Sclerotherapy of benign oral vascular lesions with non-diluted ethanolamine oleate / Escleroterapia de lesiones vasculares orales benignas con oleato de etanolamina no diluido

Benign oral vascular lesions are anomalies characterized by the blood vessels proliferation or malformation and the treatment with the sclerosing agent ethanolamine oleate acts irrigating the vessel producing a sterile inflammatory response. The objective of this study was to report and discuss the results from treatment of benign oral vascular lesions with non-diluted ethanolamine oleate through the analysis of clinical records. The sample was composed by the selection of twenty-six patients (12 male and 14 female), with oral vascular malformations. All lesions were treated with intralesional injections of undiluted ethanolamine oleate. These patients attended in Oral Medicine outpatient clinic of the Federal University of Paraná between the years of 2011 to 2015. The average age was 60.65 years, with a higher prevalence for women. The majority of the individuals had one lesion and its location was mostly in the lower lip. The main complaint was about a physical discomfort. The lesions had the average size of 6.52 mm and received a median number of 2.32 applications. Only one patient reported feeling pain in the postoperative week. In most cases the resolution of the lesion was considered partial. Follow-up was obtained up to one month after the end of treatment. The sclerotherapy with undiluted ethanolamine oleate shows acceptable results in the treatment of small benign oral vascular lesions with a few minor side effects.

Las lesiones vasculares orales benignas son anomalías caracterizadas por la proliferación o malformación de los vasos sanguíneos y el tratamiento con el agente esclerosante etanolamina oleato actúa irrigando el vaso produciendo una respuesta inflamatoria estéril. El objetivo de este estudio fue informar y discutir los resultados del tratamiento de lesiones vasculares orales benignas con oleato de etanolamina no diluido a través del análisis de historias clínicas. La muestra estuvo compuesta por la selección de veintiséis pacientes (12 hombres y 14 mujeres), con malformaciones vasculares orales. Todas las lesiones fueron tratadas con inyecciones intralesionales de oleato de etanolamina sin diluir. Estos pacientes acudieron a la clínica ambulatoria de Medicina Oral de la Universidad Federal de Paraná entre los años 2011 a 2015. La edad promedio fue de 60,65 años, con una mayor prevalencia para las mujeres. La mayoría de los individuos tenían una lesión y su ubicación era principalmente en el labio inferior. La queja principal era sobre una molestia física. Las lesiones tenían un tamaño promedio de 6,52 mm y recibieron una mediana de 2,32 aplicaciones. Solo un paciente informó haber sentido dolor en la semana postoperatoria. En la mayoría de los casos, la resolución de la lesión se consideró parcial. El seguimiento se obtuvo hasta un mes después del final del tratamiento. La escleroterapia con oleato de etanolamina sin diluir muestra resultados aceptables en el tratamiento de pequeñas lesiones vasculares orales benignas con algunos efectos secundarios menores.

Sclerotherapy as an esthetic indication in oral vascular malformations: a case series

Abstract Background The use of monoethanolamine oleate 5% is effective for the treatment of vascular malformations with low blood flow. Objectives To report a case series of vascular malformations in the mouth and oral cavity treated with monoethanolamine oleate 5%. Methods A retrospective descriptive study was performed in electronic patient charts covering seven years. Patient demographics, diagnostic resources, lesion site, size, and number of applications of monoethanolamine oleate 5% were collected. Results A total of 21 vascular malformations were recorded, located mostly on the lower lip (52.3%) and resolved in a single application in 14 patients. The authors found 19 patients treated with sclerotherapy. Thirteen were women and six were men, with a mean age of 61 years. Study limitation Small sample size. Conclusions Sclerotherapy is an effective treatment for vascular malformations of the lips and oral cavity, with resolution after only one or two applications (n = 16).

Differential effects of saturated and unsaturated fatty acids on vascular reactivity in isolated mesenteric and femoral arteries of rats

Free fatty acid (FFA) intake regulates blood pressure and vascular reactivity but its direct effect on contractility of systemic arteries is not well understood. We investigated the effects of saturated fatty acid (SFA, palmitic acid), polyunsaturated fatty acid (PUFA, linoleic acid), and monounsaturated fatty acid (MUFA, oleic acid) on the contractility of isolated mesenteric (MA) and deep femoral arteries (DFA) of Sprague–Dawley rats. Isolated MA and DFA were mounted on a dual wire myograph and phenylephrine (PhE, 1–10 µM) concentration-dependent contraction was obtained with or without FFAs. Incubation with 100 µM of palmitic acid significantly increased PhE-induced contraction in both arteries. In MA, treatment with 100 µM of linoleic acid decreased 1 µM PhE-induced contraction while increasing the response to higher PhE concentrations. In DFA, linoleic acid slightly decreased PhE-induced contraction while 200 µM oleic acid significantly decreased it. In MA, oleic acid reduced contraction at low PhE concentration (1 and 2 µM) while increasing it at 10 µM PhE. Perplexingly, depolarization by 40 mM KCl-induced contraction of MA was commonly enhanced by the three fatty acids. The 40 mM KCl-contraction of DFA was also augmented by linoleic and oleic acids while not affected by palmitic acid. SFA persistently increased alpha-adrenergic contraction of systemic arteries whereas PUFA and MUFA attenuated PhE-induced contraction of skeletal arteries. PUFA and MUFA concentration-dependent dual effects on MA suggest differential mechanisms depending on the types of arteries. Further studies are needed to elucidate underlying mechanisms of the various effects of FFA on systemic arteries.

Escleroterapia em lesões vasculares de boca: relato de dois casos clínicos / Sclerotherapy in vascular lesions of the mouth: report of two clinical cases

O hemangioma é uma neoplasia de comportamento benigno, determinada pela proliferação anormal de vasos sanguíneos. São lesões assintomáticas, porém, seu crescimento progressivo pode acarretar danos traumáticos locais, ocasionando dor, ulcerações e até sangramentos, que, dependendo da localização, se tornam de difícil controle, principalmente quando de natureza arterial. Com considerável incidência na região de cabeça e pescoço e na cavidade bucal, acomete mais frequentemente a região de mucosa jugal, lábios e língua. Tendo em vista a sua relevância clínica, por estar presente na sua área de atuação e ser relativamente comum, o conhecimento acerca dessa neoplasia benigna é de fundamental importância ao cirurgião-dentista. Entre os recursos terapêuticos, a escleroterapia química tem sido empregada, apresentando resultados satisfatórios tanto clínicos quanto estéticos. Objetivo: apresentar as características clínicas do hemangioma, os métodos de diagnóstico e o tratamento realizado por meio de escleroterapia química. Relato de caso: são descritos dois casos clínicos de hemangiomas, diagnosticados em duas pacientes do sexo feminino, localizados um em lábio superior e outro em mucosa jugal, tratados por meio de injeção de solução esclerosante. Considerações finais: em ambos os casos, foi possível proporcionar a involução das lesões mediante procedimentos não cirúrgicos, favorecendo, no período pós-operatório, o conforto e a estética, demonstrando a eficiência e a segurança na utilização do oleato de monoetanolamina a 5% (Ethamolin ®). (AU)

Hemangioma is a neoplasm of benign behavior, determined by abnormal proliferation of blood vessels. They are asymptomatic lesions, however, their progressive growth can cause local traumatic injuries, causing pain, ulcerations and even bleeding, which, depending on the location, becomes difficult to control, especially when of an arterial nature. With a considerable incidence in the head and neck region, in the oral cavity, it most frequently affects the region of jugal mucosa, lips and tongue. Due to its clinical relevance, because it is present in the area of practice of the dental surgeon and is relatively common, knowledge about this benign neoplasm is of fundamental importance. Among the therapeutic resources, chemical sclerotherapy is employed presenting satisfactory clinical and aesthetic results. Objective: the purpose of this study is to present the clinical characteristics of hemangioma, the diagnostic methods and the treatment performed through chemical sclerotherapy. Case report: this article describes the description of two clinical cases of hemangiomas diagnosed in two female patients, one located in the upper lip and the other in the jugal mucosa treated with sclerosing solution injection. Final considerations: in both cases, it was possible to provide the involution of the lesions by non-surgical procedures, favoring, in the postoperative period, comfort and aesthetics, demonstrating the efficiency and safety in the use of 5% monoethanolamine oleate (Ethamolin®). (AU)

Anti-atherosclerosis role of N-oleoylethanolamine in CB2 / 药学学报

To observe a PPAR-alpha agonist effect of N-oleoylethanolamine (OEA) on CB2 (cannabinoid receptor 2), an anti-inflammatory receptor in vascular endothelial cell, healthy HUVECs and TNF-alpha induced HUVECs were used to establish a human vascular endothelial cell inflammatory model. Different doses of OEA (10, 50 and 100 micromol x L(-1)) had been given to HUVECs, cultured at 37 degrees C for 7 h and then collected the total protein and total mRNA. CB2 protein expression was detected by Western blotting and CB2 mRNA expression was assayed by real-time PCR. As the results shown, OEA (10 and 50 micromol x L(-1)) could induce the CB2 protein and mRNA expression, but not 100 micromol x L(-1). To detect if anti-inflammation effect of OEA is partly through CB2, CB2 inhibitor AM630 was used to inhibit HUVEC CB2 expression, then the VCAM-1 expression induced by TNF-alpha was detected, or THP-1 adhere to TNF-alpha induced HUVECs was examined. OEA (50 micromol x L(-1)) could inhibit TNF-alpha induced VCAM-1 expression and THP-1 adhere to HUVECs, these effects could be partly inhibited by a CB2 inhibitor AM630. The anti-inflammation effect of OEA is induced by PPAR-alpha and CB2, suggesting that CB2 signaling could be a target for anti-atherosclerosis, OEA have wide effect in anti-inflammation, it may have better therapeutic potential in anti-inflammation in HUVECs, thus achieving anti-atherosclerosis effect.

Ponderal behavior of rats fed an omegas 3, 6 and 9 enriched diet submitted to colon carcinogenesis induced by azoxymethane

PURPOSE: To assess weight changes in rats fed diets with different ratios of omegas 3, 6 and 9 submitted to colonic carcinogenesis induced by Azoxymethane (AOM). METHODS: Sixty rats with three weeks of life were distributed into five groups of specific diets containing 12 animals each: GI- Standard diet without adminstration of AOM, GII- Standard diet with adminstration of AOM; GIII- Hyperlipidic diet with adminstration of AOM; GIV-Normolipidic diet with adminstration of AOM; GV- Hypolipidic diet with adminstration of AOM. The weight and food intake of each group were assessed four times in each week throughout the experiment until euthanasia at 36th week. RESULTS: GI and GII had no significant difference in weight. GI showed a significant increase when compared to GIII, GIV and GV. GII also showed a significant increase when compared to GIII, GIV and GV. When comparing intake of GI as compared to GII no significant difference was found, however such groups had higher intake than groups III, IV and V. There were found no difference in weight when comparing amoung rats with and without cancer within each groups: GII, GIII, GIV and GV. CONCLUSIONS: Diets rich in omega 3, 6 and 9 reduced food intake and weight. Rats with colorectal cancer had no decrease in weight as compared to those without this condition in the same group.

Fine Needle Aspiration Cytology and Intralesional Steroid Injection in a Central Giant Cell Granuloma Affecting the Gingiva: A New Clinical Approach

Central giant cell granuloma (CGCG) is a benign jaw lesion predominantly found in the mandible of young female patients with a variable clinical behavior. Although surgical management is regarded as the main treatment modality for this lesion, the use of intralesional injections of steroids has been recently advocated for its treatment. In addition to this conservative management, the use of fine needle aspiration cytology (FNAC) for diagnosing CGCGs has been proven a safe and efficient approach, especially useful in cases with lesions located in esthetic regions. Herein, it is described a case of CGCG extending to the overlying gingiva of a 15-year-old male patient diagnosed by FNAC and subsequently treated with intralesional injections of a solution of triamcinolone acetonide and ethanolamine oleate that led to an important clinical remission, allowing a more conservative surgical procedure for preservation of gingival esthetics. Therefore, both procedures can be considered as management options for CGCG of the jaws.

O granuloma central de células gigantes (GCCG) é uma lesão benigna dos maxilares predominantemente encontrada na mandíbula de pacientes jovens do sexo feminino com um variado comportamento clínico. Apesar de o manejo cirúrgico representar a principal modalidade terapêutica para esta lesão, o uso de injeções intralesionais de esteróides tem sido recentemente proposto para seu tratamento. Além do manejo conservador, o uso da punção aspirativa por agulha fina (PAAF) para o diagnóstico do GCCG tem sido comprovado ser uma abordagem segura e eficiente, especialmente útil em casos de lesões localizadas em regiões estéticas. Descrevemos aqui um caso de GCCG estendendo-se para a gengiva adjacente em um paciente do sexo masculino, 15 anos de idade, diagnosticado por meio da PAAF e subsequentemente tratado com injeções intralesionais de uma solução de acetato de triancinolona e oleato de etanolamina que levou a uma importante remissão clínica, permitindo a realização de uma abordagem cirúrgica conservadora preservando a estética periodontal. Por este motivo, ambos os procedimentos podem ser considerados opções de manejo para o GCCG dos maxilares.

Pulmonary function changes after ethanolamine oleate injection VS band ligation in the treatment of esophageal varices

Introduction: The complications of injection sclerotherapy can be divided broadly into two categories, those occurring at the site of injection and those resulting from systemic dissemination of the sclerosant through the paraesophageal and azygos veins; this has been shown radiologically. Endoscopic variceal ligation [EVL] was developed as an alternative endoscopic method of treating esophageal varices with the anticipation that EVL would be as effective as EIS, but with fewer complications. We aimed in this study to assess the safety of both procedures for the lung

Patients and methods: We studied 28 patients with chronic liver disease and portal hypertension, 14 patients underwent injection sclerotherapy of ethanolamine oleate and the other 14 underwent band ligation. All patients underwent spirometery and ABG pre, 2 days and 3 weeks from the procedures

Results: Two days after the procedures the PEF and FEF 50 decreased highly significantly in EST patients when compared to EBL patients [P value less than 0.001], and FEV1, FVC, FEF25, FEF75, Pao2 and o2 sat decreased significantly in the same group by a P value of less than 0.05. After 3 weeks from the procedures the VCin, VCex, FEV1, FVC and FEF25 decreased highly significantly in the EST group [P value was less than 0.001], and the FEF 50, PEF, PACO2, PAO2 and O2 SAT decreased significantly in the same group. And there was a significant decrease of flow, FEV1 and FVC 2 days after the EST group with a highly significant decrease of PAO2 and O2SAT when compared to the same patients before the EST and we found a highly significant decrease of VC, FEV1, FVC, PAO2 and O2 SAT pre and 3 weeks from EST

Conclusions: From this study we conclude that the band ligation is safe for the lung and may be an option to eradicate esophageal varices in chronic lung disease patients

The Role of Divided Injections of a Sclerotic Agent over Two Days in Balloon-Occluded Retrograde Transvenous Obliteration for Large Gastric Varices

OBJECTIVE: To determine the safety and usefulness of a two-tiered approach to balloon-occluded retrograde transvenous obliteration (B-RTO) as a treatment for large gastric varices after portal hypertension. MATERIALS AND METHODS: 50 patients were studied who underwent B-RTO for gastric varices between October 2004 and October 2011 in our institution. The B-RTO procedure was performed from the right femoral vein and the B-RTO catheter was retained until the following morning. Distribution of sclerotic agents in the gastric varices on fluoroscopy was evaluated in all patients on days 1 and 2. When distribution of sclerotic agents in the gastric varices on day 1 had been none or very scanty even though the volume of the sclerotic agent infused was above the acceptable level, a second infusion was administered on day 2. When distribution was satisfactory, the B-RTO catheter was removed. RESULTS: In 8 (16%) patients, little or no sclerotic agent infused on day 1 was distributed in the gastric varices. However, on day 2, sclerotic agents were distributed in all gastric varices. Mean volume of ethanolamine oleate-iopamidol infused on day 1 was 24.6 mL and was 19.4 mL on day 2. Gastric varices were well obliterated with no recurrence. Complications caused by the sclerotic agent such as pulmonary edema or renal insufficiencies were not seen. CONCLUSION: When gastric varices are very large, a strategy involving thrombosis of only the drainage vein on the first day followed by infusing the sclerotic agent on the following day might be effective and feasible.

Preparation of self-microemulsion drug delivery system of the mixture of paeonol and borneol based on Xingbi Fang / 药学学报

The aim of this study is to prepare self-microemulsifying drug delivery system (SMEDDS) of the mixture of paeonol (Pae) and borneol (Bor). Solubility test, ternary phase diagrams and simplex lattice method were employed to screen and optimize the formulation of the mixture of Pae and Bor-loaded SMEDDS. After formed into microemulsions, the particle diameter (PD) was determined and a TEM was employed to observe the microemulsions' morphology. The contents of Pae and Bor were determined by gas chromatography. As a result, while ethyl oleate (EO) as the oil phase, cremophor EL35 (EL35) as surfactant and Transcutol HP (HP) as cosurfactant, the range of the microemulsion on the ternary phase diagram was larger than other combinations. And at a ratio of 20:45:35, the microemulsions' PD was about 34 nm and the polydispersity index (PI) was about 0.2. There were 16% of Pae, 2% of Bor, 16% of EO, 37% of EL35 and 29% of HP in the prepared SMEDDS. The preparation process of the Pae and Bor-loaded SMEDDS based on Xingbi Fang is simple and feasible. This study provides a reference for the researches on the related traditional Chinese medicine and the related components.

Modulation of Antibody Responses against Gnathostoma spinigerum in Mice Immunized with Crude Antigen Formulated in CpG Oligonucleotide and Montanide ISA720

This study aimed to investigate the antibody responses in mice immunized with Gnathostoma spinigerum crude antigen (GsAg) incorporated with the combined adjuvant, a synthetic oligonucleotide containing unmethylated CpG motif (CpG ODN 1826) and a stable water in oil emulsion (Montanide ISA720). Mice immunized with GsAg and combined adjuvant produced all antibody classes and subclasses to GsAg except IgA. IgG2a/2b/3 but not IgG1 subclasses were enhanced by immunization with CpG ODN 1826 when compared with the control groups immunized with non-CpG ODN and Montanide ISA or only with Montanide ISA, suggesting a biased induction of a Th1-type response by CpG ODN. After challenge infection with live G. spinigerum larvae, the levels of IgG2a/2b/3 antibody subclasses decreased immediately and continuously, while the IgG1 subclass remained at high levels. This also corresponded to a continuous decrease of the IgG2a/IgG1 ratio after infection. Only IgM and IgG1 antibodies, but not IgG2a/2b/3, were significantly produced in adjuvant control groups after infection. These findings suggest that G. spinigerum infection potently induces a Th2-type biased response.

Evaluation of antimicrobial activity of extracts of Tibouchina candolleana (melastomataceae), isolated compounds and semi-synthetic derivatives against endodontic bacteria

This work describes the phytochemical study of the extracts from aerial parts of Tibouchina candolleana as well as the evaluation of the antimicrobial activity of extracts, isolated compounds, and semi-synthetic derivatives of ursolic acid against endodontic bacteria. HRGC analysis of the n-hexane extract of T. candolleana allowed identification of b-amyrin, a-amyrin, and b-sitosterol as major constituents. The triterpenes ursolic acid and oleanolic acid were isolated from the methylene chloride extract and identified. In addition, the flavonoids luteolin and genistein were isolated from the ethanol extract and identified. The antimicrobial activity was investigated via determination of the minimum inhibitory concentration (MIC) using the broth microdilution method. Amongst the isolated compounds, ursolic acid was the most effective against the selected endodontic bacteria. As for the semi-synthetic ursolic acid derivatives, only the methyl ester derivative potentiated the activity against Bacteroides fragilis.

Sclerotherapy of Multiple Intraoral Venous Malformations with Use of Ethanolamine Oleate: A Case Report

Expression of connexin 43 and functional modulation of gap junction in neonatal rat astrocytes in vitro / 南方医科大学学报

<p><b>OBJECTIVE</b>To determine the expression of connexin 43 (Cx43) protein and explore the functional modulation of gap junction intercellular communication in astrocytes.</p><p><b>METHODS</b>Cultured neonatal SD rat astrocytes were divided into normal control group, all-trans retinoic acid (ATRA) group (treated with 10 µmol/L ATRA for 24 h) and oleamide group (treated with 25 µmol/L oleamide for 2 h). Western blotting and immunofluorescence assay were used to detect total cellular Cx43 protein expression and Cx43 expression on the surface of the astrocytes, respectively. Parachute assay was used to evaluate the functional changes of gap junction intercellular communication of the astrocytes.</p><p><b>RESULTS</b>Compared with the normal control cells, ATRA treatment resulted in a significantly increased expression of total Cx43 protein in the astrocytes (P<0.01), and oleamide significantly suppressed its expression (P<0.01). Similarly, ATRA obviously enhanced while oleamide suppressed Cx43 protein expression on the surface of the astrocytes. The gap junction intercellular communication of the astrocytes was enhanced by ATRA (P<0.01) and inhibited by oleamide (P<0.01).</p><p><b>CONCLUSION</b>ATRA and oleamide can modulate gap junction intercellular communication of the astrocytes possibly by regulating the expression of Cx43 protein.</p>

Development of Thrombus in a Systemic Vein after Balloon-Occluded Retrograde Transvenous Obliteration of Gastric Varices

OBJECTIVE: To retrospectively evaluate the frequency and risk factors for developing thrombus in a systemic vein such as the infrarenal inferior vena cava or the iliac vein, in which a balloon-occluded retrograde transvenous obliteration (B-RTO) catheter was indwelled. MATERIALS AND METHODS: Forty-nine patients who underwent B-RTO for gastric varices were included in this study. The B-RTO procedure was performed from the right femoral vein, and the B-RTO catheter was retained overnight in all patients. Pre- and post-procedural CT scans were retrospectively compared in order to evaluate the development of thrombus in the systemic vein in which the catheter was indwelled. Additionally, several variables were analyzed to assess risk factors for thrombus in a systemic vein. RESULTS: In all 49 patients (100%), B-RTO was technically successful, and in 46 patients (94%), complete thrombosis of the gastric varices was achieved. In 6 patients (12%), thrombus developed in the infrarenal inferior vena cava or the right common-external iliac vein. All thrombi lay longitudinally on the right side of the inferior vena cava or the right iliac vein. One of the aforementioned 6 patients required anticoagulation therapy. No symptoms suggestive of pulmonary embolism were observed. Prothrombin time-international normalized ratio and the addition of 5% ethanolamine oleate iopamidol, on the second day, were related to the development of thrombus. CONCLUSION: Development of a thrombus in a systemic vein such as the inferior vena cava or iliac vein, caused by indwelling of the B-RTO catheter, is relatively frequent. Physicians should be aware of the possibility of pulmonary embolism due to iliocaval thrombosis.

Bronchoscopic Ethanolamine Injection Therapy in Patients with Persistent Air Leak from Chest Tube Drainage / 결핵및호흡기질환

BACKGROUND: Chest tube drainage (CTD) is an indication for the treatment of pneumothorax, hemothroax and is used after a thoracic surgery. But, in the case of incomplete lung expansion, and/or persistent air leak from CTD, medical or surgical thoracoscopy or, if that is unavailable, limited thoracotomy, should be considered. We evaluate the efficacy of bronchoscopic injection of ethanolamine to control the persistent air leak in patients with CTD. METHODS: Patients who had persistent or prolonged air leak from CTD were included, consecutively. We directly injected 1.0 mL solution of 5% ethanolamine oleate into a subsegmental or its distal bronchus, where it is a probable air leakage site, 1 to 21 times using an injection needle through a fiberoptic bronchoscope. RESULTS: A total of 15 patients were enrolled; 14 cases of spontaneous pneumothorax [idiopathic 9, chronic obstructive pulmonary disease (COPD) 3, post-tuberculosis 2] and one case of empyema associated with broncho-pleural fistula. Of these, five were patients with persistent air leak from CTD, just after a surgical therapy, wedge resection with plication for blebs or bullae. With an ethanolamine injection therapy, 12 were successful but three (idiopathic, COPD and post-tuberculosis) failed, and were followed by a surgery (2 cases) or pleurodesis (1 case). Some adverse reactions, such as fever, chest pain and increased radiographic opacities occurred transiently, but resolved without any further events. With success, the time from the procedure to discharge was about 3 days (median). CONCLUSION: Bronchoscopic ethanolamine injection therapy may be partially useful in controlling air leakage, and reducing the hospital stay in patients with persistent air leak from CTD.

Enhanced bioavailability of total paeony glycoside by self-microemulsifying drug delivery system / 药学学报

Total paeony glycoside (TPG) is extracted and purified from a traditional Chinese herbal medicine. It has many biological and pharmacological activities. However, there are few dosage forms of TPG in the market because of its low bioavailability. Self-microemulsifying drug delivery system (SMEDDS) is a vital tool in solving low bioavailability of poor absorption drugs. So the objective of this study is to develop a new TPG-SMEDDS for the oral delivery of poorly soluble TPG. Through the construction of pseudo-ternary phase diagrams, the optimum prescription was obtained, which consisted of 18.70% TPG, 16.27% ethyl oleate as oil, 43.34% Cremophor RH40 as surfactant and 21.73% Transcutol P as cosurfactant. The characterizations of TPG-SMEDDS including morphological characterization, droplet size, zeta-potential, emulsification time, and dissolution study of TPG-SMEDDS were evaluated. The results showed that TPG-SMEDDS is stable and its release rate is high in four different media (0.1 mol x L(-1) HCl, pH 6.8 PBS, pH 7.4 PBS, and water). The relative bioavailability of SMEDDS was dramatically enhanced in an average of 1.52-fold that of TPG-suspension. It is concluded that the bioavailability of TPG is enhanced greatly by SMEDDS.

Berberine potentizes apoptosis induced by X-rays irradiation probably through modulation of gap junctions / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Clinical combination of some traditional Chinese medical herbs, including berberine, with irradiation is demonstrated to improve efficacy of tumor radiotherapy, yet the mechanisms for such effect remain largely unknown. The present study investigated the effect of berberine on apoptosis induced by X-rays irradiation and the relation between this effect and gap junction intercellular communication (GJIC).</p><p><b>METHODS</b>The role of gap junctions in the modulation of X-rays irradiation-induced apoptosis was explored by manipulation of connexin (Cx) expression, and gap junction function, using oleamide, a GJIC inhibitor, and berberine.</p><p><b>RESULTS</b>In transfected HeLa cells, Cx32 expression increased apoptosis induced by X-rays irradiation, while inhibition of gap junction by oleamide reduced the irradiation responses, indicating the dependence of X-rays irradiation-induced apoptosis on GJIC. Berberine, at the concentrations without cytotoxicity, enhanced apoptosis induced by irradiation only in the presence of functional gap junctions.</p><p><b>CONCLUSIONS</b>These results suggest that berberine potentizes cell apoptosis induced by X-rays irradiation, probably through enhancement of gap junction activity.</p>

Tissue distribution of s-oleylpropanolamide in rats detected by liquid chromatography with tandem mass spectrometry / 药学学报

This paper is to report the development of a rapid and sensitive method for the determination of s-oleylpropanolamide (OPA) in various tissues of rat (brain, heart, lung, liver, spleen, small intestine, kidney, adipose tissue and muscle), and to assess the applicability of the assay to tissue distribution. OPA was extracted by liquid-liquid extraction method with undecylenoylethanolamide as an internal standard. The concentrations of OPA were determined by LC-MS/MS after a single intragastric dose of 50 mg x kg(-1) at 4 time points (5 rats per group). With multiple reactions monitoring mode (MRM) the limit of quantification (LLOQ) was determined at 1 microg x L(-1). The calibration curve was linear from 1 to 2 x 104 microg x L(-1) (r > or = 0.999 0) for tissue homogenates. Validation parameters such as accuracy, precision and recovery were found to be within the acceptance criteria of the assay validation guidelines. The highest concentration was found in small intestine (the highest time point is 15 min) and heart (the highest time point is 90 min). The assay is rapid, sensitive and applicable to studying tissue distribution of OPA in rats.

Effects of ambroxol combined with low-dose heparin on TNF-alpha and IL-1beta in rabbits with acute lung injury / 中国应用生理学杂志

<p><b>OBJECTIVE</b>To investigate the intervention and mechanism of ambroxol combined with low-dose heparin on oxidative stress, TNF-alpha and IL-1beta in rabbits with acute lung injury (ALI).</p><p><b>METHODS</b>Twenty-four healthy Japanese rabbits were randomly divided into three groups: (1) Normal saline control group (NC), (2) Oleic acid injury group (OA), (3) Ambroxol + low-dose heparin therapy group (AH). After the success of ALI model, AH group was injected ambroxol + low-dose heparin, while the NC group and OA group were injected the same dose of normal saline by the same method. Arterial oxygen tension (PaO2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta) at different time points were determined. The pathological manifestation of both side lungs was observed at the end of expeiment. The activity of glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), xanthine oxidase (XO) and the content of malondialdehyde (MDA) in bronchoalveolar lavage fluid (BALF) and lung tissue homogenate were tested. The apoptosis index was detected. The lung wet/dry (W/D) ratio was calculated. The pathological changes in lung tissue were observed by light microscopy, and the ultrastructural changes of lung tissue were observed by electron microscopy.</p><p><b>RESULTS</b>(1) The instructive injury induced by ALI observed under electron microscope and light microscope and W/D was decreased significantly in AH group. (2) PaO2 was improved significantly in AH group, compared with that in OA group (P < 0.01). (3) The activity of GSH-Px and SOD in AH group increased significantly (P < 0.01 or P < 0.05) but the activity of XO and the content of MDA decreased significantly (P < 0.01), compared with those in OA group. (4) Except the content of IL-1beta in serum before treatment, the content of IL-1beta and TNF-alpha in serum, BALF, lung tissue homogenate of OA group increased significantly (P < 0.01), and those were obviously improved in AH group. (5) Apoptosis index (AI) in AH group decreased significantly (P < 0.01) compared with that in OA group.</p><p><b>CONCLUSION</b>In ALI induced by OA, IL-1beta and TNF-alpha increases significantly and involved in the occurrence and development of ALI. Ambroxol combined with low-dose heparin can reduce lung cells oxidative stress to inhibit the release of IL-1beta and TNF-alpha, which play a role in the treatment of ALI.</p>