Current Medicinal Chemistry - Volume 26, Issue 24, 2019

Traditionally, natural medicines have been administered as plant extracts, which are composed of a mixture of molecules. The individual molecular species in this mixture may or may not contribute to the overall medicinal effects and some may even oppose the beneficial activity of others. To better control therapeutic effects, studies that characterized specific molecules and describe their individual activity that have been performed over the past decades. These studies appear to underline that natural products are particularly effective as antioxidants and anti-inflammatory agents. In this systematic review we aimed to identify potent anti-inflammatory natural products and relate their efficacy to their chemical structure and physicochemical properties. To identify these compounds, we performed a comprehensive literature search to find those studies, in which a dose-response description and a positive control reference compound was used to benchmark the observed activity. Of the analyzed papers, 7% of initially selected studies met these requirements and were subjected to further analysis. This analysis revealed that most selected natural products indeed appeared to possess anti-inflammatory activities, in particular anti-oxidative properties. In addition, 14% of the natural products outperformed the remaining natural products in all tested assays and are attractive candidates as new anti-inflammatory agents.

Linseed - also known as flaxseed - is known for its beneficial effects on animal health attributed to its composition. Linseed comprises linoleic and α-linolenic fatty acids, various dietary fibers and lignans, which are beneficial to health because they reduce the risk of cardiovascular diseases, as well as cancer, decreasing the levels of cholesterol and relaxing the smooth muscle cells in arteries increasing the blood flow. Essential fatty acids from flax participate in several metabolic processes of the cell, not only as structuring components of the cell membrane but also as storage lipids. Flax, being considered a functional food, can be consumed in a variety of ways, including seeds, oil or flour, contributing to basic nutrition. Several formulations containing flax are available on the market in the form of e.g. capsules and microencapsulated powders having potential as nutraceuticals. This paper revises the different lipid classes found in flaxseeds and their genomics. It also discusses the beneficial effects of flax and flaxseed oil and their biological advantages as ingredients in pharmaceuticals and in nutraceuticals products.

Brassica vegetables, particularly turnip, contain many natural antioxidants. This review focuses on antioxidant components and the influence of different processing and storage conditions on antioxidant activities of some Brassica vegetables including turnip. Long storage times had an adverse effect on antioxidant value of turnip. Also, the activity of antioxidants in cruciferous vegetables could be influenced by antioxidant breakdown and leaching during cooking. Heat treatment has a major impact on the antioxidant activity of Brassica vegetables and it has been perceived minor antioxidant ability in processed vegetables compared with uncooked samples. Food processing operations in terms of blanching, canning, sterilizing and freezing, in addition to cooking methods perhaps can have a major influence on the yield, chemical structure and bioavailability of antioxidants in Brassica family. Cooking methods such as steaming and microwaving are proper methods for a short time. Consumption of raw or slightly blanched turnip is an appropriate way to maximize its health benefits.

Background: The exploration of the plant biodiversity as a natural source to obtain sustainable food products and new bioactive pharmaceutical compounds has been growing significantly due to their abundance, safety and economy. Natural pharmaceutical and edible compounds present some advantages when compared to synthetic ones, such as being chemically inert and widely available. In this sense, plants of the genus Pereskia belonging to the Cactaceae family, have been studied. It is an unconventional wild edible plant that contains a large amount of protein and minerals. Studies have demonstrated their biological activities and potential application in different areas such as pharmaceutical, medicinal and food. Objective: This review is focused on the chemical composition, functional properties, applications on pharmaceutical, nutraceutical and food areas and formulation techniques to enhance the stability and bioavailability of bioactive compounds from the underutilized wild edible plant known as ora-pro-nobis (Pereskia aculeata or Pereskia grandifolia). Conclusion: The latest studies involving ora-pro-nobis demonstrated its great potential due to its biological activities, which could stimulate further investigations. The utilization of this plant as a natural source to supplement the diet, or to prepare new food products and pharmaceutical formulations is an attractive approach to explore and fully realize the potential of the rich biodiversity found in Brazil and in other countries.

Gac, Momordica cochinchinensis (Lour.) Spreng. belongs to the Cucurbitaceae family. It is more considered as a super fruit. The demand for this plant is growing in countries where its reputation is high, including traditional countries of gac culture and countries fond of super fruits and food supplements. In these latter countries, the industrial strategy aims at producing high added value in food supplements or nutritional rich preparations. However, when marketing is not the driving force and claims have to be related to scientific data, the situation of gac is less "heavenly", mainly because its most remarkable properties are in the field of micronutrients. These latter components are indeed very important for health but their supplementation on healthy populations brings no significant advantage. This paper proposes to review aspects important for the nutritional reputation of this plant: where it comes from, how it is cultured to have an optimal nutritional composition, what is its composition and how it can impact health of consumers, in which products it is used and what are the regulations to use it in different markets. One important goal of this review is to give a critical and scientific approach to confirm data on this fruit, which has been promoted by marketing departments injecting so many wrong and unverified information. Missing data will be highlighted and potential positive applications are proposed all along the text.

BioActive Compounds (BACs) recovered from food or food by-product matrices are useful in maintaining well being, enhancing human health, and modulating immune function to prevent or to treat chronic diseases. They are also generally seen by final consumers as safe, non-toxic and environment-friendly. Despite the complex process of production, chemical characterization, and assessment of health effects, BACs must also be manufactured in stable and bioactive ingredients to be used in pharmaceutical, food and nutraceutical industry. Generally, vegetable derivatives occur as sticky raw materials with pervasive smell and displeasing flavor. Also, they show critical water solubility and dramatic stability behavior over time, involving practical difficulties for industrial use. Therefore, the development of novel functional health products from natural sources requires the design of a suitable formulation to delivery BACs at the site of action, preserve stability during processing and storage, slow down the degradation processes, mask lousy tasting or smell, and increase the bioavailability, while maintaining the BACs functionality. The present review focuses on human health benefits, BACs composition, and innovative technologies or formulation approaches of natural ingredients from some selected foods and by-products from industrial food transformations.

Natural products are fascinating molecules in drug discovery for their exciting structure variability and also for their interaction with various targets. Drugs multi-targeting effect represents a more realistic approach to develop successful medications for many diseases. However, besides a large number of successful in vitro and in vivo studies, most of the clinical trials fail. This is generally related to the scarce water solubility, low lipophilicity and inappropriate molecular size of natural compounds, which undergo structural instability in biological milieu, rapid clearance and high metabolic rate. Additionally, some molecules are destroyed in gastric juice or suffer to a massive pre-systemic metabolism in the liver, when administered orally, limiting their clinical use. A reduced bioavailability can also be linked to drug distribution/accumulation in non-targeted tissues and organs that increase the side effects lowering the therapeutic efficacy and patient compliance. Nanomedicine represents a favourable tool to increase bioavailability and activities of natural products. Generally, nanovectors provide a large surface area and can overcome anatomic barriers. Each nanovector has its own advantages, disadvantages, and characteristics. In this review, different nanocarriers made of compounds which are Generally Recognized As Safe (GRAS) for the delivery of natural products, marketed as food supplements and medicines are reported.

Natural products are an important source of therapeutically effective compounds throughout the world. Since ancient times, a huge amount of both plant extracts and isolated compounds have been largely employed in treatment and prevention of human disorders and, currently, more than 60% of the world’s population trusts on plant medicaments as demonstrated by the increasing quantity of herbal therapeutics in the market. Unfortunately, several promising natural molecules for the treatment of the most diverse ailments are characterized by extremely unfavourable features, such as low water solubility and poor/irregular bioavailability, which hinder their clinical use. To overcome these limitations and to make herbal therapy more effective, different formulative approaches have been employed. Among the different strategies for increasing drug solubility, nanocrystals can be considered one of the most interesting and successful approaches. Drug nanocrystals are nanosized drug particles usually formulated as nanosuspensions, namely submicron dispersions in liquid media where surfactants, polymers, or a mixture of both act as stabilisers. In this review, we described the most significant results and progresses concerning drug nanocrystal formulations for the delivery of natural compounds with a significant pharmacological activity. The text is organized in nine sections, each focusing on a specific poorly water- soluble natural compound (apigenin, quercetin, rutin, curcumin, baicalin and baicalein, hesperetin and hesperidin, resveratrol, lutein, silybin). To foster the clinical translation of these natural nanomedicines, our opinion is that future research should pair the essential pharmacokinetic studies with carefully designed pre-clinical experiments, able to prove the formulation efficacy in relevant animal models in vivo.

Phytochemicals represent an important class of bioactive compounds characterized by significant health benefits. Notwithstanding these important features, their potential therapeutic properties suffer from poor water solubility and membrane permeability limiting their approach to nutraceutical and pharmaceutical applications. Lipid nanoparticles are well known carrier systems endowed with high biodegradation and an extraordinary biocompatible chemical nature, successfully used as platform for advanced delivery of many active compounds, including the oral, topical and systemic routes. This article is aimed at reviewing the last ten years of studies about the application of lipid nanoparticles in active natural compounds reporting examples and advantages of these colloidal carrier systems.