Research progress on tumor-targeting paclitaxel prodrugs / 药学实践杂志

Paclitaxel is a natural compound with efficient broad-spectrum antitumor activity .However ,the clinical ap-plication has been limited owing to the undesirable drawbacks ,such as the poor water-solubility ,cardiovascular toxicity and neurotoxicity .The design of paclitaxel prodrugs is an effective measure which can improve the drug's druggability ,alleviate its toxicity adverse effect and enhance its antitumor effect .With the in-depth research of prodrugs ,tumor-targeting paclitaxel pro-drugs which using the excessive receptors ,specific enzymes ,transporters ,reactive oxide species ,glutathione in tumor tissues as well as acidosis and hypoxia in tumors as specific targets ,have made great progress .The relevant literature about paclitaxel prodrugs were reviewed in this paper ,which targeted to the specific pathological and physiological features of tumor microenvi-ronment in recent years.

Synthesis and druggability study of triptolide stearate / 药学实践杂志

Objective To synthesize a lipophilic prodrug of triptolide (TP) and improve its druggability .Methods Trip-tolidestearate (TP-SA)was synthesized via the DMAP-catalyzed DCC method and identified by MS ,1H-NMR and 13C-NMR. The shake-flask method was used to study the oil/water partition coefficient .The preparations of TP and TP-SA liposomes and emulsions were compared .Their encapsulation efficiency and stability were investigated .Results TP-SA was synthesized suc-cessfully .Its log P in octanol/water system was 2 .33 .It was difficult to prepare TP liposome or emulsion .By contrast ,TP-SA liposome and emulsion can be prepared successfully with the same formulation process .The particle size of TP-SA lipo-somes were about 90 nm and TP-SA emulsions were about 110 nm .The encapsulation efficiency was above 95% .Their stabili-ty were studied at 4℃ and 25℃ .The preparation parameters ,such as particle size and encapsulation efficiency ,had no signif-icant change in a week .Conclusion Triptolide stearate enhanced drug lipophilicity .Its druggability was improved significant-ly .These data can be used for the TP related drug design and development .

Postoperative quality of life of cervical cancer patients treated by laparoscopic surgery / 中国内镜杂志

Objectives To investigate the postoperative quality of life of cervical cancer patients treated by laparo-scopic surgery. Methods 27 cases of cervical cancer treated by laparoscopic surgery from May 2009 to September 2010 as observation group, 27 cases of cervical cancer treated by laparotomy treatment in the same period as control group. Observe and analyzed the clinical data, operation, postoperative recurrence and survival rates and postopera-tive FACT-G score between the two groups. Results Age, body mass index has no statistical difference between the two groups ( > 0.05), the blood loss in observation group was less than that in control group ( < 0.05), the lymph node dissection number in observation group was more than that in control group ( < 0.05), the exhaust time and hospital stay in observation group were less than that in control group ( <0.05), the 1-year, 3-year and 5-year re-currence rate and survival rate in observation group showed no significant difference compared with control group ( < 0.05). The 1-year, 3-year and 5-year FACT-G score in control group were higher than that in control group ( < 0.05). Conclusion Laparoscopic surgery for cervical cancer patients can reduce bleeding, shorten exhaust time and hospitalization time, improve postoperative FACT-G score and postoperative quality of life of cervical cancer pa-tients.

Rapid simultaneous determination of ten major flavonoids in Tetrastigma hemsleyanum by UPLC-MS/MS / 药学学报

In this study, a rapid and sensitive analytical method was developed for the determination of 10 major compounds (procyanidin B1, catechin, procyanidin B2, rutin, isoquercitrin, kaempferol-3-O-rutinoside, astragalin, quercitrin, quercetin, and kaempferol) in Tetrastigma hemsleyanum by using ultra-performance liquid chromatography coupled with triple-quadrupole tandem mass spectrometry (UPLC-MS/MS) in multiple-reaction monitoring (MRM) mode. UPLC-MS/MS assay with negative ion mode was performed on a Waters CORTECS C18 (2.1 mm x 100 mm, 1.6 μm) with the mobile phase consisting of acetonitrile (A) and 0.1% aqueous formic acid (B) in gradient elution at a flow rate of 0.25 mL · min(-1) and the column temperature was set at 45 °C. Under the optimized chromatographic conditions, good separation for 10 target compounds were obtained including chiral isomer procyanidins B1 and B2 were completely separated within 8.5 min. Satisfactory linearity was achieved with wide linear range and fine determination coefficient (r > 0.996 6), the overall recoveries were ranged from 95.44%-110.40% with the RSD ranging from 2.37%-8.69%. It is the first report about simultaneous analysis of 10 major flavonoids components in Tetrastigma hemsleyanum by using UPLC-MS/MS method, which affords highly sensitive, specific, speedy and efficient method for quality control of Tetrastigma hemsleyanum

Research progress of thioredoxin-related protein 14 / 国际肿瘤学杂志

Thioredoxin-related protein 14 (TRP14),a new member of Trx family,is a novel disulfide reductase with conservative CPDC motif.Its structure and function are comparable to Trx,which is the representative member of Trx family.However,there are many differences.When tumor necrosis factor-α (TNF-α) induced cells to produce the active oxygen,TRP14 can change oxidatin state of dynein light chain(its substrate),act as a sensor of the intracellular redox state to regulate NF-κB signaling pathways induced by TNF-α,MAPK and apoptosis signaling pathways.