1.Network pharmacology: new guidelines for drug discovery.
Acta Pharmaceutica Sinica 2010;45(12):1472-7
The development of new drug is not only the main driving force for the development of pharmaceutical industry, but also plays a very important role in the social development. However, with the increasing demands, new drug development is facing great difficulties in recent years. The hypothesis of highly selective single-target is meeting the challenges because of its limitations. Network pharmacology has been one of the new strategies for new drug discovery based on single-target drug research in recent years. This paper focused on the basis of network pharmacology and its research progress, discussed its development direction and application prospects, and analyzed its limitations and problems as well. The application of network pharmacology in new drug development is discussed by comparing its guidelines with those of traditional Chinese medicine theory and Effective Components Group hypothesis of Chinese medicines.
2.Prevention on the side effects of erythromycin lactobionate via intervenous drop infusion for the gastrointestinal tract in children
Chinese Journal of Clinical Pharmacology and Therapeutics 2004;0(12):-
AIM:To observe the preventive effects of aluminum phosphate gel and smectite powder on the side effects of erythromycin lactobionate via intervenous drop infusion for the gastrointestinal tract in children.METHODS:249 cases children with mycoplasmal pneumonia were randomly divided into three groups,aluminum phosphate gel group,smectite powder group and control group,83 cases in each group.The side effects of erythromycin lactobionate(abdominal pain,diarrhea,sicchasia,disgorging)for the gastrointestinal tract among three groups were observed.RESULTS:Compared with control group,the incidence rate of side effects was much lower in aluminum phosphate gel group and smectite powder group(P0.05).CONCLUSION:Aluminum phosphate gel and smectite powder significantly decrease the side effects of erythromycin lactobionate for the gastrointestinal tract in children,and especially the former,can be widely applied in pediatric clinic.
3.Correction of over rotation of nasal tip
Ailin LI ; Dingan LUO ; Siyang LIU
Chinese Journal of Medical Aesthetics and Cosmetology 2008;14(5):315-317
Objective To investigate a safe and effective method to correct the over rotation of nasal tip in rhinoplasty. Methods 16 cases, including 11 of primary and 5 of secondary over rotation of nasal tip, were corrected with strut grafts using autologous cartilage or combined with Medpor to reconstruct the supporting structures underneath to improve the upward and forward strength of the nasal tip in order to increase the nasal height and to correct the over rotation of of nasal tip. The shield and cap grafts were also used for the patients whose nasal tip were too low, with vertical dome division technique. Results 16 cases were corrected satisfactorily, the nasal lip angles were normal and there were no complications by follow-up from 6 months to 1 year. Conclusion It is necessary to provide powerful forward and upward strength to correct the over rotation of nasal tip effectively and safely, and proper cartilage grafts can im-prove the height of the nasal tip and correct the over rotation of the nasal tip further.
4.A study on the standard of influenza neuraminidase inhibition assay.
Fan YANG ; Ailin LIU ; Guanhua DU
Acta Pharmaceutica Sinica 2012;47(6):730-3
In present study, standard method and standard operation practice for measuring the activities of influenza neuraminidase and its inhibitors have been established. The accuracy and stability of the method has been evaluated. Standard operation is as following: 10 microL sample, 30 microL neuraminidase and 60 microL substrate are added to one well of a 96-well plate, and then incubated at 37 degrees C for 1 h. The reaction was stopped with NaOH before fluorescence intensity determination. One unit of neuraminidase is defined as the amount of enzyme that produces 1 nmol 4-MU in 1 h under above conditions. The inhibition accuracy is indicated by an uncertainty measurement of 6.51 x 10(-12), and its stability was reaffirmed by determination of oseltamivir acid. In this study, systematic assessment of neuraminidase inhibitory assay not only provided theoretical basis of its application in drug discovery, but also made preliminary attempt to use uncertainty measurement as a parameter in biological measurement.
5.Correction of short collumella by using the free composite graft of ear lobe
Ailin LI ; Shengguo SHAN ; Siyang LIU
Chinese Journal of Medical Aesthetics and Cosmetology 2009;15(3):152-154
Objective To investigate a simple and safe method for correction of the flat nose tip with the short columella. Methods The flat nose tip with the extend strut graft was corrected by using the rib cartilage or Medpor and the secondary defect of columella was repaired with the free composite graft of ear lobe in 8 cases of rhinoplasties. Results The free composite graft of ear lobe survived well and the color was similar to the neighboring tissue. There was no obviously secondary deformation at the donor site in all the cases by following-up from 1 to 2 years. Conclusions It is a simple and effective method without secondary deformation to repair the short columella by using the free composite graft of ear lobe in rhinoplasty.
6.Study on DNA Damage Induced by Chlorinated By-Product MX in Drinking Water
Jianjun WU ; Ailin LIU ; Wenqing LU
Journal of Environment and Health 1989;0(06):-
Objective To study DNA damage induced by chlorinated drinking water by-product MX.Methods Hu-man hepatocellular carcinoma cell line HepG2cells was selected as target cells to test the DNA damage induced by MX using single cell gel electrophoresis assay.In this study,the cells were treated with MX at final concentrations of10,30,100and300?mol/L.DMSO and hydrogen peroxide were administered as solvent control and positive control respectively.Results MX induced DNA single strand breaks at the concentrations of30,100and300?mol/L.The length of DNA migration induced by MX increased significantly in comparison with the solvent control(DMSO)in a dose-response manner.Conclusions Chlorinated by-product MX in drinking water could induce obvious DNA damage to human hepatocellular carcinoma cell line HepG2cells.
7.Research advance in the drug target prediction based on chemoinformatics.
Jiansong FANG ; Ailin LIU ; Guanhua DU
Acta Pharmaceutica Sinica 2014;49(10):1357-64
The emerging of network pharmacology and polypharmacology forces the scientists to recognize and explore new mechanisms of existing drugs. The drug target prediction can play a key significance on the elucidation of the molecular mechanism of drugs and drug reposition. In this paper, we systematically review the existing approaches to the prediction of biological targets of small molecule based on chemoinformatics, including ligand-based prediction, receptor-based prediction and data mining-based prediction. We also depict the strength of these methods as well as their applications, and put forward their developing direction.
8.Expression and clinical significance of bone marrow sclerostin in patients with multiple myeloma
Xiaotao WANG ; Ailin TANG ; Yuwei NIE ; Jian LIU ; Ling LIU
Chongqing Medicine 2013;(26):3081-3083,3086
Objective To investigate the bone marrow supernatant expression of sclerostin in the patients with multiple myeloma (MM) and to clarify its clinical signification .Methods The sclerostin level was quantified by using ELISA ,and the gene expression of sclerostin was determined by RT-PCR .Results The sclerostin level was (0 .54 ± 0 .21)pg/mL in the MM group ,which was sig-nificantly higher than (0 .31 ± 0 .06)pg/mL in the control group (t=5 .67 ,P<0 .01) .The sclerostin level was (0 .65 ± 0 .17) pg/mL in the recurrent and refractory MM group ,which was significantly higher than (0 .47 ± 0 .21) pg/mL in the control group and the newly diagnosed group (t=8 .44 ,3 .27 ,P<0 .01) ,RT-PCR verified that the BMMNC of most patients expressed sclerostin gene .The expression of sclerostin in the MM group was negatively correlated with alkaline phosphatase (ALP)(r= -0 .379 ,P=0 .005) ,and positively related with the correction blood calcium ,bone loss points ,serum β2-micro globulin(β2-GM ) ,proportion of serum M protein and clinical International Staging System (ISS) stages .The median follow-up periods were 29(6-65) months ,the low sclerostin group had the median survival period of 48(6-65) months and the high sclerostin group had the median survival pe-riod of 24(6-52) months ,the difference between them had statistical significance (χ2 = 12 .74 ,P< 0 .01) .Conclusion Its level may reflect the bone destruction ,osteogenesis inhibition degree and myeloma burden ,and reflect the median survival period of MM patients to some extent .
9.Ultrasonic ablation in chronic deep vein thrombosis of lower extremities
Ailin WANG ; Dongmei JING ; Shenghui HAN ; Jun LIU ; Li LIU
Journal of Interventional Radiology 2001;0(05):-
Objective To evaluate the clinical efficacy of ultrasonic ablation in patients with chronic deep vein thrombosis of lower extremities. Methods Fifty-six patients with chronic deep vein thrombosis resulting in total occlusion of iliac-femoral veins accepted intra-venous ultrasonic ablation. The time for ultrasonic ablation was 12-24 minutes with the mean being 18 minutes. After the procedure, anti-coagulation was performed through the retaining catheters and venous propeller was utilized for promoting blood reflow. Results Ultrasonic ablation easily created a channel within the occlusive iliac-femoral veins and achieved successful recanalization in 49 of 56 patients (87.5%). Five patients (8.9%) were partially re-canalized and 2 (3.6%) had no recanalization. Thirty-eight of the 49 re-canalized patients were followed up, including 22 with no stent placement showed 9 (40.9%) re-occlusion and 16 received stent placement, and 2 had (12.5%) re-occlusion. Conclusions Intravascular ultrasonic ablation is an effective therapeutic modality to recanalize chronic thrombosed occlusion of iliac-femoral veins and can lay down a foundation for further balloon-expansion or stent-placement with long term patency.
10.Effects of pyrroloquinoline quinine on oxidative stress-induced apoptosis of Schwann cells and its mechanism.
Bin HE ; Haiying TAO ; Ailin WEI ; Shiqing LIU ; Haohuan LI
Chinese Journal of Plastic Surgery 2014;30(2):111-117
OBJECTIVETo investigate the effects of Pyrroloquinoline quinine (PQQ) on hydrogen peroxide-induced apoptosis of Schwann cells (SCs) and its mechanism.
METHODSSCs were isolated and cultured in vitro, and identified by S-100 immunofluorescence staining. The cultured SCs were divided into control group, hydrogen peroxide-treated group, hydrogen peroxide and PQQ treated groups. The intracellular superoxide dismutase (SOD) and malondialdehyde (MDA) content was detected; the apoptotic rate of SCs induced by hydrogen peroxide was determined by flow cytometry assay. The Hoechst33342 staining was used to detect the nuclear fragmentation and apoptotic nuclear condensation of SCs; the Rhodamine123 staining was used to detect the changes of mitochondrial membrane potential in SCs, the Western blot analysis was used to detect the expression of Bcl-2 in hydrogen peroxide induced SCs.
RESULTSThe SOD activity was significantly decreased and MDA level was increased in H2O2 induced SCs (P < 0.05), after addition of PQQ, the SOD content increased and MDA content decreased (P < 0.05). Flow cytometry results showed that the early apoptotic rate was 58.8% in H2O2 induced SCs, which has significant difference compared with the control group (P < 0.05), after addition of 10, 50, 100 nmol/L PQQ, the apoptotic rates were reduced to 33.7%, 18.7%, 3.9% respectively, showing significantly different with injured group (P < 0.05). Hoechst 33342 staining showed that H2O2 induced SCs had typical morphological characteristics, such as uptake of nuclear chromatin, nuclear shrinkage, nuclear fragmentation phenomenon. The proportion of apoptotic cells after PQQ treatment reduced. Rhodamine staining results showed that the H2O2 induced mitochondrial membrane potential reduction in SCs, which was reversed by addition of PQQ. Western blot analysis showed that the expression of Bcl-2 was decreased in H2O2 induced SCs, while it increased significantly after addition of PQQ (P < 0.05).
CONCLUSIONPQQ has a protective effect on oxidative stress-induced apoptosis of SCs.
Apoptosis ; drug effects ; Benzimidazoles ; Cell Nucleus ; drug effects ; DNA Fragmentation ; Fluorescent Dyes ; Humans ; Hydrogen Peroxide ; pharmacology ; Malondialdehyde ; metabolism ; Oxidants ; pharmacology ; Oxidative Stress ; Pyrroles ; pharmacology ; Quinine ; pharmacology ; Quinolines ; pharmacology ; Schwann Cells ; cytology ; drug effects ; Superoxide Dismutase ; metabolism