bluuebunny/crossref_metadata_2025 huggingface dataset:
Raphanus sativus Sprout Causes Selective Cytotoxic Effect on p53-Deficient Human Lung Cancer Cells in vitro
Authors: Baek Jiwon , Roh Hyun-Soo , Choi Chang-Ik , Baek Kwan-Hyuck , Kim Ki Hyun
Published: March 2019

Raphanus sativus L. (Brassicaceae) is widely consumed in many different forms worldwide. Its sprouts, in particular, are commonly consumed as a health food. R. sativus sprout has recently been shown to have anti-tumor activity on human colon cancer cells, suggesting that it may have potential use in cancer prevention and treatment. The extent of this anti-tumor activity and its underlying mechanisms, however, remain to be investigated in other types of cancer cells. In this study, we showed that the MeOH extract from R. sativus sprout exhibits significant but variable cytotoxic effects on human lung adenocarcinoma cells depending on their p53 status. The MeOH extract decreased the viability of p53-deleted human lung cancer cells (H1299 and Calu-6) by inducing apoptosis; this effect, however, did not occur for wild-type p53 cancer cells (A549), for cells expressing a p53 mutant lacking the C terminus (H1264), or for non-tumor fibroblast cells (NIH3T3). Phytochemical analyses of the MeOH extract allowed us to identify and isolate β-sitosterol as a major component of the MeOH extract. Direct treatment with β-sitosterol significantly reduced the viability of Calu-6 cells, suggesting that it may, in part, contribute to R. sativus sprout's anti-tumor activity. This work provides experimental evidence for a novel biological application of R. sativus sprout in treating human lung cancer, and it identifies the main component involved in this effect, further supporting its potential use as a functional food for cancer management.
AKR1C3 Inhibitory Potency of Naturally-occurring Amaryllidaceae Alkaloids of Different Structural Types
Authors: Hulcová Daniela , Breiterová Kateřina , Zemanová Lucie , Siatka Tomáš , Šafratová Marcela , Vaněčková Nina , Hošťálková Anna , Wsól Vladimír , Cahlíková Lucie
Published: March 2019

Aldo-keto reductase 1C3 (AKR1C3) is an important human enzyme that participates in the reduction of steroids and prostaglandins, which leads to proliferative signaling. AKR1C3 is frequently upregulated in various cancers, and this enzyme has been suggested as a therapeutic target for the treatment of these pathological conditions. The fact that the isoquinoline alkaloid stylopine has been identified as a potent AKR1C3 inhibitor has prompted us to screen a library of diverse types of Amaryllidaceae alkaloids, which biogenetically are isoquinoline alkaloids, on a recombinant form of AKR1C3. From the tested compounds, only tazettine showed moderate AKR1C3 inhibitory potency with an IC50 value of 15.8 ± 1.2 μM. Tazettine is a common Amaryllidaceae alkaloid, which could be used as a model substance for the further development of either analogues or related compounds with better inhibition potency.
Chemical Constituents of the Roots and Rhizomes of Saposhnikovia divaricata and their Cytotoxic Activity
Authors: Yokosuka Akihito , Tatsuno Satoru , Komine Takuma , Mimaki Yoshihiro
Published: March 2019

Phytochemical investigation of the MeOH extract of the roots and rhizomes of Saposhnikovia divaricata (Umbelliferae) resulted in the isolation of six chromons (1-6) and five polyacetylene derivatives (7-11). Compounds 9 and 11 were isolated from S. divaricate for the first time. The chromon derivatives (1-6) were evaluated for their cytotoxic activity against HL-60 human promyelocytic leukemia cells. Compound 1 (3′- O-angeloylhamaudol) showed the most potent cytotoxic activity with an IC50 value of 4.41 μM and was found to induce apoptotic cell death in HL-60 cells. The loss of mitochondrial membrane potential, release of cytochrome c into the cytoplasm, and activation of caspase-9 in the 1-treated HL-60 cells suggests that 1 induces apoptosis through the mitochondrial-dependent apoptotic pathway.
Cytotoxic Activity of Compounds from Styrax obassia
Authors: Cao Thao Quyen , Lee Bo Mi , Jung Yeon Woo , Nguyen Van Thu , Kim Jeong Ah , Min Byung Sun
Published: March 2019

Cancer is a major public health burden in both developed and developing countries. Plant-derived compounds have played an important role in the development of useful anti-cancer agents. The current study was designed to evaluate the cytotoxic activity of chemical compounds from the stem bark of Styrax obassia. Seven known compounds (1–7) were isolated and identified. Compound 2 exhibited cytotoxic activity against the breast cancer cell line MCF-7 with an IC50 of 27.9 μM, followed by the human cervical cancer cell line Hela with an IC50 of 23.3 μM, and the human promyelocytic leukemia cell line HL-60 with an IC50 of 47.8 μM. Compound 7 exhibited cytotoxicity against Hela cells with an IC50 of 16.8 μM, followed by MCF-7 cells with an IC50 of 53.5 μM. This is the first study to investigate the significant anti-tumor properties of isolated compounds from the stem bark of S. obassia.
Germination and Clonal Propagation of the Endemic Shrub Corema album, a Vulnerable Species with Conservation Needs and Commercial Interest
Authors: Álvarez-Cansino Leonor , Zunzunegui María , Barradas Mari Cruz Díaz
Published: March 2019

In this study, we aimed to explore regeneration possibilities of Corema album (L.) D. Don by determining germination mechanisms and testing vegetative propagation methods. We analyzed seed viability under natural conditions, carried out germination treatments and a greenhouse experiment to study clonal propagation. We confirmed that C. album seeds present physiological dormancy, broken by ingestion by natural dispersers (rabbits and foxes), and that seed viability under natural conditions is lost after one year. In vitro germination was better achieved with a 200 ppm gibberellic acid treatment. Clonal propagation proved to be a successful technique for the production of C. album. Treating cuttings with IBA 0.2, w/v, at 20% resulted in the highest rooting percentage, while planting rooted cuttings in a substrate of perlite with vermiculite 1:1 was essential for plant survival. Our results show that both germination pretreatments and cutting propagation are powerful tools for the production of this valuable species. Both methods could be incorporated for population regeneration in natural habitats, and for the potential establishment of the species as a new crop for consumption and pharmacological purposes.
In vitro and in vivo Methods for the Evaluation of Natural Products against Dermatophytes
Authors: Velázquez-Dávila Lily A. , Galindo-Rodríguez Sergio A. , Pérez-López Luis A. , González-González M. Gloria , Álvarez-Román Rocío
Published: March 2019

Dermatomycoses are infections caused by fungi called dermatophytes; these affect 20–25% of the world population and the incidence continues to grow each year. Recently, an alternative for the treatment of these diseases is the use of natural products, thanks to the fact that they possess great chemical diversity and thus biological activity. However, to understand the therapeutic potential of natural products, their microbiological assessment presents certain limitations. Currently, there is no established reference method to determine the antifungal capacity in vitro and in vivo of natural products (i.e., essential oils). This review focuses on describing the various microbiological methods as well as the many adaptations used to evaluate the antifungal activity of natural products both in vitro and in vivo. In addition, the antifungal evaluation of natural products formulated in creams, gels, nanoemulsions, nanocapsules and solid lipid nanoparticles is included.
Cell Culture of Bursera Linanoe in a Stirred Tank Bioreactor for Production of Linalool and Linalyl Acetate
Authors: Pavón-Reyes Leticia , Evangelista-Lozano Silvia , Sepúlveda-Jiménez Gabriela , Ávila Víctor Chávez , Rodríguez-Monroy Mario
Published: March 2019

Bursera linanoe cell suspension cultures were initiated from callus grown in Murashige and Skoog medium supplemented with naphthalene acetic acid (3.0 mg L−1) and 6-benzylaminopurine (0.5 mg L−1). In flasks, B. linanoe cell cultures grew over a 9 day period, reaching a maximum biomass of 11.16 g DW L−1. Throughout the growth phase, cell viability was constant at 60 – 70%. In contrast, B. linanoe cells growing in a bioreactor achieved a maximum biomass of 22.26 g DW L−1 (after 7 days), and cell viability was constant at 75 - 85%. Production of linalool and linalyl acetate in the bioreactor (3.02 and 2.40 mg g−1 DW, respectively) was significantly greater than that achieved from cells in flask cultures (1.05 and 0.97 mg g−1 DW, respectively). B. linanoe cell suspension culture has potential as an alternative method for the production of essential oils.
Antifeedant Activity of Neo-clerodane Diterpenoids from Scutellaria Altissima Against Colorado Potato Beetle Larvae
Authors: Bozov Petko I. , Georgieva Yoana P.
Published: March 2019

Fourteen neo-clerodane diterpenoids isolated from Scutellaria altissima ( Lamiaceae) were tested for insect antifeedant activity against Leptinotarsa decemlineata Say. Potato leaf disks treated with small amounts of the compounds (concentration 1000, 100, 10 ppm) resulted in good to very good antifeedant activity. Clerodin (1), scutecyprin (11) and 11-epi-scutecolumnin C (12) showed strong feeding inhibition at 1000 ppm and exhibited significant antifeedant activity at a concentration of 100 ppm. Activity was established by calculating the feeding ratio (FR) between the consumed areas of treated disks (CTD) and control disks (CCD). For comparison, FR50 values were determined as the FR at a CCD of 50%. Structural features of the compounds associated with the changes in activity and structure-antifeedant activity relationships are discussed. For the first time the anti-feedant activity has been evaluated of neo-clerodane diterpenoids with an unusual R-configuration of the carbon atom C-11.
Two New C19-Diterpenoid Alkaloids from Aconitum Nagarum var. Lasiandrum
Authors: Wen Fu-li , Jiang Ying-Ying , Tang Hua , Chen Dong-Lin , Wang Feng-Peng
Published: March 2019

Continuous investigations of the roots of Aconitum nagarum var. lasiandrum led to the isolation of two new C19-diterpenoid alkaloids, lasiandrine (1) and lasiandroline (2). Their structures were elucidated on the basis of extensive interpretation of spectroscopic and mass spectrometric data.
Physiologically Active Compounds in Four Species of Phellinus
Authors: Sułkowska-Ziaja Katarzyna , Maślanka Anna , Szewczyk Agnieszka , Muszyńska Bożena
Published: March 2019

The content of two groups of compounds with biological activity (non-hallucinogenic indole compounds and free phenolic acids) were analyzed in extracts of fruiting bodies of four species of Phellinus: P. igniarius, P. pini, P. pomaceus and P. robustus. The presence of indole compounds in methanolic extracts was analyzed by high-performance liquid chromatography and thin-layer chromatography coupled with densitometric detection. Three metabolites (serotonin, tryptamine, and L-tryptophan) were identified. The contents of individual indole compounds ranged from 1.70 (tryptamine in P. robustus) to 8.32 mg x 100 g1 dry weight (L-tryptophan in P. robustus). Four free phenolic acids were detected in methanolic extracts by the HPLC method. The total content ranged from 9.9 mg x 100 g1 DW (P. igniarius) to 32.5 mg x 100 g1 DW (P. robustus).
Simultaneous HPTLC Determination of Rhein and Aloe-emodin in Senna Alata Leaves from Thailand and their Commercial Products
Authors: Chewchinda Savita , Sithisarn Pongtip
Published: March 2019

A high performance thin layer chromatographic (HPTLC) method was developed and validated for simultaneous determination of rhein and aloe-emodin, major anthraquinone constituents, in S. alata leaves. The separation was performed on a silica gel 60 F254 HPTLC plate using ethyl acetate: methanol: water (100:17:10, v/v/v) as the development system. Validation of the analytical method for rhein and aloe-emodin promoted acceptable parameters. Good linearity in the range of 40–480 ng/band was obtained while intra-day and inter-day precisions were shown to be precise with relative standard deviations of less than 5%. The average percentage recoveries of rhein and aloe-emodin were 98.8% and 98.9%, suggesting acceptable accuracy. The content of rhein and aloe-emodin in S. alata leaves collected from 5 different provinces in Thailand analyzed by the validated HPTLC method were in the ranges of 0.098 ± 0.017 −0.30 ± 0.02%, w/w, and 0.081 ± 0.0006 - 0.34 ± 0.0009 %, w/w, respectively. Five commercial products of S. alata tea available in the market were purchased and analyzed for rhein and aloe-emodin contents. The contents of rhein and aloe-emodin in the tea samples were in the ranges of 0.085 ± 0.004 - 0.23 ± 0.04%, w/w, and 0.096 ± 0.006 - 0.30 ± 0.01 %, w/w, respectively. The HPTLC method is rapid, reliable, sensitive and economical for routine analysis of rhein and aloe-emodin contents in S. alata leaf raw materials and its commercial products.
Hydrogel Containing an Extract of Tormentillae Rhizoma for the Treatment of Biofilm-Related Oral Diseases
Authors: Tomczyk Michał , Sosnowska Katarzyna , Pleszczyńska Małgorzata , Strawa Jakub , Wiater Adrian , Grochowski Daniel M. , Tomczykowa Monika , Winnicka Katarzyna
Published: March 2019

In the present study, hydrogels containing the dried extract of tormentil ( Potentilla erecta (L.) Raeusch., Rosaceae) were designed and qualitatively evaluated regarding their viscosity, thixotropy, and texture properties. As mucoadhesiveness is a crucial factor determining drug retention within the oral cavity, mucoadhesive properties expressed as the work of adhesion and maximum detachment force under the presence of porcine buccal mucosa and two different models of mucoadhesive layers: mucin and gelatin discs were evaluated. The fingerprints of the analyzed tormentil extract were established by using a LC-ESI-MS method. The dominating compounds of the tested extract are oligomeric proanthocyanidins and agrimoniin. This study reveals that designed hydrogels are promising semi-solid delivery systems for the dry extract of tormentil with beneficial mucoadhesive, thixotropic, and texture characteristics and may be utilized as platforms for tormentil delivery to the oral cavity in periodontal diseases. In vitro evaluation of the efficacy of the tormentil hydrogel against cariogenic Streptococcus mutans biofilms was also performed. The hydrogel significantly reduced artificial biofilm formation. For all Streptococci, complete inhibition was revealed at a final concentration of the extract of 2 mg/mL. These beneficial characteristics, as well as the anti-biofilm activity, enable its use for dental care, but further clinical studies are required.
Leguminous Plants in the Indonesian Archipelago: Traditional Uses and Secondary Metabolites
Authors: Bahtiar Anton , Vichitphan Kanit , Han Jaehong
Published: March 2019

Indonesia is one of the richest countries with respect to plants resources. People from various ethnic, language, and religious groups have used the plants as alternative medicines, health foods and beverages for hundreds of years. To establish modern application for these understudied plant resources, ethnopharmacological data from more than 40 leguminous plants in Indonesia, spanning the western to the eastern parts of the Indonesian archipelago, were reviewed. In particular, bioactive secondary metabolites, including flavonoids, were described in detail to promote research into these plants as functional foods, nutraceuticals, and medicines.
Positions of Hydroxyl Groups in Chrysin are Critical for Inhibiting Plasminogen Activator Inhibitor-1 Release from Human Umbilical Vein Endothelial Cells
Authors: Ohkura Naoki , Ando Kumiko , Takata Yuko , Kanai Shiho , Ishibashi Kenichi , Taniguchi Masahiko , Tatefuji Tomoki , Atsumi Gen-ichi
Published: March 2019

Chrysin suppresses the TNFa-induced increase in the secretion of plasma plasminogen activator inhibitor 1 (PAI-1), a risk factor for thrombotic diseases, from human umbilical vein endothelial cells (HUVECs). The present study aimed to determine the association between the location of the hydroxyl groups in chrysin to levels of PAI-1 in the medium of HUVEC stimulated with TNFα, We cultured HUVEC for 3 h in medium containing chrysin or various flavonoids and then stimulated them with TNFα (10 ng/mL) for 12 h. Levels of PAI-1 antigen measured using ELISA showed that chrysin significantly inhibited the PAI-1 increase with an IC50 of 15.6 μM. The flavones, galangin, baicalein, 5-hydroxyflavone, 6-hydroxyflavone, 7-hydroxyflavone and quercetin did not significantly inhibit the PAI-1 increase. Apigenin and luteolin were cytotoxic and thus their ability to inhibit PAI-1 production could not be evaluated. Chrysin also inhibited PAI-1 mRNA expression whereas the other compounds did not. Hydroxyl groups located in the A-5 and A-7 positions were essential for the inhibitory activity, which along with cytotoxicity, was significantly influenced by adding a third hydroxyl group.
Glycosylation and Methylation of Quercetin and Myricetin by Cultured Cells of Phytolacca americana
Authors: Fujitaka Yuya , Shimoda Kei , Kubota Naoji , Araki Minami , Onishi Tatsuya , Nakayama Noriyuki , Ishihara Kohji , Tanigawa Masato , Hamada Hatsuyuki , Hamada Hiroki
Published: March 2019

The glycosylation and methylation of quercetin by cultured plant cells of Phytolacca americana gave quercetin 3- O-β-D-glucoside and isorhamnetin 3- O-β-D-glucoside. Myricetin was glycosylated and methylated to syringetin 3- O-β-D-glucoside by cultured P. americana cells.
Antioxidant Activity and Phenolic Composition of a Red Bean (Phasoelus vulgaris) Extract and its Fractions
Authors: Amarowicz Ryszard , Karamać Magdalena , Dueñas Montserrat , Pegg Ronald B.
Published: March 2019

The activities of the crude acetonic extract of red bean and its two fractions were determined using a β-carotene-linoleate model system as well as the total antioxidant activity (TAA), the total phenolics content (TPC), the DPPH radical-scavenging activity, and the reducing power assays. Results from the in vitro assays showed the highest values when tannins (fraction II) were tested. Specifically, the TAA of the tannins fraction was 4.37 mmol Trolox eq./g fraction; whereas, the crude extract and fraction I were 0.481 and 0.093 μmol Trolox eq./mg extract or fraction, respectively. The content of total phenolics in fraction II was the utmost (612 mg/g); the tannins content, assayed by the vanillin method and expressed as absorbance units at 500 nm per 1 g, was 938. RP-HPLC-PAD-MS profiling revealed the presence of 33 compounds: quercetin arabinoglucoside, quercetin rutinoside, quercetin, p-hydroxybenzoic acid, and kaempferol rutinoside were the most abundant phenolics in the extract.
Synthesis and Bioconversion of Curcumin Analogs
Authors: Martin Glenroy D. A. , McKenzie Cameron , Moore Monica
Published: March 2019

Hydrogenation of curcumin (1), a chemopreventive agent from Turmeric ( Curcuma longa L.) yielded three major compounds: 1,7-bis(4-hydroxy-3-methoxyphenyl)heptane-3,5-dione (2), 5-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)heptan-3-one (3), and 1,7-bis(4-hydroxy-3-methoxyphenyl)heptane-3,5-diol (4). Incubation of compound (2) with Beauveria bassiana ATCC 7159 afforded the hexahydrocurcumin (3) as the sole metabolite while biotransformation of curcumin (1) with B. bassiana gave metabolites 2-4 along with the curcumin-4'-O-4″'-O-methyl-β-D-glucopyranoside (5) and octahydrocurcumin-4'-O-4″'-O-methyl-β-D-glucopyranoside (6). The bioconversion of curcumin (1) with Rhizopus oryzae ATCC 11145 yielded analogs 2-4 while no transformation of curcumin (1) was observed with Aspergillus niger ATCC 16888. The preparation, structural elucidation and biological activities of these metabolites are reported herein.
Antibacterial Activity of 2-(3’,5'-Dibromo-2'-methoxyphenoxy)-3,5-dibromophenol Isolated from Phyllospongia papyracea
Authors: Sun Shi , Canning Corene , Wang Kuiwu , Zhu Wenjun , Yang Fei , Zhang Yifan , Zhou Kequan
Published: March 2019

A principal active antimicrobial compound, 2-(3’,5'-dibromo-2'-methoxyphenoxy)-3,5-dibromophenol, was isolated from the methanol extract of Phyllospongia papyracea via bioassay-guided fractionation and isolation. The crude extract and the purified compound were assayed to determine the minimal inhibitory concentration and minimal bactericidal concentration (MBC) using the broth microdilution method. The purified compound was found to be highly active against Bacillus subtilis and Staphylococcus aureus at MIC=1 μg/mL, Campylobacter jejuni at MIC=2 μg/mL, Pseudomonas aeruginosa at MIC=4 μg/mL, and Streptococcus pneumoniae and Listeria monocytogenes at MIC = 8 μg/mL. The activity of this compound was found to be comparable with antibiotics commonly used to control these species of bacteria. The results establish 2-(3’,5'-dibromo-2'-methoxyphenoxy)-3,5-dibromophenol as a potential lead molecule for the development of antibacterial agents.
Anti-dormant Mycobacterial Activity of Viomellein and Xanthomegnin, Naphthoquinone Dimers Produced by Marine-derived Aspergillus sp
Authors: Kamiya Kentaro , Arai Masayoshi , Setiawan Andi , Kobayashi Motomasa
Published: March 2019

In the course of a search for anti-dormant mycobacterial substances from marine-derived microorganisms, viomellein (1) and xanthomegnin (2) were rediscovered from the active fraction of the culture of a marine-derived Aspergillus sp. together with rubrosulphin (3) and asteltoxin (4) on the guidance of bioassay-guided separation. In particular, compound 1 showed higher activity against the dormant than against actively growing Mycobacterium bovis BCG and weak activity against M. smegmatis. Furthermore, evidence that compound 1 did not directly bind to plasmid DNA suggests its anti-mycobacterial activity differs from its direct chelating effect on the mycobacterial genome.
Elionurus tristis Essential Oil: GC-MS Analysis and Antioxidant and Antituberculosis Activities
Authors: Yedomon Brice Hervé , Saves Isabelle , Mtimet Narjes , Raoelison Emmanuel Guy , Constant Patricia , Daffé Mamadou , Bouajila Jalloul
Published: March 2019

Essential oil was obtained in a yield 1.1%, w/w, by steam distillation of Elionurus tristis leaves from Madagascar. The chemical composition was analyzed qualitatively and quantitatively by GC-MS and GC-FID, respectively. To the best of our knowledge, this is the first chemical analysis of this essential oil. Seventy-three compounds were identified, corresponding to 94.9% of the total essential oil. The principal compounds were sesquiterpenes and the more represented were β-gurjunene (18.4%), neoclovene (15.8%) and nootkatone (10.4%). Through a comparative study, we observed a large variability between the components of E. tristis essential oil and those from others species of the same genus. Evaluation of the antioxidant (ABTS and DPPH assays) and anti-tuberculosis activities of the essential oil showed weak antioxidant potency but an interesting anti-tuberculosis activity with a MIC of 32 mg/L. This activity prompted us to evaluate individually the major components for the treatment of tuberculosis.
Lathyrane Diterpenes from the Latex of Euphorbia laurifolia
Authors: Durán-Peña María Jesús , Flores-Giubi María Eugenia , Botubol-Ares José Manuel , Escobar-Montaño Felipe , Macías-Sánchez Antonio J. , Echeverri Luis F. , Collado Isidro G. , Hernández-Galán Rosario
Published: March 2019

Two new macrocyclic diterpenes, 2- epi-latazienone (4) and 15β-acetoxy-7β-nicotinoyloxy-3β8α-di-(2-methylpropanoyloxy)–4αH,9αH,11αH-lathyra-5 E,12 E-dien-14-one (5), and three known lathyrane-type diterpenes (1-3) were isolated from Euphorbia laurifolia latex. Their structures were determined on the basis of a detailed analysis of their 1D and 2D NMR spectroscopic and mass spectral data.
Pentacyclic Triterpenoids from Maytenus cuzcoina
Authors: Reyes Carolina P. , Jiménez Ignacio A. , Bazzocchi Isabel L.
Published: March 2019

Phytochemical analysis of the root bark extract of Maytenus cuzcoina (Celastraceae) led to the isolation and characterization of sixteen triterpenoids with a 6/6/6/6/6 pentacyclic system, including the new 22α-hydroxy-29-methoxy-3β-tetradecanoate-olean-12-ene, and 3β,24β-epoxy-29-methoxy-2α,3α,6α-trihydroxy- D:A-friedelane that is reported for the first time as a natural product. This is the first instance of the isolation of a tetradecanoate triterpene ester from a Celastraceae species. The structures were elucidated on the basis of spectrometric and spectroscopic methods, including 1D and 2D NMR techniques.
New Fluvirucinins C1 and C2 Produced by a Marine Derived Actinomycete
Authors: Costa Margarida , Zúñiga Paz , Peñalver Ana M , Thorsteinsdottir Margrét , Pérez Marta , Cañedo Librada M , Cuevas Carmen
Published: March 2019

Two new fluvirucin aglycones, named fluvirucinins C1 and C2 (1-2), have been isolated from the ethyl acetate mycelial cake extract of the fermentation broth of a marine sponge-associated actinomycete. Fluvirucinins C1 (1) and C2 (2) represent a new type of 14-membered macrolactam aglycon, structurally related with the common aglycon of the known fluvirucins. Their structures were elucidated on the basis of 1D and 2D NMR analyses, as well as HRESIMS experiments. The antimicrobial and cytotoxic activities of compounds 1 and 2 have been evaluated, but no significant activities found for fluvirucinins C1 and C2.
Phytochemicals and Biological Activities of Laurel Tree (Laurus nobilis)
Authors: Alejo-Armijo Alfonso , Altarejos Joaquín , Salido Sofía
Published: March 2019

This review summarizes the chemical composition reported up to date on Laurus nobilis L. (Lauraceae), an evergreen shrub or tree cultivated for its aromatic leaves and ornamental interest. It has been focused on non-volatile phytochemicals such as sesquiterpene lactones, flavonoids and proanthocyanidins, among others. Moreover, biological activities of laurel extracts and pure compounds have also been reviewed.
Encapsulation of Active Molecules in Microparticles Based on Natural Polysaccharides
Authors: Dalmoro Annalisa , Cascone Sara , Lamberti Gaetano , Barba Anna Angela
Published: March 2019

This mini-review is focused on an engineering approach to produce polysaccharides-based microparticles for nutraceutical and pharmaceutical purposes. A brief introduction about the fundamental properties of polysaccharides and their use as microsystems in food, cosmetics, and pharmaceutics, and a summary of the most important methods of preparation are described. Then, a novel method based on the ultrasonic atomization of solutions of the two most used polysaccharides, alginate and chitosan, followed by ionotropic gelation to produce enteric microsystems for oral administration and, in particular, the basic mechanisms of the encapsulation of molecules with different size and hydrophilicity, are investigated. This mini-review will show therefore the pathway to correctly design a polysaccharide microcarrier for the encapsulation of active molecules with different properties: from the choice of materials features, to the selection and the optimization of production methods with the aim to reduce costs and energy (ionotropic gelation coupled to ultrasonic atomization), to the control of the final carrier size (by purposely developed predictive models), at last to the optimization of encapsulation properties (predicting by model the drug leakage and providing different solutions to avoid it).
Lutein Regulates the Expression of Apoptosis-related Genes and Stem Cell Markers in A549 Human Lung Cancer Cells
Authors: Yamagata Kazuo , Fujiwara Ayame , Onodera Daiki , Motoki Tagami
Published: March 2019

The BCL2 family has both pro-apoptotic and anti-apoptotic functions. Furthermore, stem cell markers such as Oct4, SOX2, and NANOG enhance cancer cells’ self-renewal, resistance to anti-cancer drugs and clonal growth. Therefore, selective inhibition of BCL2 genes and downregulated expression of stem cell markers should reduce the survival of cancer cells. Previous studies have reported that lutein, a carotenoid pigment present in fruits and vegetables, can inhibit cancer cells. However, the inhibitory effects of lutein on cancer cells have not been investigated sufficiently. In this study, we used gene expression analysis by polymerase chain reaction (PCR) and Western blotting to show that lutein regulates the expression of genes involved in apoptosis and several stem cell marker genes in a human lung cancer cell line, A549. Lutein induced gene expression of pro-apoptotic BAX and CAS3 and reduced the level of the anti-apoptotic gene BCL2. Furthermore, protein expression of BCL2 and BAX was regulated by treatment with lutein. Lutein also inhibited SOX2 and NANOG gene expression in A549, but not POU5F1. In addition, lutein reduced gene expression of SLCA11, but induced CD44 and CD133 gene expression. These results indicated that lutein inhibits several events associated with apoptosis regulation in a BCL2 family-dependent pathway.
Histochemical and Phytochemical Study of Amburana cearensis (Fabaceae) Seed Oil
Authors: Pereira Margelly P. , de Melo-Júnior Afrânio F. , Royo Vanessa de A. , Mercadante-Simões Maria Olivia , da Fonseca Francine S. A. , Ferraz Vany P. , de Oliveira Dario A. , Menezes Elytânia V. , Brandão Murilo M.
Published: March 2019

Amburana cearensis seed oil is used in traditional medicine to treat respiratory diseases. However, investigations of the chemical compounds present in this oil are necessary to prove their effectiveness. Thus, we aimed to analyze the compounds present in A. cearensis seeds it was analyzed by histochemical and phytochemical tests. Fatty acids profiles were analyzed by gas chromatography coupled with flame ionization detector, which detected the presence of high concentrations of oleic (50.1%), palmitic (15.7%), linoleic (9.7%) acids and linolenic (5.0%). Volatile components were analyzed by headspace extraction and gas chromatography coupled with mass spectrometry, with emphasis on the presence of a coumarin, which may be associated with the bronchodilator effect of the oil. Histochemical analysis of the seed oil revealed presence of alkaloids in the cell vacuoles and lipophilic components in drops in the cell cytoplasm. The analysis of A. cearensis seed oil contributed to the understanding of the therapeutic actions of the species and to the prospection of promising compounds for the development of new drugs.
The Properties of the Ulcinj Peloid make it Unique Biochemical Laboratory Required for the Treatment of Problematic Skin and Health Care
Authors: Potpara Zorica , Pantovic Snezana , Duborija-Kovacevic Natasa , Tadic Vanja , Vojinovic Tanja , Marstijepovic Nada
Published: March 2019

The aim of this study was to investigate the physicochemical properties of peloid, its mineralogical composition and its antimicrobial activity, including the presence of algae, with the aim of considering its dermo-cosmetic application, such as anti-skin aging and treatment. Physicochemical analysis showed that peloid from Ulcinj coast, contains minerals, necessary for smooth performance of skin functions, as well as, the whole body. A studied peloid sample showed significant antimicrobial activity of Candida albicans strain, and the presence of algae of Bacillariophyta division, known to have a beneficial effect on skin health. Results of examination of peloid from Ulcinj locality, recommended it as a high quality natural substance applicative in dermo-cosmetic preparations for treatment of problematic skin.
Evaluation of the Drug-like Properties of Kaempferol, Chrysophanol and Emodin and their Interactions with EGFR Tyrosine Kinase - An in silico Approach
Authors: Sreelakshmi Vasudevanpillai , Raj Navya , Abraham Annie
Published: March 2019

In this study, a molecular docking was performed on EGFR tyrosine kinase with plant phenolic compounds kaempferol, chrysophanol and emodin; identified from Cassia tora, an edible plant employed for eye diseases traditionally. The results illustrated that all the compounds have strong binding abilities with epidermal growth factor receptor and validated the reported anticataractogenic potential of C. tora leaves. Further, the compounds also satisfied the criteria for being a drug through its structural features. Taken together, it was proposed that the compounds; kaempferol, chrysophanol and emodin might be helpful for further drug design and development and could be employed as efficient lead compounds in ophthalmic drug formulations.
Effect of Levopimaradiene on Terpene Trilactones Biosynthesis and Gene Expression Profiling in Ginkgo biloba Cells
Authors: Zhu Jianhua , Wang Pu , Qian Minghua , Liang Chuxin , Zi Jiachen , Yu Rongmin
Published: March 2019

Ginkgolides (GKs) and Bilobalide (BB) are rare terpene trilactones obtained from Ginkgo biloba, but their biosynthetic pathway is still unclear. In this paper, effects of levopimaradiene (LP) on increasing the production of terpene trilactones of G. biloba dedifferentiated cells (DDCs) and cambial meristematic cells (CMCs) were reported. The productions of ginkgolide A (GA) and ginkgolide B (GB) were 1.61 and 1.32 folds larger than that of the control groups when G. biloba DDCs was treated with LP, and the productions of ginkgolide C (GC) and BB reached 234 and 161 μg L−1 after treated with LP for 60 h. The production of GA, GB, GC and BB was 2.03, 1.43, 1.22 and 1.19 folds larger than that of the control groups in LP-treated CMCs groups. The results demonstrated that BB could be produced from the methylerythritol 4-phosphate (MEP) pathway. qRT-PCR experiments showed that LP was a significant precursor manipulated the biosynthesis of terpene trilactones via affecting the transcript levels of several related genes in the MEP pathway.
New Norcucurbitane Triterpenoids from Momordica charantia var. abbreviata
Authors: Chen Chiy-Rong , Liao Yun-Wen , Kuo Yueh-Hsiung , Hsu Jue-Liang , Chang Chi-I
Published: March 2019

Two new 27-norcucurbitane triterpenoids, 5β,19-epoxy-3β-hydroxy-19( S)-methoxy-27-norcucurbita-6,23( E)-dien-25-one (1) and 3β-hydroxy-25-oxo-27-norcucurbita-6,23( E)-dien-5β,19-olide (2), together with one known cucurbitane triterpene, 5β,19-epoxycucurbita-6,23( E)-diene-3β,25-diol (3), were isolated from the fruits of Momordica charantia var. abbreviata. Their structures were elucidated by spectroscopic methods including EI-MS, 1H, 13C, and 2D NMR data and comparison with the data of known analogues.
Two New Alkaloids from Polyalthia nemoralis
Authors: Oanh Nguyen Thi Tu , Tung To Hai , Hue Cao Thi , Thanh Le Nguyen , Thao Do Thi , Hang Nguyen Thi Minh
Published: March 2019

A new azaoxoaporphine alkaloid, 8,9-dimethoxysampangine (1), and a new naphthyridine alkaloid, 7-methoxy-8-hydroxyeupolauridine (2), along with two known azaoxoaporphine alkaloids, sampangine (3) and 9-methoxysampangine (4), were isolated from the EtOAc extract of the barks of Polyalthia nemoralis. Their structures were established on the basis of spectral evidences. Compound 1 exhibited significant cytotoxicity against KB, MCF7, LU-1, HepG2, LNCap, SW626 and SW480 cancer cell lines with IC50 values in the range of 5.06±0.04-7.61±0.06 μM.
Normonanchocidins G and H, New Pentacyclic Guanidine Alkaloids from the Far-Eastern Marine Sponge Monanchora pulchra
Authors: Tabakmakher Kseniya M. , Makarieva Tatyana N. , Denisenko Vladimir A. , Popov Roman S. , Kuzmich Aleksandra S. , Shubina Larisa K. , Lee Hyi-Seung , Lee Yeon-Ju , Fedorov Sergey N.
Published: March 2019

Two new pentacyclic guanidine alkaloids, normonanchocidins G (1) and H (2) containing an unusual ω-2-hydroxy fatty acid moiety were isolated from the Far-Eastern marine sponge Monanchora pulchra. The structures of 1 and 2 were determined by 1D- and 2D-NMR spectroscopic and mass spectrometric data interpretation. Compounds 1 and 2 exhibit potent cytotoxic activities against human leukemia THP-1, HL-60 cells, human cervical epithelioid carcinoma HeLa cells and also have high impact on ability of HeLa cells to migrate.
Screening of Spice Extracts Possessing Anti-Acetylcholinesterase Activity and Active Principle of Bitter Ginger, Rhizome of Zingiber zerumbet
Authors: Murata Kazuya , Ishida Yusuke , Nishio Arisa , Nakagawa Sayaka , Kawamoto Hirokazu , Matsuda Hideaki
Published: March 2019

In our research program for investigating anti-dementia agents from natural plant resources, we screened extracts from 15 spice samples. Among the plant extracts tested, ethyl acetate extract prepared from rhizome of Zingiber zerumbet showed potent activity. Activity-guided purification led to determination of afzelin and its acetylated compound as the active principles. Afzelin showed moderate inhibitory activity against acetylcholinesterase and may also be expected to possess anti-butyrylcholinesterase activity. This is the first report to reveal the anti-cholinesterase activities of ethyl acetate extract of Z. zerumbet and afzelin. Furthermore, Z. zerumbet may be a potential therapeutic agent for the improvement of dementia, especially Alzheimer's disease.
Myrislignan, a Growth Inhibitor from the Roots of Citronella grass
Authors: Suwitchayanon Prapaipit , Suenaga Kiyotake , Iwasaki Arihiro , Kato-Noguchi Hisashi
Published: March 2019

A phytotoxic compound was isolated from the root extracts of Cymbopogon nardus by bioassay-guided purification and characterized to be myrislignan. Myrislignan significantly inhibited seedling growth of cress at a concentration greater than 100 μM (p < 0.05). The concentrations required for 50% growth inhibition of myrislignan on hypocotyl and root growth of cress were 429 μM and 517 μM, respectively. The inhibition on seedling growth indicated that myrislignan had a phytotoxic activity and may contribute to the phytotoxic effect of C. nardus.
A New Stilbene from the Root of Cassia sieberiana D.C. (Fabaceae)
Authors: Jibril Saidu , Sirat Hasnah Mohd , Basar Norazah
Published: March 2019

A new stilbene (1) was isolated from the root of Cassia sieberiana D. C. together with thirteen known compounds, one stilbene (2), three flavonoids (3–5), six anthraquinones (6–11), two triterpenes (12–13), and phytosterol (14). Their structures were identified using spectroscopic techniques and by comparison of the spectral data with those previously reported in the literature. Compounds 10 – 13 were isolated from C. sieberiana for the first time. Compounds 1, 2 and 3 exhibited significant inhibitory activity on 15-lipoxygenase with IC50 values of 2.62, 1.27 and 0.98 μM, respectively. Compounds 2 and 3 showed acetylcholinesterase inhibitory activity with IC50 values of 10.57 and 2.89 μM, respectively.
Chemical Structure of an Acylated Oleanane-type Triterpene Oligoglycoside and Anti-inflammatory Constituents from the Flower Buds of Camellia sinensis
Authors: Ohta Tomoe , Nakamura Seikou , Matsumoto Tomoko , Nakashima Souichi , Ogawa Keiko , Matsumoto Takahiro , Fukaya Masashi , Yoshikawa Masayuki , Matsuda Hisashi
Published: March 2019

A new acylated oleanane-type triterpene oligoglycoside, floratheasaponin K (1), was isolated together with 11 known compounds including floratheasaponins D (2)–G (5), and I (6), chakasaponin V (7), and assamsaponin E (8) from the flower buds of Camellia sinensis cultivated in India. The chemical structure of floratheasaponin K (1) was elucidated on the basis of chemical and physicochemical evidence. In addition, chakasaponins V (7) and I (13) significantly inhibited nitric oxide (NO) production in lipopolysaccharide- (LPS) activated RAW264.7 cells without cytotoxicity.
The Aroma Profiles of Thai Green Teas Derived from Two Varieties, Chinese and Assam
Authors: Hasegawa Toshio , Hayakawa Yuka , Chueamchaitrakun Piyaporn , Takahashi Atsushi , Nakajima Kenta , Fujihara Takashi
Published: March 2019

Camellia sinensis cultivated for tea has two varieties: Camellia sinensis var. sinensis (Chinese variety) and Camellia sinensis var. assamica (Assam variety). Japanese green teas are mainly produced from the Chinese variety, whereas Thai green teas are made from both varieties. The odors of Thai green teas made from each variety differ from each other and are also distinct from that of Japanese green tea. Here, we investigated the characteristics of the aroma of Thai green teas (Chinese and Assam varieties) and Japanese green tea (Chinese variety) following fractional distillation of their hexane extracts. Each fraction was analyzed by gas chromatography-olfactometry (GC-O) and gas chromatography-mass spectrometry (GC-MS). We found that the rich aroma characteristics of Thai green tea depend on whether the Chinese or the Assam variety is used.
Rose Mentioned in the Works of Scientists of the Medieval East and Implications in Modern Science
Authors: Başer K. Hüsnü Can
Published: March 2019

Fragrant roses (e.g., Rosa damascena, R.gallica, R. centifolia) have been mentioned in ancient texts written by scientists of the Medieval East such as Al-Kindi (9th CE), Al-Dinawari (9th CE), Rhazes (9th CE), Az-Zahrawi (10th CE), Ibn Sina (11th CE), Al-Mizza (14th CE), and Ad-Dimasqi (14th CE). The great physician Ibn Sina emphasized the beneficial effects of rose fragrance on the heart and the brain. He praised rose water's effects on mind and spirit, and its beneficial effects on brain function and cognitive power. Modern studies have provided scientific evidence for this information.
Preventive Effect of Abietic Acid against Skin Cancer of Mice
Authors: Yang Nianyun , Tian Lijuan
Published: March 2019

The preventive effect of abietic acid on skin cancer in mice was investigated in this study. Skin cancer mice model was caused by the combination of UVC and DMBA, and abietic acid was meanwhile intervened. The histopathology features of skin dyed HE staining and immunohistochemical staining were observed to explore tumor formation and skin morphological alteration, and MMP-1, MMP-3, CK10 and CK5/6 were examined. Abietic acid treatment had an obvious effect on experimental mice, and decreasing the expression of the above MMPs and CKs might be one of the possible mechanisms of the therapy.
Anthocyanin Contents Enhancement with Gamma Irradiated Mutagenesis in Blackberry (Rubus fructicosus)
Authors: Won Ryu Hyung , Cho Byoung Ok , Ryu Jaihyunk , Jin Chang Hyun , Kim Jin-Baek , Kang Si Yong , Han Ah-Reum
Published: March 2019

Effects of radiation processing on the endogenous phytochemical production in blackberry ( Rubus fructicosus L.) were investigated through a metabolites analysis, using high-performance liquid chromatography with a diode array detector and a triple quadrupole mass spectrometer (HPLC-DAD-ESI-MS/MS). Four mutant cultivar lines (B, C, D, and E) were developed through the treatment of various doses of gamma irradiation (80, 60, 40, and 20 Gy) on the control blackberry cultivar (V3). These mutant cultivar lines were selected according to their different morphological variations in leaf shape and branch color. In the present study, we performed quantitative analyses of the four standard compounds in blackberry mutant cultivars: cyanidin-3- O-glucoside, cyanidin-3- O-xyloside, cyanidin-3- O-malonylglucoside, and cyanidin-3- O-dioxalylglucoside. The HPLC fingerprints displayed different profiles for six blackberry cultivar lines, demonstrating that the accumulation of total anthocyanins was affected by the gamma irradiation. The contents of cyanidin-3- O-glucoside and cyanidin-3- O-xyloside were high in the gamma-irradiated mutant cultivars of blackberries, compared to those of the control cultivar (V3) and the cross breeding cultivar ( R. fructicosus × R. parvifolius; CB). Cyanidin-3- O-malonylglucoside and cyanidin-3- O-dioxalylglucoside were also analyzed for their quantification in six cultivar lines, as metabolites contributing to the discrimination of six cultivar lines. Among gamma irradiated mutant blackberry cultivars, the highest dose level of gamma irradiation (80 Gy) resulted in the highest cyanidin-3- O-glucoside content enhancement. Therefore, these results can be useful to determine the optimized gamma irradiated value at which anthocyanins reaches an abundant level in Rubus species.
Antioxidant Metabolites from the Stems of Bakeridesia gaumeri
Authors: Escalante-Erosa Fabiola , Ruiz-Vargas Javier A. , Gómez-Guzmán Alonso , Waltenberger Birgit , Stuppner Hermann , Peña-Rodríguez Luis M.
Published: March 2019

Bakeridesia gaumeri is an endemic plant of the Yucatan peninsula, where it is used in traditional medicine for the treatment of dysentery, enterocolitis and diarrhea. The stem extract of the plant showed significant antioxidant activity in the DPPH free radical scavenging assay. Bioassay-guided fractionation of the crude extract resulted in the isolation and identification of 7-hydroxycadalenal (1, EC50 0.85 ± 0.06 mM) and trans-clovamide (2, EC50 0.15 ± 0.01 mM) as the metabolites responsible for the antioxidant activity of the crude extract.
LC-MS-based Screening of East Indian Sandalwood Oil for Mycobacterium tuberculosis Shikimate Kinase and Plasmodium falciparum Thioredoxin Reductase Inhibitory Activities
Authors: Rants'o Thankhoe A. , Alturki Mansour , Levenson Corey , Calderón Angela I.
Published: March 2019

M. tuberculosis shikimate kinase ( MtSK) and P. falciparum thioredoxin reductase ( PfTrxR) represent promising drug targets in tuberculosis and malaria therapy respectively. East Indian Sandalwood oil (EISO) has many reported therapeutic benefits including antibacterial and antiplasmodial effects. The aim of this study was to screen EISO for MtSK and PfTrxR inhibition as potential mechanisms of antimycobacterial and antiplasmodial activities. Liquid chromatography-mass spectrometry (LC-MS) functional assays were used to assess MtSK and PfTrxR inhibition. In this study, EISO displayed antitubercular activity against M. tuberculosis H37Rv at MIC value of 0.002% v/v. Subsequently preliminary screening of the MtSK inhibition by EISO showed an IC50 value of 0.015% v/v. Additionally, EISO presented 90% inhibition of PfTrxR at 0.01% v/v suggesting a potential mechanism of action for reported antimalarial activity.
Simultaneous Quantification of a Herbal Combination of Pueraria lobata, Salvia miltiorrhiza and Panax notoginseng by Rapid Resolution Liquid Chromatography
Authors: Yan Shu-Chao , Ma Jie , Huang Qian-Qian , Mani Ana , Cai Ya-ling , Chen Chun-xue , Yin Chun-Ping , Ma Yuan-Chun
Published: March 2019

Pueraria lobata, Salvia miltiorrhiza and Panax notoginseng are traditional Chinese medicines which have been used for thousands of years either singly or in combination. However, the quality of formulas containing either all or part of the three herbs is, at present, controlled by only one or two easily detectable compounds.. A rapid resolution liquid chromatography (RRLC) method has been developed for the quality control of the three herbs in combination through ten active ingredients originating from the raw herbs. The analysis was achieved in a run of less than 25 minutes. Using the same method, the finger-prints of the three herbs are detectable in the chromatogram, and so the method could be applied for identification of different species in the same genus. Four formula preparations {xinkeshu capsule (XKSC), xinkeshupian (XKSP), fufang-danshenpian (FFDSP), and naodeshengpian (NDSP)} were analyzed by this new RRLC method. Controlling only one or two easily detectable ingredients is far from enough to assure the quality of the formula preparations. However, controlling multiple ingredients originating from the raw herbs and their ratios is an effective and feasible approach to solve this problem.