Thiosemicarbazone and thiazolylhydrazones of 1-indanone: as a new class of nonacidic anti-inflammatory and antiplatelet aggregation agents

This research based on the anti-inflammatory and antiplatelet aggregation properties of some new thiazolyl hydrazone derivatives of 1-indanone. In this regard a thiosemicabazone and twelve thiazolyl derivatives of 1-indanone have been synthesized. Out of these synthetic compounds seven derivatives 1-3, 6, 11-13 exhibited varying degree of anti-inflammatory action with IC50 esteems going from 5.1+/-1.3 - 78.8+/-4.6µM/mL. Compound 1 [IC50 =5.1+/-1.9µM] displayed potent result than standard ibuprofen [IC50 = 11.2+/-1.9 µM]. In antiplatelet aggregation assay, five compounds 1, 5, 6, 8 and 11 were observed to be dynamic with IC50 esteems observed in the range of 38.34-255.7+/-4.1µM, whereas, aspirin [IC50 = 30.3+/-2.6 µM] was used as standard. However, compound 11 was found to be good active for both anti-inflammatory and antiplatelet aggregation activities [IC50 = 13.9+/-4.9µg/mL] [IC50 = 38.60+/-3.1µM], respectively

Metal-based biologically active compounds: synthesis, spectral and antioxidant studies of transition metal complexes with hydrazone derivatives

New series of Co+2, Ni+2, Cu+2 and Zn+2 complexes have been synthesized using a bio-active hydrazone compound 4-hydroxybenzaldehyde-N-[5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene], abbreviated as [HL]. Complexes were characterized using elemental analysis, FT-IR, UV-visible spectroscopy conductivity and magnetic susceptibility measurements. Results showed that the bi-dentate [HL] coordinated in a square planner manner with Cu+2 while for the rest of the M+2 ions, it coordinated in a octahedral fashion. Free ligand and its metal complexes were also studied for their antioxidant potential by employing two methods i.e. DPPH radical scavenging and reducing power assay. It was observed that the metal complexes were considerably more potent free radical scavenger and had better reducing abilities compared to the free ligand, furthermore, for both in vitro assays, metal complexes turned out to be better DPPH scavengers and had better reducing abilities than the standards used during biological assays

Synthesis of drug metal complexes and their influence on human platelet aggregation

During the past few decades the emergence of inorganic medicinal chemistry has been developed novel therapeutic agents. Researcher's perseverance in this branch of chemistry has led them to explore further valuable chemical spaces by synthesizing metal complexes already known pharmacological agents for their potential use. However, it is in its early stage, this methodology has demonstrated metal complexes with better bioactivities than the parent ligand molecules. In this study, transition metal complexes of pyrazinamide [PZ], isoniazid [INH], fluconazole [FCZ], metformin [dimethylbiguanide, DMBG] and losartan potassium [LS-K] were selected to evaluate for their possible anti-platelets aggregation in the light of reports on divalent and trivalent cations like calcium, copper, manganese, magnesium, and cadmium may influence the process of thrombocytic activity and aggregation. The required evaluation was carried out on human plasma through an APACT 4004 platelet aggregation analyzer. Arachidonic acid [ADP] was used to gauge any alteration in platelet shape and aggregation process. The parent drugs showed some antiplatelets aggregation, however, their metal complexes demonstrated better efficacy

Spectroscopic and cytotoxic studies of losartan complexes

Use of drug-metal complexes for the treatment of several human diseases has resulted in significant progress in the field of medicinal inorganic chemistry. The current study describes the synthesis and characterization of Cu [II] and Ni [II] complexes of Losartan, an antihypertensive drug. These complexes were evaluated for their cytotoxic activity against four human cancer cell lines; SNB-19, HCT-15, COLO-205 and KB-3-1. Spectroscopic characterization revealed that during complex formation, the metal was bound through the nitrogen atoms of the tetrazole moiety of the losartan molecule. The molecular formulas of copper [[Cu [LS][2] Cl[2]].6H[2]O] and nickel [[Ni [LS][2]Cl[2]]. H[2]O] complexes were found to be in agreement with the analytical data obtained through elemental analysis. For both the complexes, metal to ligand ratios of 1:2 were calculated. As revealed by FTIR, UV-Visible, and 1H-NMR studies, both the complexes displayed octahedral geometries. Scanning electron microscopy [SEM] revealed marked changes in the morphology of the complexes, compared to the pure drug. From XRD studies, characteristic crystalline peaks of pure losartan were observed whereas no prominent peaks were observed for its complexes. Complexes were found to be inactive in the cytotoxic activity test performed using SNB-19, HCT-15, COLO-205 and KB-3-1 cell lines

Fluconazole and its interaction with metal [II] complexes: SEM, Spectroscopic and antifungal studies

The human digestive tract contains some 100 trillion cells and thousands of species of micro-organisms may be present as normal flora of this tract as well as other mucocutaneous junctions of the body. Candida specie is the most common organism residing in these areas and can easily invade the internal tissues in cases of loss of host defenses. Modifications of previously existing antifungal agents may provide new options to fight against these species. Inorganic compounds of different antifungals are under investigations. Present study report six complexes of fluconazole with Cu [II]], Fe[II], Cd[II], Co[II], Ni[II] and Mn[II] have been synthesized and characterized by elemental analysis, IR, UV and H-NMR. The elemental analysis and spectroscopic data were found in agreement with the expected values as the metal to ligand value was 1:2 ratios with two chlorides in coordination sphere. The morphology of each complex was studied using scanning electron microscope and compared with fluconazole molecule the flaky-slab rock like particles of pure fluconazole was also observed as reported earlier. However, the complexes of fluconazole were showed different morphology in their micrograph. Fluconazole and its complex derivatives have also been screened in vitro for their antifungal activity against Candida albican and Aspergillus niger by MIC method. The complexes showed varied activity ranging from 2-20%

Synthesis, characterization and enzyme inhibitory activity of new pyrazinamide iron complexes

The present paper deals with synthesis, characterization and amylase inhibitory activity of pyrazinamide [PYZ] with iron in its both [II] and [III] oxidation states. The synthesized complexes were characterized on the basis of IR, UV, [1]H-NMR, [13]C-NMR, elemental analysis and SEM. Changes in IR data shows that PYZ form complex with octahedral geometry and binding sites are ring nitrogen and carbonyl group, wherein two sides are satisfied with two chloride ions. SEM images indicate the crystalline state and surface morphology of PYZ and its complexes. Elemental analysis proves the composition of complexes. Pyrazinamide and the complexes showed no significant effect on amylase activity but the activity was inhibited in the presence of ferrous chloride

Metal complexes of isonicotinylhydrazide and their antitubercular activity

The development and spreading of Multi Drug Resistant TB strains is hampering endeavours for the control and administration of tuberculosis [TB]. The expansion episodes of multi-medication safe strains of Mycobacterium tuberculosis against first and second line antituberculosis drugs on one side and the unfavourable effects of these drugs on the other side has led the enthusiasm of researcher towards the synthesis of metal complexes of various medication. This approach is born with the expectation of finding new antituberculous operators without or least reactions as well as being active against the resistant strains of Mycobacterium tuberculosis. This study concentrates on the screening of five metal complexes of isoniazid [INH] against five Mycobacterium tuberculosis strains. These strains have been confirmed by WHO being active and even proliferating safely even in the presence of pyrazinamide, isoniazid [INH], ethambutol and rifampicin. In this work INH was taken as reference medication. All synthesized complexes and INH were subjected for a month and a half in BACTEC MGIT 960 technique. INH and its Fe [II] complex restrained the development of all bacterial strains for merely two weeks, while the Fe[III], Cu[II], Co [II] and Mn [II] complexes repressed the development five strains for three weeks. Conclusively, the strains utilized in this study were discovered to be more susceptible to the later four complexes than the ligand [INH] drug and its Fe [II] complex. Furthermore, elemental analysis and atomic absorption of all complexes were conducted for the determination of metal to ligand ratio

Cytotoxic and acute toxicity studies of isoniazid derivatives

Cancer is ultimately the result of cells that hysterically grow and do not die. Cells can experience uncontrolled growth if there are mutations to DNA, and therefore, alterations to the genes involved in cell division. Cancer occurs when a cell's gene mutations make the cell unable to correct DNA damage and is unable to destroy itself. There are over 100 different types of cancer each classified by the type of initially affected cell. Isoniazid, a well-known antitubercular agent has been reported to exhibit some cytotoxic activity. This finding prompt us to carry out this study where isoniazid and its sixteen derivatives were studied for any possible cytotoxic activity against Human astrocytoma SNB-19 cells, human Dukes' type C colorectal adenocarcinoma HCT-15 cells, human Dukes' type D colorectal adenocarcinoma COLO-205 cells, and human prostate adenocarcinoma [grade IV] PC-3 cells. Among the test compounds, SN-07 [a phenacyl derivative with para phenyl substitution] demonstrated slight cytotoxic effects on two types of human colorectal adenocarcinoma cells HCT-15 and COLO-205. Moreover, the acute toxicity of the compounds was also estimated in which some compounds were evaluated with more LD[50] values than isoniazid

Cancer Cell Viability And Survival In Vitro As Function Of Cell Surface Electric Charge : An Analytical Study

Electrical charge is an indicator of the cellular state of health. In cells, the cell membrane is a leaky dielectric. Capacitors are composed of two conducting sheets separated by a thin layer of insulating material known as a dielectric. Cells contain several forms of biological capacitors, which consist of an insulating material (the membrane) covered on both sides by collection of charged dissolved minerals, which serve the function similar to a conducting metal plate. This means that any condition, illness or change in dietary intake that affects the composition of the cell membranes and their associated minerals can affect and alter cellular capacitance. Healthy cells have a higher whole cell and cytoplasm conductivity and higher membrane capacitance than the malignant cells. The electric charge of cell membranes of mammals is negative at physiological pH. It is well-known that surface of cancer and tumor cells carry negative charge in excess to that of normal cells which is responsible for their increased mobility and invasiveness. The high negative surface charge on malignant cells and trophoblasts may mediate the lack of immune rejection of these cells. Thus, neutralizing or removing the tumor cell negative charge may allow negatively charged lymphocytes to approach and destroy them and thereby, the viability and survival of the cancer cells may be affected at least in vitro. The present study serves to - test this hypothesis on invasive human breast carcinoma cell line MDA-MB-231 (ER ) using specially designed and constructed combination of circuits. Preliminary results showed that out of the 8 designed circuits, sets 1, 2 and 7 were able to produce significant growth inhibition of MDA cells in vitro. The application of electrostatic field through specially designed circuits is unique and has never been reported previously. Our long-term goal is to develop a minimally invasive device that will selectively target and destroy both metastatic and non-metastatic cancer cells in humans. Better understanding of effect of decreasing surface charge density of tumor cells may lead to device effective treatment strategy of human tumors in future.

In vivo antineoplastic activities of benzoin thiosemicarbazone and para-anisaldehyde semicarbazone against ehrlich ascites carcinoma cells

Two Schiff bases, namely benzoin thiosemicarbazone [BTSC] and para-anisaldehyde semicarbazone [PAS], were synthesized and characterized. The antineoplastic activities of these Schiff bases were studied against Ehrlich ascites carcinoma [EAC] cells in Swiss albino mice by monitoring tumor cell growth inhibition, tumor weight measurement, survival time of tumor-bearing mice, bioassay of these compounds, and counting the total number of peritoneal cells as well as macrophages. Hematological parameters were also studied. It was found that these compounds significantly reduced tumor cell growth rate, decreased tumor weight, and increased life span of EAC-bearing mice. These test compounds restored the hematological parameters of EAC-bearing mice to normal. These compounds also enhanced the number of macrophages in normal mice. The results obtained were compared with those obtained with the standard drug bleomycin

Health issues confronting muslims on hajj

Objective: To determine the prevalence of health issues among hajj pilgrims and the factors associated with them

Method: An observational study conducted during hajj [Year 2011] using a questionnaire which was filled by pilgrims on their visit to the health clinics conducted by the Imamia Medics International

Results: During the period, pilgrims presented complaints related to the respiratory system 52.5% [n=394] followed by musculoskeletal system 29.6% [n=222], gastrointestinal system 15.5%[n=116], skin problems 5.9%[n=44], central nervous system 3.1%[n=23], cardiovascular system 2.9%[n=22], reproductive system 2.7%[n=20], urinary tract problems 2.3%[n=17] were dealt with. Out of 750, 17.9% [n=134] were diabetic and 26.4% [n=198] were hypertensive. Amongst the total, 24.8% [n=186] were vaccinated against hepatitis while 35.7% [n=268] were vaccinated against pneumonia. An astonishingly high percentage of the pilgrims had no prior immunization to both hepatitis and pneumonia

Conclusion: This data tries to emphasize awareness regarding the importance of vaccination and the potential problems which are faced by diabetic, hypertensive and older population which can help to improve the health condition of hajj pilgrims and can lessen the burden faced by concerned authorities

effect of sunshine on vitamin 03 deficient patients, working in farm fields

Objectives: To determine the effect of sunshine on the blood level of vitamin D3 deficient patients working in open agriculture fields

Study Design: This is a cross sectional, prospective and descriptive study

Place And Duration: Fatima hospital, Baqai Medical University, from Jan 2010 to Dec 2011

Methodology: All adult patients between 18 and 50 years old who were working in open agricultural fields and were attending outpatient departments with unexplained chronic skeletal aches and pains were advised to get their Vitamin D3 blood level along with other relevant blood tests They had no obvious cause of aches and pains. These patients were advised to expose their body to sunlight for three months, at least half an hour daily. No supplement in the form of Vitamin D was given. Blood level of Vitamin D3 was repeated at monthly intervals

Results: In this study 500 patients were studied. Out of these 470 [94%] were females and 30 [6%] were males. Deficient levels of Vitamin D3 were found in all male and 468 [99.57 %] female patients while 2 females [0.42%] were found to have an insufficient level of Vitamin D3 in serum. Not a single patient showed improvement in three months' time

Conclusion: Vitamin D3 deficiency and insufficiency were seen in workers in open fields who were exposed to sunlight for more than six hours daily. Exposure to sunlight is not having a positive effect on improvement of vitamin D3 level incur patients. Without supplements it is not possible to improve Vitamin D level

Comparative pharmacokinetics of levofloxacin in healthy volunteers and in patients suffering from typhoid fever

The aim of this study was to characterize the effect of typhoid fever on pharmacokinetic parameters of levofloxacin [LF] and compare the pharmacokinetic parameters of the said antibiotic in healthy human volunteers and patients with typhoid fever. Total of 12 subjects were divided into two groups "A" [healthy volunteers] and "B" [typhoid patients]. Single oral dose of LF 500 mg was given and 5 mL of blood was collected from each subject at 0, 0.25, 0.5, 1, 2, 3, 6, 12, 24, 36 and 72 h. Plasma concentrations of LF were measured by HPLC. Pharmacokinetic parameters were calculated from plasma concentration-time data by using MW/PHARM pharmacological analysis. In healthy volunteers, the average pharmacokinetic parameters were as C[max] [6.79 Microg/mL], T[max] [1.84 h], T[½] [10.03 h], Ka [2.23 h[-1]], AUC [110.09 [micro]gh/mL], Vd [85.84 L], Cl [4.57 L/h] and in typhoid patients were C[max] [6.90 Microg/mL], T[max] [1.82 h], T[½] [9.42 h], Ka [2.21 h[-1]], AUC [105.55 [micro]gh/mL], Vd [64.31 L], Cl [4.75 L/h]. The difference between pharmacokinetic parameters of LF in healthy human volunteers and typhoid patients was calculated by using unpaired t-test. As the p-value in case of all pharmacokinetic parameters was more than 0.05, the difference between pharmacokinetic parameters in both healthy human volunteers and typhoid patients was insignificant. It is concluded that there is no need to adjust the dose of LF in typhoid patients

Hepatoprotective effect of acetone semicarbazone on Ehrlich ascites carcinoma induced carcinogenesis in experimental mice

<p><b>OBJECTIVE</b>To determine the hepatoprotective effect of acetone semicarbazone (ASC) in vivo in normal and Ehrlich ascites carcinoma (EAC) bearing male Swiss albino mice.</p><p><b>METHODS</b>Drug-induced changes in biochemical and behavioral parameters at dose of 2.0 mg/kg body weight for 14 d and nullifying the toxicity induced by EAC cells were studied. The histopathology studies of the protective effects of ASC on vital organs were also assessed.</p><p><b>RESULTS</b>The administration of ASC made insignificant changes in body weight and behavioral (salivation, diarrhea, muscular numbness) changes during treatment period due to minor toxicity were minimized after the treatment in normal mice. The biochemical parameters, including serum glutamate pyruvate transaminase, glutamate oxaloactate transaminase, alkaline phosphatase, serum glucose, cholesterol, urea, triglyceride and billirubin changed modestly in normal mice receiving ASC. Though the treatment continued, these values gradually decreased to normal level after the treatment. In EAC bearing mice, the toxic effects due to EAC cells in all cases were nullified by treatment with the ASC. Significant abnormalities were not detected in histology of the various organs of the normal mice treated with ASC.</p><p><b>CONCLUSIONS</b>ASC can, therefore, be considered safe in formulating novel anticancer drug, as it exhibits strong protective effect against EAC cell bearing mice.</p>

Relationship between histone modification and seizures in rat brain

To see the effect of progesterone on GABA transporter-1 and glutamate transporter-2 expression in the cerebral contex of developing rats after recurrent seizures. Quasit experimental study. This study was carried out in Experimental laboratory at Pediatrics Department, Xiangya 2[nd] Hospital, Central South University Changsha Human P.R. China, from September 2011 to April 2011. This experiment included 90 PN-7d the SD rats, Flurothyl to cause convulsions in group and progesterone in the intervention group, one died, died of status epilepticus, a mortality rate of 2.2% in each group were randomly selected eight test SD rats [72] for the analysis of experimental results. Flurothyl induced seizures stopped after the group of SD rats had no spontaneous seizures is the emergence of limb movement disorder and abnormal reactions. The cerebral cortex GAT-1 immunohistochemistry AOD changes in the control group, PN-13D [ARS-1d], the PN-15d [ARS-3d] and PN-19d Service [ARS-7d], the convulsions rats cerebral cortex GAT-1 immunohistochemistry AOD expression than the control group was significantly higher [P<0.01]; progesterone in the intervention group, the GAT-1 immunohistochemistry AOD than the convulsions were significantly lower [P<0.01] difference between the groups is not significant. The cerebral cortex GAT-1 protein expression was significantly higher and progesterone in the intervention group [P<0.01]; progesterone at each time point after the intervention of the GAT-1 expression levels than the control groups was significantly increased statistically significant [P<0.01]. Changes of expression of the GLT-1 protein in the rat cerebral cortex in the control group, the PN-13d, PN-15d and PN 19d cerebral cortex of the GLT-1 protein expression was no significant difference [F= 1, 852, P= 0.182]. In conclusion, Progesterone through its participation in regulation of neonatal recurrent seizures caused by an imbalance in the brain cerebral cortex, GAT-1, GLT-1 expression, the maintance of the central nervous system excitation-inhibition of the balance of the system, which play an anticonvulsant effect

Frequency of low birth weight in primigravida reported PUMHS hospital Nawabshah

To determine the frequency of low birth weight in primigravida reported at PMC Hospital Nawabshah. Descriptive case series study. Departments of Gynaecology and Obstetrics and paeds medicine, at Peoples University of Medical and Health Sciences Nawabshah, from Jan 2011 to the Dec 2011. this study consisted of 319 pregnant women at 16 weeks of gestational age with singleton pregnancy reporting to the Antenatal Clinic, Obstetrics and Gynaecology Department were selected. Weight was measured by using weight machine throughout antenatal checkups. Weight and height was measured by same person rechecked. Their pregnancies were followed to assess the low birth weight. The neonatologist evaluated the babies. All primigravida women in the reproductive age group between >18 to <35 years with singleton pregnancy, normal fetal lie, and Height 5 feet or more were included. Exclusion criteria were patients associated with uterine anomalies [like uterine polyp, uterine septae, submucosal fibroid], smoking, short stature, other medical disorder like diabetes, hypertension, thyroid disorders, epilepsy and asthma. Results were prepared with help of tables and graphs. Data was analyzed through SPSS software. 319 patients included in this study. There was a wide variation in age was noted. The youngest patient was 18 years old and the oldest patient was 35 years old. The mean age was 21.21 + 4.22 years and peak age group for presentation of primigravida in our study is 26 to 30 years. clinical asses the fetal weight and observed 42 [13.16%] cases were <3.5kg weight while remaining 277[86.83%] cases were 2.5 to 4 kg weight. In conclusion, we observed in our study that low body weight of primigravida mother is associated with low birth weight babies

Effect of primers on the shear bond strength of two types of acrylic resin to CO-CR partial denture alloy

The absence or poor chemical bonding of acrylic resin to Cobalt-Chromium metal frameworks, often introduces microleakage and bond failure at the interface. The aim of this study was to compare the shear bond strength of sandblasted cast and ingot cobaltchromium alloy to heat-cured and self-cured acrylic resins primed with four different metal primers. Fifty Co-Cr Ingot and fifty cast specimens were fabricated and embedded in resin. Their surfaces were sandblasted and primed with four primers except for the control group. 4 x 5 mm discs of self-cure and heat-cured resins were processed against the alloy and stored in distilled water for 24 hours. Specimens were de-bonded in shear using a Universal testing machine. The data were analyzed statistically using ANOVA, and Fisher's PLSD test. In general, primed alloy specimens showed greater bond strength than the non-primed controls and heat-cured resin bonded better than the auto-polymerized resin. ZP primer demonstrated the highest bond strength regardless of type of alloy and resin. Monobond P demonstrated the lowest bond strength. The bond strength of primed specimens improved significantly compared to the control group. Within the limitation of this study, it is shown that primers enhanced the bond strength of acrylic resin and cast Co-Cr alloy. Therefore, metal primers such as ZP Primer and SR Primer are recommended for routine use in the process of fabrication of removable partial denture to increase its longevity

Hip pain and retinoids [Isotretinoin]

The retinoids are classes of chemical compounds that are related chemically to vitamin A. Retinoids are used in medicine, primarily due to the way they regulate epithelial cell growth. Retinoids are used in the treatment of many diverse diseases and are effective in the treatment of a number of dermatological conditions such as inflammatory skin disorders, skin cancers, disorders of increased cell turnover e.g. psoriasis and photo aging. Common skin conditions treated by retinoids include acne and psoriasis. These compounds being widely used have serious documented side effects including myalgia and arthralgia. We present a case where an 18 years male patient was given Isotretinoin a higher generations of retinoid, for his acne and after taking it for three days he presented in emergency department with severe hips pain, unable to stand and walk. This case has indicated that hip pain can be a result of a side effect of retinoids and its derivatives or new generation of retinoids

Prescribing and dispensing practices in a public sector pediatric ward in D.I.Khan, Pakistan

Inappropriate prescribing practices are seen in many health facilities in developing countries. Medication errors, especially, in pediatric inpatients occur at similar rates as in adults but have three times the potential to cause harm. Antibiotic resistance secondary to poor prescription and dispensing practices are also a major concern for both doctors and patients. To evaluate the prescribing and dispensing practices in pedriatric inpatients at major public health facility and suggest strategies to over come irrational drug use. A prospective study was conducted on 50 children whose data were taken from a pediatric wards of District Headquarter Teaching Hospital D.I.Khan from April to May 2008. Medication errors were characterized by subtypes, ordering, dispensing, dose [over or under dose], adverse drug reactions, potential drug interactions, and irrational drug use, route, and frequency errors. Overall 249 medications were assessed and medication errors rate of 66% was observed. Error rates included overdose errors 27%, potential adverse drug and interactions [9%] and irrational drug use [6%]. Majority of errors [70%] occurred at the ordering stage and involved errors in dosing [42.4%], route [6.1%] and frequency [24.2%]. The most common medication error was in the dosing which ranged from normal dose to 10 times the actual dose required. Antibiotics and steroids were the most common drugs with medication errors. Overall 4 medications per prescription were recorded. Errors contributed by physician were 55%, nursing staff 41%, and pharmacy 4%. High medication error rate in public sector health care facility indicates potential health risk to the children. This problem can be easily solved by appointing a pharmacist in major public sector hospitals