1."Application of self-made blood""sampling-taking-transfusion""simulation video in management of ;safe blood transfusion"
Shouying LV ; Ailing LIU ; Guangyun ZHUANG ; Chunlin YAN
Chinese Journal of Practical Nursing 2016;32(32):2525-2528
Objective To study the effects of self-made blood sampling-taking-transfusionsimulation video in the management of safe blood transfusion. Methods According to the tracking results, the process of blood transfusion were improved. Then blood sampling-taking-transfusionsimulation video was made that was used in the safe management of blood transfusion and their effects were evaluated. Results The blood transfusion knowledge score and self-efficacy score of nurses were 87.32 ± 7.08, 2.83 ± 0.84, and that of before improvement were 78.38 ± 8.46, 2.52 ± 0.78, and there were statistically significant differences (t=-14.486,-3.274, P<0.01). The qualification rate of blood specimen collection, assessment and check before blood transfusion and nursing record were 97.14% (68/70), 98.57%(69/70), 97.14%(68/70), 98.57%(69/70), and that of before improvement were 51.43%(36/70), 78.57% (55/70), 68.57% (48/70), 82.86% (58/70), the difference was statistically significant (χ2=38.291, 13.831, 20.115, 10.206, P<0.01). The qualified rate of safe blood transfusion increased from 81.43%(57/70) before improvement to 100.00% (70/70) (χ2=14.331, P<0.01). Conclusions Self-made bloodsampling-taking-transfusionsimulation video in the safe management of blood transfusion is effective.
2.Research progress on the chemicals with cancer stem cell growth inhibitory activity
Jiao LI ; Hua TANG ; Chunlin ZHUANG ; Peng SUN ; Fujia MA ; Wen ZHANG
Chinese Journal of Biochemical Pharmaceutics 2017;37(3):20-26
Cancer stem cells play a crucial role in tumors'invasion, metastasis, recurrence and drug resistance.Investigation on the chemicals with tumor stem cell growth inhibitory activity has been greatly highlighted in the field of anti-tumor drug discovery.This paper briefly reviews the recent progress of chemical investigations on substances with tumor stem cell growth inhibitory activity , aiming to give readers a reference on anti-tumor drug discovery.
3.Methodology of drug screening and target identification for new necroptosis inhibitors
Pengchao PAN ; Zhenyu CAI ; Chunlin ZHUANG ; Xiaofei CHEN ; Yifeng CHAI
Journal of Pharmaceutical Analysis 2019;9(2):71-76
Apoptosis has been considered as the only form of regulated cell death for a long time. However, a novel form of programmed cell death called necroptosis was recently reported. The process of necroptosis is regulated and plays a critical role in the occurrence and development of multiple human diseases. Thus, the study on the molecular mechanism of necroptosis and its effective inhibitors has been an attractive field for researchers. Herein, we introduce the molecular mechanism of necroptosis and focus on the literature about necroptosis drug screening in recent years. In addition, the identification of the critical drug targets of the necroptosis is also discussed.
4.Recent research progress on anti-microtubule agents targeting multi-drug resistant cancers
Saijian SHI ; Wen ZHANG ; Tingyou LI ; Chunlin ZHUANG
Journal of Pharmaceutical Practice 2017;35(5):385-393,397
In 2015, more than 8 million people died from various kinds of cancers all over the world.Although traditional chemotherapeutic drugs are widely used in clinic, more than 50% of cancers are significantly resistant to traditional chemotherapeutic drugs.Tubulin targeting agents have been confirmed to be effective anti-cancer drugs in clinic.However, some anti-microtubule agents developed resistance after long-term use, such as paclitaxel and vinblastine.In recent years, it is reported that tubulin modulators targeting on the colchicine-binding site are extremely effective against multi-drug resistant cancer cells.In this article, different anti-microtubule agents targeting multi-drug resistant cancers are reviewed.
5.Study on chemical constitunts of sponge Agelas mauritiana from the South China Sea
Fengkai FANG ; Hua TANG ; Baoshu LIU ; Chunlin ZHUANG ; Peng SUN ; Wen ZHANG
Journal of Pharmaceutical Practice 2015;(3):242-245,274
Objective To investigate the chemical constituents of marine sponge A gelas mauritiana collected from the South China Sea .Methods The n-butanol extract of marine sponge A gelas mauritiana was separated and purified by repeated column chromatography on silica gel ,Sephadex LH-20 ,and reversed-phase high-performance liquid chromatography (RP-HPLC) .The chemical structures of those obtained compounds were determined on the basis of spectroscopic analysis and com-parison with reported data .The tumor cell growth inhibitory activity of these compounds towards human lung carcinoma cells A549 was tested .Results Eight compounds were isolated ,including agelasine A (1) ,agelasine B (2) ,epi-agelasine C (3) , (-)agelasine D (4) ,agelasine E (5) ,agelasine F (6) ,(-)ageloxime D (7) and aurantiamide acetate (8) .These compounds dis-played different level of tumor cell growth inhibitory activity towards cell A 549 in vitro .Compounds 1-3 showed significant ac-tivity towards cell A549 ,being similar to that of the positive control of adriamycin .Conclusion Compounds 1 ,2 ,4 ,5 ,6 ,8 were isolated for the first time from the sponge A gelas mauritiana .Cell A549 was selected for the first time for the activity evalua-tion of compounds 1~7 .Significant inhibition activity of compounds 2、3 may hold as a basis for further research .
6.Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years.
Chunlin ZHUANG ; Christophe PANNECOUQUE ; Erik DE CLERCQ ; Fener CHEN
Acta Pharmaceutica Sinica B 2020;10(6):961-978
Human immunodeficiency virus (HIV) is the primary infectious agent of acquired immunodeficiency syndrome (AIDS), and non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the cornerstone of HIV treatment. In the last 20 years, our medicinal chemistry group has made great strides in developing several distinct novel NNRTIs, including 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT), thio-dihydro-alkoxy-benzyl-oxopyrimidine (-DABO), diaryltriazine (DATA), diarylpyrimidine (DAPY) analogues, and their hybrid derivatives. Application of integrated modern medicinal strategies, including structure-based drug design, fragment-based optimization, scaffold/fragment hopping, molecular/fragment hybridization, and bioisosterism, led to the development of several highly potent analogues for further evaluations. In this paper, we review the development of NNRTIs in the last two decades using the above optimization strategies, including their structure-activity relationships, molecular modeling, and their binding modes with HIV-1 reverse transcriptase (RT). Future directions and perspectives on the design and associated challenges are also discussed.
7.Research progress on small molecule inhibitors of coronaviruses
Zhengguang YAO ; Zhibin WANG ; Chunnian XIA ; Chunlin ZHUANG
Journal of Pharmaceutical Practice 2020;38(5):385-397
Coronavirus infection seriously threatens human health. There is no specific medication or vaccine so far. In recent years, domestic and foreign researchers have developed a variety of small-molecule inhibitors against the ligand S protein, RdRp, PLpro and 3CLpro of three highly pathogenic coronavirus, SARS-CoV,MERS-CoV,SARS-CoV-2. This article reviews the characteristics of these coronaviruses, action targets, small molecule inhibitors, and structure-activity relationships.
8.Cytotoxicity study on FC58, an indole-chalcone, against multi-drug resistant leukemia cells
Jiawei DAI ; Saijian SHI ; Aiwei SONG ; Zhibin WANG ; Chunlin ZHUANG ; Chunnian XIA
Journal of Pharmaceutical Practice 2021;39(4):305-308
Objective To synthesize and investigate cytotoxicity of an indole-chalcone derivative FC58. Methods The target compound was synthesized through the Aldol condensation with 1-(3,4,5-trimethoxyphenyl)ethan-1-one and 1H-indole-3-carbaldehyde. The Cell Titer-Blue method was used to determine in vitro cytotoxicity. The cell cycle experiment was performed to analyze the action characteristics of FC58. Results FC58 exhibited high cytotoxicity against various leukemia cells and resulted in G2/M phase arrest. It showed stronger drug resistant index than traditional tubulin inhibitors such as paclitaxel, vinblastine and doxorubicin. Conclusion FC58 represents a promising lead compound for multi-drug resistant leukemia.
9.Research progresses on the main active components in Ningxia Sophora alopecuroides and the therapeutic activities for liver diseases
Danni QUAN ; Yue XU ; Zhuo QU ; Weiheng XU ; Wannian ZHANG ; Chunlin ZHUANG
Journal of Pharmaceutical Practice 2022;40(1):1-5
Sophora alopecuroides, a plant of the family Leguminosae, is one of the Daodi herbs in Ningxia. The active constituents of Sophora alopecuroides are abundant and complex, including alkaloids, flavonoids, volatile oils, steroids, polysaccharides, fatty acids and so on. In recent decades, a great number of domestic and overseas studies have been carried out on Sophora alopecuroides alkaloids, which have anti-hepatitis, anti-liver fibrosis, anti-cirrhosis, anti-liver failure and anti-liver cancer and other pharmacological effects. Clinically, Matrine-related drugs are used to treat hepatitis B virus infection and other diseases. This review aims to summarize the main active ingredients of Sophora alopecuroides, mainly focusing on the research progress in their treatment activities for liver diseases.
10.Ligand-based substituent-anchoring design of selective receptor-interacting protein kinase 1 necroptosis inhibitors for ulcerative colitis therapy.
Jing ZHU ; Meng XIN ; Congcong XU ; Yuan HE ; Wannian ZHANG ; Zhibin WANG ; Chunlin ZHUANG
Acta Pharmaceutica Sinica B 2021;11(10):3193-3205
Receptor-interacting protein (RIP) kinase 1 is involved in immune-mediated inflammatory diseases including ulcerative colitis (UC) by regulating necroptosis and inflammation. Our group previously identified TAK-632 (