Antitumor Effect of the Essential Oil from the Leaves of Croton matourensis Aubl. (Euphorbiaceae)

Croton matourensis Aubl. (synonym Croton lanjouwensis Jabl.), popularly known as “orelha de burro”, “maravuvuia”, and/or “sangrad’água”, is a medicinal plant used in Brazilian folk medicine as a depurative and in the treatment of infections, fractures, and colds. In this work, we investigated the chemical composition and in vitro cytotoxic and in vivo antitumor effects of the essential oil (EO) from the leaves of C. matourensis collected from the Amazon rainforest. The EO was obtained by hydrodistillation using a Clevenger-type apparatus and characterized qualitatively and quantitatively by gas chromatography coupled to mass spectrometry (GC–MS) and gas chromatography with flame ionization detection (GC–FID), respectively. In vitro cytotoxicity of the EO was assessed in cancer cell lines (MCF-7, HCT116, HepG2, and HL-60) and the non-cancer cell line (MRC-5) using the Alamar blue assay. Furthermore, annexin V-FITC/PI staining and the cell cycle distribution were evaluated with EO-treated HepG2 cells by flow cytometry. In vivo efficacy of the EO (40 and 80 mg/kg/day) was demonstrated in C.B-17 severe combined immunodeficient (SCID) mice with HepG2 cell xenografts. The EO included β-caryophyllene, thunbergol, cembrene, p-cymene, and β-elemene as major constituents. The EO exhibited promising cytotoxicity and was able to cause phosphatidylserine externalization and DNA fragmentation without loss of the cell membrane integrity in HepG2 cells. In vivo tumor mass inhibition rates of the EO were 34.6% to 55.9%. Altogether, these data indicate the anticancer potential effect of C. matourensis.

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Cytotoxic and antitumoral activity of N-(9H-purin-6-yl) benzamide derivatives and related water-soluble prodrugs

Current Molecular Pharmacology ◽

10.2174/1874467214666211014164406 ◽

2021 ◽

Vol 14 ◽

Author(s):

Emeline Cros-Perrial ◽

Steve Saulnier ◽

Muhammad Zawwad Raza ◽

Rémi Charmelot ◽

David Egron ◽

...

Keyword(s):

Cancer Cell ◽

Molecular Mechanisms ◽

Biological Evaluation ◽

Water Soluble ◽

Antitumoral Activity ◽

Cell Cycle Distribution ◽

Synergistic Activity ◽

Benzamide Derivatives

Background: The development of small molecules as cancer treatments is still of both interest and importance. Objective: Having synthesized and identified the initial cytotoxic activity of a series of chemically related N-(9H-purin-6-yl) benzamide derivatives, we continued their evaluation on cancer cell models. We also synthesized water-soluble prodrugs of the main compound and performed in vivo experiments. Method: We used organic chemistry to obtain compounds of interest and prodrugs. The biological evaluation included MTT assays, synergy experiments, proliferation assays by CFSE, cell cycle distribution and in vivo antitumoral activity. Results: Our results show activities on cancer cell lines ranging from 3-39 µM for the best compounds, with both induction of apoptosis and decrease in cell proliferation. Two compounds evaluated in vivo showed weak antitumoral activity. In addition, the lead compound and its prodrug had a synergistic activity with the nucleoside analogue fludarabine in vitro and in vivo. Conclusion: Our work allowed us to gain better knowledge on the activity of N-(9H-purin-6-yl) benzamide derivatives and showed new examples of water-soluble prodrugs. More research is warranted to decipher the molecular mechanisms of the molecules.

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Improvement in the Anti-Tumor Efficacy of Doxorubicin Nanosponges in In Vitro and in Mice Bearing Breast Tumor Models

Cancers ◽

10.3390/cancers12010162 ◽

2020 ◽

Vol 12 (1) ◽

pp. 162 ◽

Cited By ~ 4

Author(s):

Monica Argenziano ◽

Casimiro Luca Gigliotti ◽

Nausicaa Clemente ◽

Elena Boggio ◽

Benedetta Ferrara ◽

...

Keyword(s):

Breast Cancer ◽

Cancer Cell ◽

Substantial Reduction ◽

Cancer Growth ◽

Breast Cancer Cell Lines ◽

Cell Cycle Distribution ◽

High Accumulation ◽

New Formulation

Doxorubicin (DOX) is an anthracycline widely used in cancer therapy and in particular in breast cancer treatment. The treatment with DOX appears successful, but it is limited by a severe cardiotoxicity. This work evaluated the in vitro and in vivo anticancer effect of a new formulation of β-cyclodextrin nanosponges containing DOX (BNS-DOX). The BNS-DOX effectiveness was evaluated in human and mouse breast cancer cell lines in vitro in terms of effect on cell growth, cell cycle distribution, and apoptosis induction; and in vivo in BALB-neuT mice developing spontaneous breast cancer in terms of biodistribution, cancer growth inhibition, and heart toxicity. BNS-DOX significantly inhibited cancer cell proliferation, through the induction of apoptosis, with higher efficiency than free DOX. The breast cancer growth in BALB-neuT mice was inhibited by 60% by a BNS-DOX dose five times lower than the DOX therapeutic dose, with substantial reduction of tumor neoangiogenesis and lymphangiogenesis. Biodistribution after BNS-DOX treatment revealed a high accumulation of DOX in the tumor site and a low accumulation in the hearts of mice. Results indicated that use of BNS may be an efficient strategy to deliver DOX in the treatment of breast cancer, since it improves the anti-cancer effectiveness and reduces cardiotoxicity.

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Cyperus articulatus L. (Cyperaceae) Rhizome Essential Oil Causes Cell Cycle Arrest in the G2/M Phase and Cell Death in HepG2 Cells and Inhibits the Development of Tumors in a Xenograft Model

Molecules ◽

10.3390/molecules25112687 ◽

2020 ◽

Vol 25 (11) ◽

pp. 2687

Author(s):

Mateus L. Nogueira ◽

Emilly J. S. P. de Lima ◽

Asenate A. X. Adrião ◽

Sheila S. Fontes ◽

Valdenizia R. Silva ◽

...

Keyword(s):

Cell Cycle ◽

Gas Chromatography ◽

Cell Death ◽

Liver Cancer ◽

Essential Oil ◽

Cell Cycle Arrest ◽

Cell Lines ◽

Hepg2 Cells ◽

Cycle Arrest

Cyperus articulatus L. (Cyperaceae), popularly known in Brazil as “priprioca” or “piriprioca”, is a tropical and subtropical plant used in popular medical practices to treat many diseases, including cancer. In this study, C. articulatus rhizome essential oil (EO), collected from the Brazilian Amazon rainforest, was addressed in relation to its chemical composition, induction of cell death in vitro and inhibition of tumor development in vivo, using human hepatocellular carcinoma HepG2 cells as a cell model. EO was obtained by hydrodistillation using a Clevenger-type apparatus and characterized qualitatively and quantitatively by gas chromatography coupled to mass spectrometry (GC-MS) and gas chromatography with flame ionization detection (GC-FID), respectively. The cytotoxic activity of EO was examined against five cancer cell lines (HepG2, HCT116, MCF-7, HL-60 and B16-F10) and one non-cancerous one (MRC-5) using the Alamar blue assay. Cell cycle distribution and cell death were investigated using flow cytometry in HepG2 cells treated with EO after 24, 48 and 72 h of incubation. The cells were also stained with May–Grunwald–Giemsa to analyze the morphological changes. The anti-liver-cancer activity of EO in vivo was evaluated in C.B-17 severe combined immunodeficient (SCID) mice with HepG2 cell xenografts. The main representative substances of this EO sample were muskatone (11.6%), cyclocolorenone (10.3%), α-pinene (8.26%), pogostol (6.36%), α-copaene (4.83%) and caryophyllene oxide (4.82%). EO showed IC50 values for cancer cell lines ranging from 28.5 µg/mL for HepG2 to >50 µg/mL for HCT116, and an IC50 value for non-cancerous of 46.0 µg/mL (MRC-5), showing selectivity indices below 2-fold for all cancer cells tested. HepG2 cells treated with EO showed cell cycle arrest at G2/M along with internucleosomal DNA fragmentation. The morphological alterations included cell shrinkage and chromatin condensation. Treatment with EO also increased the percentage of apoptotic-like cells. The in vivo tumor mass inhibition rates of EO were 46.5–50.0%. The results obtained indicate the anti-liver-cancer potential of C. articulatus rhizome EO.

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Chemical characterization and determination of in vivo and in vitro antifungal activity of essential oils from four Eucalyptus species against the Hemileia vastatrix Berk and Br fungus, the agent of coffee leaf rust

Australian Journal of Crop Science ◽

10.21475/ajcs.20.14.09.p2249 ◽

2020 ◽

pp. 1379-1384

Author(s):

Alex Rodrigues Silva Caetano ◽

Sara Maria Chalfoun ◽

Mario Lúcio Vilela Resende ◽

Caroline Lima Angélico ◽

Wilder Douglas Santiago ◽

...

Keyword(s):

Gas Chromatography ◽

Antifungal Activity ◽

Essential Oil ◽

Essential Oils ◽

Chemical Characterization ◽

Eucalyptus Species ◽

Hemileia Vastatrix ◽

Antifungal Activities

Essential oils, also known as volatile oils, are substances produced through the secondary metabolism of plants. In this study, we determined the chemical composition and the in vitro and in vivo antifungal activity of the essential oils from four species of Eucalyptus, Eucalyptus citriodora, Eucalyptus camaldulensis, Eucalyptus grandis and Eucalyptus microcorys, against the Hemileia vastatrix fungus. The essential oils from these four species of Eucalyptus were extracted from their leaves by the hydrodistillation technique using a modified Clevenger apparatus. The chemical characterization was performed by gas chromatography coupled with a mass spectrometer detector and by gas chromatography using a flame ionization detector. The antifungal activities of the essential oils against H. vastatrix were studied by evaluating the percentage of spore germination using the microdilution test for in vitro assays. The curative and preventive effects were evaluated in in vivo tests. The principal constituents of the essential oil from E. citriodora were citronellal, citronellol and isopulegol, while E. camaldulensis produced 1,8-cineole, α-terpineol and α-pinene. 1,8-cineole, α-pinene and α-terpineol were obtained from E. grandis and 1,8-cineole, α-pinene and trans-pinocarveol were the principal components in the essential oil of E. microcorys. In vitro and in vivo antifungal activities against the fungus under study were observed for most of the essential oils, except the essential oil from E. microcorys, for which no preventive antifungal activity was observed. Only the curing of infection by the H. vastatrix fungus was observed with this oil.

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Synergistic antitumor effects of S-1 with eribulin in vitro and in vivo for triple-negative breast cancer cell lines

SpringerPlus ◽

10.1186/2193-1801-3-417 ◽

2014 ◽

Vol 3 (1) ◽

pp. 417 ◽

Cited By ~ 15

Author(s):

Masato Terashima ◽

Kazuko Sakai ◽

Yosuke Togashi ◽

Hidetoshi Hayashi ◽

Marco A De Velasco ◽

...

Keyword(s):

Breast Cancer ◽

Cell Lines ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Triple Negative Breast Cancer ◽

Triple Negative ◽

Breast Cancer Cell Lines ◽

Antitumor Effects

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In Vitro Cytotoxicity and Apoptotic Assay of Eucalyptus globulus Essential Oil in Colon and Liver Cancer Cell Lines

Journal of Gastrointestinal Cancer ◽

10.1007/s12029-021-00601-5 ◽

2021 ◽

Author(s):

Hajar Khazraei ◽

Seyedeh Azra Shamsdin ◽

Mozhdeh Zamani

Keyword(s):

Liver Cancer ◽

Essential Oil ◽

Cell Lines ◽

Cancer Cell ◽

Eucalyptus Globulus ◽

Cancer Cell Lines ◽

In Vitro Cytotoxicity ◽

Liver Cancer Cell

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In Vitro Activity of Foeniculum vulgare and Its Main Essential Oil Component Trans-Anethole on Trichomonas vaginalis

Iranian Journal of Parasitology ◽

10.18502/ijpa.v14i4.2106 ◽

2019 ◽

Author(s):

Faezeh KARAMI ◽

Dara DASTAN ◽

Mohammad FALLAH ◽

Mohammad MATINI

Keyword(s):

Gas Chromatography ◽

Essential Oil ◽

Trichomonas Vaginalis ◽

Vitro Activity ◽

Gas Chromatography Mass Spectrometry ◽

Major Constituent ◽

In Vitro Activity ◽

Foeniculum Vulgare

Background: Trichomoniasis is one of the most common nonviral sexually transmitted infections worldwide which drug-resistant cases of the infection are rising. The aim of the study was to assessment the in vitro activity of Foeniculum vulgare and its main essential oil component on Trichomonas vaginalis. Also phytochemical investigation of F. vulgare essential oil was performed. Methods: Five T. vaginalis isolates subjected to susceptibility testing against essential oil and extracts of F. vulgare and anethole using microtiter plate method. The minimum lethal concentration (MLC) of the natural products was assessed in comparison with metronidazole. Gas chromatography-mass spectrometry and gas chromatography-flame ionization detector was applied for chemical investigation of the essential oil. Results: After 48 hours incubation, the most potent antitrichomonal agents were the methanolic and hexanic extract with MLC of 360 µg/ml and followed by the essential oil and anethole (1600 µg/ml). The isolates were sensitive to metronidazole with a mean MLC of 13.7 µg/ml. E-Anethole (88.41 %) was the major constituent of F. vulgare essential oil. Conclusion: The results suggested in vitro antiprotozoal properties of F. vulgare and anethole against T. vaginalis. Therefore further studies are needed to evaluate their in vivo effects and toxicity.

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Antifungal Activity of Essential Oil and Hydrosol Extract of Ballota nigra L. and their Protective Effects Against the Black Rot of Tomatoes

Current Nutrition & Food Science ◽

10.2174/1573401314666180515114935 ◽

2019 ◽

Vol 15 (7) ◽

pp. 662-671 ◽

Cited By ~ 1

Author(s):

Nabila A. Sebaa ◽

Amina T. Zatla ◽

Mohammed E.A. Dib ◽

Boufeldja Tabti ◽

Jean Costa ◽

...

Keyword(s):

Gas Chromatography ◽

Antifungal Activity ◽

Essential Oil ◽

Essential Oils ◽

Alternaria Alternata ◽

Penicillium Expansum ◽

Protective Effects ◽

Antifungal Activities

Background: Bellota species are used to treat various diseases in traditional folk medicine. Objectives: This study aimed to chemically characterize the essential oils and the hydrosol extract and regional specificity of the major components of Ballota nigra essential oil and to evaluate their in vitro and in vivo antifungal activities. Methods: Essential oils were obtained by a Clevenger-type apparatus and analyzed by using Gas Chromatography (GC) and Gas Chromatography Mass Spectroscopy (GC/MS). The antifungal activities were tested to three phytopathogenic stains (Penicillium expansum, Aspergillus niger and Alternaria alternata). Results: Altogether, 38 compounds were identified in the essential oils, representing 92.1-96.8% of the total oil composition. Their main constituents were E-β-caryophyllene (4.8-24.6%), E-β-farnesene (3.3-22.9%), β-bisabolene (7.6-30.2%), α-humulene (2.1-13.3%) and geranyl linalool (1.1-8.2%). The statistical methods deployed confirmed that there is a relation between the essential oil compositions and the harvest locations. Hydrosol extract was constituted by seven components, represented principally by methyl eugenol (75.2%) and caryophyllene oxide (12.5%). The results of in vitro antifungal activity with essential oil and hydrosol extract have shown very interesting antifungal activities on Penicillium expansum and Alternaria alternata strains with percentage reductions up to 80%. Additionally, in in vivo assays, Ballota nigra essential oil and hydrosol extract significantly reduce decay in artificially inoculated tomato by Alternaria alternata. Conclusion: The essential oil and hydrosol extract can be used as a potential source of sustainable eco-friendly botanical fungicides to protect stored tomatoes from pathogens, saprophytic fungi causing bio-deterioration to a variety of food commodities.

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