-oncogene tyrosine protein kinase， epidermal growth factor receptor， and mitogen-activated protein kinase （MAPK） 8. The mechanism may be related to MAPK signaling pathway （pathways in cancer）， adhesion connection， focal adhesion and proteoglycans in cancer （epithelial cell signaling pathways in Helicobacter pylori infection）. ConclusionHederasaponin B exerts significant inhibitory effect on gastric cancer HGC-27 cell through multiple targets and multiple pathways.

Physiologically based pharmacokinetic modeling of the inhibitory effect of dapagliflozin on intestinal and renal SGLT / 药学学报

This study establishes and optimizes the physiologically based pharmacokinetics (PBPK) model for dapagliflozin, predicts the drug distribution into relevant tissues, and calculates the inhibitory effect on the sodium-glucose cotransporters (SGLTs) in the intestine and renal proximal tubule. Based on literature data, a PBPK model for oral administration in healthy adults was established and the predicted blood concentration-time curve characteristics, the main pharmacokinetic parameters (PK), and drug excretion in urine were compared with the published data. To verify and optimize the model and verify the accuracy of the tissue distribution and concentration predictions, a pharmacodynamics model (PD) was established. Urine glucose excretion (UGE) was simulated at the corresponding times. The characteristics of the drug-time curve predicted by the model are similar to those of the measured curve, and the ratio of the main PK parameters to the measured values is within a two-fold range; the accuracy of the established PBPK model is good. The maximal inhibition obtained with 10 mg of dapagliflozin on the duodenum and jejunum segment sodium-glucose co-transporter 1 (SGLT1s) was 1.6%-4.7%, and the inhibition rate of the sodium-glucose co-transporter 2 (SGLT2s) in the proximal tubule of the kidney was as high as 99.9%. At a dose of 10 mg, dapagliflozin delayed intestinal glucose absorption while occupying most of the sites (99.9%) of the renal sodium-glucose cotransporter 2 and inhibiting its glucose reabsorption. This physiological-pharmacokinetic model for dapagliflozin in healthy adults can provide meaningful guidance for exploring pharmacological mechanisms and potential toxicity of gliflozin by simulating drug distribution in different tissues.

In vitro inhibitory effects of acteoside on 6 kinds of CYP enzymes in liver microsomes of rats / 中国药房

OBJECTIVE To inv estigate the in vitro inhibitory effects of acteoside on cytochrome P 450（CYP）enzymes in liver microsomes of rats. METHODS Using probe substrates method ，acteoside（0.1，0.3，1，3，10，30 μmol/L）was incubated with probe substrates phenacetin ，mephentoin，diclofenac，coumarin，dextromethorphan and testosterone （substrates of CYP 1A2， CYP2C19，CYP2C9，CYP2A6，CYP2D6 and CYP 3A4 enzymes，respectively）in liver microsomes of rats. Another blank control group and positive inhibitor group [ α-naphthoflavone，ticlopidine，sulfabendazole，pilocarpine，quinidine and ketoconazole （inhibitors of CYP 1A2，CYP2C19，CYP2C9，CYP2A6，CYP2D6 and CYP 3A4 enzymes，respectively）] were set up. Using indapamide as the internal standard ， the contents of corresponding metabolites （acetaminophen， 4-hydroxymephenytoin， 4-hydroxydiclofenac，7-hydroxycoumarin，dextran，6 β-hydroxytestosterone） were detected by ultra high performance liquid chromatography-tandem mass spectrometry . The IC 50 values were calculated by GraphPad v 8.0 software. By computer molecular docking technology ，acteoside and positive inhibitors were molecularly docked with the CYP enzyme ，and the binding mode and strength of the two molecules were analyzed. RESULTS The IC 50 values of acteoside to CYP 1A2 and CYP 2A6 enzymes were more than 30 μmol/L，and those of acteoside to CYP 2D6，CYP2C19，CYP2C9 and CYP 3A4 enzymes were 24.87，21.52，12.56 and 7.55 μmol/L，respectively. The hydrogen bond and hydrophobic force could form between acteoside and CYP 3A4 enzyme，and the hydrogen bond and electrostatic interaction could form between ketoconazole and CYP 3A4 enzyme. The binding free energy of acteoside and ketoconazole to CYP 3A4 enzyme were － 10.2 and － 12.4 kcal/mol （1 kcal/mol＝4.19 kJ），respectively. CONCLUSIONS Acteoside shows moderate inhibitory effect on CYP 3A4 enzyme in liver microsomes of rats ，and its affinity is equivalent to that of positive inhibitor ；the compound shows weak inhibitory effect on other 5 CYP enzymes.

Isolation and purification of indoleamine 2,3-dioxygenase (IDO) inhibitory constituents from Rabdosia japonica / 中草药

Objective: To isolate indoleamine 2,3-dioxygenase (IDO) inhibitory constituents from Rabdosia japonica based on bioactivity tracking separation. Methods: The overground part of R. japonica was extracted with boiling water and precipitated by ethanol, the precipitation was collected and lyophilized to obtain XPS, then successively separated by DEAE Sepharose Fast Flow anion-exchange and Superdex-75 gel permeation chromatographic steps to give XPS10-1. A combination of HPGPC, monosaccharide and amino acid composition analysis and IDO inhibitory studies was performed to investigate the structure and bioactivity of XPS10-1. Results: A IDO inhibitory glycoprotein, XPS10-1, was obtained from R. japonica based on activity tracking, its average molecular weight was estimated to 8 852, monosaccharide composition analysis showed the glycosyl part of XPS10-1 was mainly composed of rhamnose and glucose with the ratio of 10.0:2.2, and the protein part was mainly composed of glutamic acid, serine and glycine with mass ratio of 37.3:16.9:45.8. XPS10-1 showed potent IDO inhibitory effect with IC50 of (46.6 ± 3.4) μg/mL, and IC50 of IDO inhibitory effect of XPS10-1 on HeLa cells was (139.0 ± 8.7) μg/mL. Conclusion: In this study, a glycoprotein with IDO inhibitory effect was isolated from R. japonica, which could lay the foundation for the substance basis study of R. japonica.

Yiqi Huoxue decoction inhibits malignant biological behavior of human lung cancer cells via the miR-21/PTEN signaling pathway / 中国临床药理学与治疗学

AIM: To investigate the inhibitory effect of Yiqi Huoxue decoction on the malignant biological behavior of lung cancer cells and its mechanism. METHODS: Human lung cancer A549 cells were treated with different doses of Yiqi Huoxue Decoction serum (5%, 10%, 15%). CCK-8 assay, transwell chamber experiment, flow cytometry, Western blot and qRT-PCR method were used to study the effect of different doses of Yiqi Huoxue Decoction-containing serum to cell proliferation, cell migration and invasion, cell apoptosis, PTEN protein and miR-21 expression. RESULTS:Compared with the drug-free serum group, survival rate, migration and invasion ability of A549 cells decreased after treatment with different doses of drug-containing serum. The apoptosis rate of A549 cells increased, PTEN mRNA and the expression of its protein increased, the expression of miR-21 decreased, and the medium-dose (10%) drug-containing serum group had the best effect. After the transfection of miR-21 mimics, miR-21 expression was up-regulated, while PTEN protein expression was down-regulated in cells. PTEN protein expression was up-regulated after treatment with medium-dose (10%) drug-containing serum. CONCLUSION: Yiqi Huoxue Decoction can effectively inhibit the malignant cell biological behavior of human lung cancer A549 cells and may be related to the regulation of the miR-21/PTEN signaling pathway.

Effects of five Chinese herbs on human demodicid mites in vitro / 中国血吸虫病防治杂志

Objective To research the effects of five Chinese herbs of Artemisia argyi, Chimonanthus praecox, Agastache rugosa, pine needles and Osmamthus fragrans on human demodicid mites in vitro. Methods The human demodicid mites were acquired with the cellophane tape method. The ethanol heat reflux extractions were carried out on the 5 kinds of Chinese herbs to be studied and Stemona sessilifolia as the positive control, so as to get the herbal extracts. Next, the drug administration was carried out to the demodicid mites, and the inhibitory or killing effects of the 6 kinds of Chinese herbs above mentioned on the vermiform mites were observed under a microscope. It was considered to be dead when the bodies of the demodicid mites stopped moving. Besides, the duration from drug administration to death of the vermiform mites was recorded. Results Artemisia argyi, Chimonanthus praecox and Agastache rugosa could effectively inhibit and kill human demodicid mites. The effect of Artemisia argyi and Agastache rugosa was similar to the effect of Stemona sessilifolia, and the effect of Chimonanthus praecox was weaker than Stemona sessilifolia’s effect. Among them, Agastache rugosa took a relatively short time (4.60 min ± 1.66 min) min and Osmamthus fragrans took the longest time (114.65min ± 80.14min) to Demodex folliculorum; Whereas, Artemisia argyi took the shortest time (3.56min ± 1.92 min) min and Osmamthus fragrans took the longest time (194.24min ± 134.96 min) min to Demodex brevis. Conclusions The effects of Artemisia argyi and Agastache rugosa on human demodicid mites are similar to that of Stemona sessilifolia. The effects of Chimonanthus praecox and pine needles are weaker than that of Stemona sessilifolia. Osmamthus fragrans has no acaricidal effect.

Effects of Bezafibrate and Fenofibrate on the Proliferation of Lung Adenocarcinoma PC- 9 Cells and the Expression of c-myc / 中国药房

OBJECTIVE： To study the effects of bezafibrate （BEZ） and fenofibrate （FEN） on the proliferation of lung adenocarcinoma PC-9 cells and the expression of c-myc. METHODS： The effects of BEZ and FEN （12.5， 25， 50， 100， 200       μmol/L） on the survival rate of PC-9 cells were detected by CCK8 method. PC-9 cells were divided into administration group and control group. Administration group was given low， medium and high concentration （25， 50， 100 μmol/L） of BEZ and FEN； control group was treated with dimethyl sulfoxide for 48 h. Cell cycle distribution and apoptosis were detected by flow cytometry. qRT-PCR was used to detect mRNA relative expression of c-myc in cells. The protein relative expression of c-myc in cells were detected by Western blot assay. RESULTS： The survival rates of PC-9 cells were （80.76±3.2）％， （74.35±5.06）％， （62.8±1.23）％， （59.03±1.55）％， （39.8±1.01）％ under the action of above concentration of BEZ； and the survival rates of PC-9 cells were （74.46±1.30）％， （61.91±4.77）％， （48.95±2.8）％， （37.05±1.55）％， （32.49±1.36）％ under the action of FEN. Compared with control group， G1 phase cell ratio increased significantly in medium and high concentration groups of BEZ and FEN； the apoptotic rate of PC-9 cells was increased significantly in low， medium and high concentration groups of BEZ and FEN； mRNA and protein relative expression of c-myc were decreased significantly， with statistical significance （P＜0.05）. CONCLUSIONS： BEZ and FEN can inhibit the proliferation of PC-9 cells， and down-regulate c-myc expression.

Study on Expression Condition Optimization of Two Recombinant Methioninases and Their Inhibitory Effects on Human Lung Adenocarcinoma Cells GLC / 中国药房

OBJECTIVE： To optimize the expression induction condition of two recombinant methioninases， and to investigate their inhibitory effects on the proliferation of human lung adenocarcinoma cells GLC. METHODS： Recombinant methioninases expression plasmid PGEX-4T1-4A1-MGL and PGEX-4T1-3B8-MGL were transfected into competent Escherichia coli Dh5α， and induced by isopropyl-β-D-thiogalactoside. Using the expression level of target protein as index， the initial OD600 nm value before induction， culture temperature and induction time were optimized by single factor test. The recombinant methioninase 4A1-MGL and 3B8-MGL were purified by affinity chromatography. The concentration of recombinant methioninase was detected by Coomassie blue method. The purity of the product was detected by sodium lauryl benzene sulfonate-polyacrylamide gel electrophoresis； its activity was detected by spectrophotometry. The proliferation of cells was detected by MTT assay after treated with low-dose， medium-dose and high-dose of recombinant methioninases （4A1-MGL or 3B8-MGL was 0.1， 0.2， 0.4 U/mL） for 24， 48， 74 h. Inhibitory rate of cells were calculated. RESULTS： The optimal induction condition of two recombinant methioninases included that initial OD600 nm of 0.9， culture temperature of 37 ℃， induction time of 5 h. The results of validation test showed that protein expression level of 4A1-MGL was 1.52±0.04， that of 3B8-MGL was 1.28±0.03 （RSD＜3％，n＝3）. After purification， the concentration， purity and activity of 4A1-MGL were （0.70±0.02）mg/mL， （96.42±3.15）％ and （0.45±0.02）    U/mg； and those of 3B8-MGL were （0.56±0.02）mg/mL， （97.43±2.96）％ and （0.91±0.03）U/mg. After treated with low-dose and medium-dose of 4A1-MGL and 3B8-MGL for 48 and 72 h， treated with high-dose of 4A1-MGL and 3B8-MGL for 24， 48 and 72 h， inhibitory rate of GLC cell was increased significantly， and high-dose group for 72 h was significantly higher than low-dose and medium-dose groups at same time point （P＜0.05）. CONCLUSIONS： The induction conditions of recombinant methioninase expression are successfully optimized in this study. The obtained 4A1-MGL and 3B8-MGL could inhibit the proliferation of GLC cells in a dose-dependent manner.

Study on the miR- 21/PTEN Signaling Pathway Mechanisms of Calycosin Inhibiting the Proliferation and Migration of Lung Adenocarcinoma Cells / 中国药房

OBJECTIVE： To investigate the mechanism of calycosin （CA） inhibiting the proliferation and migration of lung adenocarcinoma cells by regulating miR-21/PTEN signaling pathway. METHODS： Using lung adenocarcinoma SPC-A1 cells as objects， cell proliferation was detected by MTT method after treated with different doses of CA （5， 15， 25， 50， 75， 100   μg/mL） for 12， 24， 48， 72 h. Cell survival rate， 30％ cell growth inhibition concentration （IC30） and half inhibition concentration （IC50） were calculated. Transwell migration test was used to detect the migration of cells after treated with low-dose， medium-dose and high-dose of CA （50， 75， 100 μg/mL） for 24 h. The number of stained cells was recorded and inhibition rate of cell migration were calculated. Western blotting assay and real-time PCR were used to detect the expression of miR-21 as well as the proteins and their mRNAs expression of PTEN， VEGF， MMP-9 after treated with low-dose， medium-dose and high-dose of CA （50， 75， 100 μg/mL） for 24 h. After transfected with miR-21 mimics and miR-21 inhibitor， the effects of CA （75 μg/mL） on the expression of miR-21 and the protein expression of PETN， VEGF and MMP-9 were detected. RESULTS： After treated with 50， 75， 100 μg/mL CA for 12， 24， 48 h， 25， 50， 75， 100 μg/mL CA for 72 h， cell survival rate was decreased significantly （P＜0.05 or P＜0.01）. IC30 of CA were 82.24， 50.45， 46.34， 31.81 μg/mL ； IC50 of CA were 108.06， 73.35， 70.08， 49.89 μg/mL during 12-72 h. Compared with normal control group， the number of stained cells in CA groups， protein expression of VEGF in CA low-dose group， expression of miR-21 as well as proteins and their mRNAs expression of VEGF， MMP-9 in CA medium-dose and high-dose groups were decreased significantly； the medium-dose and high-dose groups were significantly less or lower than low-dose group； the high-dose group was significantly less or lower than medium-dose group （P＜0.05 or P＜0.01）. Cell migration rate of CA groups as well as protein and its mRNA expression of PTEN in CA medium-dose and high-dose groups were increased significantly； the medium-dose and high-dose groups were significantly higher than the low-dose group； the high-dose group was significantly higher than the medium-dose groups （P＜0.05 or P＜0.01）. After transfected with miR-21 mimics， expression of miR-21 as well as protein expression of VEGF and MMP-9 were increased significantly in miR-21 mimic group， compared with normal control group； protein expression of PTEN was decreased significantly （P＜0.01）. After intervened by CA， expression of miR-21 as well as protein expression of VEGF and MMP-9 in cells were decreased significantly， compared with miR-21 mimic group； protein expression of PTEN was increased significantly （P＜0.05 or P＜0.01）. After transfected with miR-21 inhibitor， expression of miR-21 as well as  protein expression of VEGF and MMP-9 were decreased significantly in miR-21 inhibitor group， compared with normal control group； protein expression of PTEN was increased significantly （P＜0.05 or P＜0.01）. After intervened by CA， the expression of miR-21 and above protein had no significant change in cells， compared with miR-21 inhibitor group （P＞0.05）. CONCLUSIONS： CA can inhibit the proliferation and migration of lung adenocarcinoma SPC-A1 cells in a dose-dependent manner， which may be associated with the regulation of miR-21/PTEN signaling pathway.

Inhibitory Effects and Mechanism of Anemoside B 4 on Hepatocellular Carcinoma Huh- 7 Cells and Tumor-bearing Nude Mice / 中国药房

OBJECTIVE： To study the anti-tumor effect of anemoside B4 （AB4） on hepatocellular carcinoma Huh-7 and tumor-bearing nude mice and its mechanism. METHODS： Huh-7 cells were divided into AB4 treatment group， negative control group （constant volume of culture medium） and positive control group （5-fluorouracil 50 μmol/L）. The inhibitory rate of Huh-7 cell proliferation was tested by MTT after treated with 0， 3， 6， 12， 25， 50， 100， 200， 400， 800， 1 600 μmol/L AB4 for 12， 24， 36， 48 h； IC50 were calculated. The number of clone cells was evaluated by clone formation tests after Huh-7 cells were treated with 50 μmol/L AB4 for 24 h. The apoptosis rate of Huh-7 cells was tested by Annexin Ⅴ-FITC/PI double staining after treated with 50 μmol/L AB4 for 24 h. The expression of apoptotic proteins such as Bcl-2， Bax， Caspase-3， Cleaved Caspase-3 and Cleaved PARP were tested by Western blot after Huh-7 cells were treated with 50 μmol/L AB4 for 24 h. Tumor-bearing nude mice were randomly divided into negative control group （normal saline）， positive control group （5-fluorouracil 50 mg/kg）， AB4 lwo-dose， medium-dose and high-dose groups （25， 50， 100 mg/kg）， with 3 mice in each group. They were given relevant medicine intraperitoneally， once a day， for consecutive 19 d. The growth of tumor was observed， and anti-tumor rate was also calculated. HE staining was used to observe the morphology of tumor cells. RESULTS： The inhibition rate of AB4 on Huh-7 cell proliferation increased with the increase of concentration of AB4， but it did not increase significantly after reaching 50 μmol/L； it increased with the increase of time， but it did not increase significantly after 24 h. The IC50 of AB4 was （56.76±1.756） μmol/L. Compared with negative control group， the number of clone cells was decreased significantly after Huh-7 cells were treated with 50 μmol/L AB4 for 24 h， while the protein expression of Bcl-2 was decreased significantly （P＜0.05）； the apoptotic rate， the protein expression of Bax， Caspase-3， Cleaved Caspase-3 and Cleaved PARP were increased significantly （P＜0.05 or P＜0.01）， there was no statistical significance， compared with positive control group. Compared with negative control group， the volume of tumor was decreased significantly in AB4 low-dose， medium-dose and high-dose groups， positive control group （P＜0.05）； the outline of tumor cells become more and more blurred； there were nuclear pyknosis， unclear nucleoplasm and nuclear fragmentation； its anti-tumor rates were 25.93％， 39.15％， 46.26％， 42.83％， respectively. CONCLUSIONS： AB4 inhibits Huh-7 cells and tumor-bearing mice， the mechanism of which may be associated with up-regulating the proportion of Bax/Bcl-2， activating Caspase-3， cracking PARP and inducing apoptosis.

Phytochemical Constituents of the Root Bark from Morus alba and Their Il-6 Inhibitory Activity

Morus alba L., known as white mulberry, is a medicinal plant belongs to family Moraceae. It has long been used commonly in Ayurvedic for the treatment of lung-heat, cough, asthma, hematemesis, dropsy and hypertension. In the present study, seven prenylated flavonoids, along with four benzofuran compounds were isolated by means of repeated column chromatography. The structures of the known compounds were identified as kuwanon G (1), kuwanon E (2), kuwanon T (3), morusin (4), sanggenon A (5), sanggenon M (6), sanggenol A (7), moracin R (8), mulberofuran G (9), mulberofuran A (10) and mulberofuran B (11), by comparing their spectroscopic data with those reported in the literature. For these isolates, containing trace compounds, the inhibitory activity against IL-6 production in TNF-α stimulated MG-63 cells was examined. All isolated compounds (1

The inhibitory effect of decorin on apoptosis of human lens epithelial cells under high glucose condition and its mechanism / 中华实验眼科杂志

Objective To investigate the effects of decorin (DCN) on apoptosis and oxidative stress in human lens epithelial cells (LECs) under high glucose condition.Methods HLE-B3 cells were cultured in vitro and the effect of DCN with different concentrations on HLE-B3 viability was determined by using cell counting kit-8 (CCK-8).The cultured cells were divided into normal control group,DCN group,high glucose group and DCN + high glucose group.Flow cytometry was used to detect the apoptosis rate and the expression of reactive oxygen species (ROS) in the cells.Microplate spectrophotometer was used to measure total superoxide dismutase (SOD) enzyme activity and the radio of glutathione (GSH)/glutathione disulfide (GSSG).Western blot was used to detect the expressions of bax and bcl-2 proteins.Results HLE-B3 cells were spindle shaped,with centered and clearly visible nuclei and neatly cell arrangment.According to CCK-8 method,survival rates of HLE-B3 in all groups were more than 90％.Different concentrations of DCN showed no significant effect on HLEoB3 survival rate (all at P＞0.05).After 48 hours of cell culture,the apoptosis rate of high glucose group was significantly higher than that of normal control group,and the apoptosis rate of DCN+high glucose group was significantly lower than that of high glucose group (both at P =0.000).The mean fluorescence intensity of intracellular ROS in the high-glucose group was significantly higher than that in the normal control group,and the mean fluorescence intensity of ROS in the DCN group was significantly higher than that in the high glucose group (both at P=0.000).The total SOD activity in the high glucose group was significantly lower than that in the normal control group and DCN group (P =0.007,0.004).The GSH/GSSG ratio of the high-glucose group was significantly lower than that of the normal control group and DCN group (both at P=0.000).Conclusions DCN can inhibit the apoptosis and oxidative stress of HLE-B3 under high glucose,which provides the basis for the treatment of diabetic cataract.

Antioxidant and Anti Cholinesterase Potential of Red Cabbage (Brassica oleracea var. capitata f. rubra)

Aim: This study aims at in-vitro evaluation of Red cabbage extracts for their antioxidant and anticholinesterase activity. Methodology: Red cabbage collected from the local market was dried and extracted with different solvents. Qualitative and quantitative phytochemical screening of these extracts was done. Then the Resulting extracts were evaluated for antioxidant activity using DPPH and H2O2 scavenging at various concentrations. Anticholinesterase activity was assessed qualitatively using TLC autobiography. Conclusions: Maximum antioxidant activity was found with methanolic extract and Maximum anticholinesterase activity is found with Hexane extract.

Inhibitory effect of recombinant oncolytic adenovirus on luciferase-labeled and non-labeled human lung cancerA549 cells / 中国肿瘤生物治疗杂志

@# Objective: To investigate the inhibitory effect of recombinant oncolytic adenovirusAd-Apoptin-hTERTp-E1A(ATV) on luciferase-labeled human lung cancer cells (A549-luc) and human lung cancerA549 cells, and to compare the differences in the inhibitory effect on two cell lines. Methods:ATV was used to infectA549-luc cells andA549 cells respectively. WST-1 and crystal violet staining were used to determine the difference in the inhibitory effect of ATV. Hoechst and Annexin V-FITC/PI staining were used to verify the inhibition mode ofATV. Results: WST-1 and crystal violet staining showed thatATV had significant inhibitory effect on bothA549-luc and A549 cells ( P <0.05). ATV showed significant inhibitory effect on both cells at 24, 48 and 72 h ( P <0.05 or P <0.01), and reached the peak at 72 h; ATV at concentrations of 1, 10 and 100 MOI all showed inhibitory effect on both cells, and reached the peak at 100 MOI. Hoechst staining showed that A549-luc cells and A549 cells infected with ATV showed typical nuclear fragmentation and marginal set. The results of Annexin V-FITC/PI Flow cytometry showed that ATV infection resulted in apoptosis of A549-luc and A549 cells, which was in a time-dependent manner and reached the peak at 72 h( P <0.05 or P <0.01). Conclusion: Insertion of luciferase didn’t significantly change the inhibitory effect and inhibitory mode ofATV onA549-luc cells.ATV exerted its in vitro inhibitory effect onA549-luc and A549 cells by inducing cell apoptosis.

Quality Characteristics of Care Food (Jelly) Prepared with Wild Carrot (Daucus carota L.) Juice

This study evaluated the quality characteristics of jelly prepared with different levels (0%, 5%, 10%, 15%, 20%, and 25%) of wild carrot (WC, Daucus carota L.) juice as a care food for the elderly. The lightness, redness, yellowness, and delta (Δ) values of the jelly (Control, WCJ5, WCJ10, WCJ15, WCJ20, and WCJ25) decreased with increasing amounts of wild carrot juice added. The mechanical properties, such as hardness, springiness, chewiness, and gumminess, of the jelly were decreased with increasing amounts of wild carrot juice added. The total polyphenol and total flavonoid contents of the jelly increased with increasing amounts of wild carrot juice added. The DPPH radical scavenging activity (IC50) also increased with increasing amounts of wild carrot juice added. The α-glucosidase inhibitory effects of wild carrot (WC) and WCJ25 were 71% and 54.4%, respectively, compared to the positive control (acarbose). The lipase inhibitory effects of WC and WCJ25 were 44.2% and 14.4%, respectively, compared to the positive control group (orlistat). On the other hand, the sensory evaluation score was the best at WCJ20, which contained 20% wild carrot juice. In conclusion, WCJ20 or WCJ25 is expected to be a care food for the elderly with respect to texture as well as the antioxidant and enzymatic activity (α-glucosidase inhibitory and lipase inhibitory activities).

Experimental study on the inhibitory effect of soap solution on rabies viruses / 中华实验和临床病毒学杂志

Objective@#To investigate the inactivating effect of soap solution on rabies virus and to explore the concentration of soap solutions which could be effective in post-exposure prophylaxis (PEP) of rabies virus infection.@*Methods@#The BSR and N2a cells were respectively infected by the mixture of different concentrations of soap solution and rabies virus CVS-11. Based on the direct immunofluorescent method (DFA) and reverse transcription PCR (RT-PCR), the inactivating effects of soap solutions on rabies viruse in BSR and N2a cells were detected, respectively.@*Results@#This experiment established the BSR or N2a cells model in 24 well cell culture plates, and we found that the upper limit of soap solution concentration which BSR or N2a cells could tolerate was 1%. The inhibitory effect test of different soap solution on rabies virus showed that the 0.5% concentration of soap solution could completely inhibit the survival of CVS-11 strain in both the BSR and N2a cells, but the 0.1% concentration of soap solution could not inhibit the rabies viruses completely.@*Conclusions@#The 0.5%-1% concentration of soap solutions could inhibit the survival of CVS-11 strain in three minutes in vivo experiment.

Acetylcholinesterase Inhibitors from Angelica polymorpha Stem

Fourteen compounds were isolated from the stem of Angelica polymorpha. On the basis of spectral data, these compounds were identified as isoimperatorin (1), phellopterin (2), bergapten (3), xanthyletin (4), cnidilin (5), geijerine (6), (−)-3'-acetyl hamaudol (7), 7-demethylsuberosine (8), dehydrogeijerin (9), (−)-hamaudol (10), (+)-visamminol (11), divaricatol (12), scopoletin (13), and decursidate (14), respectively. Among them, compounds 4 - 6, 8, 9, 13, and 14 were isolated for the first time from A. polymorpha. Dehydrogeijerin (6) and geijerin (9) were isolated for the first time from genus Angelica. All isolates tested for inhibitory activity against acetylcholinesterae. Compounds 1 to 13 showed acetylcholinesterase inhibitory activity with IC₅₀ values ranging from 1.4 to 37.5 µM.

Effects of Resistant Maltodextrin on the on Post-Prandial Blood Glucose Elevation in Japanese Individuals / 医薬品情報学

<b>Objective: </b>We conducted a meta-analysis on the suppressive effect of resistant maltodextrin on post-prandial blood glucose elevation, which is approved in Japan as food for specified health use, and the following is allowed to be indicated on the label “it is suitable for consumption by those who are concerned about their post-prandial blood glucose levels because the absorption of sugars is abated by the action of dietary fiber (resistant maltodextrin).”<br><b>Method: </b>Our literature search covered Ichushi-Web (Japan Medical Abstracts Society), Japan Science and Technology Information Aggregator, Electronic (J-stage), Google Scholar, and PubMed databases and extracted English and Japanese publications on randomized, double-blind, controlled studies comparing resistant maltodextrin and a control in Japanese subjects for the reduction of areas under the blood glucose response curves at 30, 60, and 120 min after eating as an efficacy index.<br><b>Result: </b>Among these publications, four articles with a Jadad score (an assessment of the quality of randomized controlled studies) of ≥ 3 were included in the meta-analysis.  Significant inhibitory effects were confirmed from areas under the blood glucose response curves at 30, 60, and 120 min after eating in the meta-analysis that was performed to evaluate the effects of resistant maltodextrin on post-prandial blood glucose elevation in Japanese individuals.<br><b>Conclusion: </b>However, we were not able to test for publication bias because the number of extracted publications was small, and thus, additional research and case studies are warranted.

Inhibitory Effect of Total Alkaloids from Lotus Seed on Human Hepatoma Cells / 中国药师

Objective: To study the inhibitory effect of total alkaloids from lotus seed on human hepatoma HepG2 cells.Methods: The effect of total alkaloids from lotus seed on the growth of HepG2 cells was studied by CCK-8 kit.The apoptosis rate of HepG2 cells was detected by flow cytometry.Results: When the action time was the same, with the increase of drug concentration, the inhibitory rate of total alkaloids from lotus seed on HepG2 cells increased, in a dose-dependent manner.At 72 h, the half inhibitory concentration (IC50) of total alkaloids from lotus seed on HepG2 cells was 1.501 μg·ml-1.At the same concentration, the inhibitory rate of the total alkaloids from lotus seed on HepG2 cells increased with the extension of the action time.At 72 h, the inhibition rate of 10 μg·ml-1 total alkaloids from lotus seed reached 72%.After treated with the total alkaloids from lotus seed at different concentrations, the apoptosis rate of HepG2 cells significantly increased in a dose-dependent manner.Compared with the blank control group, the difference was statistically significant (P <0.05), and the apoptosis rate of HepG2 cells was 85.6% treated with 20 μg·ml-1 total alkaloids from lotus seed.Conclusion: The total alkaloids from lotus seed can induce cell apoptosis and inhibit the proliferation of human hepatoma HepG2 cells.

Inhibitory effect of galangin on polyphenol oxidase and study of mechanism / 中国免疫学杂志

Objective:To investigated the activity inhibition and inhibitory type of polyphenol oxidase (PPO) induced by galangin and the interaction mechanism of galangin with polyphenol oxidase was preliminarily indicated,and prove the related mechanism of galangin on proliferation of on human melanoma A375 cells.Methods: The activity inhibition and inhibitory type of PPO induced by galangin were investigated by spectrophotometric method,and interation mechanism of galangin with PPO was preliminarily indicated by fluorescence quenching and molecular docking,and chelating copper ions with the inhibitory mechanism of galangin on polyphenol oxidase was measured.Results: Galangin was a competitive inhibitor,the IC50 and Ki on PPO were obtained to be (47.86±3.33) and (24.83±1.45)μmol/L,respectively.Fluorescence spectrum indicated the fluorescence of PPO was quenched effectively by galangin and the binding constant Ka was obtained to be (4.67±0.43)×104 L/mol.Chelating copper ions and molecular simulation further showed that galangin was combined with active center of copper ions,and formed hydrogen bonds with catalytic site His259.Luteolin could induce the apoptosis of A375 cells significantly,and the tyrosinase activity and melanin synthesis were decreased.Conclusion: Galangin as a competitive polyphenol oxidase inhibitor and reduced the activity of polyphenol oxidase.which provides the theoretical basis for the clinical anti skin cancer.