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.

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).

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 Selective Cytotoxic Activities of Leaf Essential Oils from Monteverde, Costa Rica

2007 ◽  
Vol 2 (12) ◽  
pp. 1934578X0700201 ◽  
Author(s):  
Debra M. Moriarity ◽  
Anita Bansal ◽  
Ramona A. Cole ◽  
Sayaka Takaku ◽  
William A. Haber ◽  
...  
Keyword(s):  
Essential Oils ◽  
Cytotoxic Activity ◽  
Human Tumor ◽  
Persea Americana ◽  
Carcinoma Cells ◽  
Mammary Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Human Tumor Cell Lines ◽  
Adenocarcinoma Cells

The leaf essential oils of Eugenia cartagensis, Myrcia sp. nov. “fuzzy leaf”, Ocotea veraguensis, O. whitei, and Persea americana, have been obtained by hydrodistillation and the essential oil compositions determined by GC-MS. The essential oils have been screened for in-vitro cytotoxic activity against a panel of human tumor cell lines, and each of the species shows selective cytotoxic activity. E. cartagensis was active against HCT-15 and SW 620 human colorectal carcinoma cells, O. veraguensis and Myrcia “fuzzy leaf” were cytotoxic to MDA-MB-231 and MDA-MB-468 mammary adenocarcinoma cells, and O. whitei and Persea americana were toxic to M-14 melanoma cells.

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.

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.

Cytotoxicity and Molecular Targeting Study of Novel 2-Chloro-3- substituted Quinoline Derivatives as Antitumor Agents

2019 ◽  
Vol 16 (3) ◽  
pp. 273-283 ◽  
Author(s):  
Mohammed A.M. Massoud ◽  
Magda A. El-Sayed ◽  
Waleed A. Bayoumi ◽  
Basem Mansour
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Growth Factor Receptor ◽  
Human Tumor ◽  
Quinoline Derivatives ◽  
Human Tumor Cell Lines ◽  
Topoisomerase 1 ◽  
Analysis Of Results ◽  
Epidermal Growth

Background: Quinoline scaffold acts as “privileged structure” for anticancer drug design. Certain derivatives showed good results through different mechanisms as topoisomerase 1 and kinase inhibition. </P><P> Methods: A new series of 2-chloro-3-(2-amino-3-cyano-4H-chromene, 4H-pyranyl and fused 1- cyclohexen-4-yl)quinoline structures (3-5, 6 and 7) were designed, synthesized, and evaluated for their in vitro antitumor activity. All compounds were tested by MTT assay against a panel of four different human tumor cell lines. The inhibitory activity of selected compounds was assessed on topoisomerase 1 and epidermal growth factor receptor tyrosine kinase via ELISA. In addition, compounds 7b and 3a were docked into the X-ray crystal structure of Topo 1 and EGFR enzymes, respectively to explain the molecular basis of the potent activity. </P><P> Results: Compounds 3a, 3b and 7b showed characteristic efficacy profile. 7b showed the best cytotoxic activity on all types of tested cell lines with IC50 range (15.8&#177;1.30 to 28.2&#177;3.37 &#181;M), relative to 5-fluoruracil of IC50 range (40.7&#177;2.46 to 63.8&#177;2.69 &#181;M). Via ELISA, 7b and 3a showed characteristic inhibition profile on Topo 1 and EGFR-TK respectively. In addition, 7b has scored binding energy (101.61 kcal/mol) and six hydrogen bonds with amino acids conserved residues in the enzyme pocket. </P><P> Conclusion: Analysis of results revealed that compounds 7a and 7b mainly were Topo 1 inhibitors while 3a was mainly EGFR inhibitor. This property may be exploited to design future quinoline derivatives as antitumor agents with enhanced selectivity towards either of the two molecular targets.

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.

scholarly journals Pharmacoinformatics and Preclinical Studies of NSC765690 and NSC765599, Potential STAT3/CDK2/4/6 Inhibitors with Antitumor Activities against NCI60 Human Tumor Cell Lines

Biomedicines ◽  
2021 ◽  
Vol 9 (1) ◽  
pp. 92
Author(s):  
Bashir Lawal ◽  
Yen-Lin Liu ◽  
Ntlotlang Mokgautsi ◽  
Harshita Khedkar ◽  
Maryam Rachmawati Sumitra ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Tumor ◽  
Cancer Cell Lines ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Anti Cancer

Signal transducer and activator of transcription 3 (STAT3) is a transcriptional regulator of a number of biological processes including cell differentiation, proliferation, survival, and angiogenesis, while cyclin-dependent kinases (CDKs) are a critical regulator of cell cycle progression. These proteins appear to play central roles in angiogenesis and cell survival and are widely implicated in tumor progression. In this study, we used the well-characterized US National Cancer Institute 60 (NCI60) human tumor cell lines to screen the in vitro anti-cancer activities of our novel small molecule derivatives (NSC765690 and NSC765599) of salicylanilide. Furthermore, we used the DTP-COMPARE algorithm and in silico drug target prediction to identify the potential molecular targets, and finally, we used molecular docking to assess the interaction between the compounds and prominent potential targets. We found that NSC765690 and NSC765599 exhibited an anti-proliferative effect against the 60 panels of NCI human cancer cell lines, and dose-dependent cytotoxic preference for NSCLC, melanoma, renal, and breast cancer cell lines. Protein–ligand interactions studies revealed that NSC765690 and NSC765599 were favored ligands for STAT3/CDK2/4/6. Moreover, cyclization of the salicylanilide core scaffold of NSC765690 mediated its higher anti-cancer activities and had greater potential to interact with STAT3/CDK2/4/6 than did NSC765599 with an open-ring structure. NSC765690 and NSC765599 met the required safety and criteria of a good drug candidate, and are thus worthy of further in-vitro and in-vivo investigations in tumor-bearing mice to assess their full therapeutic efficacy.

Antitumor Agents. 192. Antitubulin Effect and Cytotoxicity of C(7)-Oxygenated Allocolchicinoids

1999 ◽  
Vol 64 (2) ◽  
pp. 217-228 ◽  
Author(s):  
Jian Guan ◽  
Xiao-Kang Zhu ◽  
Arnold Brossi ◽  
Yoko Tachibana ◽  
Kenneth F. Bastow ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Human Tumor ◽  
Crystallographic Analysis ◽  
Antitumor Activities ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
X Ray ◽  
Tubulin Binding ◽  
Marked Resistance

Two allocolchicinoids 6 and 8, prepared from colchicine, together with allo compounds 9-11, made from 6 by reduction and regiodemethylation, were evaluated for antitubulin and antitumor activities. Structures of 6, 8, and 10 were confirmed by X-ray crystallographic analysis. Compounds 6, 8, and 9 have high tubulin binding affinity and display potent inhibitory activities against tubulin polymerization and solid human tumor cell lines. Particularly, drug-resistant KB cell lines, including KB-7d, KB-VCR, and KB-CPT, do not show marked resistance to these compounds.

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