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Cyclodextrins (CDs) are cyclic oligosaccharides of natural origin that were discovered more than 100 years ago. The peculiar cone-like conformation of the sugar ring, expressing a lipophilic cavity and a hydrophilic external surface, allows these substances to spontaneously complex poorly soluble compounds in an aqueous environment. For more than 50 years, these substances have found applicability in the pharmaceutical and food industries as solubilizing agents for poorly soluble chemical entities. Nowadays, several research groups all over the world are investigating their potential as active pharmaceutical ingredients (APIs) for the treatment of several illnesses (e.g., hypercholesterolemia, cancer, Niemann-Pick Type C disease). The aim of this review is to briefly retrace cyclodextrins’ legacy as complexing agents and describe the current and future prospects of this class of chemical entities in pharmaceutics as new APIs.

Red microalgae contain functional sulfated polysaccharides (containing dietary fibers), polyunsaturated fatty acids, zeaxanthin, vitamins, minerals, and proteins. Studies in rat models support the therapeutic properties of algal biomass and isolated polysaccharides. Algal products incorporated into rat diets were found to significantly improve total serum cholesterol, serum triglycerides, hepatic cholesterol levels, HDL/LDL ratios and increased fecal excretion of neutral sterols and bile acids. Morphological and metabolic changes were induced by consumption of algal products. These results suggest that red microalgae can be used as potent hypocholesterolemic agents, and they support the potential use of red microalgae as novel nutraceuticals.

The antibiotics have been useful in our battles against infectious bacteria and fungi for over 50 years. However, many antibiotics are used commercially, or are potentially useful, in medicine for activities other than their antibiotic action. They are used as antitumor agents, immunosuppressive agents, hypocholesterolemic agents, enzyme inhibitors, antimigraine agents, and antiparasitic agents. A number of these products were first discovered as antibiotics which failed in their development as such, or as mycotoxins. In addition to the above alternative applications, new powerful antibiotics have been discovered and commercialized in recent years and others are in clinical testing at the moment. A few successful secondary metabolites appear to have no antibiotic activity. The recently increased development of resistance to older antibacterial and antifungal drugs is being met with the use or clinical testing of older, underutilized or previously nondeveloped narrow-spectrum antibacterial products as well as powerful semisynthetic antifungal agents.

Cogon grass (Imperata cylindrica/I. cylindrica) of the Gramineae family is found abundantly in nature, and the roots of this plant possess several beneficial biological properties. The present study aimed to isolate and identify flavonoid compounds from cogon grass roots and examine their potential as hypocholesterolemic agents. The flavonoid compound was isolated using a maceration method, followed by gravity column chromatography until a pure compound was obtained. The molecular structure of the isolated compound was determined using 1H-nuclear magnetic resonance (NMR) and 13C-NMR spectroscopy. An in vivo lipid-lowering test used a randomized post-test only control group experimental design in rats with hypercholesterolemia. The animals were divided into four groups: K0, negative control; K1, positive control; K2, ethanol extract treated group; and K3, ethyl acetate fraction treated group, and the lipid profiles were examined at the end of the study. The isolated compound, 7,3',5'-trimethoxyflavonol, was collected in yellow powder form; was shown to be a flavonoids and was comprised of 18 carbon atoms and 16 hydrogen atoms. In vivo tests demonstrated that 15 mg/200 g body weight (BW) of an ethanol extract significantly lowered total cholesterol levels (P=0.001) but did not lower low-density lipoprotein (LDL) (P=0.109) and high-density lipoprotein (HDL) levels (P=0.003). The fraction of ethyl acetate administered at 15 mg/200 g BW was capable of lowering the total cholesterol levels significantly (P=0.002) and lowered LDL levels (P=0.006) but was unable to increase HDL levels (P=0.190). The in vivo tests showed that the ethyl acetate fraction of I. cylindrica reduced total cholesterol and LDL levels more effectively than the ethanol extract, but did not affect HDL levels in rats with hypercholesterolemia.

The present study was undertaken to analyze the influence of omega 3 Fish oil and Cod liver oil on serum cholesterol levels and triglycerides in albino wistar rats. Serum total cholesterol was determined by an enzymatic method using a diagnostic kit. HDL and LDL cholesterol were measured by an enzymatic method using automated analyzer. Triglycerides were analyzed using enzymatic method. VLDL cholesterol was calculated from triglycerides values. The atherogenic index was calculated as: serum total cholesterol/HDL cholesterol. Serum total cholesterol level in rats fed with diet containing 15% omega 3 Fish oil (15% OF) supplemented with cholesterol (0.5% CH) decreased significantly (P < 0.05) compared to those fed with the diet having only cholesterol (0.5% CH) and 10% Fluvastatin (10% FS) supplemented with cholesterol. Rats fed with diet containing 15% omega 3 fish oil (15% OF) supplemented with cholesterol had significantly lower serum total cholesterol than 15% Cod liver oil (15% CO) blended with cholesterol. Omega 3 fish oil is a strong hypocholesterolemic agent as that of fluvastatin (a cholesterol reducing drug). Therefore, regular ingestion of omega 3 Fish oil or supplementation with diets is important in the maintenance of human health.

Microalgae are important primary producers in the marine food chain; however, only limited efforts have been made to research their use as nutraceuticals. Our laboratory has developed the biotechnological means for producing novel biochemicals from the marine red microalga Porphyridium sp., which can be used for a variety of applications, including cosmetics, pharmaceutics, and in the food industry. Importantly, in addition to being a rich source of polyunsaturated fatty acids, proteins, vitamins, and minerals, Porphyridium sp. also contains sulfated polysaccharides, a unique source of dietary fiber. By using a foodomics approach, our group has demonstrated that consuming either the biomass (cells) or the isolated sulfated polysaccharides from Porphyridium sp. can lower plasma cholesterol levels in animals through different physiological mechanisms. Hence, these products may be used as new hypocholesterolemic food supplements that may potentially reduce risk factors for coronary vascular diseases.

Food-derived bioactive peptides are being used as important functional ingredients for health-promoting foods and nutraceuticals in recent times in order to prevent and manage several diseases thanks to their biological activities. Bioactive peptides are specific protein fractions, which show broad applications in cosmetics, food additives, nutraceuticals, and pharmaceuticals as antimicrobial, antioxidant, antithrombotic, and angiotensin-I-converting enzyme (ACE)-inhibitory ingredients. These peptides can preserve consumer health by retarding chronic diseases owing to modulation or improvement of the physiological functions of human body. They can also affect functional characteristics of different foods such as dairy products, fermented beverages, and plant and marine proteins. This manuscript reviews different aspects of bioactive peptides concerning their biological (antihypertensive, antioxidative, antiobesity, and hypocholesterolemic) and functional (water holding capacity, solubility, emulsifying, and foaming) properties. Moreover, the properties of several bioactive peptides extracted from different foods as potential ingredients to formulate health promoting foods are described. Thus, multifunctional properties of bioactive peptides provide the possibility to formulate or develop novel healthy food products.

Novel pyrrolo [2,3-b] pyrrole derivatives were synthesized and their hypolipidemic activity was assessed in hyperlipidemic rats. The chemical structures of the new derivatives were confirmed through spectral analysis. Compounds 5 and 6 were revealed to be the most effective hypolipidemic agents, with considerable hypocholesterolemic and hypotriglyceridemic effects. They appear to be promising candidates for creating new powerful derivatives with anti-atherosclerotic and hypolipidemic properties. As for antimicrobial activity, some of the tested compounds showed moderate activity against Pseudomonas aeruginosa: compound 2 revealed an MIC value of 50 μg/mL, compared to 25 μg/mL for ciprofloxacin. Compound 3 showed good antimicrobial activity against Staphylococcus aureus, comparable to ciprofloxacin, and roughly half the activity of ampicillin, according to MIC values. Compound 2 has an MIC approximately 25% of that of clotrimazole against Candida albicans. Compound 2 also showed the highest antioxidant activity with 59% inhibition of radical scavenging activity. Additionally, the cytotoxic activity of these new derivatives 1–7 was investigated and most of them showed good anticancer activity against the three tested cell lines.

Microbes are the leading producers of useful natural products. Natural products from microbes and plants make excellent drugs. Significant portions of the microbial genomes are devoted to production of these useful secondary metabolites. A single microbe can make a number of secondary metabolites, as high as 50 compounds. The most useful products include antibiotics, anticancer agents, immunosuppressants, but products for many other applications, e.g., antivirals, anthelmintics, enzyme inhibitors, nutraceuticals, polymers, surfactants, bioherbicides, and vaccines have been commercialized. Unfortunately, due to the decrease in natural product discovery efforts, drug discovery has decreased in the past 20 years. The reasons include excessive costs for clinical trials, too short a window before the products become generics, difficulty in discovery of antibiotics against resistant organisms, and short treatment times by patients for products such as antibiotics. Despite these difficulties, technology to discover new drugs has advanced, e.g., combinatorial chemistry of natural product scaffolds, discoveries in biodiversity, genome mining, and systems biology. Of great help would be government extension of the time before products become generic.

Microorganisms are remarkable producers of a wide diversity of natural products that significantly improve human health and well-being. Currently, these natural products comprise half of all the pharmaceuticals on the market. After the discovery of penicillin by Alexander Fleming 85 years ago, the search for and study of antibiotics began to gain relevance as drugs. Since then, antibiotics have played a valuable role in treating infectious diseases and have saved many human lives. New molecules with anticancer, hypocholesterolemic, and immunosuppressive activity have now been introduced to treat other relevant diseases. Smaller biotechnology companies and academic laboratories generate novel antibiotics and other secondary metabolites that big pharmaceutical companies no longer develop. The purpose of this review is to illustrate some of the recent developments and to show the potential that some modern technologies like metagenomics and genome mining offer for the discovery and development of new molecules, with different functions like therapeutic alternatives needed to overcome current severe problems, such as the SARS-CoV-2 pandemic, antibiotic resistance, and other emerging diseases. Key points • Novel alternatives for the treatment of infections caused by bacteria, fungi, and viruses. • Second wave of efforts of microbial origin against SARS-CoV-2 and related variants. • Microbial drugs used in clinical practice as hypocholesterolemic agents, immunosuppressants, and anticancer therapy.