Showing papers by "Central Drug Research Institute published in 1987"
TL;DR: Three new substituted bibenzyls (1,2-diarylethanes) aloifol I and aloIFol II and a new substituted 9,10-dihydrophenanthrene, 6-O-methylcoelonin in addition to batatasin III, coel onin and gigantol have been isolated and characterized.
70 citations
TL;DR: It is demonstrated that Ca2+ loading in human erythrocytes leads to loss of the transbilayer phospholipid asymmetry, and it is suggested that, together with spectrin, polypeptides 2.1 and 4.1 may also play an important role in maintaining the asymmetric distribution of variousospholipids across the ERYthrocyte membrane bilayer.
59 citations
TL;DR: These antibody bearing liposomes have now been found quite effective as vehicles for delivering the antimalarial drug, chloroquine, to erythrocytes in Plasmodium berghei-infected mice, demonstrating the usefulness of antibody targeted liposome as carriers for site-specific drug delivery.
51 citations
TL;DR: Identification and characterization of antigenic proteins of Setaria cervi adults and microfilariae was done by immunoblotting technique using hyperimmune rabbit sera against S. cervi and Brugia malayi showing the existence of common antigenic determinants between the bovine and human filarial parasites.
Abstract: Identification and characterization of antigenic proteins of Setaria cervi (bovine filarial parasite) adults and microfilariae was done by immunoblotting technique using hyperimmune rabbit sera against S. cervi and Brugia malayi. The antigens recognized by these sera were detected by using 125I protein-A followed by autoradiography. Fifteen different antigens were observed to be common between adult and microfilarial stages of the parasite. Some stage specific antigens were also identified. Many antigens of S. cervi adults and microfilariae were also recognized by rabbit anti-B.malayi serum showing the existence of common antigenic determinants between the bovine and human filarial parasites.
47 citations
TL;DR: The optimum dose produced significant lowering of blood sugar in fed, glucose-loaded and tolbutamide-pretreated animal models, but not in fasted rats.
42 citations
TL;DR: It is demonstrated that the intracellular malarial parasite produces stage-dependent alterations in the membrane phospholipid organization of its host erythrocyte.
Abstract: The membrane phospholipid organization in monkey erythrocytes harbouring different developmental stages of the simian malarial parasite Plasmodium knowlesi was studied using phospholipase A2 from two different sources and Merocyanine 540 as the external-membrane probes. Experiments were done to confirm that the phospholipases did not penetrate into the infected cells or hydrolyse phospholipids during membrane isolation. The parasite-free erythrocyte membrane was isolated by differential centrifugation or by using the cationic beads Affi-Gel 731. The purity of the membranes was established by optical and electron microscopy, and by assaying the parasite-specific enzyme glutamate dehydrogenase. About 10% of the phosphatidylethanolamine and none of phosphatidylserine were hydrolysed by the phospholipases in intact normal monkey erythrocytes. However, accessibility of these aminophospholipids to the enzymes was significantly enhanced in the infected cells under identical conditions. The degree of this enhancement depended on the developmental stage of the intracellular parasite, but not on the parasitaemia levels in the infected monkeys, and increased with the parasite growth inside the cells. Analogously, Merocyanine 540 was found to label the trophozoite- or schizont-infected erythrocytes, but not the ring-infected or normal cells. These results demonstrate that the intracellular malarial parasite produces stage-dependent alterations in the membrane phospholipid organization of its host erythrocyte.
41 citations
35 citations
TL;DR: Plasmodium yoelii nigeriensis infection in albino mice significantly altered the hepatic microsomal mixed function oxidase system and Cytochrome P-450 and other monooxygenases, viz. aniline hydroxylase, aminopyrine-N-demethylase and benzo(a)pyrene hydroxyase were significantly lowered while microsome heme showed 4-fold increase at 80% parasitaemia.
26 citations
TL;DR: The aerial parts of Anaphalis araneosa afforded, in addition to known compounds, three new prenylated phthalides as mentioned in this paper, which were elucidated by high-field 1 H NMR and 13 C NMR spectroscopy.
22 citations
TL;DR: A phytochemical investigation of AGLAIA ROXBURGHIANA var.
Abstract: A phytochemical investigation of AGLAIA ROXBURGHIANA var. Beddomei (Meliaceae) resulted in the isolation of the active principle and its characterisation as (+)-odorinol exhibiting strong antiviral activity against Ranikhet disease virus (RVD) in chick embryo.
22 citations
01 Jan 1987
TL;DR: In this paper, an ethanol extract of Swertia chirata (Buch-Ham) was fed to healthy albino rats consisting of fed, fasted and glucose loaded models.
Abstract: Ninety five percent ethanol extract of Swertia chirata (Buch-Ham) was fed to healthy albino rats consisting of fed, fasted and glucose loaded models. Significant blood sugar lowering effect was observed in these models. Swertia chirata fed orally caused enhancement of the blood sugar lowering effect of tolbutamide in healthy albino rats.
TL;DR: It has been found that the introduction of the novel 3-n-butylamino-2-hydroxypropyloxy moiety in place of the classical tert-beta-aminoethoxy group leads to enhancement of antifertility activity.
TL;DR: Acanthamoeba culbertsoni contains an S-adenosylmethionine decarboxylase which is strongly activated by putrescine and to a lesser extent by cadaverine; spermidine, spermine, diaminopropane and 1,6-diaminohexane are inactive.
TL;DR: The efficacy of a substituted methyl benzimidazole carbamate, methyl 5(6)-[4-N-(2-pyridyl)] piperazino carbamoyl benzimodazole-2-carbamate, was assessed against larval and adult forms of Ancylostoma ceylanicum, Nippostrongylus brasiliensis, Hymenolepis nana and Brugia malayi in experimentally-infected animals
TL;DR: In this article, the mechanism of double bond reduction occurring in certain conjugated ketones, nitriles, acids and esters under chemical ionization conditions has been studied.
Abstract: The mechanism of double bond reduction occurring in certain conjugated ketones, nitriles, acids and esters under chemical ionization conditions has been studied. The results indicate that the hydrogen radicals present in the chemically ionized plasma are responsible for the reduction of the double bond. This is further supported by experiments with radical traps.
TL;DR: New examples of synthetic applications of 2-chloro-3-formylquinoline, as evident from the novel and facile syntheses of 3-aminoisooxazolo[5,4-b]quinoline (4), 3-hydroxyfuro[2,3-d]theino[2.3]-quinoline-2-carboxamide (7), and 3hydroxymethyl-2-(3 -formyl)phenyl-quinoline(13), have been furnished as discussed by the authors.
Journal Article•
TL;DR: Effect of temperature on the sporogonic cycle of Plasmodium berghei (NK 65) has been studied in vector Anopheles stephensi and it delayed the development of sporozoites in the oocysts by 5 days as compared to control group.
Abstract: Effect of temperature on the sporogonic cycle of Plasmodium berghei (NK 65) has been studied in vector Anopheles stephensi. To determine the optimum temperature for development of parasite, fed mosquitoes were kept at 16 +/- 1 degree C, 19 +/- 1 degree C and 26 +/- 1 degree C temperature. The temperature 19 +/- 1 degree C was found to be optimum for normal development of parasite within the vector. Sporulated oocysts were observed on the 10th day post feed and salivary glands were loaded with thousands of sporozoites on day 14. Temperature 16 +/- 1 degree C, though did not exert any deleterious effect on the morphology of parasites it delayed the development of sporozoites in the oocysts by 5 days as compared to control group. In the case of long exposure to this temperature, the sporozoites obtained from salivary glands became non-infective. Temperature 26 +/- 1 degree C was responsible for deterioration of all the stages of sporogonic cycle and it also checked the formation of sporozoites in the oocysts.
TL;DR: Tracer experiments showed that the bisbenzylisoquinoline alkaloid, (S, R)-hayatidin (10) is stereospecifically biosynthesized in young Cissampelos pareira Linn plants by intermolecular oxidative coupling of (S)-(5)-and (R)-(3), N-methylcoclaurines whereas (R,R)-isochondrodendrine (14) and (R-bebeerine (12) are formed in the plants by oxidative dimerization of
TL;DR: The 13 C chemical shifts in the spectra of friedelan-7-one (1), methyl 3-oxofriedelan 25-oate (2), methyl friedelane-25-Oate (3), 7-ox-of-riedelans-3-α-yl acetate (4), friedelanolone-3one (5), 2-hydroxy-3, 4-seco-friedelan -3-oic acid (6), methyl 2-oxo-3 4-SECO-friedelin-an
Abstract: The 13 C chemical shifts in the spectra of friedelan-7-one (1), methyl 3-oxofriedelan-25-oate (2), methyl friedelan-25-oate (3), 7-oxofriedelan-3-α-yl acetate (4), friedelan-3-one (5), 2-hydroxy-3, 4-seco-friedelan-3-oic acid (6), methyl 2-oxo-3,4-seco-friedelan-3-oate (7), methyl 2-hydroxy-3,4-seco-friedelan-3-oate (8) and 3,4-seco-friedelan-2,3-diol (9) have been fully assigned using two-dimensional heteronuclear correlation NMR spectroscopy, BB proton decoupled, DEPT and selective heteronuclear spin decoupling methods. These assignments and the observation of substantial NOEs between 26-methyl and 28-methyl and between 28-methyl and 30-methyl support the boat to boat conformations for the D and E rings in 1. Corrections and correlations are made of some earlier literature assignments of friedelanones.
TL;DR: Alteration in the blood-brain barrier (BBB) by electroconvulsive shock leading to increased accumulation of dopamine in the corpus striatum may be responsible for the potentiation of stereotypy.
TL;DR: The contents of total lipids, total sterols, total and individual phospholipids were significantly lower in mature cysts of Acanthamoeba culbertsoni strain A-1 than in trophozoites while the radioactivity increased in the akali-insoluble fraction (cellulose).
Abstract: The contents of total lipids, total sterols, total and individual phospholipids: lysophosphatidyl choline, lysophosphatidyl ethanolamine, phosphatidyl choline, phosphatidyl ethanolamine and alkali-stable phospholipids I and II, were significantly lower in mature cysts of Acanthamoeba culbertsoni strain A-1 than in trophozoites. The major constituent sterols of trophozoites, viz. ergosterol, 7-dehydrostigmasterol and 7,22,25-tridehydrostigmasterol which resolved as a single spot on thin-layer chromatography, disappeared in the cysts. When trophozoites grown in the presence of [14C]acetate were transferred to encystation medium, there was a steady decrease in the radioactivity in the lipids and acid-soluble fraction (glycogen) of the encysting cells while the radioactivity increased in the akali-insoluble fraction (cellulose). The activity of isocitrate lyase in the encysting cells steadily increased up to 24 h of encystation, followed by a slight decrease during 24–32 h, but the activity of isocitrate dehydrogenase steadily decreased up to 32 h of encystation, beyond which time no enzyme activity was detected. Inhibitors of isocitrate lyase, glycolate and maleate at 8.5 to 34 mM concentration inhibited encystation by 18–67%.
TL;DR: In this article, the Nef reaction in the presence of primary, secondary and tertiary amines has been described and a convenient synthesis of N-substituted pyrroles and 3,6-dimethyl-4-hydrazinocarbonyl-5-(4-amino-3-nitrophenyl)-pyridazine 16 has been developed.
TL;DR: The infectivity and migratory pattern of Ancylostoma ceylanicum infective larvae (L3) were investigated in hamsters infected by various routes and those transmitted orally to naive hamsters developed in the normal way.
Abstract: The infectivity and migratory pattern of Ancylostoma ceylanicum infective larvae (L3) were investigated in hamsters infected by various routes. Following oral administration 40-70% of L3 attained maturity and there was no tissue migration. Following subcutaneous inoculation a small number (1-1.2%) of L3 attained maturity in the intestine after completing the broncho-oesophageal journey. Larvae which penetrated the skin also became adult in the intestine. Most of the larvae entering parenterally remained at the site of infection and in the tracheal region for more than 100 days without undergoing any development, other than desheathment. Those transmitted orally to naive hamsters developed in the normal way. Larvae inoculated parenterally into female hamsters were able to infect offspring in milk, but could not cross the placental barrier.
TL;DR: Auricularic acid, a spasmolytic diterpene, isolated from Pogostemon auricularis has been characterized as cleistanth-13,15,dien-18-oic acid ( 1 ) with the help of high resolution 2D 1H1H (COSY, NOESY) n.m.
TL;DR: In rhesus monkeys, treatment with the compound at 5 and 10 mg/kg doses on days 16-21 of the menstrual cycle induced frank vaginal bleeding between days 21 and 24, and treatment on days 21-30 or after confirmation of pregnancy on days 32-36 was ineffective.
TL;DR: The high worm burden on the population is not only responsible for several grave clinical complications but also greatly hampers the socioeconomic growth of the tropics by causing malnutrition and physical disability which finally leads to decreased working capacity in the people carrying helminth parasites.
Abstract: Among a large variety of parasitic diseases caused by the invasion of the human body by a number of bacteria, fungi, viruses, protozoa and helminths, the helminth infections undoubtedly constitute a major medical and public health problem all over the tropical and subtropical regions of the world. Despite significant advances made in the treatment of helminth diseases, the rate of incidence of these infestations has not satisfactorily declined. This is primarily because these are basically the diseases of poor masses where inappropriate sanitation, low living standards, and lack of health education along with ideal environmental conditions for the survival and replication of the parasites facilitate the dissemination of infections. Another major reason for the wide spread of helminthiasis is that, earlier, it was not considered to be involved with higher risks of morbidity and mortality, and hence, was unable to draw the attention of medicinal chemists, parasitologists and medical and health personnel. However it was soon realized that the high worm burden on the population is not only responsible for several grave clinical complications but also greatly hampers the socioeconomic growth of the tropics by causing malnutrition and physical disability which finally leads to decreased working capacity in the people carrying helminth parasites. Furthermore, the presence of helminths in domestic animals induces less production of milk, fat, meat and wool, and thus, influences the economy of agricultural and dairy countries of the world
TL;DR: Results demonstrate that loss of the transmembrane phospholipid asymmetry in chronic myeloid leukaemia erythrocytes is accompanied by an enhancement in the outer surface fluidity and suggest that the red cells membrane phase-state asymmetry originates probably from the asymmetric arrangements of phospholips across the membrane bilayer.
Abstract: The membrane phospholipid organisation in the red cells of humans suffering from chronic myeloid leukaemia has been analysed using the amino-group labelling reagent trinitrobenzenesulphonic acid and the fluid-sensing fluorophore, Merocyanine 540. Unlike the normal human erythrocytes, trinitrobenzenesulphonic acid in intact chronic myeloid leukaemia erythrocytes modified about 30% phosphatidylserine, under controlled conditions. Also, the chronic myeloid laukaemia red cells, but not the normal cells, were found to bind the fluorescent dye Merocyanine 540. These results demonstrate that loss of the transmembrane phospholipid asymmetry in chronic myeloid leukaemia erythrocytes is accompanied by an enhancement in the outer surface fluidity and, therefore, suggest that the red cells membrane phase-state asymmetry originates probably from the asymmetric arrangements of phospholipids across the membrane bilayer.