87 research outputs found
Comparison of Methods for Lipid Extraction from clam Scapharca inaequivalvis
No full textClam Scapharca inaequivalvis is a bivalve mollusk of Indo-Pacific origin, currently living also in the Adriatic Sea. Despite its content of valuable nutrients,1 it is not much appreciated as food in Mediterranean area and thus fishermen must pick it out from the clam Camelea gallina.2 Some of its precious nutrients are polyunsaturated fatty acids (PUFA) having a well-known beneficial influence on the vascular system. Considering this mollusk as a possible source of PUFA, our study was aimed at evaluating the efficiency of several methods with respect to the extraction of total lipids and the individual classes of fatty acids (saturated, monounsaturated and polyunsaturated). Conventional methods as Folch, Bligh and Dyer, and Soxhlet extraction with different solvents were tested, but also accelerated solvent extraction (ASE) and the use of low toxicity-solvents were evaluated. The highest yield of total lipid extract was 7.0 % (duplicate averaged, in relation to dry sample), obtained using ASE with chloroform/methanol, followed by a washing step with water. The next-highest yield (6.1 %) was afforded by Folch method, while the lowest yields were afforded by extraction with hexane/2-propanol and by Soxhlet extraction with hexane (2.3 %). The estimated percent total fatty acids in the total lipid extract ranged from 19.6 % (Folch method) to 39.4 % (Soxhlet extraction with hexane). The estimated percent PUFA in the total fatty acids ranged from 10.8 % (Soxhlet with hexane) to 22.5 % (ASE with chloroform/methanol).
References
1) Piretti, M.V.; Taioli, F.; Pagliuca, G. Comparative Biochemistry and Physiology 1987, 88B, 1201-1208.
2) Pierantozzi, C.; Zambuchini, B.; Giosia, L.; Faini, V.; D‘Angelo, N.; Spina, M.; Ventura, A.; Buttafoco, S.; Sturba, M.; Quagliarini, C. Progress in Nutrition 2005, 7, 1-9
A Self-Immolative Linker for the pH-Responsive Release of Amides
No full textThe administration of therapeutics using bioconjugation has been mainly limited to drugs containing amine, alcohol, or thiol functional groups. Here, we report a general procedure for the preparation of benzylic N-acyl carbamates suitable for masking the amide group in important drugs such as Linezolid, Enzalutamide, or Tasimelteon in good to acceptable yields. These N-acyl carbamates appear to be stable in plasma, while a qualitative analysis of further drug uncage demonstrates that, at pH values of 5.5, a classical 1,6-benzyl elimination mechanism takes place, releasing more than 80% of the drug in 24 h
Bioactivity of Curcuminoids in Half-Sandwich Ru(II), Rh(III) and Ir(III) Complexes: benefits from cooking to medicine
No full textCurcumin has been used for centuries in Asia as a spice, natural colouring and traditional medicine owing to its anti-inflammatory, antioxidant and antitumoral effects [1]. An alternative strategy to improve the properties of curcumin, without the need to modify the drug, is its incorporation into metal complexes [2]. Ruthenium compounds have emerged in recent years as promising alternatives to
platinum drugs by displaying specific activities against different cancers, favorable toxicity and clearance properties [3]. Recently, also metal complexes based on Rhodium and Iridium have arisen as fascinating potential alternative metallodrugs [4]. In the present work we exploit the coordination chemistry of Ru(II) arene and pentamethylcyclopentadienyl Rh(III) and Ir(III) complexes with curcumin [5] and bisdemethoxycurcumin as co-ligands and full characterization of relative RAPTA type complexes with 1,3,5-triaza-7-phosphaadamantane ligand (PTA) [6]. Hydrolysis studies were carried out under pseudopharmacological conditions to evaluate their aqueous chemistry. The antiproliferative effects in two human ovarian cancer cell lines (A2780 and A2780cisR) and non-tumorigenic human embryonic kidney cells (HEK293) will be reported
Synthesis and Characterization of New Ruthenium(II) Arene Acylpyrazolone Complexes
No full textArene ruthenium(II) complexes have been widely studied in the recent years, and their chemistry has been extensively studied for arenes such as benzene and para-cymene. They have found applications in catalysis, supramolecular assemblies, molecular devices.1 Moreover, they have shown antiviral, antibiotic and anticancer activities.2 Recently, mononuclear Ru-acylpyrazolone complexes have been shown to exhibit interesting in vitro activity in some cancer cells.3 On the basis of the our previous work,4 we extend our investigation to the interaction of several acylpyrazolones ligands with (arene)ruthenium(II)dichloride acceptors and PTA (1,3,5-triaza-7-phosphaadamantane)(Figure 1). Their structures have been confirmed by analytical and spectral data. X-ray diffraction studies and their biological activity are under investigation
Arene Ruthenium(II) Complexes with the Bioactive ortho-Hydroxydibenzoylmethane Ligand: Synthesis, Structure and Cytotoxicity
No full textThe synthesis of a series of neutral arene ruthenium(II) complexes (arene = p-cymene, hexamethylbenzene and benzene) [(arene)Ru(HDB)Cl] derived from the reaction of the appropriate arene ruthenium(II) dimers and ortho-hydroxydibenzoylmethane (HDBH), a potent inhibitor of cell proliferation, is described. In addition, related ionic complexes [(arene)Ru(HDB)(PTA)][SO3CF3] (PTA = 1,3,5-triaza-7-phosphaadamantane) have been prepared. The structure of three complexes has been confirmed by X-ray crystallography. The cytotoxicity of the complexes has been evaluated against human ovarian carcinoma cells (A2780 and A2780cisR), as well as against non-tumorigenic human embryonic kidney (HEK293) cells and compared to the free ligand and cisplatin. Two of the complexes, i.e. from the first series with p-cymene and hexamethylbenzene, display relevant activities against the cisplatin resistant A2789cisR cancer cell line
Comparison of Eleven Extraction Methods for Quantitative Evaluation of Total Lipids and Fatty Acids in the Clam Anadara inaequivalvis (Bruguière)
No full textThe clam Anadara inaequivalvis (Bruguière) is a bivalve mollusc now populating several areas of the Mediterranean Sea seafloor where it competes with other molluscs harvested as food. In fact, even though Anadara inaequivalvis has valuable nutritional properties, it has no commercial value in European countries. The aim of this study
was to evaluate quantitatively and qualitatively fatty acid content in this bivalve mollusc and to compare 11 extraction methods: conventional procedures such as Folch, Bligh and Dyer, and Soxhlet with different solvents, as well as accelerated solvent extraction (ASE) and methods using low-toxicity solvents as substitutes for chloroform (CHCl3) and methanol
(MeOH). The best method was ASE CHCl3-MeOH, affording yields of total lipids, total fatty acids, and polyunsaturated fatty acids (PUFAs) significantly higher than any other method. The estimated range of total lipids was 2.29%–6.99% (on the dry sample), and the range of fatty acids was 0.74%–1.78%. Yields of polyunsaturated fatty acids (PUFAs) ranged from 0.10% to 0.40%. The solvent mixture hexane–isopropanol as substitute for CHCl3-MeOH did not afford good results. PUFAs were 22.5% in the total fatty acids and the ratio between PUFAs n-3 and PUFA n-6 was 2.74:1
10th International School of Organometallic Chemistry
No full textThe ISOC series is the most important school on organometallic chemistry at the European level, organized under the auspices of EuCheMS (the European Association for Chemical and Molecular Sciences) and the Interdivisional Group of Organometallic chemistry of the Italian Chemical Society. The aim is to encourage the presence of young researchers and Ph.D students both from University and Industry, including those not directly involved in organometallic research projects, in order to bring together young researchers and distinguished European scientists as a contribution to the important goal of increasing the transfer of knowledge at a high level between different European countries and different generation of scientists
Selective Anticancer Ruthenium(II) Arene RAPTA Type Complexes Containing Curcuminoids
No full textRuthenium-arene complxes are considered valid alternatives to platinum drugs, owing to their lower toxicity and stronger selectivity. Since curcumin possesses anti-inflamatory, antioxidant and antitumoral effects, it has been extensively studied as a chemo preventive agent in some cancer models. As continuation of our previous work, a series of novel Ru(II) arene RAPTA type derivatives (areme = cymene and hexamethylbenzene) containing corcumin-based ligands (curcH = curcumin, bdcurcH = bisdemethoxycurcumin) and PTA (1,3,5-triaza-7-phosphaadamantane) has been synthesized and fully characterized. The antitumor activity of the complexes has been evaluated in vitroagainst human ovarian carcinoma cells, A2780 and A2780cisR, as well as against non-tumorous Human Embryonic Kidney (HEK293) cells
Synthesis, Structures and Antiproliferative Activity of Novel Ru(II)-Arene Complexes with N,O-Chelating β-Ketoamine Ligands
No full textOrganometallic compounds are attracting a considerable interest in medicinal chemistry, especially as putative anticancer compounds. Of particular interest are ruthenium-arene complexes which have been extensively studied and modified to obtain compounds with various therapeutic effects. Ruthenium arene complexes with β-ketoamine ligands derived from 4-acyl-5-pyrazolones possess relevant anticancer properties in vitro. It was found that minor changes to the β-ketoamine ligand lead to considerable changes in cytotoxicity and, consequently, a series of novel Ru(II)-arene derivatives containing β-ketoamine ligands L' (HL' in general, HLbiph,ph, HLbiph,naph, HLph,naph, HLhex,naph) has been synthetized and fully characterized by spectroscopy and single-crystal X-ray diffraction. The ligands in the anionic form coordinate to the ruthenium ion in a chelating κ2 N,O-bidentate mode, affording 1:1 derivatives of the formula [(arene)Ru(L')Cl]. The in vitro anticancer activity of both the ligands and complexes has been evaluated against the human ovarian carcinoma cell line A2780 and its cisplatin-resistant equivalent A2780R
Synthesis, Characterization and Bioactivity of Novel Pentamethylcyclopentadienyl Rh(III) and Ir(III) Complexes Containing Dibenzoylmethane
No full textOrganometallic complexes play a key role in medicinal chemistry, especially in the development of anticancer therapies [1]. Among this class of inorganic compounds Rhodium and Iridium complexes are recently attracting an increasing interest in treatment of cancer since they possess several features that make them appealing alternative metallodrugs [2]. Dibenzoylmethane is a natural β-diketone that can be found in small amount in licorice roots. It possesses biological activity against different kind of cancer such as skin, prostate, lung and mammary tumors, lymphomas and leukemia [3].
Pentamethylcyclopentadienyl Rh(III) and Ir(III) complexes bearing dibenzoylmethane and their respective derivatives with PTA (1,3,5-triaza-7- phosphaadamantane) have been synthetized and fully characterized. Preliminary results on their biological and biochemical activity will also be reported
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