cytotoxicity

The present investigation aims on the preparation and in-vitro/in-vivo examination of inclusion complex of Diacerein (DAR) an anthraquinone derivative indicated for treatment of osteoarthritis by inhibiting interlukin-1 and hydroxypropyl-β-cyclodextrin (HP-β-CD). In this study, the inclusion complexes of DAR with β-cyclodextrin (β-CD), HP-β-CD, methyl-β-cyclodextrin (M-β-CD) and γ-cyclodextrin (γ-CD) were prepared and characterized for phase solubility study and inclusion efficiency. On the basis of results obtained, HP-β-CD was selected to prepare inclusion complexes with DAR by physical mixing, kneading method and freeze drying method and subjected to solid state characterizations. Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Infra-red spectroscopy (IR) analysis confirmed the formation of perfect inclusion complex of DAR with HP-β-CD in solids. In-vitro dissolution and % drug content of DAR in freeze dried inclusion complex showed its superiority over plain drug and commercial formulation. . In-vitro cell cytotoxicity studies (MTT Assay) using Caco-2 cell line model confirmed the bio-tolerability of DAR-inclusion complex. . The relative oral bioavailability of DAR in Albino rabbits resulted from Freeze dried inclusion complex was found 3.32 fold and 2.03 fold greater than plain DAR and marketed formulation, respectively which ultimately demonstrated the enhancement of oral bioavailability of DAR in freeze dried inclusion complex with HP-β-CD.

Cancer, a disease characterized by uncontrolled proliferation of cells that have transformed from the normal cells of the body and is one of the major causes of death in developed and developing nations. Presently available treatment method, chemotherapeutic agents, suffers from drawback of toxicity such as bone marrow suppression, alopecia and vomiting. Its not within the reach of common man. Therefore challenging task is to identify quick and novel methods which can be of therapeutic value in human cancers. Plants have a long history and important role as a source of effective anti-cancer agents. Hence in the present study, one of the traditionally used plant, M.minuta was screened for cytotoxicity. Successive solvent extraction was carried out and the petroleum ether, chloroform, ethyl acetate, alcoholic and aqueous extracts of M.minuta were prepared. Extracts were subjected to Brine shrimp lethality assay and it was observed that % mortality increased gradually with the increase in concentration of the test samples. Ethyl acetate and alcoholic extracts which showed better cytotoxicty were further screened for their cytotoxicity towards breast cancer cell lines using MTT cell viability assay. In the same, ethyl acetate extract was found to be significantly cytotoxic towards cell lines compared to that of alcoholic extract which may be due to higher amount of phenolic compounds present in them. The results obtained in this study further supported the traditional usage of the drug and the activity of drug can be attributed to major bioactive phytochemical class; poly phenolics, present in the drug.

Four Pd(II) and Pd(IV) complexes with 3-thiolanespiro-5’-hydantoin and 4-thio-1H-tetrahydropyranespiro-5’-hydantoin were synthesized. Thechemical structures of newcomplexes were studied by elemental analysis, IR, 1H, 13C NMR spectra. The spectroscopic investigation of new palladium complexes in comparison with the metal free ligands show that the bonding of the ligands with metal ions is realized through the sulfur atom from the S-containing saturated rings. This coordination mode is in accordance with the data obtained for the platinum complexes with the same ligands. The new complexes were investigated for cytotoxicity on panel of human tumor cell lines. The tested compounds exerted concentration-dependent cytotoxic effects against some of the tumor cell lines.