scholarly journals Two New p-Terphenyl Derivatives from the Marine Fungal Strain Aspergillus sp. AF119

2012 ◽  
Vol 7 (8) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Shao-Song Liu ◽  
Bao-Bing Zhao ◽  
Chun-Hua Lu ◽  
Jing-Jing Huang ◽  
Yue-Mao Shen
Keyword(s):  
Cell Lines ◽  
Human Tumor ◽  
2D Nmr ◽  
Strand Break ◽  
Fungal Strain ◽  
Cytotoxic Activities ◽  
Cycle Arrest ◽  
Dna Double Strand Break ◽  
Aspergillus Sp

Two new p-terphenyl derivatives (1, 2), together with six known ones (3 - 8), have been isolated from the marine fungal strain Aspergillus sp. AF119. The structures for terphyl acid (1) and terphyl diacid (2) were determined on the basis of HR Q-TOF-MS, and 1D- and 2D-NMR spectroscopic data. The in vitro cytotoxic activities of compounds 1 – 8 were tested against human tumor cell lines HeLa, HepG-2 and MDA-MB-435; only compounds 5 – 8 exhibited inhibitory activity against the tested cell lines with IC50 values < 20 μM. Moreover, compound 5 showed a mechanism of inducing cell cycle arrest and apoptosis mediated by the generation of ROS and subsequent DNA double-strand break.

Synthesis and Characterization of New Palladium(II) Complexes with Ligands Derived from Furan-2-carbaldehyde and Benzaldehyde Thiosemicarbazone and their in vitro Cytotoxic Activities against Various Human Tumor Cell Lines

2010 ◽  
Vol 65 (10) ◽  
pp. 1271-1278 ◽  
Author(s):  
Wilfredo Hernández ◽  
Juan Paz ◽  
Fernando Carrasco ◽  
Abraham Vaisberg ◽  
Jorge Manzur ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Myelogenous Leukemia ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

With the ligands 4-phenyl-1-(furan-2-carbaldehyde)thiosemicarbazone, HTSC1, (1), 4-phenyl-1- (5´-phenyl-furan-2-carbaldehyde)thiosemicarbazone, HTSC2 (2), o-methoxy-benzaldehydethiosemicarbazone, HTSC3 (3), and o-cyano-benzaldehydethiosemicarbazone, HTSC4 (4), the corresponding palladium(II) complexes, Pd(TSC1)2 (5), Pd(TSC2)2 (6), Pd(TSC3)2 (7), and Pd(TSC4)2 (8) were synthesized and characterized by elemental analysis and spectroscopic techniques. The crystal structure of Pd(TSC3)2 (7) was determined by single-crystal X-ray diffraction. Complex 7 shows a squareplanar geometry, where two deprotonated ligands are coordinated to the PdII center through the nitrogen and sulfur atoms in a trans arrangement. In vitro antitumor studies against different human tumor cell lines have revealed that the palladium(II) complexes 5- 8 are more cytotoxic (IC50 values in the range of 0.21 - 3.79 μM) than their corresponding ligands (1 - 4) (> 60 μM). These results indicate that the antiproliferative activity is enhanced when thiosemicarbazone ligands are coordinated to the metal. Among the studied palladium(II) complexes, 8 exhibits high antitumor activity on K562 chronic myelogenous leukemia cells with a low value of the inhibitory concentration (IC50 = 0.21 μM).

scholarly journals Four New Pterosins from Pteris cretica and Their Cytotoxic Activities

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2767
Author(s):  
Jian Lu ◽  
Caiying Peng ◽  
Shuang Cheng ◽  
Jianqun Liu ◽  
Qinge Ma ◽  
...  
Keyword(s):  
Human Tumor ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
Aerial Parts ◽  
Pteris Cretica ◽  
Phytochemical Investigation ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
New Compounds

Phytochemical investigation of the aerial parts of Pteris cretica led to the isolation and elucidation of nine pterosins, including four new pterosins, creticolacton A (1), 13-hydroxy-2(R),3(R)-pterosin L (2), creticoside A (3), and spelosin 3-O-β-d-glucopyranoside (4), together with five known pterosins 5–9. Their structures were identified mainly on the basis of 1D and 2D NMR spectral data, ESI-MS and literature comparisons. Compounds 1 and 3 were new type of petrosins with a six membered ring between C-14 and C-15. The new compounds were tested in vitro for their cytotoxic activities against four human tumor cell lines (SH-SY5Y, SGC-7901, HCT-116, Lovo). Results showed that compounds 1 and 2 exhibited cytotoxic activity against HCT-116 cells with IC50 value of 22.4 μM and 15.8 μM, respectively.

scholarly journals Cytotoxic Polyketides from a Deep-Sea Sediment Derived Fungus Diaporthe phaseolorum FS431

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3062 ◽  
Author(s):  
Zheng Niu ◽  
Yuchan Chen ◽  
Heng Guo ◽  
Sai-Ni Li ◽  
Hao-Hua Li ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Deep Sea ◽  
Human Tumor ◽  
Electron Capture Detection ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Deep Sea Sediment ◽  
Diaporthe Phaseolorum

Two new chromone-derived polyketides phaseolorins, G and H (1 and 2), and one new anthraquinone derivative, phaseolorin I (3), together with three known compounds (4–6), were isolated from the deep-sea sediment-derived fungus Diaporthe phaseolorum FS431. The structures of the new compounds were determined by comprehensive analysis of their spectroscopic data, and the absolute configuration of 1 was established by quantum chemical calculations of electron capture detection (ECD). All the isolated compounds (1–6) were tested for their in vitro cytotoxic activities against four human tumor cell lines, of which compound 4 exhibited significant effect against MCF-7, HepG-2, and A549 tumor cell lines with IC50 values of 2.60, 2.55, and 4.64 µM, respectively.

scholarly journals Chemical Composition, Antimicrobial, and Cytotoxic Activities of Leaf, Fruit, and Branch Essential Oils Obtained From Zanthoxylum nitidum Grown in Vietnam

2021 ◽  
Vol 16 (1) ◽  
pp. 1934578X2098564
Author(s):  
Tran Thi Tuyen ◽  
Pham Minh Quan ◽  
Vu Thi Thu Le ◽  
Tran Quoc Toan ◽  
Do Huu Nghi ◽  
...  
Keyword(s):  
Essential Oils ◽  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Cytotoxic Activities ◽  
Human Tumor Cell Lines ◽  
Flame Ionization ◽  
Germacrene D ◽  
Zanthoxylum Nitidum

Zanthoxylum nitidum (Roxb.) DC is a traditional Vietnamese medicine to treat coughs, stomachache, toothache, blood stagnation, and sore throats. The essential oils (EOs) of the leaves, fruits, and stems of this plant were extracted by hydrodistillation and subjected to analysis by gas chromatography (GC)-flame ionization detector (FID) and GC-mass spectrometry (MS). The isolated EOs were then evaluated in terms of their antimicrobial activity by minimum inhibitory concentration (MIC) assay and in vitro cytotoxic effect against 5 human tumor cell lines. GC-MS-FID analysis showed 35, 32, and 25 compounds accounting for 97.6%, 91.7%, and 96.2% of the total EO contents from the leaves, fruits, and stems, respectively. The major compounds of the leaf EO were limonene (44.3%), β-caryophyllene (12.5%), linalool (11.0%), germacrene D (5.3%), and α-pinene (4.9%); the major compounds of the fruit EO were n-pentadecane (34.8%), sabinene (18.3%), and n-heptadecane (4.7%), and the major components of the stem EO were 2-undecanone (72.3%), β-caryophyllene (5.8%), and germacrene D (4.0%). The EOs of leaves, fruits, and stems of Z. nitidum exhibited antibacterial activity against Bacillus subtilis, Escherichia coli, and Fusarium oxysporum with MIC values of 100 µg/mL. The leaf and branch EOs exhibited cytotoxic activity against all tested cancer cell lines, especially A-549 and HepG-2. Findings from the present study provide important knowledge about the potential uses of Z. nitidum EOs as a natural antibacterial and antitumor agents.

Cytotoxic Activities of Total Saponins from Plena Clematis on Human Tumor Cell Lines In Vitro

2018 ◽  
Vol 24 (10) ◽  
pp. 763-767 ◽  
Author(s):  
Fu-rong Zhu ◽  
Yong-ning Li ◽  
Shu-lan He ◽  
Qian-shun Chen ◽  
Xun-yu Xu
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

scholarly journals Synthesis, Characterization, and In Vitro Cytotoxic Activities of Benzaldehyde Thiosemicarbazone Derivatives and Their Palladium(II) and Platinum(II) Complexes against Various Human Tumor Cell Lines

2008 ◽  
Vol 2008 ◽  
pp. 1-9 ◽  
Author(s):  
Wilfredo Hernández ◽  
Juan Paz ◽  
Abraham Vaisberg ◽  
Evgenia Spodine ◽  
Rainer Richter ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Planar Geometry ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Benzaldehyde Thiosemicarbazone

The palladium(II) bis-chelate Pd(L1−3)2and platinum(II) tetranuclearPt4(L4)4complexes of benzaldehyde thiosemicarbazone derivatives have been synthesized, and characterized by elemental analysis and IR, FAB(+)-mass and NMR(1H,13C)spectroscopy. The complexPd(L2)2[HL2=m-CN-benzaldehyde thiosemicarbazone] shows a square-planar geometry with two deprotonated ligands (L) coordinated toPdIIthrough the nitrogen and sulphur atoms in atransarrangement, while the complexPt4(L4)4[HL4=4-phenyl-1-benzaldehyde thiosemicarbazone] has a tetranuclear geometry with four tridentate ligands coordinated to fourPtIIions through the carbon (aromatic ring), nitrogen, and sulphur atoms where the ligands are deprotonated at the NH group. The in vitro antitumor activity of the ligands and their complexes was determined against different human tumor cell lines, which revealed that the palladium(II) and platinum(II) complexes are more cytotoxic than their ligands withIC50values at the range of 0.07–3.67 μM. The tetranuclear complexPt4(L4)4, with the phenyl group in the terminal amine of the ligand, showed higher antiproliferative activity (CI50= 0.07–0.12 μM) than the other tested palladium(II) complexes.

scholarly journals Chemical Constituents of Tibetan Herbal Medicine Pulicaria insignis and Their in vitro Cytotoxic Activities

2020 ◽  
Vol 15 (2) ◽  
pp. 91-102
Author(s):  
Xinzhu Wang ◽  
Peilei Hou ◽  
Yanbo Qu ◽  
Rizhen Huang ◽  
Yan Feng ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Cell Lines ◽  
Hepg2 Cells ◽  
Chemical Constituents ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
Hela Cell Lines ◽  
Ic50 Values ◽  
Hepg2 Cell Lines

One new phenolic derivative, 1-(4',5'-dihydroxy-2'-methylphenyl)-pentane-1,4-dione (1), along with eighteen known compounds including eight sesquiterpenoids (2–9), one triterpenoid (10), one bisdpoxylignan (11), one coumarin (12), and seven flavonoids (13–19) were isolated from the dried inflorescence of Tibetan herbal medicine Pulicaria insignis. The structure of 1 was established by spectroscopic methods, including HRESIMS, IR, 1D, and 2D NMR. All isolates were assessed for the cytotoxic activities against MGC-803, T24, HepG2, and HeLa cell lines using the MTT assay. The results showed that compound 1 displayed moderate cytotoxicity against Hela and HepG2, and compounds 3, 4, 5, 6, and 13 exhibited potential cytotoxic activities against the four cell lines with IC50 values ranging from 3.05 to 14.37 μM. Notably, compound 5 exhibited significant anti-proliferative activities against HepG2 cell lines with the IC50 values of 3.05 ± 0.36 μM. Further bioactivity investigation showed that compound 5 could block HepG2 cells in the G1 phase of the cell cycle, thereby inhibiting the growth of HepG2 cells and inducing apoptosis in HepG2 cells.

Novel Thiazine Substituted 9-Anilinoacridines: Synthesis, Antitumour Activity and Structure Activity Relationships

2019 ◽  
Vol 19 (11) ◽  
pp. 1350-1358 ◽  
Author(s):  
R. Kalirajan ◽  
K. Gaurav ◽  
A. Pandiselvi ◽  
B. Gowramma ◽  
S. Sankar
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Antitumour Activity ◽  
Human Tumor ◽  
Cytotoxic Activities ◽  
Anti Tumour Activity ◽  
Tumour Activity

Background: 9-anilinoacridines are acting as DNA-intercalating agents which plays an important role as antitumor drugs, due to their anti-proliferative properties. Some anticancer agents contain 9- anilinoacridines such as amsacrine (m-AMSA), and nitracrine (Ledakrine) have been already developed. Methods: In this study, novel 9-anilinoacridines substituted with thiazines 4a-r were designed, synthesized, characterized by physical and spectral data and their cytotoxic activities against DLA cell lines were evaluated. Results: Among those compounds, 4b, c, e, g, i, j, k, m, o, p, q, r exhibited significant short term in vitro cytotoxic activity against Daltons lymphoma ascites (DLA) cells with CTC50 value of 0.18 to 0.31μM. The compounds 4b, c, e, g, i, j, k, m, o, p, q, r are also exhibited significant long term in vitro anti-tumour activity against human tumor cell lines, HEp-2 (laryngeal epithelial carcinoma) by Sulforhodamine B assay with CTC50 value of 0.20 to 0.39μM. The compounds 4b, i, j exhibited significant in vivo antitumor activity with % Increase in Life Span (ILS) 48-82%. Conclusion: Results obtained in this study clearly demonstrated that many of the thiazine substituted 9- anilinoacridines exert interesting anti-tumour activity. The compounds 4b, i, j have significant anti-tumour activity and useful drugs after further refinement. The above derivatives will encourage to design future antitumor agents with high therapeutic potentials.

scholarly journals New Polyenes from the Marine-Derived Fungus Talaromyces cyanescens with Anti-Neuroinflammatory and Cytotoxic Activities

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 836
Author(s):  
Hee Jae Shin ◽  
Cao Van Anh ◽  
Duk-Yeon Cho ◽  
Dong-Kug Choi ◽  
Jong Soon Kang ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
2D Nmr ◽  
Cancer Cell Lines ◽  
Marine Fungus ◽  
Cytotoxic Activities ◽  
Two Dimensional ◽  
One Dimensional

Three new polyene compounds, talacyanols A–C (1–3), along with two known compounds, ramulosin (4) and eurothiocin A (5), were isolated from the marine fungus Talaromyces cyanescens derived from a seaweed Caulerpa sp. Structures of 1–5 were established by one-dimensional and two-dimensional (1D/2D) NMR, HR-ESIMS, and the modified Mosher’s methods, as well as comparison with previously reported literature data. All the compounds (1–5) were tested for their in vitro cytotoxic and anti-neuroinflammatory activities. Among them, 1 showed moderate cytotoxic activity against a panel of cancer cell lines (HCT-15, NUGC-3, NCI-H23, ACHN, PC-3, and MDA-MB-231) with GI50 values ranging from 44.4 to 91.6 μM, whereas compounds 2 and 5 exhibited anti-neuroinflammatory effect without cytotoxicity against all the tested cell lines.

Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone

2020 ◽  
Vol 17 (4) ◽  
pp. 512-517
Author(s):  
Ognyan Ivanov Petrov ◽  
Yordanka Borisova Ivanova ◽  
Mariana Stefanova Gerova ◽  
Georgi Tsvetanov Momekov
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Biological Activities ◽  
Human Tumor ◽  
Mannich Bases ◽  
In Vitro Cytotoxicity ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.

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