Much work has been carried out in recent years on the beneficial effect of phenolic compounds which act as natural antioxidants and help to neutralize free radicals. We analysed the antioxidant activity of the rutin (quercetin-3-rhamnosyl glucoside) using different assays including: total antioxidant activity and reducing power, hydroxyl radical scavenging assay, superoxide radical scavenging assay, 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging assay and lipid peroxidation assay which uses egg yolk as the lipid-rich source. Total antioxidant capacity was determined by the assay based on the decrease in absorbance of β-carotene by the sample. Rutin exhibited strong DPPH radical scavenging activity. At the concentration of 0.05 mg/ml, ascorbic acid (Vc), butylated hydroxytoluene (BHT) and rutin showed 92.8%, 58.8%, and 90.4% inhibition, respectively. In addition, rutin had effective inhibition of lipid peroxidation. Those various antioxidant activities were compared to standard antioxidants such as BHT and Vc.

In vitro antioxidant properties of rutin

Social immunity, which describes how individual behaviors of group members effectively reduce disease and parasite transmission at the colony level, is an emerging field in social insect biology. An understudied, but significant behavioral disease resistance mechanism in honey bees is their collection and use of plant resins. Honey bees harvest resins with antimicrobial properties from various plant species and bring them back to the colony where they are then mixed with varying amounts of wax and utilized as propolis. Propolis is an apicultural term for the resins when used by bees within a hive. While numerous studies have investigated the chemical components of propolis that could be used to treat human diseases, there is a lack of information on the importance of propolis in regards to bee health. This review serves to provide a compilation of recent research concerning the behavior of bees in relation to resins and propolis, focusing more on the bees themselves and the potential evolutionary benefits of resin collection. Future research goals are also established in order to create a new focus within the literature on the natural history of resin use among the social insects and role that propolis plays in disease resistance.

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Propolis and bee health: the natural history and significance of resin use by honey bees

A heightened interest in (trans)dermal delivery is in part driven by the need to improve the existing skin therapies and also the demand for alternative routes of administration, notably for pharmaceutical actives with undesirable oral absorption characteristics. The premise of delivering difficult actives to the skin or via the skin however is weighed down by the barrier function properties of the stratum corneum. Short of disrupting the skin by physical means, scientists have resorted to formulation with excipients known to enhance the skin penetration and permeation of drugs. A vehicle that has emerged over the years as a safe solubilizer and enhancer for a broad range of drug actives is the highly purified NF/EP grade of diethylene glycol monoethyl ether (DEGEE) commercially known as Transcutol®. Whereas numerous studies affirm its enhancing effect on drug solubilization, percutaneous absorption rate, and/or drug retention in the skin, there are few publications that unite the body of the published literature in describing the precise role and mechanisms of action for Transcutol®. In view of the current mechanistic understanding of skin barrier properties, this paper takes on a retrospective review of the published works and critically evaluates the data for potential misses due to experimental variables such as formulation design, skin model, skin hydration levels, and drug properties. The goal of this review is to mitigate the incongruence of the published works and to construct a unified, comprehensive understanding of how Transcutol® influences skin penetration and permeation.

/pdf/skin-penetration-and-permeation-properties-of-transcutol-3v36r9egn3.pdf

Skin Penetration and Permeation Properties of Transcutol®—Neat or Diluted Mixtures

Propolis is one of the most used natural products known for centuries for its beneficial effects. Due to significant differences in chemical composition of samples originating from different geographic and climatic zones it is crucial to characterize reliably each type of propolis. This article comprises the latest findings concerning the poplar type propolis, i.e. it gives a cross section of chemical composition, botanical origin and biological activity of poplar type propolis in order to encourage further investigations that would indicate its beneficial effects.

https://journals.sagepub.com/doi/pdf/10.1177/1934578X1501001117

Poplar-type Propolis: Chemical Composition, Botanical Origin and Biological Activity.

Rutin is one of the most common dietary polyphenols found in vegetables, fruits, and other plants. It is metabolized by the mammalian gut microbiota and absorbed from the intestines, and becomes bioavailable in the form of conjugated metabolites. Rutin exhibits a plethora of bioactive properties, making it an extremely promising phytochemical. Numerous studies demonstrate that rutin can act as a chemotherapeutic and chemopreventive agent, and its anticancer effects can be mediated through the suppression of cell proliferation, the induction of apoptosis or autophagy, and the hindering of angiogenesis and metastasis. Rutin has been found to modulate multiple molecular targets involved in carcinogenesis, such as cell cycle mediators, cellular kinases, inflammatory cytokines, transcription factors, drug transporters, and reactive oxygen species. This review summarizes the natural sources of rutin, its bioavailability, and in particular its potential use as an anticancer agent, with highlighting its anticancer mechanisms as well as molecular targets. Additionally, this review updates the anticancer potential of its analogs, nanoformulations, and metabolites, and discusses relevant safety issues. Overall, rutin is a promising natural dietary compound with promising anticancer potential and can be widely used in functional foods, dietary supplements, and pharmaceuticals for the prevention and management of cancer.

The anticancer potential of the dietary polyphenol rutin: Current status, challenges, and perspectives.

Rutin, a polyphenolic natural compound is described in the literature for a wide range of biological activities. The study aims to test the antiproliferative potential and the antibacterial effect for pure rutin and its β cyclodextrin complexes. On one hand, the antiproliferative assays against A2780 (human ovarian cells), MDA-MB-231 (human breast cancer cells) and SiHa (cervical cancer cells) did not show any substantial inhibition of cell growth. On the other hand, the antimicrobial screening revealed that rutin presents positive effects against: Streptococcus pyogenes, Enterococcus faecalis, Bacillus cereus, Pseudomonas aeruginosa, Klebsiella pneumoniae and Escherichia coli. A decreased, but detectable, activity was noticed for Staphylococcus aureus and Streptococcus pneumoniae. Incorporation in the ramified cyclodextrins had a mixed effect on the antibacterial activity, with increased, constant or decreased effect, depending on the strain. The study concludes that rutin can be reconsiderate as a natural active antibacterial agent, while modulation of its solubility by incorporation in β-cyclodextrins is debatable depending on the tested strain.

Antiproliferative and antimicrobial properties of pure and encapsulated rutin

Increased sugar consumption and unhealthy dietary patterns are key drivers of many preventable diseases that result in disability and death worldwide. However, health awareness has increased over the past decades creating a massive on-going demand for new low/non-caloric natural sweeteners that have a high potential and are safer for consumption than artificial ones. The current study aims to investigate the nutritional properties, in vitro toxicological profile, total/individual polyphenols content, and the antioxidant, anti-cariogenic, and antimicrobial activity of two newly obtained vegan and sugar-free chocolate (VHC1 and VHC2). The energy values for the two finished products were very similar, 408.04 kcal/100 g for VHC1 and 404.68 kcal/100 g for VHC2. Both products, VHC1 and VHC2 present strong antioxidant activities, whereas antimicrobial results show an increased activity for VHC1 compared to VHC2, because of a higher phenolic content. In vitro toxicological evaluation revealed that both samples present a safe toxicological profile, while VHC2 increased cellular turnover of dermal cell lines, highlighting its potential use in skin treatments. The current work underlines the potential use of these vegetal mixtures as sugar-free substitutes for conventional products, as nutraceuticals, as well as topic application in skin care due to antimicrobial and antioxidant effects.

https://www.mdpi.com/2304-8158/9/12/1844/pdf

Nutritional, Antioxidant, Antimicrobial, and Toxicological Profile of Two Innovative Types of Vegan, Sugar-Free Chocolate

The purpose of the study was to use a new type of in vivo animal model developed by our research group for the investigation of skin penetration, compared to the results of Franz cell measurements. The new in vivo experimental model provides possibility for the exact measurement of the quantity of the penetrated drug through the living mouse skin. Two gel formulations containing ibuprofen were investigated with or without penetration enhancer. The applied penetration enhancer was Transcutol ® . The effect of the penetration enhancer was clearly detected in both models. The in vitro diffused amount of ibuprofen was significantly higher than the one permeated through the living skin. The presence of the active agent in the plasma was also determined after the observation period. It was possible to monitor the penetration and absorption of topical formulations simultaneously. Rezumat Obiectivul studiului a fost utilizarea unui nou tip de model animal in vivo realizat de grupul nostru de cercetare in scopul investigarii penetrarii prin piele, in comparaţie cu rezultatele masuratorilor prin celula Franz. Noul model experimental in vivo ofera posibilitatea unei masurari exacte a cantitaţii de substanţa medicamentoasa care penetreaza prin pielea de soarece. Au fost investigate doua formulari de tip gel cu ibuprofen, cu sau fara promotor de absorbţie. Promotorul de absorbţie utilizat a fost Transcutol ® . Efectul promotorului de absorbţie a fost clar detectat in ambele modele. Cantitatea de ibuprofen difuzata in vitro a fost semnificativ mai mare decât cea difuzata prin pielea de soarece. Prezenţa agentului terapeutic in plasma a fost de asemenea determinata dupa perioada de observaţie. A fost posibila monitorizarea simultana a penetrarii si absorbţiei ambelor formulari topice.

Monitoring of skin penetration and absorption with a new in vivo experimental model

A series of novel hybrid chalcone N-ethyl-piperazinyl amide derivatives of oleanonic and ursonic acids were synthesized, and their cytotoxic potential was evaluated in vitro against the NCI-60 cancer cell line panel. Compounds 4 and 6 exhibited the highest overall anticancer activity, with GI50 values in some cases reaching nanomolar values. Thus, the two compounds were further assessed in detail in order to identify a possible apoptosis- and antiangiogenic-based mechanism of action induced by the assessed compounds. DAPI staining revealed that both compounds induced nuclei condensation and overall cell morphological changes consistent with apoptotic cell death. rtPCR analysis showed that up-regulation of pro-apoptotic Bak gene combined with the down-regulation of the pro-survival Bcl-XL and Bcl-2 genes caused altered ratios between the pro-apoptotic and anti-apoptotic proteins' levels, leading to overall induced apoptosis. Molecular docking analysis revealed that both compounds exhibited high scores for Bcl-XL inhibition, suggesting that compounds may induce apoptotic cell death through targeted anti-apoptotic protein inhibition, as well. Ex vivo determinations showed that both compounds did not significantly alter the angiogenesis process on the tested cell lines.

Novel Synthesized N-Ethyl-Piperazinyl-Amides of C2-Substituted Oleanonic and Ursonic Acids Exhibit Cytotoxic Effects through Apoptotic Cell Death Regulation

C. Soica

Papers

Antiproliferative and antimicrobial properties of pure and encapsulated rutin

Nutritional, Antioxidant, Antimicrobial, and Toxicological Profile of Two Innovative Types of Vegan, Sugar-Free Chocolate

Monitoring of skin penetration and absorption with a new in vivo experimental model

Novel Synthesized N-Ethyl-Piperazinyl-Amides of C2-Substituted Oleanonic and Ursonic Acids Exhibit Cytotoxic Effects through Apoptotic Cell Death Regulation

HPLC comparative analysis of polyphenolic content of propolis and black poplar foliar bud extracts.