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A novel water-soluble oral satraplatin/β-cyclodextrin inclusion complex was prepared and characterized with a variety of techniques. Molecular dynamics simulations were performed to clarify its inclusion mechanism. Enabled by encapsulation with cyclodextrin, the water solubility of satraplatin was successfully increased to 7.4 mg mL−1 and significantly improved by phase solubility studies. Meanwhile, the stability of satraplatin in acidic and weak alkaline aqueous solution was also effectively enhanced by forming the inclusion complex. Importantly, in an in vitro cytotoxicity test, the satraplatin encapsulated complex displayed superior cytotoxicity compared to free satraplatin against A549 and MCF-7 cells but was almost non-toxic to Caco-2 cells. In an in vivo antitumor test, this satraplatin encapsulated complex has shown much better activity in repressing lung cancer than free satraplatin but nearly no damage to intestinal mucosa by oral administration evaluated in xenograft mice models. Overall, the development of the current satraplatin/β-cyclodextrin inclusion complex has significantly improved the bioavailability of satraplatin and could benefit further applications in related pharmaceutical formulations.

In order to obtain a chlorogenic acid platinum complex, The intermediate Pt(C6H14N2)(H2O)2(NO3)2 solution was synthesized from Pt(C6H14N2)I2 and AgNO3, and it was treated with the anion exchange resin to give the key intermediate Pt(C6H14N2)(OH)2. The key intermediate was subsequently reacted with chlorogenic acid in butyl alcohol. The complex structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity was measured by MTT method. The result showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.

In order to obtain the mixed isobutylamine /cyclopentylamine platinum complexes with chloride and oxalic acid ions as leaving groups. The title compounds were synthetised from potassiumtetrachloroplatinate(II) by the reaction with potassium iodide, cyclopentylamine, isobutylamine, silver nitrate, potassium chloride, potassium oxalate monohydrate. The complexes structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity were measured by MTT method. The results showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.

In order to obtain a gallic acid platinum complex, the title compound was synthesed from cis-[Pt(Cyclohexylamine)]2I2 by the reaction with NH3, silver nitrate and gallic acid respectively. The complex structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity was measured by MTT method. The result showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.

In order to obtain a chlorogenic acid platinum complex, The intermediate Pt(C6H14N2)(H2O)2(NO3)2 solution was synthesized from Pt(C6H14N2)I2 and AgNO3, and it was treated with the anion exchange resin to give the key intermediate Pt(C6H14N2)(OH)2. The key intermediate was subsequently reacted with chlorogenic acid in butyl alcohol. The complex structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR and the anticancer activity was measured by MTT method. The result showed that its structure was consistent with the title compound and had inhibiting effect on the growth of tumor cell lines in vitro.

Baicalin (BA) has been shown with anti-HIV-1 activity. Zinc is a nutrient element. The anti-HIV-1 activity of zinc complex of baicalin (BA-Zn) in vitro was studied and compared with the anti-HIV-1 activities between BA and BA-Zn in the present study. Our results suggested that BA-Zn has lower cytotoxicity and higher anti-HIV-1 activity compared with those of BA in vitro. The CC50s of BA-Zn and BA were 221.52 and 101.73 microM, respectively. The cytotoxicity of BA-Zn was about 1.2-fold lower than that of BA. The BA and BA-Zn inhibited HIV-1 induced syncytium formation, HIV-1 p24 antigen and HIV-1 RT production. The EC50s of BA-Zn on inhibiting HIV-1 induced syncytium formation (29.08 microM) and RT production (31.17 microM) were lower than those of BA (43.27 and 47.34 microM, respectively). BA-Zn was more effective than BA in inhibiting the activities of recombinant RT and HIV-1 entry into host cells. Zinc coupling enhanced the anti-HIV-1 activity of baicalin.

Three water-soluble oxaliplatin complexes were prepared by inclusion complexation with β-cyclodextrin (β-CD), γ-CD and HP-β-CD. The structures of oxaliplatin/CDs were confirmed by NMR, FTIR, TGA, XRD as well as SEM analysis. The results show that the water solubility of oxaliplatin was increased in the complex with CDs in 1:1 stoichiometry inclusion modes, and the cyclohexane ring of oxaliplatin molecule was deeply inserted into the cavity of CDs. Moreover, the stoichiometry was established by a Job plot and the water stability constant (Kc) of oxaliplatin/CDs was calculated by phase solubility studies, all results show that the oxaliplatin/β-CD complex is more stable than free oxaliplatin, oxaliplatin/HP-β-CD and oxaliplatin/γ-CD. Meanwhile, the inclusion complexes displayed almost twice as high cytotoxicity compared to free oxaliplatin against HCT116 and MCF-7 cells. This satisfactory water solubility and higher cytotoxic activity of the oxaliplatin/CD complexes will potentially be useful for their application in anti-tumour therapy.

The inclusion complex of picoplatin with γ-cyclodextrin (γ-CD) was prepared and characterised by different analytical methods, including NMR, FTIR, TGA, phase solubility as well as SEM. All of these approaches indicated that picoplatin was able to form an inclusion complex with γ-CD, and that the picoplatin/γ-CD inclusion compounds exhibited different spectroscopic features and properties from free picoplatin. The stoichiometry of the complex was 1:1; the pyridine group of picoplatin was deeply inserted into the cavity of γ-CD and the amine platinum group of picoplatin was near the narrower rim of γ-CD. The calculated apparent stability constant of the complex was 10,318M(-1). Moreover, the water solubility of picoplatin was significantly improved, according to phase-solubility studies. The complex maintained its anticancer activity, as shown by an in vitro cell-survival assay on A549 and MCF-7 cancer cell lines. All of these results showed that inclusion complexation may be a promising strategy to design a novel formulation of picoplatin as an anticancer therapy.

The reaction of cis-[Pt(NO(3))(2)(NH(3))(2)] and sodium glycolate yielded the title compound, [Pt(C(2)H(2)O(3))(NH(3))(2)]. The Pt(II) atom, coordinated by two N atoms of ammine and two O atoms of the carboxyl-ate and oxido groups of the glycolate ligand, is in a square-planar environment. In the crystal structure, mol-ecules are connected by inter-molecular N-H⋯O hydrogen bonds, forming a three-dimensional network.

C2H14N6O11Pt2 ,o rthorhombic, Pnma (no. 62), a =1 2.701(3) A, b =1 0.705(2) A, c =9 .942(2) A, V =1 351.8 A 3 , Z =4 , Rgt(F) =0 .023, wRref(F 2 ) =0 .057, T =2 96 K. Source of material