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      Betulinic Acid in Complex with a Gamma-Cyclodextrin Derivative Decreases Proliferation and in Vivo Tumor Development of Non-Metastatic and Metastatic B164A5 Cells

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          Abstract

          Betulinic acid, a very promising anti-melanoma agent, has very low water solubility that causes low bioavailability. To overcome this inconvenience, a highly water-soluble cyclodextrin was used (octakis-[6-deoxy-6-(2-sulfanyl ethanesulfonic acid)]-γ-cyclodextrin). The complex was physico-chemically analyzed using differential scanning calorimetry (DSC), X-ray and scanning electron microscopy (SEM) methods and then in vitro tested for its antiproliferative activity by the MTT assay and by cell cycle analysis. Finally, the complex was tested in vivo using an animal model of murine melanoma developed in C57BL/6J mice, where it caused a reduction in tumor volume and weight. The study revealed the beneficial influence of betulinic acid inclusion into the cyclodextrin in terms of antiproliferative activity and in vivo tumor development.

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          Pharmacological properties of the ubiquitous natural product betulin.

          Sami Alakurtti, S Koskimies, Jari Yli-Kauhaluoma … (2006)
          Betulin (lup-20(29)-ene-3beta,28-diol) is an abundant naturally occurring triterpene and it is found predominantly in bushes and trees forming the principal extractive (up to 30% of dry weight) of the bark of birch trees. Presently, there is no significant use for this easily isolable compound, which makes it a potentially important raw material for polymers and a precursor of biologically active compounds. Betulin can be easily converted to betulinic acid, which possesses a wide spectrum of biological and pharmacological activities. Betulinic acid has antimalarial and anti-inflammatory activities. Betulinic acid and its derivatives have especially shown anti-HIV activity and cytotoxicity against a variety of tumor cell lines comparable to some clinically used drugs. A new mechanism of action has been confirmed for some of the most promising anti-HIV derivatives, which makes them potentially useful additives to the current anti-HIV therapy. Betulinic acid is specifically cytotoxic to several tumor cell lines by inducing apoptosis in cells. Moreover, it is non-toxic up to 500 mg/kg body weight in mice. The literature concerning derivatization of betulin for structure-activity relationship (SAR) studies and its pharmacological properties is reviewed.
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            Selective cytotoxicity of betulinic acid on tumor cell lines, but not on normal cells.

            Valentina Zuco, Rosanna Supino, Sabina Righetti … (2002)
            Betulinic acid is a triterpene with selective cytotoxicity against melanoma, neuroectodermal and malignant brain tumor cell lines. In this study the betulinic acid activity was evaluated, in comparison with doxorubicin, on different human neoplastic and non-neoplastic cell lines and on proliferating normal lymphocytes. Growth inhibition was evident in all the neoplastic cell lines independently on p53 status and histotype. Antiproliferative activity of betulinic acid was related to a cytotoxic effect on two p53 wild-type and on one p53 mutant cell lines and to a cytostatic effect on one p53 mutant melanoma clone. At the same concentrations, normal cells were unaffected indicating a selective effect of this agent. A cytotoxic activity of doxorubicin was evident on all the tested systems. In vivo experiments, performed on one of these cell lines, confirmed the antineoplastic activity of this drug. These data support further preclinical studies of betulinic acid not confined to melanoma and neuroectodermal tumors independently of p53 status.
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              Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

              Wei Xu, Peixue Ling, Tianmin Zhang (2013)
              Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Int J Mol Sci
                Journal ID (iso-abbrev): Int J Mol Sci
                Journal ID (publisher-id): ijms
                Title: International Journal of Molecular Sciences
                Publisher: Molecular Diversity Preservation International (MDPI)
                ISSN (Electronic): 1422-0067
                Publication date Collection: May 2014
                Publication date (Electronic): 09 May 2014
                Volume: 15
                Issue: 5
                Pages: 8235-8255
                Affiliations
                [1 ]Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania; E-Mails: codrutasoica@ 123456umft.ro (C.S.); fborcan@ 123456yahoo.com (F.B.); dorina_gheorgheosu@ 123456yahoo.com (D.C.); sorinaciurlea@ 123456yahoo.com (S.C.); stefana.feflea@ 123456gmail.com (S.A.); cadehelean@ 123456umft.ro (C.A.D.)
                [2 ]Institute of Pharmaceutical Technology, University of Szeged, 6 Eotvos Ut., H-6720 Szeged, Hungary; E-Mail: rita-techno@ 123456freemail.hu
                [3 ]Department of Pharmacodynamics and Biopharmacy, University of Szeged, 6 Eotvos Str., H-6720 Szeged, Hungary; E-Mail: zupko@ 123456pharm.u-szeged.hu
                [4 ]Faculty of Medicine, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania; E-Mails: florinabojin@ 123456umft.ro (F.B.); matusz@ 123456umft.ro (P.M.)
                [5 ]Faculty of Medicine, Vasile Goldis University, 310045 Arad, Romania; E-Mail: olariu.teodora@ 123456yahoo.com
                Author notes
                [* ]Authors to whom correspondence should be addressed; E-Mails: corina.danciu@ 123456umft.ro (C.D.); savoiugema@ 123456umft.ro (G.S.-B.); Tel.: +40-744-648855 (C.D.); Fax: +40-256-226134 (C.D.).
                Article
                Publisher ID: ijms-15-08235
                DOI: 10.3390/ijms15058235
                PMC ID: 4057729
                PubMed ID: 24821543
                SO-VID: 11d826f9-8df4-43af-a08a-71fcba476887
                Copyright © © 2014 by the authors; licensee MDPI, 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 : 04 January 2014
                Date revision received : 08 April 2014
                Date accepted : 10 April 2014
                Categories
                Subject: Article

                ScienceOpen disciplines: Molecular biology
                Keywords: betulinic acid,dsc,x-ray diffraction,sem,mtt test,c57bl/6j mice
                Data availability:
                ScienceOpen disciplines: Molecular biology
                Keywords: betulinic acid, dsc, x-ray diffraction, sem, mtt test, c57bl/6j mice

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