• Archives of Pharmacal Research
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• v.28 no.3
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• pp.280-284
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• 2005

The chromatographic separation of the MeOH extract from the aerial parts of Syneilesis palmata led to the isolation of a new sesquiterpene glycoside 4, together with four known compounds. Their structures were characterized to be 4$\beta$,5$\beta$-epoxy-caryophill-8,(15)-ene (1), 3$\beta$­hydroxy-gultin-5-ene (2), 4$\alpha$,5$\beta$-dihydroxy-caryophill-8,(15)-ene (3), (-)-oplopan-4-one-10-$\alpha$-O­$\beta$-D-glucose (4) and 3-hexenyl-1-O-$\beta$-D-glucopyranose (5), based on spectroscopic and chemical methods. Compound 2 showed moderate cytotoxicity against five human tumor cell lines in vitro with its EDso values ranging from 5.90-1 0.83 $\mu$g/mL.

• Archives of Pharmacal Research
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• v.23 no.5
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• pp.450-454
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• 2000

Eight 2-alkylaminosubstituted 5,8-dimethoxy-4-methylquinolines and nine 2-alkylaminosub-stituted or 2,6-disubstituted 4-methylquinoline-5,8-diones were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, HCT15 and SF295).

• Parasites, Hosts and Diseases
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• v.60 no.6
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• pp.401-407
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• 2022

Antimalarial drugs play an important role in the control and treatment of malaria, a deadly disease caused by the protozoan parasite Plasmodium spp. The development of novel antimalarial agents effective against drug-resistant malarial parasites is urgently needed. The novel derivatives, SKM13-MeO and SKM13-F, were designed based on an SKM13 template by replacing the phenyl group with electron-donating (-OMe) or electron-withdrawing groups (-F), respectively, to reverse the electron density. A colorimetric assay was used to quantify cytotoxicity, and in vitro inhibition assays were performed on 3 different blood stages (ring, trophozoite, and schizonts) of P. falciparum 3D7 and the ring/mixed stage of D6 strain after synchronization. The in vitro cytotoxicity analysis showed that 2 new SKM13 derivatives reduced the cytotoxicity of the SKM13 template. SKM13 maintained the IC₅₀ at the ring and trophozoite stages but not at the schizont stage. The IC₅₀ values for both the trophozoite stage of P. falciparum 3D7 and ring/mixed stages of D6 demonstrated that 2 SKM13 derivatives had decreased antimalarial efficacy, particularly for the SKM13-F derivative. SKM13 may be comparably effective in ring and trophozoite, and electron-donating groups (-OMe) may be better maintain the antimalarial activity than electron-withdrawing groups (-F) in SKM13 modification.

• Natural Product Sciences
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• v.8 no.3
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• pp.100-102
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• 2002

Three lignans were isolated from a methanol extract of Lindera erytherocarpa Makino (Lauraceae) are evaluated in vitro cytotoxicity using three cancer cell line assay. The compounds were identified as methyllinderone (1), linderone (2), and kanakugiol (3) by spectroscopic methods. Amongst the compounds, methyllinderone (1) showed significant cytotoxicity against mouse melanoma (B16-FlO), human acetabulum fibrosarcoma (HT1080), and choronic myelogenous leukemia (K562) cancer cell lines with $ED_{50}$ values of 2.2, 2.5, 8.3 ${\mu}g/ml$, respectively.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.9 no.1
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• pp.1-15
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• 1996

The purpose of this research was to investigate effect of water extract of DangKwi-Eum-Ja ka Sumsoo(DESE) on the cytotoxicity of human epidemloid cell, A431 cells. The effects of DESE on the proliferation of A431 cells, Balb/c 3T3 cells, mouse thymocytes and splenocnes were estimated by MTT colorimetric assay, and nitric oxide production from mouse peritoneal macrophage was estimated by Griess method. DESE inhibited the proliferation of A431 cells at $10{\mu}g/ml$, and did not affect the proliferation of Balb/c 3T3 cells. DESE decreased the cytotoxicity of mitomycin C or cisplatin on A431 cells, increased the cytotoxicity of mitomycin C or cisplatin on Balb/c 3T3 cells. DESE inhibited the proliferation of mouse thymocytes and splenocytes at $100{\mu}g/ml$. DESE did not affect the nitric oxide production from mouse peritoneal macrophage in vitro, but decreased the nitric oxide production from DESE-treated mouse peritoneal macrophage.

• Korean Journal of Plant Resources
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• v.28 no.3
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• pp.305-311
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• 2015

This study investigated in vitro antioxidant, anti-inflammatory and cytotoxicity on human lung epithelial A549 cells of different solvent extracts from Jerusalem artichoke (Helianthus tuberosus L.) tuber. The EtOH extract contained amounts of phenolics (22.20 tannic acid equivalent ㎎/ɡ) and exhibited the highest antioxidant activity and anti-inflammatory activity. Several methods were employed for measure the antioxidant activity: 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity (IC₅₀ = 206.79 ㎍/㎖), reducing power activity (21.26 ascorbic acid equivalent ㎎/ɡ) and total antioxidant activity (19.05 ascorbic acid equivalent ㎎/ɡ). Meantime, the EtOH extract inhibited the NO production completely with a concentration of 800 ㎍/㎖. Besides, the H₂O extract exhibited more potent effect on human lung epithelial A549 cells. This study suggested that Jerusalem artichoke tuber had antioxidant, anti-inflammatory and cytotoxicity on human lung epithelial A549 cells.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.421-427
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• 2002

For probing the importance of planarity of imidazolidinone motif of 4-phenyl-1-(N-acylindoline-5-sulfonyl)imidazolidinones 1 for their cytotoxicity, 4-phenyl-1-(N-acylindoline-5-sulfonyl)[1,2,5]thiadiazolidine-1,1-dioxides 2 were prepared and their cytotoxicity were measured against human lung carcinoma (A549), human colon carcinoma (COLO205), human ovarian cancer (SK-OV-3), human leukemic cancer (K562), and murine colon adenocarcinoma (Colon26) cell lines in vitro. Although only carbonyl moiety of imidazolidinone ring was replaced with sulfonyl group, compounds 2 do not show any activity against all five cancer cell lines unlike 1. Therefore the planarity of imidazolidinone ring of 1 should be an important factor for their cytotoxic activity.

• Bulletin of the Korean Chemical Society
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• v.28 no.12
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• pp.2495-2497
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• 2007

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.5
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• pp.3191-3196
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• 2013

Leaf extracts of Cassia alata L (akapulko), traditionally used for treatment of a variety of diseases, were evaluated for their potential antitumor properties in vitro. MTT assays were used to examine the cytotoxic effects of crude extracts on five human cancer cell lines, namely MCF-7, derived from a breast carcinoma, SK-BR-3, another breast carcinoma, T24 a bladder carcinoma, Col 2, a colorectal carcinoma, and A549, a nonsmall cell lung adenocarcinoma. Hexane extracts showed remarkable cytotoxicity against MCF-7, T24, and Col 2 in a dose-dependent manner. This observation was confirmed by morphological investigation using light microscopy. Further bioassay-directed fractionation of the cytotoxic extract led to the isolation of a TLC-pure isolate labeled as f6l. Isolate f6l was further evaluated using MTT assay and morphological and biochemical investigations, which likewise showed selectivity to MCF-7, T24, and Col 2 cells with $IC_{50}$ values of 16, 17, and 17 ${\mu}g/ml$, respectively. Isolate f6l, however, showed no cytotoxicity towards the non-cancer Chinese hamster ovarian cell line (CHO-AA8). Cytochemical investigation using DAPI staining and biochemical investigation using terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL)-a method used to detect DNA fragmentation-together with caspase assay, demonstrated apoptotic cell death. Spectral characterization of isolate f6l revealed that it contained polyunsaturated fatty acid esters. Considering the cytotoxicity profile and its mode of action, f6l might represent a new promising compound with potential for development as an anticancer drug with low or no toxicity to non-cancer cells used in this study.

• Journal of the Korean Society of Tobacco Science
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• v.27 no.1 s.53
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• pp.51-58
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• 2005

The objective of this study was to evaluate the effect of cigarette filter on in vitro cytotoxicity of cigarette mainstream smoke from the cigarette. In this work, we used 3 types of cigarettes included non-filtered 2R4F cigarette, cellulose acetate-filtered 2R4F cigarette, and carbon dual-filtered 2R4F cigarette which was made from original 2R4F by replacing with an acetate filter containing carbon. The cytotoxicity of both the cigarette smoke condensate (CSC), which was collected in Cambridge filter pad, and the gas/vapor phase (GVP), which was bubbled through in phosphate-buffered saline in a gas-washing bottle, was determined using a neutral red uptake assay with CHO-K1 cells. With regard to cytotoxicity when calculated on an equal puff basis, the cytotoxicity of CSC from the filtered cigarettes was lower than that of the non filtered cigarette. Also, $EC_{50}$ vlaue of GVP from carbon filter cigarette was 40.9 puff/L, indicating the cytotoxicity to be $20\%$ lower than that of the CA filter cigarette. The cytotoxicity of the GVP was correlated to the several vapor phase components (formaldehyde, acetaldehyde, acetone, acrolein, crotonaldehyde and MEK). In conclusion, carbon filter, which significantly reduced the amount of carbonyl compounds in mainstream cigarette smoke, results in significant reductions in the cytotoxicity potential of the smoke.