1.Five new triterpenoid saponins from the kernels of Momordica cochinchinensis
Ru DING ; Jia-qi WANG ; Yi-yang LUO ; Yong-long HAN ; Xiao-bo LI ; Meng-yue WANG
Acta Pharmaceutica Sinica 2025;60(2):442-448
Five saponins were isolated from the kernels of
2.Four Weeks of HIIT Modulates Lactate-mediated Synaptic Plasticity to Improve Depressive-like Behavior in CUMS Rats
Yu-Mei HAN ; Zi-Wei ZHANG ; Jia-Ren LIANG ; Chun-Hui BAO ; Jun-Sheng TIAN ; Shi ZHOU ; Huan XIANG ; Yong-Hong YANG
Progress in Biochemistry and Biophysics 2025;52(6):1499-1510
ObjectiveThis study aimed to investigate the effects of 4-week high-intensity interval training (HIIT) on synaptic plasticity in the prefrontal cortex (PFC) of rats exposed to chronic unpredictable mild stress (CUMS), and to explore its potential mechanisms. MethodsA total of 48 male Sprague-Dawley rats were randomly divided into 4 groups: control (C), model (M), control plus HIIT (HC), and model plus HIIT (HM). Rats in groups M and HM underwent 8 weeks of CUMS to establish depression-like behaviors, while groups HC and HM received HIIT intervention beginning from the 5th week for 4 consecutive weeks. The HIIT protocol consisted of repeated intervals of 3 min at high speed (85%-90% maximal training speed, Smax) alternated with one minute at low speed (50%-55% Smax), with 3 to 5 sets per session, conducted 5 d per week. Behavioral assessments and tail-vein blood lactate levels were measured at the end of the 4th and 8th weeks. After the intervention, rat PFC tissues were collected for Golgi staining to analyze synaptic morphology. Enzyme-linked immunosorbent assays (ELISA) were employed to detect brain-derived neurotrophic factor (BDNF), monocarboxylate transporter 1 (MCT1), lactate, and glutamate levels in the PFC, as well as serotonin (5-HT) levels in serum. Additionally, Western blot analysis was conducted to quantify the expression of synaptic plasticity-related proteins, including c-Fos, activity-regulated cytoskeleton-associated protein (Arc), and N-methyl-D-aspartate receptor 1 (NMDAR1). ResultsCompared to the control group (C), the CUMS-exposed rats (group M) exhibited significant reductions in sucrose preference rates, number of grid crossings, frequency of upright postures, and entries into and duration spent in open arms of the elevated plus maze, indicating marked depressive-like behaviors. Additionally, the group M showed significantly reduced dendritic spine density in the PFC, along with elevated levels of c-Fos, Arc, NMDAR1 protein expression, and increased concentrations of lactate and glutamate. Conversely, BDNF and MCT1 contents in the PFC and 5-HT levels in serum were significantly decreased. Following HIIT intervention, rats in the group HM displayed considerable improvement in behavioral indicators compared with the group M, accompanied by significant elevations in PFC MCT1 and lactate concentrations. Furthermore, HIIT notably normalized the expression levels of c-Fos, Arc, NMDAR1, as well as glutamate and BDNF contents in the PFC. Synaptic spine density also exhibited significant recovery. ConclusionFour weeks of HIIT intervention may alleviate depressive-like behaviors in CUMS rats by increasing lactate levels and reducing glutamate concentration in the PFC, thereby downregulating the overexpression of NMDAR, attenuating excitotoxicity, and enhancing synaptic plasticity.
3.Study on Kinetic and Static Tasks With Different Resistance Coefficients in Post-stroke Rehabilitation Training Based on Functional Near-infrared Spectroscopy
Ling-Di FU ; Jia-Xuan DOU ; Ting-Ting YING ; Li-Yong YIN ; Min TANG ; Zhen-Hu LIANG
Progress in Biochemistry and Biophysics 2025;52(7):1890-1903
ObjectiveFunctional near-infrared spectroscopy (fNIRS), a novel non-invasive technique for monitoring cerebral activity, can be integrated with upper limb rehabilitation robots to facilitate the real-time assessment of neurological rehabilitation outcomes. The rehabilitation robot is designed with 3 training modes: passive, active, and resistance. Among these, the resistance mode has been demonstrated to yield superior rehabilitative outcomes for patients with a certain level of muscle strength. The control modes in the resistance mode can be categorized into dynamic and static control. However, the effects of different control modes in the resistance mode on the motor function of patients with upper limb hemiplegia in stroke remain unclear. Furthermore, the effects of force, an important parameter of different control modes, on the activation of brain regions have rarely been reported. This study investigates the effects of dynamic and static resistance modes under varying resistance levels on cerebral functional alterations during motor rehabilitation in post-stroke patients. MethodsA cohort of 20 stroke patients with upper limb dysfunction was enrolled in the study, completing preparatory adaptive training followed by 3 intensity-level tasks across 2 motor paradigms. The bilateral prefrontal cortices (PFC), bilateral primary motor cortices (M1), bilateral primary somatosensory cortices (S1), and bilateral premotor and supplementary motor cortices (PM) were examined in both the resting and motor training states. The lateralization index (LI), phase locking value (PLV), network metrics were employed to examine cortical activation patterns and topological properties of brain connectivity. ResultsThe data indicated that both dynamic and static modes resulted in significantly greater activation of the contralateral M1 area and the ipsilateral PM area when compared to the resting state. The static patterns demonstrated a more pronounced activation in the contralateral M1 in comparison to the dynamic patterns. The results of brain network analysis revealed significant differences between the dynamic and resting states in the contralateral PFC area and contralateral M1 area (F=4.709, P=0.038), as well as in the contralateral PM area and ipsilateral M1 area (F=4.218, P=0.049). Moreover, the findings indicated a positive correlation between the activation of the M1 region and the increase in force in the dynamic mode, which was reversed in the static mode. ConclusionBoth dynamic and static resistance training modes have been demonstrated to activate the corresponding brain functional regions. Dynamic resistance modes elicit greater oxygen changes and connectivity to the region of interest (ROI) than static resistance modes. Furthermore, the effects of increasing force differ between the two modes. In patients who have suffered a stroke, dynamic modes may have a more pronounced effect on the activation of exercise-related functional brain regions.
4.Analysis of Animal Models of Autoimmune Thyroiditis Based on Clinical Characteristics of Traditional Chinese and Western Medicine
Sifeng JIA ; Zhuo ZHANG ; Yuyu DUAN ; Keqiu YAN ; Xinhe ZUO ; Yang LI ; Yong ZHAO
Chinese Journal of Experimental Traditional Medical Formulae 2025;31(18):235-243
ObjectiveAutoimmune thyroiditis (AIT) is a complex and immune-mediated disorder, with no established treatment protocol. Both Western and traditional Chinese medicine (TCM) focus on the pathogenesis and treatment of AIT. This study evaluated the clinical consistency of existing AIT animal models based on the diagnostic criteria of both Western and TCM, using a novel evaluation method. Additionally, it proposed recommendations and future prospects for improving these models. MethodsA comprehensive literature review was conducted on existing AIT animal models, using databases and the diagnostic criteria of both Western and TCM. Core and accompanying symptoms of these models were scored based on the diagnostic criteria of both Western and TCM, and clinical consistency was assessed. ResultsMice are the primary experimental animals used in AIT modeling. Modeling methods include vaccine immunization, iodine induction, heterologous thyroid antigen immunization, and a combination of high iodine water and antigen immunization. The average consistency of clinical syndromes based on TCM and Western medicine is 40%, 60%, 54%, and 63%, with the highest consistency observed in the combined high iodine water and antigen immunization model. Pathological models based on TCM are less common, with the liver-stagnation-spleen-deficiency rat model showing high clinical consistency. While most models are designed according to Western medical theory, meeting the surface and structural effectiveness criteria of Western medicine. However, there is a lack of fine-tuning and clear differentiation of TCM syndromes. ConclusionCurrent AIT syndrome-disease combination animal models primarily reflect the pathological features of Western medicine, with limited integration of TCM syndromes. Future research should aim to combine the syndrome characteristics of TCM with the pathological features of Western medicine, creating multi-factor and dynamic syndrome-disease models. Such models would better facilitate an experimental platform that conforms to the theories of TCM, providing more comprehensive support and guidance for the pathogenesis and treatment strategies of AIT.
5.Efficacy comparison of foldable capsular body with scleral buckling in treating experimental retinal detachment
Yifan DONG ; Baike ZHANG ; Yong JIA ; Fan YANG ; Lisha GUO ; Xiangyang ZHANG ; Cong LU ; Zhonghao ZHANG ; Haiyan WU ; Xuemin TIAN
International Eye Science 2025;25(10):1566-1573
AIM: To compare the effectiveness of foldable capsular body(FCB)with traditional scleral buckling(SB)in the treatment of experimental retinal detachment animal models.METHODS: After successfully establishing rhegmatogenous retinal detachment(RRD)animal models, 24 New Zealand white rabbits were randomly divided into three groups(RRD models group, SB group, and FCB group), with 8 rabbits in each group. The FCB and SB groups underwent SB and FCB surgeries for the RRD animal models, while the RRD models group only consists of RRD models without any surgical intervention during the follow-up period. The follow-up duration was 3 mo. Wide-field neonatal fundus imaging system and ophthalmic B-ultrasound were used to assess the fundus conditions before and after surgery. The Icare® TONOVET Plus tonometer was utilized to evaluate intraocular pressure changes before and after surgery. The Eaton and Draize scoring systems were selected to monitor postoperative inflammatory reactions.RESULTS: The retinal reattachment rates in the FCB and SB groups were 87.5% and 75.0%, respectively, with no statistically significant difference between the groups(P>0.05). The intraocular pressure in both the FCB and SB groups increased postoperatively compared to preoperative levels(P<0.01), and there were no significant differences in intraocular pressure at any time points during the follow-up period between the groups(P>0.05). The intraocular pressure in the RRD models group remained at a low level throughout the follow-up period. The average surgical time for the FCB group was 16.87±2.29 min, which was shorter than 46.25±4.74 min in the SB group(t=-15.166, P<0.001). According to the Eaton and Draize scoring systems, the FCB group had lower grades of conjunctival hyperemia and edema in the early postoperative period compared to the SB group, indicating milder inflammatory reactions(P<0.05).CONCLUSION: Both FCB and SB are effective in treating experimental RRD. Compared to SB, FCB is simpler to operate, and also has a shorter surgical time and milder postoperative inflammatory reactions.
6.Recent advances in small-molecule inhibitors targeting influenza virus RNA-dependent RNA polymerase
Hui-nan JIA ; Rui-fang JIA ; Ji-wei ZHANG ; Yuan-min JIANG ; Chuan-feng LIU ; Ying ZHANG ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2024;59(1):43-60
Influenza virus causes serious threat to human life and health. Due to the inherent high variability of influenza virus, clinically resistant mutant strains of currently approved anti-influenza virus drugs have emerged. Therefore, it is urgent to develop antiviral drugs with new targets or mechanisms of action. RNA-dependent RNA polymerase is directly responsible for viral RNA transcription and replication, and plays key roles in the viral life cycle, which is considered an important target of anti-influenza drug design. From the point of view of medicinal chemistry, this review summarizes current advances in diverse small-molecule inhibitors targeting influenza virus RNA-dependent RNA polymerase, hoping to provide valuable reference for development of novel antiviral drugs.
7.Research hotspots and trends of tigecycline drug resistance: A study based on CiteSpace
Xinjing JIA ; Yanding WANG ; Chunyuan DUAN ; Lisha LIU ; Di WU ; Xinran GONG ; Zhiqiang LI ; Meitao YANG ; Dayang ZOU ; Yong WANG
Journal of Public Health and Preventive Medicine 2024;35(1):16-19
Objective To explore the research progress, research hotspot and development trend of tigecycline resistance based on the quantitative analysis and visualization function of CiteSpace. Methods The data were collected from 4,263 Chinese and English articles on tigecycline resistance in CNKI, Wanfang, VIP and Web of Science (WOS) databases from 2012 to 2022. CiteSpace 5.8.R3 software was used to analyze the cooperative network of authors, the cooperative network of countries and institutions, the total citation times of journals, and keywords included in the literature, to reveal the hotspots and trends of tigecycline resistance research. Results The number of articles published in English literature was higher than that in Chinese literature. China had the largest number of published documents, showing a significant international academic influence in this research field. Countries all over the world were concerned about the resistance of tigecycline, but Chinese literatures focused more on the clinical infection and prevention of tigecycline resistance, while English literatures placed special emphasis on the research about the drug resistance mechanism of tigecycline. Conclusion The research direction at home and abroad is basically the same, but the research focus has gradually shifted from the clinical treatment and monitoring of tigecycline to the molecular level of drug resistance mechanism.
8.Inhibitory effects of hesperidin on estrogen-and progestin-induced mammary hyperplasia in female rats
Yang YANG ; Xiao-Fen YANG ; Pei-Sen HUANG ; Jie LENG ; Fan YANG ; Yong-Jia LI
The Chinese Journal of Clinical Pharmacology 2024;40(1):77-81
Objective To investigate the therapeutic effect of hesperidin(Hsp)on mammary gland hyperplasia(MGH)rats and the possible mechanism.Methods Sixty female rats were randomly divided into blank,model,control and experimental-L,-M,-H groups.Except for blank group,all other groups were injected intramuscularly with estrogen and progestin to induce MGH model in rats.The experimental-L,-M and-H groups were given 25,50,100 mg·kg-1 Hsp by gavage.The control group was given 5 mg·kg-1 tamoxifen by gavage.The blank and control groups were given an equal volume of 0.9%NaCl by gavage.Six groups of rats were administered once a day for 30 days.After the administration,the height and diameter of nipples and the uterine coefficient were measured.The serum sex hormone content was detected using enzyme-linked immunosorbent assay,the levels of oxidative stress indicators were detected using corresponding kits,and the expressions of related proteins were detected using Western blot.Results The nipple diameters of rats in experimental-M and-H groups,control group,model group and blank group were(1.41±0.20),(1.18±0.21),(1.23±0.20),(1.75±0.13)and(1.02±0.06)mm;the nipple heights were(1.62±0.24),(1.41±0.19),(1.47±0.16),(1.87±0.32)and(1.23±0.14)mm;the uterine indexes were(0.55±0.08),(0.37±0.05),(0.41±0.04),(0.72±0.11)and(0.34±0.03)mg·g-1;the relative expression levels of estrogen receptor alpha(ERα)were 0.54±0.05,0.13±0.02,0.13±0.03,0.89±0.08 and 0.10±0.02;the relative expression levels of progesterone receptor(PR)were 0.43±0.03,0.08±0.01,0.87±0.07,0.20±0.04 and 0.14±0.03;the phosphorylated-extracellular-regulated kinase 1/2(ERK1/2)/ERK1/2 were 0.50±0.03,0.06±0.02,0.83±0.05,0.09±0.04 and 0.04±0.01,respectively.Compared with model group,the differences of above indexes in the experimental-M,-H groups and control group were statistically significant(all P<0.05).Conclusion Hsp could reduce nipple diameter,height,and uterine coefficient,regulate sex hormone levels,resist oxidative stress,and inhibit the expression of ERα,PR and p-ERK1/2 proteins in rats.
9.Clinical trial of intraoperative intraperitoneal perfusion of raltitrexed in patients with colorectal cancer
The Chinese Journal of Clinical Pharmacology 2024;40(6):811-814
Objective To explore the application effect of intraoperative intraperitoneal perfusion of raltitrexed in patients with colorectal cancer.Methods The clinical data of patients with colorectal cancer were retrospectively analyzed.According to different treatment using cohort methods,patients were divided into control group and treatment group.Both groups underwent five-hole laparoscopic radical resection of colorectal cancer.The control group was given intraperitoneal irrigation of warm 0.9%NaCl 2 000 mL before abdominal closure.On the basis of control group,treatment group was given intraperitoneal perfusion of 0.9%NaCl 500 mL+raltitrexed 4 mg.The tumor indexes and liver-kidney function before and after surgery,postoperative recovery,complications and survival at 1 year after surgery were compared between the two groups.Results There were 40 cases in control group and 40 cases in treatment group.During postoperative chemotherapy,levels of carcinoembryonic antigen(CEA)in treatment group and control group were(9.50±2.17)and(11.47±2.06)μg·L-1,and levels of carbohydrate antigen 199(CA199)were(127.25±9.31)and(182.64±10.39)U·L-1,and the differences were statistically significant(P<0.05).Before and at 1 d after surgery,glutamic-pyruvic transaminase(GPT)levels in treatment group were(17.12±4.57)and(21.33±5.42)U·L-1,and glutamic-oxaloacetic transaminase(GOT)levels were(17.03±3.54)and(19.15±4.28)U·L-1,and the differences were statistically significant(P<0.05).There was no significant difference in postoperative recovery time of intestinal function,hospitalization time or incidence of complications between the two groups(P>0.05).At 1 year after surgery,disease-free survival in treatment group and control group were(7.49±0.98)months and(7.01±0.95)months,and the differences was statistically significant(P<0.05).There was no significant difference in overall survival between the two groups(P>0.05).Conclusion Intraoperative intraperitoneal perfusion of raltitrexed can effectively reduce levels of tumor markers and delay disease progression in patients with colorectal cancer.However,it will cause the reversible increase of GPT and GOT.
10.Clinical trial of aspirin and low molecular weight heparin for prevention of venous thromboembolism in patients with hand and foot trauma fractures after operation
Li SUN ; Rong LIU ; Yong LI ; Jia-Gang WANG
The Chinese Journal of Clinical Pharmacology 2024;40(12):1718-1722
Objective To observe the postoperative effects of aspirin and low-molecular-weight heparin(LMWH)in preventing venous thromboembolism(VTE)and improving distal circulation in patients with hand and foot trauma fractures.Methods Retrospectivey selected patients undergoing hand and foot trauma fracture surgery into control and treatment groups.The control group received enteric-coated aspirin,0.1 g per dose,once daily;the treatment group received subcutaneous injection of calcium-enoxaparin,4 000 U per dose,twice daily,for continuous treatment for 12 days.The incidence of VTE,coagulation function,hemorheological parameters,distal collateral circulation,and drug adverse reactions were compared between the two groups.Results There were 60 patients in each of the treatment and control groups.The incidence of postoperative deep vein thrombosis was 5.00%in the treatment group and 3.33%in the control group,while the incidence of pulmonary embolism was 1.67%in both groups,with no statistically significant differences(all P>0.05).After treatment,the activated partial thromboplastin time(APTT)in the treatment and control groups were(35.01±5.96)and(36.82±6.15)s,prothrombin time(PT)were(14.95±1.54)and(15.32±1.63)s;fibrinogen(FIB)were(3.97±1.25)and(4.36±1.02)g·L-1;D-dimer(D-D)were(309.69±56.55)and(319.03±55.32)μg·L-1;whole blood viscosity(WBV)were(13.26±3.80)and(12.26±3.61)mPa·s-1;plasma viscosity(PV)were(1.76±0.35)and(1.77±0.43)mPa·s-1,hematocrit(HCT)were(60.20±7.05)%and(58.60±6.71)%,with no statistically significant differences(all P>0.05).After treatment,the flow rates(Vmax)in the treatment and control groups were(54.27±6.64)and(51.18±5.67)cm·s-1;resistance indices(RI)were 0.59±0.13 and 0.65±0.15,showing statistical significance(all P<0.05).Comparison of drug adverse reactions such as nausea,vomiting,bleeding,and injection site hematoma between the treatment and control groups showed no statistically significant difference in the overall incidence of adverse drug reactions(P>0.05).Conclusion There was no significant difference in the efficacy of aspirin and LMWH in preventing postoperative VTE in patients with hand and foot trauma fractures,but LMWH demonstrated better improvement in distal collateral circulation.


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