1.Therapeutic efficacy of ruxolitinib combined with low-dose hormone in aGVHD after allogeneic hematopoietic stem cell transplantation
Yue HU ; Xupai ZHANG ; Sihan LAI ; Shan ZHANG ; Lei MA ; Xiao WANG ; Yan DENG ; Ying HAN ; Ying HE ; Guangcui HE ; Hai YI
Chinese Journal of Blood Transfusion 2026;39(4):506-512
Objective: To evaluate the efficacy and safety of ruxolitinib combined with low-dose hormone for patients with acute graft-versus-host disease (aGVHD) after allogeneic hematopoietic stem cell transplantation (allo-HSCT). Methods: Thirty patients with aGVHD after allo-HSCT admitted to the Department of Hematology of the General Hospital of Western Theater Command from November 2021 to November 2024 were retrospectively analyzed. All patients were treated with low-dose hormone (methylprednisolone 0.3-1 mg kg
-d
) combined with ruxolitinib 5-10 mg d
. The efficacy and adverse reactions were observed during the follow-up period to analyze the survival outcomes of the patients. Results: A total of 30 patients with aGVHD after allo-HSCT were included in this study, consisting of 15 (50%) males and 15 (50%) females with a median age of 34 year-old (ranging from 14 to 62). Classification by disease type: there were 18 cases of acute myeloid leukemia, 4 cases of acute lymphoblastic leukemia, 4 cases of aplastic anemia, and 4 cases of myelodysplastic syndrome. Classification by aGVHD severity: there were 27 cases (90%) of Ⅱ-Ⅳ degree aGVHD and 11 cases (36.7%) of Ⅲ-Ⅳ degree aGVHD. Ruxolitinib in combination with low-dose glucocorticoid treatment yield responses in 28 (93.3%) patients, of which 27 (90%) achieved complete remission (CR), while 1 (3.3%) showed partial remission (PR). One patient (3.3%) had no response (NR), and 1 patient (3.3%) exhibited progressed disease (PD). Overall survival (OS) at 1 year of transplantation was 73.9% (95%CI 49.5% to 87.7%), progression-free survival (PFS) was 93.3% (95%CI 75.9% to 98.3%), non-relapse mortality (NRM) was 20.6% (95%CI 7.9% to 47.4%), and median survival time was 27.6 months. Conclusion: Ruxolitinib combined with low-dose hormones is safe and effective in the treatment of aGVHD after allo-HSCT.
2.Effects of long non-coding RNA KIAA0125 on proliferation and apoptosis of acute myeloid leukemia U937 cells
Huali HU ; Fahua DENG ; Yuancheng LIU ; Siqi WANG ; Jingxin ZHANG ; Tingting LU ; Hai HUANG ; Sixi WEI
Chinese Journal of Tissue Engineering Research 2025;29(19):3983-3991
BACKGROUND:U937 cells can be used as a cell model for studying the biological characteristics,signaling pathways,and therapeutic targets of acute myeloid leukemia.Although it has been reported that long non-coding RNA KIAA0125 is highly expressed in acute myeloid leukemia,its biological function in U937 cells remains unclear,and its mechanism of action in the occurrence and development of acute myeloid leukemia needs to be further clarified. OBJECTIVE:To investigate the expression level of long non-coding RNA KIAA0125 in peripheral blood of patients with acute myeloid leukemia and its effect on the proliferation and apoptosis of U937 cells. METHODS:RNA-sequencing was used to analyze the bone marrow monocyte samples from acute myeloid leukemia patients,and the differentially expressed gene long non-coding RNA KIAA0125 was screened.The expression of long non-coding RNA KIAA0125 in peripheral blood of patients with acute myeloid leukemia was detected by qRT-PCR.The relationship between long non-coding RNA KIAA0125 mRNA expression and prognosis in bone marrow cells of 173 acute myeloid leukemia patients and 70 healthy people was statistically analyzed by GEPIA database.Subsequently,recombinant lentivirus technology and CRISPR/Cas9-SAM technology were used to construct U937 cell lines with knockdown/overexpression of long non-coding RNA KIAA0125.qRT-PCR was used to detect the knockdown/overexpression efficiency of long non-coding RNA KIAA0125.Next,CCK-8 assay,flow cytometry,and western blot assay were used to detect the effects of knockdown/overexpression of long non-coding RNA KIAA0125 on the proliferation and apoptosis of U937 cells.Finally,western blot assay was used to detect the effect of knockdown/overexpressed long non-coding RNA KIAA0125 on Wnt/β-catenin signaling pathway-related proteins. RESULTS AND CONCLUSION:(1)The results of qRT-PCR showed that long non-coding RNA KIAA0125 was highly expressed in peripheral blood of acute myeloid leukemia patients.The results of GEPIA database showed that long non-coding RNA KIAA0125 was highly expressed in bone marrow cells of acute myeloid leukemia patients,and the high expression group had worse overall survival.(2)The knockdown efficiency of long non-coding RNA KIAA0125 in knockdown group was 70%,and the U937 cells that stably down-regulated long non-coding RNA KIAA0125 expression were successfully constructed.The expression of long non-coding RNA KIAA0125 in overexpression group was four times that of vector group,and stable U937 cells were successfully constructed.(3)Knockdown of long non-coding RNA KIAA0125 inhibited the proliferation of U937 cells and promoted their apoptosis.Overexpression of long non-coding RNA KIAA0125 promoted the proliferation of U937 cells but had no significant effect on the apoptosis of U937 cells.(4)Knockdown of long non-coding RNA KIAA0125 inhibited the activity of Wnt/β-catenin signaling pathway,while overexpression of long non-coding RNA KIAA0125 activated Wnt/β-catenin signaling pathway.These results confirm that long non-coding RNA KIAA0125 is highly expressed in acute myeloid leukemia peripheral blood.Long non-coding RNA KIAA0125 may affect the proliferation and apoptosis of U937 cells by regulating the Wnt/β-catenin signaling pathway,and may be a potential prognostic marker for acute myeloid leukemia.
3.Shexiang Tongxin Dropping Pill Improves Stable Angina Patients with Phlegm-Heat and Blood-Stasis Syndrome: A Multicenter, Randomized, Double-Blind, Placebo-Controlled Trial.
Ying-Qiang ZHAO ; Yong-Fa XING ; Ke-Yong ZOU ; Wei-Dong JIANG ; Ting-Hai DU ; Bo CHEN ; Bao-Ping YANG ; Bai-Ming QU ; Li-Yue WANG ; Gui-Hong GONG ; Yan-Ling SUN ; Li-Qi WANG ; Gao-Feng ZHOU ; Yu-Gang DONG ; Min CHEN ; Xue-Juan ZHANG ; Tian-Lun YANG ; Min-Zhou ZHANG ; Ming-Jun ZHAO ; Yue DENG ; Chang-Jiang XIAO ; Lin WANG ; Bao-He WANG
Chinese journal of integrative medicine 2025;31(8):685-693
OBJECTIVE:
To evaluate the efficacy and safety of Shexiang Tongxin Dropping Pill (STDP) in treating stable angina patients with phlegm-heat and blood-stasis syndrome by exercise duration and metabolic equivalents.
METHODS:
This multicenter, randomized, double-blind, placebo-controlled clinical trial enrolled stable angina patients with phlegm-heat and blood-stasis syndrome from 22 hospitals. They were randomized 1:1 to STDP (35 mg/pill, 6 pills per day) or placebo for 56 days. The primary outcome was the exercise duration and metabolic equivalents (METs) assessed by the standard Bruce exercise treadmill test after 56 days of treatment. The secondary outcomes included the total angina symptom score, Chinese medicine (CM) symptom scores, Seattle Angina Questionnaire (SAQ) scores, changes in ST-T on electrocardiogram and adverse events (AEs).
RESULTS:
This trial enrolled 309 patients, including 155 and 154 in the STDP and placebo groups, respectively. STDP significantly prolonged exercise duration with an increase of 51.0 s, compared to a decrease of 12.0 s with placebo (change rate: -11.1% vs. 3.2%, P<0.01). The increase in METs was significantly greater in the STDP group than in the placebo group (change: -0.4 vs. 0.0, change rate: -5.0% vs. 0.0%, P<0.01). The improvement of total angina symptom scores (25.0% vs. 0.0%), CM symptom scores (38.7% vs. 11.8%), reduction of nitroglycerin consumption (100.0% vs. 11.3%), and all domains of SAQ, were significantly greater with STDP than placebo (all P<0.01). The changes in Q-T intervals at 28 and 56 days from baseline were similar between the two groups (both P>0.05). Twenty-five participants (16.3%) with STDP and 16 (10.5%) with placebo experienced AEs (P=0.131), with no serious AEs observed.
CONCLUSION
STDP could improve exercise tolerance in patients with stable angina and phlegm-heat and blood stasis syndrome, with a favorable safety profile. (Registration No. ChiCTR-IPR-15006020).
Humans
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Double-Blind Method
;
Drugs, Chinese Herbal/adverse effects*
;
Male
;
Female
;
Middle Aged
;
Angina, Stable/physiopathology*
;
Aged
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Syndrome
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Treatment Outcome
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Placebos
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Tablets
4.Efficacy of ranibizumab combined with retinal laser photocoagulation in patients with macular edema secondary to BRVO
Fengyun HU ; Lian'e DING ; Fenfen CHEN ; Xiaoli CAO ; Hai CHU ; Kai MA ; Chun DENG
Journal of Navy Medicine 2025;46(8):816-820
Objective To explore the efficacy of ranibizumab combined with retinal laser photocoagulation in patients with macular edema secondary to branch retinal vein occlusion(BRVO)and its impact on best-corrected visual acuity(BCVA)and central macular thickness(CMT).Methods A prospective analysis was conducted on 70 patients with secondary macular edema caused by BRVO who were admitted to the 901th Hospital of Joint Logistics Support Force from March 2019 to March 2023.According to the random number table method,the patients were assigned into study group or control group,with 35 cases in each group.The control group was treated with ranibizumab,while the study group was treated with ranibizumab and retinal laser photocoagulation.The efficacy,BCVA,CMT,intraocular pressure,adverse reactions,and 36-item short form health survey(SF-36)score were compared between the two groups.Results There was a significant difference in the efficacy between the two groups(Z=2.272,P<0.05),and the total effective rate of the study group was higher than that of the control group(P<0.05).The results of repeated measure ANOVA showed that CMT and intraocular pressure decreased significantly,while BCVA increased significantly in both groups after 3 months,6 months,and 12 months of treatment(P<0.05);moreover,these parameters in the study group were superior to those in the control group(P<0.05).There were no significant differences in the incidence of cataracts,transient intraocular pressure elevation,subconjunctival hemorrhage,retinal detachment,or the total incidence of adverse reactions between the two groups(P>0.05).After 12 months of treatment,the total score of SF-36 increased in both groups(P<0.05),and the difference value of total score of SF-36 in the study group was superior to that in the control group(P<0.05).Conclusion The combination of ranibizumab and retinal laser photocoagulation can achieve a good therapeutic effect on macular edema caused by BRVO.It can effectively improve BCVA,CMT and intraocular pressure,reduce the risk of adverse reactions,and enhance the quality of life.
5.Risk factor analysis and nomogram prediction model construction for pneumonia complicating infectious mononucleosis in adults
Fei HU ; Mei-Juan PENG ; Xu-Yang ZHENG ; Rui LI ; Jia-Yi ZHAN ; Hai-Feng HU ; Hong-Kai XU ; Deng-Hui YU ; Hong DU ; Jian-Qi LIAN
Medical Journal of Chinese People's Liberation Army 2025;50(11):1359-1365
Objective To investigate the risk factors for pneumonia complicating infectious mononucleosis(IM)in adults and construct a nomogram prediction model.Methods A retrospective analysis was conducted on 198 IM patients admitted to the Second Affiliated Hospital of Air Force Medical University from January 2015 to December 2021.Patients were divided into pneumonia group(n=52)and non-pneumonia group(n=146)based on whether pulmonary infection occurred during hospitalization.The baseline data(age,gender,place of onset,etc.),clinical manifestations(maximum body temperature,lymph node enlargement,splenomegaly,etc.),and inflammatory indicators[white blood cell count(WBC),C-reactive protein(CRP),etc.]were compared between the two groups.Kaplan-Meier curves were plotted to analyze the key indicators affecting the hospital stay of IM patients.Multivariate logistic regression was used to analyze the independent risk factors for pneumonia complicating IM in adults and construct a nomogram prediction model based on the identified risk factors.The predictive efficacy of the model was evaluated using the receiver operating characteristic(ROC)curve and the consistency of the model was assessed using the calibration curve.The fit of the model was evaluated using the Hosmer-Lemeshow test.Additionally,the sensitivity,specificity,and accuracy of the model were assessed using confusion matrix.Results Compared with non-pneumonia group,the pneumonia group had a significantly higher proportion of patients from rural areas,with body mass index(BMI)≥24 kg/m2,smoking history,hepatomegaly,fever duration of≥7 d,as well as increased total hospitalization costs and average daily hospitalization costs,and prolonged hospital stay(P<0.05).The proportion of patients with a history of antibiotic use was lower in the pneumonia group(P<0.05).Kaplan-Meier survival analysis showed that patients from rural areas,with BMI≥24 kg/m2,smoking history,no prophylactic use of antibiotics,fever duration≥7 d,and hepatomegaly had significantly prolonged hospital stays(P<0.05).Multivariate logistic regression analysis revealed that living in a rural area(OR=4.089,P<0.05),hepatomegaly(OR=4.082,P<0.05),and elevated WBC(OR=1.205,P<0.05)were independent risk factors for pneumonia complicating IM in adults,while the prophylactic use of antibiotics(OR=0.142,P<0.05)was an independent protective factor.The area under the ROC curve of the constructed nomogram prediction model was 0.827(95%CI 0.762-0.892),and the slope of the calibration curve was close to 1,and the Hosmer-Lemeshow test showed χ2=5.299,P=0.725,indicating good consistency and fit of the prediction model.The results of the confusion matrix assessment showed that the sensitivity of the model was 0.669(0.624-0.773),the specificity was 0.827(0.724-0.930),and the accuracy was 0.732(0.665-0.793).Conclusion The nomogram prediction model based on place of onset,hepatomegaly,the prophylactic use of antibiotics and WBC has excellent fit and discrimination,providing an effective quantitative tool for prognosis assessment of IM.
6.Clinical efficacy of modified superior gluteal artery perforator flap with V-Y advancement for the reconstruction of sacrococcygeal pilonidal sinus
Hai LI ; Xiangkui WU ; Chengliang DENG ; Shun’e XIAO ; Zairong WEI
Chinese Journal of Plastic Surgery 2025;41(11):1175-1182
Objective:To investigate the clinical efficacy of the modified superior gluteal artery perforator (SGAP) flap V-Y advancement technique in the repair of sacrococcygeal pilonidal sinus.Methods:A retrospective analysis was conducted on the clinical data of patients who underwent modified SGAP flap V-Y advancement for the reconstruction of sacrococcygeal pilonidal sinus wounds at the Department of Burns and Plastic Surgery, Affiliated Hospital of Zunyi Medical University, between January 2019 and January 2025. The surgical procedure involved two stages. During the first stage, the sinus tract was preoperatively marked with methylene blue, followed by complete excision of the sinus and surrounding involved tissues. The resultant wound was then treated with vacuum sealing drainage for 3 to 5 days. The second stage consisted of flap repair. A portable Doppler ultrasound was used to identify and mark the superior gluteal artery perforator on one side of the wound. A V-shaped flap was designed transversely, with the base corresponding to the length of the subcutaneous tissue defect on the wound side and the superior and inferior borders extending laterally along the wound margins, ensuring the 1-2 SGAP was included within the flap. Intraoperatively, the wound was re-debrided. The epidermis was removed from the base of the V-shaped flap, and the dermis and subcutaneous tissue were dissected. The dermis and superficial subcutaneous tissue of the contralateral wound edge were also dissected. The flap was then advanced in a V-Y fashion to cover the wound. The de-epithelialized portion of the flap was imbricated and sutured to the contralateral skin edge near the midline. The donor site at the apex of the V-shaped flap was closed directly after subcutaneous tissue tension relief, resulting in a Y-shaped closure. Postoperative flap survival, incision healing, and complications were observed. At the final follow-up, flap appearance, texture, surgical site scarring, and sinus recurrence were assessed, and patient satisfaction with the surgical outcome was investigated.Results:A total of eight patients were included in the study, comprising six males and two females, with ages ranging from 14 to 41 years (mean 22.4 years). Two patients presented with multiple sinus tracts, two with chronic sinus tracts and recurrent inflammation with scar formation, and four with postoperative recurrence. The area of the wound defect after debridement ranged from 4.5 cm×5.0 cm to 6.5 cm×8.0 cm. The flap dimensions ranged from 4.5 cm × 6.0 cm to 6.5 cm × 12.5 cm, with a mean V-shaped flap apex angle of 35° ± 2° (range 20° to 60°). In one patient, slight exudate was observed at the base of the flap, which healed after 12 days of dressing changes and drainage. The remaining flaps survived successfully, and primary closure was achieved in both the donor and recipient sites. The patients were followed for a period of 3 to 64 months, with a mean follow-up duration of 10.7 months. In all patients, the sacrococcygeal flap showed no evidence of bulkiness, exhibiting a color similar to the surrounding skin and a soft texture. Linear scars remained at the surgical site, with no complaints of itching, pain, or other discomfort affecting daily life. No recurrence of pilonidal sinus was observed during the follow-up period. Patients reported satisfaction with the appearance of their buttocks.Conclusion:The modified SGAP flap V-Y advancement technique for the repair of sacrococcygeal pilonidal sinus effectively elevates the gluteal cleft, facilitates off-midline closure, demonstrates reliable result, and provides a high level of patient satisfaction.
7.Mechanistic investigation of Fuzheng Hefu Zhiyang Formula in alleviating psoriasis inflammatory microenvironment via P38/Erk/NF-κB signaling pathway
Yi-jing LIAO ; Yan-jie LIU ; Yue LU ; Bin TANG ; Jun-hong ZHANG ; Jing-jie YU ; Hao DENG ; Ling HAN ; Chuan-jian LU ; Hai-ming CHEN
Chinese Traditional Patent Medicine 2025;47(8):2550-2558
AIM To investigate the effect of Fuzheng Hefu Zhiyang Formula(FZHFZY)on psoriasis-like skin lesions and immune regulation in mice.METHODS In the in vivo experiment,30 BALB/c mice were randomly divided into the blank group,the model group,the dexamethasone group(1.5 g/kg of compound dexamethasone acetate cream),and the low-dose(2.5 g/kg)and high-dose(5 g/kg)FZHFZY groups,with six mice in each group.The experiment groups were treated with respective FZHFZY and dexamethasone,and the other groups were given normal saline for 10 consecutive days,during which psoriatic skin lesions were induced with imiquimod cream for 7 consecutive days.The mice had their area and severity of psoriasis assessed by PASI score;their histological changes of skin lesions.observed with Hematoxylin-eosin(HE)staining;their F4/80 ratio of skin lesions observed with immunohistochemical(IHC)staining;their protein expressions of P38,p-P38,Erk,p-Erk,P65 and p-P65 detected by Western blot;and their mRNA expressions of tumor necrosis factor-α(TNF-α),IL-17,IL-23 and IL-1β detected by RT-qPCR.In the in vitro research,the cultured RAW264.7 cells were divided into the blank group,the LPS group,and the FZHFZY groups(1 200,600,300,150 μg/mL).The cells had their protein expressions of P38,p-P38,Erk,p-Erk,P65 and p-P65 detected with Western blot;and their mRNA expressions of IL-6,TNF-α,IL-23 and IL-8 detected by RT-qPCR.RESULTS The in vivo experiment showed that compared to the model group,the FZHFZY groups demonstrated decreased PASI score(P<0.01);improved epidermal thickening and parakeratosis of skin lesions as revealed by HE staining result and increased expression of F4/80 in IHC staining sections;decreased protein expression ratios of p-P38/P38,p-ERK/Erk and p-P65/P65 in skin(P<0.05,P<0.01);and reduced mRNA expressions of TNF-α,IL-17,IL-23 and IL-1β in the skin(P<0.01).FZHFZY(0~2 400 μg/mL)showed no significant cytotoxicity towards RAW264.7 cells in vitro(P>0.05).Compared to those of the LPS group,the cells exposed to FZHFZ at concentrations of 1 200 and 600 μg/mL demonstrated decreased protein expression ratios of p-P38/P38,p-ERK/Erk,and p-P65/P65(P<0.05,P<0.01);and significantly decreased mRNA expressions of TNF-α,IL-17,IL-23 and IL-1β(P<0.01).CONCLUSION FZHFZY alleviates imiquimod-induced psoriatic lesions in mice and suppresses inflammatory response in LPS-stimulated RAW264.7 cells by inhibiting P38/Erk/NF-κB signaling pathway.
8.Comparative efficacy of robot-assisted balloon tibioplasty and traditional open reduction and internal fixation in the treatment of AO/OTA type 41B2 tibial plateau fracture
Jialang HU ; Jing JIAO ; Yucheng HUANG ; Wen XIONG ; Jinyi WU ; Hai DENG ; Zhihua GENG ; Xuan MA ; Ming CHEN
Chinese Journal of Trauma 2025;41(4):369-376
Objective:To compare the clinical efficacy of robot-assisted balloon tibioplasty and traditional open reduction and internal fixation in the treatment of AO/OTA type 41B2 tibial plateau fracture.Methods:A retrospective cohort study was conducted to analyze the clinical data of 70 patients with AO/OTA type 41B2 tibial plateau fracture who were admitted to Wuhan Fourth Hospital from September 2019 to October 2022, including 35 males and 35 females, aged 24-62 years [(44.9±9.5)years]. Among them, 41 patients underwent traditional open reduction and internal fixation (open reduction group), while 29 patients underwent robot-assisted balloon tibioplasty (balloon group). The following parameters were compared between the two groups: incision length, operative blood loss, number of intraoperative fluoroscopies, operation duration, and length of hospital stay; Rasmussen radiological scores at 3 days, 3 months postoperatively, and at the last follow-up and the fracture healing time; pain visual analogue scale (VAS) scores preoperatively, and at 2 days and 3 months postoperatively; knee joint range of motion at 5 days, 3 months postoperatively, and at the last follow-up; Hospital for Special Surgery (HSS) knee function scores at 3, 6 months postoperatively, and at the last follow-up; incidence rate of complications at 15 days postoperatively.Results:All the patients were followed for 12-24 months [18(17, 20)months]. The incision length, operative blood loss and length of hospital stay in the balloon group were 1.6(1.5, 3.0)cm, 5.0(5.0, 5.0)ml and 11.0(9.0, 14.0)days, less than those in the open reduction group [12.0(11.0, 12.0)cm, 100.0(50.0, 120.0)ml and 15.0(13.0, 20.0)days] ( P<0.01). The number of intraoperative fluoroscopies and operation duration in the open reduction group were 9.0(7.0, 10.0)times and 75.0(60.0, 90.0)minutes, less than those in the balloon group [336.0(335.0, 340.0)times and [90.0(70.0, 105.0)minutes] ( P<0.05). There were no significant differences in the Rasmussen radiological scores between the two groups at 3 days, 3 months postoperatively, or at the last follow-up ( P>0.05). The fracture healing time in the balloon group was 3.0(3.0, 3.0)months, shorter than 3.0(3.0, 3.5)months in the open reduction group ( P<0.05). No significant differences were observed between the two groups in VAS scores before operation or at 3 months postoperatively ( P>0.05). However, the VAS score was 2.0(2.0, 3.0)points at 2 days postoperatively in the balloon group, lower than 5.0(5.0, 6.0)points in the open reduction group ( P<0.01). The knee joint range of motion at 5 days, 3 months postoperatively and at the last follow-up were 90.0(85.0, 90.0)°, 135.0(130.0, 135.0)° and 140.0(135.0, 140.0)° in the balloon group, better than 65.0(60.0, 70.0)°, 125.0(120.0, 130.0)°, 130.0(130.0, 140.0)° in the open reduction group ( P<0.01). Similarly, the HSS knee function scores at 3, 6 months postoperatively and at the last follow-up were 80.0(80.0, 81.0)points, 91.0(90.0, 92.0)points, and 95.0(93.0, 96.0)points in the balloon group, better than 71.0(70.0, 72.0)points, 83.0(81.0, 84.0)points, and 86.0(84.0, 88.0)points in the open reduction group ( P<0.01). The incidence rate of complications in the balloon group was 0, comparable to 12% (5/41) in the open reduction group ( P>0.05). Conclusion:Compared with traditional open reduction and internal fixation surgery, robot-assisted balloon tibioplasty in the treatment of AO/OTA type 41B2 tibial plateau fracture significantly reduces surgical trauma, alleviates postoperative pain, promotes fracture healing, and accelerates functional recovery of the affected limbs.
9.Preparation and intestinal absorption mechanism of herpetrione and Herpetospermum caudigerum polysaccharides based self-assembled nanoparticles.
Xiang DENG ; Yu-Wen ZHU ; Ji-Xing ZHENG ; Rui SONG ; Jian-Tao NING ; Ling-Yu HANG ; Zhi-Hui YANG ; Hai-Long YUAN
China Journal of Chinese Materia Medica 2025;50(2):404-412
In this experiment, self-assembled nanoparticles(SANs) were prepared by the pH-driven method, and Her-HCP SAN was constructed by using herpetrione(Her) and Herpetospermum caudigerum polysaccharides(HCPs). The average particle size and polydispersity index(PDI) were used as evaluation indexes for process optimization, and the quality of the final formulation was evaluated in terms of particle size, PDI, Zeta potential, and microstructure. The proposed Her-HCP SAN showed a spheroid structure and uniform morphology, with an average particle size of(244.58±16.84) nm, a PDI of 0.147 1±0.014 8, and a Zeta potential of(-38.52±2.11) mV. Her-HCP SAN significantly increased the saturation solubility of Her by 2.69 times, with a cumulative release of 90.18% within eight hours. The results of in vivo unidirectional intestinal perfusion reveal that Her active pharmaceutical ingredient(API) is most effectively absorbed in the jejunum, where both K_a and P_(app) are significantly higher compared to the ileum(P<0.001). However, the addition of HCP leads to a significant reduction in the P_(app) of Her in the jejunum(P<0.05). Furthermore, the formation of the Her-HCP SAN results in a notably lower P_(app) in the jejunum compared to Her API alone(P<0.001), while both K_a and P_(app) in the ileum are significantly increased(P<0.001, P<0.05). The absorption of Her-HCP SAN at different concentrations in the ileum shows no significant differences, and the pH has no significant effect on the absorption of Her-HCP SAN in the ileum. The addition of the transporter protein inhibitors(indomethacin and rifampicin) significantly increases the absorption parameters K_a and P_(app) of Her-HCP SAN in the ileum(P<0.05,P<0.01), whereas the addition of verapamil has no significant effect on the intestinal absorption parameters of Her-HCP SAN, suggesting that Her may be a substrate for multidrug resistance-associated protein 2 and breast cancer resistance proteins but not a substrate of P-glycoprotein.
Nanoparticles/metabolism*
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Polysaccharides/pharmacokinetics*
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Intestinal Absorption/drug effects*
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Animals
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Rats
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Particle Size
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Drugs, Chinese Herbal/pharmacokinetics*
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Male
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Rats, Sprague-Dawley
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Drug Carriers/chemistry*
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Drug Compounding
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Cucurbitaceae/chemistry*
10.Color-component correlation and mechanism of component transformation of processed Citri Reticulatae Semen.
Kui-Lin ZHU ; Jin-Lian ZOU ; Xu-Li DENG ; Mao-Xin DENG ; Hai-Ming WANG ; Rui YIN ; Zhang-Xian CHEN ; Yun-Tao ZHANG ; Hong-Ping HE ; Fa-Wu DONG
China Journal of Chinese Materia Medica 2025;50(9):2382-2390
High-performance liquid chromatography(HPLC) was used to determine the content of three major components in Citri Reticulatae Semen(CRS), including limonin, nomilin, and obacunone. The chromaticity of the CRS sample during salt processing and stir-frying was measured using a color difference meter. Next, the relationship between the color and content of the salt-processed CRS sample was investigated through correlation analysis. By integrating the oil bath technique for processing simulation with HPLC, the changes in the relative content of nomilin and its transformation products were analyzed, with its structural transformation pattern during processing identified. Additionally, RAW264.7 cells were induced with lipopolysaccharides(LPSs) to establish an inflammatory model, and the anti-inflammatory activity of nomilin and its transformation product, namely obacunone was evaluated. The results indicated that as processing progressed, E~*ab and L~* values showed a downward trend; a~* values exhibited a slow increase over a certain period, followed by no significant changes, and b~* values remained stable with no significant changes over a certain period and then started to decrease. The limonin content remained barely unchanged; the nomilin content decreased, and the obacunone increased significantly. The changing trends in content and color parameters during salt-processing and stir-frying were basically consistent. The content of nomilin and obacunone was significantly correlated with the colorimetric values(L~*, a~*, b~*, and E~*ab), while limonin content showed no significant correlation with these values. By analyzing HPLC patterns of nomylin at different heating temperatures and time, it was found that under conditions of 200-250 ℃ for heating of 5-60 min, the content of nomilin significantly decreased, while the obacunone content increased pronouncedly. The in vitro anti-inflammatory activity results indicated that compared to the model group, the group with a high concentration of nomilin and the groups with varying concentrations of obacunone showed significantly reduced release of nitric oxide(NO)(P<0.01). When both were at the same concentration, obacunone showed better performance in inhibiting NO release. In this study, the obvious correlation between the color and content of major components during the processing of CRS samples was identified, and the dynamic patterns of quality change in CRS samples during processing were revealed. Additionally, the study revealed and confirmed the transformation of nomilin into obacunone during processing, with the in vitro anti-inflammatory activity of obacunone significantly greater than that of nomilin. These findings provided a scientific basis for CRS processing optimization, tablet quality control, and its clinical application.
Mice
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Animals
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Drugs, Chinese Herbal/pharmacology*
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RAW 264.7 Cells
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Limonins/chemistry*
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Chromatography, High Pressure Liquid
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Citrus/chemistry*
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Color
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Benzoxepins/chemistry*
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Anti-Inflammatory Agents/chemistry*

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