COMPARATIVE ANALYSIS OF THE CHEMICAL COMPOSITION OF LIPOPHILIC FRACTIONS OF SHOOTS OF THREE SPECIES OF THE GENUS CRATAEGUS L.

The article presents research of the chemical composition of lipophilic fractions of shoots Crataegus sanguinea Pall. (Rosaceae), Crataegus submollis Sarg. (Rosaceae) and Crataegus almaatensis Pojark. (Rosaceae). Lipophilic extract is obtained from petroleum ether. The components of the lipophilic fraction were separated and identified by gas chromatography with mass spectrometry. 36 compounds were identified in lipophilic fractions: hydrocarbons, fatty acids, sugars, phenolic compounds, diterpenoids and sterols. Their presence may determine the pharmacological properties of hawthorn shoots. These research expand information about the chemical composition of these hawthorn species and can be used in the development of a new drug.

On the Issue of Creating a Cream of Reparative Action for the Treatment and Prevention of Cheilitis

BACKGROUND: Cheilitis is an inflammatory disease of the lips, its red border, mucous membranes, and skin. There are meteorological, actinic, hypo-, and avitaminosis cheilitis, according to medical indications. Classification of cheilitis includes many types of diseases and is somewhat conditional. For these types of cheilitis treatment are most appropriate to use biologically active substances, in particular lipophilic extract of bee pollen. Lipophilic extract of bee pollen is a complex, concentrated plant-bee product with unique consumer and medicinal qualities. It should be noted that experiments have shown that the bee pollen lipophilic extract has a reparative effect higher than the widespread sea buckthorn oil. AIM: The aim of the work is to create therapeutic and prophylactic cream with lipophilic extract of bee pollen for the cheilitis treatment and prevention. MATERIALS AND METHODS: Cream preparation was conducted by phase inversion. Thermal and colloidal stability, pH values, the quantitative content of carotenoids, viscosity, osmotic activity, and microbiological purity were determined by generally accepted methods. RESULTS: Samples of the cream containing lipophilic extract of bee pollen are a homogeneous mass of soft consistency with light yellow color and pleasant specific odor. In estimating, the thermal stability cream samples cheilitis curing were successfully tested and proved to be stable. When centrifuging, the absence of stratification of the cream into fatty and aqueous phases after the test has showed the stability of the cream. The pH of the cream samples corresponds to the pH of the skin. During a qualitative test green color indicates the presence of carotenoids. Quantitative determination of the carotenoids amount in the cream for treatment and prevention cheilitis (in recalculation to β-carotene) corresponds to the set content of carotenoids in the cream of 5.4 mg. The viscosity of the developed cream at 16.2 s−1 is 68.38 ± 0.21 Pa x s, that fully corresponds to the viscosity of creams. In the study of osmotic activity, it was found that the cream with a glycerol content of 7% provides moderate osmotic activity of the drug for 8 h, which may indicate the absence of overdrying and irritating effect. In terms of microbiological purity, the investigated cream with lipophilic extract of bee pollen meets the requirements of the State Pharmacopoeia for finished medicines for topical use (category 2). CONCLUSION: For the cheilitis treatment and prevention has suggested the composition of the cream which contains biologically active substance – lipophilic extract of bee pollen. The technology of the cream with lipophilic extract of bee pollen was developed. Thermal and colloidal stability, pH values were studied; the quantitative content of carotenoids, viscosity, osmotic activity, and microbiological purity was determined. The research carried out made it possible to make sure of the correctness and rationality of the developed technology of the cream for the treatment and prevention of cheilitis.

Increases of Lipophilic Antioxidants and Anticancer Activity of Coix Seed Fermented by Monascus purpureus

Lipophilic tocols, γ-oryzanol, and coixenolide in coix seed before and after fermentation by Monascus purpureus were determined. Antioxidant and anticancer activities of raw and fermented coix seed were evaluated using free-radical-scavenging assays and polyunsaturated fatty acid oxidation model, and human laryngeal carcinoma cell HEp2, respectively. Compared to the raw seed, the tocols, γ-oryzanol, and coixenolide contents increased approximately 4, 25, and 2 times, respectively, in the fermented coix seed. Especially, γ-tocotrienol and γ-oryzanol reached 72.5 and 655.0 μg/g in the fermented coix seed. The lipophilic extract from fermented coix seed exhibited higher antioxidant activity in scavenging free radicals and inhibiting lipid oxidation. The inhibitory concentrations for 50% cell survival (IC50) of lipophilic extract from fermented coix seed in inhibiting HEp2 cells decreased by 42%. This study showed that coix seed fermented by M. purpureus increased free and readily bioavailable lipophilic antioxidants and anticancer activity. Therefore, fermentation could enhance the efficacy of the health promoting function of coix seeds.

Addressing the phytochemical prospection of thermally treated Eucalyptus grandis wood

This work aimed to investigate phytochemical prospection in treated and untreated wood of Eucalyptus grandis to understand the dynamics of extractives in relation to heat treatment. Samples of E. grandis wood were collected and grouped into external and internal regions. Half of the samples from each region were submitted to heat treatment at 190 ºC. From the treated and untreated samples, phytochemical tests were performed to detect classes of metabolites present in the E. grandis raw wood, hydrophilic extract and lipophilic extract. Phytochemical analysis detected the presence of alkaloids, phenolic compounds and triterpenoids in all hydrophilic extracts of the studied species. Presence of flavanonols, flavanones and saponins was detected only in the internal region of the wood. Tannins, leucoanthocyanidins, triterpenoids and saponins were influenced by heat treatment. The classes of flavonoids, xanthones and alkaloids are the most resistant to heat treatment. The phytochemical analysis made it possible to identify a new class of extractives that emerged after heat treatment, flavones.

Echinacea angustifolia DC. Lipophilic Extract Patch for Skin Application: Preparation, In Vitro and In Vivo Studies

Dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamide (tetraene) is the main component of Echinacea angustifolia DC. lipophilic extract, the bioavailability and immunomodulatory effect after oral administration in soft gel capsules in healthy volunteers of which we have already demonstrated. In the present work, we assessed the transdermal administration as an alternative route of administration of such an alkamide. The first step, therefore, encompassed the preparation of a drug-in-adhesive patch with an area of 868 mm2 and containing a dose of 0.64 mg of tetraene. In vitro skin permeation studies in Franz-type diffusion chambers resulted in a tetraene flux of (103 ± 10) ng × cm−2 × h−1 with a very good linearity (r = 0.99). The relatively low lag time of just 13 min indicates low binding and the accumulation of tetraene in the skin. Finally, the patch was administered to six healthy volunteers, and the pharmacokinetic analysis was performed by nonlinear mixed effects modelling with soft gel oral capsules serving as the reference formulation. The in vivo results correlated well with the in vitro permeation and indicated an initial burst tetraene absorption from the patch that was in parallel with the zero-order kinetics of absorption. The rate of the latter process was in good agreement with the one estimated in vitro. The tetraene absorption rate was therefore slow and prolonged with time, resulting in a bioavailability of 39% relative to the soft gel capsules and a very flat plasma concentration profile.

Achiote (Bixa orellana) Lipophilic Extract, Bixin, and δ-tocotrienol Effects on Lifespan and Stress Resistance in Caenorhabditis elegans

The onset of many degenerative diseases related to aging has been associated with a decrease in the activity of antistress systems, and pharmacological interventions increasing stress resistance could be effective to prevent the development of such diseases. Achiote is a valuable source of carotenoid and tocotrienols, which have antioxidant activity. In this work, we explore the capacity of an achiote seed extract and its main compounds to modulate the lifespan and antistress responses on Caenorhabditis elegans, as well as the mechanisms involved in these effects. Achiote lipophilic extract, bixin, and δ-tocotrienol were applied on nematodes to carry out lifespan, stress resistance, and fertility assays. The achiote seed extract increased the median and maximum lifespan up to 35% and 27% and increased resistance against oxidative and thermal stresses without adverse effects on fertility. The beneficial effects were mimicked by a bixin+δ-tocotrienol mixture. All the effects on lifespan and stress resistance were independent of caloric restriction but dependent on the insulin/insulin growth factor-1 pathway. This study could provide insights for further research on a new beneficial use of this important crop in health and nutraceutical applications beyond its use as a source of natural pigments.