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.
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 original work of the present book consists of three research projects: In the first part: Synthesis, cytotoxicity evaluation, molecular docking and utility of novel chalcones as precursors for heterocycles incorporating pyrazole moiety.In the second part: Synthesis and antimicrobial activity of novel azolopyrimidines and pyrido-triazolo-pyrimidinones incorporating pyrazole moiety.In the third part: Synthesis of new pyrazolyl-pyridines as antitumor agents. The assigned structures for all the newly synthesized compounds were confirmed on the basis of elemental analyses and spectral data and the mechanisms of their formation were also discussed. In addition, some of the newly synthesized chalcones were tested for their cytotoxicity against human colon carcinoma cell line (HCT-116) and against human hepatocellular carcinoma (HEPG2) cell lines and the results revealed that some compounds have promising activities compared with the standard drug Doxorubicin. Molecular docking was also carried out for the high potent compounds.
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.
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).
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.
Diabetes mellitus is a metabolic affliction saunter that is characterized by a nobler than normal blood glucose poise. Glucose-6-phosphate dehydrogenase (G6PD) enzyme code (E.C.22.214.171.124) is an underlying enzyme in the phosphogluconate pathway. In this study, G6PD vitality in the mortal erythrocyte of male and female patients with type 2 diabetes mellitus was assessed utilizing a spectrophotometer at 340 nm. The activity of the enzyme increased with elevated glycated hemoglobin (HbA1C) levels. G6PD activity was found to be significantly associated with type 2 diabetes mellitus. The association between G6PD and diabetes mellitus was significant (P 0.001). Moreover, G6PD was positively correlated with HbA1C levels (r = 0.572). The following mean ± standard deviation values were obtained: G6PD activity (IU/g Hb), 3.1103 ± 0.79349, HbA1C (%), 8.6600 ± 1.63120, Hb (g/dL), 13.4933 ± 1.38836, platelet count (103/mil), 283.4667 ± 58.59312, WBC (103/mil), 7.4890 ± 1.49842, HCT (%), 45.0100 ± 2.63430, and BS (mg/dL), 230.2667 ± 75.67760. The results showed that an elevated HbA1C up leads to increased G6PD performance in the human erythrocyte, which is concerning to glucose levels.
This work has been carried out to investigate the following: The first project represents the reactions of ethylidenethiosemicarbazone with DMAD or substituted methylenemalononitriles gave thiazolidin-4-one or 1,3-thiazine derivatives, respectively. Also, treatment of ethylidenethiosemicarbazide with hydrazonoyl halides, -haloketones, and chloroacetic acid afforded the corresponding arylazothiazoles, thiazoles, and thiazolidenone derivative, respectively. The anti-cancer activity of the selected products against the colon carcinoma cell line (HCT-116) was determined and the results revealed promising activity.The second project involves the synthesis of a novel series of pyridine and bipyridine derivatives is described via one-pot multi-component reaction of 5-acetylimidazole, malononitrile (or ethyl cyanoacetate or diethyl malonate), substituted benzaldehyde (or terephthaldehyde) and ammonium acetate in good yields. The antimicrobial activities of the synthesized compounds were screened and the results showed that most of them exhibit considerable activities. Also, some of the newly synthesized compounds were screened for their anticancer activity against two cell lines.
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.