Recent study on the anticancer activity of nobiletin and its metabolites

The exploration of naturally occurring phytochemicals with antitumor potential has been the focus of many studies. Nobiletin, a polymethoxyflavone (PMF) exclusively derived from citrus peels, has been reported as a promising candidate for the prevention and/or treatment of cancers. Additionally, multiple demethylated derivatives of nobiletin from in vivo biotransformation, including 3′-demethylnobiletin (3′-DMN), 4′-demethylnobiletin (4′-DMN), 3′,4′-didemethylnobiletin (3′,4′-DDMN) and 5-demethylnobiletin (5-DMN), among others, have been found to show anti-cancer activity. In this review, the anticancer activity of nobiletin and its derivatives in cancer prevention are comprehensively described.

Download Full-text

Natural Polyphenols as Modulators of Etoposide Anti-Cancer Activity

International Journal of Molecular Sciences ◽

10.3390/ijms22126602 ◽

2021 ◽

Vol 22 (12) ◽

pp. 6602

Author(s):

Magdalena Kluska ◽

Katarzyna Woźniak

Keyword(s):

Fruits And Vegetables ◽

In Vivo Studies ◽

Natural Polyphenols ◽

Naturally Occurring ◽

Anti Cancer ◽

Health Promoting ◽

Synthetic Derivative ◽

Cancer Activity

Polyphenols are naturally occurring compounds found in abundance in fruits and vegetables. Their health-promoting properties and their use in the prevention and treatment of many human diseases, including cancer, have been known for years. Many anti-cancer drugs are derived from these natural compounds. Etoposide, which is a semi-synthetic derivative of podophyllotoxin, a non-alkaloid lignan isolated from the dried roots and rhizomes of Podophyllum peltatum or Podophyllum emodi (Berberidaceae), is an example of such a compound. In this review, we present data on the effects of polyphenols on the anti-cancer activity of etoposide in in vitro and in vivo studies.

Download Full-text

Synthesis and Anticancer Activity of 9-O-Pyrazole Alkyl Substituted Berberine Derivatives

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180717121208 ◽

2019 ◽

Vol 18 (11) ◽

pp. 1639-1648 ◽

Cited By ~ 5

Author(s):

Daipeng Xiao ◽

Fen He ◽

Dongming Peng ◽

Min Zou ◽

Junying Peng ◽

...

Keyword(s):

Oxidative Stress ◽

Molecular Docking ◽

Anticancer Activity ◽

Cell Lines ◽

Human Lung Cancer ◽

Drug Candidate ◽

Molecular Docking Study ◽

Protective Function ◽

Anti Cancer ◽

Cancer Activity

Background: Berberine (BBR), an isoquinoline plant alkaloid isolated from plants such as Coptis chinensis and Hydrastis canadensis, own multiple pharmacological activities. Objective: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. Methods: The anti-cancer activity was measured by MTT assay, and apoptosis was demonstrated by the annexin V-FITC/PI staining assay. The intracellular oxidative stress was investigated through DCFH-DA assay. The molecular docking study was carried out in molecular operating environment (MOE). Results: Compound B3 and B5 showed enhanced anti-cancer activity compared with BBR, the IC50 for compound B3 and B5 were significantly lower than BBR, and compound B3 at the concentration of 64 or 128 µM induced apoptosis in HeLa and A549 cell lines. The reactive oxygen species (ROS) was generated in both cell lines when treated with 100 µM of all the compounds, and compound B3 and B5 induced higher activity in the generation of ROS, while compound B3 exhibited the highest activity, these results are in accordance with the cytotoxicity results, indicating the cytotoxicity were mostly generated from the oxidative stress. In addition, molecular docking analysis showed that compound B3 had the greatest affinity with Hsp90. Upon binding, the protective function of Hsp90 was lost, which might explain its higher cytotoxicity from molecular interaction aspect. Conclusion: All the results demonstrated that compound B3 and B5 showed significantly higher anti-cancer ability than BBR, and compound B3 is a promising anticancer drug candidate.

Download Full-text

Tocotrienols and Cancer: From the State of the Art to Promising Novel Patents

Recent Patents on Anti-Cancer Drug Discovery ◽

10.2174/1574892814666190116111827 ◽

2019 ◽

Vol 14 (1) ◽

pp. 5-18 ◽

Cited By ~ 8

Author(s):

Fabrizio Fontana ◽

Michela Raimondi ◽

Monica Marzagalli ◽

Roberta M. Moretti ◽

Marina Montagnani Marelli ◽

...

Keyword(s):

Cancer Prevention ◽

State Of The Art ◽

Synergistic Effects ◽

The State ◽

Therapeutic Interventions ◽

Multiple Tumor ◽

Anti Cancer ◽

Important Health

Background: Tocotrienols (TTs) are vitamin E derivatives naturally occurring in several plants and vegetable oils. Like Tocopherols (TPs), they comprise four isoforms, α, β, γ and δ, but unlike TPs, they present an unsaturated isoprenoid chain. Recent studies indicate that TTs provide important health benefits, including neuroprotective, anti-inflammatory, anti-oxidant, cholesterol lowering and immunomodulatory effects. Moreover, they have been found to possess unique anti-cancer properties.Objective:The purpose of this review is to present an overview of the state of the art of TTs role in cancer prevention and treatment, as well as to describe recent patents proposing new methods for TTs isolation, chemical modification and use in cancer prevention and/or therapy.Methods:Recent literature and patents focusing on TTs anti-cancer applications have been identified and reviewed, with special regard to their scientific impact and novelty.Results:TTs have demonstrated significant anti-cancer activity in multiple tumor types, both in vitro and in vivo. Furthermore, they have shown synergistic effects when given in combination with standard anti-cancer agents or other anti-tumor natural compounds. Finally, new purification processes and transgenic sources have been designed in order to improve TTs production, and novel TTs formulations and synthetic derivatives have been developed to enhance their solubility and bioavailability.Conclusion:The promising anti-cancer effects shown by TTs in several preclinical studies may open new opportunities for therapeutic interventions in different tumors. Thus, clinical trials aimed at confirming TTs chemopreventive and tumor-suppressing activity, particularly in combination with standard therapies, are urgently needed.

Download Full-text

Evaluation of the anti-cancer activity of the triterpenoidal saponin fraction isolated from the traditional Chinese medicine Conyza blinii H. Lév.

RSC Advances ◽

10.1039/c6ra26361e ◽

2017 ◽

Vol 7 (6) ◽

pp. 3408-3412 ◽

Cited By ~ 11

Author(s):

Long Ma ◽

Haiyan Liu ◽

Lingpei Meng ◽

Ping Qin ◽

Botao Zhang ◽

...

Keyword(s):

Chinese Medicine ◽

Traditional Chinese Medicine ◽

Anti Cancer ◽

Saponin Fraction ◽

Cancer Activity

Triterpenoidal saponins fraction isolated from a traditional Chinese medicine Conyza blinii H. Lév. demonstrates anti-cancer activity both in vitro and in vivo.

Download Full-text

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

Dalton Transactions ◽

10.1039/c7dt01054k ◽

2017 ◽

Vol 46 (21) ◽

pp. 7005-7019 ◽

Cited By ~ 25

Author(s):

Benjamin W. J. Harper ◽

Emanuele Petruzzella ◽

Roman Sirota ◽

Fernanda Fabiola Faccioli ◽

Janice R. Aldrich-Wright ◽

...

Keyword(s):

Anticancer Activity ◽

Biological Evaluation ◽

Synthesis And Biological Evaluation ◽

Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

Download Full-text

SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF SOME SCHIFF BASES OF 1, 3, 4-OXADIAZOLE

INDIAN DRUGS ◽

10.53879/id.56.03.11589 ◽

2019 ◽

Vol 56 (03) ◽

pp. 12-17

Author(s):

Manpreet Kaur ◽

S. Singh ◽

Keyword(s):

Schiff Base ◽

Growth Inhibition ◽

Anticancer Activity ◽

Maximum Growth ◽

Schiff Base Derivatives ◽

Control Growth ◽

Anti Cancer ◽

Oxadiazole Derivatives ◽

Cancer Activity ◽

Mcf 7

A new series of 2,5-disubstituted-1,3,4-oxadiazole derivatives has been synthesized with the help of different aromatic benzaldehydes and final compounds were characterized by FTIR and 1H NMR. 2,5- disubstituted-1,3,4-oxadiazole derivatives were synthesized by the reaction of Schiff base derivatives with 2,5-disubstituted-1,3,4-oxadiazoles. All the synthesized compounds were screened for their anticancer activity. These compounds were evaluated for their anticancer activity against various cancer cell lines. Five of the compounds possessed good to moderate anti-cancer activity. Three of the synthesized compounds i.e. 6a, 6f and 6g were found to possess maximum growth inhibition. The order for the % control growth inhibition of MCF-7 was found to be 6a>6f>6g>5b>6h, as shown in Table II-VI.

Download Full-text

Synthesis, Electronic Structure and Anti-Cancer Activity of the Phenyl Substituted Pyrazolo[1,5-a][1,3,5]triazines

Current Organic Chemistry ◽

10.2174/1385272825666210607004536 ◽

2021 ◽

Vol 25 ◽

Author(s):

Evgenia S. Veligina ◽

Nataliya V. Obernikhina ◽

Stepan G. Pilyo ◽

Oleksiy D. Kachkovsky ◽

Volodymyr S. Brovarets

Keyword(s):

Electronic Transition ◽

Lone Electron Pair ◽

Electron Pair ◽

Anti Cancer ◽

Protein Molecules ◽

Biological Affinity ◽

Cancer Types ◽

Derivatives Of ◽

Cancer Activity

: Background: Synthesis of a series of 2-(dichloromethyl)pyrazolo[1,5- a][1,3,5]triazines was carried out and evaluated in vitro for their anticancer activity against a panel of 60 cell lines derived from nine cancer types. The joint quantum-chemical and experimental study of the influence of the extended πconjugated phenyl substituents on the electron structure of the pyrazolo[1,5-a][1,3,5]triazines as Pharmacophores were performed. It is shown that the decrease in the barriers to the rotation of phenyl substituents in compounds 1-7 possibly leads to an increase in the anti-cancer activity, which is in agreement with the change in the parameter biological affinity ϕ0. Analysis of the S0 → S1 electronic transitions (π→π*) of the pyrazolo[1,5-a][1,3,5]triazines shows that an increase in their intensity correlates with anti-cancer activity. Thus, the introduction of phenyl substituents increases the likelihood of investigated pyrazolo[1,5-a][1,3,5]triazines interacting with protein molecules (Biomolecule) by the π stacking mechanism. In both methyl and phenyl derivatives of pyrazolo[1,5-a][1,3,5]triazines, the second electronic transition includes the n-MO (the level of the lone electron pair in two-coordinated nitrogen atoms). The highest intensity of the η→π* electronic transition is observed in pyrazolo[1,5-a][1,3,5]triazine with pyridine residue, which does not exhibit anti-cancer activity, but exhibits antiviral activity [13]. It can be assumed that the possibility of the formation of [Pharmacophore-Biomolecule] complex by hydrogen bonding ([H-B]) mechanism with protein molecules increases.

Download Full-text