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: The article represents the results of research of
antitumor activity of different structural types of plant flavonoids
extracted by authors from Polygonum L. plants in commercial
reserves at the territory of the Republic of Kazakhstan. For the first
time ever the results comparative research of antitumor activity of
plant flavonoids of different structural groups and their synthetic
derivatives have been represented. The results of determination of
toxicity of flavonoids in single parenteral infusion conditions have
been represented. Experimental substantiation of possible
mechanisms of antiproliferative and cytotoxic action of flavonoids
has been suggested. The perspectives of usage of plant flavonoids as
medications and creation of effective dosage forms of antitumor
medicines on their basis have been substantiated.
Abstract: Epidermal Growth Factor (EGF, Mw=6,045) has been
reported to have high efficiency of wound repair and anti-wrinkle
effect. However, the half-life of EGF in the body is too short to exert
the biological activity effectively when applied in free form. Growth
Factors can be stabilized by immobilization with carbohydrates from
thermal and proteolytic degradation. Low molecular weight chitosan
(LMCS) and its derivate prepared by hydrogen peroxide has high
solubility. LM6A6DC was successfully prepared as a reactive
carbohydrate for the stabilization of EGF by the reactions of LMCS
with alkalization, tosylation, azidation and reduction. The structure of
LM6A6DC was confirmed by FT-IR, 1H NMR and elementary
analysis. For enhancing the stability of free EGF, EGF was attached
with LM6A6DC by using water-soluble carbodiimide.
EGF-LM6A6DC conjugates did not show any cytotoxicity on the
Normal Human Dermal Fibroblast (NHDF) 3T3 proliferation at least
under 100 μg/ml. In the result, it was considered that LM6A6DC is
suitable to immobilize of growth factor.
Abstract: Diminished antioxidant defense or increased
production of reactive oxygen species in the biological system can
result in oxidative stress which may lead to various
neurodegenerative diseases including Alzheimer’s disease (AD).
Microglial activation also contributes to the progression of AD by
producing several proinflammatory cytokines, nitric oxide (NO) and
prostaglandin E2 (PGE2). Oxidative stress and inflammation have
been reported to be possible pathophysiological mechanisms
underlying AD. In addition, the cholinergic hypothesis postulates that
memory impairment in patient with AD is also associated with the
deficit of cholinergic function in the brain. Although a number of
drugs have been approved for the treatment of AD, most of these
synthetic drugs have diverse side effects and yield relatively modest
benefits. Marine algae have great potential in pharmaceutical and
biomedical applications as they are valuable sources of bioactive
properties such as anticoagulation, antimicrobial, antioxidative,
anticancer and anti-inflammatory. Hence, this study aimed to provide
an overview of the properties of Malaysian seaweeds (Padina
australis, Sargassum polycystum and Caulerpa racemosa) in
inhibiting oxidative stress, neuroinflammation and cholinesterase
enzymes. These seaweeds significantly exhibited potent DPPH and
moderate superoxide anion radical scavenging ability (P
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: Although, arsenic trioxide has been the subject of
toxicological research, in vitro cytotoxicity and genotoxicity studies
using relevant cell models and uniform methodology are not well
elucidated. Hence, the aim of the present study was to evaluate the
cytotoxicity and genotoxicity induced by arsenic trioxide in human
keratinocytes (HaCaT) using the MTT [3-(4, 5-dimethylthiazol-2-yl)-
2,5-diphenyltetrazolium bromide] and alkaline single cell gel
electrophoresis (Comet) assays, respectively. Human keratinocytes
were treated with different doses of arsenic trioxide for 4 h prior to
cytogenetic assessment. Data obtained from the MTT assay indicated
that arsenic trioxide significantly reduced the viability of HaCaT cells
in a dose-dependent manner, showing an IC50 value of 34.18 ± 0.6
μM. Data generated from the comet assay also indicated a significant
dose-dependent increase in DNA damage in HaCaT cells associated
with arsenic trioxide exposure. We observed a significant increase in
comet tail length and tail moment, showing an evidence of arsenic
trioxide -induced genotoxic damage in HaCaT cells. This study
confirms that the comet assay is a sensitive and effective method to
detect DNA damage caused by arsenic.
Abstract: Complexation of anthocyanins to mimic natural
copigmentation process was investigated. Cyanidin-rich extracts from
Zea mays L. ceritina Kulesh. and delphinidin-rich extracts from
Clitoria ternatea L. were used to form 4 anthocyanin complexes,
AC1, AC2, AC3 and AC4, in the presence of several polyphenols and
a trace metal. Characterizations of the ACs were conducted by UV,
FTIR, DSC/TGA and morphological observations. Bathochromic
shifts of the UV spectra of 4 formulas of ACs were observed at peak
wavelengths of about 510-620 nm by 10 nm suggesting complex
formation. FTIR spectra of the ACs indicate shifts of peaks from
1,733 cm-1 to 1,696 cm-1 indicating interactions and a decrease in the
peak areas within the wavenumber of 3,400-3,500 cm-1 indicating
changes in hydrogen bonding. Thermal analysis of all of the ACs
suggests increases in melting temperature after complexation. AC
with the highest melting temperature was morphologically observed
by SEM and TEM to be crystal-like particles within a range of 50 to
200 nm. Particle size analysis of the AC by laser diffraction gave a
range of 50-600 nm, indicating aggregation. This AC was shown to
have no cytotoxic effect on cultured HGEPp0.5 and HGF (all p>
0.05) by MTT. Therefore, complexation of anthocyanins was simple
and self-assembly process, potentially resulting in nanosized particles
of anthocyanin complex.
Abstract: Anthocyanins are natural pigments with effective UV
protection but their topical use could be limited due to their
physicochemical characteristics. An attempt to overcome such
limitations by complexation of 2 major anthocyanin-rich sources, C.
ternatea and Z. mays, has potentiated its use as topical antiinflammatory.
Cell studies indicate no cytotoxicity of the
anthocyanin complex (AC) up to 1 mg/ml tested in HaCaT and
human fore head fibroblasts by MTT. Croton oil-induced ear edema
in Wistar rats suggests an effective dose of 5 mg/cm2 of AC as a
topical anti-inflammatory in comparison to 0.5 mg/cm2 of
fluocinolone acetonide. Niosomal encapsulation of the AC
significantly prolonged the anti-inflammatory activity particularly at
8 h after topical application (p = 0.0001). The AC was not cytotoxic
and its anti-inflammatory and activity was dose-dependent and
prolonged by niosomal encapsulation. It has also shown to promote
collagen type 1 production in cell culture. Thus, AC could be a
potential candidate for topical anti-inflammatory agent from natural
resources.
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: Abnormal adipocyte growth, in terms of increased cell numbers and increased cell differentiation, is considered to be a major pathological feature of obesity. Thus, the inhibition of preadipocyte mitogenesis and differentiation could help prevent and suppress obesity. The aim of this study was to assess whether extracts from Weissella koreensis 521 cells isolated from kimchi could exert anti-adipogenic effects in 3T3-L1 cells (fat cells). Differentiating 3T3-L1 cells were treated with W. koreensis 521 cell extracts (W. koreensis 521_CE), and cell viability was assessed by MTT assays. At concentrations below 0.2 mg/ml, W. koreensis 521_CE did not exert any cytotoxic effect in 3T3-L1 cells. However, treatment with W. koreensis 521_CE significantly inhibited adipocyte differentiation, as assessed by morphological analysis and Oil Red O staining of fat. W. koreensis 521_CE treatment (0.2 mg/ml) also reduced lipid accumulation by 24% in fully differentiated 3T3-L1 adipocytes. These findings collectively indicate that Weissella koreensis 521 may help prevent obesity.
Abstract: Protein hydrolysates prepared from a number of medicinal plants are promising sources of various bioactive peptides. In this work, proteins from dried whole plant of Euphorbia hirta Linn. were extracted and digested with pepsin for 12h. The hydrolysates of lesser than 3 KDa were fractionated by a cut-off membrane. The peptide hydrolysate was then purified by an anion-exchange chromatography on DEAE-Sephacel™ column and reverse-phase chromatography on Sep-pak C18 column, respectively. The cytotoxic effect of each peptide fraction against a gastric carcinoma cell line (KATO-III, ATCC No. HTB103) was investigated using colorimetric MTT viability assay. A human liver cell line (Chang Liver, CLS No. 300139) was used as a control normal cell line. Two purified peptide peaks, peak l and peak ll at 100µg peptides mL-1 affected cell viability of the gastric cancer cell lines to 63.85±4.94 and 66.92±6.46%, respectively. Our result showed for the first time that the peptide fractions derived from protein hydrolysate of Euphorbia hirta Linn. have anti-gastric cancer activity, which offers a potential novel and natural anti-gastric cancer remedy.
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: 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: Semiconductor nanomaterials like TiO2 nanoparticles
(TiO2-NPs) approximately less than 100 nm in diameter have become
a new generation of advanced materials due to their novel and
interesting optical, dielectric, and photo-catalytic properties. With the
increasing use of NPs in commerce, to date few studies have
investigated the toxicological and environmental effects of NPs.
Motivated by the importance of TiO2-NPs that may contribute to the
cancer research field especially from the treatment prospective
together with the fractal analysis technique, we have investigated the
effect of TiO2-NPs on colony morphology in the dark condition
using fractal dimension as a key morphological characterization
parameter. The aim of this work is mainly to investigate the cytotoxic
effects of TiO2-NPs in the dark on the growth of human cervical
carcinoma (HeLa) cell colonies from morphological aspect. The in
vitro studies were carried out together with the image processing
technique and fractal analysis. It was found that, these colonies were
abnormal in shape and size. Moreover, the size of the control
colonies appeared to be larger than those of the treated group. The
mean Df +/- SEM of the colonies in untreated cultures was
1.085±0.019, N= 25, while that of the cultures treated with TiO2-NPs
was 1.287±0.045. It was found that the circularity of the control
group (0.401±0.071) is higher than that of the treated group
(0.103±0.042). The same tendency was found in the diameter
parameters which are 1161.30±219.56 μm and 852.28±206.50 μm
for the control and treated group respectively. Possible explanation of
the results was discussed, though more works need to be done in
terms of the for mechanism aspects. Finally, our results indicate that
fractal dimension can serve as a useful feature, by itself or in
conjunction with other shape features, in the classification of cancer
colonies.
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 main aim is to perform mutational analysis of CTLA4 gene Exon 1 in SLE patients. A total of 61 SLE patients fulfilling “American College of Rheumatology (ACR) criteria" and 61 controls were enrolled in this study. The region of CTLA4 gene exon 1 was amplified by using Step-down PCR technique. Extracted DNA of band 354 bp was sequenced to analyze mutations in the exon-1 of CTLA-4 gene. Further, protein sequences were identified from nucleotide sequences of CTLA4 Exon 1 by using Expasy software and through Blast P software it was found that CTLA4 protein sequences of Pakistani SLE patients were similar to that of Chinese SLE population. No variations were found after patients sequences were compared with that of the control sequence. Furthermore it was found that CTLA4 protein sequences of Pakistani SLE patients were similar to that of Chinese SLE population. Thus CTLA4 gene may not be responsible for an autoimmune disease SLE.
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.