1.Discovery of a novel AhR-CYP1A1 axis activator for mitigating inflammatory diseases using an in situ functional imaging assay.
Feng ZHANG ; Bei ZHAO ; Yufan FAN ; Lanhui QIN ; Jinhui SHI ; Lin CHEN ; Leizhi XU ; Xudong JIN ; Mengru SUN ; Hongping DENG ; Hairong ZENG ; Zhangping XIAO ; Xin YANG ; Guangbo GE
Acta Pharmaceutica Sinica B 2025;15(1):508-525
The aryl hydrocarbon receptor (AhR) plays a crucial role in regulating many physiological processes. Activating the AhR-CYP1A1 axis has emerged as a novel therapeutic strategy against various inflammatory diseases. Here, a practical in situ cell-based fluorometric assay was constructed to screen AhR-CYP1A1 axis modulators, via functional sensing of CYP1A1 activities in live cells. Firstly, a cell-permeable, isoform-specific enzyme-activable fluorogenic substrate for CYP1A1 was rationally constructed for in-situ visualizing the dynamic changes of CYP1A1 function in living systems, which was subsequently used for discovering the efficacious modulators of the AhR-CYP1A1 axis. Following screening of a compound library, LAC-7 was identified as an efficacious activator of the AhR-CYP1A1 axis, which dose-dependently up-regulated the expression levels of both CYP1A1 and AhR in multiple cell lines. LAC-7 also suppressed macrophage M1 polarization and reduced the levels of inflammatory factors in LPS-induced bone marrow-derived macrophages. Animal tests showed that LAC-7 could significantly mitigate DSS-induced ulcerative colitis and LPS-induced acute lung injury in mice, and markedly reduced the levels of multiple inflammatory factors. Collectively, an optimized fluorometric cell-based assay was devised for in situ functional imaging of CYP1A1 activities in living systems, which strongly facilitated the discovery of efficacious modulators of the AhR-CYP1A1 axis as novel anti-inflammatory agents.
2.Pharmacological modulation of mitochondrial function as novel strategies for treating intestinal inflammatory diseases and colorectal cancer.
Boya WANG ; Xinrui GUO ; Lanhui QIN ; Liheng HE ; Jingnan LI ; Xudong JIN ; Dapeng CHEN ; Guangbo GE
Journal of Pharmaceutical Analysis 2025;15(4):101074-101074
Inflammatory bowel disease (IBD) is a chronic and recurrent intestinal disease, and has become a major global health issue. Individuals with IBD face an elevated risk of developing colorectal cancer (CRC), and recent studies have indicated that mitochondrial dysfunction plays a pivotal role in the pathogenesis of both IBD and CRC. This review covers the pathogenesis of IBD and CRC, focusing on mitochondrial dysfunction, and explores pharmacological targets and strategies for addressing both conditions by modulating mitochondrial function. Additionally, recent advancements in the pharmacological modulation of mitochondrial dysfunction for treating IBD and CRC, encompassing mitochondrial damage, release of mitochondrial DNA (mtDNA), and impairment of mitophagy, are thoroughly summarized. The review also provides a systematic overview of natural compounds (such as flavonoids, alkaloids, and diterpenoids), Chinese medicines, and intestinal microbiota, which can alleviate IBD and attenuate the progression of CRC by modulating mitochondrial function. In the future, it will be imperative to develop more practical methodologies for real-time monitoring and accurate detection of mitochondrial function, which will greatly aid scientists in identifying more effective agents for treating IBD and CRC through modulation of mitochondrial function.
3.Ultrasound guided autologous platelet-rich plasma injection for the treatment of common peroneal nerve compression syndrome: a case report
Yiqi HUANG ; Lanhui QIN ; Xixia LIU
Chinese Journal of Blood Transfusion 2024;37(9):1008-1012
【Objective】 To observe the clinical efficacy of ultrasound-guided autologous platelet- rich plasma (PRP) injection for the treatment of common peroneal nerve compression syndrome, and to provide reference for the treatment of peripheral nerve compression diseases. 【Methods】 A patient with common peroneal nerve compression syndrome was treated with ultrasound-guided injection of autologous PRP for nerve water separation. The efficacy of PRP injection treatment on common peroneal nerve compression syndrome was evaluated by observing the patient′s symptoms, electrophysiological and imaging manifestations. 【Results】 After systematic injection therapy, the patient′s symptoms, signs and electromyography showed significant improvement, and there were no significant adverse reactions after 3 months of follow-up. 【Conclusion】 Ultrasound guided PRP injection therapy improves neurological dysfunction in common peroneal nerve compression syndrome.
4.Parametric imaging of CEUS for blood perfusion in cervical lymphadenopathy
Xiaorong WANG ; Qin ZHAO ; Tao SONG ; Lanhui YAO
Chinese Journal of Medical Imaging Technology 2017;33(12):1806-1810
Objective To explore the diagnostic value of parametric imaging of CEUS in different cervical lymphatic diseases.Methods One hundred eleven patients diagnosed with cervical lymphadenopathy were included.All of the patients underwent parametric imaging of CEUS.According to the pathological results,all patients were divided into reactive hyperplasia group,tuberculosis group,metastasis group and lymphoma group.The features of perfusion phases (perfusion during the artery phase,or perfusion during the artery and parenchymal phase) and perfusion uniformity (homogeneous perfusion or heterogeneous perfusion) were compared among four groups.According to the pathological results,the reactive hyperplasia group and the tuberculosis group were merged into a benign group,and the metastasis group and the lymphoma group were merged into a malignant group.Then,the artery perfusion phase was regarded as benign,and the artery and parenchymal perfusion phase was regarded as malignant.The consistency between parametric imaging of CEUS and the pathological results was compared in two groups.Results The difference of perfusion phase and perfusion uniformity within the four groups had a statistical significance (all P<0.05).The differences of perfusion phase between the reactive hyperplasia group and the metastasis group,the reactive hyperplasia group and the lymphoma group,the tuberculosis group and the metastasis group were statistical significant respectively (all P<0.008).The differences of perfusion uniformity between the reactive hyperplasia group and the tuberculosis group,the reactive hyperplasia group and the lymphoma group,the lymphoma group and the tuberculosis group,the lymphoma group and the metastasis group were statistical significant respectively (all P<0.008).The perfusion phase between the benign group and the malignant group had a statistical significance (P<0.005),but the perfusion uniformity had no statistical significance in two groups.The consistency was good between the parametric imaging and the pathological results.Conclusion The parametric imaging of CEUS can offer valuable diagnostic information for the cervical lymph nodes underdetermined by conventional ultrasound.

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