Research progress on chemical structures and pharmacological effects of natural cytisine and its derivatives / 中国中药杂志

Cytisine derivatives are a group of alkaloids containing the structural core of cytisine, which are mainly distributed in Fabaceae plants with a wide range of pharmacological activities, such as resisting inflammation, tumors, and viruses, and affecting the central nervous system. At present, a total of 193 natural cytisine and its derivatives have been reported, all of which are derived from L-lysine. In this study, natural cytisine derivatives were classified into eight types, namely cytisine type, sparteine type, albine type, angustifoline type, camoensidine type, cytisine-like type, tsukushinamine type, and lupanacosmine type. This study reviewed the research progress on the structures, plant sources, biosynthesis, and pharmacological activities of alkaloids of various types.

Comparative Study between ZOOMit and Conventional Intravoxel Incoherent Motion MRI for Assessing Parotid Gland Abnormalities in Patients with Early- or Mid-Stage Sjögren’s Syndrome

Objective@#To compare the reproducibility and performance of quantitative metrics between ZOOMit and conventional intravoxel incoherent motion (IVIM) magnetic resonance imaging (MRI) in the diagnosis of early- and mid-stage Sjögren’s syndrome (SS). @*Materials and Methods@#Twenty-two patients (mean age ± standard deviation, 52.0 ± 10.8 years; male:female, 2:20) with early- or mid-stage SS and 20 healthy controls (46.9 ± 14.6 years; male:female, 7:13) were prospectively enrolled in our study.ZOOMit IVIM and conventional IVIM MRI were performed simultaneously in all individuals using a 3T scanner. Quantitative IVIM parameters - including tissue diffusivity (D), pseudodiffusion coefficient (D*), and perfusion fraction (f) - inter- and intra-observer reproducibility in measuring these parameters, and their ability to distinguish patients with SS from healthy individuals were assessed and compared between ZOOMit IVIM and conventional IVIM methods, appropriately. MR gland nodular grade (MRG) was also examined. @*Results@#Inter- and intra-observer reproducibility was better with ZOOMit imaging than with conventional IVIM imaging (ZOOMit vs. conventional, intraclass correlation coefficient of 0.897–0.941 vs. 0.667–0.782 for inter-observer reproducibility and 0.891–0.968 vs. 0.814–0.853 for intra-observer reproducibility). Significant differences in ZOOMit f, ZOOMit D*, conventional D*, and MRG between patients with SS and healthy individuals (all p < 0.05) were observed. ZOOMit D* outperformed conventional D* in diagnosing early- and mid-stage SS (area under receiver operating curve, 0.867 and 0.658, respectively; p = 0.002). The combination of ZOOMit D*, MRG, and ZOOMit f as a new diagnostic index for SS, increased diagnostic area under the curve to 0.961, which was higher than that of any single parameter (all p < 0.01). @*Conclusion@#Considering its better reproducibility and performance, ZOOMit IVIM may be preferred over conventional IVIM MRI, and may subsequently improve the ability to diagnose early- and mid-stage SS.

Inhibitory effects of baicalein against herpes simplex virus type 1

Herpes simplex virus type 1 (HSV-1) is a ubiquitous and widespread human pathogen, which gives rise to a range of diseases, including cold sores, corneal blindness, and encephalitis. Currently, the use of nucleoside analogs, such as acyclovir and penciclovir, in treating HSV-1 infection often presents limitation due to their side effects and low efficacy for drug-resistance strains. Therefore, new anti-herpetic drugs and strategies should be urgently developed. Here, we reported that baicalein, a naturally derived compound widely used in Asian countries, strongly inhibited HSV-1 replication in several models. Baicalein was effective against the replication of both HSV-1/F and HSV-1/Blue (an acyclovir-resistant strain)

Automatic Detection and Classification of Rib Fractures on Thoracic CT Using Convolutional Neural Network: Accuracy and Feasibility

Objective@#To evaluate the performance of a convolutional neural network (CNN) model that can automatically detect and classify rib fractures, and output structured reports from computed tomography (CT) images. @*Materials and Methods@#This study included 1079 patients (median age, 55 years; men, 718) from three hospitals, between January 2011 and January 2019, who were divided into a monocentric training set (n = 876; median age, 55 years; men, 582), five multicenter/multiparameter validation sets (n = 173; median age, 59 years; men, 118) with different slice thicknesses and image pixels, and a normal control set (n = 30; median age, 53 years; men, 18). Three classifications (fresh, healing, and old fracture) combined with fracture location (corresponding CT layers) were detected automatically and delivered in a structured report. Precision, recall, and F1-score were selected as metrics to measure the optimum CNN model. Detection/diagnosis time, precision, and sensitivity were employed to compare the diagnostic efficiency of the structured report and that of experienced radiologists. @*Results@#A total of 25054 annotations (fresh fracture, 10089; healing fracture, 10922; old fracture, 4043) were labelled for training (18584) and validation (6470). The detection efficiency was higher for fresh fractures and healing fractures than for old fractures (F1-scores, 0.849, 0.856, 0.770, respectively, p = 0.023 for each), and the robustness of the model was good in the five multicenter/multiparameter validation sets (all mean F1-scores > 0.8 except validation set 5 [512 x 512 pixels; F1-score = 0.757]). The precision of the five radiologists improved from 80.3% to 91.1%, and the sensitivity increased from 62.4% to 86.3% with artificial intelligence-assisted diagnosis. On average, the diagnosis time of the radiologists was reduced by 73.9 seconds. @*Conclusion@#Our CNN model for automatic rib fracture detection could assist radiologists in improving diagnostic efficiency, reducing diagnosis time and radiologists’ workload.

Cloning and Prokaryotic Expression of Squalene Epoxidase Gene from Panax vietnamensis var. fuscidiscus / 中国实验方剂学杂志

Objective: To clone the squalene epoxidase genes of Panax vietnamensis var. fuscidiscus(PvfSE),and perform bioinformatics analysis and prokaryotic expression. Method: Total RNA was extracted from root of P. vietnamensis var. fuscidiscus by trizol method, and reverse-transcribed into first stand of cDNA. Specific primers for PvfSE cloning were designed according to the transcriptome data of P. vietnamensis var. fuscidiscus,and the cDNA sequence of PvfSE gene was isolated. Bioinformatics of PvfSE was analyzed by relevant software. The prokaryotic expression vector pMal-c2X-PvfSE was built to express recombinant protein in Escherichia coli cells. Result: The PvfSE gene contained a 1 887 bp open reading frame,encoding a predicted protein of 628 amino acids. The calculated molecular weight was 68.8 kDa,the theoretical isoelectric point was 9.28,the aliphatic index was 95.18,the grand average of hydropathicity was -0.060, and the instability index was 40.36. The protein was unstable. Bioinformatics analysis showed that PvfSE had two transmembrane domains and no signal peptide. PvfSE was most likely to be located in chloroplast or cytoplasmic membrane. PvfSE was a mixed protein with FAD/NAD(P) binding domain and squalene epoxidase domain. Sequence alignment and phylogenetic analysis demonstrated that PvfSE had a relatively close relationship with CpSE1,CpSE3,OsSE1 and OsSE2,which was involved in the biosynthesis of triterpene saponins in Cucurbita pepo and Ononis spinosa. In addition,PvfSE protein was expressed in E. coli. Conclusion: In this study,PvfSE gene was cloned and expressed in BL21(DE3),which lays a foundation for the further study on the gene functions of PvfSE and the biosynthetic pathway of triterpenoid saponins in P. vietnamensis var. fuscidiscus.

Clinical characteristics and gene analysis of vitreous amyloidosis in a Chinese kindreds / 中华实验眼科杂志

Background Familial vitreous amyloidosis is a rare ocular regional amyloidosis,and it is a kind of autosomal dominant inheritance disease.Familial vitreous amyloidosis demonstrates a variable penetrance due to the mutation in the plasma thyroid hormone-binding protein transtheretin (TTR) gene.Many studies have reported over 100 types of TTR genetic mutation in Switzerland,Portugal and Japan,but rare in China.Objective This survey aimed to investigate the clinical and genetic mutation characteristics in familial vitreous amyloidosis.Methods Physical and eye examinations were performed on 52 family members of this vitreous amyloidosis family.Peripheral blood samples from 52 members were collected for TTR gene test by DNA extract,PCR amplification,clone,bolting and sequencing.Pars plana vitrectomy was firstly performed prior to the pathological examination of vitreous sample on 13 eyes of 8 members.Informed consent was obtained from each individual before any medical procedure.Results Seventeen members suffered from vitreous amyloidosis in this family without nervous system,heart,kidney and liver disease.Vitreous opacity was found in 34 eyes of the 17 members,and retinal vasculopathy was seen in 28 eyes of 15 members.In addition,cataract appeared in 16 eyes of 10 members.None of the members had glaucoma or ocular motility disorders.Congo red test of vitreous specimens showed a positive result in 13 eyes of 8 patients who received vitrectomy.Point mutation was verified on the 83th amine acid location of exon 3 (Gly83Arg) in TTR gene by gene sequencing.Conclusions Clinical characteristics of familial vitreous amyloidosis induced by TTR gene Arg-83 mutation is rate retinal vasculopathy without glaucoma,other ocular regional disease and systemic diseases.