Artemisia argyi extract subfraction exerts an antifungal effect against dermatophytes by disrupting mitochondrial morphology and function / 中国天然药物

Artemisia argyi (A. argyi), a plant with a longstanding history as a raw material for traditional medicine and functional diets in Asia, has been used traditionally to bathe and soak feet for its disinfectant and itch-relieving properties. Despite its widespread use, scientific evidence validating the antifungal efficacy of A. argyi water extract (AAWE) against dermatophytes, particularly Trichophyton rubrum, Trichophyton mentagrophytes, and Microsporum gypseum, remains limited. This study aimed to substantiate the scientific basis of the folkloric use of A. argyi by evaluating the antifungal effects and the underlying molecular mechanisms of its active subfraction against dermatophytes. The results indicated that AAWE exhibited excellent antifungal effects against the three aforementioned dermatophyte species. The subfraction AAWE6, isolated using D101 macroporous resin, emerged as the most potent subfraction. The minimum inhibitory concentrations (MICs) of AAWE6 against T. rubrum, M. gypseum, and T. mentagrophytes were 312.5, 312.5, and 625 μg·mL-1, respectively. Transmission electron microscopy (TEM) results and assays of enzymes linked to cell wall integrity and cell membrane function indicated that AAWE6 could penetrate the external protective barrier of T. rubrum, creating breaches ("small holes"), and disrupt the internal mitochondrial structure ("granary"). Furthermore, transcriptome data, quantitative real-time PCR (RT-qPCR), and biochemical assays corroborated the severe disruption of mitochondrial function, evidenced by inhibited tricarboxylic acid (TCA) cycle and energy metabolism. Additionally, chemical characterization and molecular docking analyses identified flavonoids, primarily eupatilin (131.16 ± 4.52 mg·g-1) and jaceosidin (4.17 ± 0.18 mg·g-1), as the active components of AAWE6. In conclusion, the subfraction AAWE6 from A. argyi exerts antifungal effects against dermatophytes by disrupting mitochondrial morphology and function. This research validates the traditional use of A. argyi and provides scientific support for its anti-dermatophytic applications, as recognized in the Chinese patent (No. ZL202111161301.9).

Study on the antifungal activity and mechanism of Huangqin decoction against Trichophyton mentagrophytes / 中国药房

OBJECTIVE To study the antifungal activity of Huangqin decoction （HQD） against Trichophyton mentagrophytes and explore its mechanism. METHODS Minimal inhibitory concentration （MIC）， minimal fungicidal concentration （MFC）， mycelial length， spore germination rate， biomass and mycelium ultrastructure observation were performed to evaluate the antifungal activity of HQD against T. mentagrophytes. The effects of HQD on the cell wall of T. mentagrophytes were detected through sorbitol protection experiment. By measuring the content of ergosterol and the activities of squalene epoxide （SE） and lanosterol 14α-demethylase （CYP51）， the activity of HQD on the cell membrane of T. mentagrophytes was investigated. The effects of HQD on T. mentagrophytes mitochondria were investigated by determining the activities of malate dehydrogenase （MDH）， succinate dehydrogenase （SDH）， and ATPases （including sodium potassium ATPase， calcium magnesium ATPase， and total ATPase）. RESULTS HQD exhibited significant antifungal activity against T. mentagrophytes with MIC of 3.13 mg/mL and MFC of 25 mg/mL. After intervention with HQD， the mycelial length of T. mentagrophytes was significantly shortened （P＜0.05）； spore germination rate， biomass， the content of ergosterol in the cell membrane， the activities of SE and CYP51 in the cell membrane and MDH， SDH and ATPase in mitochondria were all decreased significantly （P＜0.05）； cell structure had been ；damaged to a certain extent， but the integrity of the cell wall had not been affected. CONCLUSIONS HQD shows significant antifungal activity against T. mentagrophytes， the mechanism of which may be associated with reducing the 0791- content of ergosterol in the cell membrane and the activities of SE， CYP51， and mitochondria-related enzymes.

Isolation of Actinomycetes from Arachis hypogaea L. and Gossypium herbaceum L. for Screening Antibacterial and Antifungal Activities

The principal objective of the present study was to check the antimicrobial activity of Actinomycetes isolated from soil samples collected from the fields of Arachis hypogea L. and Gossipium herbaceum L. against different plant pathogenic strains. Various soil samples were isolated from fields located near the Junagadh district, Gujarat, India. Isolation was followed by a serial dilution process which was later plated on Actinomycete Isolation Agar (AIA) media. Potential colonies were subjected to screening, purification, and storage in glycerol stock. Morphological and Biochemical characterization of the isolates was performed. Isolated candidates were subjected to extraction for the production of the antimicrobial compound. The antimicrobial activity of the purified extract of isolates was tested. Total 30 actinomycete isolates were evaluated for antagonistic activity against pathogenic microorganisms. Isolates C-25, C-15, and G-1 showed the best results in the decreasing order of their potency against fungal pathogens, and C-5, C-25, C-14, and C-13 showed the best results in decreasing order of potency against bacterial pathogens. 3 isolates inhibited all 4 test fungi. 10 isolates inhibited 3 test fungi. 11 isolates inhibited 2 test fungi. 6 isolates did not inhibit any test fungi. 4 isolates show potent inhibition. 15 inhibited Macrophomina. C-10 showed a 1 cm inhibition zone & G-1 showed a 0.8 cm zone of inhibition. 12 isolates gave 0.2-0.6 cm zone and 15 isolates gave negative results against Macrophomina. C-10 showed a very potent zone of inhibition of 0.7 cm. 9 isolates showed a 0.1-0.5 cm zone of inhibition. 20 isolates did not show inhibition against Fusarium. 1 isolate C-11(a) gave the 1cm potent zone of inhibition. 15 isolates gave the 0.7-0.2cm inhibition of the growth. 14 isolates gave negative results against Alternaria fungus. From these results, it was concluded that isolates had antibacterial and antifungal activities and could be used in the development of new antibiotics for pharmaceutical or agricultural purposes.

Investigation on the antifungal activity of pyranium derivatives N2 / 药学实践杂志

Objective To study the antifungal activity of N2 derivatives. Methods The anti-fungal activity of N2 compounds was investigated by micro-liquid dilution. Then the activity of N2 compounds on hyphal and biofilm formation was investigated. Results N2 compounds had significant antifungal activity against Candida albicans. It also expressed actively inhibitory effect on hyphal and biofilm formation. The mechanism of its fungicidal function was to damage the structure of candida albicans’ cell membrane and cell wall. Conclusion The results showed that N2 had obvious antifungal activity against Candida albicans., which provided a new idea for the development of antifungal drugs and the solution of antifungal drugs resistance.

Unraveling the serial glycosylation in the biosynthesis of steroidal saponins in the medicinal plant Paris polyphylla and their antifungal action

Sugar-sugar glycosyltransferases play important roles in constructing complex and bioactive saponins. Here, we characterized a series of UDP-glycosyltransferases responsible for biosynthesizing the branched sugar chain of bioactive steroidal saponins from a widely known medicinal plant Paris polyphylla var. yunnanensis. Among them, a 2'-O-rhamnosyltransferase and three 6'-O-glucosyltrasferases catalyzed a cascade of glycosylation to produce steroidal diglycosides and triglycosides, respectively. These UDP-glycosyltransferases showed astonishing substrate promiscuity, resulting in the generation of a panel of 24 terpenoid glycosides including 15 previously undescribed compounds. A mutant library containing 44 variants was constructed based on the identification of critical residues by molecular docking simulations and protein model alignments, and a mutant UGT91AH1Y187A with increased catalytic efficiency was obtained. The steroidal saponins exhibited remarkable antifungal activity against four widespread strains of human pathogenic fungi attributed to ergosterol-dependent damage of fungal cell membranes, and 2'-O-rhamnosylation appeared to correlate with strong antifungal effects. The findings elucidated the biosynthetic machinery for their production of steroidal saponins and revealed their potential as new antifungal agents.

Expression of BmSPI38 tandem multimers in Escherichia coli and its antifungal activity / 生物工程学报

The aim of this study was to prepare tandem multimeric proteins of BmSPI38, a silkworm protease inhibitor, with better structural homogeneity, higher activity and stronger antifungal ability by protein engineering. The tandem multimeric proteins of BmSPI38 were prepared by prokaryotic expression technology. The effects of tandem multimerization on the structural homogeneity, inhibitory activity and antifungal ability of BmSPI38 were explored by in-gel activity staining of protease inhibitor, protease inhibition assays and fungal growth inhibition experiments. Activity staining showed that the tandem expression based on the peptide flexible linker greatly improved the structural homogeneity of BmSPI38 protein. Protease inhibition experiments showed that the tandem trimerization and tetramerization based on the linker improved the inhibitory ability of BmSPI38 to microbial proteases. Conidial germination assays showed that His6-SPI38L-tetramer had stronger inhibition on conidial germination of Beauveria bassiana than that of His6-SPI38-monomer. Fungal growth inhibition assay showed that the inhibitory ability of BmSPI38 against Saccharomyces cerevisiae and Candida albicans could be enhanced by tandem multimerization. The present study successfully achieved the heterologous active expression of the silkworm protease inhibitor BmSPI38 in Escherichia coli, and confirmed that the structural homogeneity and antifungal ability of BmSPI38 could be enhanced by tandem multimerization. This study provides important theoretical basis and new strategies for cultivating antifungal transgenic silkworm. Moreover, it may promote the exogenous production of BmSPI38 and its application in the medical field.

Synthesis and antifungal evaluation of chalcone derivatives combined with fluconazole against drug-resistant Candida albicans / 中国药科大学学报

@#Chalcone is a common scaffold in natural products with optimal properties and biological activities.In this study, we designed and prepared eight new coumarin-chalcone derivatives (5a-5h), and confirmed their structures by 1H NMR and 13C NMR. Their in vitro antifungal activity combined with fluconazole (FLC) against drug-resistant Candida albicans was tested by microdilution method.The results indicated that most chalcone derivatives showed good antifungal activity against drug resistant Candida albicans with FLC, particularly with compound 5g displaying better antifungal activity (MIC50 = 5.60 μg/mL) than FLC (MIC50 = 200 μg/mL) when combined with FLC, so, these derivatives could be used as synergists of antifungal drugs.

Design, synthesis and antifungal activity of novel triazoles containing propyl side chains / 药学实践杂志

Objective To study the antifungal activity of a new series of triazole compounds with n-propyl side chain and disubstituted benzyl structure. Methods Eleven target compounds were designed and synthesized. The structures were confirmed by 1H NMR, and some compounds were confirmed by 13C NMR or HRMS. Three fungal strains were selected as experimental strains, and the antifungal activity was tested in vitro according to the standardized antifungal sensitivity test method recommended by National Committee for Clinical Laboratory Standards (NCCLS). Results Compound B11 showed better activity against candida albicans SC5314 than fluconazole and was comparable to posaconazole; Compounds B10, B11 and B4 showed better activity against cryptococcus neoformanis H99 than fluconazole, while compounds B2, B3, B5, B6 and B7 showed similar activity to fluconazole against cryptococcus neoformanis H99; while all compounds showed poor activity against aspergillus fumigatus. Conclusion Some of the target compounds with n-propyl side chain and disubstituted benzyl group structure had certain antifungal activity and could be identified as potential lead antifungal drugs.

Study on the extraction and antifungal activity of volatile oil from stems，leaves and roots of Glehnia littoralis / 中国药房

OBJECTIVE To explore the extraction process of volatile oil from the stems， leaves and roots of Glehnia littoralis， analyze the chemical components of the volatile oil from the stems， leaves and roots of G. littoralis， and preliminarily evaluate its in vitro antifungal activity. METHODS Based on the steam distillation method， single factor test and orthogonal experiment were conducted to optimize the extraction method of volatile oil from the stems， leaves and roots of G. littoralis. The chemical components of the volatile oil from the stems， leaves and roots of G. littoralis were identified by using gas chromatography-mass spectrometry （GC-MS) technology and their relative contents were calculated. The antifungal activity of volatile oils from the stems， leaves and roots of G. littoralis against Fusarium solani， Fusarium incarnatum， Fusarium oxysporum， Aspergillus parasiticus and Aspergillus flavus was determined by paper diffusion method. RESULTS The optimal extraction process of G. littoralis was solid-liquid ratio of 1∶15， distillation time of 5 hours， and KCl concentration of 15%. Eleven components were identified from the volatile oil of the stems and leaves of G. littoralis， and a total of eight components were identified from the volatile oil of the roots. Ginsenethinol was a common component in the volatile oil from the stems， leaves and roots of G. littoralis， its contents in the stems and leaves， roots were 38.21% and 74.02%， respectively. The volatile oil from the stems， leaves and roots of G. littoralis had a certain E-mail：zwhjzs@126.com inhibitory effect on F. solani， F. incarnatum， F. oxysporum， A. parasiticus and A. flavus， especially volatile oil from the stems and leaves. CONCLUSIONS There is a significant difference in chemical components of the volatile oil between the roots， stems and leaves of G. littoralis， both of which have certain in vitro antifungal activity.

The activity of propolis against pathogenic fungi isolated from human infections

Abstract Propolis is a resinous hive product collected by bees from the buds or other parts of plants. It is known for having various biological properties, including antifungal activity. Among the substances present in propolis, flavonoids and phenolic acids and their esters are responsible for its antifungal properties. This means that propolis is ideal for use as an antifungal agent in alternative medicine to treat a number of both topical and systemic infections caused by Candida species and other yeast-like fungi, dermatophyte and nondermatophyte moulds, without the serious side effects typical of synthetic treatment. It is also active against strains of fungi that are resistant to polyenes and azoles, the classes of drugs most commonly used to treat fungal infections. In this article, we review current knowledge about the activity of propolis from different parts of the world and its components in vitro and in vivo against pathogenic fungi isolated from human infections. The article also indicates the possible mechanism of antifungal activity of propolis and its components.

Antifungal potential of biosurfactants produced by strains of Bacillus spp. (Bacillales: Bacillaceae) selected by molecular screening / Potencial antifúngico de biosulfactantes producidos por cepas de Bacillus spp. (Bacillales: Bacillaceae) seleccionadas por tamizaje molecular

Introduction: Bacillus species are used as biological controllers for phytopathogenic fungi, and the mechanisms to produce controllers include biosynthesis of lipopeptide biosurfactants with antifungal activity. Objective: To evaluate the antifungal potential of the biosurfactants produced by Bacillus strains, selected by molecular screening, on Fusarium oxysporum. Methods: We selected four molecular markers, related to the biosynthesis of surfactin, fengicin, and lichenysin (srfA, spf, fenB, LichAA) in nine Bacillus strains. We used two mineral media with several culture conditions, for biosurfactant production, and a well diffusion test for antifungal potential. Results: Only the biosurfactant produced by UFAB25 inhibits the mycelial growth of F. oxysporum (44 % ± 13): this biosurfactant was positive for srfA, spf, and fenB genes involved in the synthesis of surfactin and fengicine. Antifungal activity depends on culture conditions and the strain. Conclusions: Genetic markers are useful to detect strains with antifungal potential, facilitating the selection of bio-controllers. The biosurfactant profile is influenced by the strain and by culture conditions.

Introducción: Especies de Bacillus han sido empleadas como controladores biológicos contra hongos fitopatógenos. Entre los mecanismos utilizados se destaca la biosíntesis de biosurfactantes lipopeptídicos con actividad antifúngica. Objetivo: Evaluar el potencial antifúngico de los biosurfactantes producidos por cepas Bacillus nativas, previamente seleccionadas mediante tamizaje molecular, sobre Fusarium oxysporum. Métodos: Se utilizaron cuatro marcadores moleculares, relacionados con la biosíntesis de surfactina, fengicina y liquenisina (srfA, spf, fenB, LichAA) sobre nueve cepas de Bacillus. Se utilizaron dos medios minerales con diferentes condiciones de cultivo para la producción del biosurfactante. Se evaluó el potencial antifúngico de los biosurfactantes mediante la prueba de difusión en pozos. Resultados: Se determinó que solo el biosurfactante producido por UFAB25 actúa como inhibidor del crecimiento micelial de Fusarium oxysporum (43.6 % ± 13), esta cepa es positiva para los genes srfA, spf y fenB, involucrados en la síntesis de surfactina y fengicina. La actividad antifúngica depende de las condiciones de cultivo y la cepa. Conclusiones: Los marcadores genéticos ayudan a detectar cepas con potencial antifúngico, facilitando la selección de biocontroladores. El perfil del biosurfactante está influenciado no solo por la cepa, sino también por las condiciones del cultivo.

Benchmarking of different microbes for their biosurfactants antifungal action against plant pathogens

The biotic stress caused by phytopathogens (bacteria, fungus, yeast and insect pests) is a primary factor in yield loss of plants. Biocontrol agents and their active compounds are used to manage such plant pathogens. Here, in our study, we screened four bacterial isolates identified as Bacillus cereus, B. anthracis, B. velezensis and Serratia marcescens after morphological, biochemical and molecular characterization (16s rDNA sequencing) for production of biosurfactant by foam forming activity, oil spreading tests and emulsification activity. Highest foam stability (75 min) and maximum emulsification activity E24% (75%) was observed by B. velezensis strain. Among all the four isolates, Bacillus velezensis strain produced maximum biosurfactant (0.349±0.004 g/50 mL). Biosurfactant of all the four bacterial isolates were checked for fungal inhibiton on PDA plate(s). Bacillus velezensis showed comparatively the highest percent inhibition 58.82, 88.15, 78.45,72.68, 83.96, 75.47, 68.07 and 88.44% against Colletotrichum falcatum, Fusarium oxysporum f sp. ciceri, Helminthosporium maydis, F. oxysporum f. sp. lycopersici, Aspergillus niger, Mucor sp., Helminthosporium oryzae and Rhizoctonia solani, respectively. Bacillus velezensis biosurfactant among all the four bacterial isolates was found to be most effective against the tested phytopathogens

A Review of Antifungal Activity of Combined Plant Extracts or Plant Exudates from Medicinal Plants either together or with Known Antifungal Agents

Medicinal plants provide humanity with important phytochemical compounds and extracts which are widely used in treatment of many diseases. Fungal infections are one of these diseases which are widely distributed especially in developing countries; medicinal plants are extensively used in developing countries. There are few antifungal agents, most of them are expensive and have many adverse effects, also there is high incidence of drug resistance among some available antifungal agents, hence for these mentioned reasons many people, especially in developing countries, use medicinal plants (either alone, combined together or combined with known antifungal drugs) in treatment of many fungal infections. This rise a new and important issue about plant(s) – plant(s) and plant(s) - drug interactions. The aim of this review is to try to fill the gap in understanding the interactions of plant(s) - plant(s) and plant(s) – drug(s) combinations by providing an overview of some evidence-based researches done in this field, so our review highlights many interactions between medicinal plants constituents with current available antifungal agents, these interactions may be synergistic, additive, indifferent or antagonistic, so, if there is any antagonistic effect, we recommend to avoid using the combination which caused this effect. We collected a lot of studies which studied the interactions between plant(s) (including extracts, isolated active constituents, essential oils, plants latexes and other phytochemicals) used either together or with conventional antifungal agents. This will not only bring about better understanding of both phytochemicals and antifungal activity, but also may help in searching and developing new safely and effective drugs, specially with those combinations which showed synergistic effect.

Synthesis and evaluation of antifungal activity studies of novel 2-(2-pyridyl)-2H-pyrazole-3-carboxamide derivatives

Background: Invasive fungal infections have negative impact on the health of immunocompromised individuals. With the development of fungal resistance to currently available antifungal drugs, there is a need to develop novel compounds with antifungal activity. Aims and Objectives: The objectives of the study are as follows: (1) To synthesize novel 2-(2-pyridyl)-2H-pyrazole-3-carboxamide derivatives and (2) to evaluate the antifungal activity of novel 2-(2-pyridyl)-2H-pyrazole-3-carboxamide derivatives. Materials and Methods: Novel 2-(2-pyridyl)-2H-pyrazole-3-carboxamide derivatives were prepared by multi step synthesis and characterized by LC-MS, 1HNMR and 13C NMR. The antifungal activity of these derivatives was assessed using Fusarium oxysporum, Aspergillus flavus, and Candida albicans by disc diffusion method. Results: We have synthesized fourteen derivatives of 2-(2-pyridyl)-2H-pyrazole-3-carboxamide. Most of the compounds possess good antifungal activity against F. oxysporum and C. albicans strains. Conclusion: We synthesized a series of novel 2-(2-pyridyl)-2H-pyrazole-3-carboxamide derivatives having good antifungal activity against F. oxysporus and C. albicans using a simple and low cost procedure.

Antifungal activity study on HDAC inhibitor Rocilinostat / 药学实践杂志

Objective To evaluate the in vitro synergistic antifungal activity of HDAC inhibitors in combination with azole drugs against azoles-resistant Candida strains. Methods The checkerboard microdilution method was used to evaluate the antifungal activity of the HDAC inhibitors in combination with azole drugs against clinically drug-resistant strains. The fungistatic activity and toxicity of Rocilinostat was determined through time-growth curve assay and cytotoxicity assay. Results The compound Rocilinostat combined with azole drugs showed excellent synergistic antifungal activity against a variety of azoles-resistant Candida albicans and Candida glabrata. The combination of high concentration Rocilinostat with FLC exhibited fungistatic effects. Very low toxicity was detected with Rocilinostat towards normal cells. Rocilinostat showed better HDAC inhibitory activity than SAHA. Conclusion As a fungi HDAC inhibitor, Rocilinostat has excellent in vitro synergistic antifungal activity and no severe toxicity to normal human cells.

In vitro antifungal properties of Aloe vera (L.) Burm. f. films incorporated with cinnamon essential oil against Lasiodoplodia theobromae in wax apple

Aims@#Wax apple is an important fruit crop in Malaysia and other tropical countries. However, the black spot disease caused by Lasiodoplodia theobromae can damage the wax apple plants, reducing fruit production and quality. Chemical fungicides are commonly used to overcome this disease. However, their overuse might increase fungal resistance to chemicals. Therefore, this study was aimed to evaluate the in vitro antifungal properties of an Aloe vera film incorporated with cinnamon oil on L. theobromae in wax apples.@*Methodology and results@#In vitro antifungal tests were conducted using the poisoned food. This present study found that the inhibition of L. theobromae mycelia when treated with A. vera film with different percentages of cinnamon oil was significantly different compared to the control film at (P<0.05). Results suggest that A. vera film without cinnamon oil showed the highest percentage of inhibition (37.31%) than other films with cinnamon oil due to the antagonistic and less synergistic effect. However, A. vera film with 0.07% of cinnamon oil showed the highest percentage of mycelia inhibition (36.15%) compared to the film with 0.06%, 0.05% and 0.04% cinnamon oil, with mycelia inhibition of 30.55%, 24.25% and 18.82%, respectively, while the mancozeb (positive control) showed 100% inhibition.@*Conclusion, significance and impact of study@#In conclusion, A. vera film alone had 37.31% inhibition compared to 36.15% inhibition in A. vera film with 0.7% cinnamon oil. As a result, a tiny amount of cinnamon oil added to the mixture might aid in controlling the black spot disease in wax fruits.

HPLC-DAD analysis, antifungal and antioxidant activity of Solanum dolichosepalum bitter extracts and fractions

Abstract Solanum dolichosepalum is a plant with anti-infective effects. It is a healing agent and has ethnopharmacological uses. In this study, the antifungal activity of extracts and fractions of this species on C. albicans and F. oxysporum was evaluated. The antioxidant activity was measured using the ABTS and DPPH methods, and by determining the total content of phenolic compounds. An HPLC-DAD qualitative analysis was carried out to identify phenolic compounds and alkaloids. Pearson's correlation coefficients were calculated. Inhibitory effects were found in all the extracts and fractions on the analyzed microorganisms. F. oxysporum was the microorganism most sensitive to the action of S. dolichosepalum extracts. All extracts and fractions showed antioxidant activity, with the acetone extract and the acetone fraction being those that generated the best results. The content of total phenolic compounds showed that acetone has a greater affinity with the phenolic compounds present in S. dolichosepalum. In this plant, p-Hydroxybenzoic, vanillic, ferulic, trans-cinnamic, caffeic, p-coumaric, and rosmarinic acids were found, as well as theobromine, quercetin, and luteolin. The content of total phenolic compounds was determined to be directly proportional to the inhibition of the ABTS and DPPH radicals, and the inhibition of the analyzed microorganisms. It was determined that the extracts and fractions obtained from S. dolichosepalum show antioxidant and antifungal activity.

Cashmirins A and B, new antifungal and urease inhibitory prenylated coumarins from Sorbus cashmiriana

Abstract Cashmirins A (1) and B (2), new prenylated coumarins, have been isolated from the EtOAc- soluble fraction of the whole plant of Sorbus cashmiriana Hedlung, Monog. along with seselin (3), scopoletin (4), 3-hydroxyxanthyletin (5) and luteolin (6), reported for the first time from this species. Their structures were elucidated by spectroscopic techniques including MS, 1D and 2D NMR spectroscopy. Both new compounds 1 and 2 were investigated for biological activities and showed significant antifungal and urease inhibitory activities. Compounds 1 and 2 exhibited significant activity against Aspergillus flavus, Macrophomina phaseolina, Trichophyton simii, Trichophyton schoenleinii, and Pseudallescheria boydri. Both compounds also exhibited significant inhibitory activity against Jack bean urease with IC50 values of 28.2±0.12 µM and 30.3±0.18 µM, respectively compared to thiourea used as positive control.

Poloxamer-enhanced solubility of griseofulvin and its related antifungal activity against Trichophyton spp

Abstract Poorly water-soluble drugs, such as the antifungal drug griseofulvin (GF), exhibit limited bioavailability, despite their high membrane permeability. Several technological approaches have been proposed to enhance the water solubility and bioavailability of GF, including micellar solubilization. Poloxamers are amphiphilic block copolymers that increase drug solubility by forming micelles and supra-micellar structures via molecular self-association. In this regard, the aim of this study was to evaluate the water solubility increment of GF by poloxamer 407 (P407) and its effect on the antifungal activity against three Trichophyton mentagrophytes and two T. rubrum isolates. The GF water solubility profile with P407 revealed a non-linear behavior, well-fitted by the sigmoid model of Morgan-Mercer-Flodin. The polymer promoted an 8-fold increase in GF water solubility. Fourier-transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), and 2D nuclear magnetic resonance (NMR Roesy) spectroscopy suggested a GF-P407 interaction, which occurs in the GF cyclohexene ring. These results were supported by an increase in the water solubility of the GF impurities with the same molecular structure. The MIC values recorded for GF ranged from 0.0028 to 0.0172 mM, except for T. Mentagrophytes TME34. Notably, the micellar solubilization of GF did not increase its antifungal activity, which could be related to the high binding constant between GF and P407.

Phytochemical Analysis, Antioxidant and Antifungal Activity of Essential oil and Extracts of Alpinia malaccensis (Burm. f. ) Roscoe flowers

Abstract The present study describes chemical composition, phytochemicals, antifungal activities, antioxidant assays and total phenolic content of essential oil and varied polarity solvent extract from flowers of Alpinia malaccensis (Burm.f.). Total 27 components were identified in essential oil by GC-MS with terpinen-4-ol (28.6%) and α- terpineol (12.8%) as the main constituent. The essential oil was found to have maximal levels of phenolic content (64.60 µg/mL) as compared to the other extracts. The antioxidant assay evaluated in extracts and essential oil by different methods revealed good-to-moderate antioxidant potential with different IC50 values viz. (188.02 -250.25 µg/mL) in Fe3+ reducing power, (153.15-201.59 µg/mL) in Fe2+ metal-chelating ability, (130.39-181.12 µg/mL) in DPPH, (88.29-187.32 µg/mL) in OH radical, (79.04-156.79 µg/mL), in NO radical and (138.72-233.00 µg/mL) in superoxide anion scavenging activities, respectively. The methanolic extract display remarkable fungicidal activity against the tested pathogens followed by dichloromethane extract, essential oil, hexane extract and petroleum ether extract respectively, with MIC values ranging from 31.25 to 500 µg/mL. Based on results, it can be inferred that the flower of A. malaccensis if explored further for its medicinal properties, might be a good source to develop a safe and sustainable natural food preservative