Red Blood Cell Membrane-Camouflaged Polydopamine and Bioactive Glass Composite Nanoformulation for Combined Chemo/Chemodynamic/Photothermal Therapy

ACS Biomaterials Science & Engineering, Год журнала: 2023, Номер 10(1), С. 442 - 454

Опубликована: Дек. 4, 2023

Combinations of different therapeutic strategies, including chemotherapy (CT), chemodynamic therapy (CDT), and photothermal (PTT), are needed to effectively address evolving drug resistance the adverse effects traditional cancer treatment. Herein, a camouflage composite nanoformulation (TCBG@PR), an antitumor agent (tubercidin, Tub) loaded into Cu-doped bioactive glasses (CBGs) subsequently camouflaged by polydopamine (PDA), red blood cell membranes (RBCm), was successfully constructed for targeted synergetic therapies combining CT Tub, CDT doped copper ions, PTT PDA. In addition, TCBG@PRs with membrane (RBCm) improve biocompatibility, longer retention times, excellent cellular uptake properties. It integrated long circulation multimodal synergistic treatment (CT, CDT, PTT) benefit RBCms avoid immune clearance efficient delivery tumor locations, producing "all-in-one" nanoplatform. vivo results showed that prolonged improved accumulation. The combination CT, enhanced activity, light-triggered release reduced systematic toxicity increased effects.

Язык: Английский

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Synthesis of Novel Triazine-Based Chalcones and 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as Potential Leads in the Search of Anticancer, Antibacterial and Antifungal Agents

International Journal of Molecular Sciences, Год журнала: 2024, Номер 25(7), С. 3623 - 3623

Опубликована: Март 23, 2024

This study presents the synthesis of four series novel hybrid chalcones (20,21)a–g and (23,24)a–g six 1,3,5-triazine-based pyrimido[4,5-b][1,4]diazepines (28–33)a–g evaluation their anticancer, antibacterial, antifungal, cytotoxic properties. Chalcones 20b,d, 21a,b,d, 23a,d–g, 24a–g 29e,g, 30g, 31a,b,e–g, 33a,b,e–g exhibited outstanding anticancer activity against a panel 60 cancer cell lines with GI50 values between 0.01 100 μM LC50 in range 4.09 to >100 μM, several such derivatives showing higher than standard drug 5-fluorouracil (5-FU). On other hand, among synthesized compounds, best antibacterial properties N. gonorrhoeae, S. aureus (ATCC 43300), M. tuberculosis were by (MICs: 0.25–62.5 µg/mL). The antifungal studies showed that triazinylamino-chalcone 29e triazinyloxy-chalcone 31g most active compounds T. rubrum mentagrophytes A. fumigatus, respectively (MICs = 62.5 μg/mL). Hemolytic silico toxicity analysis demonstrated are safe.

Язык: Английский

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Investigation of structural, electronical and in vitro cytotoxic activity properties of some heterocyclic compounds

Journal of Molecular Structure, Год журнала: 2021, Номер 1246, С. 131127 - 131127

Опубликована: Июль 19, 2021

Язык: Английский

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Design, synthesis, and cytotoxic activities of isaindigotone derivatives as potential anti-gastric cancer agents

Journal of Enzyme Inhibition and Medicinal Chemistry, Год журнала: 2022, Номер 37(1), С. 1212 - 1226

Опубликована: Апрель 21, 2022

A series of novel derivatives isaindigotone, which comes from the root isaits indinatca Fort, were synthesised (Compound 1-26). Four human gastrointestinal cancer cells (HCT116, PANC-1, SMMC-7721, and AGS) employed to evaluate anti-proliferative activity. Among them, Compound 6 displayed most effective inhibitory activity on AGS with an IC50 (50% concentration) value 2.2 μM. The potential mechanism study suggested that induced apoptosis in cells. collapse mitochondrial membrane (MMP) was proved. In docking analysis, good affinity interaction between AKT1 discovered. Treatment also resulted significant suppression PI3K/AKT/mTOR signal pathway. MMP pathway may be responsible for induction apoptosis. This derivative could useful as underlying anti-tumour agent treatment gastric cancer.

Язык: Английский

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Current progress in the targeted therapy of breast cancer: Structure–activity correlation and docking studies (2015–2021)

Archiv der Pharmazie, Год журнала: 2023, Номер 356(8)

Опубликована: Май 21, 2023

Abstract Despite cancer research and therapy, breast remains a complicated health crisis in women represents top biomedical priority. Nowadays, is an extremely heterogeneous disease known as the leading cause of death among worldwide. The incidence mortality rates have been increasing gradually for past decades. common treatments are chemotherapy, endocrine immunotherapy, radiotherapy, surgery. most targets treatment human epidermal growth factor receptor 2 (HER2) estrogen receptors. literature suggests that several targets/pathways also involved development cancer, is, poly(ADP‐ribose) polymerase (PARP), bromodomain‐containing protein 4 (BRD4), cyclin‐dependent kinase 4/6 (CDK4/6), (EGFR), vascular endothelial (VEGFR), polo‐like 1 (PLK1), phosphoinositide 3‐kinases/protein B/mammalian target rapamycin (PI3K/AKT/mTOR), histone deacetylase (HDAC), nuclear kappa B (NF‐κB), PD‐L1, aromatase inhibitors. Meanwhile, study hot topic current scenario basic/clinical research. This review article provides information on different associated with summarizes progress synthesized inhibitors anti‐breast agents from 2015 to 2021. aims provide structure–activity relationship docking studies designing novel compounds therapy.

Язык: Английский

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