scholarly journals Potent In Vitro Antimalarial Activity of Metacycloprodigiosin Isolated from Streptomycesspectabilis BCC 4785

2002 ◽  
Vol 46 (4) ◽  
pp. 1112-1113 ◽  
Author(s):  
Masahiko Isaka ◽  
Amonlaya Jaturapat ◽  
Jarin Kramyu ◽  
Morakot Tanticharoen ◽  
Yodhathai Thebtaranonth
Keyword(s):  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Fermentation Broth ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Antimalarial Agents ◽  
Bioassay Guided Fractionation

ABSTRACT Bioassay-guided fractionation of the extract from the fermentation broth of Streptomyces spectabilis BCC 4785 led to the isolation of three principle antimalarial agents, metacycloprodigiosin, bafilomycin A1, and spectinabilin. Metacycloprodigiosin exhibited potent in vitro activity against Plasmodium falciparum K1, with a 50% inhibitory concentration of 0.0050 ± 0.0010 μg/ml, while its cytotoxicity was much weaker.

scholarly journals In Vitro Activity of Lumefantrine (Benflumetol) against Clinical Isolates of Plasmodium falciparum in Yaoundé, Cameroon

1998 ◽  
Vol 42 (9) ◽  
pp. 2347-2351 ◽  
Author(s):  
Leonardo K. Basco ◽  
Jean Bickii ◽  
Pascal Ringwald
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Geometric Mean ◽  
Vitro Activity ◽  
Clinical Isolates ◽  
Cross Resistance ◽  
In Vitro Activity ◽  
Antimalarial Agents ◽  
Fluorene Derivative

ABSTRACT The in vitro antimalarial activity of the new Chinese synthetic drug, lumefantrine, also known as benflumetol (a fluorene derivative belonging to the aminoalcohol class), was determined by an isotopic microtest against 61 fresh clinical isolates of Plasmodium falciparum and compared with that of other established antimalarial agents. The geometric mean 50% inhibitory concentration of lumefantrine was 11.9 nmol/liter (95% confidence intervals, 10.4 to 13.6 nmol/liter; range, 3.3 to 25.6 nmol/liter). The in vitro activities of lumefantrine against the chloroquine-sensitive and the chloroquine-resistant isolates did not differ (P > 0.05). There was a significant positive correlation of responses between lumefantrine and two other aminoalcohols studied, mefloquine (r = 0.688) and halofantrine (r = 0.677), and between lumefantrine and artesunate (r = 0.420), suggesting a potential for in vitro cross-resistance. Our data suggest high in vitro activity of lumefantrine, comparable to that of mefloquine, and are in agreement with the promising results of preliminary clinical trials.

Comparison of the in Vitro Activity of Daptomycin and four other Antimicrobial Agents against Staphylococci Associated with CAPD Peritonitis

1988 ◽  
Vol 8 (4) ◽  
pp. 277-279
Author(s):  
Wendy L. Vaudry ◽  
Claudia Gratton ◽  
Kinga Kowalewska ◽  
Wanda M. Wenman
Keyword(s):  
Peritoneal Dialysis ◽  
Minimum Inhibitory Concentration ◽  
Continuous Ambulatory Peritoneal Dialysis ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Coagulase Negative Staphylococci ◽  
Vancomycin Resistant

The minimum inhibitory concentration (MIC) of daptomycin was compared with that of four other antimicrobial agents against clinically relevant staphylococci. Sixtyfive isolates were obtained from patients on continuous ambulatory peritoneal dialysis (CAPD) who contracted peritonitis. These isolates comprised 29 S. Sureus strains (all sensitive to oxacillin); 25 S. epidermidis strains (14 sensitive and 9 resistant to oxacillin); and 11 unspeciated coagulase-negative staphylococci (2 sensitive and 11 resistant to oxacillin). All of the oxacillin susceptible strains were inhibited by ≤2 mg/L of the five antibiotics tested. The oxacillin resistant staphylococci were also resistant to cefuroxime and variably resistant to cefamandole, but were uniformly susceptible to both vancomycin and daptomycin. Daptomycin possesses equivalent in vitro activity to vancomycin against strains of S. Sureus and coagulase negative staphylococci associated with CAPD peritonitis. If vancomycin resistance becomes a significant problem in these patients, and daptomycin is shown to be active against vancomycin resistant organisms, then it would have potential usefulness as an alternative to vancomycin in the treatment of peritonitis caused by multiply -resistant staphylococci.

scholarly journals A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4485
Author(s):  
Veronika R. Karpina ◽  
Svitlana S. Kovalenko ◽  
Sergiy M. Kovalenko ◽  
Oleksandr G. Drushlyak ◽  
Natalya D. Bunyatyan ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Molecular Docking ◽  
Virtual Screening ◽  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Virtual Library ◽  
Antimalarial Agents ◽  
Starting Point ◽  
In Silico Studies

For the development of new and potent antimalarial drugs, we designed the virtual library with three points of randomization of novel [1,2,4]triazolo[4,3-a]pyridines bearing a sulfonamide fragment. The library of 1561 compounds has been investigated by both virtual screening and molecular docking methods using falcipain-2 as a target enzyme. 25 chosen hits were synthesized and evaluated for their antimalarial activity in vitro against Plasmodium falciparum. 3-Ethyl-N-(3-fluorobenzyl)-N-(4-methoxyphenyl)-[1,2,4]triazolo[4,3-a]pyridine-6-sulfonamide and 2-(3-chlorobenzyl)-8-(piperidin-1-ylsulfonyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one showed in vitro good antimalarial activity with inhibitory concentration IC50 = 2.24 and 4.98 μM, respectively. This new series of compounds may serve as a starting point for future antimalarial drug discovery programs.

scholarly journals In Vitro Activity of Oxazolidinone against Nontuberculous Mycobacteria, Including Macrolide-Resistant Clinical Isolates

2021 ◽  
Author(s):  
Dae Hun Kim ◽  
Su-Young Kim ◽  
Won-Jung Koh ◽  
Byung Woo Jhun
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Nontuberculous Mycobacteria ◽  
Macrolide Resistance ◽  
Vitro Activity ◽  
Clinical Isolates ◽  
In Vitro Activity

We evaluated the in vitro activities of oxazolidinone antibiotics including linezolid, sutezolid, and delpazolid against clinical nontuberculous mycobacteria isolates. Regardless of macrolide resistance, for M. avium, M. intracellulare, and M. kansasii, sutezolid showed the lowest minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) value among oxazolidinone antibiotics. However, for M. abscessus, M. massiliense, the MIC and MBC values for all oxazolidinone antibiotics showed similar values. Oxazolidinone antibiotics warrant further investigation as potential antibiotics.

scholarly journals In Vitro Activities of Tritrpticin Alone and in Combination with Other Antimicrobial Agents against Pseudomonas aeruginosa

2006 ◽  
Vol 50 (11) ◽  
pp. 3923-3925 ◽  
Author(s):  
Oscar Cirioni ◽  
Andrea Giacometti ◽  
Carmela Silvestri ◽  
Agnese Della Vittoria ◽  
Alberto Licci ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Multidrug Resistant ◽  
Procoagulant Activity ◽  
Vitro Activity ◽  
In Vitro Activity

ABSTRACT The in vitro activity of the cathelicidin tritrpticin was investigated against multidrug-resistant Pseudomonas aeruginosa. The isolates were susceptible to the peptide at concentrations of 0.50 to 8 mg/liter. Tritrpticin completely inhibits lipopolysaccharide procoagulant activity at a 10 μM concentration. Fractionary inhibitory concentration indexes (0.385, 0.312, and 0.458) demonstrated synergy between the peptide and β-lactams.

scholarly journals Trioxaquines Are New Antimalarial Agents Active on All Erythrocytic Forms, Including Gametocytes

2007 ◽  
Vol 51 (4) ◽  
pp. 1463-1472 ◽  
Author(s):  
Françoise Benoit-Vical ◽  
Joël Lelièvre ◽  
Antoine Berry ◽  
Caroline Deymier ◽  
Odile Dechy-Cabaret ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Mice Model ◽  
Additional Advantage ◽  
Antimalarial Agents ◽  
Hybrid Molecules ◽  
Resistant Strains ◽  
Antimalarial Chemotherapy

ABSTRACT Malaria is the third most significant cause of infectious disease in the world. The search for new antimalarial chemotherapy has become increasingly urgent due to parasite resistance to classical drugs. Trioxaquines are synthetic hybrid molecules containing a trioxane motif (which is responsible for the antimalarial activity of artemisinin) linked to an aminoquinoline entity (which is responsible for the antiplasmodial properties of chloroquine). These trioxaquines are highly potent against young erythrocytic stages of Plasmodium falciparum and exhibit efficient activity in vitro against chloroquine-sensitive and -resistant strains of P. falciparum (50% inhibitory concentration, 4 to 32 nM) and are also active in vivo against P. vinckei petteri and P. yoelii nigeriensis in suppressive and curative murine tests. The trioxaquine DU1302 is one of these promising antimalarial agents. The present study confirms the absence of toxicity of this drug on cell lines and in a mice model. Moreover, DU1302 exhibits potent activity against gametocytes, the form transmitted by mosquitoes, as killing of the gametocytes is essential to limit the spread of malaria. The ease of chemical synthesis of this trioxaquine prototype should be considered an additional advantage and would make these drugs affordable without perturbations of the drug supply.

scholarly journals Optimization of Xanthones for Antimalarial Activity: the 3,6-Bis-ω-Diethylaminoalkoxyxanthone Series

2002 ◽  
Vol 46 (1) ◽  
pp. 144-150 ◽  
Author(s):  
Jane Xu Kelly ◽  
Rolf Winter ◽  
David H. Peyton ◽  
David J. Hinrichs ◽  
Michael Riscoe
Keyword(s):  
Plasmodium Falciparum ◽  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Multidrug Resistant ◽  
Food Vacuole ◽  
Ionic Interactions ◽  
Side Chains ◽  
Antimalarial Agents ◽  
Unique Manner

ABSTRACT Hydroxyxanthones have been identified as novel antimalarial agents. The compounds are believed to exert their activity by complexation to heme and inhibition of hemozoin formation. Modification of the xanthone structure was pursued to improve their antimalarial activity. Attachment of R-groups bearing protonatable nitrogen atoms was conducted to enhance heme affinity through ionic interactions with the propionate side chains of the metalloporphyrin and to facilitate drug accumulation in the parasite food vacuole. A series of 3,6-bis-ω-diethylaminoalkoxyxanthones with side chains ranging from 2 to 8 carbon atoms were prepared and evaluated. Measurement of heme affinity for each of the derivatives revealed a strong correlation (R 2 = 0.97) between affinity and antimalarial potency. The two most active compounds in the series contained 5- and 6-carbon side chains and exhibited low nanomolar 50% inhibitory concentration (IC50) values against strains of chloroquine-susceptible and multidrug-resistant Plasmodium falciparum in vitro. Both of these xanthones exhibit stronger heme affinity (8.26 × 105 and 9.02 × 105 M−1, respectively) than either chloroquine or quinine under similar conditions and appear to complex heme in a unique manner.

The high efficacy of luliconazole against environmental and otomycosis Aspergillus flavus strains

2020 ◽  
Author(s):  
Maryam Moslem ◽  
Ali Zarei Mahmoudabadi
Keyword(s):  
Amphotericin B ◽  
Aspergillus Flavus ◽  
Inhibitory Concentration ◽  
Topical Therapy ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Environmental Isolates ◽  
Strong Activity ◽  
Microscopic Features

Background and Objectives: Luliconazole is currently confirmed for the topical therapy of dermatophytosis. Moreover, it is found that luliconazole has in vitro activity against some molds and yeast species. The aim of the present study was to evaluate the efficacy of luliconazole in comparison to routine used antifungals on clinical and environmental isolates of Aspergillus flavus. Materials and Methods: Thirty eight isolates of A. flavus (18 environmental and 20 clinical isolates) were detected based on morphological and microscopic features and also PCR-sequencing of β-tubulin ribosomal DNA gene. All the isolates were tested against luliconazole, voriconazole, amphotericin B and caspofungin. Minimum inhibitory concentration (MIC),   90   MIC50, MIC isolates.   and MIC Geometric (GM) were calculated using CLSI M38-A2 protocol for both environmental and clinical   GM   Results: Luliconazole with extremely low MIC range, 0.00049-0.00781 μg/mL and MIC   0.00288 μg/mL showed very   strong activity against both clinical and environmental A. flavus isolates. Moreover, voriconazole inhibited 100% of isolates at defined epidemiological cutoff values (ECV ≤ 2 µg/ml). 50% and 27.8% of clinical and environmental isolates of A. flavus, were resistant to caspofungin, respectively. Whereas, all the isolates were found to be resistant to amphotericin B.   GM   Conclusion: The analysis of our data clearly indicated that luliconazole (with MIC   0.00244 µg/ml for clinical and 0.00336   μg/ml for environmental isolates) had the highest in vitro activity against A. flavus strains.

scholarly journals Comparative Antifungal Activity of Cilofungin (LY121019) againstCandidaSpecies, Including Evaluation of Susceptibility Testing Method

1992 ◽  
Vol 3 (5) ◽  
pp. 231-234 ◽  
Author(s):  
Abdul H Chagla ◽  
John H Hii ◽  
Daryl J Hoban ◽  
Andrew E Simor ◽  
Santiago Ferro ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Amphotericin B ◽  
Candida Glabrata ◽  
Susceptibility Testing ◽  
Inhibitory Concentration ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Testing Method ◽  
Testing Susceptibility

The in vitro activity of cilofungin against 100Candidaspecies was compared with 5-flucytosine. amphotericin B and ketoconazole by two laboratories independently and in a blinded fashion using a macrotitre dilution broth method insaam-fmedium. Cilofungin showed good in vitro activity againstCandida albicans. Candida tropicalisandCandida glabrata(90% minimal inhibitory concentration [MIC] 3.2 μg/mL) but was inactive against otherCandidaspecies. When testing the susceptibility of cilofungin, 5-flucytosine and amphotericin B at the two centres, approximately 90% of theCandidastrains had MICs differing by fourfold or less. However, when testing susceptibility of ketoconazole, only 51% of theCandidastrains had MIC differences fourfold or less. MIC susceptibility testing with cilofungin, 5-flucytosine and amphotericin B insaam-fmedium is reproducible.

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