1.Research progress of antifungal drugs from natural sources
Shao-jie CHU ; Yan ZHENG ; Shuang-shuang SU ; Xue-song WU ; Hong YAN ; Shao-xin CHEN ; Hong-bo WANG
Acta Pharmaceutica Sinica 2025;60(1):48-57
As the number of patients with compromised immune function increases and fungal resistance develops, so does the risk of contracting deadly fungi in humans. Both fungi and humans are eukaryotes, so identifying unique targets for antifungal drug development is difficult. In addition, the existing antifungal drugs are limited by toxicity, drug interaction and drug resistance in practical application, which leads to the increasing incidence and fatal rate of fungal infections. Therefore, it is urgent to develop new antifungal drugs. The semi-synthetic technology using microbial fermentation products from natural sources as lead compounds has become the most used method in structural modification of antifungal drugs due to its advantages of few reaction steps and easy operation. This paper will introduce the current status of natural antifungal drugs in clinical use, as well as the latest progress in the research and development of new semi-synthetic antifungal drugs, and summarize their mechanism of action, structural modifications, advantages and disadvantages, so as to provide reference for the subsequent development of new antifungal drugs.
2.Pattern differentiation methods and its clinical application of tangible or intangible abdominal masses of kidney collaterals
Xue LI ; Jing GAO ; Shijing ZHENG ; Bo PENG ; Shichang WANG ; Xinyu ZHAO ; Yan ZHOU ; Jing LI
Journal of Beijing University of Traditional Chinese Medicine 2024;47(8):1049-1054
The pattern differentiation method is the most representative part of the inheritance of the experience of renowned practitioners of traditional Chinese medicine,reflecting their clinical thinking characteristics. Among them,Professor LYU Renhe proposed and developed the theory of abdominal masses in the long-term diagnosis and treatment of kidney diseases. Based on his clinical experience,he formed the method of differentiation of Shenluozhengjia (tangible or intangible abdominal masses of kidney collaterals). This differentiation method is characterized by its simple and easy clinical application. Tangible or intangible abdominal masses of kidney collaterals refer to chronic kidney disease,which is based on the basic cause of kidney deficiency. External or internal pathogenic factors cannot be eliminated,and prolonged illness invades the kidney collaterals,causing pathological products,such as qi stagnation,blood stasis,phlegm dampness,heat toxin,and turbid toxin to stagnate in the kidney collaterals,resulting in damage to the kidney body and loss of kidney function. The basic pathogenesis is a deficiency of kidney qi and the formation of tangible or intangible abdominal masses of the kidney collaterals. During pattern differentiation,the type is determined by the deficiency,which is fixed,and the pattern is determined by the excess,which is constantly changing with the condition and can be combined. Furthermore,he summarized the dietary principles as having more essence and less coarseness,more milk and less meat,a phased diet,and the selection of the symptomatic diet. To inherit and improve the theory and clinical practice of the pattern differentiation theory of tangible or intangible abdominal masses of kidney collaterals,this article reviews and summarizes the unique pattern differentiation method of the kidney collateral pattern from the aspects of definition,theoretical origin,etiology and pathogenesis,differentiation and treatment,and regulation,providing a basis for forming suitable diagnosis and treatment method for clinical promotion.
3.Determination of ertapenem in human plasma by UPLC-MS/MS
Yi-Ran TAO ; Bo-Yu LIU ; Lei HU ; Si-Lu LIU ; Hai-Yan ZHAO ; Xue-Cai XUE ; Lin HUANG
The Chinese Journal of Clinical Pharmacology 2024;40(5):728-731
Objective A simple,sensitive and rapid ultra high performance liquid chromatography tandem mass spectrometry(UPLC-MS/MS)method was developed and validated for the determination of ertapenem in human plasma.Methods Using ertapenem-D4 as internal standard,the protein in plasma was precipitated with acetonitrile;chromatographic column:ACQUITY HSS T3(2.1 mm × 50.0 mm,1.8 μm);the mobile phase was 0.1%formic acid aqueous solution(containing 2 mmol·L-1 ammonium formate)-acetonitrile(0.1%formic acid),using a gradient elution;flow rate:0.4 mL·min-1,injection volume:1 μL,column temperature:45 ℃,the analysis time was 4.5 min,the scanning mode is positive ion selective reaction monitoring mode(SRM)with an electric spray ion source(ESI).The specificity,standard curve and lower limit of quantification,precision and recovery,matrix effect,dilution effect and stability were investigated.Results Ertapenem had a good linearity within 0.5-80.0μg·mL-1,and the standard curve was y=4.25 × 10-1x-2.64× 10-2(r2=0.999 0),the lower limit of quantification was 0.5 μg·mL-1,the relative standard deviation within and between batches is 1.39%-4.15%.The extraction recovery rate was 58.36%-64.57%,and the relative standard deviation of dilution effect was 3.30%,and the matrix effect was 99.71%-103.23%.The relative standard deviation of room temperature,repeated freeze-thaw,4 ℃,and long-term stability are all less than 10%.Conclusion The method is sensitive,rapid and specific,which is suitable for clinical monitoring of Ertapenem.
4.Synthesis and biological evaluation of 68Ga-NOTA-CD44: a novel tracer targeting atherosclerotic plaques
Bo WANG ; Li LI ; Xue YU ; Chuxin ZHANG ; Min YAN ; Huiling LI ; Huibin RU ; Ping WU ; Ruonan WANG ; Zhifang WU ; Sijin LI
Chinese Journal of Nuclear Medicine and Molecular Imaging 2024;44(2):104-108
Objective:To construct 68Ga-1, 4, 7-trizacyclononane-1, 4, 7-triacetic acid (NOTA)-CD44 as a novel atherosclerosis tracer targeting hyaluronic acid (HA), and evaluate its biological property and molecular imaging features. Methods:Low molecular weight (LMW) recombinant human CD44 protein was selected, and the C-terminal of the protein was modified by sulfonation and coupled to the bifunctional ligand NOTA to synthesize a novel molecular probe 68Ga-NOTA-CD44 targeting HA. The biological properties of the probe, such as labeling rate and in vitro stability, were studied. Three atherosclerotic plaque model mice and three normal C57BL/6 mice were studied by 68Ga-NOTA-CD44 microPET/CT imaging and pathological examination. Results:68Ga-NOTA-CD44 tracer was synthesized and purified with the radiochemical purity above 99%, and the specific activity was up to 62.22 MBq/nmol. lts stability was good in PBS, and the radiochemical purity was over 90% after incubation for 3 h. After intravenous injection, the probe was metabolized mainly by the kidneys, and its metabolic level decreased successively in the liver, lungs and blood. MicroPET/CT imaging results of atherosclerotic model mice suggested that the uptake in the plaque of abdominal aorta was higher at 60 min after injection, with SUV max and target/background ratio (TBR) max of 1.14±0.02 and 4.95±0.93, and the probe had certain atherosclerotic plaque eroded targeting, which was consistent with the pathological result. Conclusions:As a novel probe, 68Ga-NOTA-CD44 is simple to prepare and has a high labeling rate. It has good physicochemical properties and in vivo biological properties, and can display atherosclerotic eroded plaques sensitively. 68Ga-NOTA-CD44 has a promising prospect to be a new molecular probe for early noninvasive recognition of atherosclerotic eroded plaques.
5.TCM Guidelines for Diagnosis and Treatment of Chronic Cough in Children
Xi MING ; Liqun WU ; Ziwei WANG ; Bo WANG ; Jialin ZHENG ; Jingwei HUO ; Mei HAN ; Xiaochun FENG ; Baoqing ZHANG ; Xia ZHAO ; Mengqing WANG ; Zheng XUE ; Ke CHANG ; Youpeng WANG ; Yanhong QIN ; Bin YUAN ; Hua CHEN ; Lining WANG ; Xianqing REN ; Hua XU ; Liping SUN ; Zhenqi WU ; Yun ZHAO ; Xinmin LI ; Min LI ; Jian CHEN ; Junhong WANG ; Yonghong JIANG ; Yongbin YAN ; Hengmiao GAO ; Hongmin FU ; Yongkun HUANG ; Jinghui YANG ; Zhu CHEN ; Lei XIONG
Journal of Nanjing University of Traditional Chinese Medicine 2024;40(7):722-732
Following the principles of evidence-based medicine,in accordance with the structure and drafting rules of standardized documents,based on literature research,according to the characteristics of chronic cough in children and issues that need to form a consensus,the TCM Guidelines for Diagnosis and Treatment of Chronic Cough in Children was formulated based on the Delphi method,expert discussion meetings,and public solicitation of opinions.The guideline includes scope of application,terms and definitions,eti-ology and diagnosis,auxiliary examination,treatment,prevention and care.The aim is to clarify the optimal treatment plan of Chinese medicine in the diagnosis and treatment of this disease,and to provide guidance for improving the clinical diagnosis and treatment of chronic cough in children with Chinese medicine.
6.Ten kinds of antipyretic-antidotal traditional Chinese medicine extracts against extensively drug-resistant Acinetobacter baumannii infection
Yan YANG ; Jian-Wen FENG ; Bo JI ; Jin YUAN ; Yan WANG ; Jian LI ; Xue-Jiu CAI ; Zhi-Hui JIANG
Chinese Journal of Infection Control 2024;23(3):271-276
Objective To study the activity of ten kinds of antipyretic-antidotal traditional Chinese medicine(TCM),including radix tinosporae.herb of blin conyza and turmeric,against extensively drug-resistant Acineto-bacter baumannii(XDR-AB)infection,screen out the extracts of antipyretic-antidotal TCM which have in vivo anti-infection activity,provide a research basis for the discovery of novel antimicrobials against XD-RAB infection.Methods Ten antipyretic-antidotal TCM were extracted with water,50%ethanol and 95%ethanol respectively,and TCM extracts with different concentrations were prepared,which were co-incubated with the model of XDR-AB-infected Caenorhabditis elegans previously optimized by the research group.The in vivo activity of antipyretic-antidotal TCM against XDR-AB infection was judged through the survival rate of Caenorhabditis elegans.Results With the increase of concentration of turmeric and cortex pseudolaricis extracts,the survival rate of XDR-AB-infec-ted nematodes continued to improve.The water extract,50%ethanol extract,and 95%ethanol extract of turmeric at a concentration of 1 000 μg/mL could increase the survival rates of XDR-AB-infected Caenorhabditis elegans to 54.2%(compared to the negative control group,P<0.001),18.8%,and 13.3%,respectively.The water ex-tract,50%ethanol extract,and 95%ethanol extract of cortex pseudolaricis at a concentration of 1 000 μg/mL could increase the survival rates of XDR-AB-infected Caenorhabditis elegans to 47.4%(compared to the negative control group,P<0.001),23.8%,and 15.8%,respectively.Conclusion The water extracts of turmeric and cortex pseudolaricis have good activity against XDR-AB infection,and their main chemical components can be tested for in vitro antimicrobial efficacy to discover novel antimicrobial agents against XDR-AB infection.
7.Analysis of Acupoint Selection Rules of Effective Prescriptions for Acupuncture Treatment of Non-Small Cell Lung Cancer
Rui ZHOU ; Yan-Juan ZHU ; Hao-Chuan MA ; Xue-Song CHANG ; Ya-Dong CHEN ; Yi-Han HE ; Hai-Bo ZHANG
Journal of Guangzhou University of Traditional Chinese Medicine 2024;41(7):1827-1832
Objective To analyse the acupoint selection rules of acupuncture in the treatment of non-small cell lung cancer,and to provide reference for clinical application.Methods The clinical research,practitioner's experience and academic thought of acupuncture treatment for non-small cell lung cancer were retrieved to obtain the acupuncture prescriptions of modern practitioners for the treatment of non-small cell lung cancer.Based on the statistical methods of acupoint frequency,prescription rules,acupoint clustering and core combination,the core theoretical system and acupoint selection rules of acupuncture treatment of non-small cell lung cancer by modern practitioner were analyzed.Results According to the inclusion and exclusion criteria,94 acupuncture prescriptions were finally included.There were eight acupoints used more than 20 times,which were Zusanli(ST36),Neiguan(PC6),Feishu(BL13),Sanyinjiao(SP6),Qihai(RN6),Guanyuan(RN4),Hegu(LI4)and Zhongwan(RN12).The top three high-frequency acupoint combinations were Zusanli-Neiguan,Zusanli-Sanyinjiao and Qihai-Zusanli;correlation analysis showed that the correlation strength of Zusanli-Neiguan was the highest,followed by Zusanli-Sanyinjiao and Zusanli-Hegu.The cluster analysis showed that the acupoints with frequency>10 times could be divided into three categories.Category 1 includes:Zusanli,Neiguan,Sanyinjiao,Hegu;category 2 includes Guanyuan,Qihai,Zhongwan,Xuehai(SP10),Taichong(LR3);category 3 consists of two parts,one is Danzhong(RN17),Tiantu(RN22),Fenglong(ST40),Taiyuan(LU9);the second is Feishu(BL13),Lieque(LU7),Chize(LU5),Zhongfu(LU1),Xinshu(BL15),Gaohuang(BL43),Fengmen(BL12).Conclusion The core acupoints for acupuncture treatment of non-small cell lung cancer include four categories:① invigorating the spleen and benefiting qi:Zusanli,Sanyinjiao,Zhongwan and Fenglong;②replenishing and supplementing original qi:Guanyuan,Qihai and Gaohuang;③regulating qi and broadening the chest:Danzhong,Neiguan,Tiantu and Fengmen;④ diffusing the lung and ventilating qi:Feishu,Hegu,Chize and Lieque.The three treatment methods of replenishing qi,regulating qi and venting pathogen are the basis of acupuncture treatment of advanced non-small cell lung cancer.The core idea of acupuncture treatment of non-small cell lung cancer focuses on supplementation,supplemented by dredging,and to dredge and supplement simultaneously.
8.Study on related influencing factors on the occurrence of redundant sign in the cauda equina in lumbar spinal stenosis
Bo DENG ; Xu-Dong LI ; Xiao-Zhong LUO ; Xue-Liang YAN
China Journal of Orthopaedics and Traumatology 2024;37(8):824-827
Objective To analyze the relational factors influencing the formation of cauda equina redundant nerve roots(RNRs)of the lumbar spinal stenosis.Methods Clinical data of 116 patients with lumbar spinal stenosis treated from January 2016 to June 2019 were retrospectively analyzed.The patients were divided into redundant nerve roots(RNRs)group and non-RNRs group based on the presence or absence of RNRs on sagittal T2-weighted MRI.In the non-RNRs group,there were 74 patients,including 38 males and 36 females with an average age of(62.00±10.41)years old,the body mass index(BMI)was(23.09±2.22)kg.m-2;the maximum stenosis segment was L2-L3 in 12 cases,L3-L4 in 38,L4-L5 in 20,and L5S1 in 4,respec-tively.In the RNRs group,there were 42 patients,including 18 males and 24 females with an average age of(63.36±8.73)years old,the BMI was(22.63±2.60)kg·m-2;the maximum stenosis segment was L2-L3 in 3 cases,L3-L4 in 9,L4-L5 in 27 and L5S1 in 3,respectively.MRI was performed in the supine position to observe the conshape and morphology of the redundant nerve in the sagittal position.The preoperative low back and leg pain visual analogue scale(VAS),and preoperative Oswestry disability index(ODI)were analyzed,and the rate of spondylolisthesis and ligamentum flavum hypertrophy were compared.Si-multaneously,the inter-vertebral height,intervertebral foramen height,inter-vertebral height+vertebral height,median sagittal diameter at the inter-vertebral space level(DIW-MSD),median sagittal diameter at the pedicel level(DV-MSD),range of mo-tion(ROM)of the stenotic segment were measured and analyzed.Results Among the 116 patients with lumbar spinal stenosis,42 patients developed RNRs,with an incidence of 36.2%.There were no significant differences in gender,age,BMI,preopera-tive VAS for lumbar and leg pain and ODI between two groups(P>0.05).There were statistically significant differences regard to the duration of symptoms and the rate of spondylolisthesis and ligamentum flavum hypertrophy(P<0.05);the inter-vertebral height,intervertebral foramen height,inter-vertebral height+vertebral height,DIW-MSD,ROM of the stenotic segment were al-so significantly different between two groups(P<0.05).However,there was no significant difference in DV-MSD between two groups(P>0.05).Conclusion The inter-vertebral height,inter-vertebral foramen height,inter-vertebral height+vertebral height,DIW-MSD and ROM of the stenotic segment were the crucial factors related to RNRs in lumbar spinal stenosis.
9.Screening and identification of a polyurethane-degrading bacterium G-11 and its plastic degradation characteristics.
Zhitong JIANG ; Xue CHEN ; Jinhui LEI ; Huizhen XUE ; Bo ZHANG ; Xiaofan XU ; Huijing GENG ; Zhoukun LI ; Xin YAN ; Weiliang DONG ; Hui CAO ; Zhongli CUI
Chinese Journal of Biotechnology 2023;39(5):1963-1975
Polyurethane (PUR) plastics is widely used because of its unique physical and chemical properties. However, unreasonable disposal of the vast amount of used PUR plastics has caused serious environmental pollution. The efficient degradation and utilization of used PUR plastics by means of microorganisms has become one of the current research hotspots, and efficient PUR degrading microbes are the key to the biological treatment of PUR plastics. In this study, an Impranil DLN-degrading bacteria G-11 was isolated from used PUR plastic samples collected from landfill, and its PUR-degrading characteristics were studied. Strain G-11 was identified as Amycolatopsis sp. through 16S rRNA gene sequence alignment. PUR degradation experiment showed that the weight loss rate of the commercial PUR plastics upon treatment of strain G-11 was 4.67%. Scanning electron microscope (SEM) showed that the surface structure of G-11-treated PUR plastics was destroyed with an eroded morphology. Contact angle and thermogravimetry analysis (TGA) showed that the hydrophilicity of PUR plastics increased along with decreased thermal stability upon treatment by strain G-11, which were consistent with the weight loss and morphological observation. These results indicated that strain G-11 isolated from landfill has potential application in biodegradation of waste PUR plastics.
Plastics/metabolism*
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Polyurethanes/chemistry*
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RNA, Ribosomal, 16S
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Bacteria/genetics*
;
Biodegradation, Environmental
10.Nomogram-Based Prediction of Risk of Cervical Lymph Node Metastasis in Differentiated Thyroid Carcinoma.
Yan TIAN ; Xue-Hua XI ; Jiao-Jiao MA ; Jia-Jia TANG ; Hui-Lin LI ; Qi ZHU ; Bo ZHANG
Acta Academiae Medicinae Sinicae 2023;45(3):355-360
Objective To establish a nomogram for predicting the risk of cervical lymph node metastasis in differentiated thyroid carcinoma (DTC). Methods The patients with complete clinical data of DTC and cervical lymph node ultrasound and diagnosed based on pathological evidence from January 2019 to December 2021 were assigned into a training group (n=444) and a validation group (n=125).Lasso regression was performed to screen the data with differences between groups,and multivariate Logistic regression to establish a prediction model with the factors screened out by Lasso regression.C-index and calibration chart were employed to evaluate the prediction performance of the established model. Results The predictive factors for establishing the model were lymph node short diameter≥0.5 cm,long-to-short-axis ratio<2,disappearance of lymph node hilum,cystic transformation,hyperechogenicity,calcification,and abnormal blood flow (all P<0.001).The established model demonstrated a good discriminative ability,with the C index of 0.938 (95%CI=0.926-0.961) in the training group. Conclusion The nomogram established based on the ultrasound image features of cervical lymph nodes in DTC can accurately predict the risk of cervical lymph node metastasis in DTC.
Humans
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Nomograms
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Lymphatic Metastasis
;
Lymph Nodes/pathology*
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Neck/pathology*
;
Thyroid Neoplasms/pathology*
;
Adenocarcinoma/pathology*
;
Retrospective Studies

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