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.Clinical Observation on Abdominal Penetrating Moxibustion Combined with Acupuncture at Four Chong Acupoints for the Treatment of Stroke in the Convalescent Stage
Nan YU ; Jie HU ; Hai-Ning LI ; Shan-Shan SONG ; De-Song ZHENG ; Xin-Hong XUE ; Ying GAO
Journal of Guangzhou University of Traditional Chinese Medicine 2024;41(1):116-122
Objective To observe the effects of abdominal penetrating moxibustion combined with acupuncture at the"four chong points"on balance,walking function and trunk control in patients recovering from stroke.Methods Seventy-eight patients recovering from stroke were randomly divided into an observation group and a control group,with 39 patients in each group.The control group was given conventional rehabilitation exercises,while the observation group was given abdominal penetrating moxibustion combined with acupuncture at the"four chong points"on the basis of the control group.Both groups were treated for 2 consecutive months.After 2 months of treatment,the clinical efficacy of the two groups was evaluated,and the changes in the Berg Scale score and the Timed Up and Go Test(TUGT)were observed before and after treatment.The changes in the National Institutes of Health Stroke Scale(NIHSS)scores were compared before and after treatment between the two groups.The Sheikh Trunk Control Scale scores were also evaluated.Results(1)The total effective rate of the observation group was 94.87%(37/39),and the total effective rate of the control group was 80.00%(31/39),and the efficacy of the observation group was superior to that of the control group,and the difference was statistically significant(P<0.05).(2)After treatment,the Berg scores of the patients in the two groups were significantly increased(P<0.05),and the Berg scores of the observation group were higher than those of the control group,and the difference was statistically significant(P<0.05).(3)After treatment,the TUGT time and NIHSS score of patients in the two groups were significantly improved(P<0.05),and the TUGT time of the observation group was shorter than that of the control group,and the NIHSS score was lower than that of the control group,and the difference was statistically significant(P<0.05).(4)After treatment,the Sheikh trunk control scores of the two groups were significantly increased(P<0.05),and the Sheikh trunk control score of the observation group was higher than that of the control group,and the difference was statistically significant(P<0.05).Conclusion Abdominal penetrating moxibustion method combined with acupuncture at the four chong points for the treatment of stroke recovery can effectively restore the patients'balance and walking function,improve the patients'trunk control ability,and the therapeutic effect is precise.
3.Clinical trial of Morinda officinalis oligosaccharides in the continuation treatment of adults with mild and moderate depression
Shu-Zhe ZHOU ; Zu-Cheng HAN ; Xiu-Zhen WANG ; Yan-Qing CHEN ; Ya-Ling HU ; Xue-Qin YU ; Bin-Hong WANG ; Guo-Zhen FAN ; Hong SANG ; Ying HAI ; Zhi-Jie JIA ; Zhan-Min WANG ; Yan WEI ; Jian-Guo ZHU ; Xue-Qin SONG ; Zhi-Dong LIU ; Li KUANG ; Hong-Ming WANG ; Feng TIAN ; Yu-Xin LI ; Ling ZHANG ; Hai LIN ; Bin WU ; Chao-Ying WANG ; Chang LIU ; Jia-Fan SUN ; Shao-Xiao YAN ; Jun LIU ; Shou-Fu XIE ; Mao-Sheng FANG ; Wei-Feng MI ; Hong-Yan ZHANG
The Chinese Journal of Clinical Pharmacology 2024;40(6):815-819
Objective To observe the efficacy and safety of Morinda officinalis oligosaccharides in the continuation treatment of mild and moderate depression.Methods An open,single-arm,multi-center design was adopted in our study.Adult patients with mild and moderate depression who had received acute treatment of Morinda officinalis oligosaccharides were enrolled and continue to receive Morinda officinalis oligosaccharides capsules for 24 weeks,the dose remained unchanged during continuation treatment.The remission rate,recurrence rate,recurrence time,and the change from baseline to endpoint of Hamilton Depression Scale(HAMD),Hamilton Anxiety Scale(HAMA),Clinical Global Impression-Severity(CGI-S)and Arizona Sexual Experience Scale(ASEX)were evaluated.The incidence of treatment-related adverse events was reported.Results The scores of HAMD-17 at baseline and after treatment were 6.60±1.87 and 5.85±4.18,scores of HAMA were 6.36±3.02 and 4.93±3.09,scores of CGI-S were 1.49±0.56 and 1.29±0.81,scores of ASEX were 15.92±4.72 and 15.57±5.26,with significant difference(P<0.05).After continuation treatment,the remission rate was 54.59%(202 cases/370 cases),and the recurrence rate was 6.49%(24 cases/370 cases),the recurrence time was(64.67±42.47)days.The incidence of treatment-related adverse events was 15.35%(64 cases/417 cases).Conclusion Morinda officinalis oligosaccharides capsules can be effectively used for the continuation treatment of mild and moderate depression,and are well tolerated and safe.
4.Quality evaluation for Beidougen Formula Granules
Gui-Yun CAO ; Xue-Song ZHUANG ; Bo NING ; Yong-Qiang LIN ; Dai-Jie WANG ; Wei-Liang CUI ; Hong-Chao LIU ; Xiao-Di DONG ; Meng-Meng HUANG ; Zhao-Qing MENG
Chinese Traditional Patent Medicine 2024;46(3):717-723
AIM To evaluate the quality of Beidougen Formula Granules.METHODS Fifteen batches of standard decoctions and three batches of formula granules were prepared,after which paste rate and contents,transfer rates of magnoflorine,daurisoline,dauricine were determined.HPLC specific chromatograms were established,and cluster analysis was adopted in chemical pattern recognition.RESULTS For three batches of formula granules,the paste rates were 15.1%-16.6%,the contents of magnoflorine,daurisoline,dauricine were 18.93-19.39,9.42-9.60,6.79-6.85 mg/g with the transfer rates of 34.42%-35.25%,43.81%-44.65%,27.27%-27.51%from decoction pieces to formula granules,respectively,and there were seven characteristic peaks in the specific chromatograms with the similarities of more than 0.95,which demonstrated good consistence with those of standard decoctions and accorded with related limit requirements.Fifteen batches of standard decoctions were clustered into two types,and the medicinal materials produced from Jilin,Hebei,Shangdong could be used for the preparation of formula granules.CONCLUSION This reasonable and reliable method can provide references for the quality control and clinical application of Beidougen Formula Granules.
5.Effect of behavioral vision training on post-stroke ocular motility disorders
Xue WANG ; Liping WANG ; Ning SONG ; Lanqun LIU ; Jie ZHOU ; Jun WU
Chinese Journal of Rehabilitation Theory and Practice 2024;30(6):726-730
Objective To explore the effect of behavioral vision training on post-stroke ocular motility disorders(PSOMD). Methods From August to Octobor,2023,a total of 21 PSOMD patients in Beijing Bo'ai Hospital were selected.They re-ceived behavioral vision training,including brain-based visual training and visual fusion training,for four weeks.Visual function was assessed with Snellen eye chart,strabismus prism and Titmus near stereopia. Results The vision of both right and left eyes improved after training(Z right eye=-3.601,Z left eye=3.012,P<0.01),while the strabismus prism reduced significantly(t=8.930,P<0.001).But Titmus near stereopia showed no difference(P>0.05). Conclusion Behavioral vision training could improve vision and strabismus after stroke.
6.Assessment of respiratory protection competency of staff in healthcare facilities
Hui-Xue JIA ; Xi YAO ; Mei-Hua HU ; Bing-Li ZHANG ; Xin-Ying SUN ; Zi-Han LI ; Ming-Zhuo DENG ; Lian-He LU ; Jie LI ; Li-Hong SONG ; Jian-Yu LU ; Xue-Mei SONG ; Hang GAO ; Liu-Yi LI
Chinese Journal of Infection Control 2024;23(1):25-31
Objective To understand the respiratory protection competency of staff in hospitals.Methods Staff from six hospitals of different levels and characteristics in Beijing were selected,including doctors,nurses,medical technicians,and servicers,to conduct knowledge assessment on respiratory protection competency.According to exposure risks of respiratory infectious diseases,based on actual cases and daily work scenarios,content of respira-tory protection competency assessment was designed from three aspects:identification of respiratory infectious di-seases,transmission routes and corresponding protection requirements,as well as correct selection and use of masks.The assessment included 6,6,and 8 knowledge points respectively,with 20 knowledge points in total,all of which were choice questions.For multiple-choice questions,full marks,partial marks,and no mark were given respective-ly if all options were correct,partial options were correct and without incorrect options,and partial options were correct but with incorrect options.Difficulty and discrimination analyses on question of each knowledge point was conducted based on classical test theory.Results The respiratory protection competency knowledge assessment for 326 staff members at different risk levels in 6 hospitals showed that concerning the 20 knowledge points,more than 60%participants got full marks for 6 points,while the proportion of full marks for other questions was relatively low.Less than 10%participants got full marks for the following 5 knowledge points:types of airborne diseases,types of droplet-borne diseases,conventional measures for the prevention and control of healthcare-associated infec-tion with respiratory infectious diseases,indications for wearing respirators,and indications for wearing medical protective masks.Among the 20 knowledge questions,5,1,and 14 questions were relatively easy,medium,and difficult,respectively;6,1,4,and 9 questions were with discrimination levels of ≥0.4,0.30-0.39,0.20-0.29,and ≤0.19,respectively.Conclusion There is still much room for hospital staff to improve their respiratory protection competency,especially in the recognition of diseases with different transmission routes and the indications for wearing different types of masks.
7.TSHR Variant Screening and Phenotype Analysis in 367 Chinese Patients With Congenital Hypothyroidism
Hai-Yang ZHANG ; Feng-Yao WU ; Xue-Song LI ; Ping-Hui TU ; Cao-Xu ZHANG ; Rui-Meng YANG ; Ren-Jie CUI ; Chen-Yang WU ; Ya FANG ; Liu YANG ; Huai-Dong SONG ; Shuang-Xia ZHAO
Annals of Laboratory Medicine 2024;44(4):343-353
Background:
Genetic defects in the human thyroid-stimulating hormone (TSH) receptor (TSHR) gene can cause congenital hypothyroidism (CH). However, the biological functions and comprehensive genotype–phenotype relationships for most TSHR variants associated with CH remain unexplored. We aimed to identify TSHR variants in Chinese patients with CH, analyze the functions of the variants, and explore the relationships between TSHR genotypes and clinical phenotypes.
Methods:
In total, 367 patients with CH were recruited for TSHR variant screening using whole-exome sequencing. The effects of the variants were evaluated by in-silico programs such as SIFT and polyphen2. Furthermore, these variants were transfected into 293T cells to detect their Gs/cyclic AMP and Gq/11 signaling activity.
Results:
Among the 367 patients with CH, 17 TSHR variants, including three novel variants, were identified in 45 patients, and 18 patients carried biallelic TSHR variants. In vitro experiments showed that 10 variants were associated with Gs/cyclic AMP and Gq/11 signaling pathway impairment to varying degrees. Patients with TSHR biallelic variants had lower serum TSH levels and higher free triiodothyronine and thyroxine levels at diagnosis than those with DUOX2 biallelic variants.
Conclusions
We found a high frequency of TSHR variants in Chinese patients with CH (12.3%), and 4.9% of cases were caused by TSHR biallelic variants. Ten variants were identified as loss-of-function variants. The data suggest that the clinical phenotype of CH patients caused by TSHR biallelic variants is relatively mild. Our study expands the TSHR variant spectrum and provides further evidence for the elucidation of the genetic etiology of CH.
8.LIN Chang-Song's Experience in Differentiating and Treating Behcet's Disease
Lian-Jie LIU ; Xue-Xia ZHENG ; Qi WU ; Chang-Song LIN
Journal of Guangzhou University of Traditional Chinese Medicine 2024;41(5):1329-1334
Behcet's disease can be classified into the category of fox-creeper disease in the field of traditional Chinese medicine(TCM).Professor LIN Chang-Song believes that the pathogenesis of Behcet's disease is characterized by deficiency in origin and excess in superficiality,and liver depression and spleen deficiency is the fundamental pathogenesis of Behcet's disease.The cause of Behcet's disease is due to exogenous attack of pathogenic qi,and the disease has the syndrome manifestation of internal accumulation of damp-heat.For the treatment of Bechet's disease,the use of self-made Baisai Prescription and Kouyan Prescription which were derived from Gancao Xiexin Decoction recorded in Jin Gui Yao Lve(Essentials from the Golden Cabinet)together with large dosage of Glycyrrhizae Radix et Rhizoma has achieved good clinical efficacy.According to the original records of traditional Chinese Medicine classics and by combining the clinical medication experience,Professor LIN Chang-Song proposed that the dosage of Glycyrrhizae Radix et Rhizoma should be enlarged,usually in the dose of 30-40 g.For the treatment of patients with Behcet's disease with obvious spleen and stomach deficiency syndrome,modified Baisai Prescription(composed of Glycyrrhizae Radix et Rhizoma Praeparata cum Melle,Codonopsis Radix,Pyrolae Herba,Pinelliae Rhizoma Praeparatum,Zingiberis Rhizoma Recens,Scutellariae Radix,Coptidis Rhizoma,etc.)is adopted and Glycyrrhizae Radix et Rhizoma Praeparata cum Melle should be used.For the treatment of patients with intense damp-heat type of Behcet's disease,Kouyan Prescription(composed of Glycyrrhizae Radix et Rhizoma,Scutellariae Radix,Coptidis Rhizoma,Pinelliae Rhizoma Praeparatum,Zingiberis Rhizoma Recens,Jujubae Fructus,Pseudostellariae Radix,Ganoderma Capense,Lophatheri Herba,Plantaginis Semen,etc.)is recommended and raw Glycyrrhizae Radix et Rhizoma should be adopted.Moreover,the importance of having proper eating and drinking,keeping regular living and avoiding to overwork to prevent the recurrence of Behcet's disease was stressed.
9.Diagnostic value of MRI quantitative enhancement parameters in patient with breast cancer and their relationships with HER-2 and Ang-2
Haiying HUANG ; Qiang HONG ; Jie XIE ; Feng ZHAO ; Song XUE
Journal of Practical Radiology 2024;40(5):733-736
Objective To explore the diagnostic value of MRI quantitative enhancement parameters in breast cancer and their rela-tionships with human epidermal growth factor receptor-2(HER-2)and angiopoietin-2(Ang-2).Methods A total of 80 patients with breast cancer were selected as the study objects.The MRI quantitative enhancement parameters[rate constant(Kep),extravascular extracellular space volume fraction(Ve),volume transfer constant(Ktrans)]of all patients with different clinical staging and lymph node metastasis were compared,respectively.The receiver operating characteristic(ROC)curve was used to analyze the diagnostic value of MRI quantitative enhancement parameters on the expression of HER-2 and Ang-2.Results Kep and Ktrans in stage Ⅱ group were significantly lower than those in stage Ⅲ and Ⅳ groups(F=6.322,F=6.676;P<0.05).Kep and Ktrans in lymph node metas-tasis group were significantly higher than those in lymph node non-metastasis group(t=4.265,t=4.557;P<0.05).Kep and Ktrans in HER-2 positive group were significantly higher than those in HER-2 negative group(t=3.988,t=4.616;P<0.05).ROC curve analysis showed that the area under the curve(AUC)of the combination of Kep and Ktrans for the diagnosis of HER-2 expression in breast cancer patients was 0.887,with specificity of 0.811 and sensitivity of 0.889,respectively.Kep and Ktrans in Ang-2 positive group were signifi-cantly higher than those in Ang-2 negative group(t=2.534,t=3.189;P<0.05).ROC curve analysis showed that the AUC of the com-bination of Kep and Ktrans for the diagnosis of Ang-2 expression in breast cancer patients was 0.767,with specificity of 0.867 and sensitivity of 0.569,respectively.Conclusion MRI quantitative enhancement parameters can improve the diagnostic value of breast cancer and the expression of HER-2 and Ang-2,which are beneficial to guide the selections of clinical therapeutic regimens.
10.Action mechanism of Huotu Jiji Pellets in the treatment of erectile dysfunction:An exploration based on network pharmacology and molecular docking
Xue-Qin CHEN ; Xuan ZHOU ; Hong-Ping SHEN ; Jia-Yi SONG ; Yun-Jie CHEN ; Yuan-Bin ZHANG ; Yi-Li CAI ; Yi YU ; Ya-Hua LIU
National Journal of Andrology 2024;30(3):241-248
Objective:To explore the potential action mechanism of Huotu Jiji Pellets(HJP)in the treatment of erectile dys-function(ED)based on network pharmacology and molecular docking.Methods:We identified the main effective compounds and active molecular targets of HJP from the database of Traditional Chinese Medicine Systems Pharmacology(TCMSP)and Integrative Pharmacology-Based Research Platform of Traditional Chinese Medicine(TCMIP)and the therapeutic target genes of ED from the data-bases of Genecards.Then we obtained the common targets of HJP and ED using the Venny software,constructed a protein-protein in-teraction(PPI)network of HJP acting on ED,and screened out the core targets with the Cytoscape software.Lastly we performed GO functional enrichment and KEGG pathway enrichment analyses of the core targets followed by molecular docking of HJP and the core targets using Chem3D and AutoDock Tools and QuickVina-W software.Results:A total of 64 effective compounds,822 drug-related targets,1 783 disease-related targets and 320 common targets were obtained in this study.PPI network analysis showed that the core targets of HJP for ED included ESR1,HSP90AA1,SRC,and STAT3.GO functional enrichment analysis indicated the involvement of the core targets in such biological processes as response to xenobiotic stimulus,positive regulation of kinase activity,and positive regu-lation of MAPK cascade.KEGG pathway enrichment analysis suggested that PI3K-Akt,apoptosis,MAPK,HIF-1,VEGF,autophagy and other signaling pathways may be related to the mechanism of HJP acting on ED.Molecular docking prediction exhibited a good doc-king activity of the key active molecules of HJP with the core targets.Conclusion:This study showed that HJP acted on ED through multi-components,multi-targets and multi-pathways,which has provided some evidence and reference for the clinical treatment and subsequent studies of the disease.

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