Glycyrrhetinic Acid and Its Derivatives: Anti-Cancer and Cancer Chemopreventive Properties, Mechanisms of Action and Structure- Cytotoxic Activity Relationship

2016 ◽  
Vol 23 (5) ◽  
pp. 498-517 ◽  
Author(s):  
Ali Roohbakhsh ◽  
Milad Iranshahy ◽  
Mehrdad Iranshahi
Keyword(s):  
Cytotoxic Activity ◽  
Mechanisms Of Action ◽  
Glycyrrhetinic Acid ◽  
Activity Relationship ◽  
Anti Cancer

Anticancer Properties of Essential Oils: An Overview

2018 ◽  
Vol 18 (10) ◽  
pp. 957-966 ◽  
Author(s):  
Milene Aparecida Andrade ◽  
Mariana Aparecida Braga ◽  
Pedro Henrique Souza Cesar ◽  
Marcus Vinicius Cardoso Trento ◽  
Mariana Araújo Espósito ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Essential Oils ◽  
Public Health Problem ◽  
Mechanisms Of Action ◽  
Low Molecular Weight ◽  
Anticancer Properties ◽  
Anti Cancer ◽  
Different Types ◽  
Antitumor Properties ◽  
Pharmaceutical Properties

Background: Essential oils are complex mixtures of low molecular weight compounds extracted from plants. Their main constituents are terpenes and phenylpropanoids, which are responsible for their biological and pharmaceutical properties, such as insecticidal, parasiticidal, antimicrobial, antioxidant, anti-inflammatory, analgesic, antinociceptive, anticarcinogenic, and antitumor properties. Cancer is a complex genetic disease considered as a serious public health problem worldwide, accounting for more than 8 million deaths annually. Objective: The activities of prevention and treatment of different types of cancer and the medicinal potential of essential oils are addressed in this review. Conclusion: Several studies have demonstrated anti-carcinogenic and antitumor activity for many essential oils obtained from various plant species. They may be used as a substitution to or in addition to conventional anti-cancer therapy. Although many studies report possible mechanisms of action for essential oils compounds, more studies are necessary in order to apply them safely and appropriately in cancer therapy.

Synthesis, Anti-proliferative Evaluation, and Molecular Docking Studies of 3-(alkylthio)-5,6-diaryl-1,2,4-triazines as Tubulin Polymerization Inhibitors

2019 ◽  
Vol 16 (11) ◽  
pp. 1194-1201 ◽  
Author(s):  
Farhad Saravani ◽  
Ebrahim Saeedian Moghadam ◽  
Hafezeh Salehabadi ◽  
Seyednasser Ostad ◽  
Morteza Pirali Hamedani ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Cytotoxic Activity ◽  
Binding Site ◽  
Cell Line ◽  
Cell Lines ◽  
Tubulin Polymerization ◽  
Adenocarcinoma Cell Line ◽  
Adenocarcinoma Cell ◽  
Colchicine Binding Site ◽  
Anti Cancer

Background: The role of microtubules in cell division and signaling, intercellular transport, and mitosis has been well known. Hence, they have been targeted for several anti-cancer drugs. Methods: A series of 3-(alkylthio)-5,6-diphenyl-1,2,4-triazines were prepared and evaluated for their cytotoxic activities in vitro against three human cancer cell lines; human colon carcinoma cells HT-29, human breast adenocarcinoma cell line MCF-7, human Caucasian gastric adenocarcinoma cell line AGS as well as fibroblast cell line NIH-3T3 by MTT assay. Docking simulation was performed to insert these compounds into the crystal structure of tubulin at the colchicine binding site to determine a probable binding model. Compound 5d as the most active compound was selected for studying of microtubule disruption. Results: Compound 5d showed potent cytotoxic activity against all cell lines. The molecular modeling study revealed that some derivatives of triazine strongly bind to colchicine binding site. The tubulin polymerization assay kit showed that the cytotoxic activity of 5d may be related to inhibition of tubulin polymerization. Conclusion: The cytotoxicity and molecular modeling study of the synthesized compounds with their inhibition activity in tubulin polymerization demonstrate the potential of triazine derivatives for development of new anti-cancer agents.

Design, Synthesis, In vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a]Pyridines as Potent Anti-Breast Cancer Agents

2019 ◽  
Vol 19 (2) ◽  
pp. 265-275 ◽  
Author(s):  
Faeze Khalili ◽  
Sara Akrami ◽  
Malihe Safavi ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
High Yield ◽  
Breast Cancer Cell Lines ◽  
Pyridine Derivatives ◽  
One Pot ◽  
Standard Drug ◽  
Three Component Reaction ◽  
Anti Cancer

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death. Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.

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.

Structure-Activity Relationship Analyses of Glycyrrhetinic Acid Derivatives as Anticancer Agents

2011 ◽  
Vol 11 (10) ◽  
pp. 881-887 ◽  
Author(s):  
B. Lallemand ◽  
M. Gelbcke ◽  
J. Dubois ◽  
M. Prevost ◽  
I. Jabin ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Structure Activity Relationship ◽  
Glycyrrhetinic Acid ◽  
Activity Relationship ◽  
Structure Activity

Identification of Secondary Metabolite Compounds and Cytotoxic Activity Test of Papuan Grape (Sararanga Sinuosa Hemsley) Extract using Brine Shrimp Lethality Test (BSLT) Method

2021 ◽  
Vol 3 (2) ◽  
Author(s):  
Elsye Gunawan ◽  
Enrick Kharo Etmond ◽  
Linus Yhani Chrystomo
Keyword(s):  
Cytotoxic Activity ◽  
Secondary Metabolite ◽  
Ethanol Extract ◽  
Artemia Salina ◽  
Organ System ◽  
Activity Test ◽  
Anti Cancer ◽  
Extraction Stage ◽  
Cancer Agent ◽  
Concentration Series

Papua has a diversity of flora species, one of which is the Papuan Grape (Sararanga sinuosa Hemsley). It is commonly used by the Depapre community, Jayapura, as a stamina booster. This research aims to identify the secondary metabolite compounds, to test the cytotoxic activity of Papuan Grape (Sararanga sinuosa Hemsley) extract, and to determine the best concentration that inhabits the growth of Artemia salina larvae using the BSLT method. This study was conducted with the extraction stage using the maceration method by making use of 96% ethanol solvent. Subsequently, the concentration series 0, 50, 100, 150, 200, 250, 300 ppm of Papuan Grape (Sararanga sinuosa Hemsley) extract were made to test the cytotoxic activity on the mortality of Artemia salina shrimp larvae. The results showed that Alkaloids, Flavonoids, Saponins, and Tannins were compounded as secondary metabolite. An antioxidant research that had been carried out previously had LC50 of green-white fruit (12,49 ± 0,35 mg/ml), orange-red fruit (17,62 ± 3,49 mg/ml) and red fruit (12,23 ± 0,46 mg/ml). The community process one stalk of it into juice and used or consumed it two times a day. An inappropriate dose of traditional medicine usage can affect the organ system and had adverse effects in the future The result of cytotoxic research obtained the value of LC50 in ethanol extract of Papuan Grape was 140,863 ppm, and concentration of 250 ppm was the best concentration to inhibit the growth of shrimp larvae (Artemia salina L). The conclusion of this study was the ethanol extract of Papuan Grape (Sararanga sinuosa Hemsley) showed the highest cytotoxic activity and potentially become an anti-cancer agent.

scholarly journals Anti-Cancer Efficacy of Silybin Derivatives - A Structure-Activity Relationship

PLoS ONE ◽  
2013 ◽  
Vol 8 (3) ◽  
pp. e60074 ◽  
Author(s):  
Chapla Agarwal ◽  
Ritambhara Wadhwa ◽  
Gagan Deep ◽  
David Biedermann ◽  
Radek Gažák ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Anti Cancer
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