scholarly journals Antifungal Activity of Maytenin and Pristimerin

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Fernanda P. Gullo ◽  
Janaina C. O. Sardi ◽  
Vânia A. F. F. M. Santos ◽  
Fernanda Sangalli-Leite ◽  
Nayla S. Pitangui ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Trichophyton Rubrum ◽  
Fungal Infections ◽  
Human Keratinocytes ◽  
Trichophyton Mentagrophytes ◽  
Pharmacological Activities ◽  
Etiologic Agents ◽  
High Incidence ◽  
Maytenus Ilicifolia

Fungal infections in humans have increased alarmingly in recent years, particularly in immunocompromised individuals. Among the infections systemic candidiasis, aspergillosis, cryptococcosis, paracoccidioidomycosis, and histoplasmosis mortality are more prevalent and more severe in humans. The current high incidence of dermatophytosis is in humans, especially as the main etiologic agentsTrichophyton rubrumandTrichophyton mentagrophytes. Molecules pristimerin and maytenin obtained from the plantMaytenus ilicifolia(Celastraceae) are known to show various pharmacological activities. This study aimed to evaluate the spectrum of antifungal activity of maytenin and pristimerin and their cytotoxicity in human keratinocytes (NOK cells of the oral mucosa). It was concluded that the best spectrum of antifungal activity has been shown to maytenin with MIC varying from 0.12 to 125 mg/L, although it is also active with pristimerin MIC ranging between 0.12 and 250 mg/L. Regarding the toxicity, both showed to have high IC50. The SI showed high pristimerin against some species of fungi, but SI maytenin was above 1.0 for all fungi tested, showing a selective action of fungi. However, when comparing the two substances, maytenin also showed better results. The two molecules can be a possible prototype with a broad spectrum of action for the development of new antifungal agents.

scholarly journals Antifungal Agents: Design, Synthesis, Antifungal Activity and Molecular Docking of Phloroglucinol Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3116 ◽  
Author(s):  
Xingxing Teng ◽  
Yuanyuan Wang ◽  
Jinhua Gu ◽  
Peiqi Shi ◽  
Zhibin Shen ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antifungal Activity ◽  
Protein Binding ◽  
Binding Site ◽  
Antifungal Agents ◽  
Trichophyton Rubrum ◽  
Trichophyton Mentagrophytes ◽  
Protein Binding Site ◽  
Antifungal Activities ◽  
Phloroglucinol Derivatives

Pseudoaspidinol is a phloroglucinol derivative with Antifungal activity and is a major active component of Dryopteris fragrans. In our previous work, we studied the total synthesis of pseudoaspidinol belonging to a phloroglucinol derivative and investigated its antifungal activity as well as its intermediates. However, the results showed these compounds have low antifungal activity. In this study, in order to increase antifungal activities of phloroglucinol derivatives, we introduced antifungal pharmacophore allylamine into the methylphloroglucinol. Meanwhile, we remained C1–C4 acyl group in C-6 position of methylphloroglucinol using pseudoaspidinol as the lead compound to obtain novel phloroglucinol derivatives, synthesized 17 compounds, and evaluated antifungal activities on Trichophyton rubrum and Trichophyton mentagrophytes in vitro. Molecular docking verified their ability to combine the protein binding site. The results indicated that most of the compounds had strong antifungal activity, in which compound 17 were found to be the most active on Trichophyton rubrum with Minimum Inhibitory Concentration (MIC) of 3.05 μg/mL and of Trichophyton mentagrophytes with MIC of 5.13 μg/mL. Docking results showed that compounds had a nice combination with the protein binding site. These researches could lay the foundation for developing antifungal agents of clinical value.

scholarly journals In vitro antifungal activity of Candida culture extracts against Trichophyton rubrum and Trichophyton mentagrophytes.

2021 ◽  
Vol 1 (4) ◽  
pp. 135-152
Author(s):  
Thiago Henrique Lemes ◽  
Guilherme Silva Torrezan ◽  
Carlos Roberto Polaquini ◽  
Luis Octavio Regasini ◽  
Bianca Gottardo de Almeida ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Galleria Mellonella ◽  
Trichophyton Rubrum ◽  
Fungal Infections ◽  
Trichophyton Mentagrophytes ◽  
Recurrence Rates ◽  
Isolation And Identification ◽  
Microdilution Method ◽  
Broth Microdilution Method

Onychomycoses are nail infections caused primarily by dermatophytes fungi, yeasts, and other filamentous fungi, characterized by persistent infections, prolonged therapy, and high recurrence rates. In clinical practice, some of these occurrences present two or more microorganisms, and the interactions among them can change the chemical environment mediated by small diffusible molecules, producing a competitive niche. The aim of this study was to evaluate the antifungal activity of individual extracts of pure cultures of Candida albicans and C. parapsilosis against dermatophytes. To obtain the fungal extracts, cultures were filtered through a 0.2 μm membrane and submitted to liquid-liquid extraction using ethyl acetate. The Minimal Inhibitory Concentration (MIC) of each extract was evaluated by broth microdilution method and checkerboard assay with fluconazole against clinical isolates of Trichophyton rubrum and T. mentagrophytes. The invertebrate model of Galleria mellonella was used to evaluate the toxicity of the extracts. As results, the extracts of C. albicans and C. parapsilosis showed antifungal activity with MICs between 31,2 – 2000 μg/mL. In association with fluconazole, synergistic effect was detected for all combinations. The extracts presented low toxicity in G. mellonella. In the future, isolation and identification of the extract compounds may allow new therapeutic approaches in the control of fungal infections.

Antifúngicos poliénicos. Mecanismo de acción y aplicaciones

2020 ◽  
Vol 63 (2) ◽  
pp. 7-17
Author(s):  
Evelyn Rivera-Toledo ◽  
Alan Uriel Jiménez-Delgadillo ◽  
Patricia Manzano-Gayosso
Keyword(s):  
Antifungal Activity ◽  
Key Words ◽  
Secondary Metabolism ◽  
Amphotericin B ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Variable Number ◽  
Therapeutic Failure ◽  
Morbidity And Mortality ◽  
Clinical Use

The first compounds with specific antifungal activity were identified in the middle of the last century as a product of the secondary metabolism of bacteria of the order Actinomycetales, and their clinical use significantly diminished the morbidity and mortality associated with severe fungal infections. Many of such biosynthetic compounds are characterized by a chemical polygenic structure, with a variable number of carbon-carbon double bonds. Currently, besides polygenic antimycotics, there are other antifungal agents, such as the azole compounds, that have less toxicity in patients; however, cases of therapeutic failure with such compounds have been documented, therefore, the use of polygenics is still the best alternative in such cases. This review presents data about the properties and applications of antifungal-polygenic compounds using amphotericin B as a model. Key words: Amphotericin B; antifungal polyenes; ergosterol

scholarly journals Antifungal activity and mechanism of heat-transformed ginsenosides from notoginseng against Epidermophyton floccosum, Trichophyton rubrum, and Trichophyton mentagrophytes

RSC Advances ◽  
2017 ◽  
Vol 7 (18) ◽  
pp. 10939-10946 ◽  
Author(s):  
Peng Xue ◽  
Xiushi Yang ◽  
Xiaoyan Sun ◽  
Guixing Ren
Keyword(s):  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Trichophyton Mentagrophytes ◽  
Epidermophyton Floccosum ◽  
Heat Transformation

The improved antifungal activity of notoginseng can be attributed to the formation of less polar ginsenosides by heat transformation.

Pharmacokinetics of Antifungal Agents

1993 ◽  
Vol 13 (2_suppl) ◽  
pp. 380-382 ◽  
Author(s):  
A. Fabris ◽  
M. V. Pellanda ◽  
C. Gardin ◽  
A. Contestabile ◽  
R. Bolzonella
Keyword(s):  
Abdominal Pain ◽  
Antifungal Activity ◽  
Amphotericin B ◽  
Peritoneal Fluid ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Intraperitoneal Administration ◽  
Point Of View ◽  
Severe Abdominal Pain ◽  
Fungal Peritonitis

The authors have evaluated the pharmacokinetics of four antifungal agents used in the therapy of fungal peritonitis. Amphotericin B (Amph B) poorly diffuses from blood into peritoneal fluid, which Intraperitoneal administration induces severe abdominal pain. 5-Fluorocytosine (5FC) easily crosses peritoneum, but resistance may appear when the drug is used alone. Ketoconazole (K) poorly penetrates into peritoneal fluid, while Fluconazole (F), used per os or intraperitoneally, shows a good antifungal activity both in serum and In the peritoneal fluid. In conclusion, from a pharmacokinetic point of view, all the antifungal agents examined, perhaps with the exception of F, do not offer, when used alone, sufficient guarantees In curing peritonitis. Therefore, for treating fungal infections in CAPD, drug combinations such as AmphB + 5FC, K + 5FC or 5FC + F have to be used.

scholarly journals Anti-TrichophytonActivity of Protocatechuates and Their Synergism with Fluconazole

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Luciana Arantes Soares ◽  
Fernanda Patrícia Gullo ◽  
Janaina de Cássia Orlandi Sardi ◽  
Nayla de Souza Pitangui ◽  
Caroline Barcelos Costa-Orlandi ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Trichophyton Rubrum ◽  
Biological Activities ◽  
Public Health Problem ◽  
Trichophyton Mentagrophytes ◽  
Fungal Resistance ◽  
Synergistic Activity ◽  
Global Public Health ◽  
Limited Spectrum ◽  
Promising Source

Dermatophytosis and superficial mycosis are a major global public health problem that affects 20–25% of the world’s population. The increase in fungal resistance to the commercially available antifungal agents, in conjunction with the limited spectrum of action of such drugs, emphasises the need to develop new antifungal agents. Natural products are attractive prototypes for antifungal agents due to their broad spectrum of biological activities. This study aimed to verify the antifungal activity of protocatechuic acid, 3,4-diacetoxybenzoic, and fourteen alkyl protocatechuates (3,4-dihydroxybenzoates) againstTrichophyton rubrumandTrichophyton mentagrophytesand to further assess their activities when combined with fluconazole. Susceptibility and synergism assays were conducted as described in M38-A2 (CLSI), with modifications. Three strains ofTrichophyton rubrumand three strains ofTrichophyton mentagrophyteswere used in this work. The pentyl, hexyl, heptyl, octyl, nonyl, and decyl protocatechuates showed great fungicidal effects, with minimum inhibitory concentration (MIC) values ranging from 0.97 to 7.8 mg/L. Heptyl showed a synergistic activity (FIC index= 0.49), reducing the MIC of fluconazole by fourfold. All substances tested were safe, especially the hexyl, heptyl, octyl, and nonyl compounds, all of which showed a high selectivity index, particularly in combination with fluconazole. These ester associations with fluconazole may represent a promising source of prototypes in the search for anti-Trichophytontherapeutic agents.

scholarly journals In vitro evaluation of the antifungal activity of Marco (Ambrosia arborescens Mill.) and Matico (Aristeguietia glutinosa Lam.) on the pathogenic fungi that cause dermatomycosis (ringworm)

F1000Research ◽  
2018 ◽  
Vol 7 ◽  
pp. 559
Author(s):  
Tatiana de los Ángeles Mosquera Tayupanta ◽  
Sandra Elizabeth Ayala Valarezo ◽  
Tatiana Alexandra Vasquez Villareal ◽  
María Belén Montaluisa Álvarez
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Therapeutic Potential ◽  
Pathogenic Fungi ◽  
Trichophyton Mentagrophytes ◽  
Microsporum Canis ◽  
The One ◽  
One Way Anova

Background: Currently, there is a trend towards using natural and ethnopharmacological species with therapeutic potential. This investigation evaluated the antifungal activity of two species in the Ecuadorian Andes, which are used in treating dermatomycosis: Ambrosia arborescens Mill. (Marco) and Aristeguietia glutinosa Lam. (Matico). Methods: We worked with seven concentrations (100 to 700ppm) of Ambrosia arborescens Mill. extract and ten concentrations (0.5 to 5%) of essential oil (EO) of Aristeguietia glutinosa Lam. on Trichophyton mentagrophytes ATCC 9533, Trichophyton rubrum ATCC 28188, Microsporum canis ATCC 36299 and Candida albicans ATCC 10231. The methodology used was a modified version of the Kirby-Bauer method, using diffusion in agar wells. Results: The Tukey test, after the one-way Anova, determined effective concentrations of EO: 5% for Trichophyton mentagrophytes, 4.5% for Trichophyton rubrum, 5% for Microsporum canis and 2% for Candida albicans. In the extracts, the concentration of 700ppm was used for Trichophyton mentagrophytes, Trichophyton rubrum, and 600ppm for Microsporum canis and Candida albicans. Conclusions: The evaluation of the antifungal activity of the Ambrosia arborescens extract showed inhibition in the studied dermatophytes in each one of the planted concentrations (100 to 700ppm). The evaluation of the antifungal activity of Aristeguietia glutinosa EO showed inhibition in the studied dermatophytes in each of the planted concentrations (0.5 to 5%).

scholarly journals Antifungal Activity of Pericopsis (Afrormosia) laxiflora (Benth.) Bark on Ringworm Germs

2020 ◽  
pp. 1-9
Author(s):  
Ouattara Abou ◽  
Bolou Gbouhoury Eric-Kévin ◽  
Koffi Allali Eugène ◽  
Yasseu Hyacinthe ◽  
Ouattara Karamoko ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Cote D'ivoire ◽  
Inhibitory Concentration ◽  
Trichophyton Rubrum ◽  
Trichophyton Mentagrophytes ◽  
Fungal Strain ◽  
Phytochemical Study ◽  
High Frequencies ◽  
The Subject ◽  
Hydroethanolic Extract

Dermatophytes are responsible for ringworms that are very often found on the heads of children in Africa. In Côte d'Ivoire, ringworms have been the subject of several studies revealing fairly high frequencies. Aims: The present work consisted essentially in studying the antifungal activity of the barks of Pericopsis laxiflora, a plant from the Ivorian pharmacopoeia on germs responsible for ringworm. Methodology: The 70% hydroethanolic extract of the bark of Pericopsis laxiflora was prepared and tested on Trichophyton mentagrophytes and Trichophyton rubrum. In addition, by staining and precipitation tests, phytochemical sorting was carried out on this extract. Results: Faced with the hydroethanolic extract, Trichophyton mentagrophytes recorded a Minimun Inhibitory Concentration (MIC) which is equal to the Minimun Fungicidal Concentration(MFC) (MIC = MFC = 6.25 mg/mL). For the fungal strain of T. rubrum, the MFC obtained (100 mg/mL) was twice the MIC (50 mg/mL). The phytochemical study of this extract revealed the presence of sterols and polyterpenes, flavonoids and catechic tannins. Conclusion: The results suggest that P. laxiflora extract could therefore be useful in the fight against dermatophytes.

scholarly journals UJI AKTIVITAS ANTIJAMUR BEBERAPA SENYAWA MONOKARBONIL ANALOG CURCUMIN HASIL SINTESIS

2018 ◽  
Vol 5 (2) ◽  
pp. 149
Author(s):  
Ismi Rahmawati ◽  
Desi Purwaningsih
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
1H Nmr ◽  
Aldol Condensation ◽  
Fungal Infections ◽  
Trichophyton Mentagrophytes ◽  
Curcumin Analogue ◽  
Pityrosporum Ovale ◽  
Post Hoc

Antifungal Activity of Some Synthesized Mono-Carbonyl Analogue Compounds of CurcuminABSTRACTFungal resistance can pose a threat to future fungal infections, therefore studies to find other compounds that have antifungal activity need to be done. The aim of this study was to examine antifungal activity of synthesized curcumin analogue compounds i.e. 2,6-Bis-(2'-furilidin)-cyclohexanone (26FuH); 2,5-Bis-(2'-furilidine)-cyclopentanone (25FuP) and 1,5-Difuril-1,4-pentadien-3-on (15FuA). The curcumin analogue compound was successfully synthesized with Aldol condensation using KOH 7.5% as the catalyst. The compound was purified and characterized by melting point, thin layer chromatography, gas chromatography with mass spectrometry, FTIR spectrophotometry, spectrophotometry 1H-NMR. The results showed pure compounds and have a structure that corresponds to the target compounds. All compound were assayed as antifungal against Candida albicans, Pityrosporum ovale, Aspergillus niger, and Trichophyton mentagrophytes. The activity of each compound represented by inhibitory diameter was analyzed by one-way ANOVA followed by post hoc Tukey (p<0.05). All three compounds showed antifungal activity against Candida albicans, Pityrosporum ovale, and Aspergillus niger. The best antifungal activity was shown by 26FuH against Pityrosporum ovale.Keywords: antifungal activity, curcumin, monocarbonyl, Pityrosporum ovale, synthesis ABSTRAKResistensi jamur dapat menjadi ancaman pada kasus infeksi jamur di masa mendatang, oleh sebab itu penelitian untuk menemukan senyawa lain yang memiliki aktivitas antijamur perlu dilakukan. Penelitian ini bertujuan untuk menguji aktivitas antijamur senyawa analog curcumin hasil sintesis yaitu senyawa 2,6-Bis-(2’-furilidin)-sikloheksanon (26FuH); 2,5-Bis-(2’-furilidin)-siklopentanon (25FuP) dan 1,5-Difuril-1,4-pentadien-3-on (15FuA). Senyawa analog curcumin sudah berhasil disintesis dengan metode kondensasi Aldol menggunakan katalis KOH 7,5%. Senyawa hasil sintesis dimurnikan dan dikarakterisasi dengan menggunakan pemeriksaan organoleptis, titik lebur, kromatografi lapis tipis, kromatografi gas dengan spektrometri massa, spektrofotometri FTIR, spektrofotometri 1H-NMR. Hasil menunjukkan senyawa murni dan struktur sesuai senyawa target. Hasil sintesis diuji aktivitas antijamur terhadap Candida albicans, Pityrosporum ovale, Aspergillus niger dan Trichophyton mentagrophytes. Hasil diameter daya hambat dianalisis dengan ANOVA satu arah dilanjutkan post hoc Tukey (p<0,05). Ketiga senyawa memiliki aktivitas antijamur terhadap jamur Candida albicans, Pityrosporum ovale, dan Aspergillus niger. Aktivitas antijamur terbaik adalah senyawa 26FuH terhadap jamur Pityrosporum ovale.Kata Kunci: aktivitas antijamur, curcumin, monokarbonil, Pityrosporum ovale, sintesis

scholarly journals Screening Repurposing Libraries for Identification of Drugs with Novel Antifungal Activity

2020 ◽  
Vol 64 (9) ◽  
Author(s):  
Gina Wall ◽  
Jose L. Lopez-Ribot
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Alternative Pathway ◽  
Drug Repurposing ◽  
Pathogenic Fungi ◽  
Multidrug Resistant ◽  
Modern Medicine ◽  
Antifungal Drugs ◽  
Promising Alternative

ABSTRACT Fungal organisms are ubiquitous in nature, and progress of modern medicine is creating an expanding number of severely compromised patients susceptible to a variety of opportunistic fungal infections. These infections are difficult to diagnose and treat, leading to high mortality rates. The limited antifungal arsenal, the toxicity of current antifungal drugs, the development of resistance, and the emergence of new multidrug-resistant fungi, all highlight the urgent need for new antifungal agents. Unfortunately, the development of a novel antifungal is a rather long and expensive proposition, and no new classes of antifungal agents have reached the market in the last 2 decades. Drug repurposing, or finding new indications for old drugs, represents a promising alternative pathway to drug development that is particularly appealing within the academic environment. In the last few years, there has been a growing interest in repurposing approaches in the antifungal arena, with multiple groups of investigators having performed screenings of different repurposing libraries against different pathogenic fungi in search for drugs with previously unrecognized antifungal effects. Overall, these repurposing efforts may lead to the fast deployment of drugs with novel antifungal activity, which can rapidly bring benefits to patients, while at the same time reducing health care costs.

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