To develop an ophthalmic preparation of Shedan, an in situ forming gel was prepared with the formulation containing 18% of poloxamer 407 and 5% of poloxamer 188 by response surface designs plus central composite designs. The rheology results showed that LVE range gamma should limited within 0.5%, Shedan high-frequency region, and the thixotropy recovery time is less than 5 seconds. The phase transition temperature was 33.25 °C according to curve of storage modulus and loss modulus determined by temperature scanning. Surface tension and osmometer of it determined by surface tension meter and dew point osmometer were 36.43 mN · m(-1), and 320.6 mOsm · kg(-1), respectively. Fluorescein sodium was selected as the marker to monitor the corneal residence time, and the results showed that Shedan gel could prolong drug residence for 180 min. In line with zero-order kinetics, releases of muscone and salvianolic acid B in vitro depends on gels erosion. The results of rabbit ocular irritation experiments suggested that Shedan in situ forming gel was biocompatible and nonirritant. In conclusion, a novel Shedan in situ forming gel was developed and characterized for potential drug treatment of retinal vein occlusion.
Animals ; Benzofurans ; chemistry ; Cycloparaffins ; chemistry ; Female ; Gels ; chemistry ; Male ; Ophthalmic Solutions ; Poloxamer ; chemistry ; Rabbits ; Retinal Vein Occlusion ; drug therapy ; Viscosity

Objective To study effective treatment for deep burn on the face caused by coal-dust burning and blasting to prevent severe disfigurement.Methods Early conservative eschar-scraping, delayed skin graft,early strain-diminution for the eyelids in both sides,and wound expansion with skin graft were used to treat 12 patients with deep burn on their faces caused by coal-dust burning and blasting. Results Facial wound of all the 12 patients healed within three weeks after burn.No significant cicatricial hyperplasia and deformity were found on their faces during three-month follow-up,with natural facial expression and abundant emotion.Conclusions Early eschar-scraping and delayed skin graft for deep facial burn can promote fast repair of burn-wound,diminish cicatricial hyperplasia and prevent deformity on the face.

To simplify the macrocyclic fragment and to modify the zinc binding group of the natural product apicidin, two series of S-hexyl (heptyl) ethanethioate derivatives were designed and synthesized. Twenty-six compounds were synthesized and confirmed with 1H NMR, IR, MS and HR-MS spectrum, which were not reported. Take vorinostat as control, their antiporliferative activities against cancer cell lines, MCF-7 and HL-60, were tested with MTT assay or trypan blue staining method. Generally in both series it was found that, the chiral carbon atom at 7 position is not necessary, compounds II-1, II-3, II-6 and II-13 showed good activity on HL-60 cells in vitro, with the IC50 values less than 10 micromol x L(-1). II-7 and II-8 showed stronger activity against MCF-7 than Vorinostat, with the IC50 of 3.19 and 6.29 micromol x L(-1), respectively.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Proliferation ; drug effects ; Drug Screening Assays, Antitumor ; HL-60 Cells ; Histone Deacetylase Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Humans ; Inhibitory Concentration 50 ; MCF-7 Cells ; Peptides, Cyclic ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

AIM:To investigate the effect and mechanism of osthole on increasing the cytotoxicity of doxorubi -cin(DOX)to prostate cancer cells.METHODS:MTT assay was performed to evaluate the viability of LNCaP cells trea-ted with osthole and DOX.The protein expression of silent information regulator 1(SIRT1),p53,acetylated p53 and Pu-ma,as well as release of cytochrome C and activation of caspase-9 and caspase-3 in the LNCaP cells treated with osthole and DOX were determined by Western blot.The apoptosis of the LNCaP cells treated with osthole and DOX was analyzed by flow cytometry.RESULTS:Osthole significantly increased the cytotoxicity of DOX against p 53-wildtype prostate cancer cell line LNCaP.Osthole significantly inhibited the expression of SIRT 1 in the LNCaP cells.Transfection with SIRT1 plas-mid decreased the cytotoxicity of osthole and DOX co-treatment against LNCaP cells.Combination with osthole and DOX significantly induced the over-expression and acetylation of p53.Transfection with p53 siRNA significantly decreased the synergistic effect of osthole on cytotoxicity of DOX-treated LNCaP cells.Combination with osthole and DOX significantly in-duced the release of cytochrome C into the cytoplasm from mitochondria,followed by activation of caspase-9 and its down-stream molecule caspase-3,thus leading to cell apoptosis in the LNCaP cells.CONCLUSION:Osthole promotes the p53-dependent apoptosis in DOX-treated prostate cancer LNCaP cells by down-regulating the expression of SIRT1.

Objective To evaluate the value of 64-slice spiral CT angiography based on pre- contrasted raw data in diagnosing pulmonary arteriovenous fistula.Methods 64-slice spiral CT plain scan and enhanced scan was performed in 16 patients with pulmonary arteriovenous fistula,pulmonary angiography based on pre-contrast and post-contrast raw data was performed respectively,including maximum intensity projection(MIP),shaded-surface display(SSD),and volume rendering(VR).According to the results of angiocardiography and surgical findings,comparson of the three methods was made in the display of PAVF in pre-contrast and post-contrast phase images.Results 8 of the 16 PAVF cases were single lesion,8 cases were multi-lesions.30 PAVF lesions were found in all the patients.MIP,SSD and VR based on pre-contrast raw data displayed PAVF lesions in 20,14,and 22,respectively.The combination of the 3 methods based on pre-contrast raw data could show 26 PAVF lesions.MIP,SSD,and VR based on post-contrast raw data displayed PAVF lesions in 24,18,and 30,respectively.The combination of the 3 methods based on post- contrast raw data could show 30 PAVF lesions.Conclusion 64-slice spiral CT angiography based on pre- contrasted raw data can clearly show the position,number,and shape of PAVF lesions,which is of great value in diagnosing PAVF.

Humanin(HN,its analogue [Gly14]-Humanin,HNG)was originally identified as an endogenous peptide that protects neuronal cells from apoptosis induced by various types of Alzheimer's disease-related insults.But the relative low content of this peptide in its natural sources limits its further characterization.An expression vector pET32a/HNG was corstructed and transformed it into E.coli BL21 trxB(DE3).HNG was expressed as a fusion protein in the soluble fraction and was purified by nickel affinity chromatography.Subsequently,the purified fusion protein was cleaved by enterokinase and was further purified by reverse-phase HPLC.A 23 mg recombinant HNG(rHNG)from 1 L bacterial culture was purified.The molecular weight of rHNG determined by ESI-MS was 2876.5 Da which was the expected size for correctly processed peptide.The N-terminal amino acid sequence of rHNG determined by Edman degradation method is identical to the theoretical sequence.Neuroprotective bioassay studies of rHNG exhibited its potential neuroprotective effect comparable to that of the natural HNG peptide.

Objective To establish a high performance liquid chromatography(HPLC) method for the simultaneous determination of eight components in Gynostemma pentaphyllum(Thunb.) Makino (ginsenosides Rb1, Rb3, Rd, Re, F2, and gypenosides A, XLIX and XVII). Methods HPLC was performed on Agilent Eclipse XDB-C18(4.6 mm × 250 mm, 5 μm) chromatographic column with 0.3％ formic acid solution (A)- acetonitrile (B) as the mobile phase by gradient elution, flow rate was 1.5 mL·min-1, detection wavelength was 203 nm, and column temperature was set at 50 ℃. Results There was a good linear relationship between peak area and concentration of eight components (r ≥ 0.999) , the recovery was in the range of 97％ to 100％. Conclusion The established method is simple, rapid, accurate, reliable, and reproducible, and can be used for the quality control of Gynostemma pentaphyllum(Thunb.) Makino.

OBJECTIVETo study the thin layer chromatographic (TLC) fingerprint of flavonoid constituents from Polygonatum odoratum, to set up the identification protocol of the herbal and provide scientific information for its quality control.

METHODThe ethanol extracts were separated on silica gel G precoated plate with a mixture of toluene-ethylacetate-formic acid (5:4:1) as the mobile phase. The spots were visualized with ammonia vapor, then were examined under ultraviolet light (365 nm). The plate was scanned at wavelengths of lambdaR = 500 nm, lambdaS = 280 nm.

RESULTA fingerprint of flavonoids of P. odoratum, with 10 specific fluorescent spots while examined under ultraviolet light, was set up.

CONCLUSIONThe method can be used for quality control of P. odoratum.

Chromatography, Thin Layer ; methods ; Flavonoids ; analysis ; chemistry ; Plants, Medicinal ; chemistry ; Polygonatum ; chemistry ; Quality Control ; Rhizome ; chemistry

OBJECTIVETo screen out the HAb18G/CD147 binding peptides and find out an antagonist against hepatoma invasion.

METHODSHAb18G/CD147 was purified by affinity chromatographic method and the antigen binding peptides acquired by bio-panning a phage-displayed 12-peptide library. After obtaining the sequence of the selected phage-displayed peptides, all the 9 peptides were synthesized by solid-phase method and identified by mass spectrograph. The peptides' anti-metastatic function was tested by Boyden Chamber assay.

RESULTSThe purified HAb18G/CD147, identified by Western blot (molecular weight about 65 kd) could be used to bio-pan the phage-displayed peptide library. After 3 rounds of bio-panning, 9 positive phage clones were selected and sequenced. The synthesized peptides had uneven inhibitory activities and three of them were able to markedly inhibit the hepatoma cell invasion (P < 0.01). The most effective peptide decreased by 90.1% of hepatoma cells migrating through the Boyden Chamber membrane as compared with the control.

CONCLUSIONBio-panning the phage-displayed peptide library can be used successfully to screen out the antigen binding peptides. Hepatoma metastatic potential can be inhibited by peptide antagonist which could be a good foundation of developing peptide therapeutic agent against hepatoma metastasis.

Animals ; Antibodies, Monoclonal ; therapeutic use ; Basigin ; metabolism ; Carcinoma, Hepatocellular ; drug therapy ; pathology ; Humans ; Liver Neoplasms ; drug therapy ; pathology ; Mice ; Neoplasm Invasiveness ; Peptide Library ; Peptides ; therapeutic use

OBJECTIVETo find the best condition of the preparation technology of Flos Magnoliae essential oil-beta-cyclodextrin inclusion complex.

METHODL9(3(4)) table was used to examine the effects of 4 factors, and the inclusion rate of each test was determined of orthogonal test.

RESULTThe best condition was:oil:beta-cyclodextrin:water = 1:8:60 (mL:g:mL), stirring for 1 hour at 80 degrees C.

CONCLUSIONThe complex prepared on the condition aforementioned is stable and stirring has a highest inclusion rate.

Cyclodextrins ; Drug Carriers ; Drug Stability ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; Flowers ; chemistry ; Magnolia ; chemistry ; Oils, Volatile ; administration & dosage ; isolation & purification ; Plants, Medicinal ; chemistry ; Technology, Pharmaceutical ; methods ; beta-Cyclodextrins