Latest ArticlesThis 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.
This study establishes a quantitative analysis of multi-components by single marker (QAMS) method for the simultaneous determination of gallic acid, sodium danshensu, protocatechuic acid, protocatechuic aldehyde, vanillin, rosmarinic acid, salvianolic acid B, eugenol, cryptotanshinone and tanshinone IIA in Guanxinshutong capsules (Bambusae Concretio Silicea, Salvia miltiorrhiza, clove, borneol, Bambusae Concretio Silicea) by HPLC. Sample was loaded onto an Agilent C18 (ZORBAX Extend-RP C18, 250 mm × 4.6 mm, 5 µm) column and eluted with methanol-0.4% aqueous formic acid solution as a flow phase gradient, flow speed 1.0 mL·min-1, detection wavelength 280 nm, column temperature 35 ℃ and sample intake of 5 µL. Using protocatechuic acid as the internal reference, a relative correction factor was calculated and the durability was investigated, and the content of 10 components was calculated by QAMS and external standard method (ESM). The results show that the specificity, linear relationship, precision, repeatability, and stability of the 10 components were good. The average recovery was 98.20%-103.47% and RSD was 1.26%-2.84%. The relative positive factors and contents of the other nine components were calculated as gallic acid (0.759, 227.381), sodium tanshinol (3.630, 3.283), protocatechualdehyde (0.185, 0.150), vanillin (0.532, 65.213), rosmarinic acid (4.240, 1.035), salvianolic acid B (3.245, 18.204), eugenol (1.729, 9.265), cryptotanshinone (0.691, 1.449), and tanshinone ⅡA (0.702, 1.939). The results of QAMS were consistent with ESM analysis, and the relative error was between -3% and 3%. This method is stable and reliable, and can be used for the determination of 10 components in Guanxinshutong capsules.
This study aims to construct a dynamic two-dimensional characterization technique for the hygroscopicity of traditional Chinese medicine extracts and investigate the effect of material properties of powders on hygroscopicity. The dynamic hygroscopicity-time curves of the powders were measured at 25 ℃ and 75% humidity, and the semi-equilibrium hygroscopicity time (t1/2) and equilibrium hygroscopicity (F∞) were derived as two-dimensional evaluation indicators. Finally, the correlation between the material properties and the hygroscopic behavior was analyzed by principal component analysis (PCA) and partial least squares analysis (PLS). The results showed that the dynamic two-dimensional characterization system of hygroscopicity constructed with 1/t1/2 = 0.1 h-1 and F∞ = 15% as the center can classify the hygroscopic behavior of traditional Chinese medicine extracts into four categories: fast hygroscopicity with strong hygroscopicity, slow hygroscopicity with strong hygroscopicity, fast hygroscopicity with weak hygroscopicity and slow hygroscopicity with weak hygroscopicity. The moisture absorption was negatively correlated with D50, D90, ρb and ρt; the moisture absorption rate was negatively correlated with D10, D50, D90, ρb, ρt, and positively correlated with moisture content. The hygroscopicity dynamic two-dimensional characterization indicators of Chinese medicine extracts (CMEs) constructed in this study matched with the physical properties. The method of dynamic multi-dimensional characterization technology is feasible and scientific, and the idea has strong promotional value.
Leech bites usually lead to more bleeding, and dermal tissue is damaged to form lifelong scars. If leeches enter the body cavity, it will be more dangerous. Therefore, there is an urgent need to develop effective repellents. In this study, oil in water (O/W) emulsion of tea tree oil was prepared with tea tree oil as the main ingredient, and konjac glucomannan (KGM), ethyl cellulose (EC) as the main excipients. The filter-paper ring method and repellent test in water were used to evaluate the repellent effects on leeches. The animal experiments were approved by the Ethics Committee of Academy of Military Medical Sciences and were conducted in accordance with relevant guidelines and regulations. The activities of acetylcholinesterase (AchE), glutathione S-transferase (GST) and carboxylesterase (CarE) in vivo were measured to clarify the repellent mechanisms. The results showed that a uniform and stable tea tree oil emulsion was successfully prepared, which has excellent hydrophilicity and can effectively repel leeches. The tea tree oil emulsion has a good repellent effect on leeches, which can avoid the volatilization of tea tree oil and prolong the effective repelling time. The novel formulation of tea tree oil provides a new idea for repelling effects with long time and high efficiency based on similar essential oil.
It is a common understanding that turbidity and precipitation of traditional Chinese medicine are easy to occur in the process of decocting. At present, our research group found that the cause of "multi-phase of traditional Chinese medicine decoction" mainly came from the interaction between the effective components of traditional Chinese medicine, especially the interaction of acid and base components. For example, the Liquorice and Rhizoma chinensis was a supramolecular system formed by a large number of active components in the decoction (> 30%), and could stably exist in the decoction system. In this study, the supramolecular part was extracted, and the morphology of the supramolecular part was characterized by scanning electron microscopy and dynamic light scattering. It was observed that the supramolecular particles were uniform in size and regular in shape. The main components of supramolecular sites were identified by liquid mass spectrometry (LC-MSn). The results of UV and IR spectra showed that the chemical components of Liquorice and Rhizoma chinensis in the co-decocting process collided with each other, and weak bonds were formed between the functional groups of the molecules, which then induced the aggregation to form supramolecules. Thereafter, Through the diarrhea model of mice, sensory evaluation and antibacterial activity evaluation found that Liquorice and Rhizoma chinensis decocted together enhanced the antibacterial activity of Rhizoma, and compatibility "reconcile" Rhizoma "big bitter cold" property compared with single decoction group and interval administration group. All animal experiments were approved by the Animal Ethics Committee of Beijing University of Chinese Medicine, and the relevant regulations of Beijing University of Chinese Medicine on experimental animals were strictly followed. In this study, supramolecular chemistry method was used to preliminarily discuss the scientific connotation of "increasing efficiency and decreasing toxicity" of Liquorice and Rhizoma chinensis combined decoction from three perspectives of "property, efficacy and taste", and provide new ideas for the basic research of "reconcile" compatibility of Liquorice.
In order to reveal the molecular mechanism of the small heat shock proteins (sHSPs) involved in stress resistance and active ingredients accumulation in Salvia miltiorrhiza, a small heat shock protein gene was cloned from Salvia miltiorrhiza by reverse transcription PCR according to the transcriptome data of orange root Salvia miltiorrhiza. The gene is named SmHSP21.8 based on the molecular weight of the protein, and it contains an open reading frame of 585 bp, which encodes 194 amino acids. The results of phylogenetic analysis and amino acid sequence alignment showed that SmHSP21.8 protein belongs to the endoplasmic reticulum (ER) subfamily, and contains a conserved endoplasmic reticulum-specific DPFR-I/V-LE-H/Q-x-P motif at N-terminus. The prokaryotic expression vector pMAL-c2X-SmHSP21.8 was constructed and transformed into E. coli BL21 competent cells. The recombinant protein was successfully expressed after inducted. Temporal and spatial expression analysis showed that SmHSP21.8 gene was the highest expressed in flowers and had significant tissue specificity. The relative expression of the gene was significantly increased in seedlings after induction by 38 ℃, PEG6000, abscisic acid(ABA), and indole-3-acetic acid (IAA), indicating that SmHSP21.8 gene may be involved in abiotic stress such as high temperature and drought, as well as the response to exogenous hormones ABA and IAA. These results lay the foundation for further research on the molecular mechanism of small heat shock proteins involved in adversity stress.
Age-related macular degeneration (AMD) is one of the main causes of vision loss among middle-aged and elderly people worldwide. The prevention and treatment of AMD is a current topic of interest in ophthalmology but remains challenging. Oxidative stress-induced retinal pigment epithelial cell autophagic dysfunction, cellular senescence, and an abnormal immune inflammatory response are key pathogenic factors for AMD. Many bioactive ingredients of traditional Chinese medicine not only exert anti-oxidative, anti-inflammatory, anti-aging, and anti-apoptotic effects, but also prevent/block the occurrence of AMD through different pathways. This review summarizes our current understanding of the pathogenesis of AMD, the types of natural bioactive ingredients capable of treating AMD, as well as the known mechanisms by which these agents act, and may provide new strategies for the prevention and treatment of AMD.
The advantages of local administration are as follow: release drugs directly at the lesion, increase the drug concentration in lesion location and reduce the side effects of systemic administration. Thermosensitive gel is one of typical local administration agents. It exhibits the different physical characteristics with the change of temperature. It is sol-gel at low temperature or storage temperature, while when the temperature rises to the transition temperature or near the body temperature, it is semisolid gel with a certain viscoelasticity, and can recover rapidly. It can enhance the local adhesion, which prolongs the local retention time of drugs. As a result, thermosensitive gel can control and display the release of drugs, which can significantly improve the bioavailability of drugs. This review summarizes the characteristics of thermosensitive gel, thermosensitive materials, and its application in different parts: nasal cavity, eye, vagina, periodontal, skin, tumor and joint cavity, based on clinical needs.
Hyaluronic acid is widely used in biomaterials, cosmetics, clinical medicine and other fields due to its good biocompatibility, degradability, hydrophilicity, tumor targeting, viscosity and other characteristics. Pharmacodynamic activities of natural small molecular products which derived from traditional Chinese medicine (TCM) are significant, but their low solubility and poor targeting limit the clinical application. Based on supramolecular properties of hyaluronic acid, in this review, numerous studies were reviewed on the improvement of solubility, bioavailability, targeting and suitable dosage forms of small molecular compounds in TCM by domestic and foreign scholars using hyaluronic acid as carrier. It provides new ideas and inspirations for exploring the potential application value of small molecule compounds in TCM and even for the research and development of new drugs.
Fe-based metal-organic frameworks (MOFs) are a class of polymer crystals formed by the combination of Fe ions or Fe clusters with organic ligands through coordination bonds. At present, Fe-based MOFs can be mainly prepared by solvothermal synthesis, ultrasonic synthesis, microwave synthesis, and dry-gel conversion, etc. Fe-based MOFs have the characteristics of strong drug loading capacity of inorganic nano-carrier and high safety of organic nano-carrier, and have good tumor targeting and the capacity of inducting tumor's ferroptosis, which have high potential in the delivery of antitumor drugs. Recently, Fe-based MOFs have also been developed with various functions such as imaging, magnetic hyperthermia, photothermal therapy, photodynamic therapy, and intelligent response, which can facilitate diagnosis and monitor drug distribution while delivering antitumor drugs, and can produce synergistic antitumor effects combined with thermotherapy and phototherapy, and can also control the precise release of drugs. Reviewing the advances in the synthesis methods, characteristics as well as functions and types of Fe-based MOFs can provide a basis for the further applications of Fe-based MOFs in antitumor drug delivery.
No. 86 Xueyuan South Road, Haidian District, Beijing
010-62662699(Operation and Technical Support)
qkjq@cast.org.cn
Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House
