Fuyun Chi,Wenshuang Wang,Shanshan Zhai,Man Zhang,Yuanyuan Hou,Gang Bai
Objective To explore novel anti-inflammatory strategies by targeting prostaglandin E2 (PGE2) overexpression, aiming to overcome the limitations of conventional cyclooxygenase-1/2 (COX-1/2) inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs). Methods A correlation analysis of the anti-inflammatory activities of 24 exterior- releasing herb medicines, including NF- κ B, COX2, and PGE2 activities, was conducted, and the key active ingredients in the herbs showing significant associations were screened. Using a self-assembly technique, baicalein-2,4-decadienal (BD) were formulated into stable and homogeneous carrier-free nanoparticles to enhance drug solubility and targeting. Subsequently, disease models associated with PGE2 overexpression—fever, pneumonia and rheumatoid arthritis were established to evaluate the antipyretic, analgesic and anti-inflammatory properties of BD nanomedicines. Their targeting capability and drug release profile were also investigated. Results BD nanomedicines exhibited a synergistic inhibitory effect on PGE2 production by concurrently targeting COX2 and microsomal prostaglandin E synthase-1 (mPGES1), thereby producing antipyretic, analgesic, and anti-inflammatory effects superior to those observed with either agent alone. Furthermore, BD nanoparticles demonstrated preferential accumulation in macrophages implicated in the inflammatory response and facilitated pH-responsive drug release within the inflammatory microenvironment. This targeted delivery approach not only enhances therapeutic efficacy but also enables dose reduction and mitigates the risk of adverse effects, representing a promising strategy for the treatment of PGE2-mediated inflammatory diseases. Conclusion The findings provide new insights into drug development for inflammatory diseases caused by PGE2 overexpression, emphasizing the advantages of carrier-free supramolecular bioactive materials derived from natural products in the treatment of such diseases.
The naturally occurring pentacyclic triterpenoid compounds ursolic acid (UA) and oleanolic acid (OA) are commonly found together in various fruits and find broad applications in pharmaceuticals, cosmetics, food and agricultural fields. In this study, a sensitive and practical icELISA method was developed based on a monoclonal antibody (mAb) YC23-101, with a median inhibitory concentration (IC 50 ) of 15.56 ng/mL and a linear range of 5.26 to 54.1 ng/mL. The limits of detection (LOD) ranges from 0.98-5.11 ng/mL in fruit matrices and the recoveries were 94.03-112.21% with coefficients of variation below 5.73%. Cross-reactivity analysis showed that mAb YC23-101 could also specifically recognize OA with similar sensitivity to UA, indicating feasibility for the simultaneously quantification of UA and OA in fruits. The developed icELISA was applied to several fruits, and the results showed good correlation with that of HPLC. Molecular docking analysis predicted equal binding energy of UA and OA to the mAb with hydrophobic interactions playing a predominant role. All these findings demonstrated that this icELISA is reliable, sensitive, and suitable for the high-throughput quantification of total UA and OA content in fruits composition analysis.
Hua ZHAO,Xiaohui WANG,Yuli ZHANG,Xiaowan HUANG,Yaling JIANG,Huan MA,Li AN,Xujin WU,Qiang WANG
Saikosaponin a and saikosaponin d are used as chemical standards for the quality evaluation of Bupleurum chinense DC. by the high-performance liquid chromatography method in current Chinese Pharmacopoeia. However, other saikosaponins, such as saikosaponin c and saikosaponin b2, also possess pharmaceutical activity, but are not used as chemical standards. In this study, a quantitative proton nuclear magnetic resonance (1H NMR) method was developed to determine the total mass percentage (mg/g) of SSa, SSb1, SSb2 and SSd in B. chinense DC., using the H-24 (δH 0.71) signal. Furthermore, the molality (mol/kg) of type I saikosaponins (epoxy-ether structure) was also determined by quantitative 1H NMR in the area of H-11 (δH 5.95) for a more accurate quality evaluation. Validation of the method confirmed that it has acceptable selectivity, precision, stability, and repeatability. The results indicated that this method has the potential to be a reliable method for the quantification of saikosaponins in Bupleurum scorzonerifolium Willd., vinegar baked B. chinense DC. and B. scorzonerifolium Willd., Chaihu Koufuye (oral liquid of Chaihu).
危险品化学品经营许可证（带存储）