Abstract: The aims of study were investigation on chemical
composition essential oil and the effect of extract of Coronilla varia
on antimicrobial and cytotoxicity activity. The essential oils of
Coronilla varia is obtained by hydrodistillation and analyzed by
(GC/MS) for determining their chemical composition and
identification of their components. Antibacterial activity of plant
extract was determined by disc diffusion method and anticancer
activity measured by MTT assay. The major components in essential
oil were Caryophyllene Oxide (60.19%), Alphacadinol (4.13%) and
Homoadantaneca Robexylic Acid (3.31%). The extracts from
Coronilla varia had interesting activity against Proteus mirabilis in
the concentration of 700 μg/disc and did not show any activity
against Staphylococus aureus, Bacillus subtillis, Klebsiella
pneumonia and Entrobacter cloacae. The positive control,
Ampicillin, Chloramphenicol and Cenphalothin had shown zone of
inhibition resistant all bacteria. The ethanol extract of Corohilla varia
inhibited on MCF7 cell lines. IC50 0.6(mg/ml) was the optimum
concentration of extract from Coronilla varia inhibition of cell line
growth. The MCF7 cancer cell line and Proteus mirabilis were more
sensitive to Coronilla varia ethanol extract.
Abstract: Doxorubicin, also known as Adriamycin, is an
anthracycline class of drug used in cancer chemotherapy. It is used in
the treatment of non-Hodgkin’s lymphoma, multiple myeloma, acute
leukemia, breast cancer, lung cancer, endometrium cancer and ovary
cancers. It functions via intercalating DNA and ultimately killing
cancer cells. The major side effects of doxorubicin are hair loss,
myelosuppression, nausea & vomiting, oesophagitis, diarrhea, heart
damage and liver dysfunction. The minor modifications in the
structure of compound exhibit large variation in the biological
activity, has prompted us to carry out the synthesis of sulfonamide
derivatives. Sulfonamide is an important feature with broad spectrum
of biological activity such as antiviral, antifungal, diuretics, antiinflammatory,
antibacterial and anticancer activities. Structure of the
synthesized compound N-(1-methyl-2-oxo-2-N-methyl anilinoethyl)
benzene sulfonamide confirmed by proton nuclear magnetic
resonance (1H NMR),13C NMR, Mass and FTIR spectroscopic tools
to assure the position of all protons and hence stereochemistry of the
molecule. Further we have reported the binding potential of
synthesized sulfonamide analogues in comparison to doxorubicin
drug using Auto Dock 4.2 software. Computational binding energy
(B.E.) and inhibitory constant (Ki) has been evaluated for the
synthesized compound in comparison of doxorubicin against Poly
(dA-dT).Poly (dA-dT) and Poly (dG-dC).Poly (dG-dC) sequences.
The in vitro cytotoxic study against human breast cancer cell lines
confirms the better anticancer activity of the synthesized compound
over currently in use anticancer drug doxorubicin. The IC50 value of
the synthesized compound is 7.12 μM whereas for doxorubicin is 7.2
μM.
Abstract: Since the marine environmental conditions are
extremely different from the other ones, marine actinomycetes might
produce novel bioactive compounds. Therefore, actinomycete strains
were screened from marine water and sediment samples collected
from the coastal areas of Northern Vietnam. Ninety-nine
actinomycete strains were obtained on starch-casein agar media by
dilution technique, only seven strains, named HP112, HP12, HP411,
HPN11, HP 11, HPT13 and HPX12, showed significant antibacterial
activity against both gram-positive and gram-negative bacteria
(Bacillus subtilis ATCC 6633, Staphylococcus epidemidis ATCC
12228, Escherichia coli ATCC 11105). Further studies were carried
out with the most active HP411 strain against Candida albicans
ATCC 10231. This strain could grow rapidly on starch casein agar
and other media with high salt containing 7-10% NaCl at 28-30oC.
Spore-chain of HP411 showed an elongated and circular shape with
10 to 30 spores/chain. Identification of the strain was carried out by
employing the taxonomical studies including the 16S rRNA
sequence. Based on phylogenetic and phenotypic evidence it is
proposed that HP411 to be belongs to species Streptomyces
variabilis. The potent of the crude extract of fermentation broth of
HP411 that are effective against wide range of pathogens: both grampositive,
gram-negative and fungi. Further studies revealed that the
crude extract HP411 could obtain the anticancer activity for cancer
cell lines: Hep-G2 (liver cancer cell line); RD (cardiac and skeletal
muscle letters cell line); FL (membrane of the uterus cancer cell line).
However, the actinomycetes from marine ecosystem will be useful
for the discovery of new drugs in the future.
Abstract: The nanotechnology offers some exciting possibilities in cancer treatment, including the possibility of destroying tumors with minimal damage to healthy tissue and organs by targeted drug delivery systems. Considerable achievements in investigations aimed at the use of ZnO nanoparticles and nanocontainers in diagnostics and antitumor therapy were described. However, there are substantial obstacles to the purposes to be achieved by the use of zinc oxide nanosize materials in antitumor therapy. Among the serious problems are the techniques of obtaining ZnO nanosize materials. The article presents a new vector delivery system for the known antitumor drug, doxorubicin in the form of polymeric (PEO, starch-NaCMC) hydrogels, in which nanosize ZnO film of a certain thickness are deposited directly on the drug surface on glass substrate by DC-magnetron sputtering of a zinc target. Anticancer activity in vitro and in vivo of those nanosize zinc oxide composites is shown.
Abstract: Camptothecin (CPT) is a cytotoxic quinoline alkaloid,
which inhibits the DNA enzyme topoisomerase I (topo I). It was
discovered in 1966 by M. E. Wall and M. C. Wani in systematic
screening of natural products for anticancer drugs. It was isolated
from the bark and stem of Camptotheca acuminata (Camptotheca,
Happy tree), a tree native in China. CPT showed remarkable
anticancer activity in preliminary clinical trials but also low
solubility and (high) adverse drug reaction. Because of these
disadvantages synthetic and medicinal chemists have developed
numerous syntheses of Camptothecine [1][2][3] and various
derivatives to increase the benefits of the chemical, with good results.
In our method CPT analogues has be six steps starting from available
material DL Malic acid.
Abstract: Breast cancer is the most common malignancy in the
world among women. Many therapies have been designed to treat
this disease. Mamectomy, chemotherapy and radiotherapy are still
the main therapies of breast cancer. However, the results were
unsatisfactory and still far from the ideal treatment.
PM 701is a natural product, has anticancer activity. The bioactive
fraction PMF and subfraction PMFK had been isolated from PM701.
PM 701 and its fractions were proved to have a cytotoxic properties
against different cancer cell lines. This article is directed for the
further examination of lyophilized PM701 and its active fractions on
the growth of breast cancer cells (MCF-7). PM 701, PMF or PMFK
were adding to the cultural medium, where MCF-7 is incubated.
PM 701, PMF or PMFK were able to inhibit significantly the
proliferation of MCF-7 cells, Moreover these new agents were
proved to induce apoptosis of the breast cancer cells; through its
direct effect on the nuclei.
Abstract: Aurein 1.2 is a 13-residue amphipathic peptide with antibacterial and anticancer activity. Aurein1.2 and its retro analog were synthesized to study the activity of the peptides in relation to their structure. The antibacterial test result showed the retro-analog is inactive. The secondary structural analysis by CD spectra indicated that both of the peptides at TFE/Water adopt alpha-helical conformation. MD simulation was performed on aurein 1.2 and retro-analog in water and TFE in order to analyse the factors that are involved in the activity difference between retro and the native peptide. The simulation results are discussed and validated in the light of experimental data from the CD experiment. Both of the peptides showed a relatively similar pattern for their hydrophobicity, hydrophilicity, solvent accessible surfaces, and solvent accessible hydrophobic surfaces. However, they showed different in directions of dipole moment of peptides. Also, Our results further indicate that the reversion of the amino acid sequence affects flexibility .The data also showed that factors causing structural rigidity may decrease the activity. Consequently, our finding suggests that in the case of sequence-reversed peptide strategy, one has to pay attention to the role of amino acid sequence order in making flexibility and role of dipole moment direction in peptide activity. KeywordsAntimicrobial peptides, retro, molecular dynamic, circular dichroism.