|Address:||Department of Life and Environmental Sciences,
Drug Sciences Section, Faculty of Biology and Pharmacy,
Via Ospedale 72, 09124 Cagliari, Italy.
|Phone:||+39 070 675 8979|
Assistant professor in Medicinal Chemistry at the Department of Life and Environmental Sciences – Drug Sciences Section, University of Cagliari.
- Degree: graduated at the “University of Cagliari”, “Faculty of Pharmacy”, Italy on the 12 March 1993 in Chemistry and Pharmaceutical Technology with 110/110 points, summa cum laude.
- PhD: 1995-97 doctoral studies in “Medicinal Chemistry” at University of Cagliari.
- School of specialization: specialist in Industrial Pharmacy, University of Pavia, Italy, awarded in September 2000.
- Post Doc: 1997-1999: postdoctoral position in the group of Prof. Leonardo Bonsignore at the Dipartimento Farmaco Chimico Tecnologico, University of Cagliari.
- Post Doc: 2000-2001: postdoctoral position in the group of Prof. Dr. Otto Sticher, Pharmacognosy and Phytochemistry, Institute of Pharmaceutical Sciences, Department of Applied BioSciences, ETH Zurich, Switzerland
His research focuses on isolation, structure elucidation and biological screenings of natural products from medicinal plants and marine organisms as well as on synthesis of new pharmacophores starting from natural bioactive products. In particular, he is interested in metabolites which show cytotoxic/antitumor activity, interaction with cannabinoid and opioid receptors, and anti HIV activity. The detection of biologically active metabolites is usually carried out by a bioactivity-guided fractionation of the extracts. Various chromatographic techniques are utilised for the isolation of the pure compounds from the extracts whose structures are elucidated mainly by Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS).
In particular, he has a long experience in chromatographic techniques, such as column chromatography, vacuum liquid chromatography and semipreparative HPLC and a good knowledge in NMR experiments devoted to the structure elucidation of natural compounds including one dimensional (1H and 13C NMR, APT) and two dimensional NMR (COSY, TOCSY, HSQC, HSQC-TOCSY, HMBC, NOESY, ROESY).
Publications from 2008 to 2015
- New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII. R. Meleddu, E. Maccioni, S. Distinto, G.Bianco, C. Melis, S. Alcaro, F. Cottiglia, M. Ceruso,C.T. Supuran. Bioorganic & Medicinal Chemistry Letters (2015), in press, doi: 10.1016/j.bmcl.2015.05.076.
- Methoxyflavones from Stachys glutinosa with Binding Affinity to Opioid Receptors: In Silico, in Vitro, and in Vivo Studies. S. Ruiu, N. Anzani, A. Orrù, C. Floris, P. Caboni, S. Alcaro, E. Maccioni, S. Distinto, F. Cottiglia. Journal of Natural Products 78, 69-76 (2015).
- (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase. R. Meleddu, S. Distinto, A. Corona, G. Bianco, V. Cannas, F. Esposito, A. Artese, S. Alcaro, P. Matyus, D. Bogdan,F. Cottiglia, E. Tramontano, E. Maccioni. European Journalof Medicinal Chemstry 93, 452-460 (2015).
- Withania somnifera root extract prolongs analgesia and suppresses hyperalgesia in mice treated with morphine. A. Orrù, G. Marchese, G. Casu, M. A. Casu,S. Kasture, F. Cottiglia, E. Acquas, M. P. Mascia,N. Anzani, S. Ruiu. Phytomedicine 21, 745-752 (2014).
- Design, Synthesis and Biological Evaluation of New 1,3-Diarylpropenones as Dual Inhibitors of HIV-1 RT. R. Meleddu, V. Cannas, S. Distinto, G. Sarais, C. Del Vecchio, F. Esposito, G. Bianco, A. Corona, F. Cottiglia, S. Alcaro, C. Parolin, A. Artese, D. Scalise, M. Fresta, A. Arridu, F. Ortuso, E. Maccioni, E. Tramontano. ChemMedChem 9, 1869- 1879 (2014).
- N-Alkyl dien- and trienamides from the roots of Otanthus maritimus with binding affinity for opioid and cannabinoid receptors. S. Ruiu, N. Anzani, A. Orrù, C. Floris, P. Caboni, E. Maccioni, S. Distinto, S. Alcaro, F. Cottiglia. Bioorganic & Medicinal Chemistry, 21, 7074-7082 (2013).
- Withania somnifera prevents acquisition and expressionof morphine-elicited conditioned place preference. S., Ruiu, R., Longoni,L., Spina, A., Orrù, F., Cottiglia, M., Collu, S., Kasture, E. Acquas. Behavioural Pharmacology, 24, 133-143 (2013).
- Cytotoxic phloroglucinols from the leaves of Myrtus communis. F. Cottiglia, L. Casu, M. Leonti, P. Caboni, C. Floris, B. Busonera, P. Farci, A. Ouhtit, G. Sanna. Journal of Natural Products, 75, 225-229 (2012).
- Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases. L. Casu, F. Cottiglia, M. Leonti, A. De Logu, E. Agus, Y.-C. Tse-Dinh, V. Lombardo, C. Sissi. Bioorganic & Medicinal Chemistry Letters 21, 7041–7044 (2011).
- Lumichrome and phenyllactic acid as chemical markers of thistle (Galactites tomentosa Moench) honey. C. I. Tuberoso, E. Bifulco, P. Caboni, G. Sarais, F. Cottiglia, I. Floris. Journal of Agricultural and Food Chemistry, 59, 364–369 (2011).
- Benzophenones from the roots of the popoluca amerindian medicinal plant Securidaca diversifolia (L.) S.F.Blake. L. Casu, M.N. Solinas A.R. Saba, F. Cottiglia, P. Caboni, C. Floris, S. Laconi, R. Pompei, M. Leonti. Phytochemistry Letters, 3, 226-229 (2010).
- Falcarinol is a covalent cannabinoid cb1 receptor antagonist and induces pro-allergic effects in skin. M. Leonti, L. Casu, S. Raduner, F. Cottiglia, C. Floris, K.H. Altmann, J. Gertsch. Biochemical Pharmacology 79, 1815-1826 (2010).
- Floral markers of strawberry tree (Arbutus unedo L.) honey. C.I. Tuberoso, E. Bifulco, P. Caboni, F. Cottiglia, P. Cabras, I. Floris. Journal of Agricultural and Food Chemistry 58, 384-389 (2010).
- Cytotoxic tirucullane triterpenoids from Melia azedarach fruits. N. G. Ntalli, F. Cottiglia, C. A. Bueno, L. E. Alché, Marco Leonti 2, S. Vargiu, E. Bifulco, U. Menkissoglu-Spiroudi, P. Caboni. Molecules 15, 5866-5877 (2010).
- A pterocarpan from the seeds of Bituminaria morisiana. M. Leonti, L. Casu, L. Bonsignore, J. Gertsch, C. Floris, M. Casu, F. Cottiglia. Journal of Natural Medicines 64, 654-657 (2010).
- A chromone from Seseli praecox (APIACEAE). M. leonti, L. Casu, M.N. Solinas, F. Cottiglia, P. Caboni, C. Floris, J. Gertsch, A.R. Saba. Natural Product Communications 5, 551-554 (2010).
- New cytotoxic saturated and unsaturated cyclohexanones from Anthemis maritima. F. Collu, L. Bonsignore, M. Casu, C. Floris, J. Gertsch, F. Cottiglia. Bioorganic & Medicinal Chemistry Letters 18, 1559-62 (2008).