Latest ArticlesTo predict the mechanism of Polygonum multiflorum Thunb. on attenuating lipid metabolism disorder by applying Network Pharmacology and Molecular Docking.
Using software ChemDraw, the chemical constituents of Polygonum multiflorum Thunb. were drawn and documented. Main active ingredients and potential targets of attenuating lipid metabolism disorder were screened out based on the databases like Swiss ADME, Swiss Target Prediction platform and Genecards, and DisGeNET. The drug-active ingredients-potential targets network structure model and PPI network are constructed through the software Cytoscape and STRING database, respectively. Potential targets were analyzed by GO enrichment analysis, KEGG pathway enrichment analysis and visualized. Using software PyMOL and AutoDock, the active ingredients were docked with core target molecules. The body weight and body fat rate of APP/PS1 mice with long-term intragastric administration were measured and the content of serum lipid (TG, TC, HDL-C, LDL-C) were detected.
A total of 30 active ingredients of Polygonum multiflorum Thunb. and 143 potential targets for the treatment of lipid metabolism disorder were obtained. The enrichment analysis shows that the common biological process of Polygonum multiflorum Thunb. and metabolic disorders are related to protein phosphorylation, protein binding, enzyme binding, protein kinase activity biological processes, and the signalling pathways of PI3K-Akt, HIF-1, estrogen are mainly involved in the major therapeutic role. Molecular docking predicts the stable connection structure between the active component and the core targets. The results of animal experiments showed that compared with the model group, there was no significant difference in weight between drug administered groups and the body fat rate decreased significantly (P<0.05). Steaming and sun-buring products had significant effect on the abnormal increase of TG and LDL-C, but crude Polygonum multiflorum Thunb. only had an impact on TG (P<0.05).
Polygonum multiflorum Thunb. has an significant lipid-attenuating effect. The mechanism is predicted to be related with three main active ingredients, including omega-hydroxytroxanin-8-methyl ether, Tricin and Kaempferolare, and PI3K-Akt, HIF-1 and Estrogen signaling pathways are affected through three core targets of EGFR, ESR1 and MMP9.
In recent years, pediatric clinical research has been strongly supported by the state in China. The participation of characteristic pediatric clinical research coordinator (CRC) in pediatric clinical research is urgently in need. However, due to the particularity of pediatric patients, pediatric CRC may face a higher dilemma than that of adult clinical research. This article summarizes the basic situation of pediatric CRC in China, analyzes the difficulties faced by pediatric CRC in combination with our own experience, and the possible solutions are put forward. We hope to promote the healthy development of pediatric CRC industry, which can further ensure the quality of clinical trials.
To extract and separate polysaccharide from Sophora tonkinensis Radix et Rhizoma (SRP), determine the monosaccharide composition and content of SRP, and investigate the antitumor effects of SRP in vitro.
SRP was prepared by water extraction and alcohol precipitation. The contents of polysaccharides, flavonoids, saponins, total phenols and proteins in SRP were determined by UV-Vis spectrophotometry, the contents of alkaloids were determined by high performance liquid chromatography (HPLC), and the content of organic acid was measured by back titration method. The monosaccharide analysis method of SRP was established by HPLC. A Waters X Bridge C18 column (250 mm×4.6 mm,5 μm) was used with acetonitrile: phosphate buffer (0.05 mol·L-1, pH=6.8) at the ration of 18∶82 as mobile phase, the flow rate was 0.8 mL·min-1, the column temperature was 30 ℃, and the detection wavelength was 245 nm. The contents of monosaccharides in SRP were determined and the mole ratio was calculated. MTT assay was used to detect the antitumor effects of SRP in vitro.
SRP, which is brown powder, was obtained by water extraction and alcohol precipitation with a yield of 3.95%. The contents of polysaccharides, flavonoids, saponins, organic acids and total phenols in SRP were 66.08%, 7.17%, 3.45%, 2.54% and 4.33%, respectively. No alkaloids and proteins were detected. SRP was composed of mannose, rhamnose, glucuronic acid, galacturonic acid, glucose, galactose and arabinose. The mole ratios were 1.25∶0.31∶0.28∶0.50∶40.47∶1.00∶10.46, and the percentage of polysaccharide was 64.97%. SRP had inhibitory effect on Hepa1-6, HepG2, HT29 and 4T1 cells in a concentration-dependent manner with IC50 of 770, 1 910, 1 870 and 1 880 μg·mL-1, respectively.
The SRP prepared in this study contained more than 60% polysaccharide and more than 80% known components, among which no alkaloids were detected. HPLC with pre-column derivatization of 1-phenyl-3-methyl-5-pyrazolo has good precision, reproducibility and accuracy, and is suitable for the monosaccharide composion analysis of SRP polysaccharides. SRP is a kind of heteroglycan with glucose and arabinose as the main components. SRP has significant cytotoxic effect by inhibiting tumor cell proliferation, suggesting that it may play a anti-tumor role. This study provides a reference for advancing the basic research of the composition and antitumor effect of SRP.
Tumor immunotherapy is a major breakthrough in the history of tumor therapy. New immunooncological drugs targeting PD-1/PD-L1 and CAR-T cells have achieved gratifying clinical efficacy. However, due to the complexity and particularity of tumor immune microenvironment, it is difficult for a single target treatment mode to achieve a lasting response. Recurrence, metastasis and resistance are still difficult for most advanced cancer patients to overcome. Recently, PD-(L)1/TGF-β bispecific antibodies have become a hot spot in the research of tumor immunomodulatory drugs, which contains two functional domains and interacts with PD-(L)1 and TGF-β simultaneously to restore the activity of T cells and enhance the immune response. This paper mainly analyzes the clinical research progress of PD-(L)1/TGF-β bifunctional antibodies, which have been developing rapidly in recent years. We further analyze the existing problems and make an outlook on the prospect of dual-target tumor immunotherapy, in order to provide basis and reference for bifunctional or multifunctional drugs.
To explore and analyze the clinical efficacy and safety of doxazosin mesylate sustained release tablets in the treatment of postoperative bladder spasm after electroprostatectomy (TURP).
A total of 110 patients receiving TURP admitted to our hospital from March 2020 to May 2022 were selected and randomly divided into control and observation groups, with 55 cases in each group. The control group was treated with doxazosin mesylate sustained release tablets after TURP operation, and the observation group was treated with diclofenac sodium supposal anal plug on the basis of oral treatment. The results of occurrence time and frequency of postoperative bladder spasm, visual analog scale (VAS), duration of bladder flushing solution dilution, catheter indwelling time, postoperative hospital stay and incidence of adverse reactions were compared between the two groups.
In the observation group, the duration of postoperative bladder spasm was shorter, the frequency was less, and the VAS score was lower than that in the control group 0 to 24 h, 24 to 78 h and 48 to 72 h after surgery, with statistically significant differences (P<0.05). Compared with the control group, the observation group had a significantly shorter duration of bladder flushing fluid dilution, catheter indwelling time and postoperative hospital stay (P<0.05). There was no significant difference in the incidence of postoperative adverse reactions between the two groups (P>0.05).
The application of doxazosin mesylate combined with diclofenac sodium in the treatment of postoperative bladder spasm after TURP has a singnificant effectwith high safety. It can effectively shorten the occurrence time of bladder spasm, reduce the frequency of incidence, relieve the degree of pain and shorten the duration of clinical symptoms. There is no obvious adverse reactions during medication.
To prepare and evaluate the polymer micellar thermosensitive gel of Chinese medicine chrysanthemum volatile oil.
The polymer micelles were prepared by the ethanol injection method, and the preparation process was optimized by orthogonal experiments. The morphology, particle size and zeta potential of the polymer micelles were evaluated. The thermosensitive gel was further prepared using poloxamer 407 and poloxamer 188 as the matrix. The rheological properties of the thermosensitive gel were measured by a flat plate rheometer, the irritability of the thermosensitive gel to rabbit eyes was investigated using Draize eye irritation score, and eye tissues were examined by pathological examination.
The optimal preparation process of Chinese medicine chrysanthemum volatile oil polymer micelles thermosensitive gel was as follows: the concentration of chrysanthemum volatile oil was 15 μL·mL-1, the mass ratio of surfactant (TPGS∶phospholipid) was 3∶2, the concentration of surfactant was 37.5 mg·mL-1, and the mass ratio of phospholipids (HSPC∶DSPE-PEG2000) was 1∶1. The polymer micelles were closely arranged, spherical or quasi-spherical with the average particle size of (58.60±2.37) nm and zeta potential of (0.197±0.045) mV. The thermosensitive gel prepared with 21% mass fraction of poloxamer 407 and 3% mass fraction of poloxamer 188 was a pseudoplastic fluid with good rheological properties. The gel was basically non-irritating to rabbit eyes and had no irreversible tissue damage.
The prepared TCM chrysanthemum volatile oil polymer micelle thermosensitive gel has little irritation and good stability.
To analyze the effect of Wuzhi capsule on tacrolimus concentration and clinical efficacy.
The Chinese databases of Wanfang, CNKI and Weipu were searched to collect the relevant studies on the effect of Wuzhi capsule on the plasma concentration and clinical efficacy of tacrolimus in patients with nephrotic syndrome. The literatures that met the standards were included, and the effective data were extracted. SPSS 27.0 statistical software was applied for analysis.
A total of 4 studies were included, and the statistical analysis results showed that Wuzhi capsule improved the plasma concentration of tacrolimus and standardized plasma concentration, and the difference was statistically significant (P<0.05). The 24-hour urine protein level in drug combination group was lower than that in single drug group, and the plasma albumin level was higher.
Wuzhi capsule can significantly improve the plasma concentration of tacrolimus and clinical efficacy in patients with nephrotic syndrome.
As the latest generation of sodium-glucose cotransporter-2 inhibitors (SGLT2i), ertugliflozin (ERT) has stable molecular structure, long half-life, significant hypoglycemic effect and good tolerance. It also has the protective effect of heart independent of its hypoglycemic activity. It is recommended as a priority treatment for the patients with type 2 diabetes mellitus (T2DM) complicated with atherosclerotic cardiovascular disease (ASCVD) in China and abroad. In addition, ERT has a concrete effect on controlling the body weight of T2DM patients, thus also has the value in the treatment of T2DM patients with obesity. However, ERT is not recommended to be used in those T2DM patients with renal insufficiency due to low safety profile.
Cancer has always been a major disease that threatens human lives. Traditional treatment modalities cannot guarantee efficient killing of tumor cells and good prognosis after treatment, mainly because people do not have sufficient understanding of tumors and their microenvironment. In recent years, with the advancement of tumor research, the mechanism of tumorigenesis and the impact of tumors on human immune system have become hot topics of research. Various preclinical tumor models have been developed, including in vivo models represented by patient tumor-derived xenograft models (PDX) and in vitro models represented by organoid microarrays, which have different functions in preclinical tumor research and play important roles. As a convenient and effective tool, preclinical tumor models play an irreplaceable role in exploring tumor-immune system interactions, preclinical evaluation of anti-tumor drugs, and discovery of biomarkers for immunotherapy.
To evaluate the absorption of pioglitazone hydrochloride (PGH) cocrystals in SD rats and improve the problems of poor solubility and low bioavailability of PGH.
Cocrystals of pioglitazone hydrochloride-para aminobenzoic acid, pioglitazone hydrochloride-para-aminosalicylic acid and pioglitazone hydrochloride-gallic acid were prepared by suspension method. PGH and 3 cocrystals were characterized by a variety of analytical techniques, and the concentration of PGH in rat plasma was determining by high performance liquid chromatography-mass spectrometry (HPLC-MS) to analyze the pharmacokinetic parameters of cocrystals.
The 3 cocrystals all showed good stability and solubility. Cocrystals of pioglitazone hydrochloride-para aminobenzoic acid and pioglitazone hydrochloride-gallic acid could significantly improve the bioavailability, peak concentration (Cmax), and area under the curve (AUC) of oral PGH in rats.
Cocrystallization is an important method to change PGH solubility and absorption characteristics in vivo.
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