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Effects of psoralens as anti-tumoral agents in breast cancer cells

World Journal of Clinical Oncology 2014年第3期5卷 348-358页

作者： Maria Luisa Panno Francesca Giordano Department of Pharmacy Health and Nutritional Sciences University of CalabriaArcavacata di RendeCS 87036Italy

This review examines the biological properties of coumarins, widely distributed at the highest levels in the fruit, followed by the roots, stems and leaves, by considering their beneficial effects in the prevention of some diseases and as anti-cancer agents. These compounds are well known photosensitizing drugs which have been used as pharmaceuticals for a broad number of therapeutic applications requiring cell division inhibitors. Despite this, even in the absence of ultraviolet rays they are active. The current paper mainly focuses on the effects of psoralens on human breast cancer as they are able to influence many aspects of cell behavior, such as cell growth, survival and apoptosis. In addition, analytical and pharmacological data have demonstrated that psoralens antagonize some metabolizing enzymes, affect estrogen receptor stability and counteract cell invasiveness as well as cancer drug resistance. The scientific findings summarized highlight the pleiotropic functions of phytochemical drugs, given that recently their target signals and how these are modified in thecells have been identified. The encouraging results in this field suggest that multiple modulating strategies based on coumarin drugs in combination with canonical chemotherapeutic agents or radiotherapy could be a useful approach to address the treatment of many types of cancer.

关键词： psoralens Breast tumor Bergapten Growth factors Estrogens

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Inhibition of cytochrome P450 by furanocoumarins in grapefruit juice and herbal medicines

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Acta Pharmacologica Sinica 2004年第2期25卷 3-10页

作者： Lian-qing GUO1, Yasushi YAMAZOE2Department of Clinical Pharmacology, Jinling Hospital, Nanjing 210002, China 2Division of Drug Metabolism and MolecularToxicology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan Department of Clinical Pharmacology Jinling Hospital Nanjing 210002 Division of Drug Metabolism and Molecular Toxicology Graduate School of Pharmaceutical Sciences Tohoku University Sendai 980-8578 日本

Furanocoumarins (psoralens) exist in various plants and some of them are used to cure skin diseases. Thesechemicals draw attentions recently because of their abilities to arouse drug interaction through inhibition of cyto-chrome P450. Grapefruit juice is a well-known example for food-drug interaction. But in vitro and in vivo studieshave shown that the causative components are mainly furanocoumarin derivatives with geranyloxy side chains. Invitro experiments confirmed that furanocoumarins from grapefruit juice are both competitive and mechanism-based inhibitors of CYP3A4. Although the inhibition appeared to be stronger in the dimers than that in the monomers,all contribute comprehensively to the grapefruit juice-drug interaction. Further experiments with other furanocoumarinsand related citrus fruits or umbelliferous herbal medicines indicate that drug interaction might also occur with stuffsother than grapefruit juice, especially with traditional medicine.

关键词： psoralens grapefruit juice herbal medicine enzyme inhibitors cytochrome P-450 enzyme system drug interaction

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Synthesis and Photooxygenation of Furo[3,2-c]coumarin Derivatives as Antibacterial and DNA Intercalating Agent

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Chinese Journal of Chemistry 2012年第2期30卷 316-320页

作者： Al-Sehemi,Abdullah G. EI-Gogary,Sameh R. Chemistry Department Faculty of Science(Abha)King Khaled UniversityKingdom of Saudia Arabia Chemistry Department Faculty of Science(Damietta)Mansoura UniversityEgypt

Syntheses of 2,3-dimethyl-4H-furo[3,2-c]coumarin and 3-phenyl-4H-furo[3,2-c]coumarin as angular furocou- marins were carried out through Williamson reaction of 4-hydroxycoumarin with a-haloketones followed by cycli- zation. Photooxygenation of the synthesized furocoumarin derivatives was performed and the photoproducts were isolated and characterized. The affinity of 2,3-dimethyl-4H-furo[3,2-c]coumarin towards DNA and the antibacterial activity were evaluated and compared with 8-methoxypsoralen （8-MOP）.

关键词： furocoumarins psoralens photooxygenation antibacterial activity and DNA

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