scholarly journals Cytotoxic activity of methanol extraction of Avicennia marina and taurin in the HeLa cancer cells

2021 ◽  
Vol 1751 ◽  
pp. 012045
Author(s):  
S Andriani ◽  
E L Widiastuti ◽  
N Nurcahyani ◽  
E rosa ◽  
H Busman
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Avicennia Marina ◽  
Methanol Extraction

scholarly journals Synthesis and Cytotoxic Activity of Several Novel N-Alkyl-Plinabulin Derivatives With Aryl Group Moieties

2021 ◽  
Vol 16 (4) ◽  
pp. 1934578X2110100
Author(s):  
Pham The Chinh ◽  
Pham Thi Tham ◽  
Duong Huong Quynh ◽  
Nguyen Van Tuyen ◽  
Dinh Thuy Van ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Aldol Condensation ◽  
One Pot ◽  
Aryl Group ◽  
Vascular Disrupting Agents ◽  
Benzaldehyde Derivatives ◽  
Vascular Disrupting

Seven novel N-alkyl-plinabulin derivatives with aryl groups moieties (nitroquinoline, 1,4-dihydroquinoline, 4-methoxybenzene, and 4-chlorobenzene) have been synthesized via aldol condensation and alkylation in one-pot, and tested for their cytotoxicity against 4 cancer cell lines (KB, HepG2, Lu, and MCF7). Compounds ( Z)−3-((6,8-dimethyl-4-oxo-1,4-dihydroquinolin-2-yl)methylene)−6-(( Z)−4-methoxybenzylidene)−1-(prop-2-yn-1-yl)piperazine-2,5-dione (5a), ( Z)−6-(( Z)−4-methoxybenzylidene)−1-(prop-2-yn-1-yl)−3-((1,6,8-trimethyl-4-oxo-1,4-dihydroquinolin-2-yl)methylene)piperazine-2,5-dione (5b), and ( Z)−3-(( Z)−4-chlorobenzylidene)−1,4-dimethyl-6-((8-methyl-4-nitroquinolin-2-yl)methylene)piperazine-2,5-dione (8) showed strong cytotoxicity against 3 of the cancer cells lines (KB, HepG2 and Lu) with IC50 values ranging from 3.04 to 10.62 µM. The quinoline-derived compounds had higher cytotoxic activity than the benzaldehyde derivatives. The successful synthesis of these derivatives offers useful information for the development of more potent vascular disrupting agents based on plinabulin.

scholarly journals Synergistic Action of Stilbenes in Muscadine Grape Berry Extract Shows Better Cytotoxic Potential Against Cancer Cells Than Resveratrol Alone

Biomedicines ◽  
2019 ◽  
Vol 7 (4) ◽  
pp. 96 ◽  
Author(s):  
Subramani Paranthaman Balasubramani ◽  
Mohammad Atikur Rahman ◽  
Sheikh Mehboob Basha
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Biological Activities ◽  
Grape Berry ◽  
Similar Response ◽  
Synergistic Activity ◽  
Anti Cancer ◽  
Muscadine Grape ◽  
Berry Extracts ◽  
Cancer Activity

Muscadine grape is rich in stilbenes, which include resveratrol, piceid, viniferin, pterostilbene, etc. Resveratrol has been extensively studied for its biological activities; however, the synergistic effect of stilbene compounds in berry extracts is poorly understood. The aim of this study was to evaluate the anti-cancer activity of stilbene-rich muscadine berry extract and pure resveratrol. Stilbenes were extracted from ripened berries of muscadine grape cultivars, Pineapple, and Southern Home. HPLC analysis was performed to determine quantity of stilbenes. The extracts were tested for their cytotoxic activity against A549 (lung carcinoma cells), triple negative breast cancer (HCC-1806) and HepG2 (human liver cancer) cells. The stilbene-rich extracts of the muscadine berry extracts showed cytotoxic activity against all of the cells tested. The extracts at 1 μg/mL induced death in 50–80% of cells by 72 h of treatment. About 50 μg/mL of resveratrol was required to induce a similar response in the cells. Further, modulation of genes involved in tumor progression and suppression was significantly (p < 0.0005) higher with the HepG2 cells treated with stilbene-rich berry extracts than the pure resveratrol. This shows that the synergistic activity of stilbenes present in muscadine grape berries have more potent anti-cancer activity than the resveratrol alone.

scholarly journals Cytotoxic Activity of Rearranged Drimane Meroterpenoids against Colon Cancer Cells via Down-Regulation of β-Catenin Expression

2015 ◽  
Vol 78 (3) ◽  
pp. 453-461 ◽  
Author(s):  
In Hyun Hwang ◽  
Joonseok Oh ◽  
Wei Zhou ◽  
Seoyoung Park ◽  
Joo-Hyun Kim ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Colon Cancer Cells ◽  
Down Regulation

Molecular Mechanism Mediating Cytotoxic Activity of Cabazitaxel in Docetaxel-resistant Human Prostate Cancer Cells

2021 ◽  
Vol 41 (8) ◽  
pp. 3753-3758
Author(s):  
HIROMITSU WATANABE ◽  
ASUKA KAWAKAMI ◽  
RYO SATO ◽  
KYOHEI WATANABE ◽  
YUTO MATSUSHITA ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Molecular Mechanism ◽  
Human Prostate ◽  
Human Prostate Cancer ◽  
Prostate Cancer Cells

scholarly journals Oncotoxic Properties of Serotonin Transporter Inhibitors and 5-HT1A Receptor Ligands

2018 ◽  
Vol 19 (10) ◽  
pp. 3260 ◽  
Author(s):  
Jarosław Walory ◽  
Lidia Mielczarek ◽  
Małgorzata Jarończyk ◽  
Mirosława Koronkiewicz ◽  
Jerzy Kossakowski ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Serotonin Transporter ◽  
Receptor Agonist ◽  
Antagonistic Activity ◽  
Hek293 Cells ◽  
Akt Pathway ◽  
Prostate Cancer Cells ◽  
Receptor Ligands

The cytotoxic activity of several serotonin transporter (SERT) inhibitors and subtype of serotonin receptor 1A (5-HT1A receptor) ligands have been examined in androgen-insensitive human PC-3 prostate and neuroblastoma SH-SY5Y cancer cells. Almost all of the studied compounds (except 5-HT1A receptor agonist (2R)-(+)-8-Hydroxy-2-(di-n-propylamino)tetralin hydrobromide (8-OH-DPAT)) exhibited absolute cytotoxic activity against the examined cancer cells. The compound 4-Fluoro-N-[2-[4-(7-methoxy-1-naphthalenyl)-1-piperazinyl]ethyl]benzamide hydrochloride (S14506) that showed highest activity against neuroblastoma tumors was the 5-HT1A receptor agonist (although not alike other 5-HT1A receptor agonists). On the other hand, the compound 6-nitro-2-(4-undecylpiperazin-1-yl)quinoline hydrochloride (AZ07) that had the highest activity against PC-3 prostate cancer cells was a compound exhibiting antagonistic activity against the 5-HT1A receptor. Thus, compounds of oncotoxic properties S14506 and AZ07 should be evaluated further for their potential use in the prevention and treatment of cancer. Most of the 15 compounds tested exhibited either agonistic or antagonistic activity for both the cyclic adenosine monophosphate (cAMP) and extracellular signal-regulated kinase 1 and 2 (ERK1/2) pathways in human embryonic kidney 293 (HEK293) cells that overexpress the 5HT1AR gene. However, compounds paroxetine, N-Ac-paroxetine and 2-[4-(cyclobutylmethyl)piperazin-1-yl]-6-nitroquinoline hydrochloride (AB22) simultaneously exhibited antagonistic activity on the cAMP pathway and agonistic activity on the ERK1/2 pathway. Fluoxetine relative to compound AZ07 had almost three times lower cytotoxic activity against PC-3 prostate cancer cells. However, the proapoptotic activity of fluoxetine compared to compound AZ07 is almost two times higher which would suggest that the cytotoxic activity of both compounds may be dependent on different cell death mechanisms. Compound S14506 was found to be an antagonist of the serine-threonine protein kinase B (Akt) pathway. Prosurvival Akt activity may be reversed by Akt antagonists. Therefore, the antagonistic activity of S14506 on the Akt pathway may evoke caspase-3 expression and cytotoxicity. It appears that one should not expect a straightforward relationship between the activation of particular serotonergic pathways by selective serotonin reuptake inhibitors (SSRIs) and 5-HT1A receptor ligands and their cytotoxic or cytoprotective activity. Additionally, nuclear transcription factor κB (NF-κB), which may be involved in 5-HT-dependent biochemical pathways by coordinating different subunits in the formation of a dimer, may regulate the transcription of different transduction pathways. Therefore, it can be suggested that the mechanism of the cytotoxic activity of certain compounds (serotonergic against nonserotonergic) may depend on the compound and cancer type being examined. Docking studies showed that S14506, buspirone and spiperone bind in similar ways in the 5-HT1A receptor model and interacted with similar 5-HT1A receptor residues. S14506 and spiperone were found to be located closer to both phenylalanines in TM6 than buspirone, thus exhibiting more antagonist binding modes.

scholarly journals Current Status, Distribution, and Future Directions of Natural Products against Colorectal Cancer in Indonesia: A Systematic Review

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4984
Author(s):  
Didi Nurhadi Illian ◽  
Ihsanul Hafiz ◽  
Okpri Meila ◽  
Ahmad Rusdan Handoyo Utomo ◽  
Arif Nuryawan ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Systematic Review ◽  
Natural Products ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cell Line ◽  
Current Status ◽  
Vitro Assay ◽  
Colorectal Cancer Cells

In 2020, an estimated 19.3 million new cancer cases and nearly 10 million cancer deaths have occurred worldwide, with colorectal cancer ranking as the third most frequently diagnosed (10.0%). Several attempts have been conducted against cancer, including surgery, radiation, monoclonal antibodies, and chemotherapy. Many people choose natural products as alternatives against cancer. These products will not only help in human life preservation but also work as a source of up-to-date information, leading people away from incorrect information. We discuss the current status, distribution, and future implications of protecting populations with natural products as an alternative against colorectal cancer in Indonesia. Thirty-eight studies were included in this review for data extraction. The distribution of natural products in Indonesia that have potential activity against colorectal cancer cells was predominated by terpenoids, followed by phytosterols, phenolics, alkaloids, and polyisoprenoids. The type of cell line utilized in the cytotoxic activity analysis of natural products was the WiDr cell line, followed by HT-29 cells and HCT-116 cells. This review showed that MTT in vitro assay is a general method used to analyze the cytotoxic activity of a natural product against colorectal cancer cells, followed by other in vitro and in vivo methods. The systematic review provided predictions for several secondary metabolites to be utilized as an alternative treatment against colorectal cancer in Indonesia. It also might be a candidate for a future co-chemotherapy agent in safety, quality, and standardization. In addition, computational methods are being developed to predict the drug-likeness of compounds, thus, drug discovery is already on the road towards electronic research and development.

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