1.Studies on chemical constituents possessing DNA cleavage activity
Kai XIAO ; Lijiang XUAN ; Yaming XU ; Donglu BAI
Chinese Traditional and Herbal Drugs 1994;0(03):-
Object To study the chemical structures and DNA cleavage activity of the water-soluble constituents from Polygonum bistorta L.Methods To isolate the constituents by reverse phase chromatography, and characterize their structures by the analysis of chemical property and spectral data.Results Ten compounds were isolated from the 60% acetone extract of the rhizoma from P.bistorta.Their structures were elucidated as gallic acid (Ⅰ), tryptophan (Ⅱ), 2, 6-dihydroy-bezoic acid (Ⅲ), (+)-catechin (Ⅳ), chlorogenic acid (Ⅴ), (-)-epicatechin-5-O-?-D-glucopyranoside (Ⅵ), (+)-catechin-7-O-?-D-glucopyranoside (Ⅶ), 1-(3-O-?-D-glucopyranosyl-4, 5-dihydroxy-phenyl)-ethanone (Ⅷ), (+)-catechin-5-O-?-D-glucopyranoside (Ⅸ) and (-)-epicatechin (Ⅹ), respectively.Conclusion Compounds Ⅱ, Ⅲ, Ⅴ-Ⅹ were isolated from the plant for the first time.Compounds Ⅰ, Ⅳ, Ⅵ, Ⅶ, Ⅸ, Ⅹ showed significant DNA cleavage activity.
2.Studies on water-soluble constituents in rhizome of Polygonum cuspidatum
Kai XIAO ; Lijiang XUAN ; Yaming XU ; Donglu BAI
Chinese Traditional and Herbal Drugs 1994;0(06):-
Object To study the chemical structures and bioactivity of the water-soluble constituents from Polygonum cuspidatum Sieb. et Zucc. Methods To isolate the constituents by reverse phase methods, and characterize their structures by the analysis of chemical property and spectral data. Results Six compounds were isolated from the 60% aqueous acetone extract from the rhizome of P. cuspidatum. Their structures were elucidated as reveratrol (Ⅰ); piceid (Ⅱ); 2, 3-dihydro-2-(4′-O-?-D-glucopyranosyl-3′-methoxy-phenyl)-3-hydroxymethyl-5-(3-hydroxypropyl)-7-methoxybenzofuran (Ⅲ); 2, 6-dimethoxy-p-hydroquinone-1-O-?-D-glucopyranoside (Ⅳ); 5, 7-dihydroxy-isobenzofuran (Ⅴ) and 5, 7-dihydroxy-isobenzofuran-7-O-?-D-glucopyranoside(Ⅵ), respectively. Conclusion Compounds Ⅲ-Ⅵ are isolated from the plant for the first time. Compounds Ⅰ-Ⅵ show no DNA cleavage activity. Compound Ⅱ exhibits weak cytotoxicity against two human cancer cell lines (KB and MCF-7) in vitro.
3.Model validation and evaluation of developmental toxicity of five drugs using zebrafish embryos
Bingjie XU ; Lijiang ZHANG ; Chunqi LI ; Yaoxian XUAN
Chinese Pharmacological Bulletin 2016;(1):74-78,79
Aim To explore the toxicity and safety of five kinds of known positive drugs, cyclophosphamide, acetyl salicylic acid, tetracycline hydrochloride, dexa-methasone acetate and azacitidine, using zebrafish em-bryos. Methods We selected normally developed 4 hpf zygote, and used water bath infecting method to add the drug to the artificial seawater. Each drug had five concentrating groups, a separate control group and solvent control group. We observed the dead zebrafish embryos after 120 hpf drugs, counted the number of deaths and deformities of zebrafish embryos, and cal-culated mortality abnormal rate, the median lethal con-centration (LC50 ), concentration for 50% of maximal effect (EC50 ), therapeutic index (TI) under 120 hpf condition. We also used the formula TI = LC50 / EC50 to calculate positive drug therapeutic index. Based on measured LC50 we calculated most nonlethal concentra-tion (MNLC) of each drug setting, namely 1 / 10 MN-LC, 1 / 3 MNLC, MNLC,LC10 four concentration, tha-lidomide as a positive control, vitamin C as a negative control, artificial seawater as control, 0. 5% DMSO as solvent control. Put in 28. 5 ℃ environment for 120 hours,embryo development was observed daily for de-velopmental state,mortality,deforming rate and abnor-mal condition. Results The result of five drugs LC50 in descending order: cyclophosphamide > azacitidine> tetracycline hydrochloride > acetylsalicylic acid >dexamethasone acetate. EC50 in descending order: cy-clophosphamide > tetracycline hydrochloride > azaciti-dine > acetylsalicylic acid > dexamethasone acetate. The TI values of cyclophosphamide, acetyl salicylic acid, tetracycline hydrochloride, dexamethasone ace-tate, azacitidine were 1. 92, 1. 11, 1. 05, 1. 44, 2. 99, respectively. Conclusion Zebrafish embryo model can be used in the preliminary evaluation of drugs, and the study of early developmental toxicity and safety.
4.Relationship analysis of urine RBC morphology between UF-100 and phase contrast microscope
Yun-Cheng XIA ; Xu-Guang ZANG ; Zhi-Lan LI ; Xiang-Qing XU ; Wen-Ling JIANG ; LIJIANG
Journal of Chinese Physician 2001;0(09):-
Objective To study the relationship of urine RBC morphology between UF-100 urine sediment analytic instrument andphase contrast microscope.Methods The UF-100 urine sediment analytic instrument to analyze 500 urine specimens and study the relation-ship of urine RBC morphology between urine sediment analytic instrument and phase contrast microscope.Results The according perceptionof Normocytic,Microcytic and Non-classified RBC between phase contrast microscope and UF-100 urine sediment analytic instrument RBC-info are 91.4%,94.4%,83.3% respectively,the according perception between phase contrast microscope and RBC-P70Fsc are 94.9%,95.7%,94.7% respectively,and the according perception between phase contrast microscope and RBC Fsc-DW are 84.4%,86.8%,90.5% respectively,the specificity of UF-100 and phase contrast microscope in glomerular hematuria and non-glomerular hematuria are84.3%,88.1% and 83.3%,87.9% respectively.Conclusion The results show that the UF-100 urine sediment analytic instrument issimply operating,fast and high accurate,and which can instruct clinical dignose,therapy and prognosis judgement.
5.Data mining and analysis of the rules of prescriptions in the treatment of epigastric pain in A Hundred Years of Traditional Chinese Medicine Clinicians in China
Di WU ; Zhengyu XU ; Yichen WANG ; Lijiang REN ; Ping WANG
International Journal of Traditional Chinese Medicine 2022;44(4):422-427
Objective:To analyze the prescriptions for the treatment for epigastric pain in A Hundred Years of Traditional Chinese Medicine Clinicians in China. Methods:The clinical medical records of well-known TCM doctors for the treatment of epigastric pain were included in the A Hundred Years of Traditional Chinese Medicine Clinicians in China. The database of clinical prescriptions and medicines was built, and the ancient and the Ancient and Modern Medical Records Cloud Platform (V 2.1) was applied and the evaluation of drug efficacy, sex, taste, and menstruation were conducted. Descriptive analysis, association rules, hierarchical clustering, and complex network analysis were applied in the rule of medication, drug pairs and core prescriptions. Results:Data was cleaned according to the inclusion and exclusion criteria, and 270 prescriptions were collected, involving 265 kinds of drugs, and the cumulative frequency of drug use was 3 249. The analysis showed that the drugs commonly used by famous traditional Chinese medicine doctors for the treatment of epigastric pain were mainly warm drugs, tast-balance drugs, and mildly cold drugs. The main flavors of medicines were pungent medicines, bitter medicines, sweet medicines, and effects were mainly drugs that regulate qi, clear heat, and invigorate the spleen. The frequency of drug meridians mainly belonged to spleen meridian, stomach meridian, lung meridian, liver meridian, heart meridian. The effects of the drug were mainly to dry dampness, reduce side effects, regulate qi, clear heat, invigorate spleen, and soften liver and analgesics. Association rule analysis found that the commonly used drug pairs were Pinellia- Tangerine Peel, Atractylodes Macrocephala- Poria, Poria- Tangerine Peel, Atractylodes- Tangerine Peel, Amomum tangerine Peel, Ochre- generation- Inula, Rhizoma Coptis- Evodia, and so on. Cluster analysis showed that Liujunzi Decoction, Zuojin Pill, and Shaoyao Gancao Decoction were mainly used. The drug complex network diagram showed that the core prescription of the drug is Xiangsha Liujunzi Decoction. Conclusion:The well-known TCM doctor focuses on strengthening the spleen and regulating qi, reconciling qi and blood, The treatment identified that the mutual warming and clearing, tonifying and deoppilation, and neutral are the main principles.
6.Discussion on the pathogenesis of "spleen deficiency and dampness accumulation" of colorectal polyps based on intestinal flora and glucose and lipid metabolism
Zhengyu XU ; Di WU ; Yichen WANG ; Qingqing ZHANG ; Lijiang REN ; Han WANG ; Ping WANG
International Journal of Traditional Chinese Medicine 2023;45(5):527-530
Intestinal flora imbalance and abnormal glucose and lipid metabolism are important risk factors and pathological mechanisms of colorectal polyps. "Spleen deficiency and dampness accumulation" is the core pathogenesis of colorectal polyps. The imbalance of intestinal flora is related to spleen deficiency, and the application of Chinese herbs for invigorating spleen is helpful to the recovery of intestinal flora balance. Abnormal glucose and lipid metabolism is related to dampness accumulation, and it is effective to treat it with bitter and spicy herbs or spleen-invigorating and dampness-eliminating herbs. The interaction between intestinal flora imbalance and abnormal glucose and lipid metabolism changes intestinal microenvironment, damages intestinal epithelial cells, causes abnormal proliferation of intestinal stem cells and leads to colorectal polyps, which is consistent with the pathogenesis of spleen deficiency and dampness accumulation in Traditional Chinese Medicine. Thus, we tried to explore the biological connotation of the pathogenesis of "spleen deficiency and dampness accumulation" of colorectal polyps from the perspective of the interaction of intestinal flora and glucose and lipid metabolism, in order to provide reference for identifying high-risk population and analyzing the therapeutic mechanism of compound prescription for invigorating spleen and removing dampness.
7.Analysis of prognosis and pregnancy outcomes of fertility-preserving treatment for patients with stage Ⅰa, grade 2 endometrial cancer
Yiqin WANG ; Rong ZHOU ; Lijiang XU ; Meng XIA ; Qun LU ; Guoli LIU ; Danhua SHEN ; Gang WANG ; Mian HE ; Jianliu WANG
Chinese Journal of Obstetrics and Gynecology 2020;55(5):327-332
Objective:To investigate the efficacy and pregnancy outcome of fertility-preserving treatment for patients with stage Ⅰa, grade 2 endometrial cancer (EC).Methods:Clinical data was retrospectively collected for EC or atypical endometrial hyperplasia (AEH) patients treated in Peking University People's Hospital, Foshan First People's Hospital of Guangdong Province and First Affiliated Hospital of Sun Yat-sen University, from 2010 to 2019. Inclusion criteria for fertility-preserving treatment included: (1) Age ≤45 years. (2) EC with histological differentiation of G 1, G 2 or endometrial AEH. (3) EC disease should be stage Ⅰa, confined to the endometrium without myometrial invasion, lymph node or extrauterine metastasis. Treatment regimen: patients were given oral progestin therapy and endometrial pathology was evaluated every three months. Patients were divided into three groups as G 2 EC group, G 1 EC group and AEH group based on the histological differentiation. Oncological and pregnancy outcomes were compared among them. Results:(1) Totally 57 eligible patients were included in this study, including 11 cases with G 2 EC, 22 cases with G 1 EC, and 24 cases with AEH. (2) Oncological outcome: among the three groups of G 2 EC, G 1 EC and AH, the complete remission rates (9/11, 91% and 96%, respectively) and recurrence rates (3/9, 30% and 22%, respectively) were not significantly different (all P>0.05). Median remission time was significantly longer in the G 2 EC group than those in the other two groups (8, 6 and 4 months; P=0.046). Among 9 G 2 EC patients who recurred after complete remission, three patients relapsed at 7, 18 and 53 months, respectively. All 3 patients chose fertility-sparing treatment again, and all achieved complete remission after retreatment. (3) Pregnancy outcome: among the three groups, the assisted reproduction technology rates (4/8, 5/18 and 36%, respectively) and pregnancy rates (6/8, 5/18 and 36%, respectively) had no significant difference ( P>0.05). However, time interval to pregnancy was shorter in G 2 EC patientsthan the other two groups (4, 9 and 22 months, respectively; P=0.006). Conclusions:Fertility-preserving treatment for patients with stageⅠa, G 2 endometrial cancer, may obtain a relatively high remission rate and an acceptable pregnancy rate. However, further exploration is needed due to the limited number of cases.
8.Tissue distribution and analysis of human umbilical cord mesenchymal stem cells in NOG mice following single intravenous injection
Zhichao YE ; Guoyu CHEN ; Ruolang PAN ; Yuhua SHI ; Liqiang GU ; Lijuan XIA ; Xiaobo LIN ; Qiang ZHANG ; Shasha XU ; Jinjin SHAO ; Lijiang ZHANG
Acta Laboratorium Animalis Scientia Sinica 2023;31(12):1573-1580
Objective To establish a quantitative polymerase chain reaction(PCR)method for the analysis of human-derived SRY DNA in mouse tissues,and to study the tissue distribution of human umbilical cord mesenchymal stem cells(HUCMSCs)in immunodeficient NOG mice after a single intravenous injection.Methods We established a quantitative PCR method for the analysis of human SRY DNA in mouse tissues,and validated the standard curve,linear range,accuracy,precision,and stability.Thirty-six NOG mice(18 male,18 female)were administered 3.5×107 HUCMSCs/kg by single intravenous injection.Six mice were then anesthetized and dissected after blood collection(EDTA anticoagulation)at 6,12,24,and 72 h,and at 1 and 2 weeks,respectively.DNA was extracted from lung,kidney,heart,liver,brain,spinal cord,stomach,small intestine,fat,skin,spleen,testis,uterus,and ovary tissues,and the distribution of HUCMSCs in each tissue was determined by the validated quantitative PCR method for detecting the human-derived SRY gene in mouse tissues.In addition,18 NOG mice(9 male,9 female)were divided into control(n = 6)and treatment groups(n = 12)injected intravenously with 0.9%sodium chloride and 3.5×107 cells/kg,respectively.Acute toxic reactions were observed during the administration period,and four animals were dissected at 72 h and at 2 and 4 weeks after administration to observe the gross organs.Mitochondrial protein expression was detected in paraffin sections of lung tissues by immunohistochemistry to analyze the colonization of HUCMSCs in lung tissues.Results The established RT-qPCR method for human-derived SRY DNA in mouse tissues met the validation criteria for each index.After a single intravenous injection in NOG mice,HUCMSCs were mainly distributed in the lungs and blood within 1 week after administration,with higher concentrations in lung tissues than in blood.The concentrations of HUCMSCs in lung tissue and blood remained relatively stable within 6~24 h and 6~72 h,respectively,and then decreased over time.The distribution of HUCMSCs in other tissues was not measured at all sampling points.The colonization result showed that HUCMSCs were detected in lungs 72 h after intravenous injection,but not at 2 and 4 weeks.No obvious acute toxicity was observed in NOG mice after single intravenous administration of HUCMSCs.Conclusions The above method for analyzing the distribution of HUCMSCs in mouse tissue is reliable and feasible.HUCMSCs were mainly distributed in lung and blood in NOG mice within 1 week after a single intravenous injection,and mainly colonized lung tissue at 72 h.A single intravenous administration of HUCMSCs has a good safety profile.
9.Mechanism of action and clinical research progress of iguratimod in connective tissue diseases
Xiaorong YANG ; Shuhong ZHOU ; Lijiang GUO ; Ying CHEN ; Yingying JI ; Lijie XU
China Pharmacy 2024;35(5):629-634
As a new type of immunosuppressant,iguratimod can mediate the anti-inflammatory signaling pathway by inhibiting the proliferation of inflammatory cells and reducing the release of inflammatory cytokines, and play the role of anti-inflammatory. It can affect the proliferation of immune cells and the expression of immune factors,reduce the production and deposition of immune complexes in the body,and play the role of immune regulation. It can regulate bone metabolism by mediating signaling pathways such as Wnt/β-catenin,Toll-like receptor 4/nuclear factor-κB and osteoprotegerin/nuclear factor-κB receptor activating factor ligand, and play a role in bone protection. It can inhibit pulmonary fibrosis by inhibiting the expression of transforming growth factor β1/ Smad2/3 signaling pathway,tumor necrosis factor-α,interleukin-1,interleukin-6,matrix metalloproteinase-9 and other inflammatory cytokines in lung tissue,and inhibiting the expression of collagen and fibronectin. Its efficacy and safety have been confirmed in the clinical application of rheumatoid arthritis and primary Sjogren syndrome and included in the diagnosis and treatment of the disease. It has also shown good efficacy in the clinical application of other connective tissue diseases such as systemic lupus erythematosus and ankylosing spondylitis,and no obvious safety risks have been found.
10.Antibiotics-mediated intestinal microbiome perturbation aggravates tacrolimus-induced glucose disorders in mice.
Yuqiu HAN ; Xiangyang JIANG ; Qi LING ; Li WU ; Pin WU ; Ruiqi TANG ; Xiaowei XU ; Meifang YANG ; Lijiang ZHANG ; Weiwei ZHU ; Baohong WANG ; Lanjuan LI
Frontiers of Medicine 2019;13(4):471-481
Both immunosuppressants and antibiotics (ABX) are indispensable for transplant patients. However, the former increases the risk of new-onset diabetes, whereas the latter impacts intestinal microbiota (IM). It is still unclear whether and how the interaction between immunosuppressants and ABX alters the IM and thus leads to glucose metabolism disorders. This study examined the alterations of glucose and lipid metabolism and IM in mice exposed to tacrolimus (TAC) with or without ABX. We found that ABX further aggravated TAC-induced glucose tolerance and increased insulin secretion. Combined treatment resulted in exacerbated lipid accumulation in the liver. TAC-altered microbial community was further amplified by ABX administration, as characterized by reductions in phylum Firmicutes, family Lachnospiraceae, and genus Coprococcus. Analyses based on the metagenomic profiles revealed that ABX augmented the effect of TAC on microbial metabolic function mostly related to lipid metabolism. The altered components of gut microbiome and predicted microbial functional profiles showed significant correlation with hepatic lipid accumulation and glucose disorders. In conclusion, ABX aggravated the effect of TAC on the microbiome and its metabolic capacities, which might contribute to hepatic lipid accumulation and glucose disorders. These findings suggest that the ABX-altered microbiome can amplify the diabetogenic effect of TAC and could be a novel therapeutic target for patients.