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1.
Chem Biol Drug Des ; 99(1): 103-110, 2022 01.
Artigo em Inglês | MEDLINE | ID: mdl-34331335

RESUMO

In recent years, biological macromolecules have piqued the interest of researchers owing to their vast variety of biological uses. As a result, the marine sponge is a multicellular heterotrophic parazoan with chemicals for defence against predator assaults, biofouling and microbial diseases. These priceless molecules are known as secondary metabolites, and they are essential for survival in a highly competitive environment. So far, over 5,000 marine natural compounds have been extracted from marine sponges, making them an excellent option for drug formulation. One among them is, aaptamine, a marine alkaloid with a benzo[de][1,6]-napthyridine framework extensively distributed in marine sponges. Due to this reason, aaptamine has been intensively researched for various biological purposes, including cancer and protease inhibition, offering fresh insights into novel treatments. Keeping this in mind, we reviewed the biological significance of the marine sponge alkaloid aaptamine.


Assuntos
Alcaloides/química , Antineoplásicos/química , Naftiridinas/química , Poríferos/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Animais , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antioxidantes/química , Antivirais/química , Antivirais/isolamento & purificação , Antivirais/farmacologia , Proliferação de Células/efeitos dos fármacos , HIV-1/efeitos dos fármacos , Naftiridinas/isolamento & purificação , Naftiridinas/farmacologia , Poríferos/metabolismo
2.
RSC Adv ; 11(8): 4818-4828, 2021 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-35424411

RESUMO

In recent years, the development of a nano-conjugate system for drug delivery applications has gained attention among researchers. Keeping this in mind, in this study, we developed a doxorubicin-platinum conjugate system that targeted breast cancer cell lines. To achieve this, we developed platinum nanoparticles using polyvinylpyrrolidone (PVP). High resolution-transmission electron microscopy (HR-TEM) revealed the occurrence of octopod-shaped platinum nanoparticles. Subsequently, doxorubicin (DOX) was conjugated on the surface of the as-prepared platinum octopods via an in situ stirring method. The physicochemical characterization of the doxorubicin-platinum conjugate system revealed that the PVP of PtNPs interacts with the NH2 group of doxorubicin via electrostatic interaction/hydrogen bonding. Besides, the doxorubicin-platinum conjugate system exhibited a sustained drug release profile within the cancer cells. Furthermore, the evaluation of the in vitro anticancer efficacy of the doxorubicin-platinum conjugate system in breast cancer cells (MCF-7 and MDA-MB-231) unveiled the induction of apoptosis via intracellular ROS and DNA damage, rather than free DOX and PtNPs. Remarkably, we also perceived that the doxorubicin-platinum conjugate system was strong enough to down-regulate the PI3K/AKT signalling pathway. As a result, the tumour suppressor gene PTEN was activated, which led to the stimulation of a mitochondrion-based intrinsic apoptotic pathway and its downstream caspases, triggering cell death. Hence, our findings suggested that a biologically stable doxorubicin-platinum conjugate system could be an imperative therapeutic agent for anticancer therapy in the near future.

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