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

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

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%

Antibacterial potential of Calotropis procera [flower] extract against various pathogens

Increased bacterial resistance towards commonly used antibiotics has become a debated issue all over the world in a last few decades. Due to this, consumer demand towards natural anti-microbial agents is increasing day by day

Natural anti-microbial agents have gained enormous attention as an alternative therapeutic agent in pharmaceutical industry

Current study is an effort to explore and identify a bactericidal potential of various solvent extracts of Calotropis procera flower

Flowers of C. procera were extracted with hexane, butanol, ethyl acetate and aqua to evaluate the antibacterial activity by agar well diffusion method against the various human pathogens. The microorganisms used in this study includes Salmonella typhi, Escherichia coll [O157:H7], Micrococcus luteus KJBGE-IB20 [Gen Bank accession: JQ250612] and methicillin resistant Staphylococcus aureus [MRSA] KIBGE-IB23 [Gen Bank accession: KC465400]

Zones of inhibition were observed against all four pathogenic strains. Fraction soluble in hexane showed broad spectrum of inhibition against all the studied pathogens. However, fractions soluble in ethyl acetate inhibited the growth of E. coll, MRSA, and M. luteus. In case of butanol and aqueous extracts only growth of M. luteus was inhibited. Results revealed that the flower extracts of C. procera have a potential to be used as an antibacterial agent against these pathogenic organisms

Evaluation of trihalomethanes in tap water samples of Karachi city [Pakistan]

The chlorination of water containing natural organic matter leads to the formation of disinfection by-products. Trihalomethanes [THM[s]] are the major category of disinfection by-product in chlorinated drinking water. This study aimed to investigate the presence of THM[s] in tap water samples collected from different localities of Karachi city. Liquid-liquid extraction and gas chromatography with an electron capture detector was used for the determination of THM[s]. The concentration of THM[s] in tap water samples of Karachi was found below the WHO guideline values. The mean concentration of chloroform, bromodichloromethane and dibromochloromethane were found as 30.40, 1.04 and 0.09 micro g L[-1] respectively. The relative standard deviations for these THM species were 1.15, 1.61 and 1.81 respectively. Bromoform [CHB[r3]] was not detected. On the basis of the results obtained by principal component analysis [PCA], CHCl[3] was found to be the most significant principal component. The effect of free chlorine residual and pH on the concentration of THM[s] were also assessed

Metal transfer ratio of leucocaena leucocephala: An experimental study using the soils of industrial areas of Korangi and Landhi, Karachi

The metal transfer ratio of Leucaena leucocephala in an experimental study using the soils of industrial areas was conducted. The soils were collected from Khan Towel, Tanveer Garment, One Tech Rubber and One Tech Ply Board Factories in the vicinity of Korangi and Landhi industrial areas and experimented in greenhouse under natural environmental conditions. Another soil sample was collected from a control area [Karachi University]. The plant L. leucocephala was grown in 50% above mentioned soils [respective area, including control] which mixed with 50% garden soil [one part manure + two parts fine sand in each soil type]. The level of Fe was highest in plants grown in soil of One Tech Rubber Factory [66.427 micro g-g] while, the lowest level was detected in One Tech Ply Board Factory [28.273 micro g-g]. Similarly, the level of Cu was significantly higher in plants of One Tech Rubber Factory soil [0.211 micro g-g] followed by Tanveer Garment Factory soil [0.120 micro g-g]. Significantly [p< 0.05] higher levels of Zn was found in plants of L. leucocephala grown in soil of control area [Karachi University] [0.177 micro g-g] followed by One Tech Ply Board [0.167 micro g-g] and One Tech Rubber [0.152 micro g-g] Factories. On the other hand, the level of Cr was significantly [p< 0.05] higher in One Tech Ply Board Factory [0.015 micro g-g] as compared to control [Karachi University] and other factories. The research demonstrated that the levels of different metals [Fe, Cu, Zn and Cr] were mostly higher in plants of L. leucocephala which were grown in soil of industrial areas than control. This showed that the soil of the industrial areas of Korangi and Landhi, particularly of One Tech Rubber and One Tech Ply Board Factories are contaminated by the existing pollution in the area

Impact of chemical characteristics of ground water on development of tubewell in karachi university campus

Adequate supply of potable water is essential for the smooth and trouble-free human habitation, which has almost become a paradox. During the last decade, Pakistan in general and Karachi, the biggest city of the country in particular, has experienced acute water crises due to climatic impact and rapid industrial and urban developments. Due to inadequate water supply for domestic as well as industrial purposes, the groundwater has now become a popular water source in the Karachi region. Exploration for the evaluation and assessment of groundwater in the premises of the Karachi University was carried out in view to supplement the water shortage at the campus. Four to five groundwater horizons have been identified in different types of sandstones at different depths with varying quality trends. On the basis of encouraging results of the geological and geophysical investigations, a test borehole was drilled for the actual groundwater quality and quantity assessment at one of the explored sites. Groundwater samples, collected from different horizons, have chemically been investigated to evaluate in respect of their dissolved minerals/salts, which affect the water usefulness for domestic, industrial or agricultural purposes in general, and the selection of tube well materials and its designing for a longer working life in particular