1.Chiral Resolution of Optical Isomers of α-Chloro-N-phenyl propanamide by Reversed Phase HighPerformance Liquid Chromatography
Jiehua SHI ; Xiuzhu XU ; Gensheng YANG
Chinese Journal of Analytical Chemistry 2001;29(4):431-433
The chiral resolution of the optical isomers of aryloxypropionic acid herbicide intermediate α-chloro-N-phenyl propanamide was studied by reversed phase high performance liquid chromatography on chiral column. The experimental results showed that the optical isomers of α-chloro-N-phenyl propanamide could be resolved much better on the tribenzoylcellulose (CTB) chiral column with ethanol as mobile phase. The separation factor and separation degree were 1.52 and 0.60 respectively
2.Enzymological Characteristics of Catalytic Antibody-catalyzed enantioselective Hydrolysis of Ibuprofen Ester in Water-in-oil microemulsion
Gensheng YANG ; Yingdan QI ; Zhimin OU ; Shanjing YAO
Progress in Biochemistry and Biophysics 2009;36(2):182-189
The asymmetric hydrolyzation of racemic ibuprofen ester is one of the most important methods for chiral separation of ibuprofen. A catalytic antibody that accelerates the rate of enantioselective hydrolysis of ibuprofen methyl ester was successfully elicited against an immunogen consisting of tetrahedral sulfate hapten attached to bovine serum albumin (BSA). The rate constant enhancement factor Kcat/Kuncat was about 1.6x104. The catalytic activity of the catalytic antibody in a reverse micelle reaction system based on sodium b/s (2-ethylhexyl) sodium sulfosuccinate (AOT) in isooctane was studied. Kinetic analysis of the catalytic antibody-catalyzed reaction was found to be possible in this system. Kinetic studies showed that hydrolysis in the microemulsion system follow Michaelis-Menten kinetics. The catalytic antibody can also accelerate catalysis of S-ibuprofen methyl ester in the microemulsion system. Temperature effects, the pH profile, Km,app and Kcat were determined. The dependence of the catalytic antibody hydrolytic activity on the Wo (molar ratio of water to surfactant) showed a bell-shaped curve, presenting a maximum at about wo = 21.
3. Effect of cinobufagin capsule on coagulation state, therapeutic effect and quality of life in patients with advanced lung cancer
Chinese Journal of Primary Medicine and Pharmacy 2019;26(14):1679-1682
Objective:
To explore the effects of cinobufagin capsule on coagulation status, therapeutic effect and quality of life of patients with advanced lung cancer.
Methods:
A total of 64 patients with advanced lung cancer admitted to the Second People's Hospital of Jinzhong from February 2017 to January 2018 were selected, and they were divided into control group and observation group by random number table method, with 32 cases in each group.The control group was treated with chemotherapy, and the observation group was treated with cinobufagin capsules combined with chemotherapy.Blood coagulation status, quality of life score, pain numerical rating scale (NRS) and functional status score(KPS) were observed before and after treatment in the two groups.The clinical efficacy was compared between the two groups.
Results:
Before treatment, there were no statistically significant differences in plasma fibrinogen(FIB), platelet(PLT), D-dimer, quality of life score, NRS score and KPS score between the two groups(all
4.Cyclic guanosine monophosphate-adenosine monophosphate (cGAMP): a novel vaccine adjuvant
Qinying YAN ; Xieqi WU ; Zhenghan ZHANG ; Fangyuan GUO ; Qingliang YANG ; Gensheng YANG
Chinese Journal of Microbiology and Immunology 2017;37(10):790-794
Aluminum salts are the most popular adjuvants applied in human vaccines currently. However,they can′t achieve satisfying results in the development of novel vaccines because of the cellular immune responses induced by them are weak and their adjuvant activities for some novel vaccines are poor, especially in vaccination against peptide antigens with small molecular weight. cGAMP (cyclic guanosine monophosphate-adenosine monophosphate) has recently been known as a mammalian second messenger, which plays an important role in the innate immune signaling pathway and is capable of boosting the immuno-genicity of vaccines,activating antigen-presenting cells and enhancing specific T cell responses. cGAMP is expected to become a new generation of vaccine adjuvants against infectious diseases and cancer. In this re-view,we summarize the application and current situation of vaccine adjuvants, describe the discovery of cGAMP and its mechanism as a vaccine adjuvant,and focus on the advances in using cGAMP in the fields of vaccination against infectious diseases, intradermal immunization and tumor immunotherapy. Finally, it is also pointed out that cGAMP,as a novel vaccine adjuvant,will have a broad prospect of application in areas such as anti-tumor,anti-virus,anti-inflammatory and vaccines.
5.Preparation of venlafaxine hydrochloride and fluoxetine hydrochloride multilayer tablets by stereolithography 3D printing technology
Lei XU ; Siying PAN ; Hongmei CHEN ; Qingliang YANG ; Gensheng YANG
China Pharmacy 2024;35(13):1600-1604
OBJECTIVE To prepare venlafaxine hydrochloride and fluoxetine hydrochloride multiplayer tablets by stereolithography (SLA) 3D printing technology, and to conduct its quality evaluation and in vitro release investigation. METHODS Using venlafaxine hydrochloride/fluoxetine hydrochloride, photopolymerization monomer PEGDA 400, porogen PEG 300, photoinitiator TPO and light absorber citrine as formulation, SLA 3D printer technology was employed to prepare venlafaxine hydrochloride and fluoxetine hydrochloride multiplayer tablets, with outer diameter of 10 mm, inner diameter of 5 mm, and thickness of 6 mm. Moreover, the tablets’ appearance, three-dimensional dimensions, weight uniformity, drug content, internal structural characteristics and in vitro release characteristics were all investigated. RESULTS The multilayer tablets had good printing formability, smooth and round edges, and uniform size and thickness; the outer diameter, inner diameter and thickness were (10.06±0.26), (4.94±0.06), (5.80±0.12) mm (RSD=2.58%, 1.21%, 2.07%,n=20), and the weight difference all met the requirements. The contents of venlafaxine hydrochloride and fluoxetine hydrochloride were (7.96±0.09) and (11.26±0.46) mg/tablet, respectively. The results of X-ray diffraction and scanning electron microscopy characterization showed that the two drug molecules in the multilayer film existed in an amorphous structure; after the dissolution of the venlafaxine hydrochloride layer, a clear pore structure was formed, while the fluoxetine hydrochloride layer did not show any pore structure. According to the release curve, 24 h accumulative release rates of venlafaxine hydrochloride layer and fluoxetine hydrochloride layer were(91.88±0.94)% and (106.25±1.28)%, which were in line with Rigter-Peppas release model. CONCLUSIONS This study successfully prepared venlafaxine hydrochloride and fluoxetine hydrochloride multilayer tablets using SLA 3D printing technology; the multilayer tablets have the advantages of excellent printing formability, which are in line with Rigter-Peppas release model.
6.Preparation and evaluation of doxorubicin-loaded red blood cell membrane chitosan-targeted nanoparticles
Weiyong HONG ; Xuhui ZHOU ; Chenhao JIN ; Jinming WANG ; Fangyuan GUO ; Gensheng YANG
China Pharmacy 2022;33(13):1594-1599
OBJECTIVE To prepare and evalu ate doxorubicin-loaded red blood cell membrane chitosan-targeted nanoparticles of targeting tumor cell folate acid (FA)receptor(FA-RBC-DOX-CS-NPs). METHODS Doxorubicin-loaded chitosan nanoparticles (DOX-CS-NPs) were prepared by ion cross-linking method. FA and amino polyethylene glycol phospholithin (NH2- PEG2000-DSPE)were covalently linked to modify the red blood cell membrane to construct FA-RBC-DOX-CS-NPS. FA-RBC- DOX-CS-NPs were characterized and investigated on in vitro drug release characteristics ,antitumor activity and endocytosis ability (investigation with human breast cancer MCF- 7 cells). RESULTS Average particle size of FA-RBC-DOX-CS-NPs was (254.200± 2.651)nm,and polydispersity index was 0.199±0.031;Zeta potential was (-10.100±0.213)mV. FA-RBC-DOX-CS-NPs released fast in the tumor microenvironment (pH6.5). Cellular experiments showed that ,the nanoparticles could inhibit the activity of MCF- 7 cell proliferation and improve the efficiency of endocytosis. CONCLUSIONS FA-RBC-DOX-CS-NPs are prepared successfully. The nanoparticles have good tumor cell targeting and endocytosis ability ,and can realize the enrichment of drugs in tumor cells.