Home About us Contact
|
Home About us Contact | ||
|
|
||
Significant Efficacy (significant + efficacy)
Selected AbstractsAntifungal and Antibacterial Activity of the Newly Synthesized 2-Xanthone DerivativesARCHIV DER PHARMAZIE, Issue 1 2009Henryk Marona Abstract A series of 2-substituted xanthone derivatives 8,20 containing selected allyl, cinnamyl, morpholine, and imidazole moieties were synthesized and tested for their antifungal and antibacterial in-vitro properties. Of the newly synthesized derivatives, ten revealed antifungal activity especially against Trichophyton mentagrophytes (the biggest inhibition zones ranged 35 mm for 11 and 13). 2-(3-(Allylamino)propoxy)-9H -xanthen-9-one hydrochloride 9 inhibited growth of all of the examined fungal species. Significant efficacy against evaluated yeasts and dermatophytes was also observed for 6-chloro-2-methyl-9H -xanthen-9-one derivatives 11,13 containing encyclic amine moieties. Additionally, compounds 9, 11, and 12 hindered development of bacteria species but in a lesser degree. They were efficacious against Staphylococcus aureus, Escherichia coli, and Enterococcus faecalis. [source] The Treatment of Melasma with Fractional Photothermolysis: A Pilot StudyDERMATOLOGIC SURGERY, Issue 12 2005Cameron K. Rokhsar MD Background. Melasma is a common pigmentary disorder that remains resistant to available therapies. Facial resurfacing with the pulsed CO2 laser has been reported successful but requires significant downtime, and there is a risk of adverse sequelae. Objective. To determine if melasma will respond to a new treatment paradigm, fractional resurfacing. Methods. Ten female patients (Fitzpatrick skin types III,V) who were unresponsive to previous treatment were treated at 1- to 2-week intervals with the Fraxel laser (Reliant Technologies, Palo Alto, CA, USA). Wavelengths of 1,535 and 1,550 nm were both used, and 6 to 12 mJ per microthermal zone with 2,000 to 3,500 mtz/cm2 were the treatment parameters. Four to six treatment sessions were performed. Responses were evaluated according to the percentage of lightening of original pigmentation. Two physicians evaluated the photographs, and each patient evaluated her own response. Results. The physician evaluation was that 60% of patients achieved 75 to 100% clearing and 30% had less than 25% improvement. The patients' evaluations agreed, except for one patient, who graded herself as 50 to 75% improved as opposed to the physician grading of over 75%. There was one patient with postinflammatory hyperpigmentation and no patient with hypopigmentation. No downtime was necessary for wound healing. Conclusions. Fractional resurfacing affords a new treatment algorithm for the treatment of melasma that combines decreased risk and downtime with significant efficacy. This treatment modality deserves further exploration to maximize benefits. RELIANT technologies LOANED THE FRAXEL LASER FOR THE STUDY. RICHARD E. FITZPATRICK, MD, IS A PAID CONSULTANT FOR RELIANT AND A STOCKHOLDER. [source] Treatment of erythema multiforme, Stevens,Johnson Syndrome, and toxic epidermal necrolysisDERMATOLOGIC THERAPY, Issue 4 2002Klemens Rappersberger The "erythema multiforme disease spectrum" comprises four distinct, severe, clinical subvariants: (1) bullous erythema multiforme (bullous-EM), (2) Stevens,Johnson syndrome (SJS), (3) SJS,toxic epidermal necrolysis (TEN)-overlap syndrome, and (4) TEN. These diseases are closely related to severe mucocutaneous intolerance reactions that are mostly elicited by drugs/drug metabolites and associated with a high mortality rate. Old age and area of detached skin negatively influence the course of disease, and early withdrawal of causative drugs with short half-life is a positive prognostic factor. Therapeutic management represents a multidisciplinary challenge for colleagues from various specialities including specialized nurses and usually can be performed at a dermatologic ward unless technical equipment of an intensive care unit is needed. Topical therapy with biologic and (semi-)synthetic dressings is aimed at early re-epithelialization and the prevention of scarring, synechia formation, and infection. Systemic treatment includes antibiotics, fluid and electrolyte replacement, protein preparations and blood products, etc. Various anti-inflammatory and immunosuppressive treatment regimens with corticosteroids, cyclosporine A, cyclophosphamide, plasmapheresis have been considered to halt ongoing immunologic pathomechanisms, and some of these have shown significant efficacy. However, because we lack formal clinical trials, none of these regimens can be definitively proposed as a therapy of choice in any of the severe clinical variants of the EM spectrum. [source] Mechanism of action of certolizumab pegol (CDP870): In vitro comparison with other anti-tumor necrosis factor , agentsINFLAMMATORY BOWEL DISEASES, Issue 11 2007Andrew Nesbitt PhD Abstract Background: Inhibitors of tumor necrosis factor , (TNF,) have demonstrated significant efficacy in chronic inflammatory diseases, including Crohn's disease (CD). To further elucidate the mechanisms of action of these agents, we compared the anti-TNF, agents certolizumab pegol, infliximab, adalimumab, and etanercept in several in vitro systems. Methods: The ability of each anti-TNF, agent to neutralize soluble and membrane-bound TNF,; mediate cytotoxicity, affect apoptosis of activated human peripheral blood lymphocytes and monocytes; induce degranulation of human peripheral blood granulocytes, and modulate lipopolysaccharide (LPS)-induced interleukin (IL)-1, production by human monocytes was measured in vitro. Results: All 4 agents neutralized soluble TNF, and bound to and neutralized membrane TNF,. Infliximab and adalimumab were comparable in their ability to mediate complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity, and to increase the proportion of cells undergoing apoptosis and the level of granulocyte degranulation. Etanercept generally mediated these effects to a lesser degree, while certolizumab pegol gave similar results to the control reagents. LPS-induced IL-1, production was inhibited by certolizumab pegol, infliximab, and adalimumab, but only partially inhibited by etanercept. Conclusions: In contrast to the other anti-TNF, agents tested, certolizumab pegol did not mediate increased levels of apoptosis in any of the in vitro assays used, suggesting that these mechanisms are not essential for the efficacy of anti-TNF, agents in CD. As certolizumab pegol, infliximab, and adalimumab, but not etanercept, almost completely inhibited LPS-induced IL-1, release from monocytes, inhibition of cytokine production may be important for efficacy of anti-TNF, agents in CD. (Inflamm Bowel Dis 2007) [source] A method to study sustained antimicrobial activity of rinse and dentifrice components on biofilm viability in vivoJOURNAL OF CLINICAL PERIODONTOLOGY, Issue 1 2006H. C. Van Der Mei Abstract Aim: To develop an improved method for quantitative assessment of antimicrobial efficacy and substantivity of mouth rinses and dentifrices on in vivo treated plaque. Material and Methods: Nine- and 72-h-old plaques were formed in volunteers carrying out standardized hygiene using NaF-containing dentifrice. Plaques were collected before (baseline) in vivo treatment with dentifrices or chlorhexidine mouth rinse, immediately post-treatment and after 1 or 6 h, dispersed in demineralized water and stained with live/dead stain after which bacteria were enumerated. Dispersed baseline plaques were treated with dentifrices or chlorhexidine to determine antimicrobial efficacy against planktonic bacteria. Results: Baseline plaques revealed 56,41% viable organisms in 9- and 72-h-old plaques, respectively. Treatment of planktonic (dispersed baseline plaque) bacteria resulted in 1,4% viable organisms. Chlorhexidine mouth rinse and dentifrices produced strong immediate antimicrobial effects, but after 1 or 6 h, the proportion of viable organisms in 9-h-old plaques rebounded significantly with only chlorhexidine mouth rinse retaining significant efficacy. Seventy-two-hour-old plaques were less susceptible to antimicrobials, although dentifrices appeared more effective after 6 h than initially, whereas efficacy of chlorhexidine rinse continued to drop with time post-treatment. Conclusions: The proposed method holds promise for assessment of both immediate and retained antimicrobial actions of oral treatments against dental plaque in vivo. [source] Photocrosslinked DNA Nanospheres for Drug DeliveryMACROMOLECULAR RAPID COMMUNICATIONS, Issue 13 2010Young Hoon Roh Abstract DNA has been employed as both a genetic and a generic material. X-shaped DNA (X-DNA) in particular has four branched arms, providing multivalent functionalities that can allow for simultaneous multiple crosslinking. Here we report the synthesis of four acrylate-functionalized X-DNA monomers that can be further photocrosslinked to form monodisperse and tunable DNA nanospheres. In particular, the size and surface charge of these nanospheres were precisely controlled in a linear fashion, simply by tuning the monomer concentration in the reaction. The morphology and surface properties of the nanospheres were characterized using FT-IR, HPLC, TEM, AFM, zeta potential, and DLS analysis. In vitro studies in mammalian cells revealed that these DNA nanospheres demonstrated significant efficacy in the delivery of doxorubicin. These results highlight the potential of using DNA as material building blocks to design novel nanocarriers with properties tailored for the delivery of drugs in general and DNA/RNA in particular. [source] Effect of amantadine in essential tremor: A randomized, placebo-controlled trialMOVEMENT DISORDERS, Issue 4 2006Alexandre Gironell MD Abstract There is a need for new medication for essential tremor (ET). Preliminary evidence suggests that amantadine may be effective in the treatment of ET. We studied the effects of amantadine in a double-blind, cross-over, placebo-controlled trial in ET patients. Sixteen patients with ET received amantadine 100 mg b.i.d. and placebo for 15 days, with a 1-week wash-out period between treatments. Major evaluation outcomes consisted of a tremor clinical rating scale, accelerometric recordings, and a self-reported disability scale obtained before drug intake and on study days 1 and 15 of each treatment period. A two-way repeated measures analysis of variance (treatment, time) was applied. Any P value < 0.05 was considered significant. On day 15, amantadine did not demonstrate any significant efficacy in reducing tremor with respect to baseline in any tremor measures. An increase in postural tremor as an adverse effect of amantadine was referred by 37.5% of patients. Results from the present trial indicate amantadine at 100 mg b.i.d. is not effective as a treatment for ET. © 2005 Movement Disorder Society [source] Different response to rituximab in tumor necrosis factor blocker,naive patients with active ankylosing spondylitis and in patients in whom tumor necrosis factor blockers have failed: A twenty-four,week clinical trial,ARTHRITIS & RHEUMATISM, Issue 5 2010I.-H. Song Objective Histologic studies have shown B cell clusters in the subchondral bone marrow of the spine of patients with ankylosing spondylitis (AS). An immunotherapy targeting B cells in AS is therefore of interest. We undertook this study to examine the efficacy and safety of rituximab in patients with AS refractory to nonsteroidal antiinflammatory drugs in whom previous treatment with tumor necrosis factor , (TNF,) blockers either had not been tried or had failed. Methods In this phase II clinical trial, 1,000 mg rituximab was administered intravenously at baseline and at week 2 in 20 patients with active AS. Ten of these patients had never received TNF blockers, and treatment with TNF blockers had failed in the other 10 patients. The primary end point was a 20% improvement in disease activity at week 24 according to the criteria of the Assessment of SpondyloArthritis international Society (an ASAS20 response). Results Seventy-five percent of the patients were male, 90% were HLA,B27 positive, their mean age was 39.7 years, and their mean disease duration was 16.8 years. Patients had active disease, defined as a Bath Ankylosing Spondylitis Disease Activity Index (BASDAI) score ,4. While there was no clear response at week 24 in the group in whom TNF blockers had failed (30% had achieved an ASAS20 response, 10% had achieved an ASAS40 response, none had achieved partial remission according to the ASAS criteria, and none had achieved 50% improvement on the BASDAI [a BASDAI50 response] beyond an expected placebo response), we observed a good improvement in the TNF blocker,naive group at week 24 (50% had achieved an ASAS20 response, 40% had achieved an ASAS40 response, 30% had achieved partial remission according to the ASAS criteria, and 50% had achieved a BASDAI50 response). Conclusion Although rituximab does not seem to be effective in patients with AS that does not respond to TNF blockers, it had significant efficacy in TNF blocker,naive patients. Therefore, further controlled trials with B cell,directed therapies should be performed in TNF blocker,naive AS patients in the future. [source] Evaluation of efficacy and safety of rucinol serum in patients with melasma: a randomized controlled trialBRITISH JOURNAL OF DERMATOLOGY, Issue 5 2007A. Khemis Summary Background, Melasma is a hyperpigmentation disorder predominantly affecting sun-exposed areas in women, which is often refractory to treatment. Most commercially available treatments incorporate inhibitors of tyrosinase, a key enzyme in melanin production within the melanocyte. In general, however, the efficacy of these therapies is somewhat limited. Recent studies have identified other enzymes that play an important role in melanogenesis, including tyrosinase-related protein-1 (TRP-1), which catalyses the oxidation of the melanogenetic intermediate 5,6-dihydroxyindole-2-carbolylic acid. Rucinol (4- n -butylresorcinol) has been shown to inhibit the activity of both tyrosinase and TRP-1. Objectives, To assess the efficacy of rucinol serum 0·3% vs. the corresponding vehicle as a treatment for melasma. Secondary objectives were to evaluate local and general tolerability and to assess the skin acceptability of rucinol serum in the target population. Methods, In this prospective, single-centre, double-blind, randomized, vehicle-controlled, bilateral (split-face) comparative trial, 32 women with melasma were provided with two identical tubes containing rucinol serum 0·3% or vehicle. The products were each applied to one-half of the face, according to the randomization scheme, twice daily for 12 weeks (phase 1). A broad-spectrum sunscreen (sun protection factor 60) was also applied daily. Assessments at baseline, 4, 8 and 12 weeks included clinical evaluations by a dermatologist, chromametry, ultraviolet and standard photography, and assessments of skin acceptability and tolerability. After 12 weeks, patients were given the option of an additional 3-month treatment period of open full-face rucinol treatment, with reviews at 16, 20 and 24 weeks (phase 2). Results, Twenty-eight patients completed phase 1 and 26 patients completed phase 2. After 12 weeks, the clinical pigmentation score for rucinol-treated skin was significantly lower than for vehicle-treated skin (P = 0·027). During phase 2, rucinol induced a significant reduction in mean pigmentation score on the half of the face previously treated with vehicle. There was also a further, significant improvement on the rucinol-treated side of the face. Chromametry measurements showed that skin was significantly lighter and less yellow, with a strong trend towards reduced redness, following rucinol therapy compared with vehicle. Rucinol serum showed good tolerability and acceptability and was considered to have good or fair efficacy by 78% of the patient population. Conclusions, Rucinol serum was shown to have significant efficacy compared with vehicle alone in improving melasma after 3 months of treatment, according to clinical and objective assessments of skin colour. [source] 3465: Medical cancer therapy of lacrimal gland tumoursACTA OPHTHALMOLOGICA, Issue 2010C LE TOURNEAU Purpose The most common malignant epithelial cancer of the lacrimal gland is the adenoid cystic carcinoma (ACC). Despite a slow growth, ACCs are ultimately associated with a poor outcome. Methods Given the rarity of this disease, there are actually no conclusive recommendations for optimal therapy of this tumor. Results Surgery and postoperative radiation therapy is commonly used in the initial local treatment of ACC of the lacrimal gland. In high-risk recurrence patients, concomitant platinum-based chemoradiation should be discussed in an attempt to enhance radiosensitivity. While encouraging responses were reported with intraarterial neoadjuvant chemotherapy, this strategy was associated with substantial toxicity and should not be recommended outside of clinical trials. In the metastatic setting, systemic therapy is the only available option if no surgery and/or radiation is feasible. Although some tumour shrinkage has been reported with intravenous chemotherapy, only dismal objective response rates were achieved. Most active drugs remain anthracyclines and platinum compounds. Drug combinations do not seem to add much efficacy. More recently, non-cytotoxic molecularly targeted agents have emerged and demonstrated significant efficacy in several tumour types. These agents modulate specific targets thought to be essential for tumour proliferation and/or angiogenesis. c-KIT, PDGFR,, EGFR, and VEGFR are transmembrane receptors with oncogenic tyrosine kinase activity that are commonly overexpressed in ACC. The use of drugs triggering these targets has been disappointing so far. Conclusion The recent identification of a hallmark gene fusion transcript thought to activate critical targets involved in apoptosis, cell cycle control, cell growth and angiogenesis, heralds new treatment promise. [source] | ||||||||||