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Volatile (As and Hg) and non-volatile (Pb and Cd) toxic heavy metals analysis in rhizome of Zingiber officinale collected from different locations of North Western Himalayas by Atomic Absorption Spectroscopy
No full textGinger is an important ingredient of spice and herbals. The monitoring of toxic heavy metals in the rhizome of ginger is important for protecting public health against the hazards of metal toxicity. The concentration of volatile and non-volatile metals (As, Hg, Pb and Cd), in the soil and rhizome of Zingiber officinale were analyzed using AAS. Soil analysis profile showed uniformity in the metal contents, in active root zone and subsoil, except mercury, which was present in higher quantity in one, out of the four sectors,of the field. The infield metal content in the soil in increasing order was, cadmium < arsenic < lead <
mercury. In ginger rhizome the volatile toxic heavy metals arsenic (As) and mercury (Hg) varied from not detected to 0.13 lg/g and 0.01 to 0.42 lg/g, respectively. The non-volatile metals lead (Pb) and cadmium(Cd) ranged from 0.06 to 0.64 lg/g and 0.002 to 0.03 lg/g, respectively. The results illustrated the findings that soil is the major but not the only source of metal accumulation in the plants. In our study, the volatile metal content (As, Hg) was found more in rhizomes collected from Himachal Pradesh while the non-volatile metals were predominant in samples from Uttarakhand
Anti-tubercular agents. Part 5: Synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners
No full textIn an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine
1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and in vivo study of recently reported potent molecule 4 (MIC ¼ 1 mg/mL) is also discussed
Bio-transformation of artemisinin using soil microbe: Direct C-acetoxylation of artemisinin at C-9 by Penicillium simplissimum
No full textPotent antimalarial compound artemisinin, 1 was bio-transformed to C-9 acetoxy artemisinin, 2 using
soil microbe Penicillium simplissimum along with C-9 hydroxy derivative 3. The products were characterized using high field NMR and MS–MS data. The absolute stereochemistry of the newly generated chiral centers has been ascertained by COSY and 1D NOESY experiments. This is the first Letter of direct C-acetoxylation of artemisinin using microbial strains
6-Nitro-2-(3-hydroxypropyl)-1H-benz[de]isoquinoline-1,3-dione, a potent antitumor agent, induces cell cycle arrest and apoptosis
Full text linkBackground: Anticancer activities of several substituted naphthalimides (1H-benz[de]isoquinoline-1,3-diones) are
well documented. Some of them have undergone Phase I-II clinical trials. Presently a series of ten N-(hydroxyalkyl)
naphthalimides (compounds 1a-j) were evaluated as antitumor agents.
Methods: Compounds 1a-j were initially screened in MOLT-4, HL-60 and U-937 human tumor cell lines and results
were compared with established clinical drugs. Cytotoxicities of compounds 1d and 1i were further evaluated in a battery of human tumor cell lines and in normal human peripheral blood mononuclear cells. Cell cycle analysis of compound 1i treated MOLT-4 cells was studied by flow cytometry. Its apoptosis inducing effect was carried out in MOLT-4 and HL-60 cells by flow cytometry using annexin V-FITC/PI double staining method. The activities of
caspase-3 and caspase-6 in MOLT-4 cells following incubation with compound 1i were measured at different time
intervals. Morphology of the MOLT-4 cells after treatment with 1i was examined under light microscope and transmission electron microscope. 3H-Thymidine and 3H-uridine incorporation in S-180 cells in vitro following
treatment with 8 μM concentration of compounds 1d and 1i were studied.
Results: 6-Nitro-2-(3-hydroxypropyl)-1H-benz[de]isoquinoline-1,3-dione (compound 1i), has exhibited maximum
activity as it induced significant cytotoxicity in 8 out of 13 cell lines employed. Interestingly it did not show any
cytotoxicity against human PBMC (IC50 value 273 μM). Cell cycle analysis of compound 1i treated MOLT-4 cells demonstrated rise in sub-G1 fraction and concomitant accumulation of cells in S and G2/M phases, indicating upregulation of apoptosis along with mitotic arrest and/or delay in exit of daughter cells from mitotic cycle
respectively. Its apoptosis inducing effect was confirmed in flow cytometric study in MOLT-4 and the action was
mediated by activation of both caspase 3 and 6. Light and transmission electron microscopic studies corroborated
its apoptosis inducing efficacy at a concentration of 10 μM in MOLT-4 cells. Its apoptosis induction was also observed in HL-60 cells to an extent much greater than well known apoptosis inducing agents as camptothecin and cis-platin at 10 μM concentration each. It significantly inhibited DNA and RNA synthesis in S-180.
Conclusions: In essence, compound 1i showed potential as an antitumor agent
Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine derivatives
No full textHeterocyclic amidine derivatives have been synthesized by condensation of 2-cyanopyrazine, 4-cyanopyridine
and 2-cyanopyridine with furfurylamine, histamine, 1-(3-aminopropyl)imidazole, 4-picolylamine, 2-picolylamine, and tryptamine respectively, in the presence of sodium methoxide as well as via microwave irradiation in good yields. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50 mg/kg p.o. compounds 3a (36.6%), 3d (32%), 4d (31.0%) and 4e(33.8%) exhibited good anti-inflammatory activity, comparable to standard drug ibuprofen which showed
39% activity at 50 mg/kg p.o
Simultaneous determination of etoposide and a piperine analogue (PA-1) by UPLC 13qTOF-MS: Evidence that PA-1 enhances the oral bioavailability of etoposide in mice
No full textIn the present investigation, a UPLC-qTOF-MS/MS method has been developed for the simultaneous determination of etoposide and a piperine analogue, namely, 4-ethyl 5-(3,4-methylenedioxyphenyl)-2E,4E-pentadienoic acid piperidide (PA-1). The analytes were separated on a reverse phase C18 column using methanol-water (72:28, v/v) mobile phase with a flow rate of 250 microL/min. The qTOF-MS was operated under multiple reaction monitoring mode using electro-spray ionization (ESI) technique with positive ion polarity. The major product ions for etoposide and PA-1 were at m/z 185.1350 and 164.1581, respectively. The recovery of the analytes from mouse plasma was optimized using solid phase extraction technique. The total run time was 6 min and the elution of etoposide and PA-1 occurred at 1.24 and 2.84 min, respectively. The calibration curves of etoposide as well as PA-1 were linear over the concentration range of 2-1000 ng/mL (r(2), 0.9829), and 1-1000 ng/mL (r(2), 0.9989), respectively. For etoposide intra-assay and inter-assay accuracy in terms of % bias was in between -7.65 to +6.26, and -7.83 to +5.99, respectively. For PA-1 intra-assay and inter-assay accuracy in terms of % bias was in between -7.01 to +9.10, and -7.36 to +6.71, respectively. The lower limit of quantitation for etoposide and PA-1 were 2.0 and 1.0 ng/mL, respectively. Analytes were stable under various conditions (in autosampler, during freeze-thaw, at room temperature, and under deep-freeze conditions). The method was used for a pharmacokinetic study which showed that PA-1 enhanced the oral bioavailability of etoposide in mice by 2.32-fold
Development of novel lipidated analogs of picroside as vaccine adjuvants: Acylated analogs of picroside-II elicit strong Th1 and Th2 response to ovalbumin in mice
No full textThe acylated analogs of picroside-II were synthesized and tested for immune-adjuvant activity in the presence of weak antigen ovalbumin found to stimulate anti-OVA IgG titer, neutralizing antibody (IgG1 and IgG2a) titer as well as the production of soluble mediators of a Th1 response (IL-2 and IFN-�) and Th2 response (IL-4) and proliferation of T lymphocytes sub-sets (CD4/CD8). Furthermore, these modified
analogs of picroside-II were able to elicit a substantial increase in anti-OVA IgG when compared with OVA alone. These results support the use of acylated analogs particularly PK-II-3 and PK-II-4 as potent enhancer of antigen-specific Th1 and Th2 immune responses and thus are promising immune-adjuvant
candidate for vaccines
Selective Th1 upregulation by ethyl acetate fraction of Labisia pumila
No full textAim of the study: Labisia pumila has rejuvenating properties that help women to regain the strength and
vigour after giving birth (Burkill, 1935) leading us to speculate that Labisia pumila might also modulate the immune matrix as it is one of the important aspect of healthy state of the living body.
Materials and methods: Studies were carried out for the evaluation of pro-inflammatory cytokines in murine neutrophils followed by expression of T cell-surface markers and corresponding intracellular expression of cytokines related to T helper1 (Th1) and T helper 2 (Th2) activity.
Results: The ethyl acetate fraction (A001/3b) obtained from ethanolic extract of leaves of Labisia pumila at graded doses (in vitro) showed increased expression of TNF-�, IL-6 and IL-12. IL-12 is a strong inducer of Th1 response in activated CD4+ T cells and accordingly T cell studies were carried out (in vivo). These specific studies showed A001/3b to cause marked stimulation of CD4+ T helper cells and related cytokine expression like IL-2 and IFN-gamma (a potent Th1 inducer), thereby, having a predominant Th1 upregulation pathway. This was further validated by suppression of IL-4 and IL-10 expression which are the
Th2 pathway cytokines.
Conclusion: This study showed ethyl acetate fraction (A001/3b) of Labisia pumila to have Th1 upregulating
activity and suggests its possible usefulness as a therapeutic agent in immune compromised patients
Stimulatory effects of Cuminum cyminum and flavonoid glycoside on Cyclosporine-A and restraint stress induced immune-suppression in Swiss albino mice
No full textMany herbs and spices are known to modulate the immune system and have been shown to restore the immunity in immuno-compromised individuals. Spices generally used to increase the taste and flavor of food also has the history of usage as an ayurvedic medicine. Therefore to explore the health modulating effects of Cuminum cyminum and to identify the active compound, immunomodulatory properties were evaluated using flowcytometry and ELISA in normal and immune-suppressed animals. C. cyminum and compound 1 stimulated the T cells and Th1 cytokines expression in normal animals. Swiss albino mice subjected to Cyclosporine-A induced immune-suppression were dosed orally with C.cyminum(25, 50, 100 and 200 mg/kg)onconsecutive days. The resultsshowedthat administration significantly increased T cells(CD4 and CD8) count and Th1 predominant immune response in a dose dependent manner thereby suggesting immunomodulatory activity through modulation of T lymphocytes expression. In restraint stress induced immune-suppressed animals, compound 1 countered the depleted T lymphocytes, decreased the elevated corticosterone levels and size of adrenal glands and increased the weight of thymus and spleen.Based on the data we may conclude that C. cyminum is a potent immunomodulator and may develop as a lead to recover the immunity of immuno-compromised individuals
Synthesis and biological screening of 4-(3,3-dimethylspiro{bicyclo[2.2.1]heptan-2,5′-isoxazoline-2}- 3′-yl)-2-aryl-2,3-dihydro-1H-1,5-benzodiazepines
No full textA series of novel 4-(3,3-dimethylspiro{bicyclo[2.2.1]heptan-2,50-isoxazoline-2}-30-yl)-2-phenyl-2,3-dihydro-1H-1,5-benzodiazepines were synthesized. These molecules were screened in vitro for their antifungal and antibacterial activity, and none of the tested compounds showed promising antimicrobial or antifungal activity