1.Universal strategies and methodologies in broad-spectrum antiviral drug discovery
Shu-jing XU ; Dang DING ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2022;57(5):1289-1300
Virus infection is a serious threat to human health and social development. The increase in pandemics caused by emerging and re-emerging viruses highlights the urgent need for broad-spectrum antivirals. In this perspective, we highlight recent case studies and summarize the universal strategies and methodologies in broad-spectrum antiviral drug discovery from common targets, common steps in viral life cycle, universal strategies, and broad-spectrum molecules, hoping to provide valuable guidance for the current and future development of antiviral drugs.
2.Integrated medicinal chemistry: new modalities and methodologies in drug discovery
Shu-jing XU ; Dang DING ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2022;57(10):2889-2901
New drug research and development is a technology-intensive industry with high investment, high cycle and high risk. In recent years, with the rapid development of modern disciplines such as omics technology, bioinformatics, high-throughput and high-content screening, and artificial intelligence, the research and development of small-molecule drugs has presented a new paradigm characterized by "integrated medicinal chemistry". This review summarizes new enabling drug discovery technologies, the emergence of new subfields formed through integration innovations and practical chemistry toolbox in the field of medicinal chemistry.
3.Application of saw palmetto fruit extract in the treatment of prostate diseases.
Xu-xin ZHAN ; Xue-jun SHANG ; Yu-feng HUANG
National Journal of Andrology 2015;21(9):841-846
Saw palmetto fruit extract (SPE), as a herbal product, is widely used for the treatment of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS). Recent studies show that SPE also has some therapeutic effects on chronic prostatitis, prostate cancer, sexual dysfunction, and so on. This article presents an overview on the application of SPE in the treatment of BPH, prostate cancer, and chronic prostatitis/chronic pelvic pain syndrome, with a discussion on its action mechanisms.
Chronic Disease
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Fruit
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chemistry
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Humans
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Lower Urinary Tract Symptoms
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drug therapy
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Male
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Pelvic Pain
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drug therapy
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Plant Extracts
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therapeutic use
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Prostatic Diseases
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drug therapy
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Prostatic Hyperplasia
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drug therapy
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Prostatic Neoplasms
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drug therapy
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Prostatitis
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drug therapy
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Syndrome
4.Bioinorganic chemistry strategies in antiviral drug discovery
Shu-jing XU ; Xu-jie ZHANG ; Dang DING ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2022;57(3):576-592
Over the course of human civilization, viral infections have been a part of human life and still represent one of the heaviest burdens for human and society, with a huge devastating socioeconomic impact. Inorganic and bioinorganic chemistry have made important contributions to medical science and human health in the past half century. In this paper, we selected the representative cases in recent years, and reviewed the research progress of antiviral drug discovery from the perspective of bioinorganic chemistry.
5.Influencing factors of mental health of medical students in China.
Fan, YANG ; Heng, MENG ; Hui, CHEN ; Xin-Hao, XU ; Zhuo, LIU ; Ai, LUO ; Zhan-Chun, FENG
Journal of Huazhong University of Science and Technology (Medical Sciences) 2014;34(3):443-9
This study investigated the mental health status of medical students in China, and analyzed the influencing factors in order to provide evidence for mental health education for medical students. A stratified cluster sampling method was used to recruit medical students from Huazhong University of Science and Technology, China. The questionnaire survey on general information and Symptom Checklist 90 (SCL-90) were used for investigation and analysis. The results showed among the 1137 valid questionnaires, 278 (24.45%) participants had SCL-90 score ≥ 160. The top three mental problems of medical students were obsessive-compulsive disorder, interpersonal sensitivity and depression in terms of the factor score ≥ 2.5 and the number of participants who reflected on the diseases. The third-year medical students had the worst mental health status, and fifth-year medical students had the best mental health status. Students from rural area had more psychological problems than those from urban area; furthermore, students with high professional satisfaction, those who were the single child of the family, non-poor students, and those whose parents had high education level had better mental health status. It was concluded that the mental health of medical students is not optimistic in China. Medical students have some mental health problems of different degrees. Factors that influence the mental health of medical students include academic pressure, professional satisfaction level and family environment.
6.Research progress of natural products for the treatment of hyperuricemia and gout
Zhi-jiao ZHANG ; Rui-peng LIANG ; Tong ZHAO ; Shu-jing XU ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2022;57(6):1679-1688
Although current synthetic anti-gout drugs have significant therapeutic effects in reducing serum uric acid levels, they have serious side effects such as allergic reactions and liver and kidney damage. Natural products with a wide range of uric acid-lowering and high safety have played a critical role in anti-gout drug discovery and development. This paper reviews the natural products with uric acid-lowering or anti-gout pharmacological effects and the investigation on their mechanisms of action, to provide information for drug discovery and development.
7.Recent advances of antiviral drugs based on multispecific binding strategy
Yang ZHOU ; Shu-jing XU ; Dang DING ; Shuo WANG ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2023;58(8):2203-2217
To address the continuous emergence of drug-resistant strains of viruses and the outbreaks of novel virus infections, developing new antiviral drugs based on novel strategies has become an important and urgent research topic. In recent years, the rapidly developing multi-specific binding strategy has become a focus and been widely applied in antiviral. This review summarizes the recent progress of the multi-specific binding strategy in the antiviral field from the perspective of medicinal chemistry and discusses existing challenges as well as future opportunities for antiviral drug discovery.
8.In vivo study on the body motion during the Shi's cervical reduction technique with 3D motion capture.
Hui-hao WANG ; Min ZHANG ; Wen-xin NIU ; Xu-zhe SHEN ; Hong-sheng ZHAN
China Journal of Orthopaedics and Traumatology 2015;28(10):940-944
OBJECTIVEThe clinical effect of the Shi's cervical reduction technique for cervical spondylosis and related disorders has confirmed, however, there were few studies on the body motion during manipulation in vivo study. This study is to summary the law of motion and the motion characteristics of the right operation shoulder, elbow, knee and ankle joints by data acquisition and analysis with the 3D motion capture system.
METHODSThe markers were pasted on the head, trunk, left and right acromion, elbow joint, wrist joint inner side and the outer side of the inner and the outer side and the lateral upper arm, forearm lateral, anterior superior iliac spine, posterior superior iliac spine, trochanter, femoral and tibial tubercle, inner and outer side of knee, ankle, fibular head, medial and lateral in first, 2,5 metatarsal head, heel and dual lateral thigh the calf, lateral tibia of one manipulation practioner, and the subject accepted a complete cycle of cervical "Jin Chu Cao and Gu Cuo Feng" manipulation which was repeated five times. The movement trajectory of the practioner's four markers of operation joints were captured, recorded, calculated and analyzed.
RESULTSThe movement trajectories of four joints were consistent, while the elbow joint had the biggest discrete degree. The 3D activities of the shoulder and elbow were more obvious than other two joints, but the degree of flexion and extension in the knee was significantly greater than the rotation and lateral bending.
CONCLUSIONThe flexibility of upper limb joint and stability of lower limb joint are the important guarantees for the Shi's cervical reduction technique, and the right knee facilitated the exerting force of upper limb by the flexion and extension activities. The 3D model built by the motion capture system would provide a new idea for manipulation teaching and further basic biomechanical research.
Adult ; Biomechanical Phenomena ; Cervical Vertebrae ; surgery ; Humans ; Male ; Manipulation, Orthopedic ; methods ; Movement
9.Mechanism Underlying the Role of HIF-1αduring Hepatocyte Apoptosis in Intermittent Hypoxia with Pulmonary Emphysema in Rats
Jingyan ZHAN ; Huaiyong CHEN ; Qi WU ; Xin SUN ; Jing FENG ; Xue LI ; Long XU ; Cuiping BAO
Tianjin Medical Journal 2014;(2):156-159
Objective To investigate the effect of intermittent hypoxia (IH) with pulmonary emphysema on the ex-pression of hypoxia inducible factor-1α(HIF-1α),Bax and Bcl-2, and the mechanism underlying the role of HIF-1αin he-patocyte apoptosis thereof. Methods Sixty rats were randomly divided into four groups: normal control group, rats were treated normally;IH group, rats were treated by 30 s nitrogen and then 90 s air, and rats were treated by from 9:00-17:00 daily;pulmonary emphysema group, rats were treated by smudging for half an hour, twice a day (8:00 and 18:00);IH with pul-monary emphysema group, rats were treated by 30 s nitrogen and then 90 s air from 9:00-17:00 daily. After exposure four-teen weeks, rats were killed. qRT-PCR assay was conducted to detect the expression of HIF-1α mRNA, Bax mRNA and Bcl-2 mRNA in live tissues. Results The expressions of HIF-1αmRNA, Bax mRNA and Bax/Bcl-2 were significantly higher in IH with pulmonary emphysema group than those in control group,IH group and pulmonary emphysema group (P<0.05). The expression level of Bcl-2 mRNA was significantly lower in IH with pulmonary emphysema group than that of con-trol group and pulmonary emphysema group (P < 0.05), but no significant difference compared with that of IH group (P >0.05). The levels of HIF-1αand Bax were positively correlated with the level of Bax/Bcl-2 (r=0.732 and 0.699),but the lev-els of HIF-1αand Bax were negatively correlated with the level of Bcl-2 (r=-0.705). Conclusion The expression levels of HIF-1αmRNA, Bax mRNA and Bcl-2 mRNA were over-regulated in hepatocytes induced by intermittent hypoxia with pul-monary emphysema. The HIF-1αexpression was correlated with Bax and Bcl-2, suggesting that HIF-1αmay promote the hepatocyte apoptosis through transcriptional co-activators, Bax and Bcl-2.