Showing papers by "Central Drug Research Institute published in 2009"
TL;DR: Slight increases in size were found for the Poloxamer and the Tween stabilized nanosuspensions, which is not considered to impair their use in dermal formulations.
271 citations
TL;DR: The studies presented here provide structural modification of fluconazole to give 1,2,3-trazole containing molecules which were evaluated in vivo against Candida albicans intravenous challenge in Swiss mice and antiproliferative activities were tested against human hepatocellular carcinoma Hep3B and human epithelial carcinoma A431.
268 citations
Journal Article•
TL;DR: The biological activities of some isolated chemical constituents of A. marmelos are covered and preclinical studies on some crude extracts and pure compounds to explore novel bioactive compounds for therapeutic application are covered.
Abstract: Bael (Aegle marmelos (L.) Corr.) is an important medicinal plant of India. Leaves, fruits, stem and roots of A. marmelos have been used in ethno medicine to exploit its’ medicinal properties including astringent, antidiarrheal antidysenteric, demulcent, antipyretic and anti-inflammatory activities. Compounds purified from bael have been proven to be biologically active against several major diseases including cancer, diabetes and cardiovascular diseases. Preclinical studies indicate the therapeutic potential of crude extracts of A. marmelos in the treatment of many microbial diseases, diabetes and gastric ulcer. This review covers the biological activities of some isolated chemical constituents of A.marmelos and preclinical studies on some crude extracts and pure compounds to explore novel bioactive compounds for therapeutic application.
242 citations
TL;DR: An overview of the natural presence and development of the chemistry of the 2 H -pyran-2-one ring system is delineated in this article, where 363 references are provided.
221 citations
TL;DR: A highly atom economic one pot synthesis of tetrahydropyridines was achieved by L-proline/TFA catalysed multicomponent reaction of beta-keto-esters, aromatic aldehydes and anilines.
185 citations
TL;DR: Effectiveness of antioxidant, melatonin but not of anti-cholinesterase, donepezil against STZ induced changes in IR indicates that IR is more affected with oxidative stress than cholinergic changes.
142 citations
TL;DR: The synthesized imidazole based compounds screened against Mycobacterium tuberculosis where compound 17 exhibited very good in vitro antitubercular activity and may serve as a lead for further optimization.
119 citations
TL;DR: Rare aurantiamide acetate 4 and 1,3-dibenzyl urea 5 have been isolated and characterized, the first report of isolation from this genus, and showed significant analgesic activities in a dose dependant manner.
114 citations
TL;DR: This study reveals the critical role of intra-mitochondrial ·OH generation is crucial for the development of mitochondrial pathology and activation of mitochondrial death pathway by indomethacin.
113 citations
TL;DR: The results indicate that compounds 3b, 5a and 5b have potent antifungal activity and amongst the most promising antIFungal compounds, 3b showed better antifundal activity than clinically prevalent antif fungus drug Fluconazole.
109 citations
TL;DR: Treatment with M. pruriens regulates steroidogenesis and improves semen quality in infertile men and reduced levels of FSH and PRL are seen.
TL;DR: The in vivo evaluation of a few compounds among the series led to discovery of one analog displaying 40% curative activity against mdr P. yoeillinigeriensis at an oral dose of 100 mg/kg x 4 days.
TL;DR: Five compounds showed promising osteogenic activity, attributed to increased osteoblast proliferation, differentiation and mineralization as evidenced by marked increase in expression of alkaline phosphatase, an early phase differentiation marker, and alizarin Red S staining of osteoblasts cultured for 48 h and von Kossa silverStaining of nodules formed 15 days after culture with these compounds.
TL;DR: A series of 2-chloro-3-arylsulfanyl-[1,4]naphthoquinones and 12H-benzo[b]phenothiazine-6,11-diones and their analogs 6-8 were synthesized and evaluated for their antiproliferative activity against human cervical cancer (HeLa) cells and compounds 3a and 3b were found to possess most potent antiprolliferative and cell killing ability.
TL;DR: The results suggest that AT1 receptors play a facilitatory role in STZ induced memory deficit and corroborate number of human studies that At1 receptor blockers can be used therapeutically against cognitive decline in hypertensive patients.
TL;DR: A comparison of structure-activity relationship reveals that different physicochemical and structural requirements exist for these two activities.
TL;DR: In this article, a new route to the synthesis of the isocryptolepine alkaloid with antimalarial activity using a modified Pictet-Spengler reaction has been devised.
TL;DR: The results suggest the N-terminal domain of L. donovani ppg as a potential DNA vaccine against visceral leishmaniasis as well as golden hamsters against the L.Donovani challenge.
Abstract: Leishmania produce several types of mucin-like glycoproteins called proteophosphoglycans (PPGs) which exist as secretory as well as surface-bound forms in both promastigotes and amastigotes. The structure and function of PPGs have been reported to be species and stage specific as in the case of Leishmania major and Leishmania mexicana; there has been no such information available for Leishmania donovani. We have recently demonstrated that PPG is differentially expressed in sodium stibogluconate-sensitive and -resistant clinical isolates of L. donovani. To further elucidate the structure and function of the ppg gene of L. donovani, a partial sequence of its N-terminal domain of 1.6 kb containing the majority of antigenic determinants, was successfully cloned and expressed in prokaryotic as well as mammalian cells. We further evaluated the DNA-encoding N-terminal domain of the ppg gene as a vaccine in golden hamsters (Mesocricetus auratus) against the L. donovani challenge. The prophylactic efficacy to the tune of ∼80% was observed in vaccinated hamsters and all of them could survive beyond 6 mo after challenge. The efficacy was supported by a surge in inducible NO synthase, IFN-γ, TNF-α, and IL-12 mRNA levels along with extreme down-regulation of TGF-β, IL-4, and IL-10. A rise in the level of Leishmania-specific IgG2 was also observed which was indicative of enhanced cellular immune response. The results suggest the N-terminal domain of L. donovani ppg as a potential DNA vaccine against visceral leishmaniasis.
TL;DR: This review covers about 40 species of the genus Sinularia, in which many compounds with novel chemical structures have been isolated, characterised and bioassayed for various activities since the beginning of marine chemistry until now.
TL;DR: The challenge is now to identify the precise signaling pathways and the mechanisms by which germ cells and germ cell tumors initiate cell death processes, and to utilize this information for improving reproductive health related issues.
TL;DR: It was found that PB-BM was capable of selectively inhibiting both stages of Leishmania parasites by accelerating apoptotic events by generation of reactive oxygen species targeting the mitochondria without any cytotoxicity towards macrophages.
Abstract: In the absence of effective and safe treatment for visceral leishmaniasis or Kala-azar – a devastating parasitic disease caused by Leishmania donovani – the search for anti-leishmanial agents from natural resources in common use is imperative. Recently, the comparative in vitro anti-leishmanial activity of methanolic extracts from two landraces of Piper betle – P. betle landrace Bangla Mahoba (PB-BM) and P. betle landrace Kapoori Vellaikodi (PB-KV) – has been reported. Here, the putative pathway responsible for death induced by the effective extract of PB-BM methanolic extract in promastigotes, as well as the intracellular amastigote form of L. donovani, was assessed using various biochemical approaches. It was found that PB-BM was capable of selectively inhibiting both stages of Leishmania parasites by accelerating apoptotic events by generation of reactive oxygen species targeting the mitochondria without any cytotoxicity towards macrophages. The study was extended to determine the presence or absence of activity of the methanolic extract of PB-BM and PB-KV on the basis of differences in essential oil composition present in the extract assessed by GC and MS. The essential oil from PB-BM was found to be rich in eugenol compared with that from PB-KV. The anti-leishmanial efficacy of PB-BM methanolic extract mediated through apoptosis is probably due to the higher content of eugenol in the active landrace. This observation emphasizes the need to extend studies related to traditional medicines from bioactive plants below the species level to the gender/landrace level for better efficacy and reproducibility.
TL;DR: Thiourea derivative 3 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro model with an IC(50) of 6.07ng/mL and also showed an in vivo suppression of 99.27% on day 4 against C Q resistant strain N-67 of PlAsmodium yoelii.
TL;DR: The present review summarizes the ethnic use, pharmacological activities of the extracts and phytoconstituents of T. arjuna for last 90 years.
Abstract: Terminalia arjuna Wight & Arn. (Combretaceae) is a tree having an extensive medicinal potential. The plant is used traditionally in the treatment of various aliments. T. arjuna is a very good hypocholsteremic, hypolipidemic, anticoagulant, antihypertensive, antithrombotic, antiviral, antifungal and antibacterial agent Various parts of plant have been investigated for the presence of phytoconstituents and pharmacological activities. Many useful phytoconstituents have been isolated from T. arjuna. Triterpenoids are mainly responsible for cardiovascular properties. Tannins and flavonoids are responsible for its anticancer properties. The present review summarizes the ethnic use, pharmacological activities of the extracts and phytoconstituents of T. arjuna for last 90 years.
TL;DR: Mitochondrial GSH depletion and formation of protein carbonyl indicate that mitochondrial pathology is associated with mitochondrial oxidative stress, and mitochondrial (.)OH generation correlates with the activation of both caspase-9 and caspases-3 with the progress of malarial infection, indicating the critical role of (.) OH.
TL;DR: Making analogues of the most potent molecule for developing synthetic series with rational drug design approach could pay rich dividends in menopausal osteoporosis therapy.
Abstract: Substantial body of data generated from cultured bone cells and rat models of osteoporosis supports a significant bone-conserving effect of phytochemicals. Flavonoids including isoflavones, stilbenes and lignans with variable efficacy have shown promising therapeutic application in osteoporosis. Majority of the phytochemicals assessed for their effects on bone cells revealed multiple beneficial actions such as promoting osteoblast functions, and inhibiting osteoclast and adipocyte functions. A variety of molecular targets mediate multiple effects of phytochemicals in bone cells. In vivo, quite a few phytochemicals have been found to afford bone-sparing effect and in some cases even bone restoring effect. However, important pharmacokinetic and bioavailaibility studies associated with these phytochemicals are mostly lacking. As a result, translating these findings to the clinic has been challenging, and so far only a few clinical studies have attempted to evaluate the effect of phytochemicals in menopausal osteoporosis. Clinical studies so far performed are with dietary supplements rather than pure phytochemicals. Clinical trials with pure molecules necessitate preclinical regulatory and safety studies that are not available with the phytochemicals except ipriflavone with bone-conserving properties. Ipriflavone is the only marketed anti-osteoporosis agent that was obtained following a lead from natural substance. As phytochemicals have multiple beneficial influences on bone cells, making analogues of the most potent molecule for developing synthetic series with rational drug design approach could pay rich dividends in menopausal osteoporosis therapy.
TL;DR: Artificial neural network (ANN) and genetic algorithm (GA) were applied to optimize the medium components for the production of actinomycinV from a newly isolated strain of Streptomyces triostinicus which is not reported to produce this class of antibiotics.
Abstract: Artificial neural network (ANN) and genetic algorithm (GA) were applied to optimize the medium components for the production of actinomycinV from a newly isolated strain of Streptomyces triostinicus which is not reported to produce this class of antibiotics. Experiments were conducted using the central composite design (CCD), and the data generated was used to build an artificial neural network model. The concentrations of five medium components (MgSO4, NaCl, glucose, soybean meal and CaCO3) served as inputs to the neural network model, and the antibiotic yield served as outputs of the model. Using the genetic algorithm, the input space of the neural network model was optimized to find out the optimum values for maximum antibiotic yield. Maximum antibiotic yield of 452.0 mg l−1 was obtained at the GA-optimized concentrations of medium components (MgSO4 3.657; NaCl 1.9012; glucose 8.836; soybean meal 20.1976 and CaCO3 13.0842 gl−1). The antibiotic yield obtained by the ANN/GA was 36.7% higher than the yield obtained with the response surface methodology (RSM).
TL;DR: The induction of differential T-helper cell immune response appears ideal to overcome immunosuppression as observed in case of lymphatic, filarial Brugia malayi infection which may also be extended to other infections as well.
TL;DR: 4-aminoquinolines having oxalamide and triazine functionalities in the side chain were synthesized and screened for their antimalarial activities and found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum.
TL;DR: These compounds represent new structure scaffolds that can be further optimized to give new antibacterial agents with structures significantly different from those of existing classes of antibiotics.