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11.
Duanpen Sandee Sumalee Tungpradabkul Manae Tsukio Tadayuki Imanaka Masahiro Takagi 《BMC biotechnology》2002,2(1):16-8
Background
Hep27 monoclonal (Hep27 Mab) is an antibody against hepatocellular carcinoma. Hep27 Mab itself can inhibit the growth of a hepatocellular carcinoma cell line (HCC-S102). We attempted to produce a single-chain fragment (scFv), a small fragment containing an antigen-binding site of Hep27 Mab, by using DNA-recombinant techniques.Results
The sequences encoding the variable regions of heavy (VH) and light (VL) chains of a murine Hep27 Mab were linked together by a linker peptide (Gly4Ser)3 and tagged with a hexa-histidine at the C-terminal; the resultant DNA construct was expressed in E. coli as an insoluble protein. The denatured scFv was refolded and purified by immobilized metal ion affinity chromatography (12 mg/l with a molecular weight of 27 kDa). Hep27scFv exhibited a tumoricidal activity against the HCC-S102 cell as its parental antibody (Hep27 Mab).Conclusion
This scFv may be a potential candidate for a targeting agent in HCC immunodiagnosis or immunotherapy. 相似文献12.
Jeffrey J. Billings Mei-Ping Kung Sumalee Chumpradit David Mozley Abass Alavi Hank F. Kung 《Journal of neurochemistry》1992,58(1):227-236
In developing CNS D1 dopamine receptor-imaging agents with improved specificity and longer brain retention, an iodinated D1 ligand was synthesized. In vitro and in vivo radiolabeling studies of a new iodinated benzazepine, TISCH [7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3- benzazepine], an analog of SCH 23390 (7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepin e), were investigated. After an intravenous injection, the R(+) isomer of TISCH showed high brain uptake in rats (2.20 and 0.57% dose per whole brain at 2 and 60 min, respectively). The striatum/cerebellum ratio increased progressively with time (12 at 60 min). Ex vivo autoradiography of rat brain sections, after intravenous injection of R(+)-[125I]TISCH, displayed the highest uptake in striatum and substantia nigra, regions known to have a high concentration of D1 receptors, whereas the S(-) isomer displayed no specific uptake. Furthermore, the specific uptake can be blocked by pretreatment with SCH 23390. In vitro binding studies using the rat striatum tissue preparation showed high specific and low nonspecific bindings (KD = 0.21 +/- 0.03 nM). The rank order of potency exhibiting high specificity to the D1 receptor was SCH 23390 greater than (+/-)-TISCH greater than (+)-butaclamol = (+/-)-FISCH [7-chloro-8-hydroxy-1-(4'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1 H-3-benzazepine] much greater than WB4101 = spiperone greater than dopamine, serotonin, (+/-)-propranolol, and naloxone. Imaging studies in a monkey with the resolved isomer, R(+)-[123I]TISCH, demonstrated a high uptake in the basal ganglia and prolonged retention. The preliminary data suggest that R(+)-TISCH is selective for the CNS D1 receptor and is potentially useful for in vivo and in vitro pharmacological studies. When labeled with iodine-123, it may be suitable for noninvasive imaging in humans. 相似文献
13.
Marie Hoarau Jarunee Vanichtanankul Nitipol Srimongkolpithak Danoo Vitsupakorn Yongyuth Yuthavong Sumalee Kamchonwongpaisan 《Journal of enzyme inhibition and medicinal chemistry》2021,36(1):198
In various malaria-endemic regions, the appearance of resistance has precluded the use of pyrimidine-based antifolate drugs. Here, a three-step fragment screening was used to identify new non-pyrimidine Plasmodium falciparum dihydrofolate reductase (PfDHFR) inhibitors. Starting from a 1163-fragment commercial library, a two-step differential scanning fluorimetry screen identified 75 primary fragment hits. Subsequent enzyme inhibition assay identified 11 fragments displaying IC50 in the 28-695 μM range and selectivity for PfDHFR. In addition to the known pyrimidine, three new anti-PfDHFR chemotypes were identified. Fragments from each chemotype were successfully co-crystallized with PfDHFR, revealing a binding in the active site, in the vicinity of catalytic residues, which was confirmed by molecular docking on all fragment hits. Finally, comparison with similar non-hit fragments provides preliminary input on available growth vectors for future drug development. 相似文献
14.
Orawan Chinrasri Piyanete Chantiratikul Sarunya Maneetong Sumalee Chookhampaeng Anut Chantiratikul 《Biological trace element research》2013,155(3):381-386
This study aimed to determine the effectiveness of Se from hydroponically produced Se-enriched kale sprout (HPSeKS) on productive performance, egg quality, and Se concentrations in egg and tissue of laying quails. Two-hundred quails, 63 days of age, were divided into four groups. Each group consisted of five replicates and each replicate had ten birds, according to a completely randomized design. The experiment lasted for 6 weeks. The dietary treatments were T1 (control diet), T2 (control diet plus 0.2 mg Se/kg from sodium selenite), T3 (control diet plus 0.2 mg Se/kg from Se-enriched yeast), T4 (control diet plus 0.2 mg Se/kg from HPSeKS). The findings revealed that productive performance and egg quality of quails were not altered (p?>?0.05) by Se sources. Whole egg Se concentrations of quails fed Se from HPSeKS and Se-enriched yeast were higher (p?<?0.05) than that of quails fed the control diet. Breast muscle Se concentrations in quails fed Se from HPSeKS were higher (p?<?0.05) than that of quails fed Se from sodium selenite and Se-enriched yeast. Heart tissue Se concentrations of quails fed Se from Se-enriched yeast and HPSeKS were similar (p?>?0.05), but higher (p?<?0.05) than that of quails fed Se from sodium selenite. The results reveal that Se from HPSeKS did not change the performance and egg quality of quails. The effectiveness of Se from HPSeKS was comparable to that of Se-enriched yeast, which was higher than that of Se from sodium selenite. 相似文献
15.
Boonmar S Morita Y Fujita M Sangsuk L Suthivarakom K Padungtod P Maruyama S Kabeya H Kato M Kozawa K Yamamoto S Kimura H 《Microbiology and immunology》2007,51(5):531-537
In Thailand, 51% (36/70) Campylobacter jejuni isolates from humans and 68% (47/69) isolates from poultry were classified into 10 Penner serotypes (serotype B, C, R, E, G, A, K, D, I, and L) and 9 serotypes (serotype A, C, I, K, B, E, S, D, and L), respectively. The rate of antimicrobial drug resistance to nalidixic acid, ciprofloxacin, ampicillin, tetracycline, and erythromycin shown by human isolates were 96%, 96%, 29%, 57%, and 14%, while that shown by poultry isolates were 77%, 77%, 22%, 26%, and 17%, respectively. All quinolone-resistant strains contained a mutation in the gyrA gene (T(86)-->I(86)), suggesting that the strains were already widespread in Thailand. 相似文献
16.
Wondwossen A. Gebreyes Jean Dupouy-Camet Melanie J. Newport Celso J. B. Oliveira Larry S. Schlesinger Yehia M. Saif Samuel Kariuki Linda J. Saif William Saville Thomas Wittum Armando Hoet Sylvain Quessy Rudovick Kazwala Berhe Tekola Thomas Shryock Michael Bisesi Prapas Patchanee Sumalee Boonmar Lonnie J. King 《PLoS neglected tropical diseases》2014,8(11)
Zoonotic infectious diseases have been an important concern to humankind for more than 10,000 years. Today, approximately 75% of newly emerging infectious diseases (EIDs) are zoonoses that result from various anthropogenic, genetic, ecologic, socioeconomic, and climatic factors. These interrelated driving forces make it difficult to predict and to prevent zoonotic EIDs. Although significant improvements in environmental and medical surveillance, clinical diagnostic methods, and medical practices have been achieved in the recent years, zoonotic EIDs remain a major global concern, and such threats are expanding, especially in less developed regions. The current Ebola epidemic in West Africa is an extreme stark reminder of the role animal reservoirs play in public health and reinforces the urgent need for globally operationalizing a One Health approach. The complex nature of zoonotic diseases and the limited resources in developing countries are a reminder that the need for implementation of Global One Health in low-resource settings is crucial. The Veterinary Public Health and Biotechnology (VPH-Biotec) Global Consortium launched the International Congress on Pathogens at the Human-Animal Interface (ICOPHAI) in order to address important challenges and needs for capacity building. The inaugural ICOPHAI (Addis Ababa, Ethiopia, 2011) and the second congress (Porto de Galinhas, Brazil, 2013) were unique opportunities to share and discuss issues related to zoonotic infectious diseases worldwide. In addition to strong scientific reports in eight thematic areas that necessitate One Health implementation, the congress identified four key capacity-building needs: (1) development of adequate science-based risk management policies, (2) skilled-personnel capacity building, (3) accredited veterinary and public health diagnostic laboratories with a shared database, and (4) improved use of existing natural resources and implementation. The aim of this review is to highlight advances in key zoonotic disease areas and the One Health capacity needs. 相似文献
17.
Masahiko Isaka Panida Chinthanom Sumalee Supothina Suchada Mongkolsamrit 《Phytochemistry letters》2012,5(4):734-737
Two new hopane-type triterpenenes, 6α,15α,22-trihydroxyhopane (4) and 3β-acetoxy-6α,22-dihydroxyhopane (5), together with the known 6α,22-dihydroxyhopane (1, zeorin), 15α,22-dihydroxyhopane (2, dustanin), and 3β-acetoxy-15α,22-dihydroxyhopane (3) were isolated from the scale insect pathogenic fungus Aschersonia calendulina BCC 23276. The structures were elucidated on the basis of NMR spectroscopic and mass spectrometry data. 相似文献
18.
Maitarad P Saparpakorn P Hannongbua S Kamchonwongpaisan S Tarnchompoo B Yuthavong Y 《Journal of enzyme inhibition and medicinal chemistry》2009,24(2):471-479
Comparative molecular field analysis (CoMFA) was performed on twenty-three pyrimethamine (pyr) derivatives active against quadruple mutant type (Asn51Ile, Cys59Arg, Ser108Asn, Ile164Leu) dihydrofolate reductase of Plasmodium falcipaarum (PfDHFR). The represented CoMFA models were evaluated based on the various three different probe atoms, C(sp3) (+1), O(sp3) (-1) and H (+1), resulting in the best model with combined three types of probe atoms. The statistical results were r(2)(cv) = 0.702, S(press) = 0.608, r(2)(nv) = 0.980, s = 0.156, and r(2)(test-set) = 0.698 which can explain steric contribution of about 50%. In addition, an understanding of particular interaction energy between inhibitor and surrounding residues in the binding pocket was performed by using MP2/6-31G(d,p) quantum chemical calculations. The obtained results clearly demonstrate that Asn108 is the cause of pyr resistance with the highest repulsive interaction energy. Therefore, CoMFA and particular interaction energy analyses can be useful for identifying the structural features of potent pyr derivatives active against quadruple mutant type PfDHFR. 相似文献
19.
The aim of this study was to investigate a newly synthesized dextrin–zidovudine (AZT) conjugate designed as a sustained release
prodrug of AZT for parenteral administration. AZT was first reacted with succinic anhydride to form a succinoylated AZT which
was subsequently coupled with dextrin to yield the dextrin–AZT conjugate. The structure of the conjugate was characterized
by FT-IR and 1H-NMR spectroscopy. The drug content of the conjugate was 18.9 wt.%. The release in vitro of free AZT and succinoylated AZT was investigated in buffer solutions at pH 5.5 and 7.4 and in human plasma. AZT and succinoylated
AZT release from the conjugate was 1.4% (pH 5.5), 41.7% (pH 7.4) and 78.4% in human plasma after 24 h. Release was complete
in human plasma after 48 h. A pharmacokinetic study in rats following intravenous administration of the conjugate showed prolonged
plasma levels of AZT compared to free AZT. The use of the conjugate extended the plasma half-life of AZT from 1.3 to 19.3 h
and the mean residence time from 0.4 to 23.6 h. Furthermore, the conjugate provided a significant greater area under the plasma
concentration-time curve and reduced the systemic clearance of AZT. This study suggested the potential of this novel dextrin–AZT
conjugate as a new intravenous preparation of AZT. 相似文献