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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.

The histochemical analysis of medicinal plants and raw materials makes it possible to establish the presence of certain groups of active and related substances or products of their metabolism, as well as to study their localization in tissues. The article presents the results of histochemical analysis of leaves, flowers, petioles and stems of Filipendula vulgaris and Filipendula ulmaria. These types of plant are used in traditional medicine as an anti-inflammatory, antipyretic and bactericidal agent. Our research objective - to determine the peculiarities of the localization features of individual groups of secondary metabolites in the aerial part of meadowsweet and meadowsweet growing in the territory of Central Kazakhstan at the microscopic level. Materials and Methods. Transverse sections of petioles, stem and whole flower; transverse and superficial sections of leaves of Filipendula vulgaris and Filipendula ulmaria were fixed in Strauss-Fleming solution, after which histochemical reactions were carried out to locate and identify essential oils, phenolic acids, flavonoids, sesquiterpene lactones, polysaccharides and alkaloids. The study of microscopic signs, as well as histochemical tests were carried out according to the methods of the State Pharmacopoeia of the Republic of Kazakhstan using a light microscope Biomed-4. Results and Discussion. The localization of biologically active substances in the studied types of plant raw materials was determined by histochemical methods using light microscopy. The presence of phenolic compounds, flavonoids, traces of essential oil, alkaloids and sesquiterpene lactones was established. The absence of polysaccharides in the investigated micropreparations was established. Conclusions. For the first time, the localization of secondary metabolites in the tissues of Filipendula vulgaris and Filipendula ulmaria was studied by histochemical tests. The results of histochemical studies can be used to confirm the authenticity, identification and standardization of the aerial parts of Filipendula vulgaris and Filipendula ulmaria.

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

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.

The main aim of the study was to assess the acetylcholinesterase-inhibitory potential of triterpenoid saponins (astragalosides) found in the roots of Astragalus mongholicus. For this purpose, the TLC bioautography method was applied and then the IC50 values were calculated for astragalosides II, III and IV (5.9 μM; 4.2 μM, and 4.0 μM, respectively). Moreover, molecular dynamics simulations were carried outto assess the affinity of the tested compounds for POPC and POPG-containing lipid bilayers, which in this case are the models of the blood-brain barrier (BBB). All determined free energy profiles confirmed that astragalosides exhibit great affinity for the lipid bilayer. A good correlation was obtained when comparing the logarithm of n-octanol/water partition coefficient (logPow) lipophilicity descriptor values with the smallest values of free energy of the determined 1D profiles. The affinity for the lipid bilayers changes in the same order as the corresponding logPow values, i.e.,: I > II > III~IV. All compounds exhibit a high and also relatively similar magnitude of binding energies, varying from ca. −55 to −51 kJ/mol. Apositive correlation between the experimentally-determined IC50 values and the theoretically-predicted binding energies expressed by the correlation coefficient value equal 0.956 was observed.

Achillea spp. is well known for its broad range of applications and long history of use in traditional medicine around the world. Health benefits of Achillea extracts result from the multitude of secondary metabolites identified in the plants from this genus that include flavonoids, phenolic acids, terpenes, guaianolides, phytosterols, fatty acids, and organic acids. The properties of several Achillea extracts meet also the expectations of a vividly developing cosmetic market. An increasing number of studies on the dermatological properties of Achillea spp. are observed in the recent years, with Achillea millefolium L. being the most studied and used representative of the genus. There is strong scientific evidence showing that also other yarrow species might be rich sources of effective cosmetic ingredients, with skin calming and rejuvenating properties, wound healing activity, and anti-inflammatory potential. Several Achillea extracts and isolated compounds were also shown to display significant tyrosinase inhibitory, antioxidant, and antimicrobial properties and thus are interesting candidates for active ingredients of medications and cosmetic products protecting the skin from the harmful impact of environmental stressors. The aim of this review is to collect the current information on the composition and cosmeceutical significance of different Achillea species.

Gastric cancer (GC) has high incidence rates and constitutes a common cause of cancer mortality. Despite advances in treatment, GC remains a challenge in cancer therapy which is why novel treatment strategies are needed. The interest in natural compounds has increased significantly in recent years because of their numerous biological activities, including anti-cancer action. The isolation of the bioactive compounds from

A number of studies have established the potential of chitosan and alginate-based edible film/coatings for preserving the quality attributes of fruits and vegetables. Findings demonstrate that these films/coatings act as a barrier on the surface of fruits and vegetables which causes higher moisture and water retention, create favourable micro-environments by optimizing the concentration of gases and delays ripening. Sincere efforts are being further made to improve the efficiency of edible films using functional additives such as phenolics, essential oils (EOs) and nano-forms. These additives have unlocked a new dimension for enhancing functional properties of alginate/chitosan-based films. These functional compounds are now emerging as an important component of edible films/coatings for prolonging shelf-life of fruits and vegetables. The present review comprehensively elaborates recent studies on functional additives and their mechanism of action. Here we also establish their proficiency in extending quality and shelf-life of various fruits including guava, pear, blueberries and vegetables like cucumber, capsicum and mushroom. Principles behind antimicrobial and antioxidant activities of additives in preventing the food spoilage are also reviewed. Competency of phenolics, EOs and nano-forms in extending the shelf-life without affecting the nutritional properties and safety aspects of the fruits and vegetables still require further attention.

The aim of the study was to present the fingerprint of different

A traditionally prepared aqueous extract (= decoction) of Houttuynia cordata Thunb (Yu xing cao) (HC) is widely used in Traditional Chinese Medicine (TCM) to treat inflammatory disease. Previous chemical and biological studies on HC have mainly focused on organic extracts rather than the aqueous decoction, which is the traditional formulation.The study aimed to investigate whether the chemical composition of HC aqueous decoction (HCD) varies with geographical sourcing, to investigate the mechanism of action of HCD, and to determine if chemical variation impacts on HCDs anti-inflammatory activity.Sixteen samples of HC were purchased from Sichuan, Hubei and Anhui provinces in the People's Republic of China (PRC) and were prepared by the traditional decoction method to yield their corresponding HCDs. A Quality Control (QC) sample was prepared by combining individual HCD extracts. HCDs were analysed by Nuclear Magnetic Resonance (NMR) and High-Performance Liquid Chromatography-Mass Spectrometry (HPLC-MS). The anti-inflammatory activities associated with intestinal barrier function of HCD were studied by tumor necrosis factor-α (TNF-α) activated Caco-2 monolayers in vitro and in vivo using Dextran Sulfate Sodium (DSS)-induced murine colitis. Proteins involved in inflammation, mRNA levels, disease severity scores, and histology involved in intestinal inflammation were analysed.HCD samples exhibited different chemical fingerprints and three regional outliers were identified by Principal Component Analysis (PCA). Fifteen phytochemical metabolites were identified and quantified. HCD showed in vitro anti-inflammatory activity, enhancing zonula occludens-1 (ZO-1), occludin, interleukin (IL)-10 and decreasing IL-1β, IL-6 and epidermal growth factor receptor (EGFR) via an EGFR-dependent mitogen-activated protein kinase (MAPK) extracellular signal-regulated kinase 1/2 (ERK 1/2) signaling pathway. This beneficial effect on intestinal inflammation was also seen in the in vivo colitis model at a molecular level in colonic tissues.This study shows that the test HCDs were chemically different, resulting in different levels of activity on intestinal barrier function and inflammation. Moreover, a "Daodi" product showed the greatest biological activity in this study, thus validating the importance of the "Daodi" quality material in TCM and supporting the traditional used of HCD for the treatment of inflammation.

The reduction of staphyloxanthin (STX) production in Staphylococcus aureus under trans-anethole (TA) influence was proven in former studies. However, no tests concerning the impact of TA on a biosynthetic pathway of this carotenoid pigment have been published so far. Thus, for the first time, the present preliminary study evaluated the influence of TA on the expression level of genes (crtOPQMN operon and aldH) encoding STX pathway enzymes. Additional attention was paid to the identification of STX and its intermediates. Gene expression and identification of extracted compounds were conducted using quantitative real-time PCR and HPLC-MS techniques, respectively. The analyzes showed no difference in crtM, crtN, crtO, crtP, crtQ, and aldH gene expression between bacterial samples isolated from the non-stimulated (control) medium and the stimulated one with TA. Compared to the control group that showed the presence of all metabolic intermediates and STX, the TA-treated bacteria were characterized by a lack or a significant reduction of the majority of compounds, except 4,4'-diaponeurosporenoate, the content of which was elevated in the TA-treated sample. Moreover, in silico molecular docking analysis revealed that TA is capable to create relatively strong interactions with both 4,4'-diapophytoene synthase and 4,4'-diapophytoene desaturase. The preliminary findings indicate that the previously observed TA effect reducing the number of S. aureus colonies pigmentation is probably not associated with the expression levels of genes encoding STX pathway enzymes. It has been proven that adding TA to the medium can interfere with the formation of STX at different levels of its biosynthetic pathway.

Alzheimer's disease (AD) is one of the most prevalent diseases that lead to memory deficiencies, severe behavioral abnormalities, and ultimately death. The need for more appropriate treatment of AD continues, and remains a sought-after goal. Previous studies showed palmatine (PAL), an isoquinoline alkaloid, might have the potential for combating AD because of its in vitro and in vivo activities. In this study, we aimed to assess PAL's therapeutic potential and gain insights into the working mechanism on protein level in the AD mouse model brain, for the first time. To this end, PAL was administered to 12-month-old 5xFAD mice at two doses after its successful isolation from the Siberian barberry shrub. PAL (10 mg/kg) showed statistically significant improvement in the memory and learning phase on the Morris water maze test. The PAL's ability to pass through the blood-brain barrier was verified via Multiple Reaction Monitoring (MRM). Label-free proteomics analysis revealed PAL administration led to changes most prominently in the cerebellum, followed by the hippocampus, but none in the cortex. Most of the differentially expressed proteins in PAL compared to the 5xFAD control group (ALZ) were the opposite of those in ALZ in comparison to healthy Alzheimer's littermates (ALM) group. HS105, HS12A, and RL12 were detected as hub proteins in the cerebellum. Collectively, here we present PAL as a potential therapeutic candidate owing to its alleviating effect in 5xFAD mice on not only cognitive impairment but also proteomes in the cerebellum and hippocampus.

Carduus nutans L. (Compositae) has been extensively used for medicinal purposes. As other representatives of the genus it is implemented in the treatment of liver disorders and used as diuretic and digestive agent. Previous studies have determined the predominant classes of secondary metabolites in Carduus species. Among the major representatives of their extracts flavonoids, phenolic acids, coumarins, sterols and terpenes were identified. The antiradical capacity of three extracts assessed in the DPPH test revealed the highest radical scavenging properties of methanol extract (the EC

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.

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.

Inflammation is a protective reaction of the innate immune system as a response to imbalances caused by a specific stimulus, a disease or a pathogen. A prolonged inflammatory condition may lead to the development of metabolic syndrome, which affects more than one-fourth of the world’s population. This condition leads to the development of multi-organ disorders based on disrupted blood lipid and sugar levels, hypertension and oxidative stress. The review aims to present Zingiber officinale Rosc. as a plant that exhibits a variety of healing properties and restores the organism’s equilibrium. Ginger (GI) rhizomes have been commonly used in traditional medicine to treat arthritis, stomach ache, nonalcoholic fatty liver disease, rheumatism, nervous system syndromes, asthma, diabetes and nausea caused by pregnancy or chemotherapy. This review gathers together data from in vivo experiments related to the application of ginger for the treatment of inflammatory conditions, obesity, diabetes and other related disorders as a consequence of metabolic syndrome, including the confirmed molecular mechanisms of action.

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.

Several genome-wide association studies have associated CACNA1C variants with psychiatric disorders. The molecular mechanisms involved are poorly understood. Taking advantage of the zebrafish larva as a model, we investigated how two different mutations in cacna1c – sa10930 (nonsense mutation) and sa15296 (splice site mutation), affect neuronal function. We characterized changes in cacna1c mRNA, neurotransmitter levels and behaviour, as well as whole-brain activity using single electrode local field potential recordings. Both point mutations resulted in a significant reduction in cacna1c mRNA, as well as social behaviour and prepulse inhibition deficits. Whereas sa15296 mutants displayed abnormal locomotor and open-field behaviour, we observed normal behaviour in the sa10930 mutants. Brain recordings from both mutants had lower spectral power while sa15296 displayed significant seizure-like activity. Finally, sa10930 homozygotes showed increased dopamine and serotonin levels, decreased gamma-aminobutyric acid (GABA) levels, and unchanged glutamate levels while homozygous sa15296 larvae showed increased levels of serotonin and glutamate, and unaffected levels of GABA and dopamine. Our work provides new insights into the functional role of CACNA1C in behavioural, electrophysiological and biochemical traits linked to psychiatric disorders. We show a functional role for the non-coding mutation (sa15296) in the cacna1c in vivo animal model. Consistent with existing hypotheses, our data suggest that disruption of gene expression, neurotransmission, and cortical excitability are involved in CACNA1C-related mechanisms of psychiatric disorders.

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.

Simple Summary Breast cancer (BC) is the most frequent malignancy diagnosed in 2020 worldwide. Despite significant advances in BC therapy, its pathogenesis is still not fully understood, and effective therapy is one of the most important challenges in current oncology. The article presents the state of the knowledge on vorinostat (SAHA) in the therapy of various histological subtypes of BC, individually or in polytherapy with other active compounds, in in vitro, in vivo and clinical trials settings. Abstract Vorinostat (SAHA), an inhibitor of class I and II of histone deacetylases, is the first histone deacetylase inhibitor (HDI) approved for the treatment of cutaneous T-cell lymphoma in 2006. HDIs are promising anticancer agents that inhibit the proliferation of many types of cancer cells including breast carcinoma (BC). BC is a heterogeneous disease with variable biological behavior, morphological features, and response to therapy. Although significant progress in the treatment of BC has been made, high toxicity to normal cells, serious side effects, and the occurrence of multi-drug resistance limit the effective therapy of BC patients. Therefore, new active agents which improve the effectiveness of currently used regimens are highly needed. This manuscript analyzes preclinical and clinical trials data of SAHA, applied individually or in combination with other anticancer agents, considering different histological subtypes of BC.

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.

Gastric cancer (GC) has high incidence rates and constitutes a common cause of cancer mortality. Despite advances in treatment, GC remains a challenge in cancer therapy which is why novel treatment strategies are needed. The interest in natural compounds has increased significantly in recent years because of their numerous biological activities, including anti-cancer action. The isolation of the bioactive compounds from Coptis chinensis Franch was carried out with the Centrifugal Partition Chromatography (CPC) technique, using a biphasic solvent system composed of chloroform (CHCl3)—methanol (MeOH)—water (H2O) (4:3:3, v/v) with an addition of hydrochloric acid and trietylamine. The identity of the isolated alkaloids was confirmed using a high resolution HPLC-MS chromatograph. The phytochemical constituents of Coptis chinensis such as berberine, jatrorrhizine, palmatine and coptisine significantly inhibited the viability and growth of gastric cancer cell lines ACC-201 and NCI-N87 in a dose-dependent manner, with coptisine showing the highest efficacy as revealed using MTT and BrdU assays, respectively. Flow cytometry analysis confirmed the coptisine-induced population of gastric cancer cells in sub-G1 phase and apoptosis. The combination of coptisine with cisplatin at the fixed-ratio of 1:1 exerted synergistic and additive interactions in ACC-201 and NCI-N87, respectively, as determined by means of isobolographic analysis. In in vivo assay, coptisine was safe for developing zebrafish at the dose equivalent to the highest dose active in vitro, but higher doses (greater than 10 times) caused morphological abnormalities in larvae. Our findings provide a theoretical foundation to further studies on more detailed mechanisms of the bioactive compounds from Coptis chinensis Franch anti-cancer action that inhibit GC cell survival in in vitro settings.

Thymoquinone (TQ) is a secondary metabolite found in abundance in very few plant species including Nigella sativa L., Monarda fistulosa L., Thymus vulgaris L. and Satureja montana L. Preclinical pharmacological studies have shown that TQ has many biological activities, such as anti-inflammatory, antioxidant and anticancer. Both in vivo and in vitro experiments have shown that TQ acts as an antitumor agent by altering cell cycle progression, inhibiting cell proliferation, stimulating apoptosis, inhibiting angiogenesis, reducing metastasis and affecting autophagy. In this comprehensive study, the evidence on the pharmacological potential of TQ on pancreatic cancer is reviewed. The positive results of preclinical studies support the view that TQ can be considered as an additional therapeutic agent against pancreatic cancer. The possibilities of success for this compound in human medicine should be further explored through clinical trials. © 2022 The Authors

Zingiber officinale is one of the most frequently used medicinal herbs in Asia. Using rodent seizure models, it was previously shown that Zingiber officinale hydroethanolic extract exerts antiseizure activity, but the active constituents responsible for this effect have not been determined. In this paper, we demonstrated that Zingiber officinale methanolic extract exerts anticonvulsant activity in the pentylenetetrazole (PTZ)-induced hyperlocomotion assay in larval zebrafish. Next, we isolated 6-gingerol (6-GIN)—a major constituent of Zingiber officinale rhizoma. We observed that 6-GIN exerted potent dose-dependent anticonvulsant activity in the PTZ-induced hyperlocomotion seizure assay in zebrafish, which was confirmed electroencephalographically. To obtain further insight into the molecular mechanisms of 6-GIN antiseizure activity, we assessed the concentration of two neurotransmitters in zebrafish, i.e., inhibitory γ-aminobutyric acid (GABA) and excitatory glutamic acid (GLU), and their ratio after exposure to acute PTZ dose. Here, 6-GIN decreased GLU level and reduced the GLU/GABA ratio in PTZ-treated fish compared with only PTZ-bathed fish. This activity was associated with the decrease in grin2b, but not gabra1a, grin1a, gria1a, gria2a, and gria3b expression in PTZ-treated fish. Molecular docking to the human NR2B-containing N-methyl-D-aspartate (NMDA) receptor suggests that 6-GIN might act as an inhibitor and interact with the amino terminal domain, the glutamate-binding site, as well as within the ion channel of the NR2B-containing NMDA receptor. In summary, our study reveals, for the first time, the anticonvulsant activity of 6-GIN. We suggest that this effect might at least be partially mediated by restoring the balance between GABA and GLU in the epileptic brain; however, more studies are needed to prove our hypothesis.

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.

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.

The aim of the study was to present the fingerprint of different Lepidium peruvianum tuber extracts showing glucosinolates-containing substances possibly playing an important role in preventinting dementia and other memory disorders. Different phenotypes of Lepidium peruvianum (Brassicaceae) tubers were analysed for their glucosinolate profile using a liquid chromatograph coupled with mass spectrometer (HPLC-ESI-QTOF-MS/MS platform). Qualitative analysis in 50% ethanolic extracts confirmed the presence of ten compounds: aliphatic, indolyl, and aromatic glucosinolates, with glucotropaeolin being the leading one, detected at levels between 0–1.57% depending on phenotype, size, processing, and collection site. The PCA analysis showed important variations in glucosinolate content between the samples and different ratios of the detected compounds. Applied in vitro activity tests confirmed inhibitory properties of extracts and single glucosinolates against acetylcholinesterase (AChE) (15.3–28.9% for the extracts and 55.95–57.60% for individual compounds) and butyrylcholinesterase (BuChE) (71.3–77.2% for the extracts and 36.2–39.9% for individual compounds). The molecular basis for the activity of glucosinolates was explained through molecular docking studies showing that the tested metabolites interacted with tryptophan and histidine residues of the enzymes, most likely blocking their active catalytic side. Based on the obtained results and described mechanism of action, it could be concluded that glucosinolates exhibit inhibitory properties against two cholinesterases present in the synaptic cleft, which indicates that selected phenotypes of L. peruvianum tubers cultivated under well-defined environmental and ecological conditions may present a valuable plant material to be considered for the development of therapeutic products with memory-stimulating properties.

Three curcuminoids: bisdemethoxycurcumin, demethoxycurcumin, and curcumin from turmeric were successfully separated by a high capacity solvent system composed of heptane: chloroform: methanol: water mixture (5: 6: 3: 2 v/v/v/v) tailored for centrifugal partition chromatographs at K-values of 0.504, 1.057, 1.644, respectively. These three ferulic acid derivatives obtained at a purity rate exceeding 95% were analysed by an HPLC-MS spectrometer. Turmeric extract inhibited the proliferation/viability of A549 human lung cancer, HT29 colon cancer, and T98G glioblastoma cell lines in (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) tetrazolium reduction assay (MTT). Single curcuminoids significantly decreased the viability/proliferation of lung cancer cells in a dose-dependent manner. However, total extract displayed the superior anticancer activity in the investigated cell lines. Crude extract in combination with cisplatin augmented the decrease in the viability of cancer cells compared with single compound treatment in A549 lung cancer cells. Total extract of Curcuma longa could be regarded as being more effective against lung cancer cells in vitro than its separated compounds.

The total phenolic content (TPC), total tannin content (TTC) and total flavonoid content (TFC) as well as the antioxidant activity and the cytotoxic effect of the extract from leaves ofErythrochiton brasiliensisNees & Mart. (Rutaceae) were evaluated. Raw material was collected in different European botanical gardens. Statistical analysis revealed a clear grouping of populations according to their climatic zone. The average TPC, TTC and TFC in tested samples were 35.92 (± 7.11) mg GAE·g–1DW, 14.98 (± 4.08) mg PyE·g–1DW and 2.92 (± 0.76) mg QuE·g–1DW, respectively. The scavenged DPPH and Trolox equivalents determined by EPR spectroscopy were 1.23–4.14 and 0.50–1.44 mmol·g–1of dry extract, respectively. Thirteen compounds (derivatives of bezoic acid acid andtrans-cinnammic acid) were identified in the samples. The flavonoid vitexin was also present as the major component in three investigated samples. Thein vitrocytotoxicity test of the extract on Vero cells provided IC50and IC10values of 175.6 and 72.5 μg·mL–1, respectively. Incubation of samples with HHV-1 infected Vero cells had no effect on the occurrence of cytopathic effect.

The rare coumarins stenocarpin, stenocarpin isobutyrate, oficinalin, oficinalin isobutyrate, 8-methoxypeucedanin and the known xanthotoxin, isoimperatorin, bergapten, peucedanin and 8–methoxyisoimperatorin were isolated fromPeucedanum luxuriansTamamsch. (Apiaceae) and identified by means of spectral data (1D and 2D NMR). Their immunomodulating activity was evaluated by flow cytometry and their influence on HL60 cells as well as on PHA-stimulated PBLs was tested. All tested coumarins induce apoptosis (maximal in the 48 h culture) and decrease cell proliferation in a time- and dose-dependent manner, especially in HL60 cells. They also induce partial G1 block, but only in HL60 cells (at 100 µM concentrations). Dose-dependent reduction of RNA content was also found in G1 cells treated by the coumarins. All of the tested coumarins also possessed immunomodulatory activities. Bergapten and xanthotoxin were found to be the best candidates for further evaluation as anti-cancer drugs.

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&ndash, brain barrier was determined via quantitative structure&ndash, 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.

Zingiber officinale is one of the most frequently used medicinal herbs in Asia. Using rodent seizure models, it was previously shown that Zingiber officinale hydroethanolic extract exerts antiseizure activity, but the active constituents responsible for this effect have not been determined. In this paper, we demonstrated that Zingiber officinale methanolic extract exerts anticonvulsant activity in the pentylenetetrazole (PTZ)-induced hyperlocomotion assay in larval zebrafish. Next, we isolated 6-gingerol (6-GIN) – a major constituent of Zingiber officinale rhizoma. We observed that 6-GIN exerted potent dose-dependent anticonvulsant activity in the PTZ-induced hyperlocomotion seizure assay in zebrafish, which was confirmed electroencephalographically. To obtain further insight into the molecular mechanisms of 6-GIN antiseizure activity, we assessed the concentration of two neurotransmitters in zebrafish, i.e., inhibitory γ-aminobutyric acid (GABA) and excitatory glutamic acid (GLU), and their ratio after exposure to acute PTZ dose. Here, 6-GIN decreased GLU level and reduced the GLU/GABA ratio in PTZ-treated fish compared with only PTZ-bathed fish. This activity was associated with the decrease in grin2b, but not gabra1a, grin1a, gria1a, gria2a, and gria3b expression in PTZ-treated fish. Molecular docking to the human NR2B-containing N-methyl-D-aspartate (NMDA) receptor suggests that 6-GIN might act as an inhibitor and interact with the amino terminal domain, the glutamate-binding site, as well as within the ion channel of the NR2B-containing NMDA receptor. In summary, our study reveals, for the first time, the anticonvulsant activity of 6-GIN. We suggest that this effect might at least be partially mediated by restoring the balance between GABA and GLU in the epileptic brain, however, more studies are needed to prove our hypothesis.

Horse chestnut fruits and seeds have been traditionally used as a remedy against chronic venous insufficiency symptoms. Currently the total extracts or purified saponins are extensively used as dietary supplements or medicines’ ingredients in numerous authorized pharmaceuticals. The goal of this study was to investigate the changes in the secondary metabolites content within time. The selected optimal conditions for collection could provide the highest quantity of active compounds in the extracts, which will increase the quality of the final product. The obtained results indicate that the highest content of natural products in the horse chestnut fruits was measured between the 13th and 16th week from the beginning of blooming. The quantitative analysis of escin and two flavonoids: kaempferol and procyanidin A2 was performed on the extracts within the study. The content of the selected natural products increased of ca. 90% between the 12th and 20th week for escin and of ca. 120% between the 7th and 12th week, for flavonoids. The rise in natural products quantity was also expressed in the measured antioxidant activity and total phenolic content values in DPPH and Folin–Ciocalteu tests.

The development of a fast hCCC method tailored to recover phenolics of Siberian barberry (Berberis sibirica, Berberidaceae) responsible for the observed strong antioxidant activity was performed. Initially, the optimization of extraction procedure was evaluated based on the antiradical potential assessment (DPPH and Folin-Ciocalteu assays). 100 °C methanol ASE extract exhibited the highest antiradical activity (IC50=60 ± 4 μg/mL), and a significant TPC (159 ± 2 mgGAE/g). Thorough determination of phenolic content by UHPLC-DAD-ESI(-)HRMS revealed the presence of 10 phenolics as major constituents, and several groups of alkaloids. pH-zone refining hCCC was chosen as the most promising method for the extract's fractionation due to the ionizable character of its constituents. For this purpose a MtBE-H2O (1:1) system with 10mM TEA and HCl was applied leading to a phenolic fraction, free of alkaloids, with higher antioxidant capacity (IC50=25 μg/mL, TPC=178 mg GAE/g). Additionally, fractionation of alkaloids was achieved resulting isolation of pharmacologically important alkaloids: magnoflorine and berberine.

Green tea contains a variety of biologically active constituents that are widely used in the pharmaceutical and food industries. Among them, simple catechins constitute a major group of compounds that is primarily responsible for the high biologic activity of green tea extracts. Therefore, the application of optimized extraction conditions may result in obtaining high value extracts. The main purpose of the study was to compare the content of polyphenols, mainly catechins, and the antioxidant activity of green tea extracts obtained by three different extraction methods: simple maceration, ultrasound extraction and accelerated solvent extraction using six various solvent systems. The quality of the extracts was evaluated by LC-ESI-Q-TOF-MS methodologies and spectrophotometric determinations. The obtained results revealed that catechins&rsquo, extraction efficiency was identical for the three techniques studied. However, larger quantitative differences among the samples were observed when using different solvents. The total content of major catechins and gallic acid was within a very wide range of 10.2&ndash, 842 mg/L. Ethyl acetate was by far the least effective extractant, regardless of the extraction technique used. After all, the solvent system composed of ethanol:water (1:1 v/v) was proven to be the best to recover catechins and to deliver extracts with the highest antiradical activity.

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), &alpha, sesquiphellandrene (B) and a-zingiberene (C). The identification of the components was possible thanks to the application of a TLC&ndash, 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&mdash, HD, pressurized liquid extraction or accelerated solvent extraction&mdash, ASE, shaking maceration&ndash, SM, supercritical fluid extraction&ndash, SFE, and ultrasound-assisted extraction&mdash, 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 &plusmn, 0.025, 0.77 &plusmn, 0.045, and 1.67 &plusmn, 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 &times, 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&mdash, 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&ndash, 347.27 mg GAE/g DW) and showed the most significant antioxidant activity (IC50 = 3.81&ndash, 4.05 &micro, g/mL). C. incanus extracts were also effective tyrosinase inhibitors (30&ndash, 70% inhibition at 100 &micro, g/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&ndash, 199.01 &micro, g/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&ndash, 3.77 at 100 &micro, g/mL), enhancing their anti-hyperpigmentation and anti-melanoma potential.

The review collects together some recent information on the identity and pharmacological properties of magnoflorine, a quaternary aporphine alkaloid, that is widely distributed within the representatives of several botanical families like Berberidaceae, Magnoliaceae, Papaveraceae, or Menispermaceae. Several findings published in the scientific publications mention its application in the treatment of a wide spectrum of diseases including inflammatory ones, allergies, hypertension, osteoporosis, bacterial, viral and fungal infections, and some civilization diseases like cancer, obesity, diabetes, dementia, or depression. The pharmacokinetics and perspectives on its introduction to therapeutic strategies will also be discussed.

Background: In the search for novel antidepressive drug candidates, bioguided fractionation of nonpolar constituents present in the oleoresin from ginger rhizomes (Zingiber officinale Roscoe, Zingiberaceae) was performed. This particular direction of the research was chosen due to the existing reports on the antidepressive properties of ginger total extract. The search for individual metabolites acting as MAO-A inhibitors, which correspond to the apparent effect of the total extract, is the subject of this work. Methods: Hexane extracts from ginger rhizomes were fractionated by using column chromatography (including silica gel impregnated with silver nitrate) and semi-preparative high-performance chromatography. For the activity assessment, an in vitro monoamine oxidase A (MAO-A) inhibition luminescence assay was performed on 10 purified terpenes: 1,8-cineole, α-citronellal, geraniol, β-sesquiphellandrene, γ-terpinen, geranyl acetate, isobornyl acetate, terpinen-4-ol, (E,E)-α-farnesene, and α-zingiberene. Results: Geraniol and (−)-terpinen-4-ol were found to be the strongest enzyme inhibitors with inhibition of 44.1% and 42.5%, respectively, at a concentration of 125 µg/mL. No differences in the inhibition potential were observed for the different groups of terpenes: sesquiterpenes, monoterpenes, or sesquiterpene alcohols; however, the two most active compounds contained a hydroxyl moiety. Conclusions: Terpene constituents from ginger’s extract were found to exhibit moderate inhibitory properties against the MAO-A enzyme in in vitro tests.