Objective To evaluate the feasibility of dopamine D2 receptor imaging agent (s)-(-)-N-(1-allylpyrrolidine-2-N-methyl)-5-(3-18F)-2,3-dimethoxy Benzamide (18F-Fallypride) for targeting islet cell imaging.Methods (1) Cytology experiment:Islet cells of 15×103 cells/well were incubated with 3.70 kBq/well 18F-Fallypride for 1 h and the uptake rate of cells was calculated (cell counts/(supernatant counts + cell counts)× 100％).Under the same experiment conditions,6 inhibiting groups were administrated with different concentration of dopamine inhibitors droperidol (1.0× 10-6,4.0× 10-6,2.0× 10-5,1.0× 10-4,5.0× 10-4 and 1.0× 10-3 mol/L,respectively).After 30 min,3.70 kBq of 18F-Fallypride was added to each inhibiting group,and the inhibiting rate was calculated.(2) Autoradiography:18 normal ICR mice were divided into 6 groups.For group A,ICR mice were injected with 18F-Fallypride (55 ± 5) MBq/mice through tail vein.For the other 5 inhibiting groups (group B-F),ICR mice were injected with different doses of droperidol (0.2,0.4,0.6,0.8 and 1.0 mg/kg,respectively),and after 30 min 18F-Fallypride were injected through tail vein.Ten minutes later,pancreas of ICR mice was taken for preparation of tissue section autoradiography.The data were analyzed by one-way analysis of variance and the least significant difference t test.Results (1) The 18F-Fallypride uptake rate of control group was (18.40± 1.21) ％.The uptake rates of inhibiting groups were (16.11±1.37)％,(15.76±0.99)％,(13.90±1.02)％,(8.86±0.73)％,(7.26±0.62)％ and (6.92±0.58)％,respectively,which decreased with the decreasing concentration of droperidol (F=50.01,P＜0.01).When the concentration of droperidol was 1.0× 10-4 mol/L,the uptake rate reached the lowest with inhibiting rate of 51.85％.(2) The autoradiography showed that the pancreas gray scale value of group A was 1.21×106 digital light units (DLU)/mm2.The pancreas gray scale value of groups B to F decreased with increasing concentration of inhibitor:0.93× 106,0.77× 106,0.59× 106,0.32× 106 and 0.25×106 DLU/mm2,respectively.Conclusions 18F-Fallypride may specifically and efficiently bind to dopamine receptors of islet cells.It may be a potential tracer for islet cells imaging.

Objective To evaluate the effectiveness and safety of gefitinib retreatment beyond progression(GRBP)in non-small cell lung cancer(NSCLC)patients with rare EGFR mutations.Methods We retrospectively analyzed six rare-EGFR-mutation NSCLC patients from Jan 2011 to Dec 2015.Those patients had previous disease control and then disease progression according to Response Evaluation Criteria in Solid Tumors version 1.1(RECIST v1.1)after taking oral gefitinib 250 mg once a day.After that,continuing gefitinib was decided by clinicians′ experience at the same treatment option.The primary endpoints were response rate(RR),overall survival(OS),the first and second progression-free survival(PFS-1 and PFS-2).Safety was assessed according to the NCI-CTCAE version 4.0.Results After initial treatment of gefitinib,4 patients achieved partial response(PR)and 2 patients showed stable disease(SD),with RR being 66.7％.The median PFS-1 and PFS-2 were 10 months(95％CI 6.6-13.4)and 9 months(95％CI 6.9-11.1),respectively.The median OS time was 28 months(95％CI 10.4-45.6).The most common treatment-related adverse events were fatigue,diarrhea,rash,itching and elevated transaminases.Conclusion In our study,gefitinib retreatment beyond disease progression is effective with a manageable tolerability profile.

Objective To study the correlation between the cytochrome P450 3A5 gene polymorphism and essential hypertension (EH) in Chinese population .Methods The real-time PCR genotyping at CYP3A5*3(6986A>G) position was established using Taqman minor groove binding (MGB) probes .Total 170 EH patients and 193 matched controls of Chinese Han population were genotyped at CYP3A5*3(6986A>G) position using this method .Results The GG ,GA ,AA genotyped frequencies were 51 .2% , 42 .4% and 6 .5% for the EH patients and 39 .9% ,50 .8% and 9 .3% for the control group respectively .The risk of EH for person carrying GG genotype was 1 .579 fold of the persons carrying at least one A allele(95% CI:1 .041-2 .395) .Conclusion CYP3A5*3(6986A>G) polymorphism may be associated with EH in Chinese population .The risk of EH is decreased in the persons carrying allele A ,slightly lower levels of systolic blood pressure exists .

Polygala hongkongensis Polycalaceae is mostly distributed in southern China, such as Guangdong, Jiangxi, Fujian and Sichuan provinces. And its herbs is used as a remedy of heat-clearing and detoxicating, removing food retention, promoting blood flow and expelling phlegm to arrest coughing in the folk medicine. Previous phytochemical investigations on Polygala plants have reported that the main chemical constituents are sapaonins, xanthones and oligosaccharide esters. To the best of our knowledge, there is no chemical report on the Polygala hongkongensis Hemsl. yet. In order to search and make use of natural resources from Polygala and to find the bioactive compounds and new compounds, we carried out studies on chemical constituents of this plant. The herbs of P. hongkongensis were extracted with 70% MeOH. The extract was combined and evaporated in vacuum to residue, which was suspended in water and successively partitioned with EtOAc and n-BuOH. Part of the n-BuOH extract was isolated and purified by various column chromatographs such as a macroporous resin, silica gel, Sephadex LH-20 column and semipreparative HPLC. The structures of isolated and purified compounds were determined by spectral analysis such as UV, IR, HRESI-MS, ESI-MS, 1H NMR, 13C NMR, HMQC, HMBC, H-H COSY, NOESY and physico-chemical property. Six compounds were identified as polyhongkonggaline (1), 3, 6'-di-O-sinapoyl-sucrose (2), tenuifoliside A (3), glomeratose D (4), cis-syringin (5), syringaresinol-4'-O-beta-D-monoglucoside (6). Compounds 1 is new compound, and 2-6 were isolated from this plant for the first time. Farther studies on the chemical constituents and pharmacological activities of P. hongkongensis will be carried out.
Chromatography, High Pressure Liquid ; Glucosides ; chemistry ; isolation & purification ; Molecular Structure ; Phenylpropionates ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Polygala ; chemistry ; Pyrrolidines ; chemistry ; isolation & purification ; Sucrose ; analogs & derivatives ; chemistry ; isolation & purification

OBJECTIVETo study the anatomy of Dracaena cochinchinensis systematically, and find out the distribution and detect the constituents of its resin, in order to provide substantial foundation for the formation mechanism of its red resin.

METHODThe microscopic structures of D. cochinchinensis were systematically observed by using color micrographics, including stem with and without resin, roots, barks and leaves. The HPLC fingerprints of the stem with and without resin were compared.

RESULTCharacteristics of the tangentical longitudinal section of stem with resin and surface view of leaves were elucidated. Besides xylem vessels and fibers of the stem, it was found that the red resin also exists in the cortex parenchyma cells of the stem and the medulla and xylem of the root. According to the HPLC fingerprint analysis result of the stems with and without resin, a number of flavones and stilbenoids were detected in the stem in which resin appeared after it wounded.

CONCLUSIONNo secretory tissue to secrete resin was found in D. cochinchinensis, further study is needed to elucidate the formation mechanism of its resin.

Dracaena ; anatomy & histology ; chemistry ; metabolism ; Plants, Medicinal ; anatomy & histology ; chemistry ; metabolism ; Resins, Plant ; chemistry ; metabolism

OBJECTIVETo isolate and elucidate the constituents of herbs of Polygala hongkongensis.

METHODThe constituents were isolated and purify by chromatographic on silica gel, Sephadax LH-20 and semi-preparative HPLC. The structures were determined by NMR and MS spectral analysis.

RESULTSix compounds were identified as euxanthone (1), 1, 3, 6-trihydroxyxanthone (2), 1, 4, 7-trihydroxy-3-methoxy-xanthone (3), p-hydroxybenzoic acid (4), 3, 4-dihydroxybenzoic acid (5), and methy 1 2, 5-dihydroxybenzoate (6).

CONCLUSIONThe known compounds 1-6 were isolated from this plant for the first time.

Chromatography, Gel ; Chromatography, High Pressure Liquid ; methods ; Hydroxybenzoates ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Parabens ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Polygala ; chemistry ; Xanthones ; chemistry ; isolation & purification

To identify the regulatory region that are responsible for the expression of mPC-1, we have isolated and characterized the mPC-1 gene promoter. Sequence analysis of the mPC-1 5' -flanking region and a series of truncated constructs were performed, which were transiently transfected into the prostate cancer cell lines and non-prostate cancer cell lines and analyzed through Dual-luciferase reporter assay system. The relative activity of mPC-1 gene promoter was by far higher than pGL3-control containing SV40 promoter and enhancer and p61-PSA containing hPSA 6 kb promoter in AR (androgen receptor, AR ) -positive prostate cancer cell lines. The region from 599 bp to 449 bp of mPC-1 promoter might contain a negative regulatory element. The expression of mPC-1 1.1 kb fragment is mainly restricted into prostate cancer cell lines. The relative activity of mPC-1 1.1 kb 5'-flanking region was regulated by androgen. The results demonstrated that the 1.1 kb fragment of mPC-1 5' -flanking region was relatively strong and prostate cancer cell specific promoter region.The 1.1 kb promoter of mPC-1 gene might be well suited to prostate cancer gene therapy if the promoter was properly modified.

OBJECTIVETo investigate pharmacological effects of the total flavonoid in Hypericum perforatum on depression.

METHODExperimental depression was induced by subcutaneous injection of reserpine in mice. The concentration of monoamine transmitters including 5-HT and NE, the activity of monoamine oxidase (MAO) in brain and reserpine-induced symptoms of depression, such as ptosis, attenuation of autonomous activity, behavioral despair, acquired helplessness and sleep, were measured respectively to evaluate the effects of the total flavonoid in H. perforatum on the depression.

RESULTThe total flavonoid in H. perforatum significantly decreased the activity of MAO, inhibited the ptosis and the attenuation of autonomous behavior induced by reserpine respectively. The levels of 5-HT and NE were also attenuated by the total flavonoid in H. perforatum remarkably. In addition, the total flavonoid in H. perforatum was shown to inhibit behavioral despair and acquired helplessness and to prolong the sleep time in the mice. Following the treatment with the total flavonoid in H. perforatum, 5-THP, at the dosage without any side-effects, caused the tremble in the mice.

CONCLUSIONThe results indicate that total flavonoid in H. perforatum can significantly inhibit the depression.

Animals ; Antidepressive Agents ; pharmacology ; Brain ; metabolism ; Depression ; chemically induced ; enzymology ; physiopathology ; Female ; Flavonoids ; isolation & purification ; pharmacology ; Hypericum ; chemistry ; Male ; Mice ; Mice, Inbred ICR ; Monoamine Oxidase ; metabolism ; Motor Activity ; drug effects ; Norepinephrine ; metabolism ; Plants, Medicinal ; chemistry ; Reserpine ; Serotonin ; metabolism ; Sleep ; drug effects

Aged ; Aged, 80 and over ; Cholangiopancreatography, Magnetic Resonance ; Female ; Gallstones ; diagnosis ; Humans ; Ileus ; diagnosis ; Male ; Tomography, X-Ray Computed

OBJECTIVETo investigate the efficacy and feasibility of duodenojejunal bypass(DJB)on non-severe obese patients with type 2 diabetes mellitus(T2DM).

METHODSThe body mass index (BMI), fasting plasma glucose(FPG), 2h-postprandial plasma glucose(2hPG), fasting insulin(F-ins), fasting c-peptide(F-CP), glycated hemoglobin and hypoglycemic agents dose changes were tested in 7 patients with non-severe obese T2DM undergoing DJB, preoperatively and within 24 weeks after surgery during the follow-up. Data were collected and the clinical outcomes of T2DM were analyzed.

RESULTSIn 7 cases of non-obese T2DM who underwent DJB, one patient was weaned off hypoglycemic agents with normal FPG, 2hPG and HbA1c postoperatively. Five required significantly lower dosage. No significant improvement in 1 case. Complete remission rate of hyperglycemia was 1/7, effective rate was 6/7, and effective rate of HbA1c was 5/7. No significant changes in BMI were observed between the preoperative and postoperative phases.

CONCLUSIONPlasma glucose level can be markedly reduced by duodenojejunal bypass in non-obese T2DM, independent of weight loss, and the mechanism remains unclear.

Adult ; Aged ; Bariatric Surgery ; methods ; Diabetes Mellitus, Type 2 ; surgery ; Duodenum ; surgery ; Female ; Follow-Up Studies ; Humans ; Jejunum ; surgery ; Male ; Middle Aged ; Obesity ; Treatment Outcome