Phytic acid is extensively known for its anti-nutritional properties. The wide notion about this compound is to be changed totally. Hence, the study is focused on bringing out its potential as a drug molecule. The knowledge gained by understanding the binding efficacy of phytic acid and its analogues can help in the development of a new lead molecule. The antibacterial studies and cell line studies using HCT-15 confirmed the drugability. The potency of cancer drug targets can also be screened using docking studies. The entire work can bring out an effective lead molecule which maybe subjected to clinical trials. It is hypothesized that phytic acid and its derivatives having one or more of the following chemical functional groups such as the number of phosphates, phospho-diesters, charged phosphates, halogens, heavy atoms, steriocentred atoms, hydoxyl groups, hydrogen donors and acceptors, have an effect on the binding affinity towards the selected targets. Although, there are few reports to suggest the anticancer activity of PA, there is no work on its structure-activity relationship.
Healing properties of propolis are known in folk medicine from antiquity, however, recently, the interest in propolis as a potential natural product is increasing because of its broad spectrum of biological properties. It is an anti-flammatory agent, an immunostimulant, anti-oxidant, anti-microbial, and it is also an anti-tumour and a carcinostatic agent. This study was undertaken to characterize the chemical compounds, and antioxidant and anti-tumour potentials of propolis samples collected from five different geographical locations in Iraq using in vitro and in vivo studies. Thirty-eight different compounds were identified, and clerodane diterpenoids were identified for first time in temperate zone. All propolis samples exhibited strong free radical scavenging activity. The in vitro evaluations by growth inhibition, clonogenicity and flow cytometric assays showed that propolis has cytotoxic effects on two human cell lines. The in vivo potentials were also recorded on the growth of HCT-116 xenografts in a nude mouse model. This study provides the rationale to investigate the potential beneficial effect of propolis in the diet of patients receiving anti-cancer therapies.
Master Thesis in Applied Chemical Science, it Includes studing 27 different olive tree cultivars leaves ethanolic extracts in terms of their total phenolic content, antioxidant activity, toxicity to brine shrimps, anticancer activity (cell cycle analysis, cell death assay, MTT test), safety on normal cells (MTT test), LC-MS anlysis and quntification for some of their chemical constituents like Oleuropein, Oleanolic acid, Erythrodiol with its isomer Uvaol, Quercetin, Rutin. investigation of the presence of Resveratrol and Salicin qualitatively and quantitatively using LC-MS anlysis , studing the correlation between each constituent concentration in the extracts and their toxicity to brine shrimps also their correlation with anticancer activity on 7 cancer cell lines (MCF- 7, MDA-MB-231, C32, MV3, SW480, SW620, HCT-116), LC- MS(-)ESI,(+)APCI finger print of the most potent anticancer extracts.
The book aimed to reveal degradation of Cucurbitacin E glucoside obtained from Citrullus colocynthis (L.) (Hanzal) into Cucurbitacin E and glucose by mean of microbial biotransformation using Curvularia lunata NRRL 2178 as a source of beta-glucosidase. All the instrumental data obtained by highly advanced techniques, confirmed the microbial conversion of cucurbitacin E glucoside into cucurbitacin E and glucose indicating effect of enzyme in the hydrolysis process by splitting of glucose from the anomeric carbon atom. The effect of the cucurbitacin E glucoside and cucurbitacin E on the proliferation of Hep-G2 cells was studied. The treatment of Hep-G2 cells with cucurbitacin E led to a high inhibition of the cell proliferation, which revealed a moderate anti-tumor activity of the cucurbitacin E against hepatic carcinoma, while cucurbitacin E glucoside had no cytotoxic effect on Hep-G2 cells. The study showed the effect of the compounds on the proliferation of HCT-116 cells, the two compounds were not cytotoxic as indicated by their IC50 values. On the other hand, the treatment of T-lymphocyte cells with cucurbitacin E resulted in increase in the cell proliferation.
The chemistry and an extensive spectrum of biological activities of spirooxindole have been examined since several decades and this heterocyclic core has received emerging consensus. This content aims to summarize recent advances made towards the discovery of Antituberculosis activity, AChE and BChE inhibitory activity, Anti-tumor activity, Antibacterial and Antifungal activity and Miscellaneous Activity holding spirooxindole as a nucleus with the substitution of several types of nucleophiles, and molecular patterns associated with particular potency have been identified targeting several Gram-positive and Gram-negative bacteria and some fungal species, mycobacterium tuberculosis H37Rv, and drug-resistant tuberculosis (XDR-TB), Alzheimer's disease, HCT 116 (colon), MCF 7 (Brest) and HEPG 2 (liver) human tumor cell lines. The report will be of enormous interest to gain useful information for the furtherance of drug discovery with extended spirooxindole designs.
ABSTRACT The studies presented in this work include novel analytical methods based on spectrofluorimetric techniques for determination of some organic compounds used in pharmaceutical preparations. The work is divided to three chapters. The first chapter includes general introduction of spectrofluorimetric activity of lanthanide elements and the parameters affects on these phenomena. Also, the chapter involved the review of literature for previous methods of metoclopramide and hydrochlorothiazide drugs determination. The second chapter deals with the materials and apparatus used during this work including the types, grades, sources and preparations of these materials. Also, include the methods for measurements of different factors as absorbance, excitation and emission, effect of pH, effect of reagents and the validity tests of the metoclopramide and hydrochlorothiazide proposed methods as selectivity, recovery, precision and stability. The third chapter includes the results and discussion of the proposed methods for determination of metoclopramide hydrochloride (MCP) and hydrochlorothiazide (HCT).
This research work was carried out to establish scientific based evidence on folkloric usage and knowledge. The aim of this work is Pharmacological evaluation of Melochia corchorifolia leaves (folkloric) for antioxidant, diuretic, antiurolithiatic, anticancer, antibacterial and anthelmintic activities. In this regard, Melochia corchorifolia leaves were extracted with chloroform and ethylalcohol. The obtained extracts were used for pharmacological activities, the antioxidant activity results, the extracts and its Phenolic content shows good averting activity. Diuretic and saluretic activity is due to altering renal sodium excretion.The antiurolithiatic activity may be due to the presence of secondary metabolites of the extract.The extracts produced good anticancer activity on HCT-116 cell line and MCF-07 cancer cell lines. The chloroform extracts of Melochia corchorifolia shows good antibacterial and anthelmintic activities. So it was concluded that this research work supports the folkloric usage of this herbal drug (Melochia corchorifolia) is a potential source for treating various ailments.
Recombinant technology has crucial impact in therapy development. In microbial environment, Pathogenic bacteria such as Staphylococcus aureus produces alpha hemolysin protein. This protein is used as anticancer protein. alpha hemolysin gene was isolated from pathogenic S. aureus that was isolated from blood samples of patients (chrildren). This recombinant hia gene was produced alpha hemolysin protein by using competent E. coli as a host. The recombinant - toxin protein was used as anticancer agent.In this study that high concentration of -toxin (500 mil/ ml) was effected on the cell viability of four cells line ( HepG-2, HCT-116, MCF-7, A-549). The cell viability of cell lines were represented 31.69% in HepG-2, 36.27% in HCT-116, 78.95% in MCF-7, 67.28% in A-549. From our results, Alpha hemolysin protein had high inhibitory activity against HepG-2 and HCT-116, and had weak inhibitory activity against MCF-7 and A-549. Inconclusion,The production of recombinant - toxin was very simple process, low cost, high efficiency, non-toxic, high yield and no side effect.
A new Schiff base ligand (HL) derived from the condensation of quinoline-2-carboxaldehyde with 2-aminophenol and its mixed ligand complexes of Cr(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) vis 2,2'-bipyridine/1,10-phenanthroline as secondary ligand have been synthesized and characterized by elemental analyses, spectroscopic studies (IR, mass spectra, 1H NMR, UV-vis, magnetic susceptibility and solid reflectance), molar conductance, x-ray diffraction, ESR and thermal studies. The kinetic and thermodynamic parameters were calculated using the Coats-Redfern and HorowitzMetzger methods. Also, Schiff base ligand and its mixed ligand complexes were screened against Gram positive bacteria (Streptococcus pneumoniae and Bacillis subtilis) and Gram negative bacteria (Pseudomonas aeruginosa and Escherichia coli). Antifungal activity was carried out against (Aspergillus fumigatus and Candida albicans). In addition, anti-cancer activity of Schiff base ligand and its mixed ligand complexes were also tested against breast cancer cell line (MCF-7) and colon cancer cell line (HCT-116).