Displaying publications 1 - 20 of 69 in total

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  1. A Panoramic Review on the Management of Rheumatoid Arthritis through Herbalism
    Chaudhary S, Sharma S, Fuloria S
    Curr Rheumatol Rev, 2024 Apr 05.
    PMID: 38591212 DOI: 10.2174/0115733971279100240328063232
    Arthritis is a chronic inflammatory condition that affects millions of individuals worldwide. The conventional treatment options for arthritis often come with limitations and potential side effects, leading to increased interest in herbal plants as alternative therapies. This article provides a comprehensive overview of the use of herbal plants in arthritis treatment, focusing on their traditional remedies, active components, mechanisms of action, and pharmaceutical approaches for enhancing their delivery. Various herbal plants, including turmeric, ginger, Boswellia, and willow bark, have shown anti-inflammatory and analgesic properties, making them valuable options for managing arthritis symptoms. The active components of these herbal plants, such as curcumin, gingerols, and boswellic acids, contribute to their therapeutic effects. To enhance the delivery of herbal medicines, pharmaceutical approaches like nanoparticle-based drug delivery systems, liposomes, polymeric nanoparticles, nanoemulsions, microneedles, and inhalation systems have been explored. These approaches aim to improve bioavailability, targeted delivery, and controlled release of herbal compounds. Safety considerations, including potential interactions with medications and the risk of allergic reactions, are also discussed. Future perspectives for this field involve conducting well-designed clinical studies, enhancing standardization and quality control measures, exploring novel drug delivery systems, and fostering collaborations between traditional medicine practitioners and healthcare professionals. Continued research and development in these areas will help unlock the full potential of herbal plants in arthritis treatment, offering personalized and effective care for affected individuals.
  2. Fulltext Acanthomatous ameloblastoma in anterior mandibular region of a young patient: A rare case report
    Ugrappa S, Jain A, Fuloria NK, Fuloria S
    Ann Afr Med, 2017 Apr-Jun;16(2):85-89.
    PMID: 28469123 DOI: 10.4103/aam.aam_51_16
    Ameloblastoma is the most known of the epithelial odontogenic benign tumor. It is slow growing and locally aggressive in nature and most commonly seen in the posterior mandible. Various histopathological variants exist, among which acanthomatous type of ameloblastoma is one of the rarest types. Acanthomatous ameloblastoma is usually seen in older aged human population and most commonly reported in canine region of dogs in literature. Here, we report a rare case of acanthomatous ameloblastoma in a young male patient involving mandibular anterior region crossing the midline with recurrence over a period of 2 years of follow-up after surgical resection.
  3. Anti-inflammatory and ulcerogenic activity of newer phytoisolates of Swertia alata C.B. Clarke
    Bajaj S, Wakode S, Kaur A, Fuloria S, Fuloria N
    Nat Prod Res, 2021 Dec;35(23):5055-5065.
    PMID: 32498574 DOI: 10.1080/14786419.2020.1775224
    The present study was intended to evaluate the in vitro (COX-1/COX-2) and in vivo anti-inflammatory and ulcerogenic activity of newer phytoconstituents isolated from the aerial parts of Swertia alata C.B. Clarke (Gentianaceae). For isolation of newer phytoconstituents, the ethanolic extract of aerial parts of S. alata was subjected to column chromatography using mixture of petroleum ether and chloroform in various concentrations, which yielded two phytoisolates characterised as nonacosyl triacontanoate (SA-3) and 8-O-glucpyranosyl-(2-acetyl)-1,3-dihydroxy-5-methoxy-xanthone (SA-9). Identification of compounds was based on melting point, UV, FTIR, 1H-NMR, 13C-NMR and mass spectrometric data. The isolates were screened for in vitro COX-1/COX-2 inhibitory activity, in vivo anti-inflammatory and ulcerogenic activity. Among the two compounds, SA-3 was found to be more effective than SA-9. The ulcerogenic study revealed significant gastric tolerance of SA-3 and SA-9 in comparison to indomethacin.
  4. Evidences of hepatoprotective and antioxidant effect of Citrullus colocynthis fruits in paracetamol induced hepatotoxicity
    Vakiloddin S, Fuloria N, Fuloria S, Dhanaraj SA, Balaji K, Karupiah S
    Pak J Pharm Sci, 2015 May;28(3):951-7.
    PMID: 26004728
    The objective of present study was to explore the hepatoprotective and antioxidant profile of Citrullus colocynthis fruits. Hepatoprotective profile of methanolic extract of Citrullus colocynthis fruits (MECCF) was investigated on rats, which were made hepatotoxic using paracetamol. The antioxidant profile of MECCF was evaluated by conducting Catalase, Super oxide Dismutase, Lipid Peroxidation and Diphenyl Picryl Hydrazyl tests. During hepatoprotective investigation, the Paracetamol treated group II showed significant increase in total bilirubin (TB), serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) and alkaline phosphatase (ALP) level. The results so obtained showed that pretreatment of rats with MECCF 300mg/kg p.o. decreases the elevated TB, SGOT, SGPT and ALP serum levels. Also, MECCF inhibitory profile was found comparable with toxicant group (Paracetamol 2g/kg, p.o.). The present study concludes that MECCF fruit possess significant hepatoprotective and antioxidant activity.
  5. Natural cyclic polypeptides as vital phytochemical constituents from seeds of selected medicinal plants
    Dahiya R, Dahiya S, Shrivastava J, Fuloria NK, Gautam H, Mourya R, et al.
    Arch Pharm (Weinheim), 2021 Feb 01.
    PMID: 33522644 DOI: 10.1002/ardp.202000446
    Cyclopolypeptides are among the most predominant biomolecules in nature, especially those derived from plant seeds. This category of compounds has gained extraordinary attention due to remarkable variety of structures and valuable biofunctions. These congeners display enormous variation in terms of both structure and function and are the most significant biomolecules due to their widespread bioproperties. The estrogenic activity, immunosuppressive activity, cytotoxicity, vasorelaxant activity, and other properties possessed by cyclic peptides from seeds of plants make these congeners attractive leads for the drug discovery process. The current study covers the important structural features, structure-activity relationship, synthesis methods, and bioproperties of plant seeds-originated bioactive peptides from Vaccaria segetalis, Linum usitatissimum, and Goniothalamus leiocarpus, which may prove vital for the development of novel therapeutics based on a peptide skeleton.
  6. Impact of COVID-19 in public health: Prevalence and preventive approaches
    Subramaniyan V, Chakravarthi S, Seng WY, Kayarohanam S, Fuloria NK, Fuloria S
    Pak J Pharm Sci, 2020 Jul;33(4):1739-1745.
    PMID: 33583811
    The outbreak of CoVID-19 infection rapidly increases worldwide. Most of the continents affecting from CoVID-19 and still widening its burden disease (Jones DS, 2020; Lai et al., 2020). Along with its fatality rates, CoVID-19 has caused physiological disturbances in the society and termed as "coronophobia". CoVID-19 with renal failure, severe pneumonia and respiratory syndrome patients have been reported to increase the severity of disease conditions (Sevim et al., 2020). Also, CoVID-19 with cancer patients increase the higher risk of infections. Currently, there is no vaccine or specific treatment against CoVID-19 and drug research centres continuously investigating the potential drug against CoVID-19 (Osama and Amer, 2020). For the past 20 years two major coronavirus epidemics have occurred in public includes SARS-CoV approximately 8000 cases and 800 deaths and MERS-CoV 2,500 cases and 800 deaths and these continuing sporadically (Cascella et al., 2020).
  7. Fulltext Chemical Modification of Banana Trunk Fibers for the Production of Green Composites
    Sathasivam KV, Haris MRHM, Fuloria S, Fuloria NK, Malviya R, Subramaniyan V
    Polymers (Basel), 2021 Jun 11;13(12).
    PMID: 34208069 DOI: 10.3390/polym13121943
    Natural fibers have proven to be excellent reinforcing agents in composite materials. However, a critical disadvantage of natural fibers is their hydrophilic nature. In this study, banana trunk fibers were mechanically damaged using a high-speed blender, and the resulting fibers (MDBTF) were treated with (i) stearic acid (SAMDBTF) and (ii) calcium carbonate coated with 5% (wt/wt) stearic acid (SACCMDBTF). The moisture sorption, oil sorption and thermal properties of the fibers were determined. The morphology, roughness and the functional groups present were also investigated. Study data of the present study indicate that SACCMDBTF exhibited a faster oil sorption capacity than SAMDBTF. Fast uptake of the oil occurred during the first 5 min, whereby the quantity of oil sorbed in SAMDBTF and SACCMDBTF was 5.5 and 15.0 g oil g-1 fiber, respectively. The results of a used engine oil uptake study revealed that SAMDBTF and SACCMDBTF sorbed 9.5 and 18.3 g/g-1 fiber, respectively, at equilibrium. The obtained results suggest that the mechanically damaged process improved the thermal stability of the fibers. This work reveals that the inclusion of stearic-acid-coated calcium carbonate into the interstices of MDBTF yields is environmentally safe for green hydrophobic composites. SACCMDBTF are used as efficient adsorbents for the removal of spilled oil on aqueous media.
  8. Regenerative Potential of Stem Cells Derived from Human Exfoliated Deciduous (SHED) Teeth during Engineering of Human Body Tissues
    Fuloria S, Jain A, Singh S, Hazarika I, Salile S, Fuloria NK
    Curr Stem Cell Res Ther, 2021;16(5):507-517.
    PMID: 33390148 DOI: 10.2174/1574888X16999201231213206
    The current decade witnesses the regenerative potential of Stem Cells (SCs) based lifesaving therapies for the treatment of various disease conditions. Human teeth act as a reservoir for SCs that exist in high abundance in baby, wisdom, and permanent teeth. The collection of Stem cells from Human Exfoliated Deciduous teeth (SHED) is considered a simple process as it offers the convenience of little or no pain. In comparison to the SCs from dental or bone marrow or other tissues, the SHED offers the benefit of higher cellular differentiation and proliferation. Massive in vitro and in vivo studies reveal the regenerative potential of SHED in the engineering of the dental pulp tissue, neuronal tissue, root, bio root, cardiovascular tissues, lymphatic tissues, renal tissues, dermal tissues, hepatic tissues, and bone tissues. The current review describes the methods of collection/ isolation/storage, various biomarkers, and types of SHED. This review highlights the regenerative potential of SHED in the engineering of different tissues of the human body. As per the available research evidence, the present study supports that SHED may differentiate into the endothelial cells, neurons, odontoblasts, pancreatic β-cells, hepatocytes, renal cells, fibroblasts, osteoblasts, and many other types of cells. The present study recommends that further clinical trials are required before the clinical application of SHED-based therapies.
  9. Mucoadhesive microspheres of glutaraldehyde crosslinked mucilage of Isabgol husk for sustained release of gliclazide
    Sharma VK, Sharma PP, Mazumder B, Bhatnagar A, Subramaniyan V, Fuloria S, et al.
    J Biomater Sci Polym Ed, 2021 08;32(11):1420-1449.
    PMID: 33941041 DOI: 10.1080/09205063.2021.1925389
    Mucoadhesive microspheres have their own significant amongst the various sustained release drug delivery systems. The prolonged residence time of these delivery devices at drug absorption site results in steep concentration gradient and enhanced bioavailability. In this study, the mucilage of Isabgol husk was applied as polymeric backbone to develop gliclazide loaded microspheres by crosslinking with glutaraldehyde. The formulations were studied for surface morphology, swelling behavior, particle size, in vitro release, release kinetics, in vitro mucoadhesion and gamma scintigraphy in rabbits. The release of gliclazide from microspheres was controlled by swelling of crosslinked microspheres followed by diffusion. Gamma scintigraphic images acquired for microspheres retention in gastrointestinal track of rabbits indicated the residence of formulation upto 24 h after oral administration. Gliclazide retained its integrity in polymeric matrix of microspheres as observed by Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffractometry. The sustained release of gliclazide and prolonged retention of microspheres in gastrointestinal track disclosed the rationality of mucoadhesive Isabgol husk microspheres in controlling the hyperglycemia in diabetes.
  10. Isolation of new phytometabolites from Alpinia galanga willd rhizomes
    Sharma PK, Fuloria S, Ali M, Singh A, Kushwaha SP, Sharma VK, et al.
    Pak J Pharm Sci, 2021 Jul;34(4):1397-1401.
    PMID: 34799313
    The current research was aimed to isolate newer phyto-metabolites from rhizomes of Alpinia galanga plant. Study involved preparation of Alpinia galanga rhizome methanolic extract, followed by normal phase column chromatography assisted isolation of new phytometabolites (using different combinations of chloroform and methanol), and characterization (by UV, FTIR, 13C-NMR, 1H-NMR, COSY, DEPT and Mass spectrometry). The isolation and characterization experiment offered two phytometabolites: an ester (Ag-1) and tetrahydronapthalene type lactone (Ag-2). Present study concludes and reports the two phytometabolites, benzyl myristate (Ag-1) and 3-Methyl-6α, 8β-diol-7-carboxylic acid tetralin-11, 9β-olide (Ag-2) for the first time in Alpinia galanga rhizome. The study recommends that these phytometabolites Ag-1 and Ag-2 can be utilized as effective analytical biomarkers for identification, purity and quality control of this plant in future.
  11. Fulltext Alcohol-associated liver disease: A review on its pathophysiology, diagnosis and drug therapy
    Subramaniyan V, Chakravarthi S, Jegasothy R, Seng WY, Fuloria NK, Fuloria S, et al.
    Toxicol Rep, 2021;8:376-385.
    PMID: 33680863 DOI: 10.1016/j.toxrep.2021.02.010
    One of the global burdens of health care is an alcohol-associated liver disease (ALD) and liver-related death which is caused due to acute or chronic consumption of alcohol. Chronic consumption of alcohol damage the normal defense mechanism of the liver and likely to disturb the gut barrier system, mucosal immune cells, which leads to decreased nutrient absorption. Therapy of ALD depends upon the spectrum of liver injury that causes fatty liver, hepatitis, and cirrhosis. The foundation of therapy starts with abstinence from alcohol. Corticosteroids are used for the treatment of ALD but due to poor acceptance, continuing mortality, and identification of tumor necrosis factor-alpha as an integral component in pathogenesis, recent studies focus on pentoxifylline and, antitumor necrosis factor antibody to neutralize cytokines in the therapy of severe alcoholic hepatitis. Antioxidants also play a significant role in the treatment but till today there is no universally accepted therapy available for any stage of ALD. The treatment aspects need to restore the gut functions and require nutrient-based treatments to regulate the functions of the gut system and prevent liver injury. The vital action of saturated fatty acids greatly controls the gut barrier. Overall, this review mainly focuses on the mechanism of alcohol-induced metabolic dysfunction, contribution to liver pathogenesis, the effect of pregnancy, and targeted therapy of ALD.
  12. Patient Care and Treatment Strategies for Skin Diseases in Sub-Saharan Africa: Role of Traditional and Western Medicines
    Sharma A, Sundaram S, Malviya R, Verma S, Fuloria NK, Fuloria S, et al.
    Infect Disord Drug Targets, 2023;23(3):e190922208916.
    PMID: 36121085 DOI: 10.2174/1871526522666220919105643
    The perspective of the people of Sub-Saharan Africa (SSA) toward both traditional and western healthcare systems varies. The goal of the current study is to examine the SSA's unique skin disease health care system. This study comprises numerous research that sought to examine how the general public feels about the SSA's current healthcare system. In this review, common skin conditions, such as atopic dermatitis, buruli ulcers, dermatophytosis, and scabies, are addressed. According to this report, government agencies must pay particular attention to skin illnesses in SSA and raise public awareness. Availability of medical care, socioeconomic factors, degree of education, and other factors influence patients' attitudes toward traditional and western health care differently in different geographic areas. Facts suggest that self-medication is the preference of the majority of patients before seeking dermatological care. The present study concludes that the magnitude of skin diseases is neglected or underestimated in many regions of SSA. Also, western healthcare facilities of many regions of SSA are not up to the mark. The present study recommends that proper access to the health care system and awareness about skin diseases through various government programs can be helpful in the regulation of skin disorders among people of SSA.
  13. Fulltext Improvement in Digestion Resistibility of Mandua Starch (Eleusine coracana) after Cross-Linking with Epichlorohydrin
    Malik MK, Kumar V, Sharma PP, Singh J, Fuloria S, Subrimanyan V, et al.
    ACS Omega, 2022 Aug 09;7(31):27334-27346.
    PMID: 35967061 DOI: 10.1021/acsomega.2c02327
    Starch, being a polymer of excessive demand for the development of products of pharmaceutical importance, has been tremendously treated in many ways for improving the desired characteristics such as viscosity, paste clarity, digestibility, swelling, syneresis, and so forth. In the present study, alkali-extracted starch of mandua grains (Eleusine coracana; family Poaceae) was treated with epichlorohydrin for cross-linking and the modified starch was assessed for swelling, solubility, water binding capacity, moisture content, and degree of cross-linking. The digestion resistibility of modified starch was analyzed in simulated gastric fluid (pH 1.2), simulated intestinal fluid (pH 6.8), and simulated colonic fluid (pH 7.4). The structural modifications in treated mandua starch were analyzed by Fourier transform infrared (FTIR) spectroscopy, powder X-ray diffraction (XRD), scanning electron microscopy, thermogravimetric analysis, and C13 nuclear magnetic resonance (13C NMR). The results of the study reflected the significant modification in mandua starch after treatment with epichlorohydrin (1.0% w/w sdb, solid dry basis). The degree of cross-linking of treated mandua starch was 85.15%, and the swelling capacity of mandua starch changed from 226.51 ± 2.175 to 103.14 ± 1.998% w/w after cross-linking with epichlorohydrin. A remarkable increment in digestion resistibility was observed in modified mandua starch. The XRD pattern and FTIR spectra revealed the presence of resistant starch after chemical modification. The decomposition pattern of modified mandua starch was also different from extracted mandua starch. All the results reflected the effective modification of mandua starch by epichlorohydrin and the formation of resistant starch to a significant content. The treated mandua starch may have the potential in developing various preparations of food, nutraceuticals, and pharmaceuticals.
  14. Fulltext A Comprehensive Review on Source, Types, Effects, Nanotechnology, Detection, and Therapeutic Management of Reactive Carbonyl Species Associated with Various Chronic Diseases
    Fuloria S, Subramaniyan V, Karupiah S, Kumari U, Sathasivam K, Meenakshi DU, et al.
    Antioxidants (Basel), 2020 Nov 02;9(11).
    PMID: 33147856 DOI: 10.3390/antiox9111075
    Continuous oxidation of carbohydrates, lipids, and amino acids generate extremely reactive carbonyl species (RCS). Human body comprises some important RCS namely hexanal, acrolein, 4-hydroxy-2-nonenal, methylglyoxal, malondialdehyde, isolevuglandins, and 4-oxo-2- nonenal etc. These RCS damage important cellular components including proteins, nucleic acids, and lipids, which manifests cytotoxicity, mutagenicity, multitude of adducts and crosslinks that are connected to ageing and various chronic diseases like inflammatory disease, atherosclerosis, cerebral ischemia, diabetes, cancer, neurodegenerative diseases and cardiovascular disease. The constant prevalence of RCS in living cells suggests their importance in signal transduction and gene expression. Extensive knowledge of RCS properties, metabolism and relation with metabolic diseases would assist in development of effective approach to prevent numerous chronic diseases. Treatment approaches for RCS associated diseases involve endogenous RCS metabolizers, carbonyl metabolizing enzyme inducers, and RCS scavengers. Limited bioavailability and bio efficacy of RCS sequesters suggest importance of nanoparticles and nanocarriers. Identification of RCS and screening of compounds ability to sequester RCS employ several bioassays and analytical techniques. Present review describes in-depth study of RCS sources, types, properties, identification techniques, therapeutic approaches, nanocarriers, and their role in various diseases. This study will give an idea for therapeutic development to combat the RCS associated chronic diseases.
  15. Design and synthesis of newer 1,3,4-oxadiazole and 1,2,4-triazole based Topsentin analogues as anti-proliferative agent targeting tubulin
    Naaz F, Ahmad F, Lone BA, Pokharel YR, Fuloria NK, Fuloria S, et al.
    Bioorg Chem, 2020 01;95:103519.
    PMID: 31884140 DOI: 10.1016/j.bioorg.2019.103519
    A set of two series of 1,3,4-oxadiazole (11a-n) and 1,2,4-Triazole (12a, c, e, g, h, j-n) based topsentin analogues were prepared by replacing imizadole moiety of topsentin through a multistep synthesis starting from indole. All the compounds synthesized were submitted for single dose (10 µM) screening against a NCI panel of 60-human cancer cell lines. Among all cancer cell lines, colon (HCC-2998) and Breast (MCF-7, T-47D) cancer cell lines were found to be more susceptible for this class of compounds. Among the compounds tested, compounds 11a, 11d, 11f, 12e and 12h, were exhibited good anti-proliferative activity against various cancer cell lines. Compounds 11d, 12e and 12h demonstrated better activity with IC50 2.42 µM, 3.06 µM, and 3.30 µM respectively against MCF-7 human cancer cell line than that of the standard drug doxorubicin IC50 6.31 µM. Furthermore, 11d induced cell cycle arrest at G0/G1 phase and also disrupted mitochondrial membrane potential with reducing cell migration potential of MCF-7 cells in dose dependent manner. In vitro microtubule polymerization assays found that compound 11d disrupt tubulin dynamics by inhibiting tubulin polymerization with IC50 3.89 μM compared with standard nocodazole (IC50 2.49 μM). In silico docking studies represented that 11d was binding at colchicine binding site of β-tubulin. Compound 11d emerged as lead molecule from the library of compounds tested and this may serve as a template for further drug discovery.
  16. Fulltext Chemical Characterization and Anti-Inflammatory Activity of Phytoconstituents from Swertia alata
    Bajaj S, Fuloria S, Subramaniyan V, Meenakshi DU, Wakode S, Kaur A, et al.
    Plants (Basel), 2021 May 31;10(6).
    PMID: 34072717 DOI: 10.3390/plants10061109
    Swertia alata C.B Clarke (Gentianaceae) is a well-reported plant in the traditional system of medicine. The present study was intended to isolate the phytoconstituents from the ethanolic extract of the aerial parts of S. alata; and evaluate for in vitro COX-1/COX-2 inhibition activity, in vivo anti-inflammatory and ulcerogenic activity. Phytoisolation involved partitioning of S. alata ethanolic extract into petroleum ether and chloroform soluble fractions using silica gel-based column chromatography. The isolation afforded two phytoisolates, namely oleanolic acid (SA-1) and 3-hydroxylup-12-(13)-ene-17-carboxylic acid (SA-4). Phytoisolates structures were established by melting point, ultraviolet (UV), attenuated total reflection-Fourier-transform infrared (ATR-FTIR), nuclear magnetic resonance (1H-NMR, 13C-NMR and HMBC) and mass spectrometry. Phytoisolates were further evaluated for in vitro cyclooxygenase (COX-1/COX-2) inhibitory activity, in vivo anti-inflammatory and ulcerogenic activity. The study revealed SA-4 (COX-1/COX-2 inhibition activity of 104/61.68 µM with % inhibition of 61.36) to be more effective than SA-1 (COX-1/COX-2 inhibition activity of 128.4/87.25 µM, with % inhibition of 47.72). SA-1 and SA-4, when subjected to ulcerogenic study, exhibited significant gastric tolerance. The current study reports chromatographic isolation and spectrometric characterization of SA-1 and SA-4. The present study concludes that compound SA-4 possess significant anti-inflammatory activity and less irritant property over gastric mucosa with no significant ulcerogenicity in comparison to indomethacin.
  17. Novel 9-(2-(1-arylethylidene)hydrazinyl)acridine derivatives: Target Topoisomerase 1 and growth inhibition of HeLa cancer cells
    Haider MR, Ahmad K, Siddiqui N, Ali Z, Akhtar MJ, Fuloria N, et al.
    Bioorg Chem, 2019 07;88:102962.
    PMID: 31085373 DOI: 10.1016/j.bioorg.2019.102962
    A series of 9-(2-(1-arylethylidene)hydrazinyl)acridine and its analogs were designed, synthesized and evaluated for biological activities. Various biochemical assays were performed to determine the free radical scavenging capacity of synthesized compounds (4a-4j). Anticancer activity of these compounds was assessed against two different human cancer cell lines viz cervical cancer cells (HeLa) and liver cancer cells (HepG2) as well as normal human embryonic kidney cell line (HEK 293). Compounds 4b, 4d and 4e showed potential anti-proliferative effects on HeLa cells. Based on results obtained from antioxidant and cytotoxicity studies, 4b, 4d and 4e were further studied in detail for different biological activities. 4b, 4d and 4e reduced the cell growth, inhibited metastatic activity and declined the potential of cell migration in HeLa cell lines. Topoisomerase1 (Top1) treated with compounds 4b, 4d and 4e exhibited inhibition of Top1 and prevented DNA replication. Molecular docking results validate that interaction of compounds 4b, 4d and 4e with Top1-DNA complex, which might be accountable for their inhibitory effects. Further it was concluded that compounds 4b, 4d and 4e arrests the cells at S phase and consequently induces cell death through DNA damage in HeLa cells.
  18. Identification of Phytoconstituents of Tragia Involucrata leaf Extracts and Evaluate their Correlation with Anti-inflammatory & Antioxidant Properties
    Velu V, Banerjee S, Radhakrishnan V, Gupta G, Chellappan DK, Fuloria NK, et al.
    Antiinflamm Antiallergy Agents Med Chem, 2021;20(3):308-315.
    PMID: 33573582 DOI: 10.2174/1871523020666210126144506
    AIMS: The present investigation was aimed at exploring the phytoconstituents using Gas Chromatography Mass Spectroscopy and to evaluate antioxidant and anti-inflammatory properties of the leaf extracts.

    MATERIALS AND METHODS: The extracts were obtained sequentially with petroleum ether, ethyl acetate and water using Soxhlet apparatus. The anti-inflammatory property of the identified compounds using GC- MS spectroscopy was evaluated in silico. The antioxidant activity was performed by DPPH and H2O2 method whereas anti-inflammatory study was carried out by HRBC membrane stabilization method. Terpenoids were found to be a major constituents in petroleum ether extract while, phenols and flavonoids were predominantly found in ethyl acetate extract.

    RESULTS AND DISCUSSION: The GC-MS analysis of the extract revealed six major molecules including Squalene, 19β, 28-epoxyleanan-3-ol and 2-tu-Butyl-5-chloromethyl-3-methyl-4-oxoimidazolidine- 1-carboxylic acid. The ethyl acetate extract showed a significant antioxidant activity (P<0.01) in both DPPH method (70.87%) and H2O2 method (73.58%) at 200 μg mL-1. Increased membrane stabilization of petroleum ether extract was observed in the in vitro anti-inflammatory activity study. A strong relationship between the terpenoid content and anti-inflammatory activity was obtained from the correlation (0.971) and docking study.

    CONCLUSION: These results justify T. involucrata to be a rich source of terpenoids with potent anti- inflammatory property.

  19. Fulltext Potential of Marine Terpenoids against SARS-CoV-2: An In Silico Drug Development Approach
    Sahoo A, Fuloria S, Swain SS, Panda SK, Sekar M, Subramaniyan V, et al.
    Biomedicines, 2021 Oct 20;9(11).
    PMID: 34829734 DOI: 10.3390/biomedicines9111505
    In an emergency, drug repurposing is the best alternative option against newly emerged severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection. However, several bioactive natural products have shown potential against SARS-CoV-2 in recent studies. The present study selected sixty-eight broad-spectrum antiviral marine terpenoids and performed molecular docking against two novel SARS-CoV-2 enzymes (main protease or Mpro or 3CLpro) and RNA-dependent RNA polymerase (RdRp). In addition, the present study analysed the physiochemical-toxicity-pharmacokinetic profile, structural activity relationship, and phylogenetic tree with various computational tools to select the 'lead' candidate. The genomic diversity study with multiple sequence analyses and phylogenetic tree confirmed that the newly emerged SARS-CoV-2 strain was up to 96% structurally similar to existing CoV-strains. Furthermore, the anti-SARS-CoV-2 potency based on a protein-ligand docking score (kcal/mol) exposed that the marine terpenoid brevione F (-8.4) and stachyflin (-8.4) exhibited similar activity with the reference antiviral drugs lopinavir (-8.4) and darunavir (-7.5) against the target SARS-CoV-Mpro. Similarly, marine terpenoids such as xiamycin (-9.3), thyrsiferol (-9.2), liouvilloside B (-8.9), liouvilloside A (-8.8), and stachyflin (-8.7) exhibited comparatively higher docking scores than the referral drug remdesivir (-7.4), and favipiravir (-5.7) against the target SARS-CoV-2-RdRp. The above in silico investigations concluded that stachyflin is the most 'lead' candidate with the most potential against SARS-CoV-2. Previously, stachyflin also exhibited potential activity against HSV-1 and CoV-A59 within IC50, 0.16-0.82 µM. Therefore, some additional pharmacological studies are needed to develop 'stachyflin' as a drug against SARS-CoV-2.
  20. Disruption of the biological activity of protease-activated receptors2/4 in adults rather than children in SARS CoV-2 virus-mediated mortality in COVID-19 infection
    Singh Y, Fuloria NK, Fuloria S, Subramaniyan V, Almalki WH, Gupta G, et al.
    Drug Dev Res, 2021 Dec;82(8):1075-1078.
    PMID: 34469011 DOI: 10.1002/ddr.21874
    One of the most remarkable results in 2019 is the reduced prevalence and death of children from coronavirus infection (COVID-19). In 2019, a worldwide pandemic impacted around 0.1 billion individuals, with over 3.5 million mortality reported in the literature. There is minimal knowledge on SARS-CoV-2 infection immunological responses in kids. Studies have been focused mostly on adults and children since the course of pediatric sickness is often short. In adults, severe COVID-19 is related to an excessive inflammatory reaction. Macrophages and monocytes are well known to contribute to this systemic response, although numerous lines are indicative of the importance of neutrophils. An increased number of neutrophils and neutrophil to lymphocyte ratios are early signs of SARS-CoV-2 and a worse prognosis. In this study that it is crucial to monitor PAR2 and PAR4 expression and function (since nursing children have elevated levels) and the inhibiting the normal physiology through the use of anticoagulants may exacerbate the problem in adults. Thus, in COVID-19 infection, we propose the use of antiplatelet (thromboxane A2 inhibitors), if required rather than anticoagulants (FXa and thrombin Inhibitors).
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