Pub Date : 2023-01-01DOI: 10.12677/hjmce.2023.113024
树香 李
Objective: The abnormal cell cycle caused by Cyclin-dependent kinases 6 (CDK6) overexpression is responsible for excessive proliferation of cancer cells
{"title":"Virtual Screening of Antitumor Small Molecule Inhibitors Targeting CDK6","authors":"树香 李","doi":"10.12677/hjmce.2023.113024","DOIUrl":"https://doi.org/10.12677/hjmce.2023.113024","url":null,"abstract":"Objective: The abnormal cell cycle caused by Cyclin-dependent kinases 6 (CDK6) overexpression is responsible for excessive proliferation of cancer cells","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66078794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-01DOI: 10.12677/hjmce.2023.111004
晨帆 李
{"title":"Mechanism and Treatment of Drug Resistance in Castration-Resistant Prostate Cancer Caused by Glucocorticoid Receptors","authors":"晨帆 李","doi":"10.12677/hjmce.2023.111004","DOIUrl":"https://doi.org/10.12677/hjmce.2023.111004","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66077416","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-01DOI: 10.12677/hjmce.2023.111003
晴晴 王
{"title":"Study on the HPLC Fingerprint Chromatogram of Xinhui Tangerine Peel in Different Years","authors":"晴晴 王","doi":"10.12677/hjmce.2023.111003","DOIUrl":"https://doi.org/10.12677/hjmce.2023.111003","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66077757","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-01DOI: 10.12677/hjmce.2023.113025
志梁 范
{"title":"Mechanism of Astragaloside Intervention in Osteoporosis Based on Network Pharmacology and Molecular Docking Technology","authors":"志梁 范","doi":"10.12677/hjmce.2023.113025","DOIUrl":"https://doi.org/10.12677/hjmce.2023.113025","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66078991","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-01DOI: 10.12677/hjmce.2022.113017
艳梅 董
4-cyclopropyl-1,2,5-oxadiazole-3-carboxylic acid as the bioelectronic row of amide bond has important application value in the field of pharmaceutical chemistry, but the existing conventional synthesis methods use oxidants (potassium permanganate, sodium nitrate), easy to produce explosion risks, difficult to control the reaction, low total yield. In this paper, 3-cyclopropyl isoox-董艳梅
{"title":"Continuous Synthesis of 4-Cyclopropyl-1,2,5-Oxadiazole-3-Carboxylic Acid","authors":"艳梅 董","doi":"10.12677/hjmce.2022.113017","DOIUrl":"https://doi.org/10.12677/hjmce.2022.113017","url":null,"abstract":"4-cyclopropyl-1,2,5-oxadiazole-3-carboxylic acid as the bioelectronic row of amide bond has important application value in the field of pharmaceutical chemistry, but the existing conventional synthesis methods use oxidants (potassium permanganate, sodium nitrate), easy to produce explosion risks, difficult to control the reaction, low total yield. In this paper, 3-cyclopropyl isoox-董艳梅","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66077583","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-01DOI: 10.12677/hjmce.2023.112007
津铭 康
{"title":"Optimization of Detoxification Process for Low Ginkgo Phenolic Acid in Ginkgo Powder","authors":"津铭 康","doi":"10.12677/hjmce.2023.112007","DOIUrl":"https://doi.org/10.12677/hjmce.2023.112007","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66077709","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-01DOI: 10.12677/hjmce.2023.113023
婷婷 成
Objective: To study the effect and mechanism of tiacon of Yi medicine L. franchetii on osteoarthritis in rats, and to provide relevant evidence for the development and research of Fireweed. Me-thods: 60 male SD rats were randomly divided into 6 groups of 10 rats each, namely, the blank control group, the model group, the positive drug (3.0 g/kg of Voltaline cream) group, and the L. franchetii low, medium, and high dose (1.2 g of raw drug/kg, 2.4 g of raw drug/kg, and 4.8 g of raw drug/kg) groups, and were modeled by injecting 0.2 mL of 6% papain solution. Observe the appearance of joints and hairs with the naked eye after 4 weeks; observe the HE-stained pathological sections of cartilage tissues under light microscope; the levels of TNF-α and IL-1 β in rat cartilage tissues were measured by enzyme-linked immunosorbent assay (ELISA); the levels of MMP13 and SOX-9 genes in rat cartilage tissues were measured by immunohistochemistry. Result: Compared with the blank group, the model group had severe joint redness and swelling, and the levels of inflammatory factors IL-1 β and TNF-α , the expression of MMP13 gene increased significantly ( P < 0.01), and the expression of SOX-9 gene decreased significantly ( P < 0.05) in the synovial tissue of rats in each dose group of L. franchetii ; compared with the model group, the TNF-α content and MMP13 gene expression level in the synovial tissue of rats in each dose group of L. franchetii were significantly decreased ( P < 0.01), the IL-1 β content in the low and high dose groups of L. franchetii was significantly decreased ( P < 0.05), and the SOX-9 gene expression level in the high dose group of L. franchetii was significantly increased ( P < 0.05), but the rest of the content differences were not statistically significant. Conclusion: The external application of L. franchetii drug has a joint-protective effect on the cartilage tissue of rats and has a certain repair function on the cartilage tissue, which can relieve the disease of osteoarthritis.
{"title":"The Mechanism of Action of Yi Medicine Leontopodium franchetii in the Treatment of Osteoarthritis in Rats","authors":"婷婷 成","doi":"10.12677/hjmce.2023.113023","DOIUrl":"https://doi.org/10.12677/hjmce.2023.113023","url":null,"abstract":"Objective: To study the effect and mechanism of tiacon of Yi medicine L. franchetii on osteoarthritis in rats, and to provide relevant evidence for the development and research of Fireweed. Me-thods: 60 male SD rats were randomly divided into 6 groups of 10 rats each, namely, the blank control group, the model group, the positive drug (3.0 g/kg of Voltaline cream) group, and the L. franchetii low, medium, and high dose (1.2 g of raw drug/kg, 2.4 g of raw drug/kg, and 4.8 g of raw drug/kg) groups, and were modeled by injecting 0.2 mL of 6% papain solution. Observe the appearance of joints and hairs with the naked eye after 4 weeks; observe the HE-stained pathological sections of cartilage tissues under light microscope; the levels of TNF-α and IL-1 β in rat cartilage tissues were measured by enzyme-linked immunosorbent assay (ELISA); the levels of MMP13 and SOX-9 genes in rat cartilage tissues were measured by immunohistochemistry. Result: Compared with the blank group, the model group had severe joint redness and swelling, and the levels of inflammatory factors IL-1 β and TNF-α , the expression of MMP13 gene increased significantly ( P < 0.01), and the expression of SOX-9 gene decreased significantly ( P < 0.05) in the synovial tissue of rats in each dose group of L. franchetii ; compared with the model group, the TNF-α content and MMP13 gene expression level in the synovial tissue of rats in each dose group of L. franchetii were significantly decreased ( P < 0.01), the IL-1 β content in the low and high dose groups of L. franchetii was significantly decreased ( P < 0.05), and the SOX-9 gene expression level in the high dose group of L. franchetii was significantly increased ( P < 0.05), but the rest of the content differences were not statistically significant. Conclusion: The external application of L. franchetii drug has a joint-protective effect on the cartilage tissue of rats and has a certain repair function on the cartilage tissue, which can relieve the disease of osteoarthritis.","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66078355","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-01-01DOI: 10.12677/hjmce.2023.114026
敬赫 王
Objective : In order to establish a new HPLC method for the determination of intermediate 5 of vilan-terol and its related substances. Methods : The chromatographic analysis was performed on C18 na-noscopic column (250 × 4.6 mm, 5 μm) with mobile phase acetonitrile (A) - water (B) and isodegree elution (80% A), and the flow rate was 1.0 min∙ mL − 1 . The detection wavelength was 220 nm, and the related substances were separated by preparative or semi - preparative chromatography. The quali t-ative and quantitative analysis of intermediate 5 and its related substances was realized by HPLC and LC - MS analysis. Results : The results showed that the intermediate 5 showed a good linear relationship in a certain concentration range (Y = 38705X + 21.565), the average recovery was 100.61%~104.81%, RSD < 0.2%, and the repeatability was good (RSD < 0.5%). The solution was stable within 12 h (RSD < 2.0%). The content of intermediate 5 and its related substances was determined by this method. The content of intermediate 5 was 98.0%~99.5%, and the total content of m a-jor impurities was 0.3%~0.6%. The impurity I (RT 1.47 min) was determined to be p - toluenesulfonic acid by qualitative structural analysis, and the impurity III (RT 2.82 min) was determined to be intermediate 4. It is the raw material not cleaned in synthesis. Conclusion : This study provides the o-retical and methodological support for process optimization, effective reduction or removal of impurities and quality control of key intermediates.
{"title":"Study on the Content Analysis Method of Key Intermediates of Vilanterol and Its Related Substances","authors":"敬赫 王","doi":"10.12677/hjmce.2023.114026","DOIUrl":"https://doi.org/10.12677/hjmce.2023.114026","url":null,"abstract":"Objective : In order to establish a new HPLC method for the determination of intermediate 5 of vilan-terol and its related substances. Methods : The chromatographic analysis was performed on C18 na-noscopic column (250 × 4.6 mm, 5 μm) with mobile phase acetonitrile (A) - water (B) and isodegree elution (80% A), and the flow rate was 1.0 min∙ mL − 1 . The detection wavelength was 220 nm, and the related substances were separated by preparative or semi - preparative chromatography. The quali t-ative and quantitative analysis of intermediate 5 and its related substances was realized by HPLC and LC - MS analysis. Results : The results showed that the intermediate 5 showed a good linear relationship in a certain concentration range (Y = 38705X + 21.565), the average recovery was 100.61%~104.81%, RSD < 0.2%, and the repeatability was good (RSD < 0.5%). The solution was stable within 12 h (RSD < 2.0%). The content of intermediate 5 and its related substances was determined by this method. The content of intermediate 5 was 98.0%~99.5%, and the total content of m a-jor impurities was 0.3%~0.6%. The impurity I (RT 1.47 min) was determined to be p - toluenesulfonic acid by qualitative structural analysis, and the impurity III (RT 2.82 min) was determined to be intermediate 4. It is the raw material not cleaned in synthesis. Conclusion : This study provides the o-retical and methodological support for process optimization, effective reduction or removal of impurities and quality control of key intermediates.","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"298 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135701465","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-01-01DOI: 10.12677/hjmce.2022.101005
军 王
{"title":"Rapid Analysis of Content of Terpene Lactones in Ginkgo Centrifugal Solution by Near Infrared Spectroscopy","authors":"军 王","doi":"10.12677/hjmce.2022.101005","DOIUrl":"https://doi.org/10.12677/hjmce.2022.101005","url":null,"abstract":"","PeriodicalId":64647,"journal":{"name":"药物化学","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66074597","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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