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Showing papers by "Central Drug Research Institute published in 1984"


Journal ArticleDOI
TL;DR: A reinvestigation of Clausena anisata has yielded imperatorin, xanthotoxol, lansamide-I and three new furanocoumarin lactone derivatives.

36 citations


Journal ArticleDOI
TL;DR: It is demon‐strate that grafting of tuftsin on the liposome bilayer enables theliposome to recognize specifically the PMN leukocytes and to deliver its contents to these cells.

33 citations


Journal ArticleDOI
TL;DR: In all specimens, 5-hydroxytryptamine was the highest while norepinephrine was found to be uniformly low and the female reproductive organ contained the maximum amount of dopamine while intestine was rich in histamine.

29 citations


Journal ArticleDOI
TL;DR: The aerial parts of DODONAEA VISCOSA afforded a new diterpenoid, dodonic acid, the structure and stereochemistry of which have been established by chemical and spectroscopic means.
Abstract: The aerial parts of DODONAEA VISCOSA afforded a new diterpenoid, dodonic acid, the structure and stereochemistry of which have been established by chemical and spectroscopic means.

29 citations


Journal ArticleDOI
TL;DR: A new isoprenylated flavanone has been isolated from the leaves of Azadirachta indica and characterized as 8,3′-di-isopronyl-5,7-dihydroxy-4′-methoxyflavanone on the basis of physical and spectroscopic evidence as discussed by the authors.

28 citations


Journal ArticleDOI
TL;DR: Hydroxylation in the 11 α‐position in the progesterone molecule employing immobilized spores of Aspergillus ochraceus strain No.
Abstract: Hydroxylation in the 11 alpha-position in the progesterone molecule employing immobilized spores of Aspergillus ochraceus strain No. G8 (CDRI catalogue No.) was achieved. For immobilization the activity of the spores was evaluated on a variety of matrices such as alginate beads, epoxy resin beads, polyacrylamide gel, and collagen. Spores entrapped in polyacrylamide gel were found to be the most active. Studies of various parameters, e.g. monomer content, cell loading capacity, optimum pH, temperature, and substrate concentration, were carried out on polyacrylamide gel. In polyacrylamide, the entrapped spores normal decay pattern, as indicated by loss of activity, was observed after four uses. At the end of 15 cycles, the residual activity was found to be 18% of the original. It was possible to regenerate the activity by incubating the preparation in a nutrient medium. The regenerated spores showed increasing rate of loss of activity upon recycling.

26 citations


Journal ArticleDOI
TL;DR: The results demonstrate that the transbilayer distribution of erythrocyte membrane phospholipids in unilamellar vesicles are controlled mainly by the surface curvature rather than by interlipid interactions, and suggest that phospholippid-phospholipid and phospholIPid-cholesterol interactions should not play any significant role in determining the membrane phospholipper asymmetry in red cells.

25 citations


Journal ArticleDOI
TL;DR: Age-related conformational changes in the B-cell membrane are suggested as a possible explanation for the above observation of basal insulin secretion and45Ca2+ uptake by rat islets of Langerhans.
Abstract: Thein vitro basal insulin release and45Ca2+ uptake by rat islets of Langerhans remain unaffected by the animal’s age. However, whenAgaricus bisporus lectin PHA-B is added to the medium, there is a significant stimulation of basal insulin secretion and45Ca2+ uptake. The islets isolated from younger rats are more sensitive toA. bisporus PHA-B stimulation and register 1.5-fold and 3-fold more increases of insulin release and45Ca2+ uptake respectively as compared to islets isolated from 12-month-old rats. Age-related conformational changes in the B-cell membrane are suggested as a possible explanation for the above observation.

17 citations


Journal ArticleDOI
TL;DR: The unsaturated trans dicarboxylates (III and IV) form stable (M+N2H7)+ adducts in addition to the (m+NH4)+ adduction as discussed by the authors.

16 citations


Journal ArticleDOI
TL;DR: Sagittariol, heretofore considered to be 17-hydroxymanool, has been shown to incorporate an A-B cis clerodane skeleton on the basis of a 13 C NMR spectral analysis of several labdanic and clerodanic diterpenes.

16 citations


Journal ArticleDOI
TL;DR: The structure of a new meliacin named salannolide has been elucidated by physicochemical data as discussed by the authors, the unique feature of this compound is the presence of a hydroxybutenolide side chain in place of the usual furan ring attached at C-17.

Journal ArticleDOI
TL;DR: All anthelmintics examined interfered with the mitochondrial phosphorylation of ADP, with maximum inhibition by salicylanilide compounds, and the anticestodal activity of the latter group of compounds, niclosamide for example, may, therefore, be attributed to their ability to inhibit mitochondrialosphorylation.

Journal ArticleDOI
TL;DR: These phosphatidylcholine (PC) analogs are useful for studying the possible role of phospholipases in the capture and lyses of liposomes in vivo.

Journal ArticleDOI
TL;DR: Four species of Cedus are widely distributed over the Asian subcontinent and are well known for their wood and medicinal properties and have been investigated extensively over the last three decades.

Journal ArticleDOI
TL;DR: The in vitro release of eggs in a 24-hour period by one female nematode peaked from day 25 to day 39, a second rise occurred in day 70 after infection and thereafter gradually declined.
Abstract: Ancylostoma ceylanicum is a new introduction as an experimental hookworm model. Information on the biology of this parasite in its laboratory host--the golden hamster, is meagre. Its infectivity, longevity and fecundity were studied to obtain relevant information especially on vulnerable points in the maintenance and continuation of the infection. 100% infectivity was obtained with an inoculum of 60 larvae per animal. Maximum numbers of parasites were harboured from day 15 to day 18 after infection and thereafter gradually declined. Approximately 10% of the worms were still present at the end of the third month of infection. The in vitro release of eggs in a 24-hour period by one female nematode peaked from day 25 to day 39, a second rise occurred in day 70 after infection.

Journal ArticleDOI
TL;DR: Polyacrylamide gel electrophoresis and temperature dependent binding characteristics revealed that the protein responsible for centchroman binding to human plasma resembles albumin.
Abstract: Centchroman, a non-steroidal antifertility agent showed a low affinity (Kd = 13.19 X 10(-6) M) and nonsaturable binding to human plasma. Centchroman did not compete either with sex hormone binding globulin or corticosteroid binding globulin. Polyacrylamide gel electrophoresis and temperature dependent binding characteristics revealed that the protein responsible for centchroman binding to human plasma resembles albumin.

Journal ArticleDOI
TL;DR: Two new biphenyls characterized as 4-(3-methyl-but-2-enyl)-5-methoxy-[1,1′-biphenyl]-3-ol 1 and 2-carboxy-4-(3]-methyl, but-2]-5methoxyl-5mETHoxy [1, 1, 1′)-3-, 3-ol 5 have been isolated from Rhynchosia suaveolens as discussed by the authors.

Journal ArticleDOI
TL;DR: In this paper, a study of the D 2 O chemical ionization mass spectra of certain flavonoids has shown that, besides the replaceable hydroxyl hydrogens, aromatic hydrogens also undergo exchange with deuterium.

Journal ArticleDOI
TL;DR: The feeding of garlic oil and guggulipid an exudate ofCommiphora mukul, to normal rabbits caused significant increase in the dopamine-Β-hydroxylase activity and catecholamine levels, while the feed helped the hypercholesterolemic rabbits to recover the decrease in ctcholamine biosynthesis.
Abstract: The effect of lipid lowering agents of plant origin garlic oil and guggulipid on the levels of catecholamine and dopamine Β-hydroxylase activity of normal and cholesterol fed rabbit tissues has been studied. The catecholamine levels and enzyme activity were found to be decreased in cholesterol (500 mg/kg body wt) fed animals. The feeding of garlic oil (5 mg/kg body wt) and guggulipid (100 mg/kg body wt) an exudate ofCommiphora mukul, to normal rabbits caused significant increase in the dopamine-Β-hydroxylase activity and catecholamine levels, while the feed helped the hypercholesterolemic rabbits to recover the decrease in catecholamine biosynthesis

Journal ArticleDOI
TL;DR: The structure of a triterpene lactone, palustrolide, has been elucidated as 3β,23-dihydroxylupan-13β→28 lactone on the basis of physico-chemical studies as discussed by the authors.

Journal ArticleDOI
TL;DR: The results suggested that the prostatic zinc may be under dual hormonal control, but in the epididymis and vas deferens it might be under the influence of estrogen.
Abstract: The zinc content in the three segments of the epididymis (caput, corpus, and cauda), vas deferens, seminal vesicles, and prostate of juvenile monkeys was determined by atomic absorption spectrophotometry. Zinc content (micrograms/gm wet weight) was found to be maximum (328) in the vas deferens; in the other organs it measured in the following order: caput 191, corpus 238, cauda 193, prostate 133 and seminal vesicles 85. In order to investigate the endocrine control of the zinc in these organs, two groups of animals were treated with testosterone propionate (2 mg) or estradiol dipropionate (10 micrograms) once daily for 30 days. In response to androgen, a rise in both concentration and content of zinc was evident only in the prostate. The results further suggested that the prostatic zinc may be under dual hormonal control, but in the epididymis and vas deferens it may be under the influence of estrogen. It is concluded that the hormonal effects on zinc content and growth stimulation in accessory sex organs are quite separate and may be under different hormonal control.

Journal ArticleDOI
TL;DR: Several compounds structurally related to the triarylethylene antiestrogens, but possessing weak estrogen receptor affinities, were assessed for their ability to interact with the microsomal antiestrogen binding site and the cis isomer of centchroman has however emerged as a selective ligand for the antiest estrogen binding site.

Journal ArticleDOI
TL;DR: Two tetrapeptides analogous to the C-terminal tetrapptide amide of cholecystokinin have been synthesized and their effect on the release of insulin from the isolated Langerhans islets of rat pancreas compared with that of synthetic CCK-4.
Abstract: Two tetrapeptides, Glp-Met-Asp-Phe-NH2 (I) and Pro-Met-Asp-Phe-NH2 (II), analogous to the C-terminal tetrapeptide amide of cholecystokinin (CCK-4) have been synthesized and their effect on the release of insulin from the isolated Langerhans islets of rat pancreas compared with that of synthetic CCK-4. Both the new congeners exhibited significant insulin-releasing activity at 10−8 M and 10−6 M concentrations, suggesting that the biological activity is retained when the N-terminal Trp residue of CCK-4 is replaced by Glp or Pro.

DOI
01 Sep 1984
TL;DR: Biodegradation of isoniazid and isonicotinate appears to be more complex and formation of characteristic pigments suggests the involvement of hydroxylated compounds as intermediates.
Abstract: Studies on biotransformation of pyridine derivatives have revealed two alternative patterns of biodegradation. Pyridine and α-picoline are not degradedvia the hydroxylated derivatives. A reductive pathway involving succinic semialdehyde (SSA) or glutaric semialdehyde is involved in degradation of pyridine, α-picoline and possibly other alkyl pyridines. α-Picolinate, nicotinate, isonicotinate and hydroxypyridines are degradedvia hydroxypyridine derivatives. Studies on aNocardia strain capable of growth on pyridine-N-oxide (PNO), 2-hydroxypyridine and pyridine rule out the involvement of PNO or 2-hydroxypyridine in pyridine metabolism. PNO is metabolizedvia 2-hydroxypyridine while pyridine is metabolizedvia SSA. Biodegradation of isoniazid and isonicotinate (INA) appears to be more complex. INA is degraded in several organismsvia 2-hydroxy INA and citrazinic acid. However, a strain ofBacillus brevis isolated in our, laboratory metabolises isonicotinatevia SSA, and a pathway similar to that of N-methyl-INA may be operative. Several organisms degrading quinoline and isoquinoline have been isolated. Formation of characteristic pigments suggests the involvement of hydroxylated compounds as intermediates.

DOI
01 May 1984
TL;DR: The chemical, pharmacological and biosynthetic status of alkaloids from plants which either have a reputation in folklore medicine or the extracts of which have shown consistent biological activity in a broad biological screen has been reviewed.
Abstract: The chemical, pharmacological and biosynthetic status of alkaloids from plants which either have a reputation in folklore medicine or the extracts of which have shown consistent biological activity in a broad biological screen has been reviewed.

Journal ArticleDOI
TL;DR: Isoxazolo[5,4-b]quinolines have been prepared by reacting 3-acyl or aroyl-2-chloro-6-alkoxy or 6,7-dialkoxyquinoline with hydroxylamine as discussed by the authors.

Book ChapterDOI
TL;DR: The main causes of this set-back are undoubtedly the appearance of drug-resistance in malarial parasites and Resistance to all the currently available drugs is a reality.
Abstract: Malaria is an old scourge of mankind and mention of the disease is found in ancient writings in India, Egypt and China [1]. The clinical symptoms of this disease were described by Hippocrates 400 years before the Christian era [1]. Human population affected by malaria is alarmingly large in tropical regions although in the past the disease was also prevalent in temperate regions [1]. The respite from this disease after World War II, due to the success in the control of the vector mosquitoes and development of new antimalarials, was, however, short lived and malaria has staged a come back in recent years. Only two decades back WHO had stated The clinicians have at their disposal a complete series of effective drugs for the treatment of all stages of this disease’ [2] but in 1971 the same organization considered malaria eradication as a difficult problem both technically and politically [3] and commented ‘Thus there is no avoiding the conclusion that malaria will be with us for quite sometime. In order to cope more efficiently with this world-wide problem, much more research is required’ [4]. It would, therefore, be pertinent to analyse the main causes of this set-back. The principal reason is undoubtedly the appearance of drug-resistance in malarial parasites. Resistance to all the currently available drugs is a reality; even the age-old remedy, quinine, has the same limitations as the synthetic drugs.

Journal ArticleDOI
TL;DR: The 1,4‐substituted piperidines 16–22 have been synthesized from the 1‐subStituted 4‐piperidones 5 and 6 and the antiamoebic, antileishmanial and anticancer activities of these compounds are described.
Abstract: The 1,4-substituted piperidines 16–22 have been synthesized from the 1-substituted 4-piperidones 5 and 6. The antiamoebic, antileishmanial and anticancer activities of these compounds are described. Synthese und biologische Aktivitat 1,4-disubstituierter Piperidine Die 1,4-substituierten Piperidine 16–22 wurden ausgehend von den 1-substituierten 4-Piperidonen 5 und 6 synthetisiert. Die Aktivitaten dieser Verbindungen gegenuber Amoeben, Leishmanien und lymphatischer Leukamie werden beschrieben.

Journal ArticleDOI
TL;DR: It is concluded that serotonergic mechanism does not play a significant role in the regulation of blood-brain barrier in anaesthetised cats and dogs.

Journal ArticleDOI
TL;DR: In this article, the chemical constituents present in the chloroform-soluble fraction of the ethanolic extract of Caltha palustris have been investigated and two of them, caltholide and epicaltholide, have been characterized as 24-nor-3β-hydroxylupan-13β,28-lactone and its 3α-isomer, respectively.