• Parasites, Hosts and Diseases
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• 제54권4호
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• pp.415-421
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• 2016

The drug-resistance of malaria parasites is the main problem in the disease control. The huge Brazilian biodiversity promotes the search for new compounds, where the animal kingdom is proving to be a promising source of bioactive compounds. The main objective of this study was to evaluate the antiplasmodial and cytotoxic activity of the compounds obtained from the toad venoms of Brazilian Amazon. Toad venoms were collected from the secretion of Rhinella marina and Rhaebo guttatus in Mato Grosso State, Brazil. The powder was extracted at room temperature, yielding 2 extracts (RG and RM) and a substance ('1') identified as a bufadienolide, named telocinobufagin. Growth inhibition, intraerythrocytic development, and parasite morphology were evaluated in culture by microscopic observations of Giemsa-stained thin blood films. Cytotoxicity was determined against HepG2 and BGM cells by MTT and neutral red assays. The 2 extracts and the pure substance ('1') tested were active against chloroquine-resistant Plasmodium falciparum strain, demonstrating lower $IC_{50}$ values. In cytotoxic tests, the 2 extracts and substance '1' showed pronounced lethal effects on chloroquine-resistant P. faciparum strain and low cytotoxic effect, highlighting toad parotoid gland secretions as a promising source of novel lead antiplasmodial compounds.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1987년도 Proceedings of Korea-Japan Panax Ginseng Symposium 1987 Seoul Korea
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• pp.29-37
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• 1987

This study was devised to observe the cytotoxlc activities of petroleum-ether extract of Panax ginseng root(crude Gx) and its partially purified fraction from silicon acid column chromatography(7:3 CX) against sarcoma-180(5-180) and Walker carcinosarcoma 256(Walker 256) in vivo, and murine leukemic lymphocytes(L1210) and human rectal cancer cell(HRT-18) and human colon cancer cells(HT-29 and HCT-48) in vitro . Each cell-line was cultured in medium containing serial concentrations of the crude Gx or 7:3 Gx in vitro. A highly lipid soluble compound in the extract of Panax ginseng root was cytocidal to murine leukemic cells and human colon and rectal cancer cells in vitro In the meantime, ginseng saponin derivatives did not cytotoxic effects at its corresponding concentration. The growth rates of the cancer cells in medium containing ginseng extracts were inhibited gradually to a significant degree roughly in proportion to the increase of the extract concentration. The cytotoxic activity of 7:3 Gx was about 3 times more potent than that of crude Gx, one unit of cytotoxic activity against L121f cells being equivalent to 2.54$\mu\textrm{g}$ and 0.88 $\mu\textrm{g}$ for the crude Gx and 7:3 Gx, respectively. The Rf value of the active compound on silica -gel thin layer chromatography with petroleum-ether/ethyl ether/acetic acid mixture (90:10:1, v/v/v) as a developing solvent was 0.23. The survival times of mice inoculated with S-180 cells were extended about 1.5 to 2 times by the 7:3 Gx treatment compared with their control group. The significantly decreased hemoglobin values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude Gx. The synthetic levels of protein, DNA and RNA in human colon and rectal cancer cells were significantly diminished by treatment with the crude Gx, which can explain a part of the origin of its anticancer activity.

• BMB Reports
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• 제41권2호
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• pp.119-125
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• 2008

Our previous work confirmed that Sph2/LA1029 was a sphigomyelinase-like hemolyisn of Leptospira interrogans serogroup Icterohaemorrhagiae serovar Lai. Characteristics of both hemolytic and cytotoxic activities of Sph2 were reported in this paper. Sph2 was a heat-labile neutral hemolysin and had similar hemolytic behavior as the typical sphingomyelinase C of Staphylococcus aureus upon sheep erythrocytes. The cytotoxic activity of Sph2 was shown in mammalian cells such as BALB/C mouse lymphocytes and macrophages, as well as human L-02 liver cells. Transmission electron microscopic observation showed that the Sph2 treated BALB/C mouse lymphocytes were swollen and ruptured with membrane breakage. They also demonstrated condensed chromatin as a high-density area. Cytoskeleton changes were observed via fluorescence confocal microscope in Sph2 treated BALB/C mouse lymphocytes and macrophages, where both cytokine IL-$1{\beta}$ and IL-6 were induced. In addition, typical apoptotic morphological features were observed in Sph2 treated L-02 cells via transmission electron microscope and the percentage of apoptotic cells did increase after the Sph2 treatment detected by flow cytometry. Therefore, Sph2 was likely an apoptosis-inducing factor of human L-02 liver cells.

• 동의생리병리학회지
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• 제19권4호
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• pp.950-954
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• 2005

Phellinus linteus (Berk. & M.A. Curtis) Teng, commonly referred to as Sangwhang in Korea, is a well-known species of the genus Phellinus, which attracts great attention due to its phamarcological values. P. linteus has been reported to produce anti-tumor, anti-angiogenic, anti-mutagenic and immunomodulatory activities in vivo and in vitro. However, despite extensive biochemical studies on P. linteus, the wine produced by P. linteus fermentation (WPLF) has poorly investigated. In the present study, it was compared the in vitro cytotoxic effects of WPLF with ethanol as positive control. WPLF as well as ethanol induced the inhibition of cell proliferation and morphological changes in both HepG2 and A549 cells in a concentration-dependent manner, however, WPLG treatment has less cytotoxic effects than ethanol treatment. These cytotoxic effects were associated with the induction of apoptotic cell death, but, WPLG treatment has less apoptotisis inducing effects than ethanol treatment.

• 약학회지
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• 제46권6호
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• pp.459-465
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• 2002

$\beta$-l, 3-glucans are well known to enhance the immune reactions, resulting in antitumor, antibacterial, antiviral, anticoagulatory and wound healing activities. $\beta$-1, 3-glucans have various activities depending on molecular weight, degree of branching, conformation, water-solubility and intermolecular association. However, the $\beta$-1, 3-glucans linked backbone structure is essential and $\beta$-D-glucopyranosyl units are required for immunopotentiating activities. In this study, we tested the immunophamacological activities of insoluble $\beta$-1, 3-glucan from Agrobacterium sp. R259 KCTC 10197BP and confirmed the following activities: (1) IFN-${\gamma}$ production in PBMCs in the presence or in the absence of PHA, LPS, IL-18, and IL-12; (2) the induction of various cytokines in the spleen and thymus; (3) the adjuvant effect on the antibody production; (4) the cytotoxic and antitumor effects on cell lines and ICR mice. These results strongly suggest that $\beta$-1, 3-glucan from Agrobacterium sp. R259 KCTC 10197BP possesses various immunopharmacologica1 activities.

• Asian Pacific Journal of Cancer Prevention
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• 제16권7호
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• pp.2763-2769
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• 2015

Background: Cancer is an unnatural type of tissue growth in which the cells exhibit unrestrained division, leading to a progressive increase in the number of dividing cells. It is now the second largest cause of death in the world. The present study concerned antioxidant, anticancer and anticholinesterase activities and protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in methanol extracts of flowers, fruits and seeds of Hypericum amblysepalum. Materials and Methods: Antioxidant properties including free radical scavenging activity and reducing power, and amounts of total phenolic compounds were evaluated using different tests. Protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in extracts were determined by HPLC. Cytotoxic effects were determined using the MTT test with human cervix cancer (HeLa) and rat kidney epithelium cell (NRK-52E) lines. Acetyl and butyrylcholinesterase inhibitory activities were measured by by Ellman method. Results: Total phenolic content of H. amblysepalum seeds was found to be higher than in fruit and flower extracts. DPPH free radical scavenging activity of the obtained extracts gave satisfactory results versus butylated hydroxyanisole and butylated hydroxytoluene as controls. Reducing power activity was linearly proportional to the studied concentration range: $10-500{\mu}g/mL\;LC_{50}$ values for H. amblysepalum seeds were 11.7 and 2.86 respectively for HeLa and NRK-52E cell lines. Butyryl-cholinesterase inhibitory activity was $76.9{\pm}0.41$ for seed extract and higher than with other extracts. Conclusions: The present results suggested that H. amblysepalum could be a potential candidate anti-cancer drug for the treatment of human cervical cancer, and good source of natural antioxidants.

• 약학회지
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• 제50권6호
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• pp.372-380
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• 2006

Farnesol in fruits, vegetables, herbs and leaves acts as bioactive component related with prevention of cancer and psychological malaise. We investigated the cytotoxic effects of farnesol on human leukemic cell, HL-60 cells, by MTT assay using 3- (4,5-Oirnethylthiazol-2-yl) -2,5-diphenyltetrazoliumbromide. Farnesol (0.1${\sim}$50 ${\mu}$g/ml) exhibited cytotoxicities against HL-60 cells in concentration and culture period dependent manner, In the cytotoxic condition induced by farnesol against HL-60 cells, the generation of reactive oxygen species such as O$_2$ and H$_2$O$_2$ were found to be considerably increased. The most prominent augmentations of O$_2$ and H$_2$O$_2$ were over five folds of controls. In an attempt to explore the response of HL-60 cells to the increased O$_2$ and H$_2$O$_2$, superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase activities of HL-60 cells treated with farnesol were measured. SOD and GPx activities were found to be remarkably elevated by addition of farnesol showing the best results of 273% and 167% of controls, respectively: All data suggest that farnesol may have played as an apoptosis inducer in HL-60 cells via production of reactive oxygen species (ROS) and HL-60 cells may have failed to overcome the damage of ROS on account of still defcient ROS scavengers including SOD and GPx.

• 한국식품저장유통학회지
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• 제9권3호
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• pp.338-344
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• 2002

본 연구는 포도 거봉종의 종자와 과피 추출물의 지질과산화 억제 효과와 암세포들에 대한 세포 독성을 살펴보았다. 추출 온도를 달리하여 추출한 종자와 과피의 에탄올 추출물과 추출물에 대한 분획물들을 이용하여 지질과산화물의 억제효과를 측정한 결과, 종자 및 과피 에탄올 추출물 모두 온도변화에 따른 영향은 없는 것으로 나타났으며, 추출물의 농도가 증가할수록 지질과산화물의 감소효과가 증가하였다. 종자 추출물의 경우, 3$0^{\circ}C$에서 추출한 에탄올추출물이 20 $\mu\textrm{g}$/$m\ell$ 농도에서 60.1%, 분획물 중에서는 ethyl acetate 분획물이 71.2%의 지질과산화를 억제하였다. 과피 에탄올 추출물의 경우, 5$0^{\circ}C$에서 추출한 추출물이 20 $\mu\textrm{g}$/$m\ell$ 농도에서 48.1%, 분획물 중에서는 hexane 분획물이 44.4%의 지질과산화를 각각 억제하였다. 암세포 생육 억제 효과에서는 모든 암세포(MCF-7, Hep3B 및 A549)에서 포도 종자 및 과피 에탄올 추출물 및 분획물들이 1.00 $\mu\textrm{g}$/ML 농도에서 대부분 50% 이상의 생육 억제율을 보였으며, 암세포에 대한 생육 억제와 정상 세포에 대한 selectivity에서는 종자 에탄올 추출물과 과피 에탄을 추출물간의 유의적인 차이는 나타나지 않았다. 본 연구 결과, 거봉포도종자 및 과피의 에탄올 추출물들과 각 분획물은 지질과산화 억제 효과와 암세포들에 세포 독성이 캠벨종의 포도종자 및 과피에 비하여 낮은 활성을 나타내었다.

• 대한예방한의학회지
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• 제2권1호
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• pp.13-30
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• 1998

제라니올 (1), 올리비톨 (2), 카나비노이드 (3 과 4)와 5-플로르우라실 (5)을 MTT 정량분석법과 SRB 정량분석법으로 인체 피부흑색종세포에 대하여 성장 억제효과를 평가 하였다. 이들 화합물(1, 2, 3, 4와 5)은 마이크로 몰 농도의 범위에 대하여 억제 활성을 나타내었다. 일반적으로 이들 화합물은 $1{\mu}M\;-\;100{\mu}M$ 농도범위에서는 투여량에 따라 항암활성을 나타내었다. 인체 피부흑색종세포에 대한 이들 화합물의 50 %억제 농도 효과에 대한 비교는 다음과 같은 순서로 항암활성이 감소하였다. MTT 정량분석법 ; OLVTL >CBG > CBD > 5-FU >GRNL, SRB 정량 분석법 ; CBG > OLVTL > CBD > CRNL > 5-FU, 카나비노이드 (3 과 4)와 5-플로르우라실 (5)을 MTT정량분석법과 SRB정량분석법으로 인체정상세포에 대하여 독성효과를 측정하였다. 이들 화합물은 마이크로몰농도의 농도범위에서는 투여량에 따라 세포독성을 보였다. 인체정상세포에 대한 이들 화합물의 50 % 독성효과에 대한 비교는 다음과 같은 순서로 세포독성이 감소하였다. MTT정량분석법과 SRB정량분석법 ; CBD > 5-FU > CBG. 따라서 카나비지놀 (3)은 인체정상세포에 대하여 가장 낮은 세포독성을 나타내었다. 따라서 카나비지놀 (3)은 인체 피부흑색종세포에 대하여 가장 강한 성장억제활성을 보였다.

• Bulletin of the Korean Chemical Society
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• 제35권5호
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• pp.1337-1342
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• 2014

A novel and convenient route for the synthesis of a series of thalidomide derivatives is described. Compound 2 was cyclized with different amines under alkaline condition to obtain 4-nitro substituted phthalimidines 3a-d. Hydroxylactams 4a-d were produced via bromination and hydroxylation. Different acyl chlorides were reacted with hydroxylactams to provide the desired esters 5a-d. All compounds were evaluated by MTT assay for their inhibitory activities against HCT-116, MG-63, MCF-7, HUVEC and HMVEC cell lines in vitro. Most of them showed no obvious cytotoxic effect on normal human cells, compounds 4a-d, $5a_2$, $5a_4$, $5a_5$, $5b_2$, $5c_2$ and $5d_2$ exhibited potent antitumor activities, among which compounds $5a_2$ and $5b_2$ were more effective than 5-FU.