1.Analysis and prediction of the incidence trend of congenital syphilis in China in 2005 - 2020
Yongfa QIN ; Yatao BI ; Jia ZHAO ; Zhenli WU ; Xue HAN
Journal of Public Health and Preventive Medicine 2026;37(2):12-16
Objective To analyze the incidence of congenital syphilis in four regions of China from 2005 to 2020 and predict its change trend, and to provide a scientific basis for the prevention and control of congenital syphilis. Methods The incidence data of congenital syphilis in eastern, western, central and northeastern China from 2005 to 2020 were collected. The annual change percentage (APC) and average annual change percentage (AAPC) were calculated by Joinpoint software, and the change trend was analyzed. The ARIMA model was established by SPSS26.0 software to predict the incidence from 2021 to 2025. Results From 2005 to 2020, there were 107 504 cases of congenital syphilis, and the incidence reached the peak in 2011, which was 0.90/100 000, and decreased to 0.09/100 000 in 2020. The incidence of congenital syphilis in the eastern, central, western, and northeastern regions of China decreased to 0.07/100 000, 0.06/100 000, 0.12/100 000, and 0.15/100 000 in 2020, respectively. Joinpoint regression analysis found that from 2005 to 2020, the incidence of congenital syphilis showed a downward trend in the whole country (AAPC=-8.68%, t=-5.18, P<0.05), the eastern region (AAPC=-12.01%, t=-6.81, P<0.05), the central region (AAPC=-5.45%, t=-2.09, P<0.05), and the western region (AAPC=-6.05%, t=-3.00, P<0.05), while the incidence in the northeast region was relatively stable (AAPC=-1.66%, t=-1.18,P>0.05). The ARIMA (2,2,0) model was constructed to predict that the annual incidence of congenital syphilis from 2021 to 2025 would be 0.06/100,000, 0.03/100,000, 0.02/100,000, 0.01/100,000, and 0.01/100,000, respectively. Conclusion From 2005 to 2020, the incidence of congenital syphilis in China shows an overall downward trend. The western and northeastern regions are the key prevention and control areas, and the work of "eliminating mother to child transmission of syphilis" needs to be continuously promoted.
2.IgG4-related hypertrophic pachymeningitis: A clinical analysis of seven cases
Journal of Apoplexy and Nervous Diseases 2025;42(12):1131-1135
Objective Immunoglobulin G4-related hypertrophic pachymeningitis (IgG4-RHP) is a rare autoimmune disorder. This study aims to conduct a clinical analysis of seven cases with IgG4-RHP to enhance the understanding of this disease. Methods A retrospective analysis was conducted on seven patients diagnosed with IgG4-RHP. The demographic data, clinical manifestations, laboratory examinations, cerebrospinal fluid analysis, imaging, pathological manifestations, treatments, and efficacy analysis data were collected. Results The patients’ ages ranged from 38 to 67 years, with most being males. Headache (6/7) and cranial nerve palsies (5/7) were the most common clinical symptoms. Notably, one case presented with seizures and another with limb weakness. All patients exhibited elevated serum IgG4 levels (1.48-3.25 g/L). Imaging studies revealed varying degrees of dural thickening and enhancement located in the global dura, tentorium cerebelli, cavernous sinus, and thoracic spinal dura. A definitive pathological diagnosis was obtained via biopsy (intracranial, nasal sinus, or orbital) in 3 patients. All patients received glucocorticoid therapy, with 5 receiving combined cyclophosphamide due to extensive or severe lesions. At the 6-month follow-up, 2 patients achieved complete response, 4 showed partial response, and 1 showed no response. During long-term follow-up, one patient experienced relapse during steroid tapering, which ended up in response again after immunosuppressive regimen adjustment. Conclusion IgG4-RHP is characterized by significant heterogeneous manifestations, which may involve the spinal cord or induce seizures. Diagnosis requires a combination of serological, radiological, and pathological results. While glucocorticoids with immunosuppressants are the main treatment measures, patients with long disease duration and significant fibrosis may respond poorly, highlighting the importance of early intervention and the exploration of novel therapies for refractory cases.
Diagnosis
3.Effects of LINC01772 on cell cycle,apoptosis and radiosensitivity of A549
Lifei HE ; Lin ZHU ; Feng XUE ; Zuyue BI ; Zhaoxin LI
The Journal of Practical Medicine 2025;41(5):657-663
Objective To explore the effects of long non-coding RNA LINC01772 on cell cycle,apoptosis and radiotherapy sensitivity of A549.Methods A549 cells were resuscitated and cultured for experimental pur-pose.The effects of LINC01772 knockdown on cell viability,cell cycle progression,and apoptosis were assessed using CCK-8 assays and flow cytometry,and apoptosis-related proteins were analyzed using western blotting.CCK-8 and clonogenic assays were used to measure the changes in the sensitivity of A549 cells to radiotherapy following various radiation doses,and flow cytometry to examine alterations in the cell cycle and apoptosis post-radiation treatment.Results Following lentiviral transfection that reduced LINC01772 levels in A549 cells,a significant decrease in cell viability(P<0.01)was observed alongside an increase in apoptosis(P<0.01).Notably,expres-sions of Bad and Cleaved Caspase-3 were significantly elevated(P<0.01),while Bcl-2 expression was markedly decreased(P<0.01).After exposure to different radiation doses,a dose-dependent reduction in A549 cell viability was noted(P<0.01),accompanied by a significant impairment of clonogenic ability(P<0.01),G2/M phase arrest within the cell cycle(P<0.01),and an increased incidence of apoptosis(P<0.01).Conclusion Inhibiting long non-coding RNA LINC01772 expression substantially diminishes cellular viability in A549 cells,enhances apoptotic processes,disrupts their cycling mechanisms,and augments their sensitivity to radiotherapy,suggesting that this non-coding RNA may serve as a potential target for enhancing lung cancer radiotherapy.
4.Guideline for Adult Weight Management in China
Weiqing WANG ; Qin WAN ; Jianhua MA ; Guang WANG ; Yufan WANG ; Guixia WANG ; Yongquan SHI ; Tingjun YE ; Xiaoguang SHI ; Jian KUANG ; Bo FENG ; Xiuyan FENG ; Guang NING ; Yiming MU ; Hongyu KUANG ; Xiaoping XING ; Chunli PIAO ; Xingbo CHENG ; Zhifeng CHENG ; Yufang BI ; Yan BI ; Wenshan LYU ; Dalong ZHU ; Cuiyan ZHU ; Wei ZHU ; Fei HUA ; Fei XIANG ; Shuang YAN ; Zilin SUN ; Yadong SUN ; Liqin SUN ; Luying SUN ; Li YAN ; Yanbing LI ; Hong LI ; Shu LI ; Ling LI ; Yiming LI ; Chenzhong LI ; Hua YANG ; Jinkui YANG ; Ling YANG ; Ying YANG ; Tao YANG ; Xiao YANG ; Xinhua XIAO ; Dan WU ; Jinsong KUANG ; Lanjie HE ; Wei GU ; Jie SHEN ; Yongfeng SONG ; Qiao ZHANG ; Hong ZHANG ; Yuwei ZHANG ; Junqing ZHANG ; Xianfeng ZHANG ; Miao ZHANG ; Yifei ZHANG ; Yingli LU ; Hong CHEN ; Li CHEN ; Bing CHEN ; Shihong CHEN ; Guiyan CHEN ; Haibing CHEN ; Lei CHEN ; Yanyan CHEN ; Genben CHEN ; Yikun ZHOU ; Xianghai ZHOU ; Qiang ZHOU ; Jiaqiang ZHOU ; Hongting ZHENG ; Zhongyan SHAN ; Jiajun ZHAO ; Dong ZHAO ; Ji HU ; Jiang HU ; Xinguo HOU ; Bimin SHI ; Tianpei HONG ; Mingxia YUAN ; Weibo XIA ; Xuejiang GU ; Yong XU ; Shuguang PANG ; Tianshu GAO ; Zuhua GAO ; Xiaohui GUO ; Hongyi CAO ; Mingfeng CAO ; Xiaopei CAO ; Jing MA ; Bin LU ; Zhen LIANG ; Jun LIANG ; Min LONG ; Yongde PENG ; Jin LU ; Hongyun LU ; Yan LU ; Chunping ZENG ; Binhong WEN ; Xueyong LOU ; Qingbo GUAN ; Lin LIAO ; Xin LIAO ; Ping XIONG ; Yaoming XUE
Chinese Journal of Endocrinology and Metabolism 2025;41(11):891-907
Body weight abnormalities, including overweight, obesity, and underweight, have become a dual public health challenge in Chinese adults: overweight and obesity lead to a variety of chronic complications, while underweight increases the risks of malnutrition, sarcopenia, and organ dysfunction. To systematically address these issues, multidisciplinary experts in endocrinology, sports science, nutrition, and psychiatry from various regions have held multiple weight management seminars. Based on the latest epidemiological data and clinical evidence, they expanded the guideline to include assessment and intervention strategies for underweight, in addition to the core content of obesity management. This guideline outlines the etiological mechanisms, evaluation methods, and multidimensional management strategies for overweight and obesity, covering key areas such as diagnosis and assessment, medical nutrition therapy, exercise prescription, pharmacological intervention, and psychological support. It is intended to provide a scientific and standardized approach to weight management across the adult population, aiming to curb the rising prevalence of obesity, mitigate complications associated with abnormal body weight, and improve nutritional status and overall quality of life.
5.Chemical constituents from Euphorbia humifusa and their in vitro anti-hepatoma activity
Si-fan YAO ; Wu-hui SUN ; Yi ZHANG ; Wen AI ; Xue-jing LI ; Bi-qing ZHAO ; Xiao-jiang ZHOU
Chinese Traditional Patent Medicine 2025;47(7):2243-2249
AIM To study the chemical constituents from Euphorbia humifusa Willd.and their in vitro anti-hepatoma activity.METHODS Silica gel,D101 macroporous adsorption resin and semi-preparative RP-HPLC were used for isolated and purified,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The anti-hepatocellular carcinoma activity was determined by MTT mothod.RESULTS Eighteen compounds were isolated and identified as 22-O-angeloyl-R1-barrigenol(1),dimethyl 3,3'-[oxybis(4,1-phenylene)](2E,2'E)-diacrylate(2),N-(3-methoxy-1,3-dioxopropyl)-D-tryptophan methyl ester(3),N-acetyltryptophan methyl ester(4),N-(methoxycarbonyl)-tryptophan methyl ester(5),(3β,5α,17β)-4,4,8,14-tetramethyl-18-norandrostane-3,17-diol(6),3β,18,19β-trihydroxylupane(7),pregnenolone(8),3-hydroxy-5,6-epoxy-7-megastigmen-9-one(9),dehydrovomifoliol(10),loliolide(11),2,2'-oxybis(1,4-di-tert-butylbenzene)(12),dibutyl phthalate(13),4-methoxycinnamic acid(14),3,4-dimethoxycinnamic acid(15),methyl 4-hydroxybenzoate(16),kaempferol(17),quercetin(18).The IC50 values of compounds 1,7 and 8 on HepG2 cells were(17.27±0.92),(19.11±2.14)and(7.53±1.09)μmol/L,respectively.CONCLUSION Compounds 1-16 are first isolated from this plant.Compounds 1,7 and 8 have anti-hepatoma activity.
6.Short-term outcome study on cervical deep lymph node-venous anastomosis technique in the treatment of Alzheimer’s disease
Cheng GAN ; Zhengdong KONG ; Xiaoye RAN ; Shudong QIAO ; Yixin ZHANG ; Lu YUE ; Yingjie WANG ; Hui BI ; Dong YANG ; Hongtong MA ; Yuan CHEN ; Hongli CHAI ; Ying JIA ; Chenhao MA ; Zixiang CHEN ; Ke LI ; Miao WANG ; Liguo XUE ; Siwen ZHAO ; Ke WEN ; Lin YIN ; Bo DING ; Shan ZHU ; Yuanbo LIU ; Mengqing ZANG
Chinese Journal of Plastic Surgery 2025;41(2):130-143
Objective:To explore the short-term clinical effects of deep cervical lymph node-venous anastomosis in the treatment of Alzheimer’s disease (AD).Methods:A prospective exploratory study was conducted on the treatment of AD patients using the cervical deep lymph node-venous anastomosis technique in Scar and Wound Treatment Department, Plastic Surgery Hospital, Chinese Academy of Medical Sciences, from September to October 2024. The patients underwent high-frequency ultrasound to locate deep cervical lymph nodes and the external jugular vein. Under general anesthesia, bilateral deep cervical lymph node-venous anastomoses were performed. Indocyanine green (ICG) lymphography was conducted via subcutaneous injection behind the ear to visualize lymph nodes in levels Ⅱ and Ⅲ. After making a skin incision along the posterior margin of the sternocleidomastoid muscle, the external jugular vein, internal jugular veins, and associated lymph nodes were exposed. Adjacent veins were selected for anastomosis of lymph node. Using microsurgical techniques, end-to-side or end-to-end anastomosis was completed for lymph nodes in levels Ⅱ and Ⅲ. Preoperative assessments included the mini-mental state examination (MMSE, a higher score indicates better cognitive function), Alzheimer’s disease assessment scale-cognitive subscale (ADAS-Cog, a higher score indicates greater impairment of cognitive function), Alzheimer’s disease cooperative study scale for activities of daily living (ADCS-ADL, a higher score indicates better ability to perform daily activity), and neuropsychiatric inventory (NPI, a higher score indicates more severe behavioral and emotional symptom). Postoperative follow-up included the same scales to observe changes in cognitive function, activities of daily living, and emotional communication.Results:Four patients (1 male, 3 females, aged 58-79 years) with AD were included. All were diagnosed based on cerebrospinal fluid biomarkers. All patients successfully underwent bilateral deep cervical lymph node-venous anastomoses. On average, 4.3 (2-7 per person) anastomoses were performed per patient. Surgical procedures lasted an average of 6.5 h (5.5-8.5 h) with minimal blood loss (less than 50 ml). Patients resumed normal activity within 6 hours postoperatively and were discharged after an average of 4.1 d (3.5-5.0 d). Postoperative complications included one case each of aspiration pneumonia, lower limb venous thrombosis, and transient delirium, all of whom resolved without long-term effects. Clinical symptoms, including memory decline, mood swings, and anxiety, showed varying degrees of improvement. Patients reported enhanced quality of life, emotional stability, and social engagement, confirming the procedure’s safety and potential cognitive benefits. At one month postoperatively, the MMSE scores of the four patients increased by an average of 0.8 points compared to preoperative levels. Additionally, the two patients who completed the ADAS-Cog assessments showed a decrease in their scores (reduced by 1.0 points and 11.3 points, respectively, compared to preoperative scores), indicating a certain degree of improvement in cognitive function during this period. The ADCS-ADL and NPI scores of four patients varied significantly, without showing any clear pattern.Conclusion:Lymphovenous anastomosis of the deep cervical lymph node-venous anastomosis may provide a new surgical intervention approach for AD, but further large-scale studies and long-term follow-up are needed to validate its safety and effectiveness.
7.Preparation of decellularized extracellular matrix-gelatin methacryloyl composite hydrogels and their effects on hepatocyte proliferation
Jing SHI ; Jin CHU ; Tao SUN ; Jin GAO ; Xiaolong HE ; Ning YANG ; Liang LI ; Xue ZHANG ; Hui LIU ; Guodong LYU ; Renyong LIN ; Xiaojuan BI
International Journal of Biomedical Engineering 2025;48(1):47-55
Objective:To prepare decellularized extracellular matrix (dECM)-gelatin methacryloyl (GelMA) composite hydrogels and to study their effects on hepatocyte proliferation.Methods:Hepatic dECM was prepared by elution, and GelMA hydrogel and 10%, 30% and 50% dECM-GelMA composite hydrogels were prepared by pepsin solubilization. The morphology of normal liver and dECM liver was observed by eyes and scanning electron microscopy using hematoxylin-eosin, Sirius red and periodate-Schiff staining, respectively. The internal structure of the dECM-GelMA composite hydrogels was observed by scanning electron microscopy, and the pore diameter was measured. Liver HL-7702 cells were co-cultured with GelMA hydrogel and 10%, 30% and 50% dECM-GelMA composite hydrogels, and the cell proliferation viability was determined by cell counting kit-8. The expression of proliferating cell nuclear antigen (PCNA), Wnt family protein 5a (Wnt5a), β-catenin, extracellular-regulated protein kinase 1/2 (ERK1/2) and phosphorylated ERK1/2 (p-ERK1/2) were detected by Western blotting. Comparisons were made using independent sample t-test or one-factor analysis of variance. Results:After decellularization, the hepatocyte morphology showed rounded depressions, and the extracellular matrix structure was intact. The GelMA hydrogel and 10%, 30% and 50% dECM-GelMA composite hydrogels showed inernally porous structures. The pore diameter increased from (3.06±1.35) μm in the GelMA hydrogel to (16.01±4.02) μm in the 50% dECM-GelMA composite hydrogel. On the 3rd, 5th and 7th day, the relative cell proliferation was higher in the 50% dECM-GelMA composite hydrogel group than that in the GelMA hydrogel group (1.89±0.04 vs 1.53±0.01, 9.36±0.04 vs 3.89±0.09, 7.15±0.27 vs 4.89±0.15, all P<0.05). The relative expression levels of PCNA, Wnt5a, β-catenin, and p-ERK1/2/ERK1/2 proteins in the 50% dECM-GelMA composite hydrogel group were higher than those in the GelMA hydrogel group (2.14±0.04 vs 1.00±0.03, 2.36±0.09 vs 1.00±0.08, 1.45±0.03 vs 1.00±0.04, 1.43±0.04 vs 1.00±0.01, all P<0.05). Conclusions:A dECM-GelMA composite hydrogel can be prepared, which may promote hepatocyte proliferation by upregulating the phosphorylation of ERK1/2 and activating Wnt/β-catenin signaling pathway.
8.Preparation of heparin-modified gelatin methacryloyl microspheres and their liver-targeted delivery of ADSCs
Xiaotong LI ; Jin CHU ; Hongbin ZHANG ; Bowen SHI ; Xue ZHENG ; Junlong XUE ; Liang LI ; Renyong LIN ; Xiaojuan BI
International Journal of Biomedical Engineering 2025;48(5):425-434
Objective:To prepare heparin (Hep)-modified gelatin methacryloyl (GelMA) microspheres and to investigate their application in liver-targeted delivery of adipose-derived mesenchymal stem cells (ADSCs).Methods:GelMA microspheres were modified with Hep to obtain GelMA-Hep microspheres. The surface morphology of the GelMA-Hep microspheres was observed by scanning electron microscopy. The changes of carbon atoms, nitrogen atoms and sulfur atoms on the surface of the GelMA-Hep microspheres were detected by X-ray photoelectron spectroscopy. The surface chemical group composition of the GelMA-Hep microspheres was analyzed by Fourier transform infrared spectrometer. The swelling properties of the GelMA-Hep microspheres were detected by water absorption swelling experiment. Human liver HL-7702 cells transfected with lentivirus were co-cultured with GelMA, GelMA-dopamine (GelMA-dop) and GelMA-Hep microspheres. The effects of microspheres on cell proliferation activity were evaluated by cell counting kit-8 method and live/dead cell staining experiment. The adhesion of microspheres to cells was observed by confocal microscopy. The GelMA-Hep microspheres loaded with ADSCs were injected into C57BL/6 mice through the tail vein, and its efficiency of liver-targeted delivery of ADSCs was observed by a small animal in vivo imaging system. The data were compared by independent sample t test or one-way analysis of variance. Results:The GelMA-Hep microspheres were prepared by modifying the GelMA microspheres with Hep. Compared with the GelMA microspheres, the size of the GelMA-Hep microspheres did not change significantly, and the surface did not collapse and showed some crystalline particles. The binding energy of sulfur atoms on the surface of the GelMA-Hep microspheres increased from 166 eV to 168 eV. On the surface of the GelMA-Hep microspheres, the characteristic peaks of sulfonic acid and sulfate groups of Hep were detected at 1 490 cm ?1 and from 1 135 cm ?1 to 1 050 cm ?1, respectively. The swelling rate of the GelMA-dop microspheres was uniform, while the swelling rate of the GelMA microspheres and the GelMA-Hep microsphere was quite different, but the final swelling mass of the three microspheres tended to be consistent at 5 min. After 12, 24, 36 and 48 h of culture, the relative proliferation of cells in the GelMA-Hep group (1.61±0.29, 1.78±0.05, 2.27±0.08, 2.26±0.33) were higher than those in the negative control group (1.00±0.00, 1.28±0.06, 1.39±0.02, 1.41±0.04) (all P<0.05). After 36 h of culture, the relative proliferation of cells in the GelMA-Hep group was higher than that in the GelMA-dop group (1.63±0.21), with significant difference ( P<0.05). Live/dead cell staining experiment showed that after 12 h of cell culture in the GelMA-Hep group, only a few microspheres had cell adhesion; at 24 h, the cells were densely distributed on the surface of the microspheres. After 36 h, the number of cells increased further. At 48 h, live cells were distributed throughout the microspheres. Confocal microscopy showed that after 24 h of culture, cells adhered to the surface of the microspheres in the GelMA-Hep group and showed a stretched morphology. The liver of the GelMA-Hep+ADSCs group showed strong fluorescence at 0.5 h, and the fluorescence brightness continued to 48.0 h. The number of ADSCs reaching the liver was more than that of ADSCs group and GelMA+ADSCs group. Conclusions:GelMA-Hep microspheres were successfully prepared, which can improve the efficiency of liver-targeted delivery of ADSCs.
9.Analysis of the nonlinear relationship between hypothermic machine perfusion parameters and delayed graft function and construction of an optimized predictive model based on sampling algorithms
Boqing DONG ; Chongfeng WANG ; Yuting ZHAO ; Huanjing BI ; Ying WANG ; Jingwen WANG ; Zuhan CHEN ; Ruiyang MA ; Wujun XUE ; Yang LI ; Xiaoming DING
Organ Transplantation 2025;16(4):582-590
Objective To analyze the nonlinear relationship between hypothermic machine perfusion (HMP) parameters and delayed graft function (DGF) and optimize the construction of a predictive model for DGF. Methods The data of 923 recipients who underwent kidney transplantation from deceased donors were retrospectively analyzed. According to the occurrence of DGF, the recipients were divided into DGF group (n=823) and non-DGF group (n=100). Donor data, HMP parameters and recipient data were analyzed for both groups. The nonlinear relationship between HMP parameters and the occurrence of DGF was explored based on restricted cubic splines (RCS). Over-sampling, under-sampling and balanced sampling were used to address the imbalance in the proportion of DGF to construct logistic regression predictive models. The area under the curve (AUC) of each model was compared in the validation set, and a nomogram model was constructed. Results Donor BMI, cold ischemia time of the donor kidney, and HMP parameters (initial and final pressures, resistance, and perfusion time) were significantly different between the DGF and non-DGF groups (all P<0.05). The RCS analysis revealed a threshold-like nonlinear relationship between HMP parameters and the risk of DGF. Among the models constructed using different sampling methods, the balanced sampling model had the highest AUC. Using this model, a nomogram was constructed to stratify recipients based on risk scores. Recipients in the high-risk group had higher serum creatinine levels at 1, 6, and 12 months after kidney transplantation compared to those in the low-risk group (all P<0.05). Conclusions There is a nonlinear relationship between HMP parameters and the risk of DGF, and the threshold is helpful for organ quality assessment and monitoring of graft function after transplantation. The predictive model for DGF constructed on the base of balanced sampling algorithms helps perioperative decision-making and postoperative graft function monitoring of kidney transplantation.
10.Preparation, characterization, and in vitro anti-liver tumor activity of bufalin nanoparticles with Scrophularia ningpoensis polysaccharide and ursodeoxycholic acid as carriers.
Zhen ZHENG ; Bi-Qi DENG ; Xue-Mei CHEN ; Li-Qiao ZHU ; Hua-Gang SHENG
China Journal of Chinese Materia Medica 2025;50(11):3013-3023
Bufalin(BF)has a significant anti-tumor effect, but its clinical application is severely restricted by its high toxicity and poor water solubility. In this study, Scrophularia ningpoensis polysaccharide(SNP)and ursodeoxycholic acid(UDCA) were synthesized into an SNP-UDCA conjugate. BF was encapsulated to prepare BF/SNP-UDCA nanoparticles(NPs). The amphiphilic compound SNP-UDCA was synthesized via the one-step method, and its structure was characterized by Fourier-transform infrared spectroscopy(FT-IR)and proton nuclear magnetic resonance(~1H-NMR). The preparation process of BF/SNP-UDCA NPs was optimized through single-factor investigations. The encapsulation efficiency and drug-loading capacity of BF/SNP-UDCA NPs were determined by high-performance liquid chromatography(HPLC). The molecular form of BF/SNP-UDCA NPs was characterized by using a transmission electron microscope, X-ray diffraction(XRD), and differential scanning calorimeter(DSC). Additionally, the stability of BF/SNP-UDCA NPs was evaluated. The release behavior of BF/SNP-UDCA NPs at different pH values was determined by dialysis. The in vitro anti-tumor effect of BF/SNP-UDCA NPs was evaluated by MTT cytotoxicity assay, flow cytometry for apoptosis, and cellular uptake. The in vitro liver targeting was evaluated by measuring cellular uptake by laser confocal microscopy. The results demonstrated that the SNP-UDCA conjugate was successfully synthesized through an esterification reaction between SNP and UDCA. The preparation process of BF/SNP-UDCA NPs was as follows: the feed ratio of SNP-UDCA to BF was 2∶1, the ultrasonic time was 30 minutes, and the stirring time was two hours. The prepared BF/SNP-UDCA NPs were spherical in shape, with a particle size of(252.74±6.05)nm, an encapsulation efficiency of 65.00%±2.51%, and a drug-loading capacity of 6.80%±0.44%. The XRD and DSC results indicated that BF was encapsulated within the NPs and existed in a molecular or amorphous state. The short-term stability of BF/SNP-UDCA NPs and stability in DMEM medium are good, and their in vitro release behavior followed the first-order equation and was pH-dependent according to the in vitro experiment. Compared with BF, BF/SNP-UDCA NPs at the same concentration showed significantly stronger cytotoxicity and apoptotic effects on HepG2 cells(P<0.05, P<0.01). The uptake of coumarin 6(C6)/SNP-UDCA NPs in HepG2 cells was time-dependent and higher than that in HeLa cells at the same concentration of C6/SNP-UDCA NPs. Moreover, after treatment with SNP, the uptake of C6/SNP-UDCA NPs in HepG2 cells decreased. In conclusion, the preparation process of BF/SNP-UDCA NPs was simple and feasible. BF/SNP-UDCA NPs could enhance the targeting ability and inhibitory effect of BF on liver cancer cells. This study will provide a foundation for liver-targeting nanoformulations of BF.
Bufanolides/pharmacology*
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Nanoparticles/chemistry*
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Humans
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Drug Carriers/chemistry*
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Ursodeoxycholic Acid/chemistry*
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Antineoplastic Agents/pharmacology*
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Polysaccharides/chemistry*
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Scrophularia/chemistry*
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Liver Neoplasms/physiopathology*
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Hep G2 Cells


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