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  • Semisynthetic and newly designed derivatives based on natural chemical scaffolds: moving beyond natural products to fight Trypanosoma cruzi
    Phytochem. Rev. (IF 4.257) Pub Date : 2020-01-23
    Rafael da Rosa, Eloir Paulo Schenkel, Lílian Sibelle Campos Bernardes

    Abstract Secondary metabolites obtained from natural sources are medicinally relevant molecules. About one-third of all FDA-approved drugs are derived from or based on natural products, which suggests that molecular optimization is often required for translation from benchtop to clinical practice. Chagas disease, caused by Trypanosoma cruzi, is a neglected tropical disease highly prevalent in Latin America. It has a significant impact on socioeconomic indicators and is not easily cured by the two currently available drugs, benznidazole and nifurtimox. Considering the importance of developing new bioactive molecules based on natural products, this article reviews 21 years of literature reports on the semisynthesis and total synthesis of new compounds targeting T. cruzi. From 1997 to 2018, sixty-six articles reporting five hundred and thirty-seven molecules active against different strains and life stages of the parasite were published. Quinones, alkaloids, terpenes, and lignans were the four largest classes of derivatives, the majority of which had IC50 values low enough to indicate that natural product derivatives can be an important source of potential new drugs to treat Chagas disease. We highlight important molecules in each secondary metabolite class, discussing factors such as selectivity and the basis for their design. An assessment of drug-likeness parameters was performed, which might prove useful for selecting lead compounds for preclinical drug studies.

  • Synergistic, antagonistic and additive antioxidant effects in the binary mixtures
    Phytochem. Rev. (IF 4.257) Pub Date : 2020-01-02
    Małgorzata Olszowy-Tomczyk

    Abstract Food which is consumed by living organisms contains many antioxidants often with different antioxidant abilities. In the case of antioxidants mixture its potential is not always an additive value of antioxidant properties of their individual ingredients. Despite the extensive research there is still no knowledge about the reasons for observing the antioxidant antagonism and synergism in mixtures. The paper is a review which contains the literature information available about the antioxidant activity of binary mixtures. The manuscript presents different examples of natural mixtures with the literature proposed explanation of the observed antioxidant effects. It also describes different factors (i.e.: applied method, mechanisms of radical neutralization, composition of reacting mixture—chemical structures of antioxidants, concentration and molecular ratio, applied solvent, treatment of sample or reaction time) which have influence on the observed antioxidant effects. Additionally, the ways of expressing of the antioxidant effects are presented.

  • Biocontrol capabilities of the genus Serratia
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-12-07
    Amalia Soenens, Juan Imperial

    This review focuses on the production of natural bioactive products and their biocontrol capabilities of the enterobacterial genus Serratia. Serratia represents a unique group of enterobacteria with a notable secondary metabolism, able to produce a wide range of natural bioactive products including the β-lactam antibiotic carbapenem or the antifungal compound oocydin A. However, until very recently, most of the Serratia isolates originated from human and animal infections, and a systematic approach to the isolation of Serratia from natural habitats has been missing. The paucity of environmental isolates has so far limited our understanding of the potential of Serratia to produce new natural bioactive products and their capacity to be used in sustainable agriculture as biocontrol agents. The ability to isolate Serratia from soils, together with the analytical capabilities afforded by the democratization of genome sequencing methodologies, opens the door to the isolation and characterization of such novel biocontrol agents, hitherto inaccessible.

  • It is not just artemisinin: Artemisia sp. for treating diseases including malaria and schistosomiasis
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-09-19
    B. M. Gruessner, L. Cornet-Vernet, M. R. Desrosiers, P. Lutgen, M. J. Towler, P. J. Weathers

    Artemisia sp., especially A. annua and A. afra, have been used for centuries to treat many ailments. While artemisinin is the main therapeutically active component, emerging evidence demonstrates that the other phytochemicals in this genus are also therapeutically active. Those compounds include flavonoids, other terpenes, coumarins, and phenolic acids. Artemisia sp. phytochemicals also improve bioavailability of artemisinin and synergistically improve artemisinin therapeutic efficacy, especially when delivered as dried leaf Artemisia as a tea infusion or as powdered dry leaves in a capsule or compressed into a tablet. Here results from in vitro, and in vivo animal and human studies are summarized and critically discussed for mainly malaria, but also other diseases susceptible to artemisinin and Artemisia sp. including schistosomiasis, leishmaniasis, and trypanosomiasis.

  • Only a matter of time: the impact of daily and seasonal rhythms on phytochemicals
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-08-14
    Donna J. Liebelt, Juliette T. Jordan, Colleen J. Doherty

    Plants regulate molecular bioactivity in response to daily and seasonal environmental fluctuations in temperature, light, humidity, and precipitation. These rhythms interconnect, overlap, and feedback both into each other and into the plant’s endogenous circadian clock. The resulting regulatory network tightly ensures that the overall phytochemical composition is highly adaptive to the plant’s needs at any point in time. Temporally coordinated control of primary and secondary metabolism ensures phytochemicals are in tune with the demands of the environment and the available resources. As a consequence, phytochemical composition varies throughout the day and year. This variation in phytochemical abundance and composition across time can affect experimental results and conclusions. Understanding how phytochemical composition varies across time is critical for uncovering the underlying regulatory connections and ultimately improving the quality of phytochemical products. Herein, we review the mechanisms underlying diel and seasonal variations in phytochemical composition and provide examples of temporal regulation of specific compounds within phenol, terpenoid, and alkaloid phytochemical classes.

  • Mexican copalchis of the Rubiaceae family: more than a century of pharmacological and chemical investigations
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-06-22
    Isabel Rivero-Cruz, Sol Cristians, Berenice Ovalle-Magallanes, Rachel Mata

    The term copalchi has been used in the scientific literature to define a group of plants of the Rubiaceae and Euphorbiaceae families with extremely bitter stem-barks, useful for treating diabetes and malaria. In this review we summarized the most relevant chemical and pharmacological works carried out in the last century with the copalchis of the Rubiaceae family, namely Hintonia latiflora, H. standleyana and Exostema caribaeum. Their major components are 4-phenylcoumarins 5,7,3′,4′- or 5,7,4′-substituted with oxygenated functionalities, with the former having the most common pattern. These along with a few cucurbitacins are responsible for the antidiabetic properties of both Hintonia species. E. caribaeum contained mostly 4-phenylcoumarins, which apparently are the antimalarial constituents of these plants. Toxicological reports on these plants are discussed. The quality control procedures (chromatographic and molecular) developed for the three species are summarized. These will be valuable for their unequivocal identification, which in turn will avoid their partial adulteration or substitution. Future studies are required to solve the puzzle around the toxicity of the copalchis and for better understanding their pharmacological actions. Finally, establishment of their metabolomics profiles will provide a better knowledge of their secondary metabolism and help map their biosynthesis pathways.

  • Benzylisoquinoline alkaloid biosynthesis in opium poppy: an update
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-11-27
    Aparna Singh, Ivette M. Menéndez-Perdomo, Peter J. Facchini

    For nearly eight millennia, opium poppy (Papaver somniferum) has been bred and cultivated for therapeutic purposes. The medicinal properties of the plant are conferred by specialized metabolites known as benzylisoquinoline alkaloids (BIAs), comprising the narcotic analgesics morphine and codeine, the antimicrobial agent sanguinarine, and the potential anticancer drug noscapine. In addition, naturally occurring thebaine is used for the semi-synthesis of widely prescribed pain-relievers (e.g., oxycodone and hydrocodone), valuable drugs used in the treatment of opioid addiction (i.e., naltrexone), or antidotes for opioid overdose (i.e., naloxone). The complex stereochemistry of many opiates hinders their chemical synthesis and opium poppy remains the sole commercial source of these important pharmaceuticals. For decades, opium poppy has served as a model plant for research aimed at a comprehensive understanding of BIA metabolism. Recent progress in functional genomics has enabled the discovery of a nearly complete collection of BIA biosynthetic genes, many of which are clustered in the opium poppy genome. Advances in synthetic biology have facilitated the successful reconstitution of several BIA biosynthetic pathways in heterologous hosts such as Saccharomyces cerevisiae and Escherichia coli, although the initially low production levels suggest that commercial scale-up will present additional challenges. This review provides an update of key molecular and biochemical aspects of BIA metabolism in opium poppy, including recent biosynthetic gene discoveries, genomic organization, novel BIA transporters, metabolic regulation, and major efforts in the engineering of pathways in plants and microbes.

  • Cytokinins, the Cinderella of plant growth regulators
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-11-28
    Ruth E. Márquez-López, Ana O. Quintana-Escobar, Víctor M. Loyola-Vargas

    Cytokinins (CKs) are a complex group of compounds. The complexity of CKs is not just present at the level of chemical structures, but as a family of compounds. CKs occur in plants as nucleotides, nucleosides (ribosides) that are produced during de novo biosynthesis, free bases, and conjugates that are in stored/inactivated forms. Almost all organisms make cytokinins. CKs are structural components of the tRNA, and they are located next to the anticodon loop beginning with U of a subset of tRNAs in most eukaryotes and bacteria. The biosynthesis of CKs uses several pathways, and there is evidence that its biosynthesis is also regulated by other growth regulators such as auxins, strigolactones and abscisic acid. Its signaling pathway involves a phosphotransfer signal cascade. Despite advances made so far in the knowledge of CKs, there is still a long way to go. In this review, we summarize the most up-to-date knowledge on the biosynthesis of CKs and the signaling pathway that leads to the response to the presence of CKs in plant tissue, and we identify areas that require more research to complete our understanding of the role of the CKs in plants.

  • Metabolons in plant primary and secondary metabolism
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-07-06
    Toshihiro Obata

    Metabolons are multi-enzyme protein complexes composed of enzymes catalyzing sequential reactions in a metabolic pathway. Metabolons mediate substrate channeling between the enzyme catalytic cores to enhance the pathway reactions, to achieve containment of reactive intermediates, and to prevent access of competing enzymes to the intermediates. These provide unique advantages in metabolic regulation. The discovery of plant metabolons has been accelerated by the recent technical developments and a considerable number of metabolons involved in both primary and secondary metabolism have been indicated in the last decade. These findings related with plant metabolons are comprehensively reviewed in this review, indicating metabolome-wide engagement of metabolons. However, there are still unexplored frontiers remaining for further discovery of metabolons in plant metabolism. Pathways with high potential of novel metabolon and technical issues to be solved for the future discovery will also be discussed.

  • Lonicerae japonicae flos and Lonicerae flos: a systematic review of ethnopharmacology, phytochemistry and pharmacology
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-11-22
    Yuke Li, Wen Li, Chaomei Fu, Ying Song, Qiang Fu

    Lonicerae japonicae flos (called Jinyinhua, JYH in Chinese), flowers or flower buds of Lonicera japonica Thunberg, is an extremely used traditional edible-medicinal herb. Pharmacological studies have already proved JYH ideal clinical therapeutic effects on inflammation and infectious diseases and prominent effects on multiple targets in vitro and in vivo, such as pro-inflammatory protein inducible nitric oxide synthase, toll-like receptor 4, interleukin-1 receptor. JYH and Lonicerae flos [called Shanyinhua, SYH in Chinese, flowers or flower buds of Lonicera hypoglauca Miquel, Lonicera confusa De Candolle or Lonicera macrantha (D.Don) Spreng] which belongs to the same family of JYH were once recorded as same herb in multiple versions of Chinese Pharmacopoeia (ChP). However, they were listed as two different herbs in 2005 Edition ChP, leading to endless controversy since they have close proximity on plant species, appearances and functions, together with traditional applications. In the past decades, there has no literature regarding to systematical comparison on the similarity concerning research achievements of the two herbs. This review comprehensively presents similarities and differences between JYH and SYH retrospectively, particularly proposing them the marked differences in botanies, phytochemistry and pharmacological activities which can be used as evidence of separate list of JYH and SYH. Furthermore, deficiencies on present studies have also been discussed so as to further research could use for reference.

  • Botrytis species as biocatalysts
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-11-06
    Cristina Pinedo, Javier Moraga, Isidro G. Collado, Josefina Aleu

    The search for new biocatalysts is increasing significantly in recent years, especially to obtain novel derivatives with improved properties for new drugs, agrochemicals or fragrances which are difficult to obtain using conventional methods. Fungi are traditionally the most frequently studied cell systems and from among the fungi used in biotransformations, Botrytis species stand out for being able to metabolize a wide variety of bioactive compounds. This review covers from the year 2000 up to December 2018 and reports on the application of Botrytis species as biocatalysts.

  • Commercial development of plant essential oils and their constituents as active ingredients in bioinsecticides
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-11-04
    Murray B. Isman

    Insecticidal action of plant essential oils has been an area of intensive research in the new millennium, according to a recent bibliometric analysis. Despite this overwhelming research effort, commercialization of bioinsecticides based on essential oils has lagged far behind, although such products have now been used in the USA for over a decade, and in the EU in the last 4–5 years. Recent progress in commercialization of these products is reviewed here. Essential oils and their mono- and sesquiterpenoid constituents are fast-acting neurotoxins in insects, possibly interacting with multiple receptor types. These compounds also display potentially important sublethal behavioural effects in pest insects, including feeding and oviposition deterrence and repellence. Synergy among essential oil terpenoids appears to be a common phenomenon, and a mechanism for this action in rosemary oil has recently been demonstrated. Commercial development of bioinsecticides based on plant essential oils can follow several different pathways producing products with active ingredients differing in their genesis. These include products whose active ingredients consist of (1) a mixture of essential oils; (2) a single essential oil, or a single terpenoid constituent; (3) a blend of terpenoids, synthetically produced, that emulate those in a plant essential oil; and (4) a novel (non-natural) blend of terpenoids obtained from different plant sources. Examples of each of these are provided.

  • Role of plant-derived alkaloids against diabetes and diabetes-related complications: a mechanism-based approach
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-09-21
    Ankit Kumar, Sonali Aswal, Ruchi Badoni Semwal, Ashutosh Chauhan, Sunil Kumar Joshi, Deepak Kumar Semwal

    Diabetes mellitus is a metabolic disorder of multiple etiologies, characterized by chronic hyperglycemia together with the disturbance of carbohydrate, fat, protein metabolism resulting from a defect of insulin secretion, insulin action or both which affects most of the people in both developed and developing countries. Apart from insulin therapy (mainly for type 1 diabetes mellitus), several synthetic drugs are available in the market to treat diabetes, but the treatment with synthetic drugs is costly and the chances of side effects are high. The present work aimed to compile the detailed information about the naturally-occurring alkaloids having an effect against diabetes and diabetes-related complications. A detailed literature survey was conducted to collect information. Different online scientific database such as PubMed, Scopus, and Web of Science were searched together with some relevant books. Since ancient times, plants and their derived products have been used to treat human ailments in various parts of the world where access to modern medicine is limited. About 800 species of medicinal plant have been reported for anti-diabetic effect. A wide range of active constituent derived from plants such as alkaloids, glycosides, terpenoids, steroids, flavonoids, anthocyanidins, resins and saponins have been found active against diabetes. Alkaloids are a class of naturally-occurring chemical compounds, derived from natural sources such as plants, animals, bacteria and fungi. They have a wide range of pharmacological activities such as anti-malarial, anti-asthmatic, anti-cancer, anti-hypertensive, oxytocic, CNS stimulant, muscle relaxant, anti-spasmodic, cholinomimetic, vasodilatory, anti-arrhythmic, analgesic, anti-bacterial and anti-hyperglycemic. The present paper reviews the effect of alkaloids against diabetes and diabetes-related complications such as neuropathy, diabetic ketoacidosis, kidney disease (nephropathy), cardiovascular disease (hypertension), hyperosmolar hyperglycemic nonketotic syndrome, stroke, gastroparesis and eye problems (cataract, keratopathy and retinopathy). Various alkaloids including berberine, boldine and sanguinarine were found potentially effective against different diabetic models. The present work concluded that there are many alkaloidal compounds present in nature which can be used to develop a new promising drug against diabetes and diabetes-related complications.

  • Inclusion complex with cyclodextrins enhances the bioavailability of flavonoid compounds: a systematic review
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-10-01
    Bruno dos Santos Lima, Saravanan Shanmugam, Jullyana de Souza Siqueira Quintans, Lucindo José Quintans-Júnior, Adriano Antunes de Souza Araújo

    Flavonoids are the polyphenolic compounds widely found in plants, which possess several pharmacological activities such as, antioxidant, antinociceptive, anti-inflammatory, antiviral, antidiabetic and anticancer effects. Meanwhile, the aqueous solubility of these flavonoid compounds were very less which limits its oral administration also decreases the bioavailability and pharmacological activities. Recently, the cyclodextrin inclusion complexation method effectively improve the solubility and bioavailability of the flavonoids. The purpose of this review was to evaluate the bioavailability enhancement of flavonoid compounds after complexation with cyclodextrins. The search terms “flavonoids”, “pharmacokinetics”, “bioavailability” and “cyclodextrins” were used to retrieve the articles from, PubMed, Scopus and Web of Science until May 2018. 272 publications were identified and 20 studies were selected finally for the discussion of this review. From the selected studies the pharmacokinetic results reveal that the bioavailability of flavonoid compounds, complexed with cyclodextrins were extensively improved when compared to uncomplexed flavonoids, including the parameters such as, area under curve (AUC) and maximum plasma concentration (Cmax). The use of cyclodextrins can improve the oral bioavailability of flavonoids and it can also be a way to increase the therapeutic effects. Therefore, the incorporation of flavonoids in cyclodextrins increases the development of new pharmaceutical products for the clinical application.

  • Is there a secondary/specialized metabolism in the genus Cuscuta and which is the role of the host plant?
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-10-12
    Isvett Josefina Flores-Sánchez, Ariadna Garza-Ortiz

    The parasitic plants from the genus Cuscuta have been studied from different perspectives, such as their phytochemistry, pharmacology, taxonomy, as weeds, and as a model plant for plant-plant interactions. This review attempts to discuss the host plants’ influence on the phytochemistry and pharmacology of parasitic plants like Cuscuta from the evidence that has been published until recent years in specialized literature and which has not been addressed in detail. Also, the relationship between haustorium development from the parasitic plant and its attachment to the host plant vascular system is discussed and related to the phytochemical and pharmacological information available. In addition, the genus Cuscuta’s main applications description in patents is also explored. Finally, some important recommendations are suggested for further studies in Cuscuta or any other parasitic plant. This state-of-the art about the genus Cuscuta can be a valuable source of organized information for those researchers developing projects in a great variety of aspects related to this genus.

  • Recent use of selected phytochemistry to mitigate environmental challenges facing leather tanning industry: a review
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-09-26
    Kallen Mulilo Nalyanya, Ronald Rop, Arthur Onyuka, Zephania Birech

    Leather tanning technology impacts negatively on the environment as a result of chemicals in the tannery effluents that increases the concentrations of chemical oxygen demand, Biological oxygen demand, total dissolved solids, total Kjeldahl Nitrogen and formation of Cr(VI) among others in the environment. This has led to the profiling of the industry by legislative bodies as a major source of pollution and hence urgent cleaner and eco-friendly innovative technologies are required that will mitigate the environmental pollution. Many studies have recommended green chemistry tanning protocols and systems involving plants since are non-carcinogenic, non-toxic, biodegradable, agro-renewable, sustainable and economical. Numerous studies have evaluated the potential of phytochemistry in leather tanning processes. However, these studies only focused on individual processes or individual plant phytochemicals. Hence this review compiles the selected plants, their phytochemical screening results, their applications in tanning process and their potential for leather tanning. The review has shown enormous capacity of plants and their phytochemicals that can replace synthetic inorganic materials in leather processing and guarantee quality. Plants have a greater applicability in this industry since they have multiple beneficial actions during processing and the final processed leather. Some plants can be used at all tanning processes due to wide variety of important phytochemicals and the final leather is more superior quality to the conventionally processed leather. Other studies have alluded to the possibility of some plant products that have the potential in the industry but yet to be utilized. Further studies have been recommended.

  • Plant secondary metabolites against arthropods of medical importance
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-09-22
    Nikoletta Ntalli, George Koliopoulos, Athanasios Giatropoulos, Urania Menkissoglu-Spiroudi

    Natural compounds of botanical origin are increasingly being investigated for the development of novel biocides. Intensive use of synthetic biocides and the confined array of chemical classes in use has led to the buildup of unwanted residues and to parasites’ adaptive responses and resistance. Meanwhile, the geographic and host ranges of arthropod vectors and vector-borne diseases are broadening. In an effort to develop “friendly” biocidal compounds for the environment and human health, plant secondary metabolites originating in a number of botanical families could be engaged. This mini-review compiles the recently available knowledge on plant secondary metabolites exhibiting biocidal properties and provides a brief overview on their activity against arthropods with a focus on toxic and repellent properties. The selected examples show that it is valuable to consider plants as a promising source for new products development to support the fight against arthropods related to human health. Finally, we outline the biocides regulatory framework in the European Union (EU) and pinpoint some issues of concern regarding the development of low risk biocides.

  • Rhaponticin as an anti-inflammatory component of rhubarb: a minireview of the current state of the art and prospects for future research
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-09-28
    Joanna Kolodziejczyk-Czepas, Jan Czepas

    Rhaponticin (3,3′,5-trihydroxy-4′-methoxystilbene 3-O-β-d-glucoside; synonym–rhapontin), is a stilbene compound, mainly found in various species of rhubarb (Rheum L.). The aglycone, rhapontigenin, is thought to be the biologically active form of rhaponticin. As a component of rhubarb, rhaponticin may be present in the human diet both in foods and dietary supplements. Although promising reports have been published on the various activities of rhaponticin (see: antioxidant, estrogenic, antithrombotic, anticancer and anti-inflammatory actions), no comprehensive review exists of its anti-inflammatory properties. Therefore, the aim of the present work is to summarize the existing evidence of the anti-inflammatory properties of rhaponticin and provide a prospective insight into research on this stilbenoid.

  • Chemical synthesis of terpenoids with participation of cyclizations plus rearrangements of carbocations: a current overview
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-09-20
    José Francisco Quílez del Moral, Álvaro Pérez, Alejandro F. Barrero

    Many terpenoids are biosynthesized after a cascade of cyclizations and rearrangements of carbocations mediated by terpenoid synthases, as exemplified in the biosynthesis of lanosterol. Although several reports of organisms or purified enzymes catalyzing this cascade of reactions in the laboratory have been described, the development of chemical transformations capable of mimicking such tandem cyclizations and rearrangements constitute a formidable challenge for organic chemists. From the very early works of Van Tamelen in the 1960s to our time, we present the Lewis or Brønsted acids-mediated cyclization–rearrangements of carbocations cascades aimed to mimic the action of enzymes. From all the achievements herein presented, the hypothesis of minimal enzymatic participation is reinforced, and this, if confirmed, promises new achievements in this area in the next future.

  • For antagonists and mutualists: the paradox of insect toxic secondary metabolites in nectar and pollen
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-08-30
    Philip C. Stevenson

    The plant kingdom produces an extraordinary diversity of secondary metabolites and the majority of the literature supports a defensive ecological role for them, particularly against invertebrate herbivores (antagonists). Plants also produce secondary compounds in floral nectar and pollen and these are often similar to those produced for defense against invertebrates elsewhere in the plant. This is largely because the chemical armoury within a single plant species is typically restricted to a few biochemical pathways and limited chemical products but how their occurrence in floral rewards is regulated to mediate both defence and enhanced pollination is not well understood. Several phytochemicals are reviewed here comparing the defensive function alongside their benefit to flower visiting mutualists. These include caffeine, aconitine, nicotine, thymol, linalool, lupanine and grayanotoxins comparing the evidence for their defensive function with their impacts on pollinators, their behaviour and well-being. Drivers of adaptation and the evolution of floral traits are discussed in the context of recent studies. Ultimately more research is required that helps determine the impacts of floral chemicals in free flying bees, and how compounds are metabolized, sequestered or excreted by flower feeding insects to understand how they may then affect the pollinators or their parasites. More work is also required on how plants regulate nectar and pollen chemistry to better understand how secondary metabolites and their defensive and pollinator supporting functions are controlled, evolve and adapt.

  • Reversal of multidrug resistance by amphiphilic morning glory resin glycosides in bacterial pathogens and human cancer cells
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-08-14
    Jesús Lira-Ricárdez, Rogelio Pereda-Miranda

    Pathogens that express resistance to multiple drugs are becoming the norm, complicating treatment and increasing human morbidity. Acylsugars or resin glycosides from the morning glory family (Convolvulaceae) are amphipathic modulators of the efflux pumps responsible for the drug-resistant phenotype in prokaryotic and eukaryotic cells. These inhibitory effects could be used to overcome the acquired resistance to common anticancer or antimicrobial drugs by lowering the current effective therapeutic doses, thus decreasing toxic side-effects in refractory malignancies. Active chemosensitizers identified by in vitro screening methods have demonstrated the therapeutic potential of resin glycosides for further exploration as coadjuvants to avoid drug resistance and restore the clinical utility of chemotherapy in treating infections and cancer. To date, more than 20 resin glycosides have been documented as inhibitors or modulators of efflux pumps, mainly isolated from species of the genus Ipomoea. Resin glycosides have shown the ideal structural features associated with multidrug-resistant efflux pump substrates. An overview is given to the acylsugar diversity and their amphiphilicity properties for bioactivity as leads of efflux pump inhibitors for drug development.

  • Amaranthaceae halophytes from the French Flanders coast of the North Sea: a review of their phytochemistry and biological activities
    Phytochem. Rev. (IF 4.257) Pub Date : 2019-08-07
    Gabriel Lefèvre, Céline Rivière

    Halophytes are plant species that tolerate high salinity levels. To adapt to these particular abiotic conditions, they develop multiple physiological, biochemical and molecular mechanisms, including the biosynthesis of osmolytes, enzymes and specialized metabolites. The French Flanders coast of the North Sea is an ideal environment for this kind of plant. Amaranthaceae is one of the most represented botanical families of halophytes present on this coast, with 15 species belonging to 7 genera, namely Atriplex, Beta, Halimione, Kali, Oxybasis, Salicornia and Suaeda. Some of these species are well known as wild edible plants, and some are used in traditional medicine. This review examines the chemistry of these species and their potential for human health.

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上海纽约大学William Glover