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1.
Ann Coloproctol ; 39(1): 41-49, 2023 Feb.
Article in English | MEDLINE | ID: mdl-34879637

ABSTRACT

PURPOSE: Rubber band ligation (RBL) for grade 1 to 3 internal hemorrhoids is a well-established modality of choice. But RBL is also a kind of surgical treatment; it is not free from complications (e.g., delayed bleeding [DB], rectal stenosis). This study aimed to investigate the results of the comparative treatment of RBL and BANANA-Clip (BC; Endovision). METHODS: Study participants were 632 consecutive patients with grade 1 to 3 internal hemorrhoids attended to Department of Colorectal Surgery at Wellness Hospital between January 2010 and May 2019. We retrospectively reviewed the incidence rate of complications, including DB between RBL and BC. RESULTS: There were 304 male and 328 female patients, whose ages ranged from 15 to 84 years, with a mean age of 45.7 years. The common symptom and cause of treatment was prolapse (70.1%). The number of ligated sites was 1.49±0.57 in the RBL group and 1.99±0.77 in the BC group. RBL showed a significantly higher incidence of DB (3.5%) compared to BC (0%) (P=0.001). The 1-year success rate was 95.9% in the RBL group and 99.7% in the BC group (P=0.005). CONCLUSION: In our study, BC was more reliable in treating grade 1 to 3 internal hemorrhoids with higher success rates and less post-ligation complications, especially DB, compared to RBL.

2.
Anticancer Drugs ; 19(9): 859-70, 2008 Oct.
Article in English | MEDLINE | ID: mdl-18766000

ABSTRACT

The effects of 1-(biphenyl-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol (EDL-155) on the growth of glioma was tested in vitro and in vivo. Normal cultured rat astrocytes and C6 rat glioma were used as a differential screen to test the effects of EDL-155. The compound was preferentially cytotoxic for C6 glioma (EC50=1.5 micromol/l) relative to cultured neonatal astrocytes (EC50=27.4 micromol/l). When compared with a standard chemotherapeutic agent, carmustine (1,3-bis[2-chloroethyl]-1-nitrosourea), or temozolomide, EDL-155 was more selective and more potent in our differential tissue culture assay. The effect of EDL-155 was also tested in an animal model in which C6 glioma was transplanted into the brains of Sprague-Dawley rats. EDL-155 was delivered directly onto the tumor by an osmotic minipump directly into the brain or by intraperitoneal injection. Animals treated with EDL-155 had significantly smaller tumors than did control animals treated with carrier solution. We observed anatomical changes in cultured glioma cells treated with EDL-155 that were consistent with selective destruction of mitochondria and the induction of autophagy. These changes were not observed in normal astrocytes cultured from rat pups. The selective killing of glioma in tissue culture and in the rat brain models indicates that EDL-155 has potential therapeutic value in treating this type of brain cancer.


Subject(s)
Antineoplastic Agents/therapeutic use , Brain Neoplasms/drug therapy , Glioma/drug therapy , Tetrahydroisoquinolines/therapeutic use , Animals , Astrocytes/drug effects , Carmustine/therapeutic use , Cell Line, Tumor , Dacarbazine/analogs & derivatives , Dacarbazine/therapeutic use , Disease Models, Animal , Drug Evaluation, Preclinical , Male , Rats , Rats, Sprague-Dawley , Temozolomide , Tissue Culture Techniques , Xenograft Model Antitumor Assays
3.
Dis Colon Rectum ; 51(3): 329-33, 2008 Mar.
Article in English | MEDLINE | ID: mdl-18176828

ABSTRACT

PURPOSE: Internal sphincterotomy remains the standard for treatment of anal fissure, but it is associated with risks of infection, bleeding, and incontinence. Recent studies have suggested that the complications after lateral internal sphincterotomy are related to surgical technique. This study was designed to assess the incidence of early and late complications after lateral internal sphincterotomy with marginal sutured incision. Fissure healing, pain, and complications were compared in patients undergoing a procedure involving three interrupted marginal sutures after open lateral internal sphincterotomy procedure. METHODS: Ninety patients of chronic anal fissure were randomly assigned to two groups. Both groups received open lateral internal sphincterotomy via standardized method. The incisions of the patients in Group 1 (n=45) were sutured marginally with three interrupted sutures using 2-0 chromic catgut, whereas the incisions of the patients in Group 2 (n=45) were left open. The patients were assessed at 12 weeks postoperatively by an independent observer. RESULTS: The fissure-healing rate was not significantly different in both groups (95 and 93.1 percent, respectively). The pain score was slightly higher in Group 2, and it was statistically significant. Four cases of bleeding and two abscesses were observed in Group 2. These complications were not observed in Group 1. One case of incontinence was observed at the beginning in Group 1 and four in Group 2, but the incontinence was transient in both cases. CONCLUSIONS: Marginal sutures of incision after lateral internal sphincterotomy may be beneficial to reduce complications related to early wound healing.


Subject(s)
Fissure in Ano/surgery , Suture Techniques , Adult , Analysis of Variance , Chronic Disease , Female , Humans , Incidence , Male , Pain Measurement , Postoperative Complications/epidemiology , Prospective Studies , Treatment Outcome , Wound Healing
4.
J Med Chem ; 49(19): 5845-8, 2006 Sep 21.
Article in English | MEDLINE | ID: mdl-16970409

ABSTRACT

Cultured rat astrocytes and C6 rat glioma were used as a differential screen for a variety of 1,2,3,4-tetrahydroisoquinoline (THI) derivatives. Compound 1 [1-(biphenyl-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol hydrochloride] selectively blocked the growth of C6 glioma leaving normal astrocytes relatively unaffected. The potential for clinical utility of 1 was further substantiated in human gliomas and other tumor cell lines. Preliminary SAR of this activity was characterized by synthesis and testing of several THI and conformationally flexible variants.


Subject(s)
Antineoplastic Agents/chemical synthesis , Biphenyl Compounds/chemical synthesis , Isoquinolines/chemical synthesis , Tetrahydroisoquinolines/chemical synthesis , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Astrocytes/drug effects , Biphenyl Compounds/chemistry , Biphenyl Compounds/pharmacology , Cell Line, Tumor , Cells, Cultured , Drug Screening Assays, Antitumor , Glioma , Humans , Isoquinolines/chemistry , Isoquinolines/pharmacology , Molecular Conformation , Rats , Structure-Activity Relationship , Tetrahydroisoquinolines/chemistry , Tetrahydroisoquinolines/pharmacology
5.
J Med Chem ; 46(14): 2823-33, 2003 Jul 03.
Article in English | MEDLINE | ID: mdl-12825926

ABSTRACT

A variety of amine complexes with 1-boraadamatane were synthesized and subsequently evaluated for an antiproliferative effect on CD81-enriched cell lines to provide evidence for binding and activation of CD81. CD81 is a member of the tetraspanin family of membrane proteins found in all cell lineages in the liver. CD81 signals for antiproliferation when bound by antibodies. It is known that the HCV-E2 envelope glycoprotein binds to the CD81 protein. While it is unclear whether virus entry into host cells is directly linked to virus attachment via CD81 for HCV, this step in the viral life cycle has recently proven to be an effective point of attack for other viruses including HIV and rhinoviruses. The aim of the current study concerns the synthesis of amantidine analogues by appending primary amines to 1-boraadamantane to evaluate such compounds for CD81-dependent antiproliferation of CD81-enriched cell lines (astrocyte) vs CD81-deficient cell lines (C6 glioma). If the antiproliferative effect of these amantidine analogues proves to be an effect of binding and activating CD81, then these compounds may have the potential to prevent or treat HCV infections. Each compound's potential for preventive and therapeutic activity stems from the compound's potential to block viral attachment, virus-cell fusion, or virus entry into host cells or to counter potential mechanisms of HCV immune evasion. Out of a library of over 500 compounds, including randomly selected small molecules and rationally designed small molecules, only the 1-boraadamantaneamine compounds and structurally similar analogues display a significant antiproliferative effect on the CD81-enriched astrocytes relative to the CD81-deficient cell lines. In fact, 1-boraadamantane.l-phenylalanine methyl ester complex (5), 1-boraadamantane.ethanolamine complex (8), and (S)-2-[(adamantane-1-carbonyl)amino]-3-phenylpropionic acid (15) show a dose-dependent, astrocyte-selective antiproliferative activity in the concentration range 0.1-10 microM. This is consistent with the binding and activation of CD81 and represents a 2-fold improvement compared to the clinically prescribed anti-HCV agent, amantidine, in the same concentration range. Consequently, the 1-boraadamantaneamine derivatives present a promising lead in the development of small molecules with potential to bind to CD81 and treat HCV infections.


Subject(s)
Adamantane/analogs & derivatives , Antigens, CD/metabolism , Antineoplastic Agents/chemical synthesis , Antiviral Agents/chemical synthesis , Astrocytes/drug effects , Boron Compounds/chemical synthesis , Hepacivirus/drug effects , Membrane Proteins/metabolism , Adamantane/chemical synthesis , Adamantane/chemistry , Adamantane/pharmacology , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Astrocytes/cytology , Boron Compounds/chemistry , Boron Compounds/pharmacology , Crystallography, X-Ray , Dose-Response Relationship, Drug , Glioma , Membrane Proteins/deficiency , Models, Molecular , Protein Binding , Rats , Structure-Activity Relationship , Tetraspanin 28 , Tumor Cells, Cultured
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