1.Introduction for clinical trials of aogliptin
Shuqing CHEN ; Xia ZHAO ; Yimin CUI
Chinese Journal of Biochemical Pharmaceutics 2015;(11):178-180,184
Alogliptin is a class of highly selective dipeptidyl peptidase-IV (DPP-IV) inhibitors.It can reduce the glucose level mainly through inhibiting the decomposition of dipeptidyl peptidase of glucagon peptide-1 (GLP-1), therefor promote insulin secretion.A large number of clinical trials have been conducted before and after algliptin get approved by Food and Drug Administration form different countries , which proves that alogliptin can remarkably reduce blood glucose without causing any serious risks.This article is mean to introduce most of the important clinical trials that has been conducted, from Phase I to Phase IV.
2.Study on composition, antibiotic activity and antioxidant activity of volatile oils from uyghur medicine Althaea rosea.
Abudukeremu MUNIRA ; Tu'erhong MUHETA'ER ; Yimin RESALAT ; Na XIA
China Journal of Chinese Materia Medica 2015;40(8):1614-1619
Althaea rosea is a type of mallow plant. Its dry flowers are one of common herb in Uyghur medicines and recorded to have several efficacies such as external application for detumescence, moistening lung and arresting cough, sweating and relieving asthma, diminishing swelling and promoting eruption, soothing the nerves and strengthening heart. However, there are only fewer studies on effective components of A. rosea and no literature about its volatile oil and pharmacological activity. In this paper, the volatile oil of A. rosea was obtained by using the chemical distillation and extraction method. The individual chemical components were separated from the volatile oil and identified by the Gas Chromatograph-Mass Spectrometer technique (GC-MS). The antioxidant activity against free radicals was detected by the'ultraviolet and visible spectrophotometer method. The antibiotic activity was detected by the filter paper diffusion method. The experimental results showed nearly 70 compounds in the volatile oil, with complex chemical components. With a low content, most of the compounds were aromatic and aliphatic compounds and their derivatives. A. rosea had a better antibiotic activity for common microorganisms, with a wide antibacterial spectrum. According to the results, the volatile oil of A. rosea will have a good application value in medicine, food and cosmetic industries, which provided a scientific basis for the development of natural A. rosea resources.
Althaea
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chemistry
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Anti-Bacterial Agents
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chemistry
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pharmacology
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Antioxidants
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chemistry
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pharmacology
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Bacteria
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drug effects
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China
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ethnology
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Drugs, Chinese Herbal
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chemistry
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pharmacology
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Gas Chromatography-Mass Spectrometry
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Medicine, Chinese Traditional
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Oils, Volatile
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chemistry
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pharmacology
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Plant Oils
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chemistry
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pharmacology
3.Expression of HMGB1, MMP-9 and VEGF-C in papillary thyroid carcinoma
Pei HUANG ; Daoming LI ; Qiwei HUANG ; Yimin SONG ; Xia PANG
Journal of Endocrine Surgery 2013;7(4):265-268
Objective To study the expression of high mobility group box 1 (HMGB1),matrix metalloproteinase-9(MMP-9) and vascular endothelial growth factor-C (VEGF-C)gene in papillary thyroid carcinoma (PTC) and their significance.Methods Expression of HMGB1,MMP-9,VEGF-C proteins and HMGB1 mRNA was detected by technology of immunohistochemistry(SP) and in situ hybridization in 58 cases of PTC tissues,20 cases of thyroid adenoma tissues,25 cases of nodular goiter tissues and 10 cases of normal thyroid tissues.Results Expression of HMGB1,MMP-9,VEGF-C proteins and HMGB1 mRNA in PTC tissues was much higher than that in the 3 non-cancerous tissues (P < 0.05).The positive expression rate of HMGB1,MMP-9 proteins and HMGB1 mRNA was closely associated with the thyroid carcinoma size and lymph node metastasis (P <0.05).There was also closely association between the positive expression rate of VEGF-C protein and lymph node metastasis(P < 0.05).The positive expression rate of HMGB1,MMP-9,VEGF-C proteins and HMGB1 mRNA had no association with patients' sex or age(P > 0.05).The expression of HMGB1,MMP-9 and VEGF-C proteins had positive correlation with each other(P < 0.05).The expression of HMGB1 protein and HMGB1 mRNA was also positively correlated with each other(P <0.05).Conclusion Expression of HMGB1,MMP-9,VEGFC proteins and HMGB1 mRNA in PTC is correlated with the progress,invasion,metastasis of PTC,by detecting them may help to predict the clinical progress and prognosis.
4.Combined measurement of serum CYFRA21-1,NSE,CEA,CA19-9,CA125 and SCC:diagnosis value to lung cancer
Yimin ZHANG ; Wenjin XIA ; Caiping MAO ; Xiaohong XU
China Oncology 1998;0(04):-
Background and purpose:Measurement of tumor markers in serum is widely used for the diagnosis of lung cancer, but the positive rates of single marker for diagnosis of lung cancer were not high. This study was to investigate the clinical value of combined measurement of serum CYFRA21-1,NSE,CEA,CA19-9,CA125 for the diagnosis of lung cancer. Methods:The levels of CYFRA21-1,NSE,CEA,CA19-9,CA125,SCC were assayed and compared between the lung cancer group(135 cases) and cancer-free control group(20 case) by electrochemiluminesence immunoassay.Results:The levels of CYFRA21-1,NSE,CEA,CA19-9,CA125 and SCC in the lung cancer group were (7?8) ng/ml,(30?29) ng/ml,(65?293) ng/ml,(110?379) U/ml,(122?412) U/ml and (2?7) ng/ml, respectively, which were higher than those in the control group. The levels of the six tumor markers were associated with pathology of lung cancer, the levels of CEA were (11?25)?10 ng/ml,(2?4) ?10 ng/ml,(2?3)?10 ng/ml in the adenocarcinoma , squamous cell carcinoma and small cell carcinoma cases respectively; the levels of CA125 were (21?48)?10 U/ml,(48?57) ?10 U/ml,(5?4)?10 U/ml in the adenocarcinoma ,squamous cell carcinoma and small cell carcinoma patients, respectively; the levels of CA199 were (17?44) ?10 U/ml,(5?12)?10 U/ml,(4?4) ?10 U/ml in the adenocarcinoma, squamous cell carcinoma and small cell carcinoma patients, respectively. The levels of CEA,CA125,CA19-9 in the adenocarcinoma were higher than those in the squamous cell carcinoma and small cell carcinoma, but there was no significance different(P
6.Single nucleotide polymorphism in ATM and non-small cell lung cancer susceptibility
Wenjin XIA ; Dan SU ; Peng LIU ; Shenglin MA ; Zhiming JIANG ; Yimin ZHANG
China Oncology 2010;20(2):121-124
Background and purpose: The ataxia-telangiectasia mutated (ATM) gene results in ataxia-telangiectasia (A-T) and it is closely associated with tumors. ATM is an important signal transducer that is involved in the repair of DNA double-strand break damage by phosphorylating numerous target proteins . This study was aimed to investigate the correlation between a single nucleotide polymorphism (SNP) in ATM gene (IVS62+60G>A) and the risk of non-small cell lung cancer(NSCLC) in a case-control study. Methods: From June 2004 to December 2005, a total of 264 patients with NSCLC were recruited, 264 healthy people as control. All of specimens were collected from Zhejiang Tumor Hospital. DNA was extracted from peripheral blood and then was used to determine. ATM genotype by Taqman SNP genotyping assays. Logistic regression model was employed to analyze the relationship between SNP and NSCLC risk. Results: The percentage of NSCLC patients in 86 patients with A/A genotype, 139 patients with A/G and 39 patients with G/G were 32.6% (86/264), 52.6% (139/264), 14.8% (39/264), respectively. The percentage in 68 healthy people with A/A genotype, 139 healthy people with NG and 55 healthy people with G/G were 26.0% (68/262), 53.0% (139/262) and 21.0% (55/262), respectively. The proportion of G/G genotype in 264 patients was obviously lower than that in the 264 healthy control (14.8% vs 21.2%, P<0.05). The people with G/G genotype had lower risk to NSCLC than there with A/A genotype (OR=0.561, 95% CI=0.334-0.942, P=0.029). Conclusion: The ATM SNP(IVS62+60G>A)was associated with the NSCLC risk, and homozygous G alleles may be a protective factor to NSCLC.
7.Effects of Captopril in renal ischemia reperfusion injury
Zhenghui XIAO ; Xia HU ; Zhenhua FANG ; Wu ZHOU ; Xiulan LU ; Yimin ZHU
Chinese Pediatric Emergency Medicine 2015;22(12):836-839,843
Objective To explore therapeutic mechanism of angiotensin-converting enzyme inhibitor (Captopril) in renal ischemia reperfusion (I/R) injury.Methods Wistar rats were randomly divided into sham operation group (Sham group),ischemia-reperfusion group (I/R group),captopril-treated group (CAP group),I/R model was made through ligating one side renal vessel.Renal function indexes including SCr and BUN were detected through biochemical analysis.Changes of renal tissue were observed by pathological section.ELISA detection was used to determine inflammatory cytokines such as IL-6,IL-8 and TNF-α.Activation of MAPK signaling pathway were analyzed by Western blot.Results After captopril treatment,SCr,BUN levels of the I/R group and the CAP group were higher than those of Sham group(P < 0.05),Scr,BUN concentrations of CAP group were lower than those of I/R group(P < 0.05).After captopril treatment,IL-6,IL-8,TNF-α concentrations of I/R group were higher than those of the Sham group(P <0.05);IL-6,IL-8,TNF-α concentrations of CAP group were lower than those of I/R group(P < 0.05).Renal tissue c-jun N-terminal kinase,extracellular signal-regulated protein kinases,P38 in I/R group and CAP group were phosphorylated,and there were no significant differences between the two groups.Conclusion Captopril couldimprove renal function to some degree,and reduce expression of inflammatory cytokines rather than MAPK inflammatory signaling pathway.
8.Concentration Determination of Sodium Valproate in Human Serum by HPLC-Fluorescence Detection Method
Yimin CUI ; Peihong SUN ; Yuwang LIU ; Xia ZHAO ; Rong LI ; Zhongmin SUN
China Pharmacy 1991;0(04):-
OBJECTIVE:To establish a method for the determination of sodium valproiate in human serum and to study the bioequivalence of steady state concentration C ssm in of the domestic and imported sodium valproiate sustained-release compound tablets.METHODS:Two periods of multi-oral administration of domestic and imported sodium valproiate sustained-release compound tablets were conducted alternately at random on20healthy male volunteers;the trough concentration of sodium valproate in human serum was determined by HPLC-fluorescence detection and the data were analyzed by3p97pro?gram.RESULTS:The blood concentration was steady after3d oral administration of both the domestic and imported sodium valproate sustained-release compound tablets.The C ssm in of domestic and imported products were(38.17?9.36)、(35.48?9.44)mg/L respectively.C ss min of domestic and imported sodium valproate sustained-release compound tablets were of bioe?quivalence either single or multi-oral administration.CONCLUSION:This HPLC-fluorescence method is quick,sensitive and economical,which can be used to monitor the concentration of sodium valproate in human serum.
9.Regulatory effect of edaravone on the photoreceptor autophagy at the early stage of experimental retinal detachment in rats
Ziwei KANG ; Xiuyu REN ; Yanchun ZHANG ; Cheng PEI ; Nana ZHANG ; Yimin XIA ; Jingru YANG
Chinese Journal of Experimental Ophthalmology 2021;39(9):776-784
Objective:To investigate the effect of edaravone, a free radical scavenger, on the regulation of retinal autophagy and the protection of photoreceptor cells at the early stage of experimental retinal detachment (RD) in rats.Methods:Fifty-one adult male Sprague-Dawley rats were used for RD model establishment, and another 24 rats were served as PBS injection group.The RD model was established via subretinal injection of 0.5% sodium hyaluronate into the right eye of the rats and the rats with successful modeling were randomly divided into RD model group and edaravone treatment group.The rats in the edaravone treatment group were given edaravone of 3 mg/kg intraperitoneally, twice a day after modeling, and the rats in the PBS injection group and RD model group were given equal volume of normal saline.Rats were sacrificed on the 1st day, 3rd day and 7th day following modeling.The T-superoxide dismutase (T-SOD) activity and malondialdehyde (MDA) content in the intraocular fluid was detected.The expression levels of superoxide dismutase 2 (SOD2), nuclear factor E2-related factor 2 (Nrf2), autophagy related gene 4 (Atg4), microtubule-associated protein 1 light chain 3B (LC3B) and other proteins in retinal tissue were identified by Western blot analysis.TUNEL staining was performed on paraffin sections of the whole eyeball to analyze the apoptosis of photoreceptor cells.The study protocol was approved by an Ethics Committee of Xi'an Fourth Hospital (No. 2016016). The use and care of animals complied with the Regulations on the Administration of Experimental Animals.Results:The RD area was more than 60% in rat eyes of RD model.There were significant differences in MDA content and T-SOD activity among different groups at various time points (MDA: Fgroup=385.513, P<0.01; Ftime=13.021, P<0.01.T-SOD: Fgroup=48.865, P<0.01; Ftime=7.700, P=0.003). Compared with the PBS injection group, the MDA concentration was significantly increased and the T-SOD activity was significantly decreased in the RD group and edaravone treatment group on the 1st, 3rd and 7th day after modeling (all at P<0.05). The MDA concentration was significantly reduced and the T-SOD activity was significantly elevated in the edaravone treatment group on the 1st, 3rd and 7th day after modeling in comparison with those of the RD group (all at P<0.05). Compared with the PBS injection group, the relative expression levels of SOD2 and Nrf2 proteins were significantly increased in the RD group and edaravone treatment group on the 1st, 3rd and 7th day after modeling (all at P<0.05), and Atg4 and LC3B-Ⅱ/LC3B-Ⅰ were significantly increased on the 1st, 3rd and 7th day after modeling (all at P<0.05). The expression level of SOD2 in the edaravone treatment group was significantly higher than that in the RD group on the 1st, 3rd and 7th day after modeling (all at P<0.05), and the expression level of Nrf2 was significantly increased in the edaravone treatment group on the 1st and 3rd day after modeling compared with that of the RD group (both at P<0.05), and the expression levels of Atg4 and LC3B-Ⅱ/LC3B-Ⅰ were significantly increased in the edaravone treatment group on the 3rd day after modeling in comparison with those of the RD group (both at P<0.05). No significant TUNEL positive cells were observed in PBS injection group at all time points, and TUNEL positive cells were observed on the 1st, 3rd and 7th day after modeling in the RD group, and the expression level of caspase-3 in the RD group was significantly increased in comparison with that of the PBS injection group ( P<0.05). The apoptosis of photoreceptor cells and the expression level of caspase-3 in edaravone treatment group were significantly decreased in comparison with those of the RD group on the 1st, 3rd and 7th day after modeling (all at P<0.05). Conclusions:The intraperitoneal injection of edaravone, twice a day, can significantly improve the antioxidant capacity of the retina after experimental RD in rats, regulate retinal autophagy and reduce the apoptosis of photoreceptor cells in early-stage RD.
10.Comparative study on efficacy and safety of single microneedle radiofrequency versus photodynamic therapy in the treatment of inflammatory lesions of moderate to severe facial acne vulgaris
Jiemin ZHONG ; Lei SHAO ; Yimin LIANG ; Qiongxiao HUANG ; Manqi XIA ; Yumei LIU
Chinese Journal of Dermatology 2023;56(8):751-755
Objective:To compare the clinical efficacy and safety of single microneedle radiofrequency versus photodynamic therapy in the treatment of inflammatory lesions of moderate and severe facial acne vulgaris.Methods:Sixty patients with moderate to severe facial acne vulgaris were retrospectively collected from Guangzhou Institute of Dermatology between December 2021 and July 2022, including 30 patients who had received single microneedle radiofrequency treatment, and 30 patients who had received photodynamic therapy. There were no significant differences in the age, gender distribution, and severity of acne between the two groups (all P > 0.05). The patients in the microneedle radiofrequency group were treated with single microneedle radiofrequency once every 4 weeks for 2 sessions; those in the photodynamic therapy group received aminolevulinic acid-based photodynamic therapy once every 2 weeks for 3 sessions; patients in both groups were still treated with oral doxycycline for 8 weeks. After 8-week treatment, the efficacy, pain severity and incidence of adverse reactions were compared between the two groups. Statistical analysis was carried out by using chi-square test, two independent samples t-test and Mann-Whitney U test. Results:After 8-week treatment, there was no significant difference in the response rate between the microneedle radiofrequency group (93.33%, 28/30) and photodynamic therapy group (86.67%, 25/30; χ2 = 0.74, P = 0.389). No significant difference was observed in the pain severity score between the microneedle radiofrequency group (4.80 ± 2.08) and photodynamic therapy group (4.13 ± 1.86, t = 1.32, P = 0.194), and there was also no significant difference in the pain degree between the two groups ( Z = -1.13, P = 0.260). In the microneedle radiofrequency group, burning sensation occurred in 3 cases (10.00%), swelling and pain in 4 (13.33%), erythema in 2 (6.67%), and dryness and desquamation in 2 (6.67%), and no reactive acne or hyperpigmentation was observed; in the photodynamic therapy group, burning sensation occurred in 10 cases (33.33%), swelling and pain in 9 (30.00%), erythema in 8 (26.67%), reactive acne in 11 (36.67%), hyperpigmentation in 2 (6.67%), and dryness and desquamation in 11 (36.67%). Compared with the photodynamic therapy group, the microneedle radiofrequency group showed significantly decreased incidence rates of burning sensation, erythema, reactive acne, and dryness and desquamation ( χ2 = 4.81, 4.32, 13.47, 7.95, respectively, all P < 0.05) ; there was no significant difference in the incidence rates of swelling and pain as well as hyperpigmentation between the two groups ( χ2 = 2.46, 2.07, respectively, both P > 0.05) . Conclusion:Single microneedle radiofrequency showed marked efficacy equivalent to that of photodynamic therapy in the treatment of moderate to severe facial acne vulgaris, but higher safety, providing more clinical treatment options for moderate to severe facial acne vulgaris.