This thesis aimed at the Bacillus natto TK-1 screened out from Natto.The lipopeptide was purified using Thin-Layer Chromatography(TLC),and investigated its anti-tumor activity.After acid precipitation and methanol extraction,the lipopeptide was separated on TLC.Then the authors get the monomer surfactin which molecular weight is 1036Da through the High performance liquid chromatography(HPLC),electro spray ionization-mass spectrometry(ESI-MS) and infrared(IR).MTT method was implied to testify the anti-tumor activity of the purified sample from TLC.The results indicated a concentration and time-dependent relationships.After 48h,their IC50 were 40 mg/L.The detection with inverted microscope fluorescence microscope displays that the surfactin will cause a series of Morphological changes to the cells.In TUNEL experiment,the authors noticed that surfactin has the ability to induce apoptosis,besides this inhibition shows an obvious time-dependent relationship.

The study was to develop cis-dichlorodiammineplatinum(DDP)-loaded formulations using a novel type of self-assembled compound composed of block copolymers synthesized by poly(?-glutamic acid)(?-PGA).For the potential of targeting liver cancer cells,D-galactose was conjugated on the prepared ?-PGA.In vitro,DDP can be released from the resulting conjugate in PBS:there was a burst release during the first 8 h,then followed by sustained release.DDP could be easily incorporated into poly(?-glutamic acid)-D-galactose esterifiable derivative through a covalent bond.The yield of DDP incorporation into the esterifiable derivative was 9.4%～10.2%.In vitro experiments conclusively established that the poly(?-glutamic acid)-D-galactose esterifiable derivative-Cisplatin Complex Compound(?-D+-DDP)was much less toxic to normal cell lines than DDP only.The surviving rate of cells treated with ?-D+-DDP compound is higher than those treated with free DDP.Also it has obvious antitumor efficiency on human liver tumor BEL-7402 cells.HE staining indicated that the ?-D+-DDP compound make the BEL-7402 apoptosis.These results indicated that the conjugation of DDP to the esterifiable derivative reduced its cytotoxicity activity,but retains its antitumor activity in vitro.In conclusion,the ?-D+-DDP compound could be used as a potential clinic antitumor drug.The ?-PGA obtained by fermentation can be used as a valuable drug carrier system.

DDP could be easily incorporated into poly (?-glutamic acid)-D-galactose esterifiable derivative through a covalent bond. The yield of DDP incorporation into the ?-PGA was 9.4%～10.2%. The DDP was released in the initial 8h in a burst manner,and thereafter in a sustained manner. The results that the conjugation of DDP to poly (?-glutamic acid)-D-galactose esterifiable derivative not only reduced the toxicity of the DDP but also enhanced antitumor activity and the targeting ability. The vivo experiments conclusively established that the ?-D+-DDP compound was much less toxic to animals than DDP alone. A direct evaluation showed that mice treated with ?-D+-DDP compound at a dose of 7.5 mg/kg displayed significant tumor regression. Furthermore,the implanted solid tumors disappeared completely from 35% of the H22 tumor-bearing mice after ?-D+-DDP compound administration. The aforementioned results of biodistributions of the prepared ?-D+-DDP compound in various organs in normal mice demonstrated that the ?-D+-DDP compound had a specific interaction with liver's parenchymal cells and H22 hepatocellular carcinoma tumor cells via ligand receptor recognition. In conclusion,the results indicated that the ?-D+-DDP compound prepared can effectively target the site of hepatoma tumor via the recognition and significantly reduce its size. The ?-D+-DDP compound was less toxic than the free DDP,and could effectively reduce xenografted H22 hepatocellular carcinoma cells in KM mice and prolong the survival of KM mice grafted with H22 hepatocellular carcinoma tumor cells. Therefore,the prepared ?-D+-DDP compound may be used as a potential drug delivery system for the targeted delivery to liver cancers or other liver diseases.

OBJECTIVETo observe the effect of Tangke Decoction (TD) on the expression of TGF-beta1/Smad4 of rats with early diabetes and to explore the effect and mechanism of TD against the renal injury induced by diabetes.

METHODSSD rats were randomly divided into the normal control group (n = 12), the model group (n = 10), the Chinese herbs prevented group (n =10), the Chinese herbs treated group (n = 10), and the Western medicine control group (n = 10). TD (18 mg/kg) was given by gastrogavage to rats in the Chinese herbs prevented group immediately after successful modeling for 12 weeks, once daily. At the 4th week of successful modeling, rats in the rest 4 groups were administered by gastrogavage. Equal volume of normal saline was given to rats in the model group and the normal control group. Benazepril suspension (1 mg/kg) was administered by gastrogavage to rats in the Western medicine control group for 8 weeks, once daily. TD (18 mg/kg) was given by gastrogavage to rats in the Chinese herbs treated group for 8 weeks, once daily. The body weight, kidney weight, index of kidney weight, fasting blood sugar, 24 h urinary albumin excretion rate were examined after experiment. The pathological changes of the renal tissue were observed by HE staining, Masson staining, and electron microscope. The expression of renal transforming growth factor-beta1, (TGF-beta1) and Smad4 were detected using immunohistochemical assay.

RESULTSCompared with the normal control group, the body weight of rats decreased significantly; the kidney weight, index of kidney weight, blood sugar, 24 h urinary protein excretion, the urinary albumin excretion rate,TGF-beta1 and Smad4 expression increased significantly in the model group (all P < 0.01). Compared with the model group, the aforesaid indices were improved in each treatment group with statistical difference (P < 0.05, P < 0.01). Compared with the Western medicine control group, the kidney weight, index of kidney weight, blood sugar, 24 h urinary protein excretion, and the urinary albumin excretion rate were obviously improved in the Chinese herbs prevented group (P < 0.01). The renal pathological changes were most obvious in the model group significantly, but they were improved in all treatment groups.

CONCLUSIONTD could obviously improve the symptoms of diabetes and down-regulate the expression of renal TGF-beta1 and Smad4 of early diabetic nephropathy rats, which suggested that TD had certain preventive effect on early diabetic nephropathy.

Animals ; Diabetes Mellitus, Experimental ; drug therapy ; metabolism ; Drugs, Chinese Herbal ; therapeutic use ; Kidney ; metabolism ; Male ; Rats ; Rats, Wistar ; Smad4 Protein ; metabolism ; Transforming Growth Factor beta1 ; metabolism

The most nutrients required in the human diet come from plants. The nutritional quality of plant products affects the human healthy. The advance of molecular cloning and transgenic technology has provided a new way to enhance the nutritional value of plant material. Transgenic modification of plant nutritional value has progressed greatly in the following aspects: improving the quality, composition and levels of protein, starch and fatty acid in different crops; increasing the levels of antioxidants (e.g. carotenoids and flavonoids); breeding the new type of plants with medical value for human. To date, many transgenic plants with nutritional enhancement have been developed. These transgenic plant products could be directly used as human diet or as valued materials in developing the "functional food" with especial nutritional quality and healthy effects after they are approved by a series of evaluations on their safety and nutritional efficiency for human being. We designed new zinc finger transcription factors (ZFP-TFs) that can specifically down-regulate the expression of the endogenous soybean FAD2-1 gene which catalyzes oleic acid to linoleic acid. Seed-specific expression of these ZFP-TFs in transgenic soybean somatic embryos repressed FAD2-1 transcription and increased significantly the levels of oleic acid, indicating that the engineered ZFP-TFs are capable of regulating fatty acid metabolism and modulating the expression of endogenous genes in plants.
Antioxidants ; metabolism ; Fatty Acids ; analysis ; biosynthesis ; Humans ; Isoflavones ; Nutritive Value ; Plants ; metabolism ; Plants, Genetically Modified ; genetics ; Transcription Factors ; physiology ; Zinc Fingers

Adult ; Hemostasis, Surgical ; methods ; Hepatectomy ; methods ; Humans ; Laparoscopy ; methods ; Liver ; blood supply ; Middle Aged ; Treatment Outcome

Female ; Hepatectomy ; methods ; Humans ; Laparoscopy ; methods ; Liver Neoplasms ; surgery ; Middle Aged

Objective To determine the efficacy and tolerability of docetaxel plus capecitabine as first-line treatment for breast cancer with liver metastases(BCLM).Methods Forty-two patients with BCLM received oral capecitabine 1900 mg/m~2/d(950 mg/m~2 twice daily)on days 1 through 14 and intravenous infu- sion of Docetaxel at 75 mg/m~2 on day 1 of each 21-day treatment cycle.Patients were evaluated for the re- sponse after two cycles.Results Among these 42 patients,the overall response rate was 54.76% with 4 CR, 19 PR, 9 SD and 6 PD.The clinical benefit rate was 64.28% and the median overall survival time was 17.5 months.The most common treatment-related adverse events were leukopenia(76.1%),neutropenia(71.4%), hand-foot syndrome(45.2%),nausea and vomiting(52.3%),which were mainly gradeⅠ～Ⅱ.Conclusion The combination of docetaxel plus capocitabine is a highly active and generally well-tolerated regimen for first-line treatment of BCLM.

Objective To investigate the Wallerian degeneration of neural fiber tract in medulla and bilateral middle cerebellar peduncle following pontine infarction and to explore its impacts on neurological recovery.Methods Fourteen patients with a recent unilateral pontine infarct underwent the diffusion tensor imaging(DTI)and evaluations with the NIH stroke scale(NIHSS),the Fugl-Meyer motor scale(FM), ataxia rating scale(ARS)and the Barthel index(BI)at the first week(W1),the fourth(W4)and twelfth week(W12)respectively.Mean diffusivity(MD)and fractional anisotropy(FA)were measured at pons, medulla and middle cerebellar peduncle.Fourteenth age and gender matched volunteers underwent a DTI were studied as controls.Results Compared with the matched regions in controls,the FA values of infarct side medulla and bilateral middle cerebellar peduncle in patients significantly decreased at W1,W4 and W12(on the infarct side of medulla:W1:0.43?0.01;W4:0.37?0.02;W12:0.30?0.02;on the infarct side of middle cerebellar peduncle:W1:0.50?0.01;W4:0.43?0.02;W12:0.35?0.04;on the opposite side of middle cerebellar peduncle infarction:W1:0.54?0.02;W4:0.52?0.03;W12:0.47?0.04,t values are 1.92 to 28.56,P0.05 respectively).The absolute value of percent reduction of FA in infarct side medulla and bilateral middle cerebellar peduncle was correlated negatively to the absolute value of percent change of NIHSS and BI score(P

OBJECTIVETo study the interspecies allelopathy of Glycyrrhiza uralensis and Caragana microphylla and reveal the relationship between different interactions and provided the theory reference for their application of compounding planting pattern in practice.

METHODWater extracts of G. uralensis and C. microphylla root, stem and leaf were used to dispose mutual seeds, young seedlings and transplants.

RESULTThe germination of G. uralensis seed wasn't restrained significantly by the water extract of C. microphylla root, stem and leaf (1-50 g x L(-1)). However, the inhibitory effect of a high concentration water extract of C. microphylla stem and leaf (50 g x L(-1) was stronger. There wasnt significant difference in the effect of the water extract of C. microphylla cast, root and stem on the growth and quality of G. uralensis transplant. Moreover, the water extract of G. uralensis root, stem and leaf can improve the germination of C. microphylla seeds and the growth of seedlings, while its effective extent didn't reach an obvious different level.

CONCLUSIONThere exists no significant difference between the interspecies allelopathy of G. uralensis and C. microphylla.

Caragana ; chemistry ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Germination ; drug effects ; Glycyrrhiza uralensis ; chemistry ; Seedlings ; drug effects ; growth & development ; Seeds ; drug effects ; physiology