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Jiraporn Kara Paptawan Suwanhom Chatchai Wattanapiromsakul Teerapat Nualnoi Jindaporn Puripattanavong Pasarat Khongkow Vannajan Sanghiran Lee Anand Gaurav Luelak Lomlim 《Archiv der Pharmazie》2019,352(7)
Sixteen novel coumarin‐based compounds are reported as potent acetylcholinesterase (AChE) inhibitors. The most active compound in this series, 5a (IC50 0.04 ± 0.01 µM), noncompetitively inhibited AChE with a higher potency than tacrine and galantamine. Compounds 5d , 5j , and 5 m showed a moderate antilipid peroxidation activity. The compounds showed cytotoxicity in the same range as the standard drugs in HEK‐293 cells. Molecular docking demonstrated that 5a acted as a dual binding site inhibitor. The coumarin moiety occupied the peripheral anionic site and showed π‐π interaction with Trp278. The tertiary amino group displayed significant cation‐π interaction with Phe329. The aromatic group showed π‐π interaction with Trp83 at the catalytic anionic site. The long chain of methylene lay along the gorge interacting with Phe330 via hydrophobic interaction. Molecular docking was applied to postulate the selectivity toward AChE of 5a in comparison with donepezil and tacrine. Structural insights into the selectivity of the coumarin derivatives toward huAChE were explored by molecular docking and 3D QSAR and molecular dynamics simulation for 20 ns. ADMET analysis suggested that the 2‐(2‐oxo‐2H‐chromen‐4‐yl)acetamides showed a good pharmacokinetic profile and no hepatotoxicity. These coumarin derivatives showed high potential for further development as anti‐Alzheimer agents. 相似文献
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The Location and Contents of the Lateral Ligaments of the Rectum: A Study in Human Soft Cadavers 总被引:1,自引:0,他引:1
Pak-art R Tansatit T Mingmalairaks C Pattana-arun J Tansatit M Vajrabukka T 《Diseases of the colon and rectum》2005,48(10):1941-1944
PURPOSE This study was designed to identify the location of the lateral ligaments of the rectum and to reveal its contents.
METHODS From 18 human soft cadavers (9 males), 18 pelves were sagittally sectioned into 36 hemipelvic specimens affording good anatomic
view of the lateral aspect of the rectum. All of them were dissected and mobilized by using sharp technique under direct vision
by one surgeon to avoid confounding factor. The lateral ligaments of the rectum were identified and the distances from the
center of its pelvic attachment to the promontory of sacrum and coccyx were measured. After measurement, they were transected
and brought for histologic examination.
RESULTS In 36 hemipelvic specimens, 18 lateral ligaments of the rectum were found on the right side of the rectum and 18 were found
on the left side. One cadaver had no lateral ligament on the right side and another had two lateral ligaments on the right
side 3-cm apart. The location of the lateral ligaments was posterolateral to the rectum. The distance from the lateral ligament
to sacral promontory on right side was 8.14 ± 1.82 cm (mean ± standard deviation) and 8.14 ± 1.22 cm on left side. The distances
from the lateral ligament to coccyx on the right and left sides were 5.12 ± 1.4 cm and 4.88 ± 1.29 cm, respectively. The content
of the lateral ligaments of the rectum consisted of loose connective tissue with cluster of small nerves. No artery was detected
in all specimens. The small arterioles and venules were discovered in only four specimens.
CONCLUSIONS The lateral ligaments of the rectum were located at posterolateral side of the rectum. They were closer to the coccyx than
to the sacral promontory. Its component was loose connective tissue containing multiple small nerves. There was no artery
found in any lateral ligaments by histologic study. Small arterioles and venules were detected 11 percent.
Presented at the meeting of The American Society of Colon and Rectal Surgeons, Dallas, Texas, May 8 to 13, 2004. 相似文献
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Sosothikul D Kittikalayawong Y Aungbamnet P Buphachat C Seksarn P 《Blood coagulation & fibrinolysis》2012,23(3):208-211
Thromboembolic events are an increasingly common problem encountered in children. The laboratory diagnosis of thrombotic disorders in children differs from that in adults. To establish the normal reference of natural anticoagulant parameters in children of different age groups, plasma from healthy children between the ages of 2 months and 16 years (n = 127) and adults (n = 30) were assayed for a disintegrin-like and metalloprotease with thrombospondin type 1 domain 13 (ADAMTS-13), von Willebrand factor collagen-binding activity (vWF:CB), tissue factor pathway inhibitor (TFPI), homocyteine and natural anticoagulants. Children were divided into four age groups: less than 1 year, 1-5 years, 6-10 years, and 11-16 years. The reference values for ADAMTS 13, homocysteine, and protein C activity were significantly lower in children of all age groups compared with those in the adults. Similarly, those for protein C antigen, total protein S, free protein S and antithrombin III (AT III) for children less than 1 year were significantly lower than in the adults. On the contrary, TFPI levels were significantly higher in the children for all age groups when compared with the adults. vWF:CB levels were comparable across all groups. There are age-related physiologic differences in ADAMTS-13, TFPI, homocysteine and natural anticoagulants between children and adults. Our data will provide physicians with a useful reference guide in interpreting test results of inhibitors of hemostatic parameters in children suspected of thrombotic disorders. 相似文献
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Supaporn Wacharapluesadee Thongchai Kaewpom Weenassarin Ampoot Siriporn Ghai Worrawat Khamhang Kanthita Worachotsueptrakun Phanni Wanthong Chatchai Nopvichai Thirawat Supharatpariyakorn Opass Putcharoen Leilani Paitoonpong Gompol Suwanpimolkul Watsamon Jantarabenjakul Pasin Hemachudha Artit Krichphiphat Rome Buathong Tanarak Plipat Thiravat Hemachudha 《Journal of medical virology》2020,92(10):2193-2199
In the age of a pandemic, such as the ongoing one caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the world faces a limited supply of tests, personal protective equipment, and factories and supply chains are struggling to meet the growing demands. This study aimed to evaluate the efficacy of specimen pooling for testing of SARS-CoV-2 virus, to determine whether costs and resource savings could be achieved without impacting the sensitivity of the testing. Ten previously tested nasopharyngeal and throat swab specimens by real-time polymerase chain reaction (PCR), were pooled for testing, containing either one or two known positive specimens of varying viral concentrations. Specimen pooling did not affect the sensitivity of detecting SARS-CoV-2 when the PCR cycle threshold (Ct) of original specimen was lower than 35. In specimens with low viral load (Ct > 35), 2 of 15 pools (13.3%) were false negative. Pooling specimens to test for Coronavirus Disease 2019 infection in low prevalence (≤1%) areas or in low risk populations can dramatically decrease the resource burden on laboratory operations by up to 80%. This paves the way for large-scale population screening, allowing for assured policy decisions by governmental bodies to ease lockdown restrictions in areas with a low incidence of infection, or with lower-risk populations. 相似文献
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Manosroi J Tayapiwatana C Manosroi A Beer J Bergemann K Werner RG 《Arzneimittel-Forschung》2002,52(1):60-66
Fermentation studies of batch-mode cultivation in 4-L fermenters were carried out to obtain an active recombinant DNA-derived tissue plasminogen activator (t-PA) deletion mutant, lekteplase, secreted and correctly folded from Escherichia coli. The OmpA signal sequence was used to deliver the heterologous product composed of kringle 2 plus serine protease domain (K2S) to the medium. Supplementing the complex medium with 10% glycerol and 20 mmol/l magnesium chloride led to an increase in cell numbers with final cell density reaching an OD600 of 24. The expression level of lekteplase in the medium detected by sandwich ELISA was 100 mg/L. Enzymatic activity of lysine-sepharose purified product was demonstrated by amidolytic assay, in vitro fibrin clot lysis, and copolymerization PAGE. 相似文献
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Tosukhowong P Yachantha C Sasivongsbhakdi T Ratchanon S Chaisawasdi S Boonla C Tungsanga K 《Urological research》2008,36(3-4):149-155
Potassium citrate has long been used as a prophylactic remedy for nephrolithiasis recurrence. Lemonade consumption is also suggested as an option. We compared the efficacy of consumption of solution containing manufactured lime powder with that of potassium citrate, on the improvement of metabolic risk factors, oxidative stress and renal tubular damage in nephrolithiasis patients. Patients with kidney stone were enrolled and randomly assigned to three treatment programs for 3 month period consisting of consumption of solution containing lime powder (Group 1, n = 13), potassium citrate (Group 2, n = 11) and lactose as placebo regimen (Group 3, n = 7). Lime powder and potassium citrate contained equal amounts of potassium (21 mEq) and citrate (63 mEq). After treatment, there was an increase in urinary pH, potassium and citrate in Group 1 and 2. Increased plasma potassium and red blood cell glutathione (R-GSH) and decreased urinary malondialdehyde were found in Group 1, but not observed in Group 2. R-GSH was decreased in Group 2. Urinary N-acetyl-beta-glucosaminidase activity and fractional excretion of magnesium, as renal tubular damage indicators, were decreased only in Group 1. In Group 3, all measured parameters were unaltered except for an increased urinary chloride. In conclusion, consumption of our in-house lime powder exerted citraturic and alkalinizing actions as efficient as consumption of potassium citrate. In addition, it provided an antioxidative effect and was able to attenuate renal tubular damage. These pharmacological properties may be clinically useful to diminish the stone-forming potential in kidney stone patients and hence for preventing recurrent calculi. 相似文献
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Anirut Hlosrichok Somruethai Sumkhemthong Boonchoo Sritularak Pithi Chanvorachote Chatchai Chaotham 《Journal of natural medicines》2018,72(3):615-625
Failure of current chemotherapeutic drugs leads to the recurrence of tumor pathology and mortality in lung cancer patients. This study aimed to evaluate the anticancer activity and related mechanisms of 4,5,4′-trihydroxy-3,3′-dimethoxybibenzyl (TDB), a bibenzyl extracted from Dendrobium ellipsophyllum Tang and Wang, in human lung cancer cells. Cytotoxicity of TDB (0–300 µM) in different types of human lung cancer cells (H460, H292 and H23) and human dermal papilla cells (DPCs) was evaluated via MTT viability assay. Selective anticancer activity of TDB against human lung cancer cells was demonstrated with a high IC50 (approximately > 300 µM) in DPCs, while IC50 in human lung cancer H460, H292 and H23 cells was approximately 100 ± 5.18, 100 ± 8.73 and 188.89 ± 8.30 µM, respectively. After treatment with 50 µM of TDB for 24 h, flow cytometry analysis revealed the significant increase of early and late apoptosis with absence of necrosis cell death in human lung cancer cells. The up-regulation of p53, a tumor-suppressor protein, was elucidated in human lung cancer cells treated with 10–50 µM of TDB. Alteration to down-stream signaling of p53 including activation of pro-apoptosis protein (Bcl-2-associated X protein; Bax), reduction of anti-apoptosis (B cell lymphoma 2; Bcl-2 and myeloid cell leukemia 1; Mcl-1) and suppression on protein kinase B (Akt) survival pathway were notified in TDB-treated lung cancer cells. The information obtained from this study strengthens the potential development of TDB as an anticancer compound with a favorable human safety profile and high efficacy. 相似文献
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