Sen Wang

Rutaecarpine, a representative alkaloid, has been obtained from Euodia rutaecarpa (Juss.) Benth., a well-known traditional Chinese medicine. Research has demonstrated that rutaecarpine possesses a diverse array of pharmacological activities, including exerting impacts on the cardiovascular system, as well as anti-inflammatory, anti-tumor, and hepatoprotective properties. However, as research has progressed, the poor water solubility of rutaecarpine has become a significant limiting factor. This leads to poor absorption in the body after oral administration, resulting in lower free drug concentration and ultimately decreased bioavailability. This comprehensive review of rutaecarpine’s pharmacological profile, pharmacokinetics, and formulation design provides valuable insights for future research and its potential therapeutic applications.

In recent years, with the increasing demand for high-quality Dendrobii caulis decoction piece, the identification of D. caulis decoction piece species has become an urgent issue. However, the current methods are primarily designed for professional quality control and supervision. Therefore, ordinary consumers should not rely on these methods to assess the quality of products when making purchases. This research proposes a deep learning network called improved YOLOv5 for detecting different types of D. caulis decoction piece from images. In the main architecture of improved YOLOv5, we have designed the C2S module to replace the C3 module in YOLOv5, thereby enhancing the network’s feature extraction capability for dense and small targets. Additionally, we have introduced the Reparameterized Generalized Feature Pyramid Network (RepGFPN) module and Optimal Transport Assignment (OTA) operator to more effectively integrate the high-dimensional and low-dimensional features of the network. Furthermore, a new large-scale dataset of Dendrobium images has been established. Compared to other models with similar computational complexity, improved YOLOv5 achieves the highest detection accuracy, with an average mAP@.05 of 96.5%. It is computationally equivalent to YOLOv5 but surpasses YOLOv5 by 2 percentage points in terms of accuracy.

Polygonum Cuspidate (P. cuspidatum) is a traditional topical preparation of Chinese medicine. The aim of this study was to develop HPLC fingerprints for P. cuspidatum Powder and P. cuspidatum Ointment, as well as to determine the total stilbene and total anthraquinone contents in them. A XB-C₁₈ column (250 ​mm ​× ​4.6 ​mm, 5 ​μm) was used with a mobile phase consisting of 0.1% phosphoric acid solution-acetonitrile and a gradient elution. The flow rate was 1.0 ​ml/min and the detection wavelength was 286 ​nm. The column temperature was 30 ​°C and injection volume was 10 ​μl. The similarity evaluation system for chromatographic fingerprint of traditional Chinese medicine (2012 edition) was employed to confirm the common peaks at 13 batches of samples and to assess the similarity. The study revealed that 20 common peaks were identified in both P. cuspidatum powder and P. cuspidatum ointment, with a similarity greater than 0.95. Amongst them, seven components were attributed and confirmed, which were identified as polydatin , resveratrol, emodin-8-glucoside, aloe-emodin, rhein, emodin and physcion. Under the established conditions of the chromatography, quantitative analysis of six components could be well separated, and had a good linearity and linear range, the precision, repeatability and stability were good. The method's efficacy in assessing the quality of P. cuspidatum powder and P. cuspidatum ointment is validated, and it can be employed for quality control purposes.

Glycycoumarin is a representative coumarin compound with significant pharmacological activities isolated from Glycyrrhiza uralensis Fisch., Fabaceae. Studies have shown that glycycoumarin has many biological activities, such as anti-tumor, liver protection, antispasmodic, antibacterial, and antivirus. However, the poor solubility of glycycoumarin in water and the accompanying reactions of the phase I (hydroxylation) and II (glucuronidation) metabolism limit its druggability, which manifests as low absorption in the body after oral administration and low free drug concentration, ultimately leading to low bioavailability. Therefore, a comprehensive review of the pharmacological effects and pharmacokinetics of glycycoumarin is presented to provide a reference for further research and application as a therapeutic agent. Graphical Abstract

Network pharmacology, reverse molecular docking, and rat acute pancreatitis (AP) models were used to analyze the mechanism of protection by Qingyi II granules. The chemical components of 7 Chinese herbal medicines in Qingyi II granules were searched through the TCMSP (traditional Chinese medicine systems pharmacology database and analysis platform) database. The active ingredients were screened out in the OB (oral bioavailability) and DL (drug likeness) filters as a condition for inclusion. Then, the prediction analysis of potential targets was performed through databases. A GO (gene ontology) enrichment analysis of target proteins related to AP and KEGG (Kyoto Encyclopedia of Genes and Genomes) pathway annotation was performed using the DAVID (The Database for Annotation, Visualization, and Integrated Discovery) database. Finally, the “Herbal-Compound-Target” network was constructed using Cytoscape software. The active component structure and target name were uploaded to the Systems Dock database for reverse molecular docking. With octreotide as a positive control, Qingyi II decoction and Qingyi II granules were administered to AP rats at low, medium, and high doses. The pathological changes in the pancreas were observed using HE staining. The levels of Bcl-2, AMS, BAX, IL-2, and CASP3 in plasma were determined by an ELISA kit. Real-time PCR detected the expression of AKT1 and PIK3CA mRNA in the pancreas. The database predicted 94 active components of Qingyi II granules, 76 potential targets, and 64 signaling pathways. Twenty pathways were directly or indirectly associated with acute pancreatitis, including the TNF signaling pathway and the PI3K-AKT signaling pathway. In the reverse molecular docking experiment, the matching scores of the active components and the target were mainly between 6.0 and 7.0, with strong binding activity. Compared to the normal group, the plasma concentrations of BAX, IL-2, Bcl-2, AMS, and CASP3 in the model group were significantly increased ( ). Compared with the model group, the low-dose group of Qingyi II granules only significantly reduced IL-2 levels and had no effect on other indicators. The other groups could significantly reduce the levels of AMS, BAX, and CASP3 ( ). Compared with the model group, the octreotide group and Qingyi II granules high-dose group significantly increased the Bcl-2 level ( ), and there was no statistical difference in other drug-administered groups. Compared with the normal group, the expression of AKT1 and PIK3CA in the pancreas of the model group was significantly higher. Compared to the model group, the expression of PIK3CA was low in all drug-administered groups. In addition to the low-dose group, the other drug-administered groups significantly reduced the expression of AKT1. Qingyi can reduce the levels of AMS, BAX, IL-2, and CASP3 and increase the levels of Bcl-2. This mechanism may be related to the PI3K- AKT signaling pathway.