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Article in English | WPRIM | ID: wpr-929051


Polyetheretherketone (PEEK) has been widely applied in orthopedics because of its excellent mechanical properties, radiolucency, and biocompatibility. However, the bioinertness and poor osteointegration of PEEK have greatly limited its further application. Growing evidence proves that physical factors of implants, including their architecture, surface morphology, stiffness, and mechanical stimulation, matter as much as the composition of their surface chemistry. This review focuses on the multiple strategies for the physical modification of PEEK implants through adjusting their architecture, surface morphology, and stiffness. Many research findings show that transforming the architecture and incorporating reinforcing fillers into PEEK can affect both its mechanical strength and cellular responses. Modified PEEK surfaces at the macro scale and micro/nano scale have positive effects on cell-substrate interactions. More investigations are necessary to reach consensus on the optimal design of PEEK implants and to explore the efficiency of various functional implant surfaces. Soft-tissue integration has been ignored, though evidence shows that physical modifications also improve the adhesion of soft tissue. In the future, ideal PEEK implants should have a desirable topological structure with better surface hydrophilicity and optimum surface chemistry.

Benzophenones , Ketones/chemistry , Polyethylene Glycols/chemistry , Polymers/chemistry , Surface Properties
Article in Chinese | WPRIM | ID: wpr-888109


This study explored the chemical constituents of the aerial part of Hypericum curvisepalum. Sixteen compounds were isolated from the 95% ethanol extract of H. curvisepalum with various chromatographic techniques, including a new prenylated phenyl polyketide, mysorenone D(1). Other compounds were mysorenone-A(2), mysorenone-C(3), mysorenone-B(4), peplidiforone A(5), 4-methoxy-3-(2-methylbut-3-en-2-yl)-6-phenyl-2H-pyran-2-one(6), hyperenone-A(7), 4-(3,3-dimethylallyl)oxy-6-phenyl-α-pyrone(8), peplidiforone B(9), elegaphenone(10), hypercohin A(11), hyperisampsin G(12), spathulenol(13), quercetin(14), β-sitosterol(15), and β-amyrin(16).

Benzophenones , Hypericum , Quercetin
Rev Rene (Online) ; 22: e59963, 2021. graf
Article in Portuguese | LILACS, BDENF | ID: biblio-1149524


RESUMO Objetivo identificar as atividades farmacológicas da manteiga de bacuri (Platonia insignis Mart.). Métodos revisão integrativa, realizada nas bases de dados Literatura Latino-americana e do Caribe em Ciências da Saúde, Cumulative Index to Nursing and Allied Health Literature, EMBASE, MEDLINE/PubMed, Web of Science, Cochrane Library e SCOPUS, sem delimitação temporal e de idioma. A seleção se constituiu de 13 ensaios pré-clínicos. A avaliação das informações ocorreu de forma descritiva, confrontando com os achados pertinentes. Resultados observou-se que 50,0% das publicações foram indexadas na MEDLINE/PubMed, maioria das publicações ocorreram na Inglaterra (61,5%), seguidas do Brasil e dos Estados Unidos, ambos com 13,3%. Destaca-se que 100,0% dos artigos foram ensaios pré-clínicos; atividades farmacológicas para antioxidante (38,4%) e antileishmanicidas (30,7%). Registrou-se que 38,4% dos ensaios apresentaram testes de toxicidade. Conclusão a manteiga de bacuri (Platonia insignis Mart.) apresentou atividades farmacológicas em ensaios pré-clínicos, como antioxidantes, antileshimaniose, anticonvulsivante e cicatrização de feridas.

ABSTRACT Objective to identify the pharmacological activities of bacuri butter (Platonia insignis Mart.). Methods an integrative review, carried out in the databases of Latin American and Caribbean Literature in Health Sciences, Cumulative Index to Nursing and Allied Health Literature, EMBASE, MEDLINE/PubMed, Web of Science, Cochrane Library and SCOPUS, without the time and language restriction. The selection consisted of 13 pre-clinical trials. The information assessment descriptively took place, comparing with the pertinent findings. Results it was observed that 50.0% of the publications were indexed in MEDLINE/PubMed, most publications were from England (61.5%), followed by Brazil and the United States, both with 13.3%. It is noteworthy that 100.0% of the articles were pre-clinical trials; pharmacological activities for antioxidants (38.4%) and antileishmanicides (30.7%). It was found that 38.4% of the trials presented toxicity tests. Conclusion bacuri butter (Platonia insignis Mart.) Showed pharmacological activities in pre-clinical trials, such as antioxidants, antileshimaniasis, anticonvulsant and wound healing.

Benzophenones , Clusiaceae , Drug Compounding , Drug Synergism , Drug Therapy
Article in Chinese | WPRIM | ID: wpr-942249


OBJECTIVE@#To develop dexamethasone plus minocycline-loaded liposomes (Dex/Mino liposomes) and apply them to improve bioinert polyetheretherketone (PEEK) surface, which could prevent post-operative bacterial contamination, enhance ossification for physiologic osseointegration, and finally reduce implant failure rates.@*METHODS@#Dex/Mino liposomes were covalently grafted onto the PEEK surface using polydopamine (pDA) coating as a medium. Confocal laser scanning microscopy was used to confirm the binding of fluorescently labeled liposomes onto the PEEK substrate, and a microplate reader was used to semiquantitatively measure the average fluorescence intensity of fluorescently labeled liposome-decorated PEEK surfaces. Moreover, the mouse subcutaneous infection model and the beagle femur implantation model were respectively conducted to verify the bioactivity of Dex/Mino liposome-modified PEEK in vivo, by means of micro computed tomography (micro-CT) and hematoxylin and eosin (HE) staining analysis.@*RESULTS@#The qualitative and quantitative results of fluorescently labeled liposomes showed that, the red fluorescence intensity of the PEEK-pDA-lipo group was stronger than that of the PEEK-NF-lipo group (P < 0.05); the liposomes were successfully and uniformly decorated on the PEEK surfaces due to the pDA coating. After mouse subcutaneous implantation of PEEKs for 24 hours, HE staining results showed that the number of inflammatory cells in the PEEK-Dex/Mino lipo group were lower than that in the inert PEEK group (P < 0.05), indicating a lower degree of infection in the test group. These results suggested that the Mino released from the liposome-functionalized surface provided an effective bacteriostasis in vivo. After beagle femoral implantation of PEEK for 8 weeks, micro-CT results showed that the PEEK-Dex/Mino lipo group newly formed more continuous bone when compared with the inert PEEK group; HE staining results showed that more new bones were formed in the PEEK-Dex/Mino lipo group than in the inert PEEK group, which were firmly bonded to the functionalized PEEK surface and extended along the PEEK interface. These results suggested that the Dex released from the liposome-functionalized surface induced effective bone regeneration in vivo.@*CONCLUSION@#Dex/Mino liposome modification enhanced the bioactivity of inert PEEK, the functionalized PEEK with enhanced antibacterial and osseointegrative capacity has great potential as an orthopedic/dental implant material for clinical application.

Animals , Benzophenones , Dogs , Ketones , Liposomes , Mice , Osseointegration , Polyethylene Glycols , Polymers , Surface Properties , X-Ray Microtomography
Arq. bras. oftalmol ; 83(1): 55-61, Jan.-Feb. 2020. tab, graf
Article in English | LILACS | ID: biblio-1088946


ABSTRACT Purpose: To evaluate the rate of cystoid macular edema development among cataract surgery patients on four different therapeutic regimens. Methods: The present study is a retrospective analysis of 5,380 eyes following uncomplicated phacoemulsification at Wake Forest University. The study period went from July 2007 to December 2012. Patients received one of four regimens, as follows: postoperative generic ketorolac 0.4% and prednisolone 1%, postoperative name-brand ketorolac 0.45% and prednisolone 1%, postoperative bromfenac 0.09% and prednisolone 1%, preoperative and postoperative bromfenac 0.09% alone. A statistical analysis was performed to assess the differences in rate of cystoid macular edema development among the four different therapeutic regimens. The diagnosis of cystoid macular edema required worsening of vision and evidence of increased macular thickness on optical coherence tomography. Results: The overall rate of cystoid macular edema was 0.82%. Treatment by postoperative generic ketorolac 0.45% and prednisolone 1% demonstrated the highest rate of cystoid macular edema development (2.20% of the cases). Postoperative name-brand ketorolac 0.45% and prednisolone 1% exhibited intermediate rates of cystoid macular edema development (0.90% of the cases). Postoperative administration of bromfenac 0.09% and prednisolone 1% exhibited intermediate rates of cystoid macular edema development (0.44% of the cases). Preoperative and postoperative bromfenac 0.09% alone resulted in the lowest rate of cystoid macular edema development (0.09% of the cases). The rate of cystoid macular edema was significantly lower when bromfenac was used alone vs. either regimen where ketorolac and prednisolone were used (OR 0.043, 95% CI 0.002 to 0.312; p<0.001). Conclusions: Post-cataract surgery cystoid macular edema developed less frequently following topical non-steroidal anti-inflammatory drugs regimen compared to the other therapies evaluated. Bromfenac, without corticosteroids, achieved lower rates of cystoid macular edema vs. various combinations of non-ste­roidal anti-inflammatory drugs with corticosteroids.

RESUMO Objetivo: Avaliar a taxa de desenvolvimento do edema macular cistóide em pacientes submetidos à cirurgia de catarata em quatro esquemas terapêuticos diferentes. Métodos: O presente estudo é uma análise retrospectiva de 5.380 olhos após facoemulsificação não complicada na Wake Forest University. O período do estudo foi entre julho de 2007 e dezembro de 2012. Os pacientes receberam um dos quatro esquemas: cetorolaco genérico pós-operatório 0,4% e prednisolona 1%, cetorolaco 0,45% pós-operatório e prednisolona 1%, bromfenac 0,09% e a prednisolona 1% pós-operatório, bromfenaco 0,09% no pré-operatório e isoladamente no pós-operatório. Uma análise estatística foi realizada para avaliar as diferenças na taxa de desenvolvimento do edema macular cistóide entre os quatro diferentes regimes terapêuticos. O diagnóstico de edema macular cistóide exigiu uma piora da visão e uma evidência de aumento da espessura macular na tomografia de coerência óptica. Resultados: A taxa global de edema macular cistóide foi de 0,82%. O tratamento com cetorolaco genérico pós-operatório 0,45% e prednisolona 1% demonstrou a maior taxa de desenvolvimento de edema macular cistóide (2,20% dos casos). O cetorolaco 0,45% e a prednisolona 1% no pós-operatório exibiram taxas intermediárias de desenvolvimento de edema macular cistóide (0,90% dos casos). A administração de bromofenac 0,09% e de prednisolona 1% no pós-operatório apresentou taxas interme­diárias de desenvolvimento de edema macular cistóide (0,44% dos casos). O bromfenac 0,09% no pré e pós-operatório isoladamente resultou na menor taxa de desenvolvimento de edema macular cistóide (0,09% dos casos). A taxa de edema macular cistóide foi significativamente menor quando o bromfenac foi utilizado isoladamente em relação ao esquema onde cetorolaco e a prednisolona foram usados (OR 0,043, 95% CI 0,002 a 0,312; p<0,001). Conclusões: O edema macular cistóide pós-cirurgia de catarata desenvolveu-se com menor frequência após o tratamento tópico de medicamentos anti-inflamatórios não esteroidais, comparado às outras terapias avaliadas. Bromfenac, sem corticosteróides, alcançou taxas mais baixas de edema macular cistóide vs. Várias combinações em comparação com as várias combinações de drogas anti-inflamatórias não esteroidais com corticosteróides.

Humans , Male , Female , Aged , Aged, 80 and over , Benzophenones/therapeutic use , Bromobenzenes/therapeutic use , Prednisolone/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Macular Edema/prevention & control , Phacoemulsification/adverse effects , Cataract , Macular Edema/etiology , Retrospective Studies , Drug Therapy, Combination
Bol. latinoam. Caribe plantas med. aromát ; 18(3): 336-346, mayo 2019. tab, ilus
Article in English | LILACS | ID: biblio-1008047


The chemical composition of Mangifera indica L. cv. "Kent" leaves was determined by HPLC-ESI-QTOF-MS/MS. Polyphenolic compounds characterized as benzophenone derivatives were the main components found in extracts (1, maclurin 3-C-(2-O-galloyl)-D- glucoside isomer; 2, maclurin 3-C---D-glucoside; 3, iriflophenone 3-C---D-glucoside; 5, maclurin 3-C-(2,3-di-O-galloyl)---D-glucoside; 6, iriflophenone 3-C-(2-O-galloyl)---D-glucoside; 7, methyl-iriflophenone 3-C-(2,6-di-O-galloyl)---D-glucoside) and xanthones (4, mangiferin and 8, 6-O-galloyl-mangiferin). The estrogenic and antioxidant effects of aqueous extracts from Mangifera indica L. cv. "Kent" leaves on ovariectomized rats were determined by uterotrophic assay and malondialdehyde (MDA) levels in erythrocytes, bone, liver, and stomach. We conclude that the polyphenolic compounds from extracts act as exogenous antioxidant agents against oxidative damage in ovariectomized rats.

La composición química de las hojas de Mangifera indica L. cv. "Kent" se determinó por HPLC-ESI-QTOF-MS/MS. Compuestos polifenólicos caracterizados como derivados de benzofenona fueron los componentes principales encontrados en los extractos (1, isómero de la maclurina 3-C-(2-O-galoyil)-D-glucósido; 2, maclurina 3-C-ß-D-glucósido; 3, iriflofenona 3-C-ß-D-glucósido; 5, maclurina 3-C-(2,3-di-O-galloíl)-ß-D-glucósido; 6, iriflofenona 3-C-(2-O-galloil)-ß-D-glucósido; 7, metil-iriflofenona 3-C-(2,6-di-O- galloyl)-ß-D-glucósido) y xantonas (4, mangiferina y 8, 6-O-galoyil-mangiferina). Los efectos estrogénicos y antioxidantes de los extractos acuosos de hojas de Mangifera indica L. cv. "Kent" en ratas ovariectomizadas se determinaron mediante ensayo uterotrófico y la medición de los niveles de malondialdehído (MDA) en eritrocitos, huesos, hígado y estómago. Concluimos que los compuestos polifenólicos de los extractos actúan como agentes antioxidantes exógenos contra el daño oxidativo en ratas ovariectomizadas.

Animals , Female , Rats , Plant Extracts/pharmacology , Plant Extracts/chemistry , Ovariectomy , Mangifera/chemistry , Estrogens/pharmacology , Antioxidants/pharmacology , Stomach/drug effects , Benzophenones/chemistry , Bone and Bones/drug effects , Lipid Peroxidation/drug effects , Chromatography, High Pressure Liquid , Reactive Oxygen Species , Rats, Sprague-Dawley , Plant Leaves/chemistry , Spectrometry, Mass, Electrospray Ionization , Ethanol , Tandem Mass Spectrometry , Liver/drug effects , Malondialdehyde , Antioxidants/chemistry
Article in Chinese | WPRIM | ID: wpr-941816


OBJECTIVE@#To explore a novel method for fabricating removable partial dentures (RPDs) using polyetheretherketone (PEEK) by computer-aided design and computer-aided manufacturing (CAD/CAM) technologies and to evaluate their fits for different assemblies in vitro.@*METHODS@#A standard stone cast of mandibular partial edentulous jaw was scanned using a lab scanner. Based on the digital cast, thirteen complete RPDs were designed combing dental CAD software and reverse engineering software, and then fabricated using PEEK by milling machine. Fits of assemblies were evaluated quantitatively by measuring the spaces between RPDs and casts. The gaps between RPDs and stone casts in different assemblies were duplicated using light-body silicone impression material and then measured using three-dimensional (3D) digital analysis methods in virtue of a dedicated software. Statistically, one-way analysis of variance (ANOVA) was used to compare the difference of gaps among assemblies in different shapes such as occlusal rest, denture base, and major connector. Paired-samples t test was used to compare the gaps difference for the similar shape assemblies in different areas.@*RESULTS@#One-piece PEEK RPDs were successfully designed and fabricated by CAD/CAM, and all the RPDs were well-seated on stone casts. The gaps between occlusal rests and casts [(84.3±23.6) μm] were significantly larger than those of denture bases [(32.5±27.8) μm] and major connectors [(49.9±47.0) μm], which meant that the fits of denture bases and major connectors were better than that of occlusal rests. However, the fits of all assemblies could be accepted clinically. For the similar shape assemblies in different areas, there were no significantly differences for gaps between distal extension denture bases [(25.1±55.3) μm] and non-extensive denture bases [(41.5±17.7) μm]. The gaps of occlusal rests adjacent and nonadjacent to the edentulous space were (86.1±29.8) μm and (80.8±42.1) μm respectively and there were no significantly difference between them either. These results implied that different locations had no apparent effect on the fits of assemblies.@*CONCLUSION@#With the computer-aided design and computer-aided manufacturing technology, PEEK can be used to fabricate one-piece removable partial dentures. And all assemblies of the one-piece PEEK RPDs showed satisfying fits in vitro, indicating a promising clinical application in the future.

Benzophenones , Computer-Aided Design , Denture, Partial, Removable , Ketones , Polyethylene Glycols , Polymers
Article in Chinese | WPRIM | ID: wpr-774572


Dalbergiae Odoriferae Lignum is derived from heartwood of Dalbergia odorifera,which is national Ⅱ level of rare and endangered protective plants in China. Its resources are scarce and its price is high. In order to find substitutes of D. odorifera,the chemical constituents of 70% ethanol extract of heartwood of D. catifolia were systematically studied by using silica gel,Sephadex LH-20 column chromatography,and semi-preparative HPLC. Sixteen neoflavanoids were isolated and identified as eight dalbergiphenols( 1-8),three dalbergiones( 9-11),two dalbergins( 12,13),two benzophenones( 14,15) and one other type neoflavanoids( 16) based on spectroscopic data analyses and/or comparing the spectroscopic data with those in literature. Among them,compounds 3,7 and 11 were isolated from the genus Dalbergia for the first time,and compounds 2,4-6,8,14 and 15 were isolated from the D. latifolia for the first time. Ten neoflavonoids were both discovered from D. latifolia and D. odorifera.

Benzophenones , China , Chromatography, High Pressure Liquid , Dalbergia , Plant Extracts
Article in Chinese | WPRIM | ID: wpr-774544


Five compounds were isolated from the fibrous roots of Anemarrhena asphodeloides by silica gel, Sephadex LH-20 and semi-HPLC column chromatography. On the basis of physic-chemical properties and spectroscopic data analysis, these compounds were identified as methyl 2-[2,4-dihydroxy-3-(4-hydroxybenzoyl)-6-methoxyphenyl]acetate(1), 4-[formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]butanoate(2), perlolyrine(3),syringaresinol-4'-O-β-D-glucoside(4) and 4',6-dihydroxy-4-methoxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-α-L-fructofuranoside(5). Among them, 1 was a new benzophenone. Compounds 2-5 were isolated from this plant for the first time. Compound 1 was tested for neuroprotective effects against H_2O_2-induced damage in SH-SY5 Y cells.

Anemarrhena , Chemistry , Benzophenones , Pharmacology , Cell Line , Chromatography, High Pressure Liquid , Humans , Neuroprotective Agents , Pharmacology , Phytochemicals , Pharmacology , Plant Roots , Chemistry
Acta ortop. mex ; 32(4): 203-208, Jul.-Aug. 2018. tab, graf
Article in English | LILACS | ID: biblio-1124095


Abstract: Objective: To compare results of Plate-Graff, Plate-Cage and PEEK cage in patients with cervical stenosis. Material and methods: Prospective, with before and after intervention and comparative study. From January 2005 to October 2011 we included 37 patients (male: 48.6%, female: 51.4%) post-surgery by anterior approach; 3 groups via: Group I, arthrodesis with Plate-Graff n = 12 (M 41.7%, F 58.3%) with 22 levels, group II, Plate-Cage n = 11 (M 63.6% 36.4% F) 19 levels, group III, PEEK cage, n = 14 (M 0% F 50%) with 25 levels. Functional assessment pre- and postoperative with neck disability index (NDI) and visual analogue scale for pain (VAS). The radiological assessment with X-rays only. Descriptive statistics were obtained. Wilcoxon method use according to data distribution, non parametric tests of ranges with sign of Kruskal-Wallis for comparison between more than two groups, and significance level with p < 0.05. We used the statistical package SPSS version 15. Results: The majority of patients was found between the sixth and eighth decade of life. At one year of follow up the NDI and pain with VAS shown improvement with statistical difference in three groups (p = 0.001). However, the radiographic measurements per year of follow-up showed a significant improvement of segmental lordosis (p = 0.02) only in patients with Plate-Graff. Conclusions: Using the graft offers best clinical and radiographic results compared with the Plate Cage and box peek to one year of follow-up.

Resumen: Objetivo: Comparar resultados de placa-injerto, caja-placa y caja-PEEK, en pacientes con conducto cervical estrecho. Material y métodos: Estudio prospectivo, en panel antes y después, de intervención y comparativo. De Enero de 2005 a Octubre de 2011, muestra de 37 pacientes (masculino: 48.6%, femenino: 51.4%) postoperados por vía anterior; formando tres grupos: grupo I, artrodesis con placa-injerto n = 12 (M 41.7%, F 58.3%) con 22 niveles; grupo II, caja-placa n = 11 (M 63.6%, F 36.4%) con 19 niveles; grupo III, caja-PEEK, n = 14 (M 50%, F 50%) con 25 niveles. La evaluación funcional pre- y postoperatoria mediante la escala de discapacidad cervical y escala visual análoga de dolor. La evaluación radiológica con radiografías de columna cervical. Se obtuvo estadística descriptiva. De acuerdo con la distribución de los datos se usaron pruebas no paramétricas de rangos con signo de Wilcoxon, y Kruskal-Wallis para comparación entre más de dos grupos. Con nivel de significancia de p<0.05. Se utilizó el paquete estadístico SPSS versión 15. Resultados: La mayoría de los pacientes se encontró entre la sexta y octava década de la vida. Al año de postoperados el índice de discapacidad cervical y mejoría del dolor con EVA mostraron mejoría con diferencia estadística en los tres grupos (p = 0.001). Sin embargo, las mediciones radiográficas al año de seguimiento mostraron una mejoría significativa de la lordosis segmentaria (p = 0.02) sólo en pacientes operados con placa-injerto. Conclusiones: El uso de la placa-injerto ofrece mejores resultados clínicos y radiográficos en comparación con la caja-placa y caja-PEEK, al año de seguimiento.

Humans , Male , Female , Polyethylene Glycols , Spinal Fusion/instrumentation , Diskectomy/instrumentation , Ketones , Polymers , Benzophenones , Cervical Vertebrae , Prospective Studies , Retrospective Studies , Treatment Outcome
Article in Chinese | WPRIM | ID: wpr-246098


This study is to develop a sensitive method by using reversed-phase high performance liquid chromatography coupled with UV detector (HPLC-UV) to simultaneously determine four bioactive compounds, iriflophenone 3-C-beta-D-glucoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside in the leaves of Aquilaria sinensis. An Agilent Zorbax SB-C, column (4, 6 mm x 250 mm, 5 microm) was used, and the gradient elution was performed with mobile phase of 0.1% aqueous phosphoric acid and acetonitrile at a flow rate of 1 mL x min(-1). The detection wavelength was 280 nm, and the column temperature was 25 degrees C. The four marker compounds were well separated with good linearity (R2 > 0.9990), precision, stability and repeatabili y. The-recovery rates were in the range of 98.80%-101.39%. For 15 branch of the leaves, the contents of iriflophenone 3-C-beta-D-gluoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside were between 0.41-14.48, 0.72-3.85, 4.30-29.07, 0.24-5.06 mg, respectivley. This method is precise, accurate and reliable, which provides an efficient way for the quality control of the leaves of A. sinensis. This will promote the comprehensive usage of this plant.

Benzophenones , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Plant Leaves , Chemistry , Spectrophotometry, Ultraviolet , Methods , Thymelaeaceae , Chemistry , Xanthones
Korean Journal of Radiology ; : 1029-1037, 2015.
Article in English | WPRIM | ID: wpr-163300


OBJECTIVE: To evaluate the utility of dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) using macromolecular contrast agent (P792) for assessment of vascular disrupting drug effect in rabbit VX2 liver tumor models. MATERIALS AND METHODS: This study was approved by our Institutional Animal Care and Use Committee. DCE-MRI was performed with 3-T scanner in 13 VX2 liver tumor-bearing rabbits, before, 4 hours after, and 24 hours after administration of vascular disrupting agent (VDA), using gadomelitol (P792, n = 7) or low molecular weight contrast agent (gadoterate meglumine [Gd-DOTA], n = 6). P792 was injected at a of dose 0.05 mmol/kg, while that of Gd-DOTA was 0.2 mmol/kg. DCE-MRI parameters including volume transfer coefficient (K(trans)) and initial area under the gadolinium concentration-time curve until 60 seconds (iAUC) of tumors were compared between the 2 groups at each time point. DCE-MRI parameters were correlated with tumor histopathology. Reproducibility in measurement of DCE-MRI parameters and image quality of source MR were compared between groups. RESULTS: P792 group showed a more prominent decrease in K(trans) and iAUC at 4 hours and 24 hours, as compared to the Gd-DOTA group. Changes in DCE-MRI parameters showed a weak correlation with histologic parameters (necrotic fraction and microvessel density) in both groups. Reproducibility of DCE-MRI parameters and overall image quality was not significantly better in the P792 group, as compared to the Gd-DOTA group. CONCLUSION: Dynamic contrast-enhanced magnetic resonance imaging using a macromolecular contrast agent shows changes of hepatic perfusion more clearly after administration of the VDA. Gadolinium was required at smaller doses than a low molecular contrast agent.

Animals , Antineoplastic Agents/therapeutic use , Benzophenones/therapeutic use , Disease Models, Animal , Heterocyclic Compounds/administration & dosage , Liver Neoplasms/drug therapy , Magnetic Resonance Imaging , Male , Organometallic Compounds/administration & dosage , Rabbits , Reproducibility of Results , Valine/analogs & derivatives
Yonsei Medical Journal ; : 1671-1677, 2015.
Article in English | WPRIM | ID: wpr-70403


PURPOSE: To compare the additive effects of two types of non-steroidal anti-inflammatory drugs (NSAIDs), bromfenac 0.1% or ketorolac 0.45%, relative to topical steroid alone in cataract surgery. MATERIALS AND METHODS: A total 91 subjects scheduled to undergo cataract operation were randomized into three groups: Group 1, pre/postoperative bromfenac 0.1%; Group 2, pre/postoperative preservative-free ketorolac 0.45%; and Group 3, postoperative steroid only, as a control. Outcome measures included intraoperative change in pupil size, postoperative anterior chamber inflammation control, change in macular thickness and volume, and ocular surface status after operation. RESULTS: Both NSAID groups had smaller intraoperative pupil diameter changes compared to the control group (p<0.05). There was significantly less ocular inflammation 1 week and 1 month postoperatively in both NSAID groups than the control group. The changes in central foveal subfield thickness measured before the operation and at postoperative 1 month were 4.30+/-4.25, 4.87+/-6.03, and 12.47+/-12.24 microm in groups 1 to 3, respectively. In the control group, macular thickness and volume increased more in patients with diabetes mellitus (DM), compared to those without DM. In contrast, in both NSAID groups, NSAIDs significantly reduced macular changes in subgroups of patients with or without DM. Although three ocular surface parameters were worse in group 1 than in group 2, these differences were not significant. CONCLUSION: Adding preoperative and postoperative bromfenac 0.1% or ketorolac 0.45% to topical steroid can reduce intraoperative miosis, postoperative inflammation, and macular changes more effectively than postoperative steroid alone.

Aged , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Benzophenones/administration & dosage , Bromobenzenes/administration & dosage , Cataract , Cataract Extraction , Female , Humans , Inflammation/prevention & control , Ketorolac/administration & dosage , Lens Implantation, Intraocular , Macular Edema/prevention & control , Male , Middle Aged , Miosis/prevention & control , Phacoemulsification , Postoperative Complications/drug therapy , Postoperative Period , Premedication , Treatment Outcome
Article in English | WPRIM | ID: wpr-56488


This study investigated the toxicity of commercial non-steroid anti-inflammatory drug (NSAID) eye solutions against corneal epithelial cells in vitro. The biologic effects of 1/100-, 1/50-, and 1/10-diluted bromfenac sodium, pranoprofen, diclofenac sodium, and the fluorometholone on corneal epithelial cells were evaluated after 1-, 4-, 12-, and 24-hr of exposure compared to corneal epithelial cell treated with balanced salt solution as control. Cellular metabolic activity, cellular damage, and morphology were assessed. Corneal epithelial cell migration was quantified by the scratch-wound assay. Compared to bromfenac and pranoprofen, the cellular metabolic activity of diclofenac and fluorometholone significantly decreased after 12-hr exposure, which was maintained for 24-hr compared to control. Especially, at 1/10-diluted eye solution for 24-hr exposure, the LDH titers of fluorometholone and diclofenac sodium markedly increased more than those of bromfenac and pranoprofen. In diclofenac sodium, the Na+ concentration was lower and amount of preservatives was higher than other NSAIDs eye solutions tested. However, the K+ and Cl- concentration, pH, and osmolarity were similar for all NSAIDs eye solutions. Bromfenac and pranoprofen significantly promoted cell migration, and restored wound gap after 48-hr exposure, compared with that of diclofenac or fluorometholone. At 1/50-diluted eye solution for 48-hr exposure, the corneal epithelial cellular morphology of diclofenac and fluorometholone induced more damage than that of bromfenac or pranoprofen. Overall, the corneal epithelial cells in bromfenac and pranoprofen NSAID eye solutions are less damaged compared to those in diclofenac, included fluorometholone as steroid eye solution.

Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Benzophenones/administration & dosage , Benzopyrans/administration & dosage , Bromobenzenes/administration & dosage , Cell Movement/drug effects , Cells, Cultured , Diclofenac/administration & dosage , Epithelial Cells/drug effects , Epithelium, Corneal/cytology , Fluorometholone/administration & dosage , Humans , L-Lactate Dehydrogenase/metabolism , Microscopy, Electron, Transmission , Ophthalmic Solutions , Propionates/administration & dosage
Article in Chinese | WPRIM | ID: wpr-300217


Fourteen compounds were isolated from Dalbergia odoriferae and purified by repeated column chromatography on silica and sephadex LH-20 gel and structurally identified by spectral analysis. These compounds were identified as 4, 9-dimethoxy-3-hydroxypterocarpan (1), medicarpin (2), 2', 4', 5-trihydroxy-7-methoxyisoflavone (3), 2', 3', 7-trihydroxy-4'-methoxyisoflavan (4), formononetin (5), 3, 8-dihydroxy-9-methoxypterocarpan (6), koparin (7), 3-hydroxy-9-methoxypterocarp-6a-ene (8), 2'-hydroxyformononetin (9), stevenin (10), 2', 7-dihydroxy-4', 5'-dimethoxyisoflavone (11), lyoniresinol (12), 2, 4-dihydroxy-5-methoxy-benzophenone (13) and neokhriol A (14). Compounds 1, 3, 4, 6, 8, 12 and 14 were isolated from this plant for the first time. Antibacterial activity assay showed that compound 4 had inhibitory effect on Ralstonia solanacearum.

Anisoles , Chemistry , Pharmacology , Anti-Bacterial Agents , Chemistry , Pharmacology , Benzophenones , Chemistry , Pharmacology , Chromatography , Methods , Dalbergia , Chemistry , Dextrans , Gels , Isoflavones , Chemistry , Pharmacology , Microbial Sensitivity Tests , Naphthalenes , Chemistry , Pharmacology , Plant Extracts , Chemistry , Pharmacology , Pterocarpans , Chemistry , Pharmacology , Ralstonia solanacearum , Silica Gel
Acta Pharmaceutica Sinica ; (12): 166-174, 2014.
Article in Chinese | WPRIM | ID: wpr-297997


Garcinia plants are one of the rich sources of natural xanthones and benzophenones which have attracted a great deal of attention from the scientists in the fields of chemistry and pharmacology. Recently, many structurally unique constituents with various bioactivities, especially anti-tumor activity, have been isolated from Garcinia plants. This concise review focused on the anti-cancer activity natural products isolated from Chinese Garcinia plants, and the research finding by authors and collaborators over the past several years were cited.

Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Benzophenones , Chemistry , Pharmacology , Cell Line, Tumor , Cell Proliferation , Drugs, Chinese Herbal , Chemistry , Pharmacology , Garcinia , Chemistry , Classification , Humans , Inhibitory Concentration 50 , Molecular Structure , Plants, Medicinal , Chemistry , Classification , Structure-Activity Relationship , Terpenes , Chemistry , Pharmacology , Xanthones , Chemistry , Pharmacology
Article in English | WPRIM | ID: wpr-812281


AIM@#To investigate the chemical constituents of the roots of Polygala sibirica L. (Polygalaceae)@*METHOD@#The isolation was performed by solvent extraction and various chromatographic techniques, including silica gel, Sephadex LH-20, ODS, semi-preparative HPLC, and preparative TLC. The chemical structures were elucidated based on extensive spectroscopic analysis, including HR-ESI-MS and 1D- and 2D-NMR spectroscopic data.@*RESULTS@#A total of sixteen compounds, including five xanthones (5, 7-10), five saccharide esters (1, 3, 4, 12, 13), two flavonoids (14, 16), two triterpenoids (11, 15), one phenylpropanoid (6), and one benzophenone glycoside (2) were isolated. Their structures were determined as sibiricose A7 (1), sibiriphenone A (2), polygalatenoside A (3), polygalatenoside C (4), lancerin (5), 3, 4, 5-trimethoxycinnamic acid (6), 6-hydroxy-1, 2, 3, 7-tetramethoxyxanthone (7), 1, 3, 7-trihydroxy-2-methoxyxanthone (8), onjixanthone II (9), 1, 2, 3, 6, 7-pentamethoxyxanthone (10), presenegenin (11), 3'-O-3, 4, 5-trimethoxycinnamoyl-6-O-4-methoxy benzoyl sucrose (12), tenuifoliside C (13), 5, 3'-dihydroxy-7, 4'-dimethoxyflavonol-3-O-β-D-glucopyranoside (14), tenuifolin (15), and rhamnetin 3-O-β-D-glucopyranoside (16).@*CONCLUSION@#Compounds 1 and 2 are two new compounds from P. sibirica.

Benzophenones , Chemistry , Coumaric Acids , Chemistry , Glucosides , Chemistry , Molecular Structure , Plant Extracts , Chemistry , Plant Roots , Chemistry , Polygala , Chemistry , Triterpenes , Chemistry , Xanthones , Chemistry
Braz. j. pharm. sci ; 49(2): 251-261, Apr.-June 2013. ilus, graf, tab
Article in English | LILACS | ID: lil-680636


Nanotechnology applies to diverse sectors of science. In cosmetic area, investments have strengthened the idea that nanoproducts provide innumerable benefits to consumers. Extreme exposition to solar light can cause undesirable effects, thus, adding UV filters in cosmetic products are often used as prevention. Ethylhexyl methoxycinnamate and benzophenone-3 are UV filters widely used in sunscreen formulations, this UV filters absorb UVB and UVA radiation, respectively. In this study, sunscreen formulations were developed as nano and macroemulsion, but composed by the same raw material. Nanoemulsion was obtained by phase inversion temperature method (PIT). Physical and functional properties were evaluated by visual analysis, particle size distribution and by diffuse reflectance spectrophotometry. Achieved nanoemulsion showed bluish brightness aspect, less apparent consistency than macroemulsion, stability longer than 48 hours (22.0 ± 2.0 °C) and bimodal particle size distribution with average (mean) sizes around 10 nm (61%) and 4.5 µm (39%). Macroemulsion showed milky aspect, higher consistency than nanoemulsion, instability after 48 hours (22.0 ± 2.0 °C) and bimodal particle size distribution with average (mean) size around 202 nm (9%) and 10.4 µm (91%). Effectiveness profile of sunscreen formulations remained apparently similar, based on achieved results of in vitro SPF, UVA/UVB ratio and critical wavelength assays.

A nanotecnologia se aplica a diversos setores da ciência. Na área de cosméticos, os investimentos têm reforçado a idéia de que nanoprodutos oferecem inúmeros benefícios para os consumidores. A exposição excessiva à luz solar pode causar efeitos indesejáveis, logo, a adição de filtros UV em produtos cosméticos é frequentemente usada como prevenção. O p-metoxicinamato de octila e a benzofenona-3 são filtros UV amplamente utilizados em formulações de protecção solar, que absorvem radiações UVB e UVA, respectivamente. Neste estudo, desenvolveram-se formulações de protetores solares na forma de nano e macroemulsão, mas compostos pelas mesmas matérias-primas. A nanoemulsão foi obtida pelo método da temperatura de inversão de fases (PIT). As propriedades físicas e funcionais foram avaliadas por análise visual, distribuição de tamanho de partículas e por espectrofotometria de reflectância difusa. A nanoemulsão obtida apresentou brilho azulado, menor consistência aparente quando comparada `a macroemulsão, estabilidade superior a 48 horas (22,0 ± 2,0 ° C) e distribuição de tamanhos de partícula bimodal, com média (média) de tamanhos ao redor de 10 nm (61%) e 4,5 µm (39%) . A macroemulsão apresentou aspecto leitoso, maior consistência aaprente do que nanoemulsão, instabilidade após 48 horas (22,0 ± 2,0 ºC) e distribuição de tamanhos de partícula bimodal, com média (média) de tamanhos ao redor de 202 nm (9%) e 10,4 µm (91%). O perfil de eficácia das formulações fotoprotetoras permaneceu aparentemente similar, com base em resultados obtidos por ensaios de FPS in vitro, relação UVA/UVB e comprimento de onda crítico.

In Vitro Techniques/statistics & numerical data , Particle Size , Sunscreening Agents/analysis , Benzophenones/analysis , Nanotechnology , Temperature Inversion , Ultraviolet Filters
Rio de Janeiro; s.n; 2013. ix,59 p. mapas, graf, tab.
Thesis in Portuguese | LILACS | ID: lil-736521


A triagem de compostos de origem natural é uma estratégia importante na busca por candidatos antiasmáticos. Neste contexto, estudos anteriores evidenciaram a marcada atividade antiespasmódica e antialérgica da substância 7-Epiclusianona (7-Epi). Essa benzofenona é integrante do extrato hexânico do fruto da Garcínia brasiliensis e, portanto, de difícil proteção patentária. A complexação da 7-Epi com um íon de cobre (7-EpiCu 2+ ) tornou-a estruturalmente inédita e patenteável. Assim, são três os principais objetivos deste estudo: (i) investigar os efeitos de 7-Epi sobre as características patológicas de modelos murinos de asma alérgica; (ii) caracterizar a atividade antiespasmódica de 7-EpiCu 2+ sobre modelos in vitro e in vivo, tal qual já demonstrado para a 7-Epi, bem como os efeitos do complexo sobre a hiper -reatividade das vias aéreas in vivo; (iii) investigar possíveis alvos celulares dessas substâncias. Os resultados mostraram que, em modelos animais relevantes, a administração oral de 7-Epi, tanto em regime preventivo quanto terapêutico, foi capaz de prevenir e reverter a hiper-reatividade das vias aéreas e outros aspectos fisiopatológicos importantes na asma...

Em paralelo, demonstramos que o complexo metálico 7-EpiCu 2+ possui eficácia antiespasmódica in vitro e in vivo, seguindo um mecanismo de ação dependente da integridade do epitélio da via aérea, tal qual já descrito para a 7-Epi. Por outro lado, o tratamento preventivo com o complexo 7-EpiCu 2+ não impediu o desenvolvimento da hiper-reatividade, tendo por base o modelo de asma alérgica aguda. Os estudos com células da linhagem de epitélio pulmonar humano (A549) revelaram a capacidade da 7-Epi de inibir a produção de MCP-1 induzida por IL-1β. Em sistemas baseados em fibroblastos pulmonares primários murinos, ambos os compostos foram claramente ativos em bloquear a proliferação celular e a geração de eotaxina-1 promovidas por IL-13. Entretanto, em ambos os casos, o efeito inibitório apareceu fortemente associado a uma ação aparentemente citotóxica dos compostosEm conjunto, nossos resultados caracterizam o composto 7-Epi como um agente oralmente ativo, com capacidade de inibir sinais patológicos cruciais da asma, tanto em regime profilático como terapêutico. Além disso, apesar da marcada atividade antiespasmódi ca apresentada em sistemas in vitro, o composto 7-EpiCu 2+ mostrou-se inativo em inibir o desenvolvimento da hiper-reatividade na asma aguda in vivo, o que somado às propriedades citotóxicas diretas sobre fibroblastos pulmonares murinos e células epiteliais alveolares humanas, compromete o potencial antiasmático e clínico dessa substância...

Humans , Anti-Inflammatory Agents, Non-Steroidal , Asthma , Benzophenones , Copper
Indian J Biochem Biophys ; 2012 Feb; 49(1): 18-24
Article in English | IMSEAR | ID: sea-140214


Diabetes is associated with increased formation of advanced glycation end products (AGEs), which have been implicated in micro and macrovascular complications of diabetes. Our earlier reports showed proangiogenic effect of AGE-bovine serum albumin (BSA). In order to understand the mechanism of AGE-mediated angiogenesis, the possibility of involvement of peroxisome prolifeator activated receptor (PPAR) , a ligand activated transcription factor was examined. The angiogenic effect was studied in chick chorio allantoic membrane (CAM) and by analyzing angiogenic markers in human umbilical vein endothelial cells (HUVECs) in culture. The involvement of PPAR was investigated using synthetic PPAR agonist GW 1929 and antagonist GW 9662 and by RT-PCR. In CAM assay, PPAR antagonist GW 9662 reversed the AGE-induced effect on vascularity. In HUVECs in culture, GW 9662 reversed the effect of AGE-BSA and decreased the expression of CD 31, E-Selectin and VEGF. RT-PCR analysis showed that treatment with AGE-BSA caused upregulation of PPAR mRNA levels. The reversal of the effect of AGE on angiogenesis by treatment with PPAR antagonists and up-regulation of PPAR gene in HUVECs treated with AGE-BSA suggested the possible involvement of PPAR -dependent downstream pathway in mediating the angiogenic effect of AGE.

Angiogenesis Inducing Agents/metabolism , Anilides/pharmacology , Animals , Platelet Endothelial Cell Adhesion Molecule-1/drug effects , Platelet Endothelial Cell Adhesion Molecule-1/metabolism , Benzophenones/pharmacology , Cells, Cultured , Chick Embryo , Chorioallantoic Membrane/drug effects , Chorioallantoic Membrane/metabolism , Diabetes Mellitus/metabolism , E-Selectin/metabolism , Glycation End Products, Advanced/pharmacology , Human Umbilical Vein Endothelial Cells/metabolism , PPAR gamma/antagonists & inhibitors , PPAR gamma/antagonists & inhibitors , PPAR gamma/drug effects , PPAR gamma/metabolism , RNA/drug effects , RNA/metabolism , Tyrosine/analogs & derivatives , Tyrosine/pharmacology , Vascular Endothelial Growth Factor A/drug effects , Vascular Endothelial Growth Factor A/metabolism