Chemical composition of Prunus padus L. flower extract and its anti-inflammatory activities in primary bone marrow-derived macrophages.

ETHNOPHARMACOLOGICAL RELEVANCE: Prunus padus L. has been traditionally used in European ethnomedicine as a treatment for internal and external purposes and is mainly used to reduce inflammation, pain and fever. The activities of P. padus flower extracts are not well characterized, and additional experimental studies at the molecular level are needed to confirm the ethnobotanical findings. AIM OF THE STUDY: To assess the potential of P. padus flower extract (PPFE) as a source of bioactive compounds through the characterization of its chemical composition and antioxidant, anti-collagenase, and anti-inflammatory activities. MATERIALS AND METHODS: The ethanolic extract (1:10 w/v in ethanol solution) from P. padus flowers was subjected to phytochemical analysis and evaluation of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity. Anti-collagenase activity was determined using a spectrophotometric method in vitro. The effect of PPFE on inflammation was evaluated by measuring specific markers using flow cytometry and assessing pro-inflammatory cytokine (IL-6) release by bone marrow-derived macrophages (BMDMs) ex vivo. RESULTS: The major components of the ethanolic extract of P. padus flowers were quercetin diglycosides, chlorogenic acid and N',N″-dicaffeoyl,N‴-coumaroyl spermidine. The total phenolic content of PPFE was 85.19 mg GAE/g extract, and the EC50 value in the DPPH assay was 0.55 mg/ml. PPFE exhibited the ability to inhibit collagenase activity in a dose-dependent manner. Preincubation of BMDMs with PPFE reduced the population of M1 (pro-inflammatory) and increased the population of M2 (anti-inflammatory) macrophages. Furthermore, PPFE decreased pro-inflammatory cytokine IL-6 release from BMDMs. CONCLUSIONS: PPFE is a rich source of bioactive compounds and possesses considerable anti-inflammatory properties, supporting its use in ethnomedicine for the reduction of inflammatory processes.

Data on medicinal plants in the records of Latvian folk medicine from the 19th century.

The data presented in this article is in support of the research paper "Medicinal plants and their uses recorded in the Archives of Latvian Folklore from the 19th century" [1]. This article provides the list of plant species and disorders treated with medicinal plants mentioned in the records of Latvian folk medicine and used by indigenous people of Latvia in the 19th century. In total, the data include 211 genera belonging to 71 plant families. The accepted scientific names of plant species, plant parts used, dosage forms of herbal medicines, and routes of administration are reported in the table. Plant uses are grouped into one of the 17 categories based on the body systems and psychological and social problems. The frequency of citations is indicated for each use of medicinal plant.

Medicinal plants and their uses recorded in the Archives of Latvian Folklore from the 19th century.

ETHNOPHARMACOLOGICAL RELEVANCE: The records of folk medicine present historical evidence of medicinal plant usage in the territory of Latvia and describe native and imported plants and plant products that were used as medicine. AIM OF THE STUDY: To collect and analyse the ethnobotanical knowledge found in records of Latvian folk medicine available in the Archives of Latvian Folklore. MATERIALS AND METHODS: Following the International Classification of Primary Care, plant uses were grouped into one of the 17 categories based on the body systems and psychological and social problems. Each plant was identified by its scientific name according to The Plant List website. Additionally, the plant parts used, dosage forms of herbal medicines and routes of administration were analysed. RESULTS: In total, 211 genera belonging to 71 families were mentioned in the analysed materials. The most common health conditions were digestive system disorders, respiratory system disorders and skin disorders. The plant families with the largest number of taxa were Asteraceae, Rosaceae, Lamiaceae, and Apiaceae. The most frequently mentioned native plant taxa were Achillea millefolium L., Matricaria chamomilla L., Allium cepa L., Artemisia absinthium L., and Plantago sp. L. Leaves and flowers were the most commonly used parts, and herbal tea was the most common dosage form. Only 59 out of 211 taxa mentioned in this study are included in the official herbal monographs of the European Medicines Agency. CONCLUSIONS: One hundred and fifty-two plant taxa mentioned in the records of Latvian folk medicine are not included in the European Union herbal monographs providing scientific information on the safety and efficacy and deserve further exploration as traditional herbal medicines.

Contribution of Molecular Structure to Self-Assembling and Biological Properties of Bifunctional Lipid-Like 4-(N-Alkylpyridinium)-1,4-Dihydropyridines.

The design of nanoparticle delivery materials possessing biological activities is an attractive strategy for the development of various therapies. In this study, 11 cationic amphiphilic 4-(N-alkylpyridinium)-1,4-dihydropyridine (1,4-DHP) derivatives differing in alkyl chain length and propargyl moiety/ties number and position were selected for the study of their self-assembling properties, evaluation of their cytotoxicity in vitro and toxicity on microorganisms, and the characterisation of their interaction with phospholipids. These lipid-like 1,4-DHPs have been earlier proposed as promising nanocarriers for DNA delivery. We have revealed that the mean diameter of freshly prepared nanoparticles varied from 58 to 513 nm, depending upon the 4-(N-alkylpyridinium)-1,4-DHP structure. Additionally, we have confirmed that only nanoparticles formed by 4-(N-dodecylpyridinium)-1,4-DHP derivatives 3 and 6, and by 4-(N-hexadecylpyridinium)-1,4-DHP derivatives 10 and 11 were stable after two weeks of storage. The nanoparticles of these compounds were found to be homogenous in size distribution, ranging from 124 to 221 nm. The polydispersity index (PDI) values of 1,4-DHPs samples 3, 6, 10, and 11 were in the range of 0.10 to 0.37. We also demonstrated that the nanoparticles formed by 4-(N-dodecylpyridinium)-1,4-DHP derivatives 3, 6, and 9, and 4-(N-hexadecylpyridinium)-1,4-DHP derivatives 10 and 11 had zeta-potentials from +26.07 mV (compound 6) to +62.80 mV (compound 11), indicating a strongly positive surface charge and confirming the relative electrostatic stability of these nanoparticle solutions. Transmission electron microscopy (TEM) images of nanoaggregates formed by 1,4-DHPs 3 and 11 confirmed liposome-like structures with diameters around 70 to 170 nm. The critical aggregation concentration (CAC) value interval for 4-(N-alkylpyridinium)-1,4-DHP was from 7.6 µM (compound 11) to 43.3 µM (compound 6). The tested 4-(N-alkylpyridinium)-1,4-DHP derivatives were able to quench the fluorescence of the binary 1,6-diphenyl-1,3,5-hexatriene (DPH)-1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) system, demonstrating hydrophobic interactions of 1,4-DHPs with phospholipids. Thus, 4-(N-dodecylpyridinium)-1,4-DHP derivative 3 quenched the fluorescence of the DPH⁻DPPC system more efficiently than the other 4-(N-alkylpyridinium)-1,4-DHP derivatives. Likewise the compound 3, also 4-(N-dodecylpyridinium)-1,4-DHP derivative 9 interacted with the phospholipids. Moreover, we have established that increasing the length of the alkyl chain at the quaternised nitrogen of the 4-(N-alkylpyridinium)-1,4-DHP molecule or the introduction of propargyl moieties in the 1,4-DHP molecule significantly influences the cytotoxicity on HT-1080 (human fibrosarcoma) and MH-22A (mouse hepatocarcinoma) cell lines, as well as the estimated basal cytotoxicity. Additionally, it was demonstrated that the toxicity of the 4-(N-alkylpyridinium)-1,4-DHP derivatives on the Gram-positive and Gram-negative bacteria species and eukaryotic microorganism depended on the presence of the alkyl chain length at the N-alkyl pyridinium moiety, as well as the number of propargyl groups. These lipid-like compounds may be proposed for the further development of drug formulations to be used in cancer treatment.

Acute anti-hyperglycaemic effects of an unripe apple preparation containing phlorizin in healthy volunteers: a preliminary study.

BACKGROUND: The health-promoting properties of apples are directly related to the biologically active compounds that they contain, such as polyphenols. The objective of this study was to prepare a low-sugar, fibre- and phlorizin-enriched powder from unripe apples and to gain insight regarding its anti-hyperglycaemic activity in healthy volunteers. RESULTS: The unripe apples (Malus domestica Borkh.) were collected 30 days after the full bloom day; blanched and pressed to obtain apple pomace which was then processed with a food cutter, oven-dried and milled to prepare apple powder. The concentrations of total sugars, water-soluble pectin and phlorizin in the apple preparation were 153.44 ± 2.46, 27.73 ± 0.51 and 12.61 ± 0.15 g kg(-1), respectively. Acute ingestion of the apple preparation improved glucose metabolism in the oral glucose tolerance test (OGTT) in six healthy volunteers by reducing the postprandial glucose response at 15 to 30 min by approximately two-fold (P < 0.05) and by increasing urinary glucose excretion during the 2- to 4-h interval of the OGTT by five-fold (P < 0.05). CONCLUSION: The results obtained indicate that the dried and powdered pomace of unripe apples can be used as a health-promoting natural product for the reduction of postprandial glycaemia and to improve the health of patients with diabetes.

Bioactive 1,4-dihydroisonicotinic acid derivatives prevent oxidative damage of liver cells.

1,4-Dihydroisonicotinic acid derivatives (1,4-DHINA) are compounds closely related to derivatives of 1,4-dihydropyridine, a well-known calcium channel antagonists. 1,4-DHINA we used were derived from a well-known antioxidant Diludin. Although some compounds have neuromodulatory or antimutagenic properties, their activity mechanisms are not well known. This study was performed to obtain data on antioxidant and bioprotective activities of: 2,6-dimethyl-3,5-diethoxycarbonyl-1,4-dihydroisonicotinic acid (Ia); sodium 2-(2,6-dimethyl-3,5-diethoxycarbonyl-1,4-dihydropyridine-4-carboxamido)glutamate (Ib) and sodium 2-(2,6-dimethyl-3,5-diethoxycarbonyl-1,4-dihydropyridine-4-carboxamido)ethane-sulphate (Ic). 1,4-DHINA's activities were studied in comparison to Trolox by: N,N-Diphenyl-N'-picrylhydrazyl (DPPH*), deoxyribose degradation, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) radical scavenging and antioxidative capacity assays; copper-induced lipid peroxidation of cultured rat liver cells (malondialdehyde determination by high performance liquid chromatography and 4-hydroxynonenal-protein conjugates by dot-blot); (3)H-thymidine incorporation and trypan blue assay for liver cells growth and viability. In all assays used Ia was the most potent antioxidant. Ia was also a potent antioxidant at non-toxic concentrations for liver cell cultures. It completely abolished, while Ic only slightly decreased copper-induced lipid peroxidation of liver cells. Thus, antioxidant capacities are important activity principle of Ia, which was even superior to Trolox in the cell cultures used, while activity principles of Ic and Ib remain yet to be determined.