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1.
J Craniofac Surg ; 33(8): e883-e886, 2022.
Article En | MEDLINE | ID: mdl-35920855

Secondary cleft rhinoplasty typically requires large amounts of cartilage grafts for augmentation. The purpose of this study was to present our short-term experience with alloplastic implants in cleft rhinoplasty. This was a retrospective cohort study of cleft lip and palate patients treated with secondary rhinoplasty at Hanoi Medical University Hospital and Ruby Hospital between 2017 and 2020. All rhinoplasty procedures consisted of lower lateral cartilage repositioning, a dorsal augmentation with silicone implant, columellar strut implant or graft, and onlay tip grafts. Cartilage was obtained from the septum and concha, and no cartilage was harvested from the rib. The study outcomes included the Rhinoplasty Outcome Evaluation (ROE) survey, a modified Mortier scoring scale, 8 intranasal measures of symmetry, and 4 nasofacial measures of tip projection and nasal length. Changes in patient satisfaction and nasal esthetics were compared before and after surgery. A total of 38 patients were included in the final study sample, of whom 65.79% had unilateral clefts. The overall complication rate was 7.89%, and there were 2 cases of infection and 1 case of dorsal implant displacement. Following rhinoplasty, ROE satisfaction scores significantly increased (+39.36, P <0.01) and Mortier severity scores decreased (-3.06, P <0.01). Nostril symmetry nearly normalized in width, height, and inclination. Mean columellar deviation decreased from 8.82 to 2.08 degrees, and nasal projection increased as assessed on multiple analyses. Patients with bilateral clefts had similar improvements in ROE and Mortier scores. In our experience, synthetic implants simplified the correction of cleft nasal deformity and eliminated the need for costal cartilage. We found that our protocol produced acceptable and stable short-term clinical results without increasing the complication rate above what has been reported with autologous grafts.


Cleft Lip , Cleft Palate , Costal Cartilage , Dental Implants , Rhinoplasty , Humans , Rhinoplasty/methods , Cleft Lip/surgery , Cleft Lip/complications , Retrospective Studies , Cleft Palate/surgery , Cleft Palate/complications , Treatment Outcome , Esthetics, Dental , Nose/surgery , Costal Cartilage/surgery , Nasal Septum/surgery
2.
Biodivers Data J ; 10: e77025, 2022.
Article En | MEDLINE | ID: mdl-35068979

VIETBIO [Innovative approaches to biodiversity discovery and characterisation in Vietnam] is a bilateral German-Vietnamese research and capacity building project focusing on the development and transfer of new methods and technology towards an integrated biodiversity discovery and monitoring system for Vietnam. Dedicated field training and testing of innovative methodologies were undertaken in Cuc Phuong National Park as part and with support of the project, which led to the new biodiversity data and records made available in this article collection. VIETBIO is a collaboration between the Museum für Naturkunde Berlin - Leibniz Institute for Evolution and Biodiversity Science (MfN), the Botanic Garden and Botanical Museum, Freie Universität Berlin (BGBM) and the Vietnam National Museum of Nature (VNMN), the Institute of Ecology and Biological Resources (IEBR), the Southern Institute of Ecology (SIE), as well as the Institute of Tropical Biology (ITB); all Vietnamese institutions belong to the Vietnam Academy of Science and Technology (VAST). The article collection "VIETBIO" (https://doi.org/10.3897/bdj.coll.63) reports original results of recent biodiversity recording and survey work undertaken in Cuc Phuong National Park, northern Vietnam, under the framework of the VIETBIO project. The collection consist of this "main" cover paper - characterising the study area, the general project approaches and activities, while also giving an extensive overview on previous studies from this area - followed by individual papers for higher taxa as studied during the project. The main purpose is to make primary biodiversity records openly available, including several new and interesting findings for this biodiversity-rich conservation area. All individual data papers with their respective primary records are expected to provide useful baselines for further taxonomic, phylogenetic, ecological and conservation-related studies on the respective taxa and, thus, will be maintained as separate datasets, including separate GUIDs also for further updating.

3.
J Biol Chem ; 297(3): 101057, 2021 09.
Article En | MEDLINE | ID: mdl-34389356

Over the last decade, the urotensinergic system, composed of one G protein-coupled receptor and two endogenous ligands, has garnered significant attention as a promising new target for the treatment of various cardiovascular diseases. Indeed, this system is associated with various biomarkers of cardiovascular dysfunctions and is involved in changes in cardiac contractility, fibrosis, and hypertrophy contributing, like the angiotensinergic system, to the pathogenesis and progression of heart failure. Significant investment has been made toward the development of clinically relevant UT ligands for therapeutic intervention, but with little or no success to date. This system therefore remains to be therapeutically exploited. Pepducins and other lipidated peptides have been used as both mechanistic probes and potential therapeutics; therefore, pepducins derived from the human urotensin II receptor might represent unique tools to generate signaling bias and study hUT signaling networks. Two hUT-derived pepducins, derived from the second and the third intracellular loop of the receptor (hUT-Pep2 and [Trp1, Leu2]hUT-Pep3, respectively), were synthesized and pharmacologically characterized. Our results demonstrated that hUT-Pep2 and [Trp1, Leu2]hUT-Pep3 acted as biased ago-allosteric modulators, triggered ERK1/2 phosphorylation and, to a lesser extent, IP1 production, and stimulated cell proliferation yet were devoid of contractile activity. Interestingly, both hUT-derived pepducins were able to modulate human urotensin II (hUII)- and urotensin II-related peptide (URP)-mediated contraction albeit to different extents. These new derivatives represent unique tools to reveal the intricacies of hUT signaling and also a novel avenue for the design of allosteric ligands selectively targeting hUT signaling potentially.


Intracellular Signaling Peptides and Proteins/metabolism , Peptide Hormones/metabolism , Peptides/metabolism , Receptors, G-Protein-Coupled/chemistry , Receptors, G-Protein-Coupled/metabolism , Allosteric Regulation , Cell Proliferation , HEK293 Cells , Humans , Intracellular Signaling Peptides and Proteins/chemistry , Intracellular Signaling Peptides and Proteins/genetics , Ligands , Peptide Hormones/chemistry , Peptide Hormones/genetics , Peptides/chemistry , Protein Conformation, alpha-Helical , Receptors, G-Protein-Coupled/genetics , Signal Transduction
4.
BMJ Open Qual ; 10(3)2021 07.
Article En | MEDLINE | ID: mdl-34301731

BACKGROUND: To improve maternal and neonatal outcomes, Vietnam implemented early essential newborn care (EENC) using clinical coaching and quality improvement self-assessments in hospitals to introduce policy, practice and environmental changes. Da Nang Hospital for Women and Children began EENC with caesarean section births to inform development of national guidelines. This study compared newborn outcomes after caesarean sections pre/post-EENC introduction. METHODS: Maternity records of all live in-born hospital caesarean births and separate case records of the subpopulation admitted to the neonatal intensive care unit (NICU) were reviewed pre-EENC (November 2013-October 2014) and post-EENC (November 2014-October 2015) implementation. NICU admissions and adverse outcomes on NICU admission were compared using descriptive statistics. FINDINGS: A total of 16 927 newborns were delivered by caesarean section: 7928 (46.8%) pre-EENC and 8999 post-EENC (53.2%). Total NICU admissions decreased from 16.7% to 11.8% (relative risk 0.71; 95% CI 0.66 to 0.76) after introduction of EENC. Compared with the pre-EENC period, babies with hypothermia on admission to the NICU declined from 5.0% to 3.7% (relative risk 0.73; 95% CI 0.63 to 0.84) and cases of sepsis from 3.2% to 0.8% (relative risk 0.26; 95% CI 0.20 to 0.33) post-EENC implementation. While more than half of all newborns in the NICU were fed something other than breastmilk pre-EENC introduction, 85.8% were exclusively breast fed post-EENC (relative risk 1.86; 95% CI 1.75 to 1.98). Preterm newborns <2000 g receiving kangaroo mother care (KMC) increased from 50% to 67% (relative risk 1.33; 95% CI 1.12 to 1.59). CONCLUSION: The EENC quality improvement approach with caesarean section births was associated with reduced NICU admissions, admissions with hypothermia and sepsis, and increased rates of exclusive breast feeding and KMC in the NICU.


Cesarean Section , Kangaroo-Mother Care Method , Child , Female , Humans , Infant , Infant, Newborn , Intensive Care Units, Neonatal , Pregnancy , Tertiary Care Centers , Vietnam/epidemiology
5.
Case Rep Ophthalmol ; 12(2): 476-480, 2021.
Article En | MEDLINE | ID: mdl-34177544

A 66-years-old Vietnamese healthy female patient presented with prolonged severe right ocular pain and complete vision loss in that eye. Anterior segment assessment including gonioscopy identified angle-closure configuration. A suspected ciliary body melanoma was seen through the pupil. Posterior segment examination revealed a large tumor mass and 360° retinal detachment (kissing configuration). An ultrasound examination was consistent with a uveal tumor. The painful, blind right eye with a tumor mass was enucleated. Histopathology confirmed a type A uveal spindle cell melanoma associated with total serous retinal detachment without evidence of tumor necrosis, epithelioid cells, scleral, or optic nerve infiltration. There was no evidence of metastasis after 1-year of follow-up. It is critically important to differentiate primary and secondary angle closure, especially in cases with life-threatening ocular malignancy as uveal melanoma.

6.
J Craniofac Surg ; 32(2): e153-e156, 2021.
Article En | MEDLINE | ID: mdl-33705057

ABSTRACT: The purpose of this study was to compare the outcomes between the conventional surgical approach (CSA) and the surgery-first approach (SFA) for both traditional orthognathic osteotomies (LeFort/BSSO) and anterior segmental osteotomies (ASO). This was a retrospective cohort study of patients treated at the Hanoi Plastic Surgery Center from January 2000 to December 2012. The study predictors were the type (LeFort/BSSO or ASO) and timing (CSA or SFA) of surgery. The study outcomes were total treatment time and the rates of complication and relapse. 146 patients were included in the study, of whom 99 (67.8%) were treated with traditional osteotomies and 47 (32.2%) were treated with ASO. In the traditional osteotomy group, there were no significant differences in complication (P = 0.84) or relapse (P = 0.77) rates between CSA and SFA. There were no complications or relapses in the ASO group. Total treatment time was significantly decreased when using the SFA for both orthognathic osteotomies (-3.9 months, P < 0.01) and ASO (-3.3 months, P < 0.01). Our results showed that the SFA was able to achieve similar clinical outcomes to CSA but in a shorter treatment time. The SFA was effective for not only traditional orthognathic osteotomies but also ASO.


Orthognathic Surgery , Orthognathic Surgical Procedures , Surgery, Plastic , Humans , Retrospective Studies
7.
J Craniofac Surg ; 32(5): e477-e479, 2021.
Article En | MEDLINE | ID: mdl-33481470

ABSTRACT: Mandibular condyle osteochondromas cause morphologic and functional disturbances. Multiple options exist for reconstructing the condylar segment following complete condylectomy. In this series, we describe 3 cases of mandibular condyle osteochondroma treated with complete condylectomy, orthognathic surgery, and a novel free ramus osteotomy graft. This is the first report to reconstruct the temporomandibular joint using a free ramus graft. Through this single-staged approach we were able to avoid recurrence, preserve function, and restore facial balance without a separate donor site or an alloplastic implant.


Mandibular Neoplasms , Osteochondroma , Temporomandibular Joint Disorders , Facial Asymmetry/diagnostic imaging , Facial Asymmetry/surgery , Humans , Mandibular Condyle/diagnostic imaging , Mandibular Condyle/surgery , Mandibular Neoplasms/diagnostic imaging , Mandibular Neoplasms/surgery , Neoplasm Recurrence, Local , Osteochondroma/diagnostic imaging , Osteochondroma/surgery , Osteotomy, Sagittal Split Ramus , Temporomandibular Joint Disorders/diagnostic imaging , Temporomandibular Joint Disorders/surgery
8.
Int J Drug Policy ; 87: 102990, 2021 01.
Article En | MEDLINE | ID: mdl-33099159

In 2009, Vietnam officially decriminalised drug use through amendments to the criminal law. The amendments outlined explicitly that illicit drug use would be seen as an administrative violation, but not a criminal offence. This legal transition has not been without implementation challenges, and police particularly have struggled to find a balance between drug law enforcement and decriminalisation. Despite being a health-orientated drug policy amendment, in practice it allows police to send suspected drug users to compulsory treatment centres without judicial oversight and people who use drugs continue to face challenges in their interface with law enforcement which can negatively impact access to harm reduction and community-based treatment programs. Using policy desk research combined with indepth interviews with 14 key informants from people representing a range of relevant Vietnamese government (n = 10) and non-government agencies (n = 4), this paper explores some insights and considerations into how decriminalisation of drug use in the amended law was implemented. We explore key informant perspectives into how the decriminalisation amendment could be implemented more effectively in order to improve health outcomes for people who use drugs in Vietnam through re-envisioned police protocols and practices. Findings show that while decriminalising drug use in Vietnam was designed as a progressive and health-orientated drug policy, the ongoing disconnect between the health intent of the policy and the police-led oversight of its implementation in the community persists. Part of this disconnect is explained by the lack of training and clear protocols that would enhance the police in their ability to contribute to the health intent of the policy rather than continue to view drug use through a drug law enforcement only lens. The paper calls for further collaboration across policing and the health and community-based organisations delivering services for people who use drugs. We suggest that through developing a deeper understanding of the interplay between policing and the implementation of harm reduction policy and programs, decriminalisation can co-exist within a broader and deeply entrenched drug control strategy in Vietnam.


Law Enforcement , Pharmaceutical Preparations , Government , Humans , Police , Public Policy , Vietnam
9.
Sci Rep ; 10(1): 21026, 2020 12 03.
Article En | MEDLINE | ID: mdl-33273556

Iron homeostasis is an essential biological process that ensures the tissue distribution of iron for various cellular processes. As the major producer of hepcidin, the liver is central to the regulation of iron metabolism. The liver is also home to many immune cells, which upon activation may greatly impact iron metabolism. Here, we focus on the role of invariant natural killer T (iNKT) cells, a subset of T lymphocytes that, in mice, is most abundant in the liver. Activation of iNKT cells with the prototypical glycosphingolipid antigen, α-galactosylceramide, resulted in immune cell proliferation and biphasic changes in iron metabolism. This involved an early phase characterized by hypoferremia, hepcidin induction and ferroportin suppression, and a second phase associated with strong suppression of hepcidin despite elevated levels of circulating and tissue iron. We further show that these changes in iron metabolism are fully dependent on iNKT cell activation. Finally, we demonstrate that the biphasic regulation of hepcidin is independent of NK and Kupffer cells, and is initially driven by the STAT3 inflammatory pathway, whereas the second phase is regulated by repression of the BMP/SMAD signaling pathway. These findings indicate that iNKT activation and the resulting cell proliferation influence iron homeostasis.


Homeostasis , Iron/metabolism , Killer Cells, Natural/immunology , Lymphocyte Activation , Animals , Cation Transport Proteins/genetics , Cation Transport Proteins/metabolism , Cell Proliferation , Galactosylceramides/immunology , Hepcidins/genetics , Hepcidins/metabolism , Liver/cytology , Liver/metabolism , Mice , Mice, Inbred C57BL
10.
Zootaxa ; 4683(2): zootaxa.4683.2.1, 2019 Oct 08.
Article En | MEDLINE | ID: mdl-31715924

For the goatfish genus Upeneus Cuvier 1829 (Mullidae), a new taxonomic species group called the "margarethae group" is established which can be distinguished from the six species of the most similar "tragula group" by a combination of the following characteristics: absence of dark pigmentation in the area of the first dorsal-fin tip, 21-25 total gill rakers and 28-30 lateral-line scales. Initially, three recently-described species have been included in the margarethae group: Upeneus margarethae Uiblein Heemstra, 2010, known from the Indian Ocean including the Red Sea and from the Arafura Sea (W Pacific), U. mouthami Randall Kulbicki, 2006, from New Caledonia and Vanuatu (W Pacific), and U. randalli Uiblein Heemstra, 2011, from the Arabian/Persian Gulf and the inner Gulf of Oman (NW Indian Ocean). The present taxonomic review of the margarethae group analyses a large data set of 41 morphometric, 10 meristic and many colour characters obtained from 279 preserved goatfish specimens and 166 fresh-colour photos (plus a fresh-colour drawing). For the nominal species of the group, U. margarethae, a redescription of the colour patterns is provided and new records for Myanmar, Andaman Sea (NE Indian Ocean) and the Gulf of Carpentaria, N Australia (W Pacific), are reported. Three new species are described: U. caudofasciatus n. sp. from the area of the Great Barrier Reef to Torres Strait off NE Australia (Coral Sea, W Pacific), U. gubal n. sp. from the S Gulf of Suez (Northern Red Sea), and U. heterospinus n. sp. from S Indonesia to Singapore, the Gulf of Thailand, Vietnam, Philippines, China, Taiwan and Japan (W Pacific). A comprehensive alpha-taxonomic approach is adopted, considering population differences as well as intraspecific size-related variation in morphology and colour patterns by splitting the data set into two size classes, adults (≥ 65 mm SL) and smaller subadults. Inter- and intraspecific comparisons include statistical analyses for species and population with sufficiently large samples sizes (n ≥ 20). Colour-pattern characterization and analysis are based on photos of recently collected and deceased fish (partly associated with voucher specimens), photos obtained from active or resting fishes in situ or in a tank, and inspection of pigmentation patterns retained in preserved specimens. Species differences are elaborated under consideration of distribution patterns and the characteristics found in the closest-most population of widely distributed species such as U. margarethae, resulting in clear and consistent distinction among the six species in single or in a combination of several characteristics. Comparisons among size classes revealed species-specific patterns in morphometric, meristic and colour changes with increasing size. One species, U. heterospinus n. sp., has seven or eight spines in the dorsal fin which occur in balanced ratio across populations. This is a unique characteristic for Upeneus species which usually have either seven or eight dorsal-fin spines, respectively. The best distinction of Upeneus heterospinus n. sp. from all other congeners is reached by combined examination of dorsal-fin spines with several other characters such as barbel colour, presence of a mid-lateral body stripe, pigmentation patterns (partly retained also in preserved fish), gill-raker and pectoral-fin ray numbers, and body-shape variables. The high degree of overall morphological differentation among the three most common species U. caudofasciatus n. sp., U. heterospinus n. sp. and U. margarethae, as revealed by the statistical comparisons, strongly contrasts with a still signficant, but much lower degree of differentiation among populations. The diagnostic characteristics of the margarethae group are updated and the importance to use the results of this taxonomic review in ongoing fisheries-related and ecological research is emphasized. Requirements for future taxonomic research featuring the stunning diversity of the goatfish genus Upeneus are also discussed.


Perciformes , Animal Distribution , Animals , Australia , Color , Indonesia , Pacific Ocean
11.
Zootaxa ; 4344(3): 541-559, 2017 Nov 08.
Article En | MEDLINE | ID: mdl-29245624

For Jansen's goatfish, Parupeneus jansenii (Mullidae), taxonomic knowledge has been rather poor and occurrence information restricted to a few localities only, with verified records from northern Sulawesi and Sunda Street (Indonesia), and Luzon (Philippines). This species is here included in the so-called "heptacanthus" group together with the Indo-Pacific cinnabar goatfish, P. heptacanthus, and five Indian Ocean congenerics, based on an evenly, symmetrically rounded posterior maxilla margin and similarities in meristic characters and preserved colour. In total 29 P. jansenii and 53 P. heptacanthus consisting of types, recently collected material from south-central Vietnam, southern Indonesia, and NE Australia, and geographically related reference material were studied along with single types of the other five heptacanthus-group species and P. angulatus, a morphologically similar Western Indian Ocean species. In total 62 quantitative meristic and morphometric characters including standard length (SL) were analysed after splitting the data into two size classes (small-sized fish, < 110 mm SL, vs. large-sized fish  > 110 mm SL) to account for size-related differences due to allometry. Diagnoses for P. jansenii and P. heptacanthus and a redescription for P. jansenii were prepared. Fresh-fish colour descriptions for both large- and small-sized voucher specimens of P. jansenii are provided and the effects of freshness status on colour patterns is documented. New records for P. jansenii for Vietnam, southern Indonesia and NE Australia (= first verified record for Australia) are reported and depth information (24-100 m depth range) is given for the first time. P. jansenii differs from the co-occurring P. heptacanthus - independently of size - in shallower body and caudal peduncle, smaller maximum head depth, shorter barbels, caudal and pelvic fins, shallower first dorsal fin, shallower first ray of second dorsal fin, and lack of small dark red or reddish-brown spot on or just below the eighth lateral-line scale. The populations of P. jansenii from Vietnam and Australia differ from each other in a single character, the height of the eighth dorsal-fin ray, but both overlap with the intermediate population from Indonesia. This comprehensive alpha-taxonomic approach provides a useful tool for uncovering the diversity of Parupeneus goatfishes.


Fishes , Animal Distribution , Animals , Australia , Indian Ocean , Indonesia , Pacific Ocean , Philippines , Vietnam
12.
ACS Appl Mater Interfaces ; 8(23): 14824-35, 2016 Jun 15.
Article En | MEDLINE | ID: mdl-27203860

The use of MgO nanoparticles in polyethylene for cable insulation has attracted considerable interest, although in humid media the surface regions of the nanoparticles undergo a conversion to a hydroxide phase. A facile method to obtain MgO nanoparticles with a large surface area and remarkable inertness to humidity is presented. The method involves (a) low temperature (400 °C) thermal decomposition of Mg(OH)2, (b) a silicone oxide coating to conceal the nanoparticles and prevent interparticle sintering upon exposure to high temperatures, and (c) heat treatment at 1000 °C. The formation of the hydroxide phase on these silicone oxide-coated MgO nanoparticles after extended exposure to humid air was assessed by thermogravimetry, infrared spectroscopy, and X-ray diffraction. The nanoparticles showed essentially no sign of any hydroxide phase compared to particles prepared by the conventional single-step thermal decomposition of Mg(OH)2. The moisture-resistant MgO nanoparticles showed improved dispersion and interfacial adhesion in the LDPE matrix with smaller nanosized particle clusters compared with conventionally prepared MgO. The addition of 1 wt % moisture-resistant MgO nanoparticles was sufficient to decrease the conductivity of polyethylene 30 times. The reduction in conductivity is discussed in terms of defect concentration on the surface of the moisture-resistant MgO nanoparticles at the polymer/nanoparticle interface.

13.
PLoS One ; 9(1): e87272, 2014.
Article En | MEDLINE | ID: mdl-24489886

Illicit trade carries the potential to magnify existing tobacco-related health care costs through increased availability of untaxed and inexpensive cigarettes. What is known with respect to the magnitude of illicit trade for Vietnam is produced primarily by the industry, and methodologies are typically opaque. Independent assessment of the illicit cigarette trade in Vietnam is vital to tobacco control policy. This paper measures the magnitude of illicit cigarette trade for Vietnam between 1998 and 2010 using two methods, discrepancies between legitimate domestic cigarette sales and domestic tobacco consumption estimated from surveys, and trade discrepancies as recorded by Vietnam and trade partners. The results indicate that Vietnam likely experienced net smuggling in during the period studied. With the inclusion of adjustments for survey respondent under-reporting, inward illicit trade likely occurred in three of the four years for which surveys were available. Discrepancies in trade records indicate that the value of smuggled cigarettes into Vietnam ranges from $100 million to $300 million between 2000 and 2010 and that these cigarettes primarily originate in Singapore, Hong Kong, Macao, Malaysia, and Australia. Notable differences in trends over time exist between the two methods, but by comparison, the industry estimates consistently place the magnitude of illicit trade at the upper bounds of what this study shows. The unavailability of annual, survey-based estimates of consumption may obscure the true, annual trend over time. Second, as surveys changed over time, estimates relying on them may be inconsistent with one another. Finally, these two methods measure different components of illicit trade, specifically consumption of illicit cigarettes regardless of origin and smuggling of cigarettes into a particular market. However, absent a gold standard, comparisons of different approaches to illicit trade measurement serve efforts to refine and improve measurement approaches and estimates.


Commerce/economics , Crime/statistics & numerical data , Taxes , Tobacco Products/economics , Crime/economics , Empirical Research , Humans , Smoking/epidemiology , Tobacco Industry/economics , Vietnam
14.
Bioorg Med Chem Lett ; 20(9): 2991-3, 2010 May 01.
Article En | MEDLINE | ID: mdl-20359890

In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC(50) value of 2.7 microM in inhibition of melanogenesis. The structure for potent inhibitory activity of these derivatives are required with the direct connection of pi-planar structure to thiourea without steric hinderance in PTU derivatives and the hydrophobic substituent at para position in case of semicarbazones.


Benzaldehydes/chemistry , Melanoma, Experimental/drug therapy , Peptides/chemistry , Phenylthiourea/chemistry , Thiosemicarbazones/chemistry , Animals , Mice , Monophenol Monooxygenase/antagonists & inhibitors , Monophenol Monooxygenase/metabolism , Peptides/chemical synthesis , Peptides/therapeutic use , Phenylthiourea/chemical synthesis , Phenylthiourea/therapeutic use , Structure-Activity Relationship , Thiosemicarbazones/chemical synthesis , Thiosemicarbazones/therapeutic use
15.
Eur J Med Chem ; 45(6): 2531-6, 2010 Jun.
Article En | MEDLINE | ID: mdl-20226573

A novel series of chromone analogs were synthesized and evaluated for their inhibitory activity against interleukin-5. Among them compounds 5-Cyclohexylmethoxy-3-(4-hydroxybenzyl)-4H-chromen-4-one (6a, 98% inhibition at 30 microM, IC50<3.0 microM) and 5-Cyclohyxylmethoxy-3-(hydroxymethyl)-4H-chromen-4-one (8a, 84% inhibition at 30 microM, IC50=7.6 microM) showed most potent activity. The structural requirement of chromone analogs possessing the inhibitory activity against IL-5 could be summarized as: (i) importance of hydrophobic group such as cyclohexylmethoxy at 5th position of ring A, (ii) requirement of ring B with small size of hydrogen bonding group with electron donating property such as phenolic hydroxyl group at 4th position and (iii) planarity of the chromen-4-one ring.


Chromones/chemical synthesis , Chromones/pharmacology , Interleukin-5/antagonists & inhibitors , Cell Line , Chromones/chemistry , Chromones/metabolism , Hydrophobic and Hydrophilic Interactions , Inhibitory Concentration 50 , Permeability , Structure-Activity Relationship
16.
Arch Pharm Res ; 29(9): 721-7, 2006 Sep.
Article En | MEDLINE | ID: mdl-17024843

To continue exploration of structure activity relationship of novel 1-(indoline-5-sulfonyl)-4-phenylimidazolidinones (1) reported as anticancer agent with broad spectrum, three 1-(arylsulfonyl)-4-vinylimidazolidinones (2) were synthesized from methyl serinate (3) in 8 steps. Reaction of intermediate 2-phenoxycarbonylaminobut-3-enyl p-toluenesulfonate (10) with arylsulfonamide in the presence of potassium carbonate produced corresponding 2 and N-(4-vinyloxazolidin-2-yl)arylsulfonamide 11 in approximately equal ratio. This reaction is believed to undergo through urea intermediate 16 as shown in scheme 3. 1-Arylsufonyl-4-vinylimidazolidinones 2 show much reduced activity against human colon carcinoma (Colo205), human chronic myelogenous leukemia (K562), and human ovarian adenocarcinoma (SK-OV-3) and compatible activity against human lung carcinoma (A549) compared to 1. Therefore phenyl at 4-position should be the optimum planar motif for the activity of 1.


Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Hydantoins/chemical synthesis , Hydantoins/pharmacology , Vinyl Compounds/chemical synthesis , Vinyl Compounds/pharmacology , Drug Screening Assays, Antitumor , Humans , Spectrophotometry, Ultraviolet , Structure-Activity Relationship , Tetrazolium Salts , Thiazoles
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