Ethnopharmacological survey, antioxidant and antifungal activity of medicinal plants traditionally used in Baham locality (Cameroon) to treat fungal infections

Background and Objective: The incidence of fungal infections has experienced a marked increase in the last two decades being limited to a few drugs with serious drawbacks. Combination therapy has emerged as an approach to improve the efficacy of currently used antifungal therapy that also may delay the evolution of resistance. Method: The objectives of this work are to present a bibliographic search on the plants used in traditional medicine in Argentina for ailments related to fungal infections and to investigate the antifungal activity of currently used antifungal drugs in combination with natural extracts. Results: Results of the bibliographic investigation showed that 153 species belonging to 56 families and 120 genera from Argentina are applied to treat signs and symptoms considered to maintain ethnopharmacological uses related to fungal infections, mainly for skin and mucosal conditions. Conclusion: Regarding the evaluation of the antifungal activity of combinations between extracts and antifungal drugs, we observed that extracts from plants species belonging to a genera traditionally used for ailments related to fungal infections have more chances of enhancing the activity of amphotericin B, fluconazole and itraconazole. In addition, we observed that there is a greater chance of finding an enhancement in the activity of the commercial antifungals when the combination is performed with extracts that have shown activity in solitary. Nevertheless, inactive extracts that would have been discarded according to the classic strategy displayed activity in combination and they continue being potential candidates in the search for new antifungals.

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In vitro antidermatophytic activity of bioactive compounds from selected medicinal plants

Journal of Analytical Science & Technology ◽

10.1186/s40543-021-00304-3 ◽

2021 ◽

Vol 12 (1) ◽

Author(s):

Daisy Savarirajan ◽

V. M. Ramesh ◽

Arunachalam Muthaiyan

Keyword(s):

Antifungal Activity ◽

Medicinal Plants ◽

Fungal Infections ◽

Host Cells ◽

Asparagus Racemosus ◽

Microsporum Gypseum ◽

Antifungal Compounds ◽

Antidermatophytic Activity

AbstractFungal infections are among the most difficult diseases to manage in humans. Eukaryotic fungal pathogens share many similarities with their host cells, which impairs the development of antifungal compounds. Therefore, it is desirable to harness the pharmaceutical potential of medicinal plants for antifungal drug discovery. In this study, the antifungal activity of sixteen plant extracts was investigated against selected dermatophytic fungi. Of the sixteen plants, the cladode (leaf) of Asparagus racemosus, and seed extract of Cassia occidentalis showed antifungal activity against Microsporum gypseum, Microsporum nanum, Trichophyton mentagrophytes and Trichophyton terrestre. The plant antifungal compounds were located by direct bioassay against Cladosporium herbarum. IR and NMR spectrometry analyses of these compounds identified the presence of saponin (in A. racemosus) and hydroxy anthraquinone (in C. occidentalis) in these antifungal compounds. The antidermatophytic activity of plant anthraquinone and saponins with reports of little or no hemolytic activity, makes these compounds ideal for alternative antifungal therapy and warrants further in-depth investigation in vivo.

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Efficacy of Novel Schiff base Derivatives as Antifungal Compounds in Combination with Approved Drugs Against Candida Albicans

Medicinal Chemistry ◽

10.2174/1573406415666181203115957 ◽

2019 ◽

Vol 15 (6) ◽

pp. 648-658 ◽

Cited By ~ 1

Author(s):

Manzoor Ahmad Malik ◽

Shabir Ahmad Lone ◽

Parveez Gull ◽

Ovas Ahmad Dar ◽

Mohmmad Younus Wani ◽

...

Keyword(s):

Schiff Base ◽

Candida Albicans ◽

Antifungal Activity ◽

Fungal Infections ◽

Total Sterol ◽

Antifungal Drugs ◽

New Drugs ◽

Ergosterol Biosynthesis ◽

Dependent Manner ◽

Schiff Base Derivatives

Background: The increasing incidence of fungal infections, especially caused by Candida albicans, and their increasing drug resistance has drastically increased in recent years. Therefore, not only new drugs but also alternative treatment strategies are promptly required. Methods: We previously reported on the synergistic interaction of some azole and non-azole compounds with fluconazole for combination antifungal therapy. In this study, we synthesized some non-azole Schiff-base derivatives and evaluated their antifungal activity profile alone and in combination with the most commonly used antifungal drugs- fluconazole (FLC) and amphotericin B (AmB) against four drug susceptible, three FLC resistant and three AmB resistant clinically isolated Candida albicans strains. To further analyze the mechanism of antifungal action of these compounds, we quantified total sterol contents in FLC-susceptible and resistant C. albicans isolates. Results: A pyrimidine ring-containing derivative SB5 showed the most potent antifungal activity against all the tested strains. After combining these compounds with FLC and AmB, 76% combinations were either synergistic or additive while as the rest of the combinations were indifferent. Interestingly, none of the combinations was antagonistic, either with FLC or AmB. Results interpreted from fractional inhibitory concentration index (FICI) and isobolograms revealed 4-10-fold reduction in MIC values for synergistic combinations. These compounds also inhibit ergosterol biosynthesis in a concentration-dependent manner, supported by the results from docking studies. Conclusion: The results of the studies conducted advocate the potential of these compounds as new antifungal drugs. However, further studies are required to understand the other mechanisms and in vivo efficacy and toxicity of these compounds.

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Smart Gn-Keto Nanohybrid Embedded Topical System for Effective Management of Dermatophytosis

Drug Delivery Letters ◽

10.2174/2210303108666181105112557 ◽

2019 ◽

Vol 9 (1) ◽

pp. 21-28

Author(s):

Nisha Sharma ◽

Shashikiran Misra

Keyword(s):

Antifungal Activity ◽

Fungal Infections ◽

High Surface ◽

High Surface Area ◽

Vital Role ◽

Common Disease ◽

Microdilution Method ◽

Enhanced Solubility ◽

Bioactive Agents

Background and Objectives: Dermatophytosis (topical fungal infection) is the 4th common disease in the last decade, affecting 20-25% world’s population. Patients of AIDS, cancer, old age senescence, diabetes, cystic fibrosis become more vulnerable to dermatophytosis. The conventional topical dosage proves effective as prophylactic in preliminary stage. In the advanced stage, the therapeutics interacts with healthy tissues before reaching the pathogen site, showing undesirable effects, thus resulting in pitiable patient compliance. The youngest carbon nano-trope “Graphene” is recently used to manipulate bioactive agents for therapeutic purposes. Here, we explore graphene via smart engineering by virtue of high surface area and high payload for therapeutics and developed graphene–ketoconazole nanohybrid (Gn-keto) for potent efficacy towards dermatophytes in a controlled manner. </P><P> Methods: Polymethacrylate derivative Eudragit (ERL100 and ERS 100) microspheres embedded with keto and Gn-keto nanohybrid were formulated and characterized through FTIR, TGA, and SEM. In vitro drug release and antifungal activity of formulated Gn-keto microspheres were assessed for controlled release and better efficacy against selected dermatophytes. </P><P> Results: Presence of numerous pores within the surface of ERL100 microspheres advocated enhanced solubility and diffusion at the site of action. Controlled diffusion across the dialysis membrane was observed with ERS100 microspheres owing to the nonporous surface and poor permeability. Antifungal activity against T. rubrum and M. canis using microdilution method focused on a preeminent activity (99.785 % growth inhibition) of developed nanohybrid loaded microspheres as compared to 80.876% of keto loaded microspheres for T. rubrum. The culture of M. canis was found to be less susceptible to formulated microspheres. Conclusion: Synergistic antifungal activity was achieved by nanohybrid Gn-Keto loaded microspheres against selected topical fungal infections suggesting a vital role of graphene towards fungi.

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Synthesis and Biological Activity of 3-(substitutedphenyl)-6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine: Part II

Anti-Infective Agents ◽

10.2174/2211352518666200617144227 ◽

2020 ◽

Vol 18 ◽

Author(s):

Niranjan Kaushik ◽

Nitin Kumar ◽

Anoop Kumar ◽

Vikas Sharma

Keyword(s):

Antifungal Activity ◽

Opportunistic Infections ◽

Fungal Infections ◽

Mass Spectral Data ◽

Triazole Derivatives ◽

Mass Spectral ◽

Fungal Strains ◽

Antifungal Properties ◽

Antifungal Potential ◽

Spectral Data Analysis

Background: Fungal infections are opportunistic infections that become a serious problem to human health. Objective: Considering the antifungal potential of triazole nucleus, the study was carried out with the objective to synthesize some novel triazole derivatives with antifungal potential. Method: 1,2,4-triazole derivatives were synthesized via a two step reaction (reported earlier). The first step involves reaction of substituted benzoic acid with thiocarbohydrazide to form 4-amino-3-(substituted phenyl)-5-mercapto-1, 2, 4-triazole derivatives (1a-1k) while in second step, synthesized compounds (1a-1k) were then subsequently treated with substituted acetophenone to yield substituted (4-methoxyphenyl-7H-[1, 2, 4] triazolo [3, 4-b][1,3,4] thiadiazine derivatives (2a-2k). All synthesized compounds were characterized by IR, 1H NMR, and Mass spectral data analysis and were screened for their antifungal properties against different fungal strains i.e. Candida tropicalis (ATCC-13803, ATCC-20913), Candida albicans (ATCC-60193), Candida inconspicua (ATCC-16783) and Candida glabrata (ATCC-90030, ATCC-2001). Results: Compound 2d displayed better percentage inhibition (26.29%, 24.81%) than fluconazole (24.44%, 22.96%) against ATCC-16783, ATCC-2001 fungal strains respectively at 100µg/ml. Compound 2f also displayed better percentage inhibition (28.51%) against ATCC-90030 as compared to fluconazone (27.4%) at 200 µg/ml. Similarly, compounds 2e and 2j also exhibited better antifungal properties than fluconazole at 200µg/ml. Compound 2e was found most potent against ATCC13803 (30.37%) and ATCC-90030 (30.37%) fungal strains as compared to fluconazole (28.14%, 27.4%) at 200 µg/ml respectively whereas compound 2j exhibited better antifungal activity (28.51%) against ATCC-60193 than fluconazole (27.7%) at 200 µg/ml. Conclusion: The results were in accordance with our assertions for triazole derivatives, as all compounds displayed moderate to good antifungal activity.

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Antifúngicos poliénicos. Mecanismo de acción y aplicaciones

Studies in the Economic History of Southern Africa ◽

10.22201/fm.24484865e.2020.63.2.02 ◽

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

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The Impact of Gelatin on the Pharmaceutical Characteristics of Fucoidan Microspheres with Posaconazole

Materials ◽

10.3390/ma14154087 ◽

2021 ◽

Vol 14 (15) ◽

pp. 4087

Author(s):

Marta Szekalska ◽

Aleksandra Citkowska ◽

Magdalena Wróblewska ◽

Katarzyna Winnicka

Keyword(s):

Antifungal Activity ◽

Drug Release ◽

Spray Drying ◽

Fungal Infections ◽

Drug Loading ◽

High Surface ◽

Vaginal Fluid ◽

Sustained Drug Release ◽

Candida Spp ◽

The Impact

Fungal infections and invasive mycoses, despite the continuous medicine progress, are an important globally therapeutic problem. Multicompartment dosage formulations (e.g., microparticles) ensure a short drug diffusion way and high surface area of drug release, which as a consequence can provide improvement of therapeutic efficiency compared to the traditional drug dosage forms. As fucoidan is promising component with wide biological activity per se, the aim of this study was to prepare fucospheres (fucoidan microparticles) and fucoidan/gelatin microparticles with posaconazole using the one-step spray-drying technique. Pharmaceutical properties of designed fucospheres and the impact of the gelatin addition on their characteristics were evaluated. An important stage of this research was in vitro evaluation of antifungal activity of developed microparticles using different Candida species. It was observed that gelatin presence in microparticles significantly improved swelling capacity and mucoadhesiveness, and provided a sustained POS release. Furthermore, it was shown that gelatin addition enhanced antifungal activity of microparticles against tested Candida spp. strains. Microparticles formulation GF6, prepared by the spray drying of 20% fucoidan, 5% gelatin and 10% Posaconazole, were characterized by optimal mucoadhesive properties, high drug loading and the most sustained drug release (after 8 h 65.34 ± 4.10% and 33.81 ± 5.58% of posaconazole was dissolved in simulated vaginal fluid pH 4.2 or 0.1 M HCl pH 1.2, respectively).

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Protective Antifungal Activity of Plantago major Extract Against the Phytopathogenic Fungi Phytophthora cinnamomi, Diplodia corticola and Colletotrichum Species

Proceedings ◽

10.3390/foods_2020-07678 ◽

2020 ◽

Vol 70 (1) ◽

pp. 94

Author(s):

Cláudia Ferreira ◽

Rui Oliveira

Keyword(s):

Antifungal Activity ◽

Secondary Metabolites ◽

Plant Extracts ◽

Phytophthora Cinnamomi ◽

Fungal Infections ◽

Petri Dish ◽

Phytopathogenic Fungi ◽

Colletotrichum Acutatum ◽

Lower Probability ◽

Plantago Major

Synthetic fungicides for crops protection raise environmental and human concerns due to accumulation in edible vegetables, showing significant toxicity to humans, and in soil, groundwater and rivers, affecting ecological balance. In addition, they are prone to the development of resistant strains because of the single target-based mechanism of action. Plant extracts provide attractive alternatives, as they constitute a rich source of biodegradable secondary metabolites, such as phenols, flavonoids and saponins, which have multiple modes of antifungal action and a lower probability of the development of resistant fungi. This work has the objective of identifying plant extracts with antifungal activity, aiming to contribute to food safety and sustainable agricultural practices. We selected a saponin-containing plant, Plantago major, and extracted secondary metabolites with 50% (v/v) ethanol, dried by evaporation, and dissolved in water. For antifungal activity, the phytopathogenic fungi Colletotrichum acutatum, Colletotrichum gloeosporioides, Colletotrichum godetiae, Colletotrichum nymphaeae, Diplodia corticola and Phytophthora cinnamomi were selected because they affect fruits and vegetables, such as strawberry, almond, apple, avocado, blueberry and chestnut trees. The aqueous extract was incorporated into PDA medium at different concentrations and mycelial discs were placed in the center of each Petri dish. Growth was measured as the radial mycelial growth at 3, 6, and 9 days incubation at 25 °C in the dark. The maximum growth inhibition (32.2%) was obtained against P. cinnamomi with 2000 µg/mL extract followed by C. gloeosporioides (25.7%) on the sixth day and by C. godetiae and C. nymphaeae (21.1%) on the ninth day. Results show that P. major presents antifungal activity in all phytopathogenic fungi tested and the extract can be used to protect important crops, by inhibiting the development of fungal infections and promoting food security and a sustainable agriculture.

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GROWTH INHIBITORY ACTIVITIES OF THE RHIZOME CRUDE EXTRACT OF Curcuma longa ON THE HUMAN PATHOGENIC FUNGUS Mucor circinelloides

10.18173/2354-1059.2020-0051 ◽

2020 ◽

Vol 65 (10) ◽

pp. 82-91

Author(s):

Phuong Nguyen Anh ◽

Mai Le Thi Tuyet ◽

Trung Trieu Anh

Keyword(s):

Antifungal Activity ◽

Crude Extract ◽

Fungal Infections ◽

Early Stage ◽

Curcuma Longa ◽

Pathogenic Fungus ◽

Mucor Circinelloides ◽

Antifungal Drugs ◽

Diffusion Method ◽

Dilution Method

Mucormycosis is an uncommon but life-threatening invasive fungal infection, mostly occurs in immunocompromised patients. Lacking the appropriate antifungal drugs is one of the reasons that lead to difficulties in the management of mucormycosis. Curcuma longa has been used traditionally and widely to treat various diseases, including fungal infections. In the search for novel antifungal compounds from natural resources, we evaluated the effect of rhizome crude extract of C. longa on Mucor circinelloides – a causal agent of mucormycosis. The results of screening, using broth dilution method and agar-well diffusion method, showed that the C. longa extract exhibited promising antifungal activity against the fungus M. circinelloides. In liquid medium, C. longa extract decreased the ability of spore germination and the speed of hyphae formation of M. circinelloides decreased by up to approximately 70% and 90%, respectively. Besides, in a solid medium, the crude extract presented similar activity with amphotericin B (400 μg\mL) in decreasing the growth of M. circinelloides by nearly 77%. Moreover, the extract of C. longa also likely to induce the yeast-like type of growth of the dimorphic M. circinelloides in the early stage. These results suggest the plant could be a potential source for further study on biochemical components and the mechanism of its antifungal activity.

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Antifungal Efficacy of Marine Macroalgae against Fungal Isolates from Bronchial Asthmatic Cases

Molecules ◽

10.3390/molecules23113032 ◽

2018 ◽

Vol 23 (11) ◽

pp. 3032 ◽

Cited By ~ 14

Author(s):

Suresh Mickymaray ◽

Wael Alturaiki

Keyword(s):

Antifungal Activity ◽

Fungal Pathogens ◽

Fungal Infections ◽

Algal Species ◽

Marine Macroalgae ◽

Minimum Fungicidal Concentration ◽

Asthmatic Patients ◽

The Cost ◽

Algal Extracts ◽

Airway Colonization

Fungal sensitization is very common in bronchial asthmatic cases, and the connection with airway colonization by fungi remains uncertain. Antifungal therapy failure is a significant fraction of the cost and morbidity and mortality in the majority of the asthmatic cases. Hence, the present study aimed to investigate the antifungal activity of five marine macroalgae—Acanthaophora specifera, Cladophoropsis sp., Laurencia paniculata, Tydemania sp., and Ulva prolifera—which were tested on selected fungal pathogens isolated from 15 sputum of 45 bronchial asthmatic patients. The highest antifungal activity was observed in ethanol fractions of L. paniculata followed by U. prolifera, Cladophoropsis sp., A. specifera, and Tydemania sp. The minimum fungicidal concentration and minimum inhibitory concentration values of the ethanolic fractions of algal species were found to be 125–1000 µg/mL and 125–500 µg/mL, respectively. The algal extracts contained terpene alcohol, diterpene, steroids, sesquiterpene, and sesquiterpene alcohol, as determined by GC–MS/MS analyses. The present study shows that the marine macroalgae containing bioactive compounds had excellent inhibitory activity against a variety of fungal pathogens, which may be useful for combating fungal infections and recovering from chronic asthmatic states.

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