Mutual Information Entropy Analysis of Compatibility of Traditional Chinese Patent Medicines Against Liver Diseases in Chinese Pharmacopoeia（2020 Edition） / 中国实验方剂学杂志

ObjectiveTo investigate the compatibility rule of traditional Chinese patent medicines （TCPMs） against liver diseases through network analysis. MethodWith “liver” as the search term， TCPMs against liver diseases were retrieved from volume Ⅰ of Chinese Pharmacopoeia （2020 edition）， and the basic information of them was collected. TCPMs with same Chinese medicinal materials （CMMs）， usage， and indications， but different dosage forms， were unified as one formula. Mutual information entropy （MIE） of CMM couples was calculated to quantify the relationship between them， and the top 25% CMM pairs in MIE were used to construct the compatibility network， with CMM as node and the relationship between CMM pairs as the edge. Key CMM and frequently used CMM combinations were identified based on node centrality and cluster analysis， respectively. The indications of TCPMs related to the CMMs in clusters were recorded. Cytoscape 3.6.1 was employed for visualization and topology analysis of the compatibility network. ResultA total of 179 TCPMs， involving 428 CMMs， were retrieved. Angelicae Sinensis Radix， Paeoniae Radix Alba， and Glycyrrhizae Radix et Rhizoma were identified as key CMMs with high frequency， and Cuscutae Semen-Lycii Fructus， Citri Reticulatae Pericarpium-Cyperi Rhizoma， and Ecliptae Herba-Ligustri Lucidi Fructus combinations had high MIE. Furthermore， the CMMs were clustered into ten groups corresponding to different diseases which， however， all belonged to digestive diseases. ConclusionThis study unveils potential CMM pairs and common CMM combinations against liver diseases， which can serve as a reference for revealing compatibility rules of CMMs and research and development of Chinese medicine.

Comparison of Effect of Fine Powder and Ultrafine Powder of Dendrobium nobile Stem on Intestinal Transporters of Rats / 中国实验方剂学杂志

Objective:To compare the contents of alkaloids from fine and ultrafine powder of Dendrobium nobile stem in rat plasma,and investigate the effect of D. nobile stem with different particle sizes on gene expression of intestinal transporters. Method:Rats were randomly divided into the blank group,fine powder group of D. nobile stem(0.25 g·kg-1) and ultrafine powder group of D. nobile stem(0.25 g·kg-1).The rats were gavaged every 6 h for 5 days.The samples of rat plasma and small intestine were collected.The plasma samples were detected with UPLC-MS.The chromatography separation was performed on a Hypersil Gold C18 column(2.1 mm×150 mm,1.9 μm) with acetonitrile-0.1%formic acid solution as mobile phase for gradient elution.Electrospray ionization (ESI) was applied and operated in positive ion mode.The mRNA expression of multidrug resistance protein 1(MDR1),oligopeptide transporter protein 1(PEPT1),organic cation transporter protein 2(OCT2),breast cancer resistance protein 1(BCRP1),monocarboxylate transport protein 1(MCT1) and multidrug resistance related protein 2(MRP2) in small intestine were quantified by real time fluorescence quantitative polymerase chain reaction. Result:After intragastric administration of fine and ultrafine powder of D. nobile stem,dendrobine,mubironine B and dendramine could be detected in rat plasma.The contents of dendrobine and dendramine in the ultrafine powder group were significantly higher than that in the fine powder group(PD. nobile stem(PPD. nobile stem(PConclusion:Compared with the fine powder group of D. nobile stem,the plasma concentrations of dendrobine and dendramine in the ultrafine powder group are significantly increased,it may be related to the intestinal transporters of MDR1 and BCRP1.These results can provide experimental basis for selecting particle size of D. nobile stem.

A new bibenzyl compound from Dendrobium nobile / 药学学报

In this study, seven bibenzyl compounds were isolated from the stem of Dendrobium nobile by silica gel, MCI column chromatographic and preparative HPLC technology. By using spectroscopic techniques including NMR and MS, these compounds were identified as 4, α-dihydroxy-3, 5, 3'-trimethoxybibenzyl (1), 4, 5-dihydroxy-3, 3', α-trimethoxybibenzyl (2), 4, 4'-dihydroxy-3, 5, 3'-trimethoxybibenzyl (3), 4, 5-dihydroxy-3, 3'-dimethoxybibenzyl (4), 4, 3'-dihydroxy-3, 5-dimethoxybibenzyl (5), 5, 4'-dihydroxy-3, 3'-dimethoxybibenzyl (6) and 5, 3'-dihydroxy-3-methoxybibenzyl (7). Compound 1 is a new compound and compound 4 was isolated from this plant for the first time.

Factors for Endoscopic Submucosal Dissection in Early Colorectal Neoplasms: A Single Center Clinical Experience in China

BACKGROUND/AIMS: Early colorectal (CR) neoplasm can be cured by endoscopic submucosal dissection (ESD), but clinical experience and factors associated with complications from ESD for CR neoplasms in China have not been reported. METHODS: Seventy-eight cases of early CR neoplasm treated with endoscopic resection performed between December 2012 and December 2013 at Beijing Military General Hospital were included. Factors associated with ESD complications and procedure times were evaluated. RESULTS: The en bloc resection rate was 88.5% (69/78), tumor size was 32.1+/-10.7 mm, and procedure time was 71.8+/-49.5 minutes. The major complication was perforation, which occurred in 8.97% of the ESD procedures. Multivariate logistic regression analysis indicated that only tumor size (p=0.022) was associated with ESD perforation. Tumor size (p<0.001) and the non-lifting sign (p=0.017) were independent factors for procedure time, and procedure time (p=0.016) was a key factor for en bloc resection. After a median 10 months (range, 4 to 16) of follow-up, no patients had local recurrence. CONCLUSIONS: This study indicated that ESD is an applicable method for large early CR neoplasm in the colon and rectum. Tumor size and the non-lifting sign might be considerable factors for increased complication rate and procedural time of ESD.

miR-29b Reduces Cisplatin Resistance of Gastric Cancer Cell by Targeting PI3K/Akt Pathway / 中国医学科学院学报

<p><b>OBJECTIVE</b>To investigate the regulatory effect of miR-29b on gastric cells' resistance to cisplatin.</p><p><b>METHODS</b>The expression of miR-29b in gastric cancer cell line treated with cisplatin concentration gradient was detected using quantitative reverse-transcriptase polymerase chain reaction (qRT-PCR) and Western blotting. CCK8 was used to measure the cell viability after cisplatin treatment in condition of miR-29b knock-down and overexpression.</p><p><b>RESULTS</b>The expression of miR-29b was significantly upregualted by cisplatin treatment,while its target gene AKT2 was downregulated. The up-regulation of miR-29b enhanced the sensitivity of gastric cancer cells to cisplatin,while the knock-down of miR-29b enhanced the cisplatin resistance. Rescue experiments demonstrated that the miR-29b might regulate cisplatin resistance of gastric cancer cell by targeting PI3K/Akt pathway. The expressions of the other two members of miR-29 family, miR-29a/c, were promoted by cisplatin treatment,but they had no significant effect on gastric cancer cell's resistance to cisplatin.</p><p><b>CONCLUSION</b>miR-29b can enhance the sensitivity of S gastric cancer cell by directly targeting PI3K/Akt pathway.</p>

Estradiol regulates miR-135b and mismatch repair gene expressions via estrogen receptor-beta in colorectal cells

Estrogen has anti-colorectal cancer effects which are thought to be mediated by mismatch repair gene (MMR) activity. Estrogen receptor (ER) expression is associated with microRNA (miRNA) expression in ER-positive tumors. However, studies of direct link between estrogen (especially estradiol E2), miRNA expression, and MMR in colorectal cancer (CRC) have not been done. In this study, we first evaluated the effects of estradiol (E2) and its antagonist ICI182,780 on the expression of miRNAs (miR-31, miR-155 and miR-135b) using COLO205, SW480 and MCF-7 cell lines, followed by examining the association of tissue miRNA expression and serum E2 levels using samples collected from 18 colorectal cancer patients. E2 inhibited the expressions of miRNAs in COLO205 cells, which could be reversed by E2 antagonist ICI 182.780. The expression of miR-135b was inversely correlated with serum E2 level and ER-beta mRNA expression in CRC patients' cancer tissues. There were significant correlations between serum E2 level and expression of ER-beta, miR-135b, and MMR in colon cancer tissue. This study suggests that the effects of estrogen on MMR function may be related to regulating miRNA expression via ER-beta, which may be the basis for the anti-cancer effect in colorectal cells.

Identification of metabolites of nobiletin in rats using ultra-performance liquid chromatography coupled with triple-quadrupole mass spectrometry / 药学学报

In this study, metabolism of nobiletin in rats was studied using ultra-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS). As a result, seven major metabolites were found in bile, urine and serum of rats. Three phase I products were assigned to be demethyl and di-demethyl products, and other four phase II products were assigned to be glucuronic and sulfonic conjugates. The four phase II metabolites were reported for the first time. Among the metabolites found in the present study, the glucuronic conjugates of demethyl-nobiletin played a predominant role in the metabolic pathway, indicating that its potential role for glucuronidation-related factors, such as gene polymorphism, drug-drug interaction, etc., in changing the active and toxic effect of nobiletin and that it should be paid more attention in further development.