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Studies on cytotoxic, hydroxyl radical scavenging and topoisomerase inhibitory activities of extracts of Tabernaemontana divaricata (L.) R.Br. ex Roem. and Schult
No full textIn the present investigation, the cytotoxic, hydroxyl radical scavenging and topoisomerase inhibition activities of Tabernaemontana divaricata (Apocynaceae) were evaluated. The extracts from leaves of the plant were prepared with different solvents viz. chloroform, methanol, ethyl acetate and hexane. In, invitro cytotoxicity assay, with cell lines viz HCT-15 (Colon), HT-29 (Colon), 502713 (Colon), MCF-7
(Breast), PC- 3 (Prostrate), it was observed that the ethyl acetate extract was effective against only onecolon cell line (502713) at the lowest dose i.e. 10 lg/ml, whereas the chloroform extract was effective against all the three colon cancer cell lines, at 30 lg/ ml. In order to evaluate the mechanism of cytotoxicity of these extracts, they were assessed for their ability to scavenge hydroxyl radicals in plasmid nicking assay with pBR322. It was observed that all the extracts effectively inhibited the unwinding of
supercoiled DNA except hexane extract, which showed the least effect. Since the expression of topo enzymes is linked with cell proliferation so the extracts were also checked for topo I and topo II inhibitory activities. It was noticed that ethyl acetate extract selectively showed inhibition of topo II in topoisomerase II relaxation assay
Enantiomerically pure α-methoxyaryl acetaldehydes as versatile precursors: a facile chemo-enzymatic methodology for their preparation
No full textA facile and efficient synthesis of optically active a-methoxyaryl acetic acids (up to 95% ee), a-methoxyaryl
ethanols (up to 93% ee) and a-methoxyaryl acetonitriles (up to 93% ee) was achieved via Arthrobacter sp. lipase-catalyzed kinetic resolution of masked aldehydes as the key synthons, that is, a-hydroxyaryl
acetaldehyde acetals
Hepatoprotective activity of Woodfordia fruticosa Kurz flowers against carbon tetrachloride induced hepatotoxicity
No full textEthnopharmacological relevance: Dried flowers ofWoodfordia fruticosa Kurz. Family Lythraceae are used in variety of diseases in traditional Indian system of medicine including hepatic ailments.
Aims of study: The aim of present study was to validate hepatoprotective activity of flowers ofWoodfordia
fruticosa Kurz.
Materials and methods: Petroleum ether (WF1), chloroform (WF2), ethyl alcohol (WF3) and aqueous (WF4)extracts of the flowers ofWoodfordia fruticosawere evaluated for hepatoprotective activity against carbon tetrachloride induced hepatotoxicity using biochemical markers, hexobarbitone sleep time, bromosulphalein(BSP) clearance test and effect on bile flow and bile solids.
Results: The aqueous extract (WF4)wasmost potentamongthe four extracts studied in detail.WF4showed significant hepatoprotective activity against carbon tetrachloride induced hepatotoxicity as evident by restoration of serum transaminases, alkaline phosphatase, bilirubin and triglycerides. The restoration of microsomal aniline hydroxylase and amidopyrine-N-demethylase activities indicated the improvement in functional status of endoplasmic reticulum. Restoration of lipid peroxidation and glutathione contents suggests the antioxidant property of WF4. The recovery in bromosulphalein clearance and stimulation of bile flow suggested the improved excretory and secretary capacity of hepatocytes. Light microscopy of
the liver tissue further confirmed the reversal of damage induced by hepatotoxin.
Conclusion: Present study showed that the aqueous extract of Woodfordia fruticosa significantly restores
physiological integrity of hepatocytes. WF4 did not show any sign of toxicity up to oral dose of 2 g/kg in
mice
Induction of Mitochondrial-Dependent Apoptosis by an Essential Oil from Tanacetum gracile
No full textThe essential oil of Tanacetum gracile (Accession
no. AT-01 termed AT-01 in the manuscript), a cold desert alpine highly aromatic herb, has 40 constituents including lavendulol (21.5%), lavendulol acetate (1.7 %), α-pinene (11.2%),1,8-cineole (15.2 %), cis-β-ocimene (6.9 %), borneol (6.1%), limonene (5.1%) and chamazulene (3.7 %). AT-01 was evaluated for its anticancer activity. It inhibited HL-60 cell proliferation with an IC50 of 27 μg/
mL. Furthermore, AT-01 induced apoptosis in human
leukemia HL-60 cells as measured by several biological end points. AT-01 induced apoptotic body formation, enhanced annexinV-FITC binding of the cells, increased sub-G0 DNA fraction, loss of mitochondrial membrane potential (Δψmt) and release of cytochrome c from mitochondria, activated
caspase-9 as well as caspase-3, and increased cleavage of PARP in HL-60 cells. Thus, AT-01 induced apoptosis through the mitochondrial dependant pathway in HL-60 cells
An expedient chemo-enzymatic method for the synthesis of optically active masked 1,2-amino alcohols
No full textThe expedient synthesis of enantiopure masked 1,2-amino alcohols (ee >99%) including their alkyl substituted
analogues has been achieved by the regioselective ring opening of epoxides using phthalimide,followed by highly efficient kinetic resolution under mild and environmentally friendly conditions. The addition of co-solvents during kinetic resolution significantly improved the enantioselectivity with reduction in time
Induction of apoptosis by a synergistic lignand composition from Cedrus deodarain human cancer cells
No full textAP9-cd, a synergistic lignan mixture from Cedrus deodara (Pinaceae) consisting of (−)-wikstromal, (−)-matairesinol
and dibenzyl butyrolactol, depicted cytotoxic effects against numerous human cancer cell lines reported previously.The aim of this study was to investigate the mechanism of cell death in human cancer cells. The viability, morphological and ultrastructural changes in Molt-4 cells were investigated. Using the trypan blue
exclusion assay, we demonstrated that AP9-cd significantly reduced the viability of Molt-4 cells in a time- and
dose-dependent manner. Apoptotic assays using light microscopy revealed that this agent induced Molt-4 cell
apoptosis at varied concentrations. The treatment causes a loss in cell viability by activating the apoptotic
process as identified by light and electron microscopy. The morphological changes of intracellular organelles in Molt-4 cells treated with 30 μg/ml of AP9-cd revealed the disruption of mitochondrial cristae. Other features
included the vacuolization, chromatin condensation and formation of micronuclei. Surface ultrastructural
studies of four different tumor cell lines (Molt-4, HL-60, PC-3 and A-549) treated with AP9-cd depicted loss
of surface projections, condensation and formation of apoptotic bodies. AP9-cd treatment to transgenic fruit
fly, Drosophila, carrying human adenomatous polpyposis coli (hAPC) gene enhanced eye phenotypes and therefore may inhibit Wnt/Wg pathway which is important in the aetiology of a number of human cancers
In vitro cytotoxic potential of Polyalthia longifolia on human cancer cell lines and induction of apoptosis through mitochondrial-dependent pathway in HL-60 cells
No full textPolyalthia longifolia is a lofty evergreen tree found in India and Sri Lanka. We are reporting first time the anticancer potential of P. longifolia leaves extract (A001) and its chloroform fraction (F002). Both inhibited cell proliferation of various human cancer cell lines in which colon cancer cells SW-620 showed maximum inhibition with IC50 value 6.1 �g/ml. Furthermore, F002 induce
apoptosis in human leukemia HL-60 cells as measured by several biological end points. F002 induce apoptotic bodies formation,DNA ladder, enhanced annexin-V-FITC binding of the cells, increased sub-G0 DNA fraction, loss of mitochondrial membrane potential (�Ψmt), release of cytochrome c, activation of caspase-9, caspase-3, and cleavage of poly ADP ribose polymerase (PARP)in HL-60 cells. All the above parameters revealed that F002-induced apoptosis through the mitochondrial-dependent pathway in
HL-60 cells
Lipase enzyme immobilization on synthetic beaded macroporous copolymers for kinetic resolution of chiral drugs intermediates
No full textLipase isolated from Arthrobacter sp. (bacterial strain, MTCC No. 5125) at RRL Jammu, being used for various process development.Arthrobacter sp. lipase (ABL) now has been immobilized on synthetic polymers and reused many a times. In this investigation number of various synthetic macroporous alkylated glycidyl epoxy copolymers with varying hydrophobicity, pore volume and surface area were prepared and used for this study. Among all the polymers prepared and used only two epoxy polymers GMA-EGDM 75-20(I) and GMA-EGDM 75-30(I) with particle size in the range of 150–450 nm, epoxy groups 80 and 70%, tertiary amino groups 20 and 30% was found suitable for immobilization of lipase
(ABL). Dibutyl amine (DBA) incorporation created an internal pore radii 20–50 nm and hydrophobic micro environment in both the polymers for binding the enzyme, which led to improvement in stability and enatioselectivity in racemic resolution process especially by binding to one of the isomers. The optimal ABL binding capacity of polymer GMA-EGDM 75-20(I) was 60 units, 34 mg protein and GMA-EGDM 75-30(I) was 36 units, 21 mg protein/g polymer. The immobilized lipase matrices displayed enhanced pH, thermal, organic solvent and long-term storage stability. Both the immobilized enzyme matrices were tested firstly for the hydrolysis of triglycerides using tributyrin as substrate. After testing,both the matrices were reused for racemic resolution of ethyl-3-hydroxy-3-phenyl propanoate (fluoxetine intermediate, an antidepressant drug) and
racemic chiral auxiliary, acetyl-1-phenyl ethanol (intermediate of many chiral drugs) for 15 cycles. These immobilized lipase matrices have shown very high stability on recycling, high-enantioselectivity, high conversion and faster recovery of product compare to free enzyme, therefore these
matrices may find use in kinetic resolution process developments
Comparative analysis of genetic diversity using molecular and morphometric markers in Andrographis paniculata (Burm. f.) Nees
No full textAndrographis paniculata is a medicinal plant of immense therapeutic value. The present study was aimed to elucidate its genetic diversity based on morphochemical and RAPD
markers from 53 accessions belonging to 5 ecogeographic
regions. Analysis of variance and D2 statistics revealed significant differences in all the metric traits and sufficient inter-cluster distances indicating considerable diversity among the accessions. The complementary approach of RAPD was used to evaluate the genetic dissimilarities
among all the accessions using 6 highly polymorphic primers. The average proportion of polymorphic loci across primers was 96.28%. The molecular genetic diversity based on Shannon index per primer averaged 5.585 with values
ranging from 3.08 to 8.70 indicating towards wide
genetic base. RAPD based UPGMA and D2 cluster analysis also revealed that various accessions available in different eco-geographic regions might have originated from native places of wild abundance. Similarity matrices were generated
for molecular markers and morphometric data to determine the degree of congruence between the two. A highly significant but low correlation(r = 0.547, P < 0.001) was obtained thus implying the correspondence between the two. The species is hermaphroditic and a habitual inbreeder. The
present study yielded a typical triangular congruence
between its breeding system, morphometric traits and RAPD markers thus elucidating the usefulness of complementary approaches to make diversity analysis more explanatory and purposeful for optimum genetic amelioration and effective
conservation of its genotypic variability
An essential oil and its major constituent isointermedeol induce apoptosis by increased expression of mitochondrial cytochrome c and apical death receptors in human leukaemia HL-60 cells
No full textAn essential oil from a lemon grass variety of Cymbopogon flexuosus (CFO) and its major chemical constituent sesquiterpene isointermedeol (ISO) were investigated for their ability to induce apoptosis in human leukaemia HL-60 cells because dysregulation of apoptosis is the hallmark of cancer cells. CFO and ISO inhibited cell proliferation with 48 h IC50 of∼30 and 20 �g/ml, respectively.Both induced concentration dependent strong and early apoptosis as measured by various end-points, e.g. annexinV binding, DNA
laddering, apoptotic bodies formation and an increase in hypo diploid sub-G0 DNA content during the early 6 h period of study.This could be because of early surge in ROS formation with concurrent loss of mitochondrial membrane potential observed. Both CFO and ISO activated apical death receptors TNFR1, DR4 and caspase-8 activity. Simultaneously, both increased the expression of mitochondrial cytochrome c protein with its concomitant release to cytosol leading to caspase-9 activation, suggesting thereby the involvement of both the intrinsic and extrinsic pathways of apoptosis. Further, Bax translocation, and decrease in nuclear NF- �B expression predict multi-target effects of the essential oil and ISO while both appeared to follow similar signaling apoptosis
pathways. The easy and abundant availability of the oil combined with its suggested mechanism of cytotoxicity make CFO highly useful in the development of anti-cancer therapeutics