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Boswellic acids and glucosamine show synergistic effect in preclinical anti-inflammatory study in rats
No full textThe present study revealed the synergistic effect of boswellic acid mixture (BA) and glucosamine for anti-inflammatory and anti-arthritic activities in rats. Two studies were conducted, that is, acute anti-inflammatory by carrageenan edema and chronic
anti-arthritic by Mycobacterium-induced developing arthritis. Five groups of animals were included in each of the study: the vehicle control, positive control (ibuprofen 100 mg/kg), boswellic acids (250 mg/kg), glucosamine (250 mg/kg) and a combination of boswellic acids (125 mg/kg) and glucosamine (125 mg/kg). BA when administered at 250 mg/kg in rats, carrageenan-induced paw edema and Mycobacterium-induced developing arthritis were significantly inhibited. In comparison to boswellic acids, glucosamine when
administered at 250 mg/kg showed a mild effect in carrageenan-induced edema and moderate inhibition of paw swelling against developing arthritis. Although the combination of boswellic acids and glucosamine did not affect the acute inflammation to a greater extent yet a significant anti-arthritic activity was observed in rats. In conclusion, a synergistic effect was observed in chronic inflammatory conditions when two chemical entities were administered in combination in preclinical study
A facile approach towards enantiomerically pure masked β-amino alcohols
No full textb-Amino alcohols are bioactive molecules, used also as catalysts in asymmetric C–C bond formation. While asymmetric synthesis has been the preferred route for their preparation, there was always been a need to develop a facile methodology involving environmentally friendly transformations. Masked amines in the form of phthalimide alcohols, prepared via a fast coupling reaction in an ionic liquid as a reusable reaction media together with reduction and an efficient biocatalytic resolution, offer a green methodology for enantiomerically pure products(ee . 99%, 50 g L21)
A standardized root extract of Withania somnifera and its major constituent withanolide-A elicit humoral and cell-mediated immune responses by up regulation of Th1-dominant polarization in BALB/c mice
No full textThe effects of graded doses of a chemically standardized aqueous alcoholic (1:1) root extract (AGB) of Withania somnifera on the immune system of SRBC immunized BALB/c mice were investigated. Mice were administrated AGB orally for 15 days. AGB stimulated cell mediated immunity, IgM and IgG titers reaching peak value with 30 mg/kg b.wt. Flow cytometric analysis of lymphocyte surface markers of T cells (CD3+,CD4+ and CD8+) and B cells (CD19+) indicated prominent enhancement in proliferation and differentiation of lymphocytes. The extract selectively, induced type 1 immunity because it guided enhanced expression of T helper cells (Th)1 cytokines interferon (IFN)-γ and interleukin
(IL)-2 while Th2 cytokine IL-4 observed a moderate decline. Confirmation of Th1 polarization was obtained from augmented levels of IgG2a over IgG1 in the blood sera of AGB treated groups. Withanolide-A, a major constituent of AGB appeared responsible for Th1 skewing effect of the
extract as it significantly increased the levels of Th1 cytokines, decreased moderately IL-4 and significantly restored the selective dexamethasone inhibition of Th1 cytokines in mouse splenocytes cultures in vitro. In addition, AGB also strongly activated macrophage functions ex vivo and in vitro indicated by enhanced secretion of nitrite, IL-12 and TNF-α. In contrast IL-10 remained unchanged again suggesting that AGB critically
influenced Th1 profile of the cytokines. The studies suggested that AGB supports predominantly Th1 immunity with increase in macrophage functions. The standardized root extract of no toxicological consequences might therefore, find useful applications against the intracellular
pathogens and in the management of immune suppressed diseases
A triterpenediol from Boswellia serrata induces apoptosis through both the intrinsic and extrinsic apoptotic pathways in human leukemia HL-60 cells
No full textA triterpenediol (TPD) comprising of isomeric mixture of 3a, 24-dihydroxyurs-12-ene and 3a, 24-dihydroxyolean-12-ene from Boswellia serrata induces apoptosis in cancer cells. An attempt was made in this study to investigate the mechanism of cell death by TPD in human leukemia HL-60 cells. It inhibited cell proliferation with IC50 ~ 12 lg/ml and produced apoptosis as measured by various biological end points e.g. increased sub-G0 DNA fraction, DNA ladder formation, enhanced AnnexinV-FITC binding of the cells. Further, initial events involved massive reactive oxygen species (ROS) and nitric oxide (NO) formation, which were significantly inhibited by their respective inhibitors. Persistent high levels of NO and ROS caused Bcl-2 cleavage and translocation of Bax to mitochondria, which lead to loss of mitochondrial membrane potential (Dwm) and release of cytochrome c, AIF,Smac/DIABLO to the cytosol. These events were associated with decreased expression of survivin and ICAD with attendant activation of caspases leading to PARP cleavage.Furthermore, TPD up regulated the expression of cell death receptors DR4 and TNF-R1 level, leading to caspase-8 activation. These studies thus demonstrate that TPD produces oxidative stress in cancer cells that triggers selfdemise by ROS and NO regulated activation of both the intrinsic and extrinsic signaling cascades
Cytotoxic and apoptotic activities of novel amino analogues of boswellic acids
No full text4-Amino analogues prepared from b-boswellic acid and 11-keto-b-boswellic acid, wherein the carboxyl group in ursane
nucleus was replaced by an amino function via Curtius reaction, displayed improved cytotoxicity than the parent molecules. The same molecules also exhibited apoptotic activity by inducing DNA fragmentation
Hepatoprotective potential of Aloe barbadensis Mill. against carbon tetrachloride induced hepatotoxicity
No full textAloe barbadensis Mill. Syn. Aloe vera Tourn. ex Linn.(Liliaceae) has been used in variety of diseases in traditional Indian system of medicine in India and its use for hepatic ailments is also documented. In the present study an attempt has been made to validate its hepatoprotective activity. The shade dried aerial parts of Aloe barbadensis were extracted with petroleum ether (AB-1), chloroform (AB-2) and methanol (AB-3).The plant marc was extracted with distilled water (AB-4). All the extracts were evaluated for hepatoprotective activity on limited test models as hexobarbitone sleep time, zoxazolamine paralysis time and marker biochemical parameters. AB-1 and AB-2 were observed to be devoid of
any hepatoprotective activity. Out of two active extracts (AB-3 and AB-4), the most active AB-4 was studied in detail. AB-4 showed significant hepatoprotective activity against CCl4 induced hepatotoxicity as evident by restoration of serum transaminases, alkaline phosphatase, bilirubin and triglycerides. Hepatoprotective potential was confirmed by the restoration of lipid peroxidation, glutathione, glucose-6-phosphatase and microsomal aniline hydroxylase and amidopyrine N-demethylase towards near normal. Histopathology of the liver tissue further supports the biochemical findings confirming the hepatoprotective potential of AB-4. The present study shows that the aqueous extract of Aloe barbadensis is significantly capable of restoring integrity of hepatocytes indicated by improvement in physiological parameters, excretory capacity (BSP
retention) of hepatocytes and also by stimulation of bile flow secretion. AB-4 did not show any sign of toxicity up to oral dose of 2 g/kg in mic
Immunomodulatory effect of bergenin and norbergenin against adjuvant-induced arthritis—A flow cytometric study
No full textBergenin (1), a C-glycoside of 4-O-methyl gallic acid, isolated from rhizomes of Bergenia stracheyi (Saxifragaceae) and its O-demethylated derivative norbergenin (2), prepared from 1, are reported to show anti-arthritic activity through possible modulation of Th1/Th2 cytokine balance.Flow cytometric study showed that the oral administration of 1 and 2 at doses of 5, 10, 20, 40 and 80 mg/kg per oral dose inhibit the production of
proinflammatory Th1 cytokines (IL-2, IFN-� and TNF-�) while as potentiate anti-inflammatory Th2 cytokines (IL-4 and IL-5) in the peripheral blood of adjuvant-induced arthritic balb/c mice. This shows the potential Th1/Th2 cytokine balancing activity of 1 and 2 which is strongly correlated with their anti-arthritic activity. At similar dose levels, the effect of 2 was found to be more than that of 1. The oral LD0 for 1 and 2 was more than 2000 mg/kg body weight of the mice
Anti-arthritic activity of a biopolymeric fraction from Euphorbia tirucalli
No full textThe present study was undertaken to investigate the anti-arthritic activity of a biopolymeric fraction (BET) from plant Euphorbia tirucalli Boiss (Euphorbiaceae). The fraction showed dose dependent anti-arthritic activity and also showed in vivo immunomodulatory capacity being
a major component in inhibiting arthritis. It caused suppression of CD4+ and CD8+ T cells, inhibition of intracellular Interleukin-2 (IL-2) and Interferon-gamma (IFN-�) by flowcytometry. It inhibited vascular permeability and the migration of leucocytes at the site of the insult. The oral LD0 in both rats and mice was more than 2000 mg/kg
Investigations of regio- and stereoselectivities in the synthesis of cytotoxic isoxazolidines through 1,3-dipolar cycloadditions of nitrones to dipolarophiles bearing an allylic oxygen
No full textAbstract—Regio- and stereoselectivities in cycloadditions of nitrones to dipolarophiles bearing an allylic oxygen, which furnishes substituted-isoxazolidine analogs of the furanose ring of nucleosides, have been investigated. Although the obtained regioselectivities are anticipated, a rationalization of the preferred formation of endo-cycloadducts necessitates the involvement of an allylic oxygen in secondary interaction. The obtained isoxazolidines display cytotoxic activities against a number of human cancer cell lines
Effect of acetyl 11-keto β-boswellic acid on metastatic growth factor responsible for angiogenesis
No full textBasic fibroblast growth factor (bFGF), a metastatic growth factor is known to be one of the promoting factors in the tumor induced angiogenesis. The antiangiogenic activity of acetyl 11-keto β-boswellic acid was screened against bFGF-induced angiogenesis using in-vivo Matrigel Plug Assay. Histological & colorimetric examination confirmed that numerous blood vessels were present in Matrigel+bFGF group in comparison to Matrigel alone treated mice. Acetyl 11-keto β-boswellic acids (10 mg/kg/d) inhibited the Matrigel+bFGF-induced angiogenesissignificantly (Pb0.01) in contrast to anti-inflammatory agent indomethacin (10 mg/kg/d) and alkylating agent cyclophosphamide (10 mg/kg/d)