1.A preclinical and first-in-human study of superstable homogeneous radiolipiodol for revolutionizing interventional diagnosis and treatment of hepatocellular carcinoma.
Hu CHEN ; Yongfu XIONG ; Minglei TENG ; Yesen LI ; Deliang ZHANG ; Yongjun REN ; Zheng LI ; Hui LIU ; Xiaofei WEN ; Zhenjie LI ; Yang ZHANG ; Syed Faheem ASKARI RIZVI ; Rongqiang ZHUANG ; Jinxiong HUANG ; Suping LI ; Jingsong MAO ; Hongwei CHENG ; Gang LIU
Acta Pharmaceutica Sinica B 2025;15(10):5022-5035
Transarterial radioembolization (TARE) is a widely utilized therapeutic approach for hepatocellular carcinoma (HCC), however, the clinical implementation is constrained by the stringent preparation conditions of radioembolization agents. Herein, we incorporated the superstable homogeneous iodinated formulation technology (SHIFT), simultaneously utilizing an enhanced solvent form in a carbon dioxide supercritical fluid environment, to encapsulate radionuclides (such as 131I,177Lu, or 18F) with lipiodol for the preparation of radiolipiodol. The resulting radiolipiodol exhibited exceptional stability and ultra-high labeling efficiency (≥99%) and displayed notable intratumoral radionuclide retention and in vivo stability more than 2 weeks following locoregional injection in subcutaneous tumors in mice and orthotopic liver tumors in rats and rabbits. Given these encouraging findings, 18F was authorized as a radiotracer in radiolipiodol for clinical trials in HCC patients, and showed a favorable tumor accumulation, with a tumor-to-liver uptake ratio of ≥50 and minimal radionuclide leakage, confirming the feasibility of SHIFT for TARE applications. In the context of transforming from preclinical to clinical screening, the preparation of radiolipiodol by SHIFT represents an innovative physical strategy for radionuclide encapsulation. Hence, this work offers a reliable and efficient approach for TARE in HCC, showing considerable promise for clinical application (ChiCTR2400087731).
2.Bioactivity-guided discovery of antiviral templichalasins A‒C from the endophytic fungus Aspergillus templicola.
Teng CAI ; Jingzu SUN ; Wenxuan CHEN ; Qiang HE ; Baosong CHEN ; Yulong HE ; Peng ZHANG ; Yanhong WEI ; Hongwei LIU ; Xiaofeng CAI
Chinese Journal of Natural Medicines (English Ed.) 2025;23(6):754-761
The bioactivity-guided isolation of potentially active natural products has been widely utilized in pharmaceutical discovery. In this study, by screening fungal extracts against coxsackievirus B3 (CVB3), three new aspochalasins, templichalasins A‒C (1‒3), along with six known aspochalasins (4‒9) were isolated from an active extract derived from the endophytic fungus Aspergillus templicola LHWf045. Compound 1 features a unique 5/6/5/7/5 pentacyclic ring system, while compounds 2 and 3 possess unusual 5/6/6/7 tetracyclic skeletons. Their structures were characterized through extensive spectroscopic analyses, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. Additionally, we demonstrated that compound 4 can be readily converted into compounds 1‒3 under mild acidic conditions and proposed a plausible mechanism for this conversion. Bioactivity evaluation of compounds 1‒9 against CVB3 revealed the inhibitory effects of all compounds against the virus. Notably, compound 9 exhibited superior antiviral activity, surpassing the commercial drug ribavirin in selectivity index (SI) value.
Antiviral Agents/isolation & purification*
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Aspergillus/chemistry*
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Molecular Structure
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Enterovirus B, Human/drug effects*
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Endophytes/chemistry*
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Cytochalasins/isolation & purification*
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Drug Discovery
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Humans
3.Jasurolignoside from Ilex pubescens exerts a therapeutic effect on acute lung injury in vitro and in vivo by binding to TLR4.
Shan HAN ; Chi Teng VONG ; Jia HE ; Qinqin WANG ; Qiumei FAN ; Siyuan LI ; Jilang LI ; Min LIAO ; Shilin YANG ; Renyikun YUAN ; Hongwei GAO
Chinese Journal of Natural Medicines (English Ed.) 2025;23(9):1058-1068
Acute lung injury (ALI) is a severe disease caused by viral infection that triggers an uncontrolled inflammatory response. This study investigated the capacity of jasurolignoside (JO), a natural compound, to bind to Toll-like receptor 4 (TLR4) and treat ALI. The anti-inflammatory properties of JO were evaluated in vitro through Western blotting, enzyme-linked immunosorbent assay (ELISA), immunofluorescence staining, and co-immunoprecipitation. The investigation utilized a lipopolysaccharide (LPS)-induced ALI animal model to examine the therapeutic efficacy and mechanism of JO in vivo. JO attenuated inflammatory symptoms in infected cells and tissues by modulating the NOD-like receptor family pyrin domain containing protein 3 (NLRP3) inflammasome and the nuclear factor κB (NF-κB)/mitogen-activated protein kinase (MAPK) pathway. Molecular docking simulations revealed JO binding to TLR4 active sites, confirmed by cellular thermal shift assay. Surface plasmon resonance (SPR) demonstrated direct interaction between JO and TLR4 with a Kd value of 35.1 μmol·L-1. Moreover, JO inhibited tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), and IL-6 secretion and reduced leukocyte, neutrophil, lymphocyte, and macrophage infiltration in ALI-affected mice. JO also enhanced lung function and reduced ALI-related mortality. Immunohistochemical staining demonstrated JO's ability to suppress TLR4 expression in ALI-affected mouse lung tissue. This study establishes that JO can bind to TLR4 and effectively treat ALI, indicating its potential as a therapeutic agent for clinical applications.
Toll-Like Receptor 4/chemistry*
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Animals
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Acute Lung Injury/chemically induced*
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Mice
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Humans
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Ilex/chemistry*
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Molecular Docking Simulation
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Male
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NF-kappa B/immunology*
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Mice, Inbred C57BL
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NLR Family, Pyrin Domain-Containing 3 Protein/immunology*
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Tumor Necrosis Factor-alpha/genetics*
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Interleukin-1beta/genetics*
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RAW 264.7 Cells
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Disease Models, Animal
4.Neutrophil-to-lymphocyte ratio may help predict pediatric testicular torsion in chlidren with acute scrotal pain before surgery
Xianya HE ; Chen WANG ; Yongjun YANG ; Junjie CHEN ; Xuecheng WU ; Zhuo LI ; Zhe LIU ; Guangqing SONG ; Yili TENG ; Jia CHEN ; Hongwei WANG ; Huayi ZHENG ; Yuanwei LI ; Qiang LU
Journal of Modern Urology 2024;29(9):785-789
Objective To explore the feasibility and accuracy of neutrophil-to-lymphocyte ratio(NLR)in the prediction of testicular torsion(TT)in children with acute scrotal pain.Methods A retrospective case-control study was performed on 158 pediatric patients with ultrasound suspicion of TT who underwent surgical testicular examination during Jan.2017 and Jan.2024.The patients were divided into TT group and non-TT group.Clinical data and laboratory data at admission were analyzed.Sensitivity and specificity of NLR to TT were determined with the area under the curve(AUC)represented on the receiver operating characteristic(ROC)curves.Results There were with no statistically significant differences in clinical data between the two groups(P>0.05).The NLR was significantly higher in the TT group than in the non-TT group[(4.82±2.37)vs.(2.85±0.75),P<0.05].The optimal cut-off value of TT predicted by NLR was 2.07,the AUC was 0.809(95%CI:0.709-0.909),and the sensitivity and specificity were 97.9%and 93.3%,respectively,which were significantly higher than other factors.Conclusion For suspicious ultrasound diagnosis of pediatric acute scrotal pain cases,NLR can be used to predict the possibility of TT and may help to evaluate the urgent surgical treatment in these patients.
5.Effect of ropivacaine combined with dexmedetomidine in transversus abdominis plane block on postoperative stress hormone and cognitive function in patients undergoing laparoscopic radical gastrectomy
Hongwei ZHANG ; Weiwei WANG ; Xiaofang LI ; Teng FAN ; Wenke MA ; Xiuqin YUE
Journal of Xinxiang Medical College 2024;41(3):245-250,256
Objective To explore the effect of ropivacaine combined with dexmedetomidine in transversus abdominis plane block(TAPB)on postoperative stress hormones and cognitive function in patients undergoing laparoscopic radical gastrectomy.Methods A total of 80 patients undergoing laparoscopic radical gastrectomy at the First Affiliated Hospital of Xinxiang Medical University from April to October 2023 were selected as the research subjects.According to different anesthesia methods,the patients were divided into the observation group and the control group,with 40 patients in each group.Patients in the observation group were injected bilaterally with 2.5 g·L-1 ropivacaine and 0.5 μg·kg-1 dexmedetomidine for TAPB,with 20 mL injection on each side.Patients in the control group were injected bilaterally with 2.5 g·L-1 ropivacaine for TAPB,with 20 mL injection on each side.Mean arterial pressure(MAP)and heart rate(HR)were recorded at the time of admission to the operating room(T1),immediately after endotracheal intubation(T2),40 minutes after pneumoperitoneum(T3),and 15 minutes after extubation(T4).Radioimmunoprecipitation was used to detect serum cortisol(COR)level,and enzyme-linked immunosorbent assay was used to measure serum norepinephrine(NE)and epinephrine(E)levels at 1,6,12,and 24 hours after surgery.Visual analog scale(VAS)was used to assess pain at rest,and Ramsay sedation scale(RSS)was used to evaluate sedation depth.The doses of propofol and sufentanil were compared between the two groups.Serum β-amyloid(Aβ)and S100β protein levels at 1 day before surgery,1 and 3 days after surgery were detected by using the enzyme-linked immunosorbent assay,and cognitive function was assessed at the same time points by using the mini-mental state examination(MMSE).Results At T,and T2,there was no significant difference in MAP and HR between the control group and the observation group(P>0.05).At T3 and T4,MAP and HR in the observation group were significantly lower than those in the control group(P<0.05).At 1,6,and 12 hours postoperatively,VAS score in the observation group was significantly lower than that in the control group(P<0.05).At 24 hours postoperatively,there was no significant difference in VAS score between the control group and observation group(P>0.05).At 1 and 6 hours postoperatively,RSS score in the observation group was significantly higher than that in the control group(P<0.05).At 12 and 24 hours postoperatively,there was no significant difference in RSS score between the control group and observation group(P>0.05).At 1,6,and 12 hours postoperatively,COR,NE,and E levels in the observation group were significantly lower than those in the control group(P<0.05).At 24 hours postoperatively,there was no significant difference in COR,NE,and E levels between the control group and observation group(P>0.05).The doses of propofol and sufentanil in the observation group were significantly lower than those in the control group(P<0.05).One day before surgery,there was no significant difference in MMSE score between the control group and observation group(P>0.05).At 1 and 3 days postoperatively,MMSE score in the observation group was significantly higher than that in the control group(P<0.05).One day before surgery,there was no significant difference in serum Aβ and S100β protein levels between the control group and observation group(P>0.05).At 1 and 3 days postoperatively,serum Aβ and S100β protein levels in the observation group were significantly lower than those in the control group(P<0.05).Conclusion Ropivacaine combined with dexmedetomidine in TAPB in radical gastrectomy can significantly reduce postoperative pain,increase sedative effect,prolong the duration of TAPB,and benefit patients'postoperative recovery with reduced cognitive impairment.
6.The protective effect of remimazolam combined with thoracic sympathetic nerve block on myocardial ischemia/reperfusion rats
Teng FAN ; Xiaofang LI ; Dan SHEN ; Hongwei ZHANG ; Xiuqin YUE
Chinese Journal of Arteriosclerosis 2024;32(11):955-962
Aim To investigate the protective effect of remimazolam(Re)combined with thoracic sympathetic nerve block(TSNB)on myocardial ischemia/reperfusion(MI/R)rats.Methods Rats were randomly separated into control group,MI/R group,Re group,TSNB group,and Re+TSNB group,with 12 rats in each group.Except for the control group,the remaining rats were subjected to left anterior descending coronary artery(LAD)ligation to construct an MI/R model.In the Re group,20 mg/kg Re was intraperitoneally injected 30 min before ischemia.In TSNB group,0.2%ropivacaine 50 μL was injected into the thoracic epidural catheter 30 min before ischemia.In the Re+TSNB group,20 mg/kg Re was intraperitoneally injected and 0.2%ropivacaine 50 μL was injected into the thoracic epidural catheter 30 min before ischemia.The control group and MI/R group were injected with normal saline only.Rats in each group were evaluated for cardiac function and infarct size.HE staining and TUNEL staining were applied to observe pathological changes in myocardial tissue and myocardial cell apoptosis.Serum myocardial injury markers creatine kinase(CK)and aspartate transaminase(AST),cardiac troponin(cTnⅠ),myocardial inflammatory factors interleukin-8(IL-8),tumor nec-rosis factor-α(TNF-α),and oxidative stress factors malondialdehyde(MDA),superoxide dismutase(SOD)were detec-ted.Western blot was applied to detect the expression of IL-8,TNF-α,B lymphoblastoma-2-associated X protein(Bax),and B-lymphoblastoma-2(Bcl-2)in myocardial tissue.Results Compared with the control group,the myocardial cells of rats showed edema and myocardial fiber disorder in the MI/R group,the left ventricular developmental pressure(LVDP),maximal left ventricular pressure rising rate(+dp/dtmax),maximal left ventricular pressure decreasing rate(-dp/dtmax),SOD activity,and level of Bcl-2 were significantly reduced,the myocardial infarction area,cell apoptosis rate,levels of cTnⅠ,CK,AST,IL-8,TNF-α,MDA,and Bax were increased(P<0.05).Compared with the MI/R group,the morphology of myocardial fibers and myocardial cells was significantly improved in the Re group,TSNB group and Re+TSNB group,the LVDP,±dp/dtmax,SOD activity,and level of Bcl-2 were significantly increased,the myocardial infarction area,cell apoptosis rate,levels of cTnI,CK,AST,IL-8,TNF-α,MDA,and Bax were significantly decreased(P<0.05).Compared with the Re group and TSNB group,the LVDP,±dp/dtmax,SOD activity,and level of Bcl-2 were significantly increased in the Re+TSNB group,the myocardial infarction area,cell apoptosis rate,levels of cTnⅠ,CK,AST,IL-8,TNF-α,MDA,and Bax were significantly decreased(all P<0.05).Conclusion The combination of Re and TSNB may protect against MI/R injury by reducing myocardial infarction and myocardial cell apoptosis,and inhibiting inflammatory response and oxidative stress.
7.Clinical application value of single pass scanning using multi-slice spiral CT for polytrauma patients
Gang WANG ; Ying ZHANG ; Teng TANG ; Hongyang DAI ; Nan WANG ; Mimi QIU ; Hongwei XU ; Fangfang XIA ; Xinglin XIANG ; Jian LI
Chinese Journal of Radiological Medicine and Protection 2024;44(8):693-698
Objective:To explore the clinical application value of single pass scanning using muti-slice spiral CT for polytrauma patients.Methods:Totally 60 polytrauma patients treated from January to November in 2023 were randomly enrolled in this study. They were categorized into an experimental group and a control group using a random number table, with 30 patients in each group. The patients in the experimental group underwent single pass scaning for the head, neck, chest, and abdomen, whereas those in the control group receiving separate scanning for various parts. Then, the noise, signal-to-noise ratio (SNR), and contrast-to-noise (CNR) of the CT images of both groups were recorded. Furthermore, the objective and subjective evaluation, volume CT dose index (CTDI vol), effective dose ( E), scanning time, and scan ranges of the images were compared between both groups. Results:Compared to the control group, the test group exhibited lower SNR of the head ( t = -5.47, P < 0.05) and higher SNR and CNR of the chest scans ( t = -5.95, -6.15, P < 0.05). Furthermore, the test group demonstrated decreased ED, CTDIvol, scanning time, and scan range, which dropped from 18.53 mSv to 13.81 mSv ( t = 3.29, P < 0.001), from 15.77 mGy to 10.59 mGy ( t = 4.48, P< 0.001), from 31.68 s to 10.97 s ( t = 6.95, P < 0.001), and from 64.92 cm to 45.21 cm ( t = 9.05, P < 0.001), respectively compared to the control group. Conclusions:Single pass CT scanning can reduce E, scanning time, and scan range in the treatment of polytrauma patients while ensuring the high quality of CT images, thus warranting wide clinical applications.
8.Application of MRI-related indicators of posterior cruciate ligament in the diagnosis of anterior cruciate ligament injury: an update
Yongkang NIU ; Gengxin JIA ; Yi CHEN ; Yuanjun TENG ; Dejian XIANG ; Xiaoyuan LIANG ; Zhi YI ; Hongwei ZHAN ; Yayi XIA
Chinese Journal of Trauma 2023;39(6):570-576
The main function of anterior cruciate ligament (ACL) is to maintain stability of the knee joint and prevent anterior displacement of the tibial plateau. ACL injury accounts for more than 50% of the knee joint injuries. If not timely handled, it will increase the risk of secondary injuries to structures such as the meniscus and cartilage, causing chronic pain and degeneration of the knee joint. Although most ACL injuries can be determined by their direct signs on MRI, the identification of complex situations and partial tears of ACL are still not satisfactory, which subsequently affects treatment strategies. After ACL injury, changes in anatomical relationship of the knee joint can also lead to morphological changes in other structures such as the posterior cruciate ligament (PCL) on MRI, and these indirect signs can assist in the diagnosis of ACL injury. The authors reviewed the application of MRI-related indicators of PCL in diagnosing ACL injury, hoping to provide references and new ideas for clinical decision-making.
9.Effect of superior cervical ganglion block on cardiac function and NLRP3 signaling pathway in a rat model of myocardial ischemia-reperfusion
Ziwei GUO ; Xiaofang LI ; Hongwei ZHANG ; Teng FAN ; Xueying ZHANG ; Yumiao WANG ; Xin YANG ; Mengli YANG ; Jie YIN ; Li LI ; Xiuqin YUE
Chinese Journal of Anesthesiology 2023;43(5):597-601
Objective:To evaluate the effect of superior cervical ganglion block (SCGB) on cardiac function and nucleotide like receptor protein 3 (NLRP3) signaling pathway in a rat model of myocardial ischemia-reperfusion (I/R).Methods:Sixty healthy SPF male Sprague-Dawley rats, weighing 250-300 g, aged 2-3 months, were divided into 4 groups ( n=15 each) using a random number table method: sham operation group (sham group), myocardial I/R group (IR group), myocardial I/R + normal saline group (IR+ NS group), and myocardial I/R + SCGB group (IR+ SCGB group). Myocardial I/R model was developed by ligation of the left anterior descending branch of the coronary artery for 45 min followed by restoration of blood flow in anesthetized aninals. IR+ SCGB group received SCGB (0.25% ropivacaine 0.1 ml) at 10 min before reperfusion once a day for 2 consecutive weeks, while 0.9% sodium chloride was given instead of ropivacaine in IR+ NS group. Blood samples were collected at 24 h and 14 days of reperfusion for determination of serum concentrations of norepinephrine (NE), troponin T (TnT), tumor necrosis factor-alpha (TNF-α), interleukin-18 (IL-18) and IL-1β by enzyme-linked immunosorbent assay. Echocardiography was performed before ischemia and at 14 days of reperfusion, and left ventricular short axis shortening rate (FS), ejection fraction (EF), and cardiac output (CO) were measured. The rats were sacrificed at 14 days of reperfusion and the hearts were taken for determination of the contents of norepinephrine (NE) in myocardial tissues in the infarction area (by enzyme-linked immunosorbent assay), percentage of myocardial fibrosis area (by Masson staining), M1 macrophage marker CD68 + cell count in the infarction area (by immunohistochemical method), and expression of NLRP3 and gasdermin D (GSDMD) in myocardial tissues (by Western blot). Results:Compared with Sham group, the serum concentrations of TnT, TNF-α, IL-18 and IL-1β, percentage of myocardial fibrosis area, and NE levels in serum and myocardial tissues were significantly increased, the expression of NLRP3 and GSDMD in myocardial tissues was up-regulated, CD68 + cell count was increased, and EF, CO and FS were decreased in IR group ( P<0.05). Compared with IR group, the serum concentrations of TnT, TNF-α, IL-18 and IL-1β, percentage of myocardial fibrosis area, and NE levels in serum and myocardial tissues were significantly decreased, the expression of NLRP3 and GSDMD in myocardial tissues was down-regulated, CD68 + cell count was decreased, and EF, CO and FS were increased in IR+ SCGB group ( P<0.05), and no statistically significant changes were found in the parameters mentioned above in IR+ NS group ( P>0.05). Conclusions:SCGB can improve the cardiac function in a rat model of myocardial I/R, and the mechanism may be related to the inhibition of NLRP3 signaling pathway.
10.Chaihu Longgu Mulitang in Treatment of Coronary Heart Disease Complicated with Anxiety and Depression: A Review
Bo NING ; Xishu TAN ; Hongwei HE ; Hao WEN ; Teng GE ; Yongqing WU ; Hubin YU ; Lanshuan FENG ; Shilin LI ; Jiongdong XIE ; Mingjun ZHAO
Chinese Journal of Experimental Traditional Medical Formulae 2023;29(18):218-228
Coronary heart disease (CHD) with atherosclerosis is a common chronic disease worldwide, and anxiety and depression are potential and crucial risk factors for adverse prognosis in CHD. Chaihu Longgu Mulitang (CLMT), first mentioned in the Shang Han Lun (《伤寒论》), is a classic prescription for treating Shaoyang diseases combined with disturbance of the mind and spirit, with the effects of harmonizing Shaoyang and calming the mind. Current research on mechanisms has shown that CLMT can play a role in CHD complicated with anxiety and depression through multiple pathways, including regulating related signaling pathways, inhibiting the expression of inflammatory factors, improving oxidative stress damage, modulating neurotransmitter levels, suppressing the hypothalamic-pituitary-adrenal axis, promoting mobilization of mesenchymal stem cells from the bone marrow, and inhibiting platelet activation. Clinical studies have demonstrated that CLMT significantly improves symptoms such as angina and insomnia caused by CHD complicated with anxiety and depression, effectively reduces negative emotions, improves traditional Chinese medicine (TCM) syndrome scores, and decreases levels of inflammatory factors. Furthermore, it has fewer adverse reactions and higher safety than conventional western medicine treatments. This article provides a review of the mechanisms and clinical studies of CLMT in the treatment of CHD complicated with anxiety and depression based on a comprehensive analysis of literature from the China National Knowledge Infrastructure (CNKI), Wanfang Data, VIP, PubMed, and other databases in the past 15 years, in order to provide references for further research on the use of CLMT in the management of CHD complicated with anxiety and depression.

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