Physcion and Physcion 8-O-β-D-glucopyranoside: Natural Anthraquinones with Potential Anticancer Activities

Shah, Muhammad Ajmal; Adnan, Muhammad; Rasul, Azhar; Hussain, Ghulam; Sarfraz, Iqra; Nageen, Bushra; Riaz, Ammara; Khalid, R.; Asrar, Muhammad; Selamoğlu, Zeliha; Adem, Şevki; Sarker, Satyajit D.

doi:10.2174/1389450121999201013154542

Cited by 23 publications

(17 citation statements)

References 147 publications

(222 reference statements)

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“…AQs, including PTN, act inhibiting tumour growth and metastasis, inducing apoptosis and cancer cell metabolism, re-programmation and cell cycle arrest, regulating cell signalling pathways, and improving the effectivity of other chemotherapeutics in drug-resistant cells 35 . Whereas some authors demonstrated that PTN was significantly cytotoxic in the dark when it was used at concentrations from 50 μM onwards after 72 h exposure, with a low percentage of apoptotic cells 36 ; other authors demonstrated that lower exposure time to in vitro growing cells induced no significant effect on the inhibition of cancer cell proliferation (35 µM for 16 h 37 , and 40 and 80 µM for 12 h) 38 .…”

Section: Discussionmentioning

confidence: 99%

Photosensitization of a subcutaneous tumour by the natural anthraquinone parietin and blue light

Mugas

Calvo

Marioni

et al. 2021

Sci Rep

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Photodynamic therapy (PDT) is an anticancer treatment involving administration of a tumour-localizing photosensitizer, followed by activation by light of a suitable wavelength. In previous work, we showed that the natural anthraquinone (AQ) Parietin (PTN), was a promising photosensitizer for photodynamic therapy of leukemic cells in vitro. The present work aimed to analyze the photosensitizing ability of PTN in the mammary carcinoma LM2 cells in vitro and in vivo in a model of subcutaneously implanted tumours. Photodynamic therapy mediated by parietin (PTN-PDT) (PTN 30 µM, 1 h and 1.78 J/cm2 of blue light) impaired cell growth and migration of LM2 cells in vitro. PTN per se induced a significant decrease in cell migration, and it was even more marked after illumination (migration index was 0.65 for PTN and 0.30 for PTN-PDT, *p < 0.0001, ANOVA test followed by Tukey’s multiple comparisons test), suggesting that both PTN and PTN-PDT would be potential inhibitors of metastasis. Fluorescence microscopy observation indicated cytoplasmic localization of the AQ and no fluorescence at all was recorded in the nuclei. When PTN (1.96 mg) dissolved in dimethyl sulfoxide was topically applied on the skin of mice subcutaneously implanted with LM2 cells, PTN orange fluorescence was strongly noticed in the stratum corneum and also in the inner layers of the tumour up to approximately 5 mm. After illumination with 12.74 J/cm2 of blue light, one PDT dose at day 1, induced a significant tumour growth delay at day 3, which was not maintained in time. Therefore, we administered a second PTN-PDT boost on day 3. Under these conditions, the delay of tumour growth was 28% both on days 3 and 4 of the experiment (*p < 0.05 control vs. PTN-PDT, two-way ANOVA, followed by Sidak’s multiple comparisons test). Histology of tumours revealed massive tumour necrosis up to 4 mm of depth. Intriguingly, a superficial area of viable tumour in the 1 mm superficial area, and a quite conserved intact skin was evidenced. We hypothesize that this may be due to PTN aggregation in contact with the skin and tumour milieu of the most superficial tumour layers, thus avoiding its photochemical properties. On the other hand, normal skin treated with PTN-PDT exhibited slight histological changes. These preliminary findings encourage further studies of natural AQs administered in different vehicles, for topical treatment of cutaneous malignancies.

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Section: Discussionmentioning

confidence: 99%

Photosensitization of a subcutaneous tumour by the natural anthraquinone parietin and blue light

Mugas

Calvo

Marioni

et al. 2021

Sci Rep

View full text Add to dashboard Cite

show abstract

“…AQs, including PTN, act inhibiting tumour growth and metastasis, inducing apoptosis and cancer cell metabolism, re-programmation and cell cycle arrest, regulating cell signalling pathways, and improving the effectivity of other chemotherapeutics in drug-resistant cells [34]. Whereas some authors demonstrated that PTN was signi cantly cytotoxic in the dark when it was used at concentrations from 50 µM onwards after 72 h exposure, with a low percentage of apoptotic cells [35]; other authors demonstrated that lower exposure time to in vitro growing cells induced no signi cant effect on the inhibition of cancer cell proliferation (35 µM for 16 h [36], and 40 and 80 µM for 12 h) [37].…”

Section: Discussionmentioning

confidence: 99%

Topical Application of the Anthraquinone Parietin and Blue Light Illumination Induces Delayed Cell Growth and Necrosis in the Deeper Layers of a Subcutaneously Implanted Tumour

Mugas

Calvo

Marioni

et al. 2021

Preprint

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Photodynamic therapy (PDT) is an anticancer treatment involving administration of a tumour-localizing photosensitizer, followed by activation by light of a specific wavelength.In previous work, we showed that the natural anthraquinone (AQ) Parietin (PTN), was a promising photosensitizer for photodynamic therapy of leukemic cells in vitro. The present work aimed to analyze the photosensitizing ability of PTN in the mammary carcinoma LM2 cells in vitro and in vivo in a model of subcutaneously implanted tumours.Photodynamic therapy mediated by Parietin (PTN-PDT) (PTN 30 µM, 1 h and 1.78 J/cm2 of blue light) impaired cell growth and migration of LM2 cells in vitro. PTN per se induced a significant decrease in cell migration, and it was even more marked after illumination (migration index was 0.65 for PTN and 0.30 for PTN-PDT), suggesting that both PTN and parietin-mediated PDT would be potential inhibitors of metastasis.Fluorescence microscopy observation indicated cytoplasmatic localization of the AQ and no fluorescence at all was recorded in the nuclei.When PTN (1.96 mg) dissolved in dimethyl sulfoxide was topically applied on the skin of mice subcutaneously implanted with LM2 cells, PTN orange fluorescence was strongly noticed in the stratum corneum and also in the inner layers of the tumour up to approximately 5 mm. After illumination with 12.74 J/cm2 of blue light, one PDT dose at day 1, induced a significant tumour growth delay at day 3, which was not maintained in time. Therefore, we administered a second PTN-PDT boost on day 3. Under these conditions, the delay of tumour growth was 28 % both on days 3 and 4 of the experiment.Histology of tumours revealed massive tumour necrosis up to 4 mm of depth. Intriguingly, a superficial area of viable tumour in the 1 mm superficial area, and a quite conserved intact skin was evidenced. We hypothesize that this may be due to PTN aggregation in contact with the skin and tumour milieu of the most superficial tumour layers, thus avoiding its photochemical properties.On the other hand, normal skin treated with PTN-PDT exhibited slight histological changes. These preliminary findings encourage further studies of natural AQs administered in different vehicles, for topical treatment of cutaneous malignancies.

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“…Physcion also modulates cancer cell metabolism. In particular, it inhibits the 6-phosphogluconate dehydrogenase (6PGD) enzyme, usually overexpressed in cancer cells [ 89 ].…”

Section: Anticancer Mechanisms Of Aqs Isolated From Marine Fungimentioning

confidence: 99%

Marine Anthraquinones: Pharmacological and Toxicological Issues

et al. 2021

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The marine ecosystem, populated by a myriad of animals, plants, and microorganisms, is an inexhaustible reservoir of pharmacologically active molecules. Among the multiple secondary metabolites produced by marine sources, there are anthraquinones and their derivatives. Besides being mainly known to be produced by terrestrial species, even marine organisms and the uncountable kingdom of marine microorganisms biosynthesize anthraquinones. Anthraquinones possess many different biological activities, including a remarkable antitumor activity. However, due to their peculiar chemical structures, anthraquinones are often associated with toxicological issues, even relevant, such as genotoxicity and mutagenicity. The aim of this review is to critically describe the anticancer potential of anthraquinones derived from marine sources and their genotoxic and mutagenic potential. Marine-derived anthraquinones show a promising anticancer potential, although clinical studies are missing. Additionally, an in-depth investigation of their toxicological profile is needed before advocating anthraquinones as a therapeutic armamentarium in the oncological area.

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Physcion and Physcion 8-O-β-D-glucopyranoside: Natural Anthraquinones with Potential Anticancer Activities

Cited by 23 publications

References 147 publications

Photosensitization of a subcutaneous tumour by the natural anthraquinone parietin and blue light

Photosensitization of a subcutaneous tumour by the natural anthraquinone parietin and blue light

Topical Application of the Anthraquinone Parietin and Blue Light Illumination Induces Delayed Cell Growth and Necrosis in the Deeper Layers of a Subcutaneously Implanted Tumour

Marine Anthraquinones: Pharmacological and Toxicological Issues

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