Showing papers by "Central Drug Research Institute published in 1983"
TL;DR: It is reported here that CML erythrocyte spectrin becomes abnormal due to cross-linking of its two subunits via disulphide bonds, and it is shown that this cytoskeletal defect in the ERYthrocytes is associated with loss of transmembrane phospholipid asymmetry.
Abstract: Chronic myeloid leukaemia (CML) is a clonal neoplasm that arises in a stem cell common to granulocytes and erythrocytes. Several abnormalities have been identified in the plasma membranes of granulocytes of CML patients, but to our knowledge no studies have been done on CML erythrocytes. We report here that CML erythrocyte spectrin becomes abnormal due to cross-linking of its two subunits via disulphide bonds. In addition, we show that this cytoskeletal defect in the erythrocytes is associated with loss of transmembrane phospholipid asymmetry. These observations, apart from demonstrating membrane abnormalities in CML erythrocytes, also provide strong support for the view that the asymmetric organization of phospholipids in the red cell membrane is maintained mainly by interactions between spectrin and aminophospholipids.
61 citations
TL;DR: An investigation of Dodonaea viscosa afforded a new flavonoid having an isoprenoid side chain along with the seven known flavonoids: 5-hydroxy-3,6,
56 citations
TL;DR: In this article, the assignment of the 13C NMR shift values of the dihydrobenzofuranoid lignans cedrusin and dihydronhydrodiconiferyl alcohol, their respective 4-O-β-D-glucosides and their acetates have been made.
Abstract: The assignments of the 13C NMR shift values of the dihydrobenzofuranoid lignans cedrusin and dihydrodehydrodiconiferyl alcohol, their respective 4-O-β-D-glucosides and their acetates have been made. The furanoid stereochemistry in 8,3′-lignans could be deduced from comparative 13C NMR data.
53 citations
TL;DR: A system of chromosome classification and nomenclature based on arm ratios and centromeric indices from both the long and short arms is proposed to enable one to determine the correct position of centromere to name the chromosomes according to the known Centromere locations.
Abstract: A system of chromosome classification and nomenclature based on arm ratios and centromeric indices from both the long and short arms is proposed. This will enable one to determine the correct position of centromere to name the chromosomes according to the known centromere locations. A table embodying nomenclature, notation, the arm ratio values and the values of centromeric indices is presented to serve as a key for chromosome classification. The advantage of the present system over the other systems is discussed with the help of a few examples.
46 citations
TL;DR: Two cases of mycotic keratitis caused by the Colletotrichum state of Glomerella cingulata and Acrophialophora fusispora are reported for the first time and amphotericin B showed better results than tolciclate and miconazole.
Abstract: Two cases of mycotic keratitis caused by the Colletotrichum state of Glomerella cingulata and Acrophialophora fusispora are reported for the first time. Both the isolates produced experimental corneal lesions in rabbit eyes but A. fusispora was more pathogenic. The experimental infection was more severe, with both the fungi, in rabbits pretreated with cortisone as compared with untreated animals.In vitro A. fusispora was most sensitive to miconazole and tolciclate followed by clotrimazole, amphotericin B and lactones while clotrimazole exerted maximum inhibitory effect on Colletotrichum followed by miconazole, lactones, amphotericin B and arnebins. Arnebins and tolciclate were inactive respectively against A. fusispora and Colletotrichum. Of the 3 drugs tested in vivo, against A. fusispora keratitis in rabbit, amphotericin B showed better results than tolciclate and miconazole.
37 citations
TL;DR: In this paper, a new furanoeremophilane characterized as 3-formyl-4,5-dimethyl-8-oxo-5 H -6,7-dihydronaphtho(2,3- b )furan has been isolated from the roots of Vitex negundo.
28 citations
TL;DR: It appears that the fall in zinc content of spermatozoa during their transport in the epididymis is related to sperm maturation and that oestrogen treatment interferes with this reduction in sperm zinc content.
Abstract: Zinc content of spermatozoa collected from the caput and cauda portions of the rat epididymis was determined by atomic absorption spectroscopy. The results showed about 60% reduction in the spermatozoal zinc content by the time they reach the cauda epididymis. This reduction was inhibited in rats receiving micro dose oestrogen which incuced ‘functional’ sterility. It appears that the fall in zinc content of spermatozoa during their transport in the epididymis is related to sperm maturation and that oestrogen treatment interferes with this reduction in sperm zinc content.
23 citations
TL;DR: A newer dimension has been given to the chemotherapy of helminthiasis where modern drug design is chiefly directed towards searching potent veterinary and human anthelmintics derived from benzimidazoles.
Abstract: Although benzimidazole is one of the oldest and chemically well-studied nitrogen heterocyclics, it has been quite lately recognized as the versatile nucleus for building molecules possessing broad spectrum of biological activity. The polyfunctionality associated with benzimidazole nucleus, the ease to carry out various organic reactions and its association with bio-molecules stimulated several laboratories of the world to explore its synthetic and biological avenues. This, not only, disclosed various fascinating aspects of benzimidazole chemistry but also led to the synthesis of a large variety of benzimidazole derivatives of which many have been demonstrated to exhibit powerful anthelmintic, antimicrobial, pesticidal, anticancer and pharmcological activities. Among the above areas of drug research, a newer dimension has been given to the chemotherapy of helminthiasis where modern drug design is chiefly directed towards searching potent veterinary and human anthelmintics derived from benzimidazoles.
23 citations
TL;DR: Six aporphine alkaloids glaucine, boldine, norboldine, isoboldine, Norcorydine and laurotetanine have been isolated from the ethanolic extract of the stems of LITSEA WIGHTIANA in which spasmolytic, hypothermic and blood pressure lowering activities have been confirmed.
Abstract: Six aporphine alkaloids glaucine, boldine, norboldine, isoboldine, norcorydine and laurotetanine have been isolated from the ethanolic extract of the stems of LITSEA WIGHTIANA in which spasmolytic, hypothermic and blood pressure lowering activities have been confirmed.
22 citations
01 Jan 1983
TL;DR: Ethanolic extract of the aerial part of Rubus ellipticus elicited 100% activity even at a considerably lower dose of 50 mg/kg body weight during days 1-3 of pregnancy, while the rest of the plants were found ineffective.
Abstract: Ten indigenous plants viz., Apium graveolens L., Costus speciosus Sm., Crateva nurvala Buch.-Ham., Glycyrrhiza glabra L., Hedychium spicatum Ham., Nerium indicum Mill., Rubia cordifolia L., Rubus ellipticus Sm., Terminalia bellirica Gaertn. and Urtica dioica L., have been screened for antifertility activity in albino rats. 90% ethanolic extract of 3 plants viz., Crateva nurvala (bark), Rubus ellipticus (root) and Terminalia bellirica (bark) showed 60-66% antifertility activity when administered orally at 250 mg/kg dose, in days 1-7 of pregnancy. Ethanolic extract of the aerial part of Rubus ellipticus (whole plant without root) elicited 100% activity even at a considerably lower dose of 50 mg/kg body weight during days 1-3 of pregnancy. The rest of the plants were found ineffective.
20 citations
TL;DR: Replacement of the C‐2 ester group in phosphatidylcholine by the carbamyloxy function rendered its liposomes completely stable and longer living in the circulation of rats.
TL;DR: MAO was present in mitochondria and deaminated noradrenaline at the maximal rate, although serotonin, adrenaline, tyramine and dopamine were also degraded but more slowly, while of the organs studied, the body wall, female reproductive organ and intestine showed highest MAO activity.
Abstract: Monoamine oxidase (MAO), catalysing oxidative deamination of biogenic monoamines, has been detected in adult Ascaridia galli. MAO was present in mitochondria and deaminated noradrenaline at the maximal rate, although serotonin, adrenaline, tyramine and dopamine were also degraded but more slowly. Of the organs studied, the body wall, female reproductive organ and intestine, the body wall (containing neuronal structures) showed highest MAO activity. Km value for chick ascarid mitochondrial MAO using tyramine as substrate was 1.66 X 10(-3) M and it was most active at 2.5 mM tyramine concentration, pH 7.5 and 40 degrees C. MAO of A. galli appeared to be thermolabile as nearly 80% of its activity was lost when the incubation temperature was increased 5 degrees above optimum.
TL;DR: The transbilayer aminophospholipid distributions in small unilamellar vesicles comprising of phosphatidylethanolamine or its analogs (bearing modifications in the polar headgroup) were ascertained using trinitrobenzenesulfonic acid as external membrane probe.
TL;DR: In this paper, the NMR spectra of indan derivatives bearing substituents in the 1, 2, 5 and 6 positions were reported and assigned by LIS measurements and other techniques.
Abstract: 13C NMR spectra of indan derivatives bearing substituents in the 1, 2, 5 and 6 positions are reported and assigned by LIS measurements and other techniques. Epimeric indanes bearing vicinal oxygen and phenyl or benzyl substituents show ring carbon shielding in the cis relative to the trans isomers, which is compared with corresponding cyclopentane shifts, and indicates the predominance of envelope conformations with pseudoaxial oxygen substituents for the cis isomers. Acetylation shifts show consistently larger shielding at C-β for the trans compounds. Introduction of oxygen at C-5 leads to asymmetric shielding effects at the ortho carbon atoms as soon as there is a substituent in the para position which can participate in mesomeric forms.
TL;DR: Finding would substantiate the proposition that the geminal diaryl residue and not the 1,2-diarylethylene moiety is mainly responsible for the receptor binding and activity profile characteristic of triarylethylenes and form a basis for the rationalization of the structure-activity-relationship of estrogens at the molecular level.
TL;DR: In addition to sitosterol glucoside and gallic acid, two new flavone glycosides have been isolated from Eugenia kurzii (aerial parts) and characterized as 3-C -methylapigenin 5- O -rhamnoside and 3- C -methylluteolin 5-O -RHAMnoside by spectral analysis and chemical conversion as discussed by the authors.
TL;DR: Production of 14 CO 2 from 12 carbon-labelled amino acids by Ascaridia galli was studied and the decarboxylations of alanine, aspartate and glutamate were found to be associated with the mitochondrial fraction.
TL;DR: Results suggests that reduction in brain catecholamine levels and dopamine Β-hydroxylase activity may be one of the possible ways through which the drug manifests its clinical effects.
Abstract: The effect of propranolol on the levels of catecholamine in different parts of rat brain has been studied. The catecholamine contents of different regions were lowered by the drug. Dopamine Β-hydroxylase activity was also reduced, bothin vivo andin vitro. Propranolol is taken up by the brain tissue and the uptake is time-dependent. These results suggests that reduction in brain catecholamine levels and dopamine Β-hydroxylase activity may be one of the possible ways through which the drug manifests its clinical effects.
TL;DR: Tracer experiments show that the tetrahydroprotoberberines stepholidine, corydalmine, capaurine and corynoxidine are stereospecifically biosynthesized from (S)-reticuline whereas the bisbenzylisoquinoline alkaloids cycleanine, N-desmethylcycleanine and the proaporphine alkaloid are derived from (R)-N-methylcoclaurine.
TL;DR: It is concluded that feto‐neonatal rat brain contains AFP similar to that present in fetal serum and that it may arise in brain as a result of its in situ synthesis.
Abstract: Monospecific anti-rat serum alpha-fetoprotein (AFP) IgG was coupled to cyanogen bromide-activated Sepharose-4B (4.5 mg/ml packed volume of gel) to yield an immunoaffinity matrix. The immunoaffinity column was used to isolate AFP from feto-neonatal rat brain. The purified AFP was immunologically and electrophoretically similar to serum AFP. It yielded a single band with a molecular weight of 70,000 on sodium dodecyl sulphate polyacrylamide gel electrophoresis. Polyacrylamide gel electrophoresis of the protein under nondenaturing conditions yielded two charge variants of AFP, reminiscent of AFP from feto-neonatal rat serum. The AFP was observed to bind estradiol with Ka = 5.8 X 10(8) M -1 and 1.3 X 10(8) M -1 by dextran-coated charcoal adsorption and Sephadex gel filtration techniques, respectively. Newborn rat brain cells linearly incorporated [14C]leucine into immunoprecipitable AFP during 6 h in culture. It is, therefore, concluded that feto-neonatal rat brain contains AFP similar to that present in fetal serum and that it may arise in brain as a result of its in situ synthesis.
TL;DR: A study of their antiimplantation activities (AI) and receptor binding affinities (RBA) show that trans-anti-trans compounds are biologically most potent, followed by the corresponding cis- anti-trans and cis-syn- trans compounds.
TL;DR: The 2‐substituted thiobenzimidazoles 7–19 have been synthesized and tested for their anthelminthic activity against Ancylostoma ceylanium and Hymenolepsis nana in hamsters and rats, respectively.
Abstract: The 2-substituted thiobenzimidazoles 7–19 have been synthesized and tested for their anthelminthic activity against Ancylostoma ceylanium and Hymenolepsis nana in hamsters and rats, respectively.
Synthese 2-substituierter Thiobenzimidazole als potentielle Anthelminthica
Die 2-substituierten Thiobenzimidazole 7–19 wurden synthetisiert und auf ihre anthelminthische Aktivitat gegen Ancylostoma ceylanium und Hymenolepsis nana an Hamster und Ratte getestet.
TL;DR: Levels ofAFP and albumin in brain correlated well with rates of their synthesis by brain cells in vitro at any specific stage of brain maturation implying that levels of AFP and albumIn in brain are regulated by controlling rates ofTheir synthesis in the maturing brain cells.
TL;DR: The results of the present study suggest that levonorgestrel appears to be a better ligand than dihydrotestosterone for measuring SHBG.
TL;DR: Feeding with N-[14CH3]reticuline showed that the C atom 8 in sinactine is derived from N-Me group of reticulines, and suggested that the methylenedioxy group formation probably precedes O-methylation in the bioconversion of scoulerine into sinactines.
TL;DR: The structure-activity relationship amongst the substituted diphenyl ketones indicated considerable sensitivity towards minor structural modifications and offer a tool to investigate nonsteroidal compounds in relation to progesterone related functions of uteroglobin in pregnancy.
TL;DR: It is concluded that both H1- and H2-histamine receptors are present in the brain of pigeon and are responsible for H-induced hypothermia.
Abstract: The effect of intracerebroventricular (i.c.v.) administration of histamine (H), H1- and H2-receptor agonists and their antagonists, on the cloacal temperature of pigeon has been investigated. Histamine produced a dose-dependent hypothermia at an ambient temperature of 24 degrees C which was significantly blocked by a combination of mepyramine and cimetidine but was only partially antagonized by either of them alone. H1-receptor as well as H2-receptor agonists also produced hypothermic response with a time-course similar to that of H. Their effects were also significantly antagonized by mepyramine and cimetidine respectively. The histamine response was not modified by pretreatment with alpha- or beta-adrenoceptor antagonists. Histamine produced an insignificant hyperthermia at 10 degrees C but the hypothermic effect increased as the ambient temperature was raised up to 40 degrees C. It is concluded that both H1- and H2-histamine receptors are present in the brain of pigeon and are responsible for H-induced hypothermia.
TL;DR: An ELISA was developed using cross-reacting antigens of Litomosoides carinii and Setaria cervi to detect antibodies in filarial patients but only four of 40 asymptomatic carriers and one of 50 normal subjects gave a positive ELISA response.
Abstract: An ELISA was developed using cross-reacting antigens of Litomosoides carinii and Setaria cervi to detect antibodies in filarial patients. The diagnostic potential of the test was investigated in 80 symptomatic cases of filariasis, 40 asymptomatic carriers and 50 normal subjects of an area around Lucknow endemic for Bancroftian filariasis. By the criteria laid down for ELISA positivity for filariasis, 86·2% of the symptomatic cases could be detected by this test. Only four of 40 asymptomatic carriers and one of 50 normal subjects gave a positive ELISA response. Purified antigenic fractions of S. cervi are also promising for detecting asymptomatic carriers.