Showing papers by "Central Drug Research Institute published in 1986"
TL;DR: It is contention that the antianxiety effect of cannabis is mediated through central benzodiazepine receptors, as acute cannabis treatment has no significant effect, whereas chronic cannabis treatment significantly increased 3H-diazepam binding as compared with controls.
46 citations
TL;DR: The structure of 3′- O -methylbatatasin III, a new bibenzyl of the East Himalayan orchid, Coelogyne ovalis, has been established on the basis of spectral and chemical data.
43 citations
TL;DR: A drug targeting Liposome Cell‐specific antibody F(ab')2 fragment (Erythrocyte) and its role in cell reprograming and wound healing is under investigation.
42 citations
TL;DR: The structure of viscosol, a new prenylated flavonoid isolated from the aerial parts of Dodonaea viscosa, was established on the basis of spectral studies as well as by the conversion of the flavonol penduletin into permethyl visco-sol as discussed by the authors.
35 citations
TL;DR: Results indicate that tuftsin and its derivatives may prove useful in enhancing nonspecific host resistance against protozoan infections.
29 citations
TL;DR: The results strongly suggest that lysis of liposomes in serum can be prevented by structurally modifying the ester bond(s) in the phospholipid component ofliposomes.
28 citations
01 Jan 1986
TL;DR: This chapter focuses on protoberberine alkaloids and C-NMR spectroscopy coupled with circular dichroism techniques (CD) that have been frequently employed for determination of conformation and absolute configuration.
Abstract: Publisher Summary This chapter focuses on protoberberine alkaloids and C-NMR spectroscopy coupled with circular dichroism techniques (CD) that have been frequently employed for determination of conformation and absolute configuration. The biosynthesis of several protoberberine alkaloids are investigated thoroughly, and biosynthetic pathways are traced, including aberrant biosynthetic pathway. Protoberberine alkaloids exhibit a variety of biological and pharmacological effects. Protoberberine alkaloids have been isolated from callus cultures of some plants, and orientalidine has been obtained from a cell culture of Papaver bracteatum. The occurrence of some berbines in racemic, and (+) and (−) forms in plants and their co-occurrence with their corresponding dehydro bases are of biogenetic interest.
27 citations
TL;DR: Chronic ethanol consumption by pregnant rats during early gestation also resulted in several anatomical abnormalities of prenatal growth retardation, resorption and still births, cleft palate, hydrocephaly and hydronephrosis.
24 citations
TL;DR: Observations indicate that liposomes coupled to cell-specific antibodies may serve as highly useful carriers for homing of drugs/enzymes to specific cells in biophase.
20 citations
TL;DR: It is demonstrated that both stability in blood and the clearance rate from circulation can be modulated by structurally modifying the ester linkages in the phospholipid component of liposomes.
20 citations
TL;DR: It is suggested that strong binding of tuftsin to albumin in blood may enhance its macrophage‐stimulating activity in vivo.
TL;DR: The results of this behavioral and biochemical study indicate the involvement of a cholinergic (muscarinic) transmitter system in endosulfan-induced neurotoxicity.
TL;DR: It is suggested that spleen plays an important role in maintaining the exclusive inner distribution of PS in the normal erythrocyte membrane, and that partial migration of this lipid to the outer monolayer in nonparasitized ERYthrocytes could be attributed to an abnormal physiology of this organ in malarial infection.
TL;DR: A pathway for INA degradation involving oxygenative cleavage of a partially reduced pyridine ring is proposed and is proposed as Bacillus brevis.
TL;DR: In this paper, a postcoital antifertility agent under clinical development was extensively metabolized by rat liver homogenate in vitro Employing field desorption mass spectrometry, high performance liquid chromatography, comparison with authentic samples, and studies with 2- 14 C-Centchroman, seven metabolites have so far been characterised, which include trans-3-phenyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chroman (II, 375%), trans-2,2-dimethyl
Abstract: Centchroman (trans-2,2-dimethyl-3-phenyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chroman) (I), a postcoital antifertility agent under clinical development was extensively metabolized by rat liver homogenate in vitro Employing field desorption mass spectrometry, high performance liquid chromatography, comparison with authentic samples, and studies with 2- 14 C-Centchroman, seven metabolites have so far been characterised, which include trans-3-phenyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chroman (II, 375%), trans-2,2-dimethyl-3-phenyl-4-(p-(β pyrrolidinoethoxy) phenyl)-7-hydroxy chroman (III, 25%), β pyrrolidino-ethoxy benzene (IV), 2,2-dimethyl-4-(p-(hydroxy) phenyl)-7-methoxy chromene (V, 394%), trans-2,2-dimethyl-3-phenyl-4-(p-(hydroxy) phenyl)-7-methoxy chroman (VI, 58%), 2,3-trans-3,4-trans-2-methyl-3-phenyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chorman (VII, 29%), and 2,2-dimethyl-4-(p-(β-pyrrolidinoethoxy) phenyl)-7-methoxy chroman (VIII, 88%) Formation of metabolites V and VIII are unusual cases of dephenylation during metabolism
TL;DR: This survey highlights the therapeutic potential of DEC against filariasis and trends in the design of better filaricidic drugs with DEC as a prototype molecule.
Abstract: Structural modifications of diethylcarbamazine (DEC), a drug of choice for treating different forms of human filariasis, are analyzed in order to delineate structure–activity relationships among various piperazine and nonpiperazine DEC analogues. The acyclic congeners of DEC do not possess any activity, probably because of their ability to exist in many conformations. On the other hand, many substituted piperazines display microfilaricidal activity, although they are less potent than DEC. A few rigid analogues of DEC have been found to possess promising antifilarial activity. This survey highlights the therapeutic potential of DEC against filariasis and trends in the design of better filaricidic drugs with DEC as a prototype molecule.
TL;DR: Alterations in biogenic amines and dopamineβ-hydroxylase activity may be one of the possible mechanisms for the antilipaemic effect of the compound.
Abstract: The effect of lipid lowering agent, guggulsterone, the purified fraction of guggulipid, on biogenic monoamine levels and dopamineβ-hydroxylase activity of rat brain and heart has been studied. Administration of guggulsterone caused inhibition of brain dopamineβ-hydroxylase activity with marked stimulation in heart bothin vivo andin vitro. The levels of catecholamines were similarily affected. The contents of serotonin and histamine were found to be enhanced in brain and decreased in heart. Alterations in biogenic amines and dopamineβ-hydroxylase activity may be one of the possible mechanisms for the antilipaemic effect of the compound
TL;DR: Locomotor activity and footshock-induced aggressive behaviour in rat was decreased in a dose-dependent manner by diazepam and specific 3H-diazepam binding showed an upregulation of benzodiazepine receptors in the rat frontal cortex by ECS.
TL;DR: Purified lactate dehydrogenase was inhibited almost completely when incubated with 100 microM p-chloromercuribenzoate, Ag+ or Hg+ and such inhibition could be reversed by the addition of beta-mercaptoethanol or L-cysteine and metal chelators did not show any remarkable effect.
TL;DR: A triterpenoid glycoside, glochidioside, has been isolated from Glochidion heyneanum as mentioned in this paper, its structure has been established as 3β[( O -β- D -glucopyranosyl-(1 → 3)- O -α- L -arabinopyranoyl)oxy]-16β-benzoyloxy-olean-12-ene-21β,23,28-trio
TL;DR: From a collisional activation spectral study, it has been found that certain triterpene alcohols with an ursane or oleanane skeleton undergo oxidation to the corresponding ketones under chemical ionization (NH3) conditions giving rise to abundant [M + NH4 2]- ions.
Abstract: From a collisional activation spectral study it has been found that certain triterpene alcohols with an ursane or oleanane skeleton undergo oxidation to the corresponding ketones under chemical ionization (NH3) conditions giving rise to abundant [M + NH4 2]+ ions. Mass-analysed ion kinetic energy and B2/E scan results indicate that both [M + NH4]+ and [M + N2H7 2]+ ions contribute to the formation of the [M + NH4 2]+ ion.
TL;DR: Results indicate that a combined treatment with an interferon inducer and muramyl dipeptide may prove highly useful to control effectively viral infections.
TL;DR: Effect of cholesterol and α - p -chlorophenoxyisobutyrate passage on virulence in Acanthamoeba culbertsoni strain A-1 and C-7 and passage through cholesterol caused gradual induction of invasiveness, stimulation of multiplication, increase in sterol andospholipid contents and phospholipase A activity of the trophozoites.
TL;DR: The problem of malaria which in the late 1950s seemed to have been solved, or at least controlled, is back with more serious problems of resistance of the vector mosquitoes to known insecticides and of the parasites to known antimalarial drugs.
Abstract: The problem of malaria which in the late 1950s seemed to have been solved, or at least controlled, is back with us along with more serious problems of resistance of the vector mosquitoes to known insecticides and of the parasites to known antimalarial drugs. The present drugs are proving inadequate - as the chloroquin-resistant Plasmodiumfalciparum is spreading, sensitivity to quinine is decreasing and primaquin, the only drug for tissue stages, is not devoid of toxicity. This underscores the need for new antimalarial drugs, particularly those which are active against resistant Plasmodium falciparum strains or tissue stages of P.vivax. Several valuable reviews have appeared on antimalarial chemotherapy [1–16] and the recent ones [17–20] deal with newer antimalarials.
TL;DR: Centchroman is a safe antifertility agent without risk of thrombotic episodes associated with hormonal oral contraceptives.
Abstract: The effect of centchroman, a non-steroidal oral contraceptive, has been studied on platelet aggregation and on the products of arachidonate metabolism. Centchroman inhibited platelet aggregation in vitro and ex vivo after acute as well as chronic treatment for one year in laboratory animals. It did not affect aggregation of platelets in women taking centchroman for one year. It is an inhibitor of platelet cyclooxygenase as indicated by the inhibition of malonaldehyde and thromboxane B2 but has no effect on vascular cyclooxygenase activity ex vivo or at low concentration in vitro. Thus, centchroman is a safe antifertility agent without risk of thrombotic episodes associated with hormonal oral contraceptives.
TL;DR: The results demonstrate complex nature of somatic extracts of adult stage as compared to microfilariae and also reveal some qualitative and quantitative differences between these stages.
Abstract: The protein and antigenic pattern of adult (female/male) and microfilarial stages of Setaria cervi, a bovine filarial parasite, was studied using certain immunochemical techniques. SDS-polyacrylamide gel electrophoretic analysis showed the presence of 35–40 protein bands in adults and 25–29 protein bands in microfilariae in molecular weight range of 10,000–200,000. Immunoelectrophoresis revealed the presence of 9–10 precipitin lines in adult and only 4 precipitin lines in microfilarial antigenic preparations. Crossed immuno-electrophoresis resolved these antigenic preparations further, and revealed the presence of 22–24 antigens in adults and 12–14 in microfilariae. These results demonstrate complex nature of somatic extracts of adult stage as compared to microfilariae and also reveal some qualitative and quantitative differences between these stages.
TL;DR: Mutagenicity of tolbutamide and glybenclamide was evaluated in vivo by the micronucleus test (MNT) in mice and TB only at two higher dose levels induced significant increase in the percentage of micron nucleated erythrocytes over that of the control, but GL failed to do so.
TL;DR: It is evident that the replacement of Trp in CCK- 4 by Glp and Pro residues leads to peptides which exhibit insulin releasing activity without stimulating the release of glucagon.
Abstract: Two synthetic analogs of CCK-4, Glp-Met-Asp-Phe-NH2 (I) and Pro-Met-Asp-Phe-NH2 (II) reported earlier to stimulate insulin release from the isolated rat pancreatic isletsin vitro at concentrations as low as 10−10 M, have now been found to be totally ineffective as glucagon releasers at concentrations as high as 10−6 M or higher. It is evident that the replacement of Trp in CCK- 4 by Glp and Pro residues leads to peptides which exhibit insulin releasing activity without stimulating the release of glucagon.
TL;DR: Some novel lipophilic derivatives of N-acetylmuramyl-L-alanyl-D-isoglutamine (MDP) have been prepared and rigorously evaluated by spectroscopic means and hold promise as adjuvants in immunization.