Hypericin has gained great attention as a powerful photosensitizing and fluorescent agent for photodynamic therapy (PDT) and fluorescence diagnosis (FD) of cancer. However, native hypericin is hydrophobic and nearly insoluble in aqueous media which hinders its photobiological activity. Herein, we demonstrate the encapsulation of hypericin and polyvinylpyrrolidone (hypericin@PVP) as an attractive class of water-soluble formula of hypericin with improved absorption and emission characteristics in water. The absorption and fluorescence properties of the water-soluble hypericin@PVP were studied at room temperature. Also, the photostability of the prepared hypericin@PVP was studied under visible light irradiation. The absorbance and emission measurements confirm the association and binding of hypericin and PVP with a binding constant (K) of 1.2 × 10 M. The interaction between hypericin and PVP in water could lead to the dissociation of aggregated hypericin into their monomeric state which is crucial for effective photobiological implementation in PDT and FD. Upon encapsulation with PVP, hypericin showed a significant increase in the fluorescence properties with an enhanced emission intensity of 300% at a PVP concentration of 1 × 10 M. Moreover, water-soluble hypericin@PVP demonstrated high photostability under visible light irradiation with an irradiance of 15 mW/cm and exposure time up to 150 min. This enhancement in the absorption, emission, and photostability of hypericin in water is related to the effects of encapsulation with PVP and the unique spectroscopic properties of the formulated hypericin@PVP.
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http://dx.doi.org/10.1016/j.bpc.2020.106454 | DOI Listing |
Int J Mol Sci
January 2025
Diabetes Center, First Department of Propaedeutic Internal Medicine, Medical School, National and Kapodistrian University of Athens, Laiko General Hospital, 17 Agiou Thoma Street, 11527 Athens, Greece.
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View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
Laboratory of Applied Microbiology, Center for Biotechnology of Natural Resources, Faculty of Agrarian and Forestry Sciences, Catholic University of Maule, Avda. San Miguel 3605, Talca 3460000, Chile.
, also known as St. John's Wort, pericon, or yellow grass, is known for its antidepressant potential. It could represent a natural alternative to current pharmacological antidepressant treatments, which have a high incidence of side effects in patients and therefore lead to early dropouts.
View Article and Find Full Text PDFMolecules
December 2024
Department of Biochemistry and Molecular Biology, Medical University of Lublin, 1 Chodzki Str., 20-093 Lublin, Poland.
Primary and metastatic tumors of the nervous system represent a diverse group of neoplasms, each characterized by distinct biological features, prognostic outcomes, and therapeutic approaches. Due to their molecular complexity and heterogeneity, nervous system cancers (NSCs) pose significant clinical challenges. For decades, plants and their natural products with established anticancer properties have played a pivotal role in the treatment of various medical conditions, including cancers.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
December 2024
Department of Medical Biochemistry, Faculty of Medicine, Mugla Sitki Kocman University, Mugla, Turkey.
Photodynamic therapy (PDT) has gained considerable attention in cancer treatment due to its non-invasive nature and the ability of photosensitizers to generate reactive oxygen species upon light activation, leading to tumor destruction. Glutathione S-transferase P1 (GSTP1) is a key enzyme in chemotherapy resistance, often overexpressed in various cancers, and its inhibition of GSTP1 presents a promising strategy to enhance cancer treatment. This study is aimed at assessing the potential of prominent photosensitizers as GSTP1 inhibitors through molecular docking analysis to strengthen the efficacy of PDT.
View Article and Find Full Text PDFMolecules
November 2024
Institute of Physical Chemistry and Chemical Physics STU, Radlinskeho 9, SK-81237 Bratislava, Slovakia.
The distortions and instability of high-symmetry configurations of polyatomic systems in nondegenerate states are usually ascribed to the pseudo-Jahn-Teller effect (PJTE). The geometries of hypericin, isohypericin, and fringelite D were optimized within various symmetry groups. Group-theoretical treatment and (TD-)DFT calculations were used to identify the corresponding electronic states during the symmetry descent.
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