• Archives of Pharmacal Research
• /
• 제29권1호
• /
• pp.16-25
• /
• 2006

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.

• 한국식품영양과학회지
• /
• 제28권6호
• /
• pp.1321-1325
• /
• 1999

The inhibitory effect of Ramaria botrytis on the mutagenicity in Salmonella assay and cytotoxicity on cancer cell were studied. Ramaria botrytis methanol extracts showed antimutagenic effects of 60~90% on B(a)P and AFB1 in S. typhimurium TA98 and TA100. These extracts showed 73~85% antimutagenicity on TA100 against MNNG. The methanol extracts with strong antimutagenic activities were further fractionated by ethylacetate and water, the ethylacetate fraction were found to be stronger antimutagen icity against MNNG than water fraction. Ramaria botrytis methanol extracts and ethylacetate fraction revealed the highest cytoxicity against HT 29 human colon adenocarcinoma cells in which cell growth was inhibited by 57~88% and 69~94% at 0.25~1.0mg/ml, respectively. These methanol extract and ethyl acetate fraction exhibited 53~79% and 66~87% inhibition against HepG2 human hepatocarcinoma cells, respectively. But water fraction showed only 10~24% inhibition. However, these extract and fractions did not show cytotoxic effect against human chang liver cells. From these results, it is considered that Ramaria botrytis has stronger antimutagenic and anticancer effects in vitro.

• Journal of Nutrition and Health
• /
• 제31권4호
• /
• pp.739-746
• /
• 1998

This study was designed to investigated the antitumor effect and change chemosensitivity of chitosan in 2 kinds of humen lung cancer cell lines(NCI-H522, NCI-H596). To evaluate the antitumor effect and synergistic effectof chomosensitivity, MTT assay was used in vitro. then anticancer drugs used were 챤-platin , ectoposide, and adrimycin. The results of this study were as follows; Chitosan shwoed in antitumor effect on both NCI-H522 and NCI-H596. The lung cancer viability percent for NCI-H522 and NCL-H596 showed at the lowest levels of 5.31 and 5.33% when the concentration of chitosan was 25mg/$m\ell$ media and the exposure time of chitosan was 72 hours. ID50 value of chitosan on both NCI-H522 and NCI-H596 showed at the lowest levels of 14.07, 11.68 mg/$m\ell$ media when the exposure time of chitosan was 72 hours. the synergistic effect of chomosensitivity was better in NCI-H596 than in NCI0H522 . When the synergistic effect of chomosensitivity was shown according to the kind of the anticancer drugs, in case of NCI-H522 , in the concentration of 100$\mu\textrm{g}$/$m\ell$, ectoposide showed the highest synergistic effect of chomosensitivity and then was adrimycin In case of NCI-H596, in the concentration of 100$\mu\textrm{g}$/$m\ell$,, the order of the synergistic effect of chomosensitivity was ectoposide>adrimycin>cis-platin and in the concentration of 10$\mu\textrm{g}$/$m\ell$, ectoposide>cis-platin >adrimycin. It is concluded that chitosan is an active antitumor agent and is increased chomosensitivity though there is difference according to the kind and the concentration of anticancer drugs. But to be sued to lung cancer theraphy, further studies on toxicity, the mechanism of action, animal experiment are wanted.

• Journal of Ginseng Research
• /
• 제40권1호
• /
• pp.62-67
• /
• 2016

Background: Ginseng, which is widely used in functional foods and as an herbal medicine, has been reported to reduce the proliferation of prostate cancer cells by mechanisms that are not yet fully understood. Methods: This study was designed to investigate the changes in ginsenoside content in ginseng after treatment with a microwave-irradiation thermal process and to verify the anticancer effects of the extracts. To confirm the anticancer effect of microwave-irradiated processed ginseng (MG), it was tested in three human prostate cancer cell lines (DU145, LNCaP, and PC-3 cells). Involvements of apoptosis and autophagy were assessed using Western blotting. Results: After microwave treatment, the content of ginsenosides Rg1, Re, Rb1, Rc, Rb2, and Rd in the extracts decreased, whereas the content of ginsenosides 20(S)-Rg3, 20(R)-Rg3, Rk1, and Rg5 increased. Antiproliferation results for the human cancer cell lines treated with ginseng extracts indicate that PC-3 cells treated with MG showed the highest activity with an half maximal inhibitory concentration of $48{\mu}g/mL$. We also showed that MG suppresses the growth of human prostate cancer cell xenografts in athymic nude mice as an in vivo model. This growth suppression by MG is associated with the inductions of cell death and autophagy. Conclusion: Therefore, heat processing by microwave irradiation is a useful method to enhance the anticancer effect of ginseng by increasing the content of ginsenosides Rg3, Rg5, and Rk1.

• 한국식품영양과학회지
• /
• 제41권9호
• /
• pp.1248-1252
• /
• 2012

칼륨을 첨가하여 제조한 죽염의 항암효과를 일반죽염 및 천일염, 정제염과 비교하여 칼륨 첨가의 영향을 알아보고자 하였다. DPPH radical 소거능을 측정한 결과, 칼륨죽염과 죽염의 radical 소거능이 높았고, 칼륨죽염의 소거능이 가장 높게 나타났다. 정제염과 천일염의 소거능은 상대적으로 낮았고 칼륨죽염과 20배 이상의 차이가 있었다. MNNG를 사용한 Salmonella Typhimurium TA100 돌연변이 실험결과 소금은 모두 보돌연변이 효과가 있었지만, 칼륨죽염의 보돌연변이 효과가 다른 소금보다 3~46% 낮게 나타났다. HCT-116 암세포에 성장 억제 효과에 있어서도 위와 비슷한 경향을 나타내었는데, 칼륨죽염과 일반죽염의 암세포 성장억제효과와 암세포의 apoptosis 유도 효과가 천일염 및 정제염에 비해 높았고 그중 칼륨죽염의 in vitro 항암 기능성이 가장 우수하였다. 이상의 결과로부터 죽염의 항암효과는 천일염이 정제염보다 좋으며, 이러한 죽염의 항암효과를 칼륨을 첨가함으로써 더욱 증진될 수 있는 것으로 나타났다. 본 연구에서 죽염의 항암 기능성이 증가한 주요 원인은 칼륨이라고 생각되어지며, 이것이 죽염으로 제조될 때 그 효과가 더 증진되는 것으로 보인다.

• 한국식품영양과학회지
• /
• 제30권4호
• /
• pp.732-738
• /
• 2001

두충잎에서 인간대장암에세포 HCT-116에 세포증식 억제효과를 나타내는 성분을 silica gel column chromatography TLC로 분리하고 HPLC로 정제한 다음 UV-visual spectro-photometer에 의한 흡수 spectra 특성 HPLC에 의한 retention time과 분리패턴 및 FAB/MS로 분자량을 잠정적으로 동정한 결과 TLC 상에서 분리된 Rf 0.19 band 의 화합물은 chlorophyll a에서 $Mg^{2+}$이 제거된 pheophytin a로 Rf 0.25 band의 화합물은 pyropheophytin a로 확인되었다. 동정된 화합물들의 암세포 억제작용을 확인하기 위해 두충잎의 petroleum ether extract column chromatography로 분리한 분획물 및 TLC에서 분리된 각 band들의 cytotoxic activity을 in vitro에서 HCT-116 cancer cell을 사용하여 측정한 결과 모든 시료에서 암세포 증식억제 현상을 보였으며 특히 Rf 0.19와 Rf 0.25 band에서 분리된 화합물들에서 강하게 나타났다. 이 결과로 볼 때 두충잎에서 분리한 클로로필 유도체는 인간대장암세포인 HCT-116 cell에 대해 강한 항암작용이 있는 것으로 생각된다.

• 한국식품영양과학회지
• /
• 제42권5호
• /
• pp.655-662
• /
• 2013

식용버섯(표고버섯과 아가리쿠스버섯)과 약용버섯(영지버섯, 동충하초, 차가버섯, 상황버섯) 추출물의 항산화효과와 인체 암세포(AGS, HCT-116, 및 HepG2) 성장 저해율, apoptosis 유도에 관련된 Bcl-2, Bax 유전자, 그리고 염증에 관련된 iNOS 및 COX-2 유전자의 분석을 통해 식용버섯과 약용버섯의 in vitro 항암효과를 비교하였다. DPPH와 hydroxy radical($OH{\cdot}$) 소거능력은 표고버섯, 아가리쿠스버섯, 동충하초, 영지버섯, 차가버섯, 상황버섯 순으로 높았으며, 식용버섯보다는 약용버섯의 항산화효과가 더 높았고, 약용버섯 중 차가버섯과 상황버섯의 항산화효과는 78%와 90%로 상황버섯이 가장 우수하였다(p<0.05). AGS 위암세포, HCT-116 결장암세포, HepG2 간암세포에 대한 억제효과는 식용버섯인 아가리쿠스버섯과 표고버섯 추출물은 5~40%, 약용버섯인 영지버섯과 동충하초 추출물은 28~79%, 상황버섯과 차가버섯 추출물은 75~91%로 나타났다. Apoptosis 유도에 관련된 Bcl-2 및 Bax 유전자 발현과 염증에 관련된 iNOS 및 COX-2 유전자 발현은 표고버섯, 아가리쿠스버섯, 동충하초, 영지버섯, 차가버섯, 상황버섯 순으로 apoptosis를 유도하는 작용과 세포의 발암(염증) 유도과정을 억제하는 효과가 높게 나타났다. 총 폴리페놀과 플라보노이드 화합물의 함량은 상황버섯의 폴리페놀과 플라보노이드함량이 각각 317.2 mg/g 및 35.7 mg/g으로 가장 높게 나타났으며 차가버섯, 영지버섯, 동충하초, 아가리쿠스버섯, 표고버섯 추출물 순으로 함량이 낮아졌다. 식용버섯보다 약용버섯의 총 폴리페놀과 플라보노이드 화합물의 함유량이 많았고, 이들 화합물 함량이 많을수록 항산화효과와 인체 암세포의 성장 억제효과가 높아졌다.

• 한국식품영양과학회지
• /
• 제44권9호
• /
• pp.1270-1278
• /
• 2015

시료 된장의 pH, 아미노태, 암모니아태 수치는 각 군 간 특별한 차이는 보이지 않았다. 검정콩 된장이 가장 높은 폴리페놀 농도, DPPH를 이용한 항산화 효과를 보였다. 된장 추출물은 0.1~0.5 mg/mL 범위까지는 RAW 264.7 cells의 증식을 억제하지 않았으며, HT-29를 이용한 MTT에서 BD 군이 가장 높은 암세포 성장 억제율을 보였다. HT-29에서 pro-inflammatory cytokine인 $TNF-{\alpha}$, IL-6와 염증관련 인자 COX-2의 mRNA 발현은 시료 처리군에서 대조군에 비해 낮은 수치를 나타냈으며 BD군에서 가장 낮은 수치를 보였다(P<0.05). 세포 증식에 관여하는 p21, p53과 cyclin D1의 mRNA 발현은 p21과 p53가 BD군에서 발현이 증가하였고, cyclin D1은 BD군에서 낮아졌다. Apoptosis 관련 유전자인 Bcl-2는 BD군이 가장 낮은 발현을 보였다. 이상의 결과로 BD군은 CD, SD군에 비해 높은 폴리페놀 농도, 항산화 효과, 대장암세포에서 pro-inflammatory cytokines과 세포 증식에 관여하는 유전자 등을 조절한다. 이 결과는 아마도 서목태 된장의 높은 총 페놀화합물의 양과 안토시아닌의 함량으로 얻어진 결과로 생각된다.

• Asian Pacific Journal of Cancer Prevention
• /
• 제15권18호
• /
• pp.7527-7532
• /
• 2014

Saussurea involucrata is a Mongolian medicinal plant well known for its effects in promoting blood circulation, and anti-inflammation and analgesic functions. Earlier studies reported that Saussurea involucrata has anticancer activity. The purpose of this study was to confirm the anticancer activity of an ethanol extract of Saussurea involucrata against hepatic cancer and elucidate its mechanisms of action. Hepatocellular carcinoma cells were tested in vitro for cytotoxicity, AO/EB staining for apoptotic cells, apoptotic DNA fragmentation and cell cycle distribution in response to Saussurea involucrata extract (SIE). The mRNA expression of caspase-3,-9 and Cdk2 and protein expression of caspase-3,-9, PARP, XIAP, Cdk2 and p21 were analyzed through real time PCR and Western blotting. Treatment with SIE inhibited HepG2 cell proliferation dose- and time-dependently, but SIE only exerted a modest cytotoxic effect on a viability of Chang human liver cells. Cells exposed to SIE showed typical hallmarks of apoptotic cell death. Cell cycle analysis revealed that SIE caused G1-phase arrest in HepG2 cells. In conclusion, Saussurea involucrata ethanol extract has potential cytotoxic and apoptotic effects on human hepatocellular carcinoma cells. Its mechanism of action might be associated with the inhibition of DNA synthesis, cell cycle (G1) arrest and apoptosis induction through up-regulation of the protein expressions of caspase-3,-9 a nd p21, degradation of PARP and down-regulation of the protein expression of Cdk2 and XIAP.

• Nutrition Research and Practice
• /
• 제18권1호
• /
• pp.62-77
• /
• 2024

BACKGROUND/OBJECTIVES: Colorectal cancer (CRC) is the third most common cancer worldwide with a high recurrence rate. Oxaliplatin (OXA) resistance is one of the major reasons hindering CRC therapy. β-Carotene (BC) is a provitamin A and is known to have antioxidant and anticancer effects. However, the combined effect of OXA and BC has not been investigated. Therefore, this study investigated the anticancer effects and mechanism of the combination of OXA and BC on CRC. MATERIALS/METHODS: In the present study, the effects of the combination of OXA and BC on cell viability, cell cycle arrest, and cancer stemness were investigated using HCT116, HT29, OXA-resistant cells, and human CRC organoids. RESULTS: The combination of OXA and BC enhanced apoptosis, G₂/M phase cell cycle arrest, and inhibited cancer cell survival in human CRC resistant cells and CRC organoids without toxicity in normal organoids. Cancer stem cell marker expression and self-replicating capacity were suppressed by combined treatment with OXA and BC. Moreover, this combined treatment upregulated apoptosis and the stem cell-related JAK/STAT signaling pathway. CONCLUSIONS: Our results suggest a novel potential role of BC in reducing resistance to OXA, thereby enhances the anticancer effects of OXA. This enhancement is achieved through the regulation of cell cycle, apoptosis, and stemness in CRC.