Coll, Carlos; Fernández, María Alejandra; Coll, Sebastián; Coll, Tamara; Malliardi, Pablo; Perazzo, Juan; Filinger, Ester Julia; Lemberg, Abraham
We studied if monocrotaline (MCT) portal hypertensive model modifies blood-brain barrier (BBB) condition. Male Wistar rats were used: Group MCT injected i.p. with MCT (60 mg/kg of body weight) and Group Sham (GS) with saline. Forty-four days after injection rats were sacrificed. Trypan blue and Evans blue tests were performed to evaluate BBB integrity in both groups. In cerebrospinal fluid (CF), protein and glucose were determined. Alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (AP) were measured in serum samples. Portal pressure rose after MCT injection. Trypan blue diffused into hippocampus, Evans blue increased concentrations in brain of Group...
Sonawane, Lalit V.; Bari, Sanjaykumar B.
Docking studies of few substituted 5-benzyl-2, 4-thiazolidinedione moiety, which acts as peroxisome proliferator-activated receptor γ agonist was performed by using Glide v4.5. The docking studies reveal hydrogen bond formation to Thr241 with Gscore -7.22 and energy -62.2 kcal/mole. We found hydrogen bond formation of most of compounds with good Gscore and low energy as compared to the most active rosiglitazone.
Sonawane, Leena L.; Nirmal, Sunil A.; Rub, Ruksana A.; Goswami, Dhirendra; Bhawar, Sanjay B.; Dhasade, Vipul V.; Sonawane, Sneha D.
Tephrosia purpurea L. (Leguminosae), commonly known as Unhali in Marathi is a copiously
branched perennial herb. Traditionally the roots of this plant are used in the treatment of ulcer and colic
pain. So the present work was undertaken to validate its use in the treatment of ulcerative colitis by using
suitable scientific methods. Shade dried and coarsely powdered roots were subjected to successive extraction
with ethanol and water. The dried extracts (100 and 200 mg/kg) were screened for ulcerative colitis
using the method acetic acid induced ulcerative colitis in mice. Macroscopical study of the colon, level of
myeloperoxidase in colon and histopathology of the colon tissue...
Malaviya, Shailesh; Bhalodia, Yagnik; Vaghasiya, Jitendra; Manek, Ravi; Sheth, Navinchandra; Jivani, Nurudin
The present study was designed to investigate effects of rutin on isoproterenol induced myocardial infarction (MI) by considering enzyme level in rats. Rats were treated with rutin contineously for 10 days (10 mg/kg/day, i.p.,); MI were induced by treating rats with isoproterenol for last 2 consecutive days (5.25 and 8 mg/kg, i.p). Protein kinase C (PKC), malonylaldehyde (MAL), Glutathione (GSH), superoxide dismutase (SOD) and survival rate were evaluated. Rutin enhanced survival rate evaluated at the end of experiment. Result shows significant decrease in level of PKC (P < 0.001) and MAL enzyme (P < 0.01) while elevation of GSH (P...
Márquez, Diana M.; Márquez Fernández, María Elena; Martínez, Alejandro; Thomas, Olivier P.
Ethanol and dichloromethane extracts from the marine sponge Iotrochota birotulata collected
in the Urabá Gulf (Colombia) were tested against three human tumor cellular lines, including lung (A-
549), colon (HT29) and breast (MDA-MB-231), at 1 µg/mL, 5 µg/mL and 25 µg/mL. The most bioactive extract
(ethanol), was separated by flash column chromatography obtaining six fractions which biological
activity was evaluated on the same cellular lines A-549, HT29 and MDA-MB-231, at 1µg/mL, 5 µg/mL and
25 µg/mL. The bioassay results showed that both extracts and two of the fractions totally inhibited the
growing of the cellular line A549 at 25 µg/mL, while the most active fraction showed...
Kumar, Mahesh; Jain, Sandeep; Deep, Aakash
Ten new 4-thiazolidinone derivatives have been synthesized from the alkanoic acids. Alkanoic acid hydrazides (I) on refluxing with aromatic aldehydes in the presence of a catalytic amount of glacial acetic acid in methanol furnish corresponding hydrazones (II). Thioglycolic acid react with (II) in methanol yield the title compounds (III). These 4-thiazolidinone derivatives were characterized by CHN analysis, IR and 1H NMR spectral data. All the compounds were evaluated for their in vitro antimicrobial activity against two Gram negative strains (Escherichia coli and Pseudomonas aeruginosa) and two Gram positive strains (Bacillus subtilis and Staphylococcus aureus) and fungal strain Candida albicans and...
Staak Júnior, Marcos C.; Colchon, Paulo H.; Portes, Alice G.; Mezadri, Telmo. J.; Tames, David R.; Andrade, Sergio F.
This study aimed to evaluate the action of Brazilian green propolis (5%) topic use on cutaneous
wound healing in rats, by inflammatory cell counting. Ten Wistar rats were separated in groups 24
h and 72 h, were trichotomized under anesthesia on cervical-dorsal region, and 2 wounds were provoked
with a biopsy punch (5 mm diameter). Left wound underwent Brazilian green propolis topic treatment,
and right wounds received nothing. Tissue samples were processed for light microscopy with hematoxilineosin.,
and leucocytes, macrophages and fibroblasts were counted using a histometric reticule in ocular
lens. In both groups, within 24 and 72 h evolution, treated wounds demonstrated significant bigger means
Razi, Muhammad T.; Saadullah, Malik; Murtaza, Ghulam; Hassan, Waseem
The aim of present study was to determine the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. (SMe) in alloxan induced diabetic rabbits. It was further aimed to determine the effect of SMe on various biochemical parameters, namely blood glucose levels, total cholesterol, lipoproteins (HDL and LDL), liver functions (SGOT and SGPT), serum creatinine and urea level in alloxan induced diabetic rabbits. Rabbits were divided into five groups: one non-diabetic control, treated with vehicle and four experimental (diabetic) groups. The experimental groups can be described as diabetic negative control, treated with vehicle, diabetic positive control, treated with 80 mg/kg...
Yu, Xiaomin; Xu, Ren-ai; Li, Junwei; Ma Jianshe; Deng, Jie; Wang, Xianqin
A sensitive and selective liquid chromatography/electrospray mass spectrometry (LC-ESIMS)
method for determination of tetramethylpyrazine in rat plasma was developed. After addition of
phenacetin as internal standard, protein precipitation by acetonitrile was used as sample preparation.
Chromatographic separation was achieved on a Zorbax SB-C18 (2.1 mm×150 mm, 5 µm) column with
(40:60, v/v) acetonitrile-water containing 0.1 % formic acid as mobile phase. Electrospray ionization (ESI)
source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to
quantify tetramethylpyrazine using target fragment ions m/z 136.9 for tetramethylpyrazine and m/z 179.8
for the IS. Calibration plots were linear over the range of 20-4000 ng/mL...
Oyarzábal, Ambar; Jiménez, Sonia; Curveco, Dayisell; Pérez, Yohani; Molina, Vivian; Más, Rosa
Short-term (14 days) treatment with D-004, a lipid extract from Roystonea regia fruits, has
been shown to prevent testosterone (T)-induced prostate hyperplasia (PH) and increased oxidative stress
in rat prostate, but no study has documented if such effects persist after longer treatment. This study investigated
the persistence of the effects of D-004 orally given for 60 days for preventing prostate enlargement
and increase of oxidative markers in rats with T-induced PH. Rats were randomized into three
groups: a negative control and two T-injected that received orally vehicle (positive control) or D-004 (400
mg/kg/day), respectively. Prostate weights of positive controls significantly and markedly increased over
the time, while...
Bulani, Vipin D.; Ghaisas, Mahesh M.; Kumar, Dinesh; Sarda, Anupama P.; Bhamre, Sachin S.
Calotropis gigantea (Linn.) R.Br. (Asclepiadaceae), commonly known as milkweed or swallow- wort, is found chiefly in wasteland throughout India. It has been reported as a traditional folkloric medicine in treatment of asthma in the Indian literature. Roots containing α-and β-amyrin are reported to possess anti-lipoxygenase activity. Hence, our objective was to evaluate the effect of the methanolic extract of Calotropis gigantea (CG) root on egg albumin induced passive paw anaphylaxis and compound 48/80 induced mast cell degranulation in rats. CG were given at doses of 100, 200, 400 mg/kg, p.o., to rats. We found that CG significantly increases percentage inhibition...
Saiful, Azmi J.; Mastura, Mohtar; Mazurah, Mohamed I.; Nuziah, Hashim
In this study, methanol extracts from the leaf and stem of Dolichandrone spathacea (L.f) K.
Schum., a lesser-known local mangrove tree species, was evaluated using disc diffusion and minimum inhibitory
concentration (MIC) value determination assays against six strains of local MRSA clinical isolates
and one ATCC MRSA reference strain. The stem extract exhibited a higher zone of inhibition as compared
with the leaf extract against the tested isolates. Further qualitative evaluation of the stem extract
showed MIC values between 1.25 to 1.88 mg/ml against three selected MRSA clinical isolates. Phytochemical
screening revealed that the triterpene and saponin compounds might be responsible for the better inhibitory
Loscalzo, Leonardo M.; Wasowski, Cristina; Marder, Nora Mariel
Infusions of the inflorescences of Tilia are widely used for their tranquilizing properties around the world and have been regarded as non-toxic. Despite the widespread use of the tea of silver Linden in folk medicine, the number of scientific studies for the evaluation of its therapeutic utilization is limited. In an attempt to add experimental confirmation to its popular medicinal use, the central nervous system related effects of the chronic ingestion of the infusion of Tilia petiolaris DC. inflorescences were evaluated in the holeboard, locomotor activity and light-dark tests in mice. The infusion induced significant increases in the exploration of...
Varallo, Fabiana R.; Lima, Marcos F. R.; Galduróz, José C. F.; Mastroianni, Patricia C.
The objective of this study was to estimate the prevalence of adverse drug reactions (ADR) related to hospital admission of elderly people, identifying the use of potentially inappropriate medication (PIM) , the ADR and the risk factors associated with the hospitalization. A cross-sectional study was conducted in a private hospital of São Paulo State, Brazil. All patients aged ≥ 60 years, admitted in the general practice ward in May 2006 were interviewed about the drugs used and the symptoms/complaints that resulted in hospitalization. More than a half (54.5 %) of elderly hospitalizations were related with ADR. The therapeutic classes involved...
Bhaisare, Mukesh; Sahu, Kapendra; Karthikeyan, Chandrabose; Moorthy, N.S.H.N.; Trivedi, Piyush
A simple, specific, sensitive and validated RP-HPLC method for the simultaneous estimation of amlodipine (AMB) and valsartan (VAL) in marketed tablet formulation was developed. The analysis was carried out on a phenomenex C18 (250 x 4.6 mm, 5 µm) column using a mobile phase of 0.1% ortho phosphoric acid solution: acetonitrile (35:65 v/v, pH 3.0). The flow rate of the mobile phase was adjusted to 1.0 ml/min and was detected at 238 nm. The retention time obtained from the analysis was 1.995 min and 4.910 min for AMB and VAL respectively. The developed method was validated as per ICH guidelines....
Gouda, Ayman A.; Amin, Alaa S.
Eight direct spectrophotometric methods for determination of ganciclovir has been developed and validated. These methods were based on the oxidation of the drug by different inorganic oxidants: ceric ammonium sulphate, potassium permanganate, ammonium molybdate, ammonium metavanadate, chromium trioxide, potassium dichromate, potassium iodate and potassium periodate. The oxidation reaction were performed in perchloric acid medium for ceric ammonium sulphate and in sulfuric acid medium for the other reagents. Different variables affecting the reaction conditions were carefully studied and optimized. Under the optimum conditions, linear relationships with good correlation coefficients (0.9987- 0.9993) were found between the reading and the corresponding concentration of...
Wadekar, Sharadchandra B.; Kshirsagar, Sanjay J.; Gupta, Sunil R.; Shewale, Nitin S.; Bhalekar, Mangesh R.; Supe, Santosh
The purpose of the present study was to develop and optimize floating-bioadhesive bilayer
gastroretentive drug delivery system (GRDDS) exhibiting a unique combination of floatation and bioadhesion
to prolong residence in the stomach using captopril (CP) and hydrochlorothiazide (HCTZ) as a model
drug. Captopril being unstable in intestinal pH and HCTZ has specific absorption from duodenum and
the first part of the jejunum and to a small extent in the stomach are suitable candidate for GRDDS. 32
factorial design was employed in formulating and optimizing the GRDDS for bilayer tablet of CP and
HCTZ matrix tablet. The main effect and interaction terms were quantitatively evaluated using a...
Aamir, Muhammad F.; Ahmad, Mahmood; Murtaza, Ghulam; Khan, Shujaat A.
In this study, matrix type patch formulations of flurbiprofen using certain skin permeation
enhancers [isopropyl myristate (IPM), isopropyl palmitate (IPP) and Tween 80] were formulated, evaluated
and compared. The cumulative amounts permeated and the permeation rates were higher for the prepared
formulations as compared to the controls (without enhancers). The results also revealed better skin
permeation characteristics of flurbiprofen using IPM than other enhancers. The pharmacokinetic parameters
of the optimized formulation (F7), calculated from the blood levels of the drug, revealed a profile
with the ability to maintain adequate plasma levels for 24 h (i.e. up to the next application): AUC(0-24)
10.406 ± 1.34ng.h/ml, Tmax 1.5 ±...
Souza, Claudia A. de; Farago, Paulo V.; Duarte, Márcia do Rocio; Manfron Budel Jane
Baccharis is an important genus of Asteraceae and it comprehends approximately 400 species, many of which are frequently used in folk medicine as analgesic, diuretic, spasmolytic, antidiabetic, antiseptic and stomachic. Baccharis singularis belongs to the Singularis group and is popularly known as cambará-de-praia and cambará-da-serra. It is a shrub which occurs in Brazil, from Bahia to Rio Grande do Sul. The present study has aimed to investigate the morpho-anatomy of the aerial vegetative parts of this species for pharmacognostic purposes. The plant material was processed according to standard methods of light and scanning electron microscopy. Non-glandular trichomes, flagelliform, simple and...
Salman, Demet; Dogan, Aysegul; Basci, Nursabah E.
Cabergoline (CAB) is a synthetic ergoline dopamine agonist with high affinity to D2 receptors, thus used for the treatment of Parkinson's patients and hyperprolactinemia disorders. In this study, simple, fast, reliable and validated UV-VIS and 2nd order derivative spectrophotometric methods for determination of CAB in pharmaceutical preparations were developed without any previous sample preparation step. Determination of CAB was performed at 280 nm wavelength by UV-VIS spectrophotometry and in the range of 227-232 nm by 2nd order derivative spectrophotometry. Developed both spectrophotometric methods were linear over the range of CAB concentrations from 1 to 125 µg mL-1-. The highest relative...