Network pharmacology and molecular docking reveal the mechanism of resveratrol in oral squamous cell carcinoma treatment / 口腔疾病防治

Objective@#To explore the molecular mechanism of resveratrol (RES) in the treatment of oral squamous cell carcinoma (OSCC) through the use of biological information methods such as network pharmacology and molecular docking and to provide a theoretical reference for the clinical application of RES in the treatment of OSCC.@*Methods@#The Swiss Target Prediction(http://www.swisstargetprediction.ch), SEA (http://sea.bkslab.org)database, and Pharm mapper database(http://lilab-ecust.cn) were used to retrieve RES-related targets, and the DISGENET (www.disgenet.org), OMIM (https://omim.org) and GeneCards (https://www.genecards.org) databases were used to screen OSCC disease targets. The intersection of drugs and disease targets was determined, and Cytoscape 3.7.2 software was used to construct a "drug-diseasetarget pathway" network. The Search Tool for the Retrieval of Interacting Genes/Proteins (STRING) database was used to construct a target protein interaction network, and the DAVID database was used for enrichment analysis of key proteins. Finally, molecular docking validation of key proteins was performed using AutoDock and PyMOL. The enrichment analysis and molecular docking results were integrated to predict the possible molecular mechanisms of RES treatment in OSCC; western blot was used to determine the effect of resveratrol at different concentrations (50, 100) μmol/L on the expression of Src tyrosine kinase (SRC), epidermal growth factor receptor (EGFR), estrogen receptor gene 1 (ESR1), and phosphatidylinositol 3 kinase/protein kinase B (PI3K/AKT) signaling pathway proteins in OSCC HSC-3 cells.@*Results@#A total of 243 targets of RES drugs and 6 094 targets of OSCC were identified. A total of 116 potential common targets were obtained by intersecting drugs with disease targets. These potential targets mainly participate in biological processes such as in vivo protein self-phosphorylation, peptide tyrosine phosphorylation, transmembrane receptor protein tyrosine kinase signaling pathway, and positive regulation of RNA polymerase Ⅱ promoter transcription, and they interfere with the PI3K/AKT signaling pathway to exert anti-OSCC effects. The docking results of resveratrol with OSCC molecules indicated that key targets, such as EGFR, ESR1, and SRC, have good binding activity. The results of cell-based experiments showed that resveratrol inhibited the protein expression of SRC, EGFR, ESR1, p-PI3K, and p-AKT in HSC-3 cells in a dose-dependent manner.@*Conclusion@#RES can inhibit the expression of its targets EGFR, ESR1, SRC, p-PI3K, and p-AKT in OSCC cells.

Application of platelet-rich fibrin grafts in pterygium excision / 国际眼科杂志(Guoji Yanke Zazhi)

@#AIM: To compare the effect of platelet-rich fibrin(PRF)grafts and conjunctival-limbal autografts in pterygium excision.<p>METHODS: Totally 62 cases(62 eyes)of primary pterygium were randomly divided into group 1(32 eyes)and group 2(30 eyes). After pterygium excision, conjunctival-limbal autografts was performed in group 1 and PRF grafts was performed in group 2. PRF was prepared by centrifugation and compression of venous blood from patients before the surgery. The follow-up period was 6mo. The surgery time, complications and recurrence rate were evaluated and compared between the two groups.<p>RESULTS: The operation time of group 1 and group 2 were 27.3±4.3min and 22.0±4.0min respectively. There was significant difference between the two groups(<i>t</i>=4.990, <i>P</i><0.01). Conjunctival granuloma developed only in one eye in group 2 after the surgery, and there was no significant difference between group 1 and group 2(<i>P</i>=0.484). Pterygium recurred in one eye in group 1 and in one eye in group 2. There was also no significant difference in recurrence rate between group 1 and group 2(<i>P</i>=1.000). There was no significant difference in intraocular pressure between group 1 with 14.69±2.44mmHg and group 2 with 14.96±2.93mmHg before the surgery(<i>t</i>=0.399, <i>P</i>=0.691). As well, there was no significant difference in intraocular pressure between group 1 with 14.68±1.65mmHg and group 2 with 15.11±2.12mmHg after the surgery(<i>t</i>=0.888, <i>P</i>=0.378). The dissolution time of PRF membrane in PRF grafts group was 3.5±0.8d.<p>CONCLUSION: The use of PRF in pterygium surgery is safe, effective, easier and timesaving. It's a promising method for clinical application.

Coexistence of resistance to thyroid hormone and ectopic thyroid: ten-year follow-up

SUMMARY Resistance to thyroid hormone (RTH) coexisting with ectopic thyroid is rare. Here we report a case of RTH with ectopic thyroid. A ten-year-old girl had been misdiagnosed as congenital hypothyroidism and treated with levothyroxine since she was born. Ten-year follow-up showed that the elevated thyrotropin was never suppressed by levothyroxine and no signs indicating hyperthyroidism or hypothyroidism despite elevated FT3 and FT4 levels. Therefore the girl developed no defects in physical and cognitive development. Pituitary adenoma was excluded by magnetic resonance imaging. Ultrasonography did not find the thyroid gland in the normal place, while the thyroid scan found a large lingual thyroid gland. The octreotide inhibition test showed a reduction in thyrotropin by 41.98%. No mutation was detected in the thyroid hormone receptor (THR) β, THRα, thyrotropin receptor (TSHR), and GNAS1 genes. To our knowledge, it is an interesting RTH case coexisting with lingual thyroid.

Pharmacokinetics studies of ginsenoside Rb1 in rats / 中国药学杂志

OBJECTIVE: To develop a highly snsitive and specific LC-MS/MS method to explore the pharmacokinetic propeties of ginsenoside Rb1. METHODS: Ginsenoside Rb1 dissolved in normal saline was administered in a dose of 100 mg·kg-1 via gastric in fusion and 10 mg·kg-1 by intravenous injection in rats. Plasma was collected from fundus oculi venous plexus and ginsenoside Rb1 was analyzed by a validated LC-MS/MS method in plasma after intravenous and oral administration. The pharmacokinetic parameters were evaluated by software PKSolver V2.0. RESULTS: The main pharmacokinetic parameters of ginsenoside Rb1 after oral administration of 100 mg·kg-1 dosage were as follows: ρmax (2.01 ± 0.93) μg·mL-1, tmax (7.20 ± 5.49) h, t1/2 (25.91 ± 15.84) h, AUC0~96h (88.47 ± 58.99) μg·h·mL-1. The main pharmacokinetic parameters of ginsenoside Rb1 after intravenous administration of 10 mg ·kg-1 dosage were as follows: ρmax (194.81 ± 28.84) μg·mL-1, t1/2α (0.18 ± 0.05) h, t1/2β (14.66 ± 4.19) h, AUC0~96h (1671.16 ± 388.91) μg·h·mL-1. CONCLUSION: The ginsenoside Rb1 of orally administered was 0.62%, shows poor absolute bioavailability, and intravenous injection directly distribute into the blood vessels, can be the priority.

Research progress in pharmacological activities of ginsenoside Rb1 / 中国药学杂志

OBJECTIVE: To review the pharmacological effects of ginsenoside Rb1 research progress. METHODS: According to domestic and foreign research reports of ginsenoside Rb1 in recent years, the pharmacological effects of Rb1 research progress. RESULTS: This article reviewed pharmacological effects and pharmacokinetic research of ginsenosides Rb1 from the central nervous system, cardiovascular system, immune system, and anti-tumor, anti-hepatic warm ischemia-reperfusion, lowering blood sugar and other aspects. CONCLUSION: Ginsenoside Rb1 is an important chemical material with a lot of pharmacological activities, studying its pharmacological effects can provide relevant information for further its development and utilization.

Synthesis, solubility, lipids-lowering and liver-protection activities of sulfonated formononetin / 药学学报

A water-soluble compound, sodium formononetin-3'-sulfonate with good lipid-lowering and liver-protection activities was synthesized. It was synthesized by sulfonation reaction, and its structure was characterized by IR, NMR and elemental analyses. The solubility of sodium formononetin-3'-sulfonate in water and n-octanol/water partition coefficient were determined by UV spectrophotometry. The lipid-lowering and liver-protection activities of sodium formononetin-3'-sulfonate were tested by using rat's high fat model induce by feeding with high fat food. The results showed that sodium formononetin-3'-sulfonate not only had favorable water, solubility but also had good lipid-lowering and liver-protection activities.