Isolation of Antiplasmodial Naphthylisoquinoline Alkaloids from Ancistrocladus Sp. Through Bioassay-guided Fractionation PDF Download
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Author: Mutombo Sephora Mianda Publisher: ISBN: Category : Languages : en Pages :
Book Description
Ancistrocladus is the only genus in the Ancistrocladaceae family and together with the closely related Dioncophyllaceae, they produce naphthylisoquinoline (NIQ) alkaloids. This class of compounds exhibits a very interesting large spectrum of bioactivities. Some of these compounds have shown very promising antiplasmodial activity. Leaves of an as yet unidentified Ancistrocladus sp collected in the region of Bonsolerive (Northwestern part of DRC), were investigated for their antiplasmodial activity. They were air dried at room temperature and ground. The ground plant material was extracted sequentially with n-hexane, dichloromethane, ethyl acetate, methanol, and water. Five extracts were obtained and all, except for the n-hexane extract, were assayed for their antiplasmodial activity using the Malaria SYBR Green I based assay. The results of the antiplasmodial screening of extracts showed that the methanol extract was the most active one (100 % inhibition at 10 and 20 IÌ2℗ơg/mL) and was thus chosen for further research. UPLC QTOF MS was used to chemically profile the sequentially extracted material and to identify naphthylisoquinoline alkaloids in the extracts. The methanol extract was fractionated using silica gel column chromatography to produce 18 fractions. TLC and UPLC QTOF MS were used to target fractions mainly containing naphthylisoquinoline alkaloids and based on this, five fractions were selected for screening against Plasmodium falciparum NF54 strains. They all exhibited good antiplasmodial activity (EÌ8¡2 95 % inhibition at 5 and 10 IÌ2℗ơg/mL). One fraction was further fractionated using preparative HPLC and four sub-fractions collected. They were screened against P. falciparum NF54 strains. One sub-fraction showed an excellent activity with more than 82 % inhibition at 1 IÌ2℗ơg/mL. Three compounds were isolated from the active fractions and one compound from a non-screened fraction using preparative HPLC and LC-MS-SPE-NMR. Through NMR and ECD, the structures of three compounds were fully elucidated as ealamine A (43), ancistrocladinium A (44) and ancistrocyclinone A (45). The structure of one compound was elucidated with only the relative configuration determined (compound 46). The presence of ealamine A (43), which is a 7,8'-coupled hybrid-type NIQ (R configured at C-3 with oxygen function at C-6), in this plant material has a geo- and chemotaxonomic importance. Such NIQs are mostly present in Ancistrocladus plants from the Northwestern Congo Basin. The results of antiplasmodial screening of compounds revealed that ancistrocladinium A (44) and ealamine A (43) showed good activity (IC50 EÌ80́( 10 IÌ2℗ơM) against the chloroquine-sensitive (NF54) and chloroquine-resistant (K1 and Indochina clones W2) strains with no cross-resistance towards drug resistant P. falciparum parasites (RI values
Author: Mutombo Sephora Mianda Publisher: ISBN: Category : Languages : en Pages :
Book Description
Ancistrocladus is the only genus in the Ancistrocladaceae family and together with the closely related Dioncophyllaceae, they produce naphthylisoquinoline (NIQ) alkaloids. This class of compounds exhibits a very interesting large spectrum of bioactivities. Some of these compounds have shown very promising antiplasmodial activity. Leaves of an as yet unidentified Ancistrocladus sp collected in the region of Bonsolerive (Northwestern part of DRC), were investigated for their antiplasmodial activity. They were air dried at room temperature and ground. The ground plant material was extracted sequentially with n-hexane, dichloromethane, ethyl acetate, methanol, and water. Five extracts were obtained and all, except for the n-hexane extract, were assayed for their antiplasmodial activity using the Malaria SYBR Green I based assay. The results of the antiplasmodial screening of extracts showed that the methanol extract was the most active one (100 % inhibition at 10 and 20 IÌ2℗ơg/mL) and was thus chosen for further research. UPLC QTOF MS was used to chemically profile the sequentially extracted material and to identify naphthylisoquinoline alkaloids in the extracts. The methanol extract was fractionated using silica gel column chromatography to produce 18 fractions. TLC and UPLC QTOF MS were used to target fractions mainly containing naphthylisoquinoline alkaloids and based on this, five fractions were selected for screening against Plasmodium falciparum NF54 strains. They all exhibited good antiplasmodial activity (EÌ8¡2 95 % inhibition at 5 and 10 IÌ2℗ơg/mL). One fraction was further fractionated using preparative HPLC and four sub-fractions collected. They were screened against P. falciparum NF54 strains. One sub-fraction showed an excellent activity with more than 82 % inhibition at 1 IÌ2℗ơg/mL. Three compounds were isolated from the active fractions and one compound from a non-screened fraction using preparative HPLC and LC-MS-SPE-NMR. Through NMR and ECD, the structures of three compounds were fully elucidated as ealamine A (43), ancistrocladinium A (44) and ancistrocyclinone A (45). The structure of one compound was elucidated with only the relative configuration determined (compound 46). The presence of ealamine A (43), which is a 7,8'-coupled hybrid-type NIQ (R configured at C-3 with oxygen function at C-6), in this plant material has a geo- and chemotaxonomic importance. Such NIQs are mostly present in Ancistrocladus plants from the Northwestern Congo Basin. The results of antiplasmodial screening of compounds revealed that ancistrocladinium A (44) and ealamine A (43) showed good activity (IC50 EÌ80́( 10 IÌ2℗ơM) against the chloroquine-sensitive (NF54) and chloroquine-resistant (K1 and Indochina clones W2) strains with no cross-resistance towards drug resistant P. falciparum parasites (RI values
Author: Dipakranjan Mal Publisher: Elsevier ISBN: 0128138017 Category : Science Languages : en Pages : 466
Book Description
Anionic Annulations in Organic Synthesis: A Versatile and Prolific Class of Ring-Forming Reactions is a comprehensive review of the main annulations for the construction of cyclic structures and their use in the total synthesis of functional molecules. The book explores in detail the Hauser, Robinson, Sammes, and Myers annulations, all of which are beneficial to constructing substrates with complex molecular structures suitable for pharmaceutical purposes. This volume begins with an in-depth introduction on the history and perspectives of annulations. It then covers different categories of annulation in each chapter, examining their application to drug synthesis for a range of different medicinal compounds. Anionic Annulations in Organic Synthesis delivers a thorough analysis of the topic and provides the tools necessary to master anionic organic chemistry. It is a valuable resource for chemists, researchers, and students seeking a complete and detailed understanding of anionic annulations. Serves as a useful tool to both academic and industrial researchers in the field Includes numerous examples of anionic annulations and how to apply them practically in research and industry Features anionic annulations that are particularly effective for the synthesis of polyoxygenated polycyclic compounds
Author: Surya Nandan Meena Publisher: Academic Press ISBN: 0128174986 Category : Science Languages : en Pages : 580
Book Description
Advances in Biological Science Research: A Practical Approach provides discussions on diverse research topics and methods in the biological sciences in a single platform. This book provides the latest technologies, advanced methods, and untapped research areas involved in diverse fields of biological science research such as bioinformatics, proteomics, microbiology, medicinal chemistry, and marine science. Each chapter is written by renowned researchers in their respective fields of biosciences and includes future advancements in life science research. Discusses various research topics and methods in the biological sciences in a single platform Comprises the latest updates in advanced research techniques, protocols, and methods in biological sciences Incorporates the fundamentals, advanced instruments, and applications of life science experiments Offers troubleshooting for many common problems faced while performing research experiments
Author: Anne E. Osbourn Publisher: Springer Science & Business Media ISBN: 0387854983 Category : Science Languages : en Pages : 588
Book Description
Plants produce a huge array of natural products (secondary metabolites). These compounds have important ecological functions, providing protection against attack by herbivores and microbes and serving as attractants for pollinators and seed-dispersing agents. They may also contribute to competition and invasiveness by suppressing the growth of neighboring plant species (a phenomenon known as allelopathy). Humans exploit natural products as sources of drugs, flavoring agents, fragrances and for a wide range of other applications. Rapid progress has been made in recent years in understanding natural product synthesis, regulation and function and the evolution of metabolic diversity. It is timely to bring this information together with contemporary advances in chemistry, plant biology, ecology, agronomy and human health to provide a comprehensive guide to plant-derived natural products. Plant-derived natural products: synthesis, function and application provides an informative and accessible overview of the different facets of the field, ranging from an introduction to the different classes of natural products through developments in natural product chemistry and biology to ecological interactions and the significance of plant-derived natural products for humans. In the final section of the book a series of chapters on new trends covers metabolic engineering, genome-wide approaches, the metabolic consequences of genetic modification, developments in traditional medicines and nutraceuticals, natural products as leads for drug discovery and novel non-food crops.
Author: Satya D. Sarker Publisher: Springer Science & Business Media ISBN: 1592599559 Category : Science Languages : en Pages : 518
Book Description
The term “natural products” spans an extremely large and diverse range of chemical compounds derived and isolated from biological sources. Our interest in natural products can be traced back thousands of years for their usefulness to humankind, and this continues to the present day. Compounds and extracts derived from the biosphere have found uses in medicine, agriculture, cosmetics, and food in ancient and modern societies around the world. Therefore, the ability to access natural products, understand their usefulness, and derive applications has been a major driving force in the field of natural product research. The first edition of Natural Products Isolation provided readers for the first time with some practical guidance in the process of extraction and isolation of natural products and was the result of Richard Cannell’s unique vision and tireless efforts. Unfortunately, Richard Cannell died in 1999 soon after completing the first edition. We are indebted to him and hope this new edition pays adequate tribute to his excellent work. The first edition laid down the “ground rules” and established the techniques available at the time. Since its publication in 1998, there have been significant developments in some areas in natural product isolation. To capture these developments, publication of a second edition is long overdue, and we believe it brings the work up to date while still covering many basic techniques known to save time and effort, and capable of results equivalent to those from more recent and expensive techniques.
Author: Amritpal Singh Publisher: CRC Press ISBN: 1439853614 Category : Health & Fitness Languages : en Pages : 440
Book Description
Bridging the gap between the ancient art of herbalism and the emerging sciences of ethnopharmocology and phytopharmacotherapy, this book highlights the major breakthroughs in the history of the field and focuses on future directions in the discovery and application of herb-derived medicines. Implementing the concept of reverse pharmacology, it inte
Author: Victor Kuete Publisher: Newnes ISBN: 0124059368 Category : Science Languages : en Pages : 917
Book Description
The pharmacopoeias of most African countries are available and contain an impressive number of medicinal plants used for various therapeutic purposes. Many African scholars have distinguished themselves in the fields of organic chemistry, pharmacology, and pharmacognosy and other areas related to the study of plant medicinal plants. However, until now, there is no global standard book on the nature and specificity of chemicals isolated in African medicinal plants, as well as a book bringing together and discussing the main bioactive metabolites of these plants. This book explores the essence of natural substances from African medicinal plants and their pharmacological potential. In light of possible academic use, this book also scans the bulk of African medicinal plants extract having promising pharmacological activities. The book contains data of biologically active plants of Africa, plant occurring compounds and synthesis pathways of secondary metabolites This book explores the essence of natural substances from African medicinal plants and their pharmacological potential The authors are world reknowned African Scientists
Author: Mallappa Kumara Swamy Publisher: Springer Nature ISBN: 9811517614 Category : Science Languages : en Pages : 619
Book Description
Plants produce a vast number of bioactive compounds with different chemical scaffolds, which modulate a diverse range of molecular targets and are used as drugs for treating numerous diseases. Most present-day medicines are derived either from plant compounds or their derivatives, and plant compounds continue to offer limitless reserves for the discovery of new medicines. While different classes of plant compounds, like phenolics, flavonoids, saponins and alkaloids, and their potential pharmacological applications are currently being explored, their curative mechanisms are yet to be understood in detail. This book is divided into 2 volumes and offers detailed information on plant-derived bioactive compounds, including recent research findings. Volume 1, Plant-derived Bioactives: Chemistry and Mode of Action, discusses the chemistry of highly valued plant bioactive compounds and their mode of actions at the molecular level. Volume 2, Plant-derived Bioactives: Production, Properties and Therapeutic Applications, explores the sources, biosynthesis, production, biological properties and therapeutic applications of plant bioactives. Given their scope, these books are valuable resources for members of the scientific community wishing to further explore various medicinal plants and the therapeutic applications of their bioactive compounds. They appeal to scholars, teachers and scientists involved in plant product research, and facilitate the development of innovative new drugs.
Author: Kishan Gopal Ramawat Publisher: Springer Nature ISBN: 3030307468 Category : Science Languages : en Pages : 318
Book Description
Plant classifications are based on morphological characters and it is difficult, particularly in small plants and grasses, to identify these below generic level on the basis of these characters using a dissecting microscope. Plant species have intra- and inter-specific variation in secondary metabolites which can be utilized as marker compounds for identification and classification of plants. Secondary metabolites are produced as a result of primary metabolism and the production of these compounds not only involves several genes but also it is an energy dependent process. Hence these products cannot be considered as insignificant for the plant and the environment. Modern tools of molecular biology and secondary metabolites present in them can definitively decide about classification of plants. Absence of correct identification of plant is associated to many problems of resource utilization. Due to wide availability of these tools, interest has revived in systematics and correct classification of plants based on these parameters for their sustainable utilization and resource management. The purpose of this book is to assess the potential of phytochemical and molecular tools in the systematic and classification of plants. The topics covered include species concept, barcoding and phylogenetic analysis, chemotaxonomy use of polyketides, carotenes, cuticular wax, volatile oils, biodiversity of corals, metazoans, Ruta and Echinocereus. It provides comprehensive and broad subject-based reviews, useful for students, teachers, researchers, and all others interested in the field. The field has been kept wide and general to accommodate the wide-ranging topics. This book will be useful to agriculturists, chemists, botanists, industrialists, and those involved in planning of crop plants.
Author: Victor R Preedy Publisher: Academic Press ISBN: 0124167160 Category : Technology & Engineering Languages : en Pages : 1080
Book Description
Coffee in Health and Disease Prevention presents a comprehensive look at the compounds in coffee, their reported benefits (or toxicity risks) and also explores them on a health-condition specific level, providing researchers and academics with a single-volume resource to help in identifying potential treatment uses. No other book on the market considers all the varieties of coffee in one volume, or takes the disease-focused approach that will assist in directing further research and studies. The book embraces a holistic approach and effectively investigates coffee and its specific compounds from the biochemical to the nutritional well-being of geographical populations. This book represents essential reading for researchers in nutrition, dietetics, food science, biochemistry, and public health. Presents one comprehensive, translational source for all aspects of how coffee plays a role in disease prevention and health Experts in nutrition, diet, and food chemistry (from all areas of academic and medical research) take readers from the bench research (cellular and biochemical mechanisms of vitamins and nutrients) to new preventive and therapeutic approaches Focuses on coffee composition; nutritional aspects of coffee; protective aspects of coffee-related compounds; specific coffee components and their effects on tissue and organ systems Features sections on both the general effects of coffee consumption on the body as well as the effects of specific coffee compounds on specific organ systems
Author: Mutombo Sephora Mianda
Author: Mutombo Sephora Mianda
Author: Dipakranjan Mal
Author: Surya Nandan Meena
Author: Anne E. Osbourn
Author: Satya D. Sarker
Author: Amritpal Singh
Author: Victor Kuete
Author: Mallappa Kumara Swamy
Author: Kishan Gopal Ramawat
Author: Victor R Preedy