Berners-Price S J, Johnson R K, Giovenella A J, Faucette L F, Mirabelli C K, Sadler P J
Department of Chemistry, Birkbeck College, University of London, UK.
J Inorg Biochem. 1988 Aug;33(4):285-95. doi: 10.1016/0162-0134(88)80007-2.
Tetrahedral, bischelated Ag(I) diphosphine complexes [Ag(P-P)2]NO3, where P-P is Ph2P(CH2)2PPh2 (dppe), Et2P(CH2)2PPh2 (depe), and cis-Ph2P(CH = CH)PPh2 (dppey), are potently cytotoxic to B16 melanoma cells in vitro (IC50 4 microM) and exhibit good activity against ip P388 leukemia in mice. The complex [Ag(dppe)2]NO3 is active against M5076 reticulum cell sarcoma. The antibacterial and antifungal activities of Ag(I) diphosphine and related Cu(I) and Au(I) complexes were assessed. The complexes [Au(dppey)2]Cl, [Au(dppp)2]Cl and (CuCl)2(dppe)3 show modest activity against three of the 12 bacterial strains tested, but all complexes exhibit antifungal activity against three strains of C. albicans in a "defined" medium, [Ag(depe)2]NO3 and [Au(dppp)2]Cl having comparable activity to fungizone. Antifungal activity of the complexes is reduced in Sabouraud's broth medium, and lost altogether for the Ag(I) complexes. Reactions of some of the Ag(I) complexes with glutathione and blood plasma were studied by 31P NMR.
四面体双螯合的Ag(I)二膦配合物[Ag(P-P)₂]NO₃，其中P-P为Ph₂P(CH₂)₂PPh₂（dppe）、Et₂P(CH₂)₂PPh₂（depe）和顺式-Ph₂P(CH = CH)PPh₂（dppey），在体外对B16黑色素瘤细胞具有强大的细胞毒性（IC₅₀为4 microM），并且对小鼠体内的腹腔注射P388白血病表现出良好的活性。配合物[Ag(dppe)₂]NO₃对M5076网状细胞肉瘤有活性。评估了Ag(I)二膦配合物以及相关的Cu(I)和Au(I)配合物的抗菌和抗真菌活性。配合物[Au(dppey)₂]Cl、[Au(dppp)₂]Cl和(CuCl)₂(dppe)₃对所测试的12种细菌菌株中的3种表现出适度的活性，但所有配合物在“限定”培养基中对白色念珠菌的3个菌株均表现出抗真菌活性，[Ag(depe)₂]NO₃和[Au(dppp)₂]Cl的活性与制霉菌素相当。在沙氏肉汤培养基中，配合物的抗真菌活性降低，而Ag(I)配合物则完全失去活性。通过³¹P NMR研究了一些Ag(I)配合物与谷胱甘肽和血浆的反应。
