1.Advancements in stabilization technologies for membrane protein and its application in drug screening
Jia-hao FANG ; Yu-hong CAO ; Yu-zhen HE ; Zhan-ying HONG ; Yi-feng CHAI
Acta Pharmaceutica Sinica 2021;56(9):2325-2334
Membrane proteins are the main undertakers of biofilm function, and also the most important target group for innovative drug discovery and research. About 60% of drugs targets are membrane proteins. Due to the obvious aggregation and denaturation tendency of membrane proteins in aqueous solution, it is difficult to simulate the membrane like environment to maintain the correct conformation of membrane proteins
2.In vitro study of different Chinese herbs on the proliferation and COMP expression of chondrocyte
Yue-Long CAO ; Wei FENG ; Xiang WANG ; Yu XU ; Hong-Sheng ZHAN ; Yin-Yu SHI ;
Chinese Journal of Rheumatology 2003;0(08):-
Objective To investigate the effect of different Chinese herbs on cell proliferation and cartilage oligomeric matrix protein(COMP)expression in chondrocyte culture.Methods Chondrocytes isolated from rabbit knee cartilage were cultured for 3 generations with the density of 2?10~4/cm~2 and were verified by collagenⅡimmunohistochemical staining.Rabbit sera containing herbs were obtained after animals orally ad- ministrated herbs at the dosage equivalent to human.At 5% and 10% serum density,cells were cultured in the medium that contained liver-softening herbal compound sera.Subgroups setting at 1,3 and 5 hours after herb intervention were observed.Rabbit and bovine sera were control groups.Seven days after intervention,chon- drocytes proliferation was observed using the MTT assay kit.For the study of COMP expression,chondrocytes were isolated from human knee cartilage supematant.Superuatant COMP level was tested by enzyme-linked immunoabsorbent assays(ELISA)after directly adding compound and extract from liver-softening herbs to the culture at the final concentration of 10 mg/ml for 3 days.Results Liver-softening herbal compound group had significant effect on cell proliferation compared to control,of which,3-hour subgroup was more significant than 1-and 5-hour subgroups(P
3.Influence of humic acid fertilizer on biomass accumulation and quality of Angelica sinensis.
Yan-An WU ; Hai-Ming LIN ; Zhan-Feng CAO ; Xiao-Rui LIU
China Journal of Chinese Materia Medica 2008;33(3):251-255
OBJECTIVETo study the influence of humic acid fertilizer on plant growth, assimilation base, dried biomass accumulation, yield, quality and disease infection of Angelica sinensis.
METHODThree kinds of humic acid fertilizer and an amino acid liquid fertilizer were tested in randomized groups at 1 level with 3 times repeat.
RESULTT1 promoted plant and root growth effectively, increased dried biomass accumulation and fresh root average weight remarkably, the yield was increased, the content of ethanol extract was increased by 11.31%. T3 promoted plant and root growth quickly, enlarged leaves area and increased dried plant weight, but effect lasted shortly, the content of ethanol extract was increased by 5.23%. T4 increased more leaves in late growth period, enlarged leaves area, the yield was increased, the content of ethanol extract was increased by 3.09%. T2 increased fresh root average weight remarkably, the yield was increased.
CONCLUSIONHumic acid fertilizer and amino acid liquid fertilizer could effectively promote plant growth, enlarge leaves area, promote dried biomass accumulation and transformation to root and increase yield and content of ethanol extract effectively.
Angelica sinensis ; growth & development ; metabolism ; Biomass ; Fertilizers ; Humic Substances ; Plant Leaves ; growth & development ; metabolism ; Plant Roots ; growth & development ; metabolism
4.Research progress on the traditional Chinese medicine-pharmaceutical drug interaction mediated by the ABC transporter family
Yu-zhen HE ; Hui WANG ; Jia-hao FANG ; Yu-hong CAO ; Zhan-ying HONG ; Yi-feng CHAI
Acta Pharmaceutica Sinica 2021;56(7):1778-1788
ABC transporters on the intestinal barrier, blood-brain barrier and on tumor cells will affect drug bioavailability, transport across the blood-brain barrier and multidrug resistance. The active ingredients of traditional Chinese medicines can affect the function and expression of ABC transporters. When combined with pharmaceuticals the potential interaction between the two can change the efficacy of the medicines. We review the ABC transporter superfamily and their distribution with regard to their relationship and interactions with traditional Chinese medicine on the intestinal barrier and the blood-brain barrier, as well as their role in tumor multidrug resistance mediated by ABC transporters. We summarize the research progress over the past five years.
5.Synthesis and biodistribution of a bi-functional agent 99Tcm-Gd-DTPA-DG in tumor bearing nude mice
Wei, ZHANG ; Liang, CAI ; Yue, CHEN ; Zhan-wen, HUANG ; Zhi-ling, DING ; Feng, CAO ; Li, ZHANG ; Ling, HE
Chinese Journal of Nuclear Medicine 2011;31(2):117-120
Objective To evaluate the stability and biodistribution of a novel SPECT-MRI bi-functional agem 99Tcm-Gd-DTPA-DG in tumor-bearing nude mice. Methods DTPA-DG was synthesized and then conjugated with Gd2O3 to generate Gd-DTPA-DG. The tumor-bearing nude mice were scanned by MRI to evaluate the tumor targeting ability of Gd-DTPA-DG. The orthogonal experiment was applied to optimize pH value of reaction medium and reaction temperature. The radiolabeling efficiency was measured by thin layer chromatography. The distribution of 99Tcm-Gd-DTPA-DG in nude mice was evaluated by scintigrapy in vivo. The % ID/g was measured at different time after intravenous injection of 99Tcm-Gd-DTPA-DG. Results The tumor was significantly enhanced by Gd-DTPA-DG with MRI. The radiochemical purity of 99Tcm-Gd-DTPADG was about 98.5% and remained 96.2% at room temperature for 6 h. The tumor was well visualized by 99TcmGd-DTPA-DG SPECT at 2 h after injection. The tumor uptake was (1.48 ±0.12) %ID/g, and the rumor to muscle radioactivity ratio was 2.91. Conclusions MRI contrast of Gd-DTPA-DG may enhance tumor detection. 99Tcm-labeled Gd-DTPA-DG may be useful for tumor imaging and might have a potential role as a SPECT-MRI bi-functional agent.
6.Study on distribution features of tender points in patients with knee osteoarthritis by cluster analysis.
Jian PANG ; Ying SHI ; Yue-long CAO ; Dong-Yu CHEN ; Xin-Feng GU ; Bo CHEN ; Yu-Yun WU ; Hong-Sheng ZHAN ; Yin-Yu SHI
China Journal of Orthopaedics and Traumatology 2014;27(1):21-24
OBJECTIVETo observe the distribution features of tender points in knee of patients with knee osteoarthritis in order to provide evidences for the treatment and diagnosis.
METHODSFrom November 2011 to December 2012,86 patients with knee osteoarthritis were recruited, including 21 males and 65 females, ranging in age from 45 to 85 years old, with an average of (59.98 +/- 8.23) years old. The course of disease ranged from 3 months to 15 years. The tender points and its distributions were determined by finger press carefully on their knees. Data of studying was analyzed by frequency statistics and Hierachical cluster analysis.
RESULTSThe distribution of tender points in the knee osteoarthritis was mainly in the interior region and anterior area such as in apex of patella, adductor tubercle and et al. According to the results of hierachical cluster analysis, the tender points could be divided into two categories the first cluster was in the interior region of knee, the second cluster was in the lateral region.
CONCLUSIONThe findings demonstrated that cluster analysis statistical method can be used for classification of the distribution of tender points. The distribution features of tender points in knee osteoarthritis are related to the anatomic site in knee.
Adult ; Aged ; Aged, 80 and over ; Cluster Analysis ; Female ; Humans ; Male ; Middle Aged ; Osteoarthritis, Knee ; complications ; Pain ; complications
7.Comparison of protective effects of safflor injection and extract of Ginkgo biloba on lung ischemia/reperfusion injury in rabbits.
Xiao-xi TIAN ; Bo-liang WANG ; Yi-zhan CAO ; Yue-xia ZHONG ; Yan-yang TU ; Jian-bo XIAO ; Qian-feng HE ; Li-na ZHAI
Chinese journal of integrative medicine 2015;21(3):229-233
OBJECTIVETo observe the protective effects of safflor Injection (SI) and extract of Ginkgo biloba (EGB) on lung ischemia-reperfusion injury (LIRI) and investigate its mechanism.
METHODSIn vivo rabbit model of LIRI was reconstructed. Forty rabbits were randomly and equally divided into four groups: sham-operation group (sham group), ischemia-reperfusion group (model group), ischemia-reperfusion plus SI group (safflor group) and ischemia-reperfusion plus EGB injection group (EGB group). Malondialdehyde (MDA) content, superoxide dismutase (SOD) and xanthine oxidase (XO) activity in serum were measured. The wet/dry weight ratio (W/D) of the lung tissue and activity of myeloperoxidase (MPO) were also tested. Ultrastructure change of the lung tissue was observed by the electron microscope. The expression of intercellular adhesion molecule-1 (ICAM-1) was measured by immunohistochemistry (IHC).
RESULTSIn the model group, MDA and XO increased and SOD decreased in serum compared with the sham group (P<0.01). The values of W/D, MPO and ICAM-1 of the model group were higher than those of the sham group (P<0.01), but those of the safflor group and EGB group were significantly lower than those of the model group (P<0.01). The IHC demonstrated that ICAM-1 expression in lung tissue of the model group was significantly higher than those of the safflor group (P<0.01). Compared with safflor group, in the EGB group MDA, XO, MPO decreased, SOD and ICAM-1 expression increased (P<0.05), but the change of W/D was not statistically significant (P>0.05).
CONCLUSIONSSI and EGB may attenuate LIRI through antioxidation, inhibition of neutrophil aggregation and down-regulation of ICAM-1 expression. But EGB had more effect on the antioxidation, while SI did better on regulating ICAM-1 expression.
Animals ; Female ; Ginkgo biloba ; chemistry ; Immunohistochemistry ; Injections ; Intercellular Adhesion Molecule-1 ; metabolism ; Lung ; blood supply ; pathology ; Male ; Malondialdehyde ; metabolism ; Plant Extracts ; administration & dosage ; pharmacology ; therapeutic use ; Protective Agents ; administration & dosage ; pharmacology ; therapeutic use ; Rabbits ; Reperfusion Injury ; blood ; drug therapy ; Safflower Oil ; administration & dosage ; pharmacology ; therapeutic use ; Superoxide Dismutase ; blood ; Xanthine Oxidase ; blood
8.Study on the diagnostic value of whole-organ magnetic resonance imaging score (WORMS) in knee osteoarthritis.
Xue-Zong WANG ; Yu-Xin ZHENG ; Yue-long CAO ; Xin-Feng GU ; Song-Pu WEI ; Ning-yang GAO ; Ting LIU ; Jian PANG ; Hong-Sheng ZHAN
China Journal of Orthopaedics and Traumatology 2012;25(5):364-368
OBJECTIVETo explore the diagnostic value of whole-organ magnetic resonance imaging score (WORMS) in knee osteoarthritis (KOA).
METHODSFrom November 2009 to January 2011,70 patients with KOA combined with knee effusion among outpatient and inpatient were analyzed retrospectively. Among the patients, 12 patients were male, 58 patients were female,ranging in age from 46 to 75 years,with a mean age of (59.66 +/- 9.93) years. The clinical symptoms were evaluated by WOMAC, the imaging of KOA was assessed by K-L score and WORMS, and COMP and CTX- II were measured respectively by ELISA. The correlation analyses and multiple linear regression analysis were studied to determine associations among biomarkers, clinical variables and radiographic findings of knee joints.
RESULTSThe average scores of WOMAC and WORMS were (57.50 +/- 8.20) and (64.54 +/- 16.45) respectively. The median of CTX- II nd COMP were 2.42 ng/ml and 4.56 ng/ml respectively. Grouped by less than the lowest quartile and more than the highest quartile of WORMS, COMP was significantly different (Z=2.04, P=0.039), but there was no significant difference in CTX-II (Z=0.79, P=0.427). WORMS were positively correlated with WOMAC and K-L score (r=0.777, P<0.01; r=0.716, P<0.01; respectively); WOMAC was also positively correlated with K-L score (r=0.692, P<0.01). WORMS's cartilage, osteophytes and synovitis were positively correlated with WOMAC, K-L score and COMP respectively (r=0.771, P<0.01; r=0.509, P<0.01; r=0.917, P<0.01). It was determined by stepwise regression that the KOA was mainly affected by WORMS, K-L score (P=0.015, P=0.025 respectively) when WOMAC as a dependent variable, age, gender, K-L score, WORMS, COMP and CTX- II as independent variables (F=20.327, P<0.01).
CONCLUSIONWORMS has a better reference value for diagnosis of KOA. The expression of COMP is high in the synovial fluid when WORMS at the high point. The clinical symptoms of knee osteoarthritis are mainly affected by WORMS and K-L score.
Aged ; Cartilage Oligomeric Matrix Protein ; Collagen Type I ; analysis ; Extracellular Matrix Proteins ; analysis ; Female ; Glycoproteins ; analysis ; Humans ; Magnetic Resonance Imaging ; methods ; Male ; Matrilin Proteins ; Middle Aged ; Osteoarthritis, Knee ; diagnosis ; metabolism ; physiopathology ; Peptides ; analysis
9.Beta-cell dysfunction is the primary contributor to the early postpartum diabetes among Chinese women with history of gestational diabetes mellitus.
Xiao-pei CAO ; Hai-peng XIAO ; Song-jin CHEN ; Yan-feng ZHAN ; Ling-ling XIU ; Zi-lian WANG
Chinese Medical Journal 2008;121(8):696-700
BACKGROUNDWomen with a history of gestational diabetes mellitus (GDM) are at higher risk of future development of diabetes. This study investigated the risk factors associated with early postpartum abnormal glucose regulation (AGR) among Chinese women with a history of GDM.
METHODSA total of 186 women with a history of GDM were screened for early postpartum AGR at 6-8 weeks after delivery. Those with AGR were given lifestyle intervention therapy and reevaluated in 6-12 months. The demographic, anthropometric, prenatal and delivery data were recorded. The plasma high-sensitivity C-reactive protein (HsCRP) and lipid concentration were measured, and insulin secretion were analyzed. Insulinogenic index Deltains30'/DeltaBG30', the homeostasis model assessment index (HOMA)-B, and HOMA-IR were calculated. Multiple regression analysis was performed to identify the risk factors.
RESULTSOf the GDM women 28.0% (52/186) had AGR at 6-8 weeks after delivery; 45.2% (17/40) of these AGR women reminded abnormal after 6-12 month lifestyle intervention. Compared to the women who reverted to normal, women with consistent AGR showed significantly lower fasting insulin concentration, lower Deltains30'/DeltaBG30' as well as lower HOMA-B. No significant differences in age, body mass index (BMI), waist circumference, blood pressure, lipid level, HsCRP and HOMA-IR were observed between the two groups. Pre-pregnancy BMI = 25 kg/m(2), fasting glucose level = 5.6 mmol/L and/or 75 g oral glucose tolerance test (OGTT) 2 hours glucose level = 11.1 mmol/L during pregnancy were predictors for the AGR at 6-8 weeks after delivery. Deltains30'/DeltaBG30 = 1.05 was a significant risk contributor to the consistent early postpartum AGR.
CONCLUSIONThere is a high incidence of early postpartum AGR among Chinese woman with prior GDM. Beta-cell dysfunction, rather than insulin resistance or inflammation, is the predominant contributor to the early onset and consistent AGR after delivery.
Adult ; Asian Continental Ancestry Group ; China ; Diabetes Mellitus, Type 2 ; etiology ; Diabetes, Gestational ; Female ; Humans ; Insulin-Secreting Cells ; physiology ; Pregnancy ; Puerperal Disorders ; etiology ; Risk Factors
10.Setting up a risk prediction model on metabolic syndrome among 35-74 year-olds based on the Taiwan MJ Health-checkup Database
Xing-Hua YANG ; Qiu-Shan TAO ; Feng SUN ; Chun-Keng CAO ; Si-Yan ZHAN
Chinese Journal of Epidemiology 2013;34(9):874-878
Objective This study aimed to provide an epidemiological modeling method to evaluate the risk of metabolic syndrome (MS) development in the coming 5 years among 35-74 year-olds from Taiwan.Methods A cohort of 13 973 subjects aged 35-74 years who did not have metabolic syndrome but took the initial testing during 1997-2006 was formed to derive a risk score which tended to predict the incidence of MS.Multivariate logistic regression was used to derive the risk functions and using the ‘check-up center' (Taipei training cohort) as the overall cohort.Rules based on these risk functions were evaluated in the remaining three centers (as testing cohort).Risk functions were produced to detect the MS on a training sample using the multivariate logistic regression models.Started with those variables that could predict the MS through univariate models,we then constructed multivariable logistic regression models in a stepwise manner which eventually could include all the variables.The predictability of the model was evaluated by areas under curve (AUC) the receiver-operating characteristic (ROC) followed by the testification of its diagnostic property on the testing sample.Once the final model was defined,the next step was to establish rules to characterize 4 different degrees of risks based on the cut points of these probabilities,after being transformed into normal distribution by log-transformation.Results At baseline,the range of the proportion of MS was 23.9% and the incidence of MS in 5-years was 11.7% in the non-MS cohort.The final multivariable logistic regression model would include ten risk factors as:age,history of diabetes,contractive pressure,fasting blood-glucose,triglyceride,high density lipoprotein cholesterol,low density lipoprotein cholesterol,body mass index and blood uric acid.AUC was 0.827 (95% CI:0.814-0.839) that could predict the development of MS within the next 5 years.The curve also showed adequate performance in the three tested samples,with the AUC and 95% CI as 0.813 (0.789-0.837),0.826(0.800-0.852) and 0.794(0.768-0.820),respectively.After labeling the degrees of the four risks,it was showed that over 17.6% of the incidence probability was in the population under mediate risk while over 59.0% of them was in the high risk group,respectively.Conclusion Both predictability and reliability of our Metabolic Syndrome Risk Score Model,derived based on Taiwan MJ Longitudinal Health-checkup-based Population Database,were relatively satisfactory in the testing cohort.This model was simple,with practicable predictive variables and feasible form on degrees of risk.This model not only could help individuals to assess the situation of their own risk on MS but could also provide guidance on the group surveillance programs in the community regarding the development of MS.