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      Phytochemical and pharmacological notes of plants indicated to treat tumors in Brazil

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          Abstract

          The plants used in traditional medicine have been considered an important source of molecules with pharmacological activity, including antitumor. The aim of this study was to present a pharmacological description and the phytochemical components related to antitumor activity of thirty plants commonly cited in Brazil to treat tumors as well as offering an overview of approaches that are necessary for the development of herbal medicines from these resources. In the search for studies with these plants, five database were used (SciELO, Scirus, Scopus, Biological Abstracts and Web of Science), with the following keywords: tumor AND Species AND cancer. We consider all the scientific synonyms of species available in the Tropicos® database (http://www.tropicos.org/). We surveyed papers from the period between 1980 and 2008. Twnety one species (70%) have at least one evaluation of a class of molecule or metabolite isolated against a pharmacological model. Most species (60%) has in vivo studies. Of the thirty plant species, two stood out for having pharmacological studies in vitro, in vivo and clinical with positive results: Chelidonium majus L., Papaveraceae, and Aloe arborescens Mill., Xanthorrhoeaceae. Although there is generally a good activity of species presented here, there is a need for further studies in order to evaluate the possibility of developing some byproduct.

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          Multitargeted therapy of cancer by silymarin.

          Silymarin, a flavonolignan from milk thistle (Silybum marianum) plant, is used for the protection against various liver conditions in both clinical settings and experimental models. In this review, we summarize the recent investigations and mechanistic studies regarding possible molecular targets of silymarin for cancer prevention. Number of studies has established the cancer chemopreventive role of silymarin in both in vivo and in vitro models. Silymarin modulates imbalance between cell survival and apoptosis through interference with the expressions of cell cycle regulators and proteins involved in apoptosis. In addition, silymarin also showed anti-inflammatory as well as anti-metastatic activity. Further, the protective effects of silymarin and its major active constituent, silibinin, studied in various tissues, suggest a clinical application in cancer patients as an adjunct to established therapies, to prevent or reduce chemotherapy as well as radiotherapy-induced toxicity. This review focuses on the chemistry and analogues of silymarin, multiple possible molecular mechanisms, in vitro as well as in vivo anti-cancer activities, and studies on human clinical trials.
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            Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation.

            p90 ribosomal S6 kinase (RSK) is an important downstream effector of mitogen-activated protein kinase, but its biological functions are not well understood. We have now identified the first small-molecule, RSK-specific inhibitor, which we isolated from the tropical plant Forsteronia refracta. We have named this novel inhibitor SL0101. SL0101 shows remarkable specificity for RSK. The major determinant of SL0101-binding specificity is the unique ATP-interacting sequence in the amino-terminal kinase domain of RSK. SL0101 inhibits proliferation of the human breast cancer cell line MCF-7, producing a cell cycle block in G(1) phase with an efficacy paralleling its ability to inhibit RSK in intact cells. RNA interference of RSK expression confirmed that RSK regulates MCF-7 proliferation. Interestingly, SL0101 does not alter proliferation of a normal human breast cell line MCF-10A, although SL0101 inhibits RSK in these cells. We show that RSK is overexpressed in approximately 50% of human breast cancer tissue samples, suggesting that regulation of RSK has been compromised. Thus, we show that RSK has an unexpected role in proliferation of transformed cells and may be a useful new target for chemotherapeutic agents. SL0101 will provide a powerful new tool to dissect the molecular functions of RSK in cancer cells.
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              TRPV6 mediates capsaicin-induced apoptosis in gastric cancer cells--Mechanisms behind a possible new "hot" cancer treatment.

              Capsaicin is an organic compound in chili peppers which are consumed by over one quarter of the world's population daily. Studies have shown that capsaicin can induce apoptosis in some cancer cells by unknown mechanisms. In this study, both gastric cancer and normal epithelial cells were treated with capsaicin and examined for apoptosis by Annexin V binding. Our results showed that capsaicin induces apoptosis in both cells, although cancer cells are more susceptible. This susceptibility is dependent on the availability of TRPV6, a calcium-selective channel protein, as overexpression of TRPV6 in normal cells increased capsaicin-induced apoptosis and knockdown of TRPV6 in cancer cells suppressed this action. Our results further demonstrated that capsaicin increases mitochondrial permeability through activation of Bax and p53 in a JNK-dependent manner. (1) TRPV6, rather than TRPV1 (the well-known capsaicin receptor), mediates capsaicin-induced apoptosis in gastric cells; (2) abundance of TRPV6 in gastric cells determines their live or death under capsaicin treatment; and (3) capsaicin induces apoptosis by stabilization of p53 through JNK activation. Together, our data suggest that capsaicin may be a promising dietary candidate for cancer chemoprevention.
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                Author and article information

                Contributors
                Role: ND
                Role: ND
                Role: ND
                Role: ND
                Role: ND
                Journal
                rbfar
                Revista Brasileira de Farmacognosia
                Rev. bras. farmacogn.
                Sociedade Brasileira de Farmacognosia (Curitiba )
                1981-528X
                August 2011
                : 21
                : 4
                : 744-753
                Affiliations
                [1 ] Universidade Federal Rural de Pernambuco Brazil
                [2 ] Universidade Federal de Pernambuco Brazil
                [3 ] Universidade Federal de Pernambuco Brazil
                Article
                S0102-695X2011000400027
                7e95ed12-2797-40aa-b261-910bb09009d5

                http://creativecommons.org/licenses/by/4.0/

                History
                Product

                SciELO Brazil

                Self URI (journal page): http://www.scielo.br/scielo.php?script=sci_serial&pid=0102-695X&lng=en
                Categories
                PHARMACOLOGY & PHARMACY

                Pharmacology & Pharmaceutical medicine
                cancer,ethnopharmacology,medicinal plants
                Pharmacology & Pharmaceutical medicine
                cancer, ethnopharmacology, medicinal plants

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