Antifungal Potential Research Articles

Chemical composition and antifungal potential of Vinca rosea leaf essential oil and extracts from Northern India

Chemical composition and antifungal potential of <i>Vinca rosea</i> leaf essential oil and extracts from Northern India

Chitinase-functionalized UiO-66 framework nanoparticles active against multidrug-resistant Candida Auris

Candida auris (C. auris) is a yeast that has caused several outbreaks in the last decade. Cell wall chitin plays a primary role in the antifungal resistance of C. auris. Herein, we investigated the potential of chitinase immobilized with UiO-66 to act as a potent antifungal agent against C. auris. Chitinase was produced from Talaromyces varians SSW3 in a yield of 8.97 U/g dry substrate (ds). The yield was statistically enhanced to 120.41 U/g ds by using Plackett–Burman and Box–Behnken design. We synthesized a UiO-66 framework that was characterized by SEM, TEM, XRD, FTIR, a particle size analyzer, and a zeta sizer. The produced framework had a size of 70.42 ± 8.43 nm with a uniform cubic shape and smooth surface. The produced chitinase was immobilized on UiO-66 with an immobilization yield of 65% achieved after a 6 h loading period. The immobilization of UiO-66 increased the enzyme activity and stability, as indicated by the obtained Kd and T1/2 values. Furthermore, the hydrolytic activity of chitinase was enhanced after immobilization on UiO-66, with an increase in the Vmax and a decrease in the Km of 2- and 38-fold, respectively. Interestingly, the antifungal activity of the produced chitinase was boosted against C. auris by loading the enzyme on UiO-66, with an MIC50 of 0.89 ± 0.056 U/mL, compared to 5.582 ± 0.57 U/mL for the free enzyme. This study offers a novel promising alternative approach to combat the new emerging pathogen C. auris.

The Effect of Broccoli Glucosinolates Hydrolysis Products on Botrytis cinerea: A Potential New Antifungal Agent.

The present study investigates the interactions between eight glucosinolate hydrolysis products (GHPs) sourced from broccoli by-products and the detoxifying enzymes of Botrytis cinerea, namely eburicol 14-alpha-demethylase (CYP51) and glutathione-S-transferase (GST), through in silico analysis. Additionally, in vitro assays were conducted to explore the impact of these compounds on fungal growth. Our findings reveal that GHPs exhibit greater efficacy in inhibiting conidia germination compared to mycelium growth. Furthermore, the results demonstrate the antifungal activity of glucosinolate hydrolysis products derived from various parts of the broccoli plant, including inflorescences, leaves, and stems, against B. cinerea. Importantly, the results suggest that these hydrolysis products interact with the detoxifying enzymes of the fungus, potentially contributing to their antifungal properties. Extracts rich in GHPs, particularly iberin and indole-GHPs, derived from broccoli by-products emerge as promising candidates for biofungicidal applications, offering a sustainable and novel approach to plant protection by harnessing bioactive compounds from agricultural residues.

Exploring the potential of chitin and chitosan in nanobiocomposites for fungal immunological detection and antifungal action

Chitin is a polymer of N-acetylglucosamine and an essential component of the fungal cell wall. Chitosan is the deacetylated form of chitin and is also important for maintaining the integrity of this structure. Both polysaccharides are widely distributed in nature and have been shown to have a variety of applications in biomedicine, including their potential in immune sensing and as potential antifungal agents. In addition, chitin has been reported to play an important role in the pathogen-host interaction, involving innate and adaptive immune responses. This paper will explore the role of chitin and chitosan when incorporated into nanobiocomposites to improve their efficacy in detecting fungi of medical interest and inhibiting their growth. Potential applications in diagnostic and therapeutic medicine will be discussed, highlighting their promise in the development of more sensitive and effective tools for the early diagnosis of fungal infections. This review aims to highlight the importance of the convergence of nanotechnology and biology in addressing public health challenges.

In vitro antibacterial and antifungal potentials of Ocimum tenuiflorum and Ocimum gratissimum essential oil

IntroductionOcimum known as Tulsi has various health benefits mentioned in Ayurveda. Ocimum polysaccharides are used in pharmacology as the capacity to prevent ageing, boost immunity, suppress tumor growth, reduce diabetes mellitus and function as an antioxidant. Therefore, the goal of the current investigation was to examine the antibacterial and antifungal activities of Ocimum tenuiflorum and Ocimum gratissimum essential oils. MethodEssential oils of Ocimum tenuiflorum and Ocimum gratissimum were extracted by hydrodistillation method and antibacterial and antifungal activities were done by agar well diffusion and broth micro dilution method. Furthermore, In silico toxicity analysis was done by the SwissADME server. ResultOcimum gratissimum essential oil was found to have an extraction yield of 2.75 ± 0.5 % and 3.90 ± 0.5 % for O. tenuiflorum. α-thujene (15.33 %), eugenol (16.11 %) and β-terpineol (7.75 %) were the major phytocompounds of O. tenuiflorum whereas chavibetol (17.70), α-pinene (15.16 %) and bicyclosesquiphellandrene (9.07 %) were the major phytocompounds of O. gratissimum essential oil. Forging ahead, essential oil of O. tenuiflorum showed MIC of 0.078 % against E. coli ATCC29213, 0.3125 % against K. pneumoniae MTCC39, 0.078 % against S. aureus ATCC25922, 0.625 % against both C. albicans, MTCC277 and ATCC90028, however, essential oil of O. gratissimum showed MIC of 1.25 % against E. coli ATCC29213, followed by K. pneumonia MTCC39 (2.5 %) and S. aureus ATCC25922 (2.5 %) and 5.0 % against both C. albicans MTCC277 and ATCC90028. Certainly, phytocompounds of both the Ocimum spp. also fulfilled the Lipinski rule and showed characteristics similar to drugs. β-terpinole demonstrated the best antibacterial activity with a Pa value of 0610 and β-caryophyllene and caryophyllene oxide had the best antifungal activity with a Pa value of 0647. ConclusionTo conclude, the current study showed that O. tenuiflorum and O. gratissimum have good antibacterial and antifungal activity and on the basis of further experimentation, can be used as a source of natural antimicrobials.

Antifungal activity of synthetic xanthenone against fluconazole-resistant Candida auris and its mechanism of action

Candida auris, an emerging multidrug-resistant fungal pathogen discovered in Japan in 2009, poses a significant global health threat, with infections reported in about 25 countries. The escalation of drug-resistant strains underscores the urgent need for new treatment options. This study aimed to investigate the antifungal potential of 2,3,4,4a-tetrahydro-1H-xanthen-1-one (XA1) against C. auris, as well as its mechanism of action and toxic profile. The antifungal activity of XA1 was first evaluated by determining the minimum inhibitory concentration (MIC), time-kill kinetics and biofilm inhibition. In addition, structural changes, membrane permeability, reactive oxygen species (ROS) production, and in vitro and in vivo toxicity of C. auris after exposure to XA1 were investigated. The results indicated that XA1 exhibited an MIC of 50 μg/mL against C. auris, with time-kill kinetics highlighting its efficacy. Field emission scanning electron microscopy (FE-SEM) showed structural damage in XA1-treated cells, supported by increased membrane permeability leading to cell death. Furthermore, XA1 induced ROS production and significantly inhibited biofilm formation. Importantly, XA1 exhibited low cytotoxicity in human epidermal keratinocytes (HaCaT), with a cell viability of over 90 % at 6.25 μg/mL. In addition, an LD50 of 17.68 μg/mL was determined in zebrafish embryos 24 h post fertilization (hpf), with developmental delay observed at prolonged exposure at 6.25 μg/mL (48–96 hpf). These findings position XA1 as a promising candidate for further research and development of an effective antifungal agent.

Clonal propagated 'Ek Pothi Lehsun' as a potential antifungal agent against Candida sp.

'Ek Pothi Lehsun', also known as snow mountain garlic, is a type of garlic grown in the high mountainous region of Jammu and Kashmir state of India. The present study aimed to develop a protocol for propagating snow mountain garlic in-vitro using corm seed as an explant. The study also assessed the antifungal potential of in vitro-grown bulbils against different Candida species. Four different concentrations of NAA and 2,4-D were tested for their effectiveness in promoting root formation, and eighteen different combinations of BAP (µM), KN (µM) and TDZ (µM) were investigated for effective proliferation of shoots with varied lengths. Shoot with maximum length (5.03±1.40) was obtained in MS medium containing 1.0 µM TDZ after 24 days of inoculation, whereas MS basal media was found effective for rooting plantlets. Rooted micro shoots were acclimatized successfully in hardening treys with a percent survival of nearly 80%. Seven different concentrations of Sucrose, i.e. 5%, 7%, 10%, 15%, 17%, 20%, and 25% were investigated for effective bulbil formation. Bulbil with a maximum diameter of 0.86 cm was obtained in 20% sucrose-containing MS media in 5 days. Further, the antifungal potential of aqueous extract (TC-SMG) of in vitro grown bulbils was investigated against three Candida sp. A zone of inhibition of 22.30±0.33 mm, 17.3±0.33 mm and 19.3±0.33 mm was observed against C. albicans, C. tropicalis and C. glabrata respectively, by using 200 mg/mL extract after 24 hrs depicting the remarkable potential of TC-SMG as an antifungal agent. In vitro culture of snow mountain garlic has demonstrated promising antifungal properties against Candida species.

Uncovering the Antifungal Potential of Plant-Associated Cultivable Bacteria from the Aral Sea Region against Phytopathogenic Fungi.

Two freshwater rivers, the Amu Darya and Syr Darya, flow into the Aral Sea, but they began to diminish in the early 1960s, and by the 1980s, the lake had nearly ceased to exist due to excessive water consumption for agriculture and the unsustainable management of water resources from rivers, which transformed the Aral Sea into a hypersaline lake. Despite this, the flora and fauna of the region began to evolve in the high-salinity seabed soil, which has received little attention in studies. In this study, we isolated approximately 1400 bacterial strains from the rhizosphere and phyllosphere of plant species of distinct families. Bacterial isolates were examined for antifungal activities against a range of pathogenic fungi such as Rhizoctonia gossypii, Trichothecium ovalisporum, Fusarium annulatum, F. oxysporum, F. culmorum, F. brachygibbosum, F. tricinctum, F. verticillioides, Alternaria alternata, A. terreus, Aspergillus niger, and As. flavus. Eighty-eight bacterial isolates exhibited varying antagonistic ability against pathogenic fungi. Furthermore, DNA barcoding of isolates using the 16S rRNA gene indicated that most antagonistic bacteria belonged to the Bacillus and Pseudomonas genera. The study also explored the activity of hydrolytic and cell-wall-degrading enzymes produced by antagonistic bacteria. The findings revealed that antagonistic bacteria can be utilized to widely protect seabed plants and plants growing in saline areas against pathogenic fungi, as well as agricultural crops.

In vitro Development of Two Alternaria solani Strains, Causal Agent of Alternariose in Tomato (Lycopersicon esculentum) under the Influence of Thevetia peruviana Seeds Extracts

Alternaria solani is a fungus that causes yield losses of up to 80 % in tomato production in field. Synthetic fungicides are the most widely used for its controbl, but have harmful consequences. The objective of this work was to test in vitro the antifungal potential of Thevetia peruviana seed extracts against two A. solani isolates. Aqueous, methanol, ethyl acetate and acetone extracts, at concentrations 12.5, 25, 50 and 100 µL/mL were used. Two synthetic fungicides Maneb (5.33 µg/mL) and Dimethomorph + Clorothalonil (3.75 µg/mL) and control (0 µL/mL) were also tested on two A. solani isolates (Mbal and Foum). The investigation was repeated three times. Phytochemical screening, mycelial growth, spore germination and minimum inhibitory concentrations (MIC50 and MIC90) were determined. The results showed that T. peruviana extracts are rich in many families of bioactive compounds such as alkaloids, phenolic compounds and sugars. All extracts tested show high inhibition of mycelial growth (100%) and spore germination (100%) of the two strains at highest concentration (100 µL/mL). Acetone extract at a concentration of 50 µL/mL inhibited mycelial growth by 88.45 and 86.55% and spore germination by 88.33 and 80.33%, respectively for the Mbal and Foum isolates. The lowest MIC50 (16.63 µL/mL) and MIC90 (54.6 µL/mL) were obtained with the acetone extract on the Mbal isolate while the highest MIC50 (27.5 µL/mL) and MIC90 (61.7 µL/mL) were observed with ethyl acetate on the Foum isolate These extracts can therefore be used in the biological control against Alternariose in tomato.

Design, Synthesis, and the Biological Evaluation of Some New Fused Thiazolotriazine Derivatives

Thiazolotriazine is an essential medicinal chemistry molecule due to its biological properties, particularly antifungalactivity. Antifungal drug resistance is rising worldwide, necessitating the development of innovative, safer, and more effectiveantifungals. This study intended to uncover safer and more effective thiazolotriazine antifungals. ProTox II software was employedto forecast the toxicity of the designed thiazolotriazines. The pharmacokinetic parameters were calculated using the Swiss-ADMEdatabase. The Molecular Operating Environment software (2019.0102 version) was employed for the docking studies utilizing 14-α-demethylase protein (PDB ID: 3LD6). Compounds 4c, 4d, and 4e were prepared and evaluated for in vitro antifungal activity.The computational studies revealed compounds 4a, 4b, 5b, 5c, 6b, 6c and 6d as carcinogenic; 4a, 4b, 4c, 4d and 4e demonstratedbetter pharmacokinetic behaviour; and docking results of 4c, 4d, and 4e were superior than fluconazole (FLU). The moleculardocking studies establish 4c, 4d, and 4e as SDM inhibitors, suggesting a mechanism similar to FLU and ketoconazole (KET). Theantifungal activity evaluation revealed 4d (MIC = 6.25 μg/ml) as a more potent antifungal agent than KET (MIC = 12.5 μg/ml) andFLU (MIC = 12.5 μg/ml). Compounds 4c and 4e showed equal antifungal activity to KET (MIC = 12.5 μg/ml) and FLU (MIC = 12.5μg/ml). Compounds 4c, 4d, and 4e displayed encouraging antifungal activity with a favorable safety profile. Assessing the broadspectrum of 4c, 4d, and 4e against various pathogenic fungi, including resistant forms, is recommended.

Expanding the Structural Diversity of Tubulin-Targeting Agents: Development of Highly Potent Benzimidazoles for Treating Fungal Diseases.

Benzimidazoles, the representative pharmacophore of fungicides, have excellent antifungal potency, but their simple structure and single site of action have hindered their wider application in agriculture. In order to extend the structural diversity of tubulin-targeted benzimidazoles, novel benzimidazole derivatives were prepared by introducing the attractive pyrimidine pharmacophore. 2-((6-(4-(trifluoromethyl)phenoxy)pyrimidin-4-yl)thio)-1H-benzo[d]imidazole (A25) exhibited optimal antifungal activity against Sclerotinia sclerotiorum (S. s.), affording an excellent half-maximal effective concentration (EC50) of 0.158 μg/mL, which was higher than that of the reference agent carbendazim (EC50 = 0.594 μg/mL). Pot experiments revealed that compound A25 (200 μg/mL) had acceptable protective activity (84.7%) and curative activity (78.1%), which were comparable with that of carbendazim (protective activity: 90.8%; curative activity: 69.9%). Molecular docking displayed that multiple hydrogen bonds and π-π interactions could be formed between A25 and β-tubulin, resulting in a stronger bonding effect than carbendazim. Fluorescence imaging revealed that the structure of intracellular microtubules can be changed significantly after A25 treatment. Overall, these remarkable antifungal profiles of constructed novel benzimidazole derivatives could facilitate the application of novel microtubule-targeting agents.

Antifungal Potential of Carnosic Acid from Salvia somalensis against Phytopathogenic Fungi

The aims of the present study were (i) to characterize the dichloromethane extract of the fresh aerial parts of S. somalensis, cultivated in Liguria (Italy), (ii) to quantify carnosic acid production and (iii) to find an eco-friendly alternative approach to control diseases caused by phytopathogenic fungi. The phytochemical investigation yielded several known terpenoids, as well as a diterpene, 4α,9α-epoxy-2H-dibenzo[a,d]cyclohepten-7(5H)-one, not previously described as a plant metabolite before. The results showed a noteworthy quantity of carnosic acid (113.90 µg/mg of dried extract). The potential antifungal activity of the plant surface extract and carnosic acid against five phytopathogenic fungi (Colletotrichum coccodes, Fusarium oxysporum, Sclerotinia sclerotiorum, Botrytis cinerea and Rhizoctonia solani) was considered. A complete inhibition of C. coccodes, S. sclerotiorum and R. solani mycelium growth was observed by carnosic acid at 500 µg/mL. High inhibition values were observed against B. cinerea and F. oxysporum compared to reference active ingredients. Four different B. cinerea strains exhibited a pronounced sensitivity to carnosic acid, as well as those originating from agricultural crop scenarios where a high load of active ingredient for gray mold control was historically adopted. Additionally, the formation and development of the germinative tube in B. cinerea were greatly slowed down.

Green synthesis of Curcuma longa-mediated Palladium nanoparticles as antioxidant, antimicrobial, and anticancer agents

The biosynthesis of nanomaterials using plants has become a promising substitute for conventional chemical and physical methods. This study aims to produce Palladium nanoparticles (PdNPs) utilizing Turmeric (Curcuma longa) extract and assess their pharmacological application as antioxidant, antifungal, antibacterial, and anticancer agents. PdNPs were characterized using transmission electron microscopy, field emission scanning electron microscopy, X-ray diffraction, Fourier transform infrared, and ultraviolet–visible spectroscopy. PdNPs showed antioxidant activity using the DPPH assay at all tested concentrations. The percentage of scavenging effect for 130 µg/mL PdNPs was 33 %. PdNPs at the same concentration showed noticeable antifungal and antibacterial activity using the agar well diffusion method against candida species and Escherichia coli within an inhibition range of 17 mm and 20 mm, respectively. Also, PdNPs exhibited significant cytotoxic activity at all tested concentrations using an MTT assay against the MCF-7 breast cancer cell line. MCF-7 cell viability declined to 26.53 % in the treated cells at 130 µg/mL. In conclusion, our findings demonstrate the simplicity and efficiency of synthesizing PdNPs using Curcuma longa extract in an eco-friendly manner and their significant antifungal, antibacterial, and anticancer potential.

A combined in vitro and in silico approach of thiadiazole based Schiff base derivatives as multipotent inhibitor: Synthesis, spectral analysis, antidiabetic and antimicrobial activity

We have developed new thiadiazole-containing Schiff base derivatives and examined their ability to inhibit α-amylase and α-glucosidase. Among the members of series, analogue 1 showed excellent inhibitory potential (IC50 = 1.60 ± 0.20 and 2.40 ± 0.10 µM for α-amylase and α-glucosidase) as compare to standard Acarbose (IC50 = 5.30 ± 0.20 and 6.10 ± 0.10 µM). Trifluoromethyl substituted analogue-1 showed best properties because of hydrogen bond formation. Analogue 3 and 9 were also found potent against the target enzymes. All the compounds were investigated for their antibacterial and antifungal activity. Analogue 1, 3 and 9 exhibited bacterial inhibition of 42.3 %, 40.1 %, 38.2 %, and 36.5 %, respectively in contrast to streptomycin (44 %). Analogue 1, 4 and 9 exhibited excellent anti-fungal potency of 43.4, 31.9 and 34.3 %, respectively as compared to standard terinafine (50.6675 %). Scaffolds (1–12) were analyzed through HREI-mass spectrometry, 13C NMR, and 1H NMR. The functioning of active interacting residues for the enzymes was determined by molecular docking (MD), and it was found that thiadiazole bearing Schiff base derivatives could be considered suitable anti-diabetic drugs. ADMET and DFT analysis was also performed to determine stability, drug properties and electronic properties (electrophilic, nucleophilic, HOMO, LUMO) of the synthesized compounds.

Evaluation of Neuroprotective Activity of Delonix Regia Leaves on Haloperidol Induced Parkinsonism in Experimental Animals

One of the most serious and fatal neurodegenerative disorders, Parkinson disease (PD) is characterized by low levels of dopamine. Reactive oxygen species (ROS) from both endogenous and exogenous sources have a role in the oxidative stress that leads to PD, which is a complex condition. Delo nix Regia is a prominent medicinal plant that is frequently used in Indian systems of medicine. The fruit, leaves, and bark of this plant have been utilised for its antifungal, antiemetic, larvicidal, hepatoprotective, antibacterial, antioxidant, anti-diarrheal, anti-inflammatory, wound-healing, and ant carcinogenic potential, according to Ayurvedic literature. The "antioxidant strategy" is the main topic of this study's therapeutic intervention for Parkinson's disease (PD). The investigation was completed in wistar rats, in which Parkinson’s disease (PD) was induced with haloperidol 2 mg/kg, P.O. The rats were randomly divided into six groups and the test animals received the ethanolic extract of Delo nix regia (DRLE) at a dose of 100, 250 and 500 mg/kg, orally for 15 days. Various behavioural and biochemical parameters were estimated in haloperidol exposed rats. The results of this study conclusively show that Delo nix regia has anti-oxidant activity and neuroprotective activity in haloperidol experimental model of PD.

Unmasking the Antifungal Activity of Anacardium occidentale Leaf Extract against Candida albicans.

Invasive fungal disease causes high morbidity and mortality among immunocompromised patients. Resistance to conventional antifungal drugs and the toxicity associated with high doses highlight the need for effective antifungal therapies. In this study, the antifungal potential of the ethanolic extract of Anacardium occidentale (Cashew Leaf) leaves were evaluated against Candida albicans and C. auris. The antifungal activity was tested by the broth microdilution method and growth kinetic test. To further explore its antifungal action mode, spectrofluorophotometry, confocal microscopy and scanning and transmission electron microscopy were performed. Additionally, heterozygous knockout strains associated with resistance to oxidative stress were included in the study. We found that A. occidentale could inhibit the proliferation and growth of C. albicans at concentrations of 62.5 and 125 μg/mL. The doubling time was also drastically affected, going from 2.8 h to 22.5 h, which was also observed in C. auris. The extract induced the accumulation of intracellular reactive oxygen species (ROS), resulting in endoplasmic reticulum stress and mitochondrial dysfunction, while it did not show cytotoxicity or hemolytic activity at the concentrations evaluated. Our work preliminarily elucidated the potential mechanisms of A. occidentale against C. albicans on a cellular level, and might provide a promising option for the design of a new treatment for invasive candidiasis.

Eco-Friendly Antifungal from Seven Botanical Extracts and Its Effect To Plant Pathogenic Fungi

Fusarium oxysporum has been the enemy in agriculture due to the wide range of infections in the whole crop and postharvest. Botanical extracts in traditional medicine systems were considered valuable sources for discovering new antifungals. Thus, exploration to get antifungals from eco-friendly botanical extracts as an alternative to synthetic fungicides needs to be expanded. Therefore, this study aims to test the antifungal potential of seven eco-friendly botanical aquadest extracts against F. oxysporum in vitro. The antifungal potential test was done on PDA media and the mycelial growth data was collected every two days for seven days. There were three antifungal phenomena were observed. The pandan leaf extract had a 4% fungal inhibition zone (phenomenon I). The extract of banana leaf, Hibiscus flower, papaya leaf, guava twig (phenomenon II), orange peels, and betel leaf (phenomenon III) had no values of fungal inhibition zone. Thus, pandan leaves extract revealed a fungal inhibition while other six botanical extracts had not enough antifungal potential in vitro.

Sunflower Oil and Cholesterol Nanoemulsion: A Novel Carrier for Micafungin to Combat Multi-Resistant Candida auris.

Candida auris is an emerging, multidrug-resistant yeast that causes systemic infections, mainly in hospitalized or immunosuppressed patients. This pathogen has a high mortality and morbidity rate. This study aims to evaluate the antifungal potential of micafungin (MICA) encapsulated in a nanoemulsion (NEM) against four clades of C. auris and other non-C. auris species. The antifungal potential of MICA and NEM was evaluated by determining mature biofilm inhibition (0.78-50 µg/mL). The antifungal activities of MICA and NEM (5.92 mg/Kg) were evaluated using an in vivo model of Galleria mellonella. The results showed that NEM intensified the antibiofilm action of MICA, especially in 48 h mature biofilms. In vivo results displayed a higher effectiveness of NEM against all clades of C. auris tested, inhibiting the fungal load in the hemolymph and tissues of G. mellonella with a difference of 3 log10. In addition, C. auris infection caused granulomas surrounded by hemocytes, mainly at the lower and upper ends. Conversely, C. albicans developed pseudohyphae, biofilms, filaments, and chlamydospores. In conclusion, encapsulation of MICA in a nanoemulsion enhances its antifungal activity against mature biofilms of C. auris. This strategy may be considered a therapeutic approach for the control of infections and the dissemination of this new global health threat.

Antibacterial, Antifungal, and Cytotoxic Potential of PlumbaginLoaded pH-Responsive Vaginal Nanoformulations.

Plumbagin is a naphthoquinone from the roots of the Plumbago species and exhibits anticancer activity. Translational usage of plumbagin in biomedical sciences is restricted due to its poor solubility and bioavailability. Therefore, pH-responsive plumbagin-loaded vaginal nanoformulations with polylactic acid (PLA)-chitosan polymeric coat were fabricated by inotropic gelation technique. Among the four (F1, F2, F3, F4) nanoformulations prepared, F3 exhibited good interaction of polymers with plumbagin as evidenced by FTIR, XRD, and thermal analysis. The positive zeta potential (48.4 ± 5.57mV), optimal size (694 ± 65.76nm), low PDI (0.157), and good encapsulation efficiency (77.8 ± 3.62%) of F3 were significant. The indirect method of drug loading (58.35 ± 5.00%) confirmed the drug content of about 495.44 ± 5.00µg of plumbagin in 1mg of F3. The drug loading pattern was confirmed by TEM analysis, and the spherical morphology of the nanocomposite was confirmed by SEM analysis. F3 formulation showed 46% and 25.2% of drug release in 24h in simulated vaginal fluid at pH 4.5 and 7 respectively with sustained release and hydrolyses of lactic acid from PLA. Among all the nanoformulations evaluated, nanoformulation F3 with promising physicochemical properties showed good antifungal and antibacterial activity against various fungal and bacterial strains. F3 exhibited potent cytotoxicity with an IC50 of 3.6 ± 0.12µg/ml for HeLa and an IC50 of 0.81 ± 0.01µg/ml for SiHa cells. Altogether, the nanoformulation F3 exhibited potent antimicrobial activity against vaginal infections and cytotoxicity against cervical cancer cell lines.

Study on the antifungal potential of Piper betle methanol extract against Colletotrichum gloeosporioides cutinase

Study on the antifungal potential of Piper betle methanol extract against Colletotrichum gloeosporioides cutinase