Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes.

Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.

chiro-Inositol Derivatives from Chisocheton paniculatus Showing Inhibition of Nitric Oxide Production.

Six new chiro-inositol derivatives (1-6) were isolated from the leaves of Chisocheton paniculatus collected in Vietnam. Their chemical structures were elucidated by 1D and 2D NMR and HRESIMS analyses. All isolated compounds were evaluated for their inhibitory activity against lipopolysaccharide-induced nitric oxide (NO) production in the RAW 264.7 macrophage cell line. Compound 4 exhibited potent inhibitory activity for NO production with an IC50 value of 7.1 µM.

Composition and Antibacterial Effect of Mint Flavorings in Candies and Food Supplements.

Mint flavorings are widely used in confections, beverages, and dairy products. For the first time, mint flavoring composition of mint candies and food supplements (n = 45), originating from 16 countries, as well as their antibacterial properties, was analyzed. The flavorings were isolated by Marcusson's type micro-apparatus and analyzed by GC-MS. The total content of the mint flavoring hydrodistilled extracts was in the range of 0.01 - 0.9%. The most abundant compounds identified in the extracts were limonene, 1,8-cineole, menthone, menthofuran, isomenthone, menthol and its isomers, menthyl acetate. The antimicrobial activity of 13 reference substances and 10 selected mint flavoring hydrodistilled extracts was tested on Escherichia coli and Staphylococcus aureus by broth dilution method. Linalool acetate and (-)-carvone, as most active against both bacteria, had the lowest MIC90 values. (+)-Menthyl acetate, (-)-menthyl acetate, and limonene showed no antimicrobial activity. Three of the tested extracts had antimicrobial activity against E. coli and 8 extracts against S. aureus. Their summary antimicrobial activity was not always in concordance with the activities of respective reference substances.

Effects of Hippeastrum reticulatum on memory, spatial learning and object recognition in a scopolamine-induced animal model of Alzheimer's disease.

CONTEXT: The methanol extracts from Hippeastrum reticulatum (L'Hér.) Herb. (Amaryllidaceae) (HR) display acetylcholinesterase inhibitory (AChEI) activity. OBJECTIVE: AChEI of alkaloids isolated from HR bulbs and the ameliorating effects of the alkaloid fraction (AHR) on memory and cognitive dysfunction in scopolamine-treated mice were investigated. MATERIALS AND METHODS: Alkaloids were isolated by column chromatography and identified by spectroscopy. AChEI was evaluated using the modified Ellman's method. Sixty Swiss male mice were randomly divided into six groups, received samples for 15 days. Normal group received saline, scopolamine-treated group scopolamine (1.5 mg/kg, intraperitoneal injection). Test groups received AHR (5, 10 and 15 mg/kg, per os) and positive control group donepezil (5 mg/kg, per os), administered 1 h before the test, scopolamine was injected 30 min prior to testing. The cognitive-enhancing activity of AHR against scopolamine-induced memory impairments was investigated using Y-maze, the novel object recognition test (NORT) and the Morris water maze (MWM) test. RESULTS: Seven alkaloids were isolated for the first time from the genus Hippeastrum: trans-dihydronarciclasine (1), N-chloromethylnarcissidinium (2), narciprimin (3), narciclasine-4-O-ß-d-xylopyranoside (4), N-methyltyramine (5), 3ß,11α-dihydroxy-1,2-dehydrocrinane (6) and brunsvigine (7); three are new compounds (2, 5, 6). Among them, 2-3 and 5-6 showed AChEI in vitro with IC50 values of 29.1, 46.4, 70.1 and 104.5 µg/mL, respectively. The anti-AChEI of 2, 5 and 6 are reported for the first time. In in vivo test, AHR (15 mg/kg) significantly increased in spontaneous alternation performance in the Y-maze test (p < 0.01), it significantly increased the time spent exploring the novel object (p < 0.05) comparison with scopolamine-treated group. The administration of AHR at doses 10 and 15 mg/kg significantly decreased escapes latency and swimming distance to the platform on day 6 compared to these in day 1 (p < 0.01 and p < 0.05, respectively). CONCLUSIONS: AHR could be a potential candidate of future trials for treatment of memory and cognitive dysfunction in Alzheimer's disease.

A new triterpene ester and other chemical constituents from the aerial parts of Anodendron paniculatum and their cytotoxic activity.

The aim of the research was to study the active constituents of Anodendron paniculatum Roxb. (Apocynaceae). A new triterpene ester, named anopaniester (1), and cycloartenol (2), ursolic acid (3), esculenic acid (4), bis-(2-ethylhexyl) phthalate (5), desmosterol (6), stigmasterol (7), vaniline (8), and (E)-phytol (9), were isolated from the aerial parts of A. paniculatum. Compounds 3 and 6 showed the significant inhibitory effect (IC50 values ranging from 30.89 ± 3.60 to 44.37 ± 5.40 µg/ml) against tested human cancer cell lines LU-1 and MKN-7. The compounds 1-4, and 6 were isolated from this genus Anodendron for the first time.

Antibacterial activities of chemical constituents from the aerial parts of Hedyotis pilulifera.

CONTEXT: Hedyotis pilulifera (Pit.) T.N. Ninh (Rubiaceae) has been used in Vietnamese ethnomedicine; the methanol extract exhibited antibacterial activity in our preliminary screening. OBJECTIVES: In this study, compounds from H. pilulifera were isolated and their antibacterial activity in vitro was evaluated. MATERIALS AND METHODS: The aerial parts of H. pilulifera (1.4 kg) were extracted with MeOH, suspended in water and ethyl acetate extract was chromatographed on a silica gel column. The structures of isolated compounds were elucidated by the combination analyses of spectroscopy including 1D-, 2D-NMR, HRMS and in comparison with the reported NMR data in the literature. All isolated compounds were evaluated for inhibitory effect using the microdilution method toward Staphylococcus aureus, Bacillus subtilis and Mycobacterium smegmatis, and MIC values were determined. RESULTS: Twenty compounds were isolated, including five triterpenoids, two steroids, two aromatic compounds, three fatty acids, one quinone derivative, one lignan glycoside, one ceramide and five glycolipids. Among these, oleanolic acid showed significant antibacterial activity against M. smegmatis with the MIC value of 2.5 µg/mL. Remarkably, rotungenic acid showed strong activity against S. aureus, B. subtilis, M. smegmatis with MIC values of 2.5, 2.5 and 1.25 µg/mL, respectively. Rotundic acid exhibited significant antibacterial activity against B. subtilis with the MIC value of 5 µg/mL. To the best of our knowledge, the antibacterial activity of rotungenic acid, stigmast-4-ene-3,6-dione and (2S,3S,4R,2'R)-2-(2'-hydroxytetracosanoylamino) octadecane-1,3,4-triol was reported for the first time. CONCLUSIONS: Oleanolic acid, rotungenic acid, and rotundic acid were considered to be useful for developing new antimicrobial therapeutic agents for human.

THE USE OF PANAX GINSENG AND ITS ANALOGUES AMONG PHARMACY CUSTOMERS IN ESTONIA: A CROSS-SECTIONAL STUDY.

The aim of the cross-sectional study was to evaluate the pattern of complementary self-treatment with P. ginseng and its analogues amongst pharmacy customers in Estonia. The study instrument consisted of multiple-choice items related to personal knowledge about and experience with the use of P. ginseng and its analogues. In total, 1233 customers participated in the study. Of study participants, 18.1% reported the use of P. ginseng and its analogues in their lives. P. ginseng preparations were used mostly according to the well- known indications (tiredness, weakness and decreased mental and physical capacity). Of P. ginseng users 44.3% reported positive treatment effects and 12.0% had experienced different side effects. With increase of age (p < 0.01) and at lower levels of education (p = 0.04), the use of ginseng or its analogues decreased. The better the users evaluated their health, the better they perceived the effect of P. ginseng preparations (p < 0.01). This study reported rather frequent use of P. ginseng and its analogues. P. ginseng could be seen in the treatment of conditions, where the use of local medicinal plants has not been established. Further research is needed to learn more about public knowledge and experiences about efficacy and safety of P. ginseng and its analogues.

Estonian folk traditional experiences on natural anticancer remedies: from past to the future.

CONTEXT: Despite diagnostic and therapeutic advancements, the burden of cancer is still increasing worldwide. Toxicity of current chemotherapeutics to normal cells and their resistance to tumor cells highlights the urgent need for new drugs with minimal adverse side effects. The use of natural anticancer agents has entered into the area of cancer research and increased efforts are being made to isolate bioactive products from medicinal plants. OBJECTIVE: To lead the search for plants with potential cytotoxic activity, ethnopharmacological knowledge can give a great contribution. Therefore, the attention of this review is devoted to the natural remedies traditionally used for the cancer treatment by Estonian people over a period of almost 150 years. METHODS: Two massive databases, the first one stored in the Estonian Folklore Archives and the second one in the electronic database HERBA ( http://herba.folklore.ee/ ), containing altogether more than 30 000 ethnomedicinal texts were systematically reviewed to compile data about the Estonian folk traditional experiences on natural anticancer remedies. RESULTS AND CONCLUSION: As a result, 44 different plants with potential anticancer properties were elicited, 5 of which [Angelica sylvestris L. (Apiaceae), Anthemis tinctoria L. (Asteraceae), Pinus sylvestris L. (Pinaceae), Sorbus aucuparia L. (Rosaceae), and Prunus padus L. (Rosaceae)] have not been previously described with respect to their tumoricidal activities in the scientific literature, suggesting thus the potential herbal materials for further investigations of natural anticancer compounds.

Eucalypt Extracts Prepared by a No-Waste Method and Their 3D-Printed Dosage Forms Show Antimicrobial and Anti-Inflammatory Activity.

The pharmaceutical industry usually utilizes either hydrophobic or hydrophilic substances extracted from raw plant materials to prepare a final product. However, the waste products from the plant material still contain biologically active components with the opposite solubility. The aim of this study was to enhance the comprehensive usability of plant materials by developing a new no-waste extraction method for eucalypt leaves and by investigating the phytochemical and pharmacological properties of eucalypt extracts and their 3D-printed dosage forms. The present extraction method enabled us to prepare both hydrophobic soft extracts and hydrophilic (aqueous) dry extracts. We identified a total of 28 terpenes in the hydrophobic soft extract. In the hydrophilic dry extract, a total of 57 substances were identified, and 26 of them were successfully isolated. The eucalypt extracts studied showed significant antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Candida albicans, Corynebacterium diphtheriae gravis, and Corynebacterium diphtheriae mitis. The anti-inflammatory activity of the dry extract was studied using a formalin-induced-edema model in mice. The maximum anti-exudative effect of the dry extract was 61.5% at a dose of 20 mg/kg. Composite gels of polyethylene oxide (PEO) and eucalypt extract were developed, and the key process parameters for semi-solid extrusion (SSE) 3D printing of such gels were verified. The SSE 3D-printed preparations of novel synergistically acting eucalypt extracts could have uses in antimicrobial and anti-inflammatory medicinal applications.

Application of nanofiber-based drug delivery systems in improving anxiolytic effect of new 1,2,3-triazolo-1,4-benzodiazepine derivatives.

Anxiety disorders are highly prevalent worldwide and can affect people of all ages, genders and backgrounds. Much efforts and resources have been directed at finding new anxiolytic agents and drug delivery systems (DDSs) especially for cancer patients to enhance targeted drug delivery, reduce drug adverse effects, and provide an analgesic effect. The aim of this study was (1) to design and develop novel nanofiber-based DDSs intended for the oral administration of new 1,2,3-triazolo-1,4-benzodiazepines derivatives, (2) to investigate the physical solid-state properties of such drug-loaded nanofibers, and (3) to gain knowledge of the anxiolytic activity of the present new benzodiazepines in rodents in vivo. The nanofibers loaded with 1,2,3-triazolo-1,4-benzodiazepine derivatives were prepared by means of electrospinning (ES). Field-emission scanning electron microscopy and attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy were used for the physicochemical characterization of nanofibers. The anxiolytic activity of new derivatives and drug-loaded nanofibers was studied with an elevated plus maze test and light-dark box test. New 1,2,3-triazolo-1,4-benzodiazepine derivatives showed a promising anxiolytic effect in mice with clear changes in behavioral reactions in both tests. The nanofiber-based DDS was found to be feasible in the oral delivery of the present benzodiazepine derivatives. The nanofibers generated by means of ES presented the diameter in a nanoscale, uniform fiber structure, capacity for drug loading, and the absence of defects. The present findings provide new insights in the drug treatment of anxiety disorders with new benzodiazepine derivatives.

Phytochemical, Technological, and Pharmacological Study on the Galenic Dry Extracts Prepared from German Chamomile (Matricaria chamomilla L.) Flowers.

Galenic preparations of German chamomile are used to treat mild skin diseases, inflammation, and spasms, and they have also been reported to have anxiolytic and sedative effects. The medicinal use of chamomile is well known in ethnomedicine. After obtaining its galenic preparations, there is lots of waste left, so it is expedient to develop waste-free technologies. The aims of this study were to gain knowledge of the ethnomedical status of chamomile in the past and present, develop methods for preparing essential oils and dry extracts from German chamomile flowers using complex processing, reveal the phytochemical composition of such extracts, and verify the analgesic and soporific activity of the extracts. Two methods for the complex processing of German chamomile flowers were developed, which allowed us to obtain the essential oil and dry extracts of the tincture and aqueous extracts as byproducts. A total of 22 phenolic compounds (7 hydroxycinnamic acids, 13 flavonoids, and 2 phenolic acids) were found in the dry extracts by using UPLC-MS/MS. In total, nine main terpenoids were identified in the chamomile oil, which is of the bisabolol chemotype. During the production of chamomile tincture, a raw material-extractant ratio of 1:14-1:16 and triple extraction are recommended for its highest yield. In in vivo studies with mice and rats, the extracts showed analgesic activity and improvements in sleep. The highest sedative and analgesic effects in rodents were found with the dry extract prepared by using a 70% aqueous ethanol solution for extraction at a dose of 50 mg/kg. The developed methods for the complex processing of German chamomile flowers are advisable for implementation into the pharmaceutical industry to reduce the volume of waste during the production of its essential oil and tincture, and to obtain new products.

Phytochemical, Pharmacological, and Molecular Docking Study of Dry Extracts of Matricaria discoidea DC. with Analgesic and Soporific Activities.

Pineapple weed (Matricaria discoidea DC.) is a widespread plant in Europe and North America. In ethnomedicine, it is well-known for its anti-inflammatory and spasmolytic activities. The aim of this research was to develop novel methods of M. discoidea processing to obtain essential oil and dry extracts and to investigate their phytochemical compositions. Moreover, the molecular docking of the main substances and the in vivo studies on their soporific and analgesic activities were conducted. The essential oil and two dry extracts from M. discoidea were prepared. A total of 16 phenolic compounds (seven flavonoids, seven hydroxycinnamic acids, and two phenolic acids) in the dry extracts were identified by means of UPLC-MS/MS. In the essential oil, nine main terpenoids were identified by gas chromatography (GC). It was shown that phenolic extraction from the herb was successful when using 70% ethanol in a triple extraction method and at a ratio of 1:14-1:16. The in vivo studies with rodents demonstrated the analgesic activity of the M. discoidea extracts and improvements in the sleep of animals. The dry extracts of M. discoidea did not show any toxicity. The molecular docking analysis showed a high probability of COX-1,2 inhibition and NMDA receptor antagonism by the extracts.

American Cranberry (Oxycoccus macrocarpus (Ait.) Pursh) Leaves Extract and Its Amino-Acids Preparation: The Phytochemical and Pharmacological Study.

The liver is an organ with several important biofunctions, for which there are very few effective and safe preparations that promote the functioning, protection, and regeneration of cells. Sufficiently safe preparations with hepatoprotective activity can be found in plants. The aim of our study was to investigate the chemical composition of an extract made from American cranberry (Oxycoccus macrocarpus (Ait.) Pursh) leaves and its amino-acids preparations as well as their possible hepatoprotective activity. Using the UPLC-MS/MS method, we identified 19 phenolic compounds (8 flavonoids (flavones and flavonols), 4 anthocyanins, 3 hydroxycinnamic acids, and 2 catechins). The prophylactic and therapeutic administration of the American cranberry-leaves extracts led to a decrease in the lipid-peroxidation process during a study of tetrachloromethane acute toxic damage in the liver of rats. As a result of animal studies, the most effective hepatoprotective activity was found in the extract preparations with valine and arginine.

Pharmaceutical 3D-printing of nanoemulsified eucalypt extracts and their antimicrobial activity.

Overcoming the health threatening consequences of staphylococcal infections and their negative socio-economic effects have become a priority in the medical, pharmaceutical, food and many other sectors globally. Staphylococcal infections are a big challenge for a global health care, since they are difficult to be diagnosed and treated. Therefore, the development of new medicinal products of plant-origin is timely and important, because bacteria have a limited ability to develop resistance to such products. In the present study, a modified eucalypt (Eucalyptus viminalis L.) extract was prepared and further enhanced by using different excipients (surface active agents) to obtain a water-miscible 3D-printable extract (nanoemulsified aqueous eucalypt extract). Phytochemical and antibacterial studies of the eucalypt leaves extracts were conducted as a preliminary investigation for 3D-printing experiments of the extracts. The nanoemulsified aqueous eucalypt extract was mixed with polyethylene oxide (PEO) to form a gel applicable for semi-solid extrusion (SSE) 3D printing. The key process parameters in a 3D-printing process were identified and verified. The printing quality of the 3D-lattice type eucalypt extract preparations was very good, demonstrating the feasibility of using an aqueous gel in SSE 3D printing also exhibiting compatibility of the carrier polymer (PEO) with the plant extract. The SSE 3D-printed eucalypt extract preparations presented a rapid dissolution in water within 10-15 min, suggesting the applicability of these preparations e.g., in oral immediate-release applications.

Chemical Composition and Insulin-Resistance Activity of Arginine-Loaded American Cranberry (Vaccinium macrocarpon Aiton, Ericaceae) Leaf Extracts.

One of the key pathogenetic links in type 2 diabetes mellitus (T2DM) is the formation of insulin resistance (IR). Besides a wide selection of synthetic antidiabetic drugs, various plant-origin extracts are also available to support the treatment of T2DM. This study aimed to investigate and gain knowledge of the chemical composition and potential IR correction effect of American cranberry (Vaccinium macrocarpon Aiton) leaf extracts and formulate novel 3D-printed oral dosage forms for such extracts. The bioactivity and IR of L-arginine-loaded cranberry leaf extracts were studied in vivo in rats. The cranberry leaf extracts consisted of quinic, 3-caffeoylquinic (chlorogenic), p-coumaroylquinic acids, quercetin 3-O-galactoside, quercetin-3-O-glucoside, quercetin-3-xyloside, quercetin-3-O-arabino pyranoside, quercetin-3-O-arabinofuranoside, quercetin 3-O-rhamnoside, and quercetin-O-p-coumaroyl hexoside-2 identified by HPLC. In vivo studies with rats showed that the oral administration of the cranberry leaf extracts had a positive effect on insulin sensitivity coefficients under the insulin tolerance test and affected homeostasis model assessment IR levels and liver lipid content with experimental IR. A novel 3D-printed immediate-release dosage form was developed for the oral administration of cranberry leaf extracts using polyethylene oxide as a carrier gel in semi-solid extrusion 3D printing. In conclusion, American cranberry leaf extracts loaded with L-arginine could find uses in preventing health issues associated with IR.

Factors influencing purchase of and counselling about prescription and OTC medicines at community pharmacies in Tallinn, Estonia.

The aims of the current survey were to evaluate factors influencing purchase of prescription and OTC medicines of pharmacy customers in Tallinn, Estonia and to identify the role of community pharmacists in counselling of prescription and OTC medicines. Structured questionnaire was used to interview pharmacy customers (n = 1820) in six community pharmacies of Tallinn, the capital city of Estonia. The survey instrument consisted of 15 multiple-choice items. According to the survey results, prescription and OTC medicines were bought from community pharmacies almost equally. The most popular OTC medicines were analgesics (38%), cold and cough medicines (21%). The older survey participants and these with lower income and with elementary school education bought more prescription medicines (p < 0.01). Survey participants with higher income were purchasing more OTC medicines and food supplements (p < 0.01). Before purchase of medicines recommendations were received mainly from physicians about prescription and from pharmacists about OTC medicines. However, the counselling provided by community pharmacists in selecting of both types of medicines was highly appreciated. Pharmacists as source for drug information were less trusted among the survey participants < 25 and 26-40 years (p < 0.01). Fast service and confidential counselling about medicines was less important for the respondents with elementary school education (p < 0.01).

Ethnic Identity in Transition: the Potential Impact of Ethnicity on Chronic Illness' Medication Adherence in Post-Soviet Country.

Previously, it has been shown that factors like ethnicity and proficiency of state's official language not only influence self-management abilities and medication adherence but may also indicate the level of trust in physicians, medication, and healthcare system. This research aims to examine the potential impact of ethnicity on medication adherence based on the example of a post-Soviet country. The research was carried out as a quantitative survey among 303 hypertension and type 2 diabetes patients in Estonia, involving participants from ethnic majority and minority. Research was conducted in community pharmacies and data analysed statistically with SPSS. The findings were opposite to previous research. Although members of the ethnic minority used less illness-related sources, these sources relied more on evidence-based medicine compared to the ethnic majority. Because of this, medication adherence was also slightly higher for the ethnic minority compared to the majority. Therefore, these findings indicate trust in medical authorities, their decisions, and recommendations. There was a statistically significant relationship between general and illness-related information-seeking activity; however, medication adherence was not related to information-seeking activity. The research outlines that in addition to ethnolinguistic aspect, also potential cultural influence might determine the trust in medicine and medication adherence.

Phytochemical and Pharmacological Research in Agrimonia eupatoria L. Herb Extract with Anti-Inflammatory and Hepatoprotective Properties.

The most promising plant from the genus Agrimony (Agrimonia L.) of the Rosaceae family for use in medical practice is Agrimonia eupatoria L. Phytochemical and pharmacological research in Agrimonia eupatoria L. herb extract, obtained with using 40% ethanol solution as an extractant were carried out. A total of 11 free and 17 bound monosaccharides, 17 amino acids were found in the studied extract, 9 of which are essential. Gallic and ellagic acids, gallocatechin, epigallocatechin, catechin, epicatechin, and epicatechin gallate were identified in the extract of A. eupatoria by the HPLC method; as well as hydroxycinnamic acids: hydroxyphenylacetate, caffeic, syringic, p-coumaric, ferulic, sinapic, cinnamic and quinic acid; flavonoids: quercetin-3-D-glucoside (isoquercitrin), neohesperidin, naringenin, luteolin were found, and their quantitative content was determined, as well by spectrophotometric methods. The herb extract of A. eupatoria belongs to practically non-toxic substances and has pronounced anti-inflammatory (at a dose of 10.0 mg/kg anti-exudative activity reached a maximum in 5 h (88.17%)) and hepatoprotective activity (at a dose of 25 mg/kg it reduce AlAt level by 1.1 and 1.2 times, respectively; AsAt by 1.2 and 1.1 times, respectively), reduces the level of lipid peroxidation and stabilizes the membrane structures of liver cells. Thus, the herb extract of A. eupatoria is a promising substance for the creation of phytomedicines with anti-inflammatory and hepatoprotective activity.

Arctostaphylos uva-ursi L. leaves extract and its modified cysteine preparation for the management of insulin resistance: chemical analysis and bioactivity.

Bearberry (Arctostaphylos uva-ursi L.) is a perennial plant of the heather family (Ericaceae). The leaves are dominated by arbutin, phenol carbonic acids flavonoids, saponins, etc. It was previously shown that the bearberry leaves extract reduced blood glucose level in healthy animals under glucose overload, so it need to be studied more detail. The aim of the study was to investigate the chemical composition and the effect of dry alcohol extract from bearberry leaves, which enriched with cysteine, on the rats pancreas under experimental dexamethasone-induced insulin resistance (IR). Arctostaphylos uva-ursi L. leaves extract and its modified cysteine preparation were obtained according to the developed method with 50% ethanol solution. Their phytochemical profile, hypoglycaemic and pancreatic protective effect were investigated. Phenologlycoside (arbutin), phenolic carboxylic acid (gallic acid), 5 flavonoids and 4 hydroxycinnamic acids were identified and quantified in the extracts by HPLC. Present data revealed that bearberry leaves alcoholic dry extract enriched with cysteine has a hypoglycaemic and pancreatic protective effect in treated animals under dexamethasone-induced IR model. Treatment improved hyperglycaemia, insulin resistance and beta cell reduction induced by dexamethasone injections.

Comparative Analyses of Bioactive Compounds in Inonotus obliquus Conks Growing on Alnus and Betula.

Inonotus obliquus grows in the Northern Hemisphere on some living broadleaved tree species as a pathogen, causing stem rot. In Estonia, the fungus is well known in the Betula species but can also be found on Alnus. Sterile conks of I. obliquus contain different bioactive compounds, but the quantitative and comparative research of these compounds in conks on different host species is limited. In the current work, I. obliquus was isolated and, evidently, determined from Alnus incana (L.) Moench., Alnus glutinosa (L.) Gaertn., and Betula pendula Roth, and the content of bioactive compounds in conks on these hosts were analysed. All the analysed conks sampled from A. incana and B. pendula contained betulin that varied from 111 to 159 µg/g. A significantly (p < 0.05) higher betulinic acid content was found in conks sampled from A. incana when compared with B. pendula: 474−635 and 20−132 µg/g, respectively. However, the conks from Betula were richer in total polyphenols, flavonols, and glucans. The content of inotodiol was quite similar in the conks from A. incana (7455−8961 µg/g) and B. pendula (7881−9057 µg/g). Also, no significant differences in the lanosterol content were found between the samples from these two tree species. To the best of our knowledge, this study is the first investigation of the chemical composition of I. obliquus parasitizing on Alnus. The results demonstrate that the bioactive compounds are promising in conks of I. obliquus growing not only on Betula but also on the Alnus species. It supports the opportunity to cultivate I. obliquus, also on the Alnus species, thus increasing the economic value of growing this tree species in forestry.