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1.
Br J Surg ; 99(4): 541-8, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22139553

RESUMO

BACKGROUND: Resuscitative emergency thoracotomy (ET) is performed as a salvage manoeuvre for selected patients with trauma. However, reports from European trauma centres are scarce. METHODS: A retrospective analysis was undertaken of injured patients who underwent resuscitative ET in the emergency department (ED) or operating room (OR) between January 1996 and September 2008. Survival in the ED and to hospital discharge was analysed using logistic regression. RESULTS: During the study interval 121 patients required a resuscitative thoracotomy, of which 49 (40·5 per cent) were performed in the ED and 72 (59·5 per cent) in the OR. Patients in the OR had higher blood pressure on arrival (median 110 versus 60 mmHg; P < 0·001), were less often in severe haemorrhagic shock (63 versus 94 per cent; P < 0·001), had fewer serious head injuries (Abbreviated Injury Score of 3 or above in 33 versus 53 per cent; P = 0·031) and more often had a penetrating stab wound as the dominating mechanism (25 versus 10 per cent; P = 0·042) compared with those in the ED. Ten patients (20 per cent) survived to hospital discharge after ED thoracotomy, compared with 53 (74 per cent) of those treated in the OR. Penetrating injury and Glasgow Coma Scale score above 8 were independent predictors of hospital survival following ED thoracotomy. No patient with a blunt injury and no detectable signs of life on admission survived. Three of 26 patients with blunt trauma and signs of life on admission survived to hospital discharge. CONCLUSION: Resuscitative ET may be life-saving in selected patients. Location of the procedure is dictated by injury severity and vital parameters. Outcome is best when signs of life are present on admission, even for blunt injuries.


Assuntos
Ressuscitação/métodos , Toracotomia/métodos , Ferimentos não Penetrantes/cirurgia , Ferimentos Penetrantes/cirurgia , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Emergências/epidemiologia , Serviço Hospitalar de Emergência/estatística & dados numéricos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Salas Cirúrgicas/estatística & dados numéricos , Ressuscitação/mortalidade , Estudos Retrospectivos , Suíça/epidemiologia , Toracotomia/mortalidade , Toracotomia/estatística & dados numéricos , Centros de Traumatologia/estatística & dados numéricos , Ferimentos não Penetrantes/mortalidade , Ferimentos Penetrantes/mortalidade , Adulto Jovem
2.
J Bone Joint Surg Br ; 88(10): 1394-400, 2006 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-17012435

RESUMO

Systemic factors are believed to be pivotal for the development of heterotopic ossification in severely-injured patients. In this study, cell cultures of putative target cells (human fibroblastic cells, osteoblastic cells (MG-63), and bone-marrow stromal cells (hBM)) were incubated with serum from ten consecutive polytraumatised patients taken from post-traumatic day 1 to day 21 and with serum from 12 healthy control subjects. The serum from the polytraumatised patients significantly stimulated the proliferation of fibroblasts, MG-63 and of hBM cells. The activity of alkaline phosphatase in MG-63 and hBM cells was significantly decreased when exposed to the serum of the severely-injured patient. After three weeks in 3D cell cultures, matrix production and osteogenic gene expression of hBM cells were equal in the patient and control groups. However, the serum from the polytraumatised patients significantly decreased apoptosis of hBM cells compared with the control serum (4.3% vs 19.1%, p = 0.031). Increased proliferation of osteoblastic cells and reduced apoptosis of osteoprogenitors may be responsible for increased osteogenesis in severely-injured patients.


Assuntos
Apoptose/fisiologia , Células do Tecido Conjuntivo/fisiologia , Ferimentos e Lesões/fisiopatologia , Adulto , Fosfatase Alcalina/metabolismo , Medula Óssea/patologia , Divisão Celular/fisiologia , Células Cultivadas , Matriz Extracelular/patologia , Feminino , Fibroblastos/fisiologia , Expressão Gênica , Humanos , Escala de Gravidade do Ferimento , Peptídeos e Proteínas de Sinalização Intercelular/sangue , Masculino , Pessoa de Meia-Idade , Ossificação Heterotópica/patologia , Ossificação Heterotópica/fisiopatologia , Osteoblastos/fisiologia , Osteogênese/fisiologia , RNA Mensageiro/análise , Reação em Cadeia da Polimerase Via Transcriptase Reversa/métodos , Células Estromais/fisiologia , Ferimentos e Lesões/sangue , Ferimentos e Lesões/patologia
3.
Eur J Vasc Endovasc Surg ; 32(5): 589-95, 2006 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-16859935

RESUMO

OBJECTIVES: Prophylactic vena cava filters (VCF) are efficient in preventing pulmonary embolism. Filter retrieval avoids the potential long-term complications of permanent VCF. Clinical evaluation was focused on filter-related complications and feasibility of retrieval in high-risk trauma patients. METHODS: Analysis of single-institution consecutive case series of patients who received a prophylactic OptEase VCF after multiple trauma between 08/2003 and 12/2004. Data were collected prospectively. RESULTS: A total of 37 OptEase filters were inserted prophylactically after multiple trauma (median patient age 35 years, range, 17-73 years, median ISS 41, range, 17-59). All patients had contraindications for pharmacological prophylaxis for thromboembolic events. 32 filters (86%) were retrieved after 16 days (range, 7-25 days). 12 of 33 filters (36%) demonstrated trapped clots/thrombosis within the filter structure on pre-retrieval cavography. Two patients received anticoagulation before filter retrieval due to filter thrombosis (6%). Symptomatic PE was observed in 1 patient (3%) 5 days after VCF retrieval. Minor caudal filter migration was observed in 1 patient (3%). Overall mortality was 3%. CONCLUSIONS: Retrieval of the OptEase filter is safe and feasible. Temporary filter placement avoids possible long-term complications of permanent VCF. It is an efficient form of PE prophylaxis when temporary contraindications to anticoagulation are present.


Assuntos
Cateterismo , Remoção de Dispositivo , Traumatismo Múltiplo/terapia , Embolia Pulmonar/prevenção & controle , Filtros de Veia Cava , Adolescente , Adulto , Idoso , Segurança de Equipamentos , Estudos de Viabilidade , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Traumatismo Múltiplo/complicações , Guias de Prática Clínica como Assunto , Estudos Prospectivos , Embolia Pulmonar/etiologia , Radiografia Intervencionista , Medição de Risco , Fatores de Tempo , Resultado do Tratamento , Filtros de Veia Cava/efeitos adversos
4.
Ultraschall Med ; 27(5): 473-7, 2006 Oct.
Artigo em Alemão | MEDLINE | ID: mdl-16596505

RESUMO

AIM: The goal of our study was to assess the perfusion in wounds treated by vacuum assisted closure (VAC) compared to primary wound closure. METHOD: Power Doppler Ultrasound (PDUS) was carried out under standardised conditions in 15 VAC-treated and 10 primarily closed wounds as well as on altogether 25 intraindividual reference areas. All data were sent to a work station for post-processing to determine the perfused area. Statistical data analysis was performed with the Mann-Whitney test. RESULTS: Both VAC-treated wounds and primarily closed wounds showed a significant increase of the perfusion when compared to the intraindividual reference area (p < 0.0001). In VAC-treated wounds, a markedly increased perfusion was measured compared to the wounds closed primarily (p < 0.0001). Perfusion decreased during treatment, but in two VAC-treated wounds, an initial increase of the perfusion was observed. Both these wounds were grossly infected. CONCLUSION: PDUS allows the quantification of the differences in wound perfusion. This can be helpful in the detection of progressive local wound infections.


Assuntos
Ultrassonografia Doppler Dupla/métodos , Cicatrização , Ferimentos e Lesões/diagnóstico por imagem , Ferimentos e Lesões/terapia , Feminino , Humanos , Masculino , Perfusão , Resultado do Tratamento , Vácuo
5.
Zentralbl Chir ; 131 Suppl 1: S62-7, 2006 Apr.
Artigo em Alemão | MEDLINE | ID: mdl-16575647

RESUMO

OBJECTIVE: Clinical observations have shown an accelerated wound healing in wounds of patients treated by Vacuum Assisted Closure (V.A.C.)-therapy. The mechanisms of improved wound healing on cellular level have been hitherto less investigated. In this study the levels of proinflammatory interleukins (IL-6, IL-8, IL-10) and growth factors (VEGF, FGF-2) in serum and wound were monitored. METHODS: The study included 21 patients with traumatic wounds that could not be closed during the first surgical intervention. The soft tissue defects (n = 21) were closed temporarily by Epigard. During the first second-look operation after 2.0 +/- 0.2 days in an average, Epigard was used for another 2.5 +/- 0.4 days as temporary soft tissue coverage in 13 patients (group A). In the remaining 8 patients the wound conditioning was done by V.A.C.(R) for 2.4 +/- 0.3 days (group B). A total of 428 samples of serum and wound fluid samples were collected during the first and second look operation. Levels of IL-6, IL-8, IL-10, VEGF and FGF were measured specific by ELISA. RESULTS: In all interleukins and growth factors there were significant lower serum level concentrations compared with those in wound fluids. During the first temporary dressing change after wound coverage with Epigard the wound samples showed the following levels [Mean (SEM)]: IL-6 49 816 (19 889) pg/ml, IL-8 54 (16) ng/ml, IL-10 314 (44) pg/ml, VEGF 4 746 (766) pg/ml, FGF-2 494 (89) pg/ml. During the second dressing changes we monitored the following levels in group A: IL-6 7 218 (2 542) pg/ml, IL-8 69 (27) ng/ml, IL-10 261 (58) pg/ml, VEGF 3 551 (661) pg/ml, FGF-2 355 (67) pg/ml. In group B the samples of the wound fluid showed the following results: IL-6 16 966 (4 124) pg/ml [p = 0.02], IL-8 223 (91) ng/ml [p = 0.03], IL-10 233 (76) pg/ml [p = 0.38], VEGF 7 490 (1 565) pg/ml [p = 0.01], FGF-2 352 (43) pg/ml [p = 0.48]. CONCLUSION: The increased local release of IL-6, IL-8 and VEGF in wounds after V.A.C.-therapy may be involved in the accumulation of neutrophil granulocytes and angiogenesis, which seams to play a crucial role for the accelerated granulation tissue formation after V.A.C.-therapy compared to wounds treated by Epigard.


Assuntos
Fator 2 de Crescimento de Fibroblastos/sangue , Interleucina-10/sangue , Interleucina-6/sangue , Interleucina-8/sangue , Curativos Oclusivos , Lesões dos Tecidos Moles/cirurgia , Fator A de Crescimento do Endotélio Vascular/sangue , Síndromes Compartimentais/imunologia , Síndromes Compartimentais/cirurgia , Desbridamento , Líquido Extracelular/imunologia , Polímeros de Fluorcarboneto , Fraturas Expostas/imunologia , Fraturas Expostas/cirurgia , Humanos , Reoperação , Lesões dos Tecidos Moles/imunologia , Técnicas de Sutura , Vácuo
6.
Unfallchirurg ; 109(2): 156-9, 2006 Feb.
Artigo em Alemão | MEDLINE | ID: mdl-16391935

RESUMO

We present a patient with a closed displaced distal tibia fracture with entrapment of the anterior tibial vessels in the fracture after tibial nailing. This complication was initially not recognised. After several debridements of the forefoot on the same side due to open metatarsal fractures and severe soft tissue injury, a free latissimus dorsi flap was used for covering the dorsum pedis. Preoperative angiography showed occlusion of the anterior tibial artery at the fracture line which was interpreted as a secondary occlusion due to an intima lesion of the vessel after injury. The entrapment in the fracture line was recognised intra-operatively during the preparation of the anterior tibial vessel.


Assuntos
Traumatismos do Tornozelo/cirurgia , Arteriopatias Oclusivas/cirurgia , Traumatismos do Pé/cirurgia , Fixação Intramedular de Fraturas , Complicações Pós-Operatórias/cirurgia , Artérias da Tíbia/lesões , Fraturas da Tíbia/cirurgia , Idoso , Anastomose Cirúrgica , Angiografia , Traumatismos do Tornozelo/diagnóstico por imagem , Arteriopatias Oclusivas/diagnóstico por imagem , Síndromes Compartimentais/diagnóstico por imagem , Síndromes Compartimentais/cirurgia , Desbridamento , Traumatismos do Pé/diagnóstico por imagem , Antepé Humano/irrigação sanguínea , Antepé Humano/lesões , Antepé Humano/cirurgia , Fixação Interna de Fraturas , Humanos , Masculino , Complicações Pós-Operatórias/diagnóstico por imagem , Reoperação , Retalhos Cirúrgicos/irrigação sanguínea , Fraturas da Tíbia/diagnóstico por imagem
7.
Biomed Tech (Berl) ; 50(12): 413-8, 2005 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-16429946

RESUMO

The reproducibility of a V.A.C. (Vacuum Assisted Closure) instillation system was investigated by means of an in vitro model. The relation between the volume of a delivered solution and its removal from the system was studied in foams of various size. The relationship of instillation time periods and the volume of delivered solution was determined.


Assuntos
Antibacterianos/administração & dosagem , Desbridamento/instrumentação , Sistemas de Liberação de Medicamentos/instrumentação , Sucção/instrumentação , Infecção da Ferida Cirúrgica/terapia , Cicatrização , Ferimentos e Lesões/terapia , Desbridamento/métodos , Sistemas de Liberação de Medicamentos/métodos , Desenho de Equipamento , Análise de Falha de Equipamento , Modelos Biológicos , Sucção/métodos , Vácuo
8.
Zentralbl Chir ; 129 Suppl 1: S14-9, 2004 May.
Artigo em Alemão | MEDLINE | ID: mdl-15168276

RESUMO

OBJECTIVE: The problem of the temporary vacuum assisted closure (V.A.C.) of open abdomen situation is that the fluids, following the negative pressure, pass the abdominal cavity and in case of a local infection disseminate over the whole abdominal cavity. METHODS: The usual open abdominal wound V.A.C. technique was modified by using an auxiliary, independently operating V.A.C. system positioned intra-abdominally and connected with a separate drainage tube introduced into the lateral abdominal wall. This arrangement prevents further spreading of a local intra-abdominal infection in case of a necrotising pancreatitis after traumatic pancreas rupture. RESULTS: The drainage volumes were comparable from superficial and intra-abdominal V.A.C. system. A total of 30 reoperations were necessary due to a leasion of the pancreas before a primary closure of the open abdominal wound could be applied after 72 days. No bowel fistulas or intra-abdominal abscess formations were observed. The follow-up have not shown any hernia of the abdominal wall up to the present. CONCLUSION: Additional intra-abdominally positioned V.A.C. system with an own drainage system supports open abdomen therapy with the standard abdominal V.A.C. system and prevents dissemination of intra-abdominal infection.


Assuntos
Traumatismos Abdominais/cirurgia , Desbridamento/instrumentação , Curativos Oclusivos , Pâncreas/lesões , Pancreatite Necrosante Aguda/cirurgia , Peritonite/cirurgia , Infecção da Ferida Cirúrgica/cirurgia , Técnicas de Sutura/instrumentação , Parede Abdominal/cirurgia , Adulto , Desenho de Equipamento , Feminino , Humanos , Microcomputadores , Traumatismo Múltiplo/cirurgia , Pancreatectomia , Reoperação , Cirurgia Assistida por Computador/instrumentação , Vácuo , Cicatrização/fisiologia
9.
Swiss Surg ; 9(2): 69-75, 2003.
Artigo em Alemão | MEDLINE | ID: mdl-12723286

RESUMO

The intramedullary Kirschner wire fixation of distal metacarpal fractures reported by Foucher et al. combines the known advantages of intramedullary implants with a reduction of iatrogenic soft tissue trauma. We applied this minimal invasive internal fixation technique in 38 patients with fractures dislocated by more than 20 degrees and/or with rotatory deformity. After opening the intramedullary cavity from the base of the respective metacarpal bone and after fracture reduction, two pre-bent Kirschner wires were intramedullary inserted in an orthograde fashion. The pre-bent distal end of the wire in the form of a hockey club allows an additional closed reduction of the displaced distal fracture fragment. Intraoperative complications did not occur. A fixation in a plaster splint followed for one week only. The elastic fixation of the wires working as springs is stable enough to allow physiotherapeutic exercises. After the third postoperative week, the intensity of physical exercise was increased. 36 of the 38 patients were followed. With one exception, all fractures were healed in a proper position. The wires were removed under local anaesthesia on an outpatient basis after six to eight weeks and full mobility of the fingers was achieved in 34 patients at that time. Complications included one redislocation and one distal wire perforation.


Assuntos
Fios Ortopédicos , Fixação Intramedular de Fraturas/instrumentação , Metacarpo/lesões , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Seguimentos , Consolidação da Fratura/fisiologia , Humanos , Masculino , Metacarpo/diagnóstico por imagem , Metacarpo/cirurgia , Pessoa de Meia-Idade , Complicações Pós-Operatórias/etiologia , Radiografia , Instrumentos Cirúrgicos , Resultado do Tratamento
10.
Swiss Surg ; 8(6): 266-72, 2002.
Artigo em Alemão | MEDLINE | ID: mdl-12520846

RESUMO

Within the scope of a retrospective study, the efficiency of the vacuum sealing technique, a recent alternative to methods used in treatment of both chronic or acute infected wounds and acute traumatic soft tissue defects, was evaluated in 120 patients in the period between January 1995 and November 1997. The vacuum sealing technique offers an effective therapeutic option for the temporary closure of defect as well as of infected wounds, decreases the risk of wound infection and offers advantage regarding patient's comfort and hospital hygiene.


Assuntos
Fraturas Expostas/terapia , Curativos Oclusivos , Úlcera por Pressão/terapia , Lesões dos Tecidos Moles/terapia , Infecção dos Ferimentos/terapia , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Retrospectivos , Sucção , Cicatrização/fisiologia
11.
Arch Surg ; 135(7): 849-53, 2000 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-10896381

RESUMO

HYPOTHESIS: Telemedicine for real-time transmission of clinical documents and interactive remote telediagnosis allows accurate clinical application in surgery. DESIGN: Prospective cohort study in which 2 hospitals, 120 miles apart, were connected via integrated services digital network (ISDN) teleconferencing units, and each evaluated clinical cases in real time. SETTING: A tertiary care university hospital and primary care county hospital. PARTICIPANTS: Between May 1, 1998, and June 30, 1998, 112 patients undergoing digestive or endocrine surgery were evaluated by teletransmission (study group) and direct vision (control group). Diagnosis had to be known by the viewer, and either conventional magnetic resonance imaging or computed tomographic scans were available. MAIN OUTCOME MEASURES: Picture quality, organ structure, and pathologic finding viewed on telemedicine documents were evaluated by radiologists and surgeons blind to diagnosis. Accuracy of remote 128-kilobit (kb)/s transmission-rate diagnoses and results were compared with those obtained directly. RESULTS: Picture quality was "good" or "excellent" in 92.9% of transmitted documents and 95.5% of live images (P>.4). The target organ was always recognized, structure and pathologic finding were analyzable in 98.2% of transmitted documents and 99.1% of live documents, and fine structures were assessable in 89.3% of transmitted pictures and 95.5% of live pictures (P>.05). Diagnosis was made in 84.8% of transmitted cases and 93.8% of live cases (P = .02). CONCLUSIONS: Low bandwidth (128 kb/s) telemedicine application in surgery is reliable in evaluating remote cases. Loss of image quality through teletransmission occurred in 2.7% of cases, and diagnosis was not possible in 15.2% of transmitted vs 6.2% of live cases, suggesting factors other than technical quality (choice of radiological studies, additional clinical information required, etc). This underscores the importance of real-time interactive discussion during surgical teleconferences.


Assuntos
Diagnóstico , Procedimentos Cirúrgicos Operatórios , Telemedicina , Estudos de Coortes , Interpretação Estatística de Dados , Humanos , Imageamento por Ressonância Magnética , Estudos Prospectivos , Reprodutibilidade dos Testes , Procedimentos Cirúrgicos Operatórios/estatística & dados numéricos , Suíça , Telemedicina/instrumentação , Telemedicina/organização & administração , Telemedicina/normas , Telemedicina/estatística & dados numéricos , Tomografia Computadorizada por Raios X
13.
J Med Chem ; 37(23): 3889-901, 1994 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-7966150

RESUMO

Thrombin, a serine protease, plays a central role in the initiation and propagation of thrombotic events. An extensive search for new thrombin inhibitors was performed, using an unconventional approach. Screening of small basic molecules for binding in the recognition pocket of thrombin led to the discovery of (aminoiminomethyl)piperidine (amidinopiperidine) as a weak, but intrinsically selective, thrombin inhibitor. Elaboration of this molecule provided compounds which inhibit thrombin with Ki's in the range of 20-50 nM and with selectivities of 1000-4000 against trypsin. These inhibitor compounds show a new and unexpected binding mode to thrombin. Modification of the central building block and then of one of the hydrophobic substituents led to the discovery of a new family of thrombin inhibitors which has reverted to the former binding mode to thrombin. This last class of compounds shows inhibitory activities in the picomolar range, low toxicity, and a short plasma half life which favors its use for an intravenous application. From this series of thrombin inhibitors, 19f(Ro 46-6240) was selected for clinical development as an antithrombotic agent for intravenous administration.


Assuntos
Antitrombinas/síntese química , Piperidinas/síntese química , Aminoácidos/química , Aminoácidos/farmacologia , Animais , Antitrombinas/farmacologia , Ácido Aspártico/síntese química , Ácido Aspártico/farmacologia , Desenho de Fármacos , Meia-Vida , Humanos , Piperidinas/farmacologia , Ratos , Relação Estrutura-Atividade , Inibidores da Tripsina/farmacologia
14.
J Pharmacol Exp Ther ; 237(3): 837-40, 1986 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-3754894

RESUMO

We have shown previously that the 3-beta-D-glucopyranosides of vitamin D3, 1 alpha-hydroxyvitamin D3, 1,25-dihydroxyvitamin D3 and 25-hydroxyvitamin D3 are biologically active in vivo. In order to determine whether the presence of the beta-D-glucopyranoside moiety linked to either the C-3, the C-25 or the C-1 hydroxyl function of the molecule affected the biological activity of the conjugates 1, 2, or 3 derived from 1,25-dihydroxyvitamin D3, we administered increasing amounts of compounds to vitamin D-deficient rats maintained on a low calcium diet. The aglycone, 1,25-dihydroxyvitamin D3 (4), also was administered to another group of such animals. When administered i.v., all three beta-D-glucopyranosides increased intestinal calcium transport in doses as low as 50 pmol/rat. A dose of approximately 500 pmol/rat was required to increase bone calcium mobilization in these same animals. The three glucosides were found to be equally active in both biological responses. A dose of only 5 pmol of 1,25-dihydroxyvitamin D3 (4) increased both intestinal calcium transport and bone calcium mobilization. We also performed similar experiments after the p.o. administration of these compounds to vitamin D-deficient rats maintained on a low calcium diet. The glucopyranosides 1, 2 and 3 were able to increase calcium transport in the intestine, as well as mobilize bone calcium at doses of between 500 and 5000 pmol/rat. Once again, the compounds were equipotent, but were less active than 1,25-dihydroxyvitamin D3 (4). After the i.v. or p.o. doses of the glucosides, plasma concentrations of 1,25-dihydroxyvitamin D3 increased in a dose-dependent manner. We conclude that: The C-3, C-25 and C-1 beta-D-glucopyranosides of 1,25-dihydroxyvitamin D3 are biologically active and equipotent in vivo, most likely as a result of hydrolysis to the free aglycone and they are less active than the aglycone in this respect.


Assuntos
Calcitriol/farmacologia , Glucosídeos/farmacologia , Glicosídeos/farmacologia , Administração Oral , Animais , Transporte Biológico/efeitos dos fármacos , Calcitriol/análogos & derivados , Calcitriol/sangue , Cálcio/metabolismo , Relação Dose-Resposta a Droga , Injeções Intravenosas , Mucosa Intestinal/metabolismo , Masculino , Ratos
15.
J Pharmacol Exp Ther ; 234(1): 25-9, 1985 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-2989506

RESUMO

Polar glycosidic conjugates of vitamin D compounds occur in the vegetable and possibly in the animal kingdom. The biologic activity of these conjugates has not been examined systematically. To obtain more information on the biological role of such sterol conjugates, we examined the biological activity of the 3beta-D-glucopyranosyl conjugates of vitamin D3 5, 25-hydroxyvitamin D3 6, 1alpha-hydroxyvitamin D3 7 and 1alpha,25-dihydroxyvitamin D3 8. When these compounds were administered i.v. we found that a dose of between 50 and 500 pmol/rat of the four glucopyranosides tested increased active intestinal calcium transport and increased bone calcium mobilization in vitamin D-deficient rats fed a low calcium diet. Under the same conditions, corresponding doses of the parent vitamin D3 compounds elicited comparable increases in both intestinal calcium transport and bone calcium mobilization. When these compounds were administered p.o. 3beta-D-glucopyranosyl vitamin D3 5 exhibited no biological activity at doses of up to 5000 pmole/rat, whereas the corresponding glycosides of 25-hydroxyvitamin D3 6, 1alpha-hydroxyvitamin D3 7 and 1,25-dihydroxyvitamin D3 8 were active at doses of 500 to 1000 pmol/rat in the intestinal calcium transport system. When the glucopyranosyl conjugates were administered i.v. to vitamin D-deficient rats, 25-hydroxyvitamin D3 and 1alpha,-25-dihydroxyvitamin D3 were detected in the serum at levels less than or equal to those noted in animals dosed with the respective free sterols.


Assuntos
Colecalciferol/farmacologia , Glicosídeos/farmacologia , Animais , Osso e Ossos/metabolismo , Cálcio/metabolismo , Relação Dose-Resposta a Droga , Mucosa Intestinal/metabolismo , Masculino , Ratos
16.
Int J Vitam Nutr Res ; 55(3): 263-7, 1985.
Artigo em Inglês | MEDLINE | ID: mdl-3841093

RESUMO

The biological activity of the three mono-beta-D-glucopyranosides (mono-glucosides) of 1,25-dihydroxycholecalciferol [1,25(OH)2D3] synthesized chemically has been studied in chicks and Japanese quails. While the 1- and the 3-glucoside showed no or only little effect on serum calcium, bone weight, calcium binding protein (CaBP) or calcium deposition in the egg shell, the 25-glucoside was found to be more than half as active as the aglycone 1,25(OH)2D3. The bioactivity of this glucoside parallels a higher binding constant to the intestinal 1,25(OH)2D3 receptor compared to those of the two other glucosides.


Assuntos
Calcitriol/análogos & derivados , Animais , Anexina A6 , Osso e Ossos/efeitos dos fármacos , Calcitriol/farmacologia , Cálcio/sangue , Proteínas de Ligação ao Cálcio/metabolismo , Galinhas , Coturnix , Casca de Ovo , Feminino , Masculino , Raquitismo/tratamento farmacológico , Equivalência Terapêutica
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