Current Nutraceuticals - Volume 2, Issue 1, 2021

Objective: Epidemiological data illustrates that there is a strong relationship between dietary intake of natural bioactive compounds and their beneficial properties against various diseases, and this stimulates academic and industrial interest in using plant-derived compounds for health and making medicines. For this reason, recent health related studies in the literature have focused on a variety of many plant-derived bioactive compounds. Even though the bioactivities of such compounds have widely been investigated, there are few studies about oligomeric species and their activities.

Methods: In this review, extraction and isolation methods of the plant-derived oligomers and the use of such oligomers in health applications are summarised.

Results: In the literature, many studies state that oligomeric compounds have benefits to human health. To maximize these beneficial properties, various ways to use oligomeric compounds have been examined and summarised.

Conclusion: A better understanding of the specific activities of distinct components of plant-derived oligomers is expected to open new avenues for drug discovery. This review gives an overview of oligomers with health beneficial properties and their possible applications in healthcare.

Background: Natural products are commonly used for treating health problems. These products may be associated with adverse events, which are defined as “noxious and unintended response to a medicinal product” by the European Medicine Agency.

Objectives: To identify studies describing at least one adverse event (or with potential to promote an adverse event) related to the use of natural products, as well as to describe the involved product(s) and adverse event(s).

Methods: A pre-systematic review following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses criteria. Keywords: “natural product(s)” and [“adverse drug reaction(s)” or “adverse effect(s)”]. Screened databases: PubMed, SciELO, DOAJ and Google Scholar. Inclusion criteria: Papers describing at least one adverse event associated with the use of natural products and published between 2017 and 2019. Exclusion criteria: Repeated studies, reviews and papers written in other languages than English, Portuguese, French or Spanish.

Results: 104 studies were identified (20 PubMed; 0 SciELO; 2 DOAJ; 82 Google Scholar), but only 10 were selected (4 PubMed and 6 Google Scholar): 1 in-vitro study; 2 non-clinical studies, 1 study reporting in-vitro and clinical data and 5 case reports. Globally, 997 reports of adverse drug reactions with natural products were identified, mainly non-severe cases.

Conclusion: Since a limited number of studies was found, we conclude that adverse events due to natural products may be underreported or natural products may have a good safety profile. This review contributes to assuring the safety of natural products consumers by evaluating the knowledge/information on the potential adverse events and interactions of these products.

Background:Bistorta amplexicaulis is a seasonal herb with several folkloric uses. The plant extract has been shown to possess various activities including antioxidant, anticancer, anti-bacterial, anti-fungal, cardio-protective, and anti-atherosclerosis activities.

Objective: The aim of the study was to quantify the activity of the plant extract and relate it to the activity of the isolated compound, gallic acid.

Methods: Initially, the plant was extracted, then, the activity of the extract was compared with its constituent, gallic acid. After this, the cytotoxic potential of the two against human liver cancer cell line (HepG2), breast cancer cell line (MCF-7) and human umbilical vein endothelial cells (HUVEC) was evaluated through MTS assay.

Results: The extract had better activity against HepG2 as compared to gallic acid (IC50 29µg/mL vs 37µg/mL). It also provided a better therapeutic window by having lower toxicity for HUVEC cells than gallic acid (IC50 63µg/mL vs 47µg/mL), suggesting the use of the extract over the purified gallic acid for these cells. We also performed the fluorescence study of the rhizome extract in ethanol (REE), methanol (REM), 80% ethanol (80RE), 80% methanol, (80RM) and acetone (RAC). The highest intensity of fluorescence was found in REE with excitation at 394 nm and emission at 421nm.

Conclusion: The comparison of gallic acid with ethanolic rhizome extract of B. amplexicaulis reveals important insights about utilizing the plant extract over purified gallic acid. The ethanolic extract also has the potential to be used as an autofluorescent drug during in vitro and in vivo studies.

Objective: Vitamins are nutraceutical groups involved in important processes that provide energy production, strengthening the immune system, fighting free radicals, the production of red blood cells. Biotransformation is a process involving the use of biological agents as catalysts to perform the transformation of chemical compounds. Biotransformation processes offer advantages as high regioselectivity, stereospecificity, and mild operating conditions when compared to chemical reactions. In most cases, the aim of using biotransformation is to introduce chirality into a molecule, to achieve a regioselective functionalization or to selectively convert a functional group among other groups with similar reactivity. The biotransformation of vitamins can be defined as the sum of the processes by which vitamins are altered by the biological reactions in the body. Biotransformation leading to a new way of synthesis of vitamins has recently been studied. In the literature, there are various studies about using vitamins as nutraceuticals.

Methods: The role of vitamins in the biotransformation can be diversified. They can be a source or final product in the biotransformation. In the present study, various roles of vitamins in the biotransformation were explained.

Results: When it is compared with traditional methods, obtained data showed that with biotransformation properties such as; activity of the vitamins, nutritional value of the food and productivity of the process were increased.

Conclusion: Even though the biotransformation of vitamins has been studied, there is no review paper about the biotransformation of vitamins and their benefits. In this review, the biotransformation of vitamins and vitamins that are used in the biotransformation were mentioned.

Background: Seeds of Nigella sativa, commonly referred to as “black cumin”, are rich in a spectrum of biologically active substances and thus associated with a range of potential health benefits. Unlocking the activity of these phytochemicals traditionally requires solvent extraction. Previously, we have explored nanosizing as an alternative to liberate the biological activity of natural products, such as Solanum incanum, Pterocarpus erinaceus, Loranthus micranthus and Cynomorium coccineum.

Objectives: Nanosizing natural products may increase their activity for a number of reasons ranging from an improved bioavailability to physical nano-toxicity. Because Nigella sativa is amenable to being “milled down”, this spice has been employed to explore the underlying causes of increased activity upon mechanical particle size reduction.

Methods:Nigella sativa seeds were pre-milled employing a household flour mill followed by extensive grinding exploiting a planetary ball mill. The particles were characterized employing Laser Diffraction, Photon Correlation Spectroscopy and Scanning Electron Microscopy connected with Energy Dispersive X-ray Diffraction. Finally, the samples were evaluated for sterility profile, and nematicidal and antioxidant activities.

Results: Suspensions containing fairly uniform particles of Nigella sativa showing diameters in the range of 100-1000 nm have been obtained. These nanosuspensions are characterized by considerably reduced microbial contamination when compared to the bulk material and reasonable antioxidant and nematicidal activities when employed at higher concentrations. This activity is comparable to the one of the ethanolic extract of the seeds and is significantly higher when compared to the one of aqueous extracts. A combination of “sterilization and extraction by milling”, improved liberation of soluble substances from small particles, surface activity and physical nano-activity of the particles itself is likely responsible for the activities observed.

Conclusion: Nanosizing of the entire natural products provides an interesting alternative to solvent extraction as it results in the liberation of active ingredients and certain additional activities. The resulting nanosuspensions can be investigated further and optimized for applications in Nutrition, Agriculture, Medicine, and Cosmetics.

Background: Different cellular responses influence the progress of cancer. In this study, the effects of hydrogen peroxide and quercetin induced changes on cell viability, apoptosis, and oxidative stress in human hepatocellular carcinoma (HepG2) cells were investigated.

Methods: The effects of hydrogen peroxide and quercetin on cell viability, cell cycle phases, and oxidative stress related cellular changes were investigated. Cell viability was assessed by WST-1 assay. Apoptosis rate, cell cycle phase changes, and oxidative stress were measured by flow cytometry. Protein expressions of p21, p27, p53, NF-Kβ-p50, and proteasome activity were determined by Western blot and fluorometry, respectively.

Results: Hydrogen peroxide and quercetin treatment resulted in decreased cell viability and increased apoptosis in HepG2 cells. Proteasome activity was increased by hydrogen peroxide but decreased by quercetin treatment.

Conclusion: Both agents resulted in decreased p53 protein expression and increased cell death by different mechanisms regarding proteostasis and cell cycle phases.

Background: Floating tablets extend drug residence time, enhance bioavailability and promote the delivery of local drugs to the stomach. With this objective, floating tablets were prepared for the treatment of gastric ulcers containing aqueous extract of liquorice and Isabgol.

Methods: Tablets containing HPMC K100M (hydrophilic polymer), liquorice extract, sodium bicarbonate (gas generating agent), talc, and magnesium stearate were prepared using direct compression method. Physical parameters of formulations such as diameter, thickness, hardness, friability, weight uniformity, drug content, buoyancy time, dissolution, and the mechanism for drug release, were assessed. The formulations have been optimized based on buoyancy time and in- vitro drug release.

Results: The diameter of all formulations was in the range 11.310-11.833 mm; thickness was in the range 4.02-4.071 mm. The hardness ranged from 3.1 to 3.4 kg/cm. All the formulations passed the USP requirements for friability and uniformity of weight. All tablet formulations had a buoyancy period of less than 5 min and throughout the research, the tablet stayed in floating condition. All tablet formulations were accompanied in drug discharge by zero-order kinetics and Korsmeyer-Peppas model.

Conclusion: It was discovered that the optimized formulation was F7, which released 98.5 percent of the drug in 8 hr. in-vitro, while the buoyancy time was 3.5 min. For gastroretentive drug delivery systems, formulations containing Isabgol, sodium bicarbonate and HPMC K100 M in combination may be promising.

Background: Vegetables and fruits are consumed in considerable amounts worldwide producing huge quantities of organic leftovers comprising primarily of peels. Peels of potatoes (PP) and carrots (CP), for instance, are often considered as waste, albeit they still represent a rich source of interesting phytochemicals. Traditional waste management of such materials, usually vermicomposting, therefore represents a low-value approach and also a considerable burden to the environment.

Objective: Aiming to convert some of this waste into raw materials for further applications, methods were explored to prepare suspensions of PP and CP. Antioxidant activities of these suspensions were compared to bulk-suspensions and the corresponding ethanolic extracts in anticipation of possible applications in Nutrition and Cosmetics.

Methods: The peels of potatoes and carrots were subjected to high- speed stirring (HSS) and high-pressure homogenization (HPH) to produce suspensions which were characterized for size distribution by Laser Diffraction (LD), Photon Correlation Spectroscopy (PCS), and light microscopy (LM). Ethanolic extracts of peels were also produced. Samples were evaluated for antioxidant activity employing 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay.

Results: HPH produced suspensions of peels comprising particles with diameters in the range of 268 - 335 nm for PP and 654 - 1,560 nm for CP. These suspensions exhibited a significantly stronger antioxidant activity compared to the bulk-suspensions. Moreover, the suspension of PP (1% w/w) exhibited comparable antioxidant activity to the ethanolic extract (1% w/w) whilst the CP suspension (1% w/w) exhibited lower activity compared to the ethanolic extract.

Conclusion: Production of suspensions of vegetable peels may unlock some biological potential which could be optimised for applications in Nutrition, Agriculture, Medicine and Cosmetics.

Background: The incidence of dementia is increasing as the aging population of the world is increasing. Alzheimer’s disease (AD) is a neurodegenerative disorder of the central nervous system. There are presently 7.3 million patients of AD and the number may rise to 34 million at this pace in the coming thirty years. In the disease, the level of Acetylcholine is reduced and as a result, causes the loss of cholinergic neurons in the brain. The disease is less common in Asian countries as compared to the western nations of the world. This work aimed to establish the role of the common medicinal and food plants against Alzheimer's.

Methods: The enzyme acetylcholinesterase (AChE) is the enzyme responsible for hydrolysis and reduction of Acetylcholine. The anti-acetylcholinesterase activity of different extracts of three local plants used as spices in the daily food, Curcuma longa, Cinnnamomum tamala, and Zingiber officinale, was determined using the Microplate Assay method.

Results: The phytochemical study of the selected plants revealed the presence of alkaloids, terpenes, flavones, saponins, and tannins in these plants. The chloroform extract of all the three plants presented promising AChE inhibiting activity having IC50 >200µg/ml. A probable reason will be the alkaloids and terpenes present in the chloroform extract.

Conclusion: The chloroform extract of all three plants presented promising AChE inhibiting activity and can become a reasonable therapy for the cure/prevention of Alzheimer's disease. The frequent use of these spices may be a possible reason for the fever incidence of Alzheimer's in Asian countries. Further in vivo studies are required to find its action and studies to find the exact compound responsible for the action.

Background: Colon cancer is responsible for increasing the death rate worldwide. Commonly used anticancer drugs have various side effects and their clinical usage must be restricted due to their toxicity.

Objective: The present research aimed to evaluate the anticancer potential of Lepidium sativum L. (LS) seeds aqueous extract against azoxymethane/dextran sodium sulfate (AOM/DSS) induced-colon cancer in male albino mice.

Methods: Low (200 mg/kg) and high (400 mg/kg) doses of LS seeds extract were used to treat induced colon cancer in different stages.

Results: The present results report that LS treatment for mice with colon cancer especially in high dose, decreases colon polyps/tumor incidence and size, tissues disorder, expression of P53 and increases apoptosis in colon tissue. Moreover, LS decreases micronucleus induction in polychromatic (PCE), increases PCE/normochromatic erythrocytes ratio and decreases the percentage of sperm abnormalities.

Conclusion: The present study reports anticancer potential of LS for induced colorectal cancer mice by ameliorating the inflammatory steps of colon.