scholarly journals Synthesis and In Vitro Photocytotoxicity of 9-/13-Lipophilic Substituted Berberine Derivatives as Potential Anticancer Agents

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 677 ◽  
Author(s):  
Hong-Jhih Lin ◽  
Jinn-Hsuan Ho ◽  
Li-Chen Tsai ◽  
Fang-Yu Yang ◽  
Ling-Ling Yang ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hepg2 Cells ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Dependent Manner ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Berberine Derivatives

The objective of this study was to synthesize the 9-/13-position substituted berberine derivatives and evaluate their cytotoxic and photocytotoxic effects against three human cancer cell lines. Among all the synthesized compounds, 9-O-dodecyl- (5e), 13-dodecyl- (6e), and 13-O-dodecyl-berberine (7e) exhibited stronger growth inhibition against three human cancer cell lines, (HepG2, HT-29 and BFTC905), in comparison with structurally related berberine (1). These three compounds also showed the photocytotoxicity in human cancer cells in a concentration-dependent and light dose-dependent manner. Through flow cytometry analysis, we found out a lipophilic group at the 9-/13-position of berberine may have facilitated its penetration into test cells and hence enhanced its photocytotoxicity on the human liver cancer cell HepG2. Further, in cell cycle analysis, 5e, 6e, and 7e induced HepG2 cells to arrest at the S phase and caused apoptosis upon irradiation. In addition, photodynamic treatment of berberine derivatives 5e, 6e, and 7e again showed a significant photocytotoxic effects on HepG2 cells, induced remarkable cell apoptosis, greatly increased intracellular ROS level, and the loss of mitochondrial membrane potential. These results over and again confirmed that berberine derivatives 5e, 6e, and 7e greatly enhanced photocytotoxicity. Taken together, the test data led us to conclude that berberine derivatives with a dodecyl group at the 9-/13-position could be great candidates for the anti-liver cancer medicines developments.

scholarly journals Synthesis and in vitro Photocytotoxicity of 9-/13-lipophilic Substituted Berberine Derivatives as Potential Anticancer Agents

2020 ◽  
Author(s):  
Hong-Jhih Lin ◽  
Jinn-Hsuan Ho ◽  
Li-Chen Tsai ◽  
Fang-Yu Yang ◽  
Ling-Ling Yang ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hepg2 Cells ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Dependent Manner ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Berberine Derivatives

The objective of this study was to synthesize 9-/13-position substituted berberine derivatives and evaluated their cytotoxic and photocytotoxic effects against three human cancer cell lines. Among all the synthesized compounds, 9-O-dodecyl- (5e), 13-dodecyl- (6e) and 13-O-dodecyl-berberine (7e) exhibited stronger growth inhibition against three human cancer cell lines, (HepG2, HT-29 and BFTC905), in compare with structurally related berberine (1). These three compounds also showed the photocytotoxicity in human cancer cells in a concentration-dependent and light dose-dependent manner. Through flow cytometry analysis, we found out a lipophilic group at 9-/13-position of berberine may have facilitated its penetration into test cell and hence enhanced its photocytotoxicity on human liver cancer cell HepG2. Further, in cell cycle analysis, 5e, 6e and 7e induced HepG2 cells to arrest at S phase and caused apoptosis upon irradiation. In addition, photodynamic treatment of berberine (1) and its derivatives 5e, 6e and 7e again showed a significant photocytotoxic effects on HepG2 cells, induced remarkable cell apoptosis, greatly increased intracellular ROS level and the loss of mitochondrial membrane potential. These results over and again confirmed that berberine derivatives 5e, 6e and 7e greatly enhanced photocytotoxicity. Taking together, the test data led us to conclude that berberine derivatives with a dodecyl group at 9-/13-position could be great candidates for the anti-liver cancer medicines developments.

scholarly journals A New Cytotoxic Cyclolanostane Triterpenoid Xyloside from Souliea vaginata

2017 ◽  
Vol 12 (2) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Haifeng Wu ◽  
Zhixin Yang ◽  
Qiru Wang ◽  
Nailiang Zhu ◽  
Xudong Xu ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Hepg2 Cells ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Hepatoprotective Effect ◽  
Human Cancer Cell ◽  
Inhibitory Effects ◽  
Chemical Methods ◽  
Human Cancer Cell Lines

A new cyclolanostane triterpenoid xyloside, soulieoside P (1), and a known oleanane-type saponin, hederasaponin B (2), were isolated from the rhizomes of Souliea vaginata. Their structures were established by extensive spectroscopic and HRESIMS analysis, as well as chemical methods. Compound 1 showed significant inhibitory effects with IC50 values of 7.6–11.2 μM against three human cancer cell lines, while compound 2 exhibited no hepatoprotective effect on CCl4-induced injury of human HepG2 cells, in the tested range of 0.1–100 μM.

scholarly journals GC-MS Analysis of Bioactive Compounds of Artemesia annua and Assessment of its anti-proliferative activity against Human Cancer Cell Lines

2020 ◽  
Vol 11 (2) ◽  
pp. 1840-1843
Author(s):  
Renugadevi Karthikeyan ◽  
Julius Amaldas
Keyword(s):  
Essential Oil ◽  
Cell Lines ◽  
Cancer Cell ◽  
Molecular Mechanisms ◽  
Specific Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Dependent Manner ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Plant essential oil is found to possess many beneficial effects in the field of medicine. Especially essential oil derived from different species of plants is reported to have specific activity against cancer. Artemesiaannua is an annual herb belonging to Asteraceae family has been traditionally used for treating several ailments. It is a conventional medicinal plant used in the treatment of chloroquine-resistant and cerebral malaria. The major aim of this study was to evaluate the anticancer potential of this plant against cancer cell line. Hydro distilled volatile oil obtained from aerial parts of A.annua was analysed by GCMS. The majority of the compounds derived from essential oil of Artemesiaannua are monoterpenes and sesquiterpenes. Artemisinin, the active component of Artemesiaannua is a sesquiterpenoid lactone containing unusual endoperoxide bridge that shows remarkable activity against numerous tumour growth and metastases. The pleiotropic nature of artemisinin induces oxidative stress, anti-angiogenetic effect and apoptosis triggering on cancer cells. The anti-proliferative effect of essential oil derived from Artemesiaannua on human cancer cell lines like MCF-7, HT29 and AGS was done by MTT assay. Results shows the essential oil of artemisia annua have cytotoxic potential by inhibiting cell growth in a dose dependent manner. However, further investigations in isolating active cytotoxic components and understanding its molecular mechanisms will help in therapeutic management of cancer.

scholarly journals Antiproliferative Activity of Anthocyanins Pure Extracts from Mulberries and Raspberries on HeLa and A2780 Human Cancer Cell Lines

2018 ◽  
Vol 75 (2) ◽  
pp. 156
Author(s):  
Mǎdǎlina NISTOR ◽  
Raluca GHIMAN ◽  
Huseyin AYVAZ ◽  
Dumitrița RUGINǍ ◽  
Diana MADA ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Health Benefits ◽  
Cancer Cell Lines ◽  
In Vitro Test ◽  
Dependent Manner ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Red berries are important sources of bioactive compounds and they are known to provide unique health benefits. Lately, it has been proved that anthocyanins have health benefits against degenerative diseases such as cardiovascular disease, cancer or diabetes. Accordingly, the aim of this study was to characterize the anthocyanin content of anthocyanins pure extracts (APEs) obtained from raspberries (Rubus sp.) and mulberries (Morus sp.) and to evaluate their antiproliferative effect in vitro. Upon chromatographic analysis, three anthocyanins were identified in purified extracts of mulberries (M-APEs), with cyanidin-3-O-glucoside being more abundant. On the other hand, purified extracts of raspberries (R-APEs) contained 2 anthocyanins, both identified as cyanidin-derivatives. The in vitro test demonstrated that APEs decreased the proliferation on both HeLa and A2780 human cancer cell lines in a dose dependent manner, demonstrating that these two different berries are both rich sources of anthocyanins and are able to exert antiproliferative proprieties toward cervical and ovarian cancer.

scholarly journals Cytotoxicity of Cyclodipeptides fromPseudomonas aeruginosaPAO1 Leads to Apoptosis in Human Cancer Cell Lines

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Dolores Vázquez-Rivera ◽  
Omar González ◽  
Jaquelina Guzmán-Rodríguez ◽  
Alma L. Díaz-Pérez ◽  
Alejandra Ochoa-Zarzosa ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Flow Cytometric Analysis ◽  
Human Tumor ◽  
Cancer Cell Lines ◽  
Dependent Manner ◽  
Human Cancer Cell ◽  
Apoptotic Pathway ◽  
Human Cancer Cell Lines

Pseudomonas aeruginosais an opportunistic pathogen of plants and animals, which produces virulence factors in order to infect or colonize its eukaryotic hosts. Cyclodipeptides (CDPs) produced byP. aeruginosaexhibit cytotoxic properties toward human tumor cells. In this study, we evaluated the effect of a CDP mix, comprised of cyclo(L-Pro-L-Tyr), cyclo(L-Pro-L-Val), and cyclo(L-Pro-L-Phe) that were isolated fromP. aeruginosa, on two human cancer cell lines. Our results demonstrated that the CDP mix promoted cell death in cultures of the HeLa cervical adenocarcinoma and Caco-2 colorectal adenocarcinoma cell lines in a dose-dependent manner, with a 50% inhibitory concentration (IC50) of 0.53 and 0.66 mg/mL, for HeLa and Caco-2 cells, respectively. Flow cytometric analysis, using annexin V and propidium iodide as apoptosis and necrosis indicators, respectively, clearly showed that HeLa and Caco-2 cells exhibited apoptotic characteristics when treated with the CDP mix at a concentration <0.001 mg/mL. IC50values for apoptotic cells in HeLa and Caco-2 cells were 6.5 × 10−5and 1.8 × 10−4 mg/mL, respectively. Our results indicate that an apoptotic pathway is involved in the inhibition of cell proliferation caused by theP. aeruginosaCDP mix.

Constituents of Polyalthia jucunda and their cytotoxic effect on human cancer cell lines

Planta Medica ◽  
2007 ◽  
Vol 73 (09) ◽  
Author(s):  
IO Mondranondra ◽  
A Suedee ◽  
A Kijjoa ◽  
M Pinto ◽  
N Nazareth ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cytotoxic Effect ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines
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