• Natural Product Sciences
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• 제6권2호
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• pp.56-60
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• 2000

We investigated that the extract of Aloe vera L. and its fractions exert antimutagenic activity against Salmonella typhimurium TA98 and TA100, and antileukemic effect against K562 human leukemia cell line. The aqueous ethanolic extract of A. vera L. was revealed to have antimutagenic effect on the AF-2 (2-(2-furyl)-3-(5-nitro-2-furyl)-acrylamide) in Salmonella mutation assay. Among the three fractions (fractions A, B and C) separated by silica gel chromatography, fraction C $(50\;{\mu}g/plate)$ exhibited the greatest antimutagenic effect on the AF-2 with inhibition rate of 84 and 90% in Salmonella typhimurium TA98 and TA100, respectively. The fraction C $(500\;{\mu}g/ml)$ inhibited the growth of K562 human leukemia cell line by 93% in MTT assay. However, the components of A. vera L. did not exhibit cytotoxic effect against MDBK bovine normal kidney in MTT assay.

• BMB Reports
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• 제36권4호
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• pp.387-389
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• 2003

The young developing leaves of willow (Salix safsaf, Salicaceae) trees have antileukemic activity. After a 24-h incubation in vitro, the crude water extracts of the leaves killed a majority of the blasts of acute myeloid leukemia (AML, 73.8%).

• BMB Reports
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• 제44권9호
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• pp.590-594
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• 2011

The production of antileukemic enzyme methionine ${\gamma}$-lyase (MGL) in distinctly related bacteria, Citrobacter freundii and in their recombinants expressing the Vitresocilla hemoglobin (VHb) has been studied. This study concerns the potential of Citrobacter freundii expressing the Vitreoscilla hemoglobin gene (vgb) for the methionine ${\gamma}$- liyase production. Methionine ${\gamma}$- liyase production by Citrobacter freundii and its $vgb^-$ and $vgb^+$ bearing recombinant strain was studied in shake-flasks under 200 rpm agitation, culture medium and $30^{\circ}C$ in a time-course manner. The $vgb^+$ and especially the carbon type had a dramatic effect on methionine ${\gamma}$- liyase production. The $vgb^+$ strain of C. freundii had about 2-fold and 3.1-fold higher levels of MGL than the host and $vgb^-$ strain, respectively.

• 동의생리병리학회지
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• 제19권1호
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• pp.234-241
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• 2005

Galla Rhois is a nest of parasitic bug, Mellaphis chinensis Bell, in Rhus chinensis Mill. Galla Rhois has been used for the therapy of diarrhea, peptic ulcer, hemauria, etc., that showed various antiinflammatory activity, and other biological properties. We studied the effect of Galla Rhois water extract(GRWE). The cytotoxic activity of GRWE in HL-60 cells was increased in a concentration-dependent manner. GRWE was cytotoxic to HL-60 cells, with $IC_50$ of $100{\mu}g/m{\ell}$. Treatment of GRWE to HL-60 cells showed the fragmentation of DNA in a concentration manner, suggesting that these cells underwent apoptosis. In addition, the flow cytometric analysis revealed GRWE concentration-dependently increased apoptotic cells with hypodiploid DNA content and arrested G1 phase of cell cycle. These results indicate that GRWE may have a possibility of potential anticancer activities. Treatment of HL-60 cells with GRWE was induced activation of caspase-3, caspase-8 and proteolytic cleavage of poly(ADP-ribose) polymerase. Also, caspase-3 was directly activated via caspase-8 activation. GRWE also caused the release of cytochrome c from mitochondria into the cytosol. GRWE-induced cytochrome c release was mediated by caspase-8-dependent cleavage of Bid and Bax translocation. These results suggest that caspase-8 mediates caspase-3 activation and cytochrome c release during GRWE-induced apoptosis in HL-60 cells.

• Biomolecules & Therapeutics
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• 제27권5호
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• pp.492-501
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• 2019

Nitrogen-containing heterocycles such as quinoline, quinazolinones and indole are scaffolds of natural products and have broad biological effects. During the last years those structures have been intensively synthesized and modified to yield new synthetic molecules that can specifically inhibit the activity of dysregulated protein kinases in cancer cells. Herein, a series of newly synthesized isoquinolinamine (FX-1 to 8) and isoindoloquinazolinone (FX-9, FX-42, FX-43) compounds were evaluated in regards to their anti-leukemic potential on human B- and T- acute lymphoblastic leukemia (ALL) cells. Several biological effects were observed. B-ALL cells (SEM, RS4;11) were more sensitive against isoquinolinamine compounds than T-ALL cells (Jurkat, CEM). In SEM cells, metabolic activity decreased with $10{\mu}M$ up to 26.7% (FX-3), 25.2% (FX-7) and 14.5% (FX-8). The 3-(p-Tolyl) isoquinolin-1-amine FX-9 was the most effective agent against B- and T-ALL cells with IC50 values ranging from 0.54 to $1.94{\mu}M$. None of the tested compounds displayed hemolysis on erythrocytes or cytotoxicity against healthy leukocytes. Anti-proliferative effect of FX-9 was associated with changes in cell morphology and apoptosis induction. Further, influence of FX-9 on PI3K/AKT, MAPK and JAK/STAT signaling was detected but was heterogeneous. Functional inhibition testing of 58 kinases revealed no specific inhibitory activity among cancer-related kinases. In conclusion, FX-9 displays significant antileukemic activity in B- and T-ALL cells and should be further evaluated in regards to the mechanisms of action. Further compounds of the current series might serve as templates for the design of new compounds and as basic structures for modification approaches.