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1.
Indian J Dermatol ; 69(1): 32-37, 2024.
Article En | MEDLINE | ID: mdl-38572050

Background: Narrowband UVB (NBUVB) has recently been used in Vietnam for the treatment of psoriasis. However, there are no data on Vietnamese patients to adopt a uniform national protocol. Objectives: This study aimed to establish an optimal NBUVB therapy for the treatment of psoriasis in Vietnamese patients. Materials and Methods: One hundred and twenty-two patients with psoriasis vulgaris were included. They were randomly allocated to two groups: the percentage dose (group 1, 62 patients) and the fixed dose (group 2, 60 patients). In group 1, the starting dose was 50% of the minimal erythema dose (MED) and the 10% increment dose adjusted in the next sessions. In group 2, the starting dose was based on Fitzpatrick skin types (fixed dose). Psoriasis area and severity index (PASI) was used to evaluate efficacy. Results: More than 68% of the patients get PASI75 at session 36. Group 2 had significantly fewer sessions (20 ± 5 vs 25 ± 7, P- value = 0.0004) and lower cumulative dose than group 1 (14.1 ± 4.3 J/cm2 vs 18.0 ± 8.0 J/cm2, P- value = 0.0075) to achieve PASI75. Adverse effects were more common in group 2 than group 1, including burning sensation/erythema (43.33% vs 14.52%, P- value = 0.0009) and pruritus (75.00% vs 22.58%, P- value <0.0001). Conclusion: NBUVB therapy was safe and effective for Vietnamese psoriasis patients. Fixed doses produced a quicker clinical response with fewer sessions and lower cumulative doses. Adverse effects were mild in both groups and less noted for the MED-based dose. For the recommendation, a fixed dose should be applied for patients who have less concern about side effects, while a MED-based dose can be suitable for patients having conditions related to light sensitivity.

2.
Bioorg Med Chem Lett ; 104: 129714, 2024 May 15.
Article En | MEDLINE | ID: mdl-38522589

A series of new fluorinated dihydrofurano-napthoquinone compounds were sucessfully synthesized in good yields using microwave-assisted multi-component reactions of 2-hydroxy-1,4-naphthoquinone, fluorinated aromatic aldehydes, and pyridinium bromide. The products were fully characterized using spectroscopic techniques and evaluated for their anti-inflammatory activity using lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. Among 12 new compounds, compounds 8b, 8d, and 8e showed high potent NO inhibitory activity in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells with IC50 values ranging from 1.54 to 3.92 µM. The levels of pro-inflammatory cytokines IL-1ß and IL-6 in LPS-stimulated RAW264.7 macrophages were remarkably decreased after the application of 8b, 8d, 8e and 8k. Molecular docking simulations revealed structure-activity relationships of 8b, 8d, and 8e toward NO synthase, cyclooxygenase (COX-2 over COX-1), and prostaglandin E synthase-1 (mPGES-1). Further physicochemical and pharmacokinetic computations also demonstrated the drug-like characteristics of synthesized compounds. These findings demonstrated the importance of fluorinated dihydrofurano-napthoquinone moieties in the development of potential anti-inflammatory agents.


Lipopolysaccharides , Naphthoquinones , Mice , Animals , Lipopolysaccharides/pharmacology , Molecular Docking Simulation , Naphthoquinones/pharmacology , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/chemistry , Cytokines/metabolism , RAW 264.7 Cells , Cyclooxygenase 2/metabolism , Nitric Oxide/metabolism , Nitric Oxide Synthase Type II
3.
RSC Adv ; 14(8): 5264-5275, 2024 Feb 07.
Article En | MEDLINE | ID: mdl-38343997

Epoxy resin has been extensively used in many industrial and daily applications due to its unique properties. However, the high flammability of epoxy has limited its further development. DOPO derivatives, which are organophosphorus compounds, are highly effective components of flame retardant epoxy composites due to their good compatibility with the resin and their lower toxicity compared to halogenated compounds. This study synthesized sixteen new DOPO derivatives, characterizing their chemical structures with NMR spectroscopy. The combination of synthesized DOPO derivatives and APP-PEI (ammonium polyphosphate-polyethyleneimine) has shown a synergistic effect on enhancing the flame retardancy of epoxy resin with the UL-94 V-0 rating and the LOI value of 28.6%. Moreover, the epoxy composites displayed relatively high mechanical performance with the impact strength of 26-28 kJ m-2.

4.
RSC Adv ; 14(3): 1838-1853, 2024 Jan 03.
Article En | MEDLINE | ID: mdl-38192320

Two different synthetic approaches to novel heterocyclic hybrid compounds of 4-azapodophyllotoxin were investigated. The obtained products were characterized by infrared spectroscopy, nuclear magnetic resonance spectroscopy, and high-resolution mass spectrometry. MTT protocol was then performed to examine the cytotoxic activity of these products against KB, HepG2, A549, MCF7, and Hek-293 cell lines. The cytotoxic assessment indicated that all products displayed moderate to high cytotoxicity against all tested cancer cell lines. The most active compound 13k containing the 2-methoxypyridin-4-yl group exhibited selective cytotoxicity against KB, A549, and HepG2 cell lines with the IC50 values ranging from 0.23 to 0.27 µM, which were between 5- to 10-fold more potent than the positive control ellipticine. Compounds 13a (HetAr = thiophen-3-yl) and 13d (HetAr = 5-bromofuran-2-yl) displayed high cytotoxic selectivity for A549 and HepG2 cancer cell lines when compared to the other cancer cell lines and low toxicity to the normal Hek-293 cell line. Molecular docking study was conducted to evaluate the interaction of new synthesized compounds with the colchicine-binding-site of tubulin. Besides that, physicochemical and pharmacokinetic properties of the most active compounds 13h,k were predicted.

5.
Bioorg Med Chem Lett ; 98: 129566, 2024 Jan 15.
Article En | MEDLINE | ID: mdl-38008338

In this study, new indol-fused pyrano[2,3-d]pyrimidines were designed and synthesized. These products were obtained in moderate to good yields and their structures were assigned by NMR, MS, and IR analysis. Afterwards, the biological important of the products was highlighted by evaluating in vitro for α-glucosidase inhibitory activity as well as acetylcholinesterase (AChE) inhibitory activity. Eleven products revealed substantial inhibitory activity against α-glucosidase enzyme, among which, two most potent products 11d,e were approximately 93-fold more potent than acarbose as a standard antidiabetic drug. Besides that, product 11k exhibited good AChE inhibition. The substituents on the 5-phenyl ring, attached to the pyran ring, played a critical role in inhibitory activities. The biological potencies have provided an opportunity to further investigations of indol-fused pyrano[2,3-d]pyrimidines as potential anti-diabetic agents.


Cholinesterase Inhibitors , Glycoside Hydrolase Inhibitors , Acetylcholinesterase/metabolism , alpha-Glucosidases/metabolism , Glycoside Hydrolase Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/chemistry , Hypoglycemic Agents/pharmacology , Molecular Docking Simulation , Pyrans/pharmacology , Pyrans/chemistry , Pyrimidines/pharmacology , Pyrimidines/chemistry , Structure-Activity Relationship , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/pharmacology
6.
Res Vet Sci ; 153: 105-114, 2022 Dec 31.
Article En | MEDLINE | ID: mdl-36347064

Canine distemper virus (CDV) is a pathogen causing fatal disease in a wide range of carnivores. Sequence analysis of CDV strains has been classified into several geographically-related lineages, and the evolution and emergence of these strains are not fully yet investigated. In this study, the complete H gene sequences of 15 CDV strains isolated on Vero DST cell culture from clinical samples of vaccinated domestic dogs in Vietnam were investigated. Fifteen CDV isolates belonging to Asia-1 CDV variants were predominant antigenic type circulated in Central and Northern Vietnam with notable differences regarding the region and some genetic variation, and the most closely related Asia-1 variants lineage reported in Vietnam, China, Taiwan, and Japan. All identified CDV isolates clustered into 2 novel clades Asia-1-C1 and Asia-1-C2. The major amino acid mutation variants of Vietnamese Asia-1 CDV strains were found at sites 51, 157, 159, 160, 171, 178, 186, 235, 245, 277, 288, 313, 324, 330, 337, 345, 358, 359, 365, 383, 446, 475, 517, 530, 584, 598 which include N-glycosylation sites and neutralizing epitope regions in H gene. The results of the virus neutralization titer (VNT) assay showed that the dogs vaccinated with commercial vaccines had significantly low VNT (4.89 and 12.8) against field CDV isolate strains (VNUA NA04, HN18, and NB05) isolated in northern and central Vietnam, respectively. These data may suggest the need for further research in CDV monitoring and development of preventative measures against CDV in Vietnam.

7.
RSC Adv ; 12(34): 22004-22019, 2022 Aug 04.
Article En | MEDLINE | ID: mdl-36043070

A new approach for the synthesis of podophyllotoxin-naphthoquinone compounds using microwave-assisted three-component reactions is reported in this study. Novel podophyllotoxin-naphthoquinone derivatives with modification on ring E were synthesized. All the synthetic compounds were assessed in terms of their cytotoxicity profile against four cancer cell lines (KB, HepG2, A549, and MCF7), and noncancerous Hek-293 cell lines. Notably, treatment of SK-LU-1 cells with compounds 5a and 5b resulted in G2/M phase arrest of the cell cycle, caspase-3/7 activation, and apoptosis. Additionally, molecular docking studies were performed and showed important interaction of two compounds against residues in the colchicine-binding-site of tubulin as well. Taken together, compounds 5a and 5b were identified as potent anticancer agents.

8.
Chem Biodivers ; 19(8): e202200359, 2022 Aug.
Article En | MEDLINE | ID: mdl-35920799

A convenient three-component synthetic approach was developed en route to new and significative N-arylated-dihydrobenzo[g]quinoline-5,10-diones using 2-hydroxy-1,4-naphthoquinone, a variety of aromatic aldehydes, and 4-(arylamino)furan-2(5H)-ones. A sequence of steps including Knoevenagel condensation, Michael addition, [1,3]-hydrogen shift, intramolecular cyclization and dehydration led to the formation of products. All the products were structurally characterized by spectroscopic techniques and assessed in terms of their cytotoxicity profile against four cancer cell lines (KB, HepG2, A549, and MCF7), and human embryonic kidney (Hek-293) cell lines.


Antineoplastic Agents , Quinolines , Antineoplastic Agents/pharmacology , Cyclization , HEK293 Cells , Humans , Microwaves , Quinolines/chemistry
9.
Bull World Health Organ ; 97(2): 129-141, 2019 Feb 01.
Article En | MEDLINE | ID: mdl-30728619

By 2016, Member States of the World Health Organization (WHO) had developed and implemented national action plans on noncommunicable diseases in line with the Global action plan for the prevention and control of noncommunicable diseases (2013-2020). In 2018, we assessed the implementation status of the recommended best-buy noncommunicable diseases interventions in seven Asian countries: Bhutan, Cambodia, Indonesia, Philippines, Sri Lanka, Thailand and Viet Nam. We gathered data from a range of published reports and directly from health ministries. We included interventions that addressed the use of tobacco and alcohol, inadequate physical activity and high salt intake, as well as health-systems responses, and we identified gaps and proposed solutions. In 2018, progress was uneven across countries. Implementation gaps were largely due to inadequate funding; limited institutional capacity (despite designated noncommunicable diseases units); inadequate action across different sectors within and outside the health system; and a lack of standardized monitoring and evaluation mechanisms to inform policies. To address implementation gaps, governments need to invest more in effective interventions such as the WHO-recommended best-buy interventions, improve action across different sectors, and enhance capacity in monitoring and evaluation and in research. Learning from the Framework Convention on Tobacco Control, the WHO and international partners should develop a standardized, comprehensive monitoring tool on alcohol, salt and unhealthy food consumption, physical activity and health-systems response.


En 2016, les États membres de l'Organisation mondiale de la Santé (OMS) avaient élaboré et mis en œuvre des plans d'action nationaux sur les maladies non transmissibles conformément au Plan d'action mondial pour la lutte contre les maladies non transmissibles (2013­2020). En 2018, nous avons évalué l'état de l'application des interventions les plus avantageuses recommandées en matière de maladies non transmissibles dans sept pays asiatiques: le Bhoutan, le Cambodge, l'Indonésie, les Philippines, le Sri Lanka, la Thaïlande et le Viet Nam. Nous avons recueilli des données à partir de toute une série de rapports publiés et directement auprès des ministères de la Santé. Nous avons inclus les interventions qui concernaient la consommation de tabac et d'alcool, une activité physique inadéquate et une consommation de sel élevée, ainsi que les réponses des systèmes de santé, et nous avons identifié les lacunes et proposé des solutions. En 2018, les progrès étaient variables selon les pays. Les lacunes étaient largement dues à un financement inadéquat; des capacités institutionnelles limitées (malgré des unités dédiées aux maladies non transmissibles); une action inadéquate dans les différents secteurs au sein et en dehors du système de santé; et l'absence de mécanismes de suivi et d'évaluation standardisés pour orienter les politiques. Afin de combler ces lacunes, les gouvernements doivent investir davantage dans des interventions efficaces telles que les interventions les plus avantageuses recommandées par l'OMS, améliorer l'action dans les différents secteurs, et renforcer les capacités en matière de suivi et d'évaluation, mais aussi de recherche. En s'inspirant de la Convention-cadre pour la lutte antitabac, l'OMS et ses partenaires internationaux devraient élaborer un outil de suivi complet et standardisé sur la consommation d'alcool, de sel et d'aliments malsains, l'activité physique et la réponse des systèmes de santé.


Para 2016, los Estados miembros de la Organización Mundial de la Salud (OMS) habían elaborado y aplicado planes de acción nacionales sobre las enfermedades no contagiosas de acuerdo con el Plan de acción mundial para la prevención y el control de las enfermedades no transmisibles (2013-2020). En 2018, se evaluó el estado de implementación de las intervenciones recomendadas en siete países asiáticos en materia de enfermedades no contagiosas: Bhután, Camboya, Filipinas, Indonesia, Sri Lanka, Tailandia y Vietnam. Se recopilaron datos de una serie de informes publicados y directamente de los ministerios de salud. Se incluyeron intervenciones que abordaron el uso del tabaco y el alcohol, la actividad física inadecuada y la ingesta elevada de sal, así como las respuestas de los sistemas de salud, se identificaron las deficiencias y se propusieron soluciones. En 2018, el progreso fue desigual entre los países. Las deficiencias en la aplicación se debieron en gran medida a la falta de financiación, a la limitada capacidad institucional (a pesar de las dependencias designadas para las enfermedades no contagiosas), a la inadecuación de las medidas adoptadas en los diferentes sectores dentro y fuera del sistema de salud y a la falta de mecanismos normalizados de supervisión y evaluación que sirvieran de base a las políticas. Para subsanar las deficiencias en materia de aplicación, los gobiernos deben invertir más en intervenciones eficaces, como las recomendadas por la OMS, mejorar las medidas adoptadas en los distintos sectores y aumentar la capacidad de seguimiento y evaluación y de investigación. A partir de las enseñanzas del Convenio Marco para el Control del Tabaco, la OMS y los asociados internacionales deberían elaborar un instrumento de seguimiento normalizado y completo para el consumo de alcohol, sal y alimentos no saludables, la actividad física y la respuesta de los sistemas de salud.


Health Behavior , Health Policy , Health Promotion , Noncommunicable Diseases/prevention & control , Bhutan , Cambodia , Cooperative Behavior , Health Policy/economics , Health Promotion/economics , Health Promotion/methods , Health Promotion/organization & administration , Humans , Indonesia , Interinstitutional Relations , Philippines , Smoking/economics , Smoking Prevention , Sri Lanka , Taxes , Thailand , Tobacco Products/economics , Vietnam , World Health Organization
10.
Open Access Maced J Med Sci ; 7(2): 259-263, 2019 Jan 30.
Article En | MEDLINE | ID: mdl-30745975

BACKGROUND: Chronic urticaria, a mast cell-driven condition, is common, debilitating and hard to treat. H1-antihistamines are the first line treatment of chronic urticaria, but often patients do not get satisfactory relief with the recommended dose. European guidelines recommend increased antihistamine doses up to four-fold. AIM: We conducted this study to evaluate the efficacy of increased H1-antihistamine doses up to two-fold in Vietnamese chronic urticaria patients. METHODS: One hundred and two patients with chronic urticaria were recruited for treatment with levocetirizine (n = 52) or fexofenadine (n = 50). Treatment started at the conventional daily dose of 5 mg levocetirizine or 180 mg fexofenadine for 2 weeks and then increased to 10 mg levocetirizine or 360 mg fexofenadine for 2 weeks if patients did not have an improvement in symptoms. At week 0, week 2 and week 4 wheal, pruritus, size of the wheal, total symptom scores, and associated side-effects were assessed. RESULTS: With the conventional dose, the total symptom scores after week 2 decreased significantly in both groups compared to baseline figures, i.e. 7.4 vs 2.3 for levocetirizine group and 8.0 vs 2.6 for fexofenadine group (p < 0.05). However, there were still 26 patients in each group who did not have improvements. Of these 26 patients, after having a two-fold increase of the conventional dose, 11.5% and 38.5% became symptom-free at week 4 in levocetirizine group and fexofenadine group, respectively. At week 4 in both groups, the total symptom scores had significantly decreased when compared with those at week 2 (2.8 ± 1.5 versus 4.7 ± 1.6 in levocetirizine group; 2.1 ± 1.9 versus 5.1 ± 1.4 in fexofenadine group). In both groups, there was no difference in the rate of negative side effects between the conventional dose and the double dose. CONCLUSION: This study showed that increasing the dosages of levocetirizine and fexofenadine by two-fold improved chronic urticaria symptoms without increasing the rate of negative side effects.

12.
Bioorg Med Chem Lett ; 25(16): 3355-8, 2015 Aug 15.
Article En | MEDLINE | ID: mdl-26081288

1,4-Dihydroxy-2-naphthoic acid was used as a substrate for a straightforward five-step synthesis of 3-substituted 1H-benzo[g]isochromene-5,10-diones, with a Michael addition of N-acylmethylpyridinium ylides across 2-hydroxymethyl-1,4-naphthoquinone and a subsequent acid-mediated dehydratation of intermediate hemiacetals as the key steps. The obtained benzo[g]isochromene-5,10-diones were subsequently deployed for further synthetic elaboration to produce new 3,4-dihydrobenzo[g]isochromene-5,10-diones and (3,4-dihydro-)4a,10a-epoxybenzo[g]isochromene-5,10-diones. All compounds were screened for their cytotoxic and antimicrobial effects, revealing an interesting cytotoxic activity of 1H-benzo[g]isochromene-5,10-diones against different cancer cell lines.


Epoxy Compounds/chemical synthesis , Epoxy Compounds/pharmacology , Naphthoquinones/chemical synthesis , Naphthoquinones/pharmacology , Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Carboxylic Acids/chemical synthesis , Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , Cell Line, Tumor , Drug Screening Assays, Antitumor , Epoxy Compounds/chemistry , Humans , Inhibitory Concentration 50 , Molecular Structure , Naphthalenes/chemical synthesis , Naphthalenes/chemistry , Naphthalenes/pharmacology , Naphthoquinones/chemistry , Structure-Activity Relationship
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