Special Issue "Triterpenes and Triterpenoids"

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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (31 January 2013)

Special Issue Editor

Guest Editor
Prof. Dr. Vassilios Roussis
University of Athens, School of Pharmacy, Department of Pharmacognosy and Chemistry of Natural Products, Panepistimiopolis Zografou, GR 15771, Athens, Greece
E-Mail: roussis@pharm.uoa.gr
Phone: +30 210 7274 592
Fax: +30 210 7274 592
Interests: marine natural products; chemotaxonomy; chemical ecology

Special Issue Information

Submission

All papers should be submitted to molecules@mdpi.com with copy to the guest editor. To be published continuously until the deadline and papers will be listed together at the special websites.
Submitted papers should not have been previously published nor be currently under consideration for publication elsewhere. All papers are refereed through a peer review process. A guide for authors, sample copies and other relevant information for submitting papers are available on the Instructions for Authors page. Molecules is an international peer-reviewed monthly journal published by MDPI.
Please visit the Instructions for Authors page before submitting a paper. Open Access publication fees are 1800 CHF per paper. English correction fees (250 CHF) will be added in certain cases (2050 CHF per paper for those papers that require extensive additional formatting and/or English corrections.).

Keywords

  • natural product chemistry and medicinal chemistry of triterpenes and triterpeniods
  • squalene
  • material science
  • biomaterials
  • bioassay
  • pharmacological activity
  • medicinal plant
  • herb
  • herbal medicine
  • chinese medicine
  • fungus
  • mushroom

Published Papers (36 papers)

by , , , , , , ,  and
Molecules 2013, 18(9), 10095-10107; doi:10.3390/molecules180910095
Received: 29 May 2013; in revised form: 8 August 2013 / Accepted: 12 August 2013 / Published: 22 August 2013
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by ,  and
Molecules 2013, 18(7), 7886-7909; doi:10.3390/molecules18077886
Received: 16 February 2013; in revised form: 10 June 2013 / Accepted: 27 June 2013 / Published: 4 July 2013
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by
Molecules 2013, 18(4), 4803-4815; doi:10.3390/molecules18044803
Received: 16 February 2013; in revised form: 7 April 2013 / Accepted: 19 April 2013 / Published: 22 April 2013
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by , , , , , , , , ,  and
Molecules 2013, 18(4), 4389-4402; doi:10.3390/molecules18044389
Received: 8 February 2013; in revised form: 1 April 2013 / Accepted: 9 April 2013 / Published: 15 April 2013
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by , ,  and
Molecules 2013, 18(4), 4267-4281; doi:10.3390/molecules18044267
Received: 31 January 2013; in revised form: 3 April 2013 / Accepted: 3 April 2013 / Published: 11 April 2013
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by , ,  and
Molecules 2013, 18(4), 4247-4256; doi:10.3390/molecules18044247
Received: 4 February 2013; in revised form: 7 April 2013 / Accepted: 8 April 2013 / Published: 11 April 2013
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by , , ,  and
Molecules 2013, 18(4), 4054-4080; doi:10.3390/molecules18044054
Received: 6 March 2013; in revised form: 29 March 2013 / Accepted: 1 April 2013 / Published: 5 April 2013
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by  and
Molecules 2013, 18(4), 4002-4017; doi:10.3390/molecules18044002
Received: 18 February 2013; in revised form: 19 March 2013 / Accepted: 27 March 2013 / Published: 4 April 2013
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by , , , , , , , ,  and
Molecules 2013, 18(4), 3725-3732; doi:10.3390/molecules18043725
Received: 1 February 2013; in revised form: 19 March 2013 / Accepted: 20 March 2013 / Published: 25 March 2013
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by , , , , ,  and
Molecules 2013, 18(3), 3615-3629; doi:10.3390/molecules18033615
Received: 4 February 2013; in revised form: 14 March 2013 / Accepted: 15 March 2013 / Published: 21 March 2013
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by , , , ,  and
Molecules 2013, 18(3), 3250-3265; doi:10.3390/molecules18033250
Received: 31 January 2013; in revised form: 27 February 2013 / Accepted: 6 March 2013 / Published: 13 March 2013
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by , ,  and
Molecules 2013, 18(3), 3060-3071; doi:10.3390/molecules18033060
Received: 27 December 2012; in revised form: 25 February 2013 / Accepted: 27 February 2013 / Published: 7 March 2013
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by , , , , ,  and
Molecules 2013, 18(3), 2934-2941; doi:10.3390/molecules18032934
Received: 14 January 2013; in revised form: 7 February 2013 / Accepted: 27 February 2013 / Published: 4 March 2013
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by , , ,  and
Molecules 2013, 18(3), 2726-2753; doi:10.3390/molecules18032726
Received: 28 November 2012; in revised form: 16 February 2013 / Accepted: 18 February 2013 / Published: 1 March 2013
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by , , , , ,  and
Molecules 2013, 18(3), 2598-2610; doi:10.3390/molecules18032598
Received: 21 January 2013; in revised form: 7 February 2013 / Accepted: 18 February 2013 / Published: 27 February 2013
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by , , , ,  and
Molecules 2013, 18(3), 2589-2597; doi:10.3390/molecules18032589
Received: 20 December 2012; in revised form: 1 February 2013 / Accepted: 18 February 2013 / Published: 26 February 2013
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by , , , ,  and
Molecules 2013, 18(3), 2539-2548; doi:10.3390/molecules18032539
Received: 12 December 2012; in revised form: 22 January 2013 / Accepted: 19 February 2013 / Published: 26 February 2013
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by  and
Molecules 2013, 18(2), 1405-1417; doi:10.3390/molecules18021405
Received: 11 December 2012; in revised form: 28 December 2012 / Accepted: 5 January 2013 / Published: 24 January 2013
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by , , , , , ,  and
Molecules 2013, 18(1), 1262-1269; doi:10.3390/molecules18011262
Received: 3 December 2012; in revised form: 1 January 2013 / Accepted: 7 January 2013 / Published: 21 January 2013
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by , , , , , , , , , ,  and
Molecules 2013, 18(1), 1053-1062; doi:10.3390/molecules18011053
Received: 19 November 2012; in revised form: 18 December 2012 / Accepted: 21 December 2012 / Published: 15 January 2013
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by , , ,  and
Molecules 2012, 17(12), 14795-14809; doi:10.3390/molecules171214795
Received: 9 November 2012; in revised form: 20 November 2012 / Accepted: 6 December 2012 / Published: 11 December 2012
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by , , , , , ,  and
Molecules 2012, 17(11), 13439-13456; doi:10.3390/molecules171113439
Received: 12 September 2012; in revised form: 5 November 2012 / Accepted: 7 November 2012 / Published: 12 November 2012
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by , , , , , ,  and
Molecules 2012, 17(10), 12197-12205; doi:10.3390/molecules171012197
Received: 14 September 2012; in revised form: 9 October 2012 / Accepted: 10 October 2012 / Published: 17 October 2012
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by , , , , ,  and
Molecules 2012, 17(10), 11721-11728; doi:10.3390/molecules171011721
Received: 31 August 2012; in revised form: 24 September 2012 / Accepted: 24 September 2012 / Published: 1 October 2012
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by ,  and
Molecules 2012, 17(9), 10816-10830; doi:10.3390/molecules170910816
Received: 11 July 2012; in revised form: 2 August 2012 / Accepted: 21 August 2012 / Published: 10 September 2012
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by  and
Molecules 2009, 14(11), 4690-4706; doi:10.3390/molecules14114690
Received: 22 September 2009; in revised form: 5 November 2009 / Accepted: 10 November 2009 / Published: 18 November 2009
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by  and
Molecules 2009, 14(10), 3922-3941; doi:10.3390/molecules14103922
Received: 30 June 2009; in revised form: 15 September 2009 / Accepted: 17 September 2009 / Published: 9 October 2009
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by
Molecules 2009, 14(9), 3286-3312; doi:10.3390/molecules14093286
Received: 13 August 2009; in revised form: 25 August 2009 / Accepted: 31 August 2009 / Published: 1 September 2009
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by  and
Molecules 2009, 14(8), 2959-2975; doi:10.3390/molecules14082959
Received: 24 June 2009; in revised form: 21 July 2009 / Accepted: 6 August 2009 / Published: 10 August 2009
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by , , ,  and
Molecules 2009, 14(7), 2373-2393; doi:10.3390/molecules14072373
Received: 27 May 2009; in revised form: 23 June 2009 / Accepted: 2 July 2009 / Published: 3 July 2009
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by , , ,  and
Molecules 2009, 14(6), 2016-2031; doi:10.3390/molecules14062016
Received: 22 April 2009; in revised form: 26 May 2009 / Accepted: 3 June 2009 / Published: 4 June 2009
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by , , , ,  and
Molecules 2009, 14(4), 1639-1651; doi:10.3390/molecules14041639
Received: 17 March 2009; in revised form: 15 April 2009 / Accepted: 22 April 2009 / Published: 24 April 2009
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by , , , ,  and
Molecules 2009, 14(2), 598-607; doi:10.3390/molecules14020598
Received: 20 November 2008; in revised form: 10 January 2009 / Accepted: 21 January 2009 / Published: 4 February 2009
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by ,  and
Molecules 2009, 14(1), 540-554; doi:10.3390/molecules14010540
Received: 8 January 2009; in revised form: 19 January 2009 / Accepted: 21 January 2009 / Published: 23 January 2009
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by ,  and
Molecules 2008, 13(12), 3224-3235; doi:10.3390/molecules13123224
Received: 31 October 2008; in revised form: 10 December 2008 / Accepted: 17 December 2008 / Published: 18 December 2008
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by , , ,  and
Molecules 2008, 13(11), 2717-2728; doi:10.3390/molecules13112717
Received: 22 September 2008; in revised form: 16 October 2008 / Accepted: 20 October 2008 / Published: 1 November 2008
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Manuscript ID: molecules-triterp-20080922-es-Martin
Type of Paper: Article
Title: Clavaric acid and fasciculic acid: Biosynthesis and Molecular Genetics
Authors: Juan F. Martín 1,2 and Ramiro P. Godio 2
Affiliations: 1 Área de Microbiología, Facultad de Ciencias Biológicas y Ambientales, Universidad de León, Campus de Vegazana, s/n. 24071 León, Spain
2 Instituto de Biotecnología de León (INBIOTEC), Avda. Real, 1. 24006 León, Spain; E-Mail: jf.martin@unileon.es
Abstract: Clavaric acid is a potent antitumor agent produced by the mushroom-forming basidiomycete Hypholoma sublateritium. Clavaric acid is structurally similar to fasciculic acid, a related triterpenoid produced by Hypholoma fasciculare that is described as a calmodulin inhibitor.
These two compounds are derived from squalene by the action of enzymes that convert squalene to 2,3-dioxidesqualene and this intermediate to clavarinone, a direct precursor of clavaric acid or fasciculic acid. One of these enzymes, the squalene oxidase, is common for primary metabolism (ergosterol biosynthesis) and secondary metabolism, whereas the late enzymatic steps are specific for the biosynthesis of clavaric acid and fasciculic acid. Molecular genetics studies allowed us to clone and characterise the genes encoding these enzymes. These studies have provided a considerable insight into the biosynthesis of triterpenoids in fungi, providing new potent pharmacologically-active compounds. Squalene epoxidases and oxidosqualene cyclases with modified consensus motifs in their active centers appear to play an important role in determining the oxidation and modification reactions that may result in specific secondary metabolites.

Manuscript ID: molecules-triterp-20080930-us-Nes
Type of Paper: Article
Title: Steroidal Triterpenes: Design of Substrate-based Inhibitors of Ergosterol and Sitosterol Synthesis
Authors: Jialin Liu and W. David Nes
Affiliation: Department of Chemistry and Biochemistry, Texas Tech University, Lubbock, TX 79409, USA; E-Mail: WDNES@aol.com
Abstract: This article reviews the design and study, in our own laboratory and in other laboratories, of new steroidal triterpenes with a modified lanosterol or cycloartenol frame. These compounds, along with a number of known analogs with the cholestane skeleton, have been evaluated as reversible or irreversible inhibitors of sterol C-24 methyltransferase (SMT) from plants, fungi and protozoa. The SMT catalyzes the C24-methylation reaction involved with the introduction of the C24-methyl group of ergosterol and the C24-ethyl group of sitosterol, cholesterol surrogates that function as essential membrane inserts in many photosynthetic and non-photosynthetic eukaryotic organisms. Sterol side chains constructed with a nitrogen, sulfur, bromine or fluorine atom or altered to possess a methylene cyclopropane group, or elongated to include terminal double or triple bonds are shown to exhibit different in vitro activities toward the SMT which are mirrored in the inhibition potencies detected in the growth response of treated cultured human and plant cells or microbes. Several of the substrate-based analogs surveyed here appear to be taxa-specific compounds acting as mechanism-based inactivators of the SMT, a crucial enzyme not synthesized by animals. Possible mechanisms for the inactivation process and generation of novel products catalyzed by the variant SMTs are discussed.

Manuscript ID: Molecules-triterp-20081024-Akhmetova
Type of Paper: Review
Title: Pentacyclic Triterpenes and Their Synthetic Transformations
Authors: Vnira R. Akhmetova and Elvira R. Shakurova
Affiliciation: Institute of Petrochemistry and Catalysis, Russian Academy of Sciences, 141 prosp. Oktyabrya, 450075, Ufa, Russian Faderation; E-Mails: vnirara@mail.ru, shakurovaer@mail.ru,ink@anrb.ru
Abstract: Literary data on polycyclic triterpenoids and own experimental results on separation, X-ray researches and synthetic transformations of pentacyclic triterpenoids from Scotch thistle Onopordum acanthium L. growing in the south of the Ural mountains (Russia) are generalized.
Triterpenoids rather widespread occure in nature. Their molecules containing six isoprenoid links, are predecessors of steroids, both in animals, and in plant organisms. Practically all plants produce tetra-and pentacyclic triterpenes metabolites with various types of a carbon skeleton. Among pentacyclic triterpenes 10 structural types are revealed. In a medical practice pentacyclic triterpenoids are already successfully applied in composition of regulators of cardiovascular system, antibacterial and anti-AIDS preparations, and in glycosylate form (saponin) in composition of hypochilesterinemic preparations and for hemosorption superfluous serum cholesterin from blood. Complete biological potential of polycyclic triterpenoids as medical products is still not studied. In this review there were summaried the various types of plant pentacyclic triterpenoids that have been described in the literature, such as oleanane, ursane, taraxastane and lupan (section 1); information about on biological activity (section 2), and also information available in the literature about chemical modifications triterpenoids and biological activity of their synthetic analogues (section 3). In the present review literary information for the past of 15-20 years is observed. The bibliographic list contains about 150 titles.

Type of Paper: Review
Title: Bioactivities of Plant Triterpenoids
Authors: Horacio Bach 1, Zaida N. Juarez 2 and Luis R. Hernandez 3
Affiliations: 1 Department of Medicine, Division of Infectious Diseases, University of British Columbia, 410-2660 Oak Street, V6G 3Z6, Vancouver, Canada
2 Departamento de Ciencias Biológicas, Facultad Biotecnoambiental, Universidad Popular Autónoma del Estado de Puebla, 72410, Puebla, Mexico
3 Departamento de Ciencias Químico Biológicas, Universidad de las Américas Puebla, Ex Hacienda Santa Catarina Mártir s/n, 72810, Cholula, Puebla, Mexico
Abstract: Terpenoids are secondary metabolites found in abundance in plants. Many of these compounds have been approved for use in human medicine, but a massive arsenal of these compounds is still unexploited constituting an attractive source of potential medicines to be developed. In this comprehensive review, we plan to summarize the bioactivities of triterpenoid structures isolated from plants including but not limited to their antimicrobial, antiparasitic, anti-inflammatory, and anticancer activities. We propose to compare and analyze the structure of these compounds and their relationship to their bioactivities. In this review we plan to analyze the available literature without any emphasis on a specific genus or plant family.

Type of Paper: Review
Title: The Protostanes
Authors: Ming Zhao, Tanja Goedecke, Jordan Gunn, Jin-Ao Duan and Chun-Tao Che
Affiliations: 1 The University of Illinois at Chicago, IL 60612, USA
2 Nanjing University of Traditional Chinese Medicine, 210046 Jiangsu, China
Abstract: Protostanes belong to a small group of tetracyclic triterpenes, whose distribution is primarily limited to the genus Alisma (Alismataceae), yet examples of protostanes can also be found in Lobelia (Lobeliaceae), Garcinia (Clusiaceae), and Leucas (Lamiaceae). To date, a total of about 60 protostane derivatives are known. A number of bio-activities have been reported for this group of natural products, such as improving lipotropism, liver protection, anti-viral activity against hepatitis B and HIV-I virus, anti-tumor activity, and the reversal of multidrug resistance in cancer cells. This review covers the plant sources of protostane derivatives, their structural and spectroscopic properties, and biological activities. The biosynthesis of this compound class is also discussed and a refined biogenetic pathway is proposed.

Type of Paper: Review
Title: Ursolic Acid Derivatives from Bangladeshi Medicinal Plant, Saurauja roxburghii: Isolation, Oxidative Derivatization, and Cytotoxic Activity against A431 and C6 Glioma Cell Lines
Authors: Kishor Mazumder 1,3, Katsunori Tanaka 2,3 and Koichi Fukase 3
Affiliations: 1 Department of Pharmacy, University of Science and Technology Chittagong, Japan
2 RIKEN Advanced Science Institute, 3) Department of Chemistry, Graduate School of Science, Osaka University, Japan
Abstract: Ursene-type pentacyclic triterpenes, including the ursolic acid, corosolic acid, and a new ursene-type pentacyclic triterpene, 7,24-dihydroxyl ursolic acid, were isolated from the methanolic extract of the leaves of the Bangladeshi medicinal plant, Saurauja roxburghii, a higher plant indigenous to South East Asia and some part of North America. They were tested for the cytotoxicity against C6 rat glioma and A431 human skin carcinoma cell lines. Although they have the same ursene-type pentacyclic triterpene core structure, the position and numbers of hydroxyls on the terpene structure significantly affected the activity and the selectivity to the cell lines. Derivatization of ursolic acid was then investigated by the oxidation with dioxoruthenium (VI) tetraphenyl porphyrins. Oxidation selectivity on the terpene structure was modulated by the auxiliaries introduced on the tetraphynyl porphyrin. Oxidative modifications of ursolic acid affected the cytotoxic activity against C6 and A431 tumor cell lines.

Type of the paper: Review
Title: Steroidal Triterpenes of Cholesterol Synthesis
Authors: Jure Acimovic 1 and Damjana Rozman 2*
Affiliations: 1 Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Vrazov trg 2, SI-1000 Ljubljana, Slovenia
2 Centre for Functional Genomics and Bio-Chips, Faculty of Medicine, University of Ljubljana, Zaloška 4, SI-1000 Ljubljana, Slovenia
Abstract: Cholesterol synthesis is a ubiquitous and housekeeping metabolic pathway that leads to cholesterol, an essential structural component of mammalian cell membranes, required for proper membrane permeability and fluidity. The last part of the pathway consists of steroidal triterpenes with cholestane ring structure. It starts by conversion of acyclic squalene into lanosterol, the first sterol intermediate of the pathway, followed by production of 14 structurally very similar steroidal triterpene molecules in over 10 complex enzyme reactions. Due to structural similarities of sterol intermediates and the broad substrate specificity of enzymes involved (especially sterol-Δ24-reductase DHCR24) the exact sequence of the reactions between lanosterol and cholesterol remains undefined. This article reviews all hitherto known structures of post-squalene steroidal triterpenes of cholesterol synthesis, their biological roles and the enzymes responsible for their synthesis. Furthermore, it summarises kinetic parameters of enzymes (kcat and Km) and sterol intermediates concentrations from various tissues. Due to complexity of the post-squalene cholesterol synthesis, future studies will require a comprehensive meta-analysis of the pathway to elucidate exact reaction sequence in different tissues, physiological or disease conditions. A major reasons for the standstill of detailed late cholesterol synthesis research is lack of several steroidal triterpene standards. We aid to this efforts by summarizing commercial and laboratory standards, referring also to chemical synthesis and/or biotechnological production.

Type of the paper: Article
Title: Telomerase Reverse Transcriptase (TERT) is a Therapeutic Target of Oleanane Triterpenoid CDDO-Me in Prostate Cancer
Authors: Yongbo Liu1, Xiaohua Gao1, Dorrah Deeb1, Ali S. Arbab2 and Subhash C. Gautam1,*
Affiliations: 1 Departments of Surgery, Henry Ford Health System, Detroit, Michigan, USA
2 Department of Radiology, Henry Ford Health System, Detroit, Michigan, USA
Abstract: CDDO-Me (methyl-2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate) is a synthetic triterpenoid derived from oleanolic acid with strong antiprolifertive and proapoptotic activities. However, effect of CDDO-Me on human telomerase reverse transcriptase (hTERT) and its telomerase activity in cancer cells have received little consideration. The present study investigated the role of hTERT in mediating the anticancer activity of CDDO-Me in prostate cancers. The inhibition of cell proliferation and induction of apoptosis by low doses of CDDO-Me in human prostate cancer cell lines LNCaP and PC-3 was associated with the inhibition of hTERT gene expression, hTERT telomerase activity and a number of proteins that regulate hTERT transcriptionally and post-translationally. Furthermore, ablation of hTERT protein increased the sensitivity of cancer cells to CDDO-Me, whereas its overexpression rendered cells resistant to CDDO-Me. In addition, the inhibition of progression of preneoplastic lesions (i.e. low and high-grade prostate intraepithelial neoplasms, PINs) to adenocarcinoma of the prostate by CDDO-Me in transgenic TRAMP mice was associated with significant decrease in TERT and its regulatory proteins in the prostate gland. This study demonstrated potent anticancer activity of CDDO-Me against prostate cancer in vitro and in vivo and provided evidence that telomerase is a potential target of CDDO-Me for the prevention and treatment of prostate cancer.

Last update: 4 February 2013

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