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Artemisia cina Berg ex Poljakov, a shrubby plant endemic to the semi-arid areas of Kazakhstan, has as a long history of being used in traditional medicines as an antitumour, antifungal and anthelmintic agent. In a preliminary study carried out on different methodologies to produce aqueous extracts of A. cina it was seen that a simple aqueous extract of A. cina (as in an infusion of the plant) had the strongest anti-SARS-CoV-2 activity. The profiling of this aqueous extract was performed using Liquid Chromatography-Electrospray Ionization-Quadrupole-Time-of-Flight Mass Spectrometry (LC-ESI-Q-TOF-MS) while High-Speed Countercurrent Chromatography (HSCCC) and a Sephadex LH-20 column were utilised to isolate and purify the extract in ethyl acetate obtained from the aqueous extract. Nuclear Magnetic Resonance (NMR) was used for structural elucidation. The flavonoid spinacetin-7-O-glucoside was found to be one of the main compounds present in the A. cina aqueous extract. With the emergence of the COVID-19 pandemic and the frequency in which new COVID strains occur, the demand for drugs with anti-SARS-CoV-2 activity is at an all-time high. Flavonoids and artemisinin identified by LC-MS in this extract are hypothesised to be the key compounds behind the anti-SARS-CoV-2 activity of the aqueous extract, however this needs to be further tested and explored.

IntroductionHelicobacter pylori infection is a major issue worldwide, with widespread prevalence, combined with its link to gastritis, peptic ulcers, gastric cancer, and mucosa-associated lymphoid tissue (MALT) lymphoma. Meanwhile, effectiveness of current treatment protocols is limited by increasing antibiotic resistance and patient compliance issues due to long regimens and side effects. Plukenetia volubilis, or sacha inchi, is a valuable source of bioactive molecules. However, studies on its antimicrobial activity, especially against H. pylori, are lacking.MethodsIn this study, the anti-H. pylori activity of P. volubilis leaves water extract was explored using in vitro and in silico approaches. High-Performance Liquid Chromatography coupled to Electrospray Ionisation and Quadrupole Time-of-Flight Mass Spectrometry (HPLC-ESI- QTOF-MS-MS) analysis of the water extract from the leaves was used to characterise the chemical composition of the plant and allowed identification of some flavonoids, such as astragalin, and some phenolic compounds. Then, high-speed counter current chromatography (HSCCC) was used to fractionate the ethyl acetate partition obtained from the water extract from the leaves.Results and DiscussionThe presence of flavonoids derived from kaempferol was confirmed and astragalin was isolated for the first time in P. volubilis. The P. volubilis water infusion, ethyl acetate extract and the isolated astragalin exhibited anti-bacterial activity against H. pylori J99 and two clinical isolates (e.g., minimum inhibitory concentrations of 0.53, 0.51 and 0.49 μg/mL, respectively, for clarithromycin-resistant clinical isolate SSR366). Then, using molecular docking for potential protein targets for H. pylori, it was verified that astragalin could interact with these proteins by in silico analysis.ConclusionThese findings highlight that P. volubilis and astragalin produce a bacteriostatic activity against H. pylori and may have potential to be used in treatment against H. pylori, after further research.

Adonis tianschanica is a lesser-known plant species belonging to the genus Adonis that grows in Kazakhstan. The aim of this study was to characterize the composition of the ethanolic, water, and hydroethanolic extracts from the aerial parts of A. tianschanica by HPLC-ESI-QTOF-MS/MS to isolate the major compound isoquercitrin by HSCCC (High-Speed Counter-Current Chromatography) and to determine the cytotoxicity and anti-inflammatory potential of the extracts produced with this plant. Fingerprinting of the analyzed extracts showed the presence of a multitude of metabolites comprising polyphenols, organic acids, and coumarins, and only trace quantities of cardiac glycosides in the analyzed samples. Flavonoids were certainly the best-represented group, with kaempferol, quercetin, and their derivatives as the major components of the extracts. Key findings in this paper were that the ethanol: water (50:50 v/v) extract of A. tianschanica and its major compound isoquercitrin were able to reduce the production of NO induced by LPS, in addition to demonstrating anti-inflammatory effects by reducing cytokines such as IL-6, TNF-α, and IL-1β.

Selected phenotypes of dried maca (Lepidium peruvianum) hypocotyls and supercritical CO2 extract (USPlus®) of saw palmetto (Serenoa repens) were used to determine their targeted, cytotoxic action in prostate cancer cells. Fingerprinting by HPLC-MS and PCA analysis showed compositional differences in glucosinolates, amides, macamides, and other alkaloids, which varied based on the color and the size of hypocotyls. These phytochemical differences translated into a higher antioxidant potential of red maca than black maca samples. The greatest COX-2 inhibition was demonstrated with a combination of red maca: saw palmetto (67%:33%) and red maca: saw palmetto: black maca (25%:50%:25%). The LNCaP androgen-dependent prostate cancer cell line was the most sensitive to the three-component mixture of black, red maca, and saw palmetto treatment. This combination provided the most abundant set of high-activity metabolites, and is worthy of consideration in further clinical applications and future in-depth study.

The genus Vaccinium is represented by shrubs growing in a temperate climate that have been used for ages as traditional remedies in the treatment of digestive problems, in diabetes, renal stones or as antiseptics due to the presence of polyphenols (anthocyanins, flavonoids and tannins) in their fruits and leaves. Recent studies confirm their marked potential in the treatment of skin disorders and as skin care cosmetics. The aim of this review is to present the role of Vaccinium spp. as cosmetic products, highlight their potential and prove the biological properties exerted by the extracts from different species that can be useful for the preparation of innovative cosmetics. In the manuscript both skin care and therapeutic applications of the representatives of this gender will be discussed that include the antioxidant, skin lightening, UV-protective, antimicrobial, anti-inflammatory, and chemopreventive properties to shed new light on these underestimated plants.

Moringa oleifera Lam. (Moringaceae) is a species of tree with an increasing utility, occurring naturally mainly in Pakistan and northern India. M. oleifera is currently cultivated in Africa, South America, Asia and the Middle East. The usage of its leaves, seed oil, bark, fruits, flowers and roots has positive opinions of FDA (American Food and Drug Administration), EFSA (European Food Safety Authority) and CosIng (Cosmetic Ingredients database). The chemical composition of M. oleifera is dominated by: proteins (consisting mainly of amino acids such as arginine or serine), fatty acids (omega-3 and omega-6), vitamins (vitamin A, B and C and tocopherols), mineral salts (including several bioelements, such as calcium, magnesium, sodium, and potassium), valuable polyphenolic compounds from the group of phenolic acids (e.g., gallic acid, ferulic acid) and flavonoids (e.g., myricetin, rutoside, and kaempferol). The raw materials show antioxidant, hepatoprotective, anti-inflammatory and antimicrobial properties. Dietary supplements and alimentary products containing M. oleifera are recommended as health-promoting and “novel food” preparations. The main purpose of this work was a review of the latest scientific literature on M. oleifera, with particular emphasis on the studies focusing on its chemical composition, biological activity and safety. Moreover, the review tends to discuss the results of biotechnological studies using this material and the agronomical significance.

Fucoxanthin (FX) is a carotenoid of marine origin primarily distributed in brown seaweeds and has garnered interest for its antioxidative, anti-inflammatory, and anticancer properties. Despite its potential, a comprehensive understanding of its anticancer effects and mechanisms of action remains elusive.The aim of this review is to present novel insights into the anticancer effects of FX, shedding light on previously unexplored molecular mechanisms and its synergistic potential with established chemotherapeutic agents.A comprehensive search was conducted employing databases like PubMed/MedLine, Scopus, and Web of Science to aggregate relevant pharmacological experimental studies. The results of the studies showed that FX exhibits anticancer activity against various cancer types, including breast, colorectal, and lung cancer, through multiple pathways: cell cycle arrest, apoptosis induction, and inhibition of angiogenesis. Additionally, FX potentiates the effects of existing chemotherapeutic agents, making it a potential candidate for combination therapies. The evidence suggests that FX possesses considerable anticancer properties, acting through diverse molecular mechanisms; the heterogeneity of study designs and the limited number of clinical trials make it hard to conclude. Further in-depth studies, particularly randomized controlled trials, are essential for validating FX's efficacy and for paving the way for its integration into standard cancer treatment regimens; additional research is needed to explore its pharmacokinetics, safety profile, and potential synergistic effects with existing chemotherapeutics.

Abstract Β-asarone is a phenylpropane derivative present in the rhizomes of Acorus calamus, that was proved to exhibit toxic effects in humans. Because of its presence the whole plant that is commonly used in traditional medicine for its sedative, anti-inflammatory, neuroprotective and other properties has limited application nowadays. In the study, qualitative and quantitative analysis of a collection of nine essential oil (EO) samples of European and Asian origin was performed. The final content of β-asarone in the tested samples ranged between 0.265 and 1.885 mg/mL. Having in mind a possible application of the EO as a biopesticide, this research aimed at the development of CPC-based purification protocol that could help remove β-asarone from EO. It was proved that the biphasic solvent system composed of n-hexane/EtOAc/MeOH/water, 9:1:9:1 (v/v/v/v) was capable of the removal of the toxic constituent in the CPC chromatograph operated in the ascending elution mode with 2200 rpm and a flow rate of 5 mL/min. The chromatographic analysis that lasted only 144 min effectively separated β-asarone (purity of 95.5%) and α-asarone (purity of 93.7%) directly from the crude Acorus calamus rhizome EO.

Abstract Desmodium adscendens (Sw.) DC. is a plant of the Fabaceae family especially rich in flavonoids but also in alkaloids, terpenoids, steroids, phenols, phenylpropanoids, glycosides, and volatiles. This herb has been traditionally used in numerous countries all over the world for its pharmacological and biological properties (i.e., it has been used for the treatment of diarrheas, fever, epilepsy, asthma, leishmaniasis, gastroduodenal ulcer, diabetes, hepatic diseases, etc.). Given the wide uses of D. adscendens, this review summarizes all recent data on D. adscendens evaluating its phytochemistry as well as its ethno‐traditional and pharmacological properties. In addition, an association between the phytocompounds of this plant and its potential mechanism of action in cell and animal models has been investigated, focusing with a special emphasis on human experiments.

Introduction:Capparis cartilaginea Decne. (CC) originates from the dry regions of Asia and the Mediterranean basin. In traditional medicine, tea of CC leaves is commonly used to treat inflammatory conditions such as rheumatism, arthritis, and gout. Due to the limited studies on the phytochemistry and biological activity of CC compared to other members of the Capparaceae family, this work aims to: 1) Identify the chemical composition of CC extract and 2) Investigate the potential anti-inflammatory effect of CC extract, tea and the isolated compounds.Methods: To guarantee aim 1, high-speed countercurrent chromatography (HSCC) method; Nuclear Magnetic Resonance (NMR) and High-Performance Liquid Chromatography coupled to Electrospray Ionisation and Quadrupole Time-of-Flight Mass Spectrometry (HPLC-ESIQTOF-MS/MS) were employed for this purpose. To guarantee aim 2, we studied the effect of the isolated flavonoids on matrix metalloproteinases (MMPs) −9 and −2 in murine macrophages. Molecular docking was initially performed to assess the binding affinity of the isolated flavonoids to the active site of MMP-9.Results and discussion:In silico model was a powerful tool to predict the compounds that could strongly bind and inhibit MMPs. CC extract and tea have shown to possess a significant antioxidant and anti-inflammatory effect, which can partially explain their traditional medicinal use.

Traditionally, selected plant sources have been explored for medicines to treat convulsions. This continues today, especially in countries with low-income rates and poor medical systems. However, in the low-income countries, plant extracts and isolated drugs are in high demand due to their good safety profiles. Preclinical studies on animal models of seizures/epilepsy have revealed the anticonvulsant and/or antiepileptogenic properties of, at least some, herb preparations or plant metabolites. Still, there is a significant number of plants known in traditional medicine that exert anticonvulsant activity but have not been evaluated on animal models. Zebrafish is recognized as a suitable in vivo model of epilepsy research and is increasingly used as a screening platform. In this review, the results of selected preclinical studies are summarized to provide credible information for the future development of effective screening methods for plant-derived antiseizure/antiepileptic therapeutics using zebrafish models. We compared zebrafish vs. rodent data to show the translational value of the former in epilepsy research. We also surveyed caveats in methodology. Finally, we proposed a pipeline for screening new anticonvulsant plant-derived drugs in zebrafish (“from tank to bedside and back again”).

Fermentation is used not only to preserve food but also to enhance its beneficial effects on human health and achieve functional foods. This study aimed to investigate how different treatments (spontaneous fermentation or fermentation with the use of starter culture) affect phenolic content, antioxidant potential, and cholinesterase inhibitory activity in different kale cultivars: ‘Halbhoner Grüner Krauser’, ‘Scarlet’, and ‘Nero di Toscana’. Chosen samples were further tested for their protective potential against the Caco-2 cell line. HPLC-MS analysis revealed that the fermentation affected the composition of polyphenolic compounds, leading to an increase in the content of rutin, kaempferol, sinapinic, and protocatechuic acids. In general, kale cultivars demonstrated various antioxidant activities, and fermentation led to an increase in total phenolic content and antioxidant activity. Fermentation boosted anti-cholinesterase activity most profoundly in ‘Nero di Toscana’. Extracts of spontaneously fermented ‘Scarlet’ (SS) and ‘Nero di Toscana’ (NTS) showed cytoprotective properties, as revealed by the malondialdehyde (MDA), lactate dehydrogenase (LDH), superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) assays. Additionally, strong anti-inflammatory activity of NTS was shown by decreased release of cytokines IL-1β and TNF-α. Collectively, the conducted studies suggest fermented kale cultivars as a potential source for functional foods.

In recent years, an increasing interest in phytotherapy has been observed. Parallel to the research on the total extracts of plant material, numerous studies on the activity of single molecules derived from plants are being conducted to address their mechanisms of action and determine active doses and eventual interactions. Despite this phenomenon, the isolation of individual compounds is a bottleneck due to its difficulty and cost. This work presents the results of a careful optimization of magnoflorine and berberine (isoquinoline alkaloids) recovery from a commonly distributed shrub, Berberis vulgaris, growing in Poland and Georgia, using CPC. Both compounds are known for their numerous medicinal properties, which makes the isolation methodology an important area of research. Additionally, CPC has the ability to isolate high-quality compounds in large quantities, which makes it an effective and easy-to-commercialize method. For a successful separation, the biphasic solvent system composed of hexane, butanol, ethanol, and water in a ratio (3:12:4:16 v/v/v/v) was used in the ascending mode, together with the flow rate of 8 mL/min and rotation speed of 1600 rpm. The method was selective for both compounds, and it delivered good results for both root and stem extracts from the plant. The qualitative composition of alkaloids in the studied extracts determined by HPLC-ESI-QTOF-MS/MS confirmed the presence of berberine, magnoflorine, jatrorhizine, and palmatine alkaloids from the group of isoquinolines. The isolates, magnoflorine and berberine, were subjected to the Helicobacter pylori growth inhibition assay and urease inhibition test to assess whether, next to the previously proved anticancer properties, these compounds are characterized by H. pylori inhibition. MGN was found to exhibit inhibitory potential against urease (IC50 = 25 mg/L).

Fruit peels might be a valuable source of active ingredients for cosmetics, leading to more sustainable usage of plant by-products. The aim of the study was to evaluate the phytochemical content and selected biological properties of hydroglycolic extracts from peels and pulps of Annona cherimola, Diospyros kaki, Cydonia oblonga, and Fortunella margarita as potential cosmetic ingredients. Peel and pulp extracts were compared for their antiradical activity (using DPPH and ABTS radical scavenging assays), skin-lightening potential (tyrosinase inhibitory assay), sun protection factor (SPF), and cytotoxicity toward human fibroblast, keratinocyte, and melanoma cell lines. The total content of polyphenols and/or flavonoids was significantly higher in peel than in pulp extracts, and the composition of particular active compounds was also markedly different. The HPLC-MS fingerprinting revealed the presence of catechin, epicatechin and rutoside in the peel of D. kaki, whereas kaempferol glucoside and procyanidin A were present only in the pulp. In A. cherimola, catechin, epicatechin and rutoside were identified only in the peel of the fruit, whereas procyanidins were traced only in the pulp extracts. Quercetin and luteolinidin were found to be characteristic compounds of F. margarita peel extract. Naringenin and hesperidin were found only in the pulp of F. margarita. The most significant compositional variety between the peel and pulp extracts was observed for C. oblonga: Peel extracts contained a higher number of active components (e.g., vicenin-2, kaempferol rutinoside, or kaempferol galactoside) than pulp extract. The radical scavenging potential of peel extracts was higher than of the pulp extracts. D. kaki and F. margarita peel and pulp extracts inhibited mushroom and murine tyrosinases at comparable levels. The C. oblonga pulp extract was a more potent mushroom tyrosinase inhibitor than the peel extract. Peel extract of A. cherimola inhibited mushroom tyrosinase but activated the murine enzyme. F. margarita pulp and peel extracts showed the highest in vitro SPF. A. cherimola, D. kaki, and F. margarita extracts were not cytotoxic for fibroblasts and keratinocytes up to a concentration of 2% (v/v) and the peel extracts were cytotoxic for A375 melanoma cells. To summarize, peel extracts from all analyzed fruit showed comparable or better cosmetic-related properties than pulp extracts and might be considered multifunctional active ingredients of skin lightening, anti-aging, and protective cosmetics.

Gentiopicroside (GPS) is a leading component of several plant species from the Gentianaceae botanical family. As a compound with plenty of biological activities and a component of herbal drugs, GPS has an important role in the regulation of physiological processes in humans. The results of recently published scientific studies underline a meaningful role of this molecule as an active factor in metabolic pathways and mechanisms, which may have an influence in the treatment of different diseases, including digestive tract disorders, malignant changes, neurological disorders, microbial infections, bone formation disorders, inflammatory conditions, and others. This review aims to collect previously published reports on the biological properties of GPS as a single compound that were confirmed by in vitro and in vivo studies, and to draw attention to the newly discovered role of this bitter-tasting secoiridoid. Thanks to these properties, the research on this substance could be revisited.

Ginger (Zingiber officinale Rosc.) is a plant known all over the world that is used as a spice and as an ingredient in drinks, dietary supplements, and cosmetics. The growing availability of its fresh rhizomes makes it even more likely to be used in the diet, mainly due to its beneficial health properties and high content of polyphenols (gingerols and shogaols). The main goal and motivation of the authors was to assess the bioavailability of active substances contained in the extract from ginger rhizomes in the presence of various types of diets using the in vitro digestion method, enabling simulation of the processes occurring during the digestion and absorption of metabolites in the small intestine. For the qualitative and quantitative analyses, the HPLC-MS (High Performance Liquid Chromatography–Mass Spectrometry) and HPLC (High Performance Liquid Chromatography) techniques were used, respectively. Based on the obtained results, it was found that the best bioavailability of the selected ginger polyphenols (6-gingerol, 8-gingerdione, 8-shogaol, and 10-gingerdione) was estimated for a high-fiber diet, while the weakest results were obtained for standard and basic diets. In the case of the high-fiber diet, the bioavailability of the mentioned compounds was estimated as 33.3, 21.4, 6.73, and 21.0%, while for the basic diet, it was only 21.3, 5.3, 2.0, and 1.0%, respectively.

Emodin-8-O-glucoside (E-8-O-G) is a glycosylated derivative of emodin that exhibits numerous biological activities, including immunomodulatory, anti-inflammatory, antioxidant, hepatoprotective, or anticancer activities. However, there are no reports on the activity of E-8-O-G against cancers of the nervous system. Therefore, the aim of the study was to investigate the antiproliferative and cytotoxic effect of E-8-O-G in the SK-N-AS neuroblastoma, T98G human glioblastoma, and C6 mouse glioblastoma cancer cells. As a source of E-8-O-G the methanolic extract from the aerial parts of Reynoutria japonica Houtt. (Polygonaceae) was used. Thanks to the application of centrifugal partition chromatography (CPC) operated in the descending mode using a mixture of petroleum ether:ethyl acetate:methanol:water (4:5:4:5 v/v/v/v) and a subsequent purification with preparative HPLC, E-8-O-G was obtained in high purity in a sufficient quantity for the bioactivity tests. Assessment of the cancer cell viability and proliferation were performed with the MTT (3-(bromide 4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium), CTG (CellTiter-Glo®) and BrdU (5-bromo-2′-deoxyuridine) assays, respectively. E-8-O-G inhibits the viability and proliferation of SK-N-AS neuroblastoma, T98G human glioblastoma multiforme, and C6 mouse glioblastoma cells dose-dependently. E-8-O-G seems to be a promising natural antitumor compound in the therapy of nervous system tumors.

This article presents the results of studies investigating the effect of red kale (Brassica oleracea L. ssp. acephala L. var. sabellica) extract on cancer cells (HT-29). The cytotoxicity of the red kale extract was assessed using MTT and LDH assays, while qRT-PCR was employed to analyze the expression of genes associated with the p53 signaling pathway to elucidate the effect of the extract on cancer cells. Furthermore, HPLC-ESI-QTOF-MS/MS was applied to identify bioactive compounds present in red kale. The obtained results indicated that red kale extract reduced the viability and suppressed the proliferation of HT-29 cells (the IC50 value of 60.8 µg/mL). Additionally, mRNA expression analysis revealed significant upregulation of several genes, i.e., casp9, mapk10, mapk11, fas, kat2 b, and ubd, suggesting the induction of cell apoptosis through the caspase-dependent pathway. Interestingly, the study revealed a decrease in the expression of genes including cdk2 and cdk4 encoding cell cycle-related proteins, which may lead to cell cycle arrest. Furthermore, the study identified certain bioactive compounds, such as sinigrin, spirostanol, hesperetin and usambarensine, which could potentially contribute to the apoptotic effect of red kale extracts. However, further investigations are necessary to elucidate the specific role of these individual compounds in the anti-cancer process.

The acetylcholinesterase-inhibitory potential of the oleanane-type triterpenes and their glycosides from thebark of Terminalia arjuna (Combreatceae), i.e.,arjunic acid, arjunolic acid, arjungenin, arjunglucoside I, sericic acid and arjunetin, is presented. The studies are based on in silico pharmacokinetic and biomimetic studies, acetylcholinesterase (AChE)-inhibitory activity tests and molecular-docking research. Based on the calculated pharmacokinetic parameters, arjunetin and arjunglucoside I are indicated as able to cross the blood–brain barrier. The compounds of interest exhibit a marked acetylcholinesterase inhibitory potential, which was tested in the TLC bioautography test. The longest time to reach brain equilibrium is observed for both the arjunic and arjunolic acids and the shortest one for arjunetin. All of the compounds exhibit a high and relatively similar magnitude of binding energies, varying from ca. −15 to −13 kcal/mol. The superposition of the most favorable positions of all ligands interacting with AChE is analyzed. The correlation between the experimentally determined IC50 values and the steric parameters of the molecules is investigated. The inhibition of the enzyme by the analyzed compounds shows their potential to be used as cognition-enhancing agents. For the most potent compound (arjunglucoside I; ARG), the kinetics of AChE inhibition were tested. The Michaelis–Menten constant (Km) for the hydrolysis of the acetylthiocholine iodide substrate was calculated to be 0.011 mM.

Oleanolic acid (OA), as a ubiquitous compound in the plant kingdom, is studied for both its neuroprotective and neurotoxic properties. The mechanism of acetylcholinesterase (AChE) inhibitory potential of OA is investigated using molecular dynamic simulations (MD) and docking as well as biomimetic tests. Moreover, the in vitro SH-SY5Y human neuroblastoma cells and the in vivo zebrafish model were used. The inhibitory potential towards the AChE enzyme is examined using the TLC-bioautography assay (the IC50 value is 9.22 μM). The CH-π interactions between the central fragment of the ligand molecule and the aromatic cluster created by the His440, Phe288, Phe290, Phe330, Phe331, Tyr121, Tyr334, Trp84, and Trp279 side chains are observed. The results of the in vitro tests using the SH-SY5Y cells indicate that the viability rate is reduced to 71.5%, 61%, and 43% at the concentrations of 100 µg/mL, 300 µg/mL, and 1000 µg/mL, respectively, after 48 h of incubation, whereas cytotoxicity against the tested cell line with the IC50 value is 714.32 ± 32.40 µg/mL. The in vivo tests on the zebrafish prove that there is no difference between the control and experimental groups regarding the mortality rate and morphology (p > 0.05).

Curcuma longa L. (Zingiberaceae), known as turmeric, is a perennial tuberous plant from the genus Curcuma, which includes about 100 plant species. The chemical composition of the turmeric rhizome is very diverse. Diarylheptanoid derivatives, also known as curcuminoids (of which curcumin, demethoxycurcumin and bisdemethoxycurcumin are the most important representatives), are the major active constituents of the plant rhizome. Many extracts used in the food and pharmaceutical industries are produced from thermally processed rhizome, when there are significant changes in the composition of the main compounds. Therefore, the aim of the study was to compare how the type of thermal treatment affects the content of curcuminoids and the antioxidant properties of the rhizome. The plant material was subjected to three different methods of thermal processing—microwave heating, boiling and frying in different time intervals. The chemical composition and antioxidant activity of the processed rhizome was evaluated using LC-MS (liquid chromatography–mass spectrometry), HPLC (high-performance liquid chromatography) and spectrophotometric methods (a DPPH test and TPC assay). Obtained results revealed that curcumin was the major curcuminoid present in all samples (113.92 mg/g of the fresh rhizome). Significant correlation between the type and time of the thermal processing and the composition of turmeric samples was revealed. A traditional boiling process lasting for 10 min was the most beneficial process in terms of the curcuminoid content (204 mg/g of curcumin) and antioxidant activity of the samples.

Achillea millefolium L. is one of the most known medicinal plants with a broad spectrum of applications in the treatment of inflammation, pain, microbial infections and gastrointestinal disorders. In recent years, the extracts from A. millefolium have also been applied in cosmetics with cleansing, moisturizing, shooting, conditioning and skin-lightening properties. The growing demand for naturally derived active substances, worsening environmental pollution and excessive use of natural resources are causing increased interest in the development of alternative methods for the production of plant-based ingredients. In vitro plant cultures are an eco-friendly tool for continuous production of desired plant metabolites, with increasing applicability in cosmetics and dietary supplements. The purpose of the study was to compare phytochemical composition and antioxidant and tyrosinase inhibitory properties of aqueous and hydroethanolic extracts from A. millefolium obtained from field conditions (AmL and AmH extracts) and in vitro cultures (AmIV extracts). In vitro microshoot cultures of A. millefolium were obtained directly from seeds and harvested following 3 weeks of culture. Extracts prepared in water, 50% ethanol and 96% ethanol were compared for the total polyphenolic content, phytochemical content using the ultra-high-performance liquid chromatography–quadrupole time-of-flight mass spectrometry (UHPLC-hr-qTOF/MS), antioxidant activity by DPPH scavenging assay and the influence on the activity of mushroom and murine tyrosinases. The phytochemical content of AmIV extracts was significantly different from AmL and AmH extracts. Most of the polyphenolic compounds identified in AmL and AmH extracts were present in AmIV extracts only in trace amounts and the major constituents presented in AmIV extracts were fatty acids. The total content of polyphenols in AmIV exceeded 0.25 mg GAE/g of dried extract, whereas AmL and AmH extracts contained from 0.46 ± 0.01 to 2.63 ± 0.11 mg GAE/g of dried extract, depending on the solvent used. The low content of polyphenols was most likely responsible for the low antioxidant activity of AmIV extracts (IC50 values in DPPH scavenging assay >400 µg/mL) and the lack of tyrosinase inhibitory properties. AmIV extracts increased the activity of mushroom tyrosinase and tyrosinase present in B16F10 murine melanoma cells, whereas AmL and AmH extracts showed significant inhibitory potential. The presented data indicated that microshoot cultures of A. millefolium require further experimental research before they can be implemented as a valuable raw material for the cosmetics industry.

Acetylcholinesterase inhibitors remain the mainstay of symptomatic treatment for Alzheimer’s disease. The natural world is rich in acetylcholinesterase inhibitory molecules, and research efforts to identify novel leads is ongoing. Cladonia portentosa, commonly known as reindeer lichen, is an abundant lichen species found in Irish Boglands. The methanol extract of Irish C. portentosa was identified as an acetylcholinesterase inhibitory lead using qualitative TLC-bioautography in a screening program. To identify the active components, the extract was deconvoluted using a successive extraction process with hexane, ethyl acetate and methanol to isolate the active fraction. The hexane extract demonstrated the highest inhibitory activity and was selected for further phytochemical investigations. Olivetolic acid, 4-O-methylolivetolcarboxylic acid, perlatolic acid and usnic acid were isolated and characterized using ESI-MS and two-dimensional NMR techniques. LC-MS analysis also determined the presence of the additional usnic acid derivatives, placodiolic and pseudoplacodiolic acids. Assays of the isolated components confirmed that the observed anticholinesterase activity of C. portentosa can be attributed to usnic acid (25% inhibition at 125 µM) and perlatolic acid (20% inhibition at 250 µM), which were both reported inhibitors. This is the first report of isolation of olivetolic and 4-O-methylolivetolcarboxylic acids and the identification of placodiolic and pseudoplacodiolic acids from C. portentosa.

Objectives: The objective of this study is to determine metabolomics changes in the blood of amenorrhea model rats treated with Shimshin-6, a traditional Mongolian medicine, and search the important biomarkers using the UHPLC/TOF MS platform. Methods: The influence of a traditional Mongolian Shimshin-6 preparation administered to rats with a dexamethasone induced amenorrhea model was assessed to evaluate the physiological changes and the drug's metabolites in biological samples. The metabolites responsible for the differentiation of metabolic profiles between the two groups were obtained based on a multivariate statistics variable importance in the projection (VIP) threshold of 1.0 from the PLS-DA model. The analyses were carried out using an UHPLC-TOF-MS platform. One-way analysis of variance (ANOVA) was applied to test the significance of differences between groups. Results: The metabolic pathways were identified through the online databases Metlin and HMDB. Metabolic pathways analysis found tryptophan metabolism, phenylalanine metabolism, D-Glutamine and D-glutamate metabolism, Sphingolipid metabolism, Ubiquinone and other terpenoid-quinone biosynthesis and Fatty acid biosynthesis were mainly enriched based on the differential metabolites in rats of AG. Some of these pathways were markedly altered, such as the Tryptophan metabolism and phenylalanine metabolism pathway. Conclusions: A variety of potential biomarkers of Shimshin-6 physiological activity have been identified in the tested samples. According to the results it could be clearly seen, that the administration of this traditional medication affected the metabolism of amino acids, fatty acids and energy, to improve the condition of the animals suffering from amenorrhea.

Surgical treatments and chemotherapy are the most commonly used methods of colorectal cancer treatment (CRC), unfortunately, these therapies have many side effects. Moreover, despite advances in primary and adjuvant treatments, the survival time in CRC patients is still unsatisfactory. Treatment options for patients with CRC continue to advance and recent research has shown that colorectal cancer is sensitive to plant-derived substances. The use of natural compounds contained in herbal extracts for the treatment of colon cancer or as adjunctive therapy for CRC gives patients a wide range of treatment options. In this study, we evaluate the potential toxicity of the Mongolian preparation – Gurgem-7 composed of Crocus sativus, Veronica officinalis, Capsella bursa-pastoris, Arctostaphylos uva-ursi, Calendula officinalis, Gentiana lutea, and Terminalia chebula. Therefore, the aim of this study was to determine its biological activities, biochemical and molecular features in vitro and composition analysis by HPLC-ESI-QTOF-MS/MS platform. We identified 18 metabolites and 8 of them were quantified. Majority of the secondary metabolites belonged to the group of phenolic constituents with taxifolin, chlorogenic acids’ family, hydroxysafflor yellow A and hydroxybenzoic acid as leading compounds. In turn, our in vitro results suggest that the preparation inhibits cell metabolic activity through oxidative stress, numerous DNA damage and cell cycle arrest. Simultaneously enzymatic and non-enzymatic cell protection mechanisms mediated by TP53/Keap1 and Nrf2/HO-1 pathways may be activated in a cell-specific manner in vitro. In conclusion, we provide preliminary molecular evidence of the toxic properties of Gurgem-7 preparation to Caco-2 and CT26. WT cells related to insufficient action of their repair and adaptive mechanisms to stress conditions.

Comparative analysis of flavonoids and phenolic acids composition, in plants of six species of Monarda from family Lamiaceae was carried out. The 70% (v/v) methanolic extracts of flowering herbs of Monarda citriodora Cerv. ex Lag., Monarda bradburiana L.C. Beck, Monarda didyma L., Monarda media Willd., Monarda fistulosa L. and Monarda punctata L. were analyzed for their polyphenol composition as well as antioxidant capacity and antimicrobial effect. Liquid chromatography-electrospray ionization-tandem mass spectrometry (HPLC–DAD–ESI-QTOF/MS/MS) was used to identify phenolic compounds. The in vitro antioxidant activity was assessed using a DPPH radical scavenging assay, while antimicrobial activity was measured by the broth microdilution method allowing for MIC (minimal inhibitory concentration) determination. The total polyphenol content (TPC) was assayed by the Folin–Ciocalteu method. The results showed the presence of eighteen different components including phenolic acids and flavonoids together with their derivatives. The presence of six constituents (gallic acid, hydroxybenzoic acid glucoside, ferulic acid, p-coumaric acid, luteolin-7-glucoside and apigenin-7-glucoside) was found to be dependent on the species. To differentiate the samples, the antioxidant activity of 70% (v/v) methanolic extracts was studied and expressed as a percent of DPPH radical inhibition and in EC50 values (mg/mL). The latter values were as follows: M. media (EC50 = 0.090 mg/mL), M. didyma (EC50 = 0.114 mg/mL), M. citriodora (EC50 = 0.139 mg/mL), M. bradburiana (EC50 = 0.141 mg/mL), M. punctata (EC50 = 0.150 mg/mL) and M. fistulosa (EC50 = 0.164 mg/mL). Moreover, all extracts indicated bactericidal activity against reference Gram-positive (MIC = 0.07–1.25 mg/mL) and Gram-negative bacteria (MIC = 0.63–10 mg/mL) as well as fungicidal effect towards yeasts (MIC = 1.25–10 mg/mL). Staphylococcus epidermidis and Micrococcus luteus were the most sensitive to them. All extracts showed promising antioxidant properties and noteworthy activity against the reference Gram-positive bacteria. Antimicrobial effect of the extracts against the reference Gram-negative bacteria as well as fungi (yeasts) from Candida spp. was slight. All extracts showed bactericidal and fungicidal effect. The obtained results indicated that the investigated extracts from Monarda spp. could be potential sources of natural antioxidants and antimicrobial agents, especially with activity towards Gram-positive bacteria. The differences in the composition and properties of the studied samples may influence the pharmacological effects of the studied species.

Ginger (Zingiber officinale Rosc.) is a spice, medicinal and cosmetic plant that has been known for centuries. It can be used in dried, fresh, marinated or candied form, and is also an essential ingredient in well-known curry blends. Ginger rhizomes are often freeze-dried as the first step in the preparation of the raw material. Many studies have proved that the composition and biological activity of ginger changes due to thermal processing. Therefore, the aim of the review was to summarize the scientific results on the impact of traditional and unconventional methods of the heat treatment of ginger rhizomes and their influence on the antioxidant and other selected biological activities of the plant. The review of the available scientific data is inconclusive, and it is hard to state unequivocally whether the thermal treatment of the raw material increases or decreases biological activity. Based on the presented literature review, it can be concluded that traditional cooking and microwave processing in general decrease the antioxidant activity of the ginger rhizome, whereas frying, autoclaving, blanching or traditional drying in the sun mostly lead to a significant increase in ginger activity. Interesting data were presented in the works describing the freeze-drying process during which the antioxidant potential of ginger increased.

Ziziphora species (Lamiaceae) have been used in traditional medicine as sedatives, antiseptics, carminatives, or expectorants. Despite their common applications in phytotherapy, there is still lack of evidence about the composition of their extracts and its impact on biological properties of the plants. The aim of this study was to evaluate the content of Ziziphora bungeana, a less studied species growing in Kazakhstan, using HPLC-ESI-QTOF-MS/MS instrumentation and to determine its antimicrobial, antioxidant, and cytotoxic activity together with inhibitory properties against tyrosinase and toxicity in erythrocyte lysis assay. Extracts from Z. bungeana were found to be sources of flavonoids, phenolic acids, organic acids, and terpenes that determined their antiradical activity. The minimum inhibitory concentrations of extracts were lower for Gram-positive bacteria (1.25–10 mg/mL) than for Gram-negative bacteria and fungi (5–20 mg/mL). The EC50 value calculated for antiradical activity ranged between 15.00 ± 1.06 µg/mL and 13.21 ± 3.24 µg/mL for ABTS and DPPH assays, respectively. Z. bungeana extracts were found to decrease the activity of tyrosinase by 50% (at 200 µg/mL) similarly to kojic acid and were slightly cytotoxic for human melanoma A375 cell line (at 200 µg/mL) with no effect on HaCaT keratinocytes. In the end, Z. bungeana did not reveal toxic effects in hemolytic assay as compared to the positive control Triton X-100. The performed tests show potential application of the plant in the treatment of infectious diseases, disorders caused by free radicals, and skin problems.

Ginger (Zingiber officinale Rosc.) is both a commonly used spice, and an ingredient of various dietary supplements and medications. Its diverse applications result from the range of health benefits that this plant brings thanks to the presence of active compounds (secondary metabolites) in the matrix. Even if several studies underline a stronger pharmacological activity of fresh ginger rhizomes, the unprocessed plant is relatively rarely used. Ginger rhizomes are subjected to thermal processing, such as boiling, blanching, steam drying and others, at different temperature and time settings. Additionally, freeze-drying of the rhizomes is used as the first step in the preparation of raw material. It was proved that the composition of secondary metabolites of the Zingiber officinale rhizome changes upon the influence of temperature. Therefore, the aim of the review was to put together scientific results on the impact of traditional and unconventional methods of heat treatment on ginger rhizomes and to show the compositional differences that they induce in the plant matrix. Variations in the content and the transformation of some compounds into other metabolites will be also discussed, with particular attention paid to two major groups of secondary metabolites present in the plant, namely, phenolics and terpenes.

By-products of cultivated plants are one of the major environmental concerns worldwide. Due to the high concentration of bioactive chemicals, such waste may be considered hazardous due to the interference with the plant growth, deterioration of the drinking water quality or toxic effects on sensitive marine organisms. Moreover, plant-derived by-products, with proper handling, may represent a low-cost source of bioactive compounds potentially important for pharmaceutical and cosmetics industries. The aim of the study was to evaluate the phytochemical composition, antioxidant activity, the influence of tyrosinase activity, in vitro sun protecting factor and cytotoxicity of 15 extracts from peels of five cultivars of Cucurbita maxima and C. moschata. The extracts were prepared using “green solvents” (water, 50% propylene glycol, and 20% ethanol) and ultrasound-assisted extraction. The performed analysis showed that the peel extracts from various cultivars differ significantly in respect to the phytochemical content and activity. The type of solvent also had a significant impact on the extract’s composition and bioactivity. Aqueous peel extracts contained the highest amounts of flavonoids, showed the greatest antioxidant potential and the most significant in vitro SPF values. In vitro studies showed that the analyzed peel extracts are not cytotoxic for human keratinocytes up to the concentration of 1000 µg/mL and thus might be considered as non-irritant for the skin. The study confirms the potential application of peel extracts from Cucurbita spp. cultivars in cosmetic products.

Fireweed (Epilobium angustifolium L.) has attracted attention due to its numerous biological activities. In the present work, we produced a polyphenol-rich freeze-dried infusion (407.02 ± 7.10 mg GAE/g) in order to measure, for the first time, the evolution of anticholinesterase activity during in vitro digestion. During the ‘gastric’ phase, there was an increase in the inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activity followed by a decrease during the ‘small intestinal’ phase. A strong correlation between total polyphenolic content (TPC) and the anticholinesterase activity of the digested fluids was observed (r = 0.90 for TPC/AChE; r = 0.88 for TPC/BChE, p

Halophytes are plant species widely distributed in saline habitats, such as beaches, postindustrial wastelands, irrigated lands, salt flats, and others. Excessive salt level, known to limit plant growth, is not harmful to halophytes, which have developed a variety of defense mechanisms allowing them to colonize harsh environments. Plants under stress are known to respond with several morpho-anatomical adaptations, but also to enhance the production of secondary metabolites to better cope with difficult conditions. Owing to these adaptations, halophytes are an interesting group of undemanding plants with a high potential for application in the food and pharmaceutical industries. Therefore, this review aims to present the characteristics of halophytes, describe changes in their gene expression, and discuss their synthesized metabolites of pharmacognostic and pharmacological significance. Lobularia maritima is characterized as a widely spread halophyte that has been shown to exhibit various pharmacological properties in vitro and in vivo. It is concluded that halophytes may become important sources of natural products for the treatment of various ailments and for supplementing the human diet with necessary non-nutrients and minerals. However, extensive studies are needed to deepen the knowledge of their biological potential in vivo, so that they can be introduced to the pharmaceutical and food industries.

Hedgehog (Hh) signaling aberrations trigger differentiation and proliferation in colorectal cancer (CRC). However, the current approaches which inhibit this vital cellular pathway provoke some side effects. Therefore, it is necessary to look for new therapeutic options. MicroRNAs are small molecules that modulate expression of the target genes and can be utilized as a potential therapeutic option for CRC. On the other hand, nanoformulations have been implemented in the treatment of plethora of diseases. Owing to their excessive bioavailability, limited cytotoxicity and high specificity, nanoparticles may be considered as an alternative drug delivery platform for the Hh signaling mediated CRC. This article reviews the Hh signaling and its involvement in CRC with focus on miRNAs, nanoformulations as potential diagnostic/prognostic and therapeutics for CRC.

Phytosterols (PSs) are plant-originated steroids. Over 250 PSs have been isolated, and each plant species contains a characteristic phytosterol composition. A wide number of studies have reported remarkable pharmacological effects of PSs, acting as chemopreventive, anti-inflammatory, antioxidant, antidiabetic, and antiatherosclerotic agents. However, PS bioavailability is a key issue, as it can be influenced by several factors (type, source, processing, preparation, delivery method, food matrix, dose, time of administration into the body, and genetic factors), and the existence of a close relationship between their chemical structures (e.g., saturation degree and side-chain length) and low absorption rates has been stated. In this sense, the present review intends to provide in-depth data on PS therapeutic potential for human health, also emphasizing their preclinical effects and bioavailability-related issues.

Prostate cancer (PCa) is with rising incidence in male population globally. It is a complex anomaly orchestrated by a plethora of cellular processes. Transforming growth factor-beta (TGF-β) signaling is one of the key signaling pathways involved in the tumorigenesis of PCa. TGF-β signaling has a dual role in the PCa, making it difficult to find a suitable therapeutic option. MicroRNAs (miRNAs) mediated regulation of TGF-β signaling is responsible for the TGF-ß paradox. These are small molecules that modulate the expression of target genes and regulate cancer progression. Thus, miRNAs interaction with different signaling cascades is of great attention for devising new diagnostic and therapeutic options for PCa. Natural compounds have been extensively studied due to their high efficacy and low cytotoxicity. Here, we discuss the involvement of TGF-ß signaling in PCa with the interplay between miRNAs and TGF-β signaling and also review the role of natural compounds for the development of new therapeutics for PCa.

This paper demonstrates the role of curly kale fermentation by autochthonous lactic acid bacteria in the formation of bioactive derivatives of phenolic compounds which may have anticancer properties. LC-MS and HPLC analyses were performed and the content of polyphenols in curly kale before and during fermentation were determined. Bioactive properties of salicylic and gentisic acids were tested in experiments on tumor (HT29, SW620) and normal (CCD841CoTr) epithelial cell lines. In this study, gentisic and salicylic acids were thoroughly examined. Gentisic acid has not been detected in Brasssicaceae vegetables so far, and the presence of both these acids was noted in fermented curly kale for the first time. Our results indicated that both salicylic and gentisic acids decreased the number of HT29 cells simultaneously with reduction of the intercellular interactions between these cells. Moreover, immunomodulatory and anti-inflammatory activity of gentisic acid was observed.

A comprehensive approach to the mineral composition of black teas of different origins was studied using the Flame Atomic Absorption Spectrometry (FAAS) method, supported by chemometric tools including Principal Component Analysis PCA) and Classification and Regression Trees (CART). Significant differences between the teas from seven countries (Japan, Nepal, Kenya, Iran, Sri Lanka, India, and China) were shown. K was the main element determined in all teas, with an average concentration of 11,649 mg/kg, followed by Ca, Mg and Mn. In general, regarding all investigated black teas, the element content was ranked in the following order: K > Ca > Mg > Mn > Fe > Na > Zn > Cu. The applied chemometric methods allowed us to recognize black tea clusters based on their mineral composition and place of cultivation, and allowed us to find correlations between particular elements in black teas. The performed analyses revealed interesting correlations between the concentration of various elements in black teas: K was negatively correlated with Na, Fe, Mn and Cu; K was positively correlated with the content of Ca and Mg. Significant positive correlations between Mn and Fe and Mn and Zn in the studied black tea samples were also revealed. It was shown that mineral composition may be a significant factor regarding the origin of the black tea, not only considering the country, but also the region or province.

This work aims to assess the recently established anti-inflammatory and antioxidant potential of melatonin of plant origin extracted from the plant matrix as a phytomelatonin complex (PHT-MLT), and compare its activity with synthetic melatonin (SNT-MLT) when used on its own or with vitamin C. For this purpose, a COX-2 enzyme inhibitory activity test, an antiradical activity in vitro and on cell lines assays, was performed on both PHT-MLT and SNT-MLT products. COX-2 inhibitory activity of PHT-MLT was found to be ca. 6.5 times stronger than that of SNT-MLT (43.3% and 6.7% enzyme inhibition, equivalent to the activity of acetylsalicylic acid in conc. 30.3 ± 0.2 and 12.0 ± 0.3 mg/mL, respectively). Higher antiradical potential and COX-2 inhibitory properties of PHT-MLT could be explained by the presence of additional naturally occurring constituents in alfalfa, chlorella, and rice, which were clearly visible on the HPLC-ESI-QTOF-MS fingerprint. The antiradical properties of PHT-MLT determined in the DPPH test (IC50 of 21.6 ± 1 mg of powder/mL) were found to originate from the presence of other metabolites in the 50% EtOH extract while SNT-MLT was found to be inactive under the applied testing conditions. However, the antioxidant studies on HaCaT keratinocytes stimulated with H2O2 revealed a noticeable activity in all samples. The presence of PHT-MLT (12.5, 25 and 50 µg/mL) and vitamin C (12.5, 25 and 50 µg/mL) in the H2O2-pretreated HaCaT keratinocytes protected the cells from generating reactive oxygen species. This observation confirms that MLT-containing samples affect the intracellular production of enzymes and neutralize the free radicals. Presented results indicated that MLT-containing products in combination with Vitamin C dosage are worth to be considered as a preventive alternative in the therapy of various diseases in the etiopathogenesis, of which radical and inflammatory mechanisms play an important role.

Palmatine (PLT) is a natural isoquinoline alkaloid that belongs to the class of protoberberines and exhibits a wide spectrum of pharmacological and biological properties, including anti-cancer activity. The aim of our study was to isolate PLT from the roots of Berberis cretica and investigate its cytotoxic and anti-proliferative effects in vitro alone and in combination with doxorubicine (DOX) using human ER+/HER2− breast cancer cell lines. The alkaloid was purified by column chromatography filled with silica gel NP and Sephadex LH-20 resin developed in the mixture of methanol: water (50:50 v/v) that provided high-purity alkaloid for bioactivity studies. The purity of the alkaloid was confirmed by high resolution mass measurement and MS/MS fragmentation analysis in the HPLC-ESI-QTOF-MS/MS-based analysis. It was found that PLT treatment inhibited the viability and proliferation of breast cancer cells in a dose-dependent manner as demonstrated by MTT and BrdU assays. PLT showed a quite similar growth inhibition on breast cancer cells with IC50 values ranging from 5.126 to 5.805 µg/mL. In contrast, growth of normal human breast epithelial cells was not affected by PLT. The growth inhibitory activity of PLT was related to the induction of apoptosis, as determined by Annexin V/PI staining. Moreover, PLT sensitized breast cancer cells to DOX. Isobolographic analysis revealed synergistic and additive interactions between studied agents. Our studies suggest that PLT can be a potential candidate agent for preventing and treating breast cancer.

Numerous species of Allium genus have been used in the traditional medicine based on their vast biological effects, e.g., antimicrobial, digestion stimulant, anti-sclerotic, soothing, antiradical or wound healing properties. In this work, unpolar and polar extracts from two lesser-investigated species of Allium growing in Kazakhstan, Alliumgalanthum Kar. & Kir. (AG) and A. turkestanicum Regel. (AT), were studied for their composition and biological effects. In the HPLC-ESI-QTOF-MS/MS analyses of water and alcoholic extracts simple organic acids, flavonoids and their glycosides were found to be the best represented group of secondary metabolites. On the other hand, in the GC-MS analysis diethyl ether, extracts were found to be rich sources of straight-chain hydrocarbons and their alcohols, fatty acids and sterols. The antimicrobial activity assessment showed a lower activity of polar extracts, however, the diethyl ether extract from AT bulbs and AG chives showed the strongest activity against Bacillus subtilis ATCC 6633, B. cereus ATCC 10876, some species of Staphylococcus (S. aureus ATCC 25923 and S. epidermidis ATCC 12228) and all tested Candida species (Candida albicans ATCC 2091, Candida albicans ATCC 10231, Candida glabrata ATCC 90030, Candida krusei ATCC 14243 and Candida parapsilosis ATCC 22019) with a minimum inhibitory concentration of 0.125–0.5 mg/mL. The highest antiradical capacity exhibited diethyl ether extracts from AG bulbs (IC50 = 19274.78 ± 92.11 mg Trolox eq/g of dried extract) in DPPH assay. In ABTS scavenging assay, the highest value of mg Trolox equivalents, 50.85 ± 2.90 was calculated for diethyl ether extract from AT bulbs. The same extract showed the highest inhibition of mushroom tyrosinase (82.65 ± 1.28% of enzyme activity), whereas AG bulb ether extract was the most efficient murine tyrosinase inhibitor (54% of the enzyme activity). The performed tests confirm possible cosmeceutical applications of these plants.

Growing scientific evidence indicates that Achillea biebersteinii is a valuable source of active ingredients with potential cosmetic applications. However, the data on its composition and pharmacological properties are still insufficient. This study aims to optimize the extraction procedure of the plant material, evaluate its phytochemical composition, and compare anti-tyrosinase potential of A. biebersteinii extracts obtained by various methods. In order to identify compounds responsible for the tyrosinase inhibitory activity of A. biebersteinii, the most active anti-tyrosinase extract was fractionated by column chromatography. The fractions were examined for their skin lightening potential by mushroom and murine tyrosinase inhibitory assays and melanin release assay. HPLC-ESI-Q-TOF-MS/MS analysis of the total extract revealed the presence of several phenolic acids, flavonoids, flavonoid glucosides, and carboxylic acid. Among them, fraxetin-8-O-glucoside, quercetin-O-glucopyranose, schaftoside/isoschaftoside, gmelinin B, 1,3-dicaffeoylquinic acid (1,3-DCQA), and ferulic acid were found in the fractions with the highest skin lightening potential. Based on obtained qualitative and quantitative analysis of the fractions, it was assumed that the caffeoylquinic acid derivatives and dicaffeoylquinic acid derivatives are more likely responsible for mushroom tyrosinase inhibitory activity of A. biebersteinii extracts and fractions. Ferulic acid was proposed as the most active murine tyrosinase inhibitor, responsible also for the reduced melanin release from B16F10 murine melanoma cells.

Magnoflorine (MGN) is a quaternary aporphine alkaloid that exhibits numerous therapeutic properties, including neuropsychopharmacological, anti-anxiety, immunomodulatory, anti-inflammatory, antioxidant, or antifungal activities. The aim of the present study was an investigation of the influence of MGN on viability, proliferation, induction of apoptosis, and cell cycle arrest in NCI-H1299 lung, MDA-MB-468 breast, T98G glioma, and TE671 rhabdomyosarcoma cancer cells. MGN was isolated from the roots of Berberis cretica L. by counter-current partition chromatography (CPC). Cell viability and proliferation assessments were performed by means of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and 5-bromo-2ʹ-deoxyuridine (BrDU) assays, respectively. The induction of apoptosis and cell cycle progression was measured using fluorescence-activated cell sorting analysis. MGN in high doses inhibits proliferation, induces apoptosis, and inhibits cell cycle in S/G2 phases in a dose-dependent manner. MGN seems to be a promising anti-cancer compound in therapy of some types of lung, breast, glioma, and rhabdomyosarcoma cancers, for which current standard therapies are limited or have severe strong side effects.

Studies on hydroglycolic (HG) extracts of Achillea biebersteinii (AB)—a less investigated representative of the genus—were performed to determine their potential for cosmetic applications compared to the well-known Achillea millefolium (AM). Three types of water:polyethylene glycol extracts (1:1, 4:1, 6:1 v/v) were obtained from both species and analyzed for their composition by high performance liquid chromatography coupled with mass spectrometry (HPLC-ESI-Q-TOF-MS) and assayed for their biological activities. The study led to the identification of 11 metabolites from different natural product classes with the highest share corresponding to 5-caffeoylquinic acid, axillarin, coumaroylquinic acid isomers and 3-caffeoylquinic acid. The highest antiradical capacity in DPPH and ABTS scavenging assays was shown for HG 4:1 of AB and AM extracts. HG 1:1 extracts from both species inhibited monophenolase and diphenolase activity of tyrosinase, whereas AB HG 4:1 extract showed significant monophenolase inhibition. The highest sun protection factor (SPF) was determined for AM HG 4:1 extract, equal to 14.04 ± 0.17. The AB extracts were cytotoxic for both human keratinocytes HaCaT and A375 melanoma, however HG 1:1 and 4:1 extracts were more cytotoxic for cancer than for noncancerous cells. In conclusion, AB HG 1:1 and 4:1 extracts display significant potential as active cosmetic ingredients.

The aim of the present study was to determine the composition, antiradical and antimicrobial activity of fruits, leaves and roots of an underestimated species of barberry—Berberis iliensis—growing in Kazakhstan. Particular attention was paid to the determination of the composition of its extracts by high-performance liquid chromatography coupled with mass spectrometry (HPLC-ESI-Q-TOF-MS) analysis. As a result of the chromatographic and spectrometric study 33 secondary metabolites from the groups of phenolic acids and their esters, flavonoids, alkaloids and organic acids were identified and 15 of them—quantified. The isomers of caffeoyl-glucaric acid, caffeic acid derivatives, isoquercetin, berberine and jatrorrhizine were the most abundant components of the tested extracts. The antiradical activity tests were performed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and Folin-Ciocalteu assays on four types of extracts (water, ethanol, ethanol-water 7:3 v/v, ethanol-water 1:1 v/v) from the three organs of the plant. The highest antiradical potential (IC50 = 80 ± 6.36 µg/mL) and phenolic content (440 ± 17.1 mg gallic acid equivalents/L) was calculated for ethanol- water (1:1 v/v) extracts from the leaves and could be influenced by the abundant presence of simple phenolic acids, flavonoids and glucaric acid esters. Among reference microorganisms, M. luteus, S. epidermidis, some S. aureus and B. cereus belonging to Gram-positive bacteria and yeasts from Candida species were the most sensitive to roots extract that was found the most active among the studied samples. The results of the study classify Berberis iliensis as a strong antioxidant agent and as a plant with an antimicrobial potential.

Palmatine (PALM) and berberine (BERB) are widely identified isoquinoline alkaloids among the representatives of the Berberidaceae botanical family. The antiseizure activity of BERB was shown previously in experimental epilepsy models. We assessed the effect of PALM in a pentylenetetrazole (PTZ)-induced seizure assay in zebrafish, with BERB as an active reference compound. Both alkaloids were isolated from the methanolic root extract of Berberis sibirica by counter-current chromatography, and their ability to cross the blood–brain barrier was determined via quantitative structure–activity relationship assay. PALM exerted antiseizure activity, as confirmed by electroencephalographic analysis, and decreased c-fos and bdnf levels in PTZ-treated larvae. In a behavioral assay, PALM dose-dependently decreased PTZ-induced hyperlocomotion. The combination of PALM and BERB in ED16 doses revealed hyperadditive activity towards PTZ-induced hyperlocomotion. Notably, we have indicated that both alkaloids may exert their anticonvulsant activity through different mechanisms of action. Additionally, the combination of both alkaloids in a 1:2.17 ratio (PALM: BERB) mimicked the activity of the pure extract, which indicates that these two active compounds are responsible for its anticonvulsive activity. In conclusion, our study reveals for the first time the anticonvulsant activity of PALM and suggests the combination of PALM and BERB may have higher therapeutic value than separate usage of these compounds.

Although numerous studies have been conducted on ginger extracts and fractions, the data on the pharmacological activity of single constituents of Zingiber officinale are still insufficient. To assess the antidementia properties of the plant, a thin layer chromatography (TLC)-based bioautography acetylcholinesterase inhibitory assay was performed on the Zingiber officinale diethyl ether extract. It led to the recognition of three active inhibitors among volatile constituents of the plant: ar-curcumene (A), α-sesquiphellandrene (B) and a-zingiberene (C). The identification of the components was possible thanks to the application of a TLC–HPLC-MS interface analysis of active zones and the GC-MS qualitative analysis of the tested samples. Based on the obtained results, the influence of several extraction techniques (hydrodistillation—HD, pressurized liquid extraction or accelerated solvent extraction—ASE, shaking maceration–SM, supercritical fluid extraction–SFE, and ultrasound-assisted extraction—UAE) on the recovery of the active metabolites from plant material was assessed to deliver enriched extracts. As a result, HD and SFE, were found to be the most efficient methods to recover the volatile components and the concentrations of A, B, and C reached 0.51 ± 0.025, 0.77 ± 0.045, and 1.67 ± 0.11 percent, respectively. Only HD and SFE were found to recover monoterpene hydrocarbons from the plant matrix. The remaining techniques provided extracts rich in more complex constituents, like sesquiterpenes.

Skin is constantly exposed to harmful environmental factors, causing photo-oxidative stress in cells and leading to the development of health and aesthetic problems. Multifunctional ingredients of everyday skincare products, possessing antioxidant, UV-protecting, anti-hyperpigmentation, and skin cancer-preventing properties are in high demand. Due to the high content of polyphenolic compounds Cistus × incanus L. and Cistus ladanifer L. are potentially interesting sources of cosmetic ingredients with multiple skin protecting functions. In this study eight extracts from dried C. incanus and C. ladanifer—aerial parts were prepared using 60% (v/v) or 100% (v/v) methanol, on a magnetic stirrer or in Soxhlet apparatus, and compared for their content of phytochemicals and properties important for the skin protection. Extracts from C. incanus prepared in 60% (v/v) methanol contained the highest amount of polyphenolic compounds (331.82−347.27 mg GAE/g DW) and showed the most significant antioxidant activity (IC50 = 3.81−4.05 µg/mL). C. incanus extracts were also effective tyrosinase inhibitors (30−70% inhibition at 100 µg/mL). Statistical correlation analysis revealed that epicatechin, epigallocatechin gallate (EGCG), and myricitrin may be responsible for the antioxidant and tyrosinase inhibitory potential of C. incanus extracts. All analyzed extracts were cytotoxic for human melanoma cells A375 (IC50 = 57.80−199.01 µg/mL), with C. incanus extract prepared in 100% (v/v) methanol using Soxhlet extraction being the most effective. The extracts did not significantly impair the growth of noncancerous human keratinocytes HaCaT. C. incanus and C. ladanifer extracts possess also natural sun protecting activity (SPF 3.42−3.77 at 100 µg/mL), enhancing their anti-hyperpigmentation and anti-melanoma potential.