Browsing by Author "Nilesh Rai"

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A simple TICT/ICT based molecular probe exhibiting ratiometric fluorescence Turn-On response in selective detection of Cu2+
(Elsevier B.V., 2023) Ravisen Rai; Rimpi Bhandari; Mohammed Kaleem; Nilesh Rai; Vibhav Gautam; Arvind Misra
The work reported herein describes photophysical behavior of a new fluorescent probe APDA. The probe exhibited sensitivity for Cu2+ ion in 80% aqueous acetonitrile medium. Probe shows dual emission due to TICT and ICT states and upon interaction with different metal ions Cu2+ induces hydrolysis of imine bond to rejuvenate aldehyde derivative with ratiometric “turn–On” fluorescence response, through ICT state while emission due to TICT state get diminished. Similarly, the synthesized model compound ADA under similar experimental condition supported hydrolysis of imine bond in the presence of copper. Jobs plot analysis, based on emission titration data suggested a 1:1 binding stoichiometry between probe APDA and Cu2+ ion. The limit of detection (LOD) was found to be 4.4 × 10-8 M (44 nM). The probe has been applied on test paper strip to detect Cu2+ ion with naked-eye sensitive response. Also, the cell imaging studies revealed the potential applicability of probe to detect Cu2+ ion in live cells. The mechanism of sensing was confirmed by 1H, 13C NMR, FTIR and mass spectrometry data analysis. © 2023 Elsevier B.V.
Antimicrobial Potential of Essential Oils from Aromatic Plant Ocimum sp.; A Comparative Biochemical Profiling and In-Silico Analysis
(MDPI, 2022) Prafull Salvi; Gulshan Kumar; Nishu Gandass; Kajal; Ashish Verma; Sivasubramanian Rajarammohan; Nilesh Rai; Vibhav Gautam
Medicinal and aromatic plants (MAPs) are a rich source of bioactive compounds that are immensely important due to their potential use in pharmacological and agricultural applications. Here, we have evaluated the antimicrobial activity of essential oils (EOs) from three different species of Ocimum: O. gratissimum (EO1), O. tenuiflorum (EO2), and O. sanctum (EO3). The EOs were screened for antibacterial activity against pathogenic strains of Escherichia coli, Enterobacter cloacae and methicillin-resistant Staphylococcus aureus (MRSA). The essential oils EO1 and EO3 showed significant growth inhibition of the tested bacteria. Likewise, all EOs exhibited antifungal potential against the broad-spectrum plant fungal pathogen Sclerotinia sclerotiorum that causes white-mould disease in plants. Moreover, the antimicrobial potential of the EOs correlates well with their antioxidant activity determined by DPPH free radical scavenging activity. The biochemical analysis of the EOs employing high-performance thin-layer chromatography, gas chromatography-mass spectrometry, and Fourier transform infrared spectroscopy, revealed the presence of distinct phytoconstituents that might be responsible for their differential bioactivity. Furthermore, an in-silico evaluation of the candidate phytoconstituents using molecular docking analysis suggests their potential for antimicrobial applications. Altogether, our results clearly show that EO1 and EO3 possess promising antimicrobial properties, and therefore could be utilized as a potential antimicrobial agent. © 2022 by the authors. Licensee MDPI, Basel, Switzerland.
Assessment of Biological Activities of Fungal Endophytes Derived Bioactive Compounds Isolated from Amoora rohituka
(MDPI, 2022) Ashish Verma; Priyamvada Gupta; Nilesh Rai; Rajan Kumar Tiwari; Ajay Kumar; Prafull Salvi; Swapnil C. Kamble; Santosh Kumar Singh; Vibhav Gautam
Fungal endophytes have remarkable potential to produce bioactive compounds with numerous pharmacological significance that are used in various disease management and human welfare. In the current study, a total of eight fungal endophytes were isolated from the leaf tissue of Amoora rohituka, and out of which ethyl acetate (EA) extract of Penicillium oxalicum was found to exhibit potential antioxidant activity against DPPH, nitric oxide, superoxide anion and hydroxyl free radicals with EC50 values of 178.30 ± 1.446, 75.79 ± 0.692, 169.28 ± 0.402 and 126.12 ± 0.636 µg/mL, respectively. The significant antioxidant activity of EA extract of P. oxalicum is validated through highest phenolic and flavonoid content, and the presence of unique bioactive components observed through high-performance thin layer chromatography (HPTLC) fingerprinting. Moreover, EA extract of P. oxalicum also displayed substantial anti-proliferative activity with IC50 values of 56.81 ± 0.617, 37.24 ± 1.26 and 260.627 ± 5.415 µg/mL against three cancer cells HuT-78, MDA-MB-231 and MCF-7, respectively. Furthermore, comparative HPTLC fingerprint analysis and antioxidant activity of P. oxalicum revealed that fungal endophyte P. oxalicum produces bioactive compounds in a host-dependent manner. Therefore, the present study signifies that fungal endophyte P. oxalicum associated with the leaf of A. rohituka could be a potential source of bioactive compounds with antioxidant and anticancer activity. © 2022 by the authors. Licensee MDPI, Basel, Switzerland.
Beyond the synthetic drugs: Fungal endophytes derived bioactive compounds in the management of neurodegenerative disorders
(Bentham Science Publishers, 2023) Ashish Verma; Nilesh Rai; Swapnil C. Kamble; Pradeep Mishra; Suvakanta Barik; Rajiv Kumar; Santosh Kumar Singh; Prafull Salvi; Vibhav Gautam
Fungal endophytes are a group of fungi that reside in plant tissues and show a symbiotic relationship with the host plants. They protect against pathogens and increase food availability without causing any harmful effects on the host plant. Fungal endophytes are known to produce a wide range of bioactive compounds with several biological activities, including neuroprotective effects. Neurodegenerative disorders lead to miscommunication between nerve cells, damage or loss in structure and function of the central nervous system (CNS) or peripheral nervous system (PNS). Reactive oxygen species, neuroinflammation, protein degradation or aggregation, familial history, mutation in mitochondrial genes, and aging contribute to neurodegenerative disorders. Plant-associated fungal endophytes produce bioactive compounds, which show anti-neuroinflammatory, antioxidant, and anti-cholinesterase activities. Several pro-inflammatory (TNF-α and NF-κB) and depressant (serotonin, dopamine, and noradrenaline) molecules or neuronal signaling pathways leading to neurodegenerative disorders are known to be inhibited or down-regulated by fungal endophyte-derived bioactive compounds. Therefore, bioactive compounds produced from fungal endophytes could be a promising approach to treating various health ailments. The present chapter discusses selected fungal endophyte-derived potential bioactive compounds with neuroprotective effects for managing neurodegenerative disorders. © 2023 Bentham Science Publishers. All rights reserved.
Bioinformatics: How it helps to boost modern biological research
(Indian Academy of Sciences, 2020) Suvakanta Barik; Nilesh Rai; Pradeep Mishra; Santosh K. Singh; Vibhav Gautam
[No abstract available]
Biological potential of bioactive metabolites derived from fungal endophytes associated with medicinal plants
(Springer Science and Business Media Deutschland GmbH, 2021) Priyanka Kumari Keshri; Nilesh Rai; Ashish Verma; Swapnil C. Kamble; Suvakanta Barik; Pradeep Mishra; Santosh Kumar Singh; Prafull Salvi; Vibhav Gautam
Endophytes are endosymbiotic fungi or bacteria that invade and colonize the plant tissue without harming their respective host. Since fungal endophytes live inside the host tissues, their effective isolation and identification is an important step. Endophytic fungi produce bioactive metabolites with unique chemical structures, which may help in improving the physiological condition of both the plants and endophytes. Endophytic fungi are a potent source of all major classes of secondary metabolites including terpenoids, non-ribosomal peptides, polyketides, and alkaloids. With the increase in the number of diseases and human health problems, an intensive search for new sources and effective metabolites is now in progress. The bioactive metabolites produced by the fungal endophytes are competent and effective against various diseases such as cancer, diabetes, infectious diseases, immunological disorders, and cardiovascular diseases. The present review summarizes the efficient approaches used for the screening of fungal endophytes, extraction, and purification of bioactive metabolites along with OMICS based study of endophytes. Along with this, the pharmaceutical importance of novel bioactive metabolites and their efficient production from fungal endophytes using various approaches like genetic engineering, use of elicitors, and precursor feeding are also discussed. © 2021, German Mycological Society and Springer-Verlag GmbH Germany, part of Springer Nature.
Bioprospecting of fungal endophytes from Oroxylum indicum (L.) Kurz with antioxidant and cytotoxic activity
(Public Library of Science, 2022) Nilesh Rai; Priyanka Kumari Keshri; Priyamvada Gupta; Ashish Verma; Swapnil C. Kamble; Santosh Kumar Singh; Vibhav Gautam
Oroxylum indicum (L.) Kurz, a medicinal plant, shows numerous pharmacological properties which may be attributed to the bioactive compounds produced by O. indicum or due to associated endophytes. In the present study, leaf of O. indicum was evaluated for the presence of associated fungal endophytes, and antioxidant and cytotoxic activities of bioactive compounds produced from them. Using culture-dependent approach, eight fungal endophytes belonging to five different genera were identified. Two endophytes Daldinia eschscholtzii and Ectophoma multirostrata have been reported for the first time from the leaf of O. indicum plant. High-performance thin-layer chromatography (HPTLC) of ethyl acetate (EA) extract of isolated fungal endophytes showed a distinct fingerprinting profile in EA extract of Colletotrichum gloeosporioides. Among identified endophytes, EA extract of C. gloeosporioides showed significant antioxidant activity against DPPH free radical, superoxide anion radical, nitric oxide radical and hydroxyl radical with EC50 values of 22.24±1.302 μg/mL, 67.46 ±0.576 μg/mL, 80.10±0.706 μg/mL and 61.55±1.360 μg/mL, respectively. EA extract of C. gloeosporioides exhibited potential cytotoxicity against HCT116, HeLa and HepG2 cancer cell lines with IC50 values of 76.59 μg/mL, 176.20 μg/mL and 1750.70 μg/mL, respectively. A comparative HPTLC fingerprinting and the antioxidant activity of C. gloeosporioides associated with two different hosts (leaf of O. indicum and dead twigs of other plant) showed that C. gloeosporioides produces bioactive compounds in a host-dependent manner. Copyright: © 2022 Rai et al.
Design, synthesis, and structural evaluation of metal complexes of azepane-1-carbodithioate for targeting human breast cancer: investigating cytotoxic activity against the MDA-MB-231 cell line
(Royal Society of Chemistry, 2024) Shubham Jaiswal; Nilesh Rai; Suryansh Chandra; Ashish Verma; Vibhav Gautam; Manu Adhikari; Sanjay Singh; M.K. Bharty
In this article, we have reported the synthesis and structural characterization of complexes containing Co(iii), Cu(ii), Zn(ii), and Hg(ii) metal cations. The ligand potassium azepane-1-carbodithioate (acdt) behaves as a monodentate and bidentate and forms complexes with the metals mentioned above. We investigated the electronic and emission spectra of the ligand potassium azepane-1-carbodithioate (acdt) and its metal complexes [Co(acdt)3]·CHCl3 (1), [Cu(acdt)2] (2), [Zn2(μ2-acdt)2(acdt)2] (3), and [PhHg(acdt)] (4). A photoluminescence study was also carried out and the results revealed that all compounds are fluorescent. Furthermore, this synthesized ligand and its complexes are passed through to examine their cytotoxic activity against human breast cancer cell line MDA-MB-231 and results suggested that complex [Co(acdt)3]·CHCl3 has sufficiently better activity than others. Furthermore, we have explored the impact of the synthesized ligand and its transition metal complexes on glucose metabolism within the human breast cancer cell line MDA-MB-231. Inhibiting glucose uptake can induce starvation in cancer cells, potentially resulting in cell death due to energy deprivation. Our results indicate that the Co(iii) complex-treated group exhibited a greater inhibition of glucose uptake compared to groups treated with ligands and other metal complexes such as Cu, Zn, and Hg. Furthermore, we also measured the extracellular NO level in the ligand and its metal complexes of Co(iii), Cu(ii), Zn(ii), and Hg(ii) treated MDA-MB-231 cells and results indicated that the free ligand and its metal complexes induced the production of nitric oxide in MDA-MB-231 cells. Among the four metal complexes, Co-complex 1 elevated the nitric oxide level in MDA-MB-231 cells to 75.91 μM. In contrast, the groups treated with the complexes of Cu(ii) (2), Zn(iii) (3), and Hg(ii) (4) induced NO levels of 62.91, 49.24, and 33.10 μM, respectively. This suggests that complex 1 induces nitric oxide production and enhances oxidative stress in MDA-MB-231 cells more significantly compared to the groups treated with the free ligand as well as with metal complexes 2-4. Overall, the data strongly suggest that complex 1 exhibits significant anticancer activity against the human breast cancer cell line MDA-MB-231, making it a promising candidate for combating breast cancer progression. © 2024 The Royal Society of Chemistry.
Epigenetic manipulation for secondary metabolite activation in endophytic fungi: current progress and future directions
(Taylor and Francis Ltd., 2023) Ashish Verma; Harshita Tiwari; Swati Singh; Priyamvada Gupta; Nilesh Rai; Santosh Kumar Singh; Bhim Pratap Singh; Sombir Rao; Vibhav Gautam
Fungal endophytes have emerged as a promising source of secondary metabolites with significant potential for various applications in the field of biomedicine. The biosynthetic gene clusters of endophytic fungi are responsible for encoding several enzymes and transcriptional factors that are involved in the biosynthesis of secondary metabolites. The investigation of fungal metabolic potential at genetic level faces certain challenges, including the synthesis of appropriate amounts of chemicals, and loss of the ability of fungal endophytes to produce secondary metabolites in an artificial culture medium. Therefore, there is a need to delve deeper into the field of fungal genomics and transcriptomics to explore the potential of fungal endophytes in generating secondary metabolites governed by biosynthetic gene clusters. The silent biosynthetic gene clusters can be activated by modulating the chromatin structure using chemical compounds. Epigenetic modification plays a significant role by inducing cryptic gene responsible for the production of secondary metabolites using DNA methyl transferase and histone deacetylase. CRISPR-Cas9-based genome editing emerges an effective tool to enhance the production of desired metabolites by modulating gene expression. This review primarily focuses on the significance of epigenetic elicitors and their capacity to boost the production of secondary metabolites from endophytes. This article holds the potential to rejuvenate the drug discovery pipeline by introducing new chemical compounds. © 2023 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.
Ethyl Acetate Extract of Colletotrichum gloeosporioides Promotes Cytotoxicity and Apoptosis in Human Breast Cancer Cells
(American Chemical Society, 2023) Nilesh Rai; Priyamvada Gupta; Ashish Verma; Rajan Kumar Tiwari; Prasoon Madhukar; Swapnil C. Kamble; Ajay Kumar; Rajiv Kumar; Santosh Kumar Singh; Vibhav Gautam
Fungal endophytes are known to be a paragon for producing bioactive compounds with a variety of pharmacological importance. The current study aims to elucidate the molecular alterations induced by the bioactive compounds produced by the fungal endophyte Colletotrichum gloeosporioides in the tumor microenvironment of human breast cancer cells. GC/MS analysis of the ethyl acetate (EA) extract of C. gloeosporioides revealed the presence of bioactive compounds with anticancer activity. The EA extract of C. gloeosporioides exerted potential plasmid DNA protective activity against hydroxyl radicals of Fenton’s reagent. The cytotoxic activity further revealed that MDA-MB-231 cells exhibit more sensitivity toward the EA extract of C. gloeosporioides as compared to MCF-7 cells, whereas non-toxic to non-cancerous HEK293T cells. Furthermore, the anticancer activity demonstrated by the EA extract of C. gloeosporioides was studied by assessing nuclear morphometric analysis and induction of apoptosis in MDA-MB-231 and MCF-7 cells. The EA extract of C. gloeosporioides causes the alteration in cellular and nuclear morphologies, chromatin condensation, long-term colony inhibition, and inhibition of cell migration and proliferation ability of MDA-MB-231 and MCF-7 cells. The study also revealed that the EA extract of C. gloeosporioides treated cells undergoes apoptosis by increased production of reactive oxygen species and significant deficit in mitochondrial membrane potential. Our study also showed that the EA extract of C. gloeosporioides causes upregulation of pro-apoptotic (BAX, PARP, CASPASE-8, and FADD), cell cycle arrest (P21), and tumor suppressor (P53) related genes. Additionally, the downregulation of antiapoptotic genes (BCL-2 and SURVIVIN) and increased Caspase-3 activity suggest the induction of apoptosis in the EA extract of C. gloeosporioides treated MDA-MB-231 and MCF-7 cells. Overall, our findings suggest that the bioactive compounds present in the EA extract of C. gloeosporioides promotes apoptosis by altering the genes related to the extrinsic as well as the intrinsic pathway. Further in vivo study in breast cancer models is required to validate the in vitro observations. © 2023 The Authors. Published by American Chemical Society.
Exploration of in vitro cytotoxic and in ovo antiangiogenic activity of ethyl acetate extract of Penicillium oxalicum
(John Wiley and Sons Inc, 2023) Ashish Verma; Nilesh Rai; Priyamvada Gupta; Swati Singh; Harshita Tiwari; Shashi Bhushan Chauhan; Vikas Kailashiya; Vibhav Gautam
Fungal endophytes have established new paradigms in the area of biomedicine due to their ability to produce metabolites of pharmacological importance. The present study reports the in vitro cytotoxic and in ovo antiangiogenic activity of the ethyl acetate (EA) extract of Penicillium oxalicum and their chemical profiling through Gas Chromatography–Mass Spectrometry analysis. Treatment of the EA extract of P. oxalicum to the selected human breast cancer cell lines (MDA-MB-231 and MCF-7) leads to the reduced glucose uptake and increased nitric oxide production suggesting the cytotoxic activity of EA extract of P. oxalicum. Our results further show that treatment of EA extract of P. oxalicum attenuates the colony number, cell migration ability and alters nuclear morphology in both the human breast cancer cell lines. Furthermore, the treatment of EA extract of P. oxalicum mediates apoptosis by increasing the expression of BAX, P21, FADD, and CASPASE-8 genes, with increased Caspase-3 activity. Additionally, in ovo chorioallantoic membrane (CAM) assay showed that the treatment of EA extract of P. oxalicum leads to antiangiogenic activity with perturbed formation of blood vessels. Overall, our findings suggest that the EA extract of P. oxalicum show in vitro cytotoxic and antiproliferative activity against human breast cancer cell lines, and in ovo antiangiogenic activity in CAM model. © 2023 Wiley Periodicals LLC.
Exploring the Protective Effect against 7,12-Dimethylbenz[a]anthracene-Induced Breast Tumors of Palmitoylethanolamide
(American Chemical Society, 2024) Nilesh Rai; Vikas Kailashiya; Vibhav Gautam
Breast cancer remains a global health burden, and the need for effective therapies is of chief importance. The current study explored the in vivo chemoprotective activity of palmitoylethanolamide (PEA) against 7,12-dimethylbenz[a]anthracene (DMBA)-induced breast tumor in rats. Results of noninvasive photoacoustic imaging showed real-time progression in the tumor area and volume in DMBA-induced rats, while there was a reduction in tumor area and volume in PEA-treated tumor-bearing rats. The increase in the average oxygen saturation (sO2 %) and decrease in the average total hemoglobin (HbT %) indicated the PEA-mediated attenuation of hypoxia-induced neovascularization in DMBA-induced rats. Histopathological investigations confirmed the efficacy of PEA in mitigating breast carcinoma, hepatotoxicity and nephrotoxicity driven by DMBA. Moreover, PEA-mediated alterations in the metabolic activity of the tumor microenvironment were evidenced by decreased glucose and lactate dehydrogenase enzyme level in the blood plasma and mammary tissue. PEA also maintained the redox balance by inhibiting nitric oxide level, reducing malondialdehyde (a product of lipid peroxidation), and increasing the level of antioxidant enzyme reduced glutathione. PEA altered the expression of apoptosis-related genes (BAX, P53,BCL-XL, CASPASE-8, and CASPASE-9) and induced the activity of Caspase-3 protein in the mammary tissue of tumor-bearing rats, indicating its apoptosis inducing ability. Taken together, the findings of this study suggest that PEA may have a protective effect against DMBA-induced breast tumors. © 2023 American Chemical Society
Fungal endophyte-mediated green synthesis of silver nanoparticles as potential anticancer agent: current perspective and challenges
(Springer Nature, 2024) Nilesh Rai; Priyamvada Gupta; Ashish Verma; Swati Singh; Harshita Tiwari; Rajiv Kumar; Santosh Kumar Singh; Vibhav Gautam
Endophytic microorganisms establish symbiotic relationship with their host plants and also have a unique ability to mimic bioactive metabolite produced from host plants. Bioactive compounds produced from fungal endophyte have tendency to reduce metallic ions such as silver, gold, platinum, and zinc into nanoparticles. Biosynthesis of fungal endophyte-mediated silver nanoparticles (AgNPs) has evolved as a frontier of nanotechnology. For decades, silver has been observed as a nontoxic and harmless inorganic agent which is utilized as antibacterial or antifungal agent. Silver exhibits an exceptional physical, chemical, and a wide range of potential biological activities, predominantly in the form of nanoparticles. Although the effective biosynthesis of fungal endophytemediated AgNPs and their antiapoptotic and antiproliferative property have been accounted as of now, the exact mechanism of synthesis of nanoparticles remains unclear. The current chapter gives a brief outline of the possible mechanism of fungal endophyte-mediated synthesis of AgNPs and its anticancer properties. Moreover, it also provides an insight for the mycogenic synthesis and characterization of AgNPs mediated by fungal endophyte using various highthroughput techniques including UV-Visible spectrophotometer, Fourier transform infrared spectroscopy (FT-IR), high-resolution transmission electron microscopy (HR-TEM), scanning electron microscopy (SEM) equipped with energy dispersive X-ray analysis (EDAX), and X-ray Powder Diffraction (XRD). Additionally, it also describes bottlenecks in the field of myconanotechnology including manufacturing at large scale, improved stability, and reduced time to acquire compatible size and shape of AgNPs and their potential uses in cancer research. © Springer Nature Singapore Pte Ltd. 2024. All rights reserved.
Fungal Endophytes: an Accessible Source of Bioactive Compounds with Potential Anticancer Activity
(Springer, 2022) Nilesh Rai; Priyamvada Gupta; Priyanka Kumari Keshri; Ashish Verma; Pradeep Mishra; Deepak Kumar; Ajay Kumar; Santosh Kumar Singh; Vibhav Gautam
Endophytes either be bacteria, fungi, or actinomycetes colonize inside the tissue of host plants without showing any immediate negative effects on them. Among numerous natural alternative sources, fungal endophytes produce a wide range of structurally diverse bioactive metabolites including anticancer compounds. Considering the production of bioactive compounds in low quantity, genetic and physicochemical modification of the fungal endophytes is performed for the enhanced production of bioactive compounds. Presently, for the treatment of cancer, chemotherapy is majorly used, but the side effects of chemotherapy are of prime concern in clinical practices. Also, the drug-resistant properties of carcinoma cells, lack of cancer cells-specific medicine, and the side effects of drugs are the biggest obstacles in cancer treatment. The interminable requirement of potential drugs has encouraged researchers to seek alternatives to find novel bioactive compounds, and fungal endophytes seem to be a probable target for the discovery of anticancer drugs. The present review focuses a comprehensive literature on the major fungal endophyte-derived bioactive compounds which are presently been used for the management of cancer, biotic factors influencing the production of bioactive compounds and about the challenges in the field of fungal endophyte research. © 2022, The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.
Green-Based Approach to Synthesize Silver Nanoparticles Using the Fungal Endophyte Penicillium oxalicum and Their Antimicrobial, Antioxidant, and in Vitro Anticancer Potential
(American Chemical Society, 2022) Priyamvada Gupta; Nilesh Rai; Ashish Verma; Dimple Saikia; Surya Pratap Singh; Rajiv Kumar; Santosh Kumar Singh; Deepak Kumar; Vibhav Gautam
A green-based approach for the synthesis of silver nanoparticles has gained tremendous attention in biomedical applications. Fungal endophytes have been recognized as a remarkable biological source for the synthesis of potential nanodrugs. The present study focuses on the fabrication of silver nanoparticles using the fungal endophyte Penicillium oxalicum (POAgNPs) associated with the leaf of the Amoora rohituka plant. Sharp UV-visible spectra at 420 nm appeared due to the surface plasmon resonance of POAgNPs and the reduction of silver salt. FT-IR analysis revealed the presence of functional groups of bioactive compounds of P. oxalicum responsible for the reduction of silver salt and validated the synthesis of POAgNPs. A high degree of crystallinity was revealed through XRD analysis, and microscopy-based characterizations such as AFM, TEM, and FESEM showed uniformly distributed, and spherically shaped nanoparticles. Furthermore, POAgNPs showed a potential inhibitory effect against bacterial and fungal strains of pathogenic nature. POAgNPs also exhibited potential antioxidant activity against the synthetically generated free radicals such as DPPH, superoxide, hydroxyl, and nitric oxide with EC50 values of 9.034 ± 0.449, 56.378 ± 1.137, 34.094 ± 1.944, and 61.219 ± 0.69 μg/mL, respectively. Moreover, POAgNPs exhibited cytotoxic potential against the breast cancer cell lines, MDA-MB-231 and MCF-7 with IC50 values of 20.080 ± 0.761 and 40.038 ± 1.022 μg/mL, respectively. POAgNPs showed anticancer potential through inhibition of wound closure and by altering the nuclear morphology of MDA-MB-231 and MCF-7 cells. Further anticancer activity revealed that POAgNPs induced apoptosis in MDA-MB-231 and MCF-7 cells by differential expression of genes related to apoptosis, tumor suppression, and cell cycle arrest and increased the level of Caspase-3. The novel study showed that P. oxalicum-mediated silver nanoparticles exhibit potential biological activity, which can be exploited as nanodrugs in clinical applications. © 2022 American Chemical Society.
Isolation and characterization of N-(2-Hydroxyethyl)hexadecanamide from Colletotrichum gloeosporioides with apoptosis-inducing potential in breast cancer cells
(John Wiley and Sons Inc, 2023) Nilesh Rai; Priyamvada Gupta; Ashish Verma; Santosh Kumar Singh; Vibhav Gautam
Endophytic fungi are a well-established reservoir of bioactive compounds that are pharmaceutically valuable and therefore, contribute significantly to the biomedical field. The present study aims to identify the bioactive anticancer compound from ethyl acetate extract of fungal endophyte, Colletotrichum gloeosporioides associated with the leaf of the medicinal plant Oroxylum indicum. The fatty acid amide compound N-(2-Hydroxyethyl)hexadecanamide (Palmitoylethanolamide; PEA) was identified using antioxidant activity-guided fractionation assisted with tandem liquid chromatography coupled with quadrupole time of flight mass spectrometry, Fourier transform-infrared spectroscopy, time-of-flight mass spectrometry, and nuclear magnetic resonance. In-Silico molecular docking analysis showed that PEA potentially docked to the active sites of apoptosis-inducing proteins including BAX, BCL-2, P21, and P53. Further validation was done using in vitro study that showed PEA inhibitsthe proliferation, alters nuclear morphology and attenuates the wound closure ability of MDA-MB-231 and MCF-7 cells. PEA induces apoptosis via upregulating cell-cycle arrest (P21), tumor suppression (P53), pro-apoptotic (BAX, CASPASE-8, and FADD) genes, and downregulating anti-apoptotic gene BCL-2. The upregulation of the active form of Caspase-3 was also reported. This is the first-ever report for the isolation of PEA from C. gloeosporioides with anticancer activity against human breast cancer cells and therefore holds great potential for future therapeutics. © 2023 International Union of Biochemistry and Molecular Biology.
Isolation of potassium salt of oxadiazole-2-thione and in vitro anticancer activities of its Cu(ii) and Zn(ii) complexes against MDA-MB-231 human breast carcinoma cells
(Royal Society of Chemistry, 2023) M.K. Gond; Nilesh Rai; Brijesh Chandra; Vibhav Gautam; Somenath Garai; R.J. Butcher; M.K. Bharty
A potassium 4-(pyridyl)-1,3,4-oxadiazole-2-thione was isolated in a basic medium, and its complexes [Cu(en)2(pot)2] (1) and [Zn(en)2(pot)2]HBr·CH3OH (2) containing ethylenediamine (en) as secondary ligand were synthesized and fully characterized. Upon changing the reaction conditions, the Cu(ii) complex (1) adopts an octahedral geometry around the metal center. The cytotoxic activity of ligand (Kpot·H2O) along with complexes 1 and 2 was tested, and their anticancer activity against MDA-MB-231 human breast cancer cells was demonstrated, with complex 1 exhibiting superior cytotoxicity against these cells as compared to Kpot·H2O and complex 2. According to the DNA nicking assay, the ligand (Kpot·H2O) was found to be more potent to scavenge hydroxyl radicals even at a lower concentration (50 μg mL−1) than that of both complexes. The wound healing assay revealed that ligand Kpot·H2O and its complexes 1 and 2 attenuated the migration of the above-mentioned cell line. The loss of cellular and nuclear integrity and induction in the activity of Caspase-3 suggest the anticancer potential of ligand Kpot·H2O and its complexes 1 and 2 against MDA-MB-231 cells. © 2023 The Royal Society of Chemistry.
Mass Spectrometry-Based Technology and Workflows for Studying the Chemistry of Fungal Endophyte Derived Bioactive Compounds
(American Chemical Society, 2021) Priyamvada Gupta; Ashish Verma; Nilesh Rai; Anurag Kumar Singh; Santosh Kumar Singh; Brijesh Kumar; Rajiv Kumar; Vibhav Gautam
Bioactive compounds have gained substantial attention in research and have conferred great advancements in the industrial and pharmacological fields. Highly diverse fungi and their metabolome serve as a big platform to be explored for their diverse bioactive compounds. Omics tools coupled with bioinformatics, statistical, and well-developed algorithm tools have elucidated immense knowledge about fungal endophyte derived bioactive compounds. Further, these compounds are subjected to chromatography-gas chromatography and liquid chromatography (LC), spectroscopy-nuclear magnetic resonance (NMR), and "soft ionization"technique-matrix-assisted laser desorption/ionization-time-of-flight (MALDI-TOF) based analytical techniques for structural characterization. The mass spectrometry (MS)-based approach, being highly sensitive, reproducible, and reliable, produces quick and high-profile identification. Coupling these techniques with MS has resulted in a descriptive account of the identification and quantification of fungal endophyte derived bioactive compounds. This paper emphasizes the workflows of the above-mentioned techniques, their advancement, and future directions to study the unraveled area of chemistry of fungal endophyte-derived bioactive compounds. © 2021 American Chemical Society.
Microscopy based methods for characterization, drug delivery, and understanding the dynamics of nanoparticles
(John Wiley and Sons Inc, 2024) Priyamvada Gupta; Nilesh Rai; Ashish Verma; Vibhav Gautam
Nanomedicine is an emerging field that exploits nanotechnology for the development of novel therapeutic and diagnostic modalities. Researches are been focussed in nanoimaging to develop noninvasive, highly sensitive, and reliable tools for diagnosis and visualization in nanomedical field. The application of nanomedicine in healthcare requires in-depth understanding of their structural, physical and morphological properties, internalization inside living system, biodistribution and localization, stability, mode of action and possible toxic health effects. Microscopic techniques including fluorescence-based confocal laser scanning microscopy, super-resolution fluorescence microscopy and multiphoton microscopy; optical-based Raman microscopy, photoacoustic microscopy and optical coherence tomography; photothermal microscopy; electron microscopy (transmission electron microscope and scanning electron microscope); atomic force microscopy; X-ray microscopy and, correlative multimodal imaging are recognized as an indispensable tool in material research and aided in numerous discoveries. Microscopy holds great promise in detecting the fundamental structures of nanoparticles (NPs) that determines their performance and applications. Moreover, the intricate details that allows assessment of chemical composition, surface topology and interfacial properties, molecular, microstructure, and micromechanical properties are also elucidated. With plethora of applications, microscopy-based techniques have been used to characterize novel NPs alongwith their proficient designing and adoption of safe strategies to be exploited in nanomedicine. Consequently, microscopic techniques have been extensively used in the characterization of fabricated NPs, and their biomedical application in diagnostics and therapeutics. The present review provides an overview of the microscopy-based techniques for in vitro and in vivo application in nanomedical investigation alongwith their challenges and advancement to meet the limitations of conventional methods. © 2023 Wiley Periodicals LLC.
Nanoparticulate curcumin spray imparts prophylactic and therapeutic properties against SARS-CoV-2
(Springer Nature, 2024) Swapnil C. Kamble; Prem Pandey; Vijay K. Kanuru; Nilesh Rai; Vibhav Gautam; Dinesh Amalnerkar
Prevention of transmission of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the key to limit spread of COVID-19. Pharmaceutical preparation of curcumin, a natural polyphenolic compound, has been proven to have anti-inflammatory action. To have accomplishable function, nanosized curcumin may dictate a functionality against SARS-CoV-2. Herein, we used a unique water-dispersible nano-spray formulation of curcumin with enhanced efficacy. The nano-curcumin has an average size of 20 nm. No cytotoxicity was detected at the tested concentrations on Vero E6 cells, which is consistent with curcumin’s GRAS status of FDA. Vero E6 cell-assays demonstrated effective inhibitory activity when pre-treated with curcumin nanoformulation. Therapeutic effect on infected cells by subsequent exposure to SARS-CoV-2 viral particles shows considerable control on viral particle spread. Given the safety and efficacy of nano-curcumin, it appears to be an ideal candidate for prophylactic protection as well as in reducing the viral transmission. © Qatar University and Springer Nature Switzerland AG 2024.