2025

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Synthesis, structures, and cytotoxicity insights of organotin(IV) complexes with thiazole-appended pincer ligand
(Elsevier Inc., 2025) Tushar S. Basu Baul; Swmkwr Brahma; Rupen Tamang; Andrew Duthie; Biplob Koch; Sean R. Parkin
Diorganotin complexes of the compositions [Me2Sn(L)] (1), [n-Bu2Sn(L)] (2), [Ph2Sn(L)]⋅C6H6 (3), [Bz2Sn(L)]⋅C6H6 (4) and [n-Oct2Sn(L)] (5) were synthesized by reacting R2SnO (R = Me, n-Bu, Ph, Bz or n-Oct) with the N2,N6-di(thiazol-2-yl)pyridine-2,6-dicarboxamide (H2L, where H2 denotes the two acidic protons) in refluxing toluene. Additionally, the mono-n-butyltin complex [n-BuSn(HL)Cl2]·H2O (6) was synthesized from n-BuSnCl3 and H2L in acetonitrile. Compounds were characterized by FT-IR, 1H, 13C and 119Sn NMR spectroscopy, while their solid-state structures were examined using single-crystal X-ray diffraction studies. In diorganotin compounds 1–5, the dianionic tridentate ligands (Npy, N−, N−) act as κ-N3 chelators. In 6, the L moiety (O, Npy, N−) acts as a κ-ON2 tridentate chelator, with involvement of one of the carboxamide oxygen atoms. The coordination polyhedron around the Sn(IV) ion is completed either by two axial Sn-R ligands in compounds 1–5 or by n-Bu and Cl ligands in compound 6, giving rise to distorted trigonal bipyramid or octahedral structures, respectively. The tin NMR results show that the penta-coordinated structures of compounds 1–5 and the hexacoordinated structure of compound 6, observed in the solid-state, are retained in solution. The in vitro antitumor activities of 1–5 were tested on T-47D breast cancer cells. Of these, diphenyltin compound 3 showed the highest anti-proliferative effect, with an IC50 of 10 ± 1.60 μM. Compound 3 exhibited selective toxicity, potentially inducing apoptosis via reactive oxygen species generation and nuclear changes, indicating promise as a breast cancer treatment. This study is the first to explore thiazole-appended organotin compounds for cytotoxicity. © 2024 Elsevier Inc.
“Sustainable synthesis of Camellia sinensis-mediated silver nanoparticles (CsAgNP) and their anticancer mechanisms in breast cancer cells”
(Elsevier Ltd, 2025) Rupen Tamang; Abhishesh Kumar Mehata; Virendra Pratap Singh; Madaswamy Sona S Muthu; Biplob Koch
The present investigation focuses on synthesizing eco-friendly and cost-effective silver nanoparticles (CsAgNP) utilizing Camellia sinensis ethanolic extract (CsE) as a reducing agent and investigating the potential enhancement in its anticancer efficacy as compared to CsE. The CsAgNP formation was confirmed through the color change from pale green to dark brown and further validated using UV–visible spectroscopy in the 400-450 nm range. The optimal CsAgNP synthesis parameters include 1:4 ratio of CsE: 1 mM AgNO3, 60 min of duration and 50 °C reaction temperature. The morphology and the size of nanoparticles were estimated using AFM, SEM and TEM where the results showed a smooth topography with a size <100 nm. The CsAgNP crystalline form was confirmed through SAED pictures and silver's presence confirmed through EDX analysis. FTIR study ascertained the capping agents and distortion in functional groups compared to CsE. The anticancer potency of CsAgNP and crude extract (CsE) was assessed against the T-47D breast cancer cells by MTT assay. CsAgNP displayed strong activity towards T-47D cells (IC50 8 μg/ml) compared to CsE and relatively low activity towards the normal HEK-293 cells. Further, fluorescence microscopy and flow cytometry data revealed that the CsAgNP promotes apoptosis and also induces G2-M phase cell cycle arrest. Furthermore, CsAgNP treatment decreases p53 and Bcl-2 protein expression, while increasing Bax, Cytochrome c and Caspase-3 levels, indicating mitochondrial-mediated apoptotic pathway activation. Thus, our research aims to investigate the potential of using Camellia sinensis to synthesize CsAgNP, a potent drug delivery system, to enhance anticancer effectiveness and advance cancer therapy in the future. © 2024 Elsevier B.V.
Room-Temperature-Stabilized Alpha Tin Nanocrystals for In Vivo Toxicology Evaluation and Photothermal Therapy Corroborated by FFT Modeling
(American Chemical Society, 2025) Shivesh Sabbarwal; Shreyasi Majumdar; Vivek Kumar Verma; Prachi Srivastava; Ahmad Nawaz; Virendra Pratap Singh; Biplob Koch; Sairam Krishnamurthy; Manoj Kumar
Herein, we unveil a remarkable finding for synthesizing room-temperature-stable, nontoxic, ultrasmall free-standing diamond cubic tin nanocrystals (α-Sn) with beta forms in the aqueous phase, avoiding conventional approaches that typically use toxic elements or large reactive substrates (Si/ InSb) to stabilize α-Sn above 13 °C. Herein, for the first time, we demonstrate the successful synthesis of free-standing alpha tin with extraordinary stability up to 80 °C and in the aqueous phase at room temperature, which was supported by powder X-ray diffraction and X-ray photoelectron spectroscopy characterization methods. This synthetic approach eliminates the need to use hazardous materials, bulky substrates, and elevated temperatures, offering a safer, low-cost, and more sustainable alternative. Prepared α-Sn is characterized by extraordinary NIR absorption and a photothermal efficiency of 42.4%, making it a promising photothermal agent for cancer treatment upon shining low-power (0.5 W) 980 nm NIR light using a CW laser. Using fast Fourier transform weighted bright-field imaging, a mathematical model that foretells the behavior of live malignant cells before and after photothermal treatment has been constructed. Additionally, in vivo studies in rats backed by biochemical and histopathological analyses demonstrated no adverse effects on the vital organs of Wister rats. The unusual biocompatibility of the prepared α-Sn nanocrystals is demonstrated by a low hemolysis index (3.28 ± 0.53%) of the blood, which is far below the permissible limits of 5%. Current research unveils the strong potential of free-standing alpha-tin not only in the area of nanomedicine but also in other domains. © 2024 American Chemical Society.
Sonodynamic Cancer Therapy by Mn(I)-tricarbonyl Complexes via Ultrasound-triggered CO Release and ROS Generation
(John Wiley and Sons Inc, 2025) Ashish Kumar Kumar Yadav; Virendra Pratap Singh; Sagar Acharjee; Sukanta Saha; Rajesh Kumar Kushwaha; Arnab Dutta; Biplob Koch; Samya Banerjee
A novel ferrocene conjugated Mn(I)-tricarbonyl complex viz [Mn(Fc-tpy)(CO)3Br] (Mn2) where, Fc-tpy=4′-ferrocenyl-2,2′:6′,2′′-terpyridine was synthesized and fully characterized along with its non-ferrocene analog [Mn(Ph-tpy)(CO)3Br] Ph-tpy=4′-phenyl-2,2′:6′,2′′-terpyridine (Mn1) for ultrasound (US) activated anticancer applications. The X-ray structure of Mn2 confirmed its distorted octahedral geometry. Mn1 and Mn2, for the first time, showed US-triggered release of CO and ROS generation (1O2 and ⋅OH) in an aqueous solution from any Mn(I)-tricarbonyl complexes, indicating its potential for synergetic CO gas therapy and sonodynamic therapy. The above-mentioned in-solution chemistry was successfully translated into in vitro cellular models. These complexes showed unprecedented US-triggered toxicity against T-cell lymphoma and human breast cancer cells (IC50 for Mn2<1 μM) while were minimally toxic without US or against normal spleen and human embryonic kidney cells. Mn2 was ca. 12 fold more anticancer active than Mn1, indicating that the ferrocene conjugation augmented the US sensitivity. The apoptotic sonotoxicity of Mn2 was due to US-promoted mitochondrial depolarization via ROS generation and CO release. The apoptosis was triggered by caspase 3 activation. This is the first report of Mn(I)-tricarbonyl-based sonosensitizers for cancer SDT. Overall, this study, for the first time, establishes the effectiveness of 3d metal carbonyls in SDT. © 2024 Wiley-VCH GmbH.
Formulation and Evaluation of Lipid/Soluplus-Stabilized Nanocrystals of Paclitaxel and Bosutinib for a Synergistic Effect in Non-Small Cell Lung Cancer Therapy
(American Chemical Society, 2025) Manish Kumar; Pooja Goswami; Abhishek Jha; Vividha S. Dhapte-Pawar; Biplob Koch; Brahmeshwar Mishra
Tyrosine kinase inhibitors have been employed for the treatment of lung cancer, owing to their role in regulating irregulated pathways or mutated genes. Bosutinib, a nonreceptor tyrosine kinase, has been recently investigated for lung cancer treatment. Bosutinib can also be used with paclitaxel as a combinatorial approach to receive a synergistic effect for the effective management of lung cancer. Furthermore, the nanocrystals of each can also be prepared and in combination can produce a more pronounced impact than the drug combination. Herein, the prepared Soluplus/lipid-stabilized nanocrystals of paclitaxel and bosutinib were rod to cubic in shape of about 150-250 nm. The nanocrystals were stable, provided controlled drug release, and exhibited a higher aerosolization performance. The nanocrystal combination demonstrated higher anticancer activity than the drug combination synergy against A549 cancer cells. The nanocrystals increased the level of cellular internalization in cancer cells, thereby inducing higher ROS generation and apoptosis of cancer cells. Furthermore, the lipid/Soluplus-stabilized nanocrystals exhibited higher translocation potential compared with only Soluplus-stabilized nanocrystals. The nanocrystals administered intratracheally showed a lower drug distribution to other organs, with prolonged drug retention in the lungs, suggesting the higher efficacy of developed nanocrystals in targeting the lungs. In conclusion, lipid-modified nanocrystals can be a novel approach for the effective management of lung cancer. © 2025 American Chemical Society.
Chitosan-Functionalized Fluorescent Calcium Carbonate Nanoparticle Loaded with Methotrexate: Future Theranostics for Triple Negative Breast Cancer
(American Chemical Society, 2025) Rinki Verma; Md Zeyaullah; Virendra Pratap Singh; Preeti Suman Saxena; Biplob Koch; Manoj Kumar
Herein, fluorescent calcium carbonate nanoclusters encapsulated with methotrexate (Mtx) and surface functionalized with chitosan (25 nm) (@Calmat) have been developed for the imaging and treatment of triple-negative breast cancer (TNBC). These biocompatible, pH-sensitive nanoparticles demonstrate significant potential for targeted therapy and diagnostic applications. The efficacy of nanoparticles (NPs) was evaluated in MDA-MB-231 TNBC cell lines. The enhanced permeability and retention effect facilitated the accumulation of NPs, in tumor-bearing rats, as confirmed by in vivo fluorescence imaging. Treatment with @Calmat resulted in a marked reduction in pro-inflammatory cytokines, with levels of IL-6 (1225 ± 67 pg/mL), IL-1β (379 ± 69 pg/mL), and TNF-α (14.1 ± 2 pg/mL), in contrast to the diseased control group (IL-6: 2223 ± 99; IL-1β: 1632 ± 90; TNF-α: 40 ± 3 pg/mL). A similar trend was observed for liver and kidney function biomarkers. Mechanistic studies revealed that @Calmat treatment activates the Bax/Bcl-2 signaling pathway, leading to cell cycle arrest in the G1 phase and subsequent late-phase apoptosis. As a result, the tumor inhibition rate reached 88%, with 80% of treated rats surviving beyond 100 days. These findings highlight the strong potential of @Calmat as a dual-function theranostic agent for the management of TNBC. © 2025 American Chemical Society.
Fluorescent Calcium Nanocluster-Driven Theranostic Nanoplatforms for Advanced Imaging and Therapy in Breast Tumor
(American Chemical Society, 2025) Abhishesh Kumar Mehata; Vivek Kumar Verma; Virendra Pratap Singh; Aseem Setia; None Vikas; Matte Kasi Viswanadh; Shivesh Sabbarwal; Manoj Kumar; Biplob Koch; Madaswamy Sona S Muthu
Biocompatible CaCO3 nanoclusters were prepared by using a simple biomineralization technique. Employing CaCO3 nanoclusters in breast cancer treatment provides an exciting avenue for theranostics, which merges precise imaging with individualized treatment plans. They were highly suitable for improving the efficacy and precision of breast cancer detection and therapy with minimal adverse effects due to their biocompatibility, controlled drug release, pH sensitivity, and adaptability. In our current study, we proposed a palbociclib (PBB)-loaded fluorescent calcium nanocluster-based redox-sensitive drug delivery system for efficient breast cancer imaging and therapy. The developed nanoparticles were analyzed for their morphology and various physicochemical properties. The particle sizes of the formulated FNC-PBB-CS-NPs (nonredox-sensitive) and FNC-PBB-CS-SS-NPs (redox-sensitive) nanoparticles were 150.2 ± 2.1 and 160.4 ± 1.4 nm, respectively. The zeta potential of nonredox-sensitive nanoparticles was measured to be +17.12 ± 1.34 mV, while the zeta potential of redox-sensitive nanoparticles was +14.32 ± 1.17 mV. The entrapment efficiencies of FNC-PBB-CS-NPs and FNC-PBB-CS-SS-NPs were determined to be 88.74 ± 2.34 and 89.26 ± 1.21%, respectively. FNC-PBB-CS-SS-NPs demonstrated quicker drug release at acidic pH compared to FNC-PBB-CS-NPs. The cytotoxicity assay conducted on MCF-7 and T-47D cells indicated that FNC-PBB-CS-NPs and FNC-PBB-CS-SS-NPs exhibited greater cytotoxicities than free PBB. Furthermore, the Hoechst/PI dual-staining experiment demonstrated the superior activity of FNC-PBB-CS-SS-NPs over FNC-PBB-CS-NPs and free PBB. Ultrasound/photoacoustic imaging revealed that FNC-PBB-CS-SS-NPs effectively reduced tumor size, hypoxic tumor regions, and tumor vascularity compared to FNC-PBB-CS-NPs and free PBB. Additionally, in vivo optical imaging showed that the FNC-PBB-CS-SS-NPs accumulated more specifically in tumors than the other formulations. © 2025 American Chemical Society.
Ultrasound defect sensitive mechanochromic material with blue-shifted emission for the detection of Cu2+ in Alzheimer's disease cells
(Royal Society of Chemistry, 2025) Aayoosh Singh; Pranjalee Yadav; Amit Kumar Singh; Rupen Tamang; Biplob Koch; Vinod Prasad Singh
The mechanistic investigation and design of ultra-sensitive smart materials with multi-stimuli responsive properties are attracting much interest due to their utilization in several areas concurrently, such as mechanochromic and acidochromic materials, defect sensors, and chemosensors for analytes. Herein, the tailoring of an external stimuli-responsive novel coumarin-based luminogen (CFH) exhibiting green emission (λem = 515 nm) in the liquid state and red emission (λem = 698 nm) in the solid state opens up new avenues for the design of near-infrared emitting coumarin-based materials. CFH is an aggregation-induced enhanced emission (AIEE)-active material exhibiting solvatochromism and viscochromism. The weakly emissive crystals of CFH showed a relatively rare blue-shifted (48 nm) enhanced emission (3-fold) upon grinding. Fluorescence microscopy demonstrated that defect areas on the crystal surface become extremely emissive, indicating a “turn-on” defect-sensitive mechanochromism, susceptible to impact, friction, sculpting and ultrasonic vibrations. Solid CFH displayed acidochromic properties with extraordinary reversibility when exposed to trifluoroacetic acid (TFA)/triethylamine (TEA) vapour, displaying an on-off-on emission. Furthermore, CFH demonstrated “on-off” fluorescence responses to Cu2+ in water, exhibiting a detection limit (LOD) of 1.1 nM and Stern-Volmer constant (Ksv) of 2.84 × 106 M−1. The Job's plot and SC-XRD demonstrated a 1 : 1 binding stoichiometry for the CFH-Cu2+ complex. Leveraging this fluorescence response, portable test kit devices were developed for the detection of Cu2+. Bioimaging was carried out to examine the quenching of the probe with accumulated Cu2+ in SH-SY5Y model cells for neurodegenerative disorders compared to HEK-293 cells, suggesting that CFH can also be used for the intracellular sensing of Cu2+ in Alzheimer's disease (AD) cells. © 2025 The Royal Society of Chemistry.
Synergistic combination of doxorubicin with fisetin for the treatment of lymphoma
(Elsevier B.V., 2025) Sumeet Singh; Virendra Pratap Singh; Ranjeet Kumar Singh; Vinita Gouri; Biplob Koch; Mukesh Samant
Lymphoma is a common cancer of the lymphatic system, and its treatment presents considerable clinical difficulties due to the constraints of existing medicines. Anticancer drug such as Doxorubicin (DOX) is an effective chemotherapeutic drug that is frequently used to treat lymphoma and other cancers; however, it is linked with considerable toxicities. Fisetin, a naturally occurring flavonoid, exhibits anticancer properties and has the potential to augment the therapeutic effects of DOX. This study explores the synergistic effects of combining DOX with fisetin in the treatment of lymphoma. The combination of DOX and fisetin significantly inhibits cell viability, induced membrane blabbing, chromatin condensation, and promoted apoptosis compared to monotherapies. The study also showed that the synergistic effect of fisetin along with DOX significantly promotes apoptosis in DL cells through intracellular ROS generation, mitochondrial aggregation at the periphery of the nucleus and, increased p53, Bax, cytochrome c, caspase 3, caspase 9, and cleaved caspase 9 expression. Additionally, combination therapy not only increased the mean survival of the treated group animals but also reduced the tumor burden. While histopathological parameters have shown overall improvement in combination therapy. This study proposes a novel combinational therapy for the treatment of lymphoma and requires further clinical investigation. © 2025
Ferrocene conjugated Os(ii) complex for photo-catalytic cancer therapy of triple-negative breast cancer cells
(Royal Society of Chemistry, 2025) Apurba Mandal; Virendra Pratap Singh; Silda Peters; Arif Ali Mandal; Tumpa Sadhukhan; Biplob Koch; Samya Banerjee
A novel ferrocene-conjugated bimetallic Os(ii) photocatalyst (OsFe) showed micromolar photocatalytic anticancer activity against triple-negative breast cancer cells via NADH oxidation and caspase 3 activation under visible light. © 2025 The Royal Society of Chemistry.

2025

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