Latest ArticlesRheumatoid arthritis (RA), a chronic autoimmune disease, causes progressive cartilage destruction and bone erosion, and also affects vital organs. It affects approximately 0.5%-1% of the global population. Its treatment faces challenges such as insufficient drug targeting, significant systemic side effects and low patient compliance. Responsive microneedle technology integrates inflammatory microenvironment-sensitive materials with intelligent delivery technology to construct a microneedle delivery system that can sense site-specific markers of inflammation (e.g., pH, enzyme activity, or oxidative stress level) to achieve precise local delivery of anti-RA drugs in synovial tissues. Compared with systemic drug delivery, this technology significantly improves local drug concentration in the joints, effectively avoiding the risk of myelosuppression and liver and kidney toxicity associated with traditional therapies. The intelligent response characteristics of microneedles can dynamically regulate the release rate of the drug, so that the drug can be released on demand. The microneedle patch design can significantly reduce the frequency of drug delivery, which significantly improves the long-term treatment adherence. This review systematically explains the classification of responsive microneedles in terms of mechanism of action, material innovation and therapeutic advantages, analyses the current translational bottlenecks, and explores the prospects for their development in the individualized treatment of RA.
The therapeutic efficacy of glioma treatment has long been constrained by the inefficiency of drug delivery due to the blood-brain barrier (BBB). Angiopep-2 peptide actively targets LDL receptor-related protein 1 and efficiently crosses the BBB via LRP1-mediated endocytosis, enabling precise and efficient drug delivery to tumor cells. This offers a novel therapeutic strategy for glioma treatment. Currently, Angiopep-2 has been extensively modified onto various carrier surfaces, significantly enhancing drug accumulation at brain tumor sites. This demonstrates its immense potential in constructing BBB-crossing platforms and has greatly advanced research on brain-targeted delivery systems. This paper primarily reviews the application of Angiopep-2/LRP-1-based modified formulations in glioma treatment. It summarizes research progress across different carriers in glioma, providing a reference for future studies.
The self-assembled nano systems of traditional Chinese medicine (TCM) refer to carrier-free nanostructures spontaneously formed by non-covalent interactions, such as hydrogen bonds, hydrophobic interactions, and π-π stacking, between the active components of TCM. Due to their significant advantages in drug loading, biocompatibility, and intelligent delivery characteristics, these systems have increasingly become a hotspot in the research of TCM modernization, and related research in this area has expanded rapidly. This article reviews the formation mechanisms, advantageous characteristics, and application examples of TCM self-assembled nanostructures from four dimensions: TCM compound formulas, pairs of herbs, single herbs, and individual active ingredients. It delves into the research value of these systems and highlights the key challenges currently faced. The study aims to integrate existing knowledge and provide a theoretical basis for the in-depth exploration and practical application of TCM self-assembly strategies. Furthermore, from the perspective of self-assembly nanotechnology, it not only offers new insights into the material basis of TCM efficacy and the mechanisms of herb combinations but also contributes to advancing TCM research toward precision and modernization.
Peptide therapeutics are characterized by high potency, exquisite specificity, and low toxicity, and have therefore been widely adopted for the clinical management of diverse diseases. However, their inherently low gastrointestinal permeability, rapid enzymatic degradation, and multiple physiological barriers collectively result in extremely low oral bioavailability, necessitating parenteral administration. Compared with the more convenient and patient-compliant oral route, chronic injection is associated with poor adherence and an increased incidence of adverse reactions. In recent years, extensive research has focused on permeation enhancers (PEs) based strategies to improve the oral bioavailability of peptide drugs. This review systematically summarizes the mechanisms of action and clinical applications of representative PEs-including surfactants (sodium caprylate, sodium caprate, alkyl glycosides, bile salts), chelating agents, chitosan and cell-penetrating peptides. It also summarizes related patented technologies (EligenTM, TPETM, GIPETTM, PODTM, PeptelligenceTM) to facilitate the development and clinical translation of oral peptide formulations.
Parkinson's disease (PD) is a common neurodegenerative disorder, characterized by typical symptoms such as resting tremor and muscle rigidity, which can severely impair patients' quality of life. Therefore, early and accurate diagnosis of PD is crucial for improving patient prognosis. Traditional detection methods have limitations including low sensitivity and invasiveness, whereas nanoprobes, with their high specificity, high sensitivity, and multimodal imaging capabilities, offer new opportunities for precise diagnosis and treatment of PD. This article systematically reviews recent advances in the application of nanoprobes for PD detection, with a focus on the classification and functionalization strategies of nanoprobes, as well as their applications in the detection of PD biomarkers and related fields. Additionally, it analyzes current challenges such as biocompatibility and clinical translation, and provides an outlook on future development directions, aiming to offer new insights and references for the early diagnosis and precise treatment of PD.
Trace amine-associated receptor 1 (TAAR1), a widely expressed G protein-coupled receptor in the mammalian central nervous system, serves as a key regulator of monoaminergic and glutamatergic systems and plays a pivotal role in physiological processes such as emotion, cognition, reward, and learning and memory. Recently, research on TAAR1 has expanded beyond its initial focus on psychiatric disorders to rapidly encompass metabolic syndrome and immune system diseases, revealing its considerable potential as a therapeutic target for multiple diseases. This review systematically summarizes TAAR1-associated signaling pathways and their critical roles in various diseases, with a particular emphasis on the therapeutic mechanisms and application prospects of TAAR1 agonists in schizophrenia, depression, Alzheimer's disease, Parkinson's disease, substance use disorder, and type 2 diabetes. Furthermore, this article examines recent advances in the development of TAAR1 agonists, spanning from derivatization tactics based on natural ligands to rational design guided by structural biology, and explores future research objectives, including multi-target drug strategies. The aim of this review is to provide a theoretical foundation and insights to support the development and translational application of TAAR1-targeted therapies.
In recent years, tumors have posed a serious threat to human life and health. Although conventional treatments are widely used, they still have significant limitations. As a result, researchers have increasingly focused on nanotechnology to develop more efficient and precise treatment strategies. Natural nanomaterials, including naturally occurring nanoparticles, polymeric nanomaterials derived from natural products, and self-assembled nanomaterials from natural small molecules, have demonstrated broad prospects in the medical field due to their unique physicochemical properties and excellent biocompatibility. This article reviews the current applications and future potential of several commonly used natural organic nanomaterials in tumor diagnosis and treatment. Looking ahead, natural nanomaterials are expected to not only drive innovation in cancer therapeutics and diagnostics and introduce green sustainable concepts into nanomedicine, but also accelerate clinical translation, offering safer and more effective treatment solutions for patients.
Ulcerative colitis (UC) is an intestinal disease characterized by chronic and recurrent inflammation of the colonic mucosal layer, whose main pathological feature is continuous and diffuse mucosal damage which begins in the rectum and extends towards the proximal colon. G-protein-coupled receptor 21 (GPR21) is an orphan G protein-coupled receptor (GPCR), belonging to class A GPCRs. Previous studies have reported that GPR21 is closely related to diabetes and inflammation. Levistilide A (LA), a natural terpene lactone active component mainly exists in the traditional Chinese medicinal herbs Ligusticum chuanxiong and Angelica sinensis, exhibiting multiple pharmacological activities including anti-inflammation, anti-fibrosis, and anti-tumor. In this study, GPR21-HEK293 recombinant cells were constructed by lentivirus transfection. LA was screened out as a potential GPR21 inhibitor by cell membrane chromatography. RAW264.7 cells were treated with lipopolysaccharide in vitro to establish an inflammatory cell model, which confirmed the correlation between the therapeutic effect of LA on inflammation and GPR21. Dextran sodium (DSS) was used to administrate C57BL/6 mice in vivo to induce a mouse model of UC, at the meanwhile, the mice in LA group were intragastrical administration with LA to investigate its therapeutic effect on UC. In conclusion, we demonstrated that LA as a GPR21 inhibitor improves DSS-induced UC through reducing intestinal inflammation. This work was approved by the Institutional Animals Care and Use Committee of Xi'an Jiaotong University (approval number: XJTUAE2024-1523) and strictly carried out in accordance with their requirements.
Bladder cancer has a high incidence and mortality rate worldwide. Existing treatment methods often face the challenges, such as drug resistance, recurrence and metastasis. These challenges drive our effect to explore new therapeutic compounds. 19-Hydroxycytochalasin B (19-HCB) is a new cytochalasin isolated from marine fungus. Previous studies have confirmed that its structural analogues have good anti-tumor activity, but the anti-tumor activity and mechanism of 19-HCB remain unclear. This study aims to evaluate the in vitro anti-tumor activity of 19-HCB and explore the mechanism of its action in human bladder cancer J82 cells. The anti-tumor activity was comprehensively evaluated through analyzing cell growth by MTT assay, cell scratch assay, high-content imaging and flow cytometry, colony formation and other experiments. The results showed that 19-HCB exhibited the strongest proliferative inhibitory activity (IC50 = 0.59 μmol·L-1) against bladder cancer J82 cells and could significantly inhibit the migration of J82 cells. Its mechanism of action is closely related to inducing apoptosis, manifested as the upregulation of pro-apoptotic proteins BIM and BAX and the down-regulation of anti-apoptotic protein survivin. Meanwhile, the expression of cell cycle regulatory protein p21 is upregulated while that of CDK1 is downregulated. Additionally, 19-HCB can also inhibit the AKT signaling pathway. In summary, 19-HCB exerts anti-bladder cancer effects by inducing apoptosis, inhibiting migration and regulating multiple key signaling pathways, and is a candidate drug lead compound with development potential.
Serum metabolomics reveals the mechanism of Suanzaoren Decoction (SZRD) in ameliorating anxiety-like behaviors in rats. Insomnia was induced by the modified multiple platform method. Compared with the control group, rats subjected to 18-hour daily sleep deprivation for 21 days exhibited significantly increased total locomotor distance and center zone exploration time (P < 0.01), alongside markedly reduced open arm entry time percentage and frequency (P < 0.001), indicating anxiety-like behaviors. SZRD administration significantly decreased locomotor activity and center zone duration (P < 0.01), while increasing open arm entry time and frequency (P < 0.001), thereby alleviating insomnia-associated anxiety. Pathological sections and immunofluorescence results revealed that, compared with the control group, the model group exhibited inflammatory infiltration in the intestinal mucosal epithelial cells, along with significantly decreased mean fluorescence intensities of ZO-1, occludin, and claudin-1 in the colonic tissue, together with increased hepatic lipid accumulation. SZRD ameliorated intestinal and hepatic damage while enhancing tight junction protein expression. GC-MS analysis demonstrated that the significantly reduced levels of acetic acid, propionic acid, isobutyric acid, valeric acid, isovaleric acid, and isocaproic acid in the colonic contents of sleep-deprived rats (P < 0.05) were significantly reversed by SZRD. UPLC-Q-TOF-MS/MS-based serum metabolomics identified 53 differential metabolites in model rats compared to controls; SZRD significantly reversed 36 of these, encompassing amino acids, organic acids, and lipids. KEGG pathway analysis indicated that SZRD primarily modulated phenylalanine, tyrosine and tryptophan biosynthesis, tryptophan metabolism, tyrosine metabolism, and the tricarboxylic acid cycle. These findings demonstrate that SZRD ameliorates intestinal and hepatic inflammatory injury, reduces intestinal permeability, and exerts anti-insomnia and anxiolytic effects primarily through regulating amino acid metabolism and the tricarboxylic acid cycle, providing scientific evidence for elucidating the therapeutic characteristics of SZRD in treating "consumptive disease with restlessness and insomnia". This experiment was approved by the Animal Ethics Committee of Shanxi University of Chinese Medicine (Approval No.: AWE202310391).
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