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1.
Challenging microalgal vitamins for human health.
Del Mondo, A, Smerilli, A, Sané, E, Sansone, C, Brunet, C
Microbial cell factories. 2020;(1):201
Abstract
BACKGROUND Vitamins' deficiency in humans is an important threat worldwide and requires solutions. In the concept of natural biofactory for bioactive compounds production, microalgae represent one of the most promising targets filling many biotechnological applications, and allowing the development of an eco-sustainable production of natural bioactive metabolites. Vitamins are probably one of the cutting edges of microalgal diversity compounds. MAIN TEXT Microalgae can usefully provide many of the required vitamins in humans, more than terrestrial plants, for instance. Indeed, vitamins D and K, little present in many plants or fruits, are instead available from microalgae. The same occurs for some vitamins B (B12, B9, B6), while the other vitamins (A, C, D, E) are also provided by microalgae. This large panel of vitamins diversity in microalgal cells represents an exploitable platform in order to use them as natural vitamins' producers for human consumption. This study aims to provide an integrative overview on vitamins content in the microalgal realm, and discuss on the great potential of microalgae as sources of different forms of vitamins to be included as functional ingredients in food or nutraceuticals for the human health. We report on the biological roles of vitamins in microalgae, the current knowledge on their modulation by environmental or biological forcing and on the biological activity of the different vitamins in human metabolism and health protection. CONCLUSION Finally, we critically discuss the challenges for promoting microalgae as a relevant source of vitamins, further enhancing the interests of microalgal "biofactory" for biotechnological applications, such as in nutraceuticals or cosmeceuticals.
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2.
Ambrafuran (AmbroxTM) Synthesis from Natural Plant Product Precursors.
Ncube, EN, Steenkamp, L, Dubery, IA
Molecules (Basel, Switzerland). 2020;(17)
Abstract
Ambergris, an excretion product of sperm whales, has been a valued agent in the formulation of perfumes. The composition of ambergris consists of two major components: 40-46% cholestanol type steroids and approximately 25-45% of a triterpenoid known as ambrein. Ambergris undergoes oxidative decomposition in the environment to result in odorous compounds, such as ambraoxide, methylambraoxide, and ambracetal. Its oxidized form, ambrafuran (IUPAC name: 3a,6,6,9a-tetramethyl-2,4,5,5a,7,8,9,9b-octahydro-1H-benzo[e][1]benzofuran), is a terpene furan with a pleasant odor and unique olfactive and fixative properties. The current state of the fragrance industry uses ambrafuran materials entirely from synthetic or semisynthetic sources. However, natural compounds with the potential to be converted to ambergris-like odorants have been extracted from several different types of plants. Here we review plant terpenoids suitable as starting materials for the semisyntheses of ambrafuran or intermediates, such as ambradiol, that can be used in biocatalytic transformations to yield ambrafuran.
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3.
Harnessing the biocatalytic potential of iron- and α-ketoglutarate-dependent dioxygenases in natural product total synthesis.
Zwick, CR, Renata, H
Natural product reports. 2020;(8):1065-1079
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Abstract
Covering: up to the end of 2019Iron- and α-ketoglutarate-dependent dioxygenases (Fe/αKGs) represent a versatile and intriguing enzyme family by virtue of their ability to directly functionalize unactivated C-H bonds at the cost of αKG and O2. Fe/αKGs play an important role in the biosynthesis of natural products, valuable biologically active secondary metabolites frequently pursued as drug leads. The field of natural product total synthesis seeks to contruct these molecules as effeciently as possible, although natural products continue to challenge chemists due to their intricate structural complexity. Chemoenzymatic approaches seek to remedy the shortcomings of traditional synthetic methodology by combining Nature's biosynthetic machinery with traditional chemical methods to efficiently construct natural products. Although other oxygenase families have been widely employed for this purpose, Fe/αKGs remain underutilized. The following review will cover recent chemoenzymatic total syntheses involving Fe/αKG enzymes. Additionally, related information involving natural product biosynthesis, methods development, and non-chemoenzymatic total syntheses will be discussed to inform retrosynthetic logic and synthetic design.
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4.
Broccoli sprout supplementation in patients with advanced pancreatic cancer is difficult despite positive effects-results from the POUDER pilot study.
Lozanovski, VJ, Polychronidis, G, Gross, W, Gharabaghi, N, Mehrabi, A, Hackert, T, Schemmer, P, Herr, I
Investigational new drugs. 2020;(3):776-784
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Abstract
Pancreatic ductal adenocarcinoma is a highly aggressive malignancy with short survival and limited therapeutic options. Broccoli sulforaphane is a promising new treatment due to the results of recent epidemiological, experimental and patient studies. Upon approval from the ethics committee and registration at ClinicalTrials.gov, 40 patients with palliative chemotherapy were placed into a placebo and treatment group in an unblinded fashion. Fifteen capsules with pulverized broccoli sprouts containing 90 mg/508 μmol sulforaphane and 180 mg/411 μmol glucoraphanin or methylcellulose were administered daily for up to 1 year. Twenty-nine patients were included in the treatment group and 11 patients were in the placebo group; these patients were followed for up to 1 year. The patient characteristics, overall survival and feasibility were assessed. Compared to those of the placebo group, the mean death rate was lower in the treatment group during the first 6 months after intake (day 30: 0%/18%, day 90: 0%/25%, and day 180: 25%/43%), and Kaplan-Meier analysis revealed a higher survival rate. There was a high drop-out rate (72% in the treatment group and 55% in the placebo group) after 1 year. We concluded from the Karnofsky index that the broccoli sprouts did not impact patient's self-care and overall abilities severely. The intake of 15 capsules daily was difficult for some patients, and the broccoli sprouts sometimes increased digestive problems, nausea and emesis. We did not obtain statistically significant results (p = 0.291 for the endpoint at day 180), but the knowledge about the feasibility is the basis for the development of new sulforaphane drugs.
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Isochlorogenic acid (ICGA): natural medicine with potentials in pharmaceutical developments.
Wang, HN, Shen, Z, Liu, Q, Hou, XY, Cao, Y, Liu, DH, Jiang, H, DU, HZ
Chinese journal of natural medicines. 2020;(11):860-871
Abstract
Natural products have attracted a great deal of attention as significant resources in traditional Chinese medicine (TCM) and in chemical medicine, as well as in cosmetic ingredients, nutraceuticals and food products. Isochlorogenic acid (ICGA), which has medicinal value, has been discovered in various plants. As a widespread natural medicine, ICGA should be the subject of further research and development. However, there have been no systematic analyses of ICGA. According to our investigation, ICGA was initially isolated from green coffee extracts by Barnes et al. in 1950. To date, it has been discovered in a variety of tea, vegetables, medicinal diet and TCM materials. ICGA is used as a chemical marker for the quality control of these TCM materials. The metabolic process of ICGA has been studied in detail, conforming to be linear dynamics. Thus, the clear pharmacokinetics of ICGA offers a solid foundation for its research and development. ICGA has multiple biological and pharmacological effects, and studies have mainly focused on its antioxidant, anti-inflammatory, antimicrobial, hypoglycemic, neuroprotective, and cardiovascular protective effects, and hepatoprotective properties. The mechanisms underlying these effects are summarized in this review to provide scientific support and inspiration for the future research and development of ICGA and ICGA-rich natural products.
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Efficacy and tolerability of a nutraceutical combination of red yeast rice, guggulipid, and chromium picolinate evaluated in a randomized, placebo-controlled, double-blind study.
Iskandar, I, Harahap, Y, Wijayanti, TR, Sandra, M, Prasaja, B, Cahyaningsih, P
Complementary therapies in medicine. 2020;:102282
Abstract
Hypercholesterolemia is the major risk factor in the development of coronary heart disease. Coronary heart disease is a leading cause of morbidity and mortality in many countries worldwide. An increasing attention is now paid to nutraceuticals development for prevention and cure of dyslipidemia, especially for patients who do not wish to use chemical statins. The cholesterol lowering effect and the tolerability of NutraforChol®, a nutraceutical product containing red yeast rice extract, guggulipid extract and chromium picolinate, was evaluated on subjects who had total cholesterol level 200-239 mg/dL and LDL cholesterol level 100-159 mg/dL. In this study, a randomized, placebo-controlled, double-blind study which consisted of 4 weeks run-in period and 8 weeks treatment period was performed. Based on the study results, NutraforChol® effectively decreased total cholesterol (-15.9 %) and LDL level (-19.9 %) after two weeks consumption. The total cholesterol and LDL reduction were maintained during 8 weeks study period. At study termination (week 8), there was a significant difference between total cholesterol level of NutraforChol® treated group (173.5 ± 21.7 mg/dL) and placebo-treated group (204.5 ± 22.8 mg/dL) (p < 0.05). In addition, there was a significant difference between LDL level at week 8 in NutraforChol® group (115.5 ± 22.2 mg/dL) and placebo-treated group (145.1 ± 23.7 mg/dL) (p < 0.05). The tolerability of NutraforChol® was also evaluated. There were no significant changes (p > 0.05) on renal and liver function parameters between baseline and study termination. Thus, NutraforChol® may be considered as a complementary or alternative safe nutraceuticals for the treatment of mild dyslipidemic subjects.
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Thiopurines in Pediatric Inflammatory Bowel Disease: Current and Future Place.
van Hoeve, K, Vermeire, S
Paediatric drugs. 2020;(5):449-461
Abstract
Thiopurines have been widely used to maintain steroid-free remission in children with inflammatory bowel disease (IBD). However, within the expanding treatment armamentarium, the role of these non-selective immunomodulators has been questioned, especially in pediatric patients, who often present with a more aggressive disease course, which can impact growth and development. The less favorable safety but also inferior efficacy profile associated with thiopurines, in contrast to the newer biological therapies, has interfered with their use. The future place of thiopurines in the management of childhood IBD, therefore, needs revisiting. This review provides a practical overview on the historical and current use of thiopurines in pediatric IBD with specific attention for thiopurine S-methyltransferase testing and monitoring of thiopurine metabolite levels as an approach to improve outcomes. We also give a personal expert opinion on the future role of these drugs in childhood IBD.
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Use of Biologics in Pityriasis Rubra Pilaris Refractory to First-Line Systemic Therapy: A Systematic Review [Formula: see text].
Naidoo, A, Sibbald, C, Fleming, PJ, Piguet, V
Journal of cutaneous medicine and surgery. 2020;(1):73-78
Abstract
Pityriasis rubra pilaris (PRP) is an uncommon, inflammatory, papulosquamous skin disease. Treatment of PRP is challenging as the disease is often refractory to conventional therapies, such as retinoids and methotrexate. There has been an increasing number of studies reporting the successful use of biologic therapy in patients with PRP; however, the data on the efficacy and safety are limited. Our objective was to evaluate the existing evidence for utilizing biologics, whether alone or in combination with established systemic therapies, in patients with treatment-resistant PRP. We systematically reviewed evidence within Medline and Pubmed databases between January 1, 2000, to March 31, 2019. Articles consisted of patients diagnosed with PRP who have failed to respond sufficiently to first-line systemic therapies, or who had comorbidities that precluded their use. In total, 363 unique articles were identified, 56 of which were considered relevant to the clinical question. Of the 56 articles highlighted, 35 met the inclusion criteria and were limited to case series and case studies. Therapy with biologics was found to be successful for both monotherapy (81.1% [27/33]) and when used in combination with existing systemic therapies (87.5% [14/16]). The existing evidence suggests that biologics may be regarded as a tool for PRP treatment alone or in combination therapy with existing treatments, although large-scale randomized clinical trials are necessary to better assess their efficacy and safety.
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The Role of Bioactive Compounds and other Metabolites from Mushrooms against Skin Disorders- A Systematic Review Assessing their Cosmeceutical and Nutricosmetic Outcomes.
Taofiq, O, Barreiro, MF, Ferreira, ICFR
Current medicinal chemistry. 2020;(41):6926-6965
Abstract
Bioactive compounds derived from mushrooms have been shown to present promising potential as cosmeceutical or nutricosmetic ingredients. Scientific data reviewed herein showed that extracts prepared from medicinal and edible mushrooms and their individual metabolites presented antiinflammatory, antioxidant, photoprotective, antimicrobial, anti-tyrosinase, anti-elastase, and anticollagenase activities. These metabolites can be utilised as ingredients to suppress the severity of Inflammatory Skin Diseases, offer photoprotection to the skin, and correct Hyperpigmentation. However, studies regarding the molecular mechanism behind the mentioned bioactivities are still lacking. Challenges associated with the use of mushroom extracts and their associated metabolites as cosmeceutical and nutricosmetic ingredients include several steps from the fruiting bodies to the final product: extraction optimization, estimation of the efficacy and safety claims, the use of micro and nanocarriers to allow for controlled release and the pros and cons associated with the use of extracts vs individual compounds. This systematic review highlights that mushrooms contain diverse biomolecules that can be sustainably used in the development of nutricosmetic and cosmeceutical formulations. Reports regarding stability, compatibility, and safety assessment, but also toxicological studies are still needed to be considered. Furthermore, some of the constraints and limitations hindering the development of this type of ingredients still require long-term studies to achieve major breakthroughs.
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10.
Optimization of biologics to reduce treatment failure in inflammatory bowel diseases.
Bourchany, A, Gilletta De Saint-Joseph, C, Breton, A, Barreau, F, Mas, E
Current opinion in pharmacology. 2020;:51-58
Abstract
Moderate to severe inflammatory bowel disease patients can fail to respond to conventional therapy and/or to biologic treatment. In the era of TNFα antagonists and other non-anti-TNF biologic drugs, it is important to review the literature on biologic treatment failure, which could be defined as primary non-response, secondary loss of response and intolerance. Therapeutic drug monitoring (TDM), that is, drug trough level and antidrug antibodies, should enable to determine the mechanisms of treatment failure and to optimize drug efficacy. There is a consensus on reactive TDM at the time of loss of response. Proactive TDM could be of interest during induction and/or maintenance, but randomized controlled trials are required.