Table of Content

Volume 26 Issue 3
26 March 2021

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Salvianolic acid A activates AMPK and SIRT1 to reduce palmitic acid-induced lipotoxicity in hepatocyte

ZHAO Fangqing, YANG Wenwen, YIN Yujie, ZHANG Bin, WANG Bangcai, DOU Xiaobing, LI Songtao, ZHU Linwensi

2021, 26(3):  241-249.  doi:10.12092/j.issn.1009-2501.2021.03.001

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AIM: To investigate the protective affect of salvianolic acid A on palmitic acid-induced lipotoxicity in hepatocyte and its potential molecular mechanism.  METHODS: The lipotoxicity model of AML12 hepatocytes induced by PA was established. Different concentrations of Sal A (20, 40, 80, 120 μmol/L) were intervened. The hepatocyte injury was detected by the Lactate dehydrogenase (LDH) method, the intracellular triglyceride (TG) content was detected by enzyme assay and the lipid droplets were observed by Bodipy staining, cell viability was detected by MTT, Intracellular reactive oxygen species (ROS) were detected by 2'eci'- dichlorofluorescein diacetate (DCFH-DA) and fluorescence microscope. Mitochondrial membrane potential was detected by rhodamine 123 and fluorescence microscope. The expression of phosphorylation of AMP-activated protein kinase (AMPK) protein and silent information regulator 1 (SIRT1) protein were observed by Western blot. RESULTS: Model of hepatocyte lipotoxicity was established after intervented for 12 h in vitro with PA (0.5 mmol/L). Different concentrations of Sal A could significantly reduce the lipid deposition and hepatocytes injury induced by PA (P<0.05), and the protective effect was dose-dependent. Secondly, Sal A could significantly improve cell mitochondrial membrane potential (P<0.01) and abate the ROS level of hepatocytes induced by PA (P<0.01). In addition, PA could significantly inhibit AMPK and SIRT1 protein expression (P<0.05). Salvianolic acid A can significantly up-regulate SIRT1 and AMPK protein expression (P<0.05). CONCLUSION: Sal A improves PA induced lipotoxicity in hepatocyte, AMPK and SIRT1 may be a potential molecular target.

Jolkinolide B inhibits the proliferation and metastasis of colon cancer cells via blocking PI3K/Akt/NF-κB pathway

CHEN Linjun, CHEN Wenbin

2021, 26(3):  250-257.  doi:10.12092/j.issn.1009-2501.2021.03.002

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AIM: To study the inhibitory effect and mechanism of Jolkinolide B (JB) on the proliferation and metastasis of colon cancer HT-29 cells. METHODS: HT-29 cells were treated with different concentrations of JB, the cell proliferation rate was detected by MTT method, the cell clone formation rate was detected by plate cloning experiment, the cell cycle change was detected by flow cytometry, the cell migration ability was analyzed by wound healing assay, the cell invasion ability was studied by Transwell assay, E-cadherin, N-cadherin, vimentin, Snail1, Snail2, matrix metalloproteinase (MMP)-2 and MMP-9 protein expression levels were detected by immunofluorescence and Western blotting, and p-PI3K, PI3K, p-Akt, Akt, NF-κB P65and p-NF-κB P65 protein expression levels were detected by Western blotting. HT-29 cells were treated with 100 μg/L IGF-1 and 100 μg/L IGF-1+20 μmol/L JB, respectively. The expression of PI3K/Akt/NF-κB pathway related proteins was detected by Western blotting. RESULTS: JB inhibited the proliferation of HT-29 cells in a concentration-dependent manner, with an IC50 of 52.68 μmol/L for 24 hours; JB decreased the clone formation rate of HT-29 cells in a concentration-dependent manner (P<0.05); compared with the control group, the G0/G1 phase ratio of HT-29 cells treated with JB was significantly increased, while the S phase ratio was significantly decreased (P<0.05); JB could significantly inhibit the migration and invasion of HT-29 cells in vitro (P<0.05); the E-cadherin protein level of HT-29 cells treated with JB was increased, and the expression levels of N-cadherin, vimentin, Snail1, Snail2, MMP-2, MMP-9, p-PI3K, p-Akt, p-NF-κB P65 protein were significantly decreased (P<0.05). The expression of p-PI3K, p-Akt, p-NF-κB P65 in IGF-1+JB group was significantly lower than that in IGF-1 group (P<0.05). CONCLUSION: JB can inhibit the proliferation of HT-29 cells in vitro, induce cell arrest in the G0/G1 phase, inhibit the migration and invasion of HT-29, regulate the epithelial mesenchymal transition (EMT) and MMPs, and its mechanism may be related to the blocking of PI3K/Akt/NF-κB pathway.

Segmental absorption of helicid in rat everted intestinal sac model: A preliminary study

WANG Ping, SHEN Jie, CHU Jiru, GUO Nan, XIE Haitang, ZHAN Cuijiao, WANG Changmao, YANG Bin, ZHENG Dandan, HU Rongfeng, JIA Yuanwei

2021, 26(3):  258-263.  doi:10.12092/j.issn.1009-2501.2021.03.003

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AIM: To investigate the absorption of helicid in different segments of intestine based on rat everted intestine sac model.  METHODS: To establish a high-performance liquid chromatography method for simultaneous determination of helicid and its metabolite. Krebs-ringer solution containing helicid was added to everted intestine sacs of different segments (duodenum, Jejunum, ileum and colon). Drug concentration in sacs was determined at different time points (5, 10, 15, 30, 45, 60, 75, 90 min). Adsorptions of helicid in four intestinal segments were compared. RESULTS: This high-performance liquid chromatography was successfully applied to the simultaneous determination of helicid and its metabolite. Absorption of helicid was rapid and time-dependent. The absorption and metabolism of helicid in duodenum segment were higher than these in other segments. CONCLUSION: The duodenum segment is the main site of segmental absorption and metabolism of helicid. This is the first report on intestinal segment metabolism of helicid.

Protective effect of hypoxia inducible factor-1α on intestinal mucosal barrier in sepsis

HE Rui, TENG Wenbin, YAO Liuxu, SHAN Yue, ZHU Shengmei, LI Yuhong

2021, 26(3):  264-270.  doi:10.12092/j.issn.1009-2501.2021.03.004

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AIM: To investigate the effect and mechanism of hypoxia inducible factor-1α on intestinal mucosal barrier in sepsis.  METHODS: SD rats were randomly divided into 4 groups: sham group, sepsis group, sepsis+HIF-1α stimulant (sepsis+DMOG group), sepsis+HIF-1α inhibitor (sepsis+Bay87-2243 group), 6 rats in each group. Sepsis model was established by cecal ligation and perforation (CLP). The levels of inflammatory markers IL-1β, IL-6, TNF-α, oxidative stress markers MDA and antioxidant factors SOD and CAT were detected by ELISA and the expression of HIF-1α in intestinal mucosa was detected by Western blot. The pathological damage of intestinal mucosa was detected by HE staining. RESULTS: Inflammatory factors, oxidative stress factors and HIF-1α were significantly up-regulated in septic rats (P<0.05). The contents of IL-1β, IL-6, TNF-α and MDA in plasma were significantly decreased by intraperitoneal injection of DMOG (P<0.05); the levels of SOD and CAT in plasma were increased (P<0.05), HIF-1α was up-regulated (P<0.05), and the pathological damage of intestinal mucosa was alleviated, with decreased Chiu's score (P<0.05). Oral administration of Bay87-2243 gave the opposite result. CONCLUSION: HIF-1α has a protective effect on intestinal mucosal injury in sepsis. The mechanism may be related to the alleviation of inflammatory response and inhibition of oxidative stress.

Distribution of deuterosuccinylcholine chloride in rats determined by UPLC-MS/MS method

WANG Xiangyi, SHENG Jie, WANG Xiu, GUO Yan, CHEN Zhiwu

2021, 26(3):  271-277.  doi:10.12092/j.issn.1009-2501.2021.03.005

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AIM: To establish an ultra-performance liquid chromatography-mass spectrometry (UPLC-MS/MS) method to determine the distribution of deuterosuccinylcholine chloride (2H-Suc) in rats.  METHODS: After subcutaneous injection of 2H-Suc for 4 hours, contents of 2H-Suc in serum and related organs were determined by UPLC-MS/MS. A Luna NH2 column (2 mm×100 mm, 3 μm) was used for chromatography assay, the mobile phase was 0.1% formic acid aqueous solution-acetonitrile isolution, the flow rate was 0.2 mL/min; an electrospray ionization source was used to measure 2H-Suc in multi-reaction monitoring mode via positive ionization; the linear relationship, detection limit, accuracy and precision, recovery rate, matrix effect and stability of this method were investigated. RESULTS: The detection limit of Suc was 0.04 ng/mL in serum and 0.05 ng/mL in renal tissue, respectively; range of linear relationship was 0.3-100 ng/mL in serum and 0.5-100 ng/mL in renal tissue; intraday and interday precision and accuracy were less than 15%, the recovery was between 85.30%-96.76%, and there was no obvious matrix effect in the treated samples; 2H-Suc was detected in serum, heart, liver, kidney and other organs of rats subjected to subcutaneous injection of 2H-suc for 4 h, and the highest content was found in kidney. CONCLUSION: UPLC-MS /MS analysis is an effective and reliable method for detecting 2H-Suc in rats. Heart, liver, kidney and other tissues are main organs distributed with 2H-Suc and its content in the kidney is the highest in rat. 

Correlation between soluble ST2 and coronary artery complex lesions and their severity

FANG Qiujue, WANG Zhaojun, YUAN Wei, DING Shu, WANG Zhongqun

2021, 26(3):  278-284.  doi:10.12092/j.issn.1009-2501.2021.03.006

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AIM: To investigate the relationship between serum soluble growth stimulation expressed gene 2 protein(sST2) level and coronary artery complex lesions and their severity.  METHODS: A total of 430 patients, who were sequentially admitted to hospital for selective coronary artery angiography, were divided into control group (non-coronary heart disease group, 136 patients), simple lesions group of coronary heart disease (86 patients), complex lesions group (208 patients). To quantitative evaluate the complexity of coronary artery lesions, Syntax scores were further performed on patients in complex lesions groups, including 139 patients in the low-risk group, 36 patients in the medium-risk group, and 33 patients in the high-risk group. The serum soluble ST2 level of each group of patients was tested by means of ELISA. Spearman correlation analysis was used for the correlation between the level of soluble ST2 and the severity of coronary complex lesions. RESULTS: In 430 subjects, the soluble ST2 level of all patients with coronary heart disease (including simple lesions and complex lesions) was significantly higher than that of the control group ［(3 449±1 250) vs. (2 743±961) pg/mL, P<0.001］; the sST2 levels of patients in the coronary artery simple lesions group, complex lesions low-risk group, medium-risk group and high-risk group were (3 200±1 406), (3 338±1 064), (3 728±1 228) and (4 261±1 235) pg/mL respectively, and the differences of sST2 levels among above four groups were statistically significant (P<0.001). Logistic regression analysis showed that sST2 was independently associated with coronary heart disease (OR=1.001, P<0.001) and sST2 was independently associated with the severity of coronary artery complex lesions (OR=1.001, P<0.001). Spearman-related analysis shows that the expression levels of sST2 are positively related to the severity of coronary artery lesions (rs: 0.543, P<0.001). The ROC curve showed that the area under the curve of sST2 for complex coronary lesions was AUC=0.726. CONCLUSION: Serum soluble ST2 level may be an important predictor of complicated coronary artery disease.

SUMO E3 ligase mediates androgen receptor transcription to promote tamoxifen resistance of breast cancer

SUN Hong, HOU Jialin, CAI Jiaqin, WEI Xiaoxia, ZHUANG Jie

2021, 26(3):  285-291.  doi:10.12092/j.issn.1009-2501.2021.03.007

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AIM: To investigate the mechanism of the involvement of SUMO-ylated Androgen receptor (AR) in tamoxifen resistance and the role of SUMO inhibitor ginkgolic acid in resistance.  METHODS: Real-Time PCR was used to detect AR mRNA levels in parental cells MCF-7W and drug-resistant cells MCF-7R, AR protein levels and SUMO levels in MCF-7W and MCF-7R cells was performed by western blot, and CB/IP was applied to detect AR interacts with SUMOE3 ligase PIAS1 and HSP27 in MCF-7R cell chromatin, the transcriptional activity of SUMO AR was also evaluated by the fluorescent reporter gene experiment, the CCK-8 method and the trypan blue exclusion method were used to detect cell viability and cell viability respectively. RESULTS: The mRNA and protein expression levels of AR in MCF-7R cells were significantly higher than those in MCF-7W cells (P<0.05), and there was highly SUMOylated AR in MCF-7R cells. Further research found that there had an obvious interaction between AR and SUMO E3 ligase PIAS1 and HSP27, that was, the SUMOylated AR was modified by E3 ligase. Moreover, androgen R1881 could enhance the transcriptional activity of the SUMOylated AR in a concentration-dependent manner. Compared with ginkgo acid alone, 10 μmol/L of ginkgolic acid combined with 10 μmol/L of enzalutamide treated MCF-7R cells for 3 days, the cell number was significantly reduced, and the number of cell death increased significantly (P<0.05). CONCLUSION: The resistance mechanism of tamoxifen may be due to the enhanced AR transcription and activity increased by the hyperactive SUMOylated AR, SUMO inhibitor ginkgolic acid combined with AR antagonist enzalutamide can be a new strategy for the treatment of tamoxifen resistance.

Metabolomics-based analysis of serum BAs in healthy Chinese adults taking acetaminophen

YANG Qian, YU Yunli, ZHANG Quanying

2021, 26(3):  292-298.  doi:10.12092/j.issn.1009-2501.2021.03.008

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AIM: To investigate the changes of bile acid metabolism in healthy adults after taking acetaminophen.  METHODS: Ten healthy subjects were enrolled and the serum samples of subjects before and after multiple administration of acetaminophen were collected. They were divided into pre-dose group (PD), fifth-dose gro-up (FD) and eighth-dose group (ED). A high performance liquid chromatography-tandem mass spectrometric method (HPLC-MS/MS) was used to quantify 15 target-edbile acid metabolites in human plasma, combined with principal component analysis (PCA), orthogonal partial least squares discriminant analysis (OPLS-DA)to investigate the changes of bile acid metabolism profile in healthy adults after taking acetaminophen. And the biochemical indicators of each group were detected. RESULTS: There was a change in the bile acid spectrum of human serum after taking acetaminophen. Compared with group PD, the taurochenodeoxycholicacid (TCDCA), glycocholicacid (GCA), glycochenodeoxycholic acid (GCDCA) and tauroursodeoxycholic acid (TUDCA) levels were significantly increased (P<0.05). There was no obvious changes in biochemical indicators. GCA and GCDCA were the most sen-sitive indicators of bile acid. CONCLUSION: GCA and GCDCA can be used as potential biomarkers of early liver injury caused by acetaminophen.

Bioequivalence of solifenacin succinate tablets in healthy Chinese volunteers

WANG Hui, CUI Chang, YANG Shuang, YAO An, WU Shuting, YANG Xiaoyan, YE Ling, ZOU Zhi, TANG Zhi, YANG Guoping, HUANG Jie, OUYANG Dongsheng

2021, 26(3):  299-304.  doi:10.12092/j.issn.1009-2501.2021.03.009

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AIM: To evaluate the bioequivalence of the test and reference preparations of solifenacin succinate tablets administered once orally under fasting and fed conditions in Chinese healthy volunteers.  METHODS: The study was designed as single-center, randomized, open, self-crossover and twenty four healthy volunteers were recruited respectively in fasting and fed conditions. Subjects were assigned to receive a single oral of the test or reference formulation per period at a dose of 10 mg. The plasma concentration of solifenacin was analyzed by LC-MS/MS. The major pharmacokinetic parameters were calculated by WinNonlin 7.0, then the bioequivalence was evaluated.RESULTS: The main pharmacokinetic parameters of a single oral solifenacin succinate under fasting condition for test and reference preparation were as follows: Cmax (13.99±3.34) and (13.27±3.20) ng/mL, AUC0-t (675.60±210.46) and (653.31±238.59) h·ng·mL-1, AUC0-∞(728.28±240.20) and (718.14±275.63) h·ng·mL-1, tmax (5.00±1.41) h and (4.98±1.07) h, t1/2 (39.19±9.29) and (42.44±12.66) h. The relative bioavailability was 105.06% for AUC0-t, 104.07% for AUC0-∞. The main pharmacokinetic parameters of a single oral solifenacin succinate under fed condition for test and reference preparation were as follows: Cmax (15.65±5.30), (15.02±4.42) ng/mL; AUC0-t (808.85±271.19), (793.76±256.78) h·ng·mL-1; AUC0-∞ (917.02±347.82), (875.49±310.77) h·ng·mL-1. tmax (4.29±1.48) h and (5.69±4.10) h, t1/2 (49.47±20.08) and (45.29±12.24) h. The relative bioavailability was 100.91% for AUC0-t, 102.97% for AUC0-∞. The 90% confidence intervals of the geometric mean ratios of the main pharmacokinetic parameters Cmax, AUC0-t, AUC0-∞ of the two preparations under fasting/feding conditions were all within 80%-125%.CONCLUSION: The test and reference preparation of solifenacin succinate tablets are bioequivalent under fasting and fed conditions.

Effects of individual differences on the pharmacokinetics of capecitabine in cancer patients

XU Guofang, GAO Pan, LIU Ping, LAI Yaowen, LI Guanghui, ZHAO Yue, ZHANG Yongling, LI Xiaosu, QI Qi

2021, 26(3):  305-311.  doi:10.12092/j.issn.1009-2501.2021.03.010

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AIM: To study the effects of individual differences (gender, age, body surface area, and body weight) on the pharmacokinetics of capecitabine in cancer patients in hoping of providing evidence for the rational use of capecitabine in clinic. METHODS: A total of 76 patients with various solid tumors were given a single dose of 0.6 g (0.15 g, 4 tablets) capecitabine in postprandial and blood samples were collected at multiple time points. The plasma concentration of capecitabine and its active metablolite, 5-fluorouracil (5-FU) were analyzed by HPLC-MS/MS and the pharmacokinetic parameters of the drugs were calculated by Phoenix WinNonlin7.0 software. RESULTS: Following oral administration, the Cmax values of capecitabine were 49% higher in males compared to those in females. There was no difference in capecitabine AUC0-∞, 5-FU Cmax, and 5-FU AUC0-∞ between males and females. There was a negative correlation between age (26-65 years old) and Cmax value of capecitabine, whereas no correlation in capecitabine AUC0-∞, 5-FU AUC0-∞, and 5-FU with various ages; For the body surface area, there was no significant difference in the AUC0-∞ and Cmax of capecitabine in patients with different body surface areas (1.28-2.01 m2), wheras the AUC0-∞ and Cmax of 5-FU had statistical significance (P<0.05). The values were up-regulated with the decrease of body surface area. Body weights (45.0-83.0 kg) had no effect on the AUC0-∞ and Cmax of capecitabine, whereas they had statistical correlation with AUC0-∞ and Cmax of 5-FU (P<0.05). CONCLUSION: The current data indicate that different factors affect the pharmacokinetics of capeitabine differently. Among the factors, gender and age mainly affect the absorption process and body surface area and weight mainly influence the metabolism of capeitabine.

Effect of adiponectin 45 T/G gene polymorphism on type 2 diabetes treated with liraglutide

WANG Chunling, ZHOU Renjing, FENG Rui, WU Yanneng

2021, 26(3):  312-317.  doi:10.12092/j.issn.1009-2501.2021.03.011

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AIM: To investigate the effect of genetic variation of calmodulin 45 T/G (APM1-45) gene polymorphism on the clinical efficacy and T2DM patients with type 2 diabetes mellitus treated with liralutide.  METHODS: A total of 95 patients with type 2 diabetes admitted to the third people's Hospital of Haikou City from August 2016 to October 2019 were selected as subjects of study. All patients were treated with liraglutide for 14 weeks. And the changes of blood glucose level, BMI index and relative mRNA expression were recorded before and after treatment. Besides record the occurrence of adverse reactions. RESULTS: The distribution frequency of APM1-45 (rs2241766) in the study population was 46 cases of TT type (48.42%), 43 cases of TG type (45.26%), 6 cases of GG type (6.32%). After treatment, the 2h PG, HbAIc, FPG and BMI related indexes of each group decreased significantly compared with those before treatment, and there was statistical difference (P<0.05); the FPG, HbA1c and BMI indexes of TT genotype patients decreased more compared with TG/GG genotype patients, but there was no statistical difference between them (P>0.05). The relative expression of mRNA in TT genotype was significantly lower than that in TG/GG genotype (P<0.05). The overall adverse reactions of patients were less, there was no statistical difference between the groups. CONCLUSION: For type 2 diabetic patients, the treatment of liraglutide alone has obvious effect, and the incidence of adverse reactions is low. There is a certain correlation between G allele and T2DM susceptibility, while T allele carrier has a better effect on the treatment of liraglutide.

Correlation between CYP2C19 gene polymorphism and individualized medication in patients with ischemic stroke

XIA Chunyong, ZHANG Zuowen, HE Xiaoyan, LIU Jie, LI Xiaoya, CHANG Qiuhong, QIN Lijuan, CAO Zhenming, DING Ling

2021, 26(3):  318-323.  doi:10.12092/j.issn.1009-2501.2021.03.012

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AIM: To investigate the guiding role of individualized medication adjustment based on CYP2C19 metabolic typing in the treatment of ischemic stroke with clopidogrel, and to provide reference for clinical individualized medication.  METHODS: The total of 80 patients with ischemic stroke were divided into the individualized drug instruction group with gene detection (n=40) and the control group without gene detection (n=40) according to whether they received CYP2C19 gene detection. According to the metabolism of CYP2C19, the individualized medication instruction group was divided into slow metabolic type, intermediate metabolic type, fast metabolic type and ultra-fast metabolic type. Patients with fast and ultra-fast metabolites were given clopidogrel dose of 75 mg once a day. Patients with intermediate metabolic type were given double clopidogrel dose of 150 mg once a day. Patients with slow metabolism were given tigrillo dose of 90 mg twice a day or aspirin dose of 100 mg once a day. The control group received 75 mg clopidogrel once a day. All patients enrolled in the groups were followed up for 3 months by outpatients or telephone. The incidence of vascular events and mRS scale scores were compared between the two groups. RESULTS: The incidence of vascular events in the individualized drug instruction group was significantly lower than that in the control group, and the incidence of mRS score(0-1) was significantly higher than that in the control group, with statistically significant differences (P<0.05). CONCLUSION: The individualized medication for patients with ischemic stroke by CYP2C19 gene detection can significantly reduce the incidence of adverse vascular events and improve the prognosis and living ability of patients.

Research progress on the influence of sex differences on the action of psychotropic drugs#br#

ZHANG Siliang, HU Linlin, SHAO Hua, CHEN Xijing

2021, 26(3):  324-331.  doi:10.12092/j.issn.1009-2501.2021.03.013

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Epidemiological survey shows that the prevalence, incidence rate and symptoms of mental disorders are affected by sex. A large number of studies have shown that men and women respond differently to psychotropic drugs in clinical application. Moreover, some studies have shown that there are sex specific psychotropic drug use patterns in patients with depression. This paper summarizes the sex differences in pharmacokinetics of psychotropic drugs caused by physiological differences between men and women, and collates the current pharmacodynamic studies of mainstream clinical psychotropic drugs, with special attention to the effect of sex hormones on the therapeutic response of psychotropic drugs. This paper discusses the specific role and necessity of therapeutic drug monitoring in dealing with clinical sex differences in psychotropic drugs, hoping to provide reference for individual rational drug use.

Research progress on the mechanism of miRNA in intestinal ischemia-reperfusion injury

ZHANG Jianmin, LENG Yufang, LIU Xin, REN Yixing, SHI Yajing, CHEN Feng

2021, 26(3):  332-340.  doi:10.12092/j.issn.1009-2501.2021.03.014

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microRNA (miRNA) is a class of 19-25 nucleotide highly conserved single-stranded non-coding RNA that is widely found in plants and animals. Their biological effect is to negatively regulate target gene expression at the post-transcriptional level through complementary pairing with mRNA. Intestinal I/R injury is more common in clinical practice, and ischemia-reperfusion will cause intestinal mucosal barrier damage, and it is related to the occurrence, development, and outcome of many clinical diseases. Many studies have shown that the miRNA subtype genes miR-34a-5p, miR-351-5p, miR-682, miR-21, etc. affect the intestinal I/R injury process to some extent by regulating a series of signal transduction. Therefore, revealing the role of miRNA in intestinal I/R injury and providing a new direction for the diagnosis and treatment of I/R.

Review of bleeding events in clinical studies of clopidogrel

YUAN Zhen, CHEN Bilian

2021, 26(3):  341-349.  doi:10.12092/j.issn.1009-2501.2021.03.015

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P2Y12 receptor antagonist is currently one of the commonly used drugs for the treatment of acute coronary syndromes. Clopidogrel is a representative drug among P2Y12 receptor antagonists. Bleeding events as the most common side effect of this drug have also been concerned. The incidence and risk of bleeding events in large-scale clinical studies of clopidogrel are analyzed and discussed to provide refer-ences for reasonable clinical prescription of clopidogrel. 

Advances in understanding the role of IKKβ in tumorigenesis and its inhibitors

CHEN Xuli, WEI Jing, WANG Jiabing

2021, 26(3):  350-360.  doi:10.12092/j.issn.1009-2501.2021.03.016

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In recent years, the role of inhibitor kappa B kinaseβ (IKKβ) in the process of tumorigenesis has gradually been elucidated. IKK is involved in tumor cell proliferation and survival by acting on multiple molecular pathways. Inhibition of IKKβ has been identified as a promising treatment for cancer. Researchers have developed a series of IKKβ inhibitors and found that they can effectively inhibit tumor growth, but no IKKβ inhibitors have been used clinically to treat cancer. We discuss progress in understanding the role of IKKβ in tumorigenesis and review the recent development of main inhibitors of IKKβ.