scholarly journals Anticancer Properties and Mechanism of Action of Oblongifolin C, Guttiferone K and Related Polyprenylated Acylphloroglucinols

2021 ◽  
Author(s):  
Christian Bailly ◽  
Gérard Vergoten
Keyword(s):  
Mechanism Of Action ◽  
Biological Properties ◽  
Structural Basis ◽  
Anticancer Activities ◽  
Potent Inducer ◽  
Anticancer Properties ◽  
Potential Development ◽  
Tumor Growth And Metastasis

AbstractPolyprenylated acylphloroglucinols represent an important class of natural products found in many plants. Among them, the two related products oblongifolin C (Ob-C) and guttiferone K (Gt-K) isolated from Garcinia species (notably from edible fruits), have attracted attention due to their marked anticancer properties. The two compounds only differ by the nature of the C-6 side chain, prenyl (Gt-K) or geranyl (Ob-C) on the phloroglucinol core. Their origin, method of extraction and biological properties are presented here, with a focus on the targets and pathways implicated in their anticancer activities. Both compounds markedly reduce cancer cell proliferation in vitro, as well as tumor growth and metastasis in vivo. They are both potent inducer of tumor cell apoptosis, and regulation of autophagy flux is a hallmark of their mode of action. The distinct mechanism leading to autophagosome accumulation in cells and the implicated molecular targets are discussed. The specific role of the chaperone protein HSPA8, known to interact with Ob-C, is addressed. Molecular models of Gt-K and Ob-C bound to HSPA8 provide a structural basis to their common HSPA8-binding recognition capacity. The review shed light on the mechanism of action of these compounds, to encourage their studies and potential development.

scholarly journals Biological Properties of 6-Gingerol: A Brief Review

2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Shaopeng Wang ◽  
Caihua Zhang ◽  
Guang Yang ◽  
Yanzong Yang
Keyword(s):  
Fruits And Vegetables ◽  
Biological Activities ◽  
Zingiber Officinale ◽  
Biological Properties ◽  
Anticancer Activities ◽  
Inhibition Of Angiogenesis ◽  
Underlying Mechanisms ◽  
Pharmacologically Active

Numerous studies have revealed that regular consumption of certain fruits and vegetables can reduce the risk of many diseases. The rhizome of Zingiber officinale (ginger) is consumed worldwide as a spice and herbal medicine. It contains pungent phenolic substances collectively known as gingerols. 6-Gingerol is the major pharmacologically-active component of ginger. It is known to exhibit a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation. 6-Gingerol has been found to possess anticancer activities via its effect on a variety of biological pathways involved in apoptosis, cell cycle regulation, cytotoxic activity, and inhibition of angiogenesis. Thus, due to its efficacy and regulation of multiple targets, as well as its safety for human use, 6-gingerol has received considerable interest as a potential therapeutic agent for the prevention and/or treatment of various diseases. Taken together, this review summarizes the various in vitro and in vivo pharmacological aspects of 6-gingerol and the underlying mechanisms.

scholarly journals Anticancer Ruthenium(III) Complexes and Ru(III)-Containing Nanoformulations: An Update on the Mechanism of Action and Biological Activity

2019 ◽  
Vol 12 (4) ◽  
pp. 146 ◽  
Author(s):  
Claudia Riccardi ◽  
Domenica Musumeci ◽  
Marco Trifuoggi ◽  
Carlo Irace ◽  
Luigi Paduano ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Anticancer Agents ◽  
Biomedical Applications ◽  
Special Focus ◽  
Anticancer Properties ◽  
Pharmacokinetic Properties ◽  
Pharmacological Potential

The great advances in the studies on metal complexes for the treatment of different cancer forms, starting from the pioneering works on platinum derivatives, have fostered an increasingly growing interest in their properties and biomedical applications. Among the various metal-containing drugs investigated thus far, ruthenium(III) complexes have emerged for their selective cytotoxic activity in vitro and promising anticancer properties in vivo, also leading to a few candidates in advanced clinical trials. Aiming at addressing the solubility, stability and cellular uptake issues of low molecular weight Ru(III)-based compounds, some research groups have proposed the development of suitable drug delivery systems (e.g., taking advantage of nanoparticles, liposomes, etc.) able to enhance their activity compared to the naked drugs. This review highlights the unique role of Ru(III) complexes in the current panorama of anticancer agents, with particular emphasis on Ru-containing nanoformulations based on the incorporation of the Ru(III) complexes into suitable nanocarriers in order to enhance their bioavailability and pharmacokinetic properties. Preclinical evaluation of these nanoaggregates is discussed with a special focus on the investigation of their mechanism of action at a molecular level, highlighting their pharmacological potential in tumour disease models and value for biomedical applications.

scholarly journals THE USE OF ALOE CONSTITUENTS IN SELF-ADMINISTERED CANCER TREATMENT

2012 ◽  
Vol 47 (1) ◽  
Author(s):  
Kelsie E.A. Gillies ◽  
Jonathan Blay
Keyword(s):  
Anticancer Activities ◽  
Anticancer Properties ◽  
Alternative Medicines ◽  
Popular View ◽  
Related Potentials ◽  
Aloe Emodin ◽  
Dry Climates ◽  
Succulent Plants

Complementary and alternative medicines (CAMs) include many different biologic substances that may be ingested or applied topically in an effort to mitigate disease. One source of such substances is the Aloe, a plant that has been used since antiquity to treat a multitude of conditions, and which is now being touted as a potential natural aid in the fight against cancer. There are many different classes of nutrient and modulatory chemicals isolated from Aloe, and some have now been investigated for their anticancer activities. This review will focus on the anticancer properties of four main Aloe components – aloe-emodin, aloin, acemannan and b-sitosterol – in relation to their activities against cells in human cancers and potential abilities to interfere with conventional chemotherapeutics. We build upon this background to consider the validity for Aloe in cancer care. It is evident, after considering both in vitro and in vivo findings, that there needs to be further independent studies examining the safety and efficacy of ingestion of Aloe products for human use, proper standardization of product content, and systematic identification and characterization of the wide variety of Aloe constituents.Aloe is a genus of perennial succulent plants that thrive in hot, dry climates (Choi et al., 2002; Molassiotis et al., 2005). As with many plants, its cosmetic and health-related potentials have been explored since antiquity, and it finds current use in a multitude of cosmetic, dermatologic and other healthcare products (Reynolds and Dweck, 1999; Ulbricht et al., 2007). However, more recently it has fallen into that group of biologics that have found favour in the popular view as a natural remedy for chronic diseases such as cancer. In this review we explore the emerging issue of ‘natural medicines’, the anticancer activities reported for Aloe itself, and provide a perspective on whether Aloe has a place in rational support of the cancer patient.Keywords: Natural products, alternative medicine, aloe, aloe-emodin, aloin, acemannan, cancer.Proceedings of the Nova Scotian Institute of Science (2012)Volume 47, Part 1, pp. 59-89

Parallel Solid-Phase Synthesis using a New Diethylsilylacetylenic Linker and Leading to Mestranol Derivatives with Potent Antiproliferative Activities on Multiple Cancer Cell Lines

2019 ◽  
Vol 18 (10) ◽  
pp. 1469-1481 ◽  
Author(s):  
Raphaël Dutour ◽  
René Maltais ◽  
Martin Perreault ◽  
Jenny Roy ◽  
Donald Poirier
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Solid Phase ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Multiple Cancer ◽  
Anticancer Properties ◽  
Antiproliferative Agent

Background: RM-133 belongs to a new family of aminosteroid derivatives demonstrating interesting anticancer properties, as confirmed in vivo in four mouse cancer xenograft models. However, the metabolic stability of RM-133 needs to be improved. After investigation, the replacement of its androstane scaffold by a more stable estrane scaffold led to the development of the mestranol derivative RM-581. Methods: Using solid-phase strategy involving five steps, we quickly synthesized a series of RM-581 analogs using the recently-developed diethylsilylacetylenic linker. To establish structure-activity relationships, we then investigated their antiproliferative potency on a panel of cancer cell lines from various cancers (breast, prostate, ovarian and pancreatic). Results: Some of the mestranol derivatives have shown in vitro anticancer activities that are close to, or better than, those observed for RM-581. Compound 23, a mestranol derivative having a ((3,5-dimethylbenzoyl)- L-prolyl)piperazine side chain at position C2, was found to be active as an antiproliferative agent (IC50 = 0.38 ± 0.34 to 3.17 ± 0.10 µM) and to be twice as active as RM-581 on LNCaP, PC-3, MCF-7, PANC-1 and OVCAR-3 cancer cells (IC50 = 0.56 ± 0.30, 0.89 ± 0.63, 1.36 ± 0.31, 2.47 ± 0.91 and 3.17 ± 0.10 µM, respectively). Conclusion: Easily synthesized in good yields by both solid-phase organic synthesis and classic solution-phase chemistry, promising compound 23 could be used as an antiproliferative agent on a variety of cancers, notably pancreatic and ovarian cancers, both having very bad prognoses.

scholarly journals Citrus Flavones: An Update on Sources, Biological Functions, and Health Promoting Properties

Plants ◽  
2020 ◽  
Vol 9 (3) ◽  
pp. 288 ◽  
Author(s):  
Davide Barreca ◽  
Giuseppina Mandalari ◽  
Antonella Calderaro ◽  
Antonella Smeriglio ◽  
Domenico Trombetta ◽  
...  
Keyword(s):  
Biological Properties ◽  
Anticancer Activities ◽  
Beneficial Effects ◽  
Biological Potential ◽  
Wide Range ◽  
Health Promoting ◽  
Modulate Signal ◽  
Citrus Spp

Citrus spp. are among the most widespread plants cultivated worldwide and every year millions of tons of fruit, juices, or processed compounds are produced and consumed, representing one of the main sources of nutrients in human diet. Among these, the flavonoids play a key role in providing a wide range of health beneficial effects. Apigenin, diosmetin, luteolin, acacetin, chrysoeriol, and their respective glycosides, that occur in concentrations up to 60 mg/L, are the most common flavones found in Citrus fruits and juices. The unique characteristics of their basic skeleton and the nature and position of the substituents have attracted and stimulated vigorous investigations as a consequence of an enormous biological potential, that manifests itself as (among other properties) antioxidant, anti-inflammatory, antiviral, antimicrobial, and anticancer activities. This review analyzes the biochemical, pharmacological, and biological properties of Citrus flavones, emphasizing their occurrence in Citrus spp. fruits and juices, on their bioavailability, and their ability to modulate signal cascades and key metabolic enzymes both in vitro and in vivo. Electronic databases including PubMed, Scopus, Web of Science, and SciFinder were used to investigate recent published articles on Citrus spp. in terms of components and bioactivity potentials.

scholarly journals Dual-activity PI3K–BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis

2017 ◽  
Vol 114 (7) ◽  
pp. E1072-E1080 ◽  
Author(s):  
Forest H. Andrews ◽  
Alok R. Singh ◽  
Shweta Joshi ◽  
Cassandra A. Smith ◽  
Guillermo A. Morales ◽  
...  
Keyword(s):  
Kinase Activity ◽  
Structural Basis ◽  
Therapeutic Effects ◽  
Cancer Cell Growth ◽  
Cancer Driver ◽  
The Family ◽  
Dual Action ◽  
Tumor Growth And Metastasis

MYC is a major cancer driver but is documented to be a difficult therapeutic target itself. Here, we report on the biological activity, the structural basis, and therapeutic effects of the family of multitargeted compounds that simultaneously disrupt functions of two critical MYC-mediating factors through inhibiting the acetyllysine binding of BRD4 and the kinase activity of PI3K. We show that the dual-action inhibitor impairs PI3K/BRD4 signaling in vitro and in vivo and affords maximal MYC down-regulation. The concomitant inhibition of PI3K and BRD4 blocks MYC expression and activation, promotes MYC degradation, and markedly inhibits cancer cell growth and metastasis. Collectively, our findings suggest that the dual-activity inhibitor represents a highly promising lead compound for the development of novel anticancer therapeutics.

scholarly journals Chemical Composition, Antioxidant, Anticancer Properties and Toxicity Evaluation of Leaf Essential Oil of Cupressus sempervirens

2015 ◽  
Vol 43 (2) ◽  
pp. 320-326 ◽  
Author(s):  
Sayed A. FAYED
Keyword(s):  
Essential Oil ◽  
Cell Lines ◽  
Leukemia Cell ◽  
Cancer Cell Line ◽  
Anticancer Activities ◽  
Cupressus Sempervirens ◽  
Anticancer Properties ◽  
Leukemia Cell Lines

The essential oil isolated by hydro-distillation from Cupressus sempervirens (Cypress) leaves was analysed by GC-MS and tested for antioxidant and in vitro as well as in vivo anticancer activities. In addition, the toxicity effect of the essential oil was studied using normal Swiss mice. Eighteen components of Cypress essential oil were identified and the main essential oil components were α-pinene (29.21%), δ3-carene (18.92%), α-cedrol (12.25%), α-terpinolene (7.66%) and limonene (5.50%). Cupressus sempervirens essential oil was able to reduce the stable, purple-colored radical DPPH into yellow-colored DPPH reaching 50% of reduction with IC50 value = 290.09 μg mL-1. The in vitro anticancer activity of the essential oil was studied against two human promyelocytic leukemia cell lines (HL-60 and NB4) and experimental animals model cancer cell line (EACC). Cypress essential oil exerted the highest cytotoxic activity with a LC50 of 333.79 µg mL-1 against NB4 followed by HL-60 and EACC cell lines (LC50 of 365.41, and 372.43 µg mL-1, respectively). Regarding in vivo anticancer study, pre-initiation treatment with the essential oil was more effective than initiation and post-initiation treatments respectively on the tumor (EACC) transplanted female mice (increase lifespan (%), decrease total EACC number and increase dead cells). In toxicity study, serum urea, transaminases and lactate dehydrogenase were increased. The results obtained from this study showed that the Cypress essential oil possesses antioxidant and anticancer properties, taking into consideration its mild toxicity.

scholarly journals Anti-Cancer Constituents from Plants: Mini Review

2020 ◽  
Vol 19 (1) ◽  
pp. 83-96
Author(s):  
Mohammad Kaisarul Islam ◽  
Animesh Chandra Barman ◽  
Nazmul Qais
Keyword(s):  
Treatment Options ◽  
Minor Effect ◽  
Synthetic Approach ◽  
Anticancer Activities ◽  
Anticancer Properties ◽  
Lead Compounds ◽  
Cellular Factors ◽  
Anti Cancer

Now-a-days, cancer is a major concern globally, for which a large number of deaths occur annually, instead of the accessibility to various treatment options. Nevertheless, the latest treatment options are principally conglomerate with many side effects. Consequently, the development of an effective and competent anticancer therapy with the lower or minimum adverse or unwanted minor effect is the prime direction of research in the fields of natural product chemistry, drug design, and drug discovery. Phytochemicals available in plants have already been proven as prospective candidates in this regard. In general, phytochemicals are non-selective in their functions and restricted due to their differential activity on cancer cells along with the normal cells. As a consequence, researchers show their interest in isolating bioactive phytochemicals from nature with potent anticancer properties and generate lead compounds based on the natural skeleton of a molecule as a synthetic approach. Several phytomolecules have already been in existence for their in-vitro and in-vivo anticancer activities. This article deals with these lead phytomolecules from fifty-two species belong to thirty-five families with their reported mechanisms of action on nuclear and cellular factors involved in the treatment of carcinogenesis. Dhaka Univ. J. Pharm. Sci. 19(1): 83-96, 2020 (June)

scholarly journals PHENOLIC ACID PROFILING BY RP-HPLC: EVALUATION OF ANTIBACTERIAL AND ANTICANCER ACTIVITIES OF CONOCARPUS ERECTUS PLANT EXTRACTS

2020 ◽  
Vol 2020 (1) ◽  
Author(s):  
R Khalil ◽  
Q Ali ◽  
MM Hafeez ◽  
A Malik
Keyword(s):  
Antibacterial Activity ◽  
Anticancer Activity ◽  
Folk Medicine ◽  
Bacterial Strains ◽  
Anticancer Activities ◽  
Anticancer Properties ◽  
Conocarpus Erectus ◽  
Rp Hplc

Due to the versatile application of plants the utilization of plants and their inferred substances builds up day by day for the revelation of new curative agents. Conocarpus erectus has placed in the family Combretaceae, in one of the two species of Conocarpus genus and ordinarily exists in tropical and subtropical regions of the world. In some countries it is used as folk medicine for fever, anemia, diabetes, catarrh, diarrhea and conjunctivitis. The current study was carried out to investigate the antibacterial and anticancer properties of the plant. The four defatted methanol extracts of C. erectus different parts (leaves, stems, fruits and bark) showed high antibacterial and anticancer activity even with small quantity of dose. Antimicrobial assay was used to check out the antibacterial activity against 6 bacterial strains Escherichia coli, Staphylococcus Aureus and Klebstella Pneumoniae.  The results show that gram positive bacteria show more sensitivity and zone of inhibition as compared to gram negative bacteria. For anticancer activity, MTT assay was performed on HepG2 cells for this purpose. Plant extorts show anticancer activity with a minute quantity. For phytochemical screening defatted methanol extract of Conocarpus erectus was subjected to the silica gel glass column go behind by (RP-HPLC–UV–ESI-MS). It contains phenol such as tannin and flavinoid as major component. Plant contain Ellagic acid; di-hexahydroxy diphenyl, Vascalgin isomer as foremost tannin component. Gallic Acid, Kaempferol on the base of mass spectra and time of retention. The extract of Conocarpus erectus (leaves, shoot, bark & fruit) parts shows high antibacterial, antioxidant and hepta-protective activities due to phenolic content. Tannin has high antibacterial activity than other compound. C.erectus is notable for its folkloristic curative potential. More in vivo and in vitro phytochemical studies are needed to use the plant for prevention and treatment of many diseases.

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