• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.143-155
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• 2001

Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-sub-stituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.

• Natural Product Sciences
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• v.17 no.2
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• pp.80-84
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• 2011

Five known compounds, cimigenol (1), 25-O-acetylcimigenol (2), cimigenol 3-O-${\beta}$-D-xylopyranoside (3), ferulic acid methyl ester (4), and visnagin (5), were isolated from Cimicifugae Rhizoma (Ranunculaceae). The chemical structures of these compounds were determined on the basis of spectroscopic analyses including 2D NMR. Compounds 1 - 5 were evaluated for their cytotoxic activity against the HL-60, MCF-7, and A549 cancer cell lines in in vitro. Among them, compounds 4 and 5 showed moderate inhibitory activity against HL-60 cancer cell lines with $IC_{50}$ values of 24.8 and 18.1 ${\mu}M$, respectively.

• Natural Product Sciences
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• v.14 no.1
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• pp.51-55
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• 2008

Three sesquiterpene-lignans, eudeshonokiol B (1), eudesobovatol B (2), and clovanemagnolol (3), were isolated from the stem bark of Magnolia obovata, together with magnolol (4), honokiol (5), and obovatol (6) on the basis of spectroscopic and physicochemical analyses including 2D NMR and Mass. Compounds 1 - 3 were belongs to a unique class of natural products made up of a sesquiterpene and biphenyl-type neolignan via an ether bond. All the isolated compounds were tested in vitro for their cytotoxic activity against the HeLa, A549, and HCTll6 cancer cell lines. Compounds 1 - 6 showed the cytotoxic activity against tested cancer cell lines, with $IC_{50}$ values ranging from 7.1 to 14.4 ${\mu}g/mL$.

• Advances in Traditional Medicine
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• v.6 no.2
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• pp.121-125
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• 2006

The crude ethanol extract of the stem bark of Trewia polycarpa (Family: Euphorbiaceae) was subjected to acetic acid induced writhing inhibition, Brine Shrimp lethality bioassay and 1, 1-diphenyl-2-picryl hydrazyl free radical scavenging assay for screening of analgesic, cytotoxic and antioxidant activity respectively. The extract produced significant (P < 0.001) writhing inhibition in acetic acid induced writhing in mice at the dose of 125, 250 and 500 mg/kg body weight respectively, which were comparable to the standard drug diclofenac sodium. The extract showed significant lethality to Brine Shrimp and the $LC_{50}$ value was $8\;{\mu}g/ml$. The extract showed prominent free radical scavenging activity ($IC_{50}$ about ${\sim}10\;{\mu}g/ml$) compare to standard drug ascorbic acid ($IC_{50}about\;{\sim}15\;{\mu}g/ml$). The results tend to suggest that the crude ethanol extract of the bark might possess analgesic, cytotoxic and antioxidant activities or active constituent(s) responsible for the activities.

• Journal of Oriental Neuropsychiatry
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• v.3 no.1
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• pp.84-90
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• 1992

Solvent and TLC-fractionations of the root of Salvia miltiorrhiza have yielded the results as follows ; Solvent fractions Petr. ether Ether Ethy1 acetate Water Control 100uL 0 0.2 35.1 41.9 43.0 50ul 0.7 3.7 37.2 42.0 TLC-fractionation and the Cytotoxic activity Fractions I II III IV V VI Petr. ehter Control 100uL13.0 7.1 16.8 1.2 30.9 23.2 0.5 48.3 50uL 37.1 26.1 30.0 20.1 45.7 27.2 29.7 Among the solvent fractions the petroleum ehter fraction corresponding to the concentration of 20ug/ml has showed the strongest Cytotoxic activity. (no cell survived) A double dilution of the fraction(10ug/ml) still showed strong activity.(0.2 cells survived) The ether fraction contained strong activity. Of the fraction which have veen obtained by a prcparative silicagel TLC I, II, III & IV were cytotoxic, but V and VI were inactive Howevcr, it is worthwhile to note that no one of these has no strong Cytotoxicity as the pertoleum ether fraction itself. This observation says that the active fractions could be additive or synergic to each other. The most active fraction, IV, was scrached out from the TLC and its UV-spectrum taken. The absorption maxima were 207 and 272 nm, indicating the presence of a flavanone strucuture.

• Natural Product Sciences
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• v.17 no.2
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• pp.100-103
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• 2011

Phytochemical study on the ethanol extract of a Crinum species by bioassay-guided fractionation resulted in the isolation of an active principle, which was determined as parthenin (1) on the basis of physicochemical and spectroscopic analyses. This is the first report on the existence of a sesquiterpenoid from Crinum ensifolium. Compound 1 was found to show strong cytotoxic activity against some cancer cell lines and strongly inhibit NF-${\kappa}$B activity with the $IC_{50}$ value of 1.82 ${\mu}M$.

• Natural Product Sciences
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• v.24 no.2
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• pp.93-98
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• 2018

Medicinal plants are potential sources of anticancer agents screening. A large number of phytochemicals, including triterpenoids, have been reported to have significant cytotoxic effects on cancer cells. From the fruits of Ligustrum japonicum Thunb., thirteen triterpenoids (1 - 13) were isolated and evaluated for their cytotoxic activity against Hela and HL-60 cells. As results, 8 (oleanolic acid) showed significant effects on Hela with $IC_{50}$ values of $5.5{\mu}M$, and moderate effects on HL-60 cells with $IC_{50}$ values of $55.9{\mu}M$. Meanwhile, 10 (oleanderic acid) and 11 ($3{\beta}$-acetoxy-urs-12-en-28-oic acid) exhibited moderate inhibitory effects on Hela with $IC_{50}$ value of 55.0 and $68.8{\mu}M$, respectively. Moreover, 10 showed cytotoxic effect on HL-60 cell line with $IC_{50}$ value of $63.9{\mu}M$. To our knowledge, this is the first report that oleanderic acid was isolated from L. japonicum and investigated in cytotoxic effects on Hela and HL-60 cells.

• Journal of Ginseng Research
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• v.22 no.1
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• pp.60-65
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• 1998

The effect of Korean red-ginseng extract on the proliferation and cellular activity of mouse B and T lymphocytes was examined in vitro. Both water and ethanol extract from red-ginseng increased the growth of normal B and T lymphocytes 1.5∼2.5-folds. Saponin and polysaccharide fractions from ginseng extract also stimulated the proliferation of normal lymphocytes much higher than several well-known immunostimulators. B and T lymphoma cell lines responded to the ginseng extract and fractions by growth, too, while non-lymphoid cell lines did not. Immunoglobulin production of unprimed B-lymphocytes was little affected by the ginseng extract and fractions, though the ethanol extract slightly enhanced Ini, production of B-lymphocytes. When cytolytic activity of T lymphocytes against tumor tells was induced in vitro, both of the saponin and polysaccharide fractions and the ginseng ethanol extract increased the cellular activity of cytotoxic T lymphocytes 4-5-folds, while the ginseng water extract did not. Especially, the saponin fraction exhibited 10-times higher stimulatory effect on the cytolytlc activity of cytotoxic T cells than the ethanol extract and the pclysaccharide fraction did. These results suggest that Korean red-ginseng contain potent immunomodulating components to stimulate the proliferation of B and T lymphocytes and the cellular activity of cytotoxic T lymphocytes.

• Development and Reproduction
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• v.24 no.1
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• pp.53-62
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• 2020

Natural killer (NK) cells are innate lymphocytes that play an essential role in preventing cancer development by performing immune surveillance to eradicate abnormal cells. Since ex vivo expanded NK cells have cytotoxic activity against various cancers, including breast cancers, their clinical potential as immune-oncogenic therapeutics has been widely investigated. Here, we report that the pyrazole chemical XRP44X, an inhibitor of Ras/ERK activation of ELK3, stimulates NK-92MI cells to enhance cytotoxic activity against breast cancer cells. Under XRP44X stimulation, NK cells did not show notable apoptosis or impaired cell cycle progression. We demonstrated that XRP44X enhanced interferon gamma expression in NK-92MI cells. We also elucidated that potentiation of the cytotoxic activity of NK-92MI cells by XRP44X is induced by activation of the c-JUN N-terminal kinase (JNK) signaling pathway. Our data provide insight into the evaluation of XRP44X as an immune stimulant and that XRP44X is a potential candidate compound for the therapeutic development of NK cells.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.4
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• pp.2599-2605
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• 2013

The study aimed to evaluate immune-stimulating effects of a well-known Thai folkloric remedy when used for adjuvant therapy with conventional chemotherapeutics for treatment of breast cancer. Immunostimulating influence of the remedy (215 mg/kg body weight per day) on NK cell activity and TNF-${\alpha}$ release from the monocytes/macrophages were investigated in a total of 15 healthy women and 13 female patients with breast cancer (Group 1). The effect of breast tumor surgery on NK cell activity was further investigated in 18 female patients with breast cancer (Group 2). NK cell cytotoxic activity was determined by chromium release cytotoxic assay using K562, an erythroleukemic cell line. TNF-${\alpha}$ release from monocytes/macrophages separated from blood samples was determined through a biological assay using actinomycin D-treated L929 mouse fibroblast cells in the presence and absence of LPS. Baseline NK cell activity of the monocytes/macrophages separated from Group 2 patients expressed as %cytotoxicity was significantly lower than in the healthy subjects at E:T ratios of 100:1 and 25:1. In healthy subjects, there was no change in NK cell cytotoxic activity (%cytotoxicity or LU) following 1 and 2 weeks of treatment with the remedy compared with the baseline at various E:T ratios but the binding activity (%binding) was significantly increased after 2 weeks of treatment. The addition of one or two conventional chemotherapeutic regimens did not significantly reduce the NK cytotoxic activity but did affect release of TNF-${\alpha}$ in both unstimulated and LPS-stimulated samples. Surgery produced a significant suppressive effect on NK cell activity. The use of the remedy as an adjunct therapy may improve therapeutic efficacy and safety profiles of conventional chemotherapeutic regimens through stimulation of the immune system in cancer patients.