Structure Activity Relationship of Xanthones for Inhibition of Cyclin Dependent Kinase 4 from Mangosteen (Garcinia Mangostana L.

Vemu, Bhaskar; Nauman, Mirielle C.; Veenstra, Jacob P.; Johnson, Jeremy J.

doi:10.14302/issn.2379-7835.ijn-19-2845

Cited by 21 publications

(11 citation statements)

References 20 publications

(29 reference statements)

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“…Mangosteen xanthones, especially MAG and GA, have been proven to display significant chemo-preventive and anticancer properties against numerous tumor types [12,[15][16][17][25][26][27]. Moreover, chemical modification of the xanthone structure is believed to further increase the anticancer properties, as described in [28,29].…”

Section: Discussionmentioning

confidence: 99%

Novel Xanthone Derivatives Impair Growth and Invasiveness of Colon Cancer Cells In Vitro

et al. 2021

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Natural xanthones are a large group of compounds from which promising anticancer properties could be further developed by chemical modifications. This study aimed to investigate the influence of four novel xanthone derivatives based on a naturally occurring xanthone skeleton on the invasiveness of colon cancer cells in vitro. First, the concentrations required to inhibit growth of three colorectal cancer cell lines to 50% (GI50) of all the studied compounds, as well as the natural xanthones used as a reference (gambogic acid and α-mangostin), have been established (MTS reduction test). Next, the assays determining several aspects of the GI25 xanthones influence on colorectal cancer cells, including cytotoxicity, migration and invasion potential, interaction with extracellular matrix and endothelial cells, as well as expression of selected invasiveness related genes have been performed. Our results demonstrate that these novel xanthone derivatives impair colorectal cancer proliferation, motility, adhesion to extracellular matrix and to endothelial cells, and also induce apoptosis and cell death. Moreover, their activity is comparable to cisplatin and 5-fluorouracil, used as reference compounds. Conducted research indicates our compounds for further research and development as novel drugs in colorectal cancer treatment.

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Section: Discussionmentioning

confidence: 99%

Novel Xanthone Derivatives Impair Growth and Invasiveness of Colon Cancer Cells In Vitro

et al. 2021

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“…Based on the previous studies on Garcinia mangostana, so far, researchers have found at least 80 types of xanthone compounds in various parts of the plant (Vemu, Nauman, Veenstra, & Johnson, 2019). Mangosteen pericarp has been proven by Ibrahim et al (2016) and another study of Mamat, Azizan, Baharum, Mohd Noor, and Mohd Aizat (2018) to contain high content of secondary metabolites such as xanthones, flavonoids, triterpenes and benzophenones (Ibrahim et al, 2016;Mamat et al, 2018).…”

Section: Sciex Internal Databasementioning

confidence: 99%

Enzyme-Assisted Water Extraction Optimization, Antioxidant Capacity and Phenolic Profiling of Extracts from Garcinia Mangostana Linn

Tan

Soo²,

Khor

et al. 2022

jftr

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The application of enzymes in extraction processes within the food industry has not been widely explored. In this paper, an enzyme-assisted water extraction method was employed and optimized to extract the antioxidative and phenolic compounds from the pericarp of Garcinia mangostana L. Fractional factorial design (FFD) was developed to screen out the significant factors from five extraction parameters, including enzyme concentration, liquid-solid ratio, reaction temperature, pH and reaction time. Next, a central composite design approach was used to optimize the significant parameters after the screening process. The optimal conditions according to statistical analysis were 1.46% w/w of enzyme (Celluclast® 1.5L & Pectinex® Ultra SP-L) concentration, 22.80 liquid-solid ratio, reaction temperature of 30 °C, pH 3 and 30 min of reaction time. Under the optimized conditions, antioxidant activities indicated by the 2,2-Diphenyl-2-picrylhydrazyl (DPPH) and 2,2’-azinobis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) values and total phenolic content obtained were 86.51%, 86.77% and 21.222 mg gallic acid equivalent (GAE)/g, respectively.

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“…Thus, it was suggested that the use of antioxidants are ideal to treat this inflammatory disorder (Pleguezuelos-Villa et al, 2019). As a rich source of natural antioxidants and anti-inflammatory compounds, all parts of the xanthone-rich G. mangostana L. plant were traditionally consumed and utilized for the treatment of psoriasis (Ibrahim et al, 2018a;Ibrahim et al, 2018b;Vemu et al, 2019).…”

Section: Psoriasismentioning

confidence: 99%

Natural Xanthones and Skin Inflammatory Diseases: Multitargeting Mechanisms of Action and Potential Application

et al. 2020

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The pathogenesis of skin inflammatory diseases such as atopic dermatitis, acne, psoriasis, and skin cancers generally involve the generation of oxidative stress and chronic inflammation. Exposure of the skin to external aggressors such as ultraviolet (UV) radiation and xenobiotics induces the generation of reactive oxygen species (ROS) which subsequently activates immune responses and causes immunological aberrations. Hence, antioxidant and anti-inflammatory agents were considered to be potential compounds to treat skin inflammatory diseases. A prime example of such compounds is xanthone (xanthene-9-one), a class of natural compounds that possess a wide range of biological activities including antioxidant, anti-inflammatory, antimicrobial, cytotoxic, and chemotherapeutic effects. Many studies reported various mechanisms of action by xanthones for the treatment of skin inflammatory diseases. These mechanisms of action commonly involve the modulation of various pro-inflammatory cytokines such as interleukin (IL)-1β, IL-6, IL-8, and tumor necrosis factor α (TNF-α), as well as anti-inflammatory cytokines such as IL-10. Other mechanisms of action include the regulation of NF-κB and MAPK signaling pathways, besides immune cell recruitment via modulation of chemokines, activation, and infiltration. Moreover, disease-specific activity contributed by xanthones, such as antibacterial action against Propionibacterium acnes and Staphylococcus epidermidis for acne treatment, and numerous cytotoxic mechanisms involving pro-apoptotic and anti-metastatic effects for skin cancer treatment have been extensively elucidated. Furthermore, xanthones have been reported to modulate pathways responsible for mediating oxidative stress and inflammation such as PPAR, nuclear factor erythroid 2-related factor and prostaglandin cascades. These pathways were also implicated in skin inflammatory diseases. Xanthones including the prenylated α-mangostin (2) and γ-mangostin (3), glucosylated mangiferin (4) and the caged xanthone gambogic acid (8) are potential lead compounds to be further developed into pharmaceutical agents for the treatment of skin inflammatory diseases. Future studies on the structure-activity relationships, molecular mechanisms, and applications of xanthones for the treatment of skin inflammatory diseases are thus highly recommended.

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Structure Activity Relationship of Xanthones for Inhibition of Cyclin Dependent Kinase 4 from Mangosteen (Garcinia Mangostana L.

Cited by 21 publications

References 20 publications

Novel Xanthone Derivatives Impair Growth and Invasiveness of Colon Cancer Cells In Vitro

Novel Xanthone Derivatives Impair Growth and Invasiveness of Colon Cancer Cells In Vitro

Enzyme-Assisted Water Extraction Optimization, Antioxidant Capacity and Phenolic Profiling of Extracts from Garcinia Mangostana Linn

Natural Xanthones and Skin Inflammatory Diseases: Multitargeting Mechanisms of Action and Potential Application

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