title: Betulinic acid in complex with a gamma-cyclodextrin derivative decreases proliferation and in vivo tumor development of non-metastatic and metastatic B164A5 cells.
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.
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. codrutasoica@umft.ro.
authors.forename: Codruta
authors.initials: C
authors.lastname: Soica
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. corina.danciu@umft.ro.
authors.forename: Corina
authors.initials: C
authors.lastname: Danciu
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. savoiugema@umft.ro.
authors.forename: Germaine
authors.initials: G
authors.lastname: Savoiu-Balint
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. fborcan@yahoo.com.
authors.forename: Florin
authors.initials: F
authors.lastname: Borcan
authors.affiliation: Institute of Pharmaceutical Technology, University of Szeged, 6 Eotvos Ut., H-6720 Szeged, Hungary. rita-techno@freemail.hu.
authors.forename: Rita
authors.initials: R
authors.lastname: Ambrus
authors.affiliation: Department of Pharmacodynamics and Biopharmacy, University of Szeged, 6 Eotvos Str., H-6720 Szeged, Hungary. zupko@pharm.u-szeged.hu.
authors.forename: Istvan
authors.initials: I
authors.lastname: Zupko
authors.affiliation: Faculty of Medicine, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. florinabojin@umft.ro.
authors.forename: Florina
authors.initials: F
authors.lastname: Bojin
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. dorina_gheorgheosu@yahoo.com.
authors.forename: Dorina
authors.initials: D
authors.lastname: Coricovac
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. sorinaciurlea@yahoo.com.
authors.forename: Sorina
authors.initials: S
authors.lastname: Ciurlea
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. stefana.feflea@gmail.com.
authors.forename: Stefana
authors.initials: S
authors.lastname: Avram
authors.affiliation: Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. cadehelean@umft.ro.
authors.forename: Cristina Adriana
authors.initials: CA
authors.lastname: Dehelean
authors.affiliation: Faculty of Medicine, Vasile Goldis University, 310045 Arad, Romania. olariu.teodora@yahoo.com.
authors.forename: Teodora
authors.initials: T
authors.lastname: Olariu
authors.affiliation: Faculty of Medicine, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania. matusz@umft.ro.
authors.forename: Petru
authors.initials: P
authors.lastname: Matusz
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000627:therapeutic use; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D008545:Melanoma / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D008810:Mice, Inbred C57BL; D053978:Pentacyclic Triterpenes; D012995:Solubility; D014315:Triterpenes / Q000008:administration & dosage* / Q000627:therapeutic use; D014961:X-Ray Diffraction; D047408:gamma-Cyclodextrins / Q000737:chemistry*; D000094062:Betulinic Acid
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D047408:gamma-Cyclodextrins; C023792:gamma-cyclodextrin; D000094062:Betulinic Acid