Dermal Penetration Studies of Potential Phenolic Compounds Ex Vivo and Their Antioxidant Activity In Vitro.

Phenolic compounds with miscellaneous biological activities are an interesting component in dermatology and cosmetology practices. The aim of our study was to determine the phenolic compounds released from emulsion, emulgel, gel, ointment, and oleogel formulations penetration into human skin layers, both the epidermis and dermis, and estimate their antioxidant activity. The ex vivo penetration study was performed using Bronaugh type flow-through diffusion cells. Penetration studies revealed that, within 24 h, the chlorogenic acid released from the oleogel penetrated into skin layers to a depth of 2.0 ± 0.1 µg/mL in the epidermis and 1.5 ± 0.07 µg/mL in the dermis. The oleogel-released complex of phenolic compounds penetrating into epidermis showed the strongest DPPH free radical scavenging activity (281.8 ± 14.1 µM TE/L). The study estimated a strong positive correlation (r = 0.729) between the amount of quercetin penetrated into epidermis and the antioxidant activity detected in the epidermis extract. Plant based phenolic compounds demonstrated antioxidant activity and showed great permeability properties through the skin.

Phenolic Content and Antioxidant Activity in Fruit of the Genus Rosa L.

Throughout history, people of different cultures have acknowledged the relationship between food properties and health. The pseudo-fruits of different Rosa species contain high levels of vitamin C and other beneficial biological active agents such as phenolics, and others. The purpose of the research was to determine the variability of the phenolic compound profiles in the fruit of different species of Rosa L. and to evaluate the antioxidant activity of fruit extracts in vitro. The total contents of phenolics, flavonoids, procyanidins, and hydroxycinnamic acid derivatives were performed using the spectrophotometric method. Qualitative and quantitative analysis of individual phenolics in rosehip samples was carried out by applying the HPLC method. The largest amounts of phenolic compounds 26.49 ± 1.32 mg GRE/g were found in rosehip samples of the Rosa pisocarpa species. (+)-Catechin was the predominant phenolic compound in rosehip fruit samples, and the highest content 522.48 ± 26.12 µg/g was found in rosehip samples of the Rosa subcanina species. A strong correlation was found between the total amount of phenolic compounds determined in rosehip extracts and the radical scavenging and reducing the activity of their extracts in vitro (r = 0.759 and 0.761, accordingly, p < 0.001).

Triterpene Content in Flesh and Peel of Apples Grown on Different Rootstocks.

Advancements in rootstock breeding and selection have revolutionized the manner in which apples are grown throughout the world. Fruit tree breeding has typically focused on key horticultural characteristics. Even though agents with health benefits have been investigated more frequently during the recent years, information about the effect of different cultivation factors, such as the rootstock, on triterpene concentration is still lacking. The present study aimed to evaluate triterpene profiles and the quantitative composition of different parts of apple fruit that was grown on 17 various origin and vigor rootstocks. HPLC analyses of triterpenes in apple samples were performed. The highest total content of triterpenes (7.72 ± 0.39 mg/g) was found in peel samples of apples grown on the dwarf rootstock 62-396-B10®. Depending on the rootstock, apple peel samples accumulated 3.52 to 4.74 times more triterpene compounds than apple flesh samples. Ursolic acid was the predominant triterpene compound in apple peel and flesh samples. The highest content of ursolic acid (5.84 ± 0.29 mg/g) was found in peel samples of apples grown on the dwarf rootstock 62-396-B10®. Meanwhile, the lowest amount of ursolic acid (3.25 ± 0.16 mg/g) was found in apple peel samples grown on the dwarf rootstock Cepiland-Pajam®2. A proper match of a cultivar and a rootstock can program a fruit tree to grow larger amounts of higher quality, antioxidant-rich, and high-nutrition-value fruit.

Phenolic Content and Antioxidant Activity in Apples of the 'Galaval' Cultivar Grown on 17 Different Rootstocks.

Apple cultivars are one of the main factors setting the composition of bioactive compounds in apples and the quality of the fruit. However, research has been providing increasing amounts of data on the influence of rootstocks on the variations in the composition of bioactive compounds in apples. The aim of the study was to determine the influence of rootstocks on the changes in the qualitative and quantitative composition of phenolic compounds and their antioxidant activity in vitro in apple flesh and peel. HPLC analyses of phenolic compounds in apple samples were performed. The rootstock-scion combination had a significant effect on the composition and antioxidant activity of phenolic compounds in apple samples. Depending on the rootstock, the total content of phenolic compounds in apple flesh of the 'Galaval' cultivar could vary by 2.9 times, and in the peel by up to 90%. The genotype of the rootstock resulted in the highest variation in total flavan-3-ol content in apple flesh-by as much as 4.3 times-while the total content of flavonols varied by 2.1 times. In apple peel, on the contrary, the greatest variation was recorded for the total flavonol content (by 4.4 times), and the total flavan-3-ol content varied the least (by 1.8 times). A proper match of a cultivar and a rootstock can program a fruit tree to grow larger amounts of higher-quality, antioxidant-rich, and high-nutrition-value fruit.

Formulation of Gels and Emulgels with Malus domestica Borkh: Apple Extracts and Their Biopharmaceutical Evaluation In Vitro.

Phenolic compounds that estimate apple extracts with multifaceted biological effects are potentially valuable for protection against skin disorders. The purpose of our research was to formulate gels and emulgels containing a complex of phenolic compounds of apple extracts and to perform a biopharmaceutical evaluation of semi-solid pharmaceutical forms, determining their antioxidant activity in vitro. HPLC analyses of phenolic compounds were performed. The total amount of phenolic compounds found in the sample of apples from the 'Paprastasis antaninis' cultivar was 1455.5 ± 72.8 µg/g. The release of phenolics from gels and emulgels was assessed by Franz-type diffusion cells. The in vitro release test revealed that phenolic compounds were released from the gel (G1-G6) formulations (70.6-73.8%) compared to the amounts (77.2-83.9%) released from the emulgel (E1-E6) formulations. The largest amount (83.9%) of phenolic compounds was released from the E5 formulation, while the smallest amounts (70.6%) were released from the formulations G3 and G5. The antioxidant activity evaluated by the DPPH and FRAP methods observed in all gel (G1-G6) and emulgel (E1-E6) formulations after 6 h were the strongest, compared to the activities observed in the formulations after 2 or 4 h. Gels and emulgels, which are rich in apple extracts, have strong antioxidant properties and may be promising choices for the development of new, innovative pharmaceutical forms or cosmetics.

Impact of Storage Controlled Atmosphere on the Apple Phenolic Acids, Flavonoids, and Anthocyanins and Antioxidant Activity In Vitro.

Apples are seasonal fruits, and it is important to prepare them adequately for storage and ensure proper storage conditions. In this study, we used ten different apple cultivars: 'Alva', 'Auksis', 'Connell Red', 'Cortland', 'Ligol', 'Lodel', 'Noris', 'Rubin', 'Sampion', and 'Spartan'. We studied the qualitative and quantitative composition of phenolic compounds in the apple and apple extracts antioxidants activity before placing them in the controlled atmosphere chambers and again at the end of the experiment, eight months later. Different concentrations of O2, CO2, and N2, constant temperature, relative humidity, and removal of endogenous ethylene were continually maintained. HPLC analysis showed that the highest amount of 2265.7 ± 152.5 µg/g of chlorogenic acid was found in apple samples of the 'Auksis' cultivar stored under variant IV conditions. Different concentrations of gas in the controlled atmosphere chambers caused changes in antioxidant activity in whole apple and apple peel extracts. In our study, we found that the antioxidant activity of apple extracts varied between samples of different apple cultivars and depended on the composition of the controlled atmosphere. Determining the optimal storage conditions is beneficial to providing the consumers with apples that have a known and minimally altered chemical composition of phenolic compounds and the strongest antioxidant activity, which determine the use of apples in the healthy food chain.

Antioxidant, Anti-Inflammatory, and Cytotoxic Activity of Extracts from Some Commercial Apple Cultivars in Two Colorectal and Glioblastoma Human Cell Lines.

Cancer initiation and development are closely related to oxidative stress and chronic inflammation. The aim of this study was to evaluate apple extracts and individual tritepenes antioxidant, anti-inflammatory, and cytotoxic activities. Dry extracts of apple were analyzed by HPLC-PDA. A hyaluronidase inhibition assay was selected to determine the anti-inflammatory effect. Cytotoxic activities against human colon adenocarcinoma cell line (HT-29) and human glioblastoma cell line (U-87) were determined using MTT, cell colony formation, and spheroid growth assays. Radical scavenging and reducing activities were evaluated using DPPH, ABTS, FRAP, and CUPRAC assays, respectively. The apple extracts inhibited hyaluronidase from 26.38 ± 4.4% to 35.05 ± 3.8%. The AAW extract possessed the strongest cytotoxic activity (EC50 varied from 113.3 ± 11.11 µg/mL to 119.7 ± 4.0 µg/mL). The AEW extract had four and five times stronger antiradical activity when determined by ABTS and DPPH, and two and eight times stronger reducing activity when evaluated by CUPRAC and FRAP, respectively. Understanding the mechanisms of apple extracts and individual triterpenes as hyaluronidase inhibitors and antioxidants related in cancer development may be a benefit to future study in vivo, as well as cancer prognosis or the development of new, innovative food supplements, which could be used for chronic disease prevention.

Variation of Triterpenes in Apples Stored in a Controlled Atmosphere.

Apples are seasonal fruits, and thus after harvesting apples of optimal picking maturity, it is important to prepare them properly for storage and to ensure proper storage conditions in order to minimize changes in the chemical composition and commercial quality of the apples. We studied the quantitative composition of triterpenic compounds in the whole apple, apple peel and apple flesh samples before placing them in the controlled atmosphere (CA) chambers, and at the end of the experiment, 8 months later. HPLC analysis showed that highest total amount of triterpenic compounds (1.99 ± 0.01 mg g-1) was found in the whole apple samples of the 'Spartan' cultivar stored under variant VIII (O2-20%, CO2-3%, N2-77%) conditions. Meanwhile, the highest amount of triterpenic compounds (11.66 ± 0.72 mg g-1) was determined in the apple peel samples of the 'Auksis' cultivar stored under variant II (O2-5%, CO2-1%, N2-94%) conditions. In the apple peel samples of the 'Auksis' cultivar stored under variant I (O2-21%, CO2-0.03%, N2-78.97%) conditions, the amount of individual triterpenic compounds (ursolic, oleanolic, corosolic, and betulinic acids) significantly decreased compared with amount determined before the storage. Therefore, in the apple flesh samples determined triterpenic compounds are less stable during the storage under controlled atmosphere conditions compared with triterpenic compounds determined in the whole apple and apple peel samples.

Biopharmaceutical Evaluation of Capsules with Lyophilized Apple Powder.

Apples are an important source of biologically active compounds. Consequently, we decided to model hard gelatin capsules with lyophilized apple powder by using different excipients and to evaluate the release kinetics of phenolic compounds. The apple slices of "Ligol" cultivar were immediately frozen in a freezer (at -35°C) with air circulation and were lyophilized with a sublimator at the pressure of 0.01 mbar (condenser temperature, -85°C). Lyophilized apple powder was used as an active substance filled into hard gelatin capsules. We conducted capsule disintegration and dissolution tests to evaluate the quality of apple lyophilizate-containing capsules of different encapsulating content. Individual phenolic compounds can be arranged in the following descending order according to the amount released from the capsules of different compositions: chlorogenic acid > rutin > avicularin > hyperoside > phloridzin > quercitrin > (-)-epicatechin > isoquercitrin. Chlorogenic acid was the compound that was released in the highest amounts from capsules of different encapsulating content: its released amounts ranged from 68.4 to 640.3 µg/mL. According to the obtained data, when hypromellose content ranged from 29% to 41% of the capsule mass, the capsules disintegrated within less than 30 min, and such amounts of hypromellose did not prolong the release of phenolic compounds. Based on the results of the dissolution test, the capsules can be classified as fast-dissolving preparations, as more than 85% of the active substances were released within 30 min.

The Qualitative and Quantitative Compositions of Phenolic Compounds in Fruits of Lithuanian Heirloom Apple Cultivars.

As the interest in heirloom cultivars of apple trees, their fruit, and processed products is growing worldwide, studies of the qualitative and quantitative composition of biological compounds are important for the evaluation of the quality and nutritional properties of the apples. Studies on the variations in the chemical composition of phenolic compounds characterized by a versatile biological effect are important when researching the genetic heritage of the heirloom cultivars in order to increase the cultivation of such cultivars in orchards. A variation in the qualitative and quantitative composition of phenolic compounds was found in apple samples of cultivars included in the Lithuanian collection of genetic resources. By the high-performance liquid chromatography (HPLC) method flavan-3-ols (procyanidin B1, procyanidin B2, procyanidin C2, (+)-catechin and (-)-epicatechin), flavonols (rutin, hyperoside, quercitrin, isoquercitrin, reynoutrin and avicularin), chlorogenic acids and phloridzin were identified and quantified in fruit samples of heirloom apple cultivars grown in Lithuania. The highest sum of the identified phenolic compounds (3.82 ± 0.53 mg/g) was found in apple fruit samples of the 'Kostele' cultivar.