1.Development of analgesic drugs targeting Nav1.7: advances in clinical trials and discovery of selective inhibitors
Rui HAN ; Yi-lin CAI ; Xiao-tong ZHENG ; Fan-qi LIN ; Fan ZHANG
Acta Pharmaceutica Sinica 2024;59(9):2417-2428
The voltage-gated sodium channel subtype Nav1.7 is highly expressed in nociceptive sensory neurons and is a key pathogenic target in several human hereditary pain syndromes. In recent years, a large number of studies have shown that Nav1.7 plays an important role in inflammatory, neuropathic, and nociceptive pain. Therefore, targeting Nav1.7 is a new strategy and hotspot for the development of novel analgesics. This review introduces the structure and function of Nav1.7, its regulatory role in pain, highlights the development progress of small-molecule Nav1.7 inhibitors in clinical trials, and analyzes the preclinical development of highly specific Nav1.7 inhibitors, with a view to providing reference for the development of Nav1.7 analgesic drugs.
2.Study of the Morbid Risk Factors of Chronic Tubulointerstitial Nephropathy with an Unknown Origin in Wenzhou City
Fan LIN ; Feifei XU ; Yinqiu LV ; Yi LIU ;
Chinese Journal of Pharmacoepidemiology 2007;0(03):-
Objective:To analyze the morbid risk factors of chronic tubulointerstitial nephropathy(CTN)with an unknown origin in Wenzhhou City.Method:810 residents in several big districts were investigated.652 subjects,which had complete data and were coincided with the inclusion standard,were analyzed by an unmatched case-control study.The case group contained 19 cases coincided with the diagnostic criteria for CTN with unknown causes.The controlled group contained 633 cases.Thirteen probable risk factors were selected to be investigated:age,sex,body height,body weight, occupation,education,allergic history,addiction to smoking or wine,family history,the respective exposure to heavy met- als,radioactive ray and poisons.A history of medications,including caulis aristolochiae manshuriensis,antipyretic analge- sic,antibiotics,etc.was also investigated.The odds ratio(OR)of CTN with an unknown origin caused by risk factors were calculated with Logistic regression analysis.The obtained data were investigated,and the risk factors were screened out. All the data were analyzed with SPSS 12.0.Result:The homogeneity test showed there was no significant difference in age, sex,occupation and education between the case and controlled groups.The exposure to heavy metals or caulis aristolochiae manshuriensis was screened as the valid risk factor of CTN with OR 17.50 and 103.594 respoetively(P
3.Analysis of amplitude of low-frequency fluctuation in patients with anxiety after radiofrequency catheter ablation by resting state fMRI
Jianping YANG ; Guiwen LYU ; Yi LEI ; Jun XIA ; Fan LIN
Chinese Journal of Interventional Imaging and Therapy 2017;14(8):472-475
Objective To observe brain functional activity of patients with arrhythmia after radiofrequency ablation with amplitude of low-frequency fluctuation (ALFF).Methods Twenty-six patients with anxiety disorder after radiofrequency catheter ablation (RFCA) were included as RFCA group.Age and sex matched twenty-six healthy volunteers were included as control group.The difference of ALFF between the two groups was analyzed by two-sample t test.Partial correlation between extracted values from dysfunctional brain regions and hamilton anxiety scale (HAMA) scores were investigated.Results Compared with control group,ALFF of left middle temporal gyrus,right putamen,left amygdala significantly increased,and left dorsolateral prefrontal cortex (DLPFC),right praecuneus,left middle frontal gyrus and right middle occipital gyus significantly decreased in RFCA group (Alphasim correction,P<0.01).ALFF values of left DLPFC were negatively correlated with HAMA scores (r=-0.872,P=0.013).Conclusion The brain activity of RFCA patients in resting state is abnormal.ALFF can provide more evidences for the pathogenesis of the disease.
4.Comparison of SRAP and RAPD markers for genetic analysis of plants in Dendrobium Sw.
Honghong FAN ; Tingchun LI ; Jing QIU ; Yi LIN ; Yongping CAI
Chinese Traditional and Herbal Drugs 1994;0(04):-
Objective This study was carried out in order to analyze genetic diversity in plants of Dendrobium Sw. and compare the marker index (MI) between SRAP and RAPD markers. Methods Using 40 SRAP primer combinations and 36 RAPD primers,the genetic diversity of the materials in Dendrobium Sw. was amplified. Results A total of 1 977 loci were generated by 40 SRAP primer combinations,of which 90.2% was polymorphic and the genetic similarity (GS) ranged from 0.330 2 to 0.789 2. As for RAPD,281 bands were obtained,in which 87.1% was polymorphic,and the GS was from 0.494 2 to 0.773 1. There were some differences existing in the two cluster results revealed by SRAP and RAPD markers,they were as follows:compared to that of RAPD,the result of SRAP could more comfortably reflect the kinship and geographical origin,simultaneously conform to the traditional classification. For the experiment materials,SRAP (16.46) got an MI value 4.5 folds higher than that of RAPD (3.67),which meant SRAP markers were more effective in detecting genomic polymorphisms in the plants of Dendrobium Sw. Conclusion These results show that SRAP and RAPD could be applied to detecting genetic diversity analysis of plants in Dendrobium Sw. SRAP Also shows great superiority and advantage in this study.
5.Inhibiting effects of three components of Astragalus membranaceus on oxidative stress in Chang Liver cells.
Jian LI ; Lin HAN ; Yu-fang MA ; Yi-fan HUANG
China Journal of Chinese Materia Medica 2015;40(2):318-323
The main objective of this research is to investigate the effects of astragaloside IV, calycosin separately glucoside, formononetin on oxidative stress in Chang Liver cells induced by H2O2. In the experiments, Chang Liver cells (a kind of normal human hepatocytes) were used as the research object, bifendate which has a clear hepatoprotective effect was used as the positive control drug, then the oxidative damage model of Chang Liver cells were established by H2O2. Cells were divided into six groups: blank control group, oxidative stress group, astragaloside IV group, calycosin separately glucoside group, formononetin group and positive control group. Then endogenous antioxidant system related indexes were detected by micro plate and colorimetric method; intracellular reactive oxygen species (ROS) were detected by DCFH-DA fluorescent probe; and the expressions of CYP2E1 were evaluated by liver microsomes, mRNA, and protein, respectively with spectrophotometry, Real-time PCR method, and Western blot technique. Results showed that H2O2 decreased antioxidant activity, and increased ROS level and expression of CYP2E1. The above oxidative stress status had been changed with protections of the three components of Astragalus membranaceus (compared with oxidative stress group, P < 0.05, P < 0.01), which taken as a whole had equivalent effects as the drug of positive control group( bifendate). Taken together, three Astragalus membranaceus ingredients all had significant or extremely significant inhibiting effects on oxidative damaged Chang Liver cells which were induced by H2O2, and the oxidative damage of Chang Liver cells had been relieved.
Astragalus membranaceus
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chemistry
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Cells, Cultured
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Cytochrome P-450 CYP2E1
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metabolism
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Humans
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Isoflavones
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pharmacology
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Liver
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drug effects
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Oxidative Stress
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drug effects
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Reactive Oxygen Species
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metabolism
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Saponins
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pharmacology
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Triterpenes
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pharmacology
6.Practice and System Construction of Telemedicine for Coronavirus Disease 2019 Epidemic Prevention and Control.
Jing FAN ; Hong-Yi LIN ; Ming-Wei QIN
Acta Academiae Medicinae Sinicae 2020;42(4):531-534
Telemedicine is one of the five key components of the "Internet Plus Healthcare".Due to its high speed,real-timeness,low cost,and wide spread,telemedicine is highly feasible in the prevention and control of major infectious diseases.This article introduces the practiceof telemedicine in Peking Union Medical College Hospital during the cornavirus disease 2019(COVID-19)epidemic,during which the network resources were applied to break geographical restrictions and resolve communication barriers between hospitals and departments.This article summarizes the telemedicine application before,during and after COVID-19 control and elucidates how to build a telemedicine prevention and control system for infectious diseases,with an attempt to further improve telemedicine and is application in the public health emergency system in China.
Betacoronavirus
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Coronavirus Infections
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drug therapy
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Humans
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Pandemics
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Pneumonia, Viral
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drug therapy
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Telemedicine
7.Quality Standard of Pyrethri Tatsienenis Flos
Lishi ZHOU ; Lin ZHOU ; Qinghong YUE ; Yilong CHEN ; Fan YE ; Yi ZHANG ; Gang FAN
World Science and Technology-Modernization of Traditional Chinese Medicine 2014;(1):136-140
This study was aimed to establish the quality standard of Pyrethri Tatsienenis Flos. The medical material was identified by the microscopy and the thin layer chromatography ( TLC ) methods . The moisture , total ash , acid-insoluble ash and alcohol-soluble extract were determined according to procedures recorded in the Chi-nese Pharmacopoeia (2010 edition). The content of luteolin was determined by the HPLC method. The results showed a strong characteristic microscopic of Pyrethri Tatsienenis Flos , and its TLC identification had a good resolution with clear spots . The mass fractions of luteolin was 0 . 036%~0 . 104% ( average of 0 . 078%) , moisture was 9 . 32%~15 . 82% ( average of 13 . 11%) , total ash was 6 . 65%~8 . 29% ( average of 7 . 45%) , acid-insoluble ash was 0 . 23%~0 . 59% ( average of 0 . 42%) , and the extraction was 21 . 42%~30 . 15% ( average of 24 . 86%) . It was concluded that this established standard was simple to operate with good stability and reproducibility , which can be used for quality evaluation of Pyrethri Tatsienenis Flos .
8.Protective effect of astragaloside IV on oxidative damages of chang liver cell induced by ethanol and H2O2.
Lin HAN ; Jian LI ; Xin LIN ; Yu-fang MA ; Yi-fan HUANG
China Journal of Chinese Materia Medica 2014;39(22):4430-4435
OBJECTIVETo study the protective effect of astragaloside IV on oxidative damages of Chang Liver cells induced by ethanol and H2O2.
METHODThe alcoholic and nonalcoholic oxidative damage models were established on Chang Liver cells with ethanol and H2O2, respectively. The cells viabilities were detected by MTT assay, transaminase activity and antioxidant ability were detected by micro plate and colorimetric method, reactive oxide species (ROS) was detected by DCFH-DA fluorescent probe and cell cycle was detected by flow cytometry. DNA ladder method was used to detect apoptosis.
RESULTBoth kinds of oxidative damage could decrease the viability and antioxidant enzyme activity of Chang Liver cells, and increase the transaminase activity and MDA content of extracellular fluid. The protective effects of astragaloside IV against those two kinds of oxidative damages were significant or extremely significant. Meanwhile, ethanol could decline the level of ROS significantly in the damaged cells, while H2O2 could increase it significantly. And the effect of astragaloside IV was to make ROS return to the normal level. Retardation of cell cycle progression of Chang Liver cells in G0/G1 induced by ethanol or H2O2 was relieved, and apoptosis was also inhibited.
CONCLUSIONAstragaloside IV had protective effect on oxidative damages of Chang Liver cells induced by ethanol and H2O2.
Antioxidants ; metabolism ; Apoptosis ; Cell Cycle ; drug effects ; Cell Line ; Cell Survival ; drug effects ; Ethanol ; pharmacology ; Humans ; Hydrogen Peroxide ; pharmacology ; Oxidative Stress ; drug effects ; Reactive Oxygen Species ; metabolism ; Saponins ; pharmacology ; Triterpenes ; pharmacology
9.Effect of nourishing Yin, strengthening Qi and activating blood decoction on Fas/FasL in salivary glands of NOD mice with Sjogren's syndrome and their mRNA expression.
Guo-Lin WU ; Tian-Yi LI ; Wen-Wen LU ; Guo-You YU ; Yong-Sheng FAN
China Journal of Chinese Materia Medica 2013;38(23):4148-4151
OBJECTIVETo observe the effect of nourishing Yin, strengthening Qi and activating blood decoction on Fas/FasL in salivary glands of NOD mice with Sjogren's syndrome and their mRNA expression.
METHODThirty-two NOD mice were randomly divided into the model group, the traditional Chinese medicine group (TCM group, orally given 0.4 mL nourishing Yin, strengthening Qi and activating blood decoction as per 100 g x kg(-1) everyday), the hydroxychloroquine group (given 0.4 mL hydroxychloroquine as per 60 mg x kg(-1) everyday), the traditional Chinese medicine and western medicine group (TCM WM group, given nourishing Yin, Strengthening Qi and activating blood decoction 50 g x kg(-1) and hydroxychloroquine 60 mg x kg(-1), 0.4 mL everyday), with eight mice in each group. Eight Balb/C mice were selected as the normal control group (normal group). All of mice were killed after eight weeks, and their submaxillary glands were dissected. The expression levels of Fas/FasL were examined by immunohistochemical method, and the FasL mRNA was detected by RT-PCR.
RESULTThe expression levels of Fas/FasL in salivary glands of the model group were higher than that of other groups (P < 0.05). The expression level of FasL of the normal group was much lower than that in the hydroxychloroquine group (P < 0.05). The relative expression level of Fas mRNA in salivary glands of the model group was higher than that in other groups, but the control group was notably lower than other groups (P < 0.05). The expression level of FasL mRNA in salivary glands of the model group was higher than that in TCM and TCM WM groups (P < 0.05). But the expression level in TCM WM group was notably lower than the hydroxychloroquine group (P < 0.05).
CONCLUSIONThe nourishing Yin, strengthening Qi and activating blood decoction could down-regulate the expression level of Fas/FasL in salivary glands of NOD mice with Sjogren's syndrome and their mRNA expression, and had a better efficacy after being combined with hydroxychloroquine. The nourishing Yin, strengthening Qi and activating blood decoction might treat the Sjogren's Syndrome by reducing apoptosis which is regulated by Fas/FasL
Animals ; Fas Ligand Protein ; genetics ; Female ; Gene Expression Regulation ; Medicine, Chinese Traditional ; methods ; Mice ; Mice, Inbred NOD ; Qi ; RNA, Messenger ; genetics ; metabolism ; Salivary Glands ; metabolism ; Sjogren's Syndrome ; blood ; genetics ; therapy ; Yin-Yang ; fas Receptor ; genetics
10.Study on inhibitory effects and mechanism of lipophilic components in Salvia miltiorrhiza on angiogenesis in vitro.
Xue-Mei FAN ; Gui-Xiang REN ; Qiong-Lin LIANG ; Yi-Ming WANG ; Guo-An LUO
China Journal of Chinese Materia Medica 2014;39(4):744-747
In this study, the human umbilical vein endothelial cell model was used to study the regulating effect of lipophilic components in Salvia miltiorrhiza on angiogenesis, and explore its possible mechanism. The cell model was established to determine the effect of lipophilic components in S. miltiorrhiza on the proliferative activity and migration capacity of endothelial cells. Then the realtime fluorescence quantification PCR technology was applied to detect the changes in the gene expressions of angiogenesis-related cytokines VEGF-A, VEGF-C and MMP-9. The results showed that 5 mg x L(-1) lipophilic components in S. miltiorrhiza could inhibit the proliferation and migration of endothelial cells, and reduce the expression of VEGF-A and MMP-9 genes. It indicated that lipophilic components in S. miltiorrhiza may inhibit the proliferation and migration of endothelial cells by inhibiting the expression of VEGF-A and MMP-9 genes, so as to show the inhibitory effect on angiogenesis.
Angiogenesis Inhibitors
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chemistry
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pharmacology
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Cell Movement
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drug effects
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Cell Proliferation
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drug effects
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Drugs, Chinese Herbal
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chemistry
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pharmacology
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Human Umbilical Vein Endothelial Cells
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cytology
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drug effects
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metabolism
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Humans
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Matrix Metalloproteinase 9
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genetics
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metabolism
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Salvia miltiorrhiza
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chemistry
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Vascular Endothelial Growth Factor A
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genetics
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metabolism