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Showing papers by "Central Drug Research Institute published in 1994"


Journal ArticleDOI
TL;DR: Strong stimulation of antigen specific and non-specific immunity, as evidenced by increases in humoral and delayed type hypersensitivity response to sheep red blood cells and in the macrophage migration index, has been demonstrated in mice fed with 50% ethanolic extract of seeds, flowers and leaves of this plant.

150 citations


Journal ArticleDOI
TL;DR: The cis-isomer of ebelin lactone was obtained as one of the artefacts of the aglycone and its structure revised, and the structure was established as 3-beta-[O-beta-D-glucopyranosyl(1-->3)-O- [alpha-L-arabinofuranosyl)oxy]jujubogenin by chemical and spectral analyses.

141 citations


Journal Article
TL;DR: An ethanolic extract of the fruits of T. terrestris showed significant dose dependent protection against uroliths induced by glass bead implantation in albino rats, and fractionation lead to decreased activity.
Abstract: An ethanolic extract of the fruits of T. terrestris showed significant dose dependent protection against uroliths induced by glass bead implantation in albino rats. On subsequent fractionation of the ethanol extract, maximum activity was localised in the 10% aqueous methanol fraction. It provided significant protection against deposition of calculogenic material around the glass bead. It also protected leucocytosis and elevation in serum urea levels. Further, fractionation lead to decreased activity. This could be either due to loss of active compounds during fractionation, or the antiurolithiatic activity of T. terrestris being a combined effect of several constituents present in the methanolic fraction.

76 citations


Journal ArticleDOI
TL;DR: Both oxidative stress and the antioxidant defence system were altered in myocardial ischemia and in stable angina only increased levels of superoxide anion and decreased levels ofsuperoxide dismutase, but this alteration was less marked than in unstable angina and acuteMyocardial infarction.

65 citations


Journal ArticleDOI
15 Oct 1994-Blood
TL;DR: The results suggest that NO inhibits free radical generation from rat PMNLs.

57 citations


Journal ArticleDOI
TL;DR: Antiurolithiatic activity of lupeol was assessed in rats and not only prevented the formation of vesical calculi but also reduced the size of the preformed stones.
Abstract: In the traditional Indian system of medicine Crateva nurvala (Hindi: Varuna) constitutes a major ingredient of formulations used to treat urinary disorders including urolithiasis. In an earlier study we confirmed the antiurolithiatic activity in the crude extract of the plant, and further fractionation led to the isolation of the active constituent lupeol (Lup-20(29)-en-3β-ol). Antiurolithiatic activity of lupeol was assessed in rats by observing the weight of the stone, biochemical analysis of serum and urine, and histopathology of bladder and kidney. Lupeol not only prevented the formation of vesical calculi but also reduced the size of the preformed stones.

39 citations


Journal ArticleDOI
TL;DR: The alcoholic extract of the aerial parts of Scrophularia koelzii significantly protected the rat liver against thioacetamide induced toxicity and showed maximum hepatoprotective activity.
Abstract: The alcoholic extract of the aerial parts of Scrophularia koelzii (100 mg/kg p.o. × 7 days) significantly protected the rat liver against thioacetamide induced toxicity. On its further fractionation, activity was localized in the chloroform fraction from which four iridoid glycosides, namely scropolioside-A, koelzioside, harpagoside and 6-0-(3″-0-p-methoxy-cinnamoyl)-α-L-rhamnopyranosyl catalpol were isolated. Among these, scropolioside-A showed maximum hepatoprotective activity. Immunostimulant response was observed with all the four iridoids with harpagoside exhibiting maximum induction of immune response.

39 citations


Journal ArticleDOI
TL;DR: Pippali rasayana, an Ayurvedic herbal medicine, prepared from Piper longum and Butea monosperma, and prescribed for the treatment of chronic dysentery and worm infestations was tested for anti-giardial and immuno-stimulatory activity in mice infected with Giardia lamblia trophozoites and produced up to 98% recovery from the infection.

38 citations


Journal ArticleDOI
TL;DR: The results indicate that the morphine induced straub tail response is mediated by central mu 2-opioid receptors, and that morphine induced analgesia while the straUB tail response was not affected.

38 citations


Journal ArticleDOI
TL;DR: Investigations have been carried out involving fed-batch cultivation of Bacillus thuringiensis, which is known to produce an insecticidal crystal protein during sporulation, and suggested a complex interplay of energetic requirements for protein turnover during sporulating.
Abstract: Sporeformers are sources of a large number of industrially important biological products including enzymes, antibiotics, and bioinsecticides. Cultivation of these microorganisms to high cell densities offers potential for enhancing the rates of formation as well as the concentration of the desired products in the fermentation broths in bioreactors. With this objective, investigations have been carried out involving fed-batch cultivation of Bacillus thuringiensis, which is known to produce an insecticidal crystal protein during sporulation. With appropriate management of aeration and nutrient supply, it was possible to grow the cells to > 50 g DW/l density. Nevertheless, the achievement of high cell density did not enhance the formation of crystal protein in the same proportion as the cell concentration. Further examination of this system suggested a complex interplay of energetic requirements for protein turnover during sporulation. Energy reserve material, poly-beta-hydroxybutyric acid, appeared to be linked to formation of spores and crystal protein during the sporulation phase.

37 citations


Journal ArticleDOI
TL;DR: The hypolipidaemic action of picroliv, a standarized preparaton from Picrorhiza kurrooa, has been studied in normal as well as in triton‐ and cholesterol‐fed rats and caused lowering in the lipid and protein levels constituting β‐lipoproteins followed by an increase in high density lipoprotein cholesterol in experimental animals.
Abstract: The hypolipidaemic action of picroliv, a standarized preparaton from Picrorhiza kurrooa, has been studied in normal as well as in triton- and cholesterol-fed rats. Serum lipids were found to be lowered by picroliv (25 mg/kg b.w.) in triton WR-1339-induced hyperlipaemia. Chronic feeding of this drug (6 mg/kg b.w.) in normal rats and in animals simultaneously treated with cholesterol (25 mg/kg b.w.) for 30 days caused lowering in the lipid and protein levels constituting β-lipoproteins followed by an increase in high density lipoprotein cholesterol in experimental animals. Picroliv alters lipolytic activities in plasma, liver, heart an adipose tissues and stimulated receptor mediated catabolism of low density lipoprotein. The lipid lowering action of the natural product is mediated through inhibition of cholesterol biosynthesis in liver, increased faecal bile acid excretion and enhanced plasma lecithin: cholesterol acyltransferase activity.

Journal ArticleDOI
TL;DR: The synthesis and antifertility activity of 1, 5-diaryl-3-(3'-indolyl)formazans with a substituted aryl group (2-8) are described.
Abstract: The synthesis and antifertility activity of 1, 5-diaryl-3-(3'-indolyl)formazans with a substituted aryl group (2-8) are described.

Journal ArticleDOI
TL;DR: Observations indicate that morphine exerted a dose-dependent, biphasic effect on the course of P. berghei infection in mice, apparently by modulating the macrophage-mediated protective mechanisms.

Journal ArticleDOI
TL;DR: It is suggested that the bioactive l-enantiomer of centchroman will have the 3R,4R absolute configuration, when the chroman ring system is positioned over the AB rings of estradiol, which makes the best fit.
Abstract: We have determined an X-ray crystal structure for the N-methyl iodide derivative of the nonsteroidal contraceptive centchroman. The pendant aromatic substituents on C-3 and C-4 of the chroman system are nearly perpendicular to the plane of the chroman system, an orientation expected in such a chroman, but perturbed to some degree by the gem dimethyl substituents at C-2. Structural superposition with other nonsteroidal antiestrogens, tamoxifen and nafoxidine, shows a similar disposition of the tertiary amine side chains responsible for antagonist activity. The aryl rings also show good superposition, but in contrast to tamoxifen and nafoxidine, which have the potential for ring double bond conjugation, the centchroman aryl rings show a larger dihedral twist. While different superpositions between the enantiomers of centchroman and the bioactive enantiomer of estradiol (d-estradiol, 8 beta,9 alpha,13 beta,14 alpha,17 beta) are possible, when the chroman ring system is positioned over the AB rings of estradiol, then (3R,4R)-centchroman makes the best fit. The aryl substituents in both enantiomers make comparable overlays with the steroidal skeleton, but the axial methyl group at C-2 in (3R,4R)-centchroman is directed downward along the C-7 alpha axis of estradiol, a site where many substituents are known to be well tolerated by the estrogen receptor, while in the 3S,4S-enantiomer, this methyl group is projected upward. Thus, we suggest that the bioactive l-enantiomer of centchroman will have the 3R,4R absolute configuration.

Book ChapterDOI
TL;DR: Cancer is perhaps one of the most active anti-human factor operating in the world today, and efforts are being made all over the scientific world to prevent and eradicate it.
Abstract: Cancer is perhaps one of the most active anti-human factor operating in the world today, and efforts are being made all over the scientific world to prevent and eradicate it. All possible avenues are being tapped; from the most obvious to the least probable sources are under study.

Journal ArticleDOI
TL;DR: Two recA mutants of Vibrio cholerae (classical and El Tor biotypes) were constructed by disruption of the wild-type recA gene with mutated recA sequences of V. Cholerae cloned in the suicide vector pGP704 to study adherence to isolated rabbit intestine and colonization of intestine of infant mice.
Abstract: Two recA mutants of Vibrio cholerae (classical and El Tor biotypes) were constructed by disruption of the wild-type recA gene with mutated recA sequences of V. cholerae cloned in the suicide vector pGP704. Mutants defective in the recA gene were compared with their respective RecA + parent strains with regard to their adherence to isolated rabbit intestine and colonization of intestine of infant mice. The recA mutation in V. cholerae was found to diminish adherence and markedly affected colonization.

Journal ArticleDOI
TL;DR: A precise and sensitive high-performance liquid chromatographic assay was developed and validated for determination of centchroman (I) and its 7-demethylated metabolite (II) in human serum and milk.

Journal ArticleDOI
TL;DR: The duration of the anti-implantation action of a single oral post-coital dose of a triphenylethylene anti-oestrogen, centchroman, was determined in adult rats and suggests lack of significant effect on follicular maturation, ovulation, fertilization, preim implantation development or mating behaviour.
Abstract: The duration of the anti-implantation action of a single oral post-coital dose (1.25 mg kg \m=-\1) of a triphenylethylene anti-oestrogen, centchroman, was determined in adult rats. The effects of centchroman were compared with those of tamoxifen. In rats undergoing delay, centchroman administered orally on day 7 post-coitum prevented the induction of implantation of delayed blastocysts by an implantation inducing dose (1 \g=m\gper rat, s.c.) of oestrone which was administered earlier than 120 h after centchroman treatment. In tamoxifen (0.2 mg kg \m=-\1, orally) pretreated rats, oestrone administered at 144 h or later induced implantation. In cyclic rats treated with centchroman at intervals of 168 h and mated with males of proven fertility, implantation was prevented only when the interval between centchroman treatment and nidatory oestrogen secretion was less than 120 h. None of the females conceived when treated regularly at intervals of 120 h during exposure to fertile males. Discontinuation of treatment resulted in the occurrence of normal implantations in rats that mated 48 h or later after the last dose of centchroman, since in these animals the interval between anti-oestrogen treatment and nidatory oestrogen secretion was greater than 120 h. These findings suggest that the duration of the anti-implantation action of a single oral antifertility dose of centchroman in rats is about 120 h. Recovery of normal blastocysts from rats treated continuously with this dose of centchroman at these intervals suggests lack of significant effect on follicular maturation, ovulation, fertilization, preimplantation development or mating behaviour. Tamoxifen appears to be slightly longer acting and the duration of its action was about 144 h.

Journal ArticleDOI
01 Jan 1994
TL;DR: The Ethanol Extract of T. Terrestris (Fruit) exhibited Dose-Dependent Antiurolithiatic Activity and Almost Completely Inhibited Stone Formation, which substantiate the Traditional Claim of Therapeutic Claims made for this Plant in Traditional Medicine.
Abstract: Tribulus Terrestris (Fruit) Has Been Used Widely In The Ayurvedic System Of Medicine For The Treatment Of Various Urinary Disorders Including Urolithiasis. In Order To Evaluate The Therapeutic Claims Made For This Plant In Traditional Medicine, The Ethanol Extract Of T. Terrestris (Fruit) Was Tested For Activity Against Artificially Induced Urolithiasis In Albino Rats. The Extract Was Administered At Daily Oral Doses Of 25, 50 and 100 Mg/Kg For 4 Months. It Exhibited Dose-Dependent Antiurolithiatic Activity and Almost Completely Inhibited Stone Formation. Other Biochemical Parameters In Urine and Serum, and The Histopathology Of Urinary Bladder, Which Were Altered During The Process Of Stone Formation, Were Also Normalized By The Plant Extract In A Dose-Dependent Manner. These Observations Thus Substantiate The Traditional Claim. Further Detailed Study Is In Progress To Isolate The Active Principle(S) and To Establish Their Mode(S) Of Action.

Journal ArticleDOI
01 Jan 1994-Vaccine
TL;DR: It is suggested that liposomes and microspheres could be used as carriers of protective antigens of V. cholerae for effective immunization.

Journal ArticleDOI
TL;DR: In this paper, a leishmanicidal activity against L. donovani promastigotes was evaluated using quinazolinone and triazoloquinazolone derivatives.

Journal ArticleDOI
TL;DR: The peptides appeared to exert their inhibitory and augmenting effects via delta- and mu-opioid receptors, respectively, as pretreatment of splenocytes with 100-fold higher concentration of naloxone was required to block their inhibitor effect; the augmenting effect was blocked by 1 x 10(-5) M only.

Journal ArticleDOI
TL;DR: Results show that none of the compounds induced vaginal cornification, even at doses as high as 2.5 mg/kg, and the provision of aminoethoxy side chain at para-position and a shift in the piperidinoeth oxygen side chain from position-4 to position-2 in these molecules resulted in a decrease in estrogenicity and increase in antagonistic property.

Journal ArticleDOI
01 Jan 1994-Peptides
TL;DR: The results of these studies show that changes in endogenous CHP levels may affect body temperature regulation, and a rise in hypothalamic CHP content accompanied a decrease in rectal temperature during cold exposure.

Journal ArticleDOI
TL;DR: In this article, the synthesis and hepatoprotective activity of 1,3-dithiolanes and pyrazole were described. But the synthesis of pyrazolines was not considered.

Journal Article
TL;DR: Picroliv, the standardized preparation of iridoid glycosides from Picrorhiza kurrooa, at the dose of 6 mg/kg, po for two weeks provided significant protection against depletion of reduced glutathione levels in liver and brain of Plasmodium berghei infected Mastomys natalensis.
Abstract: Picroliv, the standardized preparation of iridoid glycosides from Picrorhiza kurrooa, at the dose of 6 mg/kg, po for two weeks provided significant protection against depletion of reduced glutathione levels in liver and brain of Plasmodium berghei infected Mastomys natalensis. The activation of gamma-glutamyl transpeptidase enzyme and decreased levels of cysteine, sulphydryl groups as well as glutathione synthesis in both tissues due to P. berghei infection were reversed by picroliv. Enzymatic and non enzymatic lipid peroxidation in microsomes in vitro was significantly reduced by picroliv along with the recovery of reduced glutathione.

Journal ArticleDOI
TL;DR: Several 5-Cyano-6-substituted-2-thiouracils (1a-e) and their monocyclic (2,3,4,6) and bicyclic (5) derivatives have been prepared and evaluated for in vivo leishmanicidal activity against L. donovani in hamster as mentioned in this paper.

Journal ArticleDOI
TL;DR: The data suggest that T-87 is mutated in a regulatory gene which regulates the expression of proteins involved in intestinal colonization, and this gene is associated with Vibrio cholerae 01 strain 0395.

Journal ArticleDOI
TL;DR: The studies indicate that energy metabolism in the epididymis (as well as in the vas deferens) is strictly androgen dependent and the energy charge of these target organs is likely to fall appreciably after castration, which may in turn affect many energy dependent processes of these organs.
Abstract: The activities of nine enzymes of the TCA cycle were estimated in the initial segment, caput, corpus and cauda segments of epididymis and vas deferens of adult rhesus monkey and expressed as units per mg DNA. These enzymes were also estimated in epididymal segments and vas deferens of castrated and castrated-androgen replaced monkeys as well. Results indicated higher activities of most of the enzymes in vas deferens as compared to epididymal segments. All the enzymes showed marked reduction in epididymis and vas deferens after castration, the effect being much more pronounced in the epididymis, than in the vas. Androgen replacement in castrated monkeys stimulated most of the enzymes markedly in epididymis and in the vas deferens as compared to their castrated values. The response of cauda and vas deferens to exogenous androgen treatment was however moderate, as compared to the other epididymal segments. The studies indicate that energy metabolism in the epididymis (as well as in the vas deferens) is stric...

Journal ArticleDOI
TL;DR: A high-performance liquid chromatographic assay method using precolumn derivatization and fluorescence detection has been developed and validated for the determination of ampicillin in serum and provides improved selectivity and sensitivity over other existing HPLC methods.