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Article ; Online: Synergistic induction of apoptosis in lung cancer cells through co-delivery of PLGA phytol/α-bisabolol nanoparticles.

Kiruthiga, Chandramohan / Balan, Devasahayam Jaya / Prasath, Nagaiah Hari / Manikandakrishnan, Muthushanmugam / Jafni, Sakthivel / Prabhu, Narayanasamy Marimuthu / Pandian, Shunmugiah Karutha / Devi, Kasi Pandima

Naunyn-Schmiedeberg's archives of pharmacology

2024

Abstract: This study explored the potential of poly-(lactic-co-glycolic) acid (PLGA) nanoparticles to enhance the effectiveness of anticancer treatments through combination therapy with phytol and α-bisabolol. The encapsulation efficiency of the nanoparticles was ... ...

Abstract	This study explored the potential of poly-(lactic-co-glycolic) acid (PLGA) nanoparticles to enhance the effectiveness of anticancer treatments through combination therapy with phytol and α-bisabolol. The encapsulation efficiency of the nanoparticles was investigated, highlighting the role of ionic interactions between the drugs and the polymer. Characterization of PLGA-Phy+Bis nanoparticles was carried out using DLS with zeta potential and HR-TEM for size determination. Spectrophotometric measurements evaluated the encapsulation efficiency, loading efficiency, and in vitro drug release. FTIR analysis assessed the chemical interactions between PLGA and the drug actives, ensuring nanoparticle stability. GC-MS was employed to analyze the chemical composition of drug-loaded PLGA nanocarriers. Cytotoxicity was evaluated via the MTT assay, while Annexin V-FITC/PI staining and western blot analysis confirmed apoptotic cell death. Additionally, toxicity tests were performed on L-132 cells and in vivo zebrafish embryos. The study demonstrates high encapsulation efficiency of PLGA-Phy+Bis nanoparticles, which exhibit monodispersity and sizes of 189.3±5nm (DLS) and 268±54 nm (HR-TEM). Spectrophotometric analysis confirmed efficient drug encapsulation and release control. FTIR analysis revealed nanoparticle structural stability without chemical interactions. MTT assay results demonstrated the promising anticancer potential of all the three nanoparticle types (PLGA-Phy, PLGA-Bis, and PLGA-Phy+Bis) against lung cancer cells. Apoptosis was confirmed through Annexin V-FITC/PI staining and western blot analysis, which also revealed changes in Bax and Bcl-2 protein expression. Furthermore, the nanoparticles exhibited non-toxicity in L-132 cells and zebrafish embryo toxicity tests. PLGA-Phy+Bis nanoparticles exhibited efficient encapsulation, controlled release, and low toxicity. Apoptosis induction in A549 cells and non-toxicity in healthy cells highlight their clinical potential.
Language	English
Publishing date	2024-01-19
Publishing country	Germany
Document type	Journal Article
ZDB-ID	121471-8
ISSN	1432-1912 ; 0028-1298
ISSN (online)	1432-1912
ISSN	0028-1298
DOI	10.1007/s00210-023-02935-2
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Article: Chitosan based encapsulation increased the apoptotic efficacy of thymol on A549 cells and exhibited non toxic response in swiss albino mice

Balan, Devasahayam Jaya / Das, Mamali / Sathya, Sethuraman / Kiruthiga, Chandramohan / Jeyakumar, Mahalingam / Antoniraj, Mariya Gover / Devi, Kasi Pandima

International journal of biological macromolecules. 2022 Mar. 31, v. 202

2022

Abstract: Thymol is a plant-derived natural phenolic compound abundantly present in Thymus vulgaris species. In the present study, we developed a chitosan-based drug delivery system to deliver thymol to A549 cells. The physicochemical properties of thymol-loaded ... ...

Abstract	Thymol is a plant-derived natural phenolic compound abundantly present in Thymus vulgaris species. In the present study, we developed a chitosan-based drug delivery system to deliver thymol to A549 cells. The physicochemical properties of thymol-loaded chitosan nanoparticles (thymol-NP) were characterized using polyphasic techniques viz., FTIR, XRD, DLS, and SEM. Thymol-NP exhibited a size of 282.5 nm and encapsulation efficiency of 74.08 ± 0.73%. The IC₅₀ of thymol-NP against A549 cells was 99.57 μg/ml at 24 h, which was lower than that of the pure form. Clear apoptotic features such as cellular morphology, cell shrinkage, and augmentation of dead cells were observed in both the thymol and thymol-NP treated A549 cells. The percentage of apoptotic cells in the thymol-NP IC₅₀ treated cells was >90% which was considerably higher than the group treated with thymol alone. In vivo toxicity study showed that the swiss albino mice treated up to a concentration of 1000 mg/kg of thymol-NP neither showed signs of toxicity nor death up to 14 days. Also, no significant influence was observed on behavior, body weight, organ weight, and organ histology. Overall, the data concluded that thymol-NP can be considered a safe and potent drug candidate against A549 cells.
Keywords	Thymus vulgaris ; albino ; apoptosis ; chitosan ; death ; drug delivery systems ; drugs ; encapsulation ; histology ; shrinkage ; thymol ; tissue weight ; toxicity
Language	English
Dates of publication	2022-0331
Size	p. 620-631.
Publishing place	Elsevier B.V.
Document type	Article
ZDB-ID	282732-3
ISSN	1879-0003 ; 0141-8130
ISSN (online)	1879-0003
ISSN	0141-8130
DOI	10.1016/j.ijbiomac.2022.01.093
Database	NAL-Catalogue (AGRICOLA)

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Zs.B 2374: Show issues

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Article ; Online: Chitosan based encapsulation increased the apoptotic efficacy of thymol on A549 cells and exhibited non toxic response in swiss albino mice.

Balan, Devasahayam Jaya / Das, Mamali / Sathya, Sethuraman / Kiruthiga, Chandramohan / Jeyakumar, Mahalingam / Antoniraj, Mariya Gover / Devi, Kasi Pandima

International journal of biological macromolecules

2022 Volume 202, Page(s) 620–631

Abstract	Thymol is a plant-derived natural phenolic compound abundantly present in Thymus vulgaris species. In the present study, we developed a chitosan-based drug delivery system to deliver thymol to A549 cells. The physicochemical properties of thymol-loaded chitosan nanoparticles (thymol-NP) were characterized using polyphasic techniques viz., FTIR, XRD, DLS, and SEM. Thymol-NP exhibited a size of 282.5 nm and encapsulation efficiency of 74.08 ± 0.73%. The IC
MeSH term(s)	A549 Cells ; Animals ; Chitosan/chemistry ; Drug Delivery Systems ; Humans ; Mice ; Nanoparticles/chemistry ; Thymol/chemistry ; Thymol/pharmacology
Chemical Substances	Thymol (3J50XA376E) ; Chitosan (9012-76-4)
Language	English
Publishing date	2022-01-20
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	282732-3
ISSN	1879-0003 ; 0141-8130
ISSN (online)	1879-0003
ISSN	0141-8130
DOI	10.1016/j.ijbiomac.2022.01.093
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Article: α-bisabolol β-D-fucopyranoside inhibits β-amyloid (Aβ)25-35 induced oxidative stress in Neuro-2a cells via antioxidant approaches

Jeyakumar, Mahalingam / Sathya, Sethuraman / Gandhi, Soniya / Tharra, Prabhakararao / Aarthy, Murali / Balan, Devasahayam Jaya / Kiruthiga, Chandramohan / Baire, Beeraiah / Singh, Sanjeev Kumar / Devi, Kasi Pandima

Process biochemistry. 2022 July 23,

2022

Abstract: β-amyloid (Aβ)₂₅₋₃₅ peptide-induced oxidative stress is one of the primary reasons for the development of Alzheimer’s disease (AD). In the present study, α-bisabolol β-D-fucopyranoside (ABFP) was evaluated for its protective effect against β-amyloid (Aβ)₂ ...

Abstract	β-amyloid (Aβ)₂₅₋₃₅ peptide-induced oxidative stress is one of the primary reasons for the development of Alzheimer’s disease (AD). In the present study, α-bisabolol β-D-fucopyranoside (ABFP) was evaluated for its protective effect against β-amyloid (Aβ)₂₅₋₃₅ peptide-induced toxicity in Neuro-2a cells. The results of the current study revealed that ABFP inhibits acetylcholinesterase, apart from reducing the formation of lipid peroxides, protein carbonyls, and nitric oxides in Neuro-2a cells during the treatment of β-amyloid (Aβ)₂₅₋₃₅ peptide. Additionally, ABFP effectively prevented the mitochondrial membrane damage induced by the β-amyloid (Aβ)₂₅₋₃₅ peptide in Neuro-2a cells. Furthermore, ABFP was found to significantly inhibit caspase 3 production in Neuro-2a cells, which was confirmed through AO/EtBr, Annexin-V/FITC, and PI fluorescent microscopic images, indicating that ABFP has anti-apoptotic properties. In addition, ABFP also increased the anti-apoptotic protein expression and protected the Neuro-2a cell from β-amyloid (Aβ)₂₅₋₃₅ peptide-induced toxicity. The in silico molecular docking analysis of ABFP with GSK-3beta showed that it was able to bind with Asn 186, Asp 200, and Lys 183 residues of the enzyme. Overall, the results suggest that ABFP acts as a potent drug against oxidative stress-mediated cell death in AD.
Keywords	acetylcholinesterase ; caspase-3 ; cell death ; computer simulation ; drugs ; fluorescence ; mitochondrial membrane ; oxidative stress ; pro-apoptotic proteins ; protective effect ; protein synthesis ; toxicity
Language	English
Dates of publication	2022-0723
Publishing place	Elsevier Ltd
Document type	Article
Note	Pre-press version
ISSN	1359-5113
DOI	10.1016/j.procbio.2022.07.026
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Short interfering RNA in colorectal cancer: is it wise to shoot the messenger?

Chandramohan, Kiruthiga / Balan, Devasahayam Jaya / Devi, Kasi Pandima / Nabavi, Seyed Fazel / Reshadat, Sara / Khayatkashani, Maryam / Mahmoodifar, Sepideh / Filosa, Rosanna / Amirkhalili, Niloufar / Pishvaei, Soroush / Sargazi-Aval, Omolbanin / Nabavi, Seyed Mohammad

European journal of pharmacology

2023 Volume 949, Page(s) 175699

Abstract: Colorectal cancer (CRC) is the third most common cancer and the leading cause of gastrointestinal cancer death. 90% of people diagnosed with colorectal cancer are over the age of 50; nevertheless, the illness is more aggressive among those detected at a ... ...

Abstract	Colorectal cancer (CRC) is the third most common cancer and the leading cause of gastrointestinal cancer death. 90% of people diagnosed with colorectal cancer are over the age of 50; nevertheless, the illness is more aggressive among those detected at a younger age. Chemotherapy-based treatment has several adverse effects on both normal and malignant cells. The primary signaling pathways implicated in the advancement of CRC include hedgehog (Hh), janus kinase and signal transducer and activator of transcription (JAK/STAT), Wingless-related integration site (Wnt)/β-catenin, transforming growth factor-β (TNF-β), epidermal growth factor receptor (EGFR)/Mitogen-activated protein kinases (MAPK), phosphoinositide 3-kinase (PI3K), nuclear factor kappa B (NF-κB), and Notch. Loss of heterozygosity in tumor suppressor genes like adenomatous polyposis coli, as well as mutation or deletion of genes like p53 and Kirsten rat sarcoma viral oncogene (KRAS), are all responsible for the occurrence of CRC. Novel therapeutic targets linked to these signal-transduction cascades have been identified as a consequence of advances in small interfering RNA (siRNA) treatments. This study focuses on many innovative siRNA therapies and methodologies for delivering siRNA therapeutics to the malignant site safely and effectively for the treatment of CRC. Treatment of CRC using siRNA-associated nanoparticles (NPs) may inhibit the activity of oncogenes and MDR-related genes by targeting a range of signaling mechanisms. This study summarizes several siRNAs targeting signaling molecules, as well as the therapeutic approaches that might be employed to treat CRC in the future.
MeSH term(s)	Humans ; RNA, Small Interfering/genetics ; Phosphatidylinositol 3-Kinases/metabolism ; Hedgehog Proteins ; Signal Transduction ; ErbB Receptors/metabolism ; Colorectal Neoplasms/drug therapy ; Colorectal Neoplasms/genetics
Chemical Substances	RNA, Small Interfering ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; Hedgehog Proteins ; ErbB Receptors (EC 2.7.10.1)
Language	English
Publishing date	2023-04-01
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	80121-5
ISSN	1879-0712 ; 0014-2999
ISSN (online)	1879-0712
ISSN	0014-2999
DOI	10.1016/j.ejphar.2023.175699
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Article: Thymol induces mitochondrial pathway-mediated apoptosis via ROS generation, macromolecular damage and SOD diminution in A549 cells.

Balan, Devasahayam Jaya / Rajavel, Tamilselvam / Das, Mamali / Sathya, Sethuraman / Jeyakumar, Mahalingam / Devi, Kasi Pandima

Pharmacological reports : PR

2020 Volume 73, Issue 1, Page(s) 240–254

Abstract: Background: Thymol is a monoterpene phenol found in thyme species plants. The present study was carried out to investigate the effect of thymol and its molecular mechanism on non-small lung cancer (A549) cells.: Methods: The cytotoxic effect of ... ...

Abstract	Background: Thymol is a monoterpene phenol found in thyme species plants. The present study was carried out to investigate the effect of thymol and its molecular mechanism on non-small lung cancer (A549) cells. Methods: The cytotoxic effect of thymol on A549 cells was assessed via MTT assay. ROS production, macromolecular damage, apoptosis were determined using DCF-DA, PI, AO/EtBr stains, respectively. ROS-dependent effect of thymol was confirmed using NAC. The expression of caspase-9, Bcl-2, Bax and cell cycle profile was analyzed via western blot and FACS, respectively. Results: The antiproliferative effect of thymol on A549 cells was found to be both dose and time dependent with IC Conclusion: Overall, our results confirmed that thymol can act as a safe and potent therapeutic agent to treat NSCLC.
MeSH term(s)	A549 Cells ; Acetylcysteine/pharmacology ; Antineoplastic Agents, Phytogenic/pharmacology ; Apoptosis/drug effects ; Caspase 9/drug effects ; Caspase 9/metabolism ; Cell Cycle/drug effects ; Computer Simulation ; DNA Damage ; Genes, bcl-2/drug effects ; Humans ; Membrane Potential, Mitochondrial/drug effects ; Mitochondria/drug effects ; Reactive Oxygen Species/metabolism ; Signal Transduction/drug effects ; Superoxide Dismutase/metabolism ; Thymol/antagonists & inhibitors ; Thymol/pharmacology ; bcl-2-Associated X Protein/drug effects ; bcl-2-Associated X Protein/metabolism
Chemical Substances	Antineoplastic Agents, Phytogenic ; BAX protein, human ; Reactive Oxygen Species ; bcl-2-Associated X Protein ; Thymol (3J50XA376E) ; Superoxide Dismutase (EC 1.15.1.1) ; CASP9 protein, human (EC 3.4.22.-) ; Caspase 9 (EC 3.4.22.-) ; Acetylcysteine (WYQ7N0BPYC)
Language	English
Publishing date	2020-10-23
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2186248-5
ISSN	1734-1140
ISSN	1734-1140
DOI	10.1007/s43440-020-00171-6
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Article ; Online: Targeting STATs in neuroinflammation: The road less traveled!

Pharmacological research

2018 Volume 141, Page(s) 73–84

Abstract: JAK/STAT transduction pathway is a highly conserved pathway implicated in regulating cellular proliferation, differentiation, survival and apoptosis. Dysregulation of this pathway is involved in the onset of autoimmune, haematological, oncological, ... ...

Abstract	JAK/STAT transduction pathway is a highly conserved pathway implicated in regulating cellular proliferation, differentiation, survival and apoptosis. Dysregulation of this pathway is involved in the onset of autoimmune, haematological, oncological, metabolic and neurological diseases. Over the last few years, the research of anti-neuroinflammatory agents has gained considerable attention. The ability to diminish the STAT-induced transcription of inflammatory genes is documented for both natural compounds (such as polyphenols) and chemical drugs. Among polyphenols, quercetin and curcumin directly inhibit STAT, while Berberis vulgaris L. and Sophora alopecuroides L extracts act indirectly. Also, the Food and Drug Administration has approved several JAK/STAT inhibitors (direct or indirect) for treating inflammatory diseases, indicating STAT can be considered as a therapeutic target for neuroinflammatory pathologies. Considering the encouraging data obtained so far, clinical trials are warranted to demonstrate the effectiveness and potential use in the clinical practice of STAT inhibitors to treat inflammation-associated neurodegenerative pathologies.
MeSH term(s)	Animals ; Anti-Inflammatory Agents/pharmacology ; Anti-Inflammatory Agents/therapeutic use ; Humans ; Inflammation/drug therapy ; Inflammation/metabolism ; Nervous System Diseases/drug therapy ; Nervous System Diseases/metabolism ; Polyphenols/pharmacology ; Polyphenols/therapeutic use ; STAT Transcription Factors/antagonists & inhibitors ; STAT Transcription Factors/chemistry ; STAT Transcription Factors/metabolism
Chemical Substances	Anti-Inflammatory Agents ; Polyphenols ; STAT Transcription Factors
Language	English
Publishing date	2018-12-11
Publishing country	Netherlands
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	1003347-6
ISSN	1096-1186 ; 0031-6989 ; 1043-6618
ISSN (online)	1096-1186
ISSN	0031-6989 ; 1043-6618
DOI	10.1016/j.phrs.2018.12.004
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Article ; Online: Synergistic induction of apoptosis in lung cancer cells through co-delivery of PLGA phytol/α-bisabolol nanoparticles.

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Article: Chitosan based encapsulation increased the apoptotic efficacy of thymol on A549 cells and exhibited non toxic response in swiss albino mice

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Article ; Online: Chitosan based encapsulation increased the apoptotic efficacy of thymol on A549 cells and exhibited non toxic response in swiss albino mice.

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Article: α-bisabolol β-D-fucopyranoside inhibits β-amyloid (Aβ)25-35 induced oxidative stress in Neuro-2a cells via antioxidant approaches

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Article ; Online: Short interfering RNA in colorectal cancer: is it wise to shoot the messenger?

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Article: Thymol induces mitochondrial pathway-mediated apoptosis via ROS generation, macromolecular damage and SOD diminution in A549 cells.

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Article ; Online: Targeting STATs in neuroinflammation: The road less traveled!

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