RESUMEN
Butea monosperma (Fabaceae) has been used in traditional Indian medicine to treat a variety of ailments, including abdominal tumors. We aimed to investigate the anti-IL-6 activity of butein in ovarian cancer and elucidate the underlying molecular mechanisms. Butein was isolated and identified from B. monosperma flowers, and the inhibition of IL-6 signaling was investigated using the HEK-Blue™ IL-6 cell line. The surface plasmon resonance assay was used to estimate the binding of butein to IL-6, IL-6Rα, and gp130. After treatment with butein, ovarian cancer cell migration, apoptosis, and tumor growth inhibition were evaluated in vitro and in vivo. Furthermore, we used STAT3 siRNA to identify the mechanistic effects of butein on the IL-6/STAT3/FoxO3a pathway. Butein suppressed downstream signal transduction through higher binding affinity to IL-6. In ovarian cancer, butein inhibited cell proliferation, migration, and invasion, and induced cell cycle arrest and apoptosis. In addition, it decreased the growth of ovarian cancer cells in xenograft tumor models. Butein inhibited STAT3 phosphorylation and induced FoxO3a accumulation in the nucleus by inhibiting IL-6 signaling. The anticancer activity of butein was mediated by blocking the IL-6/IL-6Rα interaction and suppressing IL-6 bioactivity via interfering with the IL-6/STAT3/FoxO3a pathway.
Asunto(s)
Chalconas , Neoplasias Ováricas , Femenino , Humanos , Apoptosis , Línea Celular , Línea Celular Tumoral , Proliferación Celular , Chalconas/farmacología , Neoplasias Ováricas/tratamiento farmacológico , Factor de Transcripción STAT3/metabolismoRESUMEN
In this study, high-performance countercurrent chromatography was employed to isolate six anthraquinone diglucosides, namely, cascarosides A-F, from cascara sagrada (Rhamnus purshiana DC [Rhamnaceae]) bark. The n-butanol-soluble extract of cascara sagrada was separated by off-line two-dimensional high-performance countercurrent chromatography. The first-dimensional high-performance countercurrent chromatography resolved the n-butanol-soluble extract (510 mg) of cascara sagrada using the flow-rate gradient method with a chloroform-methanol-isopropanol-water (6:6:1:4, v/v/v/v, normal-phase mode) system to afford four anthraquinone diglucoside fractions (groups I [cascarosides C-D, 71 mg], II [cascarosides E-F, 56 mg], III [cascaroside A, 53 mg], and IV [cascaroside B, 31 mg]). Groups I and II were separated by the second-dimensional high-performance countercurrent chromatography using an ethyl acetate-n-butanol-water (7:3:10, v/v/v, normal-phase mode) system to yield cascarosides C (34 mg), D (26 mg), E (19 mg), and F (15 mg). Additionally, one-step preparative-scale high-performance countercurrent chromatography method was developed to isolate large amounts of cascarosides A (389 mg) and B (187 mg) from the water-soluble extract (2.1 g) of cascara sagrada using an ethyl acetate-n-butanol-water (2:8:10, v/v/v, normal-phase mode) system. The current study demonstrated that high-performance countercurrent chromatography is a powerful technique for the isolation of marker compounds from herbal materials.
Asunto(s)
Antraquinonas/aislamiento & purificación , Glucósidos/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Rhamnus/química , Antraquinonas/química , Cromatografía Líquida de Alta Presión , Distribución en Contracorriente , Glucósidos/química , Conformación Molecular , Corteza de la Planta/química , Extractos Vegetales/química , EstereoisomerismoRESUMEN
UNLABELLED: Pharmaceutical industry has been striving to reduce the costs of drug development and increase productivity. Among the many different attempts, drug repositioning (retargeting existing drugs) comes into the spotlight because of its financial efficiency. We introduce IDMap which predicts novel relationships between targets and chemicals and thus is capable of repositioning the marketed drugs by using text mining and chemical structure information. Also capable of mapping commercial chemicals to possible drug targets and vice versa, IDMap creates convenient environments for identifying the potential lead and its targets, especially in the field of drug repositioning. AVAILABILITY: IDMap executable and its user manual including color images are freely available to non-commercial users at http://www.equispharm.com/idmap
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Inteligencia Artificial , Sistemas de Administración de Bases de Datos , Bases de Datos Factuales , Diseño de Fármacos , Quimioterapia/métodos , Preparaciones Farmacéuticas/química , Programas Informáticos , Almacenamiento y Recuperación de la Información/métodosRESUMEN
Natural methane hydrates occurring in marine clay sediments exhibit heterogeneous phase behavior with high complexity, particularly in the negatively charged interlayer region. To date, the real clay interlayer effect on natural methane hydrate formation and stability remains still much unanswered, even though a few computer simulation and model studies are reported. We first examined the chemical shift difference of 27Al, 29Si, and 23Na between dry clay and clay containing intercalated methane hydrates (MH) in the interlayer. We also measured the solid-state 13C MAS NMR spectra of MH in Na-montmorillonite (MMT) and Ca-montmorillonite (MMT) to reveal abnormal methane popularity established in the course of intercalation and further performed cryo-TEM and XRD analyses to identify the morphology and layered structure of the intercalated methane hydrate. The present findings strongly suggest that the real methane amount contained in natural MH deposits should be reevaluated under consideration of the compositional, structural, and physical characteristics of clay-rich sediments. Furthermore, the intercalated methane hydrate structure should be seriously considered for developing the in situ production technologies of the deep-ocean methane hydrate.
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Chemical materials are sometimes harmful to the environment as well as humans, plants, and animals. Thus, high-performance sensor systems have become more important in the past few decades. To achieve pH scale sensing in nanosystems, we applied luminescence polymer nanowires with alumina oxide template method with electrochemical polymerization. We made polymer nanowire barcode by alternately stacking poly(3-methylthiophene) (P3MT) and poly(3,4-ethylenedioxythiophene) (PEDOT) in a nanoporous template. After polymerization, a hydrofluoric acid solvent was used to remove the template, and, for changing the pH scale, we used sodium hydroxide. We measured optical properties of each part of barcode using Raman scattering and photoluminescence and confirmed that only P3MT was changed by alkali treatment.
RESUMEN
Overexpression of cyclooxygenase-2 (COX-2) has been demonstrated in various cancers, including experimentally promoted tumors, gastrointestinal cancers, breast tumors and skin tumors. The mechanism that controls COX-2 expression is not yet clear. Currently, it is reported that COX-2 expression is frequently associated with mutated p53 genes. The goal of this study was to evaluate the expression patterns of COX-2 and p53 in several skin tumors and their correlation. An immunohistochemical method was used to investigate the expression of COX-2 and p53 proteins on formalin-fixed, paraffin-embedded tissue specimens of squamous cell carcinomas (SCC), basal cell carcinomas (BCC), Bowen's disease (BD), actinic keratosis (AK) and porokeratosis. The expression of COX-2 increased in 50% (5/10) of SCC, 80% (8/10) of BCC, 40% (4/10) of BD, 50% (5/10) of AK, and 20% (2/10) of porokeratosis cases. The expression of p53 increased in 90% (9/10) of SCC, 70% (7/10) of BCC, 70% (7/10) of BD, 50% (5/10) of AK, and 40% (4/10) of porokeratosis cases. COX-2 positivity rates of the p53-positive skin tumors were 56%, 100%, 57%, 80% and 25% in SCC, BCC, BD, AK and porokeratosis, respectively. However, the correlation between p53 and COX-2 expression in skin tumors was not statistically significant (P > 0.05). Our results indicate that skin COX-2 and p53 may play roles in skin tumors, but that there is no apparent correlation between the two markers.
Asunto(s)
Ciclooxigenasa 2/metabolismo , Regulación Neoplásica de la Expresión Génica , Neoplasias Cutáneas/metabolismo , Proteína p53 Supresora de Tumor/metabolismo , Enfermedad de Bowen/metabolismo , Carcinoma Basocelular/metabolismo , Carcinoma de Células Escamosas/metabolismo , Humanos , Inmunohistoquímica , Queratosis/metabolismo , Poroqueratosis/metabolismoRESUMEN
BACKGROUND: A venous lake lesion is a venous ectasia that occurs on the exposed skin of elderly people. Although a number of therapies such as surgical excision, laser therapy, infrared coagulation, cryotherapy and sclerotherapy have been used to treat venous lakes, there is no guideline for treating this lesion. OBJECTIVE: The purpose of this study was to determine whether 0.5% sodium tetradecyl sulfate (STS) is effective for the treatment of venous lake lesions. METHODS: Twelve patients with venous lake lesions were enrolled In this study. After proper antiseptic preparation, 0.5% STS was slowly injected into each subject's lesion, and this was followed by immediate compression for 10 minutes. RESULTS: After treatment, all of the patients' lesions cleared completely. The average number of treatments was 2.15±1.28. Two patients experienced mild side effects such as light pain and paresthesia, and these soon disappeared. There were no serious side effects reported during treatment. The mean follow up period was 29.58±13.48 months. CONCLUSION: We have demonstrated that sclerotherapy with 0.5% STS was quite effective for treating venous lake lesions, and this treatment caused no serious adverse effects.
RESUMEN
Eruptive collagenoma is an acquired connective tissue nevus without family history. It is typically described as numerous small papules or nodules on the trunk and arms with histopathological features of decreased or degenerated elastic fibers. We report a case of a 16-year-old male who presented with multiple asymptomatic 2 to 5 mm sized yellowish grouped papules on the left calf. Histopathologically, the lesion showed thickened homogenized collagen fibers highlighted by Masson trichrome stain and decreased and fragmented elastic fibers stained by Verhoeff-van Gieson stain. The skin lesion was diagnosed as eruptive collagenoma and no treatment was provided.