2012年8月14日星期二
Cannabis Enhances Bipolar Patients' Neurocognitive Performance
Crowdsourcing Cures
Shear-Activated Clot-Busting Drug
Education Lengthens Life Expectancy
2012年8月13日星期一
More Than Just A Smiley Face
Dihydrofuro pyrimidines as akt protein kinase inhibitors
Effects of intra-articular injections of bufexamac suspension in healthy horses.
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Effects of intra-articular injections of bufexamac suspension in healthy horses.
Am J Vet Res. 2001 Oct;62(10):1629-35
Authors: Suominen MM, Tulamo RM, Anttila MO, Sankari SM, Kir�ly K, Lapvetel�inen T, Helminen HJ
Abstract
OBJECTIVE: To evaluate the effects of intra-articular (IA) injections of bufexamac in horses, focusing particularly on the effects of bufexamac on articular cartilage.
ANIMALS: 20 Standardbreds.
PROCEDURE: Horses were randomly allocated into 4 groups consisting of 5 horses each, and 20, 60, or 100 mg of bufexamac or 1 ml of sterile saline (0.9% NaCl) solution (control) was injected into 1 intercarpal joint at weekly intervals for 6 treatments (days 0, 7, 14, 21, 28, and 35). Clinical signs and results of hematologic, serum biochemical, and synovial fluid (SF) analyses and radiography were used to evaluate treatment effects. On day 49, all horses were euthanatized; gross necropsy and histologic examinations of internal organs and articular tissues were performed. Glycosaminoglycan concentration of the articular cartilage was evaluated in safranin O-stained sections by use of a semiquantitative microspectrophotometric method.
RESULTS: No systemic signs were observed. Temporary mild to moderate heat and effusion were the only clinical signs observed in a number of joints after IA injections and more often only in the 100 mg group, compared with controls. The 100 mg dose resulted in significant increases in SF WBC counts, with relative neutrophilia and SF total protein concentration 24 hours after injection (day 1). No lesions suggestive of toxic effects were detected at necropsy or on histologic examination. No changes in articular cartilage glycosaminoglycan concentration were detected.
CONCLUSIONS AND CLINICAL RELEVANCE: Six injections of 20, 60, or 100 mg of bufexamac at weekly intervals did not cause any untoward systemic or local effects. These data suggest that bufexamac is a safe nonsteroidal anti-inflammatory drug for IA administration in horses.
PMID: 11592331 [PubMed - indexed for MEDLINE]
Novel agents and new therapeutics in castration-resistant prostate cancer.
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Novel agents and new therapeutics in castration-resistant prostate cancer.
Curr Opin Oncol. 2011 May;23(3):290-6
Authors: Wu Y, Rosenberg JE, Taplin ME
Abstract
PURPOSE OF REVIEW: This review highlights recent therapeutic advances in systemic therapies for prostate cancer (PCa).
RECENT FINDINGS: Progress in PCa therapeutics has been made during the past year with the approval of a vaccine therapy, second-line chemotherapy, and reported survival advantage for a CYP (17,20) lyase inhibitor in castration-resistant prostate cancer (CRPC). This report will summarize the recently reported and expected data for PCa trials including an evaluation of intermittent vs. continuous androgen deprivation therapy. Denosumab is shown to support bone mineral density in hormonal sensitive PCa patients. Targeting of androgen-dependent pathways in CRPC postchemotherapy has been shown to improve survival with the lyase inhibitor abiraterone, and lead to prostate-specific antigen and objective responses with an androgen receptor antagonist (MDV3100). However, the addition of bevacizumab to docetaxel/prednisone in treating metastatic CRPC failed to provide a survival benefit. Cabazitaxel in metastatic CRPC postdocetaxel did demonstrate a survival benefit. Provenge, an autologous dendritic cell-based vaccine, demonstrated a reduction in the risk of death in metastatic CRPC. Other immunotherapy agents, including Prostvac and ipilimumab are under investigation. We also discuss the receptor tyrosine kinase inhibitor XL184 and poly (ADP-ribose) polymerase inhibitors which are in early clinical trials.
SUMMARY: Recent advances in androgen targeting, chemotherapy, immunotherapy, and other targeted therapies have led to significant improvements in the care of CRPC patients.
PMID: 21311328 [PubMed - indexed for MEDLINE]
2012年8月12日星期日
The local antinociceptive and topical anti-inflammatory effects of propyl gallate in rodents.
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The local antinociceptive and topical anti-inflammatory effects of propyl gallate in rodents.
Br J Pharmacol. 1976 Dec;58(4):573-81
Authors: McDonald-Gibson WJ, Saeed SA, Schneider C
Abstract
1 In common with several anti-inflammatory, analgesic, local anaesthetic and antioxidant drugs, propyl gallate in vitro inhibited the biosynthesis of prostaglandin E2 and F2alpha from arachidonic acid by a prostaglandin synthetase from bull seminal vesicles. 2 In common with analgesic drugs, propyl gallate reduced the ability of arachidonic acid, acetylcholine or acetic acid to cause abdominal constriction in mice. 3 Using a new method for evaluating anti-inflammatory activity, we demonstrated the effectiveness of aspirin or indomethacin given subcuteneously before u.v. irradiation of guinea-pig ears, the prophylactic action of topically applied sunscreen agents and the therapeutic value of bufexamac and propyl gallate applied after irradiation.
PMID: 826298 [PubMed - indexed for MEDLINE]
Mutagenicity studies on bufexamac.
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Mutagenicity studies on bufexamac.
Mutat Res. 1982 Feb;103(2):107-9
Authors: Fabry L, L�onard A, Decat G, Roba J
PMID: 7035915 [PubMed - indexed for MEDLINE]