1.ANTIINFLAMMATORY, ANALGESIC & ANTICANCER EFFECTS OF FERULOFEN
Chuanbin YU ; Huapu WU ; Min GE
Chinese Pharmacological Bulletin 1986;0(05):-
Antiinf lammatory effects of Ferulofen ( FL ) were shown by im or ip on xylene-induced swellingof mice ear, carrageenin produced edema of hind paw in rats, and decreased volume of pleural exud- ate on carrageenin-induced acute pleurisy of rats, FL also inhibi-tied the proliferating granuloma by croton oil. The above dose r-ange in 50-100mg/kg im or ip which presented a good dose-effect relationship, FL also inhibited the mice writhing caused by H AC & tail-flick response to 1 light irradiation, suggesting its strong analgesic effect. In addition, its anticancer effect in vitro ( carcinoma of Ehlrich ascitis)was better than that in vivo ( Sl80 sarcoma) in mouse. So FL may be considered to be a promising new type of non-steroidal antiinflammatory & anticancer drug ,worthy of further reseaching & exploring in the future.
2.ANTIPYRETIC AND ANESTHETIC ACTIVITY OF FERULOFEN
Chuanbin YU ; Huapu WU ; Mingjin CAI ; Weihong YANG ;
Chinese Pharmacological Bulletin 1986;0(06):-
Ferulof en ( FL, 45mg and 200mg/kg im ) showed marked antipyretic effect on rabbit fever induced by typho-paratyhoid vaccine and on rat fever induced by yeast powder suspension respectively. Their potency and action phase were similar to those of aspirin ( 35mg and 100mg/kg) . Furthermore, it blocked the action potential of sciatic nerve in toad to some extent and had a certain local anesthetic effect on guinea pigs in intradermic wheal test, but much weaker than procaine and lidocaine at the same concentration. It had no obvious influence on corneal reflex in rabbits.It can be concluded from these findings that together with the results of previous paper the findings of this paper further indicated FL may be proved to be a new antiinflammatory, antipyretic and analgesic drug.
4.In vitro targeting effect of lactoferrin modified PEGylated liposomes for hepatoma cells.
Minyan WEI ; Qi ZOU ; Chuanbin WU ; Yuehong XU
Acta Pharmaceutica Sinica 2015;50(10):1272-9
A lactoferrin-containing PEGylated liposome system (Lf-PLS) was developed and tested in vitro as a hepatoma-targeting drug delivery system. PEGylated liposomes (PLS) were successfully prepared using the thin film hydration method with peglipid post insertion. Lf was covalently conjugated onto the carboxyl terminal of DSPE-PEG2000-COOH on liposomes. Coumarin-6 was used to trace Lf-PLS with fluorescence. The cellular uptake of this system was carried out in asialoglycoprotein receptor (ASGPR) positive HepG2 cells via confocal microscopy and flow cytometry. The Lf-PLS liposome was observed as spherical or oval vesicles with the particle size around 130 nm, zeta potential about -30 mV and encapsulation efficiency more than 80%. The confocal microscopy images and flow cytometry data demonstrated that Lf-PLS resulted in significantly higher cell association by ASGPR positive HepG2 cells compared to PLS. The association between Lf-PLS and cells were dependent on the concentration, time and temperature, which was inhibited by pre-incubation with excessive free Lf. The results suggest that Lf-PLS has a good targeting effect on HepG2 cells in vitro. The targeting mechanism may be related to the specific binding of Lf and ASGPR on HepG2 cells, which guides Lf-PLS to the cell surface to induce an active endocytosis process. All these results demonstrated that Lf-PLS might be a potential drug delivery system in targeting hepatocellular carcinoma, which deserves more research on its targeting ability, antitumor efficiency, and metabolism in vivo for treatment of hepatomacellular carcinoma.
5.Improving the dissolution rate of poorly water-soluble resveratrol by the ordered mesoporous silica.
Guilan QUAN ; Bao CHEN ; Zhouhua WANG ; Han WU ; Xintian HUANG ; Linna WU ; Chuanbin WU
Acta Pharmaceutica Sinica 2012;47(2):239-43
The aim of this study is to synthesize the ordered mesoporous silica (OMS) as drug carrier to improve release property of insoluble drug and investigate the dissolution profile of insoluble drug from the porous carrier. The OMS was obtained by using cetyltrimethyl ammonium bromide as the template and resveratrol was selected as the model drug. The resveratrol-loaded OMS (Res-OMS) were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), N2 adsorption-desorption, X-ray diffraction (XRD) and FT-IR spectroscopy. In vitro drug release behavior was also investigated. It was found that the synthesized OMS showed a large surface area, a narrow pore size distribution and an important mesoporosity associated to hexagonally organized channels. Compared with physical mixture and crystalline powder, resveratrol was in amorphous or molecular form after loading into OMS. The release rate ofresveratrol from drug-loaded OMS was significantly increased suggesting the great potential application of OMS for the formulation of poorly soluble drugs.
6.Preparation and release behaviour of mesoporous silica/ethylcellulose sustained-release mini-matrix.
Qiaoli WU ; Guilan QUAN ; Yu HONG ; Linna WU ; Youmei ZENG ; Ge LI ; Xin PAN ; Chuanbin WU
Acta Pharmaceutica Sinica 2015;50(4):492-9
Hot-melt extrusion was applied to prepare mesoporous silica/ethylcellulose mini-matrix for sustained release, and fenofibrate was used as a model drug, ethylcellulose and xanthan gum were chosen as sustained-release agent and releasing moderator, respectively. This novel matrix obtained the controlled release ability by combining mesoporous silica drug delivery system and hot-melt extrusion technology. And mesoporous silica particle (SBA-15) was chosen as drug carrier to increase the dissolution rate of fenofibrate in this martix. Scanning electron microscope, transmission electron microscope, small angle X-ray powder diffraction and N2 adsorption-desorption were introduced to determine the particle morphology, particle size and pore structure of the synthesized SBA-15. The results showed that SBA-15 had a very high Brunauer-Emmett-Teller specific surface area, a narrow pore size distribution, large pore volume and a ordered two-dimensional hexagonal structure of p6mm symmetry. Differential scanning calorimetry and X-ray powder diffraction results demonstrated that fenofibrate dispersed in an amorphous state inside the pores of the mesoporous silica which contributed to the improvement in the dissolution rate. The drug release of mini-matrices was influenced by ethylcellulose viscosity grades and xanthan gum concentration, which increased with the increasing of xanthan gum concentration and decreasing of ethylcellulose viscosity. Mini-matrix containing 22% xanthan gum exhibited a good sustained release performance, and the drug release behavior followed the first-order kinetics.
7.Preparation and in vitro embolic efficiency evaluation of hydroxycamptothecine-loaded liquid embolic agent.
Lingzhen QIN ; Xuan ZHANG ; Linna WU ; Jin ZHANG ; Xin PAN ; Ge LI ; Chuanbin WU
Acta Pharmaceutica Sinica 2014;49(7):1069-75
The purpose of this study is to investigate the preparation of hydroxycamptothecine (HCPT)-loaded cubic crystal liquid embolic precursor solution, and evaluate its in vitro embolic efficiency. Phytantriol was used as cubic crystal liquid embolic material, and the optimal formulation was selected according to ternary phase diagram. Polarized light microscopy, differential scanning calorimetry, and small angle X-ray scattering (SAXS) were used to characterize the cubic crystal structure. High performance liquid chromatography and X-ray diffraction analysis were used to investigate the lactone ring of HCPT. In vitro dissolution was preliminary evaluated, and the simulation embolic model was constructed to evaluate the embolic efficiency of precursor solution. Meanwhile, the gelation time and adhesion force were investigated. The results showed that HCPT-loaded precursor solution for embolization had been successfully prepared with low viscosity which was injectable. The precursor solution could transform into Pn3m structure liquid crystal phase gel rapidly when contracting with excess water. The formed HPCT gel remained its lactone form as the same in precursor solution, and expressed the good ability to block the saline flow, and HCPT could keep sustained releasing drug over 30 days. The prepared drug-loaded embolic precursor solution showed a promising potential for vascular embolization and application in clinical treatment of tumor.
8.Localization Effect of 131 I-Human Anti-HBs Fab in Nude Mice Models of Human Hepatoma
Guichen WU ; Rongcheng LUO ; Huanxing HAN ; Changxuan YOU ; Xuemei DING ; Aimin LI ; Chuanbin WANG ; Mingjang ZHANG
Chinese Journal of Cancer Biotherapy 2000;7(4):288-290
Objective: To evaluate the targeting activity in the animal model with human hepatoma, the 131I-human antiHBsAg Fab radioimmunoimaging was explored. Methods: Radioimmunoimagings were taken on different intervals after injection of 131 I-human anti-HBsAg Fab to the nude mice and tissue distribution was measured. The human anti-HBsAg Fab was compared with the murine monoclonal antibodies. Results: The experimental group developed tumor positive images after 3 days of radio-labeled monoclonal antibodies injection, and the peak accumulation of radio-activity on the 5th day.Statistics indicated the tumor/liver ratio of the human anti-HBsAg Fab, murine monoclonal antibodies and the control groups were 5.4,4.0 and 0.9 respectively on the 7th day. Conclusions: Our results suggest that the 131 I-human anti-HB-sAg Fab has a considerable targeting activity, and provide an evidence that it can be used as a novel humanized carrer for targeting therapy of hepatoma.
9.Verification of the couch automatic movement accuracy for Hi-ART tomotherapy.
Yongjie HUANG ; Yunlai WANG ; Chuanbin XIE ; Weizhang WU
Chinese Journal of Medical Instrumentation 2013;37(2):143-145
The QUASAR Penta-guide Phantom with fiducial markers was scanned, and the CT images were transferred to Pinnacle workstation. Skin and target volumes were contoured and transferred to TomoPlan treatment planning system. The phantom was scanned with Megavoltage CT (MVCT). MVCT images were matched to the planning CT. Automatic adjustment of treatment couch was completed. It was found that the green laser coincided with the etched center crosshairs in lateral and longitudinal directions with an error less than 2 mm. However 2 mm vertical tabletop lag was found, but could be eventually corrected. Verifications for specific patients with head and pelvic tumors were also completed, the residual setup error were analyzed. The automatic movement of tabletop after image match is satisfactory.
Humans
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Radiotherapy Planning, Computer-Assisted
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instrumentation
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methods
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Radiotherapy, Intensity-Modulated
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instrumentation
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methods
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Tomography, Spiral Computed
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instrumentation
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methods
10.Mechanisms and therapeutic targets of ferroptosis:Implications for nanomedicine design
Zhang MEIHONG ; Guo MENGQIN ; Gao YUE ; Wu CHUANBIN ; Pan XIN ; Huang ZHENGWEI
Journal of Pharmaceutical Analysis 2024;14(7):955-971
Ferroptosis is a nonapoptotic form of cell death and differs considerably from the well-known forms of cell death in terms of cell morphology,genetics,and biochemistry.The three primary pathways for cell ferroptosis are system Xc-/glutathione peroxidase 4(GPX4),lipid metabolism,and ferric metabolism.Since the discovery of ferroptosis,mounting evidence has revealed its critical regulatory role in several diseases,especially as a novel potential target for cancer therapy,thereby attracting increasing attention in the fields of tumor biology and anti-tumor therapy.Accordingly,broad prospects exist for identifying ferroptosis as a potential therapeutic target.In this review,we aimed to systematically summarize the activation and defense mechanisms of ferroptosis,highlight the therapeutic targets,and discuss the design of nanomedicines for ferroptosis regulation.In addition,we opted to present the advantages and disadvantages of current ferroptosis research and provide an optimistic vision of future directions in related fields.Overall,we aim to provide new ideas for further ferroptosis research and inspire new strategies for disease diagnosis and treatment.