scholarly journals Treatment of murine Candida krusei or Candida glabrata infection with L-743,872.

1997 ◽  
Vol 41 (9) ◽  
pp. 1937-1939 ◽  
Author(s):  
J R Graybill ◽  
R Bocanegra ◽  
M Luther ◽  
A Fothergill ◽  
M J Rinaldi
Keyword(s):  
Body Weight ◽  
Broad Spectrum ◽  
Candida Glabrata ◽  
Clinical Development ◽  
Candida Krusei ◽  
Murine Models ◽  
Fungal Cell ◽  
Significant Potential ◽  
Cell Counts

L-743,872 is a broad-spectrum pneumocandin antifungal drug developed by Merck Research Co., and in the present work it was evaluated in vivo in murine models of Candida krusei and Candida glabrata infection. Mice were infected intravenously with two isolates of C. krusei and treated with fluconazole or L-743,872. Fluconazole was beneficial only in immune-competent mice infected with isolate 94-2696. At > 0.5 mg/kg of body weight/day, L-743,872 was effective against both infecting isolates in immune-competent and immune-suppressed mice. Against C. glabrata, L-743,872 was effective, at doses > or = 0.5 mg/kg, in reducing fungal cell counts in the kidneys but not in the spleen. L-743,872 has significant potential for clinical development.

Leptin causes body weight loss in the absence of in vivo activities typical of cytokines of the IL-6 family

1998 ◽  
Vol 275 (3) ◽  
pp. R913-R919 ◽  
Author(s):  
Davide Agnello ◽  
Cristina Meazza ◽  
Christopher G. Rowan ◽  
Pia Villa ◽  
Pietro Ghezzi ◽  
...  
Keyword(s):  
Weight Loss ◽  
Body Weight ◽  
Body Weight Loss ◽  
Peripheral Blood Cell ◽  
Serum Corticosterone ◽  
Amyloid A ◽  
Cell Counts ◽  
Control Body ◽  
The One

To investigate if leptin shares in vivo activities with interleukin (IL)-6 family cytokines, it was tested in normal mice for the ability, after a single injection, to induce the acute-phase protein serum amyloid A, to potentiate the induction by IL-1 of serum corticosterone and IL-6, and to inhibit the induction by lipopolysaccharide of serum tumor necrosis factor and, after seven daily injections, to cause body weight loss and to change peripheral blood cell counts. At a 0.5 mg/kg dose, leptin caused body weight loss but did not show any of the other activities above. At a dose of 5 mg/kg, which also caused body weight loss, leptin potentiated the induction by IL-1 of serum corticosterone and IL-6 but did not show any other activity. In addition to causing body weight loss, leptin shows only some of the in vivo activities typical of IL-6 family cytokines and only if used at a dose that exceeds the one sufficient to affect body weight. In vivo, leptin seems to chiefly control body weight and not inflammatory or hematopoietic processes.

scholarly journals In Vivo Efficacy of Novel Monobactam LYS228 in Murine Models of Carbapenemase-Producing Klebsiella pneumoniae Infection

2019 ◽  
Vol 63 (4) ◽  
Author(s):  
W. J. Weiss ◽  
M. E. Pulse ◽  
P. Nguyen ◽  
E. J. Growcott
Keyword(s):  
Klebsiella Pneumoniae ◽  
Clinical Development ◽  
Murine Models ◽  
Bacterial Burden ◽  
In Vivo Efficacy ◽  
Content Type ◽  
Carbapenem Resistant ◽  
Infection Models ◽  
Resistant Strains

ABSTRACT LYS228 has potent antibacterial activity against carbapenem-resistant strains of Enterobacteriaceae. LYS228 was efficacious in neutropenic thigh models established with Klebsiella pneumoniae producing KPC-2 or NDM-1; pretreatment with uranyl nitrate considerably shifted calculated static doses of LYS228. In murine ascending pyelonephritis, LYS228 reduced bacterial burden in kidney, urine, and bladder. The successful treatment of murine infection models established with carbapenem-resistant K. pneumoniae further supports the clinical development of LYS228.

scholarly journals Oral Administration of the Broad-Spectrum Antibiofilm Compound Toremifene Inhibits Candida albicans and Staphylococcus aureus Biofilm FormationIn Vivo

2014 ◽  
Vol 58 (12) ◽  
pp. 7606-7610 ◽  
Author(s):  
Kaat De Cremer ◽  
Nicolas Delattin ◽  
Katrijn De Brucker ◽  
Annelies Peeters ◽  
Soña Kucharíková ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Broad Spectrum ◽  
Staphylococcus Epidermidis ◽  
Biofilm Formation ◽  
Candida Krusei ◽  
Content Type ◽  
And Staphylococcus Aureus

ABSTRACTWe here report on thein vitroactivity of toremifene to inhibit biofilm formation of different fungal and bacterial pathogens, includingCandida albicans,Candida glabrata,Candida dubliniensis,Candida krusei,Pseudomonas aeruginosa,Staphylococcus aureus, andStaphylococcus epidermidis. We validated thein vivoefficacy of orally administered toremifene againstC. albicans and S. aureusbiofilm formation in a rat subcutaneous catheter model. Combined, our results demonstrate the potential of toremifene as a broad-spectrum oral antibiofilm compound.

scholarly journals In VitroandIn VivoAntimalarial Activities of T-2307, a Novel Arylamidine

2012 ◽  
Vol 56 (4) ◽  
pp. 2191-2193 ◽  
Author(s):  
Akiko Kimura ◽  
Hiroshi Nishikawa ◽  
Nobuhiko Nomura ◽  
Junichi Mitsuyama ◽  
Shinya Fukumoto ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Body Weight ◽  
Broad Spectrum ◽  
Antimalarial Activity ◽  
Liver Stage ◽  
Rodent Malaria ◽  
Content Type ◽  
Clinically Significant

ABSTRACTT-2307, a novel arylamidine, has been shown to exhibit broad-spectrum antifungal activities against clinically significant pathogens. Here, we evaluated thein vitroandin vivoantimalarial activity of T-2307. The 50% inhibitory concentrations (IC50s) of T-2307 againstPlasmodium falciparumFCR-3 and K-1 strains were 0.47 and 0.17 μM, respectively. T-2307 at 2.5 to 10 mg/kg of body weight/day exhibited activity against blood stage and liver stage parasites in rodent malaria models. In conclusion, T-2307 exhibitedin vitroandin vivoantimalarial activity.

scholarly journals Comparison of the Fungicidal Activities of Caspofungin and Amphotericin B against Candida glabrata

2005 ◽  
Vol 49 (12) ◽  
pp. 4989-4992 ◽  
Author(s):  
Francesco Barchiesi ◽  
Elisabetta Spreghini ◽  
Serena Tomassetti ◽  
Daniela Arzeni ◽  
Daniele Giannini ◽  
...  
Keyword(s):  
Body Weight ◽  
Mouse Model ◽  
Amphotericin B ◽  
Fungal Pathogen ◽  
Candida Glabrata ◽  
Fungicidal Activity ◽  
Disseminated Infection ◽  
Fungicidal Effect ◽  
Time Kill

ABSTRACT We investigated the fungicidal activity of caspofungin (CAS) and amphotericin B (AMB) against 16 clinical isolates of Candida glabrata. The minimum fungicidal concentrations (MFCs) of CAS were similar to those of AMB, ranging from 2.0 to >8.0 μg/ml. Time-kill assays performed on selected isolates showed that AMB was fungicidal at concentrations four times the MIC while CAS was not. A neutropenic-mouse model of disseminated infection was utilized to determine the residual fungal kidney burden. While doses as low as 0.3 and 1 mg/kg of body weight/day of CAS and AMB, respectively, were effective at reducing the counts with respect to controls, organ sterilization was reached when both drugs were administered at 5 mg/kg/day. Our study reveals that, similar to AMB, CAS has the potential for a fungicidal effect in vivo against this difficult-to-treat fungal pathogen.

scholarly journals KY-62, a Polyene Analog of Amphotericin B, for Treatment of Murine Candidiasis

1998 ◽  
Vol 42 (1) ◽  
pp. 147-150 ◽  
Author(s):  
John R. Graybill ◽  
Laura K. Najvar ◽  
Annette Fothergill ◽  
Thomas Hardin ◽  
Michael Rinaldi ◽  
...  
Keyword(s):  
Body Weight ◽  
Candida Albicans ◽  
Amphotericin B ◽  
Clinical Development ◽  
Water Soluble ◽  
Clinical Isolates ◽  
In Vitro Testing ◽  
Immunocompetent Mice

ABSTRACT KY-62 is a water-soluble analog of amphotericin B. In vitro testing of five clinical isolates of Candida albicans showed KY-62 to have potency similar to that of amphotericin B. KY-62 was administered to mice infected intravenously with C. albicans. In vivo, KY-62 was effective in immunocompetent mice, with potency similar to that of amphotericin B. KY-62 was well tolerated up to 30 mg/kg of body weight per dose, an amount that would be lethal with amphotericin B. KY-62 was less effective in mice rendered neutropenic with 5-fluorouracil. The addition of flucytosine had little effect. KY-62 may have potential for clinical development.

Enhancement of the in vitro activity of amphotericin B against the biofilms of non-albicans Candida spp. by rifampicin and doxycycline

2007 ◽  
Vol 56 (5) ◽  
pp. 645-649 ◽  
Author(s):  
Mohamed El-Azizi
Keyword(s):  
Amphotericin B ◽  
Antifungal Agent ◽  
Candida Glabrata ◽  
Candida Parapsilosis ◽  
Candida Krusei ◽  
In Vitro Activity ◽  
Candida Spp ◽  
Killing Activity

The in vitro activity of amphotericin B (AMB) alone and in combination with rifampicin (RIF) and doxycycline (DOX) was tested against the biofilms of 30 clinical isolates of non-albicans Candida (NAC) species namely, Candida parapsilosis, Candida krusei and Candida glabrata. The killing activity of AMB at 10×MIC was significantly increased in combination with either antibiotic. With RIF, the killing activity increased by 20.6, 23.5 and 14 % against the biofilms of C. parapsilosis, C. krusei and C. glabrata, respectively; with DOX, the killing activity increased by 30.64, 35.28 and 31.13 %, respectively. Pre-exposure of the isolates to the same combinations significantly reduced the number of colonized cells in the biofilms by 20, 25.14 and 13.07 % with RIF for C. parapsilosis, C. krusei and C. glabrata, respectively, and by 18.94, 24.52 and 29.15 % with DOX, respectively. The data showed that combination of RIF or DOX with AMB enhanced the killing activity of the antifungal agent against biofilms of NAC species. Whether such an effect operates against biofilm-associated infections needs to be clarified by further in vivo studies.

scholarly journals Activity of ABT-773 against Mycobacterium avium Complex in the Beige Mouse Model

2000 ◽  
Vol 44 (10) ◽  
pp. 2895-2896 ◽  
Author(s):  
M. H. Cynamon ◽  
J. L. Carter ◽  
C. M. Shoen
Keyword(s):  
Body Weight ◽  
Mouse Model ◽  
Antimicrobial Agent ◽  
Mycobacterium Avium ◽  
Mycobacterium Avium Complex ◽  
Viable Cell ◽  
Beige Mouse ◽  
Cell Counts

ABSTRACT ABT-773, a new ketolide antimicrobial agent, was evaluated in comparison to clarithromycin (CLA) in vitro against Mycobacterium avium complex (MAC) and in a beige mouse model of disseminated MAC infection. The MICs at which 50 and 90% of the isolates tested were inhibited were 2 and 4 μg/ml, respectively, for CLA and 8 and 16 μg/ml, respectively, for ABT-773. Eight CLA-resistant isolates were found to be resistant to ABT-773 (MICs > 64 μg/ml). In the in vivo study mice were treated with ABT-773 (50, 100, and 200 mg/kg of body weight) or CLA (200 mg/kg). Both ABT-773 (100 and 200 mg/kg) and CLA significantly decreased the viable cell counts in spleens and lungs. ABT-773 (200 mg/kg) and CLA had similar activities in lungs, but the former was more active in spleens.

scholarly journals Antitrypanosomal Activity of Hydromethanol Extract of Leaves of Cymbopogon Citratus and Seeds of Lepidium Sativum: in-vivo Mice Model

2021 ◽  
Author(s):  
Ayechew Yetayeh Emiru ◽  
Eyasu Makonnen Eshetu ◽  
Fikru Regassa Gari ◽  
Fekadu Regassa Gudeta ◽  
Takele Beyene Tufa
Keyword(s):  
Body Weight ◽  
Plant Extracts ◽  
Field Isolate ◽  
Lepidium Sativum ◽  
Mice Model ◽  
Cymbopogon Citratus ◽  
Cell Counts ◽  
Antitrypanosomal Activity ◽  
Crude Extracts

Abstract Background: Trypanosomiasis is one of the neglected tropical diseases of both humans and animals which decreases their productivity and causes death in the worst scenario. Unavailability of vaccine, low therapeutic index of trypanocidal drugs, and development of resistance lead to the need for research focused on developing alternative treatment options especially from medicinal plants. The present study was aimed to investigate antitrypanosomal activities of leaves of Cymbopogon citratus and seeds of Lepidium sativum in in vivo mice model. Methods: The plant extracts were prepared by maceration using 80% methanol and reconstituted with 10% dimethyl sulfoxide (DMSO) to have the desired concentration. The test doses were adjusted to 100, 200 and 400mg/kg based on the toxicity profile. The Plants extracts were administered to the respective groups of mice after the 12th day of field isolate T. congolense inoculation for seven consecutive days. The level of parasitemia, body weight, packed cell volume, and differential white blood cell counts were measured.Results: The in vivo test results revealed that both plant extracts had dose dependent antitrypanosomal activity. Both crude extracts showed a significant reduction in parasite load (P<0.05), ameliorate anaemia (increased or prevent the fall of PCV value) (P<0.05), decreased lymphocytosis and increased neutrophil counts (p<0.05) and improved body weight but significant body weight increment (P<0.05) was observed only in C. citratus treated mice compared to the negative and positive controls. Comparative results from all tested parameters showed that the best activities were observed with C. citratus treated groups of mice. Conclusion: The present study concluded that the crude extracts of leaves of C. citratus and seeds of L. sativum had antitrypanosomal effects and can be potential targets for further studies on the development of alternative antitrypanosomal agents.

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