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Các hợp chất dị vòng chứa nhân quinazolinone được biết có nhiều hoạt tính sinh học như kháng viêm, kháng khuẩn, hạ huyết áp, kháng co giật, kháng ung thư và kháng sốt rét nên là một khung sườn quan trọng cho việc phát triển các loại thuốc mới hiện nay. Trong nghiên cứu này, hai quy trình tổng hợp nhân quinazolinone đã được đề xuất. Ưu điểm của quy trình là đơn giản, hiệu quả, sử dụng tác nhân oxy hóa rẻ tiền là FeCl3 và đặc biệt sử dụng dung môi là nước thân thiện với môi trường. Áp dụng quy trình này, hai dẫn xuất N-alkyl quinazolinone (2a-b) và bốn dẫn xuất N-acetamidyl quinazolinone (8a-d) đã được tổng hợp thành công với hiệu suất cao (62-81%). Kết quả đánh giá hoạt tính kháng khuẩn cho thấy hai dẫn xuất N-acetamidyl quinazolinone có hoạt tính kháng chủng vi khuẩn Bacillus cereus tốt (MIC £ 8 µg/mL) tương đương chất kháng sinh thương mại là Vancomycin hydrochloride.

There are still ongoing debates as to which cut-off percentage of tall cell (TC) should be used to define tall cell variant (TCV) papillary thyroid carcinoma (PTC). In this meta-analysis, we aimed to investigate the clinicopathological significance of PTC with tall cell features (PTC-TCF, PTC with 10–50% of TCs) in comparison with classical PTC and TCVPTC (PTC with more than 50% of TCs) to clarify the controversial issue. Four electronic databases including PubMed, Web of Science, Scopus and Virtual Health Library were accessed to search for relevant articles. We extracted data from published studies and pooled into odds ratio (OR) and its corresponding 95% confidence intervals (CIs) using random-effect modeling. Nine studies comprising 403 TCVPTCs, 325 PTC-TCFs and 3552 classical PTCs were included for meta-analyses. Overall, the clinicopathological profiles of PTC-TCF including multifocality, extrathyroidal extension, lymph node metastasis, distant metastasis and patient mortality were not statistically different from those of TCVPTC. Additionally, PTC-TCF and TCVPTC were both associated with an increased risk for aggressive clinical courses as compared to classical PTC. The prevalence of BRAF mutation in PTC-TCF and TCVPTC was comparable and both were significantly higher than that in classical PTC. The present meta-analysis demonstrated that even a PTC comprising only 10% of TCs might be associated with a poor clinical outcome. Therefore, the proportions of PTC in PTC should be carefully estimated and reported even when the TC component is as little as 10%.

1,3,4-Oxadiazole có nhiều hoạt tính sinh học bao gồm kháng khuẩn, kháng nấm, kháng viêm, giảm đau, hạ lipid máu, kháng ung thư, chống co giật, chống đái tháo đường, kháng virus và chống loét. Trong nghiên cứu này, hai dẫn xuất 2-phenyl-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole (6a) và 2-(4-methoxy-6-methylnaphthalen-2-yl)-5-phenyl-1,3,4-oxadiazole (8b) đã được tổng hợp thành công với hiệu suất rất cao. Phương pháp tổng hợp được sử dụng là phản ứng ghép vòng dẫn xuất acylhydrazone tạo nhân 1,3,4-oxadiazole sử dụng iodine làm tác nhân oxy hóa dưới sự hiện diện của potassium carbonate. Các điều kiện của phản ứng này cũng áp dụng tốt với chất nền là acylhydrazone thô thu được từ sự ngưng tụ giữa aldehyde và hydrazide. Đánh giá hoạt tính kháng khuẩn của hai dẫn xuất (6a) và (8b) cho thấy hai hợp chất này có khả năng kháng lại ba chủng vi khuẩn: Escherichia coli, Staphylococcus aureus và Bacillus cereus.

Ba hợp chất: (1) lupeol acetate, (2) 1-palmitoylglycerol và (3) tricin đã được phân lập từ cao chiết phân đoạn hexane và ethyl acetate từ cây Bạch Đầu Ông Vernonia cinerea (L.) Less. Cấu trúc của các hợp chất được nhận danh bằng các phương pháp phổ hiện đại như1H-NMR,13C-NMR, HSQC, HMBC, MS và so sánh với tài liệu đã công bố. Hàm lượng polyphenol tổng của cao chiết phân đoạn ethyl acetate (215,55 mg GAE/g) từ cây Bạch đầu ông cao nhất so với các cao chiết ethanol tổng và cao nước. Kết quả trên tương đồng với khả năng kháng oxy hoá tốt nhất của cao ethyl acetate IC50 = 24,10 mg/mL.

Background: Dengue infection during peripartum period, although rare in endemic regions, has challenged clinicians regarding its management, especially if a parturient woman experiences postpartum hemorrhage due to a classical risk factor of maternal bleeding. Case: A full-term pregnant Vietnamese woman was diagnosed with polyhydramnios and Dengue with warning signs (DWS). She was administered platelet transfusion prior to delivery and then gave birth to a healthy newborn. After active management of the third stage of labor, the patient suffered a postpartum hemorrhage which was caused by uterine atony and accompanied with thrombocytopenia. Therefore, we decided to administer uterotonic drugs and additionally transfuse platelets. Conclusion: We describe a case of postpartum hemorrhage caused by uterine atony and coinciding with Dengue infection during delivery period, which is a rare clinical entity. With timely detection and management, the patient was finally discharged without complications.

BackgroundEvidence-based medicine (EBM) has developed as the dominant paradigm of assessment of evidence that is used in clinical practice. Since its development, EBM has been applied to integrate the best available research into diagnosis and treatment with the purpose of improving patient care. In the EBM era, a hierarchy of evidence has been proposed, including various types of research methods, such as meta-analysis (MA), systematic review (SRV), randomized controlled trial (RCT), case report (CR), practice guideline (PGL), and so on. Although there are numerous studies examining the impact and importance of specific cases of EBM in clinical practice, there is a lack of research quantitatively measuring publication trends in the growth and development of EBM. Therefore, a bibliometric analysis was constructed to determine the scientific productivity of EBM research over decades.MethodsNCBI PubMed database was used to search, retrieve and classify publications according to research method and year of publication. Joinpoint regression analysis was undertaken to analyze trends in research productivity and the prevalence of individual research methods.FindingsAnalysis indicates that MA and SRV, which are classified as the highest ranking of evidence in the EBM, accounted for a relatively small but auspicious number of publications. For most research methods, the annual percent change (APC) indicates a consistent increase in publication frequency. MA, SRV and RCT show the highest rate of publication growth in the past twenty years. Only controlled clinical trials (CCT) shows a non-significant reduction in publications over the past ten years.ConclusionsHigher quality research methods, such as MA, SRV and RCT, are showing continuous publication growth, which suggests an acknowledgement of the value of these methods. This study provides the first quantitative assessment of research method publication trends in EBM.

As part of our ongoing research on new anti-diabetic compounds from ethnopharmacologically consumed plants, two previously undescribed lupane-type triterpenoids (1 and 2) with dicarboxylic groups, an undescribed nor-taraxastane-type triterpenoid (3), and 14 known compounds (4–17) were isolated from the leaves of Cleistocalyx operculatus. Extensive spectroscopic analysis (IR, HRESIMS, 1D, and 2D NMR) was used for structure elucidation, while the known compounds were compared to reference data reported in the scientific literature. All the isolates (1–17) were evaluated for their inhibitory effects on the protein tyrosine phosphatase 1B (PTP1B) enzyme. Compounds 6, 9, and 17 showed strong PTP1B inhibitory activities. The mechanism of PTP1B inhibition was studied through enzyme kinetic experiments. A non-competitive mechanism of inhibition was determined using Lineweaver–Burk plots for compounds 6, 9, and 17. Additionally, Dixon plots were employed to determine the inhibition constant. Further insights were gained through a structure–activity relationship study and molecular docking analysis of isolated compounds with the PTP1B crystal structure. Moreover, all isolates (1–17) were tested for their stimulatory effects on the uptake of 2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl) amino]-D-glucose (2-NBDG) in differentiated 3T3-L1 adipocyte cells. Compounds 6, 13, and 17 exhibited strong glucose absorption stimulation activity in a dose-dependent manner. [ABSTRACT FROM AUTHOR]

Gillnet, stow-net and trawl are the three main fishing gears used by coastal fishers in Soc Trang and Bac Lieu provinces in the lower Mekong Delta, but catches from all three have been declining in recent years. We investigated the species composition of fish stocks along this coastline of Vietnam, and examined the current status of fishers and the gears they use, their fish catches, and the economic returns from each of the three net types. We also assessed the awareness of climate change among fishers, and the actions they take to adapt to its consequences. Annual fish catches were low: 11.9 tboat-1year-1 for stow-netters, 9.3 tboat-1year-1 for trawlers, and 4.4 tboat-1year-1 for gillnetters. Despite its low catch rate, the gillnet fishery provided the highest annual profit (4,364 USDboat-1year-1) because it caught higher value fish due to both their species and size. The rate of return was 0.52 for the gillnet fishery, 0.52 for the stow-net fishery and 0.33 for the trawl fishery. Overall, fishers had a low educational status and poor understanding of climate change, and only about two-thirds of them had short-term solutions to deal with changing weather and sea conditions. Current fishing practices, coupled with climate change are likely to lead to further declines in fish stocks and catches and threaten the livelihoods of near-shore coastal fishers. [ABSTRACT FROM AUTHOR]

Background: Pancreatic cancer (PC) has a grim prognosis, and an early diagnostic biomarker has been highly desired. The molecular link between diabetes and PC has not been well established.Methods: Bioinformatics screening was performed for a serum PC marker. Experiments in cell lines (5 PC and 1 normal cell lines), mouse models, and human tissue staining (37 PC and 10 normal cases) were performed to test asprosin production from PC. Asprosin's diagnostic performance was tested with serums from multi-center cohorts (347 PC, 209 normal, and 55 additional diabetic patients) and evaluated according to PC status, stages, and diabetic status, which was compared with that of CA19-9.Results: Asprosin, a diabetes-related hormone, was found from the bioinformatics screening, and its production from PC was confirmed. Serum asprosin levels from multi-center cohorts yielded an age-adjusted diagnostic area under the curve (AUC) of 0.987 (95% confidence interval [CI] = 0.961 to 0.997), superior to that of CA19-9 (AUC = 0.876, 95% CI = 0.847 to 0.905), and a cut-off of 7.18 ng/mL, at which the validation set exhibited a sensitivity of 0.957 and a specificity of 0.924. Importantly, the performance was maintained in early-stage and non-metastatic PC, consistent with the tissue staining. A slightly lower performance against additional diabetic patients (n = 55) was restored by combining asprosin and CA19-9 (AUC = 0.985, 95% CI = 0.975 to 0.995).Conclusions: Asprosin is presented as an early-stage PC serum marker that may provide clues for PC-induced diabetes. Larger prospective clinical studies are warranted to solidify its utility. [ABSTRACT FROM AUTHOR]

Chemical investigation of the lichen Dirinaria applanata led to isolate nine compounds including a new hopane derivative, 1β-acetoxy-21α-hopane-3β,22-diol (1) together with six phenolic compounds naming divaricatinic acid (2), methyl divaricatinate (3), methyl-β-orcinolcarboxylate (4), methyl haematommate (5), divarinol (6), ramalinic acid A (7), and two xanthones namely lichenxanthone (8), 4,5-dichlorolichenxanthone (9). Their structures were elucidated by spectroscopic data in combination with published literature. Except compound 2, all compounds were isolated from this species for the first time. [ABSTRACT FROM AUTHOR]

From the extract of lichen Dirinaria applanata, two hopane derivatives including 1β -acetoxy-3β - hydroxy-21α-hopan-29-oic acid (1), hopane-3β, 6β, 21α-triol (2) and a depside namely 2-O'- methylnordivaricatic acid (3) were isolated and identified by extensive analyzing 1D-NMR, 2D-NMR, HRESIMS, and FT-IR. Notably, compound 1 and 3 were novel compounds while compound 2 was isolated from this lichen species for the first time. [ABSTRACT FROM AUTHOR]

Mười dẫn xuất benzimidazole mang các nhóm thế khác nhau ở các vị trí số 4 và số 5 trên nhân benzimidazole (aza, -H, -Cl, -NO2, -CH3) đã được tổng hợp thành công với hiệu suất 41% - 90% từ sự ngưng tụ giữa các dẫn xuất o-phenylenediamine và benzylamine, sử dụng sodium metabisulfite (Na2S2O5)là tác nhân oxi hóa. Việc sử dụng dung môi dimethylsulfoxide (DMSO) thay cho ethanol giúp tăng hiệu suất tổng hợp cũng như rút ngắn thời gian phản ứng từ 24 giờ xuống còn 18 giờ cho mỗi phản ứng tổng hợp. Hợp chất 2-(2-chlorophenyl)-5-nitro-1H-benzimidazole cho hiệu suất tổng hợp cao nhất (90%). Cấu trúc của các chất tổng hợp được xác định bằng các phương pháp phổ nghiệm MS,1H‑NMR và 13C‑NMR.

BACKGROUND: Ethics is one of the main pillars in the development of science. We performed a JoinPoint regression analysis to analyze the trends of ethical issue research over the past half century. The question is whether ethical issues are neglected despite their importance in modern research. METHOD: PubMed electronic library was used to retrieve publications of all fields and ethical issues. JoinPoint regression analysis was used to identify the significant time trends of publications of all fields and ethical issues, as well as the proportion of publications on ethical issues to all fields over the past half century. Annual percent changes (APC) were computed with their 95% confidence intervals, and a p-value < 0.05 was considered statistically significant. RESULTS: We found that publications of ethical issues increased during the period of 1965-1996 but slightly fell in recent years (from 1996 to 2013). When comparing the absolute number of ethics related articles (APEI) to all publications of all fields (APAF) on PubMed, the results showed that the proportion of APEI to APAF statistically increased during the periods of 1965-1974, 1974-1986, and 1986-1993, with APCs of 11.0, 2.1, and 8.8, respectively. However, the trend has gradually dropped since 1993 and shown a marked decrease from 2002 to 2013 with an annual percent change of -7.4%. CONCLUSIONS: Scientific productivity in ethical issues research on over the past half century rapidly increased during the first 30-year period but has recently been in decline. Since ethics is an important aspect of scientific research, we suggest that greater attention is needed in order to emphasize the role of ethics in modern research. [ABSTRACT FROM AUTHOR]

Background: Pancreatic cancer (PC) has a grim prognosis, and an early diagnostic biomarker has been highly desired. The molecular link between diabetes and PC has not been well established., Methods: Bioinformatics screening was performed for a serum PC marker. Experiments in cell lines (5 PC and 1 normal cell lines), mouse models, and human tissue staining (37 PC and 10 normal cases) were performed to test asprosin production from PC. Asprosin's diagnostic performance was tested with serums from multi-center cohorts (347 PC, 209 normal, and 55 additional diabetic patients) and evaluated according to PC status, stages, and diabetic status, which was compared with that of CA19-9., Results: Asprosin, a diabetes-related hormone, was found from the bioinformatics screening, and its production from PC was confirmed. Serum asprosin levels from multi-center cohorts yielded an age-adjusted diagnostic area under the curve (AUC) of 0.987 (95% confidence interval [CI] = 0.961 to 0.997), superior to that of CA19-9 (AUC = 0.876, 95% CI = 0.847 to 0.905), and a cut-off of 7.18 ng/mL, at which the validation set exhibited a sensitivity of 0.957 and a specificity of 0.924. Importantly, the performance was maintained in early-stage and non-metastatic PC, consistent with the tissue staining. A slightly lower performance against additional diabetic patients (n = 55) was restored by combining asprosin and CA19-9 (AUC = 0.985, 95% CI = 0.975 to 0.995)., Conclusions: Asprosin is presented as an early-stage PC serum marker that may provide clues for PC-induced diabetes. Larger prospective clinical studies are warranted to solidify its utility., (© The Author(s) 2021. Published by Oxford University Press. All rights reserved. For permissions, please email: journals.permissions@oup.com.)