• Journal of Ginseng Research
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• 제41권3호
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• pp.373-378
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• 2017

Ocotillol-type saponins are one kind of tetracyclic triterpenoids, sharing a tetrahydrofuran ring. Natural ocotillol-type saponins have been discovered in Panax quinquefolius L., Panax japonicus, Hana mina, and Vietnamese ginseng. In recent years, the semisynthesis of 20(S/R)-ocotillol-type saponins has been reported. The biological activities of ocotillol-type saponins include neuroprotective effect, antimyocardial ischemia, antiinflammatory, antibacterial, and antitumor activities. Owing to their chemical structure, pharmacological actions, and the stereoselective activity on antimyocardial ischemia, ocotillol-type saponins are subjected to extensive consideration. In this review, we sum up the discovery, semisynthesis, biological activities, and metabolism of ocotillol-type saponins.

• 한국식품영양학회지
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• 제30권5호
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• pp.1127-1131
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• 2017

당조고추의 기능성 소재로서의 가능성을 알아보기 위하여 당조고추 70% 에탄올 추출물에 대한 항산화 활성 및 항암활성을 측정하였다. 당조고추 70% 에탄올 추출물의 총 폴리페놀은 30.29 mg GAE/g extract로 나타났다. 당조고추 70% 에탄올 추출물에 대한 DPPH radical 및 hydroxyl radical 소거활성을 $IC_{50%}$ 측정한 각각 2.87, 10.55 mg/mL의 소거활성을 보여 주었으며, ${\alpha}$-glucosidase 및 ${\alpha}$-amylase 저해활성은 10 mg/mL의 농도에서 각각 35.67, 58.41%로 나타났다. 당조고추 70% 에탄올 추출물에 대한 항암활성은 대장암 세포주의 0.5 mg/mL 농도에서 50% 암세포 성장억제를 보였지만, 다른 암세포에서는 억제효과를 나타내지 않았다.

• Fisheries and Aquatic Sciences
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• 제22권6호
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• pp.13.1-13.9
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• 2019

Background: Marine invertebrates are well known as pivotal bioresources with bioactive substances such as anti-inflammatory sterols, antitumor terpenes, and antimicrobial peptides. However, there are few scientific reports on chemical compositions and bioactivities of marine invertebrates from the East Sea of South Korea. Methods: In this study, chemical compositions and biological activities were evaluated on both 70% EtOH and hot water extracts of 5 species of marine invertebrates (Crossaster papposus japonicus, Actinostola carlgreni, Stomphia coccinea, Actinostola sp., and Heliometra glacialis) collected from the East Sea of South Korea. The antioxidant activities were measured by ABTS radical scavenging assay. The cytotoxicity and anti-inflammatory activity were evaluated using MTT and Griess reagents. Moreover, the antibacterial effect was evaluated using paper disc assay and minimum inhibitory concentration (MIC) assay. Results: In the results of antioxidant activities, 70% EtOH extract of A. carlgreni showed the highest activity ($IC_{50}\;0.19{\pm}0.03mg/ml$) compared to other extracts. Moreover, 70% EtOH extract of A. carlgreni could significantly suppress the nitric oxide (NO) production in lipopolysaccharide-induced RAW 264.7. All extracts treated under $400{\mu}g/ml$ have no cytotoxic effects on RAW 264.7 macrophages. In the antibacterial test, both 70% EtOH extracts of C. papposus japonicus and H. glacialis showed a significant antibacterial effect on Staphylococcus aureus. The MIC values were evaluated at 256 and $512{\mu}g/ml$, respectively. Conclusions: These results suggested the bioactive potentials of marine invertebrates from the East Sea of South Korea in pharmaceutical and nutraceutical applications.

• 한국식품영양과학회지
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• 제22권3호
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• pp.334-339
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• 1993

Sarcoma 180 복수형 종양세포를 생쥐의 왼쪽 서혜부에 이식한 후 감잎에서 분리한 tannin. chloroform fraction 추출물 및 2, 4-decadienal을 복강 내에 각각 단독투여하여 그 효과를 형태학적으로 검토하였다. 이식된 sarcoma 180 육종에서 암화의 진행을 지연시키는데는 tannin 투여시에 가장 효과적이었고 chloroform fraction 추출물 및 2, 4-decadienal 투여시에는 형태적으로 간주할 수 있는 지연효과는 없는 것으로 나타났다. 감잎 tannin 은 종양세포를 선택적으로 파괴하여 종양의 증식을 억제하는 것이 아니라 일종의 혐기상태의 세포 환경에서 종양을 괴사과정으로 유도하지 않고, 발암성을 가지는 단백질과 같은 물질의 합성을 저해하거나 또는 자식작용을 가진 과립들로 하여금 이들을 소화시켜 이식된 종양세포를 악성종양으로 유도하는 과정을 지연시키는 효과를 나타내었다.

• Asian Pacific Journal of Cancer Prevention
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• 제15권22호
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• pp.9939-9943
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• 2014

Lobaplatin, one of the third - generation platinum compounds, has shown encouraging anticancer activity in a variety of tumor types. However, the efficacy of lobaplatin in ovarian cancer has not been systemically evaluated. In this study, lobaplatin as a single agent and in combination with taxanes was investigated in - vitro and in an in vitro model of ovarian carcinoma. Using the sulforhodamine B (SRB) assay, the cytotoxic effects of lobaplatin alone and in combination with taxanes were compared with cisplatin and carboplatin in seven ovarian cancer cell lines. In addition, in - vitro antitumor activities were evaluated with cisplatin - sensitive and cisplatin - resistant human ovarian cancer xenografts in nude mice. The cytotoxicity of lobaplatin was similar to or higher than that of cisplatin and carboplatin, with $IC_{50}$ values from 0.9 to $13.8{\mu}mol/L$ in a variety of ovarian cancer cells. The combination of lobaplatin with docetaxel yielded enhanced cytotoxic activity in vitro. In addition, in platinum - sensitive ovarian cancer xenografts, lobaplatin alone showed similar antitumor activity to cisplatin and carboplatin. Furthermore, lobaplatin alone or in combination with docetaxel exhibited significant activity in platinum - resistant ovarian cancer xenografts. These results indicate that the use of lobaplatin alone or in combination with docetaxel might be a rational and novel therapeutic strategy for ovarian cancer. Further clinical development of lobaplatin is clearly warranted.

• 동의생리병리학회지
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• 제17권3호
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• pp.711-718
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• 2003

Wanpae-tang is suggested to have antitumor activity on lung cancer. This study was performed to investigate antitumor, immune response, and apoptotic effects by Wanpae-tang in the cancer cell lines and C57BL/6 mice. Experimental studies were progressed through the anticancer activities such as, survival time, cell cytotoxicity, natural killer cell activity, productivity of interleukins and apoptotio effects. The results were summarized as follows: 1. Median survival time of Wanpae-tang treated group was prolonged to 4.1%, as compared with control group, but was not significant. 2. On the MTT assay, half-maximal inhibitory concentration(IC50) of Wanpae-tang was 15.00 ㎎/㎖ in HeLa cell, and 4.158 ㎎/㎖ in HRT-18 cell. 3. Natural killer cell activity in Wanpae-tang treated group was decreased in case of 100:1 and 10:1 effect cell/target cell ratio. 4. Production of interleukin-2, 4, 12 in Wanpae-tang treated group were significantly increased. 5. On the studies of Wanpae-tang induced apoptosis, a DNA fragmentation patterns were not appeared.

• Archives of Pharmacal Research
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• 제24권1호
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• pp.44-50
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• 2001

To search for cytotoxic components from Allium victoriallis , MTT assays on each extract and an isolated component, gitogenin 3-O-lycotetroside, were performed against cancer cell lines. Cytotoxicities of most extract were shown to be comparatively weak, though $IC_50$ values of $CHCl_3$fraction was found to be <31.3-368.4 $\mu\textrm{g}/ml$. From the incubated methanol extract at $36^{\circ}C, eleven kinds of organosulfuric flavours were predictable by CG-MS performance. The most abundant peak was revealed to be 2-vinyl-4H-1,3-dithiin(1) by its mass spectrum. Further, this extract showed significant cytotoxicities toward cancer cell lies. Silica gel column chromatography of the n-butanol fraction led to the isolation of gitogenin 3-O-lycotetroside (3) along with astragalin (4) and kaempferol 3, 4'-di-O-$\beta$-D-glycoside (5). This steroidal saponin exhibited significant cytotoxic activities ($IC_50$, 6.51-36.5 $\mu\textrm{g}/ml$) over several cancer cell lines. When compound 3 was incubated for 24 h with human intestinal bacteria, a major metabolite was produced and then isolated by silica gel column chromatography. By examining parent and prominent ion peak in FAB-MS spectrum of the metabolite, the structure was speculated not to be any of prosapogenins of 3, suggesting that spiroketal ring were labile to the bacterial reaction. These suggest that disulfides produced secondarily are the antitumor principles.

• 생약학회지
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• 제17권2호
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• pp.168-177
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• 1986

Bioassay-directed isolation has yielded some cytotoxic substances against L1210 cell from the Korean traditional medicine. These include 5,2'-dihydroxy-6,7,8,6'-teramethoxyflavone $(IV,\;scutellaria\;root,\;ED_{50}\;=\;1.7\;{mu}g/ml)$, 7-geranyloxycoumarin $(XXXII,\;poncirus\;fruit,\;10.2\;{mu}g/ml) $and panaxydol $(I,\;white\;ginseng,\;0.03\;{mu}g/ml)$. IV, XXXII and their derivatives were synthesized in the purpose of in vivo tests and for observation of structure-activity relations. Among the flavone derivatives, 5,2',6'-trihydroxy-6,7,8-trimethoxy flavone (XVIII), 5-hydroxy-6,7,8-trimethoxy-6'-benzyloxyflavone (XVII) and 5,8-dihydroxy-6,7-dimethoxyflavone (X) showed the cytotoxicity which has no correlation to the flavone structures. Of the coumarins synthesized, 7,8-dihydroxycoumarin (XXVI), 6-7-dihydroxycoumarin (XXIX) and 6-hydroxy-5,7-dimethoxycoumarin (XXXI) showed considerable activities. Acetylated XXXI has moderate activity $(ED_{50}=17.2\;{mu}g/ml)$. Monobydroxycoumarins or their methyl and allyl ether were inactive. IV inhibits the growth of the solid form of S-180 by 70% at 40 mg/kg and shows T/C of 166% on the ascitic S-180 at 40 mg/kg. It strongly inhibits the activity of the membrane bounded ATPase from L1210 cell. The most cytotoxic fraction of the antitumor materials studied is the one from the trichosanthes root showing $ED_{50}=0. 0003\;{mu}g/ml$ against L1210 cell. This fraction, obtained from ethyl acetate extract, showed T/C of 130 and 135%, on ICR mice bearing S-180 and $BDF_1$ mice bearing L1210 at 10 mg/kg and 7.5 mg/kg, respectively.

• Asian Pacific Journal of Cancer Prevention
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• 제15권15호
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• pp.6437-6441
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• 2014

Background: Oridonin isolated from Rabdosia rubescens, a plant used to treat cancer in Chinese folk medicine, is one of the most important antitumor active ingredients. Previous studies have shown that oridonin has antitumor activities in vivo and in vitro, but little is known about cell cycle effects of oridonin in gastric cancer. Materials and Methods: MTT assay was adopted to detect the proliferation inhibition of SGC-7901 cells, the cell cycle was assessed by flow cytometry and protein expression by Western blotting. Results: Oridonin could inhibit SGC-7901 cell proliferation, the $IC_{50}$ being $15.6{\mu}M$, and blocked SGC-7901 cell cycling in the $G_2/M$ phase. The agent also decreased the protein expression of cyclinB1 and CDK1. Conclusions: Oridonin may inhibit SGC-7901 growth and block the cells in the $G_2/M$ phase by decreasing Cdk1 and cyclinB1 proteins.

• 생명과학회지
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• 제8권1호
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• pp.51-59
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• 1998

Ursolic acid(UA)의 apoptosis 유도능을 F9 생쥐 기형암종세포를 대상으로 조사하였다. UA는 피부암화의 억제, tumor의 분화유도, tumor promotion의 억제 등의 항암 효과를 나타내는 pentacyclic triterpene acid로 물질로 알려져 있다. UA를 F9세포에 처리하였을 때 농도비례로 성장억제를 나타냈다. 또한 apoptosis과정에서 관찰되는 전형적인 DNA 분절을 관찰할 수 있었고, 전자현미경을 이용한 세포의 미세구조를 관찰한 결과, 역시 apoptosis과정에서 관찰되는 전형적인 형태인 염색질 응축, 핵의 분절들을 관찰할 수 있어, UA에 의한 항암 효과는 apoptosis에 의한 것임을 시사한다. UA에 의한 apoptosis는 단백질 합성저해제인 cycloheximide에 의해 저해됨을 관찰할 수 있었다. UA를 F4쎄포에 처리한 후 oncogene의 발현양상을 조사한 결과, c-myc과 laminin B1은 apoptosis과정동안 점점 감소하고 c-jun은 증가함을 관찰할 수 있었다. 이상의 결과로서 UA에 의한 F9 세포의 apoptosis에는 새로운 단백질의 합성이 요구되며, c-myc 및 laminin의 발현 감소와 c-jumd의 발현 증가가 관여하고 있음을 시사한다.