Prostaglandin receptor EP2 in the crosshairs of anti-inflammation, anti-cancer, and neuroprotection

Background: Oils and fats are the densest sources of food energy among food groups. Vegetable oils are constituted predominantly of triglycerides. Due to the importance of edible oils in nutrition, food industry and human health, great attention has been paid to them in recent years. Some minor bioactive constituents in oils include phospholipids, tocols, sterols, carotenoid, chlorophyll, phenols, phylokynon and terpenes. Objective: The aim of the present study was to examine beneficial effects of minor compounds in edible oils on human health. Results: Minor compounds of edible oils that we use daily can produce remarkable results in the prevention and treatment of various diseases like diabetes, inflammation, hypertension, cancer, allergy and central nervous system disorders due to their antimicrobial, anti-cancer, anti-viral, anti-oxidative, anti-inflammation, anti-mutagenic, hypolipidemic, and hypoglycemic properties, among others. Conclusion: The results of this study showed that the presence of beneficial minor compounds in oils could have significant impact on the prevention and treatment of various diseases. Therefore, the type of consumed oil can play an important role in human health.

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Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

International Journal of Molecular Sciences ◽

10.3390/ijms20174238 ◽

2019 ◽

Vol 20 (17) ◽

pp. 4238 ◽

Cited By ~ 15

Author(s):

Yaqi Ren ◽

Chunlan Wang ◽

Jiakun Xu ◽

Shuaiyu Wang

Keyword(s):

Furan Ring ◽

Biological Activities ◽

Pharmacological Properties ◽

Coffee Beans ◽

Anti Cancer ◽

Underlying Mechanisms ◽

Target Alternative ◽

Anti Inflammation

Cafestol and kahweol are natural diterpenes extracted from coffee beans. In addition to the effect of raising serum lipid, in vitro and in vivo experimental results have revealed that the two diterpenes demonstrate multiple potential pharmacological actions such as anti-inflammation, hepatoprotective, anti-cancer, anti-diabetic, and anti-osteoclastogenesis activities. The most relevant mechanisms involved are down-regulating inflammation mediators, increasing glutathione (GSH), inducing apoptosis of tumor cells and anti-angiogenesis. Cafestol and kahweol show similar biological activities but not exactly the same, which might due to the presence of one conjugated double bond on the furan ring of the latter. This review aims to summarize the pharmacological properties and the underlying mechanisms of cafestol-type diterpenoids, which show their potential as functional food and multi-target alternative medicine.

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Protection against peroxynitrite-induced DNA damage by mesalamine: implications for anti-inflammation and anti-cancer activity

Molecular and Cellular Biochemistry ◽

10.1007/s11010-013-1620-z ◽

2013 ◽

Vol 378 (1-2) ◽

pp. 291-298 ◽

Cited By ~ 10

Author(s):

Paul M. Graham ◽

Jason Z. Li ◽

Xueging Dou ◽

Hong Zhu ◽

Hara P. Misra ◽

...

Keyword(s):

Dna Damage ◽

Anti Cancer ◽

Anti Inflammation ◽

Cancer Activity

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An Updated Review on Pharmaceutical Properties of Gamma-Aminobutyric Acid

Molecules ◽

10.3390/molecules24152678 ◽

2019 ◽

Vol 24 (15) ◽

pp. 2678 ◽

Cited By ~ 18

Author(s):

Dai-Hung Ngo ◽

Thanh Sang Vo

Keyword(s):

Neuronal Development ◽

Aminobutyric Acid ◽

Gamma Aminobutyric Acid ◽

Peripheral Tissues ◽

Inhibitory Neurotransmitter ◽

Anti Cancer ◽

The Central Nervous System ◽

Potential Alternative ◽

Pharmaceutical Properties ◽

Anti Inflammation

Gamma-aminobutyric acid (Gaba) is a non-proteinogenic amino acid that is widely present in microorganisms, plants, and vertebrates. So far, Gaba is well known as a main inhibitory neurotransmitter in the central nervous system. Its physiological roles are related to the modulation of synaptic transmission, the promotion of neuronal development and relaxation, and the prevention of sleeplessness and depression. Besides, various pharmaceutical properties of Gaba on non-neuronal peripheral tissues and organs were also reported due to anti-hypertension, anti-diabetes, anti-cancer, antioxidant, anti-inflammation, anti-microbial, anti-allergy, hepato-protection, reno-protection, and intestinal protection. Therefore, Gaba may be considered as potential alternative therapeutics for prevention and treatment of various diseases. Accordingly, this updated review was mainly focused to describe the pharmaceutical properties of Gaba as well as emphasize its important role regarding human health.

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Synthesis of Daidzein Glycosides, α-Tocopherol Glycosides, Hesperetin Glycosides by Bioconversion and Their Potential for Anti-Allergic Functional-Foods and Cosmetics

Molecules ◽

10.3390/molecules24162975 ◽

2019 ◽

Vol 24 (16) ◽

pp. 2975

Author(s):

Yuya Fujitaka ◽

Hiroki Hamada ◽

Daisuke Uesugi ◽

Atsuhito Kuboki ◽

Kei Shimoda ◽

...

Keyword(s):

Inhibitory Activity ◽

Water Solubility ◽

Biological Activities ◽

Biological Effects ◽

Physicochemical Stability ◽

Peritoneal Mast Cells ◽

Anti Cancer ◽

New Compounds ◽

Poor Absorption ◽

Anti Inflammation

Daidzein is a common isoflavone, having multiple biological effects such as anti-inflammation, anti-allergy, and anti-aging. α-Tocopherol is the tocopherol isoform with the highest vitamin E activity including anti-allergic activity and anti-cancer activity. Hesperetin is a flavone, which shows potent anti-inflammatory effects. These compounds have shortcomings, i.e., water-insolubility and poor absorption after oral administration. The glycosylation of bioactive compounds can enhance their water-solubility, physicochemical stability, intestinal absorption, and biological half-life, and improve their bio- and pharmacological properties. They were transformed by cultured Nicotiana tabacum cells to 7-β-glucoside and 7-β-gentiobioside of daidzein, and 3′- and 7-β-glucosides, 3′,7-β-diglucoside, and 7-β-gentiobioside of hesperetin. Daidzein and α-tocopherol were glycosylated by galactosylation with β-glucosidase to give 4′- and 7-β-galactosides of daidzein, which were new compounds, and α-tocopherol 6-β-galactoside. These nine glycosides showed higher anti-allergic activity, i.e., inhibitory activity toward histamine release from rat peritoneal mast cells, than their respective aglycones. In addition, these glycosides showed higher tyrosinase inhibitory activity than the corresponding aglycones. Glycosylation of daidzein, α-tocopherol, and hesperetin greatly improved their biological activities.

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Absorption of polymethoxyflavones and their derivatives

Journal of Food Bioactives ◽

10.31665/jfb.2018.2142 ◽

2018 ◽

Vol 2 ◽

Cited By ~ 2

Author(s):

Ruolin L.Y. Wang ◽

Shiming Li ◽

Chi-Tang Ho

Keyword(s):

Water Solubility ◽

Transport Model ◽

Biological Activities ◽

Cell Monolayer ◽

Aqueous Solubility ◽

High Permeability ◽

Anti Cancer ◽

Antioxidant Effects ◽

Anti Inflammation ◽

Nutraceutical Products

Polymethoxyflavones (PMFs) are a group of flavonoids found exclusively in citrus genus that have been identified with many potent biological activities, including anti-inflammation, anti-cancer, anti-atherosclerosis, and antioxidant effects. However, the bioavailability of PMFs is seldom studied. Evaluating by aqueous solubility and permeability, absorption is the first indicator of bioavailability. In this research, we systemically investigated permeability and solubility of six PMFs and their derivatives, namely, sinensetin (SIN), 5-demethylsinensetin (5-OHSIN), 5-acetylsinensetin (5-AcSIN), 3,5,6,7,8,3′,4′-heptamethoxyflavone (HeptaMF), 5-hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone (5-OHHeptaMF), and 5-acetyl-3,6,7,8,3′,4′-hexamethoxyflavone (5-AcHeptaMF). From octanol/water solubility test, we found that PMFs and their derivatives had very low aqueous solubility. Permeability experiment via Caco-2 cell monolayer transport model indicated high permeability of all the tested compounds. Furthermore, PMFs had the greatest permeability, followed by 5-acetyl PMFs and 5-hydroxylated PMFs. Considering permeability and solubility together, PMFs and their derivatives are expected to have good absorption. This study provides indicative information on the bioavailability of PMFs and their derivatives, which offers clues on the application of PMFs in functional food or nutraceutical products.

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Characterisation and Bioactivity Analysis of Peridinin-Chlorophyll a-Protein (PCP) Isolated from Symbiodinium tridacnidorum CS-73

Journal of Marine Science and Engineering ◽

10.3390/jmse9121387 ◽

2021 ◽

Vol 9 (12) ◽

pp. 1387

Author(s):

Kanoknate M. Supasri ◽

Manoj Kumar ◽

Anna Segečová ◽

Janice I. McCauley ◽

Andrei Herdean ◽

...

Keyword(s):

Amino Acid ◽

Chlorophyll A ◽

Rna Binding ◽

Biological Activities ◽

Metastatic Breast ◽

Spectroscopic Properties ◽

Breast Adenocarcinoma ◽

Pharmaceutical Applications ◽

Anti Cancer ◽

Anti Inflammation

Peridinin-Chlorophyll a-Proteins (PCP) are the major light harvesting proteins in photosynthetic dinoflagellates. PCP shows great variation in protein length, pigment ratio, sequence, and spectroscopic properties. PCP conjugates (PerCP) are widely used as fluorescent probes for cellular and tissue analysis in the biomedical field. PCP consists of a peridinin carotenoid; thereby, it can potentially be used as a bioactive compound in pharmaceutical applications. However, the biological activities of PCP are yet to be explored. In this study, we extracted, purified, and partially characterised the PCP from Symbiodinium tridacnidorum (CS-73) and explored its antioxidant, anti-cancer and anti-inflammation bioactivities. The PCP was purified using an ÄKTA™ PURE system and predicted to be of 17.3 kDa molecular weight (confirmed as a single band on SDS-PAGE) with an isoelectric point (pI) 5.6. LC-MS/MS and bioinformatic analysis of purified PCP digested with trypsin indicated it was 164 amino acids long with >90% sequence similarity to PCP of SymA3.s6014_g3 (belonging to clade A of Symbiodinium sp.) confirmed with 59 peptide combinations matched across its protein sequence. The spectroscopic properties of purified PCP showed a slight shift in absorption and emission spectra to previously documented analysis in Symbiodinium species possibly due to variation in amino acid sequences that interact with chl a and peridinin. Purified PCP consisted of a 19-amino-acid-long signal peptide at its N terminal and nine helixes in its secondary structure, with several protein binding sites and no DNA/RNA binding site. Furthermore, purified PCP exhibited antioxidant and in vitro anti-inflammation bioactivities, and anti-cancer activities against human metastatic breast adenocarcinoma (MDA-MB-231) and human colorectal (HTC-15) cancer cell lines. Together, all these findings present PCP as a promising candidate for continued investigations for pharmaceutical applications to cure chronic diseases, apart from its existing application as a fluorescent-probe.

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Pinocembrin alleviates ulcerative colitis in mice via regulating gut microbiota, suppressing TLR4/MD2/NF-κB pathway and promoting intestinal barrier

Bioscience Reports ◽

10.1042/bsr20200986 ◽

2020 ◽

Vol 40 (7) ◽

Cited By ~ 2

Author(s):

Bei Yue ◽

Junyu Ren ◽

Zhilun Yu ◽

Xiaoping Luo ◽

Yijing Ren ◽

...

Keyword(s):

Gut Microbiota ◽

Intestinal Barrier ◽

Signaling Cascades ◽

Toll Like Receptor 4 ◽

Dss Colitis ◽

Anti Cancer ◽

Anti Inflammation ◽

Junction Proteins

Abstract Pinocembrin, a plant-derived flavonoid, has a variety of pharmacological activities, including anti-infection, anti-cancer, anti-inflammation, cardiovascular protection, etc. However, the mechanism of pinocembrin on the anti-colitis efficacy remains elusive and needs further investigation. Here, we reported that pinocembrin eased the severity of dextran sulfate sodium (DSS)-induced colitis in mice by suppressing the abnormal activation of toll-like receptor 4 (TLR4)/nuclear factor-kappa B (NF-κB) signal pathway in vivo. In addition, the gut microbiota was disordered in DSS colitis mice, which was associated with a significant decrease in microbiota diversity and a great shift in bacteria profiles; however, pinocembrin treatment improved the imbalance of gut microbiota and made it similar to that in normal mice. On the other hand, in vitro, pinocembrin down-regulated the TLR4/NF-κB signaling cascades in lipopolysaccharide (LPS)-stimulated macrophages. At the upstream level, pinocembrin competitively inhibited the binding of LPS to myeloid differentiation protein 2 (MD2), thereby blocking the formation of receptor multimer TLR4/MD2·LPS. Furthermore, pinocembrin dose-dependently promoted the expression of tight junction proteins (ZO-1, Claudin-1, Occludin and JAM-A) in Caco-2 cells. In conclusion, our work presented evidence that pinocembrin attenuated DSS-induced colitis in mouse, at least in part, via regulating intestinal microbiota, inhibiting the over-activation of TLR4/MD2/NF-κB signaling pathway, and improving the barriers of intestine.

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Medicinal Plant Centipeda Minima: A Resource of Bioactive Compounds

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557520666201021143257 ◽

2020 ◽

Vol 20 ◽

Author(s):

Nguyen Thi Thuy Linh ◽

Nguyen Thi Thu Ha ◽

Nguyen Thanh Tra ◽

Le Thi Tu Anh ◽

Nguyen Van Tuyen ◽

...

Keyword(s):

Whooping Cough ◽

Sesquiterpene Lactones ◽

Herbaceous Plant ◽

Nasal Allergy ◽

Tropical Regions ◽

Tropical Asia ◽

Anti Cancer ◽

The Family ◽

Centipeda Minima ◽

Anti Inflammation

Background: Centipeda minima (the family Asteraceae) is an annual herbaceous plant native to the tropical regions, especially in eastern tropical Asia. C. minima is well-known in the list of medicinal plants with capacities in treatment of whooping cough, nasal allergy, malaria, and asthma. More than sixty reports on phytochemical and pharmacological aspects of this plant are now available, but a supportive review is insufficient. Objective: The current review aims to make a compilation of almost of isolated compounds from the title plant together with their pharmacological activities. Methodology: Centipeda minima is the meaningful keyword to search for previous references, while the reliable databases such as Sci-Finder, Google Scholar, Pub Med, Science Direct, the Web of Science, Scopus, Bentham science, Taylor Francis, Springer, IOP Science have been utilized at most. Conclusion: More than one hundred secondary metabolites, classifying as terpenoids, flavonoids, mono-phenols, fatty acids, amides, and other types, were isolated from this plant. Among them, sesquiterpene lactones are dominant in either C. minima species or numerous plants of genus Centipeda. These phytochemical groups also possessed various biological results like anti-cancer, anti-bacteria, anti-allergy, antivirus, anti-inflammation, hepatoprotective activities. With many kinds of bioactive results such as anti-cancer, antiinflammation, the use of C. minima plant extracts and isolated compounds for drug development seems to be a futuristic strategy.

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