Astaxanthin sources:  Suitability for human health and nutrition

Background: Astaxanthin (AX) has been consumed as a nutritional supplement for approximately twenty years. The primary source has been a natural plant-based supplement from the single-cell alga Haematococcus pluvialis (NAT-AX). Recently, Astaxanthin from other sources has entered the marketplace. The primary alternative source in the human nutritional supplement market has been a synthetic form of Astaxanthin produced from petrochemicals (SYN-AX). Additionally, a very small amount of Astaxanthin from a genetically-manipulated yeast Xanthophyllomyces dendrorhous (former nomenclature Phaffia rhodozyma, still commonly referred to as “Phaffia”) (PH-AX) is also available in some supplement products. The three forms have substantial chemical differences. In addition to the chemical differences between sources of AX, in-vitro research has demonstrated profound differences in antioxidant strength and animal research has revealed fundamental differences in health benefits. In all cases, NAT-AX has proven more biologically active than the other sources. This review is designed to assist readers in understanding which form(s) of AX are suitable for consumers desiring preventive or therapeutic health benefits. Results: In head-to-head antioxidant experiments, NAT-AX demonstrated 14X to 90X greater antioxidant activity than SYN-AX. In numerous animal trials in diverse species, NAT-AX in esterified form has demonstrated superior efficacy in increasing lifespan; treating skin cancer; preventing the formation of gastric ulcers; improving resistance to stress; decreasing reactive oxygen species (ROS); increasing retinol conversion in the liver; augmenting enzyme levels; increasing growth rates; and improving exercise endurance.From a safety perspective, NAT-AX has been the subject of human clinical trials demonstrating safety and a wide variety of health benefits. In addition, no documented adverse events have surfaced during its twenty years of distribution as a food supplement for humans. SYN-AX and PH-AX have not been proven safe for direct human consumption and have not demonstrated any health benefits in clinical trials. Due to these facts, SYN-AX and PH-AX have not been allowed for human consumption by government regulators in many countries while NAT-AX is widely accepted in most countries around the world. Conclusion: Based on our review of the literature below, we recommend NAT-AX as the sole form of AX for human consumption until SYN-AX and PH-AX have been proven safe and efficacious through human clinical research.

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Fermented Foods: Definitions and Characteristics, Impact on the Gut Microbiota and Effects on Gastrointestinal Health and Disease

Nutrients ◽

10.3390/nu11081806 ◽

2019 ◽

Vol 11 (8) ◽

pp. 1806 ◽

Cited By ~ 38

Author(s):

Eirini Dimidi ◽

Selina Rose Cox ◽

Megan Rossi ◽

Kevin Whelan

Keyword(s):

Controlled Trial ◽

Health Benefits ◽

Biologically Active ◽

Fermented Foods ◽

Lactose Malabsorption ◽

Gastrointestinal Health ◽

Sourdough Bread ◽

Health And Disease ◽

The Impact

Fermented foods are defined as foods or beverages produced through controlled microbial growth, and the conversion of food components through enzymatic action. In recent years, fermented foods have undergone a surge in popularity, mainly due to their proposed health benefits. The aim of this review is to define and characterise common fermented foods (kefir, kombucha, sauerkraut, tempeh, natto, miso, kimchi, sourdough bread), their mechanisms of action (including impact on the microbiota), and the evidence for effects on gastrointestinal health and disease in humans. Putative mechanisms for the impact of fermented foods on health include the potential probiotic effect of their constituent microorganisms, the fermentation-derived production of bioactive peptides, biogenic amines, and conversion of phenolic compounds to biologically active compounds, as well as the reduction of anti-nutrients. Fermented foods that have been tested in at least one randomised controlled trial (RCT) for their gastrointestinal effects were kefir, sauerkraut, natto, and sourdough bread. Despite extensive in vitro studies, there are no RCTs investigating the impact of kombucha, miso, kimchi or tempeh in gastrointestinal health. The most widely investigated fermented food is kefir, with evidence from at least one RCT suggesting beneficial effects in both lactose malabsorption and Helicobacter pylori eradication. In summary, there is very limited clinical evidence for the effectiveness of most fermented foods in gastrointestinal health and disease. Given the convincing in vitro findings, clinical high-quality trials investigating the health benefits of fermented foods are warranted.

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SPIRULINA – A WONDER NUTRACEUTICAL AGAINST CANCER: A REVIEW

PLANT ARCHIVES ◽

10.51470/plantarchives.2021.v21.no1.177 ◽

2021 ◽

Vol 21 (No 1) ◽

Author(s):

Kawalpreet Kaur ◽

Saranjeet Kaur

Keyword(s):

Systematic Review ◽

Clinical Trials ◽

Biologically Active ◽

Human Cell Lines ◽

Endonuclease Activity ◽

Blue Green Alga ◽

Skin Cancers ◽

Mechanism Of Carcinogenesis ◽

Induction Of Apoptosis

Spirulina, a filamentous and spiral-shaped blue-green alga, contains an array of bioactive compounds and has emerged to be a nutraceutical. It has a unique blend of around 70 biologically active compounds which enhances its therapeutic significance. Its role against carcinogenesis can be attributed to its antioxidant and anti-inflammatory properties due to the presence of ingredients like C-Phycocyanin, ?-Carotene, Calcium Spirulan, Linoleic and Linolenic acids. Spirulina extracts were shown to enhance endonuclease activity, DNA repair and induction of apoptosis in cells. Some studies also reported myelosuppression and enhanced immune function. Murine studies indicated there was a possibility of reversing the mechanism of carcinogenesis, particularly in oral, stomach, breast and skin cancers as well as in doxorubicin, cyclophosphamide and DBMA-induced tumours. Spirulina also appeared to reduce cardio-, nephro- and hepato-toxicity in rodents. The chemo and radioprotective effect of Spirulina was also observed in various carcinogenic human cell lines. The C-phycocyanin component was shown to induce apoptosis in HeLa cells in vitro. Commercially available Spirulina is administered as an adjunct to chemotherapy. The evidence of effectiveness of Spirulina in cancer is extremely limited as far as the clinical trials are concerned. The Spirulina studies conducted on various types of carcinogenesis show a degree of similitude but are in a haphazard state. The current anatomization is an attempt on part of the authors to coalesce all the contemporaneous data and create a systematic review.

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Steroid sulfatase inhibitors for estrogen- and androgen-dependent cancers

Journal of Endocrinology ◽

10.1530/joe-11-0266 ◽

2011 ◽

Vol 212 (2) ◽

pp. 99-110 ◽

Cited By ~ 81

Author(s):

Atul Purohit ◽

Paul A Foster

Keyword(s):

Clinical Trials ◽

Dehydroepiandrosterone Sulfate ◽

Biologically Active ◽

Steroid Sulfatase ◽

Developmental History ◽

Estrone Sulfate ◽

Therapy Targets ◽

History Of

Estrogens and androgens are instrumental in the maturation of many hormone-dependent cancers. Consequently, the enzymes involved in their synthesis are cancer therapy targets. One such enzyme, steroid sulfatase (STS), hydrolyses estrone sulfate, and dehydroepiandrosterone sulfate to estrone and dehydroepiandrosterone respectively. These are the precursors to the formation of biologically active estradiol and androstenediol. This review focuses on three aspects of STS inhibitors: 1) chemical development, 2) biological activity, and 3) clinical trials. The aim is to discuss the importance of estrogens and androgens in many cancers, the developmental history of STS inhibitor synthesis, the potency of these compounds in vitro and in vivo and where we currently stand in regards to clinical trials for these drugs. STS inhibitors are likely to play an important future role in the treatment of hormone-dependent cancers. Novel in vivo models have been developed that allow pre-clinical testing of inhibitors and the identification of lead clinical candidates. Phase I/II clinical trials in postmenopausal women with breast cancer have been completed and other trials in patients with hormone-dependent prostate and endometrial cancer are currently active. Potent STS inhibitors should become therapeutically valuable in hormone-dependent cancers and other non-oncological conditions.

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β- sitosterol in Various Pathological Conditions: An Update

Current Bioactive Compounds ◽

10.2174/1573407218666211230144036 ◽

2021 ◽

Vol 18 ◽

Author(s):

Poonam Yadav ◽

Chandan Chauhan ◽

Sanjiv Singh ◽

Sugato Banerjee ◽

Krishna Murti

Keyword(s):

Plasma Membranes ◽

Biological Activities ◽

Pharmacological Action ◽

Nutritional Supplement ◽

Biologically Active ◽

Lipid Lowering ◽

Protective Effects ◽

Nonalcoholic Fatty Liver

Abstract: Phytosteroids are biologically active compounds found naturally in herb plasma membranes, with a chemical composition similar to animal plasma membrane cholesterol. It can be found in almost all fats abundant plant’s diets. One of the vital phytosterols is β-sitosterol which has several biological activities. It has been proved in various in-vivo and in-vitro research in which β-sitosterol stabilized several physiological activities like as antioxidant, CNS activity (like anti-alzheimer, anxiolytic and sedative effects, CNS depressant activity), lipid-lowering effects (like nonalcoholic fatty liver disease), antidiabetic, anti-inflammatory and analgesic effects, anticancer and immunomodulatory, protective effects in pulmonary fibrosis, wound healing effects and anti-viral and COVID-19 activity. The experimental research on β-sitosterol shows that it can be used as a nutritional supplement to combat various existing diseases. In this review, we are highlighting the most significant pharmacological action of β-sitosterol on the basis of available literature.

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Health Benefits of Quercetin

Defence Life Science Journal ◽

10.14429/dlsj.2.11359 ◽

2017 ◽

Vol 2 (2) ◽

pp. 142 ◽

Cited By ~ 9

Author(s):

R. Kumar ◽

S. Vijayalakshmi ◽

S. Nadanasabapathi

Keyword(s):

Health Benefits ◽

Natural Antioxidants ◽

Black Tea ◽

Biological Properties ◽

Biologically Active ◽

In Vivo Studies ◽

Agricultural Produce ◽

Storage Effects

Flavonoids are natural antioxidants derived from plant pigments and commonly found in agricultural produce such as fruits, vegetables, and also in beverages like tea and wine. Quercetin is the most important flavonoid which belongs to the class of flavonol. Quercetin is a vital biologically active compound, which is present in many products, such as onion (Allium cepa), black tea (Camellia sinensis), Broccoli (Brassica oleracea var. italic), and also in red wine and green tea, It is widely used in medicine and pharmaceutics. In particular, it is used for cancer treatment; as it restrains the growth of cancer cells. Earlier some of computational investigations of this molecule were reported in literature, but they were made at low theory level. Quercetin provided many health promoting benefits, like cardiovascular properties, cancer reducing agent, Anti-inflammatory, asthma and many more. That is why the further investigation of this molecule is important. The main important of this review is to understanding of the structure of quercetin and corresponding biological properties of quercetin expressed in vitro studies, absorption is critical, but in vivo studies, better absorbed antioxidant were observed like vitamin C, further reported studies on effect of food processing, health benefits, storage effects, and evaluate its safety and dosage.

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Modern Trends in the In Vitro Production and Use of Callus, Suspension Cells and Root Cultures of Medicinal Plants

Molecules ◽

10.3390/molecules25245805 ◽

2020 ◽

Vol 25 (24) ◽

pp. 5805

Author(s):

Olga Babich ◽

Stanislav Sukhikh ◽

Artem Pungin ◽

Svetlana Ivanova ◽

Lyudmila Asyakina ◽

...

Keyword(s):

Medicinal Plants ◽

Higher Plants ◽

Raw Materials ◽

Extraction Process ◽

Biologically Active ◽

Root Cultures ◽

In Vitro Production ◽

Suspension Cells ◽

Alternative Source

This paper studies modern methods of producing and using callus, suspension cells and root cultures of medicinal plants in vitro. A new solution for natural product production is the use of an alternative source of renewable, environmentally friendly raw materials: callus, suspension and root cultures of higher plants in vitro. The possibility of using hairy root cultures as producers of various biologically active substances is studied. It is proven that the application of the genetic engineering achievements that combine in vitro tissue culture and molecular biology methods was groundbreaking in terms of the intensification of the extraction process of compounds significant for the medical industry. It is established that of all the callus processing methods, suspension and root cultures in vitro, the Agrobacterium method is the most widely used in practice. The use of agrobacteria has advantages over the biolistic method since it increases the proportion of stable transformation events, can deliver large DNA segments and does not require special ballistic devices. As a result of the research, the most effective strains of agrobacteria are identified.

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Effect of light on contents of coumarin compounds in shoots of Ruta graveolens L. cultivated in vitro

Acta Societatis Botanicorum Poloniae ◽

10.5586/asbp.1999.026 ◽

2014 ◽

Vol 68 (3) ◽

pp. 197-200 ◽

Cited By ~ 7

Author(s):

Halina Ekiert ◽

Ewa Gomółka

Keyword(s):

Shoot Culture ◽

Total Content ◽

Biologically Active ◽

Artificial Light ◽

Ruta Graveolens ◽

Light Conditions ◽

Alternative Source ◽

Stationary Liquid ◽

Coumarin Compounds

Shoots of Ruta graveolens L. (Rutaceae) were cultivated in stationary liquid culture under different light conditions: constant artificial light (900 lx), darkness, constant artificial light (900 ix) following irradiation with UV-C light. The contents of five furanocoumarins: psoralen, bergapten, xanthotoxin, isopimpinellin and imperatorin, as well as biogenetic precursor of these metabolites, umbelliferone, were determined by HPLC method in shoots cultivated in vitro and in overground parts of plants growing in open air. It was shown that light conditions, tested in these experiments, significantly influenced contents of the metabolites in shoots cultivated in in vitro culture. Total content of the coumarin compounds in shoots cultivated under constant artificial light (900 lx) was equal or higher than in plants growing under natural conditions. Therefore, it is suggested that stationary liquid shoot culture of R. graveolens. can be an alternative source for obtaining biologically active furanocoumarins.

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IPI-504: A Novel hsp90 Inhibitor with In Vitro and In Vivo Anti-Tumor Activity.

Blood ◽

10.1182/blood.v104.11.2403.2403 ◽

2004 ◽

Vol 104 (11) ◽

pp. 2403-2403 ◽

Cited By ~ 4

Author(s):

Constantine S. Mitsiades ◽

Nicholas Mitsiades ◽

Melissa Rooney ◽

Joseph Negri ◽

Corey C. Geer ◽

...

Keyword(s):

Clinical Trials ◽

Tumor Cells ◽

Cell Lines ◽

Biologically Active ◽

Cell Surface Expression ◽

Bone Lesions ◽

Phase I Clinical Trials ◽

Anti Tumor Activity

Abstract We have previously shown that inhibitors of the hsp90 molecular chaperone (including geldanamycin, 17-allylamino-17-demethoxy-geldanamycin (17-AAG) and other members of the ansamycin family) potently induce growth arrest and apoptosis of a large panel of drug-sensitive and -resistant MM cell lines, as well as tumor cells freshly isolated from patients with relapsed refractory MM; and sensitize these cells to other pro-apoptotic anti-tumor agents. While multiple phase I clinical trials have shown that biologically active doses of 17-AAG can be administered without significant hsp90-related toxicities, the insolubility of this compound in most conventional clinical solvents, as well as the practical limitations of DMSO-based formulations that were used in the original clinical trials have generated the need to develop more effective and practical approaches to administer 17-AAG to patients. Herein we describe the in vitro and in vivo pre-clinical profile of IPI-504, a novel analog of 17-AAG, which is soluble in aqueous formulations and can bypass key limitations of the DMSO-based formulations for administration of 17-AAG. Our in vitro studies show that IPI-504 has anti-tumor activity against a broad panel of primary MM tumor cells as well as MM cell lines (including cells resistant to cytotoxic chemotherapeutics, proteasome inhibitor bortezomib, thalidomide or its immunomodulatory thalidomide derivatives, and/or Apo2L/TRAIL). Based on hierarchical clustering analyses, logistic and linear regression models, we observed that the profiles of drug sensitivity of MM cells to IPI-504 were consistent with the profiles of sensitivity to 17-AAG. Similarly, IPI-504 triggered a constellation of molecular sequelae that were consistent with hsp90 inhibition by 17-AAG, including suppression of cell surface expression and down-stream signaling (via PI-3K/Akt and Ras/Raf/MAPK) of receptors for IGF-1 and IL-6; decreased intracellular levels of several key kinases, including Akt, Raf, IKK-α; suppressed expression of several intracellular anti-apoptotic proteins (e.g. FLIP, XIAP, cIAP2); leading to tumor cell sensitization to other pro-apoptotic agents (e.g. cytotoxic chemotherapy or PS-341). Importantly, in our mouse model of diffuse MM bone lesions in SCID/NOD mice, IPI-504 (50 mg/kg, i.v. twice weekly) was able to prolong the survival of mice vs. vehicle-treated mice (p<0.01, log-rank test), without significant treatment-related toxicities. These results indicate that hsp90 inhibitors have significant anti-MM activity in vivo, which, coupled with our ex vivo mechanistic and molecular profiling studies, have provided the framework for upcoming clinical trials of this novel class of agents in patients with MM.

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Current Evidence of the Role of the Myokine Irisin in Cancer

Cancers ◽

10.3390/cancers13112628 ◽

2021 ◽

Vol 13 (11) ◽

pp. 2628

Author(s):

Evangelia Tsiani ◽

Nicole Tsakiridis ◽

Rozalia Kouvelioti ◽

Alina Jaglanian ◽

Panagiota Klentrou

Keyword(s):

Health Benefits ◽

Economic Cost ◽

Biologically Active ◽

Current Evidence ◽

Wide Range ◽

Specific Receptors ◽

Induced Apoptosis ◽

Cancer Tissues

Cancer is a disease associated with extreme human suffering, a huge economic cost to health systems, and is the second leading cause of death worldwide. Regular physical activity is associated with many health benefits, including reduced cancer risk. In the past two decades, exercising/contracting skeletal muscles have been found to secrete a wide range of biologically active proteins, named myokines. Myokines are delivered, via the circulation, to different cells/tissues, bind to their specific receptors and initiate signaling cascades mediating the health benefits of exercise. The present review summarizes the existing evidence of the role of the myokine irisin in cancer. In vitro studies have shown that the treatment of various cancer cells with irisin resulted in the inhibition of cell proliferation, survival, migration/ invasion and induced apoptosis by affecting key proliferative and antiapoptotic signaling pathways. However, the effects of irisin in humans remains unclear. Although the majority of the existing studies have found reduced serum irisin levels in cancer patients, a few studies have shown the opposite. Similarly, the majority of studies have found increased levels of irisin in cancer tissues, with a few studies showing the opposite trend. Clearly, further investigations are required to determine the exact role of irisin in cancer.

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Effects of Unfractionated and Low Molecular Weight Heparins on Platelet Thromboxane Biosynthesis “In Vivo”

Thrombosis and Haemostasis ◽

10.1055/s-0038-1648988 ◽

1994 ◽

Vol 72 (06) ◽

pp. 942-946 ◽

Cited By ~ 20

Author(s):

Raffaele Landolfi ◽

Erica De Candia ◽

Bianca Rocca ◽

Giovanni Ciabattoni ◽

Armando Antinori ◽

...

Keyword(s):

Molecular Weight ◽

Unfractionated Heparin ◽

Low Molecular Weight Heparin ◽

Primary Source ◽

In Vivo Studies ◽

Low Molecular Weight ◽

Heparin Administration ◽

To Receive

SummarySeveral “in vitro” and “in vivo” studies indicate that heparin administration may affect platelet function. In this study we investigated the effects of prophylactic heparin on thromboxane (Tx)A2 biosynthesis “in vivo”, as assessed by the urinary excretion of major enzymatic metabolites 11-dehydro-TxB2 and 2,3-dinor-TxB2. Twenty-four patients who were candidates for cholecystectomy because of uncomplicated lithiasis were randomly assigned to receive placebo, unfractionated heparin, low molecular weight heparin or unfractionaed heparin plus 100 mg aspirin. Measurements of daily excretion of Tx metabolites were performed before and during the treatment. In the groups assigned to placebo and to low molecular weight heparin there was no statistically significant modification of Tx metabolite excretion while patients receiving unfractionated heparin had a significant increase of both metabolites (11-dehydro-TxB2: 3844 ± 1388 vs 2092 ±777, p <0.05; 2,3-dinor-TxB2: 2737 ± 808 vs 1535 ± 771 pg/mg creatinine, p <0.05). In patients randomized to receive low-dose aspirin plus unfractionated heparin the excretion of the two metabolites was largely suppressed thus suggesting that platelets are the primary source of enhanced thromboxane biosynthesis associated with heparin administration. These data indicate that unfractionated heparin causes platelet activation “in vivo” and suggest that the use of low molecular weight heparin may avoid this complication.

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