A bibliometric analysis of the top 100 most-cited articles on keratoconus.

PURPOSE: To explore the characteristics of the top 100 most-cited articles on keratoconus research. METHODS: The Web of Science database was searched to identify papers published from 1950 to 2020. A bibliometric analysis of the top 100 most-cited articles was conducted in the current study. The Kruskal-Wallis test was conducted to test the citation differences between basic research, clinical research, and reviews. The Spearman correlation analysis was used to investigate the association between citations and publication year. The VOSviewer software was used to create networks of co-authorship and keywords map. RESULTS: The median values of the number of citations, citations/year since publication, and citations since 2013 were 186.5, 13.90, and 11, respectively. A total of 79% of articles were clinical research. Reviews exhibited a higher value of citations/year since publication and citations since 2013 than basic research (all P < 0.05). The number of publications, total number of citations, citations/year since publication and citations since 2013 on the top 100 most-cited articles list increased with an increase in the publication year in three article types (all P < 0.05). The Journal of Cataract and Refractive Surgery had the highest number of articles. There were 37 articles from the USA. Rabinowitz, YS was the most-cited author with the greatest total link strength. Extensive collaboration existed among the main core nodes containing "cross-linking," "refractive surgery," and "penetrating keratoplasty." CONCLUSIONS: The present study focused on the comprehensive analysis of the top 100 most-cited articles on keratoconus research, providing insight into keratoconus research developments over the past decades.

Advances in the Study of Hexokinase 2 (HK2) Inhibitors.

PURPOSE: The Warburg effect is an important metabolic feature of tumours, and hexokinase is the first ratelimiting enzyme of the glycolytic pathway during tumour metabolism. Among hexokinase subtypes, hexokinase 2 (HK2) is increasingly proving to be a key target for cancer treatment. This study presents the challenges and potential strategies for developing HK2 inhibitors by systematically summarising the characteristics of HK2 inhibitors reported in the literature and patents. METHODS: In this study, we analysed the HK2 active site using molecular docking and evaluated the structure, biochemical and physiological function, activity, and action mechanism of reported HK2 inhibitors using databases (Science, SCI Finder, CNKI, and WANFANG DATA). RESULTS: In total, 6 natural inhibitors of HK2, 9 synthetic inhibitors of HK2, and 3 compounds with patent-pending HK2 inhibitory effects were obtained by searching 87 articles. These inhibitors have poor efficacy and specificity when used alone and have numerous side effects; therefore, there is an urgent need to develop HK2 inhibitors with improved activity and high selectivity. CONCLUSION: HK2 has received much attention in anticancer drug development, but most previous studies have focused on elucidating the action mechanism of HK2 in carcinogenesis, whereas the development of its small-molecule inhibitors has rarely been reported. In this study, we analysed and illustrated the eutectic structure of small molecules with the catalytic structural domain of HK2 to develop highly selective and low-toxicity HK2 inhibitors.

Design, Synthesis and Biological Evaluation of Novel Catalpol Derivatives as Potential Pancreatic Cancer Inhibitors.

A series of C10-position imidazole-modified catalpol derivatives are specifically designed and synthesized for serving as potential pancreatic cancer inhibitors, which are characterized by 1 H NMR, 13 C NMR and high-resolution mass spectrometry (HRMS). They were evaluated by the 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) test on two human pancreatic cancer cells PANC-1, BxPC-3 and normal pancreatic cell HPDE6-C7, which showed the significant inhibitory effected on the growth of human pancreatic cancer cells of PANC-1 and BxPC-3, especially 91.6% efficacy on BxPC-3, and 73.1% on PANC-1. Simulation studies like molecular docking supported strong binding of vascular endothelial growth factor receptor 2 (VEGFR-2) protein tyrosine kinase (PDB ID: 4AGD), a target of pancreatic cancer. A novel imidazol-modified catalpol compound 3i with strong inhibitory effect on pancreatic cancer cells, which could potentially develop into anti-pancreatic cancer drug candidates in the future.

Study on the chemical reactivity difference of primary hydroxyl groups in iridoid glycosides.

Iridoid glycoside, which belongs to the polyhydroxy compound, is a kind of active ingredient of traditional Chinese medicine with a wide range of sources, and has many pharmacological effects such as anti-cancer, anti-inflammatory, anti-virus, hypoglycemic and so on. Its structure contains many hydroxyl groups, including two primary hydroxyl groups. The chemical reactivity of primary hydroxyl groups has very little difference, so it is very important to control the selectivity of hydroxyl groups under certain conditions. In this paper, the difference between the two primary hydroxyl groups in iridoid glycoside was calculated based on computer simulation and verified this result through designed experiments. This study will provide an important way for site-directed modification of hydroxyl in iridoid glycoside in the future.

Trends in research on corneal cross linking from 2001 to 2020: a bibliometric analysis.

CLINICAL RELEVANCE: The research status and hotspots in the field of corneal cross linking (CXL) can benefit clinicians, researchers and the general public. BACKGROUND: The purpose of this study was to map the publishing trend on CXL research and explore the research hotspots. METHODS: A bibliometric analysis was performed using the Web of Science Core Collection to investigate the publishing trend on CXL research. VOSviewer was used to build the knowledge map to visualise the number of annual publications, distribution of countries and institutions, international cooperation, author productivity, source journals and research hotspots in the field of CXL. RESULTS: A total of 2061 peer-reviewed articles on CXL research were collected from 2001 to 2020, and the annual research production increased over time. The United States was the country with the largest number of published articles, and the University of Zurich was the most active institution. Hafezi F published the largest number of articles on CXL, while Cornea was the journal with the largest number of studies on CXL. The most frequently cited references mainly focus on CXL in the treatment of keratoconus. The keywords were divided in 5 categories: 1) CXL mechanism, 2) ectasia diseases and refractive surgery, 3) corneal biomechanics, 4) efficacy evaluation, 5) treatment of infectious keratitis. CONCLUSION: The quantity and quality of articles on CXL were evaluated using bibliometric techniques by extracting the data from the Web of Science Core Collection. The research hotspots could provide insights on CXL research, providing valuable information for clinicians to perform research in this field and find potential partners.

Design, synthesis and anticancer activities evaluation of novel pyrazole modified catalpol derivatives.

Catalpol, a natural product mainly existed in plenty of Chinese traditional medicines, is an iridoid compound with the comprehensive effects on neuroprotective, anti-inflammatory, choleretic, hypoglycemic and anticancer. However, there are some disadvantages for catalpol such as a short half-life in vivo, low druggability, stingy binding efficiency to target proteins and so on. It is necessary to make structural modification and optimization which enhance its performance on disease treatments and clinic applications. Pyrazole compounds have been reported to have excellent anticancer activities. Based on the previous research foundation of our research group on iridoids and the anticancer activities of catalpol and pyrazole, a series of pyrazole modified catalpol compounds were synthesized by principle of drug combination for serving as potential cancer inhibitors. These derivatives are characterized by 1H NMR, 13C NMR and HRMS. The efficacy of anti-esophageal cancer and anti-pancreatic cancer activities were evaluated by the MTT assay on two esophageal cancer cells Eca-109 and EC-9706, and two pancreatic cancer cells PANC-1, BxPC-3 and normal pancreatic cell line HPDE6-C7, which showed that the compound 3e had strong inhibitory activity against esophageal cancer cells, this providing a theoretical basis for the discovery of catalpol-containing drugs.

A Bibliometric Analysis of 100 Most-Cited Articles on Corneal Cross-Linking.

Background: Highly cited papers are expected to have high-quality data that significantly contribute to the body of knowledge. The study aimed to evaluate the characters of the 100 most-cited articles on corneal cross-linking (CXL) through a bibliometric analysis. Materials and Methods: The Web of Science database was searched to identify papers published from 1950 to 2020. A bibliometric analysis of the top 100-cited articles was conducted in the current study. The citation differences between basic research, clinical research, and reviews were compared by Kruskal-Wallis test. The association between citations and publication year was evaluated by Spearman correlation analysis. The VOSviewer software was used to create networks of co-authorship and keywords map. Results: The median values of the number of citations, citations/year since publication, and citations since 2013 were 101, 9.5, and 11.92, respectively. A total of 61% of articles were clinical research. The citations since 2013 of clinical research were lower than basic research and the reviews (all p < 0.001). The publication year was positively correlated with the number of publications (r = 0.665, p = 0.013), and the total number of citations decreased for basic research (r = -0.447, p = 0.017), and clinical research (r = -0.433, p < 0.001). The J REFRACT SURG publishes the highest number of articles. The corresponding authors were predominantly from the Italy (N = 17), Germany (N = 16), and United States (N = 15). Spoerl Eberhard has the highest number of citations and total link strength with 15 articles. Extensive collaboration existed among the main core nodes containing "cross-linking (N = 45)," "riboflavin (N = 44)," and "ultraviolet A (UVA) (N = 42)." Conclusion: The present study focused on the comprehensive analysis of the top 100-cited articles on the CXL research, providing insight into research developments over the past decades.

A Hospital-Based Study on the Prevalence of Keratoconus in First-Degree Relatives of Patients with Keratoconus in Central China.

Purpose: The present study investigated the prevalence of keratoconus (KC) among first-degree relatives of KC patients in Central China. Methods: From July 2018 to March 2022, 661 first-degree relatives of 384 KC patients were included in the present study. Corneal tomography, uncorrected distance visual acuity, manifest refraction with corrected distance visual acuity, intraocular pressure, slit-lamp microscopy, and fundus examination were performed. The diagnosis of KC was based on the Belin/Ambrosio enhanced ectasia total deviation value (BAD-D value) on the Pentacam® system (Oculus GmbH). BAD-D value <1.6 was diagnosed as healthy, 1.6≤ BAD-D value <2.6 was diagnosed as suspected KC, and BAD-D value ≥2.6 was diagnosed as KC. Results: The present study included 337 (50.98%) female and 324 (49.02%) male subjects. The prevalence of KC and suspected KC in first-degree relatives was 8.77% (n = 58) and 29.05% (n = 192), respectively. The prevalence of KC was 9.70% among parents and 7.23% among siblings. Conclusions: The higher prevalence of KC among first-degree relatives of patients with KC suggests that first-degree relatives of KC are at high risk of developing KC.

Heritability of Corneal Parameters in Nuclear Families With Keratoconus.

Purpose: This study aimed to investigate the heritability of corneal parameters obtained by Pentacam in nuclear families with keratoconus (KC). Methods: A total of 82 patients with KC and their biological parents (n = 164) were recruited in the current study. All subjects underwent corneal tomography with Pentacam. Family units were analyzed to calculate the heritability of corneal parameters by linear mixed effects model using the R statistical software. Results: The pachymetry at apex, pupil, and thinnest point were all significantly heritable at 43.26%, 42.63%, and 43.09%, respectively. The heritability of flat meridian keratometry, steep meridian keratometry, and mean keratometry in the anterior surface were 10.36%, 9.05%, and 10.21%, respectively, and that of flat meridian keratometry, steep meridian keratometry, and mean keratometry in the posterior surface were 8.44%, 9.67%, and 9.06%, respectively. The posterior radius of curvature had higher heritability in comparison with anterior radius of curvature (19.16% vs. 14.37%). Moreover, among combined topometric indices, the heritability of index of vertical asymmetry was the highest (19.49%), and that of central keratoconus index was the lowest (6.64%). Conclusions: The present study demonstrated a substantial heritability of corneal parameters in nuclear families with KC. The pachymetric indices are heritable and may be suitable as KC endophenotypes, suggesting a necessity to discover the genes associated with corneal thickness in KC. Translational Relevance: The pachymetric indices are heritable and may be suitable as KC endophenotypes, indicating that the pachymetric indices might be a corneal characteristic to predict the occurrence of KC.

FeCl3-catalyzed nucleophilic substitution of propargylic acetates with enoxysilanes.

An efficient FeCl3-catalyzed substitution reaction of propargylic acetates with enoxysilanes under mild conditions to afford corresponding gamma-alkynyl ketones has been developed. The substitution reaction is followed by a TsOH-catalyzed cyclization without purification of the gamma-alkynyl ketone intermediates, offering a straightforward synthetic route to tri- or tetrasubstituted furans.