Abstract: Two new metal-based anticancer chemotherapeutic
agents, [(Ph2Sn)2(HGuO)2(phen)Cl2] 1 and [(Ph3Sn)(HGuO)(phen)]-
Cl.CH3OH.H2O 2, were designed, prepared and characterized by
analytical and spectral (IR, ESI-Mass, 1H, 13C and 119Sn NMR)
techniques. The proposed geometry of Sn(IV) in 1 and 2 is distorted
octahedral and distorted trigonal-bipyramidal, respectively. Both 1
and 2 exhibit potential cytotoxicity in vitro against MCF-7, HepG-2
and DU-145 cell lines. The intrinsic binding constant (Kb) values of 1
(2.33 × 105 M-1) and 2 (2.46 × 105 M-1) evaluated from UV-Visible
absorption studies suggest non-classical electrostatic mode of
interaction via phosphate backbone of DNA double helix. The Stern-
Volmer quenching constant (Ksv) of 1 (9.74 × 105 M-1) and 2 (2.9 ×
106 M-1) determined by fluorescence studies suggests the groove
binding and intercalation mode for 1 and 2, respectively. Effective
cleavage of pBR322 DNA is induced by 1.Their interaction with
DNA of cancer cells may account for potency.
Abstract: Environmental and toxicological characteristics of formulated pesticides may substantially differ from those of their active ingredients or other components alone. This phenomenon is demonstrated in the case of the herbicide active ingredient glyphosate. Due to its extensive application, this active ingredient was found in surface and ground water samples collected in Békés County, Hungary, in the concentration range of 0.54–0.98 ng/ml. The occurrence of glyphosate appeared to be somewhat higher at areas under intensive agriculture, industrial activities and public road services, but the compound was detected at areas under organic (ecological) farming or natural grasslands, indicating environmental mobility. Increased toxicity of the formulated herbicide product Roundup compared to that of glyphosate was observed on the indicator aquatic organism Daphnia magna Straus. Acute LC50 values of Roundup and its formulating adjuvant polyethoxylated tallowamine (POEA) exceeded 20 and 3.1 mg/ml, respectively, while that of glyphosate (as isopropyl salt) was found to be substantially lower (690-900 mg/ml) showing good agreement with literature data. Cytotoxicity of Roundup, POEA and glyphosate has been determined on the neuroectodermal cell line, NE-4C measured both by cell viability test and holographic microscopy. Acute toxicity (LC50) of Roundup, POEA and glyphosate on NE-4C cells was found to be 0.013±0.002%, 0.017±0.009% and 6.46±2.25%, respectively (in equivalents of diluted Roundup solution), corresponding to 0.022±0.003 and 53.1±18.5 mg/ml for POEA and glyphosate, respectively, indicating no statistical difference between Roundup and POEA and 2.5 orders of magnitude difference between these and glyphosate. The same order of cellular toxicity seen in average cell area has been indicated under quantitative cell visualization. The results indicate that toxicity of the formulated herbicide is caused by the formulating agent, but in some parameters toxicological synergy occurs between POEA and glyphosate.
Abstract: L-asparaginase was extracted from pathogenic
Escherichia coli which was isolated from urinary tract infection
patients. L-asparaginase was purified 96-fold by ultrafiltration, ion
exchange and gel filtration giving 39.19% yield with final specific
activity of 178.57 IU/mg. L-asparaginase showed 138,356±1,000
Dalton molecular weight with 31024±100 Dalton molecular mass.
Kinetic properties of enzyme resulting 1.25×10-5 mM Km and
2.5×10-3 M/min Vmax. L-asparaginase showed a maximum activity
at pH 7.5 when incubated at 37 ºC for 30 min and illustrated its full
activity (100%) after 15 min incubation at 20-37 ºC, while 70% of its
activity was lost when incubated at 60 ºC. L-asparaginase showed
cytotoxicity to U937 cell line with IC50 0.5±0.19 IU/ml, and
selectivity index (SI=7.6) about 8 time higher selectivity over the
lymphocyte cells. Therefore, the local pathogenic E. coli strains may
be used as a source of high yield of L-asparaginase to produce anti
cancer agent with high selectivity.
Abstract: Chitosan is an attractive polysaccharide obtained by
deacetylation of an abundant natural biopolymer called chitin. Chitin
and chitosan are excellent materials. To improve the potential of
chitin and chitosan modification is needed. In the present study,
grafting of maleic acid on to chitosan by cerium ammonium nitrate in
acetic acid solution was investigated with use of a microwave and
reflux system. The grafted chitosan was characterized by using a
Fourier-transform infrared spectrometry. The solubility and swelling
behavior of grafted chitosans were determined in acetate buffer (pH
3.6), citrophosphate buffer (pH 5.6 and pH 7.0), and boric buffer (pH
9.2) solutions. The sample obtained by microwave system with use of
a chitosan/maleic anhydride/ceric ammonium nitrate 0.2/3.922/0.99
gram of raw material within 30 minute showed the maximum
swelling ratio (13.6) in boric buffer solution.
Abstract: The characterization of κ-carrageenan could provide a
better understanding of its functions in biological, medical and
industrial applications. Chemical and physical analyses of
carrageenan from seaweeds, Euchema cottonii L., were done to offer
information on its properties and the effects of Co-60 γ-irradiation on
its thermochemical characteristics. The structural and morphological
characteristics of κ-carrageenan were determined using scanning
electron microscopy (SEM) while the composition, molecular weight
and thermal properties were determined using attenuated total
reflectance Fourier transform infrared spectroscopy (ATR-FTIR), gel
permeation chromatography (GPC), thermal gravimetric analysis
(TGA) and differential scanning calorimetry (DSC). Further chemical
analysis was done using hydrogen-1 nuclear magnetic resonance (1H
NMR) and functional characteristics in terms of biocompatibility
were evaluated using cytotoxicity test.
Abstract: The antimicrobial, antiplasmid and cytotoxic activities of marine algae Halimeda opuntia and Sarconema filiforme were investigated. Antimicrobial bioassay against some human pathogenic bacteria and yeast were conducted using disc diffusion method. Halimeda extract exhibited antibacterial activity against six species of microrganisms, with significant inhibition against Staphylococcus aureus. While Sarconema extract was better potent as antifungal against Candida albicans. Comparative antibacterial studies showed that Halimeda extract showed equivalent or better activity as compared with commercial antibiotic when tested against Staphylococcus aureus. Further tests conducted using dilution method showed both extracts as having bacteriostatic mode of action against the tested microorganisms. Methanol extract of two species showed significant cytotoxicity (LC50
Abstract: Vernonia divergens Benth., commonly known as
“Insulin Plant” (Fam: Asteraceae) is a potent sugar killer. Locally the
leaves of the plant, boiled in water are successfully administered to a
large number of diabetic patients. The present study evaluates the
putative anti-diabetic ingredients, isolated from the in vivo and in
vitro grown plantlets of V. divergens for their antimicrobial and
anticancer activities. Sterilized explants of nodal segments were
cultured on MS (Musashige and Skoog, 1962) medium in presence of
different combinations of hormones. Multiple shoots along with
bunch of roots were regenerated at 1mg l-1 BAP and 0.5 mg l-1 NAA.
Micro-plantlets were separated and sub-cultured on the double
strength (2X) of the above combination of hormones leading to
increased length of roots and shoots. These plantlets were
successfully transferred to soil and survived well in nature. The
ethanol extract of plantlets from both in vivo & in vitro sources were
prepared in soxhlet extractor and then concentrated to dryness under
reduced pressure in rotary evaporator. Thus obtainedconcentrated
extracts showed significant inhibitory activity against gram
negative bacteria like Escherichia coli and Pseudomonas
aeruginosa but no inhibition was found against gram positive
bacteria. Further, these ethanol extracts were screened for in vitro
percentage cytotoxicity at different time periods (24 h, 48 h and 72 h)
of different dilutions. The in vivo plant extract inhibited the growth of
EAC mouse cell lines in the range of 65, 66, 78, and 88% at 100, 50,
25 & 12.5μg mL-1 but at 72 h of treatment. In case of the extract of in
vitro origin, the inhibition was found against EAC cell lines even at
48h. During spectrophotometric scanning, the extracts exhibited
different maxima (ʎ) - four peaks in in vitro extracts as against single
in in vivo preparation suggesting the possible change in the nature of
ingredients during micropropagation through tissue culture
techniques.
Abstract: The aim of the study was to investigate phytochemical
properties, antimicrobial activity and cytotoxicity of Aloe vera. The
phytochemical screening of the extracts of leaves of A. vera revealed
the presence of bioactive compounds such as alkaloids, tannins,
flavonoids phenolic compounds, and etc. with absence of cyanogenic
glycosides. Three different solvents such as methanol, ethanol and
Di-Methyl sulfoxide were used to screen the antimicrobial activity of
A. vera leaves against four human clinical pathogens by agar well
diffusion method. The maximum antibacterial activities were
observed in methanol extract followed by ethanol and Di-Methyl
sulfoxide. It was also found that remarkable antibacterial activities
with methanolic and ethanolic extracts of A. vera compared with the
standard antibiotic, tetracycline that was not active against E. coli
and S. boydii and supported the view that A. vera is a potent
antimicrobial agent compared with the conventional antibiotic.
Moreover, the brine shrimps (Artemia salina) toxicity test exhibited
LC50 value was 569.52 ppm. The resulting data indicated that the A.
vera plant have less toxic effects on brine shrimp. Hence, it is
signified that Aloe vera plant extract is safe to be used as an
antimicrobial agent.
Abstract: A series of 1-(1H-benzimidazol-2-yl)-3-(substituted phenyl)-2-propen-1-one were allowed to react with hydrazine hydrate and phenyl hydrazine in submitted reactions to get pyrazoline and phenyl pyrazoline derivatives. All the compounds entered for screening at the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv strain (ATCC 27294) using Microplate Alamar Blue Assay (MABA) susceptibility test. The results expressed as MIC (minimum inhibitory concentration) in μg/mL. Among the fifteen compounds, eight compounds were found to have MIC values less than 10 μg/mL. These were subjected for cytotoxicity assay in VERO cells to determine CC50 (cytotoxic concentration 50%) values and finally SI (Selectivity Index) were calculated. Compound (XV) 2-[5-(4- fluorophenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-1Hbenzimidazole was considered the best candidate of the series that could be a good starting point to develop new lead compounds in the fight against tuberculosis.
Abstract: Spherical shaped magnetite (Fe3O4) and Au@Fe3O4
nanoparticles were successfully synthesized from Fe electrodes
immersed in water with CTAB surfactant and HAuCl4 solution using
simple method-pulsed plasma in liquid, without the use of dopants or
special conditions for stabilization. Vibrating sample magnetometer
indicated ferromagnetic behavior of particles at room temperature with
coercivity and saturation magnetization of (Hc=105 Oe, Ms=6.83
emu/g) for Fe3O4 and (Hc=175, Ms=3.56emu/g) for Au@Fe3O4
nanoparticles. Structure and morphology of nanoparticles were
characterized by X-ray Diffraction analysis and HR-TEM
measurements. The cytotoxicity of nanoparticles was indicated using a
XTT assay to be very low (cell viability: 98-89% with Fe3O4 and
99-91% for Au@Fe3O4 NPs).
Abstract: The methanolic extracts from seeds of tamarind
(Tamarindus indica) was prepared by Soxhlet apparatus extraction
and evaluated for total phenolic content by Folin-Ciocalteu method.
Then, methanolic extract was screened biological activities (In vitro)
for anti-melanogenic activity by tyrosinase inhibition test, antiinflammation
activity by cyclooxygenase 1 (COX-1) and
cyclooxygenase 2 (COX-2) inhibition test, and cytotoxic screening
test with Vero cells. The results showed that total phenolic content,
which contained in extract, was contained 27.72 mg of gallic acid
equivalent per g of dry weight. The ability to inhibit tyrosinase
enzyme, which exerted by Tamarind seed extracts (1 mg/ml) was
52.13 ± 0.42 %. The extract was not possessed inhibitory effect to
COX-1 and COX-2 enzymes and cytotoxic effect to Vero cells. The
finding is concludes that tested seed extract was possessed
antimelanogenic activity with non-toxic effects. However, there was
not exhibited anti-inflammatory activity. Further studies include the
use of advance biological models to confirm this biological activity,
as well as, the isolation and characterization of the purified
compounds that it was contained.
Abstract: Engineered nanoparticles’ usage rapidly increased in
various applications in the last decade due to their unusual properties.
However, there is an ever increasing concern to understand their
toxicological effect in human health. Particularly, metal and metal
oxide nanoparticles have been used in various sectors including
biomedical, food and agriculture. But their impact on human health is
yet to be fully understood. In this present investigation, we assessed
the toxic effect of engineered nanoparticles (ENPs) including Ag,
MgO and Co3O4 nanoparticles (NPs) on human mesenchymal stem
cells (hMSC) adopting cell viability and cellular morphological
changes as tools The results suggested that silver NPs are more toxic
than MgO and Co3O4NPs. The ENPs induced cytotoxicity and
nuclear morphological changes in hMSC depending on dose. The cell
viability decreases with increase in concentration of ENPs. The
cellular morphology studies revealed that ENPs damaged the cells.
These preliminary findings have implications for the use of these
nanoparticles in food industry with systematic regulations.
Abstract: Oleic acid (C18:1) play an important role in
proliferation of fat cells. In this study, the effect of oleate on cells
viability in 3T3-L1 cells (fat cells) was investigated. The 3T3-L1
cells were treated with various concentrations of oleate in the
presence of 23 mM glucose. Oleate was added to adipogenic media
(day 0) to investigate the influence of oleate on proliferation of
postconfluent preadipocytes after 24 h induction. 0.1 mM oleate
promoted cell division by increasing 33.9% number of cells from
basal control in postconfluent preadipocytes. However, there were no
significantly different in cells viability with control cells when oleate
concentrations were increased up to 0.5 mM. When added to
differentiated adipocytes (day 12) for 48 h, the number of cells
decreased as oleate concentrations increased. 92.7% of cells lost
demonstrated apoptosis and necrosis after 48 h with 0.5 mM oleate.
The fluorochrome staining was examined under fluorescence
microscopy using acridine orange and ethidium bromide double
staining. Furthermore, the presence of high lactate (60.6% increased
from basal control) released into plasma has shown the direct
cytotoxicity of 0.5 mM oleate on adipocytes.
Abstract: This study determines the effect of naked and heparinbased
super-paramagnetic iron oxide nanoparticles on the human
cancer cell lines of A2780. Doxorubicin was used as the anticancer
drug, entrapped in the SPIO-NPs. This study aimed to decorate
nanoparticles with heparin, a molecular ligand for 'active' targeting
of cancerous cells and the application of modified-nanoparticles in
cancer treatment. The nanoparticles containing the anticancer drug
DOX were prepared by a solvent evaporation and emulsification
cross-linking method. The physicochemical properties of the
nanoparticles were characterized by various techniques, and uniform
nanoparticles with an average particle size of 110±15 nm with high
encapsulation efficiencies (EE) were obtained. Additionally, a
sustained release of DOX from the SPIO-NPs was successful.
Cytotoxicity tests showed that the SPIO-DOX-HP had higher cell
toxicity than the individual HP and confocal microscopy analysis
confirmed excellent cellular uptake efficiency. These results indicate
that HP based SPIO-NPs have potential uses as anticancer drug
carriers and also have an enhanced anticancer effect.