Hypericin, the photoactive compound of Hypericum perforatum, is probably the most powerful photosensitizer found in nature. This compound has shown high potency in the photodynamic treatment of tumor cells. However, there is only limited knowledge regarding the photodynamic effect of hypericin on nonmelanoma skin cancer cells. The aim of this prospective study was to investigate the efficacy of photodynamic therapy with topical application of an extract of H. perforatum in actinic keratosis, basal cell carcinoma (BCC) and morbus Bowen (carcinoma in situ). The study was carried out on 34 patients--eight with actinic keratoses (AKs), 21 with BCC and five with Bowen's disease. The extract of H. perforatum was applied on the skin lesions under occlusion and that was followed by irradiation with 75 J cm(-2) of red light 2 h later. The treatment was performed weekly for 6 weeks on average. The percentage of complete clinical response was 50% for AKs, 28% in patients with superficial BCC and 40% in patients with Bowen's disease. There was only a partial remission seen in patients with nodular BCCs. A complete disappearance of tumor cells was found in the histologic preparation of 11% of patients with superficial BCCs and 80% in the patients with Bowen's disease. All patients complained of burning and pain sensations during irradiation. Although the results of this first clinical trial could be regarded as disappointing, there are still possibilities for improvement. Better preparation of the lesions, enhancement of hypericin delivery and other types of light exposure procedures could significantly improve the clinical outcomes of this relatively inexpensive treatment modality.
- MeSH
- anthraceny MeSH
- antitumorózní látky terapeutické užití MeSH
- aplikace lokální MeSH
- bazocelulární karcinom farmakoterapie MeSH
- Bowenova nemoc farmakoterapie MeSH
- dospělí MeSH
- fotochemoterapie metody MeSH
- fytoterapie MeSH
- keratóza farmakoterapie MeSH
- lidé středního věku MeSH
- lidé MeSH
- molekulární struktura MeSH
- nádory kůže farmakoterapie MeSH
- perylen analogy a deriváty terapeutické užití MeSH
- pilotní projekty MeSH
- rostlinné přípravky terapeutické užití MeSH
- senioři nad 80 let MeSH
- senioři MeSH
- třezalka * chemie MeSH
- výsledek terapie MeSH
- Check Tag
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- mužské pohlaví MeSH
- senioři nad 80 let MeSH
- senioři MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- klinické zkoušky MeSH
- práce podpořená grantem MeSH
- Názvy látek
- anthraceny MeSH
- antitumorózní látky MeSH
- hypericin MeSH Prohlížeč
- perylen MeSH
- rostlinné přípravky MeSH
St. John's Wort (Hypericum perforatum L.) is commonly accepted as a medicinal plant. The data on the physiological activities of the individual substances that are produced in different organs of H. perforatum are well known at present. The highest attention is focused on the characterization and phytochemical properties of hypericin and hyperforin. These organic compounds are used as antidepressant, anticarcinogenic (photodynamic), antimicrobial and virostatic agents. The review paper surveys the present knowledge of chemical and analytical methods for their identification and quantification, physiological activity, and pharmacological and biomedical applications of hypericin and hyperforin.
- MeSH
- anthraceny MeSH
- antidepresiva terapeutické užití MeSH
- depresivní poruchy farmakoterapie MeSH
- floroglucinol analogy a deriváty izolace a purifikace farmakologie terapeutické užití MeSH
- fytoterapie MeSH
- léčivé rostliny chemie MeSH
- lidé MeSH
- můstkové bicyklické sloučeniny izolace a purifikace farmakologie terapeutické užití MeSH
- perylen analogy a deriváty izolace a purifikace farmakologie terapeutické užití MeSH
- rostlinné extrakty izolace a purifikace farmakologie terapeutické užití MeSH
- terpeny izolace a purifikace farmakologie terapeutické užití MeSH
- třezalka chemie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
- Názvy látek
- anthraceny MeSH
- antidepresiva MeSH
- floroglucinol MeSH
- hyperforin MeSH Prohlížeč
- hypericin MeSH Prohlížeč
- můstkové bicyklické sloučeniny MeSH
- perylen MeSH
- rostlinné extrakty MeSH
- terpeny MeSH
Hypericin is a photosensitizing plant pigment from Hypericum perforatum with multiple modes of light-induced biological activities due to production of singlet oxygen and/or excited-state proton transfer with consequent pH drop in the hypericin environment. In the present work, we studied the effects of three inhibitors of crucial mechanisms responsible for intracellular pH (pHi) regulation on hypericin phototoxicity: N-ethylmaleimide (NEM), an inhibitor of H+-ATPase, 5'-(N,N-dimethyl)-amiloride (DMA), an inhibitor of Na+/H+ exchanger, and omeprazole (OME), an inhibitor of H+K+-ATPase. Our experiments show that the effect of hypericin at 1 x 10(-5) and 1 x 10(-6) mol x l(-1) was significantly potentiated by NEM (1 x 10(-7)-1 x 10(--9) mol x l(-1)) and DMA (1 x 10(-6) and 1 x 10(-7) mol x l(-1)) in leukemic CEM cell line. On the other hand, OME had no significant effect on hypericin cytotoxicity. Our results support the hypothesis that the excited-state proton transfer and the consequent acidification of hypericin environment could play a role in the biological activity of hypericin.
- MeSH
- amilorid farmakologie MeSH
- anthraceny MeSH
- antitumorózní látky terapeutické užití toxicita MeSH
- ethylmaleimid farmakologie MeSH
- inhibitory enzymů farmakologie MeSH
- intracelulární tekutina účinky léků účinky záření MeSH
- koncentrace vodíkových iontů účinky léků účinky záření MeSH
- lékové interakce účinky záření MeSH
- leukemie farmakoterapie metabolismus MeSH
- lidé MeSH
- nádorové buňky kultivované MeSH
- omeprazol farmakologie MeSH
- perylen analogy a deriváty terapeutické užití toxicita MeSH
- radiosenzibilizující látky terapeutické užití toxicita MeSH
- světlo MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- amilorid MeSH
- anthraceny MeSH
- antitumorózní látky MeSH
- ethylmaleimid MeSH
- hypericin MeSH Prohlížeč
- inhibitory enzymů MeSH
- omeprazol MeSH
- perylen MeSH
- radiosenzibilizující látky MeSH
