1.Research progress on pentacyclic triterpenoids in medicinal Ilex species and their pharmacological activities.
Yu-Ling LIU ; Yi-Ran WU ; Bao-Lin WANG ; Xiao-Wei SU ; Qiu-Juan CHEN ; Yi RAO ; Shi-Lin YANG ; Li-Ni HUO ; Hong-Wei GAO
China Journal of Chinese Materia Medica 2025;50(12):3252-3266
Traditional Chinese medicine(TCM) capable of clearing heat and removing toxin is most commonly used in clinical practice and has the effect of removing fire-heat and toxin. Studies have shown that most of the Ilex plants have the effect of clearing heat and removing toxin, among which the varieties of I. cornuta, I. pubescens, I. rotunda, I. latifolia, and I. chinensis are most widely used. These plants generally contain triterpenoids and their glycosides, alkaloids, flavonoids, phenylpropanoids, and other chemical components, especially pentacyclic triterpenoids. According to their skeletons, pentacyclic triterpenoids can be divided into the oleanane type, the ursane type, the lupinane type, etc. Among them, ursane-type components are the most abundant, and 136 species have been found so far. These components have been proved to have pharmacological effects such as anti-inflammatory, anti-tumor, hypolipidemic, anti-thrombosis, cardiomyocyte-protective, antibacterial, and hepatoprotective effects. Therefore, this paper systematically reviews the domestic and foreign literature on Ilex plants with a focus on the research progress on pentacyclic triterpenoids and their pharmacological activities, aiming to provide reference for the development of TCM resources with the effect of clearing heat and removing toxin.
Ilex/chemistry*
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Plants, Medicinal/chemistry*
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Pentacyclic Triterpenes/pharmacology*
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Medicine, Chinese Traditional
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Drugs, Chinese Herbal/pharmacology*
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Humans
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Animals
2.Enzalutamide and olaparib synergistically suppress castration-resistant prostate cancer progression by promoting apoptosis through inhibiting nonhomologous end joining pathway.
Hui-Yu DONG ; Pan ZANG ; Mei-Ling BAO ; Tian-Ren ZHOU ; Chen-Bo NI ; Lei DING ; Xu-Song ZHAO ; Jie LI ; Chao LIANG
Asian Journal of Andrology 2023;25(6):687-694
Recent studies revealed the relationship among homologous recombination repair (HRR), androgen receptor (AR), and poly(adenosine diphosphate-ribose) polymerase (PARP); however, the synergy between anti-androgen enzalutamide (ENZ) and PARP inhibitor olaparib (OLA) remains unclear. Here, we showed that the synergistic effect of ENZ and OLA significantly reduced proliferation and induced apoptosis in AR-positive prostate cancer cell lines. Next-generation sequencing followed by Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analyses revealed the significant effects of ENZ plus OLA on nonhomologous end joining (NHEJ) and apoptosis pathways. ENZ combined with OLA synergistically inhibited the NHEJ pathway by repressing DNA-dependent protein kinase catalytic subunit (DNA-PKcs) and X-ray repair cross complementing 4 (XRCC4). Moreover, our data showed that ENZ could enhance the response of prostate cancer cells to the combination therapy by reversing the anti-apoptotic effect of OLA through the downregulation of anti-apoptotic gene insulin-like growth factor 1 receptor ( IGF1R ) and the upregulation of pro-apoptotic gene death-associated protein kinase 1 ( DAPK1 ). Collectively, our results suggested that ENZ combined with OLA can promote prostate cancer cell apoptosis by multiple pathways other than inducing HRR defects, providing evidence for the combined use of ENZ and OLA in prostate cancer regardless of HRR gene mutation status.
Male
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Humans
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Prostatic Neoplasms, Castration-Resistant/genetics*
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Drug Resistance, Neoplasm/genetics*
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Cell Line, Tumor
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Receptors, Androgen/genetics*
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Nitriles
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Apoptosis
3. Mechanisms of catapol inhibiting differentiation and glycolysis of Thl7 cells through MiR-143-3p
Mei-Yu SHEN ; Qiu-Ni RONG ; Yu-Xi DI ; Feng-Xiang TIAN ; Ming-Fei ZHANG ; Xiang WANG ; Bao-Ping JIANG ; Ling-Ling ZHOU
Chinese Pharmacological Bulletin 2022;38(7):1072-1081
Aim To investigate the mechanism of eata- pol (CAT) inhibiting differentiation and glyeolysis of Thl7 eel Is through miR-143-3p.Method The peripheral hloorl CD4 ∗ T eells of HA patients were obtained to deteet the expression of miR-143-3p and the mRNA levels of key glycolytic enzymes, ineluding glucose transporter 1 ( Glutl ) , hexokinase 2 ( HK2 ) , pyruvate kinase 2 (PKM2) , laetate dehydrogenase A ( LDHA).The differentiation of Thl7 eells was induced in vitro, and the ShRNA/lentivirus was applied to achieve the overexpression or knockdown of miR- 143-3 p.Un-transfected eells were divided into control group and CAT group (20, 40, 80 mg • L 1 ) , and transfected eells were divided into four groups: negative control group, miR-143-3p inhibitor group, miR- 143-3p mimies group, miR-143-3p inhibitor + CAT group.The percentage of Thl7 eells was deteeted by flow cytometry, and the level of IL-17A was detected by EL1SA.Quantitative real-time PCR was used to detect the mRNA expression of miR-143-3p and key glycolytic enzymes, and the levels of pyruvate and lactate were also detected.Results The mRNA expression of miR-143-3p in RA peripheral blood CD4 ∗ T cells was negatively correlated with disease severity ( DAS28 ) , transcription factor ROR-yt, and the key glycolytic enzymes Glutl/HK2/LDHA.Compared with negative control group, the down-expression of miR-143-3p markedly elevated the mRNA expression of ROR-yt, Glutl, HK2, LDHA, and the levels of IL-17A, pyruvate, lactate.Catalpol groups significantly up-regula- ted the expression of miR-143-3p, decreased the mRNA expression of HK2/LDHA and the levels of pvru- vate/lactate, and inhibited Thl7 cells differentiation.Compared with miR - 1 4 3 - 3 p inhibitor group , catapol could significantly inhibit the abnormal up-regulated of HK2/LDHA mRNA relative expression, pyruvate/lactate levels and the abnormal differentiation of Thl7 eells.Conclusion MiR-143-3p inhibits the differentiation and glycolysis of Thl7 cells.Catalpol could sup-press the glycolysis and differentiation of Thl7 eells by regulating mill-143-3p.
4. The antichlamydial activity of 1, 2-disubstituted pyrrole derivatives in vitro
Shun-Xin XU ; Wen-Xia XIE ; Min NI ; Zi-Yi LIU ; Xiao-Feng BAO ; Ling-Yan LIU
Chinese Pharmacological Bulletin 2021;37(7):929-934
Aim To evaluate the antichlamydial activity of our previously synthesized sixteen 1, 2-disubstituted pyrroles in vitro, providing candidate for the development of novel agents against Chlamydia. Methods Firstly, the inhibitory effect of compounds on the generation of infectious progeny EBs at different concentrations was analyzed for Chlamydia trachomatis L2 (Ct L2), C. muridarum (Nigg II strain, known as MoPn) and C. pneumonia (Cpn AR39). The IC
5.Clinical significance of HLA-A, -B, -C, -DRB1, -DQB1 haplotype gene frequencies.
Lu Yao CHEN ; Yang LI ; Teng Teng ZHANG ; Xiao Jing BAO ; Xiao Ni YUAN ; Ying LI ; Ling Jie LI ; Tian Jie YANG ; Jun HE
Chinese Journal of Hematology 2019;40(12):1026-1030
Objective: To analyze family-based haplotype frequencies of HLA-A, -B, -C, -DRB1 and -DQB1 genes and their clinical significance. Methods: The data of HLA genotyping in 3568 families undergoing related haploidentical transplantation between 2012 and 2017 at the First Affiliated Hospital of Soochow University were retrospectively evaluated. The HLA genotyping was performed by PCR amplification with sequence-based typing (PCR-SBT) and sequence-specific oligonucleotide probe (PCR-SSOP) methods. The family genetic analysis and haplotype frequencies were also investigated. Results: All the families were divided into 3 groups, including group1 of 1 422 entire families; group2 of 1 310 patients and either of their parents or one of their children; group3 of 836 patients and their HLA≥5/10 matched sibling donors. In the haplotypes with frequencies greater than 0.1% in group1+ group2, the frequency of A*11∶01-B*40∶01-C*03∶04-DRB1*11∶01-DQB1*03∶01, A*02∶07-B*51∶01-C*14∶02-DRB1*09:01-DQB1*03∶03 were significantly different between group1 and group2 (P=0.029, 0.033) . The frequency of A*11∶01-B*46∶01-C*01∶02∶01G-DRB1*09∶01-DQB1*03∶03 was significantly different between group1 and group3 (P=0.035) . The frequency of A*02∶01-B*40∶01-C*07∶02-DRB1*09∶01-DQB1*03∶03 was significantly different between group1 and group2 (P=0.034) , or group1 and group3 (P=0.034) . The frequency of A*24∶02-B*13∶01-C*03∶04-DRB1*12∶02-DQB1*03:01 was significantly different between group2 and group3 (P=0.046) . Conclusion: In this study, we summarize the prevalence of haplotype frequencies in terms of HLA-A, -B, -C, -DRB1 and-DQB1. Based on the database of family haplotype analysis, patients and donor candidates are sorted with matched HLA genotype while unmatched HLA haplotype. Even in patients without entire family information, HLA haplotype analysis assists in choosing the optimal related or unrelated donors.
Alleles
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Child
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Gene Frequency
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HLA-A Antigens
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HLA-B Antigens
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HLA-C Antigens
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HLA-DQ beta-Chains
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HLA-DRB1 Chains
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Haplotypes
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Humans
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Retrospective Studies
6.Expert consensus statement on Pudilan Xiaoyan Oral Liquid in clinical practice.
Lian-Xin WANG ; Qing MIAO ; Yan-Ming XIE ; Da-Can CHEN ; Su-Lun SUN ; Hong-Chun ZHANG ; Zhong-Wu JIA ; Tie-Nan LI ; Jia ZHU ; Li-Qing SHI ; Ping SONG ; Feng GAO ; Bao-Lin WEI ; Cui-Ling FENG ; Yi-Qing QU ; Ni-Ni QU ; Xue-Feng YU ; Nian-Zhi ZHANG ; Xue-Qing YU
China Journal of Chinese Materia Medica 2019;44(24):5277-5281
Pudilan Xiaoyan Oral Liquid has effects in clearing away heat and detoxifying,and is used to treat pharynx and throat swelling caused by the syndrome of excessive heat and toxin accumulation. Its efficacy is to relieve swelling and pain( redness,swelling and hot pain). It is included in the Chinese Pharmacopoeia of 2015 Edition,and has been listed in provincial health insurance directories of Shaanxi,Jiangsu,Liaoning,Hunan,Tianjin,Xinjiang and Hebei. It has been recommended by health departments of Beijing,Chongqing and other provinces as a preferred drug for the prevention and treatment of H1 N1 and HFMD,and listed in the diagnosis and Treatment Guide of HFMD by the Ministry of Health,the Clinical Application Guide of Chinese Patent Medicine edited by the Lung Department Disease Branch of China Association of Chinese Medicine,and the Clinical Practice Guide of Single Administration/Combined Administration of Antibiotics in Treatment of Common Infectious Diseases by China Association of Chinese Medicine. To further improve the clinician's understanding of drugs and better guide the rational clinical application,we invited front-line clinical experts from respiratory department,infectious department and dermatology of traditional Chinese and Western medicine to develop and compile the expert consensus. The consensus fully considered the clinical evidence and the expert clinical experience to give recommendations for clinical problems with evidence support and consensus suggestions for clinical problems without evidence support by the nominal group method.This consensus is based on clinical research evidence and expert experience in a simple and clear format,which provides a preliminary reference for the clinical use of the drug.
China
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Consensus
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Drugs, Chinese Herbal/therapeutic use*
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Humans
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Medicine, Chinese Traditional
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Nonprescription Drugs
7.Efficacy and Safety of Teriflunomide in Chinese Patients with Relapsing Forms of Multiple Sclerosis: A Subgroup Analysis of the Phase 3 TOWER Study.
Wei QIU ; De-Hui HUANG ; Shi-Fang HOU ; Mei-Ni ZHANG ; Tao JIN ; Hui-Qing DONG ; Hua PENG ; Chao-Dong ZHANG ; Gang ZHAO ; Yi-Ning HUANG ; Dong ZHOU ; Wei-Ping WU ; Bao-Jun WANG ; Ji-Mei LI ; Xing-Hu ZHANG ; Yan CHENG ; Hai-Feng LI ; Ling LI ; Chuan-Zhen LU ; Xu ZHANG ; Bi-Tao BU ; Wan-Li DONG ; Dong-Sheng FAN ; Xue-Qiang HU ; Xian-Hao XU ; TOWER Trial Chinese Group
Chinese Medical Journal 2018;131(23):2776-2784
Background:
Disease-modifying therapy is the standard treatment for patients with multiple sclerosis (MS) in remission. The primary objective of the current analysis was to assess the efficacy and safety of two teriflunomide doses (7 mg and 14 mg) in the subgroup of Chinese patients with relapsing MS included in the TOWER study.
Methods:
TOWER was a multicenter, multinational, randomized, double-blind, parallel-group (three groups), placebo-controlled study. This subgroup analysis includes 148 Chinese patients randomized to receive either teriflunomide 7 mg (n = 51), teriflunomide 14 mg (n = 43), or placebo (n = 54).
Results:
Of the 148 patients in the intent-to-treat population, adjusted annualized relapse rates were 0.63 (95% confidence interval [CI]: 0.44, 0.92) in the placebo group, 0.48 (95% CI: 0.33, 0.70) in the teriflunomide 7 mg group, and 0.18 (95% CI: 0.09, 0.36) in the teriflunomide 14 mg group; this corresponded to a significant relative risk reduction in the teriflunomide 14 mg group versus placebo (-71.2%, P = 0.0012). Teriflunomide 14 mg also tended to reduce 12-week confirmed disability worsening by 68.1% compared with placebo (hazard ratio: 0.319, P = 0.1194). There were no differences across all treatment groups in the proportion of patients with treatment-emergent adverse events (TEAEs; 72.2% in the placebo group, 74.5% in the teriflunomide 7 mg group, and 69.8% in the teriflunomide 14 mg group); corresponding proportions for serious adverse events were 11.1%, 3.9%, and 11.6%, respectively. The most frequently reported TEAEs with teriflunomide versus placebo were neutropenia, increased alanine aminotransferase, and hair thinning.
Conclusions:
Teriflunomide was as effective and safe in the Chinese subpopulation as it was in the overall population of patients in the TOWER trial. Teriflunomide has the potential to meet unmet medical needs for MS patients in China.
Trial Registration
ClinicalTrials.gov, NCT00751881; https://clinicaltrials.gov/ct2/show/NCT00751881?term=NCT00751881&rank=1.
China
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Crotonates
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administration & dosage
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adverse effects
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therapeutic use
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Double-Blind Method
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Drug Administration Schedule
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Humans
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Immunosuppressive Agents
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administration & dosage
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adverse effects
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therapeutic use
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Multicenter Studies as Topic
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Multiple Sclerosis
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drug therapy
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metabolism
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Proportional Hazards Models
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Toluidines
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administration & dosage
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adverse effects
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therapeutic use
8.Vascular Endothelial Growth Factor and Cluster of Differentiation 34 for Assessment of Perioperative Bleeding Risk in Gastric Cancer Patients.
Mu-Qing HE ; Mu-Qun HE ; Jian-Feng WANG ; Bao-Ling ZHU ; Ni SUN ; Xiao-Hai ZHOU ; Rong-Xin YAO
Chinese Medical Journal 2016;129(16):1950-1954
BACKGROUNDAngiogenesis is the formation of new blood vessels to supply nutrients to tumors. Vascular endothelial growth factor (VEGF) and cluster of differentiation 34 (CD34) are important signaling proteins involved in angiogenesis. Many studies have demonstrated that VEGF and CD34 are related to tumor progression. This study focused on the relationship between VEGF, CD34, and perioperative hemorrhage in patients with gastric cancer.
METHODSTo observe the relationship between VEGF and CD34, we tracked 112 patients with advanced gastric cancer for 5 years to assess factors related to hemorrhage, using immunohistochemistry. The results were subjected to statistical analysis using a 2 × 2 contingency table, logistic regression, and receiver operating characteristic (ROC) test.
RESULTSThe concentrations of VEGF and CD34 were critically correlated with perioperative hemorrhage and neural invasion in patients with gastric cancer (P < 0.05). Expression of VEGF and CD34 was related (P < 0.05, χ2 = 6.834). VEGF and CD34 co-expression strongly increased the risk of preoperative bleeding (area under the ROC curve >0.7, P < 0.05).
CONCLUSIONSExpression of VEGF and CD34 was critically correlated with perioperative hemorrhage in gastric cancer patients. Co-expression of VEGF and CD34 could be an effective indicator for evaluating the risk of perioperative bleeding in gastric cancer patients.
Adult ; Aged ; Aged, 80 and over ; Antigens, CD34 ; metabolism ; Female ; Gastrointestinal Hemorrhage ; etiology ; metabolism ; Humans ; Immunohistochemistry ; Male ; Middle Aged ; Neovascularization, Pathologic ; complications ; metabolism ; Prognosis ; Retrospective Studies ; Risk Factors ; Stomach Neoplasms ; metabolism ; pathology ; surgery ; Vascular Endothelial Growth Factor A ; metabolism ; Young Adult
9.Efficacy of combined pranoprofen eye drops and artificial tears on the treatment of mild to moderate dry eye syndrome after trabbeculectomy
Guang-Ming, ZHAO ; Ping, ZHAO ; Bao-Ling, NI ; Zhong-Gang, YI ; Cheng, YANG ; Jing-Jing, ZHENG
International Eye Science 2015;(2):370-372
AlM:To evaluate the efficacy of combined pranoprofen eye drops and artificial tears on the treatment of mild to moderate dry eye syndrome after trabbeculectomy.METHODS:This prospective case control study included 63 cases (63 eyes) of patients with mild to moderate dry eye syndrome after trabbeculectomy in our hospital from November 2013 to June 2013. All subjects were randomly divided into two groups. Observation group was treated with combined pranoprofen eye drops and artificial tears and control group received simple artificial tears marking the eyes at 1, 2, 4wk. The patient's symptoms, signs, BUT, S▏t, and FL were observed before treatment and 1, 2, 4wk after treatment.RESULTS: After 2wk, the symptoms of observation group were improved, there was statistically significant difference (P<0. 05). FL difference of each group was statistically significant ( P<0. 05 ); After 4wk, symptoms and signs were improved. There was statistically significant difference ( P < 0. 05 ). The BUT of the observation group and corneal FL scores of two groups showed significant differences (P<0. 05). CONCLUSlON: Artificial tears joint pranoprofen eye drops has good curative effect in the treatment of mild to moderate dry eye syndrome after trabbeculectomy.
10.The characteristics of frequency distribution of KIR2DL1 alleles polymorphism and recognition HLA-C ligand in the Chinese Han population.
Miao WANG ; Jun HE ; Xiao-jing BAO ; Qiao-cheng QIU ; Yang LI ; Chao XU ; Xiao-ni YUAN ; Ling-jie LI
Chinese Journal of Hematology 2013;34(12):1038-1043
OBJECTIVETo find out the distributed characteristics of KIR2DL1 alleles frequencies and the recognition HLA-C ligand in the Chinese Han population.
METHODSThe 111 patients and 116 donors from CMDP were performed the KIR2DL1 high-resolution typing and KIR genotyping using sequence-based testing (SBT) and PCR-SSP methods.
RESULTSA total of 224 individuals with KIR2DL1 locus was predominantly observed and accounted for 98.68% (224/227). There were 3 different KIR2DL1 alleles, including KIR2DL1*00302, *00201 and *00401 alleles polymorphism. The most common phenotype observed were KIR2DL1*00302 (84.82%, 380/448), KIR2DL1*00201 (12.05%, 54/448) and KIR2DL1*00401(3.13%,14/448), present at allele genotype frequencies of 61.04%,6.22% and 1.58% respectively. The allele homozygotic types of KIR2DL1*00302 and KIR2DL1*00302 were the most frequent in 6 KIR2DL1 allele by high resolution typing. The allele heterozygous types of KIR2DL1*00302 and KIR2DL1*00401 presented statistically different in haplotypes A/A and B/x (P=0.001), and KIR2DL1*00401 lacked of all A/A haplotype. The KIR2DL1*00302 and KIR2DL1*00201 allele had significant positive associations between different KIR pairs of KIR2DS1, KIR2DL3, KIR2DS4 and KIR3DL1/S1 using linkage disequilibrium analysis (P<0.01), respectively. In the receptor-ligand of KIR/HLA model after allo-HSCT, KIR2DL1*00302 alleles correlated with their HLA-C2 group ligands. KIR2DL1*00302 and HLA-C*06:02 was the most common combination ligand model, but KIR2DL1*00302 and HLA-C*01:02 was the most frequent mismatch ligand model with the development of NK cell-induced alloreactivity, meanwhile there was statistically significant difference of frequency distribution (P<0.05).
CONCLUSIONThe KIR2DL1*00302 was the most frequent allele in Chinese Han population. The KIR2DL1 high resolution typing would be beneficial for predicting donor NK cells all activity after hematopoietic stem cell transplantation and selecting suitable donors.
Alleles ; Asian Continental Ancestry Group ; genetics ; Gene Frequency ; Genotype ; HLA-C Antigens ; genetics ; Haplotypes ; Histocompatibility Testing ; Humans ; Ligands ; Polymorphism, Genetic ; Receptors, KIR2DL1 ; genetics

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