Papers by Rajkumar Banerjee
Cell Biology International
Journal of Photochemistry and Photobiology B: Biology
ACS Applied Materials & Interfaces, 2022
Long-term application of topical therapeutics for psoriasis has a plethora of side effects. Addit... more Long-term application of topical therapeutics for psoriasis has a plethora of side effects. Additionally, skin-permeating agents used in their formulations for deeper dermal delivery damage the skin. To address these limitations, we developed novel lithocholic acid analogues that could form lipid nanoparticles (nano-LCs) spontaneously in the aqueous milieu, permeate through the skin, penetrate the deeper dermal layers, and exert anti-inflammatory effects against psoriasis-like chronic skin inflammations. Prior findings demonstrated that lithocholic acid acts as a vitamin D receptor agonist without affecting the Ca+2 metabolism and also as an antagonist for ephrin type-A receptor 2 (EphA2). Taking cues from the previous findings, lithocholic acid derivatives with twin alkyl chains (LC6, LC8, LC10, and LC-12) were synthesized, nanoparticles (nano-LCs) were prepared, and they were evaluated for their skin permeability and anti-inflammatory properties. Among these nano-LCs, nano-LC10 demonstrated superior anti-inflammatory properties and inhibition of keratinocyte proliferation in various cell-based evaluations. Furthermore, the therapeutic efficiency of nano-LC10 was evaluated in an imiquimod-induced psoriasis-like mouse model and demonstrated comparable efficiency with the standard topical formulation, Sorvate, in reducing skin inflammations. Nano-LC10 also reduced systemic inflammation, organ toxicity, and also proinflammatory serum cytokine levels. Overall, nano-lithocholic lipidoid (nano-LC10) can be a potential novel class of therapeutics for topical application in treating psoriasis.
Handbook of Oxidative Stress in Cancer: Mechanistic Aspects, 2021
Breast cancer (BC) remains one of the deadliest and most frequently diagnosed metastatic cancers ... more Breast cancer (BC) remains one of the deadliest and most frequently diagnosed metastatic cancers worldwide. Cancer stem cells (CSCs) are the cell population within the tumour niche, having an epithelial to mesenchymal (EMT) transition phenotype, high self-renewal, and vigorous metastatic capacity, drug resistance, and ultimate cause of tumour relapse in patients. Identification of targets for apoptosis induction is essential to provide novel therapeutic approaches in breast cancer. Our earlier studies showed that Vitamin C induces apoptotic cell death by losing redox balance in TNBC CSCs. In this current study, we have made an attempt to identify previously unrecognized CSC survival factor/factors that can be used as druggable targets for bCSCs apoptosis regulators isolated from the triple negative breast cancer cell line: MDA MB 468. A thorough literature review was carried out to identify candidates, and Oct-4 was identified as the most promising marker for its unique abundance in...
WIREs Nanomedicine and Nanobiotechnology, 2021
The steroid hormone receptors (SHRs) among nuclear hormone receptors (NHRs) are steroid ligand‐de... more The steroid hormone receptors (SHRs) among nuclear hormone receptors (NHRs) are steroid ligand‐dependent transcription factors that play important roles in the regulation of transcription of genes promoted via hormone responsive elements in our genome. Aberrant expression patterns and context‐specific regulation of these receptors in cancer, have been routinely reported by multiple research groups. These gave an window of opportunity to target those receptors in the context of developing novel, targeted anticancer therapeutics. Besides the development of a plethora of SHR‐targeting synthetic ligands and the availability of their natural, hormonal ligands, development of many SHR‐targeted, anticancer nano‐delivery systems and theranostics, especially based on small molecules, have been reported. It is intriguing to realize that these cytoplasmic receptors have become a hot target for cancer selective delivery. This is in spite of the fact that these receptors do not fall in the categ...
Nanomedicine, 2021
Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer ef... more Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of pancreatic tumor progression, significantly greater in vivo absorption, approximately 1.5-fold higher plasma concentration, higher bioavailability, reduced volume of distribution and improved clearance relative to TQ. Conclusion: Encapsulation of TQ in cationic liposomal formulation enhanced its bioavailability and anticancer efficacy against xenograft pancreatic tumor.
Hydrocortisone, a natural glucocorticoid secreted by adrenal and extra-adrenal tissues, locally g... more Hydrocortisone, a natural glucocorticoid secreted by adrenal and extra-adrenal tissues, locally governs the transcription of genes involved in inflammation, immune response, metabolism, and energy homeostasis via binding to its cognate glucocorticoid receptor (GR). In this study, we show that modified hydrocortisone (HC16), a cancer-selective cytotoxic molecule, showed synergism in combination with drugs like Doxorubicin and docetaxel, self-assembled into vesicles, entrapped docetaxel and complexed with anti-cancer plasmid DNA for enhanced killing of cancer cells. These vesicles exhibited GR-mediated nuclear localization, delivery of the p53 gene, and also inhibited cell viability selectively in RKO, HCT15, and CT26 colon cancer cells but not in normal cells like CHO and HEK293T. Apart from exerting its own anti-cancer activity, the self-assembled HC16 vesicles loaded with docetaxel sensitized the cancer cells to its drug cargo by downregulating the drug metabolizing CYP3A4 gene. This indirectly reduces the risk of nonspecific adverse effects in normal cells, as the viability of sensitized cancer cells could be significantly reduced even in low doses of cytotoxic docetaxel. The near infrared (NIR)-dye-associated self-assemblies accumulated in a colon tumor with higher orders of NIR intensity compared to those in a colon of healthy mice. Thereafter, the treatment of HC16-docetaxel-p53 vesicle/DNA complex led to significant tumor regression, which resulted in a cecum/body weight ratio in tumor-bearing mice similar to that of healthy mice measured at 24 h postcompletion of treatment. There was an up to 2.5-fold enhancement in the overall survivability of colon-tumor-bearing mice treated with HC16-docetaxel-p53 vesicle/DNA complexes when compared against the pristine docetaxel-treated groups. Further, the HC16-docetaxel-p53 vesicle/DNA complex-treated group showed reduced nuclear accumulation of cell proliferation marker Ki67, reduced protein levels of prosurvival and mesenchymal proteins like Bcl-2, PARP, vimentin, and N-cadherin, and increased the levels of pro-apoptotic activated caspases as compared to the pristine docetaxel-treated groups. The therapeutic package described herein is expected to find future use as a rational, multifaceted, GR-targeted approach for inhibiting colon tumor progression.
Journal of Materials Chemistry B, 2020
BBB-crossing amphetamine decorated cationic lipid nanoparticle co-loaded with paclitaxel and PDL-... more BBB-crossing amphetamine decorated cationic lipid nanoparticle co-loaded with paclitaxel and PDL-1 siRNA enhances survivability of orthotopic glioblastoma bearing mice.
Bioorganic Chemistry, 2020
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Nanoscale Advances, 2019
A carbon nanosphere-based dual strategy to target tumor-associated macrophages and tumor cells in... more A carbon nanosphere-based dual strategy to target tumor-associated macrophages and tumor cells in glioma lesions within the brain.
Journal of Molecular Structure, 2019
Synthesis of 4,6-disubstituted pyrazolo[3,4-d]pyrimidine analogues: Cyclindependent kinase 2 (CDK... more Synthesis of 4,6-disubstituted pyrazolo[3,4-d]pyrimidine analogues: Cyclindependent kinase 2 (CDK2) inhibition, molecular docking and anticancer evaluation
Journal of drug targeting
Function of steroid hormone oestrogen that transactivates oestrogen receptor (ER) is expressed in... more Function of steroid hormone oestrogen that transactivates oestrogen receptor (ER) is expressed in multiple organs. Except for malignancies of gynaecological organs, ER remains largely unutilised as a target to treat cancers of ER-expressing brain, prostate, skin etc. We have previously developed oestrogen targeting cationic lipid molecule (ES-C10), which showed targeted killing of ER + breast and skin cancer cells. In this study, we explored the targeting ability of ES-C10 as a ligand as well as its additive killing effect (if any), when incorporated in two different liposomes (DCME and DCDE), carrying two anticancer molecules MCIS3 and Docetaxel™, respectively. DCME and DCDE exhibited higher cytotoxicity in ER + cancer cells than in ER - cancer or in non-cancer cells. Both liposomes induced ER-mediated cytotoxicity and caspase 3-induced apoptosis in ER + melanoma cells. Further, decreased levels of pAkt, and increased levels of PTEN and p53 were also observed. Both the targeted lip...
Molecular and cellular biochemistry, Jan 5, 2017
Glucocorticoid, such as dexamethasone (Dex) is often used along with chemotherapy to antagonize s... more Glucocorticoid, such as dexamethasone (Dex) is often used along with chemotherapy to antagonize side effects of chemotherapy. However, sustained use of Dex frequently develops drug resistance in patients. As a strategy to re-induce drug sensitivity, we planned to modify Dex by chemically conjugating it with twin ten carbon aliphatic chain containing cationic lipid. The resultant molecule, DX10, inhibited STAT3 activation through lowering the production of IL-6. To enhance the STAT3 inhibitory effect of DX10, we used WP (a commercially available STAT3 inhibitor) along with DX10. Combination treatment of both significantly inhibited STAT3 activation when compared to either of the individual treatment. The effect of DX10, either in combination or alone, was mediated through glucocorticoid receptor (GR), thereby repurposing the role of GR in the context of p-STAT3 inhibition-mediated cancer treatment. Cellular viability study proved the synergistic effect of WP and DX10. Further, combin...
Nanomedicine, 2016
Aim: To explore the potential of glucocorticoid receptor-targeted nano-gold formulation as antitu... more Aim: To explore the potential of glucocorticoid receptor-targeted nano-gold formulation as antitumor drug sensitizing agent. Materials & methods: Simultaneous conjugation of gold nanoparticle with thiol-modified dexamethasone, a synthetic glucocorticoid and anticancer drug withaferin A afforded stable gold nanoparticle-modifed dexamethasone-withaferin A nanoconjugate. Results: This metallic nanoparticle formulation showed glucocorticoid receptor-dependent cancer cell selective cytotoxicity, inhibited growth of aggressive mouse melanoma tumor, reduced mice mortality, while reversing epithelial-to-mesenchymal transition in tumor cells. Same treatment also leads to near-complete downregulation of ABCG2 drug transporter in tumor-associated cells thus attributing it to its drug sensitizing ability. Conclusion: The presently synthesized nanoconjugate holds a great promise to sensitize cancer cells to chemotherapeutics and induce epithelial-to-mesenchymal transition reversal in tumor cells...
RSC Advances, 2016
Cationic lipids have been extensively studied for their ability to complex with nucleic acids to ... more Cationic lipids have been extensively studied for their ability to complex with nucleic acids to condense and consequently deliver them into the cells.
Data in Brief, 2016
A detailed description of steroid hormone ligand containing liposomes and their stability has bee... more A detailed description of steroid hormone ligand containing liposomes and their stability has been given. Liposomes were complexed with β-gal DNA and used to transfect cancer and noncancer cells. The stability of the liposomes and lipoplexes were analysed using dynamic light scattering and DNA-binding gel images. The formulations were used to assess the delivery of anticancer gene, p53 in cancer cells. The dataset consists of DNAbinding gel images, transfection, cytotoxicity and reverse transcriptase PCR images.
Molecular Cell, 2015
Highlights d Mycobacterial biofilm contains physiologically diverse microenvironments d Hypoxia i... more Highlights d Mycobacterial biofilm contains physiologically diverse microenvironments d Hypoxia induces expression of the alternate electron carrier polyketide quinones d PkQs are produced by type III polyketide synthases using fatty acyl-CoA precursors d PkQs maintain cellular bioenergetics in oxygen-deficient niches
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Papers by Rajkumar Banerjee