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      Anthracenedione Derivatives as Anticancer Agents Isolated from Secondary Metabolites of the Mangrove Endophytic Fungi

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          Abstract

          In this article, we report anticancer activity of 14 anthracenedione derivatives separated from the secondary metabolites of the mangrove endophytic fungi Halorosellinia sp. (No. 1403) and Guignardia sp. (No. 4382). Some of them inhibited potently the growth of KB and KBv200 cells, among which compound 6 displayed strong cytotoxicity with IC 50 values of 3.17 and 3.21 μM to KB and KBv200 cells, respectively. Furthermore, we demonstrate that the mechanism involved in the apoptosis induced by compound 6 is probably related to mitochondrial dysfunction. Additionally, the structure-activity relationships of these compounds are discussed.

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          Natural products as leads to anticancer drugs.

          M Gordaliza (2007)
          Throughout history, natural products have afforded a rich source of compounds that have found many applications in the fields of medicine, pharmacy and biology. Within the sphere of cancer, a number of important new commercialised drugs have been obtained from natural sources, by structural modification of natural compounds, or by the synthesis of new compounds, designed following a natural compound as model. The search for improved cytotoxic agents continues to be an important line in the discovery of modern anticancer drugs. The huge structural diversity of natural compounds and their bioactivity potential have meant that several products isolated from plants, marine flora and microorganisms can serve as "lead" compounds for improvement of their therapeutic potential by molecular modification. Additionally, semisynthesis processes of new compounds, obtained by molecular modification of the functional groups of lead compounds, are able to generate structural analogues with greater pharmacological activity and with fewer side effects. These processes, complemented with high-throughput screening protocols, combinatorial chemistry, computational chemistry and bioinformatics are able to afford compounds that are far more efficient than those currently used in clinical practice. Combinatorial biosynthesis is also applied for the modification of natural microbial products. Likewise, advances in genomics and the advent of biotechnology have improved both the discovery and production of new natural compounds.
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            Marine natural products as anticancer drugs.

            William Gerwick, Eric Andrianasolo, Kerry McPhail … (2005)
            The chemical and biological diversity of the marine environment is immeasurable and therefore is an extraordinary resource for the discovery of new anticancer drugs. Recent technological and methodologic advances in structure elucidation, organic synthesis, and biological assay have resulted in the isolation and clinical evaluation of various novel anticancer agents. These compounds range in structural class from simple linear peptides, such as dolastatin 10, to complex macrocyclic polyethers, such as halichondrin B; equally as diverse are the molecular modes of action by which these molecules impart their biological activity. This review highlights several marine natural products and their synthetic derivatives that are currently undergoing clinical evaluation as anticancer drugs.
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              Lapatinib (Tykerb, GW572016) reverses multidrug resistance in cancer cells by inhibiting the activity of ATP-binding cassette subfamily B member 1 and G member 2.

              Robert Robey, Yan Huang, Suresh Ambudkar … (2008)
              Lapatinib is active at the ATP-binding site of tyrosine kinases that are associated with the human epidermal growth factor receptor (Her-1 or ErbB1) and Her-2. It is conceivable that lapatinib may inhibit the function of ATP-binding cassette (ABC) transporters by binding to their ATP-binding sites. The aim of this study was to investigate the ability of lapatinib to reverse tumor multidrug resistance (MDR) due to overexpression of ABC subfamily B member 1 (ABCB1) and ABC subfamily G member 2 (ABCG2) transporters. Our results showed that lapatinib significantly enhanced the sensitivity to ABCB1 or ABCG2 substrates in cells expressing these transporters, although a small synergetic effect was observed in combining lapatinib and conventional chemotherapeutic agents in parental sensitive MCF-7 or S1 cells. Lapatinib alone, however, did not significantly alter the sensitivity of non-ABCB1 or non-ABCG2 substrates in sensitive and resistant cells. Additionally, lapatinib significantly increased the accumulation of doxorubicin or mitoxantrone in ABCB1- or ABCG2-overexpressing cells and inhibited the transport of methotrexate and E(2)17betaG by ABCG2. Furthermore, lapatinib stimulated the ATPase activity of both ABCB1 and ABCG2 and inhibited the photolabeling of ABCB1 or ABCG2 with [(125)I]iodoarylazidoprazosin in a concentration-dependent manner. However, lapatinib did not affect the expression of these transporters at mRNA or protein levels. Importantly, lapatinib also strongly enhanced the effect of paclitaxel on the inhibition of growth of the ABCB1-overexpressing KBv200 cell xenografts in nude mice. Overall, we conclude that lapatinib reverses ABCB1- and ABCG2-mediated MDR by directly inhibiting their transport function. These findings may be useful for cancer combinational therapy with lapatinib in the clinic.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Mar Drugs
                Journal ID (publisher-id): MD
                Title: Marine Drugs
                Publisher: Molecular Diversity Preservation International
                ISSN (Electronic): 1660-3397
                Publication date Collection: 2010
                Publication date (Electronic): 23 April 2010
                Volume: 8
                Issue: 4
                Pages: 1469-1481
                Affiliations
                [1 ] State Key Laboratory for Oncology in South China, Cancer Center, Sun Yat-Sen University, Guangzhou, 510060, China; E-Mails: jianyez2003@ 123456yahoo.com.cn (J.Z.); sohutly@ 123456163.com (L.T.); liangyju@ 123456mail.sysu.edu.cn (Y.L.); chlm78@ 123456yahoo.com.cn (L.C.); myjgj_77@ 123456163.com (Y.M.); lesley860221@ 123456163.com (L.Z.); wangfang0203@ 123456163.com (F.W.)
                [2 ] School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou, 510275, China
                [3 ] School of Pharmacy, The Chinese University of Hong Kong, Hong Kong, China; E-Mail: kennethto@ 123456cuhk.edu.hk (K.K.W.T.)
                Author notes
                *Authors to whom correspondence should be addressed; E-Mails: Fulw@ 123456mail.sysu.edu.cn (L.F.); cesshzhg@ 123456mail.sysu.edu.cn (Z.S.); Tel.: +86-20-87343163; Fax: +86-20-87343170.
                Article
                Publisher ID: marinedrugs-08-01469
                DOI: 10.3390/md8041469
                PMC ID: 2866493
                PubMed ID: 20479985
                SO-VID: ecf44a68-849e-4157-ae4d-ece01f70addf
                Copyright © © 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland
                License:

                This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                Date received : 12 March 2010
                Date revision received : 1 April 2010
                Date accepted : 21 April 2010
                Categories
                Subject: Article

                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: apoptosis,anticancer,structure-activity relationship,mangrove endophytic fungi,anthracenedione derivatives
                Data availability:
                ScienceOpen disciplines: Pharmacology & Pharmaceutical medicine
                Keywords: apoptosis, anticancer, structure-activity relationship, mangrove endophytic fungi, anthracenedione derivatives

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