期刊：
International Journal of Surgery,2023年109(10):2886-2891 ISSN：1743-9191
作者机构：
[Zou, Ming-Xiang MD, PhD] Department of Spine Surgery, The First Affiliated Hospital, Hengyang medical school, University of South China, Hengyang, China;Department of Pharmacy, The First Affiliated Hospital, Hengyang Medical School, University of South China, Hengyang, China;[Niu, Hua-Qing MS] Department of Ophthalmology, The Second Affiliated Hospital of Zhengzhou University, Zhengzhou, China;[Zheng, Bo-Yv MS] Department of Orthopedics Surgery, General Hospital of the Central Theater Command, Wuhan, China;[Zheng, Bo-Wen MD, PhD] Department of Musculoskeletal Tumor Center, People’s Hospital, Peking University, Beijing Key Laboratory of Musculoskeletal Tumor. Beijing, China
摘要：
Background: ChatGPT, powered by the GPT model and Transformer architecture, has demonstrated remarkable performance in the domains of medicine and healthcare, providing customized and informative responses. In our study, we investigated the potential of ChatGPT in the field of neurosurgery, focusing on its applications at the patient, neurosurgery student/resident, and neurosurgeon levels. Method: The authors conducted inquiries with ChatGPT from the viewpoints of patients, neurosurgery students/residents, and neurosurgeons, covering a range of topics, such as disease diagnosis, treatment options, prognosis, rehabilitation, and patient care. The authors also explored concepts related to neurosurgery, including fundamental principles and clinical aspects, as well as tools and techniques to enhance the skills of neurosurgery students/residents. Additionally, the authors examined disease-specific medical interventions and the decision-making processes involved in clinical practice. Results: The authors received individual responses from ChatGPT, but they tended to be shallow and repetitive, lacking depth and personalization. Furthermore, ChatGPT may struggle to discern a patient's emotional state, hindering the establishment of rapport and the delivery of appropriate care. The language used in the medical field is influenced by technical and cultural factors, and biases in the training data can result in skewed or inaccurate responses. Additionally, ChatGPT's limitations include the inability to conduct physical examinations or interpret diagnostic images, potentially overlooking complex details and individual nuances in each patient's case. Moreover, its absence in the surgical setting limits its practical utility. Conclusion: Although ChatGPT is a powerful language model, it cannot substitute for the expertise and experience of trained medical professionals. It lacks the capability to perform physical examinations, make diagnoses, administer treatments, establish trust, provide emotional support, and assist in the recovery process. Moreover, the implementation of Artificial Intelligence in healthcare necessitates careful consideration of legal and ethical concerns. While recognizing the potential of ChatGPT, additional training with comprehensive data is necessary to fully maximize its capabilities.
期刊：
International Journal of Molecular Sciences,2023年24(8):7013- ISSN：1422-0067
通讯作者：
Yimou Wu<&wdkj&>Shuzhi Wang
作者机构：
[Lu, Chunxue; Wu, Yimou; Lei, Aihua; Wang, Jiewen; Zheng, Kang; Jin, Yingqi; Wang, Chuan; Wang, Shuzhi] Univ South China, Inst Pathogen Biol, Hengyang Med Coll, Sch Basic Med, Hengyang 421001, Peoples R China.;[Lu, Chunxue; Wu, Yimou; Lei, Aihua; Wang, Jiewen; Zheng, Kang; Jin, Yingqi; Wang, Chuan; Wang, Shuzhi] Univ South China, Hunan Prov Key Lab Special Pathogens Prevent & Con, Hengyang 421001, Peoples R China.;[Zheng, Kang] Hengyang Cent Hosp, Dept Clin Lab, Hengyang 421001, Peoples R China.;[Wang, Shuzhi] Univ South China, Hengyang Med Coll, Sch Pharmaceut Sci, Dept Pharmacol, Hengyang 421001, Peoples R China.
通讯机构：
[Yimou Wu; Shuzhi Wang] A;Authors to whom correspondence should be addressed.<&wdkj&>Hunan Provincial Key Laboratory for Special Pathogens Prevention and Control, University of South China, Hengyang 421001, China<&wdkj&>Institute of Pathogenic Biology, School of Basic Medicine, Hengyang Medical College, University of South China, Hengyang 421001, China<&wdkj&>Authors to whom correspondence should be addressed.<&wdkj&>Hunan Provincial Key Laboratory for Special Pathogens Prevention and Control, University of South China, Hengyang 421001, China<&wdkj&>Institute of Pathogenic Biology, School of Basic Medicine, Hengyang Medical College, University of South China, Hengyang 421001, China<&wdkj&>Department of Pharmacology, School of Pharmaceutical Science, Hengyang Medical College, University of South China, Hengyang 421001, China
摘要：
Chlamydia psittaci (C. psittaci), a zoonotic pathogen, poses a potential threat to public health security and the development of animal husbandry. Vaccine-based preventative measures for infectious diseases have a promising landscape. DNA vaccines, with many advantages, have become one of the dominant candidate strategies in preventing and controlling the chlamydial infection. Our previous study showed that CPSIT_p7 protein is an effective candidate for a vaccine against C. psittaci. Thus, this study evaluated the protective immunity of pcDNA3.1(+)/CPSIT_p7 against C. psittaci infection in BALB/c mice. We found that pcDNA3.1(+)/CPSIT_p7 can induce strong humoral and cellular immune responses. The IFN-gamma and IL-6 levels in the infected lungs of mice immunized with pcDNA3.1(+)/CPSIT_p7 reduced substantially. In addition, the pcDNA3.1(+)/CPSIT_p7 vaccine diminished pulmonary pathological lesions and reduced the C. psittaci load in the lungs of infected mice. It is worth noting that pcDNA3.1(+)/CPSIT_p7 suppressed C. psittaci dissemination in BALB/c mice. In a word, these results demonstrate that the pcDNA3.1(+)/CPSIT_p7 DNA vaccine has good immunogenicity and immunity protection effectiveness against C. psittaci infection in BALB/c mice, especially pulmonary infection, and provides essential practical experience and insights for the development of a DNA vaccine against chlamydial infection.
通讯机构：
[Li-Chen Gao] S;School of Pharmacy, Department of Pharmacy, Phase I Clinical Trial Centre, the Affiliated Changsha Central Hospital, Hengyang Medical School, University of South China, Hengyang, China<&wdkj&>Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Changsha, China
摘要：
Ferrous ion (Fe2+) is a crucial metal ion in the body and participates in the diseases related to oxidation and reduction. Golgi apparatus is the main subcellular organelle of Fe2+ transport in cells, and the stability of its structure is related to the Fe2+ at an appropriate concentration. In this work, a turn-on type Golgi-targeting fluorescent chemosensor Gol-Cou-Fe2+ was rationally designed for sensitive and selective detection of Fe2+. Gol-Cou-Fe2+ showed excellent capacity of detecting exogenous and endogenous Fe2+ in HUVEC and HepG2 cells. It was used to capture the up-regulated Fe2+ level during the hypoxia. Moreover, the fluorescence of sensor was enhanced over time under Golgi stress combining with the reduce of Golgi matrix protein GM130. However, elimination of Fe2+ or addition of nitric oxide (NO) would restore the fluorescence intensity of Gol-Cou-Fe2+ and the expression of GM130 in HUVEC. Thus, development of chemosensor Gol-Cou-Fe2+ provides a new window for tracking Golgi Fe2+ and elucidating Golgi stress-related diseases.
作者机构：
[Chen, Yuping; Wu, Meichun; Chen, YP] Univ South China, Hengyang Med Sch, Hengyang 410001, Hunan, Peoples R China.;[Wu, Meichun] Univ South China, Sch Nursing, Hengyang 410001, Hunan, Peoples R China.;[Chen, Yuping; Xun, Min; Chen, YP] Univ South China, Inst Pharm & Pharmacol, Sch Pharmaceut Sci, Hengyang 410001, Hunan, Peoples R China.
通讯机构：
[Chen, YP ] U;Univ South China, Hengyang Med Sch, Hengyang 410001, Hunan, Peoples R China.;Univ South China, Inst Pharm & Pharmacol, Sch Pharmaceut Sci, Hengyang 410001, Hunan, Peoples R China.
关键词：
biodegradable metal stents;vascular smooth muscle cell;stent implantation;vascular microenvironment;atherosclerosis;restenosis
摘要：
Iron-, magnesium-, or zinc-based metal vessel stents support vessel expansion at the period early after implantation and degrade away after vascular reconstruction, eliminating the side effects due to the long stay of stent implants in the body and the risks of restenosis and neoatherosclerosis. However, emerging evidence has indicated that their degradation alters the vascular microenvironment and induces adaptive responses of surrounding vessel cells, especially vascular smooth muscle cells (VSMCs). VSMCs are highly flexible cells that actively alter their phenotype in response to the stenting, similarly to what they do during all stages of atherosclerosis pathology, which significantly influences stent performance. This Review discusses how biodegradable metal stents modify vascular conditions and how VSMCs respond to various chemical, biological, and physical signals attributable to stent implantation. The focus is placed on the phenotypic adaptation of VSMCs and the clinical complications, which highlight the importance of VSMC transformation in future stent design.
摘要：
The dysregulation of nuclear factor erythroid 2-related factor 2 (Nrf2) and/or solute carrier family 7 member 11 (SLC7A11) is believed to contribute to ferroptosis in the hearts suffered ischemia/reperfusion (I/R), but the mechanisms behind the dysregulation of them are not fully elucidated. Mucosa associated lymphoid tissue lymphoma translocation gene 1 (MALT1) can function as a paracaspase to cleave specified substrates and it is predicted to interact with Nrf2. This study aims to explore whether targeting MALT1 can reduce I/R-induced ferroptosis via enhancing the Nrf2/SLC7A11 pathway. The SD rat hearts were subjected to 1h-ischemia plus 3h-reperfusion to establish the I/R injury model, which showed myocardial injuries (increase in infarct size and creatine kinase release) and up-regulation of MALT1 while downregulation of Nrf2 and SLC7A11 concomitant with the increased ferroptosis, reflecting by an increase in glutathione peroxidase 4 (GPX4) level while decreases in the levels of acyl-CoA synthetase long chain family member 4 (ACSL4), total iron, Fe(2+) and lipid peroxidation (LPO); these phenomena were reversed in the presence of MI-2, a specific inhibitor of MALT1. Consistently, similar results were achieved in the cultured cardiomyocytes subjected to 8h-hypoxia plus 12h-reoxygenation. Furthermore, micafungin, an antifungal drug, could also exert beneficial effect on mitigating myocardial I/R injury via inhibition of MALT1. Based on these observations, we conclud that inhibition of MALT1 can reduce I/R-induced myocardial ferroptosis through enhancing the Nrf2/SLC7A11 pathway; and MALT1 may be used as a potential target to seek novel or existing drugs (such as micafungin) for treating myocardial infarction.
通讯机构：
[Li-Chen Gao] S;School of Pharmacy, Department of Pharmacy, Phase Ⅰ Clinical Trial Centre, Changsha Central Hospital Affiliated to University of South China, University of South China, Hengyang, Hunan, China<&wdkj&>Corresponding Author:<&wdkj&>Li-Chen Gao, School of Pharmacy, Department of Pharmacy, Phase Ⅰ Clinical Trial Centre, Changsha Central Hospital Affiliated to University of South China, University of South China, Hengyang, Hunan, 421001, China
摘要：
Cis-regulatory elements are important molecular switches in controlling gene expression and are regarded as determinant hubs in the transcriptional regulatory network. Collection and processing of large-scale cis-regulatory data are urgent to decipher the potential mechanisms of cardiovascular diseases from a cis-regulatory element aspect. Here, we developed a novel web server, Cis-Cardio, which aims to document a large number of available cardiovascular-related cis-regulatory data and to provide analysis for unveiling the comprehensive mechanisms at a cis-regulation level. The current version of Cis-Cardio catalogs a total of 45,382,361 genomic regions from 1,013 human and mouse epigenetic datasets, including ATAC-seq, DNase-seq, Histone ChIP-seq, TF/TcoF ChIP-seq, RNA polymerase ChIP-seq, and Cohesin ChIP-seq. Importantly, Cis-Cardio provides six analysis tools, including region overlap analysis,element upstream/downstream analysis, transcription regulator enrichment analysis, variant interpretation, andprotein-protein interaction-based co-regulatory analysis. Additionally, Cis-Cardio provides detailed and abundant (epi-) genetic annotations in cis-regulatory regions, such as super-enhancers, enhancers, transcription factor binding sites (TFBSs), methylation sites, common SNPs, risk SNPs, expression quantitative trait loci (eQTLs), motifs,DNase I hypersensitive sites (DHSs), and 3D chromatin interactions. In summary, Cis-Cardio is a valuable resourcefor elucidating and analyzing regulatory cues of cardiovascular-specific cis-regulatory elements. The platform is freely available at http://www.licpathway.net/Cis-Cardio/index.html.
摘要：
Nasopharyngeal carcinoma (NPC) is a highly recurrent and metastatic malignant tumor affecting a large number of individuals in southern China. Traditional Chinese herbal medicine has been found to be a rich source of natural compounds with mild therapeutic effects and minimal side effects, making them increasingly popular for treating various diseases. Trifolirhizin, a natural flavonoid derived from legu-minous plants, has gained significant attention for its therapeutic potential. In this study, we confirmed that trifolirhizin could effectively inhibit the proliferation, migration and invasion of nasopharyngeal carcinoma 6-10B and HK1 cells. Furthermore, our findings demonstrated that trifolirhizin achieves this by suppressing the PI3K/Akt signaling pathway. The findings of the present study provides a valuable perspective on the potential therapeutic applications of trifolirhizin for the treatment of nasopharyngeal carcinoma.(c) 2023 Elsevier Inc. All rights reserved.
作者机构：
[Liu, Ying; Yang, Ke; He, Longwei; Wang, Peipei; Li, Songjiao] Univ South China, Hengyang Med Sch, Canc Res Inst, Hunan Prov Cooperat Innovat Ctr Mol Target New Dru, Hengyang 421001, Peoples R China.;[Cheng, Dan] Univ South China, Affiliated Nanhua Hosp, Hengyang Med Sch, Clin Res Inst, Hengyang, Peoples R China.
通讯机构：
[Dan Cheng] C;[Longwei He] H;Clinical Research Institute, The Affiliated Nanhua Hospital, Hengyang Medical School, University of South China, Hengyang, China<&wdkj&>Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, Cancer Research Institute, Department of Pharmacy and Pharmacology, Hengyang Medical School, University of South China, Hengyang, 421001, PR China
作者机构：
[Zhang, Taolan; Hu, Haihong; Zhan, Wendi; Zhang, TL; Zhu, HongXia] Univ South China, Affiliated Hosp 1, Hengyang Med Sch, Dept Pharm, Hengyang 421000, Hunan, Peoples R China.;[Zhang, Taolan; Yang, Xiaoyan; Hu, Haihong; Zhan, Wendi; Li, Zhicheng; Zhang, TL; Wang, Hanbin; Zhu, HongXia] Univ South China, Hengyang Med Coll, Sch Pharm, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;[Zhang, Taolan; Zhang, TL] Univ South China, Affiliated Hosp 1, Hengyang Med Sch, Chinese Tradit Med CTM Res Platform Major Epidem T, Hengyang 421000, Hunan, Peoples R China.
通讯机构：
[Zhang, TL ] U;Univ South China, Affiliated Hosp 1, Hengyang Med Sch, Dept Pharm, Hengyang 421000, Hunan, Peoples R China.;Univ South China, Hengyang Med Coll, Sch Pharm, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;Univ South China, Affiliated Hosp 1, Hengyang Med Sch, Chinese Tradit Med CTM Res Platform Major Epidem T, Hengyang 421000, Hunan, Peoples R China.
摘要：
Breast cancer and diabetes are significant health challenges, and effective treatments for both diseases are lacking. Proton pump inhibitors (PPIs) have demonstrated anticancer and hypoglycemic effects, but their mechanisms of action are not yet fully understood. We used the GeneCards and PharmMapper databases to identify therapeutic targets for diabetes, breast cancerand PPIs. We identified common targets and constructed a regulatory network of diseases and drugs using the STRING database and Cytoscape software. We also explored the binding between small molecule ligands and protein receptors using Discovery Studio software. We identified 33 shared targets for breast cancer, diabetes, and PPIs including lansoprazole, omeprazole, and pantoprazole, which play a critical role in fatty acid transport, insulin resistance, apoptosis, and cancer-related signaling pathways. Our findings demonstrated that PPIs had a strong affinity for AKT1 and MMP9. This study provides insights into the mechanisms of action of PPIs in breast cancer and diabetes and identifies AKT1 and MMP9 as critical targets for future drug development. Our findings highlight the potential of PPIs as a novel therapeutic approach for these challenging diseases.
期刊：
Drug Development Research,2023年84(3):406-422 ISSN：0272-4391
通讯作者：
Tang, G.;Wang, Z.
作者机构：
[Xie, Zhizhong; Zhao, Yin; Lei, Xiaoyong; Sun, Xueyan; Zhao, Jingduo; Tang, Guotao] Heng Yang Med Sch, Inst Pharm & Pharmacol, Hunan Prov Key Lab Tumor Microenvironm Respons Dru, Hengyang, Hunan, Peoples R China.;[Li, Yong; Liu, Xingyun] Univ South China, Nanhua Hosp, Hengyang Med Sch, Hengyang, Hunan, Peoples R China.;[Huang, Sheng] Jiuzhitang Co Ltd, Changsha, Hunan, Peoples R China.;[Wang, Zhe] Univ South China, Affiliated Hosp 2, Hengyang Med Sch, Dept Pharm, Hengyang, Hunan, Peoples R China.;[Wang, Zhe] Univ South China, Affiliated Hosp 2, Dept Pharm, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Zhe Wang] T;[Guotao Tang] I;The Second Affiliated Hospital, Department of Pharmacy, Hengyang Medical School, University of South China, Hunan, Hengyang, China<&wdkj&>Institute of Pharmacy and Pharmacology, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, HengYang Medicial School, Hengyang, Hunan, China
摘要：
Treatment of Klebsiella pneumoniae causing pyogenic infections is challenging. The clinical and molecular characteristics of Klebsiella pneumoniae causing pyogenic infections are poorly understood, and antibacterial treatment strategies are limited. We analyzed the clinical and molecular characteristics of K. pneumoniae from patients with pyogenic infections and used time-kill assays to reveal the bactericidal kinetics of antimicrobial agents against hypervirulent K. pneumoniae (hvKp). A total of 54 K. pneumoniae isolates were included, comprising 33 hvKp and 21 classic K. pneumoniae (cKp) isolates, and the hvKp and cKp isolates were identified using five genes (iroB, iucA, rmpA, rmpA2, and peg-344) that have been applied as hvKp strain markers. The median age of all cases was 54 years (25th and 75th percentiles, 50.5 to 70), 62.96% of individuals had diabetes, and 22.22% of isolates were sourced from individuals without underlying disease. The ratios of white blood cells/procalcitonin and C-reactive protein/procalcitonin were potential clinical markers for the identification of suppurative infection caused by hvKp and cKp. The 54 K. pneumoniae isolates were classified into 8 sequence type 11 (ST11) and 46 non-ST11 strains. ST11 strains carrying multiple drug resistance genes have a multidrug resistance phenotype, while non-ST11 strains carrying only intrinsic resistance genes are generally susceptible to antibiotics. Bactericidal kinetics revealed that hvKp isolates were not easily killed by antimicrobials at susceptible breakpoint concentrations compared with cKp. Given the varied clinical and molecular features and the catastrophic pathogenicity of K. pneumoniae, it is critical to determine the characteristics of such isolates for optimal management and effective treatment of K. pneumoniae causing pyogenic infections.IMPORTANCE Klebsiella pneumoniae may cause pyogenic infections, which are potentially life-threatening and bring great challenges for clinical management. However, the clinical and molecular characteristics of K. pneumoniae are poorly understood, and effective antibacterial treatment strategies are limited. We analyzed the clinical and molecular features of 54 isolates from patients with various pyogenic infections. We found that most patients with pyogenic infections had underlying diseases, such as diabetes. The ratio of white blood cells to procalcitonin and the ratio of C-reactive protein to procalcitonin were potential clinical markers for differentiating hypervirulent K. pneumoniae strains from classical K. pneumoniae strains that cause pyogenic infections. K. pneumoniae isolates of ST11 were generally more resistant to antibiotics than non-ST11 isolates. Most importantly, hypervirulent K. pneumoniae strains were more tolerant to antibiotics than classic K. pneumoniae isolates. Klebsiella pneumoniae may cause pyogenic infections, which are potentially life-threatening and bring great challenges for clinical management. However, the clinical and molecular characteristics of K. pneumoniae are poorly understood, and effective antibacterial treatment strategies are limited.
期刊：
CURRENT MOLECULAR MEDICINE,2023年23(7):668-677 ISSN：1566-5240
通讯作者：
Long, Shuanglian;Mo, Zhongcheng;He, WG
作者机构：
[Luo, Min; Liu, Jiang; He, Weiguo; Mo, Zhongcheng; Gui, Zihao; Long, Shuanglian] Univ South China, Clin Anat & Reprod Med Applicat Inst, Hengyang Med Sch, Hengyang 421001, Peoples R China.;[Li, Tangluo] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dru, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Peng, Mindan; Liu, Jiang] Univ South China, Hunan Prov Innovat Training Base Med Postgrad, Yueyang 416000, Hunan, Peoples R China.;[Peng, Mindan; Liu, Jiang] Yueyang Women & Childrens Med Ctr, Yueyang 416000, Hunan, Peoples R China.;[Mo, Zhongcheng] Guilin Med Univ, Guangxi Key Lab Diabet Syst Med, Guilin 541000, Guangxi, Peoples R China.
通讯机构：
[He, WG ; Mo, ZC; Long, SL] U;Univ South China, Clin Anat & Reprod Med Applicat Inst, Hengyang Med Sch, Hengyang 421001, Peoples R China.
关键词：
CPP;Central precocious puberty;GnRH.;MKRN3;Makorin RING finger protein 3;Puberty initiation
摘要：
Puberty is initiated from the continuous and growing pulsatile secretion of gonadotropin-releasing hormone (GnRH) in the hypothalamus and then the activation of the hypothalamic-pituitary-gonadal (HPG) axis. Numerous factors involve pubertal initiation, whose abnormality may come from the dysfunction of these regulators. Makorin RING finger protein 3 (MKRN3) inhibits the secretion of GnRH and plays indispensable roles during the development of pubertal onset, and mutations of MKRN3 showed the commonest genetic cause of central precocious puberty (CPP). Recently, growing studies have revealed the functional mechanisms of MKRN3 in the pubertal initiation and the occurrence of CPP. In this review, we mainly summarized the research advances on the roles of MKRN3 in the development of pubertal onset and their underpinning mechanisms, contributing to a better understanding of the precise mechanisms of pubertal initiation and the pathogenesis of CPP.
关键词：
Breast cancer;Lead compounds;Multidrug resistance
摘要：
Chemotherapy is the mainstay in the treatment of breast cancer. However, many drugs that are commonly used in clinical practice have a high incidence of side effects and multidrug resistance (MDR), which is mainly caused by overexpression of drug transporters and related enzymes in breast cancer cells. In recent years, researchers have been working hard to find newer and safer drugs to overcome MDR in breast cancer. In this review, we provide the molecule mechanism of MDR in breast cancer, categorize potential lead compounds that inhibit single or multiple drug transporter proteins, as well as related enzymes. Additionally, we have summarized the structure-activity relationship (SAR) based on potential breast cancer MDR modulators with lower side effects. The development of novel approaches to suppress MDR is also addressed. These lead compounds hold great promise for exploring effective chemotherapy agents to overcome MDR, providing opportunities for curing breast cancer in the future.
作者机构：
[Zhang, Jing; Xie, Zhizhong; Lei, Xiaoyong; Ouyang, Chenglin; Tang, Guotao] Univ South China, Inst Pharm & Pharmacol, Hengyang Medicial Sch, Hunan Prov Key Lab Tumor Microenvironm Respons Dru, Hengyang 421001, Hunan, Peoples R China.;[Wang, Zhe] Univ South China, Affiliated Hosp 2, Hengyang Med Sch, Dept Pharm, Hengyang 421001, Hunan, Peoples R China.;[Li, Yong; Liu, Xingyun] Univ South China, Affiliated Nanhua Hosp, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.;[Huang, Sheng] Jiuzhitang Co Ltd, Changsha 410007, Hunan, Peoples R China.
通讯机构：
[Zhe Wang] T;[Guotao Tang] I;The Second Affiliated Hospital, Department of Pharmacy, Hengyang Medical School, University of South China, Hengyang 421001, Hunan, China<&wdkj&>Institute of Pharmacy and Pharmacology, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hengyang Medicial School, University of South China, Hengyang, Hunan 421001, China
摘要：
Generally, hypoxia-inducible factor-1 alpha (HIF-1 alpha) is highly expressed in solid tumors, it plays a key role in the occurrence and development of tumors, hindering cancer treatment in various ways. The antitumor activity and pharmacological mechanism of YC-1 [3-(5 '-hydroxymethyl-2 '-furyl)-1-benzyl indazole], an HIF-1 alpha inhibitor, and the design and synthesis of its derivatives have attracted tremendous attention in the field of antitumor research. YC-1 is a potential drug candidate and a lead compound for tumor therapy. Hence, the multifaceted mechanism of action of YC-1 and the structure activity relationship (SAR) of its derivatives are important factors to be considered for the development of HIF-1 alpha inhibitors. Therefore, this review aimed to provide a comprehensive overview of the various antitumor mechanisms of YC-1 in antitumor research and an in-depth summary of the SAR for the development of its derivatives. A full understanding and discussion of these aspects are expected to provide potential ideas for developing novel HIF-1 alpha inhibitors and antitumor drugs belonging to the YC-1 class. The review also highlighted the application prospects of the YC-1 class of potential antitumor candidates, and provided some unique insights about these antitumor agents.
