1.Research progress in small molecule inhibitors of complement factor B
Shuai WEN ; Yao ZHAO ; Yan WANG ; Xing LI ; Yi MOU ; Zheng-yu JIANG
Acta Pharmaceutica Sinica 2025;60(1):37-47
The alternative pathway (AP) of the complement system is a key contributor to the pathogenesis of several diseases including paroxysmal nocturnal hemoglobinuria (PNH), atypical hemolytic uremic syndrome (aHUS), C3 glomerular disease (C3G) and age-related macular degeneration (AMD). Complement factor B (CFB) is a trypsin-like serine protein that circulates in the human bloodstream in a latent form. As a key node of the alternative pathway, it is an important target for the treatment of diseases mediated by the complement system. With the successful launch of iptacopan, the CFB small molecule inhibitors has become a current research hotspot, a number of domestic and foreign pharmaceutical companies are actively developing CFB small molecule inhibitors. In this paper, the research progress of CFB small molecule inhibitors in recent years is systematically summarized, the representative compounds and their activities are introduced according to structural types and design ideas, so as to provide reference and ideas for the subsequent research on CFB small molecule inhibitors.
2.Effects of shared decision-making oriented vocational training on the social function of patients with schizophrenia
Chunyan JIANG ; Jiuhong SHUAI ; Hongyuan DENG ; Junhua ZHENG ; Chunfeng GOU ; Xiaoli YANG ; Deying TONG ; Hao FENG ; Xia HUANG ; Ru GAO
Sichuan Mental Health 2025;38(3):229-234
BackgroundAs a high prevalence disorder, schizophrenia has caused significant burden to family and society due to the impairment of occupational and social function. Currently, the dominant vocational training model in China follows a paternalistic, clinician-led decision-making approach. Although it improves patients' social function to some extent, it undermines their autonomy and treatment adherence. Therefore, it is urgently necessary to explore a new intervention method to enhance treatment compliance and social function in patients. ObjectiveTo explore the impact of shared decision-making oriented vocational training on social function in hospitalized schizophrenia patients, so as to provide references for rehabilitation interventions. MethodsA total of 68 patients diagnosed with schizophrenia according to the International Classification of Diseases, tenth edition (ICD-10) criteria were consecutively enrolled from January to June 2024 at The Third People's Hospital of Wenjiang Distric, Chengdu. Participants were randomly allocated into the research group (n=34) and the control group (n=34) using a random number table method. Both groups received routine rehabilitation training, while the research group received shared decision-making oriented vocational training for 12 weeks, 2 times a week for 2 hours each time. Before and at the 4th and 12th week of intervention, two groups were evaluated by General Self-Efficacy Scale (GSES), Stigma Scale for Mental Illness (SSMI), Scale of Social function of Psychosis Inpatients (SSFPI) and Inpatient Psychiatric Rehabilitation Outcome Scale (IPROS). ResultsA total of 63 participants completed the study, with 30 cases in the research group and 33 cases in the control group. Repeated measures ANOVA revealed statistically significant time effects and interaction effects in both groups for GSES, SSMI, SSFPI and IPROS scores (F=20.451, 16.022; 26.193, 12.944; 23.957, 5.023; 11.776, 3.985, P<0.05 or 0.01), while no significant group effects were observed (F=0.188, 0.742, 1.878, 0.474, P>0.05). At the 12th week of intervention, there were statistically significant differences in GSES, SSMI, SSFPI and IPROS scores between the two groups. ConclusionShared decision-making oriented vocational training may help to improve social function in patients with schizophrenia. [Funded by 2023 Chengdu Medical Research Project (number, 2023468)]
3.Quality evaluation of Euscaphis japonica from different habitats using chemometrics combined with weighted TOPSIS model
Yuqiu GAO ; Shuai ZHENG ; Xue YU ; Guihua ZOU ; Kai ZHANG
China Pharmacy 2025;36(14):1755-1759
OBJECTIVE To evaluate the quality of Euscaphis japonica from different habitats. METHODS The relative correction factors of gallic acid, protocatechuic acid, ellagic acid, isoquercitrin, astragalin and apigenin were calculated with quercetin as the internal reference; the relative correction factors of euscaphic acid, oleanolic acid, stigmasterol and β-sitosterol were also calculated with ursolic acid as the internal reference. The contents of 12 components in 18 batches of samples were calculated by QAMS method and were compared with external standard method. At the same time, the contents of water-soluble extract, alcohol-soluble extract, total ash and acid-insoluble ash were detected. The quality of E. japonica was evaluated by principal component analysis (PCA), orthogonal partial least squares-discriminant analysis (OPLS-DA), and weighted technique for order preference by similarity to ideal solution (TOPSIS) method. RESULTS There was no significant difference between the results of QAMS method and external standard method for the 12 components in the 18 batches of samples. However, notable content variations were observed among different batches of samples. The results of PCA and OPLS-DA showed that S1-S7, S8- S12, and S13-S18 were clustered into one category respectively. Seven key characteristic components variable importance in projection values >1, euscaphic acid, ursolic acid, protocatechuic acid, apigenin, β-sitosterol, isoquercitrin, and oleanolic acid, respectively. The analysis results of the weighted TOPSIS method revealed that the relative closeness for evaluating the quality of 18 batches of samples ranged from 0.283 5 to 0.644 1, with the samples of E. japonica from Fengjie, Chongqing, demonstrating the highest quality. CONCLUSIONS The established method is accurate and feasible, which can be used for the quality evaluation of E. japonica combined with chemometrics and weighted TOPSIS model.
4.Effect of biological amniotic membrane soaked in pirfenidone on scar formation after glaucoma filtration surgery in rabbit eyes
Shuai ZHANG ; Yihua YAO ; Yangjing ZHENG ; Ping WU ; Yihua ZHU
International Eye Science 2024;24(2):189-195
AIM: To investigate the application of biological amniotic membrane soaked in pirfenidone(PFD)and to evaluate its anti-scarring effect and toxic side effects on glaucoma model of rabbit eyes.METHODS: The right eyes of 72 healthy New Zealand white rabbits were randomly divided into 0.5%PFD+ biological amniotic membrane group, biological amniotic membrane group, mitomycin C(MMC)group and blank control group after the glaucoma model was established by anterior chamber injection of compound carbomer solution, and 18 rabbits in each group underwent trabeculectomy, in which the 0.5% PFD+ biological amniotic membrane group was placed with 0.5% PFD solution-soaked biological amniotic membrane under the scleral flap, and the biological amniotic membrane group was placed with normal saline-soaked rehydrated biological amniotic membrane under the scleral flap. In the MMC group, a cotton pad soaked in MMC was placed under the scleral flap for 3 min and immediately rinsed with normal saline, while the blank control group received no implant after the scleral flap was made. The intraocular pressure(IOP), filtration blebs, toxic side effects and complications were evaluated, and the histopathological changes in the filtration area were observed by hematoxylin-eosin(HE), Masson staining and immunohistochemical staining.RESULTS: The mean IOP at 14, 21 and 28 d after trabeculectomy were 0.5%PFD+ biological amniotic membrane group<MMC group<biological amniotic membrane group<blank control group(all P<0.05). At 28 d after trabeculectomy, 0.5%PFD+ biological amniotic membrane group had the best effect of anti-inflammatory hyperplasia and inhibition of collagen formation, the highest survival rate of filtration blebs, and the inflammatory reaction was mild.CONCLUSION: Biological amniotic membrane soaked in pirfenidone has more obvious anti-scarring effect on glaucoma model, with less toxic side effects and good safety.
5.PDCA cycle helps the continuous improvement of laboratory diagnostics teaching
Shuai YUAN ; Wanying LIN ; Qian ZHOU ; Xin LI ; Bo LI ; Lei ZHENG
Chinese Journal of Medical Education Research 2024;23(3):387-390
In the context of "New Era" and "New Medicine", the teaching team of laboratory diagnostics proposed a new teaching method of PDCA (Plan, Do, Check, Action) cycle to innovate the instructional design and implementation of laboratory diagnosis on the base of traditional teaching model. Through optimizing the curriculum system, integrating superior resources, taking full advantage of information technology, mobilizing the virtual simulation laboratory, implementing moral education and multiple comprehensive evaluation results, the self-learning enthusiasm, innovation and development ability of students were improved significantly, accompanied with high humanistic care spirit. Moreover, the enthusiasm of participating in scientific research activities and professional competitions was enhanced obviously. Therefore, we believe that the PDCA cycle, with notable successes, deserves high promotion value and wide application.
6.Virtual reality technology in ocular trauma teaching for medical students
Chao ZHENG ; Jiyuan MA ; Guoheng ZHANG ; Fei FEI ; Jiaxing SUN ; Shuai ZHANG ; Jian ZHOU ; Guorui DOU
International Eye Science 2024;24(10):1645-1649
AIM:To investigate the application of virtual reality(VR)technology in ocular trauma teaching for medical students.METHODS: A total of 90 medical students who participated in the Ophthalmology teaching program between November 2022 and April 2024 were recruited as subjects. Using a case-control method, 45 students in the case group attended traditional ocular trauma teaching program combined with VR virtual simulation experiments, and 45 students in the control group solely attended traditional ocular trauma teaching program. After the teaching practice, the two groups were compared in terms of their examination performance of theoretical knowledge and case analysis, learning ability(evaluated by the Self-Directed Learning Rating Scale), and the satisfaction survey on the quality of teaching; the statistical analyses were performed using t-test or Chi-square test.RESULTS: The scores of theoretical knowledge and case analysis examinations of the case group were significantly higher than those of the control group, and the differences were statistically significant(scores of theoretical knowledge examination: 57.27±2.78 vs 53.91±3.20; scores of case analysis examination: 35.71±3.73 vs 32.67±5.52, both P<0.05). The scores of the Self-Directed Learning Rating Scale of the case group were significantly higher than those of the control group(P<0.05), and the satisfaction with teaching quality of the case group was significantly higher than that of the control group(P<0.05).CONCLUSION: VR-enabled teaching of ocular trauma can effectively improve medical students' mastery of theoretical knowledge and practical skills, enhance students' self-directed learning ability and improve teaching satisfaction.
7.Structure-activity Omics on Anti-inflammatory and Analgesic Effect of Cyperi Rhizoma in Qizhi Weitong Granules
Ying ZHENG ; Sicong LIU ; Xi LUO ; Bing QI ; Shuai WANG ; Yongrui BAO ; Tianjiao LI ; Liang WANG ; Dong YAO ; Xiansheng MENG
Chinese Journal of Experimental Traditional Medical Formulae 2024;30(21):153-160
ObjectiveTo elucidate the pharmacodynamic substances responsible for the anti-inflammatory and analgesic effects of Cyperi Rhizoma by structure-activity omics. MethodOn the basis of the previous in vitro efficacy study by our research group, this study explored the in vivo efficacy of the flavonoids in Cyperi Rhizoma. The flavonoids in Cyperi Rhizoma and their targets were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), PharmMapper, Swiss TargetPrediction, and available articles. The targets of the anti-inflammatory and analgesic effects were collected from DisGeNET and Online Mendelian Inheritance in Man (OMIM). The common targets shared by flavonoids and the effects were selected as the direct targets of flavonoids endowing Cyperi Rhizoma with anti-inflammatory and analgesic effects, and protein-protein interaction (PPI) network of the core targets was constructed. The method of structure-activity omics was employed to correlate the structure and efficacy of one or more classes of chemical components in Cyperi Rhizoma with the targets as a bridge. The components were classified according to structure. Molecular docking of components to core targets was carried out via SYBYL-X 2.1.1, PyMol, and Discovery Studio 4.5 visualizer. Two targets with the highest binding affinity were selected to explore the relationship between compound structures and targets. ResultThe flavonoids in Cyperi Rhizoma exerted anti-inflammatory and analgesic effects on the mouse model of pain induced by formaldehyde. Eighteen components and 115 direct targets were screened out, and the core targets with high activities were protein kinase B1 (Akt1), interleukin-1β (IL-1β), cellular tumor antigen p53 (TP53), prostaglandin-endoperoxide synthase 2 (PTGS2), and matrix metalloproteinase-9 (MMP-9). According to the structures, the flavonoids in Cyperi Rhizoma were classified into bioflavonoids, flavonols, flavones, and flavanes. The molecular docking results showed that flavonoids of Cyperi Rhizoma had the highest binding affinity to TP53 and PTGS2. The results of structure-activity omics showed that bioflavonoids represented the best binding structure to the targets, while their polyhydroxyl etherification resulted in a significant decrease in the binding affinity to PTGS2. Glycosides had higher binding affinity to PTGS2. The introduction of the long-chain hydrocarbon group to the A ring of flavonols facilitated the binding to TP53, while the change of B ring substituents was not the main factor affecting the binding affinity. The 3,4-dihydroxyl flavane outperformed 3-hydroxyl flavane in the binding to TP53, while the two compounds showed similar binding affinity to PTGS2. ConclusionThe method of structure-activity omics was used to analyze the material basis for the anti-inflammatory and analgesic effects of flavonoids in Cyperi Rhizoma. Structure-activity omics provides new ideas for revealing the pharmacodynamic substances of traditional Chinese medicine.
8.Structure-activity Omics on Anti-inflammatory and Analgesic Effect of Glycyrrhizae Radix et Rhizoma in Qizhiweitong Granules
Ying MENG ; Ying ZHENG ; Xinpeng QIN ; Sicong LIU ; Tianjiao LI ; Yongrui BAO ; Shuai WANG ; Liang WANG ; Honghong JIANG ; Xiansheng MENG
Chinese Journal of Experimental Traditional Medical Formulae 2024;30(21):161-168
ObjectiveTo reveal the pharmacodynamic substances for the anti-inflammatory and analgesic effects of Glycyrrhizae Radix et Rhizoma by structure-activity omics. MethodOn the basis of the previous study about the screening of active components in vitro, this study explored the effects of flavonoids in Glycyrrhizae Radix et Rhizoma in vivo. The flavonoids in Glycyrrhizae Radix et Rhizoma and their direct targets for the anti-inflammatory and analgesic effects were obtained from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), PharmMapper, Swiss TargetPrediction, DisGeNET, and Online Mendelian Inheritance in Man (OMIM). STRING and Cytoscape 3.7.2 were employed to establish the protein-protein interaction (PPI) network of key targets. Molecular docking was performed to simulate the binding of five targets with high degrees to flavonoids in Glycyrrhizae Radix et Rhizoma, on the basis of which the key core targets were selected. The targets were used as a bridge to correlate the structures and effects of one or more classes of chemical components in Glycyrrhizae Radix et Rhizoma. According to the binding affinity between flavonoids with different structures in Glycyrrhizae Radix et Rhizoma and targets, the relationships between compound structures and core targets were discussed. ResultThe flavonoids in Glycyrrhizae Radix et Rhizoma reduced the content of prostaglandin E2 (PGE2) in the rat model of pain induced by formalin, demonstrating definite anti-inflammatory and analgesic effects. Sixty active compounds (flavonoids) with anti-inflammatory and analgesic effects of Glycyrrhizae Radix et Rhizoma were obtained. With the total score as the standard, prostaglandin-endoperoxide synthase 2 (PTGS2) and mitogen-activated protein kinase 3 (MAPK3) were selected as the key core targets of Glycyrrhizae Radix et Rhizoma for the anti-inflammatory and analgesic effects. Except that flavones showed selectivity of binding to MAPK3, the other flavonoids of Glycyrrhizae Radix et Rhizoma showed strong binding to PTGS2 and MAPK3, and the structures containing glycoside fragments showed stronger binding affinity to the targets. The introduction of chain olefins in the ring of chalcones facilitated the binding to the targets. The isopentenyl fragment in flavonols may cause the difference in binding affinity. The parallel combination of a ring into pyran ring in flavanes was not conducive to the binding to the target. The electric charge, liposolubility, and steric hindrance of the substituent group on the B ring of isoflavones directly affected the binding affinity. ConclusionThis study adopts structure-activity omics to analyze the material basis for the anti-inflammatory and analgesic effects of Glycyrrhizae Radix et Rhizoma. Structure-activity omics provides new ideas and methods for predicting the pharmacodynamic substances of traditional Chinese medicine.
9.Structure-activity Omics on Anti-inflammatory and Analgesic Effect of Paeoniae Radix Alba in Qizhi Weitong Granules
Bing QI ; Xi LUO ; Ying ZHENG ; Ying MENG ; Shuai WANG ; Yongrui BAO ; Tianjiao LI ; Ling HAN ; Xinying SHU ; Xiansheng MENG
Chinese Journal of Experimental Traditional Medical Formulae 2024;30(21):169-175
ObjectiveTo elucidate the active compounds for the anti-inflammatory and analgesic effects of Paeoniae Radix Alba from structure-activity omics. MethodOn the basis of the previous in vitro efficacy study by our research group, a mouse model of foot swelling was induced by methyl aldehyde and used to study the anti-inflammatory and analgesic effects of total glycosides of Paeoniae Radix Alba in vivo. The core targets of the active compounds for the anti-inflammatory and analgesic effects of Paeoniae Radix Alba were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), Online Mendelian Inheritance in Man (OMIM), and Search Tool for Recurring Instances of Neighbouring Genes (STRING). Molecular docking was conducted for the total glucosides of Paeoniae Radix Alba with the core targets, and the key core targets with high binding affinity were screened out according to the comprehensive score of each target and active structure. The structure-activity relationship was analyzed with targets as a bridge through the combination of compound structures and pharmacological effects. ResultThe total glucosides of Paeoniae Radix Alba had good anti-inflammatory and analgesic effects in vivo. The core targets of 23 active components of Paeoniae Radix Alba were epidermal growth factor receptor (EGFR), signal transducer and activator of transcription 3 (STAT3), vascular endothelial growth factor A (VEGFA), cellular tumor antigen p53 (TP53), and proto-oncogene transcription factor (JUN). According to the structure of the parent nucleus, there were 16 pinane monoterpene glycosides, 4 pinene monoterpene glycosides, 2 monoterpene lactone glycosides, and 1 monoterpene ketone. The key core targets screened out by molecular docking were EGFR and STAT3. The structure-activity analysis of the active compound structures and the key core targets showed that the introduction of ketone group and benzene ring group on the parent nucleus affected the binding activity. ConclusionThis study analyzed the material basis for the anti-inflammatory and analgesic effects of total glycosides of Paeoniae Radix Alba from structure-activity omics, providing new ideas and methods for revealing the pharmacodynamic substances in traditional Chinese medicine.
10.Analysis of the characteristics of platelet changes and influencing factors after transcatheter aortic valve implantation
Xiangyu LI ; Haibo ZHANG ; Fangyu YANG ; Shuai ZHENG ; Fei MENG ; Shengxun WANG ; Yuqing JIAO ; Yuehuan LI ; Kaisheng WU ; Jinglun SHEN
Chinese Journal of Clinical Thoracic and Cardiovascular Surgery 2024;31(06):832-837
Objective To analyze the characteristics of platelet changes and their influencing factors during postoperative hospitalization in patients who underwent transcatheter aortic valve implantation (TAVI). Methods The patients who underwent TAVI at Beijing Anzhen Hospital Valve Surgery Center between March 2017 and October 2021 were retrospectively selected. The patients were divided into a self-limiting group and a non-self-limiting group according to the characteristics of postoperative platelet decline. In addition, the general preoperative data, preoperative and postoperative ultrasound data, intraoperative data, and the use of anticoagulant drugs during the postoperative stay in the hospital were compared between the two groups. Results A total of 249 patients were enrolled in this study. There were 175 (70.3%) patients in the self-limiting group, including 100 males and 75 females, and there were 74 (29.7%) patients in the non-self-limiting group, including 43 males and 31 females, with no statistical difference between the two groups (P=0.863). The mean age of patients was 73.11±8.88 years in the self-limiting group and 71.54±10.39 years in the non-self-limiting group (P=0.231). The decline of platelets in the self-limiting group generally occurred on the postoperative day 2 and reached the lowest count on the postoperative day 4, and returned to the baseline level on the postoperative day 5-7, while the platelets in the non-self-limiting group changed by simple rise, fall or irregular fluctuation. Patients in the self-limiting group had severer preoperative aortic stenosis (P<0.001) and used more extracorporeal circulation assistance during surgery (P<0.001). Postoperatively, patients in the self-limiting group were more likely to have periaortic valve leakage than those in the non-self-limiting group (P=0.013). Conclusion Platelet changes in most patients after TAVI show a self-limiting decline, which may be related to the severity of patients’ preoperative aortic stenosis, intraoperative extracorporeal circulation device use, and postoperative perivalvular leakage.

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