1.Research on compaction behavior of traditional Chinese medicine compound extract powders based on unsupervised learning
Ying FANG ; Yan-long HONG ; Xiao LIN ; Lan SHEN ; Li-jie ZHAO
Acta Pharmaceutica Sinica 2025;60(2):506-513
Direct compression is an ideal method for tablet preparation, but it requires the powder's high functional properties. The functional properties of the powder during compression directly affect the quality of the tablet. 15 parameters such as Py, FES-8KN,
2.Effects of Schisandrin B on myocardial cell apoptosis in rats after myocardial infarction
Yan-Bing HUANG ; Wei-Wen CHEN ; Yan-Long HUANG ; Tian-Lai LIN
The Chinese Journal of Clinical Pharmacology 2024;40(7):999-1003
Objective To investigate the protective effect of Schisandrin B on myocardial infarction in rats and its mechanism.Methods Fifty SD rats were randomly divided into sham group,model group,positive control group(10 mg·kg-1 captopril),experimental-L group(30 mg·kg-1 schisandrin B)and experimental-H(60 mg·kg-1 schisandrin B)group,with 10 rats in each group.Cardiac function related indexes were detected,serum myocardial injury markers and serum inflammatory factors were detected by the kit,myocardial apoptosis was detected by terminal-deoxynucleoitidyl transferase mediated nick end labeling(TUNEL)method,and myocardial tissue related protein expression levels were detected by Western blot method.Results Left ventricular ejection fraction(LVEF)levels in sham group,model group,positive control group,experimental-L group and experimental-H group were(78.42±4.32)%,(41.65±2.94)%,(59.76±5.35)%,(49.13±3.92)%and(67.04±3.00)%;the contents of creatine kinase-MB(CK-MB)were(33.95±2.68),(100.51±3.92),(48.27±3.70),(70.34±2.93)and(49.13±3.67)U·mL-1;interleukin-1 β(IL-1 β)levels were(1.02±0.12),(3.02±0.20),(1.61±0.13),(2.33±0.26)and(1.34±0.14)ng·mL-1;TUNEL positive cell rates were(3.47±0.82)%,(31.79±3.68)%,(11.22±1.02)%,(19.74±1.42)%and(14.38±1.13)%;the expression levels of Nod-like receptor thermal protein domain associated protein 3(NLRP3)protein were 0.35±0.07,1.04±0.10,0.55±0.05,0.85±0.07 and 0.39±0.06;the protein levels of cysteine aspartic acid specific protease 1(caspase-1)were 0.34±0.05,1.05±0.10,0.50±0.06,0.72±0.05 and 0.46±0.03,respectively.The above indexes were compared between model group and sham group,the differences were statistically significant(all P<0.05).The positive control group,experimental-L group and experimental-H group were compared with model group,the differences were statistically significant(all P<0.05).The difference between experimental-H group and experimental-L group were statistically significant(all P<0.05).Conclusion Schisandrin B can mediate inflammatory response and cardiomyocyte apoptosis,improve cardiac function,and protect rats with myocardial infarction,which is related to NLRP3 inflammatory pathway.
3.Research progress on atrial functional mitral regurgitation
Huowang HUANG ; Peng LI ; Shen HAN ; Li LIN ; Jinting LONG ; Guihua LIU ; Yaxiong LI ; ou Hai LI
Chinese Journal of Clinical Thoracic and Cardiovascular Surgery 2024;31(09):1369-1375
Atrial functional mitral regurgitation (AFMR) is mitral regurgitation in patients with atrial fibrillation (AF), whose left atrium (LA) is enlarged, the left ventricle is not enlarged or only slightly enlarged, the left ventricular ejection fraction is preserved, and the mitral valve itself has no apparent lesion. At present, the etiology, pathophysiology and mechanism of this disease have not been completely clear yet. Existing studies have found that the causes of AFMR mainly include AF, enlargement of LA and mitral annulus, destruction of mitral annular shape, inability of mitral valve remodeling to compensate for mitral annular expansion, and hamstringing of the posterior mitral leaflet by atriogenic tethering. AFMR is demonstrated to be associated with an increased risk of mortality and readmission due to heart failure. Therefore, it serves as a primary therapeutic target for patients with heart failure and AF. However, the optimal treatment of AFMR still remains controversial. Therefore, this article will mainly expound the current definition, etiology, pathophysiological mechanism, treatment, and prognosis of AFMR.
4.Exploration on bioactive equivalent combinatorial components of Xiaoke formula and its mechanism based on insulin resistance mice
Jian ZHANG ; Wen-juan MA ; Lin-jie DONG ; Jiang-lan LONG ; Yu ZHANG ; Dan YAN
Acta Pharmaceutica Sinica 2024;59(6):1698-1705
Xiaoke formula (XKF) is a classic formula for the treatment of insulin resistance (IR), but there is still unclear on bioactive equivalent combinatorial components (BECC) of XKF. In this study, based on the previous research of our team, three components, berberine, astragaloside IV and chlorogenic acid, were selected as the BECC of XKF, and their efficacy and mechanism were investigated. A high-fat diet-induced IR mouse model was used to detect blood glucose, insulin sensitivity, lipid metabolism, immune & inflammatory factors, etc., and staining of pathology sections was used to detect histopathological changes. Network pharmacology was used to predict the potential targets and signaling pathways of XKF and its BECC, and the results of the network were verified by Western blot. The animal welfare and experimental procedures followed the regulations of the Laboratory Animal Ethics Committee of Beijing MDKN Biotech Company (MDKN-2023-019). The results showed that BECC, which was composed of berberine, astragaloside IV and chlorogenic acid in the ratio of the original formula of XKF, was comparable to XKF in improving the glycemia, insulin sensitivity, histopathological damage, dyslipidemia, and immuno-inflammation in IR mice. The results of network pharmacology and Western blot suggested that the BECC of XKF and XKF might alleviate IR by promoting the activation of hepatic phosphatidylinositol 3-kinase (PI3K), phosphorylation of protein kinase B (AKT), and inhibiting the expression of glucose-6-phosphate phosphatase (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1), the key limiting enzymes of hepatic gluconeogenesis. The above results suggest that berberine, astragaloside IV and chlorogenic acid can be used as the potential BECC of XKF to improve IR, and can regulate lipid metabolism, immuno-inflammation, and promote hepatic PI3K/AKT signaling to inhibit hepatic gluconeogenesis, regulate glucose homeostasis, and improve IR in mice.
5.Discovery of the targets and lead compounds of traditional Chinese medicine based on the molecular trajectory of diabetes evolution
Yu ZHANG ; Jiang-lan LONG ; Ai-ting WANG ; Hao LÜ ; Ke-jun DENG ; Hao LIN ; Dan YAN
Acta Pharmaceutica Sinica 2024;59(8):2199-2204
Exploring the action targets (groups) of traditional Chinese medicine (TCM) is an important proposition to promote the innovation and development of TCM, but it has attracted a lot of attention as to whether it is related to the efficacy or the disease. Our team found that the metabolomic signature molecules in the development of diabetes mellitus (DM) were significantly associated with the clinical efficacy of Yuquan Pill through a large clinical sample study. Taking this as a clue, our team intends to expand the information on the omics features of DM development, and discover the key targets (groups) and their lead compounds for the hypoglycemic effect of Yuquan Pill. The project includes: ① Based on the retrospective clinical trials, using omics technology integrated with generative artificial intelligence, mining the characteristic information of proteome and microbiome, forming driving factors together with metabolome characteristic molecules, and characterizing the molecular trajectories of diabetes evolution and their interference by Yuquan Pill; ② Taking the evolving molecular trajectories as a link and pointer, using anthropomorphic modeling and molecular biology techniques such as chemical proteomics to discover the key targets (groups) of Yuquan Pill's hypoglycemic effect, with the prospective clinical samples for validation; ③ Evaluate the overall response of key targets (groups) using graph neural network technology, and search for drug-derived/endogenous lead compounds with proven clinical pathologies and clear mechanisms of action, so as to provide a new paradigm and technology for the discovery of complex active ingredient targets (groups) of TCM that are related to their clinical efficacy, as well as for the discovery of innovative medicines.
6.Determination of Traditional Chinese Medicine Syndrome of Rat Model of Follicular Dysplasia Induced by Tripterygium Glycosides Based on Prescriptions via AMPK/mTOR/HIF-1/VEGF Pathway
Yingying HU ; Xuejuan LIN ; Zushun ZHUO ; Shanshan DING ; Mengting ZHANG ; Guorong LIN ; Long ZHU ; Yuyu XIE ; Yan XIONG
Chinese Journal of Experimental Traditional Medical Formulae 2024;30(14):46-54
ObjectiveTo determine the syndrome of a rat model of follicular dysplasia induced by Tripterygium glycosides based on prescriptions and investigate the mechanism of traditional Chinese medicine intervention via the adenosine monophosphate-activated protein kinase (AMPK)/mammalian target of rapamycin (mTOR)/hypoxia-inducible factor-1 (HIF-1)/vascular endothelial growth factor (VEGF) pathway. MethodForty-eight rats with regular estrous cycles were randomly assigned into a normal group (n=8) and a modeling group (n=40). The rats in the modeling group were administrated with Tripterygium glycoside suspension (75 mL·kg-1) by gavage for 30 days. The modeled rats were assigned into model, Siwutang (3.69 g·kg-1), Youguiyin (3.11 g·kg-1), Zuoguiyin (7.29 g·kg-1), and Guishenwan (10.35 g·kg-1) groups, with 8 rats in each group. The drug intervention lasted for 14 days. The changes of estrous cycle were detected by Pap staining, and a stereoscope was used to observe the morphology of the ovarian tissue. Hematoxylin-eosin staining was employed to observe the pathological changes and follicle count in the ovarian tissue. Enzyme-related immunosorbent assay (ELISA) was used to measure the levels of follicle-stimulating hormone (FSH), luteinizing hormone (LH), and estradiol (E2) in the serum. Real-time fluorescence quantitative polymerase chain reaction and Western blot were employed to determine the mRNA and protein levels, respectively, of AMPK, mTOR, HIF-1, and VEGF in the ovarian tissue. ResultCompared with the normal group, the model group had a disordered estrous cycle, reduced secondary and mature follicles, increased atretic follicles, elevated FSH and LH levels, lowered E2 level, up-regulated mRNA and protein levels of AMPK, and down-regulated mRNA and protein levels of mTOR, HIF-1, and VEGF (P<0.01). Compared with the model group, Guishenwan increased secondary and mature follicles, decreased atretic follicles, lowered the FSH and LH levels, elevated the E2 level, down-regulated the mRNA and protein levels of AMPK, and up-regulated the mRNA and protein levels of mTOR, HIF-1, and VEGF (P<0.01). Compared with Guishenwan group, Siwutang, Youguiyin, and Zuoguiyin decreased mature follicles, increased atretic follicles (P<0.01), elevated the LH (P<0.01) and FSH (P<0.05) levels, and lowered the E2 level (P<0.05). In addition, Youguiyin up-regulated the protein level of AMPK (P<0.05) and down-regulated the mRNA levels of mTOR and HIF-1 (P<0.01) as well as the mRNA and protein levels of VEGF (P<0.01). Siwutang down-regulated the mRNA levels of mTOR and HIF-1 as well as the mRNA and protein levels of VEGF (P<0.05). Zuoguiyin down-regulated the mRNA level of mTOR and the protein and mRNA levels of VEGF (P<0.05). ConclusionGuishenwan may improve the ovarian function and promote follicle maturation in a rat model of follicular dysplasia by inhibiting the AMPK/mTOR/HIF-1/VEGF pathway, with the therapeutic effect superior to Zuoguiyin, Youguiyin, and Siwutang. It was hypothesized that this model presented the syndrome of kidney-essence deficiency.
7. Advances in relationship between pyroptosis and pulmonary arterial hypertension and therapeutic drugs
Qian YAN ; Yang SUN ; Jun-Peng LONG ; Jiao YAO ; Yu-Ting LIN ; Song-Wei YANG ; Yan-Tao YANG ; Gang PEI ; Qi-Di AI ; Nai-Hong CHEN ; Qian YAN ; Yang SUN ; Jun-Peng LONG ; Jiao YAO ; Yu-Ting LIN ; Song-Wei YANG ; Yan-Tao YANG ; Gang PEI ; Qi-Di AI ; Nai-Hong CHEN ; Sha-Sha LIU ; Nai-Hong CHEN
Chinese Pharmacological Bulletin 2024;40(1):25-30
Pyroptosis is the programmed death of cells accompanied by an inflammatory response and is widely involved in the development of a variety of diseases, such as infectious diseases, cardiovascular diseases, and neurodegeneration. It has been shown that cellular scorching is involved in the pathogenesis of pulmonary arterial hypertension ( PAH) in cardiovascular diseases. Patients with PAH have perivascular inflammatory infiltrates in lungs, pulmonary vasculopathy exists in an extremely inflam-matory microenvironment, and pro-inflammatory factors in cellular scorching drive pulmonary vascular remodelling in PAH patients. This article reviews the role of cellular scorch in the pathogenesis of PAH and the related research on drugs for the treatment of PAH, with the aim of providing new ideas for clinical treatment of PAH.
8.Influencing factors of the TEG maximum amplitude reduction in emergency trauma patients
Changfu JI ; Dong LAI ; Yan TIAN ; Fei LAI ; Shuting LIN ; Min LONG ; Fangyuan LI ; Fangling LIAN
Chinese Journal of Blood Transfusion 2024;37(6):638-642
Objective To investigate the causes of abnormal decrease in maximum amplitude(MA)of thromboelastog-raphy(TEG)and its effect on prognosis by monitoring the changes of coagulation-related indexes in emergency trauma pa-tients.Methods A total of 319 cases of trauma patients admitted to our hospital from September 2020 to September 2023 were retrospectively analyzed,and the coagulation-related indexes of 0 h and 24 h after admission were observed.According to the MA results,they were divided into normal MA group(>50 mm)and reduced MA group(≤50 mm)to compare the hemoglobin(Hb),platelets count(Plt),activated partial thromboplastin time(APTT),prothrombin time(PT),fibrinogen(Fib),thrombin time(TT),D-dimer(D-D),coagulation reaction time(R),clot formation kinetics(Angle),30 min clot dissolution rate(Ly30),MA,thrombine-antithrombin complex(TAT)and plasminase-α2 plasminase inhibitor complex(PIC).The correlation between MA and fibrinolysis indexes in 319 trauma patients was analyzed.According to whether tranexamic acid(TXA)was used,the reduced MA group was divided into a TXA group and a non-drug group.The differ-ences in the change of the above coagulation-related indexes,mortality rate and changes in blood product dosage were com-pared between the two groups.Results Compared with the normal MA group,Hb,Plt,Fib,diastolic blood pressure and GCS scores decreased,while heart rate,ISS score and mortality increased significantly in the reduced MA group(P<0.05).The R,PT and TT were prolonged significantly(P<0.05),and PIC and D-D increased significantly(P<0.05)in the re-duced MA group.Correlation analysis found that MA had no correlation with Ly30,TAT and APTT,but was correlated with Angle(r=0.803),Plt(r=0.544),Fib(r=0.581),PIC(r=-0.443)and D-D(r=-0.343).Compared with the non-drug group,the change of Angle,MA and FIB in the TXA group increased significantly(P<0.05),while the change of PIC de-creased(P<0.05).Cryoprecipitate and platelet transfusion in the TXA group reduced significantly(P<0.05),and red blood cell transfusion had a decreasing trend,but the difference was not significant(P>0.05).The mortality rate in the TXA group was reduced significantly(P<0.05).Conclusion Hyperfibrinolysis may be an important factor in the abnormal decrease of MA in emergency trauma patients.Treatment with TXA can improve its effect on MA,and reduce the transfusion of blood products and the patient mortality.
9.Spiral Microfluidic for Particle Focusing by Stabilization and Acceleration of Secondary Flow
Han-Jie BAI ; Zhi-Hui LIN ; Shi-Chao GUO ; Dan-Dan LONG ; Yan-Bing NIU ; Lei ZHAO ; Shao-Fei SHEN
Chinese Journal of Analytical Chemistry 2024;52(4):504-512
Inertial microfluidics,as a microfluidic technology with the ability to precisely manipulate particles and cells with high throughput,has attracted widespread attention.However,challenges remain in achieving particle focusing with insensitivity to flow rates in large-scale channels,mainly due to the instability of secondary flows within the inertial microfluidic chip.This study developed a microstructure-assisted ultra-low aspect ratio spiral microchannel,which utilized the stability and acceleration of secondary flows to achieve inertial particle focusing.The research results demonstrated successful particle focusing within a 1 mm-wide spiral channel chip,for different diameter sizes(7.3 μm and 15.5 μm),within a wide range of flow rates(0.5-3 mL/min).The focusing efficiencies for these particles were measured to be above 94%and 99%,respectively.Additionally,it was observed that the particle focusing position was approximately 100 μm away from the channel walls,significantly larger than other inertial focusing chips.Consequently,by incorporating ordered microstructures within the spiral channel chip,the stability and enhancement of secondary flows were achieved,resulting in flow rate and particle size-insensitive inertial focusing.Compared to traditional methods of inertial focusing,this design had advantages of not requiring additional sheath flow operations,and boasted high throughput and ease of manufacturing.This innovative structure opened up vast prospects for the development of portable inertial microfluidic chips,and could be used in the fields such as cell analysis and detection,flow cytometry,and online sample processing.
10.Exploring the Acupoint Selection Rules of Acupuncture for the Treatment of Lower Limb Spasm After Stroke Based on Data Mining Techniques
Shan CONG ; Jun-Feng ZHANG ; Hong LI ; Meng WANG ; Long YAN ; Yu-Lin QIAN ; Tao YU
Journal of Guangzhou University of Traditional Chinese Medicine 2024;41(6):1522-1529
Objective To explore the acupoint selection rules of acupuncture for the treatment of lower limb spasm after stroke based on data mining technology.Methods Through the computer retrieval of CNKI,Wanfang,VIP,PubMed,EMbase,web of science databases and other databases,the literature that meets the inclusion criteria was selected to establish a database.Descriptive analysis,cluster analysis and association rule analysis were performed on the data through Microsoft Excel 2016,IBM SPSS Statistics 21 and IBM SPSS Modeler 18.0 software.Results(1)A total of 68 acupuncture prescriptions were included,involving 100 acupoints and a total frequency of 536 uses;(2)the top five in terms of frequency of use of acupoints were Yanglingquan(GB34),Zusanli(ST36),Xuanzhong(GB39),Qiuxu(GB40),Sanyinjiao(SP6);(3)the core acupoint pairing was Yanglingquan(GB34)-Xuanzhong(GB39),and five valid clustering clusters were obtained,which were Shenmai(BL62)-Zhaohai(KI6),Weizhong(BL40)-Kunlun(BL60),Xuehai(SP10)-Huantiao(GB30)-Fenglong(ST40)-Zusanli(ST36),Taixi(KI3)-Yinlingquan(SP9)-Sanyinjiao(SP6),Jiexi(ST41)-Taichong(LR3)-Xuanzhong(GB39)-Qiuxu(GB40)-Yanglingquan(GB34).Conclusion Through data mining,it is found that acupuncture treatment of lower limb spasm after stroke is mostly based on Yanglingquan,Zusanli,Xuanzhong,Qiuxu and Xuanzhong.Priority should be given to the application of three yang channels of the foot and five shu acupoint,syndrome differentiation and treatment,and modification should be adjusted according to the syndromes,so as to provide reference for clinical treatment of lower limb spasm after stroke.

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