• Mycobiology
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• 제40권1호
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• pp.47-52
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• 2012

$Elfvingia$ $applanata$, a medicinal mushroom belonging to Basidiomycota, has been used in the effort to cure cancers of the esophagus and stomach, and is also known to have inhibitory effects on hepatitis B virus infection. The hot water soluble fraction (as Fr. HW) was extracted from fruiting bodies of the mushroom. $In$ $vitro$ cytotoxicity tests showed that hot water extract was not cytotoxic against cancer cell lines such as Sarcoma 180, HT-29, HepG2, and TR at concentrations of 10-2,000 ${\mu}g/mL$. Intraperitoneal injection with Fr. HW resulted in a life prolongation effect of 45.2% in mice previously inoculated with Sarcoma 180. Treatment of Fr. HW resulted in a 2.53-fold increase in the numbers of murine spleen cells at a concentration of 50 ${\mu}g/mL$, compared with control. Incubation of murine spleen cells with Fr. HW at a concentration of 500 ${\mu}g/mL$ resulted in improved immune-potwntiating activity of B lymphocytes through an 8.3-folds increase in alkaline phosphatase activity, compared with control. Fr. HW generated 12.5 ${\mu}M$ of nitric oxide (NO) when cultured with RAW 264.7, a mouse macrophage cell line, at the concentration of 50 ${\mu}g/mL$, while lipopolysaccharide, a positive control, produced 15.2 ${\mu}M$ of NO. Therefore, the results suggested that antitumor activities of Fr. HW from $E.$ $applanata$ might, in part, be due to host mediated immunostimulating activity.

• 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.

• KSBB Journal
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• 제18권4호
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• pp.324-328
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• 2003

도꼬마리 추출물의 발암성의 유무를 검토하기 위하여 시험균 S. typhimurium TA98 및 TA100에 대한 변이원성 실험 결과, 추출물 XE-N과 XEA-N의 농도가 증가해도 TA 98 및 TA100 두 균주의 복귀변이 colony 수가 대조구에 비해 변화가 크지 않은 점을 미루어 보아 각 추출물은 변이원성이 없는 것으로 확인되었다. 도꼬마리 추출물 XEA-A, XEA-B 및 XE-A)의 $H_2O$$_2$로 유도된 세포 독성에 대한 억제효과는 각각 58%, 53%, 63%로서 생존율이 2배 이상 증가하였다. 면역 증강 활성은 TNF의 경우 XE-N 추출물에서 2.7배로 가장 높은 활성을 나타내었으며 XEA-N 추출물에서도 2.3배로 높은 활성을 나타내었다. IL-1$\beta$의 생성은 XE-B 추출물에서 높게 나타났으며, IL-2의 생성에는 뚜렷한 활성을 나타내지 않았다. 도꼬마리 추출물 및 정제물을 이용하여 동물에 강력한 발암물질인 MNNG를 투여한 후 항산화 효소계를 측정한 결과, 조직의 해독물질인 glutathione (GSH)의 함량이 도꼬마리 정제물 0.2% 투여군에서 약 44.6%, 도꼬마리 추출물 투여군에서 약 41.5% 증가되었다. 또한 도꼬마리 추출물 및 정제물질은 암억제 유전자인 p53의 발현을 매우 증가시켰다. 이상의 결과에서 도꼬마리 추출물은 전반적으로 항산화능, 면역증강효과, 암 예방효과 등의 기능성이 있는 것으로 입증되었으며, 각 기능에 따른 다양한 물질을 분리하여 신소재로의 개발 가능성이 큰 약제임이 확인되었다.

• 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.

• 생약학회지
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• 제40권3호
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• pp.205-212
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• 2009

Antitumor activity of Korean mistletoe extract (KM-110) and European commercial mistletoe preparation (Helixor) was investigated. KM-110 showed the cytotoxic effect that it is high for various tumor cell lines and normal splenocytes in comparison with Helixor. Administration of two mistletoe extracts ($100{\mu}g$) to mice did not show any significant changes on the level of glutamic-oxaloacetic transaminase (GOT), glutamic-pyruvate transaminase (GTP), blood creatinine (CRE) and blood urea nitrogen (BUN) in sera. The culture supernatant of macrophages stimulated with KM-110 inhibited effectively tumor growth whereas Helixor had little effect. Administration of KM-110 or Helixor resulted in a effective inhibition of lung metastasis after the i.v. inoculation of colon 26-M3.1 lung carcinoma, B16-BL6 melanoma and L5178Y-ML25 lymphomas. In all cases, the mice treated with KM-110 showed more effective anti-tumor metastatic activity than the mice of Helixor. These results suggest that Korean mistletoe extracts, KM-110 might be used as an alternative methods having antitumor activity like European mistletoe preparation, Helixor.

• 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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• 제15권7호
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• pp.3185-3189
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• 2014

Background: Breast cancer evolution and tumor progression are controlled by complex interactions between steroid receptors and growth factor receptor signaling. Aberrant growth factor receptor signaling can augment or suppress estrogen receptor function in hormone-dependent breast cancer cells. Thus, we aimed to investigate antitumor effects of sorafenib and lapatinib alone and in combination on MCF-7 breast cancer cells. Materials and Methods: Cytotoxicity of the sorafenib and lapatinib was tested in MCF-7 cells by XTT assays. 50, 25, 12.5 and $6.25{\mu}M$ concentrations of sorafenib and 200, 100, 50 and $25{\mu}M$ concentrations of lapatinib were administered alone and in combination. Results were evaluated as absorbance at 450nM and $IC_{50}$ values are calculated according to the absorbance data Results: Both sorafenib and lapatinib showed concentration dependent cytotoxic effects on MCF-7 cells. Sorafenib exerted cytotoxic effects with an $IC_{50}$ value of $32.0{\mu}M$; in contrast with lapatinib the $IC_{50}$ was $136.6{\mu}M$. When sorafenib and lapatinib combined, lapatinib increased cytotoxic effects of sorafenib at its ineffective concentrations. Also at the concentrations where both drugs had cytotoxic effects, combination show strong anticancer effects and killed approximately 70 percent of breast cancer cells. Conclusions: Combinations of tyrosine kinase inhibitors and cytotoxic agents or molecular targeted therapy has been successful for many types of cancer. The present study shows that both sorafenib and lapatinib alone are effective in the treatment of breast cancer. Also a combination of these two agents may be a promising therapeutic option in treatment of breast cancer.

• Asian Pacific Journal of Cancer Prevention
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• 제15권2호
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• pp.611-616
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• 2014

Objectives: Dendritic cell (DC)-based tumor immunotherapy needs an immunogenic tumor associated antigen (TAA) and an effective approach for its presentation to lymphocytes. In this study we explored whether transduction of DCs with lentiviruses (LVs) expressing the human interleukin-12 gene could stimulate antigen-specific cytotoxic T cells (CTLs) against human lung cancer cells in vitro. Methods: Peripheral blood monocyte-derived DCs were transduced with a lentiviral vector encoding human IL-12 gene (LV-12). The anticipated target of the human IL-12 gene was detected by RT-PCR. The concentration of IL-12 in the culture supernatant of DCs was measured by ELISA.Transduction efficiencies and CD83 phenotypes of DCs were assessed by flow cytometry. DCs were pulsed with tumor antigen of lung cancer cells (DC+Ag) and transduced with LV-12 (DC-LV-12+Ag). Stimulation of T lymphocyte proliferation by DCs and activation of cytotoxic T-lymphocytes (CTL) stimulated by LV-12 transduced DCs pulsed with tumor antigen against A549 lung cancer cells were assessed with methyl thiazolyltetrazolium (MTT). Results: A recombinant lentivirus expressing the IL-12 gene was successfully constructed. DC transduced with LV-12 produced higher levels of IL-12 and expressed higher levels of CD83 than non-transduced. The DC modified by interleukin -12 gene and pulsed with tumor antigen demonstrated good stimulation of lymphocyte proliferation, induction of antigen-specific cytotoxic T lymphocytes and antitumor effects. Conclusions: Dendritic cells transduced with a lentivirus-mediated interleukin-12 gene have an enhanced ability to kill lung cancer cells through promoting T lymphocyte proliferation and cytotoxicity.