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Lokesh Pathak

Bio: Lokesh Pathak is an academic researcher from Al-Ameen College of Pharmacy. The author has contributed to research in topics: Health effects of natural phenols and polyphenols & Identification (biology). The author has an hindex of 4, co-authored 7 publications receiving 161 citations. Previous affiliations of Lokesh Pathak include Gujarat Forensic Sciences University.

Papers
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Journal ArticleDOI
TL;DR: The review article discusses the antidepressant potential of some important polyphenols such as amentoflavone, apigenin, chlorogenic acid, curcumin, ferulic acid, hesperidin, rutin, quercetin, naringenin, resveratrol, ellagic acid, nobiletin and proanthocyanidins.
Abstract: Introduction: Natural polyphenols, the non-essential micronutrients, found in array of plant products, are known to affect various physiological and biochemical functions in the body. Studies have shown the protective effect of these polyphenols in different neurological and mental disorders. These polyphenols modulate monoaminergic neurotransmission in the brain and thus possess antidepressant-like activity at least in animal models of depression. Areas covered: The present review discusses the use of these natural polyphenols in the treatment of major depression. The review article discusses the antidepressant potential of some important polyphenols such as amentoflavone, apigenin, chlorogenic acid, curcumin, ferulic acid, hesperidin, rutin, quercetin, naringenin, resveratrol, ellagic acid, nobiletin and proanthocyanidins. The mechanism of action of these polyphenols in the treatment of major depression is also discussed in detail. Expert opinion: There is an exciting prospect in the discovery of natura...

97 citations

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TL;DR: It was found that nano-encapsulated curcumin were roughly spherical in shape, presented high positive zeta potential, monodisperse, amorphous in nature, stable in the pH range of 2–6 and have enhanced antioxidant potency in comparison to crystallineCurcumin in aqueous media.
Abstract: The supramolecular nano-assemblies formed by electrostatic interactions of two oppositely charged lipid and polymer have been made and used as nanocarriers for curcumin to address its bioavailability and solubility issues. These curcumin encapsulated nano-supramolecular assemblies were characterized with respect to their size (dynamic light scattering), morphology (TEM, SEM), zeta potential (Laser Doppler Velocimetry), encapsulation efficiency (EE), curcumin loading (CL) etc. Stability of the nano-assemblies was assessed at different storage times as a function of varying pH and temperature. The physicochemical characterization of nano-assemblies was performed using Fourier Transform Infra Red Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC). The in-vitro antioxidant lipid peroxidation (TBARS), radical scavenging (DPPH, NO, H2O2, reducing power) activity assays of powdered curcumin and nano-encapsulated curcumin were performed. It was found that nano-encapsulated curcumin were roughly spherical in shape, presented high positive zeta potential (>30 mV), monodisperse (polydispersity index <0.3), amorphous in nature, stable in the pH range of 2–6 and have enhanced antioxidant potency in comparison to crystalline curcumin in aqueous media. In conclusion, the curcumin encapsulated nanocarriers system has great potential as functional food ingredient of natural origin.

43 citations

Journal ArticleDOI
TL;DR: This study has depicted successful and stepwise application of pharmacophore mapping, molecular docking, and QSAR studies in target identification and lead optimization of flavonoids.
Abstract: In silico molecular modeling studies were carried out on some newly synthesized flavanoid analogues. Search for potential targets for these compounds was performed using pharmacophore-mapping algorithm employing inverse screening of some representative compounds to a large set of pharmacophore models constructed from human target proteins. Further, molecular docking studies were carried out to assess binding affinity of these compounds to proteins mediating tumor growth. In vitro anticancer studies were carried out on colon cancer cell lines (HCT116) to assess validity of this approach for target identification of the new compounds. Further important structural features of compounds for anticolon cancer activity were assessed using Monte Carlo-based SMILES and hydrogen graph-Based QSAR studies. In conclusion this study have depicted successful and stepwise application of pharmacophore mapping, molecular docking, and QSAR studies in target identification and lead optimization of flavonoids.

35 citations

Journal ArticleDOI
TL;DR: Although many compounds exhibited significant zones of inhibition, their minimum inhibitory concentrations established by broth assay were higher, suggesting these molecules are not potent at lower concentrations.
Abstract: Infectious diseases are on the rise due to development of multidrug-resistant strains, and this renders the search for newer antimicrobials. Hybrid compounds of different scaffolds are expected to enhance the bioactivity by improved affinity to target proteins while retaining the biological efficacy of each of the components. In view of this, a series of pyrazolines with aryloxy acid in the side chain are synthesized and evaluated for their antimicrobial potential. Pyrazoline-substituted aryloxy acids were synthesized in very good yields, starting from chalcones. Synthetic method is adopted in such a way that the use of any solvents is avoided. The structures of these compounds were confirmed using FTIR, NMR, and Mass spectrometry. The potential of these molecules as antimicrobial agents was predicted using molecular docking studies. The activities were also assessed using zone of inhibition and minimum inhibitory concentration (MIC) measurement against tuberculosis variant bacteria, Mycobacterium...

21 citations

Journal ArticleDOI
TL;DR: Alginate coating offered more controlled release of the curcumin in acidic conditions suggesting that these alginate coated nanoparticles imparted enteric coating character.
Abstract: Alginate-chitosan coated lecithin nanoparticles loaded with Curcumin have been prepared by layer deposition of alginate on lecithin/chitosan nanoparticles and were characterized. The prepared nanoparticles were physicochemically characterized to ensure alginate coating. The encapsulation efficiency and loading of the active nutraceutical were assessed using spectrophotometric measurements. The biological activities of the prepared nanoparticles were assessed by membrane stabilization effect of the nanoparticles on goat RBCs under hypotonic and thermally induced conditions. The biocompatibility of blank nanocarriers was assessed by performing In vitro cytotoxicity studies on HEK cell lines. The release profile of curcumin from alginate uncoated and alginate coated nanoparticles were compared to analyze effect of surface charge of the particles on studied bioactivities. It was found that uniformly sized alginate coated nanoparticles were formed with negative surface charge. It was also observed that there was no significant difference due to surface charge of the nanoparticles on cytotoxicity and membrane stabilization activity. However alginate coating offered more controlled release of the curcumin in acidic conditions suggesting that these alginate coating imparted enteric coating character.

4 citations


Cited by
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Journal ArticleDOI
TL;DR: This review examines and details a model through which a complex series of environmental factors and biological pathways contribute to increased redox signaling and consequently increased O&NS in mood disorders.

317 citations

Journal ArticleDOI
TL;DR: It is argued that the consumption of fermented foods may be particularly relevant to the emerging research linking traditional dietary practices and positive mental health, and that properly controlled fermentation may often amplify the specific nutrient and phytochemical content of foods, the ultimate value of which may associated with mental health.
Abstract: The purposeful application of fermentation in food and beverage preparation, as a means to provide palatability, nutritional value, preservative, and medicinal properties, is an ancient practice. Fermented foods and beverages continue to make a significant contribution to the overall patterns of traditional dietary practices. As our knowledge of the human microbiome increases, including its connection to mental health (for example, anxiety and depression), it is becoming increasingly clear that there are untold connections between our resident microbes and many aspects of physiology. Of relevance to this research are new findings concerning the ways in which fermentation alters dietary items pre-consumption, and in turn, the ways in which fermentation-enriched chemicals (for example, lactoferrin, bioactive peptides) and newly formed phytochemicals (for example, unique flavonoids) may act upon our own intestinal microbiota profile. Here, we argue that the consumption of fermented foods may be particularly relevant to the emerging research linking traditional dietary practices and positive mental health. The extent to which traditional dietary items may mitigate inflammation and oxidative stress may be controlled, at least to some degree, by microbiota. It is our contention that properly controlled fermentation may often amplify the specific nutrient and phytochemical content of foods, the ultimate value of which may associated with mental health; furthermore, we also argue that the microbes (for example, Lactobacillus and Bifidobacteria species) associated with fermented foods may also influence brain health via direct and indirect pathways.

197 citations

Journal ArticleDOI
TL;DR: This comprehensive review of the current evidence defining the position of polyphenols in the prevention/treatment of human chronic diseases, including prostate cancer and other types of cancer, cardiovascular diseases, diabetes mellitus and neurodegenerative diseases such as Alzheimer's and Parkinson's disease focuses on their ability to modulate multiple signalling transduction pathways involved in the pathophysiology of these diseases.

184 citations

Journal ArticleDOI
TL;DR: Resveratrol is a potent activator of SIRT1, and thus may mimic caloric restriction to prevent diseases of aging in animals and in individuals with mild‐to‐moderate AD.
Abstract: The amyloid hypothesis suggests that the progressive accumulation and deposition of central nervous system (CNS) amyloid with aging is the proximate cause of Alzheimer's disease (AD). Thus, targeting molecular mechanisms of aging may be a viable treatment approach. Caloric restriction prevents diseases of aging, including AD, in animal models, perhaps by activation of sirtuins. The sirtuins (e.g., mammalian SIRT1) are deacetylases that link energy balance (NAD+ /NADH) to regulation of gene transcription. Resveratrol is a potent activator of SIRT1, and thus may mimic caloric restriction to prevent diseases of aging. We conducted a randomized, double-blind, placebo-controlled, phase II trial of resveratrol for individuals with mild-to-moderate AD. Resveratrol (1) is detectable in cerebrospinal fluid (at low nanomolar levels), (2) is safe and well tolerated, (3) alters AD biomarker trajectories, (4) preserves blood-brain barrier integrity, and (5) modulates the CNS immune response. Further studies are needed to determine the safety and efficacy of resveratrol and the validity of this approach in the treatment and prevention of AD and other diseases of aging.

181 citations

Journal ArticleDOI
TL;DR: Two phytochemicals from bioactive dietary polyphenols are identified, shown to show their antidepressant effect in a rodent model of depression, and that this effect is mediated by epigenetic and anti-inflammatory mechanisms.
Abstract: Major depressive disorder is associated with abnormalities in the brain and the immune system. Chronic stress in animals showed that epigenetic and inflammatory mechanisms play important roles in mediating resilience and susceptibility to depression. Here, through a high-throughput screening, we identify two phytochemicals, dihydrocaffeic acid (DHCA) and malvidin-3′-O-glucoside (Mal-gluc) that are effective in promoting resilience against stress by modulating brain synaptic plasticity and peripheral inflammation. DHCA/Mal-gluc also significantly reduces depression-like phenotypes in a mouse model of increased systemic inflammation induced by transplantation of hematopoietic progenitor cells from stress-susceptible mice. DHCA reduces pro-inflammatory interleukin 6 (IL-6) generations by inhibiting DNA methylation at the CpG-rich IL-6 sequences introns 1 and 3, while Mal-gluc modulates synaptic plasticity by increasing histone acetylation of the regulatory sequences of the Rac1 gene. Peripheral inflammation and synaptic maladaptation are in line with newly hypothesized clinical intervention targets for depression that are not addressed by currently available antidepressants.

172 citations