2023 Vol. 41, No. 12
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2023, 41(12): 705-709, 732.
doi: 10.12206/j.issn.2097-2024.202211025
Abstract:
As a highly malignant tumor, the diagnosis of cholangiocarcinoma (CCA) is often late and the prognosis is poor for which the early symptoms are atypical and the lack of accurate biomarkers. Metabolomics is an emerging science that researches the alterations of all endogenous small molecule metabolites in an organism under the influence of pathological, physiological or genetic modification. The development and progress of CCA is closely related to metabolism. Metabolomic is characterized by global analysis, high throughput and reflects real-time alterations in biology system, providing a new avenue for biomarker screening and diseases diagnosis and treatment. The advances of metabolomics studies on CCA in the recent years were reviewed in this paper which could provide the reference for further research.
As a highly malignant tumor, the diagnosis of cholangiocarcinoma (CCA) is often late and the prognosis is poor for which the early symptoms are atypical and the lack of accurate biomarkers. Metabolomics is an emerging science that researches the alterations of all endogenous small molecule metabolites in an organism under the influence of pathological, physiological or genetic modification. The development and progress of CCA is closely related to metabolism. Metabolomic is characterized by global analysis, high throughput and reflects real-time alterations in biology system, providing a new avenue for biomarker screening and diseases diagnosis and treatment. The advances of metabolomics studies on CCA in the recent years were reviewed in this paper which could provide the reference for further research.
2023, 41(12): 710-713, 721.
doi: 10.12206/j.issn.2097-2024.202204043
Abstract:
The transcription factor ZNF24 (also known as ZNF191 or KOX17) is a member of the Krüppel-like zinc finger transcription factor family, with a leucine-rich (Leu) SCAN domain (also known as LeR domain) at the N-terminus and four consecutive typical Kruppel-like zinc finger modities at the C-terminus. ZNF24 is a multifunctional transcription factor involved in the regulation of kinase transcriptional activity, vascular proliferation and development, especially in tumorigenesis and tumor progression. ZNF24 plays an important and complex dual-directional regulation role (promoting and inhibiting) in tumor development, invasion and metastasis by regulating the transcriptional expression of different target genes (such as VEGF, Wnt8B, Twist1, β-catenin and DGL1, etc.) and the competitive binding with protein factors (such as β-catenin). Therefore, elucidating the mechanism of ZNF24 in tumors would provide clues and ideas for the treatment of tumors. The researches status of ZNF24 in tumors were summarized in this paper.
The transcription factor ZNF24 (also known as ZNF191 or KOX17) is a member of the Krüppel-like zinc finger transcription factor family, with a leucine-rich (Leu) SCAN domain (also known as LeR domain) at the N-terminus and four consecutive typical Kruppel-like zinc finger modities at the C-terminus. ZNF24 is a multifunctional transcription factor involved in the regulation of kinase transcriptional activity, vascular proliferation and development, especially in tumorigenesis and tumor progression. ZNF24 plays an important and complex dual-directional regulation role (promoting and inhibiting) in tumor development, invasion and metastasis by regulating the transcriptional expression of different target genes (such as VEGF, Wnt8B, Twist1, β-catenin and DGL1, etc.) and the competitive binding with protein factors (such as β-catenin). Therefore, elucidating the mechanism of ZNF24 in tumors would provide clues and ideas for the treatment of tumors. The researches status of ZNF24 in tumors were summarized in this paper.
2023, 41(12): 714-721.
doi: 10.12206/j.issn.2097-2024.202209051
Abstract:
Objective To explore the potential mechanism of artemisinin in the treatment of polycystic ovary syndrome (PCOS) by network pharmacology and molecular docking technology. Methods The corresponding targets of natural product artemisinin were obtained from PubChem, Swiss Target Prediction and PharmMapper databases, targets related to PCOS were obtained through GeneCards and DisGeNET databases; the intersection target genes of Artemisinin and PCOS were screened by Draw Venn diagram. Then the protein-protein interaction network (PPI) was constructed according to the intersection target genes through the STRING Database, and the core targets were screened by Cytoscape. Besides, gene ontology (GO) function and Kyoto encyclopedia of genes and genomes (KEGG) pathway analysis was performed by DAVID Database, and finally the data were analyzed visually by the online platform. Molecular docking of artemisinin and core targets were performed by Chemdraw, Pymol, Auto Dock Tools and RCSB PDB database. Results A total of 229 targets of artemisinin and 1292 targets of PCOS were screened out, 90 overlapping targets were obtained by Draw Venn diagram, and 5 potential core targets, AKT1, ESR1, MMP9, PPARG, MMP2, were mainly act on PI3K Akt, MAPK, RAS, endocrine resistance and other signal pathways. Molecular docking results showed that there were molecular binding sites between artemisinin and core targets. Conclusion It is preliminarily analyzed that artemisinin may play a therapeutic role in PCOS through multiple targets and mechanisms.
2023, 41(12): 722-732.
doi: 10.12206/j.issn.2097-2024.202302001
Abstract:
Objective To analyze the main active components and potential molecular mechanism of Sophora flavescens against breast cancer based on network pharmacology and molecular docking. Methods The chemical constituents were collected and screened by TCMSP, ETCM database and literature review. The targets of active ingredients were predicted by Swiss Target Prediction database. Breast cancer-related targets were collected by GeneCards, TTD, Drugbank and OMIM. The anti-breast cancer targets of Sophora flavescens were screened by Venny 2.1.0 software. Cytoscape software was used to construct the network diagram of Sophora flavescens-key active ingredients-targets. STRING database was used to analyze the common targets, and PPI network diagram was constructed. GO function enrichment analysis and KEGG pathway enrichment analysis of key target proteins were performed by DAVID database and Hiplot online platform. Schrodinger software was used to calculate the molecular docking between the active ingredients and targets. Molecular biological methods were used to verify the key targets. Results A total of 36 active components with clear structures were screened from Sophora flavescens. 70 anti-breast cancer targets of Sophora flavescens were screened out. 12 core targets including EGFR, AKT1, ESR1, SRC, CYP19A1, AR and ABCB1 participate in endocrine resistance, EGFR tyrosine kinase inhibitors and estrogen signaling pathways in breast cancer. Moreover, the docking score between the core component and the key target AR is the highest. In vitro experiments showed that the extract of Sophora flavescens can inhibit the proliferation of breast cancer cells, induce cell apoptosis and up-regulate AR protein expression. Conclusion It was revealed that Sophora flavescens plays an anti-breast cancer role by regulating complex biological processes through multiple components acting on multiple targets and signaling pathways. The upregulation of AR protein by Sophora flavescens may become a new therapeutic strategy for the treatment of breast cancer.
2023, 41(12): 733-736.
doi: 10.12206/j.issn.2097-2024.202208022
Abstract:
Objective To conduct in vitro transdermal test on triamcinolone acetonide spray solution, and investigate the effects of ethanol and propylene glycol alone or in combination on the in vitro transdermal function of triamcinolone acetonide spray solution. Methods Rabbit abdominal skin was selected, and the in vitro penetration test of triamcinolone acetonide spray solution was carried out by Franz diffusion cell method, and the content of triamcinolone acetonide was determined by HPLC. The rate of transdermal absorption was compared. Results The transdermal absorption rate of the combined use of ethanol and propylene glycol was significantly higher than that of the single use (P<0.05), and the order of promoting the penetration of triamcinolone acetonide spray solution when ethanol and propylene glycol were combined by 10% ethanol + 25% propylene glycol >10% ethanol + 20% propylene glycol >15% ethanol + 25% propylene glycol >15% ethanol + 20% propylene glycol. Conclusion The combination of 10% ethanol and 25% propylene glycol could optimize the transdermal function of triamcinolone acetonide spray solution.
2023, 41(12): 737-740.
doi: 10.12206/j.issn.2097-2024.202303021
Abstract:
Objective To find a more effective alternative therapy for antibiotic therapy and fecal microbiota transplantation in current primary treatment of clostridioides difficile infection (CDI) because of the high recurrence rate. Methods A series of 8-hydroxyquinoline derivatives were designed and synthesized based on 8-hydroxyquinoline scarffold. Results The activity test against C. difficile showed that most of the molecules exhibited good antibacterial activity against C. difficile, and compound 6 f showed attractive anti-C. difficile activity. Conclusion A new type of 8-hydroxyquinoline derivatives with anti-clostridium difficile was found, which could be used as good lead compounds for further development.
2023, 41(12): 741-746.
doi: 10.12206/j.issn.2097-2024.202206052
Abstract:
Objective To evaluate the release characteristics in vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of silymarin phospholipid complex microporous osmotic pump controlled release tablets（SM-PC MPOP）. Methods The release characteristics of SM-PC MPOP in vitro were detected by HPLC in the artificial gastric fluid. Six beagle dogs were subjected to double cycle cross control, which were given SM-PC MPOP and Legalon（30 mg/kg）. The concentration of silybin in plasma was determined by HPLC and the data were processed by software. Results The cumulative release rate of SM-PC MPOP in vitro was over 85% in 12 h. The pharmacokinetics in beagle dogs showed that SM-PC MPOP and legalon conformed to double compartment first-order absorption model and the pharmacokinetic parameters were obtained: tmax:（3.2±0.4）and（0.9±0.1）h, Cmax:（0.298 6±0.068 9）and（0.629 9±0.076 5）μg/ml, AUC0→24:（2.996 8±0.583 3）and（2.268 9±0.432 8）h·μg /ml. The relative bioavailability of SM-PC MPOP was（162.21 ± 30.82）%. Conclusion SM-PC MPOP could release slowly, which could increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro was fine（r = 0.839 0）.
2023, 41(12): 747-752, 759.
doi: 10.12206/j.issn.2097-2024.202208101
Abstract:
Objective To explore the regularity of traditional Chinese medicine (TCM) in the treatment of postembolization syndrome (PES) after transcatheter arterial chemoembolization (TACE). Methods CNKI, WANFANG and VIP were used as data sources to search the journals and literatures related to TCM treatment from January 2000 to December 2021. Then, relevant TCM formula or Chinese patent medicines preparations were screened out. The Chinese medicinal materials contained were entered into Excel 2019 table database, and the data were analyzed by SPSS Statistics 21.0 and SPSS Modeler 18.0 statistical software. Results 86 qualified prescriptions were included, containing 181 Chinese medicinal materials, with a total frequency of 942 times. Of the 181 Chinese herbs included, there were 28 herbs with frequency ≥10%, with a total frequency of 587. The top 5 Chinese medicinal materials of frequency were licorice, Poria, Atractylodes, Bupleurum and Astragalus. Among the efficacy classifications, tonifying deficiency drugs, heat-clearing drugs and diuretics were most used. In four properties and five tastes, the top three of four properties were warm, flat and cold, and the top three of five tastes were sweet, bitter and pungent. In the classification of meridians, the first three meridians were spleen meridian, lung meridian and liver meridian. 30 association rules were obtained in association rules analysis, 11 common factors were obtained by factor analysis, 6 clustering combinations were obtained by cluster analysis, and 4 commonly used drug combinations were obtained. Conclusion The prescription drugs for the treatment of PES after TACE were mainly tonic drugs, heat-clearing drugs and diuresis and dampness-draining drugs. The treatment methods were mainly invigorating spleen and replenishing qi, clearing heat and dampness and detoxification.
2023, 41(12): 753-759.
doi: 10.12206/j.issn.2097-2024.202302040
Abstract:
Objective To screen potential metabolites and significantly altered metabolic pathways of liver lesions by central carbon pathway metabolites. Methods 32 healthy volunteers (HC), 23 patients with biliary cysts (CYST), 19 patients with biliary stones (Stone), 45 patients with hepatocellular carcinoma (HCC), and 50 patients with hilarcholangiocarcinoma (HCCA) were recruited. Their serum samples were collected for UPLC-QQQ-MS analysis and further MPP statistical analysis. Pattern recognition was further used to discovery the differences in metabolome between groups, and to explore the significantly altered metabolic pathway and possible pathogenic mechanism of liver diseases. Results A total of 15, 7, 7, and 3 metabolites and a total of 8, 4, 4, and 1 metabolic pathway that were significantly different in serum between CYST, Stone, HCC, HCCA and healthy controls were identified and enriched through serum metabolomics analysis, respectively. Conclusion According to the above identified differential metabolites and enriched metabolic pathway results, it is shown that liver lesions mainly involved in the energy metabolism and amino acid metabolism & transport, in addition, inositol phosphate metabolism were significantly changed both in CYST, Stone, HCC and HCCA.
2023, 41(12): 760-762.
doi: 10.12206/j.issn.2097-2024.202204122
Abstract:
Objective To investigate the antithrombotic therapy for acute myocardial infarction patients after PCI stenting combined with tricuspid valve repair. Methods The risk of bleeding and embolization was evaluated, relevant data were reviewed, professional knowledges of pharmacy were utilized through the whole treatment process, individualized medication plan for patients was designed and used. Results A better therapeutic effect was achieved through the implementation of pharmaceutical care and medication education to the patients. Conclusion Clinical pharmacists carry out pharmaceutical care in antithrombotic drugs utilities, which could improve the safety level of drug use and provide basis for clinical rational drug use.
2023, 41(12): 763-766.
doi: 10.12206/j.issn.2097-2024.202208080
Abstract:
Objective To explore the effect of metformin hydrochloride tablets on the clinical efficacy, number of dominant follicles and ovarian volume of polycystic ovary syndrome. Methods 150 patients diagnosed with polycystic ovary syndrome who were diagnosed and treated in our hospital from January 2019 to March 2021 were selected .The patients were divided into observation group and control group by random number table. The control group was treated with letrozole + gonadotropin, and the observation group was treated with letrozole + gonadotropin + hydrochloric acid + Metformin tablets. The clinical efficacy, endometrial thickness, number of high-quality follicles, sex hormone levels, blood lipid levels, and adverse reactions were compared between the two groups. Results ① The effective rate of treatment in the observation group was 90.67%, which was significantly higher than that in the control group, 78.67% (P<0.05). ② After treatment, the endometrial thickness of the observation group was lower than that of the control group, and the number of high-quality follicles was more than that of the control group(P<0.05). ③ After treatment, the levels of Luteinizing Hormone-LH, Follicle Stimulating Hormone-FSH and Testosterone (T) in the observation group were lower than those in the control group (P<0.05). ④ After treatment, the total cholesterol (TC) and triglyceride (TG) in the observation group were lower than those in the control group (P<0.05). ⑤ The incidence of adverse reactions in the observation group was 8.00%, which was significantly lower than 20.00% in the control group (P<0.05). Conclusion Letrozole + gonadotropin + metformin hydrochloride tablets could significantly improve the sex hormone and blood lipid levels in patients with polycystic ovary syndrome, relieve the symptoms of the patients, and improve their uterine condition, which had a good clinical effect.
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