Azelaic Acid Esters as Pluripotent Immunomodulatory Molecules: Nutritional Supplements or Drugs

Azelaic acid and its esters, the azelates, occur naturally in organisms ranging from plants to humans. We have shown that diethyl azelate (DEA) exhibits a broad range of immunomodulatory activities in vitro and in vivo, and mitigates insulin resistance. To further investigate the therapeutic utility of DEA, we evaluated its mutagenicity in Salmonella typhimurium strains, examined metabolism of DEA in rat, dog, monkey and human primary hepatocytes and in human saliva, determined pharmacokinetics of DEA after an oral dose in rats, and queried its physicochemical properties for drug-like characteristics. DEA was not mutagenic in bacterial strains ± rat liver metabolic activation system S-9. It was chemically unstable in hepatocyte culture medium with a half-life of <1 h and was depleted by the hepatocytes in <5 min, suggesting rapid hepatic metabolism. DEA was also quickly degraded by human saliva in vitro. After an oral administration of DEA to rats, the di- and monoester were undetectable in plasma while the levels of azelaic acid increased over time, reached maximum at <2 h, and declined rapidly thereafter. The observed pharmacological properties of DEA suggest that it has value both as a drug or a nutritional supplement.

Genotoxicity and Carcinogenicity of Medicinal Herbs and Their Nanoparticles

Medicinal plants (MPs) account for 70–80% of use in primary care around the world, and this percentage indicates that the number of MP users is high; thus, it is necessary to focus studies on medicinal herbs to ensure their proper use. In addition, MPs have strong genotoxic effects, as some types of MPs can cause DNA damage. Any substance that raises the risk of cancer or a tumor in an organism is called a carcinogen. There are many genotoxic and carcinogenic substances in the environment that can directly or indirectly affect genetic material. There are also nanoparticles (NPs) derived from MPs. Carbon-based NPs contain many nanoscale materials, such as fullerenes and carbon nanotubes, as well as metals such as gold (Au), silver (Ag), and aluminum (Al). Unfortunately, few studies are concerned with the carcinogenicity of NPs from MPs, whereas many researchers are interested in genotoxic assessment. For this reason, there is an urgent need for more studies into the safety of MPs and NPs. Therefore, this study reviewed the genotoxicity and carcinogenicity of MPs and their derived NPs. We also emphasized the need for strict regulation and monitoring of MP usage.

Friends or Foes? Cytotoxicity, HPTLC and NMR Analyses of Some Important Naturally Occurring Hydroxyanthraquinones

Hydroxyanthraquinones from plants have been used as both medicinal active ingredients and adulterants in slimming food supplements. Although sensible doses of certain natural hydroxyanthraquinones for laxative effects are generally safe in the short term, chronic intake has been related to tumorigenic, carcinogenic, and genotoxic effects. However, an increasing number of researchers are reporting the antiproliferative properties of the same ingredients in cancer cells, pointing towards a potential nutraceutical value for cancer prevention. Previous studies have evaluated anthraquinones’ anti-proliferative activity against various tumour cell lines and bioavailability in Caco-2 cells. However, there are scarce data about both their cytotoxicity in the later cell line and long-term stability. Therefore, this study will check the purity of several ‘aged’ samples using mutually complementary analytical techniques such as HPTLC and NMR assays as well as evaluate the anti-proliferative activity of the purest of these samples using the Caco-2 cell line. The chromatographic and spectroscopic analyses confirmed the long-term stability of those compounds, and their cytotoxic activity resulted in chrysazin (15 µg/mL) > catenarin (27.29 µg/mL) > rhein (49.55 µg/mL) > helminthosporin (52.91 µg/mL) > aloe-emodin (55.34 µg/mL). Our succinct review of the cytotoxicity of these compounds afforded two results: that this is the first clear report for catenarin being active in colon cancer cells and that this class of compounds needs to be better studied to clearly evaluate their benefit/risk profile in regard to both new chemo preventative nutraceuticals and anticancer therapies.

Publisher’s Note: Nutraceuticals Is Launched

We first planned to launch the journal Nutraceuticals in 2007 and obtained ISSN: 1661-3821 for Nutraceuticals on 28 March 2007 [...]

Effects of Zembrin® (Sceletium tortuosum) Supplementation on Mood, Soreness, and Performance Following Unaccustomed Resistance Exercise: A Pilot Study

The purpose of this study was to investigate acute Zembrin® (Sceletium tortuosum) supplementation on muscle soreness, markers of muscle damage, mood, and exercise performance following unaccustomed resistance exercise. Untrained females (n = 16) were divided into two groups with a different three-day treatment regimen: (1) placebo (PL) and (2) Zembrin® (ZEM). During the initial visit, baseline perceived soreness, range of motion (ROM), mood state (profile of mood states (POMS) questionnaire), and plasma lactate dehydrogenase concentrations (LDH) were measured followed by the performance of an eccentric bicep curl protocol with their non-dominant arm. The total repetitions and rate of perceived exertion (RPE) were recorded throughout the exercise. The participants then supplemented with the corresponding treatment immediately following, the subsequent day, and 30 min prior to completing a 48 h follow-up visit. For the 48 h visit, all procedures were repeated and comparisons were drawn for perceived soreness, ROM, LDH, mood scores, total repetitions, and RPE. The findings indicate that short-term ZEM supplementation resulted in lower perceived soreness (p = 0.020) and a greater preservation of ROM (p = 0.028) at 48 h versus the PL group. Mood worsened from the baseline to 48 h regardless of the treatment (p = 0.043) but the decrements were exacerbated in the PL group compared with the ZEM group (p < 0.001). LDH levels (p = 0.019) and RPE (p = 0.008) were higher and total repetitions were lower (p < 0.001) at 48 h irrespective of the treatment. Although short-term dietary enrichment with ZEM did not alter the exercise performance or biomarkers of muscle damage, the current results suggest ZEM supplementation may be effective in reducing the markers of soreness and preserve mood following unaccustomed eccentric exercise.

Update on Nutraceuticals

Plants provide us with not only nutritional value but have been used throughout history for medicinal purposes [...]