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1.
Folia Biol (Praha) ; 56(5): 195-200, 2010.
Article in English | MEDLINE | ID: mdl-21138650

ABSTRACT

Reactivation of tumour suppressor genes that have been silenced by promoter methylation is a very attractive molecular target for cancer therapy. The treatment of a squamous cervical cancer cell line, SiHa, with 20 µM curcumin and genistein resulted in demethylation of promoter of the RARß2 gene and led to the reactivation of the gene. The degree of methylation as observed by MSP decreased as the time period of treatment was increased from 72 h to 6 days. In HeLa cells (an adenocarcinoma cervical cancer cell line) there was also reversal of hypermethylation of the RARß2 gene after six days of treatment with 20 µM curcumin. However, allyl sulphide treatment (20 µM) did not cause the reversal of hypermethylation until 72 h of treatment in the SiHa cell line. This is the first report to show the reversal of hypermethylation of the RARß2 gene by genistein and curcumin in cervical cancer cell lines. Furthermore, these compounds acted as doublepronged agents as they caused apoptosis in the treated cervical cancer cell lines in addition to reversal of promoter hypermethylation.


Subject(s)
Antineoplastic Agents , Curcumin , DNA Methylation/drug effects , Genistein , Receptors, Retinoic Acid/genetics , Uterine Cervical Neoplasms/drug therapy , Uterine Cervical Neoplasms/genetics , Uterine Cervical Neoplasms/physiopathology , Allyl Compounds/pharmacology , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Biological Products/pharmacology , Cell Line, Tumor , Curcumin/pharmacology , Curcumin/therapeutic use , Female , Genistein/pharmacology , Genistein/therapeutic use , Humans , Sulfides/pharmacology
2.
Eur J Med Chem ; 45(3): 857-63, 2010 Mar.
Article in English | MEDLINE | ID: mdl-20034707

ABSTRACT

A series of 9H, 10H, 3-[N- 4 methyl -2-benzamido thiophen 3-yl carbonyl amino [2-(2'-phenyl 1'- ethylenyl)] 10-(aryl) thiazolidino [4, 5-b] 1, 5 benzodiazepine [7a-7h] were designed and synthesized to meet the structural requirements essential for anticonvulsant activity. Anticonvulsant activity was determined after intra-peritoneal administration to mice by supramaximal electroshock seizures model and Isoniazide Hydrazone induced seizures model. Motor impairement was determined using actophotometer and rotarod apparatus. Among the synthesized compounds two [JG 7a and JG 7e] compounds exhibited significant anticonvulsant activity after intra-peritoneal administration. Active compounds carry hydroxy substitutent at 2-position and methoxy at 4-position in the phenyl ring at C(5) of benzodiazepine. In present we study conclude that small polar and electron rich groups contribute significantly for anticonvulsant activity while electronegative substitutents showed lesser contribution for anticonvulsant activity.


Subject(s)
Anticonvulsants/chemical synthesis , Benzodiazepines/chemistry , Drug Design , Pharmacology , Thiazolidinediones/chemistry , Animals , Anticonvulsants/pharmacology , Dose-Response Relationship, Drug , Injections, Intraperitoneal , Locomotion/drug effects , Mice , Molecular Structure
4.
Talanta ; 80(2): 565-71, 2009 Dec 15.
Article in English | MEDLINE | ID: mdl-19836521

ABSTRACT

A novel humidity sensor made up of nano-crystalline zinc oxide (ZnO) film, coated onto the U-shaped typical glass substrate as a wave guide, conjugated with an optical fiber and He-Ne un-polarized laser source. The nano-crystalline zinc oxide (ZnO) was synthesized using single molecular precursor method. The resulting material was characterized with Fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD), thermogravimetric-differential thermal analysis (TG-DTA) and scanning electron microscopy (SEM). In the thin film, ZnO particles exhibited the wurtzite phase structure with the particle size in a diameter range of 70-80 nm. The humidity sensing characteristic has been estimated by measuring the optical permeability (OP) as a function of percentage relative humidity (%RH) in the ranging from 5 to 90 inside a closed chamber. The OP decreases linearly with increase in %RH with a respond time of about 30 and recovery time of 35s. The sensor exhibits the sensitivity of 0.45 in the %RH range 5-50 and 0.30 from 50 to 90.


Subject(s)
Environmental Monitoring/methods , Humidity , Nanostructures/chemistry , Optical Fibers , Zinc Oxide/chemistry , Crystallization , Environmental Monitoring/instrumentation , Microscopy, Electron, Scanning , Nanostructures/ultrastructure , Nanotechnology/instrumentation , Nanotechnology/methods , Particle Size , Reproducibility of Results , Spectroscopy, Fourier Transform Infrared
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