• 한국미생물·생명공학회지
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• 제21권1호
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• pp.59-65
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• 1993

방선균 분리주 GMT 1153로부터 ts/NRK 세포의 형태를 변형된 세포형태에서 정상세포의 형태로 전환하는 활성물질을 분리, 정제하였다. 활성물질 MT 1155는 UV, IR, 1H-NMR, 13C-NMR, mass,원소분석 등의 기기분석을 통하여 항진균성 항암물질인 toyocamycin으로 동정되었다. MT 1155는 ts/NRK 세포의 형태전환에 대한 활성외에도 PKA 효소활성 저해와 CTLL 세포에 대한 세포독성이 있으나 K562 소포형성 억제 및 PKC 효소활성에 대한 저해효과도 없었다.

• 약학회지
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• 제42권5호
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• pp.507-512
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• 1998

In the course of developing novel antitumor intercalating agents. We synthesized 4-carbamoyloxymethyl-l-azaanthraquinones 7-12, incorporating the latent alkylating functi onality. These compounds were designed to explore the effect of substituent on the nitrogen of carbamate. The target compounds were prepared by hetero Diels-Alder reaction as a key step followed by functionalization of benzylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354; liver and MCF7; breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The compounds were less potent than doxorubicin against sensitive cell lines. However, the most active compound 12 was not cross-resistant with doxorubicin against KB-V-1.

• 약학회지
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• 제41권6호
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• pp.718-723
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• 1997

In the course of developing novel antitumor intercalating agents, we synthesized 3- carbamoyloxymethyl-azaanthraquinones 6-12, incorporating the latent alkylating functionality. These compounds were designed to explore the effect of heteroatom incorporation into anthraquinone chromophore and the effect of the incorporation of the latent alkylating functionality. The derivatives were prepared by hetero Diels-Alder reaction as a key step followed by functionality of allylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354: liver and MCF7: breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The derivatives were 10 to 100-fold less potent than doxorubicin against sensitive cell lines. However, they were marginally cross-resistant with doxorubicin against KB-V-1.

• Archives of Pharmacal Research
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• 제29권8호
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• pp.624-626
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• 2006

Four known butenolides were isolated from the ethyl acetate extracts of the culture broth of the marine-derived bacterium, Streptoverticillium luteoverticillatum, by bioassay-guided fractionation. The structures were identified on the basis of spectral data. The absolute configuration of compound (1) was determined by CD spectrum for the first time. Compounds 1-4 showed in vitro cytotoxicity against the murine lymphoma P388 and human leukemia K562 cell lines. This is the first report on the isolation of butenolides from the marine bacterium, Streptoverticillium luteoverticillatum, and their cytotoxic activities.

• 한국자원식물학회지
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• 제5권2호
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• pp.85-93
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• 1992

This experiment was Conducted ta screening for the anti-cancer efficacy from the wild plants which are naturally growing in the Korea. The results are as follows. The results were shown thatZea may L. nad significantly effects on mediculal efficacy anganist anti-tumor by usulg the totalpacked cell volume methods and also, severals plants, such as Sofonum nigrum, Patrinia hispidoBunge, Eragrostis, ferrugenia Beauv, Salaginela pouzolgiana Spring, Platrycarya strobilacea Bunge,Codonopsis lanceolata Benth. et Hook fil. which are collected from Giri and Mooju mountain in Koreaand Nagano in Japan were showed effects on auti-tumor. But the pharmaceologial activities ofPharbitis nil Choisy was believed to strong effec on anti - cancer tumors, while toxicity of its wasshown high that induced te kill all used mice. Extraction of Patrinia hispida Bunge, Pharbitis nilChoisy, Toilis japonica DC, Eragrostis erruginea Beauv. and Forsythia koreana Nakai showed effec-tively supressed on growth rate of cancer tumor by the below 50 percent of T/C ratio at 30mg /mlof extraction from plant. That Is strong activity while Reynouxria japonica Houtt. was observed onlymild activities. The above results many possibly suggest that Patrinia hispido Bunge and Eragrostisferrugina Beauv. inhibited the growth of cancer tumor by the both total packed cell volume methodand cytotoxicity method. Although basic research is still going on, we will find out an accurate moth-od for developing useful medicinal plant to improve pharmacological activites against anti-cancertumor, especialy, in Eragrostis ferruginea Beauv.

• Natural Product Sciences
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• 제8권4호
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• pp.170-172
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• 2002

In continuous efforts for discovery of novel potent antitumor agents from natural products, fifty-seven methanolic extracts derived from indigenous Korean plants were primarily evaluated for in vitro cytotoxic activity in cultured human lung (A549) and colon (Col2) cancer cells. As a result, 16 plant extracts were found to be active against A549 cells and 15 extracts were active against Col2 cells in the criteria of $IC_{50}$<$50\;{\mu}g/ml$. In particular, the extracts of Calystegia soldanella $(IC_{50}$<$8.0\;{\mu}g/ml\;in\;A549;IC_{50}=27.4\;{\mu}g/ml\;in\;Col2)$, Heloniopsis orientalis $(IC_{50}=4.6\;{\mu}g/ml\;in\;A549; IC_{50}=4.5\;{\mu}g/ml\;in\;Col2)$, and Thuja koraiensis $(IC_{50}=1.2\;{\mu}g/ml\;in\;A549;IC_{50}=0.6\;{\mu}g/ml\;in\;Col2)$ showed a potent cytotoxic activity. Further study for the identification of active compounds from these lead extracts might be warranted.

• Archives of Pharmacal Research
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• 제25권4호
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• pp.550-555
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• 2002

The discovery and development of the taxane class of antitumor compounds represent significant advances in the treatment of patients with a variety of malignancies. These drugs are effectively used in the treatment of breast cancer. In this study we evaluated the efficacy of fractionated usage of both paclitaxel and docetaxel as a single agent in the breast cancer cell line MCF-7. It has been shown that the cytotoxic effect of paclitaxel was increased when the divided $IC_{50}$ concentrations were used sequentially and in contrast to paclitaxel, cytotoxic effect of docetaxel was decreased with the same schema and the single dose of $IC_{50}$ concentration was optimal. The cause of the difference between the cytotoxic effects of two agents with this schedule is obscure. Demonstrating mechanisms, which are responsible for these differences, will be important for more rational use of taxoids and to provide basis for the following clinical trials.

• Archives of Pharmacal Research
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• 제27권1호
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• pp.44-47
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• 2004

Loranthus tanakae Fr. et Sav. (Loranthaceae) is a species of mistletoe, a semiparasitic plant growing on the branches of Quercus and Betula species as host trees. In our ongoing search for bioactive compounds from endemic species in Korea, we have investigated to isolate the chemical constituents responsible for the antitumor effect of the MeOH extract of L. tanakae. The ethyl acetate soluble part of the MeOH extract demonstrated a marginal inhibition on the proliferation of the tumor cell lines such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system), and HCT-15 (colon) in vitro. Thus, the activity-guided isolation procedure upon the ethyl acetate soluble part of the extract has been carried out and finally four flavonoid rhamnopyranosides (1-4) were isolated as active principle. The structures of 1-4 were elucidated by the physicochemical and spectral data as rhamnetin 3-O-$\alpha$-L-rhamnoside (1), quercetin 3-O-$\alpha$-L-rhamnoside (2), rhamnocitrin 3-O-$\alpha$rhamnoside (3), and kaempferol 3-O-$\alpha$-L-rhamnoside (4).

• 대한의생명과학회지
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• 제25권2호
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• pp.159-169
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• 2019

Breast cancer stem cells (BCSCs) in breast cancer cells have self-renewal ability and differentiation potential. They are also resistant to drugs after chemotherapy. To overcome this resistance, we designed negatively charged 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol (DMPG)-based liposomes for drug delivery. These liposomes have enhanced the therapeutic effects of a range of antitumor therapies by increasing the cellular uptake and improving drug delivery to targets sites. In this study, we investigated whether DMPG-POPC liposomes, including the neutral lipid 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholin (POPC), can specifically bind to MCF-7 breast cancer cells and increase cellular uptake compared with that by CHOL-POPC liposomes. We also estimated the cytotoxicity of DMPG-POPC liposomes encapsulated with both metformin (Met) and sodium salicylate (Sod) against breast cancer cells and BCSCs compared with that of the free drugs. Our results demonstrated that these dual drug-encapsulated liposomes significantly enhanced the cytotoxic and anti-colony formation abilities compared with individual drug-encapsulated liposomes or free drugs in BCSCs. Overall, our results suggest that DMPG-POPC liposomes containing two drugs (Met + Sod) show promise for synergistic anti-cancer therapy of breast cancer by increasing drug delivery efficiency into breast cancer cells and BCSCs.

• 대한약침학회지
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• 제22권2호
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• pp.55-67
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• 2019

The incidences of cancer are continuously increasing worldwide, affecting life of millions of people. Several factors associated with the internal and external environment are responsible for this deadly disease. The key internal determinants like abnormal hormonal regulation, genetic mutations and external determinants such as lifestyle and occupational factors enhances onset of cancer. From the ancient time, plants were remained as the most trusted source of medicine for the treatment of diverse disease conditions. Extensive studies have been performed for the discovery of effective anticancer agent from the plant and still it is going on. Pentacyclic triterpenoids are biologically active phytochemicals having a different range of activities such as anti-inflammatory, hepatoprotective, anti-hypertensive, antiulcerogenic and anti-tumor. These compounds generally contain ursane, oleanane, lupane and friedelane as a chief skeleton of pentacyclic triterpenoids which are generally present in higher plants. Isoprene unit, phytochemical, with good antitumor/anticancer activity is required for the biosynthesis of pentacyclic triterpenoids. Mechanisms such as cytotoxicity, DNA polymerase inhibition, regulation of apoptosis, change in signal transductions, interfere with angiogenesis and dedifferentiation, antiproliferative activity and metastasis inhibition are might be responsible for their anticancer effect. Present review spotlights diverse targets, mechanisms and pathways of pentacyclic triterpenoids responsible for anticancer effect.