farid badria

Phytochemical investigation of Aglaia duppereana flowers led to the isolation of a new rocaglamide derivative and twelve known congeners. The structure of the new compound was unambiguously elucidated by spectroscopic techniques (1D- and 2D-NMR, HRESIMS). The isolated compounds exhibited a potent cytotoxic activity against mouse lymphoma (L5178Y) cells with EC50 values ranging from 5.1 to 54.8 nM.

Ethyl (coumarin-4-oxy)acetate 1 was prepared through the reaction of 4-hydroxycoumarin with ethyl bromoacetate. Compound 1 was allowed to react with hydrazine hydrate to produce coumarin-4-oxyacetic hydrazide 2. The synthesis of N-(arylidene and alkylidene)-coumarin-4-oxyacetic hydrazones 3-20 was performed. The preparation of 2-substituted-3-[(coumarin-4-oxy) acetamido]thiazolidinones 21-26 and 2-[(coumarin-4-oxy)methyl]-4-acetyl-5-substituted-delta2-1,3,4-oxadiazolines 27-33 was performed by the reaction of the hydrazones 3, 4, 7, 9, 12, 14 with mercaptoacetic acid and the hydrazones 3, 4, 5, 7, 12, 15, 16 with acetic anhydride, respectively. The antiviral activities, cytotoxicities and structure-activity relationship (SAR) towards different microorganisms of the prepared compounds were studied.

Garlic (Allium sativum L.) is used in the household and as an ingredient in many pharmaceutical products. Tissue culture technique provides an excellent source for induction of both chemical and genetic variation in garlic. A callus was induced on root meristem cultured on Murashige and Skoog (MS) medium in the presence of kinetin, indole acetic acid, and 2,4-dichlorophenoxyacetic acid. Shoots with a small bulb were produced on medium containing MS salts, B vitamins, and naphthalene acetic acid. Regenerated plants were transplanted into soil, and a nondivided bulb was formed in the first somaclonal generation (SCI). Plants were normal in their phenotypes in SC2. After four cycles of field cultivation, the selected somaclones (variants) in the fourth generation showed significant differences in bulb character compared with the original plants. Mitotic division and chromosomal abnormalities were investigated in meristimic root tip cells of regenerated plants for the first and fourth regeneration and for control plants. Somaclonal variant metaphase cells had the same chromosome number (2n = 16) as those of the controls. Allicin was measured quantitatively in the regenerated clones by high-performance liquid chromatography. The results showed that some clones contained as much as 14.50 mg/g allicin, compared with 3.80 mg/g in the control plant. This finding suggests that this technique may be useful to improve the allicin content of Egyptian garlic, which could be utilized as a good source for garlic-containing pharmaceutical preparations.

Selected natural compounds were evaluated for their effects on dental caries due to different strains of Streptococcus mutans bacteria. Out of 39 tested compounds, four (catechol, emetine, quinine, and flavone) showed potent inhibitory activity on different strains of S. mutans at 6.25 microg/mL or less with inhibition of adherence <50%, two compounds (5,7-dihydroxy-4'-methoxy isoflavone and ellagic acid) exhibited a moderate inhibitory effect at 12.5 microg/mL with inhibition to adherence <50%, and 12 compounds exhibited weak antibacterial activity at 125 microg/mL or more with inhibition of adherence <25%. These compounds represent three major classes of natural products: tannins, alkaloids, and flavonoids. Further study for possible application of these compounds as inhibitors for dental caries is underway.

Selected natural compounds were evaluated for their effects on dental caries due to different strains of Streptococcus mutans bacteria. Out of 39 tested compounds, four (catechol, emetine, quinine, and flavone) showed potent inhibitory activity on different strains of S. mutans at 6.25 microg/mL or less with inhibition of adherence <50%, two compounds (5,7-dihydroxy-4'-methoxy isoflavone and ellagic acid) exhibited a moderate inhibitory effect at 12.5 microg/mL with inhibition to adherence <50%, and 12 compounds exhibited weak antibacterial activity at 125 microg/mL or more with inhibition of adherence <25%. These compounds represent three major classes of natural products: tannins, alkaloids, and flavonoids. Further study for possible application of these compounds as inhibitors for dental caries is underway.

Selected natural compounds were evaluated for their effects on dental caries due to different strains of Streptococcus mutans bacteria. Out of 39 tested compounds, four (catechol, emetine, quinine, and flavone) showed potent inhibitory activity on different strains of S. mutans at 6.25 microg/mL or less with inhibition of adherence <50%, two compounds (5,7-dihydroxy-4'-methoxy isoflavone and ellagic acid) exhibited a moderate inhibitory effect at 12.5 microg/mL with inhibition to adherence <50%, and 12 compounds exhibited weak antibacterial activity at 125 microg/mL or more with inhibition of adherence <25%. These compounds represent three major classes of natural products: tannins, alkaloids, and flavonoids. Further study for possible application of these compounds as inhibitors for dental caries is underway.

Garlic (Allium sativum L.) is used in the household and as an ingredient in many pharmaceutical products. Tissue culture technique provides an excellent source for induction of both chemical and genetic variation in garlic. A callus was induced on root meristem cultured on Murashige and Skoog (MS) medium in the presence of kinetin, indole acetic acid, and 2,4-dichlorophenoxyacetic acid. Shoots with a small bulb were produced on medium containing MS salts, B vitamins, and naphthalene acetic acid. Regenerated plants were transplanted into soil, and a nondivided bulb was formed in the first somaclonal generation (SCI). Plants were normal in their phenotypes in SC2. After four cycles of field cultivation, the selected somaclones (variants) in the fourth generation showed significant differences in bulb character compared with the original plants. Mitotic division and chromosomal abnormalities were investigated in meristimic root tip cells of regenerated plants for the first and fourth regeneration and for control plants. Somaclonal variant metaphase cells had the same chromosome number (2n = 16) as those of the controls. Allicin was measured quantitatively in the regenerated clones by high-performance liquid chromatography. The results showed that some clones contained as much as 14.50 mg/g allicin, compared with 3.80 mg/g in the control plant. This finding suggests that this technique may be useful to improve the allicin content of Egyptian garlic, which could be utilized as a good source for garlic-containing pharmaceutical preparations.

Three acetylenic brominated derivatives were isolated from a Red Sea sponge, Haliclona sp. One of them, 18-bromooctadeca-9(E),17(E)-dien-7,15-diynoic acid (3), is a known metabolite, and the other two are new compounds, (1E,5E,12E,19E)-1,22-dibromodocosa-1,5,12,19-tetraen-3,14,21-triyne (1) and methyl 18-bromooctadeca-9(E),17(E)-dien-7,15-diynoate (2) which was isolated for the first time as a natural metabolite. Structures of all compounds were determined based on extensive spectroscopic measurements [1D (1H, 13C and DEPT) and 2D (HSQC, HMBC and NOESY) NMR, MS, UV, and IR]. All compounds, except 3, were evaluated for their cytotoxicity employing four cancer cell lines, i.e. MCF-7 (human breast cancer), HepG2 (human hepatocellular carcinoma), WI-38 (skin carcinoma), and Vero (African green monkey kidney). Compounds 1 and 2 had potent selective antitumour activity towards MCF-7 cells with IC50 values of 32.5 and 50.8 microM, respectively.

The synthesis, in vivo and in vitro antitumor evaluation, and QSAR studies of some novel pyrazole analogs against Ehrlich Ascites Carcinoma (EAC) cells were described. In vitro results revealed that compounds 10, 6 and 4 were the most potent analogs against EAC, respectively. Moreover, in vivo evaluation of compounds 6 and 10 proved their capability to normalize the blood picture in comparison to 5-FU, a well known anticancer drug. These novel pyrazole analogs were molecularly designed with the goal of having significant potent cytotoxic effect against EAC cells. To develop a QSAR model capable of identifying the key molecular descriptors associated with the biological activity of the novel pyrazole analogs and predicting the cytotoxic effect for other novel pyrazole analogs against EAC cells, different QSAR models, using different physicochemical and topological molecular descriptors, were developed. Different molecular descriptors were predicted solely from the chemical structures of 16 pyrazolo-diazine and triazine analogs following the prediction of the equilibrium molecular geometry of each analog at the DFT level using B88-LYP functional energy and double zeta valence polarized (DZVP) basis set. It was found that dipole moment, excitation energy, the energy value of LUMO, solvent accessible surface area, and heat of formation were the key molecular descriptors in descriping the cytotoxic effect of those compounds against EAC.

... Also, AFMl was found in one blood sample out of 20 patient suffering from liver cirrhosis only in concentration of 8.3 ppb. Abaza et al. (27) studied 50 patients with HCC. AFBl was detected in sera of 37 (74 %) patients and in the liver tissues in 9 (18 %). ...

Sixty-two Egyptian food and medicinal preparations were extensively examined for antimutagenic/anticarcinogenic activity using short-term and host-mediated assays. The antimutagenic activity of the substances examined was ranked as follows: thirteen (strong), seven (mild) and five (weak) after metabolic activation. Metabolic activation seems to be necessary for most antimutagenic substances in this study, e.g. radish inhibits 29% of mutagenicity produced in direct antimutagenic assay and inhibits 89% of mutagenicity induced in host-mediated assay.

Fumonisins are a series of sphingosine‐analog mycotoxins produced by Fusarium verticillioides, a ubiquitous contaminant of stored corn (maize) world‐wide. Extensive alterations in the structures of fumonisins are possible without complete loss of in vitro toxicity. ...

Cancer chemotherapies have been improved dramatically over the last two decades. In the case of human breast cancer, the combination chemotherapeutic protocol, cyclophosphamide (CPA), doxorubicin (DOX), and 5-fluorouracil (5-FU) (CDF), is often used. Nevertheless, the clinical usefulness of CDF is limited by its remarkably low therapeutic window and frequent eruption of resistance. These limitations prompted our search for a more effective and safe drug candidate that may raise the therapeutic benefits for breast cancer patients. Gingerols' wide therapeutic indices as well as their high efficacy in the suppression of carcinogenesis are well established. However, no thorough study to date has profiled their antibreast cancer activities in depth. Therefore, the aims of the present study are to evaluate the antibreast cancer activities of gingerols in comparison to CDF and to gain insight into the structure activity relationships (SARs) responsible for the observed effect using a breast cancer cell model, MCF-7. Our data revealed that 6-gingerol showed the highest anticancer potency that is superior to that of CDF with IC50 = 30.4 μM. Guided by these results, semisynthetic modifications of 6-gingerol have been carried out to characterize 6-gingerol's SARs. The obtained results showed that the acquisition of free hydroxyl group in the aliphatic side chain of 6-gingerol is essential for the antibreast cancer activity. Likewise, the length of aliphatic side chain in 6-gingerol is optimum for its anticancer activity because any decrease in the side chain length resulted in a dramatic loss of anticancer activity. Additionally, allylation of phenolic group has shown antibreast cancer activity superior to that of 6-gingerol per se. Conversely, methylation or isoprenylation of phenolic group has led to a potential decrease in the anticancer activity, whereas loss of aromaticity resulted in a complete loss of 6-gingerol's cytotoxic activity.…

... AinShams University, Egypt 1990. Abaza H., El-Mallah S., El-Kady A., Helmy M., Yehia N., Assal A., El-Deeb S. Mycotoxins and Hepatocellular Carcmoma in Egypt, Abstract Book. Int. Symp. and Workshop on Food Contamination Mycotoxins. CairoEgypt 1992; T26. Saadi MG ...

Farid A. Badria, Ph.D, Eman A. Mohammed, M.Sc., Mohammed K. El-Badrawy, MD, and ... of thoracic medicine at Mansoura Uni-versity Hospital and Mansoura Chest Hospital, both in Mansoura, Egypt, from ... selected for the study ranged in age from 18 to 59, with a mean of 37.86 ...

Three acetylenic brominated derivatives were isolated from a Red Sea sponge, Haliclona sp. One of them, 18-bromooctadeca-9(E),17(E)-dien-7,15-diynoic acid (3), is a known metabolite, and the other two are new compounds, (1E,5E,12E,19E)-1,22-dibromodocosa-1,5,12,19-tetraen-3,14,21-triyne (1) and methyl 18-bromooctadeca-9(E),17(E)-dien-7,15-diynoate (2) which was isolated for the first time as a natural metabolite. Structures of all compounds were determined based on extensive spectroscopic measurements [1D (1H, 13C and DEPT) and 2D (HSQC, HMBC and NOESY) NMR, MS, UV, and IR]. All compounds, except 3, were evaluated for their cytotoxicity employing four cancer cell lines, i.e. MCF-7 (human breast cancer), HepG2 (human hepatocellular carcinoma), WI-38 (skin carcinoma), and Vero (African green monkey kidney). Compounds 1 and 2 had potent selective antitumour activity towards MCF-7 cells with IC50 values of 32.5 and 50.8 microM, respectively.

... Also, AFMl was found in one blood sample out of 20 patient suffering from liver cirrhosis only in concentration of 8.3 ppb. Abaza et al. (27) studied 50 patients with HCC. AFBl was detected in sera of 37 (74 %) patients and in the liver tissues in 9 (18 %). ...