Background: This study has mainly focused on finding pharmacological effects of ginsenosides that can reduce the unwanted side effects of the cytotoxic anticancer drugs and are highly effective on prostate cancer, colorectal cancer, liver cancer, hormone-dependent breast cancer, triple-negative breast cancer, and brain cancer (neuroblastoma). Methods: Minor and rare ginsenosides (GS) of Rh2 which have a high absorption ability and excellent pharmacological actions were treated with the 6 different types of cancer cell lines and their anticancer activities were investigated by analyzing gene expressions associated with various cancers through qPCR and other relevant methods. Results: In cancer cells exposed to Rh2, cell viability and cell migration were reduced, and apoptosis was induced. Each cancer cell was divided into three groups according to the cell proliferation response by Rh2; 1) A group in which the cell viability decreases inversely to an increase in Rh2 treatment concentration; 2) A group in which the cell viability rapidly decreases in Rh2 treatment above a certain level of concentration; 3) A group in which the cell viability was not suppressed below 20-30% even with 100 μL of Rh2, the highest concentration used in this study. Conclusions: It was shown that Rh2 has a significant effect on inhibiting the proliferation of prostate cancer cells and hormone-dependent breast cancer cells.

In this study, the quality characteristics of kimchi, such as its salinity, pH, and acidity, were measured and compared, and the HT-29 human colon cancer cells were used to show the anticancer effects of kimchi. The kimchi samples used herein included standard kimchi (SK), turnip kimchi (TK), and turnip-powder-added kimchi (TPK). The measured pH and acidity of TK and TPK showed no significant differences with those of SK. Compared to SK and TK, TPK had higher DPPH scavenging activity and higher total flavonoid content, confirming its antioxidant activity. The cancer cell growth inhibition rates of TK and TPK were significantly higher than that of SK. In HT-29 cells treated with TPK, the mRNA expression of Bcl-xL, an anti-apoptosis-related gene, was lower, and the mRNA expressions of the apoptosis-related genes Bax, Bad, and caspase-9 were higher. TPK showed significantly higher levels of mRNA expressions for the cell-cycle-related genes p53 and p21 than the other samples, in addition to suppression effects on cancer cell proliferation. Compared to SK, TK and TPK suppressed the growth of colon cancer cells and showed higher anticancer effects. Therefore, it is shown that kimchi with added turnip powder had high anticancer effects.

This study was carried out to investigate anticancer activities fruiting body extracts and fractions of Cordyceps militaris. Fruiting body of this mushroom was extracted using by 80% MeOH. Fractionations of these extracts were performed by n-hexane, methylene chloride, ethyl acetate, n-BuOH. AGS(human gastric cancer line) was cultured in media conditions (10% FBS, 1% Penicillin-Streptomycin in RPMI). Anticancer activities of each fractions of Cordyceps militaris were examined by using MTT, Cell titer Glo.

This study is focused on the synthesis of urea and amide derivatives particularly, since the amide moiety is an essential binding group at the binding site. Urea derivatives 3-7 and 13-14 were obtained by reaction of 2-aminopyrimidines and other amines with diverse isocyanates in pyridine as a solvent under reflux. The urea derivatives were obtained in low yield because of the highly electron deficient nature of the amino group of the 2-aminopyrimidine. Amide derivatives 8-10 were obtained in moderate yields by reaction of compound 1 with aryl chloride derivatives. Also, arylamine 11 was synthesized by Buchwald-Hartwig amination in moderate yields. Most of the compound did not show good activity against A375P melanoma cells, compared with Sorafenib as control compound.

In this study, we investigated the effect of the extracts from Vaccinium oldhamii on cell proliferation and the regulatory mechanisms of cyclin D1 protein level in human cancer cells. The branch extracts from Vaccinium oldhamii (VOB) showed higher inhibitor effect against the cell growth than leave extracts (VOL) and fruit extracts (VOF) in human colorectal cancer, breast cancer, prostate cancer, non-small lung cancer, pancreatic cancer and liver cancer cells. In addition, VOB decreased cyclin D1 level at both protein and mRNA level. MG132 treatment attenuated VOB-mediated cyclin D1 downregulation. A point mutation of threonine-286 to alanine attenuated cyclin D1 degradation by VOB. In addition, the inhibition of nuclear export by leptomycin B (LMB) attenuated cyclin D1 degradation by VOB. But, the treatment of PD98059 (ERK1/2 inhibitor), SB203580 (p38 inhibitor), SP600125 (JNK inhibitor), LiCl (GSK3β inhibitor), LY294002 (PI3K inhibitor) or BAY 11-7082 (IκK inhibitor) did not affect VOB-induced cyclin D1 degradation. In conclusion, VOB induced cyclin D1 degradation through redistribution of cyclin D1 from the nucleus to cytoplasm via T286 phosphorylation of cyclin D1, which resulted in the inhibition of cancer cell proliferation.

The seed of safflower (Carthamus tinctorius L) has been reported to suppress human cancer cell proliferation. However, the mechanisms by which safflower seed inhibits cancer cell proliferation have remained nuclear. In this study, the inhibitory effect of the safflower seed (SS) on the proliferation of human colorectal cancer cells and the potential mechanism of action were examined. SS inhibited markedly the proliferation of human colorectal cancer cells (HCT116, SW480, LoVo and HT-29). In addition, SS suppressed the proliferation of human breast cancer cells (MDA-MB-231 and MCF-7). SS treatment decreased cyclin D1 protein level in human colorectal cancer cells and breast cancer cells. But, SS-mediated downregulated mRNA level of cyclin D1 was not observed. Inhibition of proteasomal degradation by MG132 attenuated cyclin D1 downregulation by SS and the half-life of cyclin D1 was decreased in SS-treated cells. In addition, SS increased cyclin D1 phosphorylation at threonine-286 and a point mutation of threonine-286 to alanine attenuated SS-mediated cyclin D1 degradation. Inhibition of ERK1/2 by PD98059 suppressed cyclin D1 phosphorylation and downregulation of cyclin D1 by SS. In conclusion, SS has anti-proliferative activity by inducing cyclin D1 proteasomal degradation through ERK1/2-dependent threonine-286 phosphorylation of cyclin D1. These findings suggest that possibly its extract could be used for treating colorectal cancer.

본 연구에서는 척리 즉 물이끼를 이용한 고부가가치 기능성 소재를 개발하기 위하여 물이끼의 Ethanol 추출물을 이용한 항암활성과 식물화학적 성분연구를 수행 하였다. 3종의 암세포주(A549, HeLa, SK-OV-3)에 대하여 세포독성연구를 수행해 본 결과 폐암세포주인 A549에서 유의성 있는 결과를 보였다. 이 결과는 난치성 질환인 암을 치료하려는 목적 의약품 보다는 Chemopreventive agent로서의 예방 의학적 기능성 소재로 충분한 가치가 있음이 사료 되어지기에 식물화학적 성분연구를 실시하여 7종의 화합물(Comp.1 : Coumarin, Comp.2 : Caffeic acid, Comp.3 : Quercetin, Comp.4 : Astragalin, Comp.5 : Luteolin, Comp.6 : Chlorogenic acid, Comp.7 : Rutin) 를 분리하여 구조동정 하였다.

We investigated a method to improve anticancer activities of Acer mono wood extracts by ultra high pressure extraction process. The A. mono was extracted by water at 40℃ and 300 MPa for 15 min (High Pressure Extraction, HPE). The extraction yield by ultra high pressure extraction process was 5.42%. The cytotoxicity on human normal lung cell (HEL299) of the extracts from HPE showed 21.54% lower than that from conventional water extraction at 100℃ in adding the maximum concentration of 1.0 mg/ml. Ultra high pressure extracts process for 15 minutes extracts (HPE15) showed more potent scavenging effect than the control, BHA. On SOD-like test, the HPE15 showed highest activity as 32.4% at 1.0 mg/ml concentration. Human stomach adenocarcinoma, liver adenocarcinoma, breast adenocarcinoma and lung adenocarcinoma cell growth were inhibited up to about 67~79%, in adding 1.0 mg/ml of extracts from HPE. HPE was 20~25% higher than conventional water extraction. It was interesting that, among several cancer cell lines (stomach adenocarcinoma, liver adenocarcinoma), the growth of digestive related cancer cells were most effectively inhibited as about 75~79%. On in vivo experiment using ICR mice, the variation of body weight of mice group treated A. mono wood extracts from HPE of 100 mg/kg/day concentration was very lower than control and other group. The survival times of group treated this extracts was 61.96% longer than that of the control group and this extracts showed the lower tumor weight, which were 10.49 g than positive control as 16.17 g. Based on these results, we could tell that the HPE wood extracts of A. mono had higher anticancer activity than conventional water extraction. The results of HPE showed obvious advantages in higher efficiency, shorter extraction time, at lower energy costs.

The potential antioxidant and anticancer activities of Hexane, EtOAc (Ethyl acetate), BuOH (n-Buthanol) and water fractions from methanolic (MeOH) extract of Picrasma quassioides (D. Don) Benn. were evaluated in vitro. Tested fractions showed strong antioxidant activity, especially EtOAc fraction had the highest activity (IC50 = 114.01 μg/mL), containing high total phenolics and total flavonoids contents, showed 67.59 Tan μg/mg and 64.95 Que μg/mg respectively. Anticancer activity of these fractions was tested by MTT assay on HT-29 (the human colon carcinoma cells) cell line. BuOH fraction not only showed very high anticancer activity, but also had no cytotoxic effect on 293 (the human normal kidney cells) cell line. Considering these results, we used BuOH fraction of MeOH crude extract from P. quassioides (D.Don) Benn. to do assessment of apoptosis by flow cytometry and the mRNA expression levels of widely established apoptotic-related genes on HT-29 cell line. All the experiments showed that BuOH fraction can induce apoptosis on HT-29 cell line strongly. Taken together, methanolic extract of P. quassioides has potential for antioxidant and anticancer activities products.

Tocotrienol의 건강식품 및 의료용 가공품으로의 고부가가치화 가능성을 평가하기 위하여 미강에서 추출한 tocotrienol의 항암 효과 및 독성평가를 실시하였다. HepG2 간암 세포를 대상으로 한 항암효과 분석 결과 tocotrienol이 간암세포의 증식을 억제함을 입증할 수 있었다. 또한 랫드를 이용한 경구독성 검사를 수행한 결과 tocotrienol 최종 생산물은 경구투여 한계량인 2,000mgkg1 수준에서도 사망률, 일반 증상, 체중 변화 등에 이상을 보이지 않았으며, 부검 후 흉강 및 복강의 모든 장기에 대한 육안적 부검 소견 등에서도 아무런 독성학적 변화가 유발되지 않음을 알 수 있었다.

양파고추장에 대한 항암 및 면역활성을 조사한 결과는 다음과 같다. 고추장 메탄을 추출물은 aflatoxin 으로 돌연변이를 유도한 Salmonella typhimurium에 대하여 농도 의존적으로 항돌연변이 효과가 큰 것으로 나타났으며, 양파를 첨가하지 않은 대조구 고추장보다 양파고추장이 그 효과가 더욱 크게 나타났다. 양파고추장 메탄올추출물은 A549 및 MCF-7 암세포주에 처리한 결과 대조구에 비하여 농도에서 모두 이상 그 성장을 억제하였

Allergen-removed-extract was produced from Rush verniciflua by two phase methods. Phase one was high temperature treatment of Rush verniciflua tree to get allergen-removed-extract. Phase two was extraction of solution from phase one product using water or organic solvents. The solutions from above method show high antioxidant activity, anticancer activity, and improvement in lung function, but did not contain urushiol family compounds.

Ethanol and butanol fractionation of E. senticosus showed strong anti-oxidant activity, and methanol and water extracts also had high anti-oxidant activity. The anti-oxidant activities in ethanol and butanol fractionation were higher than or similar to those of α-tocopherol. The cytotoxic effect of root extract of E. senticosus was evaluated on seven different human cancer cell lines, The extracts of leaf and stem of E. senticosus also had strong antioxidant activity, but the antioxidant activity in root extract was higher than those in leaf and stem extracts. Methanol, hexane, and aqueous fraction layer had much higher inhibitory activities on lipid peroxidation in rat liver microsomes compared with α-tocopherol. The effect of root extract of E. senticosus was evaluated on six human cancer cell lines. The values of 50% growth inhibition (GI50) for the extracts were mostly below 30μg/ml, and the extracts are considered as active inhibitory compounds on cancer cells.