4.Searching for drug targets in microbial genomes
Jianhe SUN ; Ping LU ;
Chinese Pharmacological Bulletin 1987;0(01):-
Genome sequencing and bioinformatics is driving the discovery of drug targets and development of novel classes of broad spectrum antimicrobial compounds. The analysis of the complete genome sequences of microorganism available in the public databases offers the first insights into the drug targets discovery. This review discusses the use of genomic information in the finding of target genes for antimicrobial drug discovery.
5.S-1 as first-fine treatment for advanced gastric cancer
Journal of International Oncology 2014;41(3):211-213
Patients with advanced gastric cancer lose the surgical indications.Chemotherapy can improve the overall survival and quality of life,which is the main treatment option.But there is no standard chemotherapy regimen for the patients with advanced gastric cancer.Since its initial approval,S-1 is widely used in gastric cancer.Several studies were performed to explore combinations of S-1 with other cytotoxic drugs such as platinum,docetaxel,paclitaxel,and irinotecan.All these combinations were found to be promising,with response rates of around 40%-50% and relatively favorable safety profiles.
6.Transient receptor potential channels 6 in tumor
Journal of International Oncology 2011;38(9):656-659
Transient receptor potential (TRP) is a kind of novel Ca2+ permeant channel.It is later found that TRP channels are expressed broadly in many organisms,tissues and cell types.It is involved in the regulation of sensory conduction and cell signal transduction.Further studies are required to assess which TRPC6(a member of TRPC subfamily) is associated with the cytosolic Ca2+ levels,development and progression of cancer and tumor cell cycle.TRPC6 may be regarded as new targets for the treatment of cancer.
7.Evaluating the effect of embelin combined with paclitaxel on inhibiting A549 lung cancer cell proliferation and tumor growing in tumor-bearing nude mice growing
Chinese Journal of Biochemical Pharmaceutics 2014;(2):7-9
Objective To evaluate the effect of embelin combined with paclitaxel on the inhibition of A 549 lung cancer cell proliferation and tumor growing in tumor bearing nude mice. Methods The anti-proliferation efficiency of embelin combined with paclitaxel were evaluated by MTT assay, and A 549 cell apoptosis were evaluated by lfow cytometry. A 549 cells were xenografted in mice to establish the animal model, which were used to evaluate the effect of anti-tumor. Results compared to saline group、embelin group and paclitaxel group, the (paclitaxel+embelin) group could inhibit the growth of A 549 cells effectively(P<0.05). The embelin combined with paclitaxel induced the apoptosis of A 549 cells more effective than paclitaxel alone. The (paclitaxel+embelin) group significantly inhibited the growth of tumor tissue. Conclusion the paclitaxel can inhibit the growth of A 549 cells, the embelin can induce the apoptosis of A 549 cells, and the combination of paclitaxel and embelin may be a potentially effective treatment for lung cancer.
8.Protective effect of Xiongbitongcapsule on liver injury in hyperlipemic rats
International Journal of Traditional Chinese Medicine 2014;(11):997-1001
Objective To investigate the protective role of Xiongbitong capsule against liver injury in hyperlipemic rats.Methods Sixty Wistar male rats were randomly divided into 5 groups(12 rats in each group): a blank group, a model group, a simvastatin group(10 mg/kg, 2 ml intragastric administration daily), a Xiongbitong capsule high-dose group(25 mg/kg, 2 ml intragastric administration daily), and a Xiongbitong capsule low-dose group(12.5 mg/kg, 2 ml intragastric administration daily). Hyperlipidemia model in rats was indeuced by hyperlipidemic diet. The simvastatin group was intragastric administrated with simvastatin suspension 2 ml(10 mg/kg daily), and the rats in the control group and the model group were intragastric administrated with equal volume of saline. After 10 weeks, the serum leves of total cholesterol(TC), triacylglycerol(TG), low-density lipoprotein cholesterol(LDL-C), high-density lipoprotein cholesterol (HDL-C), nitric oxide(NO), endothelin1(ET-1), and the whole blood viscosities(high-, medium-, low-shear)were measured. Liver injury were evaluated with histopathologic examination by H.E. staining. The expressions of intercellular adhesion molecule-1(ICAM-1), monocyte chemoattractant protein-1(MCP-1)in hepatic tissue were measured by immunohistochemical staining.Results The serum leves of TC(1.47± 0.10 mmol/Lvs. 3.48±0.19 mmol/L), TG(0.38±0.11 mmol/Lvs. 0.95±0.14 mmol/L), LDL-C(1.48± 0.18 mmol/Lvs. 2.39±0.22 mmol/L), ET-1(145.81±18.65 pg/mlvs. 177.70±17.70 pg/ml) in the Xiongbitong capsule high-dose group were significantly lower than those in the model group(allP<0.01), HDL-C(1.21±0.14 mmol/Lvs. 0.65±0.10 mmol/L)and NO(31.28±2.36μmol/Lvs. 19.61±1.28μmol/L) significantly lower than those in the model group(allP<0.01), the expressions of ICAM-1(0.133±0.019vs. 0.187±0.011)and MCP-1(0.153±0.014vs. 0.264±0.020)significantly lower than those in the model group(allP<0.01). The liver injury in the Xiongbitong capsule high-dose group decreased than that in the model group. Conclusions Xiongbitong capsule can protect against liver injury via regulating lipid metabolism, protecting endothelial function and down regulating expressions of MCP-1 and ICAM-1.
9.Preparation of transferrin and RGD co-modified PLGA nanoparticles and its targeting to melanoma
Chinese Journal of Biochemical Pharmaceutics 2014;37(4):19-21
Objective To prepare transferrin and Arg-Gly-Asp polypeptide co-modified nanoparticles(TF/RGD-NPs)and evaluate its targeting efficiency to melanoma.Methods The co-modified nanoparticles were prepared by emulsion method and its appearance,particle size and Zeta potential were evaluated.The cellular uptake experiment and melanoma tumor spheroids penetration test were used to evaluate the affinity and ability to penetrate tumor tissues of TF/RGD-NPs to melanoma B16 cells. Results The particle diameter of co-modified nanoparticles was(113.4 ±12.5)nm and the Zeta potential was(4.53 ±2.15)mV.In vitro uptake test demonstrated that the efficacy of cellular uptaken TF/RGD-NPs by B16 cells were 2.7 times and 2.9 times to TF-NPs and RGD-NPs,respectively,the differences were all significant(P<0.05 ).Tumor spheroid penetration test results showed that TF/RGD-NPs has good affinity to melanoma cells.Conclusion TF/RGD-NPs can target to melanoma B16 cell efficiency in vitro,it may be serve as a potential drug delivery system for targeting melanoma.
10.Adjuvant chemotherapy of stage Ⅱ colon cancer
Journal of International Oncology 2013;(6):463-465
For stage Ⅱ colon cancer patients after surgery,the benefit of adjuvant chemotherapy remains controversial.Several studies indicate that the patients with high-risk stage Ⅱ colon cancer can benefit from adjuvant chemotherapy after surgery.According to the clinical and pathological features,the stage Ⅱcolon cancer patients including T4 lesion,perforation,peritumoral lymphovascular invasion can benefit from the adjuvant chemotherapy of oxaliplatin.In the horizontal of molecular and genetic levels,the stage Ⅱ colon cancer patients can express high microsatellite instability (MSI-H) and cannot benefit from the chemotherapy of Fluorouracil.The guiding functions of 18q loss of heterozygosity (18q LOH),Cx43 and gene expression profiling in adjuvant chemotherapy are still unclear,and need further study.