scholarly journals Toxicity and Antitumor Activity of a Thiophene–Acridine Hybrid

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 64 ◽  
Author(s):  
Thaís Lisboa ◽  
Daiana Silva ◽  
Sâmia Duarte ◽  
Rafael Ferreira ◽  
Camyla Andrade ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Leukemia Cell Line ◽  
Zebrafish Embryos ◽  
Cell Line Hela ◽  
Hct 116

The antitumor effects of thiophene and acridine compounds have been described; however, the clinical usefulness of these compounds is limited due to the risk of high toxicity and drug resistance. The strategy of molecular hybridization presents the opportunity to develop new drugs which may display better target affinity and less serious side effects. Herein, 2-((6-Chloro-2-methoxy-acridin-9-yl)amino)-5,6,7,8-tetrahydro-4H-cyclohepta[b]-thiophene-3-carbonitrile (ACS03), a hybrid thiophene–acridine compound with antileishmanial activity, was tested for toxicity and antitumor activity. The toxicity was evaluated in vitro (on HaCat and peripheral blood mononuclear cells) and in vivo (zebrafish embryos and acute toxicity in mice). Antitumor activity was also assessed in vitro in HCT-116 (human colon carcinoma cell line), K562 (chronic myeloid leukemic cell line), HL-60 (human promyelocytic leukemia cell line), HeLa (human cervical cancer cell line), and MCF-7 (breast cancer cell line) and in vivo (Ehrlich ascites carcinoma model). ACS03 exhibited selectivity toward HCT-116 cells (Half maximal inhibitory concentration, IC50 = 23.11 ± 1.03 µM). In zebrafish embryos, ACS03 induced an increase in lactate dehydrogenase, glutathione S-transferase, and acetylcholinesterase activities. The LD50 (lethal dose 50%) value in mice was estimated to be higher than 5000 mg/kg (intraperitoneally). In vivo, ACS03 (12.5 mg/kg) induced a significant reduction in tumor volume and cell viability. In vivo antitumor activity was associated with the nitric oxide cytotoxic effect. In conclusion, significant antitumor activity and weak toxicity were recorded for this hybrid compound, characterizing it as a potential anticancer compound.

Antitumor activity of a polysaccharide from longan seed on lung cancer cell line A549 in vitro and in vivo

Tumor Biology ◽  
2014 ◽  
Vol 35 (7) ◽  
pp. 7259-7266 ◽  
Author(s):  
Hongmin Wang ◽  
Xiaohong Zhang ◽  
Yuexia Li ◽  
Ruiying Chen ◽  
Songyun Ouyang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Antitumor Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Lung Cancer Cell Line ◽  
Lung Cancer Cell ◽  
Longan Seed

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

scholarly journals In vitro antineoplastic activity in triple-negative breast cancer cell line and in vivo

2014 ◽  
Vol 8 (Suppl 4) ◽  
pp. P22
Author(s):  
Klesia Madeira ◽  
Murilo Cerri ◽  
Renata Daltoé ◽  
Alice Herlinger ◽  
João Filho ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Triple Negative Breast Cancer ◽  
Breast Cancer Cell Line ◽  
Triple Negative ◽  
Cancer Cell Line

Analysis on Homoeopathic Preparation of Asterias Rubens for Evaluating Anti Breast Cancer Cell Line using Similia Principle

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 805-808
Author(s):  
Ravikumar Raju ◽  
Teja ◽  
Sravanathi P ◽  
Muthu Babu K
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
In Vitro Study ◽  
In Vivo Studies ◽  
Asterias Rubens ◽  
Mcf 7

Breast cancer is the subsequent foremost reason of cancer death in a woman and ranks as the primary foremost reason of death in India. In its conduct, several measures and recommendation are considered. Homoeopathic medicines are one of the part of a corresponding, and another medicine is utilized for the treatment of cancer. The main purpose of the investigation is to evaluate the anticancer action of homoeopathic arrangements of Asterias rubens  on the basis of the similia principle. We directed an in vitro study using MTT assay to control the result of ultra diluted homoeopathic preparation in contradiction of two human breast glandular cancer cell lines(MCF-7 and MDA-MD- 231), frequently used for the breast cancer treatment, by testing the feasibility of breast cancer (MCF-7 and MDA-MD-231) cell line, with various attenuations of Asterias rubens  at 24 hrs. Multiple comparisons between tested reagents at different concentrations confirmed the significance of the said results. At a dilution of 1:25 6CH and 30CH potency shown superior activity on MCF-7 and no such significant changes on MDA-MD-231 at any dilutions As it fails to offer estrogen receptor(ER) Also progesterone receptor (PR) expression, and also HER2 (human epidermal development variable receptor2) so continuously a triple-negative breast cancer it will be a hostility manifestation for breast cancer with restricted medicine choices. However, further potency needs to be tested. These preliminary significant results warrant further in vitro and in vivo studies to estimate the possible of Asterias rubens  a medicine to treat breast cancer.

scholarly journals Cytotoxic Activity of Compounds from Styrax obassia

2017 ◽  
Vol 12 (2) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Thao Quyen Cao ◽  
Bo Mi Lee ◽  
Yeon Woo Jung ◽  
Van Thu Nguyen ◽  
Jeong Ah Kim ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Cancer Cell Line ◽  
Stem Bark ◽  
Leukemia Cell Line ◽  
Cervical Cancer Cell Line ◽  
Cell Line Hela ◽  
Mcf 7

Cancer is a major public health burden in both developed and developing countries. Plant-derived compounds have played an important role in the development of useful anti-cancer agents. The current study was designed to evaluate the cytotoxic activity of chemical compounds from the stem bark of Styrax obassia. Seven known compounds (1–7) were isolated and identified. Compound 2 exhibited cytotoxic activity against the breast cancer cell line MCF-7 with an IC50 of 27.9 μM, followed by the human cervical cancer cell line Hela with an IC50 of 23.3 μM, and the human promyelocytic leukemia cell line HL-60 with an IC50 of 47.8 μM. Compound 7 exhibited cytotoxicity against Hela cells with an IC50 of 16.8 μM, followed by MCF-7 cells with an IC50 of 53.5 μM. This is the first study to investigate the significant anti-tumor properties of isolated compounds from the stem bark of S. obassia.

scholarly journals Jaceidin Flavonoid Isolated from Chiliadenus montanus Attenuates Tumor Progression in Mice via VEGF Inhibition: In Vivo and In Silico Studies

Plants ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 1031 ◽  
Author(s):  
Sameh S. Elhady ◽  
Enas E. Eltamany ◽  
Amera E. Shaaban ◽  
Alaa A. Bagalagel ◽  
Yosra A. Muhammad ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
In Silico ◽  
Cancer Cell Line ◽  
Control Group ◽  
Phytochemical Study ◽  
Aerial Parts ◽  
In Silico Studies

Phytochemical study of Chiliadenus montanus aerial parts afforded six compounds; Intermedeol (1), 5α-hydroperoxy-β-eudesmol (2), 5,7-dihydroxy-3,3’,4’-trimethoxyflavone (3), 5,7,4’-trihydroxy-3,6,3’-trimethoxyflavone (jaceidin) (4), eudesm-11,13-ene-1β,4β,7α-triol (5) and 1β,4β,7β,11-tetrahydroxyeudesmane (6). These compounds were identified based on their NMR spectral data. The isolated compounds were tested for their cytotoxicity against liver cancer cell line (HepG2) and breast cancer cell line (MCF-7). Jaceidin flavonoid (4) exhibited the highest cytotoxic effect in vitro. Therefore, both of jaceidin and C. montanus extract were evaluated for their in vivo anti-tumor activity against Ehrlich’s ascites carcinoma (EAC). Compared to control group, jaceidin and C. montanus extract decreased the tumor weight, improved the histological picture of tumor cells, lowered the levels of VEGF and ameliorate the oxidative stress. Molecular docking and in silico studies suggested that jaceidin was a selective inhibitor of VEGF-mediated angiogenesis with excellent membrane permeability and oral bioavailability.

scholarly journals Cytotoxic Activity of Alkaloids from the Fruits of Piper nigrum

2018 ◽  
Vol 13 (11) ◽  
pp. 1934578X1801301
Author(s):  
Quynh Mai Thi Ngo ◽  
Thao Quyen Cao ◽  
Le Son Hoang ◽  
Manh Tuan Ha ◽  
Mi Hee Woo ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Cancer Cell Line ◽  
Leukemia Cell Line ◽  
Piper Nigrum ◽  
Cervical Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Anticancer Properties ◽  
Cell Line Hela

Medicinal plants have been shown to have tremendous potential for the development of new drug molecules for various serious diseases. Piper nigrum L. (Piperaceae) is a well-known spice considered to be the “The King of Spices” among various spices. The phytochemicals isolated from P. nigrum L. are potent biological agents with anticancer properties. Our study was designed to evaluate the cytotoxic activities of chemical compounds from the dried fruits of P. nigrum L. Sixteen known compounds (1–16), including fifteen alkaloids, were isolated and identified. Compounds 10, 11, 12, 13, 14, and 15 exhibited cytotoxic activities against a human cervical cancer cell line, Hela, with IC50 values of 49.8, 40.4, 23.1, 22.1, 41.0, and 26.9 μM, respectively. Compounds 10, 12, and 15 exhibited cytotoxicities against a breast cancer cell line, MCF-7, with IC50 values of 36.9, 55.7, and 36.0 μM, respectively. Compounds 6, 12, 13, 14, 15, and 16 exhibited cytotoxic activities against the human promyelocytic leukemia cell line, HL-60, with IC50 values of 26.9, 51.4, 51.6, 54.4, 16.0, and 21.1 μM, respectively.

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