Displaying publications 21 - 40 of 296 in total

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  1. Chellappan DK, Yenese Y, Wei CC, Chellian J, Gupta G
    J Environ Pathol Toxicol Oncol, 2017;36(4):283-291.
    PMID: 29431061 DOI: 10.1615/JEnvironPatholToxicolOncol.2017020182
    Oral delivery of insulin is one of the most promising and anticipated areas in the treatment of diabetes, primarily because it may significantly improve the quality of life of diabetics who receive insulin regularly. Several problems have been reported regarding the subcutaneous delivery of insulin, ranging from cardiovascular complications to weight gain. One of the approaches to overcoming these issues is to administer insulin through the oral route. However, there are several challenges in developing an oral route for insulin delivery; insulin has extremely poor bioavailability and a low diffusion rate through the mucus layer. A wide range of oral insulin delivery techniques have recently been researched, ranging from nanoparticles to liposomes, self-emulsifying systems, and hydrogels. These techniques have shown promising potential in the oral delivery of insulin. This review considers the current literature on the advances and challenges in the development of oral insulin.
  2. Madhu A, Gupta G, Arali B, Chellappan DK, Dua K
    Recent Pat Drug Deliv Formul, 2017;11(1):36-41.
    PMID: 27993107 DOI: 10.2174/1872211310666161216111515
    AIMS AND BACKGROUND: Psychosis is a neurological disorder, which is usually defined as the "loss of contact with reality." As medicine 'Hemidesmusindicus' holds a reputed place in all systems of medicine in India. It is given in the form of infusion, fine particles, or syrup. It is also a component of several medicinal preparations. The present research work is pertaining to find out an anti-psychotic activity of an aqueous root extract of Hemidesmusindicus- a time bound study in rats.

    METHODS: In the present study, the dried roots of Hemidesmusindicus were crushed to a coarse powder and extracted with water under reflux for 36 hours to obtain the aqueous extract of roots of Hemidesmusindicus (AERHI). The extract was reconstituted in 2% aqueous tragacanth just before use and administered orally at a dose 0f 100 mg/kg, 300 mg/kg and 500 mg/kg. In a single dose study, the parameters were assessed after oral administration of the single dose of the AERHI, whereas in a multiple dose study, the animals daily received the suitable oral dose of the AERHI for a period of 30 days. The parameters were assessed on the 15th and 30th day. The antipsychotic activity was screened using Apomorphine induced Stereotyped behavior in rats and Haloperidol induced catalepsy models were used. In Apomorphine induced Stereotyped behavior inhibition of the Stereotyped behavior was considered to be anti-psychotic activity and in Haloperidol induced catalepsy, we observed whether the AERHI potentate or attenuate the catalepsy in rats.

    RESULTS: In this study, the extract of Hemidesmusindicus significantly inhibited the stereotyped behavior induced by apomorphine in rats and also potentiate the catalepsy induced by haloperidol, thereby showing its anti-psychotic activity.

    CONCLUSION: All these observations imply that Hemidesmusindicus extract possesses anti-psychotic activity in experimental animals.

  3. Rana S, Kumar A, Lai CW, Sharma G, Dhiman P
    Chemosphere, 2024 May;356:141800.
    PMID: 38554860 DOI: 10.1016/j.chemosphere.2024.141800
    In pursuit of advancing photocatalysts for superior performance in water treatment and clean energy generation, researchers are increasingly focusing on layered double hydroxides (LDHs) which have garnered significant attention due to their customizable properties, morphologies, distinctive 2D layered structure and flexible options for modifying anions and cations. No review has previously delved specifically into ZnCr and NiCr LDH-based photocatalysts and therefore, this review highlights the recent surge in ZnCr and NiCr-based LDHs as potential photocatalysts for their applications in water purification and renewable energy generation. The structural and fundamental characteristics of layered double hydroxides and especially ZnCr-LDHs and NiCr-LDHs are outlined. Further, the various synthesis techniques for the preparation of ZnCr-LDHs, NiCr-LDHs and their composite and heterostructure materials have been briefly discussed. The applicability of ZnCr-LDH and NiCr-LDH based photocatalysts in tackling significant issues in water treatment and sustainable energy generation is the main emphasis of this review. It focuses on photocatalytic degradation of organic pollutants in wastewater, elucidating the principles and advancements for enhancing the efficiency of these materials. It also explores their role in H2 production through water splitting, conversion of CO2 into valuable fuels and NH3 synthesis from N2, shedding light on their potential for clean energy solutions. The insights presented herein offer valuable guidance for researchers working towards sustainable solutions for environmental remediation and renewable energy generation.
  4. Bin LK, Helaluddin ABM, Islam Sarker MZ, Mandal UK, Gaurav A
    Pak J Pharm Sci, 2020 Mar;33(2):551-559.
    PMID: 32276897
    Orally disintegrating tablet (ODT) is a friendly dosage form that requires no access to water and serves as a solution to non-compliance. There are many co-processed adjuvants available in the market. However, there is no single product possesses all the ideal characteristics such as good compressibility, fast disintegration and good palatability for ODT application. The aim of this research was to produce a xylitol-starch base co-processed adjuvant which is suitable for ODT application. Two processing methods namely wet granulation and freeze drying were used to compare the characteristics of co-processed adjuvant comprising of xylitol, starch and crospovidone XL-10 mixed at various ratios. The co-processed excipients were compressed into ODT and physically characterized for powder flow, particle size, hardness, thickness, weight, friability, in-vitro disintegration time and in-situ disintegration time, lubricant sensitivity, dilution potential, Fourier transform infrared spectroscopy, scanning electronic microscopy and x-ray diffraction analysis. Formulation F6 was selected as the optimum formulation due to the fastest in-vitro (135.33±11.52 s) and in-situ disintegration time (88.67±13.56s) among all the formulations (p<0.05). Increase in starch component decreases disintegration time of ODT. The powder flow fell under the category of fair flow. Generally, it was observed that freeze drying method produced smaller particle size granules compared to wet granulation method. ODT produced from freeze drying method had shorter disintegration time compared to ODT from wet granulation batch. In conclusion, a novel co-processed excipient comprised of xylitol, starch and crospovidone XL-10, produced using freeze drying method with fast disintegration time, good compressibility and palatability was developed and characterized. The co-processed excipient is suitable for ODT application.
  5. Awasthi R, Singh AK, Mishra G, Maurya A, Chellappan DK, Gupta G, et al.
    Adv Exp Med Biol, 2018 9 28;1087:3-14.
    PMID: 30259353 DOI: 10.1007/978-981-13-1426-1_1
    Circular RNAs (cirRNAs) are long, noncoding endogenous RNA molecules and covalently closed continuous loop without 5'-3' polarity and polyadenylated tail which are largely concentrated in the nucleus. CirRNA regulates gene expression by modulating microRNAs and functions as potential biomarker. CirRNAs can translate in vivo to link between their expression and disease. They are resistant to RNA exonuclease and can convert to the linear RNA by microRNA which can then act as competitor to endogenous RNA. This chapter summarizes the evolutionary conservation and expression of cirRNAs, their identification, highlighting various computational approaches on cirRNA, and translation with a focus on the breakthroughs and the challenges in this new field.
  6. Kara J, Suwanhom P, Wattanapiromsakul C, Nualnoi T, Puripattanavong J, Khongkow P, et al.
    Arch Pharm (Weinheim), 2019 Jul;352(7):e1800310.
    PMID: 31125474 DOI: 10.1002/ardp.201800310
    Sixteen novel coumarin-based compounds are reported as potent acetylcholinesterase (AChE) inhibitors. The most active compound in this series, 5a (IC50 0.04 ± 0.01 µM), noncompetitively inhibited AChE with a higher potency than tacrine and galantamine. Compounds 5d, 5j, and 5 m showed a moderate antilipid peroxidation activity. The compounds showed cytotoxicity in the same range as the standard drugs in HEK-293 cells. Molecular docking demonstrated that 5a acted as a dual binding site inhibitor. The coumarin moiety occupied the peripheral anionic site and showed π-π interaction with Trp278. The tertiary amino group displayed significant cation-π interaction with Phe329. The aromatic group showed π-π interaction with Trp83 at the catalytic anionic site. The long chain of methylene lay along the gorge interacting with Phe330 via hydrophobic interaction. Molecular docking was applied to postulate the selectivity toward AChE of 5a in comparison with donepezil and tacrine. Structural insights into the selectivity of the coumarin derivatives toward huAChE were explored by molecular docking and 3D QSAR and molecular dynamics simulation for 20 ns. ADMET analysis suggested that the 2-(2-oxo-2H-chromen-4-yl)acetamides showed a good pharmacokinetic profile and no hepatotoxicity. These coumarin derivatives showed high potential for further development as anti-Alzheimer agents.
  7. Al-Nema M, Gaurav A, Lee MT, Okechukwu P, Nimmanpipug P, Lee VS
    PLoS One, 2022;17(12):e0278216.
    PMID: 36454774 DOI: 10.1371/journal.pone.0278216
    Phosphodiesterase 1B (PDE1B) and PDE10A are dual-specificity PDEs that hydrolyse both cyclic adenosine monophosphate and cyclic guanosine monophosphate, and are highly expressed in the striatum. Several reports have suggested that PDE10A inhibitors may present a promising approach for the treatment of positive symptoms of schizophrenia, whereas PDE1B inhibitors may present a novel mechanism to modulate cognitive deficits. Previously, we have reported a novel dual inhibitor of PDE1B and PDE10A, compound 2 [(3-fluorophenyl)(2-methyl-2,3-dihydro-4H-benzo[b][1,4]oxazin-4-yl)methanone] which has shown inhibitory activity for human recombinant PDE1B and PDE10A in vitro. In the present study, the safety profile of compound 2 has been evaluated in rats in the acute oral toxicity study, as well as; the antipsychotic-like effects in the rat model of schizophrenia. Compound 2 was tolerated up to 1 g/kg when administered at a single oral dose. Additionally, compound 2 has strongly suppressed ketamine-induced hyperlocomotion, which presented a model for the positive symptoms of schizophrenia. It has also shown an ability to attenuate social isolation induced by chronic administration of ketamine and enhanced recognition memory of rats ​in the novel object recognition test. Altogether, our results suggest that compound 2 represents a promising therapy for the treatment of the three symptomatic domains of schizophrenia.
  8. Thakur P, Arivarasan VK, Kumar G, Pant G, Kumar R, Pandit S, et al.
    Appl Biochem Biotechnol, 2024 Jan;196(1):491-505.
    PMID: 37145344 DOI: 10.1007/s12010-023-04550-6
    The current study reports the synthesis of sustainable nano-hydroxyapatite (nHAp) using a wet chemical precipitation approach. The materials used in the green synthesis of nHAp were obtained from environmental biowastes such as HAp from eggshells and pectin from banana peels. The physicochemical characterization of obtained nHAp was carried out using different techniques. For instance, X-ray diffractometer (XRD) and FTIR spectroscopy were used to study the crystallinity and synthesis of nHAp respectively. In addition, the morphology and elemental composition of nHAP were studied using FESEM equipped with EDX. HRTEM showed the internal structure of nHAP and calculated its grain size which was 64 nm. Furthermore, the prepared nHAp was explored for its antibacterial and antibiofilm activity which has received less attention previously. The obtained results showed the potential of pectin-bound nHAp as an antibacterial agent for various biomedical and healthcare applications.
  9. Nwabueze OP, Sharma M, Balachandran A, Gaurav A, Abdul Rani AN, Małgorzata J, et al.
    Pharmaceuticals (Basel), 2022 Oct 25;15(11).
    PMID: 36355489 DOI: 10.3390/ph15111317
    (1) Insulin resistance, a symptom of type 2 diabetes mellitus (T2DM), is caused by the inactivation of the insulin signaling pathway, which includes IRS-PI3K-IRS-1-PKC-AKT2 and GLUT4. Metformin (biguanide) and glimepiride (sulfonylurea) are both drugs that are derivatives of urea, and they are widely used as first-line drugs for the treatment of type 2 diabetes mellitus. Palmatine has been previously reported to possess antidiabetic and antioxidant properties. (2) The current study compared palmatine to metformin and glimepiride in a type 2 diabetes model for ADME and insulin resistance via the PI3K/Akt/GLUT4 signaling pathway: in vitro, in vivo, ex vivo, and in silico molecular docking. (3) Methods: Differentiated L6 skeletal muscle cells and soleus muscle tissue were incubated in standard tissue culture media supplemented with high insulin and high glucose as a cellular model of insulin resistance, whilst streptozotocin (STZ)-induced Sprague Dawley rats were used as the diabetic model. The cells/tissue/animals were treated with palmatine, while glimepiride and metformin were used as standard drugs. The differential gene expression of PI3K, IRS-1, PKC-α, AKT2, and GLUT4 was evaluated using qPCR. (4) Results: The results revealed that the genes IRS-PI3K-IRS-1-PKC-AKT2 were significantly down-regulated, whilst PKC-α was upregulated significantly in both insulin-resistant cells and tissue animals. Interestingly, palmatine-treated cells/tissue/animals were able to reverse these effects. (5) Conclusions: Palmatine appears to have rejuvenated the impaired insulin signaling pathway through upregulation of the gene expression of IRS-1, PI3K, AKT2, and GLUT4 and downregulation of PKC-expression, according to in vitro, in vivo, and ex vivo studies.
  10. Gupta G, Jia Jia T, Yee Woon L, Kumar Chellappan D, Candasamy M, Dua K
    Adv Pharmacol Sci, 2015;2015:164943.
    PMID: 26681936 DOI: 10.1155/2015/164943
    The present study was designed to evaluate the acute and chronic antidepressant effect of genistein in combination with amitriptyline in mice. Animals were divided into six groups (n = 6) for treatment with water, genistein, or amitriptyline, either alone or in combination for ten days. Animals were subjected to locomotor activity testing; tail suspension test (TST); and forced swim test (FST) and immobility time was recorded on day one and day ten. Acute treatment of all treatment groups did not significantly reduce the immobility time (p > 0.05). Chronic treatment of combination of genistein (10 mg/kg) and amitriptyline (5 mg/kg and 10 mg/kg) significantly reduced the immobility time as compared to control group (p < 0.001) and was comparable to amitriptyline alone (10 mg/kg). However, no changes in anti-immobility activity in combination of subeffective doses of genistein (5 mg/kg) and amitriptyline (5 mg/kg) were observed. Genistein at its standard dose (10 mg/kg) rendered synergistic effects in combination with subeffective dose of amitriptyline (5 mg/kg) and additive effects in combination with therapeutic dose of amitriptyline (10 mg/kg).
  11. Candasamy M, Murthy TE, Gubiyappa KS, Chellappan DK, Gupta G
    J Basic Clin Pharm, 2014 Jun;5(3):62-7.
    PMID: 25278668 DOI: 10.4103/0976-0105.139728
    Diabetes mellitus is a syndrome of multiple etiologies. Both type 1 and type 2 diabetes lead to multiple abnormalities of lipid and lipoprotein metabolism. The aim of this investigation was to study the influence of fenofibrate on the blood glucose lowering effect of glibenclamide.
  12. Satija S, Mehta M, Sharma M, Prasher P, Gupta G, Chellappan DK, et al.
    Future Med Chem, 2020 09;12(18):1607-1609.
    PMID: 32589055 DOI: 10.4155/fmc-2020-0149
  13. Singh Y, Gupta G, Kazmi I, Al-Abbasi FA, Negi P, Chellappan DK, et al.
    Dermatol Ther, 2020 11;33(6):e13871.
    PMID: 32558055 DOI: 10.1111/dth.13871
    Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), the primary causative organism in corona virus disease-19 (COVID-19) infections, is a novel member of the human coronavirus family which was first identified in Wuhan, China, towards the end of 2019. This letter reveals new vital missing links in our current understanding of the mechanisms that lead to cell death triggered by ferroptotic stress in COVID-19 infection. It further reveal the importance of homocysteine mediated trans-sulfuration pathway in COVID-19 infection. Hence, Vitamin B6, folic acid, and Vitamin B12 should be incorporated in the treatment regimen for SARS CoV-2 infections to suppress complications, as the virus mediates altered host cell metabolism.
  14. Agarwal G, Pradeep PV, Aggarwal V, Yip CH, Cheung PS
    World J Surg, 2007 May;31(5):1031-40.
    PMID: 17387549
    Breast cancer is the leading cause of cancer-related deaths in Asia, and in recent years is emerging as the commonest female malignancy in the developing Asian countries, overtaking cancer of the uterine cervix. There have been no studies objectively comparing data and facts relating to breast cancer in the developed, newly developed, and developing Asian countries thus far.
  15. Chellappan DK, Yap WS, Bt Ahmad Suhaimi NA, Gupta G, Dua K
    Panminerva Med, 2018 Sep;60(3):117-131.
    PMID: 29696964 DOI: 10.23736/S0031-0808.18.03455-9
    The prevalence of type 2 diabetes mellitus (T2DM) has been increasing at an alarming rate. With an increased understanding of the pathophysiology and pathogenesis of T2DM, various new therapeutic options have been developed to target different key defects in T2DM. Incremental innovations of existing therapies either through unprecedented drug combinations, modified drug molecules, or improved delivery systems are capable to nullify some of the undesirable side effects of traditional therapies as well as to enhance effectiveness. The existing administration routes include inhalation, nasal, buccal, parenteral and oral. Newer drug targets such as protein kinase B (Akt/PKB), AMP-activated protein kinase (AMPK), sirtuin (SIRT), and others are novel approaches that act via different mechanisms and possibly treating T2DM of distinct variations and aetiologies. Other therapies such as endobarrier, gene therapy, and stem cell technology utilize advanced techniques to treat T2DM, and the potential of these therapies are still being explored. Gene therapy is plausible to fix the underlying pathology of T2DM instead of using traditional reactive treatments, especially with the debut of Clustered Regularly Interspaced Short Palindromic Repeats-CRISPR associated protein9 (CRISPR-Cas9) gene editing tool. Molecular targets in T2DM are also being extensively studied as it could target the defects at the molecular level. Furthermore, antibody therapies and vaccinations are also being developed against T2DM; but the ongoing clinical trials are relatively lesser and the developmental progress is slower. Although, there are many therapies designed to cure T2DM, each of them has their own advantages and disadvantages. The preference for the treatment plan usually depends on the health status of the patient and the treatment goal. Therefore, an ideal treatment should take patient's compliance, efficacy, potency, bioavailability, and other pharmacological and non-pharmacological properties into account.
  16. Dua K, Chellappan DK, Singhvi G, de Jesus Andreoli Pinto T, Gupta G, Hansbro PM
    Panminerva Med, 2018 Dec;60(4):230-231.
    PMID: 30563304 DOI: 10.23736/S0031-0808.18.03459-6
  17. Sunkara K, Allam VR, Shukla SD, Chellappan DK, Gupta G, MacLoughlin R, et al.
    EXCLI J, 2021;20:248-251.
    PMID: 33628161 DOI: 10.17179/excli2021-3322
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