Combination therapy of methotrexate and iguratimod for female patients with moderate to severe active rheumatoid arthritis and its impact on ovarian function.

Rheumatoid arthritis is systemic inflammatory disease, presenting as symmetrical polyarthritis, mainly affecting hands and feet. Female patients with rheumatoid arthritis have also decreased fertility and premature ovarian failure. Methotrexate is used in treatment of rheumatoid arthritis. However, single treatment of Methotrexate is not ideal and often needs to be combined with other drugs like Iguratimod for intensive treatment of refractory rheumatoid arthritis. We aim to explore efficacy of combined use of MTX and IGU for female patients with rheumatoid arthritis and its impact on ovarian reserve function. Total 80 female patients with moderate to severe active rheumatoid arthritis were selected and randomly divided into MTX and MTX + IGU groups. The MTX + IGU group showed lower levels of IL-1ß, IL-6, IL-17 and TNF-α after treatment as compared to MTX group. The MTX + IGU group showed significantly higher level of AMH at the end of treatment. However, no statistical differences were observed in FSH, LH, E2 and AFC levels between the two groups. The combined therapy of MTX and IGU has better efficacy with less impact on ovarian function, even improving ovarian reserve function through effective control of rheumatoid inflammatory activity.

Pharmacokinetics, Safety, and Tolerability of Single-Dose Orally Administered Venglustat in Healthy Chinese Volunteers.

BACKGROUND AND OBJECTIVE: Deficiencies of enzymes acting downstream of glucosylceramide synthase (GCS) can cause severe substrate accumulation. Venglustat is a small-molecule, brain-penetrant GCS inhibitor under investigation for multiple diseases involving pathogenic glycosphingolipid accumulation. Here, we evaluate the pharmacokinetics, safety, and tolerability of venglustat in healthy Chinese volunteers. METHODS: Study PKM16116 was a phase I, single-center, non-randomized, open-label study to investigate the pharmacokinetics, safety, and tolerability of a single 15 mg dose of orally administered venglustat in healthy Chinese volunteers aged 18 to 45 years. RESULTS: A total of 14 volunteers (7 male; 7 female) with a body mass index from 20.9 kg/m2 to 27.1 kg/m2 were enrolled. The median time to reach the venglustat maximum plasma concentration was 2.50 h post-dose. The mean terminal half-life of venglustat was 30.6 ± 7.40 h. The mean systemic exposures across all participants were 60.3 ± 17.3 ng/mL for the maximum plasma concentration, and 2280 ± 697 ng·h/mL for the area under the plasma concentration-time curve extrapolated to infinity. There were no relevant differences in venglustat pharmacokinetics between male and female volunteers. A post hoc cross-study comparison analysis showed comparable venglustat pharmacokinetics in Chinese and non-Chinese volunteers. Venglustat was safe and well tolerated in the current study (a total of five Grade 1 treatment-emergent adverse events were reported in three volunteers). CONCLUSION: Venglustat showed a favorable pharmacokinetic, safety, and tolerability profile in healthy Chinese volunteers following a single oral 15 mg dose. CLINICAL TRIAL REGISTRY NO: CTR20201012 ( http://www.chinadrugtrials.org.cn ) registered on 24 February 2021 and ChiCTR2200066559 ( http://www.chictr.org.cn ) retrospectively registered on 9 December 2022.

Study on the objectivity and biological mechanism of Psoralea corylifolia Linn.'s 'Great dryness damages the liver' / 药学学报

According to the theory of 'Xingben Dazao' of Psoralea corylifolia Linn. (BL), the susceptible syndromes and biomarkers of liver injury caused by BL were searched. Rat models of kidney-yin deficiency syndrome (M_yin) and kidney-yang deficiency syndrome (M_yang) were established, and all animal experimental operations and welfare following the provisions of the First Affiliated Experimental Animal Ethics and Animal Welfare Committee of Henan University of Traditional Chinese Medicine (No. YFYDW2020017). The results showed that BL significantly decreased the body weight, water intake, and urine weight of M_yin rats and increase the organ indexes of the liver, testis, adrenal gland, and spleen and the expression of alanine aminotransferase (ALT). Meantime, BL significantly increased the urine weight of M_yang rats and decreased the expression of ALT and aspartate aminotransferase (AST). Hematoxylin and eosin (HE) staining showed that BL could aggravate inflammatory infiltration of hepatocytes in rats with M_yin and alleviate liver injury in rats with M_yang. Metabolomics identified 17 BL co-regulated significant differential metabolic markers in M_yin and M_yang rats. Among them, 8 metabolites such as glutamine, quinolinate, biliverdin, and lactosylceramide showed opposite trends, mainly involving cysteine and methionine metabolism, tyrosine metabolism, tryptophan metabolism, purine metabolism, sphingolipid metabolism, glycerol phospholipid metabolism, glutamine metabolism, and other pathways. M_yin/M_yang may be the susceptible constitution of BL for liver damage or protection, which may be related to the regulation of amino acid metabolism and sphingolipid metabolism. The study can provide some experimental data support for the safe and accurate use of BL in the clinical practice of traditional Chinese medicine.

Clinical efficacy and safety of venetoclax combined with multidrug chemotherapy in the treatment of 15 patients with relapsed or refractory early T-cell precursor acute lymphoblastic leukemia / 中华血液学杂志

Objective: To explore the efficacy and safety of Venetoclax combined with multidrug chemotherapy in patients with relapsed or refractory early T-cell precursor acute lymphoblastic leukemia (R/R ETP-ALL) . Methods: This study retrospectively analyzed 15 patients with R/R ETP-ALL who received Venetoclax combined with multidrug chemotherapy from December 2018 to February 2022. Among them, eight cases were combined with demethylated drugs, four cases were combined with demethylated drugs and HAAG chemotherapy regimen, two cases were combined with demethylated drugs and CAG regimen, and one case was combined with Cladribine. Specific usage and dosage of Venetoclax: 100 mg on day 1, 200 mg on day 2, 400 mg on day 3-28, orally; when combined with azole antifungal drugs, dosage was reduced to 100 mg/d. Results: Fifteen patients (10 males and 5 females) with R/R ETP-ALL were treated with Venetoclax and multidrug chemotherapy with a median age of 35 (12-42) years old. Of 4 refractory and 11 relapsed patients, the efficacy was evaluated on the 21th day following combined chemotherapy: the overall response rate, the complete response (CR) rate, and the CR with incomplete hematological recovery (CRi) rate were 67.7% (10/15), 60.0% (9/15), and 6.7% (1/15), respectively. For the overall study population, the 12-month overall survival (OS) rate was 60.0%, and the median OS was 17.7 months. The disease-free survival (DFS) rate of all CR patients at 12 months was 60.0%, and the median DFS did not reach. About 14 patients had Ⅲ-Ⅳ hematological toxicity, but these adverse reactions were all controllable. No adverse reaction in the nervous system and tumor lysis syndrome occurred in this study, and no adverse reaction of organs above grade Ⅲ occurred. Conclusion: Venetoclax combined with multidrug chemotherapy may be a safe and promising treatment option for patients with R/R ETP-ALL.

The anti-tumour mechanism of Shuanghuang Qizhen Keliu Prescription based on network pharmacology / 中国药理学通报

Aim To explore the anti-tumour mechanism of Shuanghuang Qizhen Keliu Prescription based on network pharmacology. Methods The active components and targets of Shuanghuang Qizhen Keliu Prescription were searched and selected through the TCM-SP database. Related targets of tumor were screened and retrieved by OMIM. The key anti-tumor targets of Shuanghuang Qizhen Keliu Prescription were obtained by using Venn diagram analysis. The key target PPI network was constructed and the key targets were obtained by Cytoscape. Metascape platform was used for GO and KEGG enrichment analysis of key targets. Results There were many active components such as quercetin, kaempferol, and beta-sitosterol in Shuanghuang Qizhen Keliu Prescription, and their targets might be TP53, AKT1, JUN, MAPK1, TNF, RELA, IL-6 and so on. The anti-tumour mechanism might be proliferation inhibition, migration inhibition and apoptosis promotion. Conclusions This study preliminarily discusses the potential anti-tumour mechanism of Shuanghuang Qizhen Keliu Prescription, providing ideas and basis for subsequent experimental research.

The Antileukemia Activity of ZSTK474 on U937 Cells / 中国实验血液学杂志

OBJECTIVE@#To investigate the antileukemia activity of phosphatidylinositol-3 kinase (PI3K) inhibitor ZSTK474 on human leukemia cell line U937.@*METHODS@#MTT, soft agar assay, flow cytometric analysis and western blot were used to detect the effect of ZSTK474 on U937 cell proliferation, tumorigenicity, cell cycle, cell apoptosis and phosphorylation levels of the key factor of PI3K/AKT pathway. Chou-Talalay method was used to evaluate the combination of ZSTK474 with Cytarabine or Homoharringtonine.@*RESULTS@#PI3K inhibitor ZSTK474 could inhibit the proliferation and tumorigenicity of U937 cell, induce G@*CONCLUSION@#ZSTK474 can inhibit the pathway of PI3K/AKT, ZSTK474 alone or in combination with Homoharringtonine shows potential antileukemia activity on U937 cells.

Machine learning models based on radiomics in diagnosis of pituitary prolactin macroadenoma / 中华放射学杂志

Objective:To explore the effectiveness and feasibility of the machine learning models based on radiomics in the diagnosis of pituitary prolactin macroadenoma.Methods:Totally 122 histologically proven pituitary macroadenoma patients, including 70 cases of pituitary prolactin macroadenoma (PPM) and 52 cases of non-pituitary prolactin macroadenoma (NPPM), were retrospectively recruited. The differences of age, sex, serum prolactin value, bleeding, cystic degeneration and Knosp classification were compared between PPM and NPPM. The pre-processing, delineation of the region of interest and feature extraction of the preoperative axial contrast-enhanced T 1WI image were performed in the 3Dslicer software. The optimal feature set were selected by least absolute shrinkage and selection operator. All patients were randomly divided into the training group ( n=85) and the test group ( n=37) at a ratio of 7∶3. The models were established in the training group by logistic regression and support vector machine (SVM), and then verified by the test group. ROC curves were drawn respectively, and specificity, sensitivity, accuracy and area under the ROC curve (AUC) were calculated. Results:The age [(38±12) years vs . (43±11) years], gender ratio (male/female 50 cases/20 cases vs . 14 cases/38 cases) and prolactin value [366.00 (117.75, 1 156.25)μg/L vs . 47.25 (32.68, 62.40) μg/L] of patients with PPM and NPPM were statistically different ( P<0.05). The AUC values of logistic regression and SVM in the training group were 0.936 and 0.946, and the AUC values of the test group were 0.768 and 0.774, respectively. The diagnostic accuracy of logistic regression and SVM in the training group were 88.2% and 91.8%, and the accuracy of the test group were 73.0% and 77.8%. Conclusion:The machine learning models based on the radiomics can predict the pituitary prolactin macroadenoma well with a high accuracy.

Research progress of lateral flow immunochromatographic detection system / 中华检验医学杂志

Lateral flow immunochromatography is a real-time detection technology based on chromatographic membranes and nano-markers. Because of its simplicity, fastness and low cost, it is widely used in many fields, such as biomedicine, pathogen detection and food safety. Traditional lateral-flow immunochromatography relies on the naked eye, that has lower sensitivity, and can only provide qualitative or semi-quantitative results. With the application of different types of markers and sensitive detection equipment, lateral flow immunochromatography has enabled the quantitative and multi-component detection of analytes. The purpose of this paper is to describe the latest research progress of lateral flow immunochromatographic detection systems in combination with nano-labels, chromatographic membranes and band detectors, with a view to providing a basis for the selection of markers, improvement of chromatography membrane materials and detection instruments.

Research progress in targeting homologous recombination repair for tumor therapy / 药学学报

Applying poly(ADP-ribose) polymerase inhibitors (PARPi) to the treatment of cancers with homologous recombination deficiency (HRDness) has been a great advance in the field of molecular therapeutics. However, in the clinic patients lacking the specific mutations or developing reverse mutations in the process of PARPi treatment may not benefit from PARPi monotherapy. Therefore, targeting homologous recombination (HR) repair with molecularly targeted agents is becoming an attractive research focus and is raising the concept of "chemical HRDness". HR repair is an evolutionarily conserved and extensively regulated process that employs sister chromatids as the template to repair DNA double-strand breaks with high fidelity. In addition to directly targeting HR components, modulation of regulatory pathways controlling HR repair is effective in achieving the "HRDness" phenotype; this includes modulation of the cell cycle checkpoint regulatory pathway, the phosphatidylinositol 3-kinase (PI3K) signaling pathway, the chromatin remodeling pathway, etc. Targeting HR repair can not only result in "synthetic lethality" when combined with PARPi, but also sensitizes cancers to traditional radio/chemotherapy and novel immunotherapy. In this review we describe the HR repair pathway and its regulatory pathways, summarize the preclinical and clinical outcomes of targeting HR repair, discuss the remaining problems in this field and provide a prospective on its application in tumor therapy.

Serum-and-glucocorticoid-inducible-kinase-2 is overexpressed and mediates glycogen synthase kinase-3β/ β-catenin signal transduction in hepatocellular carcinoma / 中华肝脏病杂志

Objective@#To investigate the differential expression of serum-and-glucocorticoid-inducible-kinase-2 (SGK2) in hepatocellular carcinoma (HCC) and normal liver tissues and the related mechanism mediating signal transduction of GSK-3 β / β catenin in HCC cells.@*Methods@#Twenty pairs of matched HCC and normal tissues were collected and the situation of expression of SGK2 mRNA was detected by real-time fluorescence quantitative PCR. Western blot was used to detect the levels of SGK2 protein in human HCC cell lines (Huh-7, SMMC-7721) and normal human liver cell line (L02). SGK2 siRNA was used to transfect human HCC cell lines (SMMC-7721 and Huh-7), and then the protein expression levels of GSK-3 β/ β - catenin was successfully detected with the above-mentioned transfected cell line by western blot. Measurement data were expressed as mean ± standard deviation (±s), and the Student t -test was used as the statistical method.@*Results@#SGK2 mRNA expression was up-regulated in all 20 HCC samples than that of the expression of matched normal liver tissues. SGK2 protein levels were significantly higher in Huh-7 and SMMC-7721 than normal human liver cell lines (P < 0.01). The downregulation of SGK2 expression in human HCC cell lines (SMMC-7721 and Huh-7) had inhibited the expression of unphosphorylated GSK-3 β. In addition, the downregulation of SGK2 expression in HCC cell lines had decreased the dephosphorylation of β - catenin to prevent degradation of the β - catenin proteasome.@*Conclusion@#SGK2 is overexpressed in HCC and mediates GSK-3β/β- catenin signaling in HCC cells.

Expansion of Dental Care for Low-Income Children Through a Mobile Services Program.

BACKGROUND: Although access to dental care has improved over time, many children still face difficulty in obtaining services. One strategy to increase access is through mobile dental services, often in collaboration with schools, Head Start programs, and school-based health centers. This study evaluates a large mobile dental care program based in Minnesota. METHODS: Thematic analysis of interview data collected during a 2-day site visit and multivariate regression analysis of electronic records of patients (adults and children) that received care from 2000 through 2015, representing 84,279 unique patients. RESULTS: The number of patients increased from 5558 in 2000 to 13,863 in 2015. There was a decline in the share of preventive procedures over this period, from 45.7% to 29.4%, and an increase in the share of patients seen at fixed sites. The interview data revealed that program growth relied on relationships with school leaders, expanded scope of practice for dental assistants and dental therapists, and high Medicaid reimbursement. CONCLUSIONS: Mobile dental care programs can increase both preventive and restorative dental care for individuals who otherwise would not easily access oral health care services; mobile dental programs could be an option in many other communities and schools.

Anti-atherosclerotic effect of extract of traditional Chinese medicine formula Dan-yi-Iian in ApoE(-/-)mice / 中国药理学与毒理学杂志

OBJECTIVE To explore the anti-atherosclerotic effect of the extract of traditional Chinese medicine formula Dan-yi-lian(DYL)and the related mechanism.METHODS Atherosclerosis(AS)mod-el was established in ApoE(-/-)mice with a western diet. The mice were orally administered with differ-ent doses of DYL or vehicle daily for 28 d.The anti-atherosclerotic effect was evaluated by measuring the aortic atherosclerotic lesion area and media thickness with ultrasound imaging and histological sec-tions staining method. The effect on blood lipid was investigated by determining TC, TG, LDL, HDL, Apo-A1, Apo-B, etc. The anti-oxidative activity as assessed by determining the level of SOD, CAT, GSH,GSH-Px and MDA.Western blot analysis was used to determine the effect on ICAM-1,VCAM-1, MMP-2 and TNF-α. RESULTS In Dan-yi-lian administered ApoE(-/-)mice,the plaque area and media thickness were significantly reduced. Meanwhile, serum TC, TG, LDL and Apo-B were decreased, in contrast to the increased level of HDL and Apo-A1.On the other hand,SOD,CAT,GSH and GSH-Px were increased, while MDA was reduced in liver homogenate. In addition, the expression of ICAM-1, VCAM-1,MMP-2 and TNF-α was obviously inhibited by Dan-yi-lian.CONCLUSION Dan-yi-lian exhibit-ed potent anti-athero-sclerotic efficacy,in which the lipid-regulating,anti-oxidative and anti-inflammato-ry mechanism might be involved.

Effects of the PI3K inhibitor,ZSTK474,on the proliferation and cell cycle of human melanoma A375 cells / 国际药学研究杂志

Objective To investigate the effect and molecular mechanisms of phosphatidylinositol-3 kinase(PI3K)inhibitor ZSTK474 on human melanoma A375 cells in vitro. Methods The effect of ZSTK474 on the proliferation of A375 cells was deter?mined by MTT assay.Flow cytometric analysis was carried out to examine effect of ZSTK474 on the cell cycle of A375 cells.Western-blot was conducted to evaluate the effect of ZSTK474 on the expression of the cell cycle related proteins,cyclin B1 and cdc2.Chou-Talalay method was used to evaluate the combination of ZSTK474 with PD0332991.Results In the MTT assay,ZSTK474 inhibited the proliferation of A375 cells in a dose-dependent manner with the IC50value of 1.535 μmol/L.Furthermore,ZSTK474 arrested the cell cycle progression of the A375 cells at the G2/M phase via downregulating the expression of cyclin B1 and cdc2 at 1 and 5 μmol/L. In the synergistic assay,the combination of ZSTK474 with PD0332991 in the ratio 8×IC50 ZSTK474:1×IC50 PD0332991showed a synergistic ef?fect,with the combination index(CI)values of 0.463 ± 0.113,0.658 ± 0.009 and 0.941 ± 0.034 for ED50、ED75and ED90,respectively. Conclusion ZSTK474 could inhibit the proliferation of A375 cells and arrest the cell cycle at the G2/M phase.The combination of ZSTK474 with PD0332991 could exert a synergistic effect.The precent result has revealed that the PI3K inhibitor ZSTK474 is likely to be applied alone or in combination with the CDK4/6 inhibitor PD0332991 for the human melanoma therapy.

Effects of Pb stress on antioxidase system and growth of Rabdosia Rubescentis Folium / 中草药

Objective: To study the effect of different concentration of plumbum (Pb) stress on antioxidase activity in different organs of Rabdosia Rubescentis Folium (RRF, the aerial parts of Rabdosia rubescens) and their growth, and provide the basis for the growth regulation of R. rubescens under Pb pollution. Methods: Ramets hydroponic test was performed with the concentration of Pb (0, 135, 270, and 540 mg/L) and the stress time (50 d), taking superoxide dismutase (SOD), peroxidase (POD), catalase (CAT), relative growth rate (RGR), biomass, and Pb mass fraction as indexes, the determination of antioxidant enzyme activity was performed with spectrophotometer, and plant's Pb mass fraction of plant with plasma emission spectrometer was carried out. Results: Under Pb stress at different concentration (135-540 mg/L), SOD activity in the leaves and the roots of R. rubescens was increased first and then decreased, but no significant difference on SOD activity in the leaves at each level; POD activity in the leaves under Pb concentration (135-270 mg/L) was no significant difference compared with the control group, but was significantly increased at the concentration of 540 mg/L, while the POD activity in the roots under Pb stress at various concentration was significantly lower than that of the control group which gradually went up after declined; CAT activity in the leaves increased significantly with Pb concentration rising, and the activity in the root decreased gradually with Pb concentration rising. No significant effect on the growth of R. rubescens at low and mid levels of Pb concentration (135 and 270 mg/L), but under high concentration (540 mg/L) of Pb treatment compared with the control group, the biomass and RGR decreased by 33.33% and 46.59%, respectively. Conclusion: The stimulus response is different obviously for antioxidase activities between the leaves and roots of R. rubescens; Through fitting model predictive analysis, the critical Pb concentration is 301.99 mg/L, which decreases RGR by 10% compared with control group (P < 0.01). RRF shows a strong resistance to Pb stress.

Research Progress on Cytometric Bead Assay for Platelet Antibody Detection / 中国实验血液学杂志

Anti-platelet specific antibody is one of the most important reasons leading to thrombocytopenia and megakaryocyte dysmaturity. The detection of platelet autoantibodies is an important step in the diagnosis of ITP because of the absence of specific clinic feature. The monoclonal antibody-specific immobilization of platelet antigens (MAIPA) has become a "gold standard" for determination of PLT specific antibody, which has high specificity and low sensitivity. However, this assay is time-consuming and tedious work. Routine use of this assay in hospital is difficult. Recently, some researches reporded the cytometric bead assay that has higher sensitivity than MAIPA, and so probably solves the problem of time-consuming partly, that also can use different beads for simultaneous detection. This review focuses on recent progress of the cytometric bead assay.

Effects of Pb2+ stress on seed germination & seedling growth of Rabdosia rubescens / 中国中药杂志

The seeds of Rabdosia rubescens were as the materials to research the impacts of different lead (Pb2+) concentrations(0, 135, 270, 540, 1 080 mg x L(-1)) on seed germination and seedling growth. The results show that: Low concentration of lead had no obvious effect on early germination of the seed, the germination vigor and germination speed were lightly higher but not significantly differed at the level of Pb concentration 135 mg x L(-1) with control group; Mid-high concentration of Pb solution (270-1 080 mg x L(-1)) significantly inhibited the seed germination and seedling growth, which reduced the seed germination rate, germination vigor, germination index, embryo root length and shoot length, growth index with increasing of Pb concentrations. There was a inhibitory effect on embryo shoot length and root length at mid-high lead concentrations stress, and stronger inhibitory effect on root , which was more sensitive than shoot to Pb stress(P < 0.05). Pb bioaccumulation coefficient (BC) was 0.76-2.59, increased with concentration of Pb; Pb enrichment in seedling mainly caused the growth inhibition. The fitting model predictive analyses show, the critical concentration of Pb, which causes the germination rate and biomass fresh weight reducing 10%, is 195.18, 101.65 mg x L(-1).

Clinical Analysis of Postoperative Hyponatremia of Pituitary Tumor In 32 patients / 中国基层医药

Objective To explore clinical treatment of postoperative hyponatremia of pituitary tumor. Meth-ods 32 cases of patients with postoperative hyponatremia of pituitary tumor were randomly divided into control group and treatment group. The control group(n = 15) was treated with routine western medicine, and the treatment group(n = 17) was treated with water limited and sodium supplemented based on the control group. The clinical effect was observed between control group and treatment group. Results The clinical effect in the treatment group was signifi-cantly higher than that of the control group(P <0.05). Conclusion The treatment of water limited and sodium sup-plemented on postoperative hyponatremia of pituitary tumor is better.

Analysis of all publications in Chinese Journal of Perinatal Medcine in the past ten-years(1998-2007) / 中华围产医学杂志

Objective To collect the basic information on publications in Chinese Journal of Perinatal Medicine,and understand the current situation and set the goals for the future. Methods Information on all publications in this journal from 1998 to 2007 was collected.The distribution of all publications,Price Index and relative data were analyzed. Results There were 1368 publications altogether during the past 10 years.The first six kinds of papers were original articles(508,31.7%),short articles(258,18.9%),case reports(194,14.2%),reviews(122,8.9%),experimental studies(90,6.6%)and brief communications(83,14.2%).47.9% of all publications were from Beijing,Guangdong and Shanghai.The first three areas who had the most submissions were Beijing,Shandong and Guangdong in 2007.The citation frequency analysis showed that 708 publications were cited at 1east once and only two were cited over 80 times.53.4% of all cited publications were original articles and experimental studies. Conclusions Original articles and short articles are the two main types of publications in this journal,however original articles and experimental studies contributed to half of the publications being cited.Publications in this journal are focused in few areas and this might be related to the number of submissions.

Inhibition of multidrug resistance gene 1 expression in glioma by antisense oligodeoxynucleotides / 中国医学科学院学报

<p><b>OBJECTIVE</b>To investigate the effectiveness of phosphorothioate multidrug resistance gene 1 (MDR1) antisense oligodeoxynucleotides (MDR1-AS) suppressing MDR1 expression in multidrug-resistant glioma cell line C6/adr.</p><p><b>METHODS</b>The glioma cell line C6/adr served as the tested model in vitro, MDR1-AS (5'-CTCCATCACCACCTC-3'), complementary to the -9- +6 sequence of first exon, was synthesized and phosphorothioate-modified. As control of sequence specificity, MDR1-S (5'-GAGGTGGTGA TGGAG-3') was used. Both antisense and sense oligodeoxynucleotides were transduced to C6/adr cells by lipofectin. The cytotoxity of MDR1-AS was tested using morphological observation and 3- (4,5-dimethylthiazol-2-yl) -2, 5-diphenyl tetrazolium bromide assay. Semi-quantitative reverse transcription polymerase chain reaction was used to monitor the expression levels of the MDR1 mRNA in the different groups. The positive rate of the MDR1 gene product P glycoprotein (P-gp) was determined by flow cytometry assessment.</p><p><b>RESULTS</b>No cytotoxicity of MDR1-AS was observed. The MDR1 mRNA expression level was decreased from 106% to about 30.44% 48 h after MDR1-AS treatment. The P-gp positive rate of MDR1-AS treated C6/adr cells decreased from 100% to 32.77%, with that of C6/adr cells considered as 100%.</p><p><b>CONCLUSIONS</b>MDR1-AS can effectively inhibit MDR1 expression in the C6/adr cell line at both the mRNA and protein level, and may be an alternative treatment of drug-resistant gliomas.</p>