The chemical and biological properties of hypericin—a compound with a broad spectrum of biological activities

Lavie, Gad; Mazur, Yehuda; Lavie, David; Meruelo, Daniel

doi:10.1002/med.2610150203

Cited by 172 publications

(94 citation statements)

References 53 publications

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“…Hypericin has been regarded as a promising photosensitizing agent for its characteristic of light-dependent antineoplastic and antiviral activity [16]. Hypericin-mediated PDT has obtained increasing interests as a potential treatment for various cancers [17][18][19].…”

Section: Introductionmentioning

confidence: 99%

Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro

Zhang

Shao

et al. 2014

Cancer Cell Int

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Section: Introductionmentioning

confidence: 99%

Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro

Zhang

Shao

et al. 2014

Cancer Cell Int

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“…We have recently been focusing on hypericin, a natural compound isolated from Hypericum plants (Lavie et al, 1995a), as a potent photosensitiser with a high antitumoral PDT efficacy (Chen and de Witte, 2000;Chen et al, 2001Chen et al, , 2002. In the course of our study, we found that the compound accumulated to a large extent in tumour tissues.…”

mentioning

confidence: 77%

Elucidation of the tumoritropic principle of hypericin

Putte¹,

Roskams

Vandenheede

et al. 2005

Br J Cancer

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Hypericin is a potent agent in the photodynamic therapy of cancers. To better understand its tumoritropic behaviour, we evaluated the major determinants of the accumulation and dispersion of hypericin in subcutaneously growing mouse tumours. A rapid exponential decay in tumour accumulation of hypericin as a function of tumour weight was observed for each of the six tumour models investigated, and a similar relationship was found between tumour blood flow and tumour weight. Moreover, there was a close correlation between the higher hypericin uptake in RIF-1 tumours compared to R1 tumours and tumour vessel permeability. To define the role of lipoproteins in the transport of hypericin through the interstitial space, we performed a visual and quantitative analysis of the colocalisation of hypericin and DiOC 18 -labelled lipoproteins in microscopic fluorescent overlay images. A coupled dynamic behaviour was found early after injection (normalised fluorescence intensity differences were on the whole less than 10%), while a shifted pattern in localisation of hypericin and DiOC 18 was seen after 24 h, suggesting that during its migration through the tumour mass, hypericin is released from the lipoprotein complex. In conclusion, we were able to show that the tumour accumulation of hypericin is critically determined by a combination of biological (blood flow, vessel permeability) and physicochemical elements (affinity for interstitial constituents).

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“…1(A, B)), found naturally in St John's wort (genus, Hypericum) or obtained semisynthetically from emodine (1). Hypericin has been shown to have antiviral and antineoplastic activities (2). It is one of the most potent photosensitizers and has been successfully used in photodynamic therapy (PDT) for the ablation of some tumors, notably carcinoma in situ of the bladder and some subcutaneous lesions (3)(4)(5)(6).…”

Section: Introductionmentioning

confidence: 98%

Evaluation of tumor affinity of mono‐[¹²³I]iodohypericin and mono‐[¹²³I]iodoprotohypericin in a mouse model with a RIF‐1 tumor

Fonge

Putte

Huyghe

et al. 2007

Contrast Media & Molecular

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In this study we have compared the tumour-seeking properties of mono-[(123)I]iodoprotohypericin and mono-[(123)I]iodohypericin in C3H mice with a subcutaneous radiation-induced fibrosarcoma-1 tumor. After intravenous injection, both tracers were rapidly cleared from all organs and were retained by the tumors. There was no significant difference in tumor uptake of the two tracers at all studied time points (p > 0.05). To study the plausible mechanism of hypericin and mono-iodohypericin uptake in tumor, their plasma binding profile was investigated. Both agents show high affinity for low-density lipoproteins and to a lesser extent high-density lipoproteins and other heavy proteins. Mono-[(123)I]iodohypericin appears to be more promising as a tumor diagnostic agent, given its faster clearance from all organs.

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The chemical and biological properties of hypericin—a compound with a broad spectrum of biological activities

Cited by 172 publications

References 53 publications

Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro

Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro

Elucidation of the tumoritropic principle of hypericin

Evaluation of tumor affinity of mono‐[¹²³I]iodohypericin and mono‐[¹²³I]iodoprotohypericin in a mouse model with a RIF‐1 tumor

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The chemical and biological properties of hypericin—a compound with a broad spectrum of biological activities

Cited by 172 publications

References 53 publications

Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro

Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro

Elucidation of the tumoritropic principle of hypericin

Evaluation of tumor affinity of mono‐[123I]iodohypericin and mono‐[123I]iodoprotohypericin in a mouse model with a RIF‐1 tumor

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Evaluation of tumor affinity of mono‐[¹²³I]iodohypericin and mono‐[¹²³I]iodoprotohypericin in a mouse model with a RIF‐1 tumor