Feasibility and safety of bipolar-plasmakinetic transurethral enucleation and resection of the prostate in day surgery mode / 浙江大学学报·医学版

OBJECTIVES@#To evaluate the feasibility and safety of bipolar-plasmakinetic transurethral enucleation and resection of the prostate (B-TUERP) in day surgery.@*METHODS@#From January 2021 to August 2022, 34 patients with benign prostatic hyperplasia (BPH) underwent B-TUERP in day surgery in the First Affiliated Hospital of Anhui Medical University. Patients completed the screening and anesthesia evaluation before admission and received the standard surgery which implements "anatomical enucleation of the prostate" and "absolute bleeding control" on the same day of admission, and by the same doctor. Bladder irrigation was stopped, catheter was removed and the discharge evaluation was performed on the first day after operation. The baseline data, perioperative conditions, time of recovery, treatment outcomes, hospitalization costs, and postoperative complications were analyzed.@*RESULTS@#All operations were successfully conducted. The average age of the patients was (62.2±7.8) years, average prostate volume was (50.2±29.3) mL. The average operation time was (36.5±19.1) min, the average hemoglobin and blood sodium were decreased by (16.2±7.1) g/L and (2.2±2.0) mmol/L, respectively. The average postoperative length of hospital stay, and total length of hospital stay were (17.7±2.2) and (20.8±2.1) h, respectively, and the average hospitalization cost was (13 558±2320) CNY. All patients were discharged on the day after surgery except for one patient who was transferred to a general ward. Three patients received indwelling catheterization after catheter removal. The 3-month follow-up results showed a substantial improvement in the International Prostate Symptom Score, quality of life score and maximum urinary flow rate (all P<0.01). Three patients experienced temporary urinary incontinence, 1 patient experienced urinary tract infection, 4 patients were diagnosed with urethral stricture and 2 patients experienced bladder neck contracture. No complications above Clavien grade Ⅱ occurred.@*CONCLUSIONS@#The preliminary results showed that B-TUERP ambulatory surgery is a safe, feasible, economical and effective treatment for appropriately selected patients with BPH.

450 nm semiconductor blue laser vaporization combined with triamcinolone acetonide injection in the treatment of bladder neck contracture: a case report / 现代泌尿外科杂志

【Objective】 To evaluate the efficacy and safety of 450 nm semiconductor blue laser combined with triamcinolone acetonide injection in the treatment of bladder neck contracture (BNC). 【Methods】 A 61-year-old male patient with BNC and urethral stricture was treated with 450 nm semiconductor blue laser vaporization combined with triamcinolone acetonide injection. The surgery was performed with a small-caliber laser resectoscope of F22. The follow-up results 3 months after surgery were reported. 【Results】 The operation was successful, the operation time was 30 minutes, and the patient was discharged the next day after operation. Follow-up 3 months after operation showed the maximum urinary flow rate (Qmax) was 22.1 mL/s, the International Prostate Symptom Score (IPSS) was 2, the Quality of Life Scale (QoL) was 0, and no recurrence was observed. 【Conclusion】 It is safe and feasible to use 450 nm semiconductor blue laser combined with triamcinolone acetonide injection to treat bladder neck contracture through a small-caliber laser resectoscope of F22, especially for patients with urethral stricture. The short-term efficacy is satisfactory.

Design,synthesis and activity evaluation of novel 2-indolone derivatives as the c-Met kinase inhibitors / 国际药学研究杂志

Objective To design and synthesize novel 2-indolone derivatives as the c-Met kinase inhibitors. Methods With c-Met kinase inhibitor SU11274 as lead compound,a series of 2-indolone derivatives were designed according to the concept of bioiso-sterism. Then the target compounds(10a-10r)were synthesized from 2-indolone through 5-chlorosulfonation with chlorosulfonic acid, sulfonamidation with intermediate 3,condensation with 6a-6h,7a-7h and 4a-4b,respectively. Their inhibitory activity against c-Met and proliferation of MCF-7 cells were evaluated. Results and Conclusion The designed compounds were successfully prepared and their structures were confirmed by 1H NMR and ESI-MS. Some compounds had certain inhibitory activity against c-Met and prolif-eration of MCF-7 cells. An initial structure-activity relationship analysis of these compounds was performed to provide useful informa-tion for further optimization of their structures.

Synthesis and activity evaluation of novel tyrosine kinase inhibitors / 国际药学研究杂志

Objective To design and synthesize compounds with protein tyrosine kinase(PTK)inhibitory activity with L029 as the lead compound. Methods L029 derivatives were designed and synthesized from L029 by reduction and/or substitution with the 3-dimethylamino-1-propyl,methyl acetate,methyl propionate in its active H and other sites. PTK activity was measured by enzyme-linked immunosorbent assay(ELISA). The inhibitory rate was calculated to screen out the compounds with PTK inhibitory activity. Re-sults Five target compounds were synthesized and their structures were confirmed by 1H NMR and MS. Three compounds T2,T3 and T5 were screened out with strong PTK inhibitory activity. Conclusion The synthetic routes of the target compounds are simple with mild reaction condition,and 3 compounds show strong inhibitory activity by ELISA. These results can provide reference for the further design and synthesis of this kind of molecules.

Simultaneous determination of five furostanol saponins in rhizome and fibrous root of Anemarrhena asphodeloides Bge. by HPLC-CAD / 国际药学研究杂志

Objective To develop a method for the determination of five furostanol saponins(timosaponin N,timosaponin L, timosaponin BⅡ,25R-timosaponin BⅡ,and 25S-officinalisnin-Ⅰ)in rhizome and fibrous root of Anemarrhena asphodeloides Bge. by HPLC with the charged aerosol detector(CAD). Methods The analysis was performed on TechMate C18-ST-II(250 mm×4.6 mm,5μm)with acetonitrile:water(22:78,V/V),the flow rate of 1.0 ml/min and column temperature at 30℃. The Corona parameters were as follows:sampling rate 10 Hz,filter 5 s,and the nebulizer temperature 55℃. Results The approach showed good linearity for five saponins. The correlation coefficients(r2)for calibration curves varied from 0.9992 to 0.9998. The limits of detection(LOD)were 0.28,0.92,0.92,0.92 and 0.92 ng for five steroidal saponins,respectively. The limits of quantitation(LOQ)were found to be 0.92, 2.77,2.77,2.77 and 2.76 ng,respectively. RSD calculated from peak area of precision,repeatability and stability in 48 h were all less than 3.0%. The average recoveries of timosaponin N,timosaponin L,timosaponin BⅡ,25R-timosaponinBⅡ,and 25S-officinalis-nin-Ⅰwere 98.17%,101.37%,98.53%,97.63%,and 98.17%,respectively. Conclusion The developed method is accurate,reli-able,which could be applied to the quality control of multiple components in A. asphodeloides Bge.

Synthesis and protein tyrosine kinases inhibitory activity of aroyl derivatives / 国际药学研究杂志

Objective Using Ex-Rad as a lead compound to design and synthesize aroyl derivatives with protein tyrosine ki?nases(PTK)inhibitiory activity. Methods 1-[(4-Fluorophenyl)amioncarbonyl]cyclopropanecarboxylic acid,and 2-oxo-1-phenyl-imidazolidine were used as raw materials to synthesize intermediates 3a-3d,respectively. The target compounds T1-T7 were synthe?sized by chloroformylation reaction with 3a-3d. Enzyme-linked immunosorbent assay(ELISA)was used and inhibitory rate was calcu?lated to screen out the compounds with PTK inhibitory activity. Results Seven new compounds containing aroyl groups were synthe?sized and their structures were confirmed by 1H NMR. The evaluation of the seven compounds demonstrated that PTK inhibitory activi?ty of T2 and T6 were stronger than that of the lead compound. Conclusion The synthetic method is simple,and the materials are cheap and readily available. T2 and T6 show strong PTK inhibitory activity by ELISA.

Fast Structure Confirmation of Daptomycin by Matrix_assisted Laser Desorption Ionization Mass Spectrometry and Electrospray Ionization Mass Spectrometry / 分析化学

Matrix_assisted laser desorption ionization_time of flight tandem mass spectrometry ( MALDI_TOF/TOF MS) and electrospray ionization_quadrupole_time of flight mass spectrometry ( ESI_Q_TOF MS) were used to confirm the structure of cyclic lipopeptide daptomycin fastly. First, the relative molecular weight 1916. 7107 of daptomycin was measured by ESI with error 0. 0007. The sample’s doubly charged peak m/z 809. 848 was selected as precursor ion for ESI_MS/MS analysis, and the exocyclic amino acid sequence C9 H19 CO_Trp_Asn_Asp was successfully matched. Second, the experimental conditions of cleaving daptomycin by lithium hydroxide ( LiOH) were optimized and the ring_opened process was monitored by MALDI_TOF/TOF MS. After obtaining ring_opened product with purity of above 95%, the MS/MS measurements by MALDI and ESI were carried out. The b+and y+of ring_opened product were completely matched, which confirmed the amino acid sequence of daptomycin. Finally, ESI_MS/MS conditions of ring_opened product were further optimized to obtain more low mass fragment ions for analyzing the structure of fatty acid chain and the cleavage pattern of fat chain in mass spectrometry was proposed. The method was fast, convenient, accurate and reliable for identifying cyclic lipopeptide compounds.