Showing papers in "Natural Product Communications in 2016"
TL;DR: A rapid and sensitive analytical method was developed using reverse phase high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry for qualitative analysis to determine the array of bioactive phytochemicals and their variations in different plant parts.
Abstract: Terminalia arjuna is a medicinal plant used in ethnomedicine and the codified traditional medicine. A number of active constituents are reported, but there is no information on the whole range of gallic and ellagic acid derivatives present in this plant A rapid and sensitive analytical method was developed using reverse phase high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (HPLC-ESI-QTOF-MS/MS) for qualitative analysis to determine the array of bioactive phytochemicals and their variations in different plant parts viz. bark, unripe fruit, ripe fruit, leaf, root and stem. Separation was performed on a Thermo Betasil C8 column (250 mm x 4.5 mm, 5 µm) with a mobile phase consisted of 0.1% formic acid aqueous solution and acetonitrile at a flow rate of 0.5 mL/min in 55 min. A wide range of constituents of T. arjuna were characterized and broadly grouped as 27 gallic acid and 52 ellagic acid derivatives.
83 citations
TL;DR: The results suggest a new ecofriendly and economically sustainable method for obtaining chestnut fractions with differentiated, stable and reproducible chemical compositions, which can be marketed for innovative uses in several sectors.
Abstract: Sweet Chestnut (Castanea sativa Mill.) wood extracts, rich in Hydrolyzable Tannins (HTs), are traditionally used in the tanning and textile industries, but recent studies suggest additional uses. The aim of this work is the HPLC-DAD-ESI-MS characterization of Sweet Chestnut aqueous extracts and fractions obtained through a membrane separation technology system without using other solvents, and the evaluation of their antioxidant and antiradical activities. Total tannins range between 2.7 and 138.4 mM; gallic acid ranges between 6% and 100%; castalagin and vescalagin range between 0% and 40%. Gallic Acid Equivalents, measured with the Folin-Ciocalteu test, range between 0.067 and 56.99 g/100 g extract weight; ORAC test results for the marketed fractions are 450.4 and 3050 µmol/g Trolox Equivalents/extract weight. EC₅₀ values, measured with the DPPH test, range between 0.444 and 2.399 µM. These results suggest a new ecofriendly and economically sustainable method for obtaining chestnut fractions with differentiated, stable and reproducible chemical compositions. Such fractions can be marketed for innovative uses in several sectors.
42 citations
Journal Article•
TL;DR: This paper makes a review of the botanical, chemical, pharmacological and clinical propierties of the most investigated Peruvian medicinal plants.
Abstract: It is estimated that there are as many as 1400 plant species currently used in traditional Peruvian medicine; however, only a few have undergone scientific investigation. In this paper, we make a review of the botanical, chemical, pharmacological and clinical propierties of the most investigated Peruvian medicinal plants. The plant species selected for this review are: Smallanthus sonchifolius (yacon), Croton lechleri (sangre de grado), Uncaria tomentosa/U. guianensis (una de gato), Lepidium meyenii (maca), Physalis peruviana (aguaymanto), Minthostachys mollis (muna), Notholaena nivea (cuti-cuti), Maytenus macrocarpa (chuchuhuasi), Dracontium loretense (jergon sacha), Gentianella nitida (hercampuri), Plukenetia volubilis (sacha inchi) and Zea mays (maiz morado). For each of these plants, information about their traditional uses and current commercialization is also included.
39 citations
TL;DR: The tricyclic sesquiterpene (–)-englerin A isolated from the stem bark of the Phyllanthus engleri plant (Euphorbiaceae) is highly active against certain renal cancer cell lines, and recent studies showed that engler in A is also a potent and selective activator of TRPC4 and TRPC5 calcium channels.
Abstract: Terpenoids are a very prominent class of natural compounds produced in diverse genera of plants, fungi, algae and sponges. They gained significant -pharmaceutical value since prehistoric times, due to their broad spectrum of medical applications. The fragrant leaves of Eucalyptus trees are a rich source of terpenoids. Therefore this review starts by summarizing the main terpenoid compounds present in Eucalyptus globulus, E. citriodora, E. radiata.and E. resinifera and describing their biosynthetic pathways. Of the enormous number of pharmaceutically important terpenoids, this paper also reviews some well established and recently discovered examples and discusses their medical applications. In this context, the synthetic processes for (-)-menthol, (-)-cis-carveol, (+)-artemisinine, (+)-merrilactone A and (-)-sclareol are presented. The tricyclic sesquiterpene (-)-englerin A isolated from the stem bark of the Phyllanthus engleri plant (Euphorbiaceae) is highly active against certain renal cancer cell lines. In addition, recent studies showed that englerin A is also a potent and selective activator of TRPC4 and TRPC5 calcium channels. These important findings were the motivation for several renowned research labs to achieve a total synthesis of (-)-englerin A. Two prominent examples - Christmann and Metz - are compared and discussed in detail.
39 citations
TL;DR: Results reveal that cordycepin induces apoptosis in human breast cancer cells via caspase-dependent pathways, shedding light on the possibility of cordyCEpin being a safe agent for breast cancer treatment.
Abstract: Cordycepin, a major compound separated from Cordyceps sinensis, is known as a potential novel candidate for cancer therapy. Breast cancer, the most typical cancer diagnosed among women, remains a global health problem. In this study, the anti-breast cancer property of cordycepin and its underlying mechanisms was investigated. The direct effects of cordycepin on breast cancer cells both in in vitro and in vivo experiments were evaluated. Cordycepin exerted cytotoxicity in MCF-7 and MDA-MB-231 cells confirmed by reduced cell viability, inhibition of cell proliferation, enhanced lactate dehydrogenase release and reactive oxygen species accumulation, induced mitochondrial dysfunction and nuclear apoptosis in human breast cancer cells. Cordycepin increased the activation of pro-apoptotic proteins, including caspase-8, caspase-9, caspase-3 and Bax, and suppressed the expression of the anti-apoptotic protein, B-cell lymphoma 2 (Bcl-2). The inhibition on MCF-7-xenografted tumor growth in nude mice further confirmed cordycepin's anti-breast cancer effect. These aforementioned results reveal that cordycepin induces apoptosis in human breast cancer cells via caspase-dependent pathways. The data shed light on the possibility of cordycepin being a safe agent for breast cancer treatment.
34 citations
TL;DR: Important inhibitory activity on lipoxygenase and acetylcholinesterase was observed supporting potential anti-inflammatory, anti-Alzheimer and insecticidal activities, mainly due to carvacrol, which support the potential use of oregano EOs as natural cosmetic and natural pharmaceutical ingredients.
Abstract: Oregano (Thymbra capitata and Origanum vulgare) essential oils (EOs), cultivated and extracted in the South-East of Spain, were analysed by GC/MS to determine their composition. (E)-β-Caryophyllene...
30 citations
TL;DR: In this paper, a scientific guide for the evaluation of traditional herbal medicines (THMs) in terms of their toxicity risks based on the published regulatory documents is presented, where in vitro and in vivo toxicity tests on medicinal products for human use are overviewed and they are then adopted to be used for the toxicity assessment of THMs.
Abstract: Herbal remedies have been used for thousands of years in worldwide traditional medicines for their potential health benefits. Although they are generally presumed safe unless a significant risk has been identified in humans, increasing number of case reports notify acute or chronic intoxications resulting from their use. This study aims to produce a scientific guide for the evaluation of traditional herbal medicines (THMs) in terms of their toxicity risks based on the published regulatory documents. For this purpose recommended in vitro and in vivo toxicity tests on medicinal products for human use issued by the international regulatory bodies are overviewed and they are then adopted to be used for the toxicity assessment of THMs. Accordingly, based on compilation of these issued regulations, the following tests are recommended for the toxicity assessment of THMs; in vitrocytotoxicity, genotoxicity, acute and repeated dose toxicity, carcinogenicity, reproductive and developmental toxicity, local tolerance tests, toxicokinetic studies, and additional toxicity tests including safety pharmacology, immunotoxicity and antigenicity, endocrine system toxicity, gastro-intestinal toxicity, renal and hepatotoxicity, and drug interaction studies. This study describes and discusses the applicability of these tests for the risk assessment in THMs.
29 citations
TL;DR: The EOs capacity for scavenging peroxyl radicals-was also influenced by the presence of cyclodextrins, as a synergism seemed to occur between EOs and those carbohydrates.
Abstract: The in viro antioxidant, anti-inflammatory, anti-hyperglycaemic, and anti-acetylcholinesterase activities of the essential oils (EOs) isolated from six Lamiaceae species (Thymbra capitata,. Thymus albicans, Th. caespititius, Th. carnosus, Th. lotocephalus and Th. mastichina) grown in Portugal, were evaluated. Th. caespititius and T. capitata carvacrol/thymol-rich EOs showed the best capacity for preventing lipid peroxidation, and scavenging the 2,2'-azino- bis(3-ethylbenzothiazoline-6-sulphonid acid) (ABTS) and peroxyl free radicals, as well as for inhibiting lipoxygenase and a-amylase. However, Th. caespititius and Th. lotocephalus 1,8-cineole and linalool rich EOs were the best inhibitors of a-glucosidase. T capitata, Th. lotocephalus and Th. albicans EOs were the: most active for inhibiting acetyleholinesterase. Th. caespititius and Th. mastichina EOs were the main scavengers of nitric oxide (NO) radicals. The comparison between the present data with a survey of the existing literature on the in vitro biological activities of the essential oils isolated from the same species from Portuguese origin, using other.methodologies, showed some differences. For instance the use of two oxidizable substrates (egg yolk andlecithin liposomes) led to distinct results mainly for those samples with relatively low activity. In addition, the EOs capacity for scavenging peroxyl radicals-was also influenced by the presence of cyclodextrins, as a synergism seemed to occur between EOs and those carbohydrates.
28 citations
TL;DR: This review addresses the most important Amaryllidaceae alkaloids with anticancer potential, particularly those that have been studied for the purpose of gaining a better understanding of the basis of the activity at the cellular and molecular level.
Abstract: Modern research has shown that Amaryllidaceae alkaloids represent a rich reservoir of potential small chemical molecules exhibiting several medicinal properties through various mechanisms. Among th...
27 citations
TL;DR: Two major alkaloids, scoulerine and cheilanthifoline, are reported on and their inhibitory activities against acetylcholinesterase (anti-AChE), tumor necrosis factor alpha (anti TNF-α) and a bacterial strain, Helicobacter pylori are shown.
Abstract: Corydalis plants containing isoquinoline alkaloids are reported to possess promising phamacological properties for the treatment of important diseases including cancer, inflammation, Alzheimer's disease and microbial infections. As part of a wider program investigating Bhutanese medicinal plants,.we have previously identified eight isoquinoline alkaloids from C. dubia. Out of these, we report here on two of the major alkaloids, scoulerine (1) and cheilanthifoline (2) and their inhibitory activities against acetylcholinesterase (anti-AChE),-tumor necrosis factor alpha (anti TNF-α) and a bacteial strain, Helicobacterpylori. Both alkaloids showed weak anti TNF-α and antibacterial activities. However, the anti-AChE activity of scoulerine (1) was promising as it-significantly inhibited AChE with a minimum inhibitory requirement (MIR) value of 0.0015 nmol, which was two-fold better than the reference drug, galanthamine (MIR value of 0.003 nmol). As there are limited.anti-Alzheimer's chemotherapeutics, scoulerine (1) is worthy of further exploration, including lead optimization, structure-activity-relationship studies, analog development,.pharmacodynanics and in vivo animal studies.
26 citations
TL;DR: The hydrodistilled essential oils and volatile compounds (by static headspaces technique) of Mentha piperita L. and M. spicata L. were characterized by GC-MS and certain differences were discussed.
Abstract: The hydrodistilled essential oils and volatile compounds (by static headspaces technique) of Mentha piperita L. and M spicata L. were characterized by GC-MS. Headspace analysis of Mentha piperita revealed the existence of menthone (25.4%), 1,8-cineole (17.7%) and menthol (12.1%) as the main components, while the essential oil contained high amounts of menthol (46.8%) and menthone (25.6%). By contrast, headspace analysis of M. spicata showed a high content of limonene (37.0%) together with carvone (13.0%), β-pinene (10.4%) and α-pinene (9.8%), while the essential oil was reach in carvone (51.7%), dihydrocarveol (11.5%) and cis-dihydrocarvone (9.1%). Eleven samples of peppermint tea available on the Romanian market were analysed by headspace GC-MS. The volatile profile of the tea samples was compared with that of Mentha piperita L. and certain differences were emphasized and discussed.
TL;DR: Thyme, oregano and rosemary EOs exhibited important antioxidant activities by ABTS•+ assay compared with trolox, and that of M. suaveolens showed a stronger cytotoxic activity on HaCaT cells.
Abstract: The chemical composition, antifungal, antioxidant and cytotoxic activities of the essential oils (EOs) of mint (Mentha suaveolens), thyme (Coridothymus capitatus), oregano (Origanum hirtum) and ros...
TL;DR: In this review, pharmacological, toxicological and phytochemical data on medicinal plants used in local traditional medicine in Mali are reported to improve the actual herbal drugs and to propose new phytomedicines for the management of malaria and liver diseases.
Abstract: Today, ethno-pharmacology is a very important resource in order to discover new therapies for the current diseases. Moreover, another good justification for the ethno-pharmacological approach is to obtain new, effective, less expensive and simple therapies, limiting at the same time the cost of pharmaceutical research. Two major anti-malarial drugs widely used today, i.e. quinine and artemisinin, came respectively from Peruvian and Chinese ancestral treatments reported in the traditional medicines. In this contest, there is an urgent need for the discovery of new drugs, due to the critical epidemiological situation of this disease and to the growth of resistances. In Mali, malaria and liver diseases remain one of the leading public health problems. Many medicinal plants are often used, in local traditional medicine, for the treatment at the same time of malaria and liver diseases, including hepatic syndromes, jaundice, hepatitis and other hepatic disorders. Moreover, in the local language Bamanan, the word "Sumaya" is used both for malaria and some liver diseases. In addition, we noted that some of the improved traditional phytomedicines produced by the Department of Traditional Medicine are prescribed by modern doctors both for malaria and liver diseases. In this review, pharmacological, toxicological and phytochemical data on Argemone mexicana L. (Papaveraceae), Cochlospermum tinctorium Perr. ex A. Rich (Cochlospermaceae), Combretum micranthum G.Don (Combretaceae), Entada africana Guillet Perr. (Mimosaceae), Erythrina senegalensis A. DC (Fabaceae), Mitragyna inermis (Willd) Kuntze (Rubiaceae), Nauclea latifolia Smith syn. Sarcocephalus latifolius (Smith) Bruce (Rubiaceae), Securidaca longepedunculata Fresen (Polygalaceae), Trichilia emetica Vahl. (Meliaceae), and Vernonia colorata (Willd) Drake (Asteraceae) are reported. Some of the collected data could be used to improve the actual herbal drugs and to propose new phytomedicines for the management of malaria and liver diseases.
TL;DR: GC/MS analysis of all essential oils showed that oxygenated monoterpenoids are the major components of these oils, with the exception of Mentha arvensis 'Banana', and piperitenone oxide as the major component.
Abstract: The major purpose of this study was to determine the chemical relationships between the essential oils (EO) obtained form 18 mint samples of different species and its cultivrs. GC/MS analysis of all essential oils showed that oxygenated monoterpenoids are the major components of these oils, with the exception of Mentha arvensis 'Banana'. Based on the. chemical composition of the essential oils, the analyzed mints can be divided into five groups. Group I was characterized by the-presence of menthol and menthone, piperitenone oxide is the major constituent of group II, linalool of group III, carvone characterizes group IV, while 3-octanone is the most characteristic compound for group V. A reference strain of biofilm forming Staphylococcus epidermidis ATTC 35984 was tested against the obtained essential oils. Two of them, M suaveolens 'Variegata' and M x piperita 'Almira' exhibited significant bacteriostatic activity. The MIC values of these EOs were 0.25% and 0.5% respectively in comparison with an average MIC of 4% of the other tested mint EOs. Both active EOs are characterized by the presence of piperitenone oxide as the major component.
TL;DR: The efficacy of several of these plants has been supported by some scientific evidence, while other plants have to be submitted to further investigations to prove the beneficial medicinal properties attributed to them.
Abstract: Medicinal plants are a vital source of medication in developing countries. In Kachin State, Northern Myanmar, the people have a long history of the use of traditional plants for medicinal purposes. This article deals with the 25 most used medicinal plants in Kachin State. They are: Drynariafortunei, Tetrastigma serrulatum, Bauhinia championii, Goniothalamus cheliensis, Juglans regia, Houttuynia cordata, Osmanthus fragrans, Pothos chinensis, Tabemaemontana coronaria, Eryngiumfoetidum, Chloranthus spicatus, Peperomia pellucida, Zanthoxylum armatum, Polygonumfagopyrum, Cymbidiumfloribundum, Amomum kravanh, Coscinium fenestratum, Solanum nigrum, Gnetum parvifolium, Desmodium triquetum, Begonia augustinec, Mappianthus iodoides, Erycibe obtusifolia, Schefflera venulosa, Holarrhena antidysenterica. The different traditional applications, the known chemical constituents and medicinal properties are reported for each plant. The efficacy of several of these plants has been supported by some scientific evidence, while other plants have to be submitted to further investigations to prove the beneficial medicinal properties attributed to them.
TL;DR: Research indicates that polypores - a large group of fungi of the phylum Basdioinycota - exhibit antiviral, antimicrobial, anticancer, anti-allergic,Anti-atherogenic, hypoglycemic, hepatoprotective and anti-inflammatory activities.
Abstract: Mushrooms have been widely used in traditional medicine for the treatment of various diseases. Today, their therapeutic value is scientifically studied and appreciated. Research indicates that poly...
TL;DR: A reproducible sequence of extraction, fractionation and chromatographic purification was adopted and was guided by HPLC fingerprinting to develop a reproducible procedure for preparation of specific extracts and isolation of the major phenolic constituents present in nutmeg kernel.
Abstract: Many studies on the biological activities of nutmeg continue to appear in the literature. The most common targets include GIT, CNS, oxidative stress and inflammation. However, results obtained from most studies are often inconsistent due to the variability of utilized samples, lack of standardized nutmeg products or insufficient amounts of pure compounds for comprehensive follow-up investigation. To address the consistency and supply issue we utilized available technology to develop a reproducible procedure for preparation of specific extracts and isolation of the major phenolic constituents present in nutmeg kemel. A well-defined and reproducible sequence of extraction, fractionation and chromatographic purification was adopted and was guided by HPLC fingerprinting. Spectroscopic methods, mainly NMR, and mass spectrometry were utilized to identify each compound. Thirteen compounds were isolated in a pure form and identified as: elemicin (1), isoelemicin (2), myristicin (4), surinamensin (5), malabaricone C (6), 2-(3'-allyl-2',6'-dimethoxy-phenyloxy)-l- acetoxy-(3,4-dimethoxyphenyl)-propyl ester (7), methoxylicarin A (8), licarin A (9), malabaricone B (10), licarin C (11), 5'-methoxylicarin B (12), licarin B (13), and 2-(3'-allyl-2',6'-dimethoxy-phenyloxy)-l-methyl-5-methoxy-1,2-dihydrobenzofuran (3, a new compound). With repeated isolation runs, these pure compounds can be prepared in quantities sufficient for biological evaluation as needed. The availability of purified compounds will also allow the development of specific, accurate, and sensitive analytical procedures for pharmacokinetic studies and for quality control of nutmeg products. Both aspects are essential for nutmeg-focused drug discovery. The same approach can also be adapted to other medicinal plants of potential interest.
TL;DR: The objective of this review is to update the ethnopharmacological and phytochemical studies accomplished on the Ecuadorian flora, pointing to the 253 native families and more than 15,000 species registered at present.
Abstract: Ecuador owns many high quantity and wealthy ecosystems that contain an elevated biodiversity in flora and fauna. The use of native medicinal plants has been maintained by at least 18 different indigenous cultures; furthermore, this country has been the witness of the discovery of important medicinal plants, such as Cinchona, and is an understudied resource of new natural products. The objective of this review is to update the ethnopharmacological and phytochemical studies accomplished on the Ecuadorian flora, pointing to the 253 native families and more than 15,000 species registered at present.
TL;DR: A variety of new and earlier synthesized lupane, oleanane, ursane and dammarane triterpenoids have been investigated for their inhibitory activity against α-glucosidase, and 2,3-Indole-21β-acetyl-20β,28-epoxy-18α,19βH-ursane, 3-oxo-3A-homo-3a-aza-20(S)-hydroxyd
Abstract: A variety of new and earlier synthesized lupane, oleanane, ursane and dammarane triterpenoids have been investigated for their inhibitory activity against α-glucosidase. 2,3-Indole-21 β-acetyl-20β,28-epoxy-18α,19βH-ursane and 3-oxo-3A-homo-3a-aza-20(S)-hydroxydammar-24(25)-ene were synthesized for the first time. The compounds 3, 4, 8-11 and 14 demonstrated strong in vitro inhibitory activity towards α-glucosidase with IC₅₀ values of 37.5-115.1 µM. 3-Deoxy-3a-homo-3a-aza-28-cinnamoyloxy-20(29)-lupene, with an IC₅₀ of 6.67 µM was 60-fold more active than the market drug acarbose.
TL;DR: Results indicate that A. mearnsii leaves, a forest waste product, could be a valuable natural source of anti-inflammatory and functional components related to human health.
Abstract: This study was performed to investigate potential bioactive secondary metabolites from the leaves of Acacia mearnsii, a forest waste product in China. The polyphenol constituents and bioactivity of crude extract (L) and semi purified fractions (L1-L4) were examined. The L and L1-L4 showed qualitative and quantitative differences in their phenolic content, antioxidant activities and the activities against inflammation-related genes such as the inducible forms of COX-2, iNOS, and the pro-inflammatory IL in lipopolysaccharide (LPS)-stimulated mouse macrophage cell line RAW 264.7. All the fractions depressed reactive oxygen species (ROS) in LPS-stimulated RAW 264.7 macrophage cells, and (except L2) inhibited the release of nitric oxide (NO). Fractions L3 and L4 significantly inhibited the mRNA expression levels of the anti-inflammatory cytokine IL-1β, COX-2, iNOS, and IL-6. In addition, L4 (1.8 g obtained from 5 g crude leaves extract) which contained 646.6 mg/g gallic acid equivalent total phenolic content and consisted of primarily proanthocyanidins (12.6 mg/g as procyanidin B2 equivalent by the DMAC assay) showed the best activity in all the assays. Results indicate that A. mearnsii leaves, a forest waste product, could be a valuable natural source of anti-inflammatory and functional components related to human health.
TL;DR: The results indicate intensive metabolism of thymol in liver and its accumulation in kidney tissue and it is necessary to keep in mind the selection of a sufficient concentration of EO in the feed additive for animals without the risk ofThymol residues in edible tissues.
Abstract: The absorption and metabolism of phytogenic feed additives in poultry is studied related to the metabolism and deposition of their main compounds in tissues intended for food production. Fifty-six non-sexed Ross 308 broilers were allocated to seven dietary treatments and fed a diet containing graded levels of thyme (Thymus vulgaris L.) essential oil (EO) (0, 0.01, 0.02, 0.03, 0.04, 0.05, 0.1%, w/w). Thymol concentration was measured in plasma, liver, kidney and breast muscle tissue using solid phase micro-extraction followed by gas chromatography/mass spectrometry. We found the highest concentrations of thymol in kidney and plasma, and the lowest in breast muscle and liver. Thymol content in plasma and kidney significantly increased when 0.05 and 0.1%, w/w, EO and in liver and breast muscle only when 0.1%, w/w, EO was added to the diet (p<0.05). Our results indicate intensive metabolism of thymol in liver and its accumulation in kidney tissue. We confirm low deposition of thymol in the muscle tissue. It is necessary to.-keep in mind the selection of a sufficient concentration of EO in the feed additive for animals without the risk of thymol residues in edible tissues.
TL;DR: It is concluded that VCO shows promising effects in improving the biochemical derangements associated with CVD, thus lowering the CVD risk and future investigations are needed to examine the health benefits of VCO in human intervention studies.
Abstract: Cardiovascular disease (CVD) is known as the number one cause of death worldwide. It is associated with huge health care costs and loss of productivity in the population. Poor diet is an important risk factor in CVD. Diet rich in polyunsaturated fatty acids, such as virgin coconut oil (VCO), has been associated with a reduced risk of CVD. This systematic review focused on studies that reported the association between VCO and the biochemical measurements associated with CVD. These studies conclude that VCO shows promising effects in improving the biochemical derangements associated with CVD, thus lowering the CVD risk. However, most of these studies were performed in animals with very limited data from human. Future investigations are needed to examine the health benefits of VCO in human intervention studies.
TL;DR: The aminonaphthoquinone, spinamine E, was isolated for the first time from the sea urchins and showed a high antiradical activity, which was up to 1.5 times higher than that of α-tocopherol.
Abstract: The aminonaphthoquinone, spinamine E (5), was isolated for the first time from the sea urchins Strongylocentrotus pallidus (Sars G.O., 1872) and Mesocentrotus nudus (A. Agassiz, 1864). The structur...
TL;DR: From the whole plant of Dendrobium signatum, a new bibenzyl-dihydrophenanthrene derivative, named dendrosignatol was isolated and showed appreciable cytotoxic activity against three human cancer cell lines, including MDA-231, HepG2 and HT-29 cells.
Abstract: From the whole plant of Dendrobium signatum, a new bibenzyl-dihydrophenanthrene derivative, named dendrosignatol was isolated, together with the known compounds 3,4-dihydroxy-3,4'-dimethoxybibenzyl, dendrocandin B, dendrocandin I and dendrofalconerol A. The structure of the new compound was elucidated through analysis of its spectroscopic and mass spectrometric data. All of the isolates showed appreciable cytotoxic activity against three human cancer cell lines, including MDA-23 1, HepG2 and HT-29 cells.
TL;DR: This study confirms the prior in vitro data and proposes quebrachamine, cephalotaxine, cryptolepine, (22S,25S)-tomatidine, ( 22R, 25S)-solanidine, and (22R,25R)-solasodine as new alkaloid scaffold leads in the search for more potent and selective TryR inhibitors.
Abstract: Trypanothione reductase (TryR) is a key enzyme in the metabolism of Trypanosoma cruzi, the parasite responsible for Chagas disease. The available repertoire of TryR inhibitors relies heavily on synthetic substrates of limited structural diversity, and less on plant-derived natural products. In this study, a molecular docking procedure using a Lamarckian Genetic Algorithm was implemented to examine the protein-ligand binding interactions of strong in vitro inhibitors for which no X-ray data is available. In addition, a small, skeletally diverse, set of natural alkaloids was assessed computationally against T. cruzi TryR in search of new scaffolds for lead development. The preferential binding mode (low number of clusters, high cluster population), together with the deduced binding interactions were used to discriminate among the virtual inhibitors. This study confirms the prior in vitro data and proposes quebrachamine, cephalotaxine, cryptolepine, (22S,25S)-tomatidine, (22R,25S)-solanidine, and (22R,25R)-solasodine as new alkaloid scaffold leads in the search for more potent and selective TryR inhibitors.
TL;DR: Comprehensive information on the nutritional characteristics, traditional functions, chemical constituents, and biological activities of the Juglans species, together with the seeds used as walnuts is provided to explore their potential and to advance research.
Abstract: Walnuts are seeds with a hard shell from the genus Juglans (J. mandshurica, J. regia, J. sinensis, J. cathayensis, J. nigra and J. sigillata). Walnuts can nourish brain cells to improve human memory. Other parts of the plant are also employed as traditional Chinese medicines. Modern research on Juglans species has been mostly focused on the above-mentioned species, the seeds of which are all called walnuts. Juglans species have diverse chemical constituents, including diarylheptanoids, quinones, polyphenols, flavones and terpenes. The diarylheptanoids and quinones have notable antitumor activity, supplying new lead compounds for preparing antitumor drugs. The potent pain-relieving, antioxidant, antibacterial and antitumor activities of these plants are significant. In the review, comprehensive information on the nutritional characteristics, traditional functions, chemical constituents, and biological activities of the Juglans species, together with the seeds used as walnuts is provided to explore their potential and to advance research.
TL;DR: Findings demonstrate that C. minima possesses anti-angiogenic activity, and 6-O-angeloylenolin is a promising candidate for the development of an anti-ANGiogenic agent.
Abstract: Centipeda minima is a Chinese herbal medicine used in the treatment of various diseases including cancer. An ethanol extract of the herb, its four fractions with different polarities, and two volatile oils prepared by steam distillation (SD) and supercritical fluid extraction (SFE) were investigated for their anti-angiogenic activity in a wild-type zebrafish model using a quantitative endogenous alkaline phosphatase (EAP) assay. The SFE oil displayed potent anti-angiogenic activity. Fifteen sesquiterpene lactones (SLs; compounds 1-15) isolated from the SFE oil were evaluated for their anti-angiogenic effect. Results revealed that pseudoguaianolide type SLs (1-8) inhibited vessel formation in the zebrafish embryos while guaianolide type SLs (9-15) showed little effect. Among the active ones, 6-O-angeloylenolin (1), a major component of SFE oil, possessed the strongest effect by reducing vessel formation in zebrafish embryos to 40% of the control value at 29.7 µM. Further study using the Tg (fli1a:EGFP) y1-type zebrafish model revealed that it blocked both intersegmental blood vessels (ISVs) and subintestinal vessels plexus (SIVs) formation in zebrafish embryos. Real-time polymerase chain reaction assay on the wild-type zebrafish embryos suggested that 6-O-angeloylenolin affected multiple molecular targets related to angiogenesis including VEGF receptor, angiopoietin, and its receptors. Taken together, our findings demonstrate that C. minima possesses anti-angiogenic activity, and 6-O-angeloylenolin is a promising candidate for the development of an anti-angiogenic agent.
TL;DR: It is thought that the essential oils of Litsea cubeba are capable of multipurpose applications and present a potentially good choice as antibacterial agents.
Abstract: The essential oils of leaves, fruits, flowers, stems and twigs of Litsea cubeba were extracted by hydrodistillation. A total of 53, 50, 76, 94 and 90 compounds were identified from the leaf, fruit, flower, stem and twig oils, respectively, and their yields were 13.9 ± 0.09, 4.0 ± 0.03, 10.4 ± 0.05, 0.09 ± 0.01 and 0.4 ± 0.02 mL/100 g of the oven-dried (o.d.) materials, respectively. The main component in the leaf, flower and twig oils was 1,8-cineole, whereas in the fruit oil it was citral, and in the stem oil limonene, citronellal, and citronellol. When tested for their antibacterial activities using the paper disc diffusion method, oils from all parts showed excellent activities, particularly the fruit oil. When the oils were infused onto filter paper and tested for their antimicrobial paper capability according to the JIS L 1902 method, the fruit oil exhibited excellent antimicrobial activities. Citral was deemed the main cause of the antimicrobial activity. With the multiplicity of contagious diseases and their prevalence in hospitals, these essential oils present a potentially good choice as antibacterial agents. We think that the essential oils of this species are capable of multipurpose applications.
TL;DR: The essential oils of Actinodaphne macrophylla and A. pruinosa were analyzed and evaluated for their antioxidant and anti-inflammatory activities and demonstrated significant activity on DPPH, phenolic content, and lipoxygenase assays.
Abstract: The essential oils of Actinodaphne macrophylla and A. pruinosa were analyzed by GC and GC-MS and evaluated for their antioxidant and anti-inflammatory activities. The essential oil of the leaves of A. macrophylla was characterized by the presence of 31 components (78.2%), with germacrene B (16.8%) and globulol (16.0%) as the major components. A total of 28 components (71.6%) were characterized in the leaf oil of A. pruinosa with the most abundant components being globulol (17.8%) and spathulenol (12.0%). The antioxidant activity was determined by DPPH radical scavenging and total phenolic content, while anti-inflammatory activity by lipoxygenase assay. The essential oil of A. pruinosa demonstrated significant activity on DPPH (IC50 85.6 μg/mL), phenolic content (190.2 mg GA/g) and in the lipoxygenase (IC50 85.2 μM) assays.
TL;DR: Consumption of turmeric constituents may prevent dementia, according to the results of a pharmacokinetic absorption experiment.
Abstract: The need for a preventive agent against dementia led us to screen natural plant resources. Among the herbs and spices tested, turmeric, from rhizomes of Curcuma longa, showed high potency against β-secretase. The active principles were determined as α-turmerone, β-turmerone and ar-turmerone, with IC(50) values of 39, 62 and 92 μM respectively. In this study, the efficiency of collecting the essential oil using steam distillation of the volatile substance was disclosed The active principles were explored, and four sesquiterpenoids and five monoterpenoids were revealed as active principles against β-secretase; On the other hand, α-turmerone, β-turmerone and ar-turmerone were also investigated in a pharmacokinetic absorption experiment. After oral administration, these compounds were detected in an intact form in the brain and serum. These results suggest that consumption of-turieric constituents may prevent dementia.